CN101541778B - 作为ep4受体配体的噻吩甲酰胺衍生物 - Google Patents

作为ep4受体配体的噻吩甲酰胺衍生物 Download PDF

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Publication number
CN101541778B
CN101541778B CN200780037574.4A CN200780037574A CN101541778B CN 101541778 B CN101541778 B CN 101541778B CN 200780037574 A CN200780037574 A CN 200780037574A CN 101541778 B CN101541778 B CN 101541778B
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CN
China
Prior art keywords
compound
formula
alkyl
compounds
methyl
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Expired - Fee Related
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CN200780037574.4A
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English (en)
Chinese (zh)
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CN101541778A (zh
Inventor
M·布劳因
J·伯奇
Y·汉
C·梅伦
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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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D333/38—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
CN200780037574.4A 2006-08-11 2007-08-10 作为ep4受体配体的噻吩甲酰胺衍生物 Expired - Fee Related CN101541778B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US83725206P 2006-08-11 2006-08-11
US60/837,252 2006-08-11
PCT/CA2007/001404 WO2008017164A1 (en) 2006-08-11 2007-08-10 Thiophenecarboxamide derivatives as ep4 receptor ligands

Publications (2)

Publication Number Publication Date
CN101541778A CN101541778A (zh) 2009-09-23
CN101541778B true CN101541778B (zh) 2014-10-08

Family

ID=39032586

Family Applications (1)

Application Number Title Priority Date Filing Date
CN200780037574.4A Expired - Fee Related CN101541778B (zh) 2006-08-11 2007-08-10 作为ep4受体配体的噻吩甲酰胺衍生物

Country Status (8)

Country Link
US (1) US8969394B2 (enExample)
EP (1) EP2054401B1 (enExample)
JP (1) JP5259592B2 (enExample)
CN (1) CN101541778B (enExample)
AU (1) AU2007283404B2 (enExample)
CA (1) CA2660133C (enExample)
ES (1) ES2421453T3 (enExample)
WO (1) WO2008017164A1 (enExample)

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US20110028463A1 (en) * 2007-07-03 2011-02-03 Astellas Pharma Inc. Amide compounds
CA2694347A1 (en) * 2007-08-09 2009-02-12 Merck Sharp & Dohme Corp. Process for making thiophene carboxamide derivative
SI2565191T1 (sl) * 2008-05-14 2014-12-31 Astellas Pharma Inc. Derivati 4-(indol-7-ilkarbonilaminometil)cikloheksan karboksilne kisline kot EP4 receptorski antagonisti, uporabni za zdravljenje kronične ledvične odpovedi ali diabetične nefropatije
EP2320906B1 (en) * 2008-08-14 2016-02-24 Beta Pharma Canada Inc. Heterocyclic amide derivatives as ep4 receptor antagonists
JP2013508282A (ja) 2009-10-14 2013-03-07 ジェンムス ファーマ インコーポレイティド ウイルス感染のための併用療法処置
MX341482B (es) * 2010-02-22 2016-08-22 Raqualia Pharma Inc Antagonistas del receptor ep4 y su uso en el tratamiento de enfermedades mediadas por la il-23.
PH12013500467A1 (en) 2010-09-21 2013-04-29 Eisai R&D Man Co Ltd Pharmaceutical composition
CA2820109C (en) 2010-12-10 2018-01-09 Rottapharm S.P.A. Pyridine amide derivatives as ep4 receptor antagonists
UA115576C2 (uk) 2012-12-06 2017-11-27 Байєр Фарма Акцієнгезелльшафт Похідні бензимідазолу як антагоністи ер4
US10391086B2 (en) 2013-03-19 2019-08-27 Askat Inc. Use of EP4 receptor antagonists in the treatment of cartilage disease
KR102556734B1 (ko) 2013-03-19 2023-07-18 에스크엣 인크. 연골질환 치료에서의 ep4 수용체 길항제의 용도
PT3009426T (pt) 2013-06-12 2018-06-08 Kaken Pharma Co Ltd Derivado de 4-alquinilimidazole e medicamento compreendendo o mesmo como ingrediente ativo
EP3492106B1 (en) 2013-08-09 2021-02-17 Ardelyx, Inc. Compounds and methods for inhibiting phosphate transport
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
TW201623277A (zh) 2014-03-26 2016-07-01 安斯泰來製藥股份有限公司 醯胺化合物
US20170182003A1 (en) * 2014-05-23 2017-06-29 Eisai R&D Management Co., Ltd. Combination therapies for the treatment of cancer
US9926262B2 (en) * 2014-06-06 2018-03-27 Allergan, Inc. EP4 agonists as therapeutic compounds
CN105037186A (zh) * 2015-06-17 2015-11-11 苏州敬业医药化工有限公司 一种氨甲苯酸的制备方法
CR20180323A (es) 2015-11-20 2018-08-06 Idorsia Pharmaceuticals Ltd Derivados de indol n-sustituídos como moduladores de los receptores de pge2
WO2018162562A1 (en) 2017-03-10 2018-09-13 Bayer Pharma Aktiengesellschaft Use of an ep4 antagonist for the treatment of inflammatory pain
AR111941A1 (es) 2017-05-18 2019-09-04 Idorsia Pharmaceuticals Ltd Derivados de pirimidina como moduladores del receptor de pge2
MX388257B (es) 2017-05-18 2025-03-19 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
US20200069686A1 (en) 2017-05-18 2020-03-05 Idorsia Pharmaceuticals Ltd N-substituted indole 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
WO2019038156A1 (en) 2017-08-22 2019-02-28 Bayer Pharma Aktiengesellschaft USE OF AN EP4 ANTAGONIST FOR THE TREATMENT OF ARTHRITIS
US10202415B1 (en) 2017-10-19 2019-02-12 King Saud University Method of synthesizing of 3-oxolupenal nanoparticles
EP3972599B1 (en) 2019-05-21 2025-10-22 Ardelyx, Inc. Combination for lowering serum phosphate in a patient
CN112552200B (zh) * 2019-09-10 2024-03-12 烟台药物研究所 一种光学纯4-(1-氨基)乙基苯甲酸酯及其盐的制备方法
US20240002388A1 (en) * 2020-08-18 2024-01-04 Hutchison Medipharma Limited Pyrimidinone compounds and uses 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

