Cyclic imide derivatives

C - Chemistry – Metallurgy – 07 – K

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Details

C07K 5/062 (2006.01) A61K 38/05 (2006.01) C07D 209/48 (2006.01) C07D 471/04 (2006.01) C07D 487/04 (2006.01) C07K 5/02 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2072551

CH155"Comp" - 79 - ABSTRACT CYCLIC IMIDE DERIVATIVES Compounds are described of the formula Image (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) Image (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" - 80- 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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