SG11201805235XA - Polymorphic crystalline forms of obeticholic acid - Google Patents
Polymorphic crystalline forms of obeticholic acidInfo
- Publication number
- SG11201805235XA SG11201805235XA SG11201805235XA SG11201805235XA SG11201805235XA SG 11201805235X A SG11201805235X A SG 11201805235XA SG 11201805235X A SG11201805235X A SG 11201805235XA SG 11201805235X A SG11201805235X A SG 11201805235XA SG 11201805235X A SG11201805235X A SG 11201805235XA
- Authority
- SG
- Singapore
- Prior art keywords
- international
- cambridge
- owe
- crystalline forms
- obeticholic acid
- Prior art date
Links
- 229960001601 obeticholic acid Drugs 0.000 title abstract 4
- ZXERDUOLZKYMJM-ZWECCWDJSA-N obeticholic acid Chemical compound 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)CCC(O)=O)CC[C@H]21 ZXERDUOLZKYMJM-ZWECCWDJSA-N 0.000 title abstract 3
- 239000003795 chemical substances by application Substances 0.000 abstract 2
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 abstract 2
- 239000003814 drug Substances 0.000 abstract 2
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- 206010008635 Cholestasis Diseases 0.000 abstract 1
- 206010016654 Fibrosis Diseases 0.000 abstract 1
- 241000124008 Mammalia Species 0.000 abstract 1
- LUTSRLYCMSCGCS-BWOMAWGNSA-N [(3s,8r,9s,10r,13s)-10,13-dimethyl-17-oxo-1,2,3,4,7,8,9,11,12,16-decahydrocyclopenta[a]phenanthren-3-yl] acetate Chemical compound C([C@@H]12)C[C@]3(C)C(=O)CC=C3[C@@H]1CC=C1[C@]2(C)CC[C@H](OC(=O)C)C1 LUTSRLYCMSCGCS-BWOMAWGNSA-N 0.000 abstract 1
- 235000012000 cholesterol Nutrition 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 230000004761 fibrosis Effects 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 230000008520 organization Effects 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 238000000746 purification Methods 0.000 abstract 1
- 102220240796 rs553605556 Human genes 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
- 150000003626 triacylglycerols Chemical class 0.000 abstract 1
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
- 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
- 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
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
-
- 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
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J17/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta(a)hydrophenanthrene skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
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)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Virology (AREA)
- Urology & Nephrology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Molecular Biology (AREA)
- Diabetes (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Gastroenterology & Hepatology (AREA)
- Steroid Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US14/979,005 US9982008B2 (en) | 2012-06-19 | 2015-12-22 | Preparation and uses of obeticholic acid |
| PCT/US2016/012651 WO2017111979A1 (en) | 2015-12-22 | 2016-01-08 | Polymorphic crystalline forms of obeticholic acid |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SG11201805235XA true SG11201805235XA (en) | 2018-07-30 |
Family
ID=55650649
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG11201805235XA SG11201805235XA (en) | 2015-12-22 | 2016-01-08 | Polymorphic crystalline forms of obeticholic acid |
Country Status (15)
| Country | Link |
|---|---|
| EP (1) | EP3394081A1 (https=) |
| JP (1) | JP2018538331A (https=) |
| KR (1) | KR20180095070A (https=) |
| CN (1) | CN108495858A (https=) |
| AU (1) | AU2016375566A1 (https=) |
| BR (1) | BR112018012590A2 (https=) |
| CA (1) | CA3009149A1 (https=) |
| CL (1) | CL2018001720A1 (https=) |
| CO (1) | CO2018006701A2 (https=) |
| EA (1) | EA201891491A1 (https=) |
| IL (1) | IL259998A (https=) |
| MX (1) | MX2018007776A (https=) |
| PH (1) | PH12018501318A1 (https=) |
| SG (1) | SG11201805235XA (https=) |
| WO (1) | WO2017111979A1 (https=) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105801653B (zh) * | 2014-12-30 | 2018-04-17 | 苏州晶云药物科技有限公司 | 奥贝胆酸的晶型a及其制备方法 |
| WO2018211413A1 (en) * | 2017-05-15 | 2018-11-22 | Dr. Reddy’S Laboratories Limited | Solid forms of obeticholic acid and process for preparation |
| CN109280071A (zh) * | 2017-07-19 | 2019-01-29 | 东莞东阳光药物研发有限公司 | 奥贝胆酸的晶型及其制备方法 |
| CN107383139A (zh) * | 2017-08-09 | 2017-11-24 | 杭州和泽医药科技有限公司 | 一种3α‑羟基‑7‑氧代‑5β‑胆烷酸新衍生物制备奥贝胆酸的方法 |
| CZ31099U1 (cs) * | 2017-09-05 | 2017-10-17 | Zentiva, K.S. | Krystalické formy (3a,5B,6a,7a)-6-ethyl-3,7- dihydroxycholan-24-ové kyseliny |
| CN109485687A (zh) * | 2017-09-12 | 2019-03-19 | 成都弘达药业有限公司 | 奥贝胆酸的晶型j及其制备方法 |
| WO2019106043A1 (en) | 2017-11-29 | 2019-06-06 | Hexal Ag | Pharmaceutical composition comprising obeticholic acid |
