KR101747477B1 - Ｃｇｒｐ 수용체 길항제 - Google Patents

Ｃｇｒｐ 수용체 길항제 Download PDF

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Publication number
KR101747477B1
KR101747477B1 KR1020127028213A KR20127028213A KR101747477B1 KR 101747477 B1 KR101747477 B1 KR 101747477B1 KR 1020127028213 A KR1020127028213 A KR 1020127028213A KR 20127028213 A KR20127028213 A KR 20127028213A KR 101747477 B1 KR101747477 B1 KR 101747477B1
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cgrp
compound
mmol
concentration
mixture
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KR20130076807A (ko
Inventor
프라사드 브이. 차투르베둘라
진 엠. 듀보우칙
존 이. 마코
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브리스톨-마이어스 스큅 컴퍼니
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    • 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)
  • Dermatology (AREA)
  • Cardiology (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)
KR1020127028213A 2010-03-30 2011-03-11 Ｃｇｒｐ 수용체 길항제 Active KR101747477B1 (ko)

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

Related Child Applications (1)

Application Number Title Priority Date Filing Date
KR1020177015456A Division KR101854249B1 (ko) 2010-03-30 2011-03-11 Cgrp 수용체 길항제

Publications (2)

Publication Number Publication Date
KR20130076807A KR20130076807A (ko) 2013-07-08
KR101747477B1 true KR101747477B1 (ko) 2017-06-14

Family

ID=43896902

Family Applications (3)

Application Number Title Priority Date Filing Date
KR1020127028213A Active KR101747477B1 (ko) 2010-03-30 2011-03-11 Ｃｇｒｐ 수용체 길항제
KR1020177015456A Active KR101854249B1 (ko) 2010-03-30 2011-03-11 Cgrp 수용체 길항제
KR1020187011875A Ceased KR20180049168A (ko) 2010-03-30 2011-03-11 Cgrp 수용체 길항제

Family Applications After (2)

Application Number Title Priority Date Filing Date
KR1020177015456A Active KR101854249B1 (ko) 2010-03-30 2011-03-11 Cgrp 수용체 길항제
KR1020187011875A Ceased KR20180049168A (ko) 2010-03-30 2011-03-11 Cgrp 수용체 길항제

Country Status (29)

Country Link
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)
ES (1) ES2562610T3 (enExample)
HR (1) HRP20160287T1 (enExample)
HU (1) HUE028735T2 (enExample)
IL (1) IL221665A (enExample)
MX (1) MX2012010725A (enExample)
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)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201519195D0 (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
GB201519194D0 (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
AU2020210024A1 (en) * 2019-01-20 2021-07-01 Biohaven Pharmaceutical Holding Company Ltd. CGRP antagonists for treating migraine breakthrough
WO2020210722A1 (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
EP4076395A4 (en) * 2019-12-17 2024-02-07 Pfizer Ireland Pharmaceuticals INTRANASAL PHARMACEUTICAL COMPOSITIONS 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
WO2022109077A1 (en) * 2020-11-19 2022-05-27 Biohaven Pharmaceutical Holding Company Ltd. Compositions for improved delivery of cgrp inhibitors
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
EP4320113A1 (en) 2021-04-09 2024-02-14 Teva Czech Industries s.r.o. Solid state forms of zavegepant and process for preparation thereof
US20250109188A1 (en) 2021-08-24 2025-04-03 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
US20250276959A1 (en) 2022-11-09 2025-09-04 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
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
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 (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003104236A1 (en) 2002-06-01 2003-12-18 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
US20070049577A1 (en) 2005-08-25 2007-03-01 Bristol-Myers Squibb Company CGRP antagonists

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7220862B2 (en) 2002-06-05 2007-05-22 Bristol-Myers Squibb Company Calcitonin gene related peptide receptor 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

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003104236A1 (en) 2002-06-01 2003-12-18 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
US20070049577A1 (en) 2005-08-25 2007-03-01 Bristol-Myers Squibb Company CGRP antagonists

Also Published As

Publication number Publication date
BR112012024785B1 (pt) 2020-12-01
TW201139414A (en) 2011-11-16
AR080746A1 (es) 2012-05-02
TWI483937B (zh) 2015-05-11
CA2794950A1 (en) 2011-10-06
SG183918A1 (en) 2012-10-30
RS54608B1 (sr) 2016-08-31
DK2552906T3 (en) 2016-03-29
ZA201207292B (en) 2014-03-26
HK1174914A1 (zh) 2013-06-21
CN102834388B (zh) 2014-07-16
CY1117593T1 (el) 2017-06-28
PE20130340A1 (es) 2013-03-30
ES2562610T3 (es) 2016-03-07
EA022815B1 (ru) 2016-03-31
KR20170068615A (ko) 2017-06-19
CA2794950C (en) 2017-09-26
EP2552906A1 (en) 2013-02-06
BR112012024785A8 (pt) 2017-10-17
AU2011233627A1 (en) 2012-11-15
BR112012024785A2 (pt) 2016-06-07
SI2552906T1 (sl) 2016-05-31
KR20180049168A (ko) 2018-05-10
SMT201600078B (it) 2016-04-29
US8481546B2 (en) 2013-07-09
HUE028735T2 (en) 2017-01-30
KR20130076807A (ko) 2013-07-08
CL2012002739A1 (es) 2013-03-22
PT2552906E (pt) 2016-03-18
HRP20160287T1 (hr) 2016-04-08
IL221665A (en) 2016-07-31
JP5908455B2 (ja) 2016-04-26
NZ603231A (en) 2014-02-28
MX2012010725A (es) 2012-10-05
KR101854249B1 (ko) 2018-05-03
CN102834388A (zh) 2012-12-19
JP2013523733A (ja) 2013-06-17
EA201270751A1 (ru) 2013-02-28
US20120059017A1 (en) 2012-03-08
AU2011233627B2 (en) 2013-09-12
PL2552906T3 (pl) 2016-06-30
EP2552906B1 (en) 2016-01-06
WO2011123232A1 (en) 2011-10-06

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