Provided is a composition comprising Aflibercept and a variant thereof, wherein the variant is a truncated variant of the VEGF-binding moiety of Aflibercept, and the content of the truncated variant is less than or equal to about 20% by mass. Further provided are a pharmaceutical formulation comprising the described composition and a preparation method therefor. In addition, further provided are a detection method for the described variant and use thereof in quality inspection or quality control of an Aflibercept-containing product.
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
C07K 14/71 - ReceptorsCell surface antigensCell surface determinants for growth factorsReceptorsCell surface antigensCell surface determinants for growth regulators
C12Q 1/37 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving hydrolase involving peptidase or proteinase
G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids
C12P 21/06 - Preparation of peptides or proteins produced by the hydrolysis of a peptide bond, e.g. hydrolysate products
2.
COMPOSITION COMPRISING AFLIBERCEPT AND A VARIANT THEREOF, AND RELATED METHODS AND USES
Provided is a composition comprising aflibercept and a variant thereof, wherein the variant is a truncation variant with a truncated VEGF binding portion of aflibercept, and wherein the content of the truncation variant is less than or equal to about 20% by mass percentage. Also provided is a pharmaceutical formulation comprising the composition. Further, provided are a method for detecting the variant and use of the variant in quality inspection or quality control of an aflibercept-containing product.
C07K 14/71 - ReceptorsCell surface antigensCell surface determinants for growth factorsReceptorsCell surface antigensCell surface determinants for growth regulators
C12Q 1/37 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving hydrolase involving peptidase or proteinase
G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids
Provided in the present application are an isoxazoline compound as shown in formula (I), a pharmaceutical composition thereof, and the use thereof in the prevention or treatment of infestation or infection by animal parasites. The compound has excellent insecticidal and acaricidal activities against internal or external parasites of mammals, poultry or fishes.
C07D 261/04 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
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
A01N 43/80 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms, as ring hetero atoms five-membered rings with one nitrogen atom and either one oxygen atom or one sulfur atom in positions 1,2
A01N 47/30 - Derivatives containing the group N—CO—N—aryl or N—CS—N—aryl
A01N 47/34 - Ureas or thioureas containing the groups N—CO—N or N—CS—N containing the groups , e.g. biuretThio-analogues thereofUrea-aldehyde condensation products
A01N 47/40 - Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom not being member of a ring and having no bond to a carbon or hydrogen atom, e.g. derivatives of carbonic acid the carbon atom having a double or triple bond to nitrogen, e.g. cyanates, cyanamides
Provided is a pharmaceutical composition containing an anti-GPC3 and CD3 bispecific antigen binding molecule and an excipient. The pharmaceutical composition has an excellent antibody stability.
The present invention pertains to the technical field of drug application and particularly relates to clinical use of a KRAS G12D inhibitor. The inhibitor can be clinically used to effectively treat patients with advanced solid tumors carrying the KRAS G12D mutation and can produce beneficial effects.
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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
6.
CRYSTAL FORM OF SPIROCYCLIC AMINE ARYL PHOSPHORUS OXIDE COMPOUND AND PREPARATION METHOD THEREFOR
The present invention relates to a crystal form of a compound of Formula (I), i.e. (2-((5-chloro-2-((2-methoxy-4-(9-methyl-3,9-diaza-spiro[5.5]undecan-3-yl)phenyl)amino)pyrimidin-4-yl)amino)phenyl)dimethylphosphine oxide. The present invention further relates to a pharmaceutical composition of the crystal form, and the pharmaceutical use thereof and a preparation method therefor.
The present invention relates to a crystal form of a compound of Formula (I), i.e. (2-((5-chloro-2-((2-methoxy-4-(9-methyl-3,9-diaza-spiro[5.5]undecan-3-yl)phenyl)amino)pyrimidin-4-yl)amino)phenyl)dimethylphosphine oxide. The present invention further relates to a pharmaceutical composition of the crystal form, and the pharmaceutical use thereof and a preparation method therefor.
C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
Provided in the present invention are a polymorph and salt form of a compound 2-(4-cyclopropyl-6-methoxypyrimidine-5-yl)-9-((2-(trifluoromethyl)-6,7-dihydro-5H-benzo[c]imidazo[1,2-a]azolin-9-yl)methyl)-9H-pyrimido[4,5-b]indole-7-nitrile of formula (I). The polymorph and salt form provided by the present invention have good chemical stability and physical stability, low hygroscopicity, and are less affected by heat, humidity and illumination, thereby facilitating storage and preparation into formulations.
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 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
Provided is a stable pharmaceutical composition comprising an anti-PD-1 antibody. More particularly, the present invention relates to a pharmaceutical composition of pembrolizumab. The stability of the composition is ensured while the viscosity of a formulation is reduced, effectively solving the problems of high-concentration antibody formulations in drug manufacturing, storage and transportation, and drug delivery.
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
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 47/34 - 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 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
A61K 9/19 - Particulate form, e.g. powders lyophilised
The present disclosure provides a high drug-loading fulvestrant pharmaceutical composition and a preparation method thereof, and the pharmaceutical composition comprises an active ingredient, an excipient, and an aqueous carrier, free of ethanol and an oily substrate, wherein the active ingredient is fulvestrant or an ester derivative of fulvestrant, the excipient comprises one or more selected from the group consisting of a wetting agent, a suspending agent, a buffer agent, and an osmotic pressure regulator, the active ingredient is dispersed in the aqueous carrier, the excipient is dissolved in the aqueous carrier, and a concentration of the active ingredient is from 150 mg/ml to 550 mg/ml, calculated on the basis of fulvestrant itself. The pharmaceutical composition of the present disclosure has a high concentration of the drug, and can effectively reduce the dosing volume to about 2 ml-8 ml, and achieve an efficient drug delivery for high-dose treatment of patients. The pharmaceutical composition of the present disclosure can be administered by intramuscular injection to obtain a sustained release of the drug for up to 1-3 months, thereby effectively improving the patient compliance.
