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37 条记录 (耗时 0.099 秒)

    Six-membered heterocycles useful as serine protease inhibitors
    31.
    发明授权
    Six-membered heterocycles useful as serine protease inhibitors 有权
    用作丝氨酸蛋白酶抑制剂的六元杂环

    公开(公告)号：US08163749B2

    公开(公告)日：2012-04-24

    申请号：US12097080

    申请日：2006-12-13

    申请人： James R. Corte

    发明人： James R. Corte

    IPC分类号： A01N43/58 ,  A61K31/50 ,  A61K31/44 ,  A61K31/13 ,  C07D221/18 ,  C07D421/00

    CPC分类号： C07D213/40 ,  C07D213/54 ,  C07D213/63 ,  C07D213/64 ,  C07D213/73 ,  C07D213/89 ,  C07D239/26 ,  C07D401/04 ,  Y10S514/822

    摘要： The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, R3 and R11 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

    摘要翻译： 本发明提供式（I）化合物或其立体异构体，互变异构体，药学上可接受的盐或溶剂合物形式，其中变量A，B，R 3和R 11如本文所定义。 式（I）的化合物可用作凝血级联和/或接触激活系统的丝氨酸蛋白酶的选择性抑制剂; 例如凝血酶，因子Xa，因子XIa，因子IXa，因子VIIa和/或血浆激肽释放酶。 特别地，它涉及作为选择性因子XIa抑制剂或fXIa和血浆激肽释放酶的双重抑制剂的化合物。 本发明还涉及包含这些化合物的药物组合物和使用其制备血栓栓塞和/或炎症性疾病的方法。

    SIX-MEMBERED HETEROCYCLES USEFUL AS SERINE PROTEASE INHIBITORS
    33.
    发明申请
    SIX-MEMBERED HETEROCYCLES USEFUL AS SERINE PROTEASE INHIBITORS 有权
    作为丝氨酸蛋白酶抑制剂有作用的六组分异构体

    公开(公告)号：US20090181983A1

    公开(公告)日：2009-07-16

    申请号：US12097080

    申请日：2006-12-13

    申请人： James R. Corte

    发明人： James R. Corte

    IPC分类号： A61K31/505 ,  C07D213/55 ,  A61K31/44 ,  C07D239/26 ,  A61P7/02

    CPC分类号： C07D213/40 ,  C07D213/54 ,  C07D213/63 ,  C07D213/64 ,  C07D213/73 ,  C07D213/89 ,  C07D239/26 ,  C07D401/04 ,  Y10S514/822

    摘要： The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, R3 and R11 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

    摘要翻译： 本发明提供式（I）化合物或其立体异构体，互变异构体，药学上可接受的盐或溶剂合物形式，其中变量A，B，R 3和R 11如本文所定义。 式（I）的化合物可用作凝血级联和/或接触激活系统的丝氨酸蛋白酶的选择性抑制剂; 例如凝血酶，因子Xa，因子XIa，因子IXa，因子VIIa和/或血浆激肽释放酶。 特别地，它涉及作为选择性因子XIa抑制剂或fXIa和血浆激肽释放酶的双重抑制剂的化合物。 本发明还涉及包含这些化合物的药物组合物和使用其制备血栓栓塞和/或炎症性疾病的方法。

    3-arylquinazoline derivatives as selective estrogen receptor beta modulators
    34.
    发明授权
    3-arylquinazoline derivatives as selective estrogen receptor beta modulators 有权
    3-芳基喹唑啉衍生物作为选择性雌激素受体β调节剂

