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18 条记录 (耗时 0.014 秒)

    Substituted 5-(2-(2-aryl-2-hydroxyethyl)-amino)propyl)-1,3-benzodioxoles
    5.
    发明授权
    Substituted 5-(2-(2-aryl-2-hydroxyethyl)-amino)propyl)-1,3-benzodioxoles 失效
    取代的5-（2-（2-亚甲基-2-羟基乙基） - 氨基）丙基）-1,3-苯并二氧杂环戊烯

    公开(公告)号：US5245053A

    公开(公告)日：1993-09-14

    申请号：US896319

    申请日：1992-06-10

    申请人： Jonathan D. Bloom ,  Thomas H. Claus ,  Vern G. Devries ,  Jo A. Dolan ,  Minu D. Dutia

    发明人： Jonathan D. Bloom ,  Thomas H. Claus ,  Vern G. Devries ,  Jo A. Dolan ,  Minu D. Dutia

    IPC分类号： C07D317/46 ,  C07D413/06

    CPC分类号： C07D413/06 ,  C07D317/46

    摘要： A process is disclosed for obtaining the R,R isomer of: ##STR1## wherein R.sub.1 and R.sub.2 may be one or more groups which may be the same or different and are selected from the group consisting of hydrogen, C.sub.1 to C.sub.4 alkyl, C.sub.1 to C.sub.4 alkoxy, hydroxy, halogen, trifluoromethyl, carboxy, hydroxyalkyl, alkoxycarbonyl, C.sub.1 to C.sub.4 thioalkyl, sulfonyl and sulfinyl; X is a divalent radical consisting of ##STR2## wherein R' is hydrogen; R.sub.2 and R.sub.3 may be the same or different and are selected from the group consisting of hydrogen and C.sub.1 to C.sub.4 alkyl; R.sub.5 and R.sub.6 are selected from the group consisting of hydrogen, carboxy, alkoxycarbonyl, hydroxymethyl, --CH.sub.2 OCH.sub.2 COOR.sub.7 and --CH.sub.2 OCH.sub.2 CH.sub.2 OR.sub.7 where R.sub.7 is hydrogen or C.sub.1 to .sub.4 alkyl; except that R.sub.5 and R.sub.6 may not both be hydrogen; and the asterisks denote asymmetric carbon atoms; said process comprising the steps of:(a) reacting Mosher's acid with a compound of formula I to attach a group of the formula ##STR3## at the N-9 position of a mixture of (+) and (-) enantiomers of said compound to form a new pair of diastereoisomers; and(b) separating said new pair of diastereoisomers by HPLC and recovering the R,R isomer.The process is based on reacting Mosher's acid with the compound of formula I and thereafter using HPLC to separate the R,R isomer.

    摘要翻译： 公开了获得R 1 R 4异构体的方法：其中R 1和R 2可以是一个或多个可以相同或不同并且选自氢，C 1至C 4烷基，C 1至C 4烷基， C4烷氧基，羟基，卤素，三氟甲基，羧基，羟基烷基，烷氧基羰基，C1-C4硫代烷基，磺酰基和亚磺酰基; X是由组成的二价基团，其中R'是氢; R2和R3可以相同或不同，并且选自氢和C1-C4烷基; R5和R6选自氢，羧基，烷氧基羰基，羟甲基，-CH2OCH2COOR7和-CH2OCH2CH2OR7，其中R7是氢或C1-4烷基; 不同之处在于R5和R6不能都是氢; 星号表示不对称碳原子; 所述方法包括以下步骤：（a）使Mosher's酸与式I化合物反应，以在所述化合物的（+）和（ - ）对映异构体的混合物的N-9位上连接一组式 形成一对新的非对映异构体; 和（b）通过HPLC分离所述新对非对映异构体并回收R，R异构体。 该方法基于Mosher酸与式I化合物的反应，然后使用HPLC分离R，R异构体。

    Dibenzocycloalkanamido and dibenzothioxanthenyl benzoic acids
    8.
    发明授权
    Dibenzocycloalkanamido and dibenzothioxanthenyl benzoic acids 失效
    二苯并环烷酰胺和二苯并噻吨苯甲酸

    公开(公告)号：US4489090A

    公开(公告)日：1984-12-18

    申请号：US492097

    申请日：1983-05-06

    申请人： Vern G. DeVries ,  Robert G. Shepherd

    发明人： Vern G. DeVries ,  Robert G. Shepherd

    IPC分类号： C07D335/14 ,  A61K31/22 ,  A61K31/38 ,  C07C103/733 ,  C07D335/12

    CPC分类号： C07D335/14 ,  Y10S514/824

    摘要： This disclosure describes novel dibenzocycloalkanamido-benzoic acids and esters. Also described are dibenzothioxanthenyl-benzoic acids and esters. These compounds are useful pharmaceutical agents for ameliorating atherosclerosis by inhibiting the formation and development of atherosclerotic lesions in the arterial walls of mammals.

    摘要翻译： 本公开描述了新的二苯并环烷酰氨基 - 苯甲酸和酯。 还描述了二苯并噻二苯并苯甲酸和酯。 这些化合物是通过抑制哺乳动物动脉壁中动脉粥样硬化病变的形成和发展来改善动脉粥样硬化的有用的药剂。