EA200000888A1 - Производные желчных кислот - Google Patents
Производные желчных кислотInfo
- Publication number
- EA200000888A1 EA200000888A1 EA200000888A EA200000888A EA200000888A1 EA 200000888 A1 EA200000888 A1 EA 200000888A1 EA 200000888 A EA200000888 A EA 200000888A EA 200000888 A EA200000888 A EA 200000888A EA 200000888 A1 EA200000888 A1 EA 200000888A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- bile
- fatty acids
- acid
- acids
- bile acid
- Prior art date
Links
- 239000002253 acid Substances 0.000 title 1
- 150000007513 acids Chemical class 0.000 title 1
- 239000003833 bile salt Substances 0.000 abstract 4
- 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 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)C[C@H](C)C(O)=O)CC[C@H]21 HSINOMROUCMIEA-FGVHQWLLSA-N 0.000 abstract 3
- 239000003613 bile acid Substances 0.000 abstract 3
- 235000014113 dietary fatty acids Nutrition 0.000 abstract 3
- 229930195729 fatty acid Natural products 0.000 abstract 3
- 239000000194 fatty acid Substances 0.000 abstract 3
- 150000004665 fatty acids Chemical class 0.000 abstract 3
- 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
- 150000001875 compounds Chemical class 0.000 abstract 2
- 150000004671 saturated fatty acids Chemical class 0.000 abstract 2
- 235000003441 saturated fatty acids Nutrition 0.000 abstract 2
- 201000001320 Atherosclerosis Diseases 0.000 abstract 1
- 210000000941 bile Anatomy 0.000 abstract 1
- 239000003858 bile acid conjugate Substances 0.000 abstract 1
- 229940093761 bile salts Drugs 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 201000001883 cholelithiasis Diseases 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
- 238000000034 method Methods 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
-
- 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
-
- 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
- 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
- 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
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
- C07J41/0005—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring the nitrogen atom being directly linked to the cyclopenta(a)hydro phenanthrene skeleton
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Gastroenterology & Hepatology (AREA)
- Steroid Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Fats And Perfumes (AREA)
Abstract
Данное изобретение относится к конъюгатам (продуктам соединения) желчных кислот или желчных солей с жирными кислотами, называемым «BAFAC», к их использованию для растворения холестериновых желчных конкрементов в желчи, предотвращения их появления или рецидива, к их использованию для ослабления или профилактики атеросклероза и способам лечения указанных заболеваний. Конъюгаты желчной кислоты имеют общую формулу W-X-G, в которой G представляет собой радикал желчной кислоты или желчной соли, W представляет собой один или два радикала насыщенных жирных кислот и X представляет собой направленную связь или связующий элемент между указанной желчной кислотой или желчной солью и жирной кислотой(ами). Соединение преимущественно выполнено в положении, выбранном из 3, 6, 7, 12 и 24 положений кольца желчной кислоты или желчной соли. Жирные кислоты являются преимущественно насыщенными жирными кислотами, имеющими 14-22 атомов углерода.Международная заявка была опубликована вместе с отчетом о международном поиске.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IL12399898A IL123998A (en) | 1998-04-08 | 1998-04-08 | Conjugates of bile salts and pharmaceutical preparations containing them |
