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

Info

Publication number
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
Authority
JP
Japan
Prior art keywords
compound
hydrogen
tgr5
methyl
acid
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
JP2011537624A
Other languages
English (en)
Japanese (ja)
Other versions
JP2012509348A5 (enExample
JP2012509348A (ja
Inventor
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
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=41668454&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=JP5535233(B2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by 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 filed Critical 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
Publication of JP2012509348A publication Critical patent/JP2012509348A/ja
Publication of JP2012509348A5 publication Critical patent/JP2012509348A5/ja
Application granted granted Critical
Publication of JP5535233B2 publication Critical patent/JP5535233B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/575Compounds 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
    • 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
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • 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
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • 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
    • A61P3/04Anorexiants; Antiobesity agents
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • 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
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J31/00Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J31/00Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/006Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Pulmonology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Emergency Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Transplantation (AREA)
  • Vascular Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Hospice & Palliative Care (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 2008-11-19
EP08169462.2 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)

Application Number Title Priority Date Filing Date
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)

Publication Number Publication Date
JP2012509348A JP2012509348A (ja) 2012-04-19
JP2012509348A5 JP2012509348A5 (enExample) 2012-12-13
JP5535233B2 true JP5535233B2 (ja) 2014-07-02

Family

ID=41668454

Family Applications (5)

Application Number Title Priority Date Filing Date
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

Family Applications After (4)

Application Number Title Priority Date Filing Date
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)

