CN106380502A - 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
CN106380502A
CN106380502A CN201610680498.XA CN201610680498A CN106380502A CN 106380502 A CN106380502 A CN 106380502A CN 201610680498 A CN201610680498 A CN 201610680498A CN 106380502 A CN106380502 A CN 106380502A
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compound
disease
group
salt
acid
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Chinese (zh)
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R·佩里恰里
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Ntercept Pharmaceuticals Inc
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Ntercept Pharmaceuticals Inc
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J9/00Normal 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
    • C07J9/005Normal 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system

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  • 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)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Transplantation (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
CN201610680498.XA 2008-11-19 2009-11-19 G蛋白偶联受体5(tgr5)调节剂及其使用方法 Pending CN106380502A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP08169460 2008-11-19
EP08169460.6 2008-11-19
CN200980154703.7A 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

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN200980154703.7A Division 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

Publications (1)

Publication Number Publication Date
CN106380502A true CN106380502A (zh) 2017-02-08

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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
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

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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

Country Status (10)

Country Link
US (1) US8999964B2 (enExample)
EP (2) EP3150620B1 (enExample)
JP (1) JP5639073B2 (enExample)
CN (2) CN106380502A (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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US8940716B2 (en) 2010-05-06 2015-01-27 Bristol-Myers Squibb Company Bicyclic heteroaryl compounds as GPR119 modulators
TW201247627A (en) 2011-04-28 2012-12-01 Bristol Myers Squibb Co Novel bicyclic nitrogen containing heteroaryl TGR5 receptor modulators
KR102068381B1 (ko) * 2012-10-26 2020-01-20 인터셉트 파마슈티컬즈, 인크. 담즙산 유도체의 제조 방법
CA2891348C (en) * 2012-11-28 2020-04-28 Intercept Pharmaceuticals, Inc. Treatment of pulmonary disease
CN105636984A (zh) 2013-06-13 2016-06-01 法斯特弗沃德制药有限公司 用于治疗慢性炎症和预防胃肠道癌或纤维化的cd40信号转导抑制剂和其他化合物,该其他化合物是胆汁酸、胆汁酸衍生物、tgr5受体激动剂、fxr激动剂或其组合
EP3149019B1 (en) 2014-05-29 2019-12-04 Bar Pharmaceuticals S.r.l. Cholane derivatives for use in the treatment and/or prevention of fxr and tgr5/gpbar1 mediated diseases
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
TWI688571B (zh) * 2014-11-19 2020-03-21 英商Nzp英國有限公司 化合物(四)
PL3221331T3 (pl) * 2014-11-19 2020-03-31 NZP UK Limited Steroidy, 6-alkilo-7-hydroksy-4-en-3-ony jako związki pośrednie do wytwarzania steroidowych modulatorów fxr
WO2016079518A1 (en) * 2014-11-19 2016-05-26 Dextra Laboratories Limited 5.beta.-6-alkyl-7-hydroxy-3-one steroids as intermediates for the production of steroidal fxr modulators
MX2017006833A (es) * 2014-11-26 2018-02-13 Enanta Pharm Inc Análogos de ácido biliar como agonistas de fxr/tgr5 y métodos para el uso de los mismos.
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
GB201608776D0 (en) 2016-05-18 2016-06-29 Dextra Lab Ltd Methods and compounds
GB201608777D0 (en) 2016-05-18 2016-06-29 Dextra Lab Ltd Compounds
WO2018054300A1 (zh) * 2016-09-20 2018-03-29 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
WO2021071837A1 (en) 2019-10-07 2021-04-15 Kallyope, Inc. Gpr119 agonists
BR112022017039A2 (pt) 2020-02-28 2022-11-16 Kallyope Inc Agonistas de gpr40
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.
EP1591120A4 (en) 2003-01-28 2009-06-10 Takeda Chemical Industries Ltd RECEPTOR AGONISTS
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Non-Patent Citations (3)

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L. R. HAGEY ET AL.: "《A novel primary bile acid in the Shoebill stork and herons and its phylogenetic significance》", 《JOURNAL OF LIPID RESEARCH》 *
ROBERTO PELLICCIARI ET AL: "《Nongenomic actions of bile acids. Synthesis and preliminary characterization of 23-and 6,23-alkyl-substituted bile Acid derivatives as selective modulators for theG-protein coupled receptor TGR5》", 《J. MED. CHEM.》 *
TAKASHI IIDA ET AL.: "《Potential Bile Acid Metabolites. 25. Synthesis and Chemical Properties of Stereoisomeric 3a,7a,16- and 3a,7a,15-Trihydroxy-5b -cholan-24-oic Acids》", 《CLREM. PHARM. BULL》 *

Also Published As

Publication number Publication date
CN102282157B (zh) 2017-02-22
AU2009316484A1 (en) 2010-05-27
JP2012509349A (ja) 2012-04-19
EP3150620A1 (en) 2017-04-05
US20110263555A1 (en) 2011-10-27
EP2373673B1 (en) 2016-07-27
BRPI0921992A2 (pt) 2018-06-05
US8999964B2 (en) 2015-04-07
EP2373673A1 (en) 2011-10-12
WO2010059859A1 (en) 2010-05-27
CA2744135A1 (en) 2010-05-27
IL212970A (en) 2017-07-31
ES2774368T3 (es) 2020-07-20
EP3150620B1 (en) 2020-01-08
CA2744135C (en) 2017-07-04
BRPI0921992B1 (pt) 2021-12-14
ES2592452T3 (es) 2016-11-30
CN102282157A (zh) 2011-12-14
AU2009316484B2 (en) 2015-04-16
JP5639073B2 (ja) 2014-12-10
IL212970A0 (en) 2011-07-31

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