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    Tetrazolyl containing naphthyridine 3-carboxamides
    42.
    发明授权
    Tetrazolyl containing naphthyridine 3-carboxamides 失效
    含有四氮唑的三氮杂萘-3-甲酰胺

    公开(公告)号：US3943141A

    公开(公告)日：1976-03-09

    申请号：US455072

    申请日：1974-03-27

    申请人： Gwynn Pennant Ellis ,  Ian Collins ,  David Martin Waters ,  David Edmund Bays

    发明人： Gwynn Pennant Ellis ,  Ian Collins ,  David Martin Waters ,  David Edmund Bays

    IPC分类号： C07D471/04 ,  C07D401/14

    CPC分类号： C07D471/04 ,  Y10S514/826 ,  Y10S514/861

    摘要： Compounds of the general formulae I and II and pharmaceutically acceptable salts thereof: ##SPC1##In which:R.sub.1 represents a hydrogen atom, a halogen atom, an alkenyl or alkyl group; or a group OR.sub.3 or NR.sub.3 R.sub.4 where R.sub.3 and R.sub.4 which may be the same or different and may represent a hydrogen atom, or an alkenyl group, or an alkyl group which alkyl group may optionally be substituted by one or more hydroxy, alkoxy, acyloxy, aryl, amino, alkylamino, dialkylamino, diaralkylamino or alkylaralkylamino groups; or R.sub.3 and R.sub.4 together with the nitrogen atom form a 5 or 6 membered heterocyclic ring that may optionally contain other hetero atoms.R.sub.2 has the same meanings as R.sub.3.The compounds have utility for the treatment of conditions in which combination of an antigen with a reaginic antibody is primarily responsible.

    摘要翻译： 通式I和II的化合物及其药学上可接受的盐：

    9H-pyrimido[4,5-B]indoles, 9H-pyrido[4',3':4,5]pyrrolo[2,3-D]pyridines, and 9H 1,3,6,9 tetraaza-fluorenes as CHK1 kinase function inhibitors
    46.
    发明授权
    9H-pyrimido[4,5-B]indoles, 9H-pyrido[4',3':4,5]pyrrolo[2,3-D]pyridines, and 9H 1,3,6,9 tetraaza-fluorenes as CHK1 kinase function inhibitors 有权
    9H-嘧啶并[4,5-B]吲哚，9H-吡啶并[4'，3'：4,5]吡咯并[2,3-D]吡啶，和9H 1,3,6,9四氮杂芴作为CHK1 激酶功能抑制剂

    公开(公告)号：US08618121B2

    公开(公告)日：2013-12-31

    申请号：US12665961

    申请日：2008-07-01

    申请人： Ian Collins ,  John Charles Reader ,  Suki Klair ,  Jane Scanlon ,  Glynn Addison ,  Michael Cherry

    发明人： Ian Collins ,  John Charles Reader ,  Suki Klair ,  Jane Scanlon ,  Glynn Addison ,  Michael Cherry

    IPC分类号： A01N43/54 ,  A61K31/505 ,  C07D239/00 ,  C07D471/00 ,  C07D487/00 ,  C07D491/00

    CPC分类号： C07D471/14 ,  C07D487/04 ,  C07D487/14

    摘要： The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain tricyclic compounds (referred to herein as TC compounds), and especially certain 9H-pyrimido[4,5-b]indole, 9H-pyrido[4′,3′:4,5]pyrrolo[2,3-d]pyridine, and 9H-1,3,6,9-tetraaza-fluorene compounds, which, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation.

    摘要翻译： 本发明一般涉及治疗化合物领域，更具体地涉及某些三环化合物（本文称为TC化合物），特别是某些9H-嘧啶并[4,5-b]吲哚，9H-吡啶并[4' 3'：4,5]吡咯并[2,3-d]吡啶和9 H-1,3,6,9-四氮杂芴化合物，其特别地抑制检测点激酶1（CHK1）激酶功能。 本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以抑制CHK1激酶功能，以及治疗由CHK1介导的疾病和病症，即 通过抑制CHK1激酶功能等改善，包括增殖条件如癌症等，任选地与另一种试剂组合，例如（a）DNA拓扑异构酶I或II抑制剂; （b）DNA损伤剂; （c）抗代谢物或TS抑制剂; （d）微管靶向剂; 和（e）电离辐射。

    Antibacterial agents
    48.
    发明授权
    Antibacterial agents 有权
    抗菌剂

    公开(公告)号：US08492414B2

    公开(公告)日：2013-07-23

    申请号：US12678767

    申请日：2008-09-22

    申请人： David John Haydon ,  Ian Collins ,  Lloyd George Czaplewski

    发明人： David John Haydon ,  Ian Collins ,  Lloyd George Czaplewski

    IPC分类号： A61K31/41

    CPC分类号： C07D285/08

    摘要： Compounds of formula (IA) or (IB) have antibacterial activity: wherein W is ═CH— or ═N—; Ri and R2 are independently selected from hydrogen, fluoro and chloro, provided that Ri and R2 are not each hydrogen when W is ═CH—; n is 0 or 1; X is —O—, —S—, or —CH2—; and Q is (i) a phenyl radical, a naphthyl radical, a monocyclic carbocyclic or heteroaryl radical having 3 to 6 ring atoms, or a bicyclic heteroaryl radical having 5 to 10 ring atoms, any of which radicals being optionally substituted; or (ii) an optionally substituted C1-C6 alkyl, C2-C6 alkenyl, or C2-C6 alkynyl radical, which may optionally be interrupted by —O—, —S—, —S(O)—, —S(O2)—, —NH—, —N(CH3)—, —N(CH2CH3)—, —C—K═Oh or —C(═O)—O—.

    摘要翻译： 式（IA）或（IB）的化合物具有抗菌活性：其中W为= CH-或= N-; R 1和R 2独立地选自氢，氟和氯，条件是当W = CH-时，R 1和R 2不是氢。 n为0或1; X是-O - ， - S-或-CH 2 - ; Q为（i）具有3〜6个环原子的苯基，萘基，单环碳环或杂芳基，或环原子数为5〜10的双环杂芳基，其中任意一个为任选被取代的基团; 或（ⅱ）任选被-O - ， - S - ， - S（O） - ， - S（O 2））间隔的任选取代的C 1 -C 6烷基，C 2 -C 6烯基或C 2 -C 6炔基， - ， - NH - ， - N（CH 3） - ， - N（CH 2 CH 3） - ， - K = O或-C（= O）-O-。