CN102282157B - G蛋白偶联受体5(tgr5)调节剂及其使用方法 - Google Patents

G蛋白偶联受体5(tgr5)调节剂及其使用方法 Download PDF

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Publication number
CN102282157B
CN102282157B CN200980154703.7A CN200980154703A CN102282157B CN 102282157 B CN102282157 B CN 102282157B CN 200980154703 A CN200980154703 A CN 200980154703A CN 102282157 B CN102282157 B CN 102282157B
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CN
China
Prior art keywords
compound
protein
acid
tgr5
bile
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Expired - Fee Related
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CN200980154703.7A
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English (en)
Chinese (zh)
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CN102282157A (zh
Inventor
R·佩里恰里
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Intercept Pharmaceuticals Inc
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Intercept Pharmaceuticals Inc
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Priority to CN201610680498.XA priority Critical patent/CN106380502A/zh
Publication of CN102282157A publication Critical patent/CN102282157A/zh
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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
    • C07J9/005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane containing a carboxylic function directly attached or attached by a chain containing only carbon atoms to the cyclopenta[a]hydrophenanthrene skeleton
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Transplantation (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
CN200980154703.7A 2008-11-19 2009-11-19 G蛋白偶联受体5(tgr5)调节剂及其使用方法 Expired - Fee Related CN102282157B (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201610680498.XA CN106380502A (zh) 2008-11-19 2009-11-19 G蛋白偶联受体5(tgr5)调节剂及其使用方法

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP08169460.6 2008-11-19
EP08169460 2008-11-19
PCT/US2009/065199 WO2010059859A1 (en) 2008-11-19 2009-11-19 Tgr5 modulators and methods of use thereof

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN201610680498.XA Division CN106380502A (zh) 2008-11-19 2009-11-19 G蛋白偶联受体5(tgr5)调节剂及其使用方法

Publications (2)

Publication Number Publication Date
CN102282157A CN102282157A (zh) 2011-12-14
CN102282157B true CN102282157B (zh) 2017-02-22

Family

ID=41666760

Family Applications (2)

Application Number Title Priority Date Filing Date
CN200980154703.7A Expired - Fee Related CN102282157B (zh) 2008-11-19 2009-11-19 G蛋白偶联受体5(tgr5)调节剂及其使用方法
CN201610680498.XA Pending CN106380502A (zh) 2008-11-19 2009-11-19 G蛋白偶联受体5(tgr5)调节剂及其使用方法

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN201610680498.XA Pending CN106380502A (zh) 2008-11-19 2009-11-19 G蛋白偶联受体5(tgr5)调节剂及其使用方法

Country Status (10)

Country Link
US (1) US8999964B2 (enExample)
EP (2) EP2373673B1 (enExample)
JP (1) JP5639073B2 (enExample)
CN (2) CN102282157B (enExample)
AU (1) AU2009316484B2 (enExample)
BR (1) BRPI0921992B1 (enExample)
CA (1) CA2744135C (enExample)
ES (2) ES2592452T3 (enExample)
IL (1) IL212970A (enExample)
WO (1) WO2010059859A1 (enExample)

