MX2017010376A - Análogos de ácido biliar como agonistas de fxr/tgr5 y métodos para el uso de los mismos. - Google Patents
Análogos de ácido biliar como agonistas de fxr/tgr5 y métodos para el uso de los mismos.Info
- Publication number
- MX2017010376A MX2017010376A MX2017010376A MX2017010376A MX2017010376A MX 2017010376 A MX2017010376 A MX 2017010376A MX 2017010376 A MX2017010376 A MX 2017010376A MX 2017010376 A MX2017010376 A MX 2017010376A MX 2017010376 A MX2017010376 A MX 2017010376A
- Authority
- MX
- Mexico
- Prior art keywords
- disease
- fxr
- methods
- bile acid
- acid analogs
- Prior art date
Links
- HSINOMROUCMIEA-FGVHQWLLSA-N (2s,4r)-4-[(3r,5s,6r,7r,8s,9s,10s,13r,14s,17r)-6-ethyl-3,7-dihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthren-17-yl]-2-methylpentanoic acid Chemical class C([C@@]12C)C[C@@H](O)C[C@H]1[C@@H](CC)[C@@H](O)[C@@H]1[C@@H]2CC[C@]2(C)[C@@H]([C@H](C)C[C@H](C)C(O)=O)CC[C@H]21 HSINOMROUCMIEA-FGVHQWLLSA-N 0.000 title 1
- 239000000556 agonist Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 3
- 102100025353 G-protein coupled bile acid receptor 1 Human genes 0.000 abstract 2
- 101000857733 Homo sapiens G-protein coupled bile acid receptor 1 Proteins 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 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 abstract 1
- 208000023275 Autoimmune disease Diseases 0.000 abstract 1
- 208000020446 Cardiac disease Diseases 0.000 abstract 1
- 208000018522 Gastrointestinal disease Diseases 0.000 abstract 1
- 208000008839 Kidney Neoplasms Diseases 0.000 abstract 1
- 206010038389 Renal cancer Diseases 0.000 abstract 1
- 208000010643 digestive system disease Diseases 0.000 abstract 1
- 208000016097 disease of metabolism Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 208000018685 gastrointestinal system disease Diseases 0.000 abstract 1
- 208000019622 heart disease Diseases 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 201000010982 kidney cancer Diseases 0.000 abstract 1
- 208000017169 kidney disease Diseases 0.000 abstract 1
- 208000019423 liver disease Diseases 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 208000030159 metabolic disease Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
-
- 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
- C07J41/0055—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of at least three carbon atoms which may or may not be branched, e.g. cholane or cholestane derivatives, optionally cyclised, e.g. 17-beta-phenyl or 17-beta-furyl derivatives
- C07J41/0061—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of at least three carbon atoms which may or may not be branched, e.g. cholane or cholestane derivatives, optionally cyclised, e.g. 17-beta-phenyl or 17-beta-furyl derivatives one of the carbon atoms being part of an amide group
-
- 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
- A61P1/16—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
- A61P3/04—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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- 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
- 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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
- C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Immunology (AREA)
- Urology & Nephrology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Virology (AREA)
- Transplantation (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Vascular Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
La presente invención proporciona compuestos de Fórmula I, composiciones farmacéuticas que comprenden estos compuestos y métodos para usar estos compuestos para tratar o prevenir una enfermedad o trastorno mediadao por FXR y/o TGR5. En ciertas modalidades, una enfermedad que conlleva la modulación del receptor TGR5 es seleccionado de enfermedad metabólica, enfermedad inflamatoria, enfermedad hepática, enfermedad autoinmune, enfermedad cardíaca, enfermedad renal, cáncer, y enfermedad gastroinstestinal. (Ver Fórmula I).
