BR9909908A - Derivados de ácidos graxos de ácidos biliares e derivados de ácidos biliares - Google Patents
Derivados de ácidos graxos de ácidos biliares e derivados de ácidos biliaresInfo
- Publication number
- BR9909908A BR9909908A BR9909908-0A BR9909908A BR9909908A BR 9909908 A BR9909908 A BR 9909908A BR 9909908 A BR9909908 A BR 9909908A BR 9909908 A BR9909908 A BR 9909908A
- Authority
- BR
- Brazil
- Prior art keywords
- bile
- acid
- salt
- bile acid
- fatty acid
- Prior art date
Links
- 239000003613 bile acid Substances 0.000 title abstract 7
- 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 title abstract 4
- 229940053200 antiepileptics fatty acid derivative Drugs 0.000 title 1
- 235000014113 dietary fatty acids Nutrition 0.000 abstract 4
- 229930195729 fatty acid Natural products 0.000 abstract 4
- 239000000194 fatty acid Substances 0.000 abstract 4
- 239000003833 bile salt Substances 0.000 abstract 3
- 150000004665 fatty acids Chemical class 0.000 abstract 3
- 210000000941 bile Anatomy 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
- 150000003839 salts Chemical class 0.000 abstract 2
- 206010003210 Arteriosclerosis Diseases 0.000 abstract 1
- 208000011775 arteriosclerosis disease Diseases 0.000 abstract 1
- -1 bile acid fatty acid Chemical class 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 235000012000 cholesterol Nutrition 0.000 abstract 1
- 230000021615 conjugation Effects 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 238000004090 dissolution Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 150000004671 saturated fatty acids Chemical class 0.000 abstract 1
- 235000003441 saturated fatty acids Nutrition 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)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Heart & Thoracic Surgery (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Urology & Nephrology (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
Patente de Invenção: <B>"DERIVADOS DE áCIDOS GRAXOS DE áCIDOS BILIARES E DERIVADOS DE áCIDOS BILIARES"<D>. A presente invenção refere-se a conjugados de ácidos graxo de sal biliar ou ácido biliar (daqui em diante denominados "BAFAC"), a seu uso na dissolução de cálculos de colesterol na bile, prevenindo sua ocorrência ou recorrência, a seu uso na redução e prevenção de arteriosclerose e a processos para tratamento das referidas doenças. Os conjugados são de fórmula W - X - G, em que G é um radical de ácido biliar ou sal biliar, W representa um ou dois radicais de ácido graxo saturado e X é ou uma ligação direta ou um membro de ligação entre o referido sal biliar ou ácido biliar e o(s) ácido(s) graxo(s). A conjugação é vantajosamente realizada em uma posição selecionada dentre as posições 3, 6, 7, 12, e 24 do núcleo de ácido ou sal biliar. Os ácidos graxos são preferivelmente ácidos graxos saturados tendo (14-22) átomos de carbono.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IL123998 | 1998-04-08 | ||
| 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 (3)
| Publication Number | Publication Date |
|---|---|
| BR9909908A true BR9909908A (pt) | 2000-12-26 |
| BR9909908B1 BR9909908B1 (pt) | 2014-03-18 |
| BRPI9909908B8 BRPI9909908B8 (pt) | 2021-05-25 |
Family
ID=11071405
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI9909908A BRPI9909908B8 (pt) | 1998-04-08 | 1999-03-25 | conjugados de ácido graxo de sal ou ácido biliar, composição farmacêutica compreendendo os mesmos e seus usos |
Country Status (25)
| Country | Link |
|---|---|
| US (3) | US6395722B1 (pt) |
| EP (1) | EP1071702B1 (pt) |
| JP (1) | JP5031942B2 (pt) |
| KR (1) | KR100615560B1 (pt) |
| CN (1) | CN100386339C (pt) |
| AT (1) | ATE222923T1 (pt) |
| AU (1) | AU742944B2 (pt) |
| BR (1) | BRPI9909908B8 (pt) |
| CA (1) | CA2325933C (pt) |
| CZ (1) | CZ300824B6 (pt) |
| DE (1) | DE69902647T2 (pt) |
| DK (1) | DK1071702T3 (pt) |
| EA (1) | EA003392B1 (pt) |
| ES (1) | ES2183526T3 (pt) |
| HU (1) | HU229513B1 (pt) |
| ID (1) | ID26042A (pt) |
| IL (1) | IL123998A (pt) |
| NO (1) | NO316875B1 (pt) |
| NZ (1) | NZ507309A (pt) |
| PL (1) | PL199271B1 (pt) |
| PT (1) | PT1071702E (pt) |
| SI (1) | SI1071702T1 (pt) |
| TR (1) | TR200002876T2 (pt) |
| UA (1) | UA70318C2 (pt) |
| WO (1) | WO1999052932A1 (pt) |
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 |
| US20090035348A1 (en) * | 2005-11-22 | 2009-02-05 | Z & Z Medical Holdings, Inc. | Dissolution of arterial plaque |
| 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 |
| 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 |
| WO2008009512A1 (en) * | 2006-07-18 | 2008-01-24 | Symrise Gmbh & Co. Kg | Cyclodextrin blends with crystal growth inhibitors |
| AU2008242583B2 (en) | 2007-04-23 | 2013-10-10 | Alnylam Pharmaceuticals, Inc. | Glycoconjugates of RNA interference agents |
