The present invention belongs to the field of medicinal chemistry, and particularly relates to an N-(3-fluorobenzyl)-1H-indazole-5-amine derivative having a structure as shown in general formula (I), and the preparation and the use thereof. The N-(3-fluorobenzyl)-1H-indazole-5-amine derivative having a structure as shown in general formula (I), and a stereoisomer, pharmaceutically acceptable salt, hydrate, solvate or prodrug thereof provided in the present invention have an activity as a protein kinase inhibitor, particularly an inhibitory activity against tropomyosin receptor kinase (TRK).
C07D 261/20 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings condensed with carbocyclic rings or ring systems
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
The present invention relates to the technical field of drug synthesis. Specifically disclosed are an azole derivative as shown in general formula (I), or a stereoisomer or pharmaceutically acceptable salt, hydrate, solvate or prodrug thereof, a preparation method therefor and a use thereof in preparation of drugs for preventing or treating various diseases caused by fungal infection.
C07D 249/10 - 1,2,4-TriazolesHydrogenated 1,2,4-triazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
3.
CEMBRANOID MACROCYCLIC DITERPENE DERIVATIVES, PREPARATION METHOD THEREFOR, AND USE THEREOF
Cembranoid macrocyclic diterpene derivatives, a preparation method therefor, and a use thereof, belonging to the field of medical technology. Disclosed are cembranoid macrocyclic diterpene derivatives, a preparation method therefor, and a use thereof. In the present invention, a series of cembranoid macrocyclic diterpene derivatives are obtained by means of column chromatography and high-performance liquid chromatography separation of an extract from Croton oleifera. Said derivatives are capable of inhibiting LPS-induced NO release in BV-2 cells and have great potential for the preparation of a medicament for neuritis-related diseases.
C07C 49/703 - Unsaturated compounds containing a keto group being part of a ring containing hydroxy groups
C07D 311/94 - Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems condensed with rings other than six-membered or with ring systems containing such rings
C07C 45/78 - SeparationPurificationStabilisationUse of additives
C07C 45/79 - SeparationPurificationStabilisationUse of additives by solid-liquid treatmentSeparationPurificationStabilisationUse of additives by chemisorption
A61K 31/34 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
A61K 31/122 - Ketones having the oxygen atom directly attached to a ring, e.g. quinones, vitamin K1, anthralin
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 25/00 - Drugs for disorders of the nervous system
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
The present invention relates to a cabazitaxel prodrug anti-tumor preparation, designs and synthesizes a small molecule cabazitaxel prodrug with branched fatty alcohol involving formulas (I), (II) and (III) and containing different fatty alcohol side chains and different linking chains, and prepares a self-assembled nanoparticle. Results showed that the self-assembled nanoparticle of the small molecule cabazitaxel prodrug with branched fatty alcohol can effectively improve the efficacy of cabazitaxel, reduce toxic and side effects. The length of branched fatty alcohol side chains, the structure of the fatty alcohol side chains, the elemental composition of the linking chains and the length of the linking chains significantly affect preparation properties, in vivo fate and anti-tumor activity of the cabazitaxel-branched fatty alcohol prodrug self-assembled nanoparticle, which exhibits higher anti-tumor activity and lower toxicity compared with the self-assembled nanoparticle of small molecule cabazitaxel prodrug with straight-chain fatty alcohol.
The present invention relates to a cabazitaxel prodrug anti-tumor preparation, designs and synthesizes a small molecule cabazitaxel prodrug with branched fatty alcohol involving formulas (I), (II) and (III) and containing different fatty alcohol side chains and different linking chains, and prepares a self-assembled nanoparticle. Results showed that the self-assembled nanoparticle of the small molecule cabazitaxel prodrug with branched fatty alcohol can effectively improve the efficacy of cabazitaxel, reduce toxic and side effects. The length of branched fatty alcohol side chains, the structure of the fatty alcohol side chains, the elemental composition of the linking chains and the length of the linking chains significantly affect preparation properties, in vivo fate and anti-tumor activity of the cabazitaxel-branched fatty alcohol prodrug self-assembled nanoparticle, which exhibits higher anti-tumor activity and lower toxicity compared with the self-assembled nanoparticle of small molecule cabazitaxel prodrug with straight-chain fatty alcohol.
Provided is a biaryloxazolidinone compound, wherein the compound is a compound of general formula I and a stereoisomer, pharmaceutically acceptable salt, solvate or prodrug thereof. The present invention relates to the field of pharmaceutical chemistry, and in particular to a bbiaryloxazolidinone compound and a use thereof. The compound has better antibacterial activity than linezolid and has significant antibacterial activity against drug-resistant bacteria. In addition, the compound exhibits lower MAO inhibition and better safety compared to linezolid.
C07D 413/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
The present application relates to a tetravalent cisplatin prodrug, a liposome thereof, and a use thereof. The tetravalent cisplatin prodrug has a structure of formula I. The tetravalent cisplatin prodrug liposome prepared from the tetravalent cisplatin prodrug of the present application significantly improves the anti-tumor activity, and reduces the toxicity. Moreover, the prepared liposome has high drug loading capacity and high stability, involves a simple preparation process, and has industrial application value.
The present invention belongs to the technical field of drug synthesis. Specifically, disclosed are an azole derivative as shown in general formula I, or a stereoisomer thereof, or a pharmaceutically acceptable salt, a hydrate, a solvate or a prodrug thereof, a preparation method therefor, and the use thereof in the preparation of a drug for preventing or treating various diseases caused by fungal infections.
Disclosed in the present invention are a preparation method for a brain-targeting agomelatine nasal spray micelle and use thereof, which belong to the technical field of pharmaceutical formulations. According to the present invention, an injectable pharmaceutical excipient polyethylene glycol (15)-hydroxystearate (HS15) is taken as a carrier material, HS15 and agomelatine are dissolved in an organic solvent, and the resulting solution is subjected to rotary evaporation under reduced pressure to form a uniform film, which, upon hydration, forms an agomelatine micelle solution capable of being sprayed nasally for treating depression and insomnia. According to the present invention, the problem of low oral bioavailability of agomelatine due to poor solubility, serious first pass effect of hepar, difficulty in penetrating a blood-brain barrier, etc., is solved. The micelle structure constructed in the present invention is quickly delivered into the brain after nasal administration, and it is stable in cerebrospinal fluid and can achieve slow release of the drug, thereby improving the intracerebral bioavailability of the drug and achieving high brain targeting property and low systemic toxic and side effects. The micelle structure has good clinical application value and market prospects.
The present invention relates to the technical field of medicinal chemistry, and in particular to a quinoline derivative, a pharmaceutical composition thereof, and a use thereof in the preparation of drugs for preventing or treating PDE4-related diseases. The provided quinoline derivative exhibits good PDE4 inhibitory activity, and can be used for preventing or treating PDE4-related diseases, especially inflammatory diseases. The quinoline derivative is a compound represented by general formula (I), or a pharmaceutically acceptable salt, a geometric isomer, an enantiomer thereof, or a pyridine N-oxide thereof.
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 11/00 - Drugs for disorders of the respiratory system
10.
GINSENOSIDE F1 NASAL MUCOSA FORMULATION AND PREPARATION METHOD THEREFOR AND USE THEREOF
Provided are a ginsenoside F1 nasal mucosa formulation and a preparation method therefor and use thereof. The ginsenoside F1 nasal mucosa formulation is prepared using ginsenoside F1 as an active ingredient, together with a nasal mucosa absorption promoter and water, and optionally contains borneol and a bacteriostatic agent. The ranges of the mass percentage of the components are preferably as follows: 0.4-15% of ginsenoside F1, 0-0.8% of borneol, 0.05-40% of the absorption promoter, and 0-0.3% of the bacteriostatic agent. The nasal formulation can be used for treating senile dementia and can improve and restore memory. The nasal solution has the following advantages: improving the solubility of the ginsenoside F1 in water and thereby significantly improving the bioavailability of systemic absorption of ginsenoside F1, and enabling increase in the concentration of ginsenoside F1 in the intracerebral focus by means of formula adjustment according to therapeutic requirements and thereby significantly improving the therapeutic effect for diseases and the safety of drug use.
A61K 31/704 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin, digitoxin
A61K 47/26 - Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharidesDerivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
A61K 47/44 - Oils, fats or waxes according to two or more groups of Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
11.
BREAST-CANCER-TARGETED MILK-DERIVED EXOSOME DRUG DELIVERY SYSTEM, AND PREPARATION METHOD THEREFOR AND USE THEREOF
Disclosed are a breast-cancer-targeted milk-derived exosome drug delivery system, and a preparation method therefor and the use thereof, which belong to the technical field of pharmaceuticals. The method for preparing the breast-cancer-targeted milk-derived exosome drug delivery system involves: adding sodium citrate to animal milk to remove casein, performing differential centrifugation under a low-temperature condition by using a centrifuge, separating and enriching milk-derived exosomes, performing ultrasonic drug loading on the drug solution and the milk-derived exosome suspension at 37°C, and performing freeze drying to obtain drug-loaded exosomes. In the preparation method, the exosomes are obtained by taking animal milk as a source. The source of animal milk is abundant and the operation of the method is simple, which reduces the production cost. Moreover, natural ligands on the milk-derived exosomes can specifically target and bind to breast-cancer cells, so that uptake by cancer cells is enhanced, the cytotoxicity of the drug to normal cells is reduced, and the effect of specifically treating breast cancer is achieved. The present application is widely used in the field of targeted delivery of drugs for breast cancer treatment.