| PCT/IL1999/000173 WO1999052932A1 (en) | 1998-04-08 | 1999-03-25 | Fatty acid derivatives of bile acids and bile acid derivatives |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA200000888A1 true EA200000888A1 (ru) | 2001-04-23 |
| EA003392B1 EA003392B1 (ru) | 2003-04-24 |
Family
ID=11071405
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA200000888A EA003392B1 (ru) | 1998-04-08 | 1999-03-25 | Производные желчных кислот |
Country Status (25)
| Country | Link |
|---|---|
| US (3) | US6395722B1 (ru) |
| EP (1) | EP1071702B1 (ru) |
| JP (1) | JP5031942B2 (ru) |
| KR (1) | KR100615560B1 (ru) |
| CN (1) | CN100386339C (ru) |
| AT (1) | ATE222923T1 (ru) |
| AU (1) | AU742944B2 (ru) |
| BR (1) | BRPI9909908B8 (ru) |
| CA (1) | CA2325933C (ru) |
| CZ (1) | CZ300824B6 (ru) |
| DE (1) | DE69902647T2 (ru) |
| DK (1) | DK1071702T3 (ru) |
| EA (1) | EA003392B1 (ru) |
| ES (1) | ES2183526T3 (ru) |
| HU (1) | HU229513B1 (ru) |
| ID (1) | ID26042A (ru) |
| IL (1) | IL123998A (ru) |
| NO (1) | NO316875B1 (ru) |
| NZ (1) | NZ507309A (ru) |
| PL (1) | PL199271B1 (ru) |
| PT (1) | PT1071702E (ru) |
| SI (1) | SI1071702T1 (ru) |
| TR (1) | TR200002876T2 (ru) |
| UA (1) | UA70318C2 (ru) |
| WO (1) | WO1999052932A1 (ru) |
Families Citing this family (45)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL123998A (en) * | 1998-04-08 | 2004-09-27 | Galmed Int Ltd | Conjugates of bile salts and pharmaceutical preparations containing them |
| IL142650A (en) * | 1998-04-08 | 2007-06-03 | Galmed Int Ltd | Use of bile acid conjugates or bile salts and fatty acids or fatty acids in the preparation of pharmaceuticals for lowering cholesterol, for the treatment of fatty liver and for the treatment of hyperglycemia and diabetes |
| US20030083231A1 (en) * | 1998-11-24 | 2003-05-01 | Ahlem Clarence N. | Blood cell deficiency treatment method |
| US8975246B2 (en) | 2001-04-17 | 2015-03-10 | Galmed Research And Development Ltd. | Bile acid or bile salt fatty acid conjugates |
| US7053076B2 (en) | 2001-08-29 | 2006-05-30 | Xenoport, Inc. | Bile-acid derived compounds for enhancing oral absorption and systemic bioavailability of drugs |
| ITMI20021025A1 (it) * | 2002-05-14 | 2003-11-14 | Nicox Sa | Farmaci per il trattamento acuto di disfunzioni del circolo venoso epatico e portale |
| US20080026077A1 (en) * | 2002-11-12 | 2008-01-31 | John Hilfinger | Methods and compositions of gene delivery agents for systemic and local therapy |
| US7906137B2 (en) * | 2004-05-21 | 2011-03-15 | Mediplex Corporation, Korea | Delivery agents for enhancing mucosal absorption of therapeutic agents |
| WO2007084549A2 (en) * | 2006-01-20 | 2007-07-26 | Filiberto Zadini | Drug-eluting stent with atherosclerotic plaques dissolving pharmacological preparation |
| US8304383B2 (en) | 2005-11-22 | 2012-11-06 | Atheronova Operations, Inc. | Dissolution of arterial plaque |
| US20090035348A1 (en) * | 2005-11-22 | 2009-02-05 | Z & Z Medical Holdings, Inc. | Dissolution of arterial plaque |
| US20070212470A1 (en) * | 2006-03-13 | 2007-09-13 | Nutracea | Therapeutic uses of an anti-cancer composition derived from rice bran |
| US20080038385A1 (en) * | 2006-03-13 | 2008-02-14 | Nutracea | Therapeutic uses of an anti-cancer composition derived from rice bran |
| US20090305943A1 (en) * | 2006-07-18 | 2009-12-10 | Sven Siegel | Cyclodextrin blends with crystal growth inhibitors |
