CA2744135C - Tgr5 modulators and methods of use thereof - Google Patents

Tgr5 modulators and methods of use thereof Download PDF

Info

Publication number
CA2744135C
CA2744135C CA2744135A CA2744135A CA2744135C CA 2744135 C CA2744135 C CA 2744135C CA 2744135 A CA2744135 A CA 2744135A CA 2744135 A CA2744135 A CA 2744135A CA 2744135 C CA2744135 C CA 2744135C
Authority
CA
Canada
Prior art keywords
compound
disease
salt
solvate
hydrate
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.)
Active
Application number
CA2744135A
Other languages
English (en)
French (fr)
Other versions
CA2744135A1 (en
Inventor
Roberto Pellicciari
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Intercept Pharmaceuticals Inc
Original Assignee
Intercept Pharmaceuticals Inc
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=41666760&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CA2744135(C) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Intercept Pharmaceuticals Inc filed Critical Intercept Pharmaceuticals Inc
Publication of CA2744135A1 publication Critical patent/CA2744135A1/en
Application granted granted Critical
Publication of CA2744135C publication Critical patent/CA2744135C/en
Active 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Transplantation (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
CA2744135A 2008-11-19 2009-11-19 Tgr5 modulators and methods of use thereof Active CA2744135C (en)

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 (2)

Publication Number Publication Date
CA2744135A1 CA2744135A1 (en) 2010-05-27
CA2744135C true CA2744135C (en) 2017-07-04

Family

ID=41666760

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2744135A Active CA2744135C (en) 2008-11-19 2009-11-19 Tgr5 modulators and methods of use thereof

Country Status (10)

Country Link
US (1) US8999964B2 (OSRAM)
EP (2) EP3150620B1 (OSRAM)
JP (1) JP5639073B2 (OSRAM)
CN (2) CN102282157B (OSRAM)
AU (1) AU2009316484B2 (OSRAM)
BR (1) BRPI0921992B1 (OSRAM)
CA (1) CA2744135C (OSRAM)
ES (2) ES2592452T3 (OSRAM)
IL (1) IL212970A (OSRAM)
WO (1) WO2010059859A1 (OSRAM)

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2566860B1 (en) 2010-05-06 2014-09-10 Bristol-Myers Squibb Company Bicyclic heteroaryl compounds as gpr119 modulators
US9062028B2 (en) 2011-04-28 2015-06-23 Bristol-Myers Squibb Company Bicyclic nitrogen containing heteroaryl TGR5 receptor modulators
WO2014066819A1 (en) * 2012-10-26 2014-05-01 Intercept Pharmaceuticals, Inc. Process for preparing bile acid derivatives
KR102106186B1 (ko) * 2012-11-28 2020-05-04 인터셉트 파마슈티컬즈, 인크. 폐 질환의 치료
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
ES2938874T3 (es) 2014-05-29 2023-04-17 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
EA033603B1 (ru) * 2014-11-19 2019-11-08 Nzp Uk Ltd 6-альфа-алкил-6,7-дионовые стероиды в качестве промежуточных соединений для получения стероидных модуляторов fxr
TWI686400B (zh) * 2014-11-19 2020-03-01 英商Nzp英國有限公司 化合物(二)
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)
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
HK1244708A1 (zh) * 2014-11-26 2018-08-17 英安塔制药有限公司 作爲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
ES2873088T3 (es) * 2015-06-19 2021-11-03 Intercept Pharmaceuticals Inc Moduladores de TGR5 y métodos para su uso
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
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
JP2022552655A (ja) 2019-10-07 2022-12-19 キャリーオペ,インク. Gpr119アゴニスト
PH12022552277A1 (en) 2020-02-28 2024-03-04 Kallyope Inc Gpr40 agonists
CA3178994A1 (en) 2020-05-19 2021-11-25 Iyassu Sebhat Ampk activators
JP2023531726A (ja) 2020-06-26 2023-07-25 キャリーオペ,インク. Ampkアクチベーター

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.
CA2514547A1 (en) 2003-01-28 2004-08-12 Takeda Pharmaceutical Company Limited Receptor agonists
CA2928178C (en) * 2007-01-19 2019-09-10 Intercept Pharmaceuticals, Inc. Tgr5 modulators and methods of use thereof

Also Published As

Publication number Publication date
AU2009316484B2 (en) 2015-04-16
EP2373673A1 (en) 2011-10-12
IL212970A (en) 2017-07-31
ES2592452T3 (es) 2016-11-30
US20110263555A1 (en) 2011-10-27
ES2774368T3 (es) 2020-07-20
BRPI0921992B1 (pt) 2021-12-14
AU2009316484A1 (en) 2010-05-27
CN106380502A (zh) 2017-02-08
WO2010059859A1 (en) 2010-05-27
EP3150620A1 (en) 2017-04-05
JP5639073B2 (ja) 2014-12-10
JP2012509349A (ja) 2012-04-19
EP3150620B1 (en) 2020-01-08
EP2373673B1 (en) 2016-07-27
BRPI0921992A2 (pt) 2018-06-05
US8999964B2 (en) 2015-04-07
CA2744135A1 (en) 2010-05-27
IL212970A0 (en) 2011-07-31
CN102282157B (zh) 2017-02-22
CN102282157A (zh) 2011-12-14

Similar Documents

Publication Publication Date Title
CA2744135C (en) Tgr5 modulators and methods of use thereof
CA2732323C (en) Tgr5 modulators and methods of use thereof
AU2009316566B9 (en) TGR5 modulators and method of use thereof
AU2014204505B2 (en) TGR5 Modulators and Method of Use Thereof
HK1158212B (en) Tgr5 modulators and methods of use thereof
HK1234067A1 (en) Tgr5 modulators and methods of use thereof
HK1164887A (en) Tgr5 modulators and methods of use thereof
HK1164887B (en) Tgr5 modulators and methods of use thereof

Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20141110