A61K 47/46 - Ingredients of undetermined constitution or reaction products thereof, e.g. skin, bone, milk, cotton fibre, eggshell, oxgall or plant extracts
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
A61K 31/704 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin, digitoxin
Provided are a preparation method for and the use of an icaritin carbamate prodrug and a salt thereof, which belong to the pharmaceutical field. In particular, provided are an icaritin carbamate prodrug represented by formula 3-N or 7-N and a pharmaceutically acceptable salt thereof, and a preparation method therefor and the use thereof. Specifically, the icaritin carbamate prodrug is formed by subjecting a main metabolic site (3-site or 7-site hydroxyl) of a natural flavonoid compound icaritin to structural modification by means of a chemical synthesis method, and introducing a suitable group at the position. Amines used in such carbamates are aliphatic amines. The presence of the carbamate structure reduces the phase II metabolism of icaritin in SD rats. Compared with an icaritin bulk drug, the 3-N-01 prodrug has a significantly improved oral bioavailability, making same the optimal prodrug. In clinical medication, the prodrug is expected to be able to reduce the administration dosage and improve patient compliance, and is expected to offer an effective strategy for improving the oral bioavailability of phenolic drugs.
C07D 311/30 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4 with aromatic rings attached in position 2 or 3 with aromatic rings attached in position 2 only not hydrogenated in the hetero ring, e.g. flavones
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/352 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. cannabinols, methantheline
A method for synthesizing a nano ZnO multi-level structure material having high catalytic and antibacterial activity, belonging to the field of preparation of nano inorganic materials. The present invention utilizes the formation characteristics of ZnO to provide a new, simple and green one-step method for preparing a nano ZnO multi-level structure material having different morphologies at normal pressure and within a relatively low temperature range, using ethylene glycol and an organic solvent as a mixed solvent. For the first time, a highly active bowl-shaped multi-level structure formed by self-assembly of nano ZnO is obtained in a simple system, which is mild and does not require additional additives or strong bases, realizing convenient and controllable green synthesis of a highly active nano ZnO multi-level structure. The prepared nano ZnO multi-level structure material has excellent antibacterial properties, while also having functionality of photocatalytic degradation of organic dyes.
The present invention relates to the field of medicinal chemistry, and in particular to a C-3 pyrazole substituted indazole derivative (a general formula compound, and a stereoisomer, pharmaceutically acceptable salt, hydrate, solvate or prodrug thereof) and a use (a use in the preparation of a therapeutic agent, especially a TRK inhibitor). The derivative is a C-3 pyrazole substituted indazole compound having a structure represented by general formula (I), or a stereoisomer, pharmaceutically acceptable salt, hydrate, solvate or prodrug thereof. According to the present invention, the C-3 pyrazole substituted indazole derivative having a structure represented by general formula (I), or the stereoisomer, pharmaceutically acceptable salt, hydrate, solvate or prodrug thereof have activity as a protein kinase inhibitor, especially against a TRK.
HEBEI UNIVERSITY OF SCIENCE AND TECHNOLOGY (China)
3D BIOOPTIMA (China)
Inventor
Zhao, Yanfang
Gao, Zibin
Tong, Minghui
Hou, Yunlei
Li, Shuo
Miao, Zhenyu
Zhang, Huimin
Shi, Xuan
Sun, Yanping
Sun, Yongjun
Abstract
The present invention relates to the field of pharmaceutical chemistry, and in particular to a new aryl urea derivative, namely a compound of general formula I, or a pharmaceutically acceptable salt, solvate or prodrug thereof, a pharmaceutical composition comprising the compound, and the use thereof, wherein substituents R1, R2, R3and R4, X, Y, Z, m and n have the significances given in the description. The present invention further relates to the use of the compound of general formula I in the preparation of a drug for treating and/or preventing sEH-mediated diseases, and in particular in the preparation of a drug for treating inflammatory diseases, cardiovascular and cerebrovascular diseases, pain, diabetes, complications of diabetes, diabetes-related diseases, fibrotic diseases, neurological and psychiatric diseases, ulcerative diseases, etc.
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/428 - Thiazoles condensed with carbocyclic rings
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/541 - Non-condensed thiazines containing further heterocyclic rings
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
A61P 9/00 - Drugs for disorders of the cardiovascular system
A61P 25/00 - Drugs for disorders of the nervous system
16.
BENZOTRIAZOLE DERIVATIVE SERVING AS CDKS INHIBITOR, AND PHARMACEUTICAL COMPOSITION THEREOF AND USE THEREOF
SHANDONG LABORATORY OF YANTAI DRUG DISCOVERY (China)
Inventor
Cheng, Maosheng
Li, Jia
Liu, Yang
Sun, Yili
Zhong, Ye
Xu, Jing
Tang, Li
Ren, Zhaohui
Abstract
The present invention relates to the technical field of medicinal chemistry, and particularly relates to a benzotriazole derivative serving as a CDKs inhibitor, and a pharmaceutical composition thereof and a use thereof in preparation of antitumor drugs. The benzotriazole derivative of the present invention has strong inhibitory activity against CDK9 and other CDK subtypes, has strong antitumor activity, and has strong inhibitory activity against cell proliferation of human blood cancer cells K562 and colorectal cancer cells HCT116. The structure of the benzotriazole derivative of the present invention is shown as general formula (I).
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
A61K 31/541 - Non-condensed thiazines containing further heterocyclic rings
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
The present application relates to the technical field of medicines, and in particular to a compound, and a preparation method therefor and a use thereof in the preparation of a soluble epoxide hydrolase (sEH) inhibitor and a peroxisome proliferators-activated receptors (PPARs) agonist. The present application provides a compound, having a structure represented by formula I, II, III, IV, V or VI. The compound provided by the present application has a typical urea structure as the primary pharmacophore of an sEH, and the thiazolidinedione part serves as the primary pharmacophore of PPARs. The sEH inhibitor and PPARs agonist compound provided by the present application has high inhibitory activity against human-derived HsEH and high agonistic activity against a PPAR, and can be used for the preparation of a drug for treating soluble epoxide enzyme and PPARs-mediated diseases.
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07C 275/34 - Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by singly-bound oxygen atoms having nitrogen atoms of urea groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
C07C 275/26 - Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of rings other than six-membered aromatic rings
C07C 273/18 - Preparation of urea or its derivatives, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups of substituted ureas
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
A61P 11/00 - Drugs for disorders of the respiratory system
An indoline compound containing a thiazole structure, a preparation method therefor, and an application thereof, which belong to the technical field of medicine. Specifically disclosed is an indoline compound containing a thiazole structure, as shown in general formula (I), or a stereoisomer or a pharmaceutically acceptable salt thereof, a preparation method for each of same, and the use thereof in the preparation of a drug for treating diseases related to PD-1/PD-L1 protein/protein interaction and NAMPT. The disclosed compound has a high level of inhibitory activity with regard to PD-1/PD-L1 protein/protein interaction and NAMPT, has remarkable anti-proliferative activity with regard to A2780 cells with high expression of NAMPT, and a representative compound can inhibit tumor growth in animal models having overexpression of NAMPT and PD-L1, and can be used for preparing drugs for treating diseases related to PD-1/PD-L1 protein/protein interaction and NAMPT, such as cancer and viral infection.
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
The present application discloses a heteropolysaccharide, comprising galacturonic acid, arabinose, galactose, glucose, rhamnose, xylose, and mannose. Specifically, the present application relates to a Panax ginseng heteropolysaccharide (GAPS-FL), which is a novel polysaccharide substance separated from Panax ginseng roots, can nonspecifically change or enhance the immune response reaction of multiple types of vaccines including influenza vaccines, can enhance humoral immunity of influenza vaccine immune mice, and can also enhance cellular immunity thereof.
C08B 37/00 - Preparation of polysaccharides not provided for in groups Derivatives thereof
A61K 39/39 - Medicinal preparations containing antigens or antibodies characterised by the immunostimulating additives, e.g. chemical adjuvants
A61K 31/715 - Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkagesDerivatives thereof, e.g. ethers, esters
The present disclosure relates to the field of tumor drug therapy, in particular to use of a methylaminocolchicine and salts thereof. The use includes use of a methylamino-substituted colchicine at C10 position and salts thereof in preparation of antitumor drugs, use thereof in antitumor drugs for antagonizing microtubule inhibitor resistance, or use thereof in combination an antitumor drug. In the present disclosure, the methylaminocolchicine and the salts thereof have significant antitumor effects, are more active than paclitaxel, vincristine, and colchicine, do not exhibit cross resistance to the paclitaxel and the vincristine, and inhibit paclitaxel-resistant cell growth in vivo. With in vivo acceptable therapeutic indexes, the methylaminocolchicine and the salts thereof have a synergistic antitumor effect when used in combination with an anti-apoptotic protein Bcl-2/Bcl-xL inhibitor.