| AU2008242583B2 (en) | 2007-04-23 | 2013-10-10 | Alnylam Pharmaceuticals, Inc. | Glycoconjugates of RNA interference agents |
| WO2008144458A1 (en) * | 2007-05-15 | 2008-11-27 | Z & Z Medical Holdings, Inc. | Dissolution of arterial cholesterol plaques by pharmacologically induced elevation of endogenous bile salts |
| PT2182954T (pt) * | 2007-07-25 | 2019-02-06 | Univ Graz Medizinische | Utilização de ácidos nor-biliares no tratamento de arteriosclerose |
| CN101367859B (zh) * | 2007-08-17 | 2011-05-11 | 中国人民解放军军事医学科学院毒物药物研究所 | 脂肪酸胆汁酸偶合物及其医药用途 |
| CZ301037B6 (cs) * | 2007-09-06 | 2009-10-21 | Vysoká škola chemicko-technologická v Praze | Amidové konjugáty steroidních a žlucových kyselin s D-glukosaminem a zpusob jejich prípravy |
| CA2708171C (en) | 2007-12-04 | 2018-02-27 | Alnylam Pharmaceuticals, Inc. | Folate conjugates |
| CA2910760C (en) | 2007-12-04 | 2019-07-09 | Muthiah Manoharan | Targeting lipids |
| US20100021538A1 (en) * | 2008-02-29 | 2010-01-28 | Youngro Byun | Pharmaceutical compositions containing heparin derivatives |
| WO2009126933A2 (en) | 2008-04-11 | 2009-10-15 | Alnylam Pharmaceuticals, Inc. | Site-specific delivery of nucleic acids by combining targeting ligands with endosomolytic components |
| EP2367839A4 (en) * | 2008-11-03 | 2012-07-04 | Univ Tufts | METHODS AND COMPOSITIONS FOR PREVENTING GERMINATION AND EXCROIDANCE OF C. DIFFICILE SPORES |
| EP2391370B1 (en) * | 2009-02-02 | 2015-06-03 | Galmed Research and Development Ltd. | Methods and compositions for treating alzheimer's disease |
| GB2480632A (en) | 2010-05-25 | 2011-11-30 | Kythera Biopharmaceuticals Inc | Preparation of 12-keto and 12-alpha-hydroxy steroids |
| CN102115486B (zh) * | 2009-12-30 | 2015-06-03 | 上海特化医药科技有限公司 | 一种3-β-花生酰胺基-7α,12α,5β-胆烷-24-羧酸的制备方法 |
| TWI572616B (zh) * | 2011-06-16 | 2017-03-01 | 凱瑟拉生物製藥有限公司 | 去氧膽酸之組成物及用途及其相關方法 |
| JP2016527307A (ja) * | 2013-08-08 | 2016-09-08 | ガルデルム セラピューティクス リミテッド | 胆汁酸−脂肪酸抱合体を含む抗座瘡組成物 |
| PT3077047T (pt) * | 2013-12-04 | 2019-07-11 | Galmed Res & Development Ltd | Sais de aramchol |
| US11571431B2 (en) | 2013-12-04 | 2023-02-07 | Galmed Research And Development Ltd | Aramchol salts |
| EP3148549A4 (en) * | 2014-06-01 | 2017-11-15 | Galmed Research and Development Ltd. | Fatty acid bile acid conjugates for treatment of lipodystrophy |
| JOP20200092A1 (ar) | 2014-11-10 | 2017-06-16 | Alnylam Pharmaceuticals Inc | تركيبات iRNA لفيروس الكبد B (HBV) وطرق لاستخدامها |
| US10849911B2 (en) | 2015-06-10 | 2020-12-01 | Galmed Research And Development Ltd. | Low dose compositions of Aramachol salts |
| IL243707A0 (en) | 2016-01-20 | 2016-05-01 | Galmed Res And Dev Ltd | Treatment to regulate the microbiota in the intestine |
| CN106496300B (zh) * | 2016-10-19 | 2018-05-18 | 上海博志研新药物技术有限公司 | 花生胆酸及其中间体的制备方法 |
| US11197870B2 (en) | 2016-11-10 | 2021-12-14 | Galmed Research And Development Ltd | Treatment for hepatic fibrosis |
| WO2018087600A1 (en) * | 2016-11-10 | 2018-05-17 | Galmed Research And Development Ltd. | Inhibition of fibrosis in non-alcoholic fatty liver disease patients |
| US11324820B2 (en) | 2017-04-18 | 2022-05-10 | Alnylam Pharmaceuticals, Inc. | Methods for the treatment of subjects having a hepatitis b virus (HBV) infection |
| WO2018223836A1 (zh) | 2017-06-07 | 2018-12-13 | 苏州科睿思制药有限公司 | 一种脂肪酸胆汁酸偶合物的晶型及其制备方法和用途 |
| US11492623B2 (en) | 2018-08-13 | 2022-11-08 | Alnylam Pharmaceuticals, Inc. | Hepatitis B virus (HBV) dsRNA agent compositions and methods of use thereof |