Country Link
US (5) US8114862B2 (enExample)
EP (2) EP2698375B1 (enExample)
JP (5) JP5535233B2 (enExample)
KR (2) KR101667436B1 (enExample)
CN (2) CN104370990A (enExample)
AU (1) AU2009316566B9 (enExample)
BR (1) BRPI0921983B8 (enExample)
CA (1) CA2744189C (enExample)
DK (2) DK2376519T3 (enExample)
EA (2) EA020140B1 (enExample)
ES (2) ES2458168T3 (enExample)
HK (1) HK1205132A1 (enExample)
HU (1) HUE039171T2 (enExample)
IL (3) IL212969A (enExample)
LT (1) LT2698375T (enExample)
MX (1) MX2011005295A (enExample)
NO (1) NO2698375T3 (enExample)
PL (2) PL2376519T3 (enExample)
PT (2) PT2376519E (enExample)
SG (1) SG10201400162QA (enExample)
SI (1) SI2698375T1 (enExample)
WO (1) WO2010059853A1 (enExample)
ZA (1) ZA201104077B (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Families Citing this family (49)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1392714B1 (en) 2001-03-12 2005-08-31 Intercept Pharmaceuticals, Inc. Steroids as agonists for fxr
US10987362B2 (en) 2004-03-12 2021-04-27 Intercept Pharmaceuticals, Inc. Treatment of fibrosis using FXR ligands
ES2533993T3 (es) 2004-03-12 2015-04-16 Intercept Pharmaceuticals, Inc. Tratamiento de fibrosis usando ligandos de FXR
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
CN101679476B (zh) 2007-01-19 2014-05-07 英特塞普特医药品公司 23取代的胆汁酸作为tgr5调节剂及其使用方法
EP2324046B1 (en) 2008-07-30 2014-09-03 Intercept Pharmaceuticals, Inc. Tgr5 modulators and methods of use thereof
US9339480B2 (en) 2008-11-26 2016-05-17 Satiogen Pharmaceuticals, Inc. Bile acid recycling inhibitors for treatment of obesity and diabetes
CN102316889B (zh) 2008-11-26 2014-11-26 萨蒂奥根制药公司 组合物及使用方法
US20110294767A1 (en) 2010-05-26 2011-12-01 Satiogen Pharmaceuticals, Inc. Bile acid recycling inhibitors and satiogens for treatment of diabetes, obesity, and inflammatory gastrointestinal conditions
ES2633766T3 (es) 2011-10-28 2017-09-25 Lumena Pharmaceuticals Llc Inhibidores de reciclaje de ácido biliar para el tratamiento de enfermedades de hígado colestático pediátrico
AU2012328453B2 (en) 2011-10-28 2017-05-04 Shire Human Genetic Therapies, Inc. Bile acid recycling inhibitors for treatment of hypercholemia and cholestatic liver disease
US9982008B2 (en) 2012-06-19 2018-05-29 Intercept Pharmaceuticals, Inc. Preparation and uses of obeticholic acid
NZ734451A (en) 2012-06-19 2018-12-21 Intercept Pharmaceuticals Inc Preparation, uses and solid forms of obeticholic acid
US9726663B2 (en) 2012-10-09 2017-08-08 The Procter & Gamble Company Method of identifying or evaluating synergistic combinations of actives and compositions containing the same
CN104704362B (zh) 2012-10-09 2018-08-28 宝洁公司 鉴定或评估有益活性物质的方法以及包含其的组合物
EP3004132A4 (en) 2013-06-06 2017-01-18 Yissum, Research Development Company of the Hebrew Bile acid-basic amino acid conjugates and uses thereof
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.
EP3985118A1 (en) 2013-11-22 2022-04-20 MiNA Therapeutics Limited C/ebp alpha short activating rna compositions and methods of use
MX388957B (es) * 2014-05-29 2025-03-20 Bar Pharmaceuticals S R L Derivados del colano para uso en el tratamiento y/o prevencion de enfermedades en las que intervienen el fxr y el tgr5/gpbar1
