EA030681B1 - Модуляторы tgr5 и способы их применения - Google Patents

Модуляторы tgr5 и способы их применения Download PDF

Info

Publication number
EA030681B1
EA030681B1 EA201400258A EA201400258A EA030681B1 EA 030681 B1 EA030681 B1 EA 030681B1 EA 201400258 A EA201400258 A EA 201400258A EA 201400258 A EA201400258 A EA 201400258A EA 030681 B1 EA030681 B1 EA 030681B1
Authority
EA
Eurasian Patent Office
Prior art keywords
disease
compound
tgr5
compounds
cells
Prior art date
Application number
EA201400258A
Other languages
English (en)
Russian (ru)
Other versions
EA201400258A1 (ru
Inventor
Роберто Пелличьяри
Original Assignee
Интерсепт Фармасьютикалз, Инк.
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=EA030681(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Интерсепт Фармасьютикалз, Инк. filed Critical Интерсепт Фармасьютикалз, Инк.
Publication of EA201400258A1 publication Critical patent/EA201400258A1/ru
Publication of EA030681B1 publication Critical patent/EA030681B1/ru

Links

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
    • 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
    • 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
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • 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
    • A61P9/12—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

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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (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)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Vascular Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Hospice & Palliative Care (AREA)
  • Transplantation (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
EA201400258A 2008-11-19 2009-11-19 Модуляторы tgr5 и способы их применения EA030681B1 (ru)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP08169462 2008-11-19

Publications (2)

Publication Number Publication Date
EA201400258A1 EA201400258A1 (ru) 2015-02-27
EA030681B1 true EA030681B1 (ru) 2018-09-28

Family

ID=41668454

Family Applications (2)

Application Number Title Priority Date Filing Date
EA201400258A EA030681B1 (ru) 2008-11-19 2009-11-19 Модуляторы tgr5 и способы их применения
EA201170714A EA020140B1 (ru) 2008-11-19 2009-11-19 Модуляторы tgr5 и способы их применения

Family Applications After (1)

Application Number Title Priority Date Filing Date
EA201170714A EA020140B1 (ru) 2008-11-19 2009-11-19 Модуляторы tgr5 и способы их применения

Country Status (23)

Country Link
US (5) US8114862B2 (enExample)
EP (2) EP2376519B1 (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) EA030681B1 (enExample)
ES (2) ES2663948T3 (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) PL2698375T3 (enExample)
PT (2) PT2698375T (enExample)
SG (1) SG10201400162QA (enExample)
SI (1) SI2698375T1 (enExample)
WO (1) WO2010059853A1 (enExample)
ZA (1) ZA201104077B (enExample)