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562114773P | 2015-02-11 | 2015-02-11 | |
| PCT/US2016/017554 WO2016130809A1 (en) | 2015-02-11 | 2016-02-11 | Bile acid analogs as fxr/tgr5 agonists and methods of use thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX2017010376A true MX2017010376A (es) | 2017-12-20 |
Family
ID=56565728
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2017010376A MX2017010376A (es) | 2015-02-11 | 2016-02-11 | Análogos de ácido biliar como agonistas de fxr/tgr5 y métodos para el uso de los mismos. |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US10246483B2 (es) |
| EP (1) | EP3256134A4 (es) |
| JP (1) | JP2018505190A (es) |
| KR (1) | KR20170133339A (es) |
| CN (1) | CN107249594A (es) |
| AU (1) | AU2016219266A1 (es) |
| BR (1) | BR112017017238A2 (es) |
| CA (1) | CA2975257A1 (es) |
| HK (1) | HK1245100A1 (es) |
| MX (1) | MX2017010376A (es) |
| PH (1) | PH12017501339A1 (es) |
| RU (1) | RU2017130466A (es) |
| SG (1) | SG11201706089RA (es) |
| WO (1) | WO2016130809A1 (es) |
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|---|---|---|---|---|
| WO2016073767A1 (en) | 2014-11-06 | 2016-05-12 | Enanta Pharmaceuticals, Inc. | Bile acid analogs an fxr/tgr5 agonists and methods of use thereof |
| US11578097B2 (en) | 2014-11-26 | 2023-02-14 | Enanta Pharmaceuticals, Inc. | Tetrazole derivatives of bile acids as FXR/TGR5 agonists and methods of use thereof |
| JP2017535570A (ja) | 2014-11-26 | 2017-11-30 | エナンタ ファーマシューティカルズ インコーポレイテッド | Fxr/tgr5アゴニストとしての胆汁酸類似体およびその使用方法 |
| US10208081B2 (en) | 2014-11-26 | 2019-02-19 | Enanta Pharmaceuticals, Inc. | Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof |
| CA2981503C (en) | 2015-03-31 | 2023-09-19 | Enanta Pharmaceuticals, Inc. | Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof |
| US10517321B2 (en) | 2015-07-10 | 2019-12-31 | Sweet Green Fields USA LLC | Compositions of steviol multiglycosylated derivatives and stevia components |
| 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 |
| WO2017147159A1 (en) | 2016-02-23 | 2017-08-31 | Enanta Pharmaceuticals, Inc. | Deuterated bile acid derivatives 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 |
| CN106237332A (zh) * | 2016-08-11 | 2016-12-21 | 河南大学 | 核受体fxr在肝癌干细胞靶向治疗中的应用 |
| CA3045023A1 (en) | 2016-11-29 | 2018-06-07 | 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 |
| CA3058754A1 (en) | 2017-04-07 | 2018-10-11 | Enanta Pharmaceuticals, Inc. | Process for preparation of sulfonyl carbamate bile acid derivatives |
| JP7224307B2 (ja) | 2017-06-23 | 2023-02-17 | インターセプト ファーマシューティカルズ, インコーポレイテッド | 胆汁酸誘導体の調製のための方法及び中間体 |
| GB201812382D0 (en) | 2018-07-30 | 2018-09-12 | Nzp Uk Ltd | Compounds |
| EP3999101A1 (en) | 2019-07-18 | 2022-05-25 | ENYO Pharma | Method for decreasing adverse-effects of interferon |
| KR20220150270A (ko) | 2019-10-07 | 2022-11-10 | 칼리오페, 인크. | Gpr119 효능제 |
| WO2021144330A1 (en) | 2020-01-15 | 2021-07-22 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Use of fxr agonists for treating an infection by hepatitis d virus |
| TW202140440A (zh) | 2020-02-28 | 2021-11-01 | 美商克力歐普股份有限公司 | Gpr40激動劑 |
