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    Substituted &bgr;-alanines
    2.
    发明授权
    Substituted &bgr;-alanines 有权
    取代的β-丙氨酸

    公开(公告)号：US06352977B1

    公开(公告)日：2002-03-05

    申请号：US09589825

    申请日：2000-06-08

    Applicant: Peter Charles Astles ,  Neil Victor Harris ,  Andrew David Morley

    Inventor： Peter Charles Astles ,  Neil Victor Harris ,  Andrew David Morley

    IPC: C07C27542

    CPC classification number: C07D207/27 ,  C07C275/42

    Abstract: The invention is directed to physiologically active compounds of general formula (I): wherein R1 is hydrogen, halogen, lower alkyl or lower alkoxy; X1, X2 and X6 independently represent N or CR2; and one of X3, X4 and X5 represents CR3 and the others independently represents N or CR2 where R2 is hydrogen, halogen, lower alkyl or lower alkoxy; and R3 represents a group —L1—(CH2)n—C(═O)—N(R4)—CH2—CH2—Y; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs. Such compounds have valuable pharmaceutical properties, in particular the ability to regulate the interaction of VCAM-1 and fibronectin with the integrin VLA-4 (&agr;4&bgr;1).

    Abstract translation: 本发明涉及通式（I）的生理活性化合物：其中R 1是氢，卤素，低级烷基或低级烷氧基; X1，X2和X6独立地表示N或CR2; X 3，X 4和X 5中的一个表示CR 3，其余的独立地表示N或CR 2，其中R 2为氢，卤素，低级烷基或低级烷氧基; 并且R 3表示基团-L 1 - （CH 2）n -C（= O）-N（R 4）-CH 2 -CH 2 -Y; 及其前药，以及这些化合物及其前药的药学上可接受的盐和溶剂合物。 这些化合物具有有价值的药物性质，特别是调节VCAM-1和纤连蛋白与整联蛋白VLA-4（α4β1）的相互作用的能力。

    Substituted azabicyclic compounds
    7.
    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

    Applicant: 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

    Inventor： 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: A61K3147

    CPC classification number: 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

    Abstract: 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.

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