BRPI0921983B8 - moduladores tgr5, usos dos mesmos e kit - Google Patents

moduladores tgr5, usos dos mesmos e kit

Info

Publication number
BRPI0921983B8
BRPI0921983B8 BRPI0921983A BRPI0921983A BRPI0921983B8 BR PI0921983 B8 BRPI0921983 B8 BR PI0921983B8 BR PI0921983 A BRPI0921983 A BR PI0921983A BR PI0921983 A BRPI0921983 A BR PI0921983A BR PI0921983 B8 BRPI0921983 B8 BR PI0921983B8
Authority
BR
Brazil
Prior art keywords
diseases
tgr5 modulators
kit
compounds
formula
Prior art date
Application number
BRPI0921983A
Other languages
English (en)
Portuguese (pt)
Inventor
Pelicciari Roberto
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=41668454&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=BRPI0921983(B8) "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 BRPI0921983A2 publication Critical patent/BRPI0921983A2/pt
Publication of BRPI0921983B1 publication Critical patent/BRPI0921983B1/pt
Publication of BRPI0921983B8 publication Critical patent/BRPI0921983B8/pt

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
    • 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
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pulmonology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Neurosurgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Transplantation (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Vascular Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
BRPI0921983A 2008-11-19 2009-11-19 moduladores tgr5, usos dos mesmos e kit BRPI0921983B8 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP08169462 2008-11-19
EP08169462.2 2008-11-19
PCT/US2009/065188 WO2010059853A1 (en) 2008-11-19 2009-11-19 Tgr5 modulators and method of use thereof

Publications (3)

Publication Number Publication Date
BRPI0921983A2 BRPI0921983A2 (pt) 2018-07-10
BRPI0921983B1 BRPI0921983B1 (pt) 2021-04-20
BRPI0921983B8 true BRPI0921983B8 (pt) 2021-05-25

Family

ID=41668454

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0921983A BRPI0921983B8 (pt) 2008-11-19 2009-11-19 moduladores tgr5, usos dos mesmos e kit

Country Status (23)

