JP5301469B2 - Ｅｐ４受容体アンタゴニストとしてのインドール及びインドリンシクロプロピルアミド誘導体 - Google Patents

Ｅｐ４受容体アンタゴニストとしてのインドール及びインドリンシクロプロピルアミド誘導体 Download PDF

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Publication number
JP5301469B2
JP5301469B2 JP2009550652A JP2009550652A JP5301469B2 JP 5301469 B2 JP5301469 B2 JP 5301469B2 JP 2009550652 A JP2009550652 A JP 2009550652A JP 2009550652 A JP2009550652 A JP 2009550652A JP 5301469 B2 JP5301469 B2 JP 5301469B2
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compounds
formula
compound
mmol
acid
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JP2010519260A (ja
JP2010519260A5 (cg-RX-API-DMAC7.html
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ボイド，マイケル
コルッチ，ジョン
ハン，ヨンシン
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Merck Canada Inc
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Merck Canada Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • C07D403/02—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 two hetero rings
    • C07D403/12—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 two hetero rings linked by a chain containing hetero atoms as chain links

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2009550652A 2007-02-26 2008-02-22 Ｅｐ４受容体アンタゴニストとしてのインドール及びインドリンシクロプロピルアミド誘導体 Expired - Fee Related JP5301469B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US90349407P 2007-02-26 2007-02-26
US60/903,494 2007-02-26
PCT/CA2008/000351 WO2008104055A1 (en) 2007-02-26 2008-02-22 Indole and indoline cyclopropyl amide derivatives as ep4 receptor antagonists

Publications (3)

Publication Number Publication Date
JP2010519260A JP2010519260A (ja) 2010-06-03
JP2010519260A5 JP2010519260A5 (cg-RX-API-DMAC7.html) 2011-03-31
JP5301469B2 true JP5301469B2 (ja) 2013-09-25

Family

ID=39720805

Family Applications (1)

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JP2009550652A Expired - Fee Related JP5301469B2 (ja) 2007-02-26 2008-02-22 Ｅｐ４受容体アンタゴニストとしてのインドール及びインドリンシクロプロピルアミド誘導体

Country Status (8)

Country Link
US (1) US8158671B2 (cg-RX-API-DMAC7.html)
EP (1) EP2114877B1 (cg-RX-API-DMAC7.html)
JP (1) JP5301469B2 (cg-RX-API-DMAC7.html)
CN (1) CN101622230B (cg-RX-API-DMAC7.html)
AU (1) AU2008221194B2 (cg-RX-API-DMAC7.html)
CA (1) CA2679175C (cg-RX-API-DMAC7.html)
ES (1) ES2400293T3 (cg-RX-API-DMAC7.html)
WO (1) WO2008104055A1 (cg-RX-API-DMAC7.html)

