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    Compounds
    3.
    发明授权
    Compounds 失效
    化合物

    公开(公告)号：US07410984B2

    公开(公告)日：2008-08-12

    申请号：US10524028

    申请日：2003-08-08

    申请人： Jason Witherington ,  Richard Leonard Elliott

    发明人： Jason Witherington ,  Richard Leonard Elliott

    IPC分类号： C07D211/72 ,  A61K31/44

    CPC分类号： C07D213/64 ,  C07D211/76 ,  C07D401/12

    摘要： The present invention relates to novel pyridone derivatives capable of inhibiting α4 integrin mediated cell adhesion, processes for their preparation, compositions comprising them and their use in the treatment of diseases capable of being modulated by the inhibition of cell adhesion.

    摘要翻译： 本发明涉及能够抑制α4H整联蛋白介导的细胞粘附的新型吡啶酮衍生物，其制备方法，包含它们的组合物及其在治疗能够通过抑制细胞调节的疾病中的用途 附着力。

    Pyrimidinone derivatives and their use in the treatment of atherosclerosis
    5.
    发明授权
    Pyrimidinone derivatives and their use in the treatment of atherosclerosis 失效

    公开(公告)号：US07169924B2

    公开(公告)日：2007-01-30

    申请号：US10398977

    申请日：2001-10-05

    申请人： Richard Leonard Elliott ,  Deirdre Mary Bernadette Hickey ,  Robert John Ife ,  Colin Andrew Leach ,  Ivan Leo Pinto ,  Stephen Allan Smith

    发明人： Richard Leonard Elliott ,  Deirdre Mary Bernadette Hickey ,  Robert John Ife ,  Colin Andrew Leach ,  Ivan Leo Pinto ,  Stephen Allan Smith

    IPC分类号： C07D239/70 ,  A61K31/517 ,  A61P9/01

    CPC分类号： C07D239/36 ,  C07D239/70 ,  C07D239/91 ,  C07D401/12 ,  C07D403/12 ,  C07D409/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

    摘要： Compound of formula (I): are disclosed in which: R1 is an aryl group, optionally substituted by 1, 2, 3 or 4 substituents which may be the same or different selected from C(1-6)alkyl, C(1-6)alkoxy, C(1-6)alkylthio, hydroxy, halogen, CN, and mono to perfluoro-C(1-4)alkyl; R2 is halogen, C(1-3)alkyl, C(1-3)alkoxy, hydroxyC(1-3)alkyl, C(1-3)alkylthio, C(1-3)alkylsulphinyl, aminoC(1-3)alkyl, mono- or di-C(1-3)alkylaminoC(1-3)alkyl, C(1-3)alkylcarbonylaminoC(1-3)alkyl, C(1-3)alkoxyC(1-3)alkylcarbonylaminoC(1-3)alkyl, C(1-3)alkylsulphonylaminoC(1-3)alkyl, C(1-3)alkylcarboxy, C(1-3)alkylcarboxyC(1-3)alkyl, and R3 is hydrogen, halogen, C(1-3)alkyl, or hydroxyC(1-3)alkcyl; or R2 and R3 together with the pyrimidone ring carbon atoms to which they are attached form a fused 5-or 6-membered carbocyclic ring; or R2 and R3 together with the pyrimidone ring carbon atoms to which they are attached form a fused benzo or heteroaryl ring ring optionally substituted by 1, 2, 3 or 4 substituents which may be the same or different selected from halogen, C(1-4)alkyl, cyano, C(1-6)alkoxy, C(1-6)alkylthio or mono to perfluoro-C(1-4)alkyl; R4 is hydrogen, C(1-6)alkyl which may be unsubstituted or substituted by 1, 2 or 3 substituents selected from hydroxy, halogen, OR7, COR7, carboxy, COOR7, CONR9R10, NR9R10, NR7COR8, mono- or di-(hydroxyC(1-6)alkyl) amino and N-hydroxyC(1-6)alkyl-N—C(1-6)allkylamino; or R4 is Het-C(0-4)alkyl in which Het is a 5- to 7- membered heterocyclyl ring comprising N and optionally O or S, and in which N may be substituted by COR7, COOR7, CONR9R10, or C(1-6)alkyl optionally substituted by 1, 2 or 3 substituents selected from hydroxy, halogen, OR7, COR7, carboxy, COOR7, CONR9R10 or NR9R10, for instance, piperidinyl-4-yl, pyrrolidin-3-yl; R5 is an aryl or a heteroaryl ring optionally substituted by 1, 2, 3 or 4 substituents which may be the same or different selectd from C(1-6)alkyl, C(1-6)alkoxy, C(1-6)alkylthio, arylC(1-6)alkoxy, hydroxy, halogen, CN, COR7, carboxy, COOR7, NR7COR8, CONR9R10, SO2NR9R10, NR7SO2R8, NR9R10, mono to perfluoro-C(1-4)alkyl and mono to perfluoro-C(1-4)alkoxy; R6 is an aryl or a heteroaryl ring which is further optionally substituted by 1, 2, 3 or 4 substituents which may be the same or different selected from C(1-18)alkyl, C(1-18)alkoxy, C(1-6)alkylthio, C(1-6)alkylsulfonyl, arylC(1-6)alkoxy, hydroxy, halogen, CN, COR7, carboxy, COOR7, CONR9R10, NR7COR8, SO2NR9R10, NR7SO2R8, NR9R10, mono to perfluoro-C(1-4)alkyl and mono to perfluoro-C(1-4)alkoxy, or C(5-10)alkyl; These compound are useful for treating diseases associated with abnormal activity of the phospholipase A2 enzyme, for example athereosclosis.

