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6 条记录 (耗时 0.042 秒)

    Substituted azabicyclic compounds
    6.
    发明授权
    Substituted azabicyclic compounds 失效

    公开(公告)号：US06800645B1

    公开(公告)日：2004-10-05

    申请号：US09612530

    申请日：2000-07-07

    申请人： Paul Joseph Cox ,  Shelley Bower ,  David John Aldous ,  Peter Charles Astles ,  Daniel Gerard McGarry ,  Christopher Hulme ,  John Robinson Regan ,  Fu-Chih Huang ,  Stevan Wakefield Djuric ,  Kevin Joseph Moriarty ,  Rose Mappilakunnel Mathew ,  Gregory Bernard Poli

    发明人： Paul Joseph Cox ,  Shelley Bower ,  David John Aldous ,  Peter Charles Astles ,  Daniel Gerard McGarry ,  Christopher Hulme ,  John Robinson Regan ,  Fu-Chih Huang ,  Stevan Wakefield Djuric ,  Kevin Joseph Moriarty ,  Rose Mappilakunnel Mathew ,  Gregory Bernard Poli

    IPC分类号： A61K3147

    CPC分类号： C07D235/24 ,  C07D209/12 ,  C07D209/42 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14

    摘要： This invention is directed to physiologically active compounds of formula (I) wherein represents a bicyclic ring system, of about 10 to about 13 ring members, in which the ring is an azaheterocycle, and the ring represents an azaheteroaryl ring, or an optionally halo substituted benzene ring; R1 represents hydrogen or a straight- or branched-chain alkyl group of 1 to about 4 carbon atoms, optionally substituted by hydroxy or one or more halogen atoms, or when Z1 represents a direct bond R1 may also represent a lower alkenyl or lower alkynyl group, or a formyl group; R2 represents hydrogen, alkenyl, alkoxy, alkyl, alkylsulphinyl, alkylsulphonyl, alkylthio, aryl, arylalkyloxy, arylalkylsulphinyl, arylalkylsulphonyl, arylalkylthio, aryloxy, arylsulphinyl, arylsulphonyl, arylthio, cyano, cycloalkenyl, cycloalkenyloxy, cycloalkyl, cycloalkyloxy, heteroaryl, heteroarylalkyloxy, heteroaryloxy, hydroxy, —SO2NR4R5, —NR4SO2R5, —NR4R5, —C(═O)R5, —C(═O)C(═O)R5, —C(═O)NR4R5, —C(═O)OR5, —O(C═O)NR4R5, or —NR4C(═O)R5; R3 represents —C(═Z)—N(R7)R6, —C(═Z)—CHR12R6, —C(═Z)—R6, —CR8═C(R9)(CH2)p—R6, —C(R10)═C(R11)R12, —C(R13)(R10)C(R11)(R14)R12, —C(R8)(R15)CH(R9)(CH2)p—R6, —R6, —V(═Z)—R6, —C(R17)═N—OC(═O)R18, —C(═O)—N(R19)OR20, —C≡C—R6, —CH2—C(═Z)—R6, —C(═Z)—C(═Z)R6, —CH2—NHR6, —CH2—ZR6, —CH2—SOR6, —CH2—SO2R6, —CF2—OR6, —NH—CH2R6, —Z—CH2R6, —SO—CH2R6, —SO2—CH2R6, —O—CF2R6, —O—C(═Z)R6, —N═N—R6, —NH—SO2R6, —SO2—NR21R22, —CZ—CZ—NHR6, —NH—CO—OR6, —O—CO—NHR6, —NH—CO—NHR6, —R23, —CX1═CX2R6, —C(═NOR24), —(CH2)qR6, —CH2—CO—NH(CH2)qR6, —CH2—NH—CO(CH2)qR6, —CH2—CO—CH2R6, —C(═NR25)—NH(CH2)qR6, —C(X3)═N—(CH2)qR6 or —CH(X4)—CH2R6; A1 represents a direct bond, or a straight or branched C1-6alkylene chain optionally substituted by hydroxyl, alkoxy, oxo, cycloalkyl, aryl or heteroaryl, or A1 represents a straight or branched C2-6alkenylene or C2-6alkynylene chain; Z1 represents a direct bond, an oxygen or sulphur atom or NH; n and m each represent zero or 1, provided that n is 1 when m is zero and n is zero when m is 1; and N-oxides thereof, and their prodrugs, and pharmaceutically acceptable salts and solvates of the compounds of formula (I) and N-oxides thereof, and their prodrugs. Such compounds inhibit the production or physiological effects of TNF and inhibit cyclic AMP phosphodiesterase. The invention is also directed to pharmaceutical compositions comprising compounds of formula (I), their pharmaceutical use and methods for their preparation.