ES2592452T3 - Moduladores de TGR5 y métodos de uso de los mismos - Google Patents

Moduladores de TGR5 y métodos de uso de los mismos Download PDF

Info

Publication number
ES2592452T3
ES2592452T3 ES09759854.4T ES09759854T ES2592452T3 ES 2592452 T3 ES2592452 T3 ES 2592452T3 ES 09759854 T ES09759854 T ES 09759854T ES 2592452 T3 ES2592452 T3 ES 2592452T3
Authority
ES
Spain
Prior art keywords
compound
disease
bile
animals
cells
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
ES09759854.4T
Other languages
English (en)
Spanish (es)
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=ES2592452(T3) "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
Application granted granted Critical
Publication of ES2592452T3 publication Critical patent/ES2592452T3/es
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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
    • 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
    • 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
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Diabetes (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)
ES09759854.4T 2008-11-19 2009-11-19 Moduladores de TGR5 y métodos de uso de los mismos Active ES2592452T3 (es)

Applications Claiming Priority (3)

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

Publications (1)

Publication Number Publication Date
ES2592452T3 true ES2592452T3 (es) 2016-11-30

Family

ID=41666760

Family Applications (2)

Application Number Title Priority Date Filing Date
ES09759854.4T Active ES2592452T3 (es) 2008-11-19 2009-11-19 Moduladores de TGR5 y métodos de uso de los mismos
ES16181337T Active ES2774368T3 (es) 2008-11-19 2009-11-19 Moduladores de TGR5 y métodos de uso de los mismos

Family Applications After (1)

Application Number Title Priority Date Filing Date
ES16181337T Active ES2774368T3 (es) 2008-11-19 2009-11-19 Moduladores de TGR5 y métodos de uso de los mismos

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
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
CA2744135C (en) 2017-07-04
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
ES2592452T3 (es) Moduladores de TGR5 y métodos de uso de los mismos
US7932244B2 (en) Bile acid derivatives as FXR ligands for the prevention or treatment of FXR-mediated diseases or conditions
ES2671427T3 (es) Derivados 11-hidroxil-6-sustituidos de ácidos biliares y conjugados de aminoácidos de los mismos como moduladores de receptores farnesoides X
JP7021080B2 (ja) ファルネソイドｘ受容体調節剤
Brauner et al. Phytosterols reduce cholesterol absorption by inhibition of 27-hydroxycholesterol generation, liver X receptor α activation, and expression of the basolateral sterol exporter ATP-binding cassette A1 in Caco-2 enterocytes
Marchianò et al. Beneficial effects of UDCA and norUDCA in a rodent model of steatosis are linked to modulation of GPBAR1/FXR signaling
EA020140B1 (ru) Модуляторы tgr5 и способы их применения
BR112018068278B1 (pt) Derivado de 3-desóxi, ácido livre, sal e conjugado de aminoácido, composição farmaceutica compreendendo o referido composto e seu uso
Wang et al. New insights into the role of Lith genes in the formation of cholesterol-supersaturated bile
Jones et al. Impact of physiological levels of chenodeoxycholic acid supplementation on intestinal and hepatic bile acid and cholesterol metabolism in Cyp7a1-deficient mice
Mendoza et al. Changes in the pattern of bile acids in the nuclei of rat liver cells during hepatocarcinogenesis
HK1130187B (en) Bile acid derivatives as fxr ligands for the prevention or treatment of fxr-mediated deseases or conditions
HK1164887A (en) Tgr5 modulators and methods of use thereof