    Carbacephalosporin compound, their preparation and use
    7.
    发明授权
    Carbacephalosporin compound, their preparation and use 失效
    碳青霉素化合物，其制备和用途

    公开(公告)号：US5665717A

    公开(公告)日：1997-09-09

    申请号：US522411

    申请日：1996-01-18

    申请人： Richard Leonard Elliott ,  Neville Hubert Nicholson ,  Andrew Kenneth Takle

    发明人： Richard Leonard Elliott ,  Neville Hubert Nicholson ,  Andrew Kenneth Takle

    IPC分类号： A61K31/435 ,  A61P31/04 ,  C07D463/00 ,  A61K31/395 ,  C07D221/06

    CPC分类号： C07D463/06 ,  C07D463/18 ,  Y02P20/55

    摘要： Carbacephalosporin compounds of formula (I), ##STR1## salts thereof, processes for their synthesis and uses thereof, wherein: R.sup.1 is hydrogen, methoxy or formamido; R.sup.2 is an acyl group; CO.sub.2 R.sup.3 is a carboxy group or a carboxylate anion, or R.sup.3 is a carboxy protecting group or a pharmaceutically acceptable salt-forming group or in vivo hydrolysable ester group; R.sup.4, R.sup.5, R.sup.6 and R.sup.7 represent hydrogen or a substituent; R.sup.4 and R.sup.7 may be replaced by a chemical bond between the two carbon atoms shown; R.sup.5 and R.sup.6 may be linked together into a cyclic system. The compounds (I) have antibacterial properties.

    摘要翻译： PCT No.PCT / EP94 / 00811 Sec。 371日期：1996年1月18日 102（e）日期1996年1月18日PCT 1994年3月10日PCT公布。 公开号WO94 / 21633 1994年9月29日，具有式（I）的乙酰菌素化合物，其化合物及其用途，其中：R1是氢，甲氧基或甲酰氨基; R2是酰基; CO 2 R 3是羧基或羧酸根阴离子，或R3是羧基保护基或药学上可接受的成盐基团或体内可水解的酯基; R4，R5，R6和R7表示氢或取代基; R4和R7可以被所示的两个碳原子之间的化学键取代; R5和R6可以连接在一起成为循环系统。 化合物（I）具有抗菌性。