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26 条记录 (耗时 0.024 秒)

    TYROSINE KINASE INHIBITORS
    1.
    发明公开
    TYROSINE KINASE INHIBITORS 审中-公开
    酪氨酸激酶抑制剂

    公开(公告)号：EP1496897A1

    公开(公告)日：2005-01-19

    申请号：EP03723935.7

    申请日：2003-04-08

    申请人： Merck & Co., Inc.

    发明人： KIM, Annette ,  STUMP, Craig, A. ,  DINSMORE, Christopher, J. ,  GRAHAM, Samuel, L. ,  WILLIAMS, Theresa, M. ,  NGUYEN, Diem, N. ,  TROTTER, B. Wesley

    IPC分类号： A61K31/439 ,  C07D221/22 ,  A61P35/00

    CPC分类号： C07D471/08 ,  A01M31/06

    摘要： The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating signal transduction of both receptor-type and non-receptor type tyrosine kinases. The compounds of the instant invention possess a core structure that comprises a benzazocine moiety. The present invention is also related to the pharmaceutically acceptable salts, hydrates and stereoisomers of these compounds.

    摘要翻译： 本发明涉及能够抑制，调节和/或调节受体型和非受体型酪氨酸激酶的信号转导的化合物。 本发明的化合物具有包含苯并佐菌酮部分的核心结构。 本发明还涉及这些化合物的药学上可接受的盐，水合物和立体异构体。

    INHIBITORS OF FARNESYL-PROTEIN TRANSFERASE
    2.
    发明公开
    INHIBITORS OF FARNESYL-PROTEIN TRANSFERASE 失效
    法尼蛋白转移酶抑制剂

    公开(公告)号：EP0891337A1

    公开(公告)日：1999-01-20

    申请号：EP97917131.0

    申请日：1997-03-31

    申请人： MERCK & CO., INC.

    发明人： GRAHAM, Samuel, L. ,  ANTHONY, Neville, J. ,  WAI, John, S.

    IPC分类号： A61K31 ,  A61P13 ,  A61P27 ,  A61P31 ,  A61P35 ,  A61P43 ,  C07D243 ,  C07D403

    CPC分类号： C07D243/24

    摘要： The present invention is directed to substituted benzodiazepine compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.

    摘要翻译： 本发明涉及抑制法尼基蛋白转移酶（FTase）和癌基因蛋白Ras的法尼基化的取代的苯并二氮杂类化合物。 本发明还涉及含有本发明化合物的化学治疗组合物以及抑制法尼基蛋白转移酶和癌基因蛋白Ras的法尼基化的方法。

    INHIBITORS OF FARNESYL-PROTEIN TRANSFERASE
    5.
    发明公开
    INHIBITORS OF FARNESYL-PROTEIN TRANSFERASE 失效
    法尼蛋白转移酶抑制剂

    公开(公告)号：EP0783305A1

    公开(公告)日：1997-07-16

    申请号：EP95934549.0

    申请日：1995-09-25

    申请人： Merck & Co., Inc.

    发明人： ANTHONY, Neville, J. ,  deSOLMS, S., Jane ,  GRAHAM, Samuel, L.

    IPC分类号： C12N9 ,  A61K31 ,  A61K38 ,  A61P35 ,  A61P43 ,  C07D207 ,  C07K5

    CPC分类号： C07D207/09 ,  A61K38/00 ,  C07K5/06078

    摘要： The present invention comprises analogs of the CA1A2X motif of the protein Ras that is modified by farnesylation in vivo. These CA1A2X analogs inhibit the farnesylation of Ras. Furthermore, these CA1A2X analogs differ from those previously described as inhibitors of Ras farnesly transferase in that they have a prolyl like moiety in the A1 position. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.

    摘要翻译： 本发明包括被体内法尼基化修饰的蛋白质Ras的CA1A2X基序的类似物。 这些CA1A2X类似物抑制Ras的法尼基化。 此外，这些CA1A2X类似物不同于之前描述为Ras法尼基转移酶的抑制剂，因为它们在A1位具有脯氨酰样部分。 本发明还包含含有这些法尼基转移酶抑制剂的化学治疗组合物及其制备方法。

    BICYCLIC SPIROPIPERIDINE BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE
    7.
    发明公开
    BICYCLIC SPIROPIPERIDINE BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE 有权
    双环螺哌啶β-分泌酶抑制剂用于治疗阿尔茨海默氏病的治疗

    公开(公告)号：EP2117309A1

    公开(公告)日：2009-11-18

    申请号：EP07868113.7

    申请日：2007-12-28

    申请人： Merck & Co., Inc.

    发明人： STAUFFER, Shaun, R. ,  GRAHAM, Samuel, L.

    IPC分类号： A01N43/42 ,  A61K31/44

    CPC分类号： C07D471/20

    摘要： The present invention is directed to bicyclic spiropiperidine compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.