DK3149019T3 - Cholan-derivater til anvendelse ved behandling og/eller forebyggelse af FXR- og TGR5/GPBAR1-formidlede sygdomme - Google Patents
Cholan-derivater til anvendelse ved behandling og/eller forebyggelse af FXR- og TGR5/GPBAR1-formidlede sygdomme Download PDFInfo
- Publication number
- DK3149019T3 DK3149019T3 DK15731260.4T DK15731260T DK3149019T3 DK 3149019 T3 DK3149019 T3 DK 3149019T3 DK 15731260 T DK15731260 T DK 15731260T DK 3149019 T3 DK3149019 T3 DK 3149019T3
- Authority
- DK
- Denmark
- Prior art keywords
- gpbar1
- cholan
- tgr5
- fxr
- prevention
- Prior art date
Links
- 102100025353 G-protein coupled bile acid receptor 1 Human genes 0.000 title 2
- 101000857733 Homo sapiens G-protein coupled bile acid receptor 1 Proteins 0.000 title 2
- IGRCWJPBLWGNPX-UHFFFAOYSA-N 3-(2-chlorophenyl)-n-(4-chlorophenyl)-n,5-dimethyl-1,2-oxazole-4-carboxamide Chemical compound C=1C=C(Cl)C=CC=1N(C)C(=O)C1=C(C)ON=C1C1=CC=CC=C1Cl IGRCWJPBLWGNPX-UHFFFAOYSA-N 0.000 title 1
- QSHQKIURKJITMZ-BRPMRXRMSA-N cholane Chemical class C1CC2CCCC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCC)[C@@]1(C)CC2 QSHQKIURKJITMZ-BRPMRXRMSA-N 0.000 title 1
- 201000010099 disease Diseases 0.000 title 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title 1
- 230000001404 mediated effect Effects 0.000 title 1
- 230000002265 prevention Effects 0.000 title 1
Classifications
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- 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
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- 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
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- 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
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- 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
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
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- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
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- A—HUMAN NECESSITIES
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- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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
- A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
-
- 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
- A61P9/10—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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J11/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 3
-
- 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
- C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
- C07J41/0094—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 containing nitrile radicals, including thiocyanide radicals
-
- 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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Virology (AREA)
- Toxicology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Immunology (AREA)
- Molecular Biology (AREA)
- Endocrinology (AREA)
- Rheumatology (AREA)
- Neurology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Urology & Nephrology (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Epidemiology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Dermatology (AREA)
- Biomedical Technology (AREA)
- Vascular Medicine (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Biotechnology (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ITFI20140130 | 2014-05-29 | ||
| PCT/EP2015/061802 WO2015181275A1 (en) | 2014-05-29 | 2015-05-28 | Cholane derivatives for use in the treatment and/or prevention of fxr and tgr5/gpbar1 mediated diseases |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DK3149019T3 true DK3149019T3 (da) | 2020-02-17 |
Family
ID=51454763
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK15731260.4T DK3149019T3 (da) | 2014-05-29 | 2015-05-28 | Cholan-derivater til anvendelse ved behandling og/eller forebyggelse af FXR- og TGR5/GPBAR1-formidlede sygdomme |
| DK19204247.1T DK3626725T3 (da) | 2014-05-29 | 2015-05-28 | Cholan-derivater til anvendelse ved behandlingen og/eller forebyggelsen af fxr- og tgr5/gpbar1-medierede sygdomme |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK19204247.1T DK3626725T3 (da) | 2014-05-29 | 2015-05-28 | Cholan-derivater til anvendelse ved behandlingen og/eller forebyggelsen af fxr- og tgr5/gpbar1-medierede sygdomme |
Country Status (25)
| Country | Link |
|---|---|
| US (2) | US10407462B2 (da) |
| EP (2) | EP3626725B1 (da) |
| JP (1) | JP6820253B2 (da) |
| KR (1) | KR102491556B1 (da) |
| CN (2) | CN110003301B (da) |
| AU (1) | AU2015265893B2 (da) |
| CA (1) | CA2948585C (da) |
| CY (1) | CY1122631T1 (da) |
| DK (2) | DK3149019T3 (da) |
| EA (1) | EA032820B1 (da) |
| ES (2) | ES2938874T3 (da) |
| FI (1) | FI3626725T3 (da) |
| HR (2) | HRP20230170T1 (da) |
| HU (2) | HUE061506T2 (da) |
| LT (2) | LT3149019T (da) |
| MA (1) | MA39881B1 (da) |
| MX (2) | MX373721B (da) |
| PH (1) | PH12016502327A1 (da) |
| PL (2) | PL3626725T3 (da) |