A61K 31/565 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol
Provided is a pharmaceutical composition containing anti-CTLA-4 and anti-PD-1 mixed antibodies, which has an excellent effect in terms of the stability, the safety, and the therapeutic efficacy, thereby effectively solving the problems of poor stability and high toxicity of a pharmaceutical composition containing anti-CTLA-4 and anti-PD-1 mixed antibodies.
Provided is a triple-agonist polypeptide compound having activation efficacy for three receptors, i.e., GLP-1R, GIPR, and GCGR. The polypeptide compound has strong target activation efficacy, and exhibits excellent effects in lowering blood glucose and blood lipids and controlling body weight. Further provided is a use of the polypeptide compound in the treatment of metabolic-related diseases, especially type II diabetes and related diseases thereof.
Provided is a composition comprising aflibercept and a variant thereof, wherein the variant is a truncation variant with a truncated VEGF binding portion of aflibercept, and wherein the content of the truncation variant is less than or equal to about 20% by mass percentage. Also provided is a pharmaceutical formulation comprising the composition. Further, provided are a method for detecting the variant and use of the variant in quality inspection or quality control of an aflibercept-containing product.
C07K 14/71 - ReceptorsCell surface antigensCell surface determinants for growth factorsReceptorsCell surface antigensCell surface determinants for growth regulators
C12Q 1/37 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving hydrolase involving peptidase or proteinase
G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids
14.
PHARMACEUTICAL PREPARATION OF ANTI-HUMAN CCR8 MONOCLONAL ANTIBODY AND USE THEREOF
SHANGHAI QILU PHARMACEUTICAL RESEARCH AND DEVELOPMENT CENTRE LTD. (China)
Inventor
Li, Huihui
Zhang, Le
An, Zhenming
Liu, Jun
Sun, Lixia
Li, Na
Shen, Qinyong
Yang, Yong
Cao, Yawen
Abstract
Provided are a stable pharmaceutical preparation of an anti-human CCR8 monoclonal antibody and the use thereof. The pharmaceutical preparation of the anti-human CCR8 antibody is very stable, can still meet the requirements for pharmaceutical use after enduring long-term storage, high temperatures or low temperatures, freeze-thaw cycles and oscillation, and has wide application prospects.
Crystal forms of Entrectinib and preparation method therefor, such as crystal form A and crystal form B of Entrectinib are provided. Compared with existing crystal forms of Entrectinib, the crystal form has better solubility, chemical and crystal form stability, is free of static electricity, has good fluidity, is easy for large-scale preparation, and can be better suitable for preparing pharmaceutical formulations and large-scale production.
C07D 405/14 - 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 three or more hetero rings
16.
USE OF 3CLPRO INHIBITOR IN PREPARATION OF DRUG FOR TREATING DISEASES CAUSED BY FELINE CORONAVIRUS
A use of a 3CLpro inhibitor in the preparation of a drug for treating diseases caused by feline coronavirus, specifically, a compound represented by formula (I) or a pharmaceutically acceptable salt thereof.
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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 401/06 - 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 401/14 - 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 11/00 - Drugs for disorders of the respiratory system
Provided in the present application are the use of a compound represented by formula (I) or pharmaceutically acceptable salts thereof in the preparation of drugs used for treating mast cell tumors in non-human mammals, and a method of using same to treat mast cell tumors in non-human mammals.
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
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 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
A crystal form of a compound of formula (I) that serves as a PARP7 inhibitor, a crystal form of a pharmaceutically acceptable salt of the compound of formula (I), and the use thereof in the preparation of a drug for treating related diseases.
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 403/14 - 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 31/4412 - Non-condensed pyridinesHydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
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
Provided is a preparation method for a PARP7 inhibitor. The method has high reaction yield, short reaction period and simple aftertreatment, and is suitable for industrial production. Further provided are an intermediate for the preparation of a PARP7 inhibitor and a synthesis method for the intermediate.
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
20.
PHARMACEUTICAL COMPOSITION, AND PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
A pharmaceutical composition, and a preparation method therefor and an application thereof. The pharmaceutical composition comprises a spiro-aryl phosphorus oxide or a pharmaceutically acceptable salt thereof as an active ingredient and a pharmaceutically acceptable carrier. D90 of the spiro-aryl phosphorus oxide or the pharmaceutically acceptable salt thereof is in a range of 40.3 μm to 79.6 μm. The pharmaceutical composition has high content uniformity, a high dissolution rate, and high in-vivo bioavailability, and can be used for treating cancer.
The present invention provides an inhalation spray of Semaglutide with good patient compliance and high bioavailability at the targeted site, which belongs to the technical field of pharmaceutical preparation. The inhalation spray of Semaglutide according to the invention comprising, by weight to volume, 0.01% to 20% of Semaglutide in the inhalation spray, wherein the proportion of fine particles with a particle size less than 5 μm formed after the inhalation spray is atomized by a spray device is not less than 10%. The inhalation spray of Semaglutide according to the invention has a simple formulation, low toxic and side effects, atomization administration of the medicinal liquid through an inhalation device, uniform distribution of spray droplets, a high lung deposition rate, low irritation and convenient administration, which is suitable for industrial production. The invention further provides a preparation method of the inhalation spray of Semaglutide.
Provided is a stable high-concentration self-buffering pharmaceutical composition, comprising a VEGF binding molecule, a stabilizer, a surfactant, and the like. The pH of the composition is 5.0-7.0. The pharmaceutical composition features no additionally added buffering agent, very high stability, convenient storage, and wide application prospects.
