CN100386339C - 胆汁酸和胆汁酸衍生物的脂肪酸衍生物 - Google Patents

胆汁酸和胆汁酸衍生物的脂肪酸衍生物 Download PDF

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Publication number
CN100386339C
CN100386339C CNB998049034A CN99804903A CN100386339C CN 100386339 C CN100386339 C CN 100386339C CN B998049034 A CNB998049034 A CN B998049034A CN 99804903 A CN99804903 A CN 99804903A CN 100386339 C CN100386339 C CN 100386339C
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CN
China
Prior art keywords
bile
acid
fatty acid
conjugate
bile salt
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Lifetime
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CNB998049034A
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English (en)
Chinese (zh)
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CN1296492A (zh
Inventor
图维亚·吉拉特
沃纳·克雷默
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Galmed Research and Development Ltd
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Gstx Ltd
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    • 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

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  • 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)
CNB998049034A 1998-04-08 1999-03-25 胆汁酸和胆汁酸衍生物的脂肪酸衍生物 Expired - Lifetime CN100386339C (zh)

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
IL123998 1998-04-08

Publications (2)

Publication Number Publication Date
CN1296492A CN1296492A (zh) 2001-05-23
CN100386339C true CN100386339C (zh) 2008-05-07

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ID=11071405

Family Applications (1)

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CNB998049034A Expired - Lifetime CN100386339C (zh) 1998-04-08 1999-03-25 胆汁酸和胆汁酸衍生物的脂肪酸衍生物

Country Status (25)

Country Link
US (3) US6395722B1 (https=)
EP (1) EP1071702B1 (https=)
JP (1) JP5031942B2 (https=)
KR (1) KR100615560B1 (https=)
CN (1) CN100386339C (https=)
AT (1) ATE222923T1 (https=)
AU (1) AU742944B2 (https=)
BR (1) BRPI9909908B8 (https=)
CA (1) CA2325933C (https=)
CZ (1) CZ300824B6 (https=)
DE (1) DE69902647T2 (https=)
DK (1) DK1071702T3 (https=)
EA (1) EA003392B1 (https=)
ES (1) ES2183526T3 (https=)
HU (1) HU229513B1 (https=)
ID (1) ID26042A (https=)
IL (1) IL123998A (https=)
NO (1) NO316875B1 (https=)
NZ (1) NZ507309A (https=)
PL (1) PL199271B1 (https=)
PT (1) PT1071702E (https=)
SI (1) SI1071702T1 (https=)
TR (1) TR200002876T2 (https=)
UA (1) UA70318C2 (https=)
WO (1) WO1999052932A1 (https=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

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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
US20080038385A1 (en) * 2006-03-13 2008-02-14 Nutracea Therapeutic uses of an anti-cancer composition derived from rice bran
US20070212470A1 (en) * 2006-03-13 2007-09-13 Nutracea Therapeutic uses of an anti-cancer composition derived from rice bran
EP2043451B1 (en) * 2006-07-18 2012-03-21 Symrise AG Cyclodextrin blends with crystal growth inhibitors
CA2685127C (en) 2007-04-23 2019-01-08 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
SI2182954T1 (sl) * 2007-07-25 2019-04-30 Medizinische Universitat Graz Uporaba nor-žolčnih kislin pri zdravljenju arterioskleroze
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
WO2009082606A2 (en) 2007-12-04 2009-07-02 Alnylam Pharmaceuticals, Inc. Folate conjugates
WO2009073809A2 (en) 2007-12-04 2009-06-11 Alnylam Pharmaceuticals, Inc. Carbohydrate conjugates as delivery agents for oligonucleotides
US20100021538A1 (en) * 2008-02-29 2010-01-28 Youngro Byun Pharmaceutical compositions containing heparin derivatives
CA2721183C (en) 2008-04-11 2019-07-16 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
US20120157419A1 (en) * 2009-02-02 2012-06-21 Tuvia Gilat 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
WO2015019359A1 (en) * 2013-08-08 2015-02-12 Galderm Therapeutics Ltd. Anti-acne compositions comprising bile acid-fatty acid conjugates
US11571431B2 (en) 2013-12-04 2023-02-07 Galmed Research And Development Ltd Aramchol salts
HUE045209T2 (hu) * 2013-12-04 2019-12-30 Galmed Res & Development Ltd Aramchol-sók
WO2016199137A1 (en) 2015-06-10 2016-12-15 Galmed Research And Development Ltd. Low dose compositions of aramchol salts
WO2015186126A1 (en) * 2014-06-01 2015-12-10 Galmed Research And Development Ltd. Fatty acid bile acid conjugates for treatment of lipodystrophy
KR102545316B1 (ko) 2014-11-10 2023-06-22 알닐람 파마슈티칼스 인코포레이티드 Ｂ형 간염 바이러스(ｈｂｖ) ｉｒｎａ 조성물 및 그의 이용 방법
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
JP2019537607A (ja) * 2016-11-10 2019-12-26 ガルメド リサーチ アンド ディベロップメント リミテッド 非アルコール性脂肪性肝疾患の患者における線維化の抑制
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
JP7625512B2 (ja) 2018-08-13 2025-02-03 アルナイラム ファーマシューティカルズ， インコーポレイテッド Ｂ型肝炎ウイルス（ＨＢＶ）ｄｓＲＮＡ物質組成物およびその使用方法
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