The present application relates to the field of pharmaceutical therapy of tumors, and relates to the use of methylaminocolchicine and salts thereof, involving the use of C10-position methylamino-substituted colchicine and salts in preparation of antitumor drugs, or the use in drugs for tubulin inhibitor-resistant tumors, or the use in drugs for combined therapy of tubulin inhibitor-resistant tumors. The methylaminocolchicine and the salts in the present application have an obvious anti-tumor effect, have activities superior to that of paclitaxel, vincristine and colchicine, have no cross drug resistance with paclitaxel and vincristine, have an in-vivo inhibition effect on growth of paclitaxel-resistant cells, have in-vivo acceptable therapeutic indexes, and achieve a synergistic anti-tumor effect when being combined with an anti-apoptotic protein Bcl-2/Bcl-xL inhibitor.
The present invention pertains to the technical field of pharmaceutical formulations and particularly relates to a low-aggregate ophthalmic nano-formulation for efficient drug delivery, a preparation method therefor, and use thereof. The use mainly relates to the treatment of ocular diseases. The described low-aggregate ophthalmic nano-formulation of the present invention is prepared from a drug molecule, a phospholipid or a derivative thereof, and an amphiphilic surfactant. The concentration of the phospholipid or the derivative thereof is 0.05%-60% by weight, and the concentration of the amphiphilic surfactant is 0.05%-25% by weight. The ocular delivery system of the low-aggregate nano-formulation prepared in the present invention has the advantages of a particle size smaller than 10 nm, good tissue permeability, good stability, and a low irritation level, which greatly improve the bioavailability of ocular drug administration.
A61K 47/24 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
A61K 47/28 - Steroids, e.g. cholesterol, bile acids or glycyrrhetinic acid
A61K 47/44 - Oils, fats or waxes according to two or more groups of Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
The present invention relates to the field of pharmaceutical chemistry, and in particular, to an indolin-2-one derivative having a structure shown in general formula (I) and a use thereof. The indolin-2-one derivative having the structure shown in general formula (I), or a stereoisomer, pharmaceutically acceptable salt, hydrate, solvate or prodrug thereof provided by the present invention has the activity as a protein kinase inhibitor, especially against wild enzymes and various mutants of TRK kinase.
C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
The present invention belongs to the field of drug synthesis; and relates to a high-selectivity PLK4 inhibitor, a preparation method therefor, and the use thereof as a PLK4 inhibitor. The inhibitor is a pyrazolopyrimidine derivative as shown in formula I, and a geometric isomer, an enantiomer or a pharmaceutically acceptable salt thereof; preferably, the compound has the activity of acting as a protein kinase inhibitor, especially as a PLK4 kinase inhibitor.
MEMANTINE UREA DERIVATIVE, PREPARATION METHOD THEREFOR, AND USE THEREOF IN PREPARATION OF MEDICAMENT FOR TREATING SOLUBLE EPOXIDE ENZYME-MEDIATED DISEASES
122 are all methyl groups (i.e., 3,5-dimethyl substitution), the van der Waals force can be enhanced. Therefore, the memantine urea derivative provided by the present application has high inhibitory activity against human sEH (HsEH) and murine sEH (MsEH), and can be used as an sEH inhibitor for preparing a medicament for treating a soluble epoxide enzyme-mediated disease.
C07D 211/60 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 295/205 - Radicals derived from carbonic acid
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 243/08 - Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 not condensed with other rings
C07C 273/18 - Preparation of urea or its derivatives, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups of substituted ureas
C07C 275/42 - Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by carboxyl groups
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 9/00 - Drugs for disorders of the cardiovascular system
A61P 25/00 - Drugs for disorders of the nervous system
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
A61P 11/00 - Drugs for disorders of the respiratory system
A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
26.
BIPHENYL HETEROARYL-CONTAINING DIHYDROPTERIDINONE DERIVATIVE, AND USE THEREOF
123455, X, m, and A have the meanings given in the description. The present invention further relates to use of the compound of general formula Ⅰ and the pharmaceutically acceptable salt, solvate or prodrug thereof in the preparation of a drug for treating diseases caused by abnormally high expression of PLK1 kinase, and especially in the preparation of a drug for treating and/or preventing cancers.
The present invention relates to a 2-aminopyrimidine compound as represented by general formula (I) and a pharmaceutically acceptable salt, solvate, or prodrug thereof, preparation methods therefor, and a pharmaceutical composition containing the compound, wherein R1, R2, Ar, X, Y, Z, m, and n have the meanings given in the description. The present invention further relates to a use of the compound of general formula (I) in preparation of a drug for treating and/or preventing hematological malignancies and inflammatory bowel disease.
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
A61P 35/02 - Antineoplastic agents specific for leukemia
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/541 - Non-condensed thiazines containing further heterocyclic rings
28.
VACCINE ADJUVANT, VACCINE COMPOSITION, AND USE THEREOF
Provided is a vaccine adjuvant, comprising a ginseng acidic polysaccharide (GAPS) adjuvant and an aluminum salt adjuvant. The mixture of the ginseng acidic polysaccharide (GAPS) and the aluminum salt can significantly improve the titer of a specific antibody (or a neutralizing antibody) after antigen immunization, can effectively enhance the immune response level of an organism to a vaccine, and has an activity significantly higher than that of a single aluminum salt adjuvant.
Provided is a vaccine adjuvant comprising ginseng acidic polysaccharide (GAPS), which can significantly improve the titer of a specific antibody (or a neutralizing antibody) after antigen immunization and can effectively enhance the immune response activity of a rabies vaccine, an influenza vaccine, a hepatitis B vaccine, a hepatitis A vaccine, a hepatitis C vaccine, a hand-foot-and-mouth vaccine, an HPV vaccine, and a novel coronavirus vaccine.
The present invention provides a mutant of an antibody, and use thereof. Specifically, according to a Kabat numbering system, the mutant of the antibody has an engineered cysteine residue at any one or more positions selected from the following: positions 12, 34, 35, 38, 44, 47, 51, 60, 61, 67, 69, 78, 79, 114, or any combination thereof in a heavy chain variable region; or positions 19, 21, 44, 46, 47, 48, 62, 71, 75, 78, 87, or any combination thereof in a light chain variable region. The sulfhydryl group on the engineered cysteine can keep part of activity in the antibody expression process. The sulfhydryl group that keeps activity can be directly used for reacting with other active groups without reduction treatment. According to the cysteine-engineered antibody, the active group for drug conjugation can be obtained, which is beneficial to simplifying the production process of an antibody-drug conjugate, thereby improving the uniformity of the antibody-drug conjugate, improving the drug effect, and reducing toxic and side effects.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
An aromatic six-membered ring-fused imidazole derivative, and a preparation method therefor and the use thereof, which belongs to the field of drug synthesis. Specifically, the present invention relates to an aromatic six-membered ring-fused imidazole derivative as represented by general formula (I), and a preparation method therefor and the use thereof as an LSD1 inhibitor. The compound provided in the present invention exhibits a relatively good activity at an in-vitro enzyme level and is different from an existing irreversible inhibitor having an anti-phenyl cyclopropanamine parent nucleus structure, and a new skeleton compound is provided in the present invention for the field of research of LSD1 inhibitors. According to the synthesis route used in the present invention, the raw material is cheap and easily available, the reagent used is a common reagent, the reaction conditions are mild, the post-treatment is simple, and the type of compound can be efficiently prepared. The compound, which can be used as a lysine-specific demethylase-1 inhibitor, provided in the present invention can be administered alone or in combination for treating various tumor diseases.
C07D 235/18 - BenzimidazolesHydrogenated benzimidazoles with aryl radicals directly attached in position 2
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
32.
FUSED PYRIMIDINE DERIVATIVE AND APPLICATION THEREOF
122, A, Y, L, and n are provided the description. The invention further relates to an application of the compound and the pharmaceutically acceptable salt, solvate or prodrug thereof in the preparation of a drug for treating diseases caused by abnormally high ATR expression, in particular to the application of the compound in the preparation of a drug for treating and/or preventing hyperproliferative diseases, including but not limited to gastric cancer, liver cancer, colorectal cancer, ovarian cancer, pancreatic cancer etc.
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
The present invention provides ophthalmic double and triple compound pharmaceutical compositions for treating glaucoma and ocular hypertension. The stability of the pharmaceutical compositions is obviously improved by means of a salt modification technology. The double compound pharmaceutical composition is prepared from a netarsudil free alkali or a pharmaceutically acceptable salt thereof, and an adrenergic β receptor blocker. The triple compound pharmaceutical composition is prepared from a netarsudil free alkali or a pharmaceutically acceptable salt thereof, an adrenergic β receptor blocker, and a prostaglandin analog. The double and triple compound pharmaceutical compositions have excellent stability at pH 4.5-5.4. An effective amount of the pharmaceutical compositions of the present invention are administered once a day to the eyes of patients in need thereof at or near bedtime, such that the intraocular pressure can be efficiently and quickly reduced and is maintained in a physiological range more persistently, showing small side effects and high patient compliance.
The present invention relates to the technical field of pharmaceutics, and particularly, to use of a terpene compound in regulating intrameningeal lymphatic circulation to promote removal of abnormal proteins in brain via lymphatic pathway. Disclosed is use of a terpene compound in regulating meninges lymphatic drainage to treat the accumulation of abnormal proteins in a neurodegenerative disease. The terpene compound or a formulation thereof may be administered alone as a monotherapy of the terpene compound, or in combination with an additional therapeutic agent. The terpene compound can improve the expression of vascular endothelial growth factor, promote the development of the lymphatic system, accelerate the flow of cerebrospinal fluid, expand lymphatic vessels, and enhance lymphatic drainage. The terpene compound enhances the removal of accumulated abnormal proteins in neurodegenerative diseases by regulating lymphatic drainage in the dura mater, thereby effectively improving the prophylactic and therapeutic effects of the terpene compound on neurodegenerative diseases.