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61K 31/498 - Pyrazines or piperazines ortho- or peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
The present invention relates to a crystal form of a compound of formula (I), i.e. (2-((5-chloro-2-((2-methoxy-4-(9-methyl-3,9-diaza-spiro[5.5]undecane-3-yl)phenyl)amino)pyrimidin-4-yl)amino)phenyl)dimethylphosphine oxide. The present invention further relates to a pharmaceutical composition of the crystal form, and the pharmaceutical use thereof and a preparation method therefor.
C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
The present application provides a polymorph of a compound of formula (A), i.e., N-(1-((4-((3S,5S)-3,5-dimethylpiperazine-1-yl)phenyl)sulfonyl)piperidin-4-yl)-4-((S)-tetrahydrofuran-3-yl)oxy)-5(trifluoromethyl)pyrimidine-2-amine, and a polymorph of a phosphate of the compound of formula (A). A crystalline form provided by the present application has good chemical stability and physical stability, and low hygroscopicity, is less affected by temperature, humidity, and illumination, and facilitates storage and preparation development.
C07D 405/14 - 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 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 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
Provided are a class of compounds, represented by formula (I′″), as selective EGFR inhibitors, a pharmaceutical composition containing the compounds, useful intermediates for preparing the compounds, and a method for using the compounds of the present invention to treat cell proliferative diseases, such as cancers.
Provided are a class of compounds, represented by formula (I′″), as selective EGFR inhibitors, a pharmaceutical composition containing the compounds, useful intermediates for preparing the compounds, and a method for using the compounds of the present invention to treat cell proliferative diseases, such as cancers.
C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
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
Disclosed in the present invention are a pharmaceutical composition comprising a mixed antibody of anti-CTLA4 and anti-PD1, a pharmaceutical composition comprising the mixed antibody and a chemotherapeutic drug, and use of the above pharmaceutical composition in treating non-small cell lung cancer.
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
The present disclosure relates to an anti-CTLA4 and anti-PD1 antibody mixture or use of the antibody mixture in combination with a chemotherapeutic drug and/or an anti-angiogenic agent to treat hepatocellular carcinoma.
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 39/00 - Medicinal preparations containing antigens or antibodies
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
Provided are an anti-CTLA4 and anti-PD1 antibody mixture, a combination of the antibody mixture, a chemotherapeutic drug and an anti-angiogenic agent, and use thereof for treating colorectal cancer.
A61K 39/00 - Medicinal preparations containing antigens or antibodies
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
30.
PHARMACEUTICAL COMPOSITION CONTAINING MIXED ANTIBODY OF ANTI-CTLA4 AND ANTI-PD1 AND THERAPEUTIC USE THEREOF
Provided is a use of a combination chemotherapy agent containing a mixed antibody of anti-CTLA4 and anti-PD1, for example, carboplatin/cisplatin and etoposide, in treating small cell lung cancer.
The present disclosure relates to the use of a pharmaceutical composition comprising mixed antibodies anti-CTLA4 and anti-PD1 in combination with lenvatinib to treat kidney cancer.
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
32.
DRUG COMPOSITION OF SPIRO ARYL PHOSPHINE OXIDE AND ANTI-VEGF ANTIBODY
Disclosed in the present invention is a drug composition of an ALK inhibitor and an antibody, the drug composition comprising a spiro aryl phosphine oxide and an anti-VEGF antibody, and the ALK inhibitor being a compound of formula (I) or a pharmaceutically acceptable salt thereof. The drug composition disclosed by the present invention is used for treating lung cancer and shows high anti-tumor activity.
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
Disclosed is a pharmaceutical combination of an ALK inhibitor and an antibody, which comprises a spirocyclic aryl phosphorus oxide and an anti-EGFR antibody, wherein the ALK inhibitor is a compound of formula (I) or a pharmaceutically acceptable salt thereof. The pharmaceutical combination of the present invention is used for treating lung cancer and displays good anti-tumor activity.
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
The present invention provides a novel aminopyrimidine compound as a fourth-generation EGFR (T790M/C797S mutation) selective inhibitor, a pharmaceutical composition comprising the compound, an intermediate useful for preparing the compound, and a method for treating a cell proliferative disease, such as a cancer, by using the compound of the present invention.
The present invention provides a novel aminopyrimidine compound as a fourth-generation EGFR (T790M/C797S mutation) selective inhibitor, a pharmaceutical composition comprising the compound, an intermediate useful for preparing the compound, and a method for treating a cell proliferative disease, such as a cancer, by using the compound of the present invention.
C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed 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 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
Provided is a compound of formula (A), N-(6-((5-bromo-2-((6-isopropyl-8-methoxy-3-methyl-3,4,5,6-tetrahydrobenzo[b]pyrazolo[4,3-D]aza-9-yl)amino)-pyrimidin-4-yl)amino)-quinoxaline-5-yl)methanesulfonamide, and a compound of formula (I), and polymorphs thereof. The provided polymorphs have a good chemical stability, physical stability and low hygroscopicity, are less affected by heat, humidity and illumination, and are convenient to store and prepare.
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 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
The present invention provides a use of a compound represented by formula (A) or a pharmaceutically acceptable salt thereof in the preparation of drugs for treating cancer mediated by EGFR, FGFR2, KIT, ALK and/or ROS1 mutations. The compound has obvious inhibitory activity against cancer mediated by these mutation types.
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 31/495 - 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
The present invention relates to a high-concentration anti-HER2 antibody preparation and use thereof. The antibody preparation of the present invention does not have an additional buffering agent, but has high-concentration protein self-buffering, so that the impact of histidine oxidation products such as aspartate and formamide on the activity of the antibody is reduced. The preparation can fully prevent protein aggregation, degradation, oxidation or denaturation and the like, so that the biological activity of effective components of the preparation is maintained, and the preparation is suitable for clinical use.
