NOVEL IMIDAZOLE LIPOXYGENASE INHIBITORS
    1.
    发明公开
    NOVEL IMIDAZOLE LIPOXYGENASE INHIBITORS 失效
    新咪唑脂氧合酶抑制剂

    公开(公告)号:EP0863905A1

    公开(公告)日:1998-09-16

    申请号:EP96923010.0

    申请日:1996-07-24

    申请人: PFIZER INC.

    摘要: The present invention provides a compound of formula (I) and a pharmaceutically acceptable salt thereof, wherein Ar is phenylene optionally substituted with halo, hydroxy, cyano, amino, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkylthio, C1-C4 halo-substituted alkyl or C1-C4 halo-substituted alkoxy; X is -A-X?1- or -X1¿-A-, wherein A is a direct bond or C¿1?-C4 alkylene, and X?1¿ is oxy, thio, sulfinyl or sulfonyl; Ar1 is phenylene, pyridylene or thienylene optionally substituted with halo, hydroxy, cyano, nitro, amino, C¿1?-C4 alkyl, C1-C4 alkoxy, C1-C4 alkylthio, C1-C4 halo-substituted alkyl, C1-C4 halo-substituted alkoxy, C1-C4 alkylamino or di(C1-C4)alkylamino; Y is CN or CONR?1R2¿ wherein R?1 and R2¿ are independently hydrogen or C¿1?-C4 alkyl; and R is hydrogen or C1-C6 alkyl; W is C2-C3 alkylene, one carbon atom of which may be replaced by an oxygen atom. Further the invention provides a pharmaceutical composition for treating an inflammatory disease, allergy or cardiovascular diseases or the like in a mammalian subject which comprises a compound of formula (I) and a pharmaceutically acceptable carrier.

    QUINOXALINEDIONE NMDA RECEPTOR ANTAGONISTS
    3.
    发明公开
    QUINOXALINEDIONE NMDA RECEPTOR ANTAGONISTS 失效
    QUINOXALINDION,NMDA受体拮抗剂

    公开(公告)号:EP0781279A1

    公开(公告)日:1997-07-02

    申请号:EP95931989.0

    申请日:1995-09-01

    IPC分类号: C07D401 A61K31 A61P25 A61P43 C07D403

    CPC分类号: C07D403/06

    摘要: Compounds of formula (I) wherein R?1 and R2¿ are each independently F, Cl, Br, CH¿3?, CH2CH3 or CF3; R?3¿ is H, CH¿3? or CH2CH3; and X is a 5-membered heterocyclic group containing up to four nitrogen atoms, attached via a nitrogen atom, the said group being optionally benzofused and/or substituted by C1-C6 alkyl or (CH2)nNR?4R5¿, wherein n is an integer from 1 to 5 and R?4 and R5¿ are each independently H, C¿1?-C6 alkyl, C3-C6 cycloalkyl or C1-C4 alkyl substituted by phenyl or pyridyl, or R?4 and R5¿ are linked to form, together with the nitrogen atom to which they are attached, a pyrrolidine, piperidine, piperazine, N-(C¿1?-C4 alkyl) piperazine, morpholine or azepine group; and their pharmaceutically acceptable salts, are NMDA antagonists of utility in the treatment of acute neurodegenerative disorders, e.g. arising from stroke or traumatic head injury and in chronic neurological disorders, e.g. senile dementia and Alzheimer's disease.

    DIHYDRO PYRAZOLOPYRROLES
    6.
    发明公开
    DIHYDRO PYRAZOLOPYRROLES 失效
    DIHYDRO吡唑并吡咯

    公开(公告)号:EP0738270A1

    公开(公告)日:1996-10-23

    申请号:EP94931665.0

    申请日:1994-11-18

    申请人: PFIZER INC.

    CPC分类号: C07D487/04

    摘要: The compounds of formula (I) and the pharmaceutically acceptable salts thereof; whrein X1, R?1, R2, R3 and R4¿ are as defined herein, are inhibitors of PDE IV and the production of tumor necrosis factor. As such, they are active in the treatment of inflammatory diseases, shock, etc.

    摘要翻译: 式(I)化合物及其药学上可接受的盐; 其中X 1,R 1,R 2,R 3和R 4如本文所定义,是PDE IV的抑制剂和肿瘤坏死因子的产生。 因此,他们积极治疗炎症性疾病,休克等。