A61K 31/045 - Hydroxy compounds, e.g. alcoholsSalts thereof, e.g. alcoholates
A61K 9/00 - Medicinal preparations characterised by special physical form
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
HEBEI UNIVERSITY OF SCIENCE AND TECHNOLOGY (China)
Inventor
Zhao, Yanfang
Gao, Zibin
Han, Yufei
Li, Shuo
Hou, Yunlei
Zhang, Huimin
Xu, Sicong
Sun, Yanping
Qin, Mingze
Sun, Yongjun
Liu, Yajing
Gong, Ping
Abstract
A compound represented by general formula (I) or stereoisomers thereof and pharmaceutically acceptable salts, solvates or prodrugs thereof, a preparation method therefor and a pharmaceutical composition containing the compound. An application of the compound of general formula (I) in preparation of drugs for treating and/or preventing she-mediated diseases, especially an application in preparation of drugs for treating inflammatory diseases, cardiovascular and cerebrovascular diseases, diabetes, diabetes complications, diabetes-related diseases, fibrotic diseases, neurological and mental diseases, pain, and ulcer diseases, etc.
A compound represented by general formula (I) or stereoisomers thereof and pharmaceutically acceptable salts, solvates or prodrugs thereof, a preparation method therefor and a pharmaceutical composition containing the compound. An application of the compound of general formula (I) in preparation of drugs for treating and/or preventing she-mediated diseases, especially an application in preparation of drugs for treating inflammatory diseases, cardiovascular and cerebrovascular diseases, diabetes, diabetes complications, diabetes-related diseases, fibrotic diseases, neurological and mental diseases, pain, and ulcer diseases, etc.
Provided is a mutant of an antibody or fragment thereof, characterized in that the antibody or fragment thereof contains a light-chain constant region, and according to the Kabat numbering system, the amino acid at position 166 is mutated to cysteine.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 47/50 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
37.
METHOD FOR PREPARING QUINAZOLINE DERIVATIVE AND ANALOG THEREOF AND USE THEREOF
A quinazoline derivative of general formula (I), a geometric isomer or a pharmaceutically acceptable salt thereof, and a preparation method therefor. The quinazoline derivative of general formula (I) can be used as a protein kinase inhibitor, particularly as a TRK inhibitor.
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A docetaxel prodrug anti-tumor preparation of the present invention, relating to the field of new adjuvants and new dosage forms of pharmaceutical preparations. A docetaxel-fatty alcohol prodrug comprising different fatty alcohol side chains and different linking chains as shown in the following general formula (I) is specifically designed and synthesized, and self-assembled nanoparticles are prepared. The results show that the self-assembled nanoparticles of the docetaxel-fatty alcohol prodrug can effectively improve the curative effect of docetaxel and reduce the toxic and side effects thereof. The length of a branched chain fatty alcohol side chain, the structure (branched chain or straight chain) of the fatty alcohol side chain and the length of the linking chain can significantly influence the pharmaceutics properties, the in-vivo fate, the anti-tumor activity and the safety of the self-assembled nanoparticles of the docetaxel prodrug. Self-assembled nanoparticles of a docetaxel-branched chain fatty alcohol prodrug have higher anti-tumor activity and lower toxicity than self-assembled nanoparticles of a docetaxel-straight chain fatty alcohol prodrug.
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
A61K 47/69 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
The present invention relates to a cabazitaxel prodrug anti-tumor preparation, designs and synthesizes a cabazitaxel-fatty alcohol small molecule prodrug containing different fatty alcohol side chains and different connecting chains of general formulas (I), (II) and (III), and prepares a self-assembly nanoparticle. A result shows that the cabazitaxel-fatty alcohol small molecule prodrug self-assembly nanoparticle can effectively improve a curative effect of cabazitaxel and reduce toxic and side effects thereof. The length of a side chain of a branched chain fatty alcohol, the structure of the side chain of the fatty alcohol, the composition of a connecting chain element and the length of a connecting chain can significantly affect the pharmaceutical property and the anti-tumor activity of the cabazitaxel prodrug self-assembly nanoparticle. The prodrug self-assembly nanoparticle has higher anti-tumor activity and lower toxicity than a cabazitaxel-linear fatty alcohol small molecule prodrug self-assembly nanoparticle.
C07D 305/14 - Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
A61K 47/60 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
A61K 47/69 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
The present invention relates to the field of drug synthesis, and relates to a novel pyrazolopyrimidine derivative and an analog thereof, and a preparation method therefor and a use thereof in serving as a therapeutic agent, especially as a PLK4 inhibitor. Also disclosed are a compound of general formula (I) and a geometric isomer thereof or a pharmaceutically acceptable salt thereof, and a preparation method therefor. Preferably, the compound has activity as a protein kinase inhibitor, especially a PLK4 kinase inhibitor.
The present disclosure relates to the field of pharmaceutical chemistry, and specifically relates to an aminopyrimidine derivative having a structure represented by general formula (I) or general formula (II), a stereoisomer, pharmaceutically acceptable salt, hydrate, solvate or prodrug thereof, a preparation method therefor, and a use thereof in the preparation of a therapeutic agent, in particular an tropomyosin receptor kinase (TRK) inhibitor. Preferably, the aminopyrimidine derivative, the stereoisomer, pharmaceutically acceptable salt, hydrate, solvate or prodrug thereof have activity as a protein kinase inhibitor, in particular as a TRK inhibitor.
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
Provided in the present invention are an sEH inhibitor or a pharmaceutically acceptable composition thereof, and a preparation method therefor and the use thereof, which belong to the technical field of medicine. According to the sEH inhibitor or the pharmaceutically acceptable composition thereof provided by the present invention, the sEH inhibitor has a structure as represented by formula I. The sEH inhibitor provided by the present invention can stabilize an endogenous substance epoxy fatty acid having a wide range of physiological activities, has a very strong inhibitory effect on human recombinant sEH, and can obviously relieve neuropathic pain by means of various action mechanisms of adjusting the generation of various pro-inflammatory cytokines, reducing endoplasmic reticulum stress, preventing or reversing endothelial dysfunction and stabilizing mitochondrial functions, and can also effectively avoid adverse reactions related to a target. Moreover, the sEH inhibitor structure provided by the present invention contains no free carboxyl, can prevent adverse reactions, such as gastrointestinal irritation caused by oral administration, and has a low adverse reaction, a high bioavailability, an excellent analgesic effect and the dosage amount thereof is small.
A cabazitaxel weakly-alkaline derivative, preparation, and synthesis thereof, a liposome preparation containing the cabazitaxel weakly-alkaline derivative and application of the cabazitaxel weakly-alkaline derivative in a drug delivery system are provided. Cabazitaxel is connected with a weakly-alkaline intermediate through an ester bond, the ester bond can be broken under the action of esterase in vivo, and an active drug is released. A connecting group is C1-C4 alkyl, C3-C6 naphthenic base or phenyl; [N] is an N-methyl piperazinyl group, a piperidinyl group, a 4-(1-piperidinyl) piperidinyl group, a morpholinyl group, a pyrrolidine group or other tertiary amine structures. The cabazitaxel weakly-alkaline derivative can be prepared into the liposome preparation having high drug loading capacity, high encapsulation efficiency, and good stability. The in-vivo circulation time of the drug can be greatly prolonged, the accumulation amount of the drug at a tumor part is increased, and the anti-tumor effect and the tolerance dose are improved.
122 are methyl (i.e., 3,5-dimethyl substituted), the van der Waals force can be enhanced. Therefore, the memantine urea derivative provided by the present invention has high inhibiting activity on human sEH (HsEH), and can be used as an sEH inhibitor to prepare a drug for treating soluble epoxidase-mediated diseases.
C07D 211/62 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
C07D 211/60 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 211/58 - Nitrogen atoms attached in position 4
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A61P 25/00 - Drugs for disorders of the nervous system
The present invention relates to a 2-aminopyrimidine compound shown in formula I, a pharmaceutically acceptable salt, solvate or prodrug thereof, preparation methods for the 2-aminopyrimidine compound, and the pharmaceutically acceptable salt, solvate or prodrug thereof, and a pharmaceutical composition comprising the compound. Substituents R1, R2, R3, R4, X, Y, Z, Q, m, and n have meanings given in the description. The present invention further relates to the application of the compound of formula I in the preparation of a medication for treating and/or preventing a malignant hematologic disease and other proliferative diseases.
The present invention relates to a 2-aminopyrimidine compound shown in formula I, a pharmaceutically acceptable salt, solvate or prodrug thereof, preparation methods for the 2-aminopyrimidine compound, and the pharmaceutically acceptable salt, solvate or prodrug thereof, and a pharmaceutical composition comprising the compound. Substituents R1, R2, R3, R4, X, Y, Z, Q, m, and n have meanings given in the description. The present invention further relates to the application of the compound of formula I in the preparation of a medication for treating and/or preventing a malignant hematologic disease and other proliferative diseases.
