Goods & Services

Vitamins, nutritional supplements, and non-prescription pharmaceutical products for the prevention and treatment of viral, metabolic, endocrine, musculoskeletal, cardiovascular, cardiopulmonary, genitourinary, sexual dysfunction, oncological, hepatological, ophthalmic, respiratory, neurological, gastrointestinal, hormonal, dermatological, psychiatric and immune-related conditions; preparations for the delivery of pharmaceutical ingredients; specialized tablets, capsules, gel capsules, powders, syrups, gummies, gels, ointments, lotions, creams, patches, liquids, liquid drops, and sprays, all for the delivery of pharmaceutical ingredients

Abstract

The present invention relates to a P2X3 inhibitor compound, a salt thereof, a polymorph thereof and use thereof. The present invention provides a crystalline form of a compound of formula I, which has good medicinal properties. A pharmaceutically acceptable salt of the compound of formula I is also obtained, and a crystalline form product of the salt is further obtained, such as a hydrochloride crystalline form A, a maleate crystalline form A, a p-toluenesulfonate crystalline form A, a benzenesulfonate crystalline form A, or a malonate crystalline form A. The present invention has great significance for developing effective therapeutic drugs.

IPC Classes  ?

• 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 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61P 11/14 - Antitussive agents
• G01N 30/02 - Column chromatography

Abstract

Provided is a solid dispersion containing a P2X3 receptor antagonist compound shown in formula I, which can increase the solubility of the compound shown in formula I, and improve the dissolution rate and bioavailability of the drug, ensuring the therapeutic effect of the drug. Meanwhile, the solid dispersion has good stability. During the storage process, the solid dispersion does not experience crystal form transformation and does not exhibit a significant increase in related substances, which improves the safety of the clinical use of the drug.

IPC Classes  ?

• A61K 9/20 - Pills, lozenges or tablets
• A61K 9/28 - DrageesCoated pills or tablets
• A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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
• A61P 11/00 - Drugs for disorders of the respiratory system
• A61P 11/06 - Antiasthmatics
• A61P 11/14 - Antitussive agents
• A61P 13/00 - Drugs for disorders of the urinary system
• A61P 13/02 - Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
• A61P 13/08 - Drugs for disorders of the urinary system of the prostate
• A61P 13/10 - Drugs for disorders of the urinary system of the bladder
• A61P 15/00 - Drugs for genital or sexual disordersContraceptives
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 25/04 - Centrally acting analgesics, e.g. opioids
• A61P 25/02 - Drugs for disorders of the nervous system for peripheral neuropathies
• A61P 25/06 - Antimigraine agents
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]

Abstract

Provided in the present invention are compounds shown as formula (II), and tautomers, stereoisomers, hydrates, solvates, pharmaceutically acceptable salts or prodrugs thereof. The compounds have good Nav1.8 inhibitory effect.

IPC Classes  ?

• 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 307/24 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
• C07D 411/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• A61K 31/443 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
• A61K 31/341 - 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 not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
• A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
• 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
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]

Abstract

222 to a coupling reaction to obtain 1D; subjecting the compound 1D and 2-bromo-5-methylthiazole to a coupling reaction to obtain 1E; substituting the compound 1E with 1F to then obtain a compound 1H; hydrolyzing 1H under the action of a base to obtain 1I, and subjecting the compound 1I and 1L to a condensation reaction to obtain a product I-1. The synthesis route provided by the present invention makes it easy to control product quality, has a high yield and is suitable for industrial production.

IPC Classes  ?

• 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

Abstract

The present invention relates to a P2X3 inhibitor compound, a salt thereof, a polymorph thereof and use thereof. The present invention provides a crystalline form of a compound of formula I, which has good medicinal properties. A pharmaceutically acceptable salt of the compound of formula I is also obtained, and a crystalline form product of the salt is further obtained, such as a hydrochloride crystalline form A, a maleate crystalline form A, a p-toluenesulfonate crystalline form A, a benzenesulfonate crystalline form A, or a malonate crystalline form A. The present invention has great significance for developing effective therapeutic drugs.

