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17 条记录 (耗时 0.021 秒)

    HIV protease inhibitors having polyether substituents
    1.
    发明公开
    HIV protease inhibitors having polyether substituents 失效
    HIV-Proteaseinhibitoren mit Polyether-Substituenten。

    公开(公告)号：EP0487270A2

    公开(公告)日：1992-05-27

    申请号：EP91310590.4

    申请日：1991-11-15

    申请人： MERCK & CO. INC.

    发明人： Graham, Samuel L. ,  Hungate, Randall W. ,  Huff, Joel R. ,  Lyle, Terry A. ,  Young, Steven D. ,  Britcher, Susan F. ,  Scholz, Thomas H. ,  Payne, Linda S. ,  Dorsey, Bruce D.

    IPC分类号： C07C271/22 ,  A61K31/27 ,  C07C323/60 ,  C07F9/40 ,  A61K31/66

    CPC分类号： C07C323/60 ,  C07C271/22 ,  C07C317/50 ,  C07C2602/08 ,  C07F9/091

    摘要： Polyether derivatives of the form,

            A-G-B-B-J


       wherein G is a dipeptide isostere substituted with a polyether, B an amino acid or analog thereof, and J a small terminal group are described. These compounds are useful in the inhibition of DIV protease, the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.

    摘要翻译： 形式为A-G-B-B-J的聚醚衍生物，其中G是由聚醚取代的二肽等排物，B是氨基酸或其类似物，J是小端基。 这些化合物可用作抑制DIV蛋白酶，预防或治疗艾滋病毒和艾滋病感染，作为化合物，药学上可接受的盐，药物组合物成分，无论是否与其他抗病毒剂，免疫调节剂，抗生素或其他抗生素组合使用 疫苗。 还描述了治疗AIDS的方法和预防或治疗HIV感染的方法。

    Benzoxazinones as inhibitors of HIV reverse transcriptase
    4.
    发明公开
    Benzoxazinones as inhibitors of HIV reverse transcriptase 失效
    苯并恶嗪酮抑制剂逆转逆转录酶HIV。

    公开(公告)号：EP0582455A1

    公开(公告)日：1994-02-09

    申请号：EP93306114.5

    申请日：1993-08-03

    申请人： MERCK & CO. INC.

    发明人： Young, Steven D. ,  Tran, Lekhanh O. ,  Britcher, Susan F. ,  Lumma, William C. Jr. ,  Payne, Linda S.

    IPC分类号： C07D265/18 ,  A61K31/535

    CPC分类号： C07D265/18 ,  A61K45/06

    摘要： Certain benzoxazinones of the formula:

    wherein:
       X is halo,
       X¹ is trihalomethy, or pentahaloethyl;
       Z is O;
    are useful in the inhibition of HIV reverse transcriptase (including its resistant varieties), the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.

    摘要翻译： 某些具有下式的苯并恶嗪酮：其中：X是卤素，X 1是三卤代或五卤代乙基; Z是O; 可用于抑制HIV逆转录酶（包括其抗性品种），预防或治疗艾滋病毒感染和艾滋病治疗，作为化合物，药学上可接受的盐，药物组合物成分，无论是否与其他抗病毒药物组合 ，免疫调节剂，抗生素或疫苗。 还描述了治疗AIDS的方法和预防或治疗HIV感染的方法。

    4-(5H-Dibenzo[a,d]cyclohepten-5-yl) piperidine compounds
    7.
    发明公开
    4-(5H-Dibenzo[a,d]cyclohepten-5-yl) piperidine compounds 失效
    4-（5H-二苯并咪唑，叔丁氧羰基-5-基）哌啶化合物

    公开(公告)号：EP0157399A3

    公开(公告)日：1986-02-05

    申请号：EP85103884

    申请日：1985-04-01

    申请人： MERCK & CO. INC.

    发明人： Young, Steven D.

    IPC分类号： C07D211/14 ,  C07D211/16 ,  C07D211/18 ,  C07D211/96 ,  C07D401/04 ,  C07D487/04 ,  A61K31/445 ,  C07D241/00 ,  C07D235/00

    CPC分类号： C07D401/04 ,  C07D211/14 ,  C07D211/16 ,  C07D211/18 ,  C07D211/96 ,  C07D487/04

    摘要： Novel 4-(5H-dibenzo[a,d]cyclohepten-5-yl)-piperidine compounds of the formula:
    are disclosed wherein the bond designation between the 10 and 11 positions indicates that the bond may be a saturated single bond or an unsaturated double bond,
    X is hydrogen, halogen, trifluoromethyl or lower alkoxy; R is, e.g., selected from the group consisting of:
    a) a substituted aralkyl group represented by the formula:
    wherein A is di(lower alkyl)amino or lower alkoxy; b) an aralkenyl group represented by the formula:
    where D is lower alkoxy; c) a nitrogen containing alkyl group represented by the formula:
    wherein Y is -CN,
    or
    d) an acyl group represented by the formula:
    wherein R' is lower alkyl, substituted lower alkyl, phenyl or substituted phenyl, styryl or substituted styryl; and acid addition salts thereof. The compounds have the property of inhibiting calcium induced contraction of the smooth muscle.