ES2400293T3 - Derivados de indol e indolina ciclopropilamida como antagonistas de receptores EP4 - Google Patents

Derivados de indol e indolina ciclopropilamida como antagonistas de receptores EP4 Download PDF

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Publication number
ES2400293T3
ES2400293T3 ES08714673T ES08714673T ES2400293T3 ES 2400293 T3 ES2400293 T3 ES 2400293T3 ES 08714673 T ES08714673 T ES 08714673T ES 08714673 T ES08714673 T ES 08714673T ES 2400293 T3 ES2400293 T3 ES 2400293T3
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Spain
Prior art keywords
pharmaceutically acceptable
formula
compound according
compounds
acceptable salt
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Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
ES08714673T
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English (en)
Spanish (es)
Inventor
Michael Boyd
John Colucci
Yongxin Han
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Canada Inc
Original Assignee
Merck Canada Inc
Merck Frosst Canada Ltd
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Classifications

    • 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)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (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)
  • Vascular Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
ES08714673T 2007-02-26 2008-02-22 Derivados de indol e indolina ciclopropilamida como antagonistas de receptores EP4 Active ES2400293T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US90349407P 2007-02-26 2007-02-26
US903494P 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 (1)

Publication Number Publication Date
ES2400293T3 true ES2400293T3 (es) 2013-04-08

Family

ID=39720805

Family Applications (1)

Application Number Title Priority Date Filing Date
ES08714673T Active ES2400293T3 (es) 2007-02-26 2008-02-22 Derivados de indol e indolina ciclopropilamida como antagonistas de receptores EP4

Country Status (8)

Country Link
US (1) US8158671B2 (Direct)
EP (1) EP2114877B1 (Direct)
JP (1) JP5301469B2 (Direct)
CN (1) CN101622230B (Direct)
AU (1) AU2008221194B2 (Direct)
CA (1) CA2679175C (Direct)
ES (1) ES2400293T3 (Direct)
WO (1) WO2008104055A1 (Direct)