IPC Classes  ?

• 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 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61P 13/00 - Drugs for disorders of the urinary system
• A61P 25/04 - Centrally acting analgesics, e.g. opioids
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]

Abstract

Provided are a novel compound that effectively antagonizes P2X3 receptor, a preparation method thereof, and use thereof in the preparation of drugs. The compound is a compound represented by Formula I, or a tautomer, a stereoisomer, a hydrate, a solvate, a pharmaceutically acceptable salt, or a prodrug thereof. Provided are a novel compound that effectively antagonizes P2X3 receptor, a preparation method thereof, and use thereof in the preparation of drugs. The compound is a compound represented by Formula I, or a tautomer, a stereoisomer, a hydrate, a solvate, a pharmaceutically acceptable salt, or a prodrug thereof.

IPC Classes  ?

• 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 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
• A61P 11/14 - Antitussive agents

Abstract

The present invention relates to bioavailable fill compositions containing one or more of a decongestant, an expectorant, an antitussive, an analgesic, and/or an antihistamine; capsules filled with the bioavailable fill compositions; and methods of making same.

IPC Classes  ?

• 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 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• A61K 31/09 - Ethers or acetals having an ether linkage to aromatic ring nuclear carbon having two or more such linkages
• A61K 31/137 - Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine
• A61K 31/138 - Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
• A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine

Goods & Services

pharmaceuticals for use in treatment of seizures, hypertension, cardiovascular disease, disease of the endocrine system, gastroenterological disease, hematological disease, infectious disease, disease of the immune system, musculoskeletal disease, kidney disease, disease of the nervous system, gynecological disease, cancer, diseases of the eye, ear, nose and throat, mental illness, rheumatological disease, bone disease, skin wounds, contact dermatitis, headaches, migraine headaches, muscle pain, inflammation, and for use in dental, cosmetic, maxillofacial, and plastic surgery, all available as tablets, capsules, softgels, liquids, creams, and powders

Goods & Services

pharmaceuticals for use in treatment of seizures, hypertension, cardiovascular disease, disease of the endocrine system, gastroenterological disease, hematological disease, infectious disease, disease of the immune system, musculoskeletal disease, kidney disease, disease of the nervous system, gynecological disease, cancer, diseases of the eye, ear, nose and throat, mental illness, rheumatological disease, bone disease, skin wounds, contact dermatitis, headaches, migraine headaches, muscle pain, inflammation, and for use in dental, cosmetic, maxillofacial, and plastic surgery, all available as tablets, capsules, softgels, liquids, creams, and powders

Goods & Services

Manufacturing of pharmaceuticals for others Product development for others of pharmaceuticals

Goods & Services

Manufacturing of pharmaceuticals for others Product development for others of pharmaceuticals

Abstract

Clear bioavailable liquid softgel fill compositions comprising a) at least one analgesic and one or more of decongestants, expectorants, antitussives and/or antihistamines; b) a matrix comprising a pharmaceutically acceptable poly(alkylene glycol) and a pharmaceutically acceptable alkylene glycol; c) a solubilizing agent comprising a pharmaceutically acceptable polymeric solubilizing agent and water are disclosed. Also disclosed are methods for the preparation of such clear fill compositions, and softgel capsules containing the clear bioavailable liquid fill composition.

IPC Classes  ?

• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• A61K 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
• A61K 47/32 - Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers
• 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 31/09 - Ethers or acetals having an ether linkage to aromatic ring nuclear carbon having two or more such linkages
• A61K 31/137 - Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine
• A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine

Abstract

The present invention relates to a compound capable of effectively antagonizing EP4, which is a compound represented by formula I, or a tautomer, a stereoisomer, a hydrate, a solvate, a pharmaceutically-acceptable salt or a prodrug of the compound represented by formula I. R13233; R2263626366 cycloalkyl; R312122 alkyl; R4161616166 alkoxy.

