EA201270751A1 - Антагонист рецептора cgrp - Google Patents
Антагонист рецептора cgrpInfo
- Publication number
- EA201270751A1 EA201270751A1 EA201270751A EA201270751A EA201270751A1 EA 201270751 A1 EA201270751 A1 EA 201270751A1 EA 201270751 A EA201270751 A EA 201270751A EA 201270751 A EA201270751 A EA 201270751A EA 201270751 A1 EA201270751 A1 EA 201270751A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- cgrp
- compound
- neurogenic
- antagonist receptor
- relates
- Prior art date
Links
- 108090000932 Calcitonin Gene-Related Peptide Proteins 0.000 title abstract 2
- 102100025588 Calcitonin gene-related peptide 1 Human genes 0.000 title abstract 2
- 239000005557 antagonist Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000004484 1-methylpiperidin-4-yl group Chemical group CN1CCC(CC1)* 0.000 abstract 1
- -1 7-methyl-1H-indazol-5-yl Chemical group 0.000 abstract 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 abstract 1
- 206010020565 Hyperaemia Diseases 0.000 abstract 1
- 208000019695 Migraine disease Diseases 0.000 abstract 1
- 206010027603 Migraine headaches Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 208000007920 Neurogenic Inflammation Diseases 0.000 abstract 1
- 208000006673 asthma Diseases 0.000 abstract 1
- 239000003735 calcitonin gene related peptide receptor antagonist Substances 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 230000005796 circulatory shock Effects 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 230000002757 inflammatory effect Effects 0.000 abstract 1
- 230000001272 neurogenic effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 208000023504 respiratory system disease Diseases 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 230000003685 thermal hair damage Effects 0.000 abstract 1
- 230000024883 vasodilation Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—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
- C07D401/14—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—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
- A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
-
- 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
- A61K31/435—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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric 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
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/06—Antimigraine agents
-
- 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
- A61P35/00—Antineoplastic 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- 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
- C07D403/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0802—Tripeptides with the first amino acid being neutral
- C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
- C07K5/0806—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Epidemiology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Pulmonology (AREA)
- Pain & Pain Management (AREA)
- Reproductive Health (AREA)
- Endocrinology (AREA)
- Cardiology (AREA)
- Dermatology (AREA)
- Rheumatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Изобретение в целом относится к соединению формулы I, (R)-N-(3-(7-метил-1Н-индазол-5-ил)-1-(4-(1-метилпиперидин-4-ил)пиперазин-1-ил)-1-оксопропан-2-ил)-4-(2-оксо-1,2-дигидрохинолин-3-ил)пиперидин-1-карбоксамиду, включающему в себя фармацевтически приемлемые соли, которое представляет собой антагонист CGRP-рецептора. Изобретение также относится к фармацевтическим композициям и способам для применения соединения в лечении расстройств, связанных с CGRP, включающих в себя мигренозные головные боли, нейрогенную вазодилатацию, нейрогенное воспаление, термическое повреждение, циркуляторный шок, гиперемию, связанную с менопаузой, воспалительные заболевания дыхательных путей, такие как астма, хроническое обструктивное заболевание легких (ХОЗЛ) и раковая опухоль.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US31901510P | 2010-03-30 | 2010-03-30 | |
| PCT/US2011/028168 WO2011123232A1 (en) | 2010-03-30 | 2011-03-11 | Cgrp receptor antagonist |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201270751A1 true EA201270751A1 (ru) | 2013-02-28 |
| EA022815B1 EA022815B1 (ru) | 2016-03-31 |
Family
ID=43896902
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201270751A EA022815B1 (ru) | 2010-03-30 | 2011-03-11 | Антагонист рецептора cgrp |
Country Status (30)
| Country | Link |
|---|---|
| US (1) | US8481546B2 (ru) |
| EP (1) | EP2552906B1 (ru) |
| JP (1) | JP5908455B2 (ru) |
| KR (3) | KR101747477B1 (ru) |
| CN (1) | CN102834388B (ru) |
| AR (1) | AR080746A1 (ru) |
| AU (1) | AU2011233627B2 (ru) |
| BR (1) | BR112012024785B1 (ru) |
| CA (1) | CA2794950C (ru) |
| CL (1) | CL2012002739A1 (ru) |
| CY (1) | CY1117593T1 (ru) |
| DK (1) | DK2552906T3 (ru) |
| EA (1) | EA022815B1 (ru) |
| ES (1) | ES2562610T3 (ru) |
| HK (1) | HK1174914A1 (ru) |
| HR (1) | HRP20160287T1 (ru) |
| HU (1) | HUE028735T2 (ru) |
| IL (1) | IL221665A (ru) |
| MX (1) | MX2012010725A (ru) |
| NZ (1) | NZ603231A (ru) |
| PE (1) | PE20130340A1 (ru) |
| PL (1) | PL2552906T3 (ru) |
| PT (1) | PT2552906E (ru) |
| RS (1) | RS54608B1 (ru) |
| SG (1) | SG183918A1 (ru) |
| SI (1) | SI2552906T1 (ru) |
| SM (1) | SMT201600078B (ru) |
| TW (1) | TWI483937B (ru) |
| WO (1) | WO2011123232A1 (ru) |
| ZA (1) | ZA201207292B (ru) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201519194D0 (en) * | 2015-10-30 | 2015-12-16 | Heptares Therapeutics Ltd | CGRP receptor antagonists |
| GB201519196D0 (en) * | 2015-10-30 | 2015-12-16 | Heptares Therapeutics Ltd | CGRP Receptor Antagonists |
| GB201519195D0 (en) | 2015-10-30 | 2015-12-16 | Heptares Therapeutics Ltd | CGRP Receptor Antagonists |
| GB201707938D0 (en) | 2017-05-17 | 2017-06-28 | Univ Sheffield | Compounds |
| BR112021005873A2 (pt) * | 2018-10-13 | 2021-07-27 | Biohaven Pharmaceutical Holding Company Ltd. | profármacos de antagonistas de cgrp |
| US20210338654A1 (en) * | 2019-01-20 | 2021-11-04 | Biohaven Pharmaceutical Holding Company Ltd. | Cgrp antagonists for treating migraine breakthrough |
| KR20210151187A (ko) * | 2019-04-11 | 2021-12-13 | 알.피.쉐러 테크놀러지즈 엘엘씨 | 난투과성 단백질, 펩타이드 및 소분자의 경구 전달을 위한 제형 |
| KR20220114613A (ko) * | 2019-12-17 | 2022-08-17 | 바이오하벤 파마슈티컬 홀딩 컴퍼니 엘티디. | Cgrp 저해제의 비강내 약제학적 조성물 |
| EP4247364A1 (en) * | 2020-11-19 | 2023-09-27 | Pfizer Ireland Pharmaceuticals | Compositions for improved delivery of cgrp inhibitors |
| EP4301362A1 (en) | 2021-03-02 | 2024-01-10 | CGRP Diagnostics GmbH | Treatment and/or reduction of occurrence of migraine |
| EP4320113A1 (en) | 2021-04-09 | 2024-02-14 | Teva Czech Industries s.r.o. | Solid state forms of zavegepant and process for preparation thereof |
| WO2023026205A1 (en) | 2021-08-24 | 2023-03-02 | Cgrp Diagnostics Gmbh | Preventative treatment of migraine |
| CN117624191A (zh) * | 2022-08-30 | 2024-03-01 | 熙源安健医药（上海）有限公司 | 吲唑甲酰胺类衍生物及其制备方法和用途 |
