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    Quinoxaline inhibitors of the hedgehog signalling
    1.
    发明授权
    Quinoxaline inhibitors of the hedgehog signalling 失效
    刺猬信号的喹喔啉抑制剂

    公开(公告)号：US08273743B2

    公开(公告)日：2012-09-25

    申请号：US11587963

    申请日：2005-04-29

    申请人： Michael F. T. Koehler ,  Richard Goldsmith ,  Daniel P. Sutherlin

    发明人： Michael F. T. Koehler ,  Richard Goldsmith ,  Daniel P. Sutherlin

    IPC分类号： A61K31/495 ,  A61K31/44

    CPC分类号： C07D413/12 ,  C07D241/42 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12

    摘要： The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A is a carbocycle or heterocycle; X is alkylene, NR4C(O), NR4C(S), NR4C(NH), NR4SO, NR4SO2, NR4C(O)NH, NR4C(S)NH, C(O)NR4, C(S)NR4, C(NH)NR4, NR4PO or NR4PO(OH) wherein R4 is H or alkyl; R1 is selected from the group consisting of alkyl, cycloalkyl, aryl or a heterocycle each of which is optionally substituted with hydroxy, halogen, amino, nitro, alkyl, acyl, alkylsulfonyl or alkoxy; R2 is halogen, hydroxy, alkyl, acyl or alkoxy each optionally substituted with hydroxy, halogen, amino, nitro, alkyl, acyl, alkylsulfonyl or alkoxy; R3 is halogen, hydroxy, alkyl, acyl or alkoxy each optionally substituted with hydroxy, halogen, amino, nitro, alkyl, acyl, alkylsulfonyl or alkoxy; m is 0-3; n is 0-3; and salts and solvates thereof. The invention also provides methods of using these compounds for therapy and/or prophylaxis in a mammal of hyperproliferative diseases and angiogenesis mediated diseases due to their activity for inhibiting the hedgehog signaling pathway.

    摘要翻译： 本发明提供了可用作治疗恶性肿瘤的治疗剂的刺猬蛋白信号传导的新型抑制剂，其中化合物具有通式I：其中A是碳环或杂环; X是亚烷基，NR4C（O），NR4C（S），NR4C（NH），NR4SO，NR4SO2，NR4C（O）NH，NR4C（S）NH，C（O）NR4，C（S）NR4，C ）NR4，NR4PO或NR4PO（OH），其中R4是H或烷基; R1选自烷基，环烷基，芳基或杂环，其各自任选被羟基，卤素，氨基，硝基，烷基，酰基，烷基磺酰基或烷氧基取代; R2是卤素，羟基，烷基，酰基或烷氧基，各自任选被羟基，卤素，氨基，硝基，烷基，酰基，烷基磺酰基或烷氧基取代; R3是卤素，羟基，烷基，酰基或烷氧基，各自任选被羟基，卤素，氨基，硝基，烷基，酰基，烷基磺酰基或烷氧基取代; m为0-3; n为0-3; 及其盐和溶剂合物。 本发明还提供了使用这些化合物治疗和/或预防哺乳动物由于其抑制刺猬蛋白信号通路的活性而引起的过度增殖性疾病和血管生成介导的疾病的方法。

    Arylsulfonamide compounds
    5.
    发明授权
    Arylsulfonamide compounds 有权
    芳基磺酰胺化合物

    公开(公告)号：US08168645B2

    公开(公告)日：2012-05-01

    申请号：US12513835

    申请日：2007-11-15

    申请人： Jonathan Bayldon Baell ,  Guillaume Laurent Lessene ,  Brad Edmund Sleebs ,  Wayne J. Fairbrother ,  John A. Flygare ,  Michael F. T. Koehler

    发明人： Jonathan Bayldon Baell ,  Guillaume Laurent Lessene ,  Brad Edmund Sleebs ,  Wayne J. Fairbrother ,  John A. Flygare ,  Michael F. T. Koehler

    IPC分类号： A61K31/517 ,  C07D239/72

    CPC分类号： C07D239/94

    摘要： The invention relates generally to small molecules that mimic the biological activity of certain peptides and proteins, to compositions containing them and to their use. In particular, the invention relates to compounds of the general formula (I) that mimic the biological activity of BH3-only proteins and are capable of binding to and neutralizing pro-survival Bcl-2 proteins: wherein A1, A2, B1, B2, B3, X, Z, R1, R2, R3 and t are as described herein. The invention also relates to processes of preparing the benzenesulfonamide compounds that mimic portions of peptides and proteins, and to the use of such compounds in the regulation of cell death and the treatment and/or prophylaxis of diseases or conditions associated with the deregulation of cell death.

    摘要翻译： 本发明一般涉及模拟某些肽和蛋白质的生物学活性的小分子，含有它们的组合物及其用途。 特别地，本发明涉及模拟仅含BH3蛋白的生物学活性的通式（I）的化合物，并能够结合并中和原生存Bcl-2蛋白：其中A1，A2，B1，B2， B3，X，Z，R1，R2，R3和t如本文所述。 本发明还涉及制备模仿肽和蛋白质的一部分的苯磺酰胺化合物的方法，以及这些化合物在调节细胞死亡中的用途以及治疗和/或预防与细胞死亡调节相关的疾病或病症 。

    Imidazopyridine inhibitors of IAP
    6.
    发明授权
    Imidazopyridine inhibitors of IAP 有权
    IAP的咪唑并吡啶抑制剂

    公开(公告)号：US08063218B2

    公开(公告)日：2011-11-22

    申请号：US12520205

    申请日：2007-12-14

    申请人： Michael F. T. Koehler

    发明人： Michael F. T. Koehler

    IPC分类号： C07D491/02

    CPC分类号： C07D471/04

    摘要： The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein Q, X1, X2, Y, Z R1, R2, R3, R3′, R4, R4′, R5, R6, R6′ and n are as described herein.

    摘要翻译： 本发明提供了可用作治疗恶性肿瘤的治疗剂的新的IAP抑制剂，其中化合物具有通式I：其中Q，X1，X2，Y，Z R1，R2，R3，R3'，R4，R4'，R5 ，R6，R6'和n如本文所述。