IPC Classes  ?

• C07D 231/20 - One oxygen atom attached in position 3 or 5
• A61K 31/415 - 1,2-Diazoles
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 35/00 - Antineoplastic agents

Abstract

A pyrimidine compound, relating more specifically to a pyrimidine compound and a preparation method therefor, and a use thereof in the preparation of a drug. Provided is a compound represented by formula (I), or a tautomer, stereoisomer, hydrate, solvate, pharmaceutically acceptable salt or prodrug of the compound represented by formula (I). The described compound has an obvious inhibitory effect on an ATX enzyme, exhibits excellent liver metabolism stability, is metabolized more slowly in the human body, and has higher exposure.

IPC Classes  ?

• C07D 255/00 - Heterocyclic compounds containing rings having three nitrogen atoms as the only ring hetero atoms, not provided for by groups
• C07D 255/02 - Heterocyclic compounds containing rings having three nitrogen atoms as the only ring hetero atoms, not provided for by groups not condensed with other rings
• C07D 401/02 - 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
• 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
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61P 35/00 - Antineoplastic agents
• A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis

Abstract

The present invention provides a phenylpyrrolidine compound, i.e., a compound represented by general formula (A-1) or (A), to provide a PDE4 inhibitor having a novel structure, a good medical effect, high bioavailability and good druggability, and used for effectively treating PDE4-related diseases and disorders, including, but not limited to, inflammatory diseases, allergic diseases, autoimmune diseases, transplant rejection, joint inflammatory diseases, skin inflammatory diseases, inflammatory bowel diseases, and smooth muscle contraction-related diseases, etc. (A-1) (A)

IPC Classes  ?

• 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 31/4439 - 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 37/00 - Drugs for immunological or allergic disorders
• A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
• A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
• A61P 17/00 - Drugs for dermatological disorders
• A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
• A61P 11/06 - Antiasthmatics
• A61P 11/00 - Drugs for disorders of the respiratory system
• A61P 17/06 - Antipsoriatics
• A61P 19/06 - Antigout agents, e.g. antihyperuricemic or uricosuric agents
• A61P 13/10 - Drugs for disorders of the urinary system of the bladder

Abstract

The present invention provides a new compound effectively inhibiting ATX, which is a compound represented by formula I, or a tautomer, stereoisomer, hydrate, solvate, salt or prodrug of the compound represented by formula I: formula (I) wherein: R1and R233, provided that R1and R233 simultaneously.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems

Abstract

121103101103451103101101321233.

IPC Classes  ?

• 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 31/4439 - 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 31/497 - Non-condensed pyrazines containing further heterocyclic rings
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61P 13/10 - Drugs for disorders of the urinary system of the bladder
• 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 11/00 - Drugs for disorders of the respiratory system
• A61P 13/00 - Drugs for disorders of the urinary system
• A61P 17/00 - Drugs for dermatological disorders
• A61P 19/00 - Drugs for skeletal disorders
• A61P 37/00 - Drugs for immunological or allergic disorders

Abstract

Fast-acting, bioavailable liquid softgel fill compositions comprising (al) a pain reliever/fever reducer; (a2) a diuretic; (a3) an antihistamine; (b1) a pharmaceutically acceptable polyalkylene glycol; (b2) a pharmaceutically acceptable alkylene glycol; (cl) a pharmaceutically acceptable polymeric solubilizer; (c2) water; and (d) an antioxidant/preservative are disclosed, where the liquid softgel fill composition does not crystallize or otherwise deposit any of the active ingredients. Also disclosed are methods for the preparation of such fill compositions, and softgel capsules containing the bioavailable liquid fill composition.

IPC Classes  ?

