CN106380502A - G蛋白偶联受体5(tgr5)调节剂及其使用方法 - Google Patents

G蛋白偶联受体5(tgr5)调节剂及其使用方法 Download PDF

Info

Publication number
CN106380502A
CN106380502A CN201610680498.XA CN201610680498A CN106380502A CN 106380502 A CN106380502 A CN 106380502A CN 201610680498 A CN201610680498 A CN 201610680498A CN 106380502 A CN106380502 A CN 106380502A
Authority
CN
China
Prior art keywords
compound
disease
group
salt
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.)
Pending
Application number
CN201610680498.XA
Other languages
English (en)
Chinese (zh)
Inventor
R·佩里恰里
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.)
Ntercept Pharmaceuticals Inc
Original Assignee
Ntercept 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=CN106380502(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Ntercept Pharmaceuticals Inc filed Critical Ntercept Pharmaceuticals Inc
Publication of CN106380502A publication Critical patent/CN106380502A/zh
Pending legal-status Critical Current

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)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
CN201610680498.XA 2008-11-19 2009-11-19 G蛋白偶联受体5(tgr5)调节剂及其使用方法 Pending CN106380502A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP08169460.6 2008-11-19
EP08169460 2008-11-19
CN200980154703.7A CN102282157B (zh) 2008-11-19 2009-11-19 G蛋白偶联受体5(tgr5)调节剂及其使用方法

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN200980154703.7A Division CN102282157B (zh) 2008-11-19 2009-11-19 G蛋白偶联受体5(tgr5)调节剂及其使用方法

Publications (1)

Publication Number Publication Date
CN106380502A true CN106380502A (zh) 2017-02-08

Family

ID=41666760

Family Applications (2)

Application Number Title Priority Date Filing Date
CN201610680498.XA Pending CN106380502A (zh) 2008-11-19 2009-11-19 G蛋白偶联受体5(tgr5)调节剂及其使用方法
CN200980154703.7A Expired - Fee Related CN102282157B (zh) 2008-11-19 2009-11-19 G蛋白偶联受体5(tgr5)调节剂及其使用方法

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN200980154703.7A Expired - Fee Related CN102282157B (zh) 2008-11-19 2009-11-19 G蛋白偶联受体5(tgr5)调节剂及其使用方法

Country Status (10)

Country Link
US (1) US8999964B2 (https=)
EP (2) EP3150620B1 (https=)
JP (1) JP5639073B2 (https=)
CN (2) CN106380502A (https=)
AU (1) AU2009316484B2 (https=)
BR (1) BRPI0921992B1 (https=)
CA (1) CA2744135C (https=)
ES (2) ES2774368T3 (https=)
IL (1) IL212970A (https=)
WO (1) WO2010059859A1 (https=)

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2798610A1 (en) 2010-05-06 2011-11-10 Bristol-Myers Squibb Company Bicyclic heteroaryl compounds as gpr119 modulators
WO2012149236A1 (en) 2011-04-28 2012-11-01 Bristol-Myers Squibb Company Novel bicyclic nitrogen containing heteroaryl tgr5 receptor modulators
SG11201503247UA (en) * 2012-10-26 2015-06-29 Intercept Pharmaceuticals Inc Process for preparing bile acid derivatives
AU2013352288B2 (en) * 2012-11-28 2017-11-23 Intercept Pharmaceuticals, Inc. Treatment of pulmonary disease
WO2014200349A1 (en) 2013-06-13 2014-12-18 Fast Forward Pharmaceutical 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.
SMT202000070T1 (it) * 2014-05-29 2020-03-13 Bar Pharmaceuticals S R L Derivati del colano per l'uso del trattamento e/o la prevenzione di malattie mediate da fxr e tgr5/gpbar1
KR102546748B1 (ko) * 2014-11-19 2023-06-22 엔제트피 유케이 리미티드 스테로이드 FXR 조절인자를 제조하기 위한 중간체로서의 6α-알킬-3,7-다이온 스테로이드
CN107207559B (zh) * 2014-11-19 2019-10-25 Nzp英国有限公司 作为制备类固醇fxr调节剂的中间体的6-烷基-7-羟基-4-烯-3-酮类固醇
KR102527821B1 (ko) * 2014-11-19 2023-05-02 엔제트피 유케이 리미티드 스테로이드 FXR 조절인자를 제조하기 위한 중간체로서의 6α-알킬-6,7-다이온 스테로이드
EA033445B1 (ru) * 2014-11-19 2019-10-31 Nzp Uk Ltd 5-бета-6-алкил-7-гидрокси-3-оновые стероиды в качестве промежуточных соединений для получения стероидных модуляторов fxr
EP3223823A4 (en) * 2014-11-26 2018-10-17 Enanta Pharmaceuticals, Inc. Bile acid analogs as fxr/tgr5 agonists and methods of use thereof
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
US10800807B2 (en) 2015-06-19 2020-10-13 Intercept Pharmaceuticals, Inc. TGR5 modulators and methods of use thereof
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
GB201608776D0 (en) 2016-05-18 2016-06-29 Dextra Lab Ltd Methods and compounds
GB201608777D0 (en) 2016-05-18 2016-06-29 Dextra Lab Ltd 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
IL295825A (en) 2020-02-28 2022-10-01 Kallyope Inc gpr40 agonists
WO2021236617A1 (en) 2020-05-19 2021-11-25 Kallyope, Inc. Ampk activators
CA3183575A1 (en) 2020-06-26 2021-12-30 Iyassu Sebhat Ampk activators