Citations (3)

* Cited by examiner, † Cited by third party
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
US4439366A (en) * 1981-07-24 1984-03-27 Carlo Scolastico Derivatives of chenodeoxycholic acid
US4440688A (en) * 1981-07-24 1984-04-03 Carlo Scolastico Novel derivatives of ursodeoxycholic acid

Family Cites Families (3)

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Publication number Priority date Publication date Assignee Title
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

Patent Citations (3)

* Cited by examiner, † Cited by third party
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
US4439366A (en) * 1981-07-24 1984-03-27 Carlo Scolastico Derivatives of chenodeoxycholic acid
US4440688A (en) * 1981-07-24 1984-04-03 Carlo Scolastico Novel derivatives of ursodeoxycholic acid

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Also Published As

Publication number Publication date
EP1071702A1 (en) 2001-01-31
IL123998A (en) 2004-09-27
US6395722B1 (en) 2002-05-28
NO316875B1 (no) 2004-06-07
NO20004998L (no) 2000-12-06
PL199271B1 (pl) 2008-09-30
NO20004998D0 (no) 2000-10-04
HUP0101653A2 (hu) 2001-12-28
US20020091111A1 (en) 2002-07-11
CZ300824B6 (cs) 2009-08-19
AU3051599A (en) 1999-11-01
DK1071702T3 (da) 2002-12-30
KR100615560B1 (ko) 2006-08-25
TR200002876T2 (tr) 2000-12-21
EA003392B1 (ru) 2003-04-24
ES2183526T3 (es) 2003-03-16
WO1999052932A1 (en) 1999-10-21
BR9909908A (pt) 2000-12-26
SI1071702T1 (en) 2003-04-30
US6384024B1 (en) 2002-05-07
JP5031942B2 (ja) 2012-09-26
BR9909908B1 (pt) 2014-03-18
JP2002511482A (ja) 2002-04-16
PL343360A1 (en) 2001-08-13
HU229513B1 (en) 2014-01-28
ATE222923T1 (de) 2002-09-15
HUP0101653A3 (en) 2002-02-28
DE69902647D1 (de) 2002-10-02
UA70318C2 (uk) 2004-10-15
CA2325933A1 (en) 1999-10-21
EA200000888A1 (ru) 2001-04-23
ID26042A (id) 2000-11-16
CZ20003625A3 (cs) 2001-01-17
DE69902647T2 (de) 2003-04-24
AU742944B2 (en) 2002-01-17
US6589946B2 (en) 2003-07-08
KR20010042342A (ko) 2001-05-25
CN1296492A (zh) 2001-05-23
CA2325933C (en) 2008-06-10
PT1071702E (pt) 2003-01-31
NZ507309A (en) 2003-06-30
EP1071702B1 (en) 2002-08-28
BRPI9909908B8 (pt) 2021-05-25

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