Pyrazoloquinolones as anticancer agents
    12.
    发明授权
    Pyrazoloquinolones as anticancer agents 失效
    吡唑并喹啉酮作为抗癌剂

    公开(公告)号:US5334595A

    公开(公告)日:1994-08-02

    申请号:US967470

    申请日:1992-10-23

    申请人: Mark P. Wentland

    发明人: Mark P. Wentland

    IPC分类号: C07D471/04 A61K31/44

    CPC分类号: C07D471/04

    摘要: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, lower-alkyl, or trifluoromethyl;R.sub.2 is lower-alkyl, trifluoromethyl or CH.sub.2 Y where Y is hydroxy, chloro, lower-alkylamino or dilower-alkylaminoR.sub.3 and R.sub.4 are each independently hydrogen or fluoro;R.sub.5 is hydrogen, lower-alkyl or(a) phenyl, 2-pyridyl, 4-pyridyl, 1-naphthyl or such groups substituted with one or more, the same or different, lower-alkyl, fluoro, hydroxy, or lower-alkoxy;(b) cycloalkyl or cycloalkyl substituted with amino, lower-alkylamino, dilower-alkylamino, formamido, acetamido, lower-alkyl, hydroxy, lower-alkoxy, trifluoromethyl, carboxy, lower-alkoxycarbonyl or halo, or cycloalkyl having a phenyl ring fused thereto;(c) A saturated heterocyclic 5- or 6-membered ring containing oxygen and/or nitrogen or such ring substituted with lower-alkyl; or(d) (CH.sub.2).sub.n -Z wherein n is an integer from about one to four and Z is amino, dilower-alkylamino, bis(hydroxylower-alkyl)lower-alkylamino; or a pharmaceutically acceptable acid addition salt thereof are topoiosmerase II inhibitors and are useful in the treatment of cancer in mammalian hosts.

    摘要翻译: 其中R 1是氢,低级烷基或三氟甲基的式IMA化合物; R2是低级烷基,三氟甲基或CH2Y,其中Y是羟基,氯,低级烷基氨基或二元 - 烷基氨基R3和R4各自独立地是氢或氟; R5是氢,低级烷基或(a)苯基,2-吡啶基,4-吡啶基,1-萘基或被一个或多个相同或不同的低级烷基,氟,羟基或低级 - 烷氧基取代的基团 ; (b)被氨基,低级烷基氨基,二低级烷基氨基,甲酰氨基,乙酰氨基,低级烷基,羟基,低级烷氧基,三氟甲基,羧基,低级烷氧基羰基或卤素取代的环烷基或环烷基或与其稠合的苯环的环烷基 ; (c)含有氧和/或氮或这样被低级烷基取代的环的饱和杂环5或6元环; 或(d)(CH 2)n -Z其中n是约1至4的整数,Z是氨基,二卤代烷基氨基,双(羟基低级烷基)低级烷基氨基; 或其药学上可接受的酸加成盐是拓扑异构酶II抑制剂,并且可用于哺乳动物宿主中的癌症治疗。

    1-Amino-1,8-naphthyridine compounds useful as bactericides
    13.
    发明授权
    1-Amino-1,8-naphthyridine compounds useful as bactericides 失效
    可用作杀菌剂的1-氨基-1,8-萘啶化合物

    公开(公告)号:US4517191A

    公开(公告)日:1985-05-14

    申请号:US537195

    申请日:1983-09-29

    IPC分类号: C07D471/04 A61K31/44

    CPC分类号: C07D471/04

    摘要: Compounds of the formula ##STR1## wherein R is hydrogen or formyl; and R' and R" are hydrogen or lower-alkyl, are useful as antibacterial agents or as intermediates, and are prepared from the corresponding compounds unsubstituted in the 1-position.

    摘要翻译: 式的化合物:其中R是氢或甲酰基; 并且R'和R“是氢或低级烷基,可用作抗菌剂或作为中间体,并且由相应的1-位未取代的化合物制备。

    Aminomethanobenzazocine intermediates
    14.
    再颁专利
    Aminomethanobenzazocine intermediates 失效
    氨基甲基苯并吖嗪中间体

    公开(公告)号:USRE29943E

    公开(公告)日:1979-03-20

    申请号:US826683

    申请日:1977-08-22

    IPC分类号: C07D221/22

    CPC分类号: C07D221/22

    摘要: N-Alkylated-8-aminated-2,6-methano-3-benzazocines, useful as strong analgesics, are prepared by one route comprising reduction of 8-nitro intermediates or by another route comprising Birch type reduction of 8-methoxy intermediates followed by dehydration-rearrangement of the oximes of the resulting 8-oxo intermediates.

    CDKI PATHWAY INHIBITORS AND USES THEREOF
    15.
    发明申请
    CDKI PATHWAY INHIBITORS AND USES THEREOF 有权
    CDKI路径抑制剂及其用途

    公开(公告)号:US20140378683A1

    公开(公告)日:2014-12-25

    申请号:US13923872

    申请日:2013-06-21

    IPC分类号: C07D239/94 C07D403/12

    CPC分类号: C07D239/94 C07D403/12

    摘要: The invention relates to the compounds and methods for inhibiting the Cyclin-Dependent Kinase Inhibitor (CDKI) pathway. More particularly, the invention relates to compounds and methods for inhibiting the CDKI pathway for studies of and intervention in senescence-related and other CDKI-related diseases.

    摘要翻译: 本发明涉及抑制细胞周期蛋白依赖性激酶抑制剂(CDKI)途径的化合物和方法。 更具体地,本发明涉及用于抑制CDKI途径用于衰老相关和其他CDKI相关疾病的研究和干预的化合物和方法。