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17 条记录 (耗时 0.087 秒)

    Substituted 1,4-diazepines and uses thereof
    2.
    发明授权
    Substituted 1,4-diazepines and uses thereof 有权
    取代的1,4-二氮杂及其用途

    公开(公告)号：US07115598B2

    公开(公告)日：2006-10-03

    申请号：US10829040

    申请日：2004-04-21

    申请人： Tianbao Lu ,  Karen L. Milkiewicz ,  Pierre Raboisson ,  Maxwell David Cummings ,  Raul R. Calvo ,  Daniel J. Parks ,  Louis V. Lafrance, III ,  Juan Jose Marugan Sanchez ,  Joan Gushue ,  Kristi Leonard

    发明人： Tianbao Lu ,  Karen L. Milkiewicz ,  Pierre Raboisson ,  Maxwell David Cummings ,  Raul R. Calvo ,  Daniel J. Parks ,  Louis V. Lafrance, III ,  Juan Jose Marugan Sanchez ,  Joan Gushue ,  Kristi Leonard

    IPC分类号： C07D243/14 ,  A61K31/55

    CPC分类号： C07D243/14

    摘要： The present invention is directed to novel 1,4-diazepines, pharmaceutical compositions thereof, and the use thereof as inhibitors of HDM2-p53 interactions. Compounds have Formula I: or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein: R1, R2, R9, R10, Ra, Rd and M are defined herein;X is a bivalent radical of: an alkane, a cycloalkane, an optionally-substituted arene, an optionally-substituted heteroarene, an optionally-substituted arylalkane or an optionally-substituted heteroarylalkane; andR3 is —CO2Rd, —CO2M, —OH, —NHRd, —SO2Rd, —NHCONHRd, optionally-substituted amidino or optionally-substituted guanidino;or R3—X— is hydrogen or an electron pair;R4 is oxygen or —NR9R10;R5 is cycloalkyl, aryl, heteroaryl, cycloalkylalkyl, aralkyl, heteroarylalkyl, or a saturated or partially unsaturated heterocycle, each of which is optionally substituted; andR6, R7 and R8 are independently hydrogen, alkyl, cycloalkyl, aryl, heteroaryl, a saturated or partially unsaturated heterocycle, cycloalkylalkyl, aralkyl or heteroarylalkyl, each of which is optionally substituted; or R6 and R7, together with the carbon atom to which they are attached form a 3- to 7-membered carbocyclic ring optionally substituted 1 to 3 times with Ra.

    摘要翻译： 本发明涉及新的1,4-二氮杂，其药物组合物及其作为HDM2-p53相互作用抑制剂的用途。 化合物具有式I：或其溶剂合物，水合物或其药学上可接受的盐; 其中：R 1，R 2，R 9，R 10，R a， >，R d和M在本文中定义; X是二价基团：烷烃，环烷烃，任选取代的芳烃，任选取代的杂芳烃，任选取代的芳基烷烃或任选取代的杂芳基烷烃; 和R 3是-CO 2 R 2，-CO 2 M，-OH，-NHR 0 任选取代的脒基或任选取代的胍基;其中R 1，R 2，R 3，R 4， 或R 3 -X-是氢或电子对; R 4是氧或-NR 9 R 10; R 5是环烷基，芳基，杂芳基，环烷基烷基，芳烷基，杂芳基烷基或饱和或部分不饱和的杂环，其各自任选被取代; R 6和R 8独立地是氢，烷基，环烷基，芳基，杂芳基，饱和或部分不饱和的杂环，环烷基烷基 ，芳烷基或杂芳基烷基，其各自任选被取代; 或R 6和R 7与它们所连接的碳原子一起形成3-至7-元碳环，任选地被R 1取代1至3倍， SUP> a 。

    Method for designing protein kinase inhibitors
    4.
    发明授权
    Method for designing protein kinase inhibitors 有权
    蛋白激酶抑制剂的设计方法

    公开(公告)号：US07070936B1

    公开(公告)日：2006-07-04

    申请号：US09482585

    申请日：2000-01-13

    申请人： David G. Hangauer, Jr. ,  Thomas H. Marsilje ,  Karen L. Milkiewicz

    发明人： David G. Hangauer, Jr. ,  Thomas H. Marsilje ,  Karen L. Milkiewicz

    IPC分类号： C12Q1/48 ,  G06F19/00 ,  G01N33/48

    CPC分类号： C12Q1/485

    摘要： The present invention provides a method for identifying inhibitors of protein kinases. Methods are also provided for inhibiting protein kinase activity. Specific non-peptide protein tyrosine kinase inhibitor are provided. The protein kinases produced using the method of the present invention may be used to treat a number of conditions in patients, including cancer, psoriasis, arthrosclerosis, or immune system activity.

    摘要翻译： 本发明提供了鉴定蛋白激酶抑制剂的方法。 还提供了用于抑制蛋白激酶活性的方法。 提供了特异性的非肽蛋白酪氨酸激酶抑制剂。 使用本发明的方法产生的蛋白激酶可用于治疗患者的许多病症，包括癌症，牛皮癣，关节动脉粥样硬化或免疫系统活性。

    Kinase inhibitors
    9.
    发明授权
    Kinase inhibitors 有权
    激酶抑制剂

    公开(公告)号：US07901894B2

    公开(公告)日：2011-03-08

    申请号：US11261858

    申请日：2005-10-27

    申请人： David G. Hangauer ,  Karen L. Milkiewicz

    发明人： David G. Hangauer ,  Karen L. Milkiewicz

    IPC分类号： G01N33/53 ,  C12Q1/48 ,  C12P7/38 ,  C07K5/00 ,  C07K7/00 ,  C07K16/00 ,  C07K17/00 ,  C07D293/00 ,  C07D421/00

    CPC分类号： C12Q1/485 ,  G01N2500/04

    摘要： The present invention provides a method for identifying inhibitors of protein kinases. Methods are also provided for inhibiting protein kinase activity. Specific non-peptide protein tyrosine kinase inhibitors are provided. The protein kinases produced using the method of the present invention may be used to treat a number of conditions in patients, including cancer, psoriasis, atherosclerosis, or immune system activity.

    摘要翻译： 本发明提供了鉴定蛋白激酶抑制剂的方法。 还提供了用于抑制蛋白激酶活性的方法。 提供了特异性的非肽蛋白酪氨酸激酶抑制剂。 使用本发明的方法产生的蛋白激酶可用于治疗患者的许多病症，包括癌症，牛皮癣，动脉粥样硬化或免疫系统活性。