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:WO-0032619-A1 优先权日:1998-11-30 标题:Methods and compositions for identification of inhibitors of ribosome assembly 发明人:DAMMEL CAROL S; WATSON JULIE C 权利人:RIBOGENE INC 摘要:The invention provides a means for identifying novel antibiotics by screening for compounds that inhibit bacterial ribosome assembly and ribosomal protein synthesis, which comprises the screening of test compounds to identify those that inhibit the activity of a bacterial ribosomal protein. The in vitro and in vivo assays detect (a) increased translation of a reporter mRNA that is normally repressed in the presence of a ribosomal protein, (b) increased growth in cells that over-express ribosomal protein, and (c) decreased binding of the ribosomal protein to its target RNA. The invention encompasses the (a) methods of screening and testing compounds by the above methods, (b) compounds that are identified in the assay which inhibit ribosome assembly and protein synthesis and (c) methods for treatment using said compounds.
专利号:US-6132993-A 优先权日:1995-08-11 标 题:Process for the production of amphotericin-B inhibiting production of amphotericin-A 发明人:SCHAFFNER CARL P; KIENTZLER DAVID J 权利人:UNIV RUTGERS 摘要:Methods are provided for improving the microbial production of amphotericin B by the selective inhibition of amphotericin A by means of protein synthesis inhibitors.
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-2011104052-A1 优先权日:2007-12-03 标 题 :Methods of synthesis and use of chemospheres 发明人:BARNETT BRADLEY POWERS; GESCHWIND JEFFREY 权利人:UNIV JOHNS HOPKINS 摘要:The present invention provides, in general, compositions comprising a hydrogel and an agent, for example a therapeutic agent or an imaging agent, for locoregional delivery. In certain preferred embodiments of the invention, the hydrogel compositions are detectable by Magnetic Responance and CT Scan and are used for locoregional delivery of therapeutic agents, for example chemotherapeutic agents. The invention also features polymer matrix compositions comprising nanoparticles that can be loaded after polymerization with bioactive agents, for example a diagnostic agent or therapeutic agent.
专利号:EP-1819715-A2 优先权日:2004-11-08 标 题 :Synthesis of cardiolipin analogues and uses thereof
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摘要:S55 | ZINC15PHARMA | Pharmaceuticals from ZINC15 | DOI:10.5281/zenodo.3247749