| PT (2) | PT3149019T (da) |
| RS (2) | RS64050B1 (da) |
| SG (2) | SG10201809362RA (da) |
| SI (2) | SI3626725T1 (da) |
| SM (2) | SMT202000070T1 (da) |
| WO (1) | WO2015181275A1 (da) |
Families Citing this family (52)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2545964A1 (en) | 2011-07-13 | 2013-01-16 | Phenex Pharmaceuticals AG | Novel FXR (NR1H4) binding and activity modulating compounds |
| 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 |
| WO2016045480A1 (zh) * | 2014-09-28 | 2016-03-31 | 上海源力生物技术有限公司 | 一种奥贝胆酸的制备方法 |
| 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 |
| CN111944006B (zh) * | 2014-11-17 | 2021-12-17 | 正大天晴药业集团股份有限公司 | 新的7-酮-6β-烷基胆烷酸衍生物在制备奥贝胆酸以及其在医药领域的用途 |
| 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 |
| 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 |
| 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 |
| 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 |
| US10208081B2 (en) | 2014-11-26 | 2019-02-19 | Enanta Pharmaceuticals, Inc. | Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof |
| RU2017121457A (ru) | 2014-11-26 | 2018-12-26 | Энанта Фармасьютикалс, Инк. | Аналоги желчной кислоты в качестве агонистов fxr/tgr5 и способы их применения |
| WO2016086115A1 (en) | 2014-11-26 | 2016-06-02 | Enanta Pharmaceuticals, Inc. | Tetrazole derivatives of bile acids as fxr/tgr5 agonists and methods of use thereof |
| AU2016219266A1 (en) | 2015-02-11 | 2017-08-10 | Enanta Pharmaceuticals, Inc. | Bile acid analogs as FXR/TGR5 agonists and methods of use thereof |
| RU2712099C2 (ru) | 2015-03-31 | 2020-01-24 | Энанта Фармасьютикалс, Инк. | Производные желчных кислот в качестве агонистов fxr/tgr5 и способы их применения |
| DK3310801T3 (da) * | 2015-06-19 | 2021-06-21 | Intercept Pharmaceuticals Inc | Tgr5-modulatorer og fremgangsmåder til anvendelse deraf |
| KR20180052756A (ko) | 2015-09-24 | 2018-05-18 | 인터셉트 파마슈티컬즈, 인크. | 담즙산 유도체 제조를 위한 방법 및 중간체 |
| US10364267B2 (en) | 2016-02-23 | 2019-07-30 | Enanta Pharmaceuticals, Inc. | Deuterated bile acid derivatives as FXR/TGR5 agonists and methods of use thereof |
| WO2017147174A1 (en) * | 2016-02-23 | 2017-08-31 | Enanta Pharmaceuticals, Inc. | Heteroaryl containing bile acid analogs as fxr/tgr5 agonists and methods of use thereof |
| US10323060B2 (en) | 2016-02-23 | 2019-06-18 | Enanta Pharmaceuticals, Inc. | Benzoic acid derivatives of bile acid as FXR/TGR5 agonists and methods of use thereof |
| EA038632B1 (ru) * | 2016-03-11 | 2021-09-27 | Интерсепт Фармасьютикалз, Инк. | 7,11-дигидрокси-6-этил-5-холан-24-овая кислота и фармацевтические композиции на ее основе для лечения или предупреждения заболевания или состояния, опосредованных фарнезоидным х-рецептором (fxr) |
| CN105859817A (zh) * | 2016-05-09 | 2016-08-17 | 成都宇西医药技术有限公司 | 一种制备3α-羟基-6-乙烯基-7-酮基-5β-胆烷酸的方法 |
| GB201608777D0 (en) | 2016-05-18 | 2016-06-29 | Dextra Lab Ltd | Compounds |
| WO2017207648A1 (en) | 2016-05-31 | 2017-12-07 | Bionice, S.L.U | Process and intermediates for the preparation of obeticholic acid and derivatives thereof |
| EP3464316A4 (en) * | 2016-06-01 | 2020-02-19 | Dr. Reddy's Laboratories Ltd. | PROCESS FOR THE PREPARATION OF OBETICHOLIC ACID |
| CA2968836C (en) | 2016-06-13 | 2025-09-02 | Gilead Sciences, Inc. | FXR MODULATING COMPOUNDS (NR1H4) |
| NZ748641A (en) | 2016-06-13 | 2020-04-24 | Gilead Sciences Inc | Fxr (nr1h4) modulating compounds |
| IT201600068742A1 (it) * | 2016-07-01 | 2018-01-01 | Bar Pharmaceuticals Soc A Responsabilita Limitata | Derivati dell'acido iodesossicolico e loro uso |
| AU2017368069B2 (en) | 2016-11-29 | 2021-07-08 | Enanta Pharmaceuticals, Inc. | Process for preparation of sulfonylurea bile acid derivatives |
| US10472386B2 (en) | 2017-02-14 | 2019-11-12 | Enanta Pharmaceuticals, Inc. | Bile acid derivatives as FXR agonists and methods of use thereof |
| ES2982801T3 (es) | 2017-03-28 | 2024-10-17 | Gilead Sciences Inc | Combinaciones terapéuticas para el tratamiento de las enfermedades hepáticas |
| MX388300B (es) * | 2017-04-07 | 2025-03-19 | Enanta Pharm Inc | Proceso para la preparación de derivados de ácidos biliares de sulfonil carbamato |
| CN109021054B (zh) * | 2017-06-09 | 2021-04-09 | 博瑞生物医药（苏州）股份有限公司 | 一种fxr激动剂 |
| CN109021055B (zh) * | 2017-06-09 | 2021-04-09 | 博瑞生物医药（苏州）股份有限公司 | Fxr激动剂 |
| 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 |
| US11059854B2 (en) * | 2017-07-26 | 2021-07-13 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Method for preparing steroid derivative FXR agonist |
| WO2019085963A1 (zh) * | 2017-11-02 | 2019-05-09 | 正大天晴药业集团股份有限公司 | 一种胆酸类化合物的制备方法 |
| KR102692309B1 (ko) | 2019-01-15 | 2024-08-07 | 길리애드 사이언시즈, 인코포레이티드 | Fxr (nr1h4) 조정 화합물 |
| WO2020172075A1 (en) | 2019-02-19 | 2020-08-27 | Gilead Sciences, Inc. | Solid forms of fxr agonists |
| JP2022552655A (ja) | 2019-10-07 | 2022-12-19 | キャリーオペ，インク． | Ｇｐｒ１１９アゴニスト |
| CN112824425B (zh) * | 2019-11-21 | 2023-10-03 | 成都西岭源药业有限公司 | 一种6-位烯基取代胆酸化合物及其制备方法和应用 |
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