Disclosed is a biarylamide compound as a Pan-RAF kinase inhibitor, and specifically disclosed are a compound as shown in formula (III) and a pharmaceutically acceptable salt thereof.
Disclosed is a biarylamide compound as a Pan-RAF kinase inhibitor, and specifically disclosed are a compound as shown in formula (III) and a pharmaceutically acceptable salt thereof.
C07D 405/14 - 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 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
C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
A pharmaceutical composition, and a preparation method therefor and an application thereof. The pharmaceutical composition comprises a spiro-aryl phosphorus oxide or a pharmaceutically acceptable salt thereof as an active ingredient and a pharmaceutically acceptable carrier. D90 of the spiro-aryl phosphorus oxide or the pharmaceutically acceptable salt thereof is in a range of 40.3 μm to 79.6 μm. The pharmaceutical composition has high content uniformity, a high dissolution rate, and high in-vivo bioavailability, and can be used for treating cancer.
Provided are an anti-CLDN18.2 antibody or an antigen-binding fragment thereof, a derivative comprising said antibody or antigen-binding fragment thereof, a pharmaceutical composition, and related use of said antibody or antigen-binding fragment thereof for treating, diagnosing and detecting cancers.
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 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
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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
The present invention relates to a crystal form of Entrectinib and a preparation method therefor, and specifically relates to a crystal form A and crystal form B of Entrectinib. Compared with existing crystal forms of Entrectinib, the crystal form has better solubility, chemical and crystal form stability, is free of static electricity, has good fluidity, is easy for large-scale preparation, can be better suitable for preparing pharmaceutical formulations and large-scale production, and has a wide application prospect.
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 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
Provided are an anti-CLDN18.2 ADCC-enhanced humanized antibody, a pharmaceutical composition comprising the antibody and a related application thereof in treatment of cancers.
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 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
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
C12N 5/20 - Murine cells, e.g. mouse cells one of the fusion partners being a B lymphocyte
Provided are a class of compounds, represented by formula (I"'), as selective EGFR inhibitors, a pharmaceutical composition containing the compounds, useful intermediates for preparing the compounds, and a method for using the compounds of the present invention to treat cell proliferative diseases, such as cancers.
C07D 223/14 - Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
C07D 243/00 - Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
C07D 313/06 - Seven-membered rings condensed with carbocyclic rings or ring systems
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 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 31/495 - 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
The present invention provides a novel aminopyrimidine compound as a fourth-generation EGFR (T790M/C797S mutation) selective inhibitor, a pharmaceutical composition comprising the compound, an intermediate useful for preparing the compound, and a method for treating a cell proliferative disease, such as a cancer, by using the compound of the present invention.
C07D 403/10 - 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 aromatic 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
C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
A61K 31/5386 - 1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
Disclosed in the present disclosure are a crystal form of a β-lactamase inhibitor and a preparation method therefor, as well as an application of the crystal form in preparing a β-lactamase inhibitor drug. (I)
Provided are an anti-CLDN18.2 antibody or an antigen-binding fragment thereof, a derivative comprising said antibody or antigen-binding fragment thereof, a pharmaceutical composition, and related use of said antibody or antigen-binding fragment thereof for treating, diagnosing and detecting cancers.
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 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
C12N 5/20 - Murine cells, e.g. mouse cells one of the fusion partners being a B lymphocyte
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Medicines for human purposes; pharmaceutical preparations;
vitamin preparations; drugs for medical purposes; ointments
for pharmaceutical purposes; antibiotics; preparations of
microorganisms for medical or veterinary use; crude drugs;
medicines for veterinary purposes; veterinary preparations.
48.
Polymorphic form of compound, preparation method and use thereof
The present disclosure relates to polymorphic forms of the compound methyl (3R,6S)-6-amino-sulfonylamino-1-(thiazol-2-yl)-3-(2,3,4-trifluorophenyl)-3,5,6,7-tetrahydropyrrolo[1,2-c]pyrimidin-4-formate (compound 1). The present disclosure further relates to a pharmaceutical composition and pharmaceutical use and a preparation method of the polymorphic forms of compound 1.
Disclosed in the present invention is a type of novel β-lactamase inhibitors, and specifically disclosed are a compound represented by formula (I) or a pharmaceutically acceptable salt thereof.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Anti-infective preparations for veterinary purposes; anti-infectives; anti-inflammatory ointments; antibiotics for human use; antibiotics for veterinary purposes; mixed antibiotic preparations; penicillin preparations; pharmaceutical preparations for the treatment of digestive diseases; pharmaceutical preparations for treating respiratory diseases; vitamin supplements
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Medicines for the prevention and treatment of cancer, nervous system diseases, cardio-cerebrovascular disease, psychiatric disorders, ophthalmic diseases, andrology diseases, all for human purposes; Pharmaceutical preparations for the prevention and treatment of cancer, nervous system diseases, cardio-cerebrovascular disease, psychiatric disorders, ophthalmic diseases, andrology diseases, all for human purposes; Drugs for medical purposes for the prevention and treatment of cancer, nervous system diseases, cardio-cerebrovascular disease, psychiatric disorders, ophthalmic diseases, andrology diseases, all for human purposes; Ointments for pharmaceutical purposes for the prevention and treatment of cancer, nervous system diseases, cardio-cerebrovascular disease, psychiatric disorders, ophthalmic diseases, andrology diseases, all for human purposes; Crude drugs, namely, extracts of hops for pharmaceutical purposes, eucalyptus for pharmaceutical purposes, Mint for pharmaceutical purposes, Malt for pharmaceutical purposes, Pepsins for pharmaceutical purposes, Thymol for pharmaceutical purposes, Turpentine for pharmaceutical purposes, Flaxseed for pharmaceutical purposes, Ferments for pharmaceutical purposes, Cytostatics for pharmaceutical purposes, Balms for pharmaceutical purposes, Digestives for pharmaceutical purposes, Iodine for pharmaceutical purposes, Alcohol for pharmaceutical purposes, and Starch for pharmaceutical purposes, all for the prevention and treatment of cancer, nervous system diseases, cardio-cerebrovascular disease, psychiatric disorders, ophthalmic diseases, andrology diseases, all for human purposes; Cultures of microorganisms for medical or veterinary use; Nutritive substances for microorganisms for medical purposes; Veterinary preparations for pig, farm animals, companion animals, pets, ruminants, namely, vaccine, anti-parasite, antipyretic, analgesic, anti-inflammatory, antibiotic, disinfectants and feed additive preparations; Medicines for veterinary purposes for pig, farm animals, companion animals, pets, ruminants, namely, vaccine, anti-parasite, antipyretic, analgesic, anti-inflammatory, antibiotic, disinfectants and feed additive preparations; antibiotics
52.
