JP5639073B2 - Tgr5モジュレーターおよびその使用方法 - Google Patents

Tgr5モジュレーターおよびその使用方法 Download PDF

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Publication number
JP5639073B2
JP5639073B2 JP2011537627A JP2011537627A JP5639073B2 JP 5639073 B2 JP5639073 B2 JP 5639073B2 JP 2011537627 A JP2011537627 A JP 2011537627A JP 2011537627 A JP2011537627 A JP 2011537627A JP 5639073 B2 JP5639073 B2 JP 5639073B2
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compound
disease
salt
solvate
amino acid
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JP2012509349A (ja
JP2012509349A5 (enExample
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ロベルト ペリッキアーリ,
ロベルト ペリッキアーリ,
Original Assignee
インターセプト ファーマシューティカルズ, インコーポレイテッド
インターセプト ファーマシューティカルズ, インコーポレイテッド
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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)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
JP2011537627A 2008-11-19 2009-11-19 Tgr5モジュレーターおよびその使用方法 Expired - Fee Related JP5639073B2 (ja)

Applications Claiming Priority (3)

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

Publications (3)

Publication Number Publication Date
JP2012509349A JP2012509349A (ja) 2012-04-19
JP2012509349A5 JP2012509349A5 (enExample) 2013-01-10
JP5639073B2 true JP5639073B2 (ja) 2014-12-10

Family

ID=41666760

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2011537627A Expired - Fee Related JP5639073B2 (ja) 2008-11-19 2009-11-19 Tgr5モジュレーターおよびその使用方法

Country Status (10)

Country Link
US (1) US8999964B2 (enExample)
EP (2) EP3150620B1 (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)

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2012012902A (es) 2010-05-06 2012-12-17 Bristol Myers Squibb Co Analogos heteroarilo biciclicos como moduladores de receptor acoplado a la proteina g gpr119.
US9062028B2 (en) 2011-04-28 2015-06-23 Bristol-Myers Squibb Company Bicyclic nitrogen containing heteroaryl TGR5 receptor modulators
SMT201700602T1 (it) * 2012-10-26 2018-03-08 Intercept Pharmaceuticals Inc Processo per la preparazione di derivati dell’acido biliare
SG11201503697TA (en) * 2012-11-28 2015-06-29 Intercept Pharmaceuticals Inc Treatment of pulmonary disease
AU2014278833A1 (en) 2013-06-13 2016-01-07 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.
LT3626725T (lt) 2014-05-29 2023-03-10 Bar Pharmaceuticals S.R.L. Cholano dariniai skirti naudoti ligų, kurių atsiradimui tarpininkauja fxr ir tgr5/gpbar1, gydymui ir (arba) profilaktikai
KR102527821B1 (ko) * 2014-11-19 2023-05-02 엔제트피 유케이 리미티드 스테로이드 FXR 조절인자를 제조하기 위한 중간체로서의 6α-알킬-6,7-다이온 스테로이드
MX375863B (es) * 2014-11-19 2025-03-07 Nzp Uk Ltd Esteroides de 6-alquil-7-hidroxi-4-en-3-ona como intermedios para la produccion de moduladores esteroideos del receptor x farnesoide (fxr)
WO2016079519A1 (en) * 2014-11-19 2016-05-26 Dextra Laboratories Limited 6.alpha.-alkyl-3,7-dione steroids as intermediates for the production of steroidal fxr modulators
KR102526632B1 (ko) 2014-11-19 2023-04-27 엔제트피 유케이 리미티드 스테로이드 FXR 조절인자를 제조하기 위한 중간체로서의 5β-6-알킬-7-하이드록시-3-온 스테로이드
CN107231795A (zh) * 2014-11-26 2017-10-03 英安塔制药有限公司 作为fxr/tgr5激动剂的胆汁酸类似物及其使用方法
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
CA3156985A1 (en) 2019-10-07 2021-04-15 Kallyope, Inc. Gpr119 agonists
JP7745559B2 (ja) 2020-02-28 2025-09-29 キャリーオペ,インク. Gpr40アゴニスト
CA3178994A1 (en) 2020-05-19 2021-11-25 Iyassu Sebhat Ampk activators
CN116390925A (zh) 2020-06-26 2023-07-04 卡尔优普公司 Ampk活化剂

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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.
WO2004067008A1 (ja) 2003-01-28 2004-08-12 Takeda Pharmaceutical Company Limited 受容体作動薬
EA017714B1 (ru) * 2007-01-19 2013-02-28 Интерсепт Фармасьютикалз, Инк. Модуляторы tgr5 и способы их применения

Also Published As

Publication number Publication date
US20110263555A1 (en) 2011-10-27
IL212970A0 (en) 2011-07-31
BRPI0921992B1 (pt) 2021-12-14
US8999964B2 (en) 2015-04-07
WO2010059859A1 (en) 2010-05-27
CN106380502A (zh) 2017-02-08
ES2592452T3 (es) 2016-11-30
BRPI0921992A2 (pt) 2018-06-05
JP2012509349A (ja) 2012-04-19
CN102282157A (zh) 2011-12-14
AU2009316484A1 (en) 2010-05-27
EP2373673A1 (en) 2011-10-12
CA2744135C (en) 2017-07-04
AU2009316484B2 (en) 2015-04-16
EP3150620A1 (en) 2017-04-05
ES2774368T3 (es) 2020-07-20
CA2744135A1 (en) 2010-05-27
EP2373673B1 (en) 2016-07-27
IL212970A (en) 2017-07-31
EP3150620B1 (en) 2020-01-08
CN102282157B (zh) 2017-02-22

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