专利号:US-7250510-B2 优先权日:2005-08-24 标 题:Transition metal complexes of N-heterocyclic carbenes, method of preparation and use in transition metal catalyzed organic transformations 发明人:ORGAN MICHAEL G; O'BRIEN CHRISTOPHER J; KANTCHEV ASSAM ERIC B 权利人:TOTAL SYNTHESIS LTD 摘要:The present invention relates to catalysts of transition metal complexes of N-heterocyclic carbenes, their methods of preparation and their use in chemical synthesis. The synthesis, ease-of-use, and activity of the compounds of the present invention are substantial improvements over in situ catalyst generation. Further, the transition metal complexes of N-heterocyclic carbenes of the present invention may be used as precatalysts in metal-catalyzed cross-coupling reactions.
专利号:US-2005209355-A1 优先权日:2004-03-22 标 题:[Novel Reactions and the Products of Such Reactions] 发明人:ROITMAN LIPA L 权利人:ROITMAN LIPA L 摘要:A process for the synthesis of novel compounds is described comprising reacting tetrachloroethylene with substances containing active methylene group in the presence of free radical initiators. Also, a process for grafting tetrachloroethylene is described comprising reacting these compounds with polymers containing active methylene group in the presence of free radical initiators. Furthermore, a method of conducting such reactions to high conversion is described, comprising conducting the reactions in the reflux condensate. The present invention provides a novel and high yield route for heretofore unobtainable materials.
专利号:US-12295961-B2 优先权日:2009-12-31 标 题:Modulation of solubility, stability, absorption, metabolism, and pharmacokinetic profile of lipophilic drugs by sterols 发明人:DHINGRA OM 权利人:MARIUS PHARMACEUTICALS INC 摘要:A formulation for drug delivery, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of a lipophilic therapeutic agent by formulation with sterols and/or sterol esters, resulting in higher bioavailability of a therapeutic agent administered to a subject in need of such therapeutic agent. The formulation contains a therapeutic agent and a sterol or sterol ester, and can, optionally, further contain a solubilizer and/or an enhancing agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.
专利号:US-7344868-B2 优先权日:2003-06-03 标题:Method for synthesizing ceramide-type compounds 发明人:LASSALLE LAURENT; YVERGNAUX FLORENT 权利人:LASSALLE LAURENT; YVERGNAUX FLORENT 摘要:The invention relates to the fields of fatty substance chemistry, specifically of the ceramide-type compound synthesis. The invention resides substantially in the synthesis of ceramide-type compounds. Specifically, the aim of the invention is a new enzymatic synthesis method, comprising at least one amidification step and one esterification step, achieved through lipases, among fatty acids and/or esters thereof and amino alcohols. The resulting ceramide-type compounds can be used as cosmetic and/or pharmaceutical compositions, in particular as dermatological compositions in conjunction or in admixture with one or more suitable cosmetic and/or pharmaceutical excipients or carriers. The method has an interest particularly in the synthesis of active compounds useful in the fields of cosmetology and/or pharmacology and specifically of dermatology.
专利号:WO-2011095125-A1 优先权日:2010-02-02 标 题:Synthesis methods and purification methods of dasatinib 发明人:YAN RONG; YANG HAO; HOU WEN; XU YONGXIANG 权利人:NAN JING CAVENDISH BIO ENGINEERING TECHNOLOGY CO LTD; YAN RONG; YANG HAO; HOU WEN; XU YONGXIANG 摘要:Synthesis methods of dasatinib are provided, which comprise the following steps: reacting a compound of formula I with a compound of formula II to obtain a compound of formula III, and then connecting the compound of formula III with 2-chloro-6-methylaniline and 1-(2-hydroxyethyl)piperazine in any order to give dasatinib. Furthermore, purification methods of dasatinib are also provided.
专利号:US-11617758-B2 优先权日:2009-12-31 标 题 :Emulsion formulations 发明人:DHINGRA OM; BERNSTEIN JAMES S 权利人:MARIUS PHARMACEUTICALS LLC 摘要:A SEDDS or SMEDDS or SNEDDS formulation for drug delivery of a lipophilic therapeutic agent, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of the therapeutic agent by formulation with a lipophilic surfactant, a hydrophilic surfactant, one or more solubilizers and, optionally, digestible oils, resulting in higher bioavailability of the therapeutic agent administered to a subject in need of such therapeutic agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.
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