Country Link
US (5) US8114862B2 (enExample)
EP (2) EP2698375B1 (enExample)
JP (5) JP5535233B2 (enExample)
KR (2) KR101789960B1 (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) ES2458168T3 (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) PT2376519E (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
EP1392714B1 (en) 2001-03-12 2005-08-31 Intercept Pharmaceuticals, Inc. Steroids as agonists for fxr
US9498484B2 (en) 2004-03-12 2016-11-22 Intercept Pharmaceuticals, Inc. Treatment of fibrosis using 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
WO2008091540A2 (en) 2007-01-19 2008-07-31 Intercept Pharmaceuticals, Inc. 23-substituted bile acids as tgr5 modulators and methods of use thereof
AU2009276507B2 (en) 2008-07-30 2015-11-19 Intercept Pharmaceuticals, Inc. TGR5 modulators and methods of use thereof
SG10201400162QA (en) * 2008-11-19 2014-05-29 Intercept Pharmaceuticals Inc Tgr5 modulators and methods of use thereof
EP2364161B1 (en) 2008-11-26 2020-03-11 Satiogen Pharmaceuticals, Inc. Compositions containing satiogens and methods of use
EP2367554A4 (en) 2008-11-26 2020-03-25 Satiogen Pharmaceuticals, Inc. Bile acid reflux inhibitor for the treatment of obesity and diabetes
EP4137137A1 (en) 2010-05-26 2023-02-22 Satiogen Pharmaceuticals, Inc. Bile acid recycling inhibitors and satiogens for treatment of diabetes, obesity, and inflammatory gastrointestinal conditions
SG10201909122QA (en) 2011-10-28 2019-11-28 Lumena Pharmaceuticals Inc Bile acid recycling inhibitors for treatment of pediatric cholestatic liver diseases
US20140323412A1 (en) 2011-10-28 2014-10-30 Lumena Pharmaceuticals, Inc. Bile acid recycling inhibitors for treatment of hypercholemia and cholestatic liver disease
SG10201607230SA (en) 2012-06-19 2016-10-28 Intercept Pharmaceuticals Inc Preparation, Uses And Solid Forms Of Obeticholic Acid
US9982008B2 (en) 2012-06-19 2018-05-29 Intercept Pharmaceuticals, Inc. Preparation and uses of obeticholic acid
EP2906946A1 (en) 2012-10-09 2015-08-19 The Procter & Gamble Company Method of identifying or evaluating beneficial actives and compositions containing the same
JP6189962B2 (ja) 2012-10-09 2017-08-30 ザ プロクター アンド ギャンブル カンパニー 相乗作用する美容成分の組み合わせを特定する方法
WO2014195950A1 (en) * 2013-06-06 2014-12-11 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. Bile acid-basic amino acid conjugates and uses thereof
EP3008091A1 (en) * 2013-06-13 2016-04-20 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.
KR102507624B1 (ko) 2013-11-22 2023-03-09 미나 테라퓨틱스 리미티드 Ｃ/ｅｂｐ 알파 짧은 활성화 ｒｎａ 조성물 및 사용 방법
WO2015181275A1 (en) * 2014-05-29 2015-12-03 Bar Pharmaceuticals S.R.L. Cholane derivatives for use in the treatment and/or prevention of fxr and tgr5/gpbar1 mediated diseases
WO2016054208A1 (en) * 2014-10-03 2016-04-07 Mayo Foundation For Medical Education And Research Targeting tgr5 to treat disease
BR112017009657A2 (pt) * 2014-11-06 2018-01-23 Enanta Pharmaceuticals, Inc análogos de ácidos biliares como agonistas de fxr/tgr5 e métodos de uso dos mesmos
WO2016079520A1 (en) 2014-11-19 2016-05-26 Dextra Laboratories Limited 6.alpha.-alkyl-6,7-dione steroids as intermediates for the production of steroidal fxr modulators
KR102526631B1 (ko) 2014-11-19 2023-04-27 엔제트피 유케이 리미티드 스테로이드 fxr 조절인자를 제조하기 위한 중간체로서의 6-알킬-7-하이드록시-4-엔-3-온 스테로이드
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
MX375864B (es) 2014-11-19 2025-03-07 Nzp Uk Ltd Esteroides de 5.beta-6-alquil-7-hidroxi-3-ona 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
US10800807B2 (en) 2015-06-19 2020-10-13 Intercept Pharmaceuticals, Inc. TGR5 modulators and methods of use thereof
PT3310801T (pt) * 2015-06-24 2021-06-18 Intercept Pharmaceuticals Inc Moduladores de tgr5 e métodos de utilização dos mesmos
HK1254057A1 (zh) * 2015-09-24 2019-07-12 英特塞普特医药品公司 用於制备胆汁酸衍生物的方法和中间体
CN108348530B (zh) 2015-10-07 2023-09-29 英特塞普特医药品公司 法尼醇x受体调节剂
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
CN109071452A (zh) 2016-04-13 2018-12-21 英特塞普特医药品公司 治疗癌症的方法
GB201608777D0 (en) 2016-05-18 2016-06-29 Dextra Lab Ltd Compounds
WO2017210147A1 (en) 2016-05-29 2017-12-07 Wei Jia Liver disease-related biomarkers and methods of use thereof
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
CA3070837A1 (en) 2017-07-24 2019-01-31 Intercept Pharmaceuticals, Inc. Isotopically labeled bile acid derivatives
EP4183882A1 (en) 2017-09-08 2023-05-24 MiNA Therapeutics Limited Stabilized hnf4a sarna compositions and methods of use
GB201812382D0 (en) 2018-07-30 2018-09-12 Nzp Uk Ltd Compounds
WO2020163201A1 (en) * 2019-02-04 2020-08-13 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
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
JP2023526625A (ja) 2020-05-19 2023-06-22 キャリーオペ，インク． Ａｍｐｋアクチベーター
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