| IT202000000328A1 (it) | 2020-01-10 | 2021-07-10 | Ice S P A | Metodo di preparazione dell'aramchol |
| CN114524857B (zh) * | 2022-02-22 | 2023-06-30 | 中国科学院微生物研究所 | 胆酸衍生物及其应用 |
| CN116687850A (zh) | 2022-02-24 | 2023-09-05 | 甘莱制药有限公司 | 包含环状膦酸酯化合物的药物组合物及其制备方法与用途 |
| WO2023227723A1 (en) * | 2022-05-26 | 2023-11-30 | Pharmazell Gmbh | An improved process for the preparation of aramchol and salts thereof |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3856953A (en) * | 1973-05-15 | 1974-12-24 | Intellectual Property Dev Corp | Method of treating fatty liver |
| IT1167479B (it) * | 1981-07-24 | 1987-05-13 | Carlo Scolastico | Derivati dell'acido chenodesossicolico |
| IT1167478B (it) * | 1981-07-24 | 1987-05-13 | Carlo Scolastico | Derivati dell'acido ursodesossicolico |
| DE3930696A1 (de) * | 1989-09-14 | 1991-03-28 | Hoechst Ag | Gallensaeurederivate, verfahren zu ihrer herstellung, verwendung als arzneimittel |
| IL123998A (en) * | 1998-04-08 | 2004-09-27 | Galmed Int Ltd | Conjugates of bile salts and pharmaceutical preparations containing them |
| DE19824123A1 (de) * | 1998-05-29 | 1999-12-02 | Hoechst Marion Roussel De Gmbh | Gallensäurederivat, Verfahren zu deren Herstellung, diese Verbindungen enthaltende Arzneimittel und deren Verwendung |
-
1998
- 1998-04-08 IL IL12399898A patent/IL123998A/en not_active IP Right Cessation
-
1999
- 1999-03-25 PT PT99912026T patent/PT1071702E/pt unknown
- 1999-03-25 TR TR2000/02876T patent/TR200002876T2/xx unknown
- 1999-03-25 EP EP99912026A patent/EP1071702B1/en not_active Expired - Lifetime
- 1999-03-25 DE DE69902647T patent/DE69902647T2/de not_active Expired - Lifetime
- 1999-03-25 WO PCT/IL1999/000173 patent/WO1999052932A1/en active IP Right Grant
- 1999-03-25 HU HU0101653A patent/HU229513B1/hu unknown
- 1999-03-25 SI SI9930142T patent/SI1071702T1/xx unknown
- 1999-03-25 CN CNB998049034A patent/CN100386339C/zh not_active Expired - Lifetime
- 1999-03-25 ID IDW20001998A patent/ID26042A/id unknown
- 1999-03-25 CZ CZ20003625A patent/CZ300824B6/cs not_active IP Right Cessation
- 1999-03-25 BR BRPI9909908A patent/BRPI9909908B8/pt not_active IP Right Cessation
- 1999-03-25 ES ES99912026T patent/ES2183526T3/es not_active Expired - Lifetime
- 1999-03-25 AT AT99912026T patent/ATE222923T1/de active
- 1999-03-25 DK DK99912026T patent/DK1071702T3/da active
- 1999-03-25 NZ NZ507309A patent/NZ507309A/xx not_active IP Right Cessation
- 1999-03-25 JP JP2000543488A patent/JP5031942B2/ja not_active Expired - Lifetime
- 1999-03-25 PL PL343360A patent/PL199271B1/pl unknown
- 1999-03-25 EA EA200000888A patent/EA003392B1/ru not_active IP Right Cessation
- 1999-03-25 UA UA2000095546A patent/UA70318C2/ru unknown
- 1999-03-25 CA CA002325933A patent/CA2325933C/en not_active Expired - Lifetime
- 1999-03-25 AU AU30515/99A patent/AU742944B2/en not_active Expired
- 1999-03-25 KR KR1020007010903A patent/KR100615560B1/ko not_active IP Right Cessation
-
2000
- 2000-09-29 US US09/675,656 patent/US6395722B1/en not_active Expired - Lifetime
- 2000-10-04 NO NO20004998A patent/NO316875B1/no not_active IP Right Cessation
- 2000-10-23 US US09/693,928 patent/US6384024B1/en not_active Expired - Lifetime
-
2002
- 2002-02-21 US US10/078,671 patent/US6589946B2/en not_active Expired - Lifetime
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ KG MD TJ TM |
|
| PC4A | Registration of transfer of a eurasian patent by assignment | ||
| MK4A | Patent expired |
Designated state(s): BY KZ RU |