AU2009316484B2 - TGR5 modulators and methods of use thereof - Google Patents

TGR5 modulators and methods of use thereof Download PDF

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Publication number
AU2009316484B2
AU2009316484B2 AU2009316484A AU2009316484A AU2009316484B2 AU 2009316484 B2 AU2009316484 B2 AU 2009316484B2 AU 2009316484 A AU2009316484 A AU 2009316484A AU 2009316484 A AU2009316484 A AU 2009316484A AU 2009316484 B2 AU2009316484 B2 AU 2009316484B2
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Australia
Prior art keywords
compound
disease
salt
amino acid
solvate
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Ceased
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AU2009316484A
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AU2009316484A1 (en
Inventor
Roberto Pellicciari
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Intercept Pharmaceuticals Inc
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Intercept Pharmaceuticals Inc
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    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (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)
AU2009316484A 2008-11-19 2009-11-19 TGR5 modulators and methods of use thereof Ceased AU2009316484B2 (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
AU2009316484A1 AU2009316484A1 (en) 2010-05-27
AU2009316484B2 true AU2009316484B2 (en) 2015-04-16

Family

ID=41666760

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2009316484A Ceased AU2009316484B2 (en) 2008-11-19 2009-11-19 TGR5 modulators and methods of use thereof

Country Status (10)

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

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102971311B (zh) 2010-05-06 2015-07-08 百时美施贵宝公司 作为gpr119调节剂的二环杂芳基化合物
US9062028B2 (en) 2011-04-28 2015-06-23 Bristol-Myers Squibb Company Bicyclic nitrogen containing heteroaryl TGR5 receptor modulators
NZ707389A (en) * 2012-10-26 2018-08-31 Intercept Pharmaceuticals Inc Process for preparing bile acid derivatives
WO2014085474A1 (en) * 2012-11-28 2014-06-05 Intercept Pharmaceuticals, Inc. Treatment of pulmonary disease
CA2914924A1 (en) 2013-06-13 2014-12-18 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.
SI3626725T1 (sl) 2014-05-29 2023-04-28 Bar Pharmaceuticals S.R.L. Derivati holana za uporabo pri zdravljenju in/ali preprečevanju bolezni, posredovanih s FXR in TGR5/GPBAR1
ES2748692T3 (es) * 2014-11-19 2020-03-17 Nzp Uk Ltd Esteroides 6.alfa.-alquil-3,7-diona como intermedios para la producción de moduladores FXR de esteroides
KR102526632B1 (ko) * 2014-11-19 2023-04-27 엔제트피 유케이 리미티드 스테로이드 FXR 조절인자를 제조하기 위한 중간체로서의 5β-6-알킬-7-하이드록시-3-온 스테로이드
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
JP6698085B2 (ja) * 2014-11-19 2020-05-27 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６α−アルキル−６，７−ジオン−ステロイド
RU2017121457A (ru) * 2014-11-26 2018-12-26 Энанта Фармасьютикалс, Инк. Аналоги желчной кислоты в качестве агонистов fxr/tgr5 и способы их применения
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
DK3310801T3 (da) * 2015-06-19 2021-06-21 Intercept Pharmaceuticals Inc Tgr5-modulatorer og fremgangsmåder til anvendelse deraf
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
CN109641934B (zh) * 2016-09-20 2021-07-02 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
MX2022010548A (es) 2020-02-28 2022-09-23 Kallyope Inc Agonistas de gpr40.
MX2022014505A (es) 2020-05-19 2022-12-13 Kallyope Inc Activadores de la ampk.
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.
EP1591120A4 (en) 2003-01-28 2009-06-10 Takeda Chemical Industries Ltd RECEPTOR AGONISTS
CA2928178C (en) 2007-01-19 2019-09-10 Intercept Pharmaceuticals, Inc. Tgr5 modulators and methods of use thereof

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
NONAPPA & MAITRA, U. Eur. J. Org. Chem. 2007, 3331-3336 *
PELLICCARI, R. et al. J. Med. Chem. 2007, 50, 4265-4268 *

Also Published As

Publication number Publication date
US8999964B2 (en) 2015-04-07
IL212970A (en) 2017-07-31
BRPI0921992B1 (pt) 2021-12-14
EP2373673A1 (en) 2011-10-12
CA2744135A1 (en) 2010-05-27
CN106380502A (zh) 2017-02-08
ES2592452T3 (es) 2016-11-30
CN102282157A (zh) 2011-12-14
AU2009316484A1 (en) 2010-05-27
US20110263555A1 (en) 2011-10-27
ES2774368T3 (es) 2020-07-20
IL212970A0 (en) 2011-07-31
EP3150620A1 (en) 2017-04-05
JP5639073B2 (ja) 2014-12-10
CN102282157B (zh) 2017-02-22
CA2744135C (en) 2017-07-04
EP2373673B1 (en) 2016-07-27
JP2012509349A (ja) 2012-04-19
BRPI0921992A2 (pt) 2018-06-05
WO2010059859A1 (en) 2010-05-27
EP3150620B1 (en) 2020-01-08

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