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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JP2010519260A5 (OSRAM
JP2010519260A (ja
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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)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole 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 (OSRAM) 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 (OSRAM)
EP (1) EP2114877B1 (OSRAM)
JP (1) JP5301469B2 (OSRAM)
CN (1) CN101622230B (OSRAM)
AU (1) AU2008221194B2 (OSRAM)
CA (1) CA2679175C (OSRAM)
ES (1) ES2400293T3 (OSRAM)
WO (1) WO2008104055A1 (OSRAM)

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JP5289308B2 (ja) 2007-04-26 2013-09-11 武田薬品工業株式会社 二環性化合物およびその医薬用途
EP2565191B1 (en) 2008-05-14 2014-10-08 Astellas Pharma Inc. 4-(Indol-7-ylcarbonylaminomethyl)cyclohexanecarboxylic acid derivatives as EP4 receptor antagonists useful for the treatment of chronic renal failure or diabetic nephropathy
US8404736B2 (en) 2008-08-14 2013-03-26 Beta Pharma Canada Inc. Heterocyclic amide derivatives as EP4 receptor antagonists
EP2392323A4 (en) 2009-01-30 2012-09-26 Univ Kyoto INHIBITOR OF PROSTATE CANCER PROGRESSION AND METHOD OF INHIBITING PROGRESSION
WO2010121382A1 (en) * 2009-04-21 2010-10-28 Merck Frosst Canada Ltd. Process for making indole cyclopropyl amide derivatives
EP2566327B1 (en) * 2010-05-07 2017-03-29 Glaxosmithkline LLC Indoles
PT2619182T (pt) 2010-09-21 2017-01-17 Eisai R&D Man Co Ltd Composição farmacêutica
ES2545110T3 (es) 2010-12-10 2015-09-08 Rottapharm Biotech S.R.L. Derivados de piridinamida como antagonistas del receptor EP4
WO2013004290A1 (en) 2011-07-04 2013-01-10 Rottapharm S.P.A. Cyclic amine derivatives as ep4 receptor antagonists
EP2729141B1 (en) 2011-07-04 2015-12-09 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
CN105431416B (zh) 2013-06-12 2019-01-08 科研制药株式会社 4-炔基咪唑衍生物和含有其作为有效成分的药物
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
ES2900306T3 (es) 2016-07-07 2022-03-16 Ono Pharmaceutical Co Combinación que comprende un antagonista de EP4 y un inhibidor de puntos de control inmunitario
WO2018162562A1 (en) 2017-03-10 2018-09-13 Bayer Pharma Aktiengesellschaft Use of an ep4 antagonist for the treatment of inflammatory pain
IL270021B (en) 2017-04-18 2022-08-01 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
WO2018210992A1 (en) 2017-05-18 2018-11-22 Idorsia Pharmaceuticals Ltd Pyrimidine derivatives
JP7093791B2 (ja) 2017-05-18 2022-06-30 イドーシア ファーマシューティカルズ リミテッド Ｐｇｅ２レセプター調節剤としてのベンゾフラン及びベンゾチオフェン誘導体
SI3625224T1 (sl) 2017-05-18 2021-11-30 Idorsia Pharmaceuticals Ltd N-substituirani indolni derivati
MA49126B1 (fr) 2017-05-18 2021-10-29 Idorsia Pharmaceuticals Ltd Dérivés de phényle utilisés en tant que modulateurs des récepteurs des pge2
WO2018210988A1 (en) 2017-05-18 2018-11-22 Idorsia Pharmaceuticals Ltd Pyrimidine derivatives as pge2 receptor modulators
WO2019038156A1 (en) 2017-08-22 2019-02-28 Bayer Pharma Aktiengesellschaft USE OF AN EP4 ANTAGONIST FOR THE TREATMENT OF ARTHRITIS
WO2019166022A1 (en) 2018-03-02 2019-09-06 Shenzhen Ionova Life Science Co., Ltd. Heterobicyclic carboxylic acids and salts thereof
EP3781550B1 (en) 2018-04-17 2024-10-30 Tempest Therapeutics, Inc. Bicyclic carboxamides and methods of use thereof
AU2019300449A1 (en) 2018-07-12 2021-03-04 Rottapharm Biotech S.R.L. (R)-4-(1-(1-(4-(trifluoromethyl)benzyl)pyrrolidine-2-carboxamide)cyclopropyl)-benzoic acid as EP4 receptor antagonist
US12240812B2 (en) 2019-01-22 2025-03-04 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
TW202228674A (zh) 2020-11-13 2022-08-01 日商小野藥品工業股份有限公司 藉由併用ｅｐ４拮抗藥與免疫檢查點抑制物質而進行之癌症治療
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
US20240294511A1 (en) * 2021-08-27 2024-09-05 Keythera (Suzhou) Bio-Pharmaceuticals Co., Limited Solid form of indole compound, preparation method therefor and use thereof

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JP4292742B2 (ja) * 2000-03-09 2009-07-08 小野薬品工業株式会社 インドール誘導体、その製造方法および用途
AU2000234451B2 (en) * 2000-03-24 2005-09-29 Asterand Uk Acquisition Limited Use of prostanoid ep4 receptor antagonists for the treatment of headache and assays for such antagonists
JP2004513076A (ja) * 2000-07-25 2004-04-30 メルク　エンド　カムパニー　インコーポレーテッド 糖尿病治療で有用なｎ−置換インドール類
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JP5289046B2 (ja) * 2005-05-19 2013-09-11 メルク カナダ インコーポレイテッド Ｅｐ４アンタゴニストとしてのキノリン誘導体
ES2392192T3 (es) 2006-04-24 2012-12-05 Merck Canada Inc. Derivados de indol amida como antagonistas del receptor EP4
JP5183628B2 (ja) * 2006-06-12 2013-04-17 メルク カナダ インコーポレイテッド Ｅｐ４受容体リガンドとしてのインドリンアミド誘導体

Also Published As

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

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