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| CN116390925A (zh) | 2020-06-26 | 2023-07-04 | 卡尔优普公司 | Ampk活化剂 |
| KR20230154806A (ko) | 2021-01-14 | 2023-11-09 | 엔요 파마 | Hbv 감염 치료를 위한 fxr 작용제 및 ifn의 상승작용효과 |
| CN117320722A (zh) | 2021-04-28 | 2023-12-29 | 埃尼奥制药公司 | 使用fxr激动剂作为联合治疗强烈增强tlr3激动剂的作用 |
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| CN105175473B (zh) | 2015-08-19 | 2018-12-21 | 丽珠医药集团股份有限公司 | 一种奥贝胆酸晶型i及其制备方法、药物组合物和用途 |
| CN106478759A (zh) | 2015-08-31 | 2017-03-08 | 陕西合成药业股份有限公司 | 奥贝胆酸衍生物及其制备方法和用途 |
| CN106518946A (zh) | 2015-09-10 | 2017-03-22 | 上海迪诺医药科技有限公司 | 磺酰脲衍生物、其药物组合物及应用 |
| EP3353189A4 (en) | 2015-09-24 | 2019-06-19 | Intercept Pharmaceuticals, Inc. | METHOD AND INTERMEDIATE PRODUCTS FOR THE PREPARATION OF GALLENIC ACID DERIVATIVES |
| EP3981779A1 (en) | 2015-10-07 | 2022-04-13 | Intercept Pharmaceuticals, Inc. | Farnesoid x receptor modulators |
| US10875888B2 (en) | 2016-01-28 | 2020-12-29 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Steroid derivative FXR agonist |
| 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 |
| WO2017147159A1 (en) | 2016-02-23 | 2017-08-31 | Enanta Pharmaceuticals, Inc. | Deuterated bile acid derivatives 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 |
| EP3426348B1 (en) | 2016-03-11 | 2021-05-05 | Intercept Pharmaceuticals, Inc. | 3-desoxy derivative and pharmaceutical compositions thereof |
| US10472386B2 (en) | 2017-02-14 | 2019-11-12 | Enanta Pharmaceuticals, Inc. | Bile acid derivatives as FXR agonists and methods of use thereof |
-
2016
- 2016-02-11 MX MX2017010376A patent/MX2017010376A/es unknown
- 2016-02-11 RU RU2017130466A patent/RU2017130466A/ru unknown
- 2016-02-11 US US15/041,811 patent/US10246483B2/en active Active
- 2016-02-11 CA CA2975257A patent/CA2975257A1/en not_active Abandoned
- 2016-02-11 KR KR1020177025456A patent/KR20170133339A/ko not_active Withdrawn
- 2016-02-11 WO PCT/US2016/017554 patent/WO2016130809A1/en not_active Ceased
- 2016-02-11 JP JP2017541843A patent/JP2018505190A/ja active Pending
- 2016-02-11 CN CN201680010001.1A patent/CN107249594A/zh active Pending
- 2016-02-11 SG SG11201706089RA patent/SG11201706089RA/en unknown
- 2016-02-11 BR BR112017017238A patent/BR112017017238A2/pt not_active Application Discontinuation
- 2016-02-11 AU AU2016219266A patent/AU2016219266A1/en not_active Abandoned
- 2016-02-11 HK HK18104548.9A patent/HK1245100A1/zh unknown
- 2016-02-11 EP EP16749885.6A patent/EP3256134A4/en not_active Withdrawn
-
2017
- 2017-07-25 PH PH12017501339A patent/PH12017501339A1/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CA2975257A1 (en) | 2016-08-18 |
| AU2016219266A1 (en) | 2017-08-10 |
| BR112017017238A2 (pt) | 2018-04-10 |
| RU2017130466A (ru) | 2019-03-12 |
| JP2018505190A (ja) | 2018-02-22 |
| SG11201706089RA (en) | 2017-09-28 |
| US20160229886A1 (en) | 2016-08-11 |
| KR20170133339A (ko) | 2017-12-05 |
| EP3256134A1 (en) | 2017-12-20 |
| PH12017501339A1 (en) | 2017-12-18 |
| CN107249594A (zh) | 2017-10-13 |
| WO2016130809A1 (en) | 2016-08-18 |
| US10246483B2 (en) | 2019-04-02 |
| HK1245100A1 (zh) | 2018-08-24 |
| EP3256134A4 (en) | 2018-10-03 |
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