| US20080287429A1 (en) * | 2007-05-15 | 2008-11-20 | Z & Z Medical Holdings, Inc. | Dissolution of Arterial Cholesterol Plaques by Pharmacologically Induced Elevation of Endogenous Bile Salts |
| WO2009013334A1 (en) * | 2007-07-25 | 2009-01-29 | Medizinische Universität Graz | Use of nor-bile acids in the treatment of arteriosclerosis |
| 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 |
| JP5635412B2 (ja) | 2007-12-04 | 2014-12-03 | アルニラム ファーマスーティカルズ インコーポレイテッドＡｌｎｙｌａｍ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． | 標的化脂質 |
| EP2231194B1 (en) | 2007-12-04 | 2017-02-22 | Alnylam Pharmaceuticals Inc. | Folate-irna conjugates |
| US20100021538A1 (en) * | 2008-02-29 | 2010-01-28 | Youngro Byun | Pharmaceutical compositions containing heparin derivatives |
| EP2274425A2 (en) | 2008-04-11 | 2011-01-19 | Alnylam Pharmaceuticals Inc. | Site-specific delivery of nucleic acids by combining targeting ligands with endosomolytic components |
| JP5620392B2 (ja) * | 2008-11-03 | 2014-11-05 | タフツ ユニヴァーシティーＴｕｆｔｓ Ｕｎｉｖｅｒｓｉｔｙ | クロストリジウム・ディフィシレ胞子の発芽および伸長を阻害するための方法および組成物 |
| WO2010086864A1 (en) * | 2009-02-02 | 2010-08-05 | Galmed International 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 |
| EP3138850B8 (en) * | 2011-06-16 | 2019-09-11 | Allergan Sales, LLC | Compositions containing deoxycholic acid and 10% deionized water in ethanol, directed to the purification of deoxycholic acid |
| 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 |
| CN110437298A (zh) * | 2013-12-04 | 2019-11-12 | 盖尔梅德研究与发展有限公司 | Aramchol盐 |
| WO2016199137A1 (en) | 2015-06-10 | 2016-12-15 | Galmed Research And Development Ltd. | Low dose compositions of aramchol salts |
| 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 |
| 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 |
| AU2017357868A1 (en) * | 2016-11-10 | 2019-06-27 | Galmed Research And Development Ltd. | Inhibition of fibrosis in non-alcoholic fatty liver disease patients |
| US11197870B2 (en) | 2016-11-10 | 2021-12-14 | Galmed Research And Development Ltd | Treatment for hepatic fibrosis |
| US11324820B2 (en) | 2017-04-18 | 2022-05-10 | Alnylam Pharmaceuticals, Inc. | Methods for the treatment of subjects having a hepatitis b virus (HBV) infection |
| CN110730785B (zh) * | 2017-06-07 | 2022-05-17 | 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 |
| CA3106701A1 (en) | 2018-08-13 | 2020-02-20 | 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 |
| IT1167478B (it) * | 1981-07-24 | 1987-05-13 | Carlo Scolastico | Derivati dell'acido ursodesossicolico |
| IT1167479B (it) * | 1981-07-24 | 1987-05-13 | Carlo Scolastico | Derivati dell'acido chenodesossicolico |
| 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 DE DE69902647T patent/DE69902647T2/de not_active Expired - Lifetime
- 1999-03-25 JP JP2000543488A patent/JP5031942B2/ja not_active Expired - Lifetime
- 1999-03-25 ES ES99912026T patent/ES2183526T3/es not_active Expired - Lifetime
- 1999-03-25 ID IDW20001998A patent/ID26042A/id unknown
- 1999-03-25 WO PCT/IL1999/000173 patent/WO1999052932A1/en not_active Ceased
- 1999-03-25 DK DK99912026T patent/DK1071702T3/da active
- 1999-03-25 KR KR1020007010903A patent/KR100615560B1/ko not_active Expired - Lifetime
- 1999-03-25 UA UA2000095546A patent/UA70318C2/uk unknown
- 1999-03-25 EP EP99912026A patent/EP1071702B1/en not_active Expired - Lifetime
- 1999-03-25 HU HU0101653A patent/HU229513B1/hu unknown
- 1999-03-25 CA CA002325933A patent/CA2325933C/en not_active Expired - Lifetime
- 1999-03-25 PL PL343360A patent/PL199271B1/pl unknown
- 1999-03-25 AT AT99912026T patent/ATE222923T1/de active
- 1999-03-25 BR BRPI9909908A patent/BRPI9909908B8/pt not_active IP Right Cessation
- 1999-03-25 SI SI9930142T patent/SI1071702T1/xx unknown
- 1999-03-25 PT PT99912026T patent/PT1071702E/pt unknown
- 1999-03-25 CZ CZ20003625A patent/CZ300824B6/cs not_active IP Right Cessation
- 1999-03-25 EA EA200000888A patent/EA003392B1/ru not_active IP Right Cessation
- 1999-03-25 AU AU30515/99A patent/AU742944B2/en not_active Expired
- 1999-03-25 CN CNB998049034A patent/CN100386339C/zh not_active Expired - Lifetime
- 1999-03-25 NZ NZ507309A patent/NZ507309A/xx not_active IP Right Cessation
- 1999-03-25 TR TR2000/02876T patent/TR200002876T2/xx unknown
-
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 |
|---|---|---|---|
| B07A | Application suspended after technical examination (opinion) [chapter 7.1 patent gazette] | ||
| B06A | Patent application procedure suspended [chapter 6.1 patent gazette] | ||
| B07D | Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette] | ||
| B07E | Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette] |
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