专利号:US-2008300418-A1 优先权日:2004-11-08 标 题:Synthesis of Cardiolipin Analogues and Uses Thereof 发明人:AHMAD MOGHIS U; UKKALAM MURALI K; ALI SHOUKATH M; AHMAD IMRAN 权利人:AHMAD MOGHIS U; UKKALAM MURALI K; ALI SHOUKATH M; AHMAD IMRAN 摘要:The invention provides novel synthetic methodologies for preparing cardiolipin, migrated caridiolipin (1,2-positional isomer of cardiolipin) and their analogues having varying fatty acids and/or alkyl chains with varying length and degrees of saturation/unsaturation. The method comprises (a) reacting an optically pure 1,2-O-dialkyl-sn-glycerol or 1,2-O-dialkyl-sn-glycerol with one or more phosphoramidite reagent(s), wherein a phosphite triester is produced; (b) coupling the product of (a) with glycerol, wherein a protected cardiolipin is produced; and (c) deprotecting the protected cardiolipin, such that cardiolipin is prepared. The cardiolipins and analogues thereof, prepared by the present methods, can be incorporated into liposomes, which can also include active agents such as hydrophobic or hydrophilic drugs, antisense nucleotides or diagnostic agents. Such liposomes can be used to treat diseases or can be used in diagnostic and/or analytical assays.
专利号:US-2006078560-A1 优先权日:2003-06-23 标 题 :Method of inducing apoptosis and inhibiting cardiolipin synthesis 发明人:JAMIL HARIS; AHMAD MOGHIS U; AHMAD IMRAN 权利人:NEOPHARM INC 摘要:The present invention provides a method for inducing apoptosis within a cell by exposing the cell to an inhibitor of cardiolipin synthesis under conditions sufficient to induce apoptosis within the cell. The method can be used to investigate or treat disorders such as cancer, obesity, and cardiovascular disorders. The invention also provides a pharmaceutical composition including an inhibitor of cardiolipin synthesis and a liposomal carrier.
专利号:US-2008286351-A1 优先权日:2004-06-29 标 题:Pegylated Cardiolipin Analogs, Methods of Synthesis, and Uses Thereof 发明人:AHMAD MOGHIS U; UKKALAM MURALI K; ALI SHOUKATH M; AHMAD IMRAN 权利人:AHMAD MOGHIS U; UKKALAM MURALI K; ALI SHOUKATH M; AHMAD IMRAN 摘要:The invention provides synthetic methods for PEGylated cardiolipins with varying linkers. The methods can be employed to prepare PEGylated cardiolipin with different fatty acid and/or alkyl chain length with or without unsaturation. The PEGylated cardiolipin, prepared by the present methods, can be incorporated into liposomes that can also include active agents such as hydrophilic or hydrophobic drugs for the treatment of human and animal diseases. In addition, the PEGylated cardiolipin can be incorporated into liposomes that include compounds for therapeutic and diagnostic imaging. The use of such liposomes with PEGylated cardiolipin prolongs the period of liposomal circulation without disrupting the lipid bilayer.
专利号:US-2005266068-A1 优先权日:2002-05-24 标题 :Cardiolipin molecules and methods of synthesis 发明人:AHMAD MOGHIS U; UKKALAM MURALI K; AHMAD IMRAN 权利人:NEOPHARM INC 摘要:The invention provides new synthetic routes for cardiolipin with different fatty acids and/or alkyl chains with varying chain length and also with or without unsaturation, particularly a short-chain cardiolipin. The methods comprise reacting a 1,2-O-sn-diacyl/1,2-O-sn-dialkyl glycerol or a 2-O-protected glycerol, with a phosphoramidite reagent or a phosphate triester to produce a protected cardiolipin, which is deprotected to prepare the short chain cardiolipin. The reaction schemes can be used to generate new variants of cardiolipin. The cardiolipin prepared by the present methods can be incorporated into liposomes, which can also include active agents such as hydrophobic or hydrophilic drugs. Such liposomes can be used to treat diseases or in diagnostic and/or analytical assays. Liposomes can also include ligands for targeting a particular cell type or specific tissue.
专利号:US-3953604-A 优先权日:1972-01-14 标 题:1-(2-Substituted-chromonyloxy)-2-hydroxy-3-(substituted phenoxy)propanes 发明人:WARREN BRIAN THOMAS; SPICER JOHN WILLIAM 权利人:MILES LAB 摘要:Definitions: in the following Formulae I, II and IV, R 1 represents hydrogen, alkyl of 1 to 4 carbon atoms, or a nontoxic cation, while each of R 2 , R 3 , R 4 , R 5 , and R 6 symbolizes hydrogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, carboxy, carbalkoxy of 1 to 4 carbon atoms, trihalomethyl, halogen, nitro or cyano. n Certain 1-(2-substituted-chromon-yloxy)-2-hydroxy-3-(substituted-phenoxy)propanes (Formula I), ##SPC1## n can be synthesized from intermediate bis-(substituted-phenoxy)propanes (Formula II), ##SPC2## n by condensation with diethyl oxalate in the presence of sodium ethoxide followed by cyclization with a mixture of glacial acetic acid and concentrated sulfuric or a mixture of concentrated hydrochloric acid and a lower alcohol containing up to 4 carbon atoms. n The bis-(substituted-phenoxy)propane intermediates (Formula II) are prepared by reacting a dihydroxyacetophenone (Formula III), ##SPC3## n with a (substituted-phenyl)glycidyl ether (Formula IV), ##SPC4## n in an organic solvent in the presence of a catalyst. n The 1-(2-substituted-chromon-yloxy)-2-hydroxy-3-(substituted-phenoxy)propanes (Formula I) are useful in the treatment of allergic conditions in mammals. The bis-(substituted-phenoxy)propanes (Formula II) are useful as intermediates in the synthesis of the latter compounds. Methods of preparing compounds having Formulae I and II are described. Methods of treating allergic conditions in mammals utilizing compounds of Formula I are also disclosed.
专利号:WO-2004039817-A9 优先权日:2002-10-16 标题 :Cardiolipin molecules and method of synthesis 发明人:AHMAD MOGHIS U; UKKALAM MURALI K; AHMAD IMRAN 权利人:NEOPHARM INC; AHMAD MOGHIS U; UKKALAM MURALI K; AHMAD IMRAN 摘要:The invention provides new synthetic routes for cardiolipin with different fatty acids and/or alkyl chains with varying chain length and also with or without unsaturation, particularly a short-chain cardiolipin. The methods comprise reacting a 1,2-O-sn-diacyl/1,2-O-sn-dialkyl glycerol or a 2-O-protected glycerol, with a phosphoramidite reagent or a phosphate triester to produce a protected cardiolipin, which is deprotected to prepare the short chain cardiolipin. The reaction schemes can be used to generate new variants of cardiolipin. The cardiolipin prepared by the present methods can be incorporated into liposomes, which can also include active agents such as hydrophobic or hydrophilic drugs. Such liposomes can be used to treat diseases or in diagnostic and/or analytical assays. Liposomes can also include ligands for targeting a particular cell type or specific tissue.