ANTI-HUMAN PD-1 MONOCLONAL ANTIBODY FORMULATION, COMBINED MEDICAMENT AND USE THEREOF
Disclosed in the present application are a stable pharmaceutical formulation of an antibody against human PD-1, a combined medicament and the use thereof. Said pharmaceutical formulation comprises an antibody against human PD-1, a stabilizer, a buffer and a surfactant. The pharmaceutical formulation of the antibody against human PD-1 of the present invention can effectively inhibit the aggregation and deamidation of the antibody, thereby preventing the degradation of an antibody protein and obtaining a stable pharmaceutical formulation. With regard to the combined medicament of the present invention, the pharmaceutical formulation of the antibody against human PD-1 is used in combination with other additional therapeutic agents. Further disclosed is the use of the pharmaceutical formulation or the combined medicament in the preparation of an anti-tumor medicament.
C07C 269/06 - 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 by reactions not involving the formation of carbamate groups
54.
POLYMORPH OF COMPOUND, PREPARATION METHOD THEREFOR AND USE THEREOF
The present invention relates to a polymorph of a compound (3R,6S)-6-aminosulfonylamino-1-(thiazol-2-yl)-3-(2,3,4-trifluorophenyl)-3,5,6,7-tetrahydropyrrolo[1,2-c]pyrimidin-4-methyl formate (compound 1). The present invention further relates to a pharmaceutical composition and pharmaceutical use of the polymorph of compound 1, and a preparation method for the polymorph of compound 1.
Disclosed is a dihydropyrimido fused ring derivative as a HBV inhibitor, and in particular relates to a compound shown as formula (I) or a pharmaceutically acceptable salt thereof.
Disclosed is a spirocyclic aryl phosphorus oxide or sulfide as an ALK inhibitor, particularly, a compound represented by formula (I) as an ALK inhibitor or pharmaceutically acceptable salt thereof.
A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
01 - Chemical and biological materials for industrial, scientific and agricultural use
05 - Pharmaceutical, veterinary and sanitary products
10 - Medical apparatus and instruments
42 - Scientific, technological and industrial services, research and design
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
Chemicals used in industry; chemicals for science; Chemicals used in photography; Chemicals for use in agriculture; horticulture chemicals; Chemicals used in forestry; Unprocessed artificial resins; Unprocessed plastics; Manures; Fire extinguishing compositions; Metal tempering preparations; Soldering preparations; Chemical substances for preserving foodstuffs; Tanning substances; Adhesives used in industry; Active chemical ingredients for use in the manufacture of pharmaceuticals; Active chemical ingredients for use in the manufacture of anti-cancer drugs; Chemical preparations for use in the manufacture of pharmaceuticals; Chemical preparations for use in the manufacture of pharmaceuticals; Chemical substances for use in the manufacture of pharmaceuticals; chemical reagents for use in genetic research. Pharmaceuticals; Veterinary preparations; Sanitary preparations for medical purposes; Foodstuffs and dietetic substances for medical or veterinary purposes; Baby food; Dietary supplements for humans and animals; Plasters, materials for dressings; Material for stopping teeth, dental wax; Disinfectants; Preparations for destroying vermin; Fungicides; Herbicides; Chemical preparations for pharmaceutical purposes; Chemical preparations for veterinary purposes; Chemical preparations for medical purposes; Active pharmaceutical ingredients; Hormones for medical purposes; Steroids; Chemico-pharmaceutical preparations; Antihistamines; Biological tissue cultures for medical purposes; Biological tissue cultures for veterinary purposes; Blood for medical purposes; Blood plasma; Bracelets for medical purposes; Contact lens cleaning preparations; Dental abrasives; Solutions for contact lenses; Stem cells for medical purposes; Stem cells for veterinary purposes; Surgical implants comprised of living tissues; Medicine; Cachets for pharmaceutical purposes; Drug delivery agents in the form of coatings for tablets that facilitate the delivery of pharmaceutical preparations. Surgical apparatus and instruments; Medical apparatus and instruments; Dental apparatus and instruments; Veterinary apparatus and instruments; Artificial limbs; Artificial eyes; Artificial teeth; Orthopedic articles; Suture materials; Injection syringes; Injection devices for pharmaceuticals; Surgical implants [artificial materials]. Scientific and technological services and research and design relating thereto; industry analysis and research services; Design and development of computer hardware and software; Pharmaceutical research and development; Provision of information and data relating to medical and veterinary research and development; Conducting clinical trials for pharmaceutical products; Analytical laboratory services; Scientific research relating to genetics; Analysis and evaluation of product development; Design and development of new technology for others; Information, advisory and consultancy services relating to all of the aforementioned services. Medical services; Veterinary services; Hygienic and beauty care for human beings or animals; Agriculture, horticulture and forestry services.
