AR080746A1 - (r)-n-(3-(7-metil-1h-indazol-5-il)1-(4-(1-metilpiperidin-4-il)piperazin-1-il)-1-oxopropan-2-il)-4-(2-oxo-1,2-dihidroquinolin-3-il)piperidina-1-carboxamida antagonista de receptores cgrp. - Google Patents
(r)-n-(3-(7-metil-1h-indazol-5-il)1-(4-(1-metilpiperidin-4-il)piperazin-1-il)-1-oxopropan-2-il)-4-(2-oxo-1,2-dihidroquinolin-3-il)piperidina-1-carboxamida antagonista de receptores cgrp.Info
- Publication number
- AR080746A1 AR080746A1 ARP110101057A ARP110101057A AR080746A1 AR 080746 A1 AR080746 A1 AR 080746A1 AR P110101057 A ARP110101057 A AR P110101057A AR P110101057 A ARP110101057 A AR P110101057A AR 080746 A1 AR080746 A1 AR 080746A1
- Authority
- AR
- Argentina
- Prior art keywords
- cgrp
- oxopropan
- indazol
- methylpiperidin
- piperazin
- 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
- JSPCTNUQYWIIOT-UHFFFAOYSA-N piperidine-1-carboxamide Chemical compound NC(=O)N1CCCCC1 JSPCTNUQYWIIOT-UHFFFAOYSA-N 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
- 206010003497 Asphyxia Diseases 0.000 abstract 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 abstract 1
- 208000019695 Migraine disease 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
- 230000009245 menopause Effects 0.000 abstract 1
- 206010027599 migraine Diseases 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)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Pain & Pain Management (AREA)
- Pulmonology (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)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
Abstract
Compuesto de formula 1, (R)-N-(3-(7-metil-1H-indazol-5-iI)-1-(4-(1-metilpiperidin-4-il)piperazin-1-iI)-1-oxopropan-2-iI)-4-(2-oxo-1,2-dihidroquinolin-3-iI)piperidin-1-carboxamida, incluyendo sales farmacéuticamente aceptables, que es un antagonista del receptor de CGRP. También composiciones farmacéuticas y uso del compuesto en el tratamiento de trastornos relacionados con CGRP, incluyendo migrana, vasodilatacion neurogena, inflamacion neurogena, dano térmico, choque circulatorio, sofoco asociado con menopausia, enfermedades de las vías respiratorias inflamatorias tales como asma, enfermedad pulmonar obstructiva cronica (EPOC) y cáncer.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US31901510P | 2010-03-30 | 2010-03-30 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR080746A1 true AR080746A1 (es) | 2012-05-02 |
Family
ID=43896902
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP110101057A AR080746A1 (es) | 2010-03-30 | 2011-03-30 | (r)-n-(3-(7-metil-1h-indazol-5-il)1-(4-(1-metilpiperidin-4-il)piperazin-1-il)-1-oxopropan-2-il)-4-(2-oxo-1,2-dihidroquinolin-3-il)piperidina-1-carboxamida antagonista de receptores cgrp. |
Country Status (30)
| Country | Link |
|---|---|
| US (1) | US8481546B2 (es) |
| EP (1) | EP2552906B1 (es) |
| JP (1) | JP5908455B2 (es) |
| KR (3) | KR101747477B1 (es) |
| CN (1) | CN102834388B (es) |
| AR (1) | AR080746A1 (es) |
| AU (1) | AU2011233627B2 (es) |
| BR (1) | BR112012024785B1 (es) |
| CA (1) | CA2794950C (es) |
| CL (1) | CL2012002739A1 (es) |
| CY (1) | CY1117593T1 (es) |
| DK (1) | DK2552906T3 (es) |
| EA (1) | EA022815B1 (es) |
| ES (1) | ES2562610T3 (es) |
| HK (1) | HK1174914A1 (es) |
| HR (1) | HRP20160287T1 (es) |
| HU (1) | HUE028735T2 (es) |
| IL (1) | IL221665A (es) |
| MX (1) | MX2012010725A (es) |
| NZ (1) | NZ603231A (es) |
| PE (1) | PE20130340A1 (es) |
| PL (1) | PL2552906T3 (es) |
| PT (1) | PT2552906E (es) |
| RS (1) | RS54608B1 (es) |
| SG (1) | SG183918A1 (es) |
| SI (1) | SI2552906T1 (es) |
| SM (1) | SMT201600078B (es) |
