EA201300857A1 - Пиразолы в качестве антагонистов crth2 - Google Patents
Пиразолы в качестве антагонистов crth2Info
- Publication number
- EA201300857A1 EA201300857A1 EA201300857A EA201300857A EA201300857A1 EA 201300857 A1 EA201300857 A1 EA 201300857A1 EA 201300857 A EA201300857 A EA 201300857A EA 201300857 A EA201300857 A EA 201300857A EA 201300857 A1 EA201300857 A1 EA 201300857A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- pyrazoles
- compounds
- crth2
- antagonists
- antagonists crth2
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/02—Nasal agents, e.g. decongestants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/04—Antipruritics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/14—Decongestants or antiallergics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—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
- C07D405/02—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
- C07D405/12—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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—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
- C07D409/12—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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Epidemiology (AREA)
- Dermatology (AREA)
- Rheumatology (AREA)
- Ophthalmology & Optometry (AREA)
- Physical Education & Sports Medicine (AREA)
- Pain & Pain Management (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Oncology (AREA)
- Otolaryngology (AREA)
- Communicable Diseases (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Изобретение относится к пиразолам формулы (Ia) или (Ib) и их фармацевтически приемлемым солям, в которых R, R, R, R, Y, Y, Y, Y, Y, Z, R, R, n и Rимеют одно из значений, приведенных в описании и формуле изобретения, к их применению в качестве лекарственных средств, к фармацевтическому составу, содержащему указанные соединения, и к фармацевтическим составам, содержащим указанные соединения в комбинации с одним или несколькими активными веществами. Эти соединения обладают антагонистической активностью по отношению к CRTH2.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11151876 | 2011-01-24 | ||
| PCT/EP2012/050830 WO2012101043A1 (en) | 2011-01-24 | 2012-01-20 | Pyrazole compounds as crth2 antagonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201300857A1 true EA201300857A1 (ru) | 2013-12-30 |
| EA022559B1 EA022559B1 (ru) | 2016-01-29 |
Family
ID=43799503
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201300857A EA022559B1 (ru) | 2011-01-24 | 2012-01-20 | Пиразолы в качестве антагонистов crth2 |
Country Status (36)
| Country | Link |
|---|---|
| US (1) | US8759386B2 (ru) |
| EP (1) | EP2668181B1 (ru) |
| JP (1) | JP5695216B2 (ru) |
| KR (2) | KR101923365B1 (ru) |
| CN (4) | CN104628705B (ru) |
| AP (1) | AP3343A (ru) |
| AR (1) | AR084916A1 (ru) |
| AU (1) | AU2012210718B2 (ru) |
| BR (1) | BR112013017570B1 (ru) |
| CA (1) | CA2825458C (ru) |
| CL (1) | CL2013001945A1 (ru) |
| CO (1) | CO6801731A2 (ru) |
| CY (1) | CY1116012T1 (ru) |
| DK (1) | DK2668181T3 (ru) |
| EA (1) | EA022559B1 (ru) |
| EC (1) | ECSP13012832A (ru) |
| ES (1) | ES2529452T3 (ru) |
| GE (1) | GEP20156332B (ru) |
| HK (3) | HK1186183A1 (ru) |
| HR (1) | HRP20150069T1 (ru) |
| IL (1) | IL226920A (ru) |
| MA (1) | MA34838B1 (ru) |
| MX (1) | MX342830B (ru) |
| MY (1) | MY163012A (ru) |