Families Citing this family (50)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE303399T1 (de) 2001-03-12 2005-09-15 Intercept Pharmaceuticals Inc Steroide als agonisten für fxr
DK2712617T3 (en) 2004-03-12 2017-02-13 Intercept Pharmaceuticals Inc Treatment of fibrosis with Fxr ligands.
US10987362B2 (en) 2004-03-12 2021-04-27 Intercept Pharmaceuticals, Inc. Treatment of fibrosis using FXR ligands
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
US8410083B2 (en) 2007-01-19 2013-04-02 Intercept Pharmaceuticals, Inc. 23-substituted bile acids as TGR5 modulators and methods of use thereof
CN102164940B (zh) 2008-07-30 2015-08-19 英特塞普特医药品公司 Tgr5调节剂及其使用方法
US8114862B2 (en) * 2008-11-19 2012-02-14 Intercept Pharmaceuticals, Inc. TGR5 modulators and methods of use thereof
WO2010062861A2 (en) 2008-11-26 2010-06-03 Satiogen Pharmaceuticals, Inc. Bile acid recycling inhibitors for treatment of obesity and diabetes
JP2012509892A (ja) * 2008-11-26 2012-04-26 サティオゲン ファーマシューティカルズ，インク． サティオゲン類を含有する組成物及び使用の方法
EP2995317A1 (en) 2010-05-26 2016-03-16 Satiogen Pharmaceuticals, Inc. Bile acid recycling inhibitors and satiogens for treatment of diabetes, obesity, and inflammatory gastrointestinal conditions
DK2771003T3 (en) 2011-10-28 2017-07-17 Lumena Pharmaceuticals Llc Bile acid recycling inhibitors for the treatment of pediatric cholestatic liver disease
US20140323412A1 (en) 2011-10-28 2014-10-30 Lumena Pharmaceuticals, 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
SI3336097T1 (sl) 2012-06-19 2021-07-30 Intercept Pharmaceuticals, Inc. Priprava nekristalinične oblike obetiholne kisline
WO2014059008A1 (en) 2012-10-09 2014-04-17 The Procter & Gamble Company Method of identifying or evaluating beneficial actives and compositions containing the same
CN104703585A (zh) 2012-10-09 2015-06-10 宝洁公司 鉴定协同化妆品组合的方法
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.
DK3071696T3 (da) 2013-11-22 2019-10-07 Mina Therapeutics Ltd C/ebp alfa kort aktiverings-rna-sammensætninger og fremgangsmåder til anvendelse
ES2768718T3 (es) * 2014-05-29 2020-06-23 Bar Pharmaceuticals S R L Derivados de colano para su uso en el tratamiento y/o prevención de enfermedades mediadas por FXR y TGR5/GPBAR1
US20180236064A1 (en) * 2014-10-03 2018-08-23 Mayo Foundation For Medical Education And Research Targeting tgr5 to treat disease
MX2017005935A (es) * 2014-11-06 2018-01-11 Enanta Pharm Inc Análogos de ácido biliar como agonistas fxr/tgr5 y métodos de uso de los mismos.
CA2968310A1 (en) 2014-11-19 2016-05-26 NZP UK Limited 6.alpha.-alkyl-6,7-dione steroids as intermediates for the production of steroidal fxr modulators
US10301350B2 (en) 2014-11-19 2019-05-28 NZP UK Limited 6-alkyl-7-hydroxy-4-en-3-one steroids as intermediates for the production of steroidal FXR modulators
TWI686400B (zh) 2014-11-19 2020-03-01 英商Ｎｚｐ英國有限公司 化合物（二）
MX375865B (es) 2014-11-19 2025-03-07 Nzp Uk Ltd Esteroides de 6.alfa-alquil-3,7-diona como intermedios para la produccion de moduladores esteroideos del receptor x farnesoide (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
WO2016173397A1 (zh) * 2015-04-28 2016-11-03 上海翰森生物医药科技有限公司 胆酸衍生物及其制备方法和医药用途
DK3310801T3 (da) 2015-06-19 2021-06-21 Intercept Pharmaceuticals Inc Tgr5-modulatorer og fremgangsmåder til anvendelse deraf
PT3310801T (pt) * 2015-06-24 2021-06-18 Intercept Pharmaceuticals Inc Moduladores de tgr5 e métodos de utilização dos mesmos
CN108350020A (zh) * 2015-09-24 2018-07-31 英特塞普特医药品公司 用于制备胆汁酸衍生物的方法和中间体
AR106293A1 (es) * 2015-10-07 2018-01-03 Intercept Pharmaceuticals Inc Moduladores del receptor x farnesoide
CN109467585A (zh) * 2016-03-11 2019-03-15 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
EP3442946A4 (en) 2016-04-13 2019-12-04 Intercept Pharmaceuticals, Inc. METHOD FOR THE TREATMENT OF CANCER
GB201608777D0 (en) 2016-05-18 2016-06-29 Dextra Lab Ltd Compounds
JP7036805B2 (ja) 2016-05-29 2022-03-15 深▲じぇん▼市▲絵▼云生物科技有限公司 肝疾患関連バイオマーカーおよびその使用方法
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
WO2019023103A1 (en) 2017-07-24 2019-01-31 Intercept Pharmaceuticals, Inc. BILIARY ACID DERIVATIVES WITH ISOTOPIC MARKING
CA3075205A1 (en) 2017-09-08 2019-03-14 Mina Therapeutics Limited Stabilized hnf4a sarna compositions and methods of use
GB201812382D0 (en) 2018-07-30 2018-09-12 Nzp Uk Ltd Compounds
US20220096495A1 (en) * 2019-02-04 2022-03-31 Intercept Pharmaceuticals, Inc. Treatment and prevention of intestinal inflammatory 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
PH12022550852A1 (en) 2019-10-07 2023-05-03 Kallyope Inc Gpr119 agonists
KR20220149558A (ko) 2020-02-28 2022-11-08 칼리오페, 인크. Gpr40 작용제
EP4153589A4 (en) 2020-05-19 2024-06-12 Kallyope, Inc. AMPK ACTIVATORS
CN116390925A (zh) 2020-06-26 2023-07-04 卡尔优普公司 Ampk活化剂
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