WO2016054208A1 (en) * 2014-10-03 2016-04-07 Mayo Foundation For Medical Education And Research Targeting tgr5 to treat disease
CA2966885A1 (en) * 2014-11-06 2016-05-12 Enanta Pharmaceuticals, Inc. Bile acid analogs an fxr/tgr5 agonists and methods of use thereof
MX381239B (es) 2014-11-19 2025-03-12 Nzp Uk Ltd Esteroides de 6.alfa.-alquil-6,7-diona como intermedios para la producción de moduladores esteroideos del receptor x farnesoide (fxr).
JP6724004B2 (ja) 2014-11-19 2020-07-15 エヌゼットピー ユーケー リミテッド ステロイドFXRモジュレーター製造のための中間体としての5β−6−アルキル−7−ヒドロキシ−3−オンステロイド
EA033427B1 (ru) 2014-11-19 2019-10-31 Nzp Uk Ltd 6-алкил-7-гидрокси-4-ен-3-оновые стероиды в качестве промежуточных соединений для получения стероидных модуляторов fxr
EA034739B1 (ru) 2014-11-19 2020-03-16 ЭнЗедПи ЮКей ЛИМИТЕД 6-альфа-алкил-3,7-дионовые стероиды в качестве промежуточных соединений для получения стероидных модуляторов fxr
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
EP3290429A1 (en) * 2015-04-28 2018-03-07 Jiangsu Hansoh Pharmaceutical Group Co., Ltd. Cholic acid derivative, and preparation method and medical use thereof
US10800807B2 (en) * 2015-06-19 2020-10-13 Intercept Pharmaceuticals, Inc. TGR5 modulators and methods of use thereof
CN107771180B (zh) * 2015-06-19 2021-03-23 英特塞普特医药品公司 Tgr5调节剂及其使用方法
JP2018528230A (ja) * 2015-09-24 2018-09-27 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 胆汁酸誘導体の調製のための方法および中間体
TW201718621A (zh) * 2015-10-07 2017-06-01 英特賽普醫藥品公司 法尼醇x受體調節劑
CN106008639B (zh) * 2016-03-11 2019-01-08 深圳市塔吉瑞生物医药有限公司 用于预防或治疗fxr-介导疾病的胆烷酸化合物
CA3020698A1 (en) 2016-04-13 2017-10-19 Intercept Pharmaceuticals, Inc. Methods of treating or preventing hepatocellular carcinoma
GB201608777D0 (en) 2016-05-18 2016-06-29 Dextra Lab Ltd Compounds
CN108990420B (zh) 2016-05-29 2022-06-24 深圳市绘云生物科技有限公司 肝病相关生物标志物和其使用方法
WO2018005794A2 (en) * 2016-07-01 2018-01-04 Venenum Biodesign Llc Novel non-systemic tgr5 agonists
WO2018222701A1 (en) * 2017-05-30 2018-12-06 Intercept Pharmaceuticals, Inc. Treatment of renal diseases with a bile acid derivative
CN109021056B (zh) * 2017-06-09 2021-03-09 博瑞生物医药(苏州)股份有限公司 法尼酯x受体激动剂
JP2020528892A (ja) 2017-07-24 2020-10-01 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 同位体標識化胆汁酸誘導体
AU2018330494A1 (en) 2017-09-08 2020-03-26 Mina Therapeutics Limited HNF4a saRNA compositions and methods of use
GB201812382D0 (en) 2018-07-30 2018-09-12 Nzp Uk Ltd Compounds
EP3920937A4 (en) * 2019-02-04 2022-11-02 Intercept Pharmaceuticals, Inc. TREATMENT AND PREVENTION OF INFLAMATORY BOWEL DISEASES WITH A BILE ACID DERIVATIVE
CN116925168A (zh) * 2019-08-23 2023-10-24 深圳云合医药科技合伙企业(有限合伙) 胆汁酸衍生物及其组合物和应用
JP2022552655A (ja) 2019-10-07 2022-12-19 キャリーオペ,インク. Gpr119アゴニスト
TW202140440A (zh) 2020-02-28 2021-11-01 美商克力歐普股份有限公司 Gpr40激動劑
AU2021275038A1 (en) 2020-05-19 2022-12-22 Kallyope, Inc. AMPK activators
CA3183575A1 (en) 2020-06-26 2021-12-30 Iyassu Sebhat Ampk activators
KR102693566B1 (ko) * 2020-07-03 2024-08-08 주식회사 큐라클 지방간 질환의 예방 또는 치료를 위한 약학적 조성물
CN113774142A (zh) * 2021-10-11 2021-12-10 北京化工大学 Tgr5在制备治疗肠癌药物及诊断性试剂盒中的应用