• A61K 31/047 - Hydroxy compounds, e.g. alcoholsSalts thereof, e.g. alcoholates having two or more hydroxy groups, e.g. sorbitol
• A61K 31/05 - Phenols
• A61K 31/085 - Ethers or acetals having an ether linkage to aromatic ring nuclear carbon

Abstract

Disclosed in the present invention are a salt type and crystal type of 4H-pyrazolo[1, 5-alpha]benzimidazole compound and the preparation method and intermediate thereof. The 4H-pyrazolo[1,5-alpha]benzimidazole compound has the structure of Compound 2.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• C07D 401/04 - 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 directly linked by a ring-member-to-ring- member bond
• C07C 57/145 - Maleic acid

Abstract

The present invention relates to bioavailable fill compositions containing one or more of a decongestant, an expectorant, an antitussive, an analgesic, and/or an antihistamine; capsules filled with the bioavailable fill compositions; and methods of making same.

IPC Classes  ?

• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• A61K 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
• A61K 47/32 - Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers
• 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 9/08 - Solutions

Abstract

Disclosed in the present invention are a salt type and crystal type of 4H-pyrazolo[1,5-alpha]benzimidazole compound and a preparation method and intermediate thereof. The 4H-pyrazolo[1,5-alpha]benzimidazole compound is represented by formula I:

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• C07D 401/04 - 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 directly linked by a ring-member-to-ring- member bond
• C07C 57/145 - Maleic acid

Abstract

The present invention provides a pyrimidine derivative and a use thereof. The pyrimidine derivative is the compound shown in formula I or a pharmaceutically acceptable salt, hydrate, solvate, metabolite or prodrug thereof, wherein, R1, R2, R3, R4 and R5 are, for example, as defined in the specification. The compound can act as an ALK inhibitor, and is for preparing an anti-tumor medicament for suppressing an anaplastic lymphoma kinase.

IPC Classes  ?

• C07D 409/12 - 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 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
• 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 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 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 239/48 - Two nitrogen atoms
• 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
• A61P 35/00 - Antineoplastic agents

Abstract

Clear bioavailable liquid softgel fill compositions comprising a) at least one analgesic and one or more of decongestants, expectorants, antitussives and/or antihistamines; b) a matrix comprising a pharmaceutically acceptable poly(alkylene glycol) and a pharmaceutically acceptable alkylene glycol; c) a solubilizing agent comprising a pharmaceutically acceptable polymeric solubilizing agent and water are disclosed. Also disclosed are methods for the preparation of such clear fill compositions, and softgel capsules containing the clear bioavailable liquid fill composition.

IPC Classes  ?

• A61K 9/08 - Solutions
• 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 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
• A61K 47/32 - Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate

Abstract

Disclosed in the present invention are a salt type and crystal type of 4H-pyrazolo [1, 5-alpha] benzimidazole compound and the preparation method and intermediate thereof.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• C07D 401/04 - 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 directly linked by a ring-member-to-ring- member bond
• A61P 35/00 - Antineoplastic agents

Abstract

Disclosed is a series of analogs of 4H-pyrazolo[1,5-α]benzimidazole compound as PARP inhibitors. In particular, disclosed in the invention is a compound as shown by formula (I) or a pharmaceutically acceptable salt thereof as a PARP inhibitor.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• 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

Abstract

Provided are a photoreaction device and a system for preparing a compound. The photoreaction device comprises a reaction vessel (100) and a light source (400), wherein the reaction vessel (100) defines a photoreaction space (200), and the reaction vessel (100) is made of a transparent material (300); and the light source (400) is arranged outside the reaction vessel (100).

IPC Classes  ?

• B01J 19/12 - Processes employing the direct application of electric or wave energy, or particle radiationApparatus therefor employing electromagnetic waves
• C07C 50/36 - Quinones containing groups having oxygen atoms singly bound to carbon atoms the quinoid structure being part of a condensed ring system having four or more rings
• C07C 46/00 - Preparation of quinones
• C07C 45/63 - 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 introduction of halogenPreparation 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 substitution of halogen atoms by other halogen atoms
• C07C 49/567 - Unsaturated compounds containing keto groups bound to rings other than six-membered aromatic rings containing halogen

Abstract

The present invention provides a pyrimidine derivative serving as an ALK inhibitor. The compound is a compound shown in Formula I or a pharmaceutical salt, hydrate, solvate, metabolite or prodrug of the compound shown in Formula I, where R1, R2, R3 and R4 are defined in the description.