Family Cites Families (51)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0101554B1 (en) 1982-07-29 1986-10-15 Lehner A.G. 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.
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
IT1196377B (it) 1984-12-21 1988-11-16 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.
EP0433899B1 (en) * 1989-12-13 1995-04-12 Mitsubishi Chemical Corporation New pyrazolyl acrylic acid derivatives, useful as systemic fungicides for plant and material protection
WO1997028149A1 (en) 1996-02-02 1997-08-07 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
PL331148A1 (en) 1996-07-12 1999-06-21 Smithkline Beecham Plc Novel method of treating the leptin immunity
US6008237A (en) * 1997-12-19 1999-12-28 Merck & Co., Inc. Arylthiazolidinedione derivatives
EP1053227B1 (en) 1998-01-29 2008-11-05 Amgen Inc. Ppar-gamma modulators
WO2000025134A1 (en) 1998-10-23 2000-05-04 Glaxo Group Limited Assays for ligands for nuclear receptors
JP2002532729A (ja) * 1998-12-23 2002-10-02 グラクソ グループ リミテッド 核内受容体のリガンドのアッセイ
US6465258B1 (en) 1999-01-07 2002-10-15 Tularik, Inc. FXR receptor-mediated modulation cholesterol metabolism
US20020132223A1 (en) 1999-03-26 2002-09-19 City Of Hope Methods for modulating activity of the FXR nuclear receptor
EP1473042B1 (en) 1999-03-26 2006-06-21 City of Hope Screening for FXR receptor modulators
DE60013417T2 (de) 1999-03-26 2005-09-15 City Of Hope, Duarte Verfahren zum screenen von fxr-rezeptormodulatoren
US6906057B1 (en) * 1999-06-11 2005-06-14 Allergan, Inc. Methods for modulating FXR receptor activity
JP2003501477A (ja) 1999-06-11 2003-01-14 アラーガン・セイルズ・インコーポレイテッド Ｆｘｒ受容体活性を調節する方法
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
CA2386750A1 (en) 1999-10-22 2001-05-03 Merck & Co. Inc. Pharmaceuticals for treating obesity
EP1273659A4 (en) 2000-04-12 2004-04-21 Takeda Chemical Industries Ltd G-PROTEIN COUPLED RECEPTOR PROTEIN AND ITS DNA
US6627636B2 (en) * 2000-06-15 2003-09-30 Bristol-Myers Squibb Company HMG-CoA reductase inhibitors and method
AU2001288623A1 (en) * 2000-09-05 2002-03-22 Tularik, Inc. Fxr modulators
US20020119958A1 (en) 2001-02-13 2002-08-29 Shinichiro Tojo Therapeutic agent for hyperlipidemia
EP1392714B1 (en) 2001-03-12 2005-08-31 Intercept Pharmaceuticals, Inc. Steroids as agonists for fxr
WO2002084286A1 (en) 2001-04-12 2002-10-24 Takeda Chemical Industries, Ltd. Screening method
EP1423113A4 (en) 2001-08-13 2007-04-18 Phenex Pharmaceuticals Ag NR1H4 NUCLEAR RECEPTOR BINDING COMPOUNDS
US20070010562A1 (en) 2001-08-13 2007-01-11 Ulrike Bauer Nr1h4 nuclear receptor binding compounds
ATE381542T1 (de) 2001-08-13 2008-01-15 Phenex Pharmaceuticals Ag Nr1h4-kern-rezeptor-bindende verbindungen
US20030144360A1 (en) 2001-11-19 2003-07-31 Allergan Sales, Inc. Composition and method for modulating BAR/FXR receptor activity
AU2003225903A1 (en) 2002-03-21 2003-10-08 Curagen 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
JPWO2004000752A1 (ja) 2002-06-19 2005-10-20 株式会社アベイラス 人造石壁材
ITMI20021532A1 (it) 2002-07-12 2004-01-12 Roberto Pellicciari Composti chimici
EP1562915A1 (en) 2002-11-22 2005-08-17 SmithKline Beecham Corporation Farnesoid x receptor agonists
US7625887B2 (en) 2003-01-28 2009-12-01 Takeda Pharmaceutical Company Limited 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
US9498484B2 (en) 2004-03-12 2016-11-22 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
DK2040713T3 (da) 2006-06-27 2014-09-29 Intercept Pharmaceuticals Inc Galdesyrederivater som fxr-ligander til forebyggelsen eller behandlingen af fxr-medierede sygdomme eller tilstande
WO2008091540A2 (en) 2007-01-19 2008-07-31 Intercept Pharmaceuticals, Inc. 23-substituted bile acids as tgr5 modulators and methods of use thereof
EP1947108A1 (en) 2007-01-19 2008-07-23 Intercept Pharmaceuticals, Inc. TGR5 modulators and methods of use thereof
SG10201400162QA (en) * 2008-11-19 2014-05-29 Intercept Pharmaceuticals Inc Tgr5 modulators and methods of use thereof