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EA201270778A1 (ru) 2010-05-06 2013-04-30 Бристол-Майерс Сквибб Компани Бициклические гетероарильные аналоги в качестве модуляторов рецептора gpr119
EP2702042A1 (en) 2011-04-28 2014-03-05 Bristol-Myers Squibb Company Novel bicyclic nitrogen containing heteroaryl tgr5 receptor modulators
BR112015009395A2 (pt) * 2012-10-26 2017-07-04 Intercept Pharmaceuticals Inc processo para preparação de derivados do ácido biliar
BR112015012312A2 (pt) * 2012-11-28 2017-07-11 Intercept Pharmaceuticals Inc método de tratamento, redução do risco, prevenção ou alívio de uma afecção ou doença pulmonar em um sujeito; método de redução ou supressão de inflamação no pulmão em um sujeito; e método de promoção de reparo pulmonar em um sujeito
EP3008091A1 (en) 2013-06-13 2016-04-20 Fast Forward Pharmaceuticals B.V. Cd40 signalling inhibitor and a further compound, wherein the further compound is a bile acid, a bile acid derivative, an tgr5-receptor agonist, an fxr agonist or a combination thereof, for the treatment of chronic inflammation, and the prevention of gastrointestinal cancer or fibrosis.
WO2015181275A1 (en) * 2014-05-29 2015-12-03 Bar Pharmaceuticals S.R.L. Cholane derivatives for use in the treatment and/or prevention of fxr and tgr5/gpbar1 mediated diseases
MX375864B (es) * 2014-11-19 2025-03-07 Nzp Uk Ltd Esteroides de 5.beta-6-alquil-7-hidroxi-3-ona como intermedios para la produccion de moduladores esteroideos del receptor x farnesoide (fxr)
WO2016079520A1 (en) * 2014-11-19 2016-05-26 Dextra Laboratories Limited 6.alpha.-alkyl-6,7-dione steroids as intermediates for the production of steroidal fxr modulators
CN107108688B (zh) * 2014-11-19 2019-10-29 Nzp英国有限公司 作为制备类固醇FXR调节剂的中间体的6α-烷基-3,7-二酮类固醇
KR102526631B1 (ko) * 2014-11-19 2023-04-27 엔제트피 유케이 리미티드 스테로이드 fxr 조절인자를 제조하기 위한 중간체로서의 6-알킬-7-하이드록시-4-엔-3-온 스테로이드
CA2968404A1 (en) * 2014-11-26 2016-06-02 Enanta Pharmaceuticals, Inc. Bile acid analogs as fxr/tgr5 agonists and methods of use thereof
CN105348365A (zh) * 2014-12-03 2016-02-24 四川百利药业有限责任公司 一种胆酸衍生物及其制备方法、药物组合物和用途
CN104523703A (zh) * 2014-12-24 2015-04-22 聂飚 一种游离脂肪酸转运蛋白小分子抑制物的应用
CN104672290B (zh) * 2015-01-05 2017-06-06 北京普禄德医药科技有限公司 一种用于预防或治疗fxr‑介导的疾病的药物及其制备方法和用途
CN105330554B (zh) 2015-02-15 2017-07-11 上海迪赛诺药业股份有限公司 手性环丙基乙炔基叔醇类化合物的合成方法
CN105985396A (zh) 2015-02-16 2016-10-05 苏州泽璟生物制药有限公司 氘代鹅去氧胆酸衍生物以及包含该化合物的药物组合物
US10800807B2 (en) * 2015-06-19 2020-10-13 Intercept Pharmaceuticals, Inc. TGR5 modulators and methods of use thereof
CN106854229A (zh) * 2015-12-08 2017-06-16 陈剑 一类脂肪酸盐,其制备及其在医药上的应用
GB201608777D0 (en) 2016-05-18 2016-06-29 Dextra Lab Ltd Compounds
GB201608776D0 (en) 2016-05-18 2016-06-29 Dextra Lab Ltd Methods and compounds
CN109641934B (zh) * 2016-09-20 2021-07-02 江苏豪森药业集团有限公司 胆酸衍生物游离碱，晶型及其制备方法和应用
GB201812382D0 (en) 2018-07-30 2018-09-12 Nzp Uk Ltd Compounds
JP2022552655A (ja) 2019-10-07 2022-12-19 キャリーオペ，インク． Ｇｐｒ１１９アゴニスト
PH12022552277A1 (en) 2020-02-28 2024-03-04 Kallyope Inc Gpr40 agonists
JP2023526625A (ja) 2020-05-19 2023-06-22 キャリーオペ，インク． Ａｍｐｋアクチベーター
CN116390925A (zh) 2020-06-26 2023-07-04 卡尔优普公司 Ampk活化剂

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FR2696934B1 (fr) 1992-10-20 1995-06-02 Conservatoire Nal Arts Metiers Dérivés de stéroïdes naturels 3B hydroxyles ayant des propriétés de déclenchement et de stimulation de l'immunité, composition les contenant et procédé pour les obtenir.
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Also Published As

Publication number Publication date
IL212970A (en) 2017-07-31
AU2009316484B2 (en) 2015-04-16
CN106380502A (zh) 2017-02-08
EP2373673B1 (en) 2016-07-27
ES2774368T3 (es) 2020-07-20
US8999964B2 (en) 2015-04-07
ES2592452T3 (es) 2016-11-30
CA2744135C (en) 2017-07-04
WO2010059859A1 (en) 2010-05-27
CA2744135A1 (en) 2010-05-27
BRPI0921992B1 (pt) 2021-12-14
EP3150620B1 (en) 2020-01-08
IL212970A0 (en) 2011-07-31
EP2373673A1 (en) 2011-10-12
US20110263555A1 (en) 2011-10-27
JP2012509349A (ja) 2012-04-19
CN102282157A (zh) 2011-12-14
JP5639073B2 (ja) 2014-12-10
BRPI0921992A2 (pt) 2018-06-05
EP3150620A1 (en) 2017-04-05
AU2009316484A1 (en) 2010-05-27

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