| WO2024100599A1 (en) | 2022-11-09 | 2024-05-16 | Teva Czech Industries S.R.O. | Solid state forms of zavegepant hydrochloride and process for preparation thereof |
| CN116003387B (zh) * | 2022-11-20 | 2024-03-26 | 药康众拓(北京)医药科技有限公司 | 一种氘代吲唑丙酰胺类化合物、药物组合物和用途 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| LT1539766T (lt) * | 2002-06-05 | 2017-03-10 | Bristol-Myers Squibb Company | Su kalcitonino genu susijusio peptido receptoriaus antagonistai |
| US7220862B2 (en) | 2002-06-05 | 2007-05-22 | Bristol-Myers Squibb Company | Calcitonin gene related peptide receptor antagonists |
| WO2005084672A1 (de) | 2004-03-03 | 2005-09-15 | Boehringer Ingelheim International Gmbh | Ausgewählte cgrp-antagonisten, verfahren zu deren herstellung sowie deren verwendung als arzneimittel |
| US7834007B2 (en) | 2005-08-25 | 2010-11-16 | Bristol-Myers Squibb Company | CGRP antagonists |
| CN101495480B (zh) * | 2006-05-03 | 2013-07-10 | 百时美施贵宝公司 | 作为降钙素基因相关肽受体拮抗剂的受限化合物 |
| WO2010006168A2 (en) | 2008-07-09 | 2010-01-14 | University Of Rochester | Methods of treating cancer using and agent that modulates activity of the calcitonin-gene related peptide ("cgrp") receptor |
-
2011
- 2011-03-02 US US13/038,550 patent/US8481546B2/en active Active
- 2011-03-11 ES ES11710087.5T patent/ES2562610T3/es active Active
- 2011-03-11 MX MX2012010725A patent/MX2012010725A/es active IP Right Grant
- 2011-03-11 SG SG2012065744A patent/SG183918A1/en unknown
- 2011-03-11 KR KR1020127028213A patent/KR101747477B1/ko active IP Right Grant
- 2011-03-11 SI SI201130765A patent/SI2552906T1/sl unknown
- 2011-03-11 JP JP2013502610A patent/JP5908455B2/ja active Active
- 2011-03-11 KR KR1020177015456A patent/KR101854249B1/ko active IP Right Grant
- 2011-03-11 PL PL11710087T patent/PL2552906T3/pl unknown
- 2011-03-11 RS RS20160164A patent/RS54608B1/en unknown
- 2011-03-11 PE PE2012001746A patent/PE20130340A1/es active IP Right Grant
- 2011-03-11 CA CA2794950A patent/CA2794950C/en active Active
- 2011-03-11 AU AU2011233627A patent/AU2011233627B2/en active Active
- 2011-03-11 WO PCT/US2011/028168 patent/WO2011123232A1/en active Application Filing
- 2011-03-11 HU HUE11710087A patent/HUE028735T2/en unknown
- 2011-03-11 EA EA201270751A patent/EA022815B1/ru not_active IP Right Cessation
- 2011-03-11 PT PT117100875T patent/PT2552906E/pt unknown
- 2011-03-11 BR BR112012024785-9A patent/BR112012024785B1/pt active IP Right Grant
- 2011-03-11 EP EP11710087.5A patent/EP2552906B1/en active Active
- 2011-03-11 KR KR1020187011875A patent/KR20180049168A/ko not_active Application Discontinuation
- 2011-03-11 CN CN201180016888.2A patent/CN102834388B/zh active Active
- 2011-03-11 DK DK11710087.5T patent/DK2552906T3/en active
- 2011-03-11 NZ NZ603231A patent/NZ603231A/en unknown
- 2011-03-30 TW TW100111106A patent/TWI483937B/zh active
- 2011-03-30 AR ARP110101057A patent/AR080746A1/es not_active Application Discontinuation
-
2012
- 2012-08-27 IL IL221665A patent/IL221665A/en active IP Right Grant
- 2012-09-28 ZA ZA2012/07292A patent/ZA201207292B/en unknown
- 2012-09-28 CL CL2012002739A patent/CL2012002739A1/es unknown
-
2013
- 2013-02-19 HK HK13102079.5A patent/HK1174914A1/zh unknown
-
2016
- 2016-03-21 SM SM201600078T patent/SMT201600078B/xx unknown
- 2016-03-21 HR HRP20160287TT patent/HRP20160287T1/hr unknown
- 2016-03-24 CY CY20161100254T patent/CY1117593T1/el unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ BY KZ KG MD TJ TM |