CN104136437B - N-(5s,6s,9r)-4-(2-氧代-2,3-二氢-1h-咪唑并[4,5-b]吡啶-1-基)哌啶-1-羧酸5-氨基-6-(2,3-二氟苯基)-6,7,8,9-四氢-5h-环庚三烯并[b]吡啶-9-基酯半硫酸盐 - Google Patents

N-(5s,6s,9r)-4-(2-氧代-2,3-二氢-1h-咪唑并[4,5-b]吡啶-1-基)哌啶-1-羧酸5-氨基-6-(2,3-二氟苯基)-6,7,8,9-四氢-5h-环庚三烯并[b]吡啶-9-基酯半硫酸盐 Download PDF

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Publication number
CN104136437B
CN104136437B CN201380011305.6A CN201380011305A CN104136437B CN 104136437 B CN104136437 B CN 104136437B CN 201380011305 A CN201380011305 A CN 201380011305A CN 104136437 B CN104136437 B CN 104136437B
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compound
hemisulfate
salt
crystalline form
hemisulfate salt
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CN104136437A (zh
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D.R.罗伯茨
R.R.沙特曼
魏正国
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Bristol Myers Squibb Co
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    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/4353—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
    • A61K31/437—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
    • 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
    • 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
    • A61P25/06—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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN201380011305.6A 2012-02-27 2013-02-25 N-(5s,6s,9r)-4-(2-氧代-2,3-二氢-1h-咪唑并[4,5-b]吡啶-1-基)哌啶-1-羧酸5-氨基-6-(2,3-二氟苯基)-6,7,8,9-四氢-5h-环庚三烯并[b]吡啶-9-基酯半硫酸盐 Active CN104136437B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261603598P 2012-02-27 2012-02-27
US61/603,598 2012-02-27
PCT/US2013/027648 WO2013130402A1 (en) 2012-02-27 2013-02-25 N- (5s, 6s, 9r) - 5 -amino- 6 - (2, 3 - difluorophenyl) -6, 7, 8, 9 - tetrahydro - 5h - cyclohepta [b] pyridin-9 -yl- 4 - (2 - oxo-2, 3 - dihydro - 1h- imidazo [4, 5 -b] pyridin - 1 - yl) piperidine - 1 - carboxylate, hemisulfate salt

Publications (2)

Publication Number Publication Date
CN104136437A CN104136437A (zh) 2014-11-05
CN104136437B true CN104136437B (zh) 2016-05-11

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US (1) US8759372B2 (https=)
EP (2) EP3254681B1 (https=)
JP (2) JP6208154B2 (https=)
KR (2) KR102220969B1 (https=)
CN (1) CN104136437B (https=)
AU (1) AU2013226361B2 (https=)
BR (1) BR112014021032B1 (https=)
CA (1) CA2865585C (https=)
CY (2) CY1119448T1 (https=)
DK (2) DK2820016T3 (https=)
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ES (2) ES2746031T3 (https=)
HK (1) HK1248111B (https=)
HR (2) HRP20171620T1 (https=)
HU (2) HUE047050T2 (https=)
IL (1) IL234272B (https=)
LT (2) LT3254681T (https=)
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NO (1) NO2935439T3 (https=)
PL (2) PL3254681T3 (https=)
PT (2) PT3254681T (https=)
RS (2) RS59295B1 (https=)
SG (1) SG11201404834XA (https=)
SI (2) SI2820016T1 (https=)
SM (1) SMT201700489T1 (https=)
WO (1) WO2013130402A1 (https=)