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EA200971003A1 (ru) 2007-04-26 2010-04-30 Такеда Фармасьютикал Компани Лимитед Бициклическое соединение и его фармацевтическое применение
DK2565191T3 (da) 2008-05-14 2014-11-10 Astellas Pharma Inc 4-(Indol-7-ylcarbonylaminomethyl)cyclohexancarboxylsyrederivater som EP4-receptorantagonister der er anvendelige til behandlingen af kronisk nyresvigt eller diabetisk nephropati
JP5536773B2 (ja) * 2008-08-14 2014-07-02 ベータ・ファーマ・カナダ・インコーポレイテッド Ｅｐ４受容体アンタゴニストとしてのヘテロ環式アミド誘導体
US20110287112A1 (en) 2009-01-30 2011-11-24 Ono Pharmaceutical Co., Ltd. Prostate cancer progression inhibitor and progression inhibition method
WO2010121382A1 (en) * 2009-04-21 2010-10-28 Merck Frosst Canada Ltd. Process for making indole cyclopropyl amide derivatives
CN102970869B (zh) * 2010-05-07 2014-07-16 葛兰素史密斯克莱有限责任公司 吲哚
JP5956448B2 (ja) 2010-09-21 2016-07-27 エーザイ・アール・アンド・ディー・マネジメント株式会社 医薬組成物
US8828987B2 (en) 2010-12-10 2014-09-09 Rottapharm Biotech S.R.L. Pyridine amide derivatives as EP4 receptor antagonists
DK2729445T3 (en) 2011-07-04 2016-01-18 Rottapharm Biotech Srl CYCLIC AMINE DERIVATIVES AS EP4 RECEPTOR ANTAGONISTS
US9120824B2 (en) 2011-07-04 2015-09-01 Rottapharm Biotech S.R.L. Cyclic amine derivatives as EP4 receptor agonists
UA115576C2 (uk) 2012-12-06 2017-11-27 Байєр Фарма Акцієнгезелльшафт Похідні бензимідазолу як антагоністи ер4
US9295665B2 (en) 2013-03-12 2016-03-29 Allergan, Inc. Inhibition of neovascularization by simultaneous inhibition of prostanoid IP and EP4 receptors
LT3009426T (lt) 2013-06-12 2018-07-25 Kaken Pharmaceutical Co., Ltd. 4-alkinilimidazolo darinys ir jį, kaip veiklųjį ingredientą, apimantis vaistas
TW201607943A (zh) 2013-12-19 2016-03-01 拜耳製藥公司 作為ｅｐ４配體之新穎苯并咪唑衍生物
CN108473497B (zh) 2015-10-16 2021-09-10 卫材R&D 管理有限公司 Ep4拮抗剂
CR20180323A (es) 2015-11-20 2018-08-06 Idorsia Pharmaceuticals Ltd Derivados de indol n-sustituídos como moduladores de los receptores de pge2
HUE057799T2 (hu) 2016-07-07 2022-06-28 Ono Pharmaceutical Co EP4 antagonistát és immunellenõrzõpont gátlót tartalmazó kombináció
WO2018162562A1 (en) 2017-03-10 2018-09-13 Bayer Pharma Aktiengesellschaft Use of an ep4 antagonist for the treatment of inflammatory pain
WO2018195123A1 (en) 2017-04-18 2018-10-25 Tempest Therapeutics, Inc. Bicyclic compounds and their use in the treatment of cancer
US11066405B2 (en) * 2017-04-18 2021-07-20 Tempest Therapeutics, Inc. Bicyclic compounds and their use in the treatment of cancer
PE20191787A1 (es) 2017-05-18 2019-12-24 Idorsia Pharmaceuticals Ltd Derivados de indol n-sustituidos
KR102626982B1 (ko) 2017-05-18 2024-01-18 이도르시아 파마슈티컬스 리미티드 Pge2 수용체 조절제로서의 피리미딘 유도체
WO2018210994A1 (en) 2017-05-18 2018-11-22 Idorsia Pharmaceuticals Ltd Phenyl derivatives as pge2 receptor modulators
CA3063632A1 (en) 2017-05-18 2018-11-22 Idorsia Pharmaceuticals Ltd Benzofurane and benzothiophene derivatives as pge2 receptor modulators
ES2896476T3 (es) 2017-05-18 2022-02-24 Idorsia Pharmaceuticals Ltd Derivados de pirimidina
WO2019038156A1 (en) 2017-08-22 2019-02-28 Bayer Pharma Aktiengesellschaft USE OF AN EP4 ANTAGONIST FOR THE TREATMENT OF ARTHRITIS
CN111936502B (zh) * 2018-03-02 2024-05-31 深圳市原力生命科学有限公司 杂二环羧酸及其盐
AU2019255717B2 (en) 2018-04-17 2022-12-08 Tempest Therapeutics, Inc. Bicyclic carboxamides and methods of use thereof
ES2948293T3 (es) 2018-07-12 2023-09-07 Rottapharm Biotech Srl Acido (R)-4-(1-(1-(4-(trifluorometil)bencil)pirrolidina-2-carboxamida)ciclopropil)-benzoico como antagonista del receptor EP4
EP3889134B1 (en) 2019-01-22 2024-09-25 Keythera (Suzhou) Pharmaceuticals Co. Ltd. Compound for inhibiting pge2/ep4 signaling transduction inhibiting, preparation method therefor, and medical uses thereof
EP3722319A1 (en) 2019-04-09 2020-10-14 Rottapharm Biotech S.r.l. Pharmaceutical combination of an ep4 antagonist and immune checkpoint inhibitors for the treatment of tumours
EP3827828A1 (en) 2019-11-29 2021-06-02 Rottapharm Biotech S.r.l. (r)-4-(1-(6-(4-(trifluoromethyl)benzyl)-6-azaspiro[2.5]octane-5-carboxamido)-cyclopropyl) benzoic acid or its salt also in polymorphic form a for use in the prevention of heterotopic ossification
WO2021115560A1 (en) 2019-12-09 2021-06-17 Rottapharm Biotech S.R.L. New fyn and vegfr2 kinase inhibitors
EP3885339A1 (en) 2020-03-27 2021-09-29 Rottapharm Biotech S.r.l. Process for the preparation of (r)-4-(1-(6-(4-(trifluoromethyl)benzyl)-6-azaspiro[2.5]octane-5-carboxamido)-cyclopropyl) benzoic acid or a salt thereof
EP4245301A4 (en) 2020-11-13 2024-08-21 ONO Pharmaceutical Co., Ltd. TREATMENT OF CANCER BY COMBINED USE OF AN EP4 ANTAGONIST AND AN IMMUNE CHECKPOINT INHIBITOR
WO2022247881A1 (zh) * 2021-05-28 2022-12-01 凯复(苏州)生物医药有限公司 治疗肿瘤的联合疗法
WO2022257960A1 (zh) * 2021-06-08 2022-12-15 武汉人福创新药物研发中心有限公司 用于治疗ep2、ep4受体介导的疾病的双环化合物
CA3230102A1 (en) * 2021-08-27 2023-03-02 Yongqi Deng Solid form of indole compound, preparation method therefor and use thereof

