CN102834388B - Cgrp受体拮抗剂 - Google Patents

Cgrp受体拮抗剂 Download PDF

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Publication number
CN102834388B
CN102834388B CN201180016888.2A CN201180016888A CN102834388B CN 102834388 B CN102834388 B CN 102834388B CN 201180016888 A CN201180016888 A CN 201180016888A CN 102834388 B CN102834388 B CN 102834388B
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compound
cgrp
pharmaceutically acceptable
methyl
concentration
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Chinese (zh)
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CN102834388A (zh
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P.V.查特维度拉
G.M.杜博奇克
J.E.马科
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Bristol Myers Squibb Co
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Bristol Myers Squibb Co
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/4151,2-Diazoles
    • A61K31/4161,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0804Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0806Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Dermatology (AREA)
  • Rheumatology (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)
CN201180016888.2A 2010-03-30 2011-03-11 Cgrp受体拮抗剂 Active CN102834388B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US31901510P 2010-03-30 2010-03-30
US61/319,015 2010-03-30
PCT/US2011/028168 WO2011123232A1 (en) 2010-03-30 2011-03-11 Cgrp receptor antagonist

Publications (2)

Publication Number Publication Date
CN102834388A CN102834388A (zh) 2012-12-19
CN102834388B true CN102834388B (zh) 2014-07-16

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US (1) US8481546B2 (enExample)
EP (1) EP2552906B1 (enExample)
JP (1) JP5908455B2 (enExample)
KR (3) KR101747477B1 (enExample)
CN (1) CN102834388B (enExample)
AR (1) AR080746A1 (enExample)
AU (1) AU2011233627B2 (enExample)
BR (1) BR112012024785B1 (enExample)
CA (1) CA2794950C (enExample)
CL (1) CL2012002739A1 (enExample)
CY (1) CY1117593T1 (enExample)
DK (1) DK2552906T3 (enExample)
EA (1) EA022815B1 (enExample)
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HR (1) HRP20160287T1 (enExample)
HU (1) HUE028735T2 (enExample)
IL (1) IL221665A (enExample)
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NZ (1) NZ603231A (enExample)
PE (1) PE20130340A1 (enExample)
PL (1) PL2552906T3 (enExample)
PT (1) PT2552906E (enExample)
RS (1) RS54608B1 (enExample)
SG (1) SG183918A1 (enExample)
SI (1) SI2552906T1 (enExample)
SM (1) SMT201600078B (enExample)
TW (1) TWI483937B (enExample)
WO (1) WO2011123232A1 (enExample)
ZA (1) ZA201207292B (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2024222889A1 (zh) 2023-04-28 2024-10-31 成都思倍博医药科技有限公司 含氧代吡啶并脂肪环或脂杂环结构的化合物及其医药用途

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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
EP3863629A4 (en) * 2018-10-13 2022-06-22 Biohaven Pharmaceutical Holding Company Ltd. Prodrugs of cgrp antagonists
SG11202106721VA (en) * 2019-01-20 2021-07-29 Biohaven Pharm Holding Co Ltd Cgrp antagonists for treating migraine breakthrough
JP7654561B2 (ja) 2019-04-11 2025-04-01 アール.ピー. シェーラー テクノロジーズ エルエルシー 浸透性が低いタンパク質、ペプチド、及び小分子の経口送達用の製剤
US20220401439A1 (en) * 2019-12-17 2022-12-22 Biohaven Pharmaceutical Holding Company Ltd. Intranasal pharmaceutical compositions of cgrp inhibitors
CA3202137A1 (en) * 2020-11-19 2022-05-27 Pfizer Ireland Pharmaceuticals Compositions for improved delivery of cgrp inhibitors
CN116456981A (zh) * 2020-11-19 2023-07-18 辉瑞爱尔兰制药公司 用于改善的grp抑制剂递送的组合物
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
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
IL320431A (en) 2022-11-09 2025-06-01 Teva Czech Ind S R O Crystalline forms of zibagen hydrochloride and process for their preparation
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
WO2025003905A1 (en) 2023-06-29 2025-01-02 Pfizer Inc. Solid forms of (r)-n-(3-(7-methyl-1h-indazol-5-yl)-1-(4-(1-methylpiperidin-4-yl)piperazin-1-yl)-1-oxopropan-2-yl)-4-(2-oxo-1,2-dihydroquinolin-3-yl)piperidine-1-carboxamide
CN119462607B (zh) * 2023-08-10 2025-11-28 南京宁丹新药技术股份有限公司 一类喹啉酮衍生物及其用途
CN117551081A (zh) * 2023-11-13 2024-02-13 北京康立生医药技术开发有限公司 一种偏头痛治疗药物新的制备方法
ES3027457A1 (es) 2023-12-13 2025-06-13 Moehs Iberica Sl Metodo de preparacion de zavegepant, intermedios de sintesis de zavegepant y metodos de preparacion de los mismos
WO2025238595A1 (en) 2024-05-16 2025-11-20 Olon S.P.A. Process for preparing (r)-2-amino-3-(7-methyl-1h-indazol-5-yl) methyl propanoate, and use thereof as intermediate for the synthesis of zavegepant
WO2026033478A1 (en) 2024-08-09 2026-02-12 Olon S.P.A. Process for preparing 3-piperidin-4-il-1h- quinolin-2-one or a salt thereof and its use as an intermediate for the preparation of pharmaceutical active ingredients antagonists of the cgrp peptide receptor
CN119306698B (zh) * 2024-10-09 2025-10-21 浙江工业大学 一种制备扎维吉泮中间体的新方法