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HUE047050T2 (hu) * 2012-02-27 2020-04-28 Bristol Myers Squibb Co N-(5S,6S,9R)-5-amino-6-(2,3-difluorfenil)-6,7,8,9-tetrahidro-5H-ciklohepta[B]piridin-9 -yl-4-(2-oxo-2,3-dihidro-1H-imidazo[4,5-B]piridin-1-il)piperidin-1-karboxilát só
EP2815749A1 (en) 2013-06-20 2014-12-24 IP Gesellschaft für Management mbH Solid form of 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione having specified X-ray diffraction pattern
CA3182565A1 (en) 2015-03-06 2016-09-15 Atea Pharmaceuticals, Inc. .beta.-d-2'-deoxy-2'-.alpha.-fluoro-2'-.beta.-c-substituted-2-modified-n6-substituted purine nucleotides for hcv treatment
CA3035561A1 (en) * 2016-09-02 2018-03-08 Christopher J. Soares Use of cgrp receptor antagonists in neuroprotection and neurological disorders
WO2018048937A1 (en) 2016-09-07 2018-03-15 Atea Pharmaceuticals, Inc. 2'-substituted-n6-substituted purine nucleotides for rna virus treatment
IL288737B (en) * 2017-02-01 2022-09-01 Atea Pharmaceuticals Inc Hemisulfate nucleotide salt for treatment of hepatitis c virus
MX2020009856A (es) * 2018-03-25 2020-10-08 Biohaven Pharm Holding Co Ltd Rimegepant para trastornos relacionados con el peptido relacionado con el gen para calcitonina (cgrp).
EP3773753A4 (en) 2018-04-10 2021-12-22 ATEA Pharmaceuticals, Inc. TREATMENT OF PATIENTS INFECTED WITH THE HEPATITIS C VIRUS WITH CIRRHOSIS
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.
US12521389B2 (en) * 2019-06-14 2026-01-13 The Regents Of The University Of California Therapeutic approach to lung disease
US10874687B1 (en) 2020-02-27 2020-12-29 Atea Pharmaceuticals, Inc. Highly active compounds against COVID-19
JP2024509165A (ja) 2021-03-02 2024-02-29 シージーアールピー ダイアグノスティクス ゲーエムベーハー 片頭痛の治療及び／又は発生の低減
IL308921A (en) 2021-06-17 2024-01-01 Atea Pharmaceuticals Inc Combination anti-HCV therapy is beneficial
US20250109188A1 (en) 2021-08-24 2025-04-03 Cgrp Diagnostics Gmbh Preventative treatment of migraine
WO2023034466A1 (en) * 2021-09-02 2023-03-09 Pfizer Ireland Pharmaceuticals Cgrp antagonists for treating psoriasis
CN115850266A (zh) * 2021-09-26 2023-03-28 奥锐特药业(天津)有限公司 瑞美吉泮新晶型及其制备方法
CN116554164B (zh) * 2022-01-27 2025-10-03 奥锐特药业(天津)有限公司 一种瑞美吉泮的制备方法
WO2023175632A1 (en) * 2022-03-17 2023-09-21 Msn Laboratories Private Limited, R&D Center Solid state forms of (5s,6s,9r)-5-amino-6-(2,3difluorophenyl)-6,7,8,9-tetrahydro-5h-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1h-imidazo[4,5-b]pyridin-1-yl)-1-piperidinecarboxylate hemisulfate and processes for preparation thereof
WO2024180562A1 (en) * 2023-03-02 2024-09-06 Natco Pharma Limited A process for the preparation of pure crystalline rimegepant and its salts thereof
WO2025193980A2 (en) * 2024-03-13 2025-09-18 CNS Biosciences, Inc. Method of treating neuropathic pain using an anti-cgrp inhibitor
WO2026074002A1 (en) 2024-10-02 2026-04-09 Krka, D.D., Novo Mesto Crystalline salts of rimegepant

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JP2015511581A (ja) 2015-04-20
CN104136437A (zh) 2014-11-05
ES2746031T3 (es) 2020-03-04
ES2642737T3 (es) 2017-11-17
RS56556B1 (sr) 2018-02-28
BR112014021032B1 (pt) 2022-09-27
JP6476253B2 (ja) 2019-02-27
SI3254681T1 (sl) 2019-10-30
JP6208154B2 (ja) 2017-10-04
DK3254681T3 (da) 2019-09-30
KR20200016993A (ko) 2020-02-17
DK2820016T3 (da) 2017-11-13
AU2013226361A1 (en) 2014-10-16
EA201491585A1 (ru) 2015-01-30
IL234272B (en) 2018-10-31
MX2014009544A (es) 2014-11-10
PL2820016T3 (pl) 2018-01-31
SI2820016T1 (sl) 2017-11-30
CA2865585C (en) 2019-12-10
PT3254681T (pt) 2019-10-01
HK1248111B (en) 2020-04-17
EA025358B1 (ru) 2016-12-30
LT3254681T (lt) 2019-09-25
HRP20171620T1 (hr) 2017-12-01
EP3254681A1 (en) 2017-12-13
CY1119448T1 (el) 2018-03-07
LT2820016T (lt) 2017-10-25
KR102076118B1 (ko) 2020-02-11
PL3254681T3 (pl) 2019-12-31
KR102220969B1 (ko) 2021-02-25
JP2017226693A (ja) 2017-12-28
HUE034936T2 (hu) 2018-03-28
BR112014021032A2 (https=) 2017-06-20
KR20140130140A (ko) 2014-11-07
SG11201404834XA (en) 2014-09-26
SMT201700489T1 (it) 2017-11-15
WO2013130402A1 (en) 2013-09-06
US8759372B2 (en) 2014-06-24
CY1122121T1 (el) 2020-11-25
EP2820016B1 (en) 2017-08-02
HRP20191655T1 (hr) 2019-12-13
PT2820016T (pt) 2017-10-18
CA2865585A1 (en) 2013-09-06
AU2013226361B2 (en) 2017-09-21
EP2820016A1 (en) 2015-01-07
US20130225636A1 (en) 2013-08-29
NO2935439T3 (https=) 2018-03-31
EP3254681B1 (en) 2019-06-19
MX352171B (es) 2017-11-13
HUE047050T2 (hu) 2020-04-28
RS59295B1 (sr) 2019-10-31

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