CAS: 1104-22-9; Meclizine Dihydrochloride

上下游产品

1-chloromethyl-3-methyl-benzene N-(4-chlorobenzhydryl)piperazineMeclozin-N,N'-dioxid 25H27ClN2*ClHC25H27ClN2*ClH 25H27ClN2C25H27ClN2 25H27ClN2C25H27ClN2

3-甲基苄基氯,1-(4-氯二苯甲基)哌嗪置于四丁基溴化铵,Potassium Carbonate,盐酸体系中,用 水 用作溶剂,化学反应 2.0H,反应生成1-[(4-氯苯基)苄基]-4-[(M-甲苯基)甲基]哌嗪盐酸盐
参考文献:Novel Water Based Process For The Preparation Of Substituted Diphenylmethyl Piperazines
标题:Novel Water Based Process For The Preparation Of Substituted Diphenylmethyl Piperazines
摘要:本发明涉及一种用水为基础的新型过程,用于制备化合物i的取代二苯甲基哌嗪及其药用盐,其中x1和x2分别代表氢,卤素,直链或支链低碳基,烷氧基或羟基基团,R选自酰基,烷基,烯基,芳基烷基,芳基烯基,芳基,芳基烯基或芳基羟基烷基,芳基氧基烷基,烷氧基烷基,氨基烷基或其衍生物等,包括将化合物ii与化合物r-X反应,其中r如上定义,X是适当的离去基团,包括卤素等卤素,但不限于其他离去基团,如对甲苯磺酸酯,甲磺酸酯和活化酸基团,如酰卤,酸酐,混合酸酐等,使用水作用作溶剂,在催化剂和碱的存在下,在25-100oc条件下进行.

专利信息

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-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-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-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.

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.