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    MONOCYCLIC PYRIMIDINE/PYRIDINE COMPOUNDS AS INHIBITORS OF P97 COMPLEX
    1.
    发明申请
    MONOCYCLIC PYRIMIDINE/PYRIDINE COMPOUNDS AS INHIBITORS OF P97 COMPLEX 有权
    作为P97复合物的抑制剂的单环吡嗪/吡啶化合物

    公开(公告)号：US20160304495A1

    公开(公告)日：2016-10-20

    申请号：US15103828

    申请日：2014-12-10

    申请人： CLEAVE BIOSCIENCES, INC.

    发明人： David Wustrow ,  Han-Jie Zhou

    IPC分类号： C07D403/04

    CPC分类号： C07D403/04 ,  A61K31/506

    摘要： Monocyclic pyrimidine and pyridine compounds having a benzyl amine substituent at the 4 position and a 5:6 bicyclic heteroaryl substituent at the 2 position of the pyrimidine or pyridine ring as well as optional aliphatic, functional and/or aromatic components substituted at other positions of the ring are disclosed. These compounds are inhibitors of the AAA proteasome complex containing p97 and are effective medicinal agents for treatment of diseases associated with p97 bioactivity such as cancer.

    摘要翻译： 在嘧啶或吡啶环的2位具有苄基胺取代基的四唑化合物和嘧啶或吡啶环2位上的5：6双环杂芳基取代基的单环嘧啶和吡啶化合物以及在其它位置上被取代的任选的脂族，官能和/ 环被披露。 这些化合物是含有p97的AAA蛋白酶体复合物的抑制剂，并且是用于治疗与p97生物活性相关的疾病如癌症的有效药物。

    NITROGEN HEXACYCLE COMPOUNDS AS INHIBITORS OF p97 COMPLEX
    5.
    发明申请
    NITROGEN HEXACYCLE COMPOUNDS AS INHIBITORS OF p97 COMPLEX 审中-公开
    作为p97复合物的抑制剂的硝酸六异氰酸酯化合物

    公开(公告)号：US20160355503A1

    公开(公告)日：2016-12-08

    申请号：US15173294

    申请日：2016-06-03

    申请人： Cleave Biosciences, Inc.

    发明人： Han-Jie Zhou ,  David Wustrow

    IPC分类号： C07D403/04

    CPC分类号： C07D403/04

    摘要： Nitrogen hexacycle compounds having an arylalkyl amine substituent at the P4 position and a substituted 5:6 bicyclic group at the P2 position of the nitrogen hexacycle as well as optional aliphatic, functional and/or aromatic components substituted at other positions of the nitrogen hexacycle, the aryl alkyl group and the 5:6 bicyclic group are disclosed. These compounds are inhibitors of the AAA proteasome complex containing p97 and are effective medicinal agents for treatment of diseases associated with p97 bioactivity such as cancer.

    摘要翻译： 在P4位具有芳烷基胺取代基的氮六元环化合物和在氮六元环的P2位置上的取代的5：6双环基团以及在氮六环的其它位置被取代的任选的脂族，官能和/或芳族组分， 芳基烷基和5：6双环基团。 这些化合物是含有p97的AAA蛋白酶体复合物的抑制剂，并且是用于治疗与p97生物活性相关的疾病如癌症的有效药物。

    Fused pyrimidines as inhibitors of p97 complex
    8.
    发明授权
    Fused pyrimidines as inhibitors of p97 complex 有权

    公开(公告)号：US10174005B2

    公开(公告)日：2019-01-08

    申请号：US15792514

    申请日：2017-10-24

    申请人： Cleave Biosciences, Inc.

    发明人： Han-Jie Zhou ,  David Wustrow

    IPC分类号： C07D403/04 ,  C07D471/04 ,  C07D491/048 ,  C07D491/052

    摘要： The present invention is directed to certain fused pyrimidines having a homo or hetero cyclopentyl, cyclohexyl or cycloheptyl ring as the pyrimidine fusion partner; having an amino benzyl or substituted amino benzyl group at the 4 position of the pyrimidine ring; and a 5:6 heterobicyclo ring with at least one N, O or S at the 2 position of the pyrimidine ring. These compounds are useful for treatment of cancer by inhibition of the p97 complex.