发明Bile salt conjugates

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申请号 US20000693928 申请日 2000年10月23日 最早公开日 2002年05月07日 所属国家/地区 美国
公开号及公开日 US6384024B1   2002年05月07日
授权日 2002年05月07日 说明书附图
申请人 GALMED INT LTD (马耳他)  
发明人 GILAT TUVIA  
优先权 IL19980123998   19980408
专利分类号 A61K31/575   A61P1/16   A61K31/56   A61P9/10   C07J9/00   C07J41/00   A61P43/00  
代理机构 Jacobson Holman, PLLC   代理人

名称及摘要

Bile salt conjugates
The present invention relates to bile acid or bile salt fatty acid conjugates (hereinafter called "BAFAC), to their use in dissolving cholesterol gallstones in bile, preventing their occurrence or recurrence, to their use in reducing or preventing arteriosclerosis and to methods for the treatment of said diseases. The conjugates are of the formula W-X-G in which G is a bile acid or bile salt radical, W stands for one or two saturated fatty acid radicals and X is either a direct bond or a bonding member between said bile acid or bile salt and the fatty acid(s). The conjugation is advantageously performed at a position selected among the 3, 6, 7, 12 and 24 positions of the bile acid or bile salt nucleus.
Bile salt conjugates
The present invention relates to bile acid or bile salt fatty acid conjugates (hereinafter called "BAFAC), to their use in dissolving cholesterol gallstones in bile, preventing their occurrence or recurrence, to their use in reducing or preventing arteriosclerosis and to methods for the treatment of said diseases. The conjugates are of the formula W-X-G in which G is a bile acid or bile salt radical, W stands for one or two saturated fatty acid radicals and X is either a direct bond or a bonding member between said bile acid or bile salt and the fatty acid(s). The conjugation is advantageously performed at a position selected among the 3, 6, 7, 12 and 24 positions of the bile acid or bile salt nucleus.

同族及引用

同族专利 (28) 引用其他专利(56) 被其他专利引用(11)

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EP1071702B1 FATTY ACID DERIVATIVES OF BILE ACIDS AND BILE ACID DERIVATIVES
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DE69902647D1 【Title of corresponding document:us2002091111A1】
DK1071702T3 Fatty acid derivatives of bile acids and bile acid derivatives
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ES2183526T3 DERIVED FROM GREASY ACIDS OF BILE ACIDS AND DERIVATIVES OF BILE ACID.
DE69902647T2 【Title of corresponding document:us2002091111A1】
SI1071702T1 FATTY ACID DERIVATIVES OF BILE ACIDS AND BILE ACID DERIVATIVES
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IL123998A BILE SALT CONJUGATES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
UA70318C2 FATTY ACID DERIVATIVES OF BILE ACIDS AND DERIVATIVFATTY ACID DERIVATIVES OF BILE ACIDS AND DERIVATIVES OF BILE ACID, A PHARMACETICAL PREPARATION FOR DES OF BILE ACID, A PHARMACETICAL PREPARATION FOR DISSOLVING CHOLESTEROL GALLSTONES AND PREVENTING ATISSOLVING CHOLESTEROL GALLSTONES AND PREVENTING ATHERIOSCLEROSIS, A METHOD FOR THE TREATMENT (VARIANHERIOSCLEROSIS, A METHOD FOR THE TREATMENT (VARIANTS) TS)
KR100615560B1 Fatty acid derivatives of bile acids and bile acid derivatives
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花生胆酸及其中间体的制备方法
Pharmaceutical composition comprising conjugate of bile acid or a salt of bile acid with fatty acid for treatment of fatty liver syndrome
Amide conjugates of steroidal and bile acids with D-glucosamine and process for preparing thereof
USE OF BILE ACID OR BILE SALT FATTY ACID COMPOUNDS FOR THE TREATMENT OF FATTY LEVER INFILTRATION
Use of bile acid or bile salt fatty acid conjugates
METHODS FOR THE SYNTHESIS AND PURIFICATION OF DEOXYCHOLIC ACID
ANTI-ACNE COMPOSITIONS COMPRISING BILE ACID-FATTY ACID CONJUGATES
TARGETING LIPIDS
COMPOSITIONS CONTAINING DEOXYCHOLIC ACID AND C1-3-ALCOHOLS, DIRECTED TO THE PURIFICATION OF DEOXYCHOLIC ACID
USE OF BILE ACID OR BILE SALT FATTY ACID CONJUGATES
Bile salt conjugates
Blood cell deficiency treatment method
Bile-acid derived compounds for enhancing oral absorption and systemic bioavailability of drugs
Bile acid or bile salt fatty acid conjugates
Delivery agents for enhancing mucosal absorption of therapeutic agents
Bile-acid derived compounds for enhancing oral absorption and systemic bioavailability of drugs
Therapeutic uses of an anti-cancer composition derived from rice bran
METHODS AND COMPOSITIONS OF GENE DELIVERY AGENTS FOR SYSTEMIC AND LOCAL THERAPY
METHOD FOR TREATING COLON CANCER WITH RICE BRAN COMPOSITION
THERAPEUTIC USES OF AN ANTI-CANCER COMPOSITION DERIVED FROM RICE BRAN
Dissolution of arterial plaque
Glycoconjugates of RNA interference agents
Dissolution of Arterial Cholesterol Plaques by Pharmacologically Induced Elevation of Endogenous Bile Salts
DISSOLUTION OF ARTERIAL PLAQUE
Carbohydrate conjugates as delivery agents for oligonucleotides
Folate conjugates
Bile acid or bile salt fatty acid conjugates
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Site-specific delivery of nucleic acids by combining targeting ligands with endosomolytic components
Methods and compositions for inhibiting clostridium difficile spore germination and outgrowth
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Carbohydrate conjugates as delivery agents for oligonucleotides
Bile acid or bile salt fatty acid conjugates
Dissolution of arterial plaque
Carbohydrate conjugates as delivery agents for oligonucleotides
Site specific delivery of nucleic acids by combining targeting ligands with endosomolytic components
Targeting lipids
Carbohydrate conjugates as delivery agents for oligonucleotides
Carbohydrate conjugates as delivery agents for oligonucleotides
Carbohydrate conjugates as delivery agents for oligonucleotides
Methods for the purification of deoxycholic acid
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Site-specific delivery of nucleic acids by combining targeting ligands with endosomolytic components
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METHODS AND COMPOSITIONS FOR INHIBITING CLOSTRIDIUM DIFFICILE SPORE GERMINATION AND OUTGROWTH
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NEW DERIVATIVES OF ACID URSODESOXYCHOLIQUE, THEIR METHOD OF PREPARATION AND THEIR APPLICATION INTO THERAPEUTIC
NEW DERIVATIVES OF ACID CHENODESOXYCHOLIQUE
Bile acid derivatives, processes for their preparation and their use as pharmaceuticals
CHENODEOXYCHOLIC ACID DERIVATIVE, MANUFACTURE AND MEDICINAL COMPOSITION
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Bile salt conjugates

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