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0186023A2 (en) * 1984-12-21 1986-07-02 Lehner A.G. Biliary acid derivatives, process for their preparation and pharmaceutical compositions containing them
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
WO2008091540A2 (en) * 2007-01-19 2008-07-31 Intercept Pharmaceuticals, Inc. 23-substituted bile acids as tgr5 modulators and methods of use thereof

Family Cites Families (48)

* 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.
IT1223313B (it) 1987-10-20 1990-09-19 Gipharmex Spa Derivati 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
IT1229570B (it) 1989-04-17 1991-09-04 Giuliani Spa Derivati fluorurati di acidi biliari, loro preparazione e composizioni farmaceutiche che li contengono.
US5055477A (en) 1989-12-13 1991-10-08 Mitsubishi Kasei Corporation Pyrazolyl acrylic acid derivatives, useful as systemic fungicides for plant and material protection
AU1856997A (en) 1996-02-02 1997-08-22 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
CA2260044A1 (en) 1996-07-12 1998-01-22 Stephen Alistair Smith Novel treatment of leptine resistance
US6008237A (en) 1997-12-19 1999-12-28 Merck & Co., Inc. Arylthiazolidinedione derivatives
CA2318731C (en) 1998-01-29 2012-05-29 Tularik Inc. Ppar-gamma modulators
JP2002528721A (ja) 1998-10-23 2002-09-03 グラクソ グループ リミテッド 核内受容体のリガンド用のアッセイ
ATE433106T1 (de) 1998-12-23 2009-06-15 Glaxo Group Ltd Bestimmungsmethode fur liganden der nuklearen rezeptoren
WO2000040965A1 (en) 1999-01-07 2000-07-13 Tularik, Inc. Fxr receptor-mediated modulation of cholesterol metabolism
EP1165135B1 (en) 1999-03-26 2004-09-01 City of Hope Methods of screening for compounds modulating fxr receptors
EP1473042B1 (en) 1999-03-26 2006-06-21 City of Hope Screening for FXR receptor modulators
US20020132223A1 (en) 1999-03-26 2002-09-19 City Of Hope Methods for modulating activity of the FXR nuclear receptor
DE60023493T2 (de) 1999-06-11 2006-07-20 Allergan, Inc., Irvine Verwendung von synthetischen FXR Liganden zur Behandlung von Krankheiten die mit einem gestörten Gleichgewicht des Cholesterin-Spiegels verbunden sind und von Kolonkrebs
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
AU1215701A (en) 1999-10-22 2001-05-08 Merck & Co., Inc. Pharmaceuticals for treating obesity
CA2401290A1 (en) 2000-04-12 2001-10-18 Takeda Chemical Industries, Ltd. Novel g protein-coupled receptor protein and dna thereof
US6627636B2 (en) 2000-06-15 2003-09-30 Bristol-Myers Squibb Company HMG-CoA reductase inhibitors and method
WO2002020463A2 (en) 2000-09-05 2002-03-14 Tularik Inc. Fxr modulators
US20020119958A1 (en) 2001-02-13 2002-08-29 Shinichiro Tojo Therapeutic agent for hyperlipidemia
ATE303399T1 (de) 2001-03-12 2005-09-15 Intercept Pharmaceuticals Inc Steroide als agonisten für 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
US20070010562A1 (en) 2001-08-13 2007-01-11 Ulrike Bauer 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
WO2003080803A2 (en) 2002-03-21 2003-10-02 Smithkline Beecham Corporation Methods of using farnesoid x receptor (fxr) agonists
CA2482195A1 (en) 2002-04-12 2003-10-23 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
AU2003244312B2 (en) 2002-06-19 2008-07-03 Availvs Corporation Artificial stone wall material
ITMI20021532A1 (it) 2002-07-12 2004-01-12 Roberto Pellicciari Composti chimici
JP2006515838A (ja) 2002-11-22 2006-06-08 スミスクライン ビーチャム コーポレーション ファルネソイドｘ受容体アゴニスト
EP1591120A4 (en) 2003-01-28 2009-06-10 Takeda Chemical Industries Ltd RECEPTOR AGONISTS
EP1696910A4 (en) 2003-09-26 2009-12-09 Smithkline Beecham Corp COMPOSITIONS AND METHOD FOR THE TREATMENT OF FIBROSIS
EP1568706A1 (en) 2004-02-26 2005-08-31 Intercept Pharmaceuticals, Inc. Novel steroid agonist for FXR
DK2712617T3 (en) 2004-03-12 2017-02-13 Intercept Pharmaceuticals Inc Treatment of fibrosis with Fxr ligands.
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
US8114862B2 (en) * 2008-11-19 2012-02-14 Intercept Pharmaceuticals, Inc. TGR5 modulators and methods of use thereof

