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12 条记录 (耗时 0.013 秒)

    STEREOSELECTIVE PROCESS FOR PREPARING (CYCLO)ALKYL PHENYLGLYCOLIC ACIDS
    2.
    发明公开
    STEREOSELECTIVE PROCESS FOR PREPARING (CYCLO)ALKYL PHENYLGLYCOLIC ACIDS 审中-公开
    STEREO选择性工艺生产式（环）烷基PHENYLGLYKOLSÄUREN

    公开(公告)号：EP1127043A1

    公开(公告)日：2001-08-29

    申请号：EP99956816.5

    申请日：1999-10-29

    申请人： Sepracor Inc.

    发明人： SENANAYAKE, Chris, H. ,  GROVER, Paul T.

    IPC分类号： C07C51/353 ,  C07C59/54 ,  C07D317/34

    CPC分类号： C07D317/34 ,  C07C51/353 ,  C07C59/54

    摘要： A process for preparing an alkyl phenylglycolic acid is disclosed. It follows the sequence of condensing a substituted acetaldehyde with mandelic acid to provide a 5-phenyl-1,3-dioxolan-4-one, which is condensed with an alkyl ketone or aldehyde to provide a 5-(1-hydroxyalkyl)-5-phenyl-1,3-dioxolan-4-one, which is dehydrated to a 5-(1-alkenyl)-5-phenyl-1,3-dioxolan-4-one. The 5-(1-alkenyl)-5-phenyl-1,3-dioxolan-4-one may be hydrolyzed and reduced to an α-alkylphenylglycolic acid or the hydrolysis and reduction steps may be reversed. The process enables the production of single enantiomers of cyclohexylphenylglycolic acid (CHPGA). An analogous process for racemic CHPGA is disclosed employing racemic mandelic acid and acetone. Novel intermediates in the process are also disclosed.

    2$i(R),4$i(S),$i(R),$i(S)- AND 2$i(S),4$i(R),$i(R),$i(S)-HYDROXYITRACONAZOLE- AND HYDROXYSAPERCONAZOLE DERIVATIVES
    4.
    发明公开
    2$i(R),4$i(S),$i(R),$i(S)- AND 2$i(S),4$i(R),$i(R),$i(S)-HYDROXYITRACONAZOLE- AND HYDROXYSAPERCONAZOLE DERIVATIVES 失效
    （S），$ i（R），$ i（S） - 和2 $ i（S），4 $ i（R），$ i（R），$ i（R） S） - 羟基吡咯烷酮和羟基吡咯烷衍生物

    公开(公告)号：EP0938487A2

    公开(公告)日：1999-09-01

    申请号：EP97946663.0

    申请日：1997-11-12

    申请人： SEPRACOR, INC.

    发明人： MCCULLOUGH, John, R. ,  SENANAYAKE, Chris, H. ,  TANOURY, Gerald, J. ,  HONG, Yaping ,  KOCH, Patrick

    IPC分类号： A61K31 ,  A61P31 ,  C07D249 ,  C07D405 ,  C07D521

    CPC分类号： C07D249/08 ,  C07D231/12 ,  C07D233/56 ,  C07D249/12

    摘要： A substantially pure single enantiomer of a compound of formula (1), wherein X?1 and X2¿ are independently chlorine or fluorine and R is hydrogen, -P(O)(OH)¿2? or -SO3H, or a salt thereof. A method of preparation of optically pure isomers of hydroxyitraconazole, in particular the two cis dioxolane diastereomers of the sec-butyl (R,S)-isomer, and to phosphate and sulfate derivatives thereof is disclosed. Pharmaceutical compositions containing these compounds and their use for the treatment of fungal infection are also disclosed.

    摘要翻译： 式（1）化合物的基本上纯的单一对映体，其中X 1和X 2独立地为氯或氟，R为氢，-P（O）（OH）2' 或-SO 3 H或其盐。 公开了制备羟基依他康唑的光学纯异构体的方法，特别是仲丁基（R，S） - 异构体的两个顺式二氧戊环非对映异构体，以及其磷酸酯和硫酸酯衍生物。 还公开了含有这些化合物的药物组合物及其用于治疗真菌感染的用途。

    METHOD OF RESOLVING AMLODIPINE RACEMATE
    7.
    发明公开
    METHOD OF RESOLVING AMLODIPINE RACEMATE 审中-公开
    解聚阿米地平杀鼠剂的方法

    公开(公告)号：EP1448527A1

    公开(公告)日：2004-08-25

    申请号：EP02802193.9

    申请日：2002-10-23

    申请人： Sepracor, Inc.

    发明人： SENANAYAKE, Chris, H. ,  TANOURY, Gerald, J. ,  WILKINSON, Harold, S. ,  BAKALE, Roger, P. ,  ZLOTA, Andrei, A. ,  SARANTEAS, Kostas

    IPC分类号： C07D211/90

    CPC分类号： C07D211/90

    摘要： The invention relates to methods of resolving racemic amlodipine into enantiomerically enriched compositions by precipation with tartaric acid in the presence of a non-aqueous solvent, such as N,N'-dimethylacetamide. The molar ratio of tartaric acid:amlodipine is preferably less than 0.25:1.0 greater than 0.75:1.0.

    摘要翻译： 本发明涉及通过在非水溶剂如N，N'-二甲基乙酰胺存在下用酒石酸沉淀将外消旋氨氯地平拆分成对映体富集的组合物的方法。 酒石酸：氨氯地平的摩尔比优选小于0.25:1.0，大于0.75:1.0。

    METHODS OF PREPARING AND USING 2-HYDROXY DERIVATIVES OF SIBUTRAMINE AND ITS METABOLITES
    10.
    发明公开
    METHODS OF PREPARING AND USING 2-HYDROXY DERIVATIVES OF SIBUTRAMINE AND ITS METABOLITES 审中-公开
    方法制备和使用西布曲明及其代谢产物2-羟基衍生物的

    公开(公告)号：EP1434575A1

    公开(公告)日：2004-07-07

    申请号：EP02761634.1

    申请日：2002-09-12

    申请人： Sepracor Inc.

    发明人： SENANAYAKE, Chris, H. ,  JERUSSI, Thomas, P. ,  CURRIE, Mark, G. ,  FANG, Qun, K. ,  HSU, Bob

    IPC分类号： A61K31/135 ,  C07C211/08

    CPC分类号： C07C215/28 ,  A61K31/135 ,  C07C2601/04

    摘要： The invention is directed, in part, to racemic and stereomerically pure 2-hydroxy derivatives of sibutramine and its metabolites, and 2-hydroxy derivatives of desmethylsibutramine and didesmethylsibutramine in particular. The invention is further directed to novel methods of preparing these derivatives are also disclosed. The invention is also directed to pharmaceutical compositions and dosage forms that comprise therapeutically or prophylactically effective amounts of the compounds, optionally in combination with an additional pharmacologically active compound. These pharmaceutical compositions and dosage forms can be used in the methods of the invention, which provide for the treatment or prevention of a variety of diseases and disorders.