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    CYCLIC IMIDE DERIVATIVES
    3.
    发明专利
    CYCLIC IMIDE DERIVATIVES 未知

    公开(公告)号：CA2072551A1

    公开(公告)日：1992-12-28

    申请号：CA2072551

    申请日：1992-06-26

    Applicant: GLAXO INC

    Inventor： MYERS PETER L ,  MCELROY ANDREW B ,  GREGSON MICHAEL ,  BROWN PETER J ,  DAVIES HOWARD G ,  DREWRY DAVID H ,  FOLEY MICHAEL A

    IPC: A61K38/55 ,  A61K38/00 ,  A61P1/02 ,  A61P17/00 ,  A61P19/10 ,  A61P25/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D209/48 ,  C07D209/66 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D487/14 ,  C07K1/06 ,  C07K1/113 ,  C07K5/02 ,  C07K5/06 ,  C07K5/08 ,  C07K5/062 ,  A61K38/05

    Abstract: CH155"Comp" CYCLIC IMIDE DERIVATIVES Compounds are described of the formula (I) wherein: R1 is C3-6alkyl or C1-3alkylthioC1-3alkyl; R2 is an optionally substituted C1-6alkyl or C1-6alkoxy group, aryl, heteroaryl, arylC1-4alkyl, heteroarylC1-4alkyl or a side-chain of a natural .alpha.-amino acid; R3 is hydrogen, C1-6alkyl, CHR4COR5(where R4 is a side-chain of a natural .alpha.-amino acid and R5 is hydroxyl, C1-6alkoxy or NHR6 where R6 represents a hydrogen atom or a C1-6alkyl group) or a group (CH2)nX (where n is 1 to 6 and X is hydroxyl, C1-4alkoxy, heteroaryl or a group NR7R8 where R7 and R8 are each hydrogen or C1-6alkyl or the group NR7R8 forms a 5 to 7 membered cyclic amine); and Het is an optionally substituted cyclic imide where the cyclic imide ring system has the formula (i),(ii)or(iii) (i) (ii) (iii) in which A, B, C and D are each CH or 1 or 2 of A, B, C and D represents N and the others represent CH, and E and F may each independently represent CH or N; and physiologically acceptable salts and solvates thereof. These compounds inhibit metalloproteases involved in tissue degradation. Compounds of the invention may be formulated for use in a variety of conditions CH155"Comp" involving tissue degradation including arthropathy, dermatological conditions, bone resorption, inflammatory diseases, tumour invasion and multiple sclerosis and related diseases involving myelin degradation, and in the promotion of wound healing.

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