| GB201812382D0 (en) | 2018-07-30 | 2018-09-12 | Nzp Uk Ltd | Compounds |
| CN113264972B (zh) * | 2020-02-14 | 2024-07-12 | 四川科伦药物研究院有限公司 | 一种制备奥贝胆酸的方法 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| SI3336097T1 (sl) * | 2012-06-19 | 2021-07-30 | Intercept Pharmaceuticals, Inc. | Priprava nekristalinične oblike obetiholne kisline |
| CN106459136B (zh) * | 2014-09-28 | 2018-06-26 | 江苏盛迪医药有限公司 | 一种奥贝胆酸的制备方法 |
| 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 |
| KR102546748B1 (ko) * | 2014-11-19 | 2023-06-22 | 엔제트피 유케이 리미티드 | 스테로이드 FXR 조절인자를 제조하기 위한 중간체로서의 6α-알킬-3,7-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 |
-
2016
- 2016-01-08 JP JP2018532396A patent/JP2018538331A/ja active Pending
- 2016-01-08 CN CN201680079793.8A patent/CN108495858A/zh active Pending
- 2016-01-08 EA EA201891491A patent/EA201891491A1/ru unknown
- 2016-01-08 CA CA3009149A patent/CA3009149A1/en not_active Abandoned
- 2016-01-08 AU AU2016375566A patent/AU2016375566A1/en not_active Abandoned
- 2016-01-08 KR KR1020187020850A patent/KR20180095070A/ko not_active Withdrawn
- 2016-01-08 SG SG11201805235XA patent/SG11201805235XA/en unknown
- 2016-01-08 BR BR112018012590A patent/BR112018012590A2/pt not_active Application Discontinuation
- 2016-01-08 WO PCT/US2016/012651 patent/WO2017111979A1/en not_active Ceased
- 2016-01-08 EP EP16714049.0A patent/EP3394081A1/en not_active Withdrawn
- 2016-01-08 MX MX2018007776A patent/MX2018007776A/es unknown
-
2018
- 2018-06-13 IL IL259998A patent/IL259998A/en unknown
- 2018-06-20 PH PH12018501318A patent/PH12018501318A1/en unknown
- 2018-06-22 CL CL2018001720A patent/CL2018001720A1/es unknown
- 2018-06-27 CO CONC2018/0006701A patent/CO2018006701A2/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CA3009149A1 (en) | 2017-06-29 |
| CL2018001720A1 (es) | 2018-08-10 |
| KR20180095070A (ko) | 2018-08-24 |
| PH12018501318A1 (en) | 2019-02-18 |
| IL259998A (en) | 2018-07-31 |
| BR112018012590A2 (pt) | 2018-12-04 |
| CO2018006701A2 (es) | 2018-07-10 |
| EA201891491A1 (ru) | 2018-11-30 |
| EP3394081A1 (en) | 2018-10-31 |
| CN108495858A (zh) | 2018-09-04 |
| WO2017111979A1 (en) | 2017-06-29 |
| JP2018538331A (ja) | 2018-12-27 |
| MX2018007776A (es) | 2018-08-09 |
| AU2016375566A1 (en) | 2018-07-05 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| SG11201805235XA (en) | Polymorphic crystalline forms of obeticholic acid | |
| SG11201408501UA (en) | Preparation, uses and solid forms of obeticholic acid | |
| SG11201906209SA (en) | Bicyclic compounds as allosteric shp2 inhibitors | |
| SG11201407662WA (en) | Process for the preparation of treprostinil and derivatives thereof | |
| SG11201906412SA (en) | Pyridine compounds as allosteric shp2 inhibitors | |
| SG11201803686UA (en) | Prodrugs of a jak inhibitor compound for treatment of gastrointestinal inflammatory disease | |
| SG11201809344QA (en) | Process for synthesizing 2-hydroxy-6-((2-(1-isopropyl-1h-pyrazol-5-yl)-pyridin-3-yl)methoxy)benzaldehyde | |
| SG11201804170RA (en) | Polycyclic tlr7/8 antagonists and use thereof in the treatment of immune disorders | |
| SG11201901140QA (en) | Compounds and methods for reducing tau expression | |
| SG11201900745VA (en) | Substituted thiazolo-pyridine compounds as malt1 inhibitors | |
| SG11201808003RA (en) | Bromodomain inhibitors | |
| SG11201909960UA (en) | Methods for improving memory and cognition and for treating memory and cognitive disorders | |
| SG11201900349VA (en) | Somatostatin modulators and uses thereof | |
| SG11201807012QA (en) | Acid addition salts of piperazine derivatives | |
| SG11201804647TA (en) | Dosing regimens for 2-hydroxy-6-((2-(1-isopropyl-1h-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde | |
| SG11201807784SA (en) | 3-desoxy derivative and pharmaceutical compositions thereof | |
| SG11201811230RA (en) | Compositions and methods for reducing ocular neovascularization | |
| SG11201804811WA (en) | Fenfluramine compositions and methods of preparing the same | |
| SG11201810177VA (en) | Pet-imaging immunomodulators | |
| SG11201408251SA (en) | A pharmaceutical composition containing nicotinic acid and/or nicotinamide and/or tryptophan for positively influencing the intestinal microbiota | |
| SG11201807597UA (en) | Methods of treating depression using orexin-2 receptor antagonists | |
| SG11201908512YA (en) | Somatostatin modulators and uses thereof | |
| SG11201407402TA (en) | Carbazole-containing sulfonamides as cryptochrome modulators | |
| SG11201808713YA (en) | Ophthalmic compositions comprising levodopa, an antioxidant and an aqueous carrier | |
| SG11201804100UA (en) | Pharmaceutical composition comprising a potent inhibitor of urat1 |