01 - Chemical and biological materials for industrial, scientific and agricultural use
05 - Pharmaceutical, veterinary and sanitary products
10 - Medical apparatus and instruments
42 - Scientific, technological and industrial services, research and design
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
Chemicals used in industry; chemicals for science; Chemicals used in photography; Chemicals for use in agriculture; horticulture chemicals; Chemicals used in forestry; Unprocessed artificial resins; Unprocessed plastics; Manures; Fire extinguishing compositions; Metal tempering preparations; Soldering preparations; Chemical substances for preserving foodstuffs; Tanning substances; Adhesives used in industry; Active chemical ingredients for use in the manufacture of pharmaceuticals; Active chemical ingredients for use in the manufacture of anti-cancer drugs; Chemical preparations for use in the manufacture of pharmaceuticals; Chemical preparations for use in the manufacture of pharmaceuticals; Chemical substances for use in the manufacture of pharmaceuticals; chemical reagents for use in genetic research. Pharmaceuticals; Veterinary preparations; Sanitary preparations for medical purposes; Foodstuffs and dietetic substances for medical or veterinary purposes; Baby food; Dietary supplements for humans and animals; Plasters, materials for dressings; Material for stopping teeth, dental wax; Disinfectants; Preparations for destroying vermin; Fungicides; Herbicides; Chemical preparations for pharmaceutical purposes; Chemical preparations for veterinary purposes; Chemical preparations for medical purposes; Active pharmaceutical ingredients; Hormones for medical purposes; Steroids; Chemico-pharmaceutical preparations; Antihistamines; Biological tissue cultures for medical purposes; Biological tissue cultures for veterinary purposes; Blood for medical purposes; Blood plasma; Bracelets for medical purposes; Contact lens cleaning preparations; Dental abrasives; Solutions for contact lenses; Stem cells for medical purposes; Stem cells for veterinary purposes; Surgical implants comprised of living tissues; Medicine; Cachets for pharmaceutical purposes; Drug delivery agents in the form of coatings for tablets that facilitate the delivery of pharmaceutical preparations. Surgical apparatus and instruments; Medical apparatus and instruments; Dental apparatus and instruments; Veterinary apparatus and instruments; Artificial limbs; Artificial eyes; Artificial teeth; Orthopedic articles; Suture materials; Injection syringes; Injection devices for pharmaceuticals; Surgical implants [artificial materials]. Scientific and technological services and research and design relating thereto; industry analysis and research services; Design and development of computer hardware and software; Pharmaceutical research and development; Provision of information and data relating to medical and veterinary research and development; Conducting clinical trials for pharmaceutical products; Analytical laboratory services; Scientific research relating to genetics; Analysis and evaluation of product development; Design and development of new technology for others; Information, advisory and consultancy services relating to all of the aforementioned services. Medical services; Veterinary services; Hygienic and beauty care for human beings or animals; Agriculture, horticulture and forestry services.
60.
SPIROCYCLIC ARYL PHOSPHORUS OXIDE AND ARYL PHOSPHORUS SULFIDE
Disclosed is a spirocyclic aryl phosphorus oxide or sulfide as an ALK inhibitor, particularly a compound represented by formula (I) as an ALK inhibitor or pharmaceutically acceptable salt thereof.
C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
The present invention belongs to the field of medicine and the chemical industry, and in particular relates to N-(5-((Z)-(5-fluoro-2-carbonyl indole-3-yl)methyl)-2,4-dimethyl-1H-pyrrol-3-yl)-3-(4-methyl piperazin-1-yl)propionamide dimaleate (compound I) and polymorphs thereof. The present invention also relates to a method for preparing polymorphs of compound I, a pharmaceutical composition comprising compound I and polymorphs thereof, and the pharmaceutical use of compound I and the polymorphs thereof. The polymorph of compound I of the present invention has a good crystallinity and physical and/or chemical stability.
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 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
The present invention relates to a xanthine derivative, a pharmaceutically acceptable salt thereof, a solvate of the derivative, a solvate of the pharmaceutically acceptable salt, a chemically protected form or prodrug thereof and a preparation method and a use thereof; and also relates to an intermediate compound used for preparing the xanthine derivative and a preparation method of the intermediate compound. The xanthine derivative and a pharmaceutical composition thereof effectively inhibit the activity of DPP-IV, and can be used for preparing a drug for diseases associated with dipeptidyl peptidase (DPP-IV).
C07D 473/04 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
63.
BICYCLE SUBSTITUTED PYRAZOLONEAZO DERIVATIVES AND PREPARATION METHOD AND USE THEREOF
The present invention is in the medical and chemical field, and relates to a class of bicycle substituted pyrazoloneazo derivatives, the preparation method and a pharmaceutical composition and use thereof. In particular, the present invention relates to a compound shown as formula (I) and a pharmaceutically acceptable salt and solvate thereof. The present invention also relates to the preparation method of the compound of formula (I), a pharmaceutical composition comprising same and the use thereof in preparing medicine. The compound of formula (I) of the present invention is an effective TPO agonist and a good drug for treating thrombocytopenia.
C07D 231/48 - Oxygen atom in position 3 or 5 and nitrogen atom in position 4 with hydrocarbon radicals attached to said nitrogen atom
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
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 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 31/4152 - 1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
A61K 31/4155 - 1,2-Diazoles not condensed and containing further heterocyclic rings
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
A61P 7/00 - Drugs for disorders of the blood or the extracellular fluid
A61P 35/02 - Antineoplastic agents specific for leukemia
C12N 5/078 - Cells from blood or from the immune system
64.
