利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

50 条记录 (耗时 0.186 秒)

    Heterocyclic inhibitors of 5-.alpha.-testosterone reductase
    33.
    发明授权
    Heterocyclic inhibitors of 5-.alpha.-testosterone reductase 失效
    5-α-睾酮还原酶的杂环抑制剂

    公开(公告)号：US5302589A

    公开(公告)日：1994-04-12

    申请号：US927091

    申请日：1992-08-07

    申请人： Stephen V. Frye ,  David Middlemiss ,  Francis G. Fang

    发明人： Stephen V. Frye ,  David Middlemiss ,  Francis G. Fang

    IPC分类号： C07D471/06 ,  A61K31/435

    CPC分类号： C07D471/06

    摘要： The present invention relates to certain substituted 17 .beta.-substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 arei) independently hydrogen or lower alkyl and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single or a double bond, orii) taken together are a --CH.sub.2 -- group to form a cyclopropane ring, and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single bond;X is ##STR2## wherein R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are independently hydrogen or lower alkyl,p and q are independently either 0 or 1;R.sup.3 is lower alkyl, lower alkenyl, lower cycloalkyl, lower alkoxy, thiopyridyl, adamantyl, --NR.sup.9 R.sup.10 or --Ar--NR.sup.9 R.sup.10 whereinR.sup.9 and R.sup.10 arei) independently, hydrogen or lower alkyl, lower alkenyl, lower alkynyl, lower cycloalkyl, lower alkoxy, adamantyl, aryl, benzyl, diphenylmethyl, norbornyl orii) taken together with the linking nitrogen to form a 4 to 8 atom heterocyclic group, ##STR3## wherein; Y represents O, CH.sub.2, --N.dbd., NH or N(lower alkyl) optionally substituted with one or more lower alkyl groups;Ar is an aromatic group of 6 to 12 carbons;R.sup.4 is hydrogen or methyl;Z is --O--, --NH--, --N(lower alkyl), --S--, --SO--, --SO.sub.2, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, CO, CO.sub.2, O.sub.2 C, --N.dbd.N-- --CH.dbd.N-- or --N.dbd.CH--;n and m are independently 0, 1 or 2;and pharmaceutically acceptable salts thereof;their preparation, medical use and pharmaceutical formulations.

    摘要翻译： 本发明涉及式（I）的某些取代的17β-取代的羰基-6-氮杂雄甾-4-烯-3-酮：其中R 1和R 2独立地是氢或低级烷基， 带有R1和R2的碳之间的键是单键或双键，或ii）一起形成-CH 2 - 基以形成环丙烷环，并且具有R 1和R 2的碳之间的键是单键; X为，其中R 5，R 6，R 7和R 8独立地为氢或低级烷基，p和q独立地为0或1; R3为低级烷基，低级烯基，低级环烷基，低级烷氧基，硫代吡啶基，金刚烷基，-NR9R10或-Ar-NR9R10，其中R9和R10为i）独立地为氢或低级烷基，低级烯基，低级炔基，低级环烷基， ，金刚烷基，芳基，苄基，二苯甲基，降冰片基或ii）与连接氮一起形成4至8个原子的杂环基，其中; Y表示任选被一个或多个低级烷基取代的O，CH 2，-N =，NH或N（低级烷基） Ar为6〜12个碳原子的芳香族基团; R4是氢或甲基; Z是-O - ， - NH - ， - N（低级烷基），-S - ， - SO - ， - SO 2，-CH 2 CH 2 - ， - CH = CH-，CO，CO 2， CH = N-或-N = CH-; n和m独立地为0,1或2; 及其药学上可接受的盐; 其制剂，医疗用途和药物配方。

    Heterocyclic compounds
    40.
    发明申请
    Heterocyclic compounds 审中-公开
    杂环化合物

    公开(公告)号：US20120041195A1

    公开(公告)日：2012-02-16

    申请号：US13201165

    申请日：2010-02-09

    申请人： Caroline Leriche ,  Eric Auclair ,  Jacques Le Roux ,  David Middlemiss

    发明人： Caroline Leriche ,  Eric Auclair ,  Jacques Le Roux ,  David Middlemiss

    IPC分类号： C07D471/04

    CPC分类号： C07D471/04

    摘要： The invention is directed to certain novel compounds, methods for producing them and methods for treating or ameliorating a kinase-mediated disorder. More particularly, this invention is directed to substituted triazolopyridine compounds useful as selective kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase-mediated disorder. In particular, the methods relate to treating or ameliorating a kinase-mediated disorder including cardiovascular diseases, diabetes, diabetes-associated disorders, inflammatory diseases, immunological disorders, cancer and diseases of the eye such as retinopathies or macular degeneration or other vitreoretinal diseases, and the like.

    摘要翻译： 本发明涉及某些新化合物，其制备方法和用于治疗或改善激酶介导的病症的方法。 更具体地，本发明涉及可用作选择性激酶抑制剂的取代的三唑并吡啶化合物，用于制备这些化合物的方法和用于治疗或改善激酶介导的病症的方法。 特别地，所述方法涉及治疗或改善包括心血管疾病，糖尿病，糖尿病相关疾病，炎性疾病，免疫学疾病，癌症和眼睛疾病如视网膜病变或黄斑变性或其他玻璃体视网膜疾病的激酶介导的疾病，以及 类似。