| PE (1) | PE20140860A1 (ru) |
| PH (1) | PH12018501531A1 (ru) |
| PL (1) | PL2668181T3 (ru) |
| PT (1) | PT2668181E (ru) |
| RS (1) | RS53785B1 (ru) |
| SG (1) | SG192096A1 (ru) |
| SI (1) | SI2668181T1 (ru) |
| TN (1) | TN2013000280A1 (ru) |
| TW (1) | TWI527809B (ru) |
| UA (1) | UA109696C2 (ru) |
| UY (1) | UY33873A (ru) |
| WO (1) | WO2012101043A1 (ru) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8759386B2 (en) * | 2011-01-24 | 2014-06-24 | Boehringer Ingelheim International Gmbh | Pyrazole compounds as CRTH2 antagonists |
| EP2688882B1 (en) * | 2011-03-25 | 2015-05-13 | Boehringer Ingelheim International GmbH | Pyrazole compounds as crth2 antagonists |
| US20140148484A1 (en) * | 2012-11-23 | 2014-05-29 | Boehringer Ingelheim International Gmbh | Pyrazole compounds for treating hairloss |
| WO2014079803A1 (en) | 2012-11-23 | 2014-05-30 | Boehringer Ingelheim International Gmbh | Bicyclosubstituted pyrazole compounds for treating hairloss |
| EP3768245A4 (en) * | 2018-03-23 | 2023-10-18 | Palatin Technologies, Inc. | MELANOCORTIN RECEPTOR-SPECIFIC PEPTIDE FORMULATIONS AND METHODS OF ADMINISTRATION SPECIFIC TO THE GASTROINTESTINAL TRACT |
| CN113874015B (zh) | 2018-12-21 | 2024-05-24 | 细胞基因公司 | Ripk2的噻吩并吡啶抑制剂 |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5260322A (en) | 1990-10-08 | 1993-11-09 | Merck & Co., Inc. | Angiotension II antagonists in the treatment of hyperuricemia |
| PL356487A1 (en) | 1999-11-10 | 2004-06-28 | Takeda Chemical Industries, Ltd. | 5-membered n-heterocyclic compounds with hypoglycemic and hypolipidemic activity |
| DE60303238T2 (de) | 2003-04-25 | 2006-09-14 | Actimis Pharmaceuticals, Inc., La Jolla | Pyrimidin-Essigsäure Derivate geeignet zur Behandlung von CRTH2-bedingten Krankheiten |
| JP2007509104A (ja) * | 2003-10-24 | 2007-04-12 | グラクソ グループ リミテッド | 複素環式化合物 |
| CN101084209A (zh) * | 2004-12-21 | 2007-12-05 | 德福根有限公司 | 具有Kv4离子通道活性的化合物 |
| JP4950542B2 (ja) * | 2006-04-07 | 2012-06-13 | 岩手東芝エレクトロニクス株式会社 | 固体撮像装置およびその製造方法 |
| WO2007141267A1 (en) | 2006-06-06 | 2007-12-13 | Glaxo Group Limited | N- (phenylmethyl) -2- (1h-pyraz0l-4-yl) acetamide derivatives as p2x7 antagonists for the treatment of pain, inflammation and neurodegeneration |
| EP2097407A1 (en) * | 2006-11-27 | 2009-09-09 | Pfizer Products Inc. | Pyrazole analogs |
| MX2010003178A (es) * | 2007-09-25 | 2010-04-30 | Actimis Pharmaceuticals Inc | Primidinas sustituidas con 2-s-bencilo como antagonistas de crth2. |
| TW200922587A (en) | 2007-09-25 | 2009-06-01 | Actimis Pharmaceuticals Inc | Alkylthio pyrimidines as CRTH2 antagonists |
| JP2011088826A (ja) * | 2008-01-31 | 2011-05-06 | Astellas Pharma Inc | 芳香族カルボン酸化合物 |
| US20110144160A1 (en) * | 2008-07-03 | 2011-06-16 | Amira Pharmaceuticals, Inc. | Antagonists of Prostaglandin D2 Receptors |
| GB2463788B (en) * | 2008-09-29 | 2010-12-15 | Amira Pharmaceuticals Inc | Heteroaryl antagonists of prostaglandin D2 receptors |
| WO2010057118A2 (en) | 2008-11-17 | 2010-05-20 | Amira Pharmaceuticals, Inc. | Heterocyclic antagonists of prostaglandin d2 receptors |
| WO2010089391A1 (en) * | 2009-02-09 | 2010-08-12 | Boehringer Ingelheim International Gmbh | New pharmaceutical compositions for treatment of respiratory and gastrointestinal disorders |
| AP3360A (en) * | 2010-01-27 | 2015-07-31 | Boehringer Ingelheim Int | Pyrazole compounds as CRTH2 antagonists |