POLYMORPHS OF N-(4-(3-FLUOROBENZYLOXY)-3-CHLOROPHENYL)-6-(5-((2-(METHYLSULFINYL)ETHYLAMINO)METHYL)-2-FURANYL)-QUINAZOLINE-4-AMINEXYLENE SULFONATE AND PREPARATION METHOD AND USES THEREOF
The invention relates to the polymorphs of N-(4-(3-fluorobenzyloxy)-3-chlorophenyl)-6-(5-((2-(methylsulfinyl)ethylamino)methyl)-2-furanyl)-quinazoline-4-aminexylene sulfonate (compound I) used as tyrosine kinase inhibitors. In particular, the invention relates to the crystal forms A, B, C and D of compound I. The invention also relates to a preparation method for the polymorphs of compound I, and comprises its pharmaceutical compositions and their pharmaceutical uses. The polymorphs of compound I of the invention are efficient tyrosine kinase inhibitors.
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
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
Shanghai Institute of Materia Medica, Chinese Academy of Sciences (China)
QILU Pharamceutical Co., Ltd. (China)
Inventor
Gan, Yong
Zhu, Chunliu
Yang, Qingmin
Wang, Jingyi
Zheng, Xiaoqing
Gan, Li
Zhang, Xinxin
Abstract
A paliperidone double-layered osmotic pump controlled release tablet and the preparation method thereof are disclosed. The double-layered osmotic pump controlled release tablet comprises a rigid membrane, a push layer, a drug layer, an isolation layer and an aesthetic coating, wherein the rigid membrane contains a semi-permeable polymer, a porogen and/or a plasticizer and has one or more drug release orifices on one end, the push layer comprises an expanding material, an osmotic agent, a binder, a colorant and a lubricant, the drug layer contains a pharmaceutically active ingredient, a hydrophilic polymer, an osmotic agent, a colorant, a lubricant and an antistatic agent, the isolation layer is located between the inner surface of the rigid membrane and the push layer, and contains a hydrophilic polymer. The paliperidone double-layered osmotic pump controlled release tablet shows an increasing drug release rate at early stage and keeps a constant drug release rate at later stage.
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
66.
4-(SUBSTITUTED PHENYLAMINO)QUINAZOLINE DERIVATIVE AND PREPARATION METHOD THEREFOR, PHARMACEUTICAL COMPOSITION AND USE THEREOF
The present invention relates to a 4-(substituted phenylamino)quinazoline derivative and a preparation method therefor, a pharmaceutical composition and a use thereof. In particular, the present invention relates to a compound of formula I or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2 and R3 are as defined in the specification and claims. The present invention further relates to a method for preparing the compound of formula I, a pharmaceutical composition comprising the compound and pharmaceutical uses of the compound and pharmaceutical composition. The compounds of formula I according to the present invention are potent irreversible inhibitors of tyrosine kinases.
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
C07D 405/14 - 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 three or more hetero rings
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 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
The present invention relates to 4-(substituted anilino)-quinazoline derivatives as tyrosine kinase inhibitors. Specifically, compounds of formula I, or pharmaceutically acceptable salts or solvates thereof are disclosed, in which each substitutent in formula I is defined in the description. Preparation method of the compounds of formula I, pharmaceutical compositions and pharmaceutical uses thereof are also disclosed. The compounds of formula I are effective tyrosine kinase inhibitors.
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
C07D 401/00 - 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
Disclosed is a preparation method of lapatinib. Specifically, a method for preparing a compound represented by formula I or its pharmaceutical salts is disclosed. The method has advantages of high yield and high purity of end-product and so on.
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
Provided are pyrrolyl substituted dihydroindol-2-one derivatives represented by formula (I), pharmaceutically acceptable salts or solvates thereof, or solvates of said salts, which are effective tyrosine kinase inhibitors. Also provided are the preparation methods of the above compounds, pharmaceutical compositions containing these compounds, and the uses of these compounds in manufacturing drugs useful for the treatment or adjunctive treatment of tumors mediated by tyrosine kinases or proliferation or migration of tumor cells driven by tyrosine kinases in mammals (including human).
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
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 413/14 - 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 31/4439 - 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 31/496 - 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
SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES (China)
QILU PHARMACEUTICAL CO., LTD. (China)
Inventor
Gan, Yong
Zhu, Chunliu
Yang, Qingmin
Wang, Jingyi
Zheng, Xiaoqing
Gan, Li
Zhang, Xinxin
Abstract
A paliperidone double-layered osmotic pump controlled release tablet and the preparation method thereof are disclosed. The double-layered osmotic pump controlled release tablet comprises rigid membrane, push layer, drug layer, separating layer and aesthetic coating is disclosed. The rigid membrane contains semi-permeable polymer, hole-forming agent and/or plasticizer and has one or more delivery orifices on one end. The push layer comprises expanding material, permeation-promoter, binder, colorant and lubricant. The drug layer contains pharmaceutical active component, hydrophilic polymer carrier, permeation-promoter, colorant, lubricant and antistatic agent. The separating layer is between the inner surface of the rigid membrane and core comprised of drug layer and push layer and contains hydrophilic polymer. The paliperidone double-layered osmotic pump controlled release tablet shows increased release at initial stage and keeps constant release at late stage.
4-(substituted anilino)quinazoline derivatives used as inhibitors of tyrosine kinase are disclosed. Specifically, compounds of formula I, pharmaceutically acceptable salts or solvates thereof are disclosed, in which each substitutent of formula I is defined in the description. Preparation method of the compounds of formula I, pharmaceutical compositions and pharmaceutical uses thereof are also disclosed. The compounds of formula I are efficacious inhibitors of tyrosine kinase.