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AU2001241068A1 (en) 2000-03-09 2001-09-17 Ono Pharmaceutical Co., Ltd. Indole derivatives, process for preparation of the same and use thereof
EP1267867B1 (en) * 2000-03-24 2008-05-14 Asterand Uk Limited Use of prostanoid ep4 receptor antagonists for the treatment of headache and assays for such antagonists
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AU2004268839A1 (en) * 2003-09-03 2005-03-10 Pfizer Inc. Phenyl or pyridyl amide compounds as prostaglandin E2 antagonists
US8013159B2 (en) * 2005-05-19 2011-09-06 Merck Canada Inc. Quinoline derivatives as EP4 antagonists
CA2648729A1 (en) * 2006-04-24 2007-11-01 Merck Frosst Canada Ltd. Indole amide derivatives as ep4 receptor antagonists
EP2035376B1 (en) * 2006-06-12 2014-08-27 Merck Canada Inc. Indoline amide derivatives as ep4 receptor ligands

Also Published As

Publication number Publication date
AU2008221194B2 (en) 2013-06-27
ES2400293T3 (es) 2013-04-08
CA2679175A1 (en) 2008-09-04
US8158671B2 (en) 2012-04-17
EP2114877A1 (en) 2009-11-11
WO2008104055A1 (en) 2008-09-04
JP2010519260A (ja) 2010-06-03
CN101622230B (zh) 2012-08-22
CA2679175C (en) 2015-01-13
US20090318518A1 (en) 2009-12-24
EP2114877B1 (en) 2012-12-26
AU2008221194A1 (en) 2008-09-04
CN101622230A (zh) 2010-01-06
EP2114877A4 (en) 2010-10-27

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