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
A61P 35/02 - Antineoplastic agents specific for leukemia
A series of new-type dual-targeting degradation compounds, which have two independent inhibitor units and an E3 ligase ligand, or a pharmaceutically acceptable salt, hydrate, stereoisomer or prodrug thereof, a preparation method therefor and the use thereof in the preparation of a drug for treating or preventing tumors. The compounds can simultaneously and effectively induce E3 ligase-dependent degradation of EGFR and PARP in pancreatic cancer cell lines and 1299 cells, effectively inhibit the growth of cancer cells, solve the target diversity of advanced cancers in terms of tumor heterogeneity and the reversal of chemotherapy drug resistance, and provide a new form of treatment for treating EGFR- and PARP-mediated tumors and/or other diseases.
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A dry powder inhaler of β2-adrenergic receptor agonist Trantinterol and hydrochloride thereof, a preparation method for the dry powder inhaler, and an application of the dry powder inhaler in preparation of a drug for treating asthma and chronic obstructive pulmonary disease. The drug comprises Trantinterol as an active ingredient of the dry powder inhaler, and a surface-modified carrier; and the components consist of, by weight, 0.05%-0.25% of active ingredient and 99.75%-99.95% of surface-modified carrier. In the surface-modified carrier, one or a mixture of more of magnesium stearate, lactose, leucine, and the like is used as a surface modifier, and one or a mixture of more of lactose, mannitol, and leucine is used as a carrier. The surface modifier is added to exert the effect of surface modification on the carrier, thereby improving aerodynamic properties of a final dry powder inhaler, and facilitating better deposition of drug particles in a lung. The fluidity of the dry powder inhaler is improved, the filling is facilitated, the hygroscopicity of the drug is reduced, and storage is facilitated.
A compound for targeted degradation of focal adhesion kinase and an application thereof, relating to the technical field of medicine. Specifically relating to the compound of general formula (I) and a geometric isomer or pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, and preparation methods therefor. The compound has good degradation activity for focal adhesion kinase (FAK).
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
The present invention relates to 2,4,4-trisubstituted dihydrooxazole derivatives and preparation methods therefor and the use thereof, belonging to the technical field of pharmaceutical synthesis. Specifically, the present invention relates to a class of 2,4,4-trisubstituted dihydrooxazole derivatives and pharmaceutically acceptable salts thereof, hydrates, solvates or prodrugs thereof, preparation methods therefor, and the use thereof as drugs for treating various diseases caused by fungal infections. The general formula of the 2,4,4-trisubstituted dihydrooxazole derivative of the present invention and stereoisomers or pharmaceutically acceptable salts, hydrates, solvates or prodrugs thereof is as shown in (I): wherein MBG, X, Y, M and R1 are as described in the claims and description.
C07D 413/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
A61K 31/422 - Oxazoles not condensed and containing further heterocyclic rings
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
50.
LYMPHATIC MEDIATED TRANSPORT-BASED TRIGLYCERIDE PRODRUG, AND PREPARATION METHOD THEREFOR
In the field of medical technologies, there is a triglyceride prodrug based on lymphatic-mediated transport, particularly a triglyceride prodrug with different linking chains for lymphatic-mediated transport, and a method for preparing the same and use thereof in drug delivery. The prodrugs are linked by different linking bonds and methods for synthesizing the same. The structures of the prodrugs are as follows:
In the field of medical technologies, there is a triglyceride prodrug based on lymphatic-mediated transport, particularly a triglyceride prodrug with different linking chains for lymphatic-mediated transport, and a method for preparing the same and use thereof in drug delivery. The prodrugs are linked by different linking bonds and methods for synthesizing the same. The structures of the prodrugs are as follows:
In the field of medical technologies, there is a triglyceride prodrug based on lymphatic-mediated transport, particularly a triglyceride prodrug with different linking chains for lymphatic-mediated transport, and a method for preparing the same and use thereof in drug delivery. The prodrugs are linked by different linking bonds and methods for synthesizing the same. The structures of the prodrugs are as follows:
wherein X, R1, R2, n, m are as described in the claims and specification. A mechanism of digestion and absorption of glycerol in the gastrointestinal tract is simulated by using a triglyceride-like structure, so as to promote the lymphatic transport of the drugs and avoid a first-pass effect. The prodrugs have targeting properties and can significantly increase or improve oral bioavailability.
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
Disclosed are an indole derivative, a preparation method therefor and the use thereof; and a pharmaceutically acceptable salt, a hydrate, a solvate or a prodrug of the compound, preparation methods therefor and the use thereof as a therapeutic agent, in particular, as a PAK inhibitor. The indole derivative and a geometric isomer or a pharmaceutically acceptable salt, a hydrate, a solvate or a prodrug thereof is represented by general formula (I), wherein each variable is as described in the claims and description.
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
HEBEI UNIVERSITY OF SCIENCE AND TECHNOLOGY (China)
Inventor
Zhao, Yanfang
Gao, Zibin
Han, Yufei
Li, Shuo
Hou, Yunlei
Zhang, Huimin
Xu, Sicong
Sun, Yanping
Qin, Mingze
Sun, Yongjun
Liu, Yajing
Gong, Ping
Abstract
A compound represented by general formula (I) or stereisomers thereof and pharmaceutically acceptable salts, solvates or prodrugs thereof, a preparation method therefor and a pharmaceutical composition containing the compound. An application of the compound of general formula (I) in preparation of drugs for treating and/or preventing she-mediated diseases, especially an application in preparation of drugs for treating inflammatory diseases, cardiovascular and cerebrovascular diseases, diabetes, diabetes complications, diabetes-related diseases, fibrotic diseases, neurological and mental diseases, pain, and ulcer diseases, etc.
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 9/00 - Drugs for disorders of the cardiovascular system
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
A61P 25/00 - Drugs for disorders of the nervous system
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
The present invention relates to a compound for targeted degradation of focal adhesion kinase and a medical application thereof. The present invention belongs to the technical field of medicines and provides a compound represented by general formula (I) or a geometric isomer, pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof and a preparation method therefor. The compound has good degradation activity on FAK kinase.
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
Disclosed are a p-phenylenediamine derivative as represented by general formula I, a pharmaceutically acceptable salt, and a stereoisomer thereof. The p-phenylenediamine derivative as represented by general formula I, the pharmaceutically acceptable salt thereof and the stereoisomer thereof can be used alone or in combination as lysine-specific demethylase-1 (LSD1) inhibitors.
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 405/04 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 409/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 213/74 - Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
123456788, R, X, and L are as defined in the claims and the description of the present invention. The compound of the present invention can be used as a potent ATX inhibitor and is used for the treatment of related diseases, such as fibrosis and cancers.
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
14366 cycloalkyl or phenyl; [N] is N-methylpiperazinyl, piperidinyl, 4-(l-piperidinyl)piperidinyl, morpholinyl, tetrahydropyrrolyl, or other tertiary amine structure. The weak alkaline cabazitaxel derivative can be used to prepare a liposome formulation. The liposome formulation has the characteristics of high drug loading, high encapsulation efficiency, and good stability. After the administration by injection, the liposome formulation can greatly improve the circulation time of the drug in vivo, increase the accumulation amount of the drug in the tumor site, and improve the anti-tumor effect and tolerance dosage.
C07D 305/14 - Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
A61K 9/127 - Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
The present invention relates to the technical field of medicines, and specifically relates to a weakly acidic derivative of a poorly soluble drug and a liposome preparation thereof. According to the weakly acidic derivative, a hydroxyl-containing drug is used as a raw material, and by means of an esterification reaction, is connected to a saturated or unsaturated anhydride or diacid having different carbon length chains (elements such as oxygen, sulfur, nitrogen, and silicon can be contained in the middle of a carbon chain), so that the drug has weak acidity of different strength. The weakly acidic derivative can be actively loaded into a liposome by means of a pH gradient method. By means of a prepared liposome, the maximum tolerated dosage of the compound is significantly increased, a half-life period is prolonged, and the bioavailability of the drug can be improved, thereby achieving the purpose of enhancing an effect and reducing toxicity.
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
A61K 9/127 - Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
A61K 47/24 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
A61K 47/28 - Steroids, e.g. cholesterol, bile acids or glycyrrhetinic acid
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
11 is as described in the claims and description. The described paclitaxel derivative is actively encapsulated in an inner aqueous phase of the liposome by a pH gradient method, reducing the use of surfactants such as polyoxyethylene castor oil and Tween 80, and avoiding the generation of an allergic reaction. The prepared liposome has an encapsulation efficiency of greater than 95%, and has high drug loading capacity, good stability and long circulation in vivo, and can significantly increase the drug tolerance dosage, thereby achieving the purposes of efficacy improvement and toxicity reduction.
C07D 305/14 - Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
A61K 9/127 - Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
A61K 47/24 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
A61K 47/28 - Steroids, e.g. cholesterol, bile acids or glycyrrhetinic acid
A novel amphiphilic dual-targeting functional material belonging to the field of new auxiliary materials and new dosage forms of drug preparations, and the use thereof as a targeting material in an active targeting drug delivery system. The structural general formula of the amphiphilic targeting material is as follows: wherein A and Linker are as claimed in the claims and the description. The amphiphilic targeting material uses tyrosine as a target head, and after chemical modification, the targeting material can self-assemble to form micelles or can also be modified to the surface of a liposome or a nanoparticle, and is used as a carrier for targeted delivery of anti-tumour drugs. The material can simultaneously interact with large and medium-sized amino acid transporter 1 (LAT1) and amino acid transporter ATB0,+ expressed on tumour cell membranes by means of surface-modified tyrosine, thereby effectively improving the cellular uptake and anti-tumour activity of the nano-preparation.