C07D 405/10 - 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 carbon chain containing aromatic rings
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
[ Pharmaceutical preparations, namely, injections, capsules and tablets for use in ophthalmology, oncology, and chemotherapy; pharmaceutical preparations, namely, injections, capsules and tablets for the treatment of disorders of the nervous system, cardio-vascular system and respiratory system; pharmaceutical preparations, namely, injections, capsules and tablets for the treatment of diseases and disorders in the gastrointestinal system, endocrine system and psychiatric system; pharmaceutical preparations, namely, injections, capsules and tablets for the treatment of inflammation; ] biomedical medicines for use in ophthalmology, oncology and chemotherapy; [ biomedical medicines for the treatment of disorders of the nervous system, cardio-vascular system and respiratory system; biomedical medicines for the treatment of diseases and disorders in the gastrointestinal system, endocrine system and psychiatric system; biomedical medicines for the treatment of inflammation; ] medicines for humans for use in ophthalmology, oncology and chemotherapy; [ medicines for humans for the treatment of disorders of the nervous system, cardio-vascular system and respiratory system; medicines for humans for the treatment of gastrointestinal system, endocrine system and psychiatric system related diseases and disorders; medicines for humans for the treatment of inflammation; ] drugs for medical purposes for use in ophthalmology, oncology and chemotherapy [ ; drugs for medical purposes for the treatment of disorders of the nervous system, cardio-vascular system and respiratory system; drugs for medical purposes for the treatment of gastrointestinal system, endocrine system and psychiatric system related diseases and disorders; drugs for medical purposes, namely, the treatment of inflammation ]
01 - Chemical and biological materials for industrial, scientific and agricultural use
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Nausea treatment medications; antibiotics; cough treatment medication; eye washes; pharmaceutical preparations for use in ophthalmology; pharmaceutical preparations for the treatment of cancer; sleeping pills; pharmaceutical preparations for the treatment of blood disorders; pharmaceutical preparations for the treatment of cardiovascular diseases; pharmaceutical preparations for use in oncology; diagnostic preparations or reagents, namely, diagnostic preparations or reagents for medical diagnostic use; liniments; pharmaceutical preparations for the treatment of psychiatric diseases, namely, mood disorders, anxiety disorders, cognitive disorders; pharmaceutical preparations for the treatment of the central nervous system, namely, central nervous system infections, brain diseases, central nervous system movement disorders, ocular motility disorders, spinal cord diseases; biochemical preparations for use in oncology; biochemical preparations for the treatment of cancer; pharmaceutical preparations for use in dermatology, namely, dermatitis, skin pigmentation diseases, sexually transmitted diseases; pharmaceutical preparations for the treatment of psychiatric diseases, namely, schizophrenia .
The invention provides a more handy and environment friendly process for preparing risperidone, which comprises reacting 6-fluoro-3-(4-piperidinyl)-1,2-benzisoxazole hydrochloride with 3-(2-chloroethyl)-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2a] pyrimidin-4-one in a basic aqueous solution. The concentration of alkali metal carbonate in the basic aqueous solution is ranged from 15% to 40%. The reaction is carried out at temperature range of 101-140°C and the reaction is completed within 10 minutes to 2 hours.
Disclosed is a dihydropyrimido fused ring derivative as a HBV inhibitor, and in particular relates to a compound shown as formula (1) or a pharmaceutically acceptable salt thereof.
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/527 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim spiro-condensed
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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
Disclosed in the present invention are a crystal form of a dihydropyrido ring compound, and preparation method and intermediate thereof.(see compound 1)
Provided are an anti-CLDN18.2 antibody or an antigen-binding fragment thereof, a derivative comprising said antibody or antigen-binding fragment thereof, a pharmaceutical composition, and related use of said antibody or antigen-binding fragment thereof for treating, diagnosing and detecting cancers.
C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
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
C12N 5/20 - Murine cells, e.g. mouse cells one of the fusion partners being a B lymphocyte
A pharmaceutical composition, and a preparation method therefor and an application thereof. The pharmaceutical composition comprises a spiro-aryl phosphorus oxide or a pharmaceutically acceptable salt thereof as an active ingredient and a pharmaceutically acceptable carrier. D90 of the spiro-aryl phosphorus oxide or the pharmaceutically acceptable salt thereof is in a range of 40.3 ?m to 79.6 ?m. The pharmaceutical composition has high content uniformity, a high dissolution rate, and high in-vivo bioavailability, and can be used for treating cancer.
Provided are a class of compounds, represented by formula (I"'), as selective EGFR inhibitors, a pharmaceutical composition containing the compounds, useful intermediates for preparing the compounds, and a method for using the compounds of the present invention to treat cell proliferative diseases, such as cancers.
C07D 223/14 - Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
C07D 313/06 - Seven-membered rings condensed with carbocyclic rings or ring systems
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
Disclosed in the present invention is a type of novel 13-1actamase inhibitors, and specifically disclosed are a cornpound represented by formula (1) or a pilaf ____________ maceutically acceptable salt thereof, wherein. X is defined in description. The cornpound can be used to inhibit various p-lactarnases, and the bacteriostatic activity is remarkably enhanced.
A61K 31/439 - 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 the ring forming part of a bridged ring system, e.g. quinuclidine
The present invention relates to a polymorph of a compound (3R,6S)-6-aminosulfonylamino-1-(thiazol-2-yl)-3-(2,3,4-trifluorophenyl)-3,5,6,7-tetrahydropyrrolo[1,2-c]pyrimidin-4-methyl formate (compound 1). The present invention further relates to a pharmaceutical composition and pharmaceutical use of the polymorph of compound 1, and a preparation method for the polymorph of compound 1.
Disclosed in the present invention are a crystal form of a ß-lactamase inhibitor and a preparation method therefor, as well as an application of the crystal form in preparing a ß-lactamase inhibitor drug. (I)
A61K 31/439 - 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 the ring forming part of a bridged ring system, e.g. quinuclidine