IPC Classes  ?

• 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 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 239/48 - Two nitrogen atoms
• C07D 409/12 - 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 linked by a chain containing hetero atoms as chain links
• 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
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention provides a kinase inhibitor and application thereof. The compound is a compound shown in Formula I or a pharmaceutical salt, hydrate, solvate, metabolite or prodrug of the compound shown in Formula I, where R1 and R2 are defined in the description.

IPC Classes  ?

• 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 409/12 - 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 linked by a chain containing hetero atoms as chain links
• C07D 239/48 - Two nitrogen atoms
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61P 35/00 - Antineoplastic agents

Abstract

Desmodium Styracifolium and a pharmaceutically acceptable excipient.

IPC Classes  ?

• A61K 36/00 - Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
• A61K 36/48 - Fabaceae or Leguminosae (Pea or Legume family)CaesalpiniaceaeMimosaceaePapilionaceae
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• A61K 9/16 - AgglomeratesGranulatesMicrobeadlets

Abstract

Provided are a series of BTK inhibitors, and specifically disclosed are a compound, pharmaceutically acceptable salt thereof, tautomer thereof or pro-drug thereof represented by formula (I), (II), (III) or (IV).

IPC Classes  ?

• C07D 239/04 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
• C07D 239/48 - Two nitrogen atoms
• C07D 235/04 - BenzimidazolesHydrogenated benzimidazoles
• C07D 471/04 - Ortho-condensed systems
• C07D 401/04 - 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 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 213/73 - Unsubstituted amino or imino radicals
• C07D 213/74 - Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
• A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61K 31/5383 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
• A61P 35/00 - Antineoplastic agents
• A61P 35/02 - Antineoplastic agents specific for leukemia

Abstract

The present invention provides a method for detecting the content of impurities, namely, 4-(3-fluorobenzyloxy)3-chlorobenzenamine and 2-aminoethylmethylsulfone hydrochloride in lapatinib by using LC-MS/MS.

IPC Classes  ?

• G01N 30/02 - Column chromatography
• A61P 35/00 - Antineoplastic agents
• A61P 35/04 - Antineoplastic agents specific for metastasis

Abstract

The present invention provides a substituted heterocyclic compound as a kinase inhibitor, and a preparation method therefor and uses thereof. The compound is a compound represented by the formula I or a medicinal salt, a hydrate, a solvate or a prodrug of the compound represented by the formula I, wherein R1, R2, R3 and R4 are defined in the specification.

IPC Classes  ?

• C07D 237/28 - Cinnolines
• 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 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 409/12 - 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 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 31/5377 - 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
• A61P 35/00 - Antineoplastic agents
• A61P 35/02 - Antineoplastic agents specific for leukemia

Abstract

Use of microcrystalline cellulose in the manufacture of a 4-methoxynimesulide formulation, and a method for preparing 4-methoxynimesulide formulation.

IPC Classes  ?

• A61K 47/38 - CelluloseDerivatives thereof
• A61K 31/18 - Sulfonamides
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]

Abstract

Provided are a Methosulide tablet and a preparation method therefor. The Methosulide tablet comprises Methosulide and a pharmaceutically acceptable excipient.

IPC Classes  ?

• A61K 9/20 - Pills, lozenges or tablets
• A61K 47/38 - CelluloseDerivatives thereof
• 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 47/32 - Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers
• A61K 31/18 - Sulfonamides
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61J 1/10 - Bag-type containers

Abstract

Provided is 4-methoxynimesulide thin film coated tablets comprising 4-methoxynimesulide and pharmaceutically acceptable excipients.