Citations (2)

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CN1671711A (zh) * 2002-06-05 2005-09-21 布里斯托尔-迈尔斯斯奎布公司 降钙素基因相关肽受体拮抗剂
CN101495480A (zh) * 2006-05-03 2009-07-29 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

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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
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

Patent Citations (2)

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CN1671711A (zh) * 2002-06-05 2005-09-21 布里斯托尔-迈尔斯斯奎布公司 降钙素基因相关肽受体拮抗剂
CN101495480A (zh) * 2006-05-03 2009-07-29 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

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2024222889A1 (zh) 2023-04-28 2024-10-31 成都思倍博医药科技有限公司 含氧代吡啶并脂肪环或脂杂环结构的化合物及其医药用途
EP4703362A1 (en) 2023-04-28 2026-03-04 Chengdu Sibeibo Pharmaceutical Technology Co., Ltd Compound containing oxo-pyrido-aliphatic ring or aliphatic heterocyclic structure, and medical use thereof

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TW201139414A (en) 2011-11-16
AR080746A1 (es) 2012-05-02
PE20130340A1 (es) 2013-03-30
SG183918A1 (en) 2012-10-30
EP2552906A1 (en) 2013-02-06
CA2794950A1 (en) 2011-10-06
KR101854249B1 (ko) 2018-05-03
PL2552906T3 (pl) 2016-06-30
US20120059017A1 (en) 2012-03-08
EA022815B1 (ru) 2016-03-31
KR20170068615A (ko) 2017-06-19
AU2011233627B2 (en) 2013-09-12
DK2552906T3 (en) 2016-03-29
HK1174914A1 (zh) 2013-06-21
CY1117593T1 (el) 2017-06-28
CN102834388A (zh) 2012-12-19
IL221665A (en) 2016-07-31
CA2794950C (en) 2017-09-26
EP2552906B1 (en) 2016-01-06
JP2013523733A (ja) 2013-06-17
ES2562610T3 (es) 2016-03-07
RS54608B1 (sr) 2016-08-31
KR20180049168A (ko) 2018-05-10
US8481546B2 (en) 2013-07-09
MX2012010725A (es) 2012-10-05
SI2552906T1 (sl) 2016-05-31
PT2552906E (pt) 2016-03-18
AU2011233627A1 (en) 2012-11-15
KR101747477B1 (ko) 2017-06-14
EA201270751A1 (ru) 2013-02-28
HRP20160287T1 (hr) 2016-04-08
KR20130076807A (ko) 2013-07-08
NZ603231A (en) 2014-02-28
SMT201600078B (it) 2016-04-29
ZA201207292B (en) 2014-03-26
WO2011123232A1 (en) 2011-10-06
BR112012024785A2 (pt) 2016-06-07
JP5908455B2 (ja) 2016-04-26
HUE028735T2 (en) 2017-01-30
TWI483937B (zh) 2015-05-11
CL2012002739A1 (es) 2013-03-22
BR112012024785B1 (pt) 2020-12-01
BR112012024785A8 (pt) 2017-10-17

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