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
B82Y 5/00 - Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
C08G 65/333 - Polymers modified by chemical after-treatment with organic compounds containing nitrogen
C08G 65/332 - Polymers modified by chemical after-treatment with organic compounds containing oxygen containing carboxyl groups, or halides or esters thereof
Provided is a mutant of an antibody or fragment thereof, characterized in that the antibody or fragment thereof contains a light-chain constant region, and according to the Kabat numbering system, the amino acid at position 166 is mutated to cysteine.
C07K 16/18 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
C07K 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 51/10 - Antibodies or immunoglobulinsFragments thereof
61.
2-AMINOPYRIMIDINE COMPOUND AND APPLICATION THEREOF
12344, X, Y, Z, Q, m, and n have meanings given in the description. The present invention further relates to the application of the compound of formula I in the preparation of a medication for treating and/or preventing a malignant hematologic disease and other proliferative diseases.
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/541 - Non-condensed thiazines containing further heterocyclic rings
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
The invention relates to a premix membrane emulsification based process using polyvinylpyrrolidone as a porogenic agent for the preparation of porous microparticles for inhalation formulations for pulmonary drug delivery as well as the microparticles and the pharmaceutical compositions produced hereof.
122, n, and m are described in the claims and description. According to the prodrug provided by the present invention, the digestion and absorption mechanism of glycerol in the gastrointestinal tract is simulated by using the structure of triglycerides, the lymphatic transport of drugs is promoted, the first pass effect is avoided, and the prodrug has the targeting property and can obviously enhance or improve the drug oral bioavailability.
C07D 305/14 - Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
64.
SUBSTITUTED 5-OXOPYRROLIDINE DERIVATIVE, PREPARATION METHOD THEREFOR AND USE THEREOF
A61K 31/4015 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
A61P 25/00 - Drugs for disorders of the nervous system
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
65.
INTESTINAL MCT1 CARRIER PROTEIN DESIGN-BASED PRODRUG AND PREPARATION METHOD THEREFOR
The present invention belongs to the field of medical technology and relates to an intestinal MCT1 carrier protein design-based prodrug and a preparation method therefor, and in particular relates to a preparation method for a short-chain fatty acid analogue taking an intestinal mono-carboxylate transporter 1, MCT1 as a target point, comprising design and synthesis of a prodrug structure containing hydroxyl or amino antitumor drugs modified with acetic acid, lactic acid and pyroracemic acid analogues. A series of prodrugs provided by the present invention can improve the oral bioavailability of drugs and adjust the release speed of prodrugs. The related derivative shown in formula (I) or (II), and a pharmaceutically acceptable salt, a hydrate, a solvate or a prodrug structure thereof are as follows, wherein X, Y, n and Drug have the definitions given in the description and claims.
C07H 1/00 - Processes for the preparation of sugar derivatives
C07H 19/073 - Pyrimidine radicals with 2-deoxyribosyl as the saccharide radical
A61K 31/7068 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
The invention relates to an albumin conjunction-type maleimide functionalized gemcitabine prodrug as well as application thereof in transferring an antitumor prodrug. The albumin conjunction-type maleimide functionalized gemcitabine prodrug is a compound consisting of gemcitabine and maleimide connected by virtue of an amido bond, a carbonate bond or an amino formate bond, and a maleimide group is used as an albumin 34-site cysteine free mercapto group jointed target. The prodrug compound can be rapidly specifically bonded with albumin in blood to form an albumin prodrug compound, thereby lowering the drug metabolism speed, significantly prolonging a half-life period of the drug, and realizing the long cycling effect. In addition, under the EPR effect and the albumin receptor mediation, the tumor targeting can be realized, and the antitumor effect can be improved. The gemcitabine precursor drug is used for intravenous injection and larger in market application prospect.
C07H 19/073 - Pyrimidine radicals with 2-deoxyribosyl as the saccharide radical
C07H 1/00 - Processes for the preparation of sugar derivatives
A61K 31/7068 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
The present invention relates to the technical field of medicine and relates to a polyionic complex formed by polysialic acid (PSA) and a cationic compound, a preparation method therefor and an application thereof. The polyionic complex comprises PSA and a cationic compound, wherein the mass ratio of the PSA to the cationic compound is 2: 1-50: 1; the formed polyionic complex comprises one or more cationic compounds. The polyionic complex is prepared by means of the following method: (1) dissolving a cationic compound in pure water to obtain a solution A; (2) dissolving PSA in pure water to obtain a solution B; (3) mixing the solution A with the solution B to obtain a polyionic complex (PICs) liquid. The efficacy of the polyionic complex of the present invention is significantly higher than that of a covalently coupled nanoparticle. The polyionic complex may improve the efficacy of a drug, and may also reduce the toxicity thereof.
A61K 47/61 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule the organic macromolecular compound being a polysaccharide or a derivative thereof
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
A61K 31/704 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin, digitoxin
A61K 31/136 - Amines, e.g. amantadine having aromatic rings, e.g. methadone having the amino group directly attached to the aromatic ring, e.g. benzeneamine
The present application relates to a series of redox-sensitive albumin-bound prodrugs specifically responsive to tumor tissue, and in particular, to three small-molecule docetaxel-maleimide prodrugs. A maleimide ring in the prodrug structure is used as a target for binding a free thiol group at position 34 of a plasma albumin in the body, such that the drug rapidly and specifically binds to the albumin after intravenous injection into the body and forms an albumin-drug complex, thereby enhancing drug stability and significantly prolonging the circulation time of the drug in the body. Furthermore, the EPR effect is leveraged to achieve drug accumulation in tumor tissue.
A61K 47/64 - Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
69.
METHOD FOR SYNTHESIZING 1,7-DI-(4-HYDROXYPHENYL)-HEPTANE-1,4-DIEN-3-ONE
The present invention relates to the field of pharmaceutical synthesis, and relates to a method for the synthesis of 1,7-di-(4-hydroxyphenyl)-heptane-1,4-dien-3-one. A method for synthesizing 1,7-di-(4-hydroxyphenyl)-heptane-1,4-dien-3-one uses 3-(4-hydroxyphenyl)propionic acid and 4-hydroxybenzaldehyde as raw materials, and comprises the following steps: (I) using 3-(4-hydroxyphenyl)propionic acid as a raw material, and subjecting same to esterification, methylation protection, reduction and oxidation to obtain 3-(4-(methoxymethyl)phenyl)propanal; (II) subjecting 4-hydroxybenzaldehyde to etherification and aldol condensation reaction to obtain 4-(4-(methoxymethyl)phenyl)but-3-en-2-one; and (III) performing aldol condensation reaction of 4-(4-(methoxymethoxy)phenyl)but-3-en-2-one with 3-(4-(methoxymethoxy)phenyl)propanal, and then reacting the resultant with hydrochloric acid, so as to obtain 1,7-di-(4-hydroxyphenyl)-heptane-1,4-dien-3-one. The method is simple, easy to operate, has high yield, and can acheive high purity.
C07C 45/65 - Preparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by reactions not involving the formation of C=O groups by splitting-off hydrogen atoms or functional groupsPreparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by reactions not involving the formation of C=O groups by hydrogenolysis of functional groups
C07C 49/248 - Unsaturated compounds containing keto groups bound to acyclic carbon atoms containing hydroxy groups containing six-membered aromatic rings having unsaturation outside the aromatic rings
C07C 279/16 - Derivatives of guanidine, i.e. compounds containing the group the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to carbon atoms of rings other than six-membered aromatic rings
A61K 31/196 - Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
A61K 31/215 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
A61K 31/27 - Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, e.g. meprobamate, carbachol, neostigmine
An octahydroanthracene compound having the structure shown in formula (I) and (II), preparation method and application thereof are disclosed. The octahydroanthracene compound has a good therapeutic effect on tumors and neurodegenerative diseases. The preparation of the octahydroanthracene compound is mainly carried out by using benzene as a starting material, and being subjected to Friedel-Crafts reaction, nitration, reduction, (sulfo-) amide formation, reduction, urea formation or amide formation, thus obtaining a target compound.
C07C 275/38 - Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by doubly-bound oxygen atoms
C07C 2/86 - Preparation of hydrocarbons from hydrocarbons containing a smaller number of carbon atoms by condensation between a hydrocarbon and a non-hydrocarbon
C07C 201/08 - Preparation of nitro compounds by substitution of hydrogen atoms by nitro groups
C07C 209/36 - Preparation of compounds containing amino groups bound to a carbon skeleton by reduction of nitrogen-to-oxygen or nitrogen-to-nitrogen bonds by reduction of nitro groups by reduction of nitro groups bound to carbon atoms of six-membered aromatic rings
C07C 231/02 - Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
C07C 269/04 - Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups the nitrogen atom not being part of nitro or nitroso groups from amines with formation of carbamate groups
C07C 271/28 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring to a carbon atom of a non-condensed six-membered aromatic ring
C07C 273/18 - Preparation of urea or its derivatives, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups of substituted ureas
C07C 303/38 - Preparation of esters or amides of sulfuric acidsPreparation of sulfonic acids or of their esters, halides, anhydrides or amides of amides of sulfonic acids by reaction of ammonia or amines with sulfonic acids, or with esters, anhydrides, or halides thereof
C07C 311/48 - Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups having nitrogen atoms of sulfonamide groups further bound to another hetero atom
C07D 211/62 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
C07D 295/195 - Radicals derived from nitrogen analogues of carboxylic acids
A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
C07C 259/10 - Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids having carbon atoms of hydroxamic groups bound to carbon atoms of six-membered aromatic rings
C07C 233/65 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
C07C 233/80 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
72.