Also Published As

Publication number Publication date
IL264796B (en) 2020-11-30
AU2009316566B9 (en) 2014-05-15
EP2698375B1 (en) 2018-02-21
IL212969A (en) 2016-04-21
US20100152151A1 (en) 2010-06-17
US20120115832A1 (en) 2012-05-10
US20210269473A1 (en) 2021-09-02
ES2458168T3 (es) 2014-04-30
EP2376519B1 (en) 2013-11-13
BRPI0921983B1 (pt) 2021-04-20
EA030681B1 (ru) 2018-09-28
DK2698375T3 (en) 2018-05-28
JP2014159456A (ja) 2014-09-04
US9650409B2 (en) 2017-05-16
US8445472B2 (en) 2013-05-21
CA2744189A1 (en) 2010-05-27
AU2009316566B2 (en) 2014-04-17
LT2698375T (lt) 2018-07-10
AU2009316566A1 (en) 2010-05-27
KR20110086177A (ko) 2011-07-27
JP2015232020A (ja) 2015-12-24
CN102325784B (zh) 2014-11-19
IL212969A0 (en) 2011-07-31
EA020140B1 (ru) 2014-08-29
CN102325784A (zh) 2012-01-18
SG10201400162QA (en) 2014-05-29
IL244812A0 (en) 2016-05-31
US8114862B2 (en) 2012-02-14
EA201170714A1 (ru) 2012-01-30
KR101667436B1 (ko) 2016-10-18
AU2009316566A2 (en) 2011-07-14
HUE039171T2 (hu) 2018-12-28
PL2698375T3 (pl) 2018-08-31
CN104370990A (zh) 2015-02-25
US20140100209A1 (en) 2014-04-10
PT2376519E (pt) 2014-02-20
HK1166327A1 (en) 2012-10-26
JP2017132803A (ja) 2017-08-03
US20180016295A1 (en) 2018-01-18
WO2010059853A1 (en) 2010-05-27
JP5535233B2 (ja) 2014-07-02
JP2018100304A (ja) 2018-06-28
PT2698375T (pt) 2018-05-25
ZA201104077B (en) 2012-02-29
EP2698375A2 (en) 2014-02-19
DK2376519T3 (da) 2014-02-03
EP2698375A3 (en) 2014-03-12
KR20160122272A (ko) 2016-10-21
HK1205132A1 (en) 2015-12-11
EA201400258A1 (ru) 2015-02-27
BRPI0921983A2 (pt) 2018-07-10
EP2376519A1 (en) 2011-10-19
ES2663948T3 (es) 2018-04-17
KR101789960B1 (ko) 2017-10-25
MX2011005295A (es) 2011-06-24
NO2698375T3 (enExample) 2018-07-21
CA2744189C (en) 2016-10-11
SI2698375T1 (sl) 2018-10-30
JP2012509348A (ja) 2012-04-19
IL244812B (en) 2019-03-31
PL2376519T3 (pl) 2014-04-30

