JP5535233B2 - 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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JP5535233B2
JP5535233B2 JP2011537624A JP2011537624A JP5535233B2 JP 5535233 B2 JP5535233 B2 JP 5535233B2 JP 2011537624 A JP2011537624 A JP 2011537624A JP 2011537624 A JP2011537624 A JP 2011537624A JP 5535233 B2 JP5535233 B2 JP 5535233B2
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compound
hydrogen
tgr5
methyl
acid
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JP2012509348A5 (OSRAM
JP2012509348A (ja
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ロベルト ペリッキアーリ，
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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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    • 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
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
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    • 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
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    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
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    • 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
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • 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
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/006—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Pulmonology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Endocrinology (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Emergency Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Transplantation (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
JP2011537624A 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 JP5535233B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP08169462.2 2008-11-19
EP08169462 2008-11-19
PCT/US2009/065188 WO2010059853A1 (en) 2008-11-19 2009-11-19 Tgr5 modulators and method of use thereof

Related Child Applications (1)

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JP2014088019A Division JP2014159456A (ja) 2008-11-19 2014-04-22 Ｔｇｒ５モジュレーターおよびその使用方法

Publications (3)

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JP2012509348A JP2012509348A (ja) 2012-04-19
JP2012509348A5 JP2012509348A5 (OSRAM) 2012-12-13
JP5535233B2 true JP5535233B2 (ja) 2014-07-02

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ID=41668454

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JP2011537624A Expired - Fee Related JP5535233B2 (ja) 2008-11-19 2009-11-19 Ｔｇｒ５モジュレーターおよびその使用方法
JP2014088019A Withdrawn JP2014159456A (ja) 2008-11-19 2014-04-22 Ｔｇｒ５モジュレーターおよびその使用方法
JP2015160141A Pending JP2015232020A (ja) 2008-11-19 2015-08-14 Ｔｇｒ５モジュレーターおよびその使用方法
JP2017083045A Withdrawn JP2017132803A (ja) 2008-11-19 2017-04-19 Ｔｇｒ５モジュレーターおよびその使用方法
JP2018059922A Withdrawn JP2018100304A (ja) 2008-11-19 2018-03-27 Ｔｇｒ５モジュレーターおよびその使用方法

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JP2014088019A Withdrawn JP2014159456A (ja) 2008-11-19 2014-04-22 Ｔｇｒ５モジュレーターおよびその使用方法
JP2015160141A Pending JP2015232020A (ja) 2008-11-19 2015-08-14 Ｔｇｒ５モジュレーターおよびその使用方法
JP2017083045A Withdrawn JP2017132803A (ja) 2008-11-19 2017-04-19 Ｔｇｒ５モジュレーターおよびその使用方法
JP2018059922A Withdrawn JP2018100304A (ja) 2008-11-19 2018-03-27 Ｔｇｒ５モジュレーターおよびその使用方法

Country Status (23)

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US (5) US8114862B2 (OSRAM)
EP (2) EP2376519B1 (OSRAM)
JP (5) JP5535233B2 (OSRAM)
KR (2) KR101789960B1 (OSRAM)
CN (2) CN104370990A (OSRAM)
AU (1) AU2009316566B9 (OSRAM)
BR (1) BRPI0921983B8 (OSRAM)
CA (1) CA2744189C (OSRAM)
DK (2) DK2698375T3 (OSRAM)
EA (2) EA020140B1 (OSRAM)
ES (2) ES2458168T3 (OSRAM)
HK (1) HK1205132A1 (OSRAM)
HU (1) HUE039171T2 (OSRAM)
IL (3) IL212969A (OSRAM)
LT (1) LT2698375T (OSRAM)
MX (1) MX2011005295A (OSRAM)
NO (1) NO2698375T3 (OSRAM)
PL (2) PL2376519T3 (OSRAM)
PT (2) PT2698375T (OSRAM)
SG (1) SG10201400162QA (OSRAM)
SI (1) SI2698375T1 (OSRAM)
WO (1) WO2010059853A1 (OSRAM)
ZA (1) ZA201104077B (OSRAM)

Cited By (1)

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JP2014159456A (ja) * 2008-11-19 2014-09-04 Intercept Pharmaceuticals Inc Ｔｇｒ５モジュレーターおよびその使用方法

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US10987362B2 (en) 2004-03-12 2021-04-27 Intercept Pharmaceuticals, Inc. Treatment of fibrosis using FXR ligands
PT1734970E (pt) 2004-03-12 2015-03-11 Intercept Pharmaceuticals Inc Tratamento de fibrose utilizando ligandos de rfx
ITMI20050912A1 (it) 2005-05-19 2006-11-20 Erregierre Spa Processo di preparazione di acidi 3-a-ya(b)-diidrossi-6-a(b)-alchil-5b-colanici
CA2928178C (en) 2007-01-19 2019-09-10 Intercept Pharmaceuticals, Inc. Tgr5 modulators and methods of use thereof
EA020310B1 (ru) 2008-07-30 2014-10-30 Интерсепт Фармасьютикалз, Инк. Модуляторы рецептора tgr5 и их применение
CN102316872B (zh) 2008-11-26 2016-12-21 萨蒂奥根制药公司 治疗肥胖症和糖尿病的胆汁酸再循环抑制剂
EP2364161B1 (en) 2008-11-26 2020-03-11 Satiogen Pharmaceuticals, Inc. Compositions containing satiogens and methods of use
EP3593802A3 (en) 2010-05-26 2020-03-25 Satiogen Pharmaceuticals, Inc. Bile acid recycling inhibitors and satiogens for treatment of diabetes, obesity, and inflammatory gastrointestinal conditions
WO2013063526A1 (en) 2011-10-28 2013-05-02 Lumena Pharmaceuticals, Inc. Bile acid recycling inhibitors for treatment of hypercholemia and cholestatic liver disease
EA030839B1 (ru) 2011-10-28 2018-10-31 ЛУМЕНА ФАРМАСЬЮТИКАЛС ЭлЭлСи Ингибиторы рециклинга желчных кислот при лечении холестатических заболеваний печени у детей
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EP2906197A1 (en) 2012-10-09 2015-08-19 The Procter & Gamble Company Method of identifying synergistic cosmetic combinations
EP2906946A1 (en) 2012-10-09 2015-08-19 The Procter & Gamble Company Method of identifying or evaluating beneficial actives and compositions containing the same
WO2014195950A1 (en) * 2013-06-06 2014-12-11 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. Bile acid-basic amino acid conjugates and uses thereof
US20160151486A1 (en) 2013-06-13 2016-06-02 Fast Foward 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
KR102507624B1 (ko) 2013-11-22 2023-03-09 미나 테라퓨틱스 리미티드 Ｃ/ｅｂｐ 알파 짧은 활성화 ｒｎａ 조성물 및 사용 방법
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CA2966885A1 (en) * 2014-11-06 2016-05-12 Enanta Pharmaceuticals, Inc. Bile acid analogs an fxr/tgr5 agonists and methods of use thereof
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)
TWI686400B (zh) 2014-11-19 2020-03-01 英商Ｎｚｐ英國有限公司 化合物（二）
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