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
EP0186023A2 (en) * 1984-12-21 1986-07-02 Lehner A.G. Biliary acid derivatives, process for their preparation and pharmaceutical compositions containing them
WO2008091540A2 (en) * 2007-01-19 2008-07-31 Intercept Pharmaceuticals, Inc. 23-substituted bile acids as tgr5 modulators and methods of use thereof

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
SATO Hiroyuki el al., Novel Potent and Selective Bile Acid Derivatives as TGR5 Agonists:Biological Screening, Structure-Activity Relationships, and Molecular Modeling Studies. Journal of Medicinal Chemistry, 2008, 51 (6), p. 1831-1841, (реферат) [он-лайн] CAS(STN), 148:441185, RN 951694-85-2 *

Also Published As

Publication number Publication date
EA020140B1 (ru) 2014-08-29
AU2009316566B2 (en) 2014-04-17
IL212969A (en) 2016-04-21
JP2015232020A (ja) 2015-12-24
PL2698375T3 (pl) 2018-08-31
AU2009316566A1 (en) 2010-05-27
HK1166327A1 (en) 2012-10-26
PT2376519E (pt) 2014-02-20
HUE039171T2 (hu) 2018-12-28
IL264796B (en) 2020-11-30
ZA201104077B (en) 2012-02-29
EP2698375B1 (en) 2018-02-21
US20210269473A1 (en) 2021-09-02
SI2698375T1 (sl) 2018-10-30
IL244812A0 (en) 2016-05-31
BRPI0921983A2 (pt) 2018-07-10
CN102325784B (zh) 2014-11-19
CN104370990A (zh) 2015-02-25
KR20110086177A (ko) 2011-07-27
CA2744189A1 (en) 2010-05-27
LT2698375T (lt) 2018-07-10
US20100152151A1 (en) 2010-06-17
US20120115832A1 (en) 2012-05-10
JP2012509348A (ja) 2012-04-19
IL212969A0 (en) 2011-07-31
MX2011005295A (es) 2011-06-24
EP2698375A3 (en) 2014-03-12
KR101667436B1 (ko) 2016-10-18
WO2010059853A1 (en) 2010-05-27
JP2014159456A (ja) 2014-09-04
CN102325784A (zh) 2012-01-18
CA2744189C (en) 2016-10-11
BRPI0921983B1 (pt) 2021-04-20
US20140100209A1 (en) 2014-04-10
EA201170714A1 (ru) 2012-01-30
PT2698375T (pt) 2018-05-25
US20180016295A1 (en) 2018-01-18
IL244812B (en) 2019-03-31
KR20160122272A (ko) 2016-10-21
KR101789960B1 (ko) 2017-10-25
US8445472B2 (en) 2013-05-21
JP5535233B2 (ja) 2014-07-02
BRPI0921983B8 (pt) 2021-05-25
EP2376519A1 (en) 2011-10-19
EP2376519B1 (en) 2013-11-13
JP2018100304A (ja) 2018-06-28
NO2698375T3 (enExample) 2018-07-21
PL2376519T3 (pl) 2014-04-30
ES2458168T3 (es) 2014-04-30
ES2663948T3 (es) 2018-04-17
EP2698375A2 (en) 2014-02-19
JP2017132803A (ja) 2017-08-03
DK2376519T3 (da) 2014-02-03
US8114862B2 (en) 2012-02-14
DK2698375T3 (en) 2018-05-28
AU2009316566B9 (en) 2014-05-15
AU2009316566A2 (en) 2011-07-14
HK1205132A1 (en) 2015-12-11
EA201400258A1 (ru) 2015-02-27
US9650409B2 (en) 2017-05-16
SG10201400162QA (en) 2014-05-29

Similar Documents

Publication Publication Date Title
EA030681B1 (ru) Модуляторы tgr5 и способы их применения
CN102282157B (zh) G蛋白偶联受体5(tgr5)调节剂及其使用方法
US9540414B2 (en) TGR5 modulators and methods of use thereof
AU2014204505B2 (en) TGR5 Modulators and Method of Use Thereof

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): MD