IPC Classes  ?

• A61K 31/18 - Sulfonamides
• A61K 9/28 - DrageesCoated pills or tablets
• A61K 47/38 - CelluloseDerivatives thereof
• A61K 47/32 - Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers

Abstract

Disclosed is a compound and a preparation method and use thereof. The compound is a compound as shown by formula I or a stereoisomer, a tautomer, a medicine active metabolite, a pharmaceutically acceptable salt, a hydrate, a solvate or a prodrug of the compound as shown by formula I, wherein X, R1 and R2 are as defined in the specification.

IPC Classes  ?

• C07D 473/16 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 two nitrogen atoms
• A61K 31/52 - Purines, e.g. adenine
• A61P 35/00 - Antineoplastic agents
• A61P 19/06 - Antigout agents, e.g. antihyperuricemic or uricosuric agents
• A61P 35/02 - Antineoplastic agents specific for leukemia
• A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 17/06 - Antipsoriatics
• A61P 37/08 - Antiallergic agents

Abstract

The present invention provides a compound and a preparation method therefor and uses thereof. The compound is a compound represented by formula I or an enantiomer, a diastereoisomer, a racemate, a pharmaceutically acceptable salt, a crystalline hydrate or a solvate thereof. In the compound represented by formula I, R1, R2, R3 and R4 are defined in the specification.

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems
• 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 31/437 - 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 31/5377 - 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 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
• A61K 31/5355 - Non-condensed oxazines containing further heterocyclic rings
• 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
• A61P 35/00 - Antineoplastic agents
• A61P 35/02 - Antineoplastic agents specific for leukemia
• C07D 213/00 - Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
• C07D 207/00 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
• C07D 233/00 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings

Abstract

Provided are a pyrazolopyrimidinone compound and a derivative (a compound represented by formula I) as well as a preparation method therefor and an application thereof. The compound is the compound represented by formula I or a pharmaceutically acceptable salt, a hydrate or a solvate of the compound represented by formula I. In the compound represented by formula I, R1, R2, R3 and R4 are as defined in the specification.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61K 31/541 - Non-condensed thiazines containing further heterocyclic rings
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61P 35/00 - Antineoplastic agents
• A61P 35/02 - Antineoplastic agents specific for leukemia

Abstract

Disclosed is a series of analogues of 4H-pyrazolo[1,5-α]benzimidazole compound as PARP inhibitors. In particular, disclosed in the invention is a compound as shown by formula (I) or a pharmaceutically acceptable salt thereof as a PARP inhibitor.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• 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
• A61P 35/00 - Antineoplastic agents
• 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
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics

Abstract

A Desmodium styracifolium (Osb.) Merr. flavonoids capsule, a method of preparing same, and use thereof. The Desmodium styracifolium (Osb.) Merr. flavonoids capsule comprises: Desmodium styracifolium (Osb.) Merr. flavonoids, being alcohol extract of Desmodium styracifolium (Osb.) Merr.; and a pharmaceutically acceptable excipient. The capsule is used for treating urinary tract calculi.

IPC Classes  ?

• A61K 36/48 - Fabaceae or Leguminosae (Pea or Legume family)CaesalpiniaceaeMimosaceaePapilionaceae
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• A61P 13/04 - Drugs for disorders of the urinary system for urolithiasis

Abstract

Provided is a drug combination, a method of same, and use thereof. The drug combination is formed of a Desmodium styracifolium (Osb.) Merr. flavonoids extract being used as an active ingredient and a pharmaceutically acceptable excipient. The drug combination may be made into a tablet, a granule, a capsule, a pill, powder, and the like. The drug combination has effects of eliminating damp and heat, induce diuresis, and calculi removal, and can be used to treat urinary tract calculi.

IPC Classes  ?