| TW (1) | TWI483937B (es) |
| WO (1) | WO2011123232A1 (es) |
| ZA (1) | ZA201207292B (es) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201519196D0 (en) * | 2015-10-30 | 2015-12-16 | Heptares Therapeutics Ltd | CGRP Receptor Antagonists |
| GB201519194D0 (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 |
| EA202190966A1 (ru) * | 2018-10-13 | 2021-10-15 | Биохэйвен Фармасьютикал Холдинг Компани Лтд. | Пролекарства антагонистов cgrp |
| MX2021008191A (es) * | 2019-01-20 | 2021-08-11 | Biohaven Pharm Holding Co Ltd | Antagonistas del péptido relacionado con el gen de calcitonina (cgrp) para el tratamiento de la irrupción de migraña. |
| CA3134550A1 (en) * | 2019-04-11 | 2020-10-15 | R.P. Scherer Technologies, Llc | Formulation for oral delivery of proteins, peptides and small molecules with poor permeability |
| WO2021127070A1 (en) * | 2019-12-17 | 2021-06-24 | Biohaven Pharmaceutical Holding Company Ltd. | Intranasal pharmaceutical compositions of cgrp inhibitors |
| KR20230088442A (ko) * | 2020-11-19 | 2023-06-19 | 화이자 아일랜드 파마슈티컬즈 | Cgrp 억제제의 개선된 전달을 위한 조성물 |
| WO2022185224A1 (en) | 2021-03-02 | 2022-09-09 | Mark Hasleton | Treatment and/or reduction of occurrence of migraine |
| WO2022217008A1 (en) | 2021-04-09 | 2022-10-13 | 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 |
| WO2024046223A1 (zh) * | 2022-08-30 | 2024-03-07 | 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 |
|---|---|---|---|---|
| AU2003237255B8 (en) * | 2002-06-05 | 2010-01-07 | Bristol-Myers Squibb Company | Calcitonin gene related peptide receptor antagonists |
| US7220862B2 (en) | 2002-06-05 | 2007-05-22 | Bristol-Myers Squibb Company | Calcitonin gene related peptide receptor antagonists |
| EP1722792A1 (de) | 2004-03-03 | 2006-11-22 | 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 HU HUE11710087A patent/HUE028735T2/en unknown
- 2011-03-11 PT PT117100875T patent/PT2552906E/pt unknown
- 2011-03-11 KR KR1020127028213A patent/KR101747477B1/ko active IP Right Grant
- 2011-03-11 WO PCT/US2011/028168 patent/WO2011123232A1/en active Application Filing
- 2011-03-11 SG SG2012065744A patent/SG183918A1/en unknown
- 2011-03-11 JP JP2013502610A patent/JP5908455B2/ja active Active
- 2011-03-11 RS RS20160164A patent/RS54608B1/en unknown
- 2011-03-11 PL PL11710087T patent/PL2552906T3/pl unknown
- 2011-03-11 CA CA2794950A patent/CA2794950C/en active Active
- 2011-03-11 BR BR112012024785-9A patent/BR112012024785B1/pt active IP Right Grant
- 2011-03-11 CN CN201180016888.2A patent/CN102834388B/zh active Active
- 2011-03-11 MX MX2012010725A patent/MX2012010725A/es active IP Right Grant
- 2011-03-11 EP EP11710087.5A patent/EP2552906B1/en active Active
- 2011-03-11 EA EA201270751A patent/EA022815B1/ru not_active IP Right Cessation
- 2011-03-11 PE PE2012001746A patent/PE20130340A1/es active IP Right Grant
- 2011-03-11 NZ NZ603231A patent/NZ603231A/en unknown
- 2011-03-11 AU AU2011233627A patent/AU2011233627B2/en active Active
- 2011-03-11 KR KR1020187011875A patent/KR20180049168A/ko not_active Application Discontinuation
- 2011-03-11 ES ES11710087.5T patent/ES2562610T3/es active Active
- 2011-03-11 SI SI201130765A patent/SI2552906T1/sl unknown
- 2011-03-11 KR KR1020177015456A patent/KR101854249B1/ko active IP Right Grant
- 2011-03-11 DK DK11710087.5T patent/DK2552906T3/en active
- 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 CL CL2012002739A patent/CL2012002739A1/es unknown
- 2012-09-28 ZA ZA2012/07292A patent/ZA201207292B/en 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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