Compound and use thereof and platinum complex and lipidosome thereof
Provided are a platinum complex and a liposome thereof, and a use thereof. The platinum complex contains a carboxyl group having pH sensitivity, wherein in a comparatively low pH environment (such as in tumour tissues), the carboxyl group is liable to deprotonate, facilitating an improvement in the drug release inside tumour tissues and improving the therapeutic effect of drugs. In addition, the platinum complex can be well combined with the membrane materials of lipidosomes, so as to improve the encapsulation ratio and drug loading capacity of lipidosomes. Experiments indicate that the lipidosomes of the platinum complex can reduce the toxic and side effects of drugs and increase the therapeutic effect thereof.
The preset invention relates to a new medical use of a chiral compound. The chemical name is R-/S-2-lactamide-based benzoic acid, having a structural formula shown below. The compound is originally extracted from a secondary metabolite of microorganisms, and can be obtained by means of chemical synthesis. Initial pharmacological experiments showed that the compound has good analgesic and anti-inflammatory activities, and had less stimulation a gastrointestinal tract. Recent studies show that an enantiomer of the compound has better antiplatelet agglutination and antithrombotic activities, and the compound is expected to become a new nonsteroidal antiplatelet agglutination and antithrombotic drug.
C07C 235/16 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
A61K 31/196 - Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
The present invention falls within the technical field of medicine and relates to amide and thioamide derivatives and preparation methods therefor and the use thereof, and particularly relates to derivatives of the general formula (I) and geometrical isomers thereof or pharmaceutically acceptable salts, hydrates, solvates and prodrugs thereof and the preparation methods therefor. The derivatives have an activity as protein kinase inhibitors, especially PAK kinase inhibitors.
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
The present invention relates to the technical field of medicine, and provides mosapride active metabolites (R)-N-[2-hydroxy-3-(4-fluorobenzyl)amino]propyl-5-chloro-4-amino-2-ethoxy benzamide (levo isomer) and (S)-N-[2-hydroxy-3-(4-fluorobenzyl)amino]propyl-5-chloro-4-amino-2-ethoxy benzamide (dextro isomer), salts thereof, a synthesis method for (R,S)-N-[2-hydroxy-3-(4-fluorobenzyl)amino]propyl-5-chloro-4-amino-2-ethoxy benzamide (racemate), and applications in gastrointestinal tract motility drug preparation. The present invention also relates to a drug composition comprising the three active ingredients and applications in gastrointestinal tract motility drug preparation. By means of the present invention, a mouse small intestine charcoal powder propelling model is used for respectively investigating the gastrointestinal motility promoting effects of the levo isomer, the dextro isomer and the racemate, and the results show that under the same dose, the activity of the levo isomer is relatively weak, the racemate and the dextro isomer have significant gastrointestinal motility promoting effects, and the activity of the dextro isomer is significantly surprior to the activity of the racemate.
C07C 237/44 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having carbon atoms of carboxamide groups, amino groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
C07C 231/02 - Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
C07C 231/12 - Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
C07C 231/18 - Preparation of optical isomers by stereospecific synthesis
C07C 215/18 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic with hydroxy groups and at least two amino groups bound to the carbon skeleton
C07D 209/48 - Iso-indolesHydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
A61K 31/166 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon atom of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
Disclosed are an opctahydroanthracene compound as represented by formula (I) or (II), a preparation method for same, and uses of same, which provides great therapeutic effects for tumors and neurodegenerative diseases and is prepared mainly with benzene that serves as the starting material and undergoes reactions such as Friedel-Crafts reactions, nitration, reduction, sulfonamide formation, reduction, urea formation or amide formation to produce the target compound.
C07C 233/65 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
C07C 259/10 - Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids having carbon atoms of hydroxamic groups bound to carbon atoms of six-membered aromatic rings
C07C 233/80 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
The present application relates to inhibitors of VGSCβ3 protein and use thereof and methods of using the VGSCβ3 protein or an inhibitor thereof to diagnose, prevent and treat cancer, and to screen antineoplastic agents using the VGSCβ3 Protein or its regulatory sequences.
C07K 14/435 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
C12Q 1/6886 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material for cancer
G01N 33/50 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing
G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids
A61K 39/00 - Medicinal preparations containing antigens or antibodies
Provided are a platinum complex and a lipidosome thereof, and a use thereof. The platinum complex contains a carboxyl group having pH sensitivity, wherein in a comparatively low pH environment (such as in tumour tissues), the carboxyl group is liable to deprotonate, facilitating an improvement in the drug release inside tumour tissues and improving the therapeutic effect of drugs. In addition, the platinum complex can be well combined with the membrane materials of lipidosomes, so as to improve the encapsulation efficiency and drug loading capacity of lipidosomes. Experiments indicate that the lipidosomes of the platinum complex can reduce the toxic and side effects of drugs and increase the therapeutic effect thereof.
Provided are a 3-(N,N-disubstituted amino group) propanamide derivative shown in a general formula (I) and a pharmaceutically acceptable salt thereof. Also provided are a 3-(N,N-disubstituted amino group) propanamide compound and a preparation method of a derivative thereof. The general formula (I) has the following structure: R 1, R 2, R 3 and R 4, as described in the specification. Moreover, the compound and a combination thereof can be used as therapeutic agents, and can be used as cholesterylester transfer protein (CETP) inhibitors in particular.
C07D 295/185 - Radicals derived from carboxylic acids from aliphatic carboxylic acids
C07D 213/75 - Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
C07C 237/04 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
C07C 311/21 - Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
C07C 311/29 - Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
C07C 231/02 - Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
C07C 231/12 - Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
C07C 303/40 - Preparation of esters or amides of sulfuric acidsPreparation of sulfonic acids or of their esters, halides, anhydrides or amides of amides of sulfonic acids by reactions not involving the formation of sulfonamide groups
A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
A61P 9/00 - Drugs for disorders of the cardiovascular system
The present invention relates to the technical field of chemical synthesis, and in particular to a cyclic oligomeric carbazole derivative, a preparation method therefor, and an application thereof. A structural formula of the cyclic oligomeric carbazole derivative of the present invention is shown as Formula (I), where each variable is described in the specification and claims. The method of the present invention can prepare a plurality of new large oligomeric rings by means of only one-step reaction. The oligomeric carbazole of the present invention has an excellent optical performance, and can be detected by an ultraviolet instrument and a fluorometer. The present invention enables a synthetic oligomeric carbazole structure to have richer π electrons, and the synthetic oligomeric carbazole structure and cationic quaternary ammonium of a positive charge can form a host-guest compound based on a 'cation-π' weak interaction force.
C07D 487/22 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups in which the condensed system contains four or more hetero rings
C07D 209/86 - CarbazolesHydrogenated carbazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the ring system
C07D 209/88 - CarbazolesHydrogenated carbazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the ring system
81.
PROCESS FOR THE PREPARATION OF POROUS MICROPARTICLES
The invention relates to a single-emulsion based process using polyvinylpyrrolidone as a porogenic agent for the preparation of porous microparticles for inhalation formulations for pulmonary drug delivery as well as the microparticles and the pharmaceutical compositions produced hereof.
Disclosed are an inhibitor of a VGSC β3 protein and uses thereof; a method for diagnosing, preventing and treating cancers using the VGSC β3 protein or an inhibitor thereof; and a method for screening anti-tumour drugs using the VGSC β3 protein or regulatory sequences thereof.
4 are as defined in the Description. The derivatives and compositions thereof can be prepared into clinically acceptable tablets, capsules, injections, ointments, etc., and thus have pharmaceutical uses in the treatment and/or prevention of cancers.
An application of large-dose glycerinum in freeze-thawing tolerable lipid emulsion and freeze-thawing tolerable lipid emulsion. The lipid emulsion comprises oily solution, glycerinum, phospholipid and water, the content of the glycerinum in the ingredients of the emulsion is greater than or equal to 3 w/v%, and the maximum content of the glycerinum in the ingredients of the emulsion is 50 w/v%. When the content of the oily solution in the ingredients of the emulsion is 2 w/v% to 30 w/v%, the content of the glycerinum is greater than or equal to 1/3 of the oil content in the emulsion. Drugs can be added in the lipid emulsion to obtain drug-containing emulsion, so the stability of drug products is improved and the cost of drugs is reduced.
CHINA RESOURCES SANJIU MEDICAL & PHARMACEUTICAL CO., LTD. (China)
Inventor
Gong, Ping
Zhao, Yanfang
Liu, Yajing
Zhai, Xin
Abstract
2, X, Y and n are defined as claims. And the compounds of general formula I show potent inhibitory activity against c-Met kinase. The present invention further relates to the uses of the compounds, pharmaceutically acceptable salts and hydrates for the preparation of medicaments for the treatment and/or prevention of diseases caused by abnormal expression of c-Met kinase, especially for treatment and/or prevention of cancer.