• A61K 36/48 - Fabaceae or Leguminosae (Pea or Legume family)CaesalpiniaceaeMimosaceaePapilionaceae
• 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
• A61K 9/14 - Particulate form, e.g. powders
• A61K 9/20 - Pills, lozenges or tablets
• A61K 9/22 - Sustained or differential release type
• A61K 9/46 - Pills, lozenges or tablets effervescent
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• A61P 13/04 - Drugs for disorders of the urinary system for urolithiasis

Abstract

A solid dispersion containing Desmodium styracifolium (Osb.) Merr. flavonoids, method of preparing same, and use thereof. The Desmodium styracifolium (Osb.) Merr. flavonoids are alcohol extract of Desmodium styracifolium (Osb.) Merr., and the solid dispersion is used for preparing a drug for treating urinary tract calculi.

IPC Classes  ?

• A61K 36/48 - Fabaceae or Leguminosae (Pea or Legume family)CaesalpiniaceaeMimosaceaePapilionaceae
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 9/14 - Particulate form, e.g. powders
• A61K 9/16 - AgglomeratesGranulatesMicrobeadlets
• A61K 9/20 - Pills, lozenges or tablets
• A61K 9/22 - Sustained or differential release type
• A61K 9/24 - Layered or laminated unitary dosage forms
• A61K 9/26 - Discrete particles in supporting matrix
• A61K 9/28 - DrageesCoated pills or tablets
• A61K 9/30 - Organic coatings
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• A61P 13/04 - Drugs for disorders of the urinary system for urolithiasis

Abstract

A pharmaceutical formulation contains 10-60% by weight acetaminophen as the only active ingredient and a solvent system for dissolving the acetaminophen. The formulation is free of any ionizing agent and its solvent system includes water, polyethylene glycol, and polyvinylpyrrolidone that is 2-50% by weight and has a molecular weight of 2,000 to 1,500,000. Also disclosed is another acetaminophen formulation containing polyvinylpyrrolidone as high as 25-50% by weight.

IPC Classes  ?

• 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

Goods & Services

[ Air purifying preparations; ] Anaesthetics; Anti-inflammatory and antipyretic preparations; Antibacterial pharmaceuticals; Cardiovascular pharmaceuticals; [ Dental lacquer; ] Diagnostic preparations for medical purposes; [ Disinfectants for hygiene purposes; ] Medicines for the treatment of gastrointestinal diseases; Nutraceuticals for use as a dietary supplement; Oral contraceptives; Pharmaceutical preparations acting on the central nervous system; Pharmaceutical preparations for use in urology [ ; Pharmaceutical skin lotions; Pregnancy test kits for home use; Sanitary towels ] [ Accounting services; Advertising services; Business management consultancy services; Business management of hotels for others; Business organization and management consultancy including personnel management; Goods import-export agencies; Layout services for advertising purposes; Organizing exhibitions for commercial or advertising purposes; Rental of office machinery and equipment; Sales promotion services ]

Goods & Services

[ Air purifying preparations; ] Anaesthetics; Anti-inflammatory and antipyretic preparations; Antibacterial pharmaceuticals; Cardiovascular pharmaceuticals; [ Dental lacquer; ] Diagnostic preparations for medical purposes; [ Disinfectants for hygiene purposes; ] Medicines for the treatment of gastrointestinal diseases; Nutraceuticals for use as a dietary supplement; Oral contraceptives; Pharmaceutical preparations acting on the central nervous system; Pharmaceutical preparations for use in urology [ ; Pharmaceutical skin lotions; Pregnancy test kits for home use; Sanitary towels ] [ Accounting services; Advertising services; Business management consultancy services; Business management of hotels for others; Business organization and management consultancy including personnel management; Goods import-export agencies; Layout services for advertising purposes; Organizing exhibitions for commercial or advertising purposes; Rental of office machinery and equipment; Sales promotion services ]