    公开(公告)号：US07381730B2

    公开(公告)日：2008-06-03

    申请号：US10387666

    申请日：2003-03-13

    申请人： Timur Gungor ,  James R. Corte

    发明人： Timur Gungor ,  James R. Corte

    IPC分类号： A61K31/517 ,  C07D239/88 ,  C07D239/93

    CPC分类号： C07D273/00 ,  C07D209/38 ,  C07D239/91 ,  C07D401/04

    摘要： Novel quinazoline derivatives possessing activity as estrogen receptor beta (ERβ) modulators are provided which have the general formula I wherein X is O or S; A and B are each independently CR′″ or N; R, R′ and R″ are each independently hydrogen, alkyl, benzyl, p-methoxybenzyl, allyl, or Si(R4)3, wherein at least one of R, R′ and R″ is hydrogen; R′″ is hydrogen, halogen, CF3, OR5, S(O)nR6, NR7R8, cycloalkyl or alkyl; R1, R2 and R3 are each independently hydrogen, halogen, CF3, OR5, S(O)nR6, NR7R8, cycloalkyl or alkyl; R4 is a alkyl; R5, R6, R7 and R8 in each functional group are each independently hydrogen, cycloalkyl or alkyl; and n is an integer from 0 to 2. In addition, a method is provided for preventing, inhibiting or treating the progression or onset of pathological conditions associated with the estrogen receptor and to pharmaceutical compositions containing such compounds.

    摘要翻译： 提供具有雌激素受体β（ERbeta）调节剂活性的新型喹唑啉衍生物，其具有通式I，其中X为O或S; A和B各自独立地为CR“或N; R，R'和R“各自独立地为氢，烷基，苄基，对甲氧基苄基，烯丙基或Si（R 4 N 3）3，其中至少一个 R，R'和R“是氢; R“'是氢，卤素，CF 3或OR 5，S（O）n R 6 R 6， NR 7 R 8，环烷基或烷基; R 1，R 2和R 3各自独立地为氢，卤素，CF 3或OR 3， 5，S（O）n R 6，NR 7 R 8，环烷基或烷基 ; R 4是烷基; 各官能团中的R 5，R 6，R 7和R 8分别独立地为氢，环烷基或 烷基; n为0-2的整数。此外，提供了用于预防，抑制或治疗与雌激素受体相关的病理状况的进展或发作的方法以及含有这些化合物的药物组合物。

    C-5 substituted quinazolinone derivatives as selective estrogen receptor beta modulators
    37.
    发明授权
    C-5 substituted quinazolinone derivatives as selective estrogen receptor beta modulators 有权
    C-5取代喹唑啉酮衍生物作为选择性雌激素受体β调节剂

    公开(公告)号：US07456188B1

    公开(公告)日：2008-11-25

    申请号：US11411456

    申请日：2006-04-26

    申请人： James R. Corte ,  John K. Dickson ,  Timur Gungor

    发明人： James R. Corte ,  John K. Dickson ,  Timur Gungor

    IPC分类号： A61K31/517 ,  C07D239/88

    CPC分类号： C07D239/91 ,  C07D239/93

    摘要： The present application describes compounds according to Formula I, wherein Q, R1, R2 and X are described herein, that are useful as Estrogen Receptor Beta (ERβ) modulators. Additionally, the present application describes pharmaceutical compositions containing the compounds according to Formula I and optionally additional therapeutic agents. Finally, the present application describes methods utilizing the compounds according to Formula I for modulating the function of ERβ in the treatment of diseases and disorders associated with ERβ such as, for example, bone disorders; cardiovascular diseases; hypercholesterolemia; hypertriglyceridemia; vasomotor disorders; urogenital disorders; prostatic hypertrophy; endometrial hyperplasia; cancer and central nervous system disorders, such as, neurodegenerative disorders.

    摘要翻译： 本申请描述了根据式I的化合物，其中Q，R 1，R 2和X在本文中描述，其可用作雌激素受体β（ERβ）调节剂。 此外，本申请描述了含有根据式I的化合物和任选的另外的治疗剂的药物组合物。 最后，本申请描述了利用式I化合物调节ERbeta在治疗与ERBeta相关的疾病和病症（例如骨病）中的功能的方法; 心血管疾病; 高胆固醇血症 高甘油三酯血症 血管舒缩障碍 泌尿生殖系统疾病 前列腺肥大; 子宫内膜增生; 癌症和中枢神经系统疾病，如神经变性疾病。