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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。

    Fused pyrimidines as inhibitors of p97 complex
    4.
    发明授权
    Fused pyrimidines as inhibitors of p97 complex 有权
    融合的嘧啶作为p97复合物的抑制剂

    公开(公告)号：US09475824B2

    公开(公告)日：2016-10-25

    申请号：US14416033

    申请日：2013-07-19

    申请人： Cleave Biosciences, Inc.

    发明人： Han-Jie Zhou ,  Francesco Parlati ,  David Wustrow

    IPC分类号： C07D403/04 ,  C07D471/04 ,  C07D495/04 ,  C07D491/048 ,  C07D491/052 ,  A61K31/517 ,  A61K31/519 ,  C07D513/04 ,  C07D405/04 ,  C07D473/34 ,  C07D487/04

    CPC分类号： A61K31/519 ,  A61K31/517 ,  C07D403/04 ,  C07D405/04 ,  C07D471/04 ,  C07D473/34 ,  C07D487/04 ,  C07D491/048 ,  C07D491/052 ,  C07D495/04 ,  C07D513/04

    摘要： Disclosed are fused pyrimidine compounds having scaffolds composed of left and right rings, the left ring being a saturated carbocyclic or heterocyclic ring and the right ring being a pyrimidine ring. The left saturated ring is fused to the pyrimidine ring at the 5 and 6 carbons of the pyrimidine. The saturated ring may be 5 or 6 members in size and may be all carbon or may contain a single oxygen, sulfur or nitrogen atom as one of the non-fused members of the ring. The pyrimidine ring is substituted at the two position by a 5:6 bicyclic aromatic heterocycle such as indole, benzimidazole or benzopyrazole and at the four position by an aryl methyl amino group. The 5:6 bicyclic aromatic heterocycle is substituted at its 2 position by hydrogen or an aliphatic or functional aliphatic group and at the 4 position by a functional group as described herein. The aryl methyl amino group may be aminobenzyl or aminomethyl-substituted phenyl. These fused pyrimidine compounds are inhibitors of the AAA proteosome complex containing the enzyme complex p97 and are effective medicinal agents for the treatment of diseases associated with p97 bioactivity such as cancer.

    摘要翻译： 公开了具有由左右环构成的支架的稠合嘧啶化合物，左环为饱和碳环或杂环，右环为嘧啶环。 在嘧啶的5和6个碳上，左饱和环与嘧啶环稠合。 饱和环的大小可以是5或6个成员，并且可以是全部碳，或者可以含有作为环的非稠合成员之一的单个氧，硫或氮原子。 嘧啶环在两个位置被5：6双环芳族杂环如吲哚，苯并咪唑或苯并吡唑取代，在四位被芳基甲基氨基取代。 5：6双环芳族杂环在其2位被氢或脂族或官能脂族基团取代，在4位被官能团取代。 芳基甲基氨基可以是氨基苄基或氨基甲基取代的苯基。 这些稠合的嘧啶化合物是含有酶复合物p97的AAA蛋白质复合物的抑制剂，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
    6.
    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.

    Monocyclic pyrimidine/pyridine compounds as inhibitors of P97 complex
    10.
    发明授权
    Monocyclic pyrimidine/pyridine compounds as inhibitors of P97 complex 有权

    公开(公告)号：US09868722B2

    公开(公告)日：2018-01-16

    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 ,  A61K31/506

    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.