Goods & Services

[ Air purifying preparations; ] Anaesthetics; Anti-inflammatory and antipyretic preparations; Antibacterial pharmaceuticals; Cardiovascular pharmaceuticals; [ Dental lacquer; ] Diagnostic preparations for medical purposes; [ Disinfectants for hygiene purposes; ] Medicines for the treatment of gastrointestinal diseases; Nutraceuticals for use as a dietary supplement; Oral contraceptives; Pharmaceutical preparations acting on the central nervous system; Pharmaceutical preparations for use in urology [ ; Pharmaceutical skin lotions; Pregnancy test kits for home use; Sanitary towels ]

Goods & Services

Pharmaceuticals for use in treatment of seizures, hypertension, cardiovascular disease, disease of the endocrine system, gastroenterological disease, hematological disease, infectious disease, disease of the immune system, musculoskeletal disease, kidney disease, disease of the nervous system, gynecological disease, cancer, diseases of the eye, ear, nose and throat, mental illness, rheumatological disease, bone disease, skin wounds, contact dermatitis, headaches, migraine headaches, muscle pain, inflammation, and for use in dental, cosmetic, maxillofacial, and plastic surgery, all available as tablets, capsules, softgels, liquids, creams, and powders; nutritional supplements available as tablets, capsules, softgels, liquids, creams and powders.

Goods & Services

Pharmaceuticals for use in treatment of seizures, hypertension, cardiovascular disease, disease of the endocrine system, gastroenterological disease, hematological disease, infectious disease, disease of the immune system, musculoskeletal disease, kidney disease, disease of the nervous system, gynecological disease, cancer, diseases of the eye, ear, nose and throat, mental illness, rheumatological disease, bone disease, skin wounds, contact dermatitis, headaches, migraine headaches, muscle pain, inflammation, and for use in dental, cosmetic, maxillofacial, and plastic surgery, all available as tablets, capsules, softgels, liquids, creams, and powders; nutritional supplements available as tablets, capsules, softgels, liquids, creams, and powders.

Goods & Services

(1) Pharmaceutical preparations for use in dermatology, namely, skin barrier emulsion for the treatment for atopic dermatitis (AD).

Abstract

The present invention relates to a novel compound, which effectively antagonizes P2X3 receptors and is represented by formula (I), a tautomer, stereoisomer, hydrate, solvate, pharmaceutically acceptable salt or prodrug thereof, and a preparation method and a use thereof in the preparation of drugs.

IPC Classes  ?

• 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
• A61P 13/08 - Drugs for disorders of the urinary system of the prostate
• A61P 25/04 - Centrally acting analgesics, e.g. opioids
• 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
• 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 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

Abstract

Disclosed in the present invention are a salt type and crystal type of 4H-pyrazolo [1, 5-alpha] benzimidazole compound and the preparation method and intermediate thereof.

IPC Classes  ?

• A61P 35/00 - Antineoplastic agents
• C07D 401/04 - 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 directly linked by a ring-member-to-ring- member bond
• C07D 487/04 - Ortho-condensed systems

Abstract

Disclosed is a series of analogues of 4H-pyrazolo[1,5-.alpha.]benzimidazole
compound as PARP
inhibitors. In particular, disclosed in the invention is a compound as shown
by formula (I) or a
pharmaceutically acceptable salt thereof as a PARP inhibitor.

IPC Classes  ?

• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• 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
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 35/00 - Antineoplastic agents
• C07D 487/04 - Ortho-condensed systems
• 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

Abstract

The present invention relates to a P2X3 inhibitor compound, a salt thereof, a polymorph thereof and use thereof. The present invention provides a crystalline form of a compound of formula I, which has good medicinal properties. A pharmaceutically acceptable salt of the compound of formula I is also obtained, and a crystalline form product of the salt is further obtained, such as a hydrochloride crystalline form A, a maleate crystalline form A, a p-toluenesulfonate crystalline form A, a benzenesulfonate crystalline form A, or a malonate crystalline form A. The present invention has great significance for developing effective therapeutic drugs.

IPC Classes  ?

• A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61P 25/04 - Centrally acting analgesics, e.g. opioids
• 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