| EP2598145A1 (en) * | 2010-07-28 | 2013-06-05 | Boehringer Ingelheim International GmbH | Pharmaceutical composition for treatment of respiratory and inflammatory diseases |
| US8759386B2 (en) * | 2011-01-24 | 2014-06-24 | Boehringer Ingelheim International Gmbh | Pyrazole compounds as CRTH2 antagonists |
-
2012
- 2012-01-19 US US13/353,621 patent/US8759386B2/en active Active
- 2012-01-19 TW TW101102302A patent/TWI527809B/zh not_active IP Right Cessation
- 2012-01-20 PT PT127006955T patent/PT2668181E/pt unknown
- 2012-01-20 MA MA36130A patent/MA34838B1/fr unknown
- 2012-01-20 GE GEAP201213204A patent/GEP20156332B/en unknown
- 2012-01-20 KR KR1020137019577A patent/KR101923365B1/ko active IP Right Grant
- 2012-01-20 MX MX2013008082A patent/MX342830B/es active IP Right Grant
- 2012-01-20 PE PE2013001586A patent/PE20140860A1/es active IP Right Grant
- 2012-01-20 SG SG2013056106A patent/SG192096A1/en unknown
- 2012-01-20 ES ES12700695.5T patent/ES2529452T3/es active Active
- 2012-01-20 EP EP12700695.5A patent/EP2668181B1/en active Active
- 2012-01-20 PL PL12700695T patent/PL2668181T3/pl unknown
- 2012-01-20 RS RS20150037A patent/RS53785B1/en unknown
- 2012-01-20 DK DK12700695.5T patent/DK2668181T3/da active
- 2012-01-20 SI SI201230126T patent/SI2668181T1/sl unknown
- 2012-01-20 UA UAA201310232A patent/UA109696C2/uk unknown
- 2012-01-20 CN CN201410837969.4A patent/CN104628705B/zh not_active Expired - Fee Related
- 2012-01-20 AU AU2012210718A patent/AU2012210718B2/en not_active Ceased
- 2012-01-20 KR KR1020187033824A patent/KR102251939B1/ko active IP Right Grant
- 2012-01-20 BR BR112013017570-2A patent/BR112013017570B1/pt not_active IP Right Cessation
- 2012-01-20 WO PCT/EP2012/050830 patent/WO2012101043A1/en active Application Filing
- 2012-01-20 CN CN201280006303.3A patent/CN103339125B/zh not_active Expired - Fee Related
- 2012-01-20 CN CN201710440429.6A patent/CN107011332B/zh not_active Expired - Fee Related
- 2012-01-20 CA CA2825458A patent/CA2825458C/en active Active
- 2012-01-20 JP JP2013549819A patent/JP5695216B2/ja not_active Expired - Fee Related
- 2012-01-20 MY MYPI2013002719A patent/MY163012A/en unknown
- 2012-01-20 AP AP2013006942A patent/AP3343A/xx active
- 2012-01-20 EA EA201300857A patent/EA022559B1/ru not_active IP Right Cessation
- 2012-01-20 CN CN201510362688.2A patent/CN104961732B/zh not_active Expired - Fee Related
- 2012-01-23 AR ARP120100213A patent/AR084916A1/es active IP Right Grant
- 2012-01-24 UY UY0001033873A patent/UY33873A/es unknown
-
2013
- 2013-06-13 IL IL226920A patent/IL226920A/en active IP Right Grant
- 2013-06-28 CL CL2013001945A patent/CL2013001945A1/es unknown
- 2013-06-28 TN TNP2013000280A patent/TN2013000280A1/fr unknown
- 2013-07-26 CO CO13177740A patent/CO6801731A2/es active IP Right Grant
- 2013-08-15 EC ECSP13012832 patent/ECSP13012832A/es unknown
- 2013-12-10 HK HK13113692.9A patent/HK1186183A1/xx not_active IP Right Cessation
- 2013-12-10 HK HK16103130.7A patent/HK1215247A1/zh not_active IP Right Cessation
- 2013-12-10 HK HK15111230.0A patent/HK1210467A1/xx not_active IP Right Cessation
-
2015
- 2015-01-20 HR HRP20150069AT patent/HRP20150069T1/hr unknown
- 2015-02-02 CY CY20151100103T patent/CY1116012T1/el unknown
-
2018
- 2018-07-18 PH PH12018501531A patent/PH12018501531A1/en unknown
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