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MX2009011511A (es) 2007-04-26 2009-11-12 Takeda Pharmaceutical Compuesto biciclico y uso farmaceutico del mismo.
BRPI0912778B1 (pt) 2008-05-14 2019-04-30 Astellas Pharma Inc. Composto de amida, composição farmacêutica compreendedo dito composto e uso do mesmo para o tratamento de insuficiência renal crônica ou nefropatia diabética
WO2010019796A1 (en) 2008-08-14 2010-02-18 Chemietek, Llc Heterocyclic amide derivatives as ep4 receptor antagonists
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
MX2012012966A (es) * 2010-05-07 2013-01-22 Glaxosmithkline Llc Indoles.
CN103097358B (zh) 2010-09-21 2015-04-08 卫材R&D管理有限公司 药物组合物
CA2820109C (en) 2010-12-10 2018-01-09 Rottapharm S.P.A. Pyridine amide derivatives as ep4 receptor antagonists
KR101760164B1 (ko) 2011-07-04 2017-07-20 로타팜 바이오테크 에스.알.엘 Ep4 수용체 길항제로서 사이클릭 아민 유도체
WO2013004291A1 (en) 2011-07-04 2013-01-10 Rottapharm S.P.A. Cyclic amine derivatives as ep4 receptor agonists
UA115576C2 (uk) 2012-12-06 2017-11-27 Байєр Фарма Акцієнгезелльшафт Похідні бензимідазолу як антагоністи ер4
WO2014143591A1 (en) 2013-03-12 2014-09-18 Allergan, Inc. Inhibition of neovascularization by simultaneous inhibition of prostanoid ip and ep4 receptors
NO3009426T3 (Direct) * 2013-06-12 2018-09-29
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
AU2016338679B2 (en) 2015-10-16 2021-05-06 Eisai R&D Management Co., Ltd. EP4 antagonists
CR20180323A (es) 2015-11-20 2018-08-06 Idorsia Pharmaceuticals Ltd Derivados de indol n-sustituídos como moduladores de los receptores de pge2
CA3029611A1 (en) * 2016-07-07 2018-01-11 Ono Pharmaceutical Co., Ltd. Combination comprising ep4 antagonist and immune checkpoint inhibitor
WO2018162562A1 (en) 2017-03-10 2018-09-13 Bayer Pharma Aktiengesellschaft Use of an ep4 antagonist for the treatment of inflammatory pain
US11066405B2 (en) * 2017-04-18 2021-07-20 Tempest Therapeutics, Inc. Bicyclic compounds and their use in the treatment of cancer
EP3612517B1 (en) 2017-04-18 2022-03-02 Tempest Therapeutics, Inc. Bicyclic compounds and their use in the treatment of cancer
DK3625224T3 (da) 2017-05-18 2021-11-08 Idorsia Pharmaceuticals Ltd N-substituerede indolderivater
AR111807A1 (es) 2017-05-18 2019-08-21 Idorsia Pharmaceuticals Ltd Derivados de benzofurano y benzotiofeno como moduladores del receptor pge2
ES2893452T3 (es) 2017-05-18 2022-02-09 Idorsia Pharmaceuticals Ltd Derivados de pirimidina como moduladores del receptor de PGE2
ES2887041T3 (es) 2017-05-18 2021-12-21 Idorsia Pharmaceuticals Ltd Derivados de pirimidina como moduladores del receptor de PGE2
EP3625223B1 (en) 2017-05-18 2021-08-11 Idorsia Pharmaceuticals Ltd Pyrimidine derivatives
WO2019038156A1 (en) 2017-08-22 2019-02-28 Bayer Pharma Aktiengesellschaft USE OF AN EP4 ANTAGONIST FOR THE TREATMENT OF ARTHRITIS
AU2019229130B2 (en) 2018-03-02 2021-11-25 Foshan Ionova Biotherapeutics Co., Inc. Heterobicyclic carboxylic acids and salts thereof
BR112020021042A2 (pt) 2018-04-17 2021-01-19 Tempest Therapeutics, Inc. Carboxamidas bicíclicas e métodos de uso das mesmas
CA3105786A1 (en) * 2018-07-12 2020-01-16 Rottapharm Biotech S.R.L. (r)-4-(1-(1-(4-(trifluoromethyl)benzyl)pyrrolidine-2-carboxamide)cyclopropyl)-benzoic acid as ep4 receptor antagonist
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
US20230390303A1 (en) 2020-11-13 2023-12-07 Ono Pharmaceutical Co., Ltd. Cancer treatment by combination of ep4 antagonist and 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
CN115448913A (zh) * 2021-06-08 2022-12-09 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
JP2024532601A (ja) * 2021-08-27 2024-09-05 キーセラ（スーチョウ）バイオ－ファーマスーティカルズ カンパニー，リミテッド インドール化合物の固体形態、その調製方法及びその使用

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EP1262475A4 (en) 2000-03-09 2005-01-05 Ono Pharmaceutical Co INDOIND DERIVATIVES, METHOD FOR THE PRODUCTION THEREOF AND THEIR USE
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
CA2415742A1 (en) 2000-07-25 2002-01-31 Merck & Co., Inc. N-substituted indoles useful in the treatment of diabetes
KR100747401B1 (ko) * 2003-09-03 2007-08-08 화이자 인코포레이티드 프로스타글란딘 ｅ2 길항제로서의 페닐 또는 피리딜 아미드 화합물
AU2006246930C1 (en) * 2005-05-19 2012-01-19 Merck Canada Inc. Quinoline derivatives as EP4 antagonists
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
AU2008221194B2 (en) 2013-06-27
WO2008104055A1 (en) 2008-09-04
CN101622230B (zh) 2012-08-22
EP2114877A4 (en) 2010-10-27
US20090318518A1 (en) 2009-12-24
JP5301469B2 (ja) 2013-09-25
CA2679175A1 (en) 2008-09-04
US8158671B2 (en) 2012-04-17
EP2114877B1 (en) 2012-12-26
JP2010519260A (ja) 2010-06-03
CA2679175C (en) 2015-01-13
EP2114877A1 (en) 2009-11-11
AU2008221194A1 (en) 2008-09-04
CN101622230A (zh) 2010-01-06

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