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    Compounds modifying apoptosis
    6.
    发明授权
    Compounds modifying apoptosis 有权
    化合物修饰凋亡

    公开(公告)号：US08318717B2

    公开(公告)日：2012-11-27

    申请号：US11914994

    申请日：2006-05-23

    申请人： Ole Thastrup ,  Jens Chr. Norrild

    发明人： Ole Thastrup ,  Jens Chr. Norrild

    IPC分类号： A61K31/397 ,  C07C233/00 ,  C07D207/16

    CPC分类号： C07C237/22 ,  C07B2200/11 ,  C07D207/16 ,  C07D211/64

    摘要： The present invention relates to compounds capable of inhibiting binding of the Smac protein to Inhibitors of apoptosis (IAPs). Such compounds are preferably capable of inhibiting IAP and thus may promote apoptosis or sensitize cells for apoptosis. The compounds may be used in the treatment of proliferative diseases, such as cancer.

    摘要翻译： 本发明涉及能够抑制Smac蛋白与凋亡抑制剂（IAP）结合的化合物。 这些化合物优选能够抑制IAP，从而可以促进细胞凋亡或使细胞增殖以进行细胞凋亡。 该化合物可用于治疗增殖性疾病，例如癌症。

    Methods for making 4-tetrazolyl-4-phenylpiperidine compounds
    8.
    发明授权
    Methods for making 4-tetrazolyl-4-phenylpiperidine compounds 有权
    制备4-四唑基-4-苯基哌啶化合物的方法

    公开(公告)号：US08039636B2

    公开(公告)日：2011-10-18

    申请号：US12466797

    申请日：2009-05-15

    申请人： Kevin Brown ,  Timothy J. Doyle ,  John W. F. Whitehead

    发明人： Kevin Brown ,  Timothy J. Doyle ,  John W. F. Whitehead

    IPC分类号： C07D257/04 ,  C07D405/00

    CPC分类号： C07D211/64 ,  C07D257/04 ,  C07D307/22 ,  C07D401/04

    摘要： Methods, composition, and intermediates are disclosed that are useful for making 4-Tetrazolyl-4-phenylpiperidine Compounds according to Formula I, where Ar1 is —C3-C8 cycloalkyl, phenyl, naphthyl, anthryl, phenanthryl or -(5-7-membered) heteroaryl, each being unsubstituted or substituted with one or more R2 groups; Ar2 is phenyl, naphthyl, anthryl, phenanthryl or -(5-7-membered) heteroaryl, each being unsubstituted or substituted with one or more R2 groups; Z1 and Z2 are each independently a —(C1-C4 alkyl) group; R1 is —(CH2)nC(O)N(R3)(R4) where R3 and R4 are each independently H or —(C1-C4 alkyl); R2 is halogen, —C1-C3 alkyl, —O—(C1-C3 alkyl), —NH(C1-C3 alkyl) or —N(C1-C3 alkyl)2; n is an integer ranging from 1 to 4; m is an integer ranging from 0 to 4; and, in certain embodiments, the phenyl moiety attached to the 4-position of the piperidine ring of a compound according to Formula I can be optionally substituted with one or more R2 groups.

    摘要翻译： 公开了可用于制备根据式I的4-四唑基-4-苯基哌啶化合物的方法，组合物和中间体，其中Ar 1是-C 3 -C 8环烷基，苯基，萘基，蒽基，菲基或 - （5-7-元） ）杂芳基，各自为未取代的或被一个或多个R 2基团取代; Ar 2是苯基，萘基，蒽基，菲基或 - （5-7-元）杂芳基，各自是未取代的或被一个或多个R 2基团取代; Z 1和Z 2各自独立地为 - （C 1 -C 4烷基）基团; R1是 - （CH2）nC（O）N（R3）（R4）其中R3和R4各自独立地是H或 - （C1-C4烷基）; R2是卤素，-C1-C3烷基，-O-（C1-C3烷基），-NH（C1-C3烷基）或-N（C1-C3烷基）2; n为1〜4的整数; m为0〜4的整数; 并且在某些实施方案中，连接到根据式I的化合物的哌啶环的4-位的苯基部分可以任选地被一个或多个R 2基团取代。

    THERAPEUTIC AGENTS USEFUL FOR TREATING PAIN
    10.
    发明申请
    THERAPEUTIC AGENTS USEFUL FOR TREATING PAIN 有权
    治疗药物有用的治疗药物

    公开(公告)号：US20100069437A1

    公开(公告)日：2010-03-18

    申请号：US12615510

    申请日：2009-11-10

    申请人： Zhengming Chen

    发明人： Zhengming Chen

    IPC分类号： A61K31/451 ,  C07D211/62 ,  A61K31/454 ,  A61P1/12 ,  A61P25/00

    CPC分类号： C07D401/04 ,  C07D211/64 ,  C07D401/14

    摘要： 4-Tetrazolyl-4-phenylpiperidine Compounds, compositions comprising an effective amount of a 4-Tetrazolyl-4-phenylpiperidine Compound, methods for treating or preventing pain or diarrhea in an animal comprising administering to an animal in need thereof an effective amount of a 4-Tetrazolyl-4-phenylpiperidine Compound and methods for stimulating opioid-receptor function in a cell comprising contacting a cell capable of expressing an opioid receptor with an effective amount of a 4-Tetrazolyl-4-phenylpiperidine Compound are disclosed.

    摘要翻译： 4-四唑基-4-苯基哌啶化合物，包含有效量的4-四唑基-4-苯基哌啶化合物的组合物，用于治疗或预防动物疼痛或腹泻的方法，包括向有需要的动物施用有效量的4 - 四唑基-4-苯基哌啶化合物和用于刺激细胞中阿片受体功能的方法，包括使能够表达阿片受体的细胞与有效量的4-四唑基-4-苯基哌啶化合物接触。