Family Cites Families (51)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3366932D1 (en) 1982-07-29 1986-11-20 Lehner Ag New derivatives of biliary acids, process for the production thereof and pharmaceutical compositions containing the same
IT1206112B (it) 1983-04-29 1989-04-14 Lehner Ag Nuovi derivati di acidi biliari, procedimento per la loro preparazione e relative composizioni farmaceutiche.
IT1212835B (it) 1983-08-18 1989-11-30 Lehner Ag Derivati di acidi biliari, procedimento per la loro preparazione e relative composizioni farmaceutiche.
US4892868A (en) * 1984-08-17 1990-01-09 Gipharmex, S.P.A. Derivatives of biliary acids, process for the production thereof and corresponding pharmaceutical compositions
IT1196377B (it) 1984-12-21 1988-11-16 Lehner Ag Derivati di acidi biliari,procedimento per la loro preparazione e relative composizioni farmaceutiche
IT1223313B (it) * 1987-10-20 1990-09-19 Gipharmex Spa Derivati di acidi biliari loro preparazione e composizioni farmaceutiche che li contengono
IT1229570B (it) 1989-04-17 1991-09-04 Giuliani Spa Derivati fluorurati di acidi biliari, loro preparazione e composizioni farmaceutiche che li contengono.
US5175320A (en) * 1989-04-17 1992-12-29 Giuliani S.P.A. Fluorinated bile acid derivatives, processes for the preparation thereof and pharmaceutical compositions containing them
ATE121080T1 (de) * 1989-12-13 1995-04-15 Mitsubishi Chem Corp Pyrazolylacrylsäure-derivate, verwendbar als systemische fungiziden in pflanzen- und materialschutz.
WO1997028149A1 (en) 1996-02-02 1997-08-07 Merck & Co., Inc. Method for raising hdl cholesterol levels
GB9604242D0 (en) 1996-02-28 1996-05-01 Glaxo Wellcome Inc Chemical compounds
GB9606805D0 (en) 1996-03-30 1996-06-05 Glaxo Wellcome Inc Medicaments
US5689791A (en) 1996-07-01 1997-11-18 Xerox Corporation Electrically conductive fibers
EP0921798A1 (en) 1996-07-12 1999-06-16 Smithkline Beecham Plc Novel treatment of leptine resistance
US6008237A (en) * 1997-12-19 1999-12-28 Merck & Co., Inc. Arylthiazolidinedione derivatives
US6200995B1 (en) 1998-01-29 2001-03-13 Tularik Inc. PPAR-γ modulators
WO2000025134A1 (en) 1998-10-23 2000-05-04 Glaxo Group Limited Assays for ligands for nuclear receptors
JP2002532729A (ja) 1998-12-23 2002-10-02 グラクソ グループ リミテッド 核内受容体のリガンドのアッセイ
WO2000040965A1 (en) 1999-01-07 2000-07-13 Tularik, Inc. Fxr receptor-mediated modulation of cholesterol metabolism
AU780658B2 (en) 1999-03-26 2005-04-07 City Of Hope Method of affecting cholesterol catabolism using nuclear bile acid receptor
US20020132223A1 (en) 1999-03-26 2002-09-19 City Of Hope Methods for modulating activity of the FXR nuclear receptor
EP1473042B1 (en) 1999-03-26 2006-06-21 City of Hope Screening for FXR receptor modulators
EP1185277B1 (en) 1999-06-11 2005-10-26 Allergan, Inc. Use of FXR synthetic ligands for the treatment of diseseas linked to cholesterol imbalance and colon cancer
US6906057B1 (en) * 1999-06-11 2005-06-14 Allergan, Inc. Methods for modulating FXR receptor activity
US6559188B1 (en) * 1999-09-17 2003-05-06 Novartis Ag Method of treating metabolic disorders especially diabetes, or a disease or condition associated with diabetes
WO2001030343A1 (en) 1999-10-22 2001-05-03 Merck & Co., Inc. Pharmaceuticals for treating obesity
EP1273659A4 (en) 2000-04-12 2004-04-21 Takeda Chemical Industries Ltd G-PROTEIN COUPLED RECEPTOR PROTEIN AND ITS DNA
US6627636B2 (en) * 2000-06-15 2003-09-30 Bristol-Myers Squibb Company HMG-CoA reductase inhibitors and method
US6777446B2 (en) * 2000-09-05 2004-08-17 Tularik, Inc. FXR modulators
US20020119958A1 (en) 2001-02-13 2002-08-29 Shinichiro Tojo Therapeutic agent for hyperlipidemia
EP1392714B1 (en) * 2001-03-12 2005-08-31 Intercept Pharmaceuticals, Inc. Steroids as agonists for fxr
US7354726B2 (en) 2001-04-12 2008-04-08 Takeda Pharmaceutical Company Limited Screening method
EP1285914B1 (en) 2001-08-13 2007-12-19 PheneX Pharmaceuticals AG Nr1h4 nuclear receptor binding compounds
WO2003016280A1 (en) 2001-08-13 2003-02-27 Lion Bioscience Ag Nr1h4 nuclear receptor binding compounds
WO2003015777A1 (en) 2001-08-13 2003-02-27 Lion Bioscience Ag Nr1h4 nuclear receptor binding compounds
US20030144360A1 (en) 2001-11-19 2003-07-31 Allergan Sales, Inc. Composition and method for modulating BAR/FXR receptor activity
US20050107475A1 (en) 2002-03-21 2005-05-19 Jones Stacey A. Methods of using farnesoid x receptor (frx) agonists
EP1494533A2 (en) 2002-04-12 2005-01-12 The University of Chicago Farnesoid x-activated receptor agonists
US6987121B2 (en) 2002-04-25 2006-01-17 Smithkline Beecham Corporation Compositions and methods for hepatoprotection and treatment of cholestasis
WO2004000752A1 (ja) 2002-06-19 2003-12-31 Availvs Corporation 人造石壁材
ITMI20021532A1 (it) 2002-07-12 2004-01-12 Roberto Pellicciari Composti chimici
AU2003290700A1 (en) 2002-11-22 2004-06-18 Smithkline Beecham Corporation Farnesoid x receptor agonists
EP1591120A4 (en) 2003-01-28 2009-06-10 Takeda Chemical Industries Ltd RECEPTOR AGONISTS
WO2005032549A1 (en) 2003-09-26 2005-04-14 Smithkline Beecham Corporation Compositions and methods for treatment of fibrosis
EP1568706A1 (en) 2004-02-26 2005-08-31 Intercept Pharmaceuticals, Inc. Novel steroid agonist for FXR
ES2533993T3 (es) 2004-03-12 2015-04-16 Intercept Pharmaceuticals, Inc. Tratamiento de fibrosis usando ligandos de FXR
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
SI2040713T1 (sl) 2006-06-27 2014-11-28 Intercept Pharmaceuticals, Inc. Derivati žolčne kisline kot FXR ligandi za preprečevanje ali zdravljenje bolezni ali stanj, posredovanih s FXR
EP1947108A1 (en) 2007-01-19 2008-07-23 Intercept Pharmaceuticals, Inc. TGR5 modulators and methods of use thereof
CN101679476B (zh) * 2007-01-19 2014-05-07 英特塞普特医药品公司 23取代的胆汁酸作为tgr5调节剂及其使用方法
CN104370990A (zh) * 2008-11-19 2015-02-25 英特塞普特医药品公司 G蛋白偶联受体5(tgr5)调节剂及其使用方法