Similar Documents

Publication Publication Date Title
BRPI0921983B8 (pt) moduladores tgr5, usos dos mesmos e kit
BRPI0916735B8 (pt) compostos moduladores de tgr5, composições farmacêuticas compreendendo os mesmos e seus usos
WO2016205475A3 (en) Tgr5 modulators and methods of use thereof
EA025302B8 (ru) Модуляторы кальциевого канала, активируемого высвобождением кальция, представляющие собой производные пиразола, и способы лечения немелкоклеточного рака легких
EA201100037A1 (ru) Органические соединения
MX2013011921A (es) Compuestos de benceno substituidos con arilo o heterorilo.
CY1110900T1 (el) Χημικες ενωσεις
CY1108275T1 (el) Χημικες ενωσεις
CL2012001821A1 (es) Compuestos derivados de 5-alquinil-pirimidinas, inhibidores de quinasas; composiciones farmaceuticas que los contienen; y su uso para el tratamiento y/o prevencion de cancer, infecciones, enfermedades inflamatorias y autoinmunitarias.
EA201101341A1 (ru) Соединения, ингибирующие киназы, и фармацевтическая композиция на их основе
EA201070786A1 (ru) Бензофуропиримидиноны
EA201001242A1 (ru) ПИРРОЛО[2,3-d]ПИРИДИНЫ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ИНГИБИТОРОВ ТИРОЗИНКИНАЗЫ
EA201100447A1 (ru) Органические соединения
EA201400412A1 (ru) ЗАМЕЩЕННЫЕ БЕНЗИЛИНДАЗОЛЫ ДЛЯ ПРИМЕНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ Bub1 КИНАЗЫ ДЛЯ ЛЕЧЕНИЯ ГИПЕРПРОЛИФЕРАТИВНЫХ ЗАБОЛЕВАНИЙ
EA201070395A1 (ru) Ингибиторы polo-подобных киназ
EA200801428A1 (ru) Производные пиридиазинона для лечения опухолей
EA200970149A1 (ru) Производные n-(аминогетероарил)-1h-индол-2-карбоксамидов, их получение и их применение в терапии
EA201170832A1 (ru) Пуриновые соединения
EA201290642A1 (ru) Соединения и способы
EA201500182A1 (ru) 4-МЕТИЛ-2,3,5,9,9b-ПЕНТААЗАЦИКЛОПЕНТА[a]НАФТАЛИНЫ
UY31065A1 (es) Heterociclos ciclicos
CR10654A (es) Agentes que comprenden compuestos marcados con 18f y metodos relacionados
UY29047A1 (es) Derivados de sulfonamidas, su preparación y su aplicación en terapéutica
DE502008002375D1 (de) Wässrige Dispersionen von Organosiliciumverbindungen
BRPI0906444B8 (pt) compostos de 4-piridinona, composição farmacêutica que os compreende, bem como uso dos mesmos

Legal Events

Date Code Title Description
B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]

Free format text: DE ACORDO COM O ARTIGO 229-C DA LEI NO 10196/2001, QUE MODIFICOU A LEI NO 9279/96, A CONCESSAO DA PATENTE ESTA CONDICIONADA A ANUENCIA PREVIA DA ANVISA. CONSIDERANDO A APROVACAO DOS TERMOS DO PARECER NO 337/PGF/EA/2010, BEM COMO A PORTARIA INTERMINISTERIAL NO 1065 DE 24/05/2012, ENCAMINHA-SE O PRESENTE PEDIDO PARA AS PROVIDENCIAS CABIVEIS.

B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]
B06U Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette]
B09A Decision: intention to grant [chapter 9.1 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]

Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 19/11/2009, OBSERVADAS AS CONDICOES LEGAIS. PATENTE CONCEDIDA CONFORME MEDIDA CAUTELAR DE 07/04/2021 - ADI 5.529/DF

B16C Correction of notification of the grant [chapter 16.3 patent gazette]

Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 19/11/2009 OBSERVADAS AS CONDICOES LEGAIS. PATENTE CONCEDIDA CONFORME ADI 5.529/DF

B25G Requested change of headquarter approved

Owner name: INTERCEPT PHARMACEUTICALS, INC. (US)

B21F Lapse acc. art. 78, item iv - on non-payment of the annual fees in time

Free format text: REFERENTE A 15A ANUIDADE.

B24J Lapse because of non-payment of annual fees (definitively: art 78 iv lpi, resolution 113/2013 art. 12)

Free format text: EM VIRTUDE DA EXTINCAO PUBLICADA NA RPI 2801 DE 10-09-2024 E CONSIDERANDO AUSENCIA DE MANIFESTACAO DENTRO DOS PRAZOS LEGAIS, INFORMO QUE CABE SER MANTIDA A EXTINCAO DA PATENTE E SEUS CERTIFICADOS, CONFORME O DISPOSTO NO ARTIGO 12, DA RESOLUCAO 113/2013.