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    Metalloprotease inhibitors containing a heterocyclic moiety
    5.
    发明申请
    Metalloprotease inhibitors containing a heterocyclic moiety 失效
    含有杂环部分的金属蛋白酶抑制剂

    公开(公告)号：US20080221091A1

    公开(公告)日：2008-09-11

    申请号：US12074994

    申请日：2008-03-07

    Applicant: Christian Gege ,  Arthur Taveras

    Inventor： Christian Gege ,  Arthur Taveras

    IPC: A61K31/5383 ,  C07D498/04 ,  A61P19/02 ,  A61P29/00

    CPC classification number: C07D498/02 ,  C07D487/02 ,  C07D519/00

    Abstract: The present invention relates generally to pharmaceutical agents containing a heterocyclic moiety, and in particular, to heterocyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of heterocyclic MMP-13 inhibiting compounds with a modified benzoxazine moiety, that exhibit an increased potency and selectivity in relation to currently known MMP-13 inhibitors.

    Abstract translation: 本发明一般涉及含有杂环部分的药剂，尤其涉及杂环金属蛋白酶抑制化合物。 更具体地说，本发明提供了一种具有改性苯并恶嗪部分的新一类杂环基MMP-13抑制化合物，与目前已知的MMP-13抑制剂相比，其表现出增加的效力和选择性。

    Antitumoral d-homoestra-1,3,5 (10)-trien-3-yl 2-substituted sulfamates
    8.
    发明申请
    Antitumoral d-homoestra-1,3,5 (10)-trien-3-yl 2-substituted sulfamates 有权
    抗肿瘤D-同型异构-1,3,5（10） - 三烯-3-基2-取代的亚磺酸盐

    公开(公告)号：US20060154985A1

    公开(公告)日：2006-07-13

    申请号：US10546230

    申请日：2004-02-19

    Applicant: Alexander Hillisch ,  Olaf Peters ,  Christian Gege ,  Gerhard Siemeister ,  Ebehard Unger ,  Bernd Menzenbach

    Inventor： Alexander Hillisch ,  Olaf Peters ,  Christian Gege ,  Gerhard Siemeister ,  Ebehard Unger ,  Bernd Menzenbach

    IPC: A61K31/255

    CPC classification number: C07J63/00

    Abstract: This invention relates to 2-substituted D-homo-estra-1,3,5(10)-trien-3-yl sulfamates of general formula I (I), in which R3 means a C1-C5-alkyl or C1-C5-alkyloxy group as well as their use for the production of a pharmaceutical agent for treating tumor diseases, which can be influenced positively by the inhibition of tubulin polymerization. The compounds according to the invention are distinguished by a D-homosubstitution. They have a special action with respect to tubulin polymerization inhibition and can be used, for example, for treating prostate cancer.

    Abstract translation: 本发明涉及通式I（I）的2-取代的D-均 - 雌-1,3,5（10） - 三烯-3-基氨基磺酸酯，其中R 3表示C 1 -C 5 - 烷基或C 1 -C 5 - 烷氧基以及它们用于生产用于治疗肿瘤疾病的药剂的用途，其可通过抑制微管蛋白聚合而受到积极的影响。 根据本发明的化合物通过D-均质化来区分。 它们在微管蛋白聚合抑制方面具有特殊的作用，可用于例如治疗前列腺癌。

    New 2-substituted estra-1,3,5(10)-trien-17-ones as inhibitors of 17beta-hydroxy steroid dehydrogenase type 1
    9.
    发明申请
    New 2-substituted estra-1,3,5(10)-trien-17-ones as inhibitors of 17beta-hydroxy steroid dehydrogenase type 1 失效

    公开(公告)号：US20060009434A1

    公开(公告)日：2006-01-12

    申请号：US11154947

    申请日：2005-06-17

    Applicant: Alexander Hillisch ,  Olaf Peters ,  Christian Gege ,  Wilko Regenhardt ,  Andrea Rosinus ,  Jerzy Adamski ,  Gabriele Moeller

    Inventor： Alexander Hillisch ,  Olaf Peters ,  Christian Gege ,  Wilko Regenhardt ,  Andrea Rosinus ,  Jerzy Adamski ,  Gabriele Moeller

    IPC: A61K31/57 ,  C07J1/00

    CPC classification number: C07J1/00

    Abstract: The invention relates to new 2-substituted estra-1,3,5(10)-trien-17-ones of general formula I in which R2 means a saturated or unsaturated C1-C8-alkyl group, a C1-C5-alkyloxy group, an aralkyl radical or alkylaryl radical, a radical —O—CnFmHo, whereby n=1, 2, 3, 4, 5 or 6, m≧1 and m+o=2n+1, or a group CH2XY, in which X stands for an oxygen atom and Y stands for an alkyl radical with 1 to 4 carbon atoms, as well as a halogen atom or a nitrile group, R13 means a hydrogen atom or a methyl group, R16 means a hydrogen atom or a fluorine atom, Z means an oxygen atom or a sulfur atom, R3 and R5, in each case independently of one another, mean an α- or β-position hydrogen atom, R4 and R6, in each case independently of one another, mean an α- or β-position hydrogen atom, a C1-C5-alkyl group, a C1-C5-alkyloxy group, a C1-C5-acyl group or a hydroxy group or an aralkyl radical or alkylaryl radical, R3 and R4 together mean an oxygen atom, R5 and R6 together mean an oxygen atom, R7 and R8 in each case mean a hydrogen atom or together a CH2 group, as well as their pharmaceutically acceptable salts, their manufacture and use as medicaments for prophylaxis and therapy of estrogen-dependent diseases that can be influenced by the inhibition of 17β-hydroxy steroid dehydrogenase type 1.

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