C07D 215/42 - Nitrogen atoms attached in position 4
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
86.
6, 7-DIMETHOXY-1, 2, 3, 4-TETRAHYDROISOQUINOLINE DERIVATIVE AND MANUFACTURING METHOD THEREOF, PHARMACEUTICAL COMPOSITION COMPRISED THEREOF, AND APPLICATION THEREOF
Disclosed in the present invention is a formula (I) compound and manufacturing method thereof, pharmaceutical composition comprised thereof, and application thereof, wherein R, R1 and R2 are as defined herein. The compound set forth in the present invention shows good activity in in-vitro anti-tumour tests, and has good physiological activity.
C07D 217/16 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring other than aralkyl radicals substituted by oxygen atoms
A61K 31/472 - Non-condensed isoquinolines, e.g. papaverine
The invention belongs to the technical field of medicines and relates to a nitrogen-heterocyclic-substituted dihydroartemisinin derivative described by formulae I and II and an optical isomer thereof, wherein substituents of X, Y, R, R1, R2, R3 and R4 are defined as in the description. The derivative and the composition thereof can be made into clinically acceptable tablets, capsules, injections, ointments, et cetera for use in medicines for treating and/or preventing various cancers.
A61K 31/4025 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
A61K 31/453 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61K 31/366 - Lactones having six-membered rings, e.g. delta-lactones
The present invention relates to a heterocyclic ring-containing 5-hydroxy indole derivative as represented by formula I, comprising a racemate of the derivative, an optical isomer of same, and a pharmaceutically acceptable salt and/or hydrate thereof, where substituent R1, R2, X, Y, and Z have the meanings as provided in the description. The compound of formula I is applicable in preparing a medicament for treatment and/or prevention of viral infections, and particularly for preparing an anti-hepatitis B virus medicament and anti-influenza virus medicament.
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61P 31/16 - Antivirals for RNA viruses for influenza or rhinoviruses
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
The present invention relates to quinoline derivatives as represented by general formula I and pharmaceutically acceptable salt, hydrate or prodrug thereof, wherein the substituents M, R1, R2, X, Y and n are as defined in the specification. The present invention also relates to the use of the compounds as represented by general formula I as a c-Met kinase inhibitor, and also relates to the uses of the compounds and pharmaceutically acceptable salt and hydrate thereof in the preparation of drugs for treating the diseases caused by the abnormally high expression of c-Met kinase, in particular to the uses thereof in the preparation of drugs for treating and/or preventing cancers.
Provided is a 2-(3-cyan-4-isobutoxyphenyl)-4-methyl-1, 3-selenazole-5- formic acid compound as represented by formula I, or pharmaceutically acceptable salt, hydrate, solvate and pro-drug thereof. Also provided are a preparation method and uses thereof. The compound as represented by formula I has the capability of reducing uric acid content in blood, and can be used to treat hyperuricemia and relevant diseases caused by hyperuricemia.
A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
A61P 19/06 - Antigout agents, e.g. antihyperuricemic or uricosuric agents
91.
COMPOUND WITH XANTHINE OXIDASE INHIBITORY ACTIVITY AND SALT THEREOF, PREPARATION METHOD AND USAGE FOR THE SAME
Compound with xanthine oxidase inhibitory activity and salt, a midbody, a preparation method, and pharmaceutical composition thereof are provided. The preparation method of the compound is simple and easy to be implemented. The product can be used as an inhibitor of the xanthine oxidase, and used for curing or preventing hyperuricemia or gout disease.
C07D 233/54 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
A61P 19/06 - Antigout agents, e.g. antihyperuricemic or uricosuric agents
A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
SHENYANG PHARMACEUTICAL UNIVERSITY (BENXI) PHARMACEUTICAL SCIENCE AND TECHNOLOGY CO., LTD. (China)
Inventor
Gong, Ping
Zhao, Yanfang
Liu, Yajing
Zhai, Xin
Li, Sai
Zhu, Wufu
Qin, Mingze
Abstract
Disclosed are quinoline and cinnoline derivatives shown in general formula I, and pharmaceutically acceptable salts, hydrates, solvates and prodrugs thereof. The compounds of general formula I have strong effect in restraining c-Met kinase. Disclosed also is the use of the compounds, the pharmaceutically acceptable salts and hydrates thereof in preparing drugs for treating diseases caused by c-Met kinase overexpression, particularly in preparing drugs for treating and/or preventing a cancer.
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/502 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A solid dispersion and solid dispersion microsphere of paclitaxel or a homologue thereof and a preparation method therefor. By means of preparing a solid dispersion and solid dispersion microsphere to improve the rapid release in vivo and in vitro of paclitaxel or a homologue thereof, and by maintaining a supersaturated drug concentration or, in the case of high molecularity, increasing the apparent solubility of the drug, the bioavailability of the drug is increased. The solid dispersion carrier of paclitaxel or a homologue thereof is either hydroxypropyl methylcellulose acetate succinate or hypromellose phthalate or a mixture thereof or a silica gel-based micropowder mixture. The prepared solid dispersion microsphere has a particle size of between 100 and 600 μm and a yield rate of over 80%; the appropriate drug content therefore is between 5% and 40%.
Disclosed are furo[3,2-g]chromene derivatives represented by formula (I), stereoisomers, pharmaceutically acceptable salts, and pharmaceutical compositions thereof, as well as uses thereof as estrogen receptor modulators.
A61K 31/35 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
A61K 31/352 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. cannabinols, methantheline
Disclosed are cardenolide compounds of general formula (I) ,wherein R1 = CH3, CHO or CH2OH, R2 = H or is a linear or branched carbohydrate chain consisting of carbohydrates. The cardenolide compounds are obtained by separation of Streptocaulon juventas from Streptocaulon griffithii. The compounds have the effect of inhibiting tumour cells, such as the cells of cervical cancer, colon cancer, lung cancer, leukemia, gastric cancer, liver cancer, etc.
A61K 31/585 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin containing lactone rings, e.g. oxandrolone, bufalin
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
C07J 19/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, substituted in position 17 by a lactone ring
Provided is a kind of scorpion venom-derived peptide with analgesic activity and the preparation method thereof, and the amino acid sequence of the said peptide is shown as SEQ ID No:1. Also provided are derivatives and active fragments of the said peptide and the preparation methods thereof. The said peptide with analgesic activity can be mixed with pharmaceutically acceptable carriers to prepare injection, oral formulation, formulation for transdermal absorption, formulation for mucosal absorption and the like.
C07K 14/435 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
A61P 25/04 - Centrally acting analgesics, e.g. opioids
A disulfiram formulation comprising disulfiram or a derivative thereof together with a component that increases the in vivo half life of the disulfiram or the derivative thereof, and uses thereof. In particular for use with or without a separate copper formulation for the treatment of cancer.
A61K 31/145 - Amines, e.g. amantadine having sulfur atoms, e.g. thiurams (N—C(S)—S—C(S)—N or N—C(S)—S—S—C(S)—N)Sulfinylamines (—N=SO)Sulfonylamines (—N=SO2)
A61K 9/127 - Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
The present invention provides an active peptide derived from scorpions, and derivatives, analogues, and active fragments thereof. The peptide is obtained from scorpions through extraction, separation, and purification, and has an amino acid sequence of VKDGYIADDRNCPYFCGRNAYCDGECKKNRAESGYCQWASKYGNACWCYKLPDDARIMKPGRCNGG. The present invention further provides a use of the peptide in preparation of an analgesic drug, where the peptide is mixed with a pharmaceutically acceptable carrier to prepare into forms for injection, oral administration, transdermal absorption, and transmucosal absorption.
C07K 1/16 - ExtractionSeparationPurification by chromatography
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
99.
CURCUMALACTONE DERIVATIVES WITH ANTITUMOR ACTIVITY AND PREPARATION PROCESS THEREOF
The invention relates to the field of medicine. Curcumalactone derivatives with antitumor activity and the process for their preparation are disclosed. The said curcumalactone derivatives and their oxidized derivatives have a spironolactone structure as in formula (I). The preparation process for these compounds are also provided, wherein biotransformation is used. The intermediates of the process as in formula (II) are disclosed. The present compounds have antitumor activity.
C07D 307/94 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom spiro-condensed with carbocyclic rings or ring systems, e.g. griseofulvins
C07D 407/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C12P 17/04 - Oxygen as only ring hetero atoms containing a five-membered hetero ring, e.g. griseofulvin
C12P 17/16 - Preparation of heterocyclic carbon compounds with only O, N, S, Se, or Te as ring hetero atoms containing two or more hetero rings
C12P 17/18 - Preparation of heterocyclic carbon compounds with only O, N, S, Se, or Te as ring hetero atoms containing at least two hetero rings condensed among themselves or condensed with a common carbocyclic ring system, e.g. rifamycin
Disclosed are furo[3,2-g]chromene derivatives represented by formula (I), stereoisomers and pharmaceutically acceptable salts, pharmaceutical compositions and uses thereof as estrogen receptor modulators.
A61K 31/352 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. cannabinols, methantheline
A61P 19/08 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
A61P 19/10 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
patents