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.
US7625887B2 (en) 2003-01-28 2009-12-01 Takeda Pharmaceutical Company Limited Receptor agonists
KR101555716B1 (ko) * 2007-01-19 2015-09-25 인터셉트 파마슈티컬즈, 인크. Tgr5 조절제로서의 23-치환 담즙산 및 이의 사용 방법

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
L. R. HAGEY ET AL.: "《A novel primary bile acid in the Shoebill stork and herons and its phylogenetic significance》", 《JOURNAL OF LIPID RESEARCH》 *
ROBERTO PELLICCIARI ET AL: "《Nongenomic actions of bile acids. Synthesis and preliminary characterization of 23-and 6,23-alkyl-substituted bile Acid derivatives as selective modulators for theG-protein coupled receptor TGR5》", 《J. MED. CHEM.》 *
TAKASHI IIDA ET AL.: "《Potential Bile Acid Metabolites. 25. Synthesis and Chemical Properties of Stereoisomeric 3a,7a,16- and 3a,7a,15-Trihydroxy-5b -cholan-24-oic Acids》", 《CLREM. PHARM. BULL》 *

Also Published As

Publication number Publication date
IL212970A0 (en) 2011-07-31
JP5639073B2 (ja) 2014-12-10
ES2592452T3 (es) 2016-11-30
EP2373673A1 (en) 2011-10-12
EP3150620A1 (en) 2017-04-05
ES2774368T3 (es) 2020-07-20
CA2744135C (en) 2017-07-04
BRPI0921992A2 (pt) 2018-06-05
IL212970A (en) 2017-07-31
JP2012509349A (ja) 2012-04-19
US20110263555A1 (en) 2011-10-27
AU2009316484B2 (en) 2015-04-16
US8999964B2 (en) 2015-04-07
CN102282157B (zh) 2017-02-22
AU2009316484A1 (en) 2010-05-27
CA2744135A1 (en) 2010-05-27
CN102282157A (zh) 2011-12-14
EP3150620B1 (en) 2020-01-08
EP2373673B1 (en) 2016-07-27
WO2010059859A1 (en) 2010-05-27
BRPI0921992B1 (pt) 2021-12-14

Similar Documents

Publication Publication Date Title
CN106380502A (zh) G蛋白偶联受体5(tgr5)调节剂及其使用方法
Fiorucci et al. Bile acid-activated receptors and the regulation of macrophages function in metabolic disorders
CN104370990A (zh) G蛋白偶联受体5(tgr5)调节剂及其使用方法
CN105037476B (zh) Tgr5调节剂及其使用方法
JP6892457B2 (ja) 3−デスオキシ誘導体およびその医薬組成物
EP3626725B1 (en) Cholane derivatives for use in the treatment and/or prevention of fxr and tgr5/gpbar1 mediated diseases
CN106232612B (zh) 骨选择性成骨性氧固醇双膦酸盐类似物
CN104672290B (zh) 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
CN107771180A (zh) Tgr5调节剂及其使用方法
CN108245523A (zh) 作为法尼醇x受体调节剂的胆汁酸的11-羟基衍生物及其氨基酸共轭物
CN106083978A (zh) 磺酰基氨基羰基衍生物、其药物组合物及应用
Donna et al. Novel FXR (farnesoid X receptor) modulators: Potential therapies for cholesterol gallstone disease
BR112018006892B1 (pt) Composto, composição farmacêutica do mesmo e seus usos como moduladores do receptor farnesoide x
Yun et al. Identification of betulinic acid derivatives as potent TGR5 agonists with antidiabetic effects via humanized TGR5H88Y mutant mice
CN100375752C (zh) 齐墩果酸及其衍生物、制法及用途
CN106967143A (zh) 结构新颖的pyxinol衍生物及其制备方法和用途
Lu et al. Chemical biology studies on human and mouse secondary bile acids
HK1234067A1 (en) Tgr5 modulators and methods of use thereof
CN109206470A (zh) 刺囊酸衍生物制备方法及医药新用途
HK1164887A (en) Tgr5 modulators and methods of use thereof
HK1164887B (en) Tgr5 modulators and methods of use thereof
Shen et al. Synthesis of non-steroidal cholic acid analogues as potent and selective TGR5 allosteric agonists with antidiabetic effects
WO2025202883A1 (en) Cholane derivatives for the treatment and the prevention of fxr and tgr5gp-bar1 receptors mediated diseases
KR20240150765A (ko) 사르사사포게닌 구조에 기반한 유도체 및 이의 약학적 조성물의 용도
CN118178426A (zh) 一种植物甾醇改善神经脂代谢的用途

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1234067

Country of ref document: HK

WD01 Invention patent application deemed withdrawn after publication
WD01 Invention patent application deemed withdrawn after publication

Application publication date: 20170208

REG Reference to a national code

Ref country code: HK

Ref legal event code: WD

Ref document number: 1234067

Country of ref document: HK