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
JP2017132803A (ja) * 2008-11-19 2017-08-03 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 Tgr5モジュレーターおよびその使用方法

Also Published As

Publication number Publication date
US20180016295A1 (en) 2018-01-18
KR20160122272A (ko) 2016-10-21
LT2698375T (lt) 2018-07-10
AU2009316566B2 (en) 2014-04-17
US20120115832A1 (en) 2012-05-10
JP2018100304A (ja) 2018-06-28
KR101789960B1 (ko) 2017-10-25
US20210269473A1 (en) 2021-09-02
HK1205132A1 (en) 2015-12-11
CN104370990A (zh) 2015-02-25
US9650409B2 (en) 2017-05-16
JP2012509348A (ja) 2012-04-19
HK1166327A1 (en) 2012-10-26
PL2376519T3 (pl) 2014-04-30
IL212969A0 (en) 2011-07-31
ES2458168T3 (es) 2014-04-30
EP2698375B1 (en) 2018-02-21
KR101667436B1 (ko) 2016-10-18
US8445472B2 (en) 2013-05-21
CN102325784A (zh) 2012-01-18
IL264796B (en) 2020-11-30
BRPI0921983A2 (pt) 2018-07-10
IL244812A0 (en) 2016-05-31
PT2376519E (pt) 2014-02-20
IL244812B (en) 2019-03-31
CA2744189A1 (en) 2010-05-27
AU2009316566A1 (en) 2010-05-27
KR20110086177A (ko) 2011-07-27
PL2698375T3 (pl) 2018-08-31
AU2009316566B9 (en) 2014-05-15
DK2698375T3 (en) 2018-05-28
WO2010059853A1 (en) 2010-05-27
JP2014159456A (ja) 2014-09-04
JP2017132803A (ja) 2017-08-03
HUE039171T2 (hu) 2018-12-28
EP2376519A1 (en) 2011-10-19
US20140100209A1 (en) 2014-04-10
PT2698375T (pt) 2018-05-25
DK2376519T3 (da) 2014-02-03
SG10201400162QA (en) 2014-05-29
BRPI0921983B1 (pt) 2021-04-20
EP2376519B1 (en) 2013-11-13
IL212969A (en) 2016-04-21
AU2009316566A2 (en) 2011-07-14
EP2698375A3 (en) 2014-03-12
JP2015232020A (ja) 2015-12-24
EA201400258A1 (ru) 2015-02-27
CA2744189C (en) 2016-10-11
BRPI0921983B8 (pt) 2021-05-25
EA030681B1 (ru) 2018-09-28
EA020140B1 (ru) 2014-08-29
SI2698375T1 (sl) 2018-10-30
EP2698375A2 (en) 2014-02-19
US20100152151A1 (en) 2010-06-17
EA201170714A1 (ru) 2012-01-30
ZA201104077B (en) 2012-02-29
MX2011005295A (es) 2011-06-24
NO2698375T3 (enExample) 2018-07-21
CN102325784B (zh) 2014-11-19
ES2663948T3 (es) 2018-04-17
US8114862B2 (en) 2012-02-14

Similar Documents

Publication Publication Date Title
JP5535233B2 (ja) Tgr5モジュレーターおよびその使用方法
JP5639073B2 (ja) Tgr5モジュレーターおよびその使用方法
AU2014204505B2 (en) TGR5 Modulators and Method of Use Thereof

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20121024

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20121024

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20140325

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20140422

R150 Certificate of patent or registration of utility model

Ref document number: 5535233

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

LAPS Cancellation because of no payment of annual fees