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WO2005021508A1 (en) * 2003-09-03 2005-03-10 Pfizer Inc. Phenyl or pyridyl amide compounds as prostaglandin e2 antagonists
WO2005102389A2 (en) * 2004-04-20 2005-11-03 Pfizer Products Inc. Combinations comprising alpha-2-delta ligands and ep4 receptor antagonists
WO2005105732A1 (en) * 2004-05-04 2005-11-10 Pfizer Japan Inc. Substituted methyl aryl or heteroaryl amide compounds
WO2005105733A1 (en) * 2004-05-04 2005-11-10 Pfizer Japan Inc. Ortho substituted aryl or heteroaryl amide compounds
WO2005116010A1 (en) * 2004-05-26 2005-12-08 Merck Frosst Canada Ltd. Ep4 receptor agonist, compositions and methods thereof

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US5962490A (en) * 1987-09-25 1999-10-05 Texas Biotechnology Corporation Thienyl-, furyl- and pyrrolyl-sulfonamides and derivatives thereof that modulate the activity of endothelin
EP0752421B1 (en) 1995-07-07 2005-10-12 AstraZeneca AB Ortho-substituted aromatic compounds, containing three (het)aryl moieties, their preparation and their use as prostaglandin E2-(PGE2)-antagonists
BR0116850A (pt) * 2001-01-31 2004-02-25 Pfizer Prod Inc Derivados de amida de ácido tiazolil-, oxazolil-, pirrolil- e imidazolil- úteis como inibidores de isoenzimas de pde4
WO2004099127A1 (en) 2003-05-07 2004-11-18 Novo Nordisk A/S Novel compounds as kinase inhibitors
GB0324269D0 (en) * 2003-10-16 2003-11-19 Pharmagene Lab Ltd EP4 receptor antagonists

Patent Citations (5)

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WO2005021508A1 (en) * 2003-09-03 2005-03-10 Pfizer Inc. Phenyl or pyridyl amide compounds as prostaglandin e2 antagonists
WO2005102389A2 (en) * 2004-04-20 2005-11-03 Pfizer Products Inc. Combinations comprising alpha-2-delta ligands and ep4 receptor antagonists
WO2005105732A1 (en) * 2004-05-04 2005-11-10 Pfizer Japan Inc. Substituted methyl aryl or heteroaryl amide compounds
WO2005105733A1 (en) * 2004-05-04 2005-11-10 Pfizer Japan Inc. Ortho substituted aryl or heteroaryl amide compounds
WO2005116010A1 (en) * 2004-05-26 2005-12-08 Merck Frosst Canada Ltd. Ep4 receptor agonist, compositions and methods thereof

Also Published As

Publication number Publication date
US20090247596A1 (en) 2009-10-01
WO2008017164A1 (en) 2008-02-14
ES2421453T3 (es) 2013-09-02
CA2660133A1 (en) 2008-02-14
AU2007283404A1 (en) 2008-02-14
JP5259592B2 (ja) 2013-08-07
JP2010500293A (ja) 2010-01-07
CA2660133C (en) 2015-10-27
EP2054401A1 (en) 2009-05-06
EP2054401B1 (en) 2013-05-01
AU2007283404B2 (en) 2013-04-18
CN101541778A (zh) 2009-09-23
EP2054401A4 (en) 2010-10-13
US8969394B2 (en) 2015-03-03

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Address after: Quebec

Applicant after: Merck Canada Inc.

Address before: Quebec

Applicant before: Merck Frosst Canada Ltd.

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Free format text: CORRECT: APPLICANT; FROM: MERCK FROSST CANADA LTD. TO: MERCK (CANADA) CO., LTD.

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Granted publication date: 20141008

Termination date: 20170810

CF01 Termination of patent right due to non-payment of annual fee