Oxiranes

Details Oxiranes Oxiranes

C - Chemistry, Metallurgy

07

D

260/369, 260/304

C07D 303/00 (2006.01) C07C 17/26 (2006.01) C07C 17/354 (2006.01) C07C 33/20 (2006.01) C07C 33/30 (2006.01) C07D 257/04 (2006.01) C07D 303/04 (2006.01) C07D 303/14 (2006.01) C07D 303/32 (2006.01) C07D 303/38 (2006.01) C07D 303/40 (2006.01) C07D 307/88 (2006.01) C07D 309/12 (2006.01) C07D 405/06 (2006.01) C07D 405/10 (2006.01) C07K 5/06 (2006.01) C07K 5/062 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1301181

NOVEL ORGANIC COMPOUNDS AND THEIR PHARMACEUTICAL USE ABSTRACT OF THE INVENTION There are described compounds of formula Image (I) in which n is 0, 1 or 2, R1 is a hydrocarbyl group optionally substituted with an optionally substituted phenyl group and containing from 5 to 30 carbon atoms, R2 is optionally substituted phenyl or C1-10alkyl optionally substituted by one or more substituents selected from optionally protected hydroxyl, optionally protected carboxyl, nitrile, optionally protected tetrazolyl, -COR6 where R6 is C1-4alkyl, C1-4alkoxy, an optionally protected amino acid residue or -NR27 where each R7 is hydrogen or C1-4alkyl, and -NHR8 where R8 is hydrogen, a protecting group, an optionally protected amino acid residue, C1-4alkyl or -COR9 where R9 is C1-4alkyl or C1-alkoxy, and R3, R4 and R5 are each selected from hydrogen, carboxyl, C2-5alkoxycarbonyl, C1-4alkyl, C1-4alkoxy, hydroxyl, optionally protected tetrazolyl, halo, trifluoromethyl, nitrile, nitro and -CONR?10 where each R10 is hydrogen or C1-4 alkyl; and salts thereof. The compounds are leukotriene antagonists. Also described are intermediate compounds of the formula ii Image in which R1 is an alkenyl or alkynyl group having from 10 to 20 carbon atoms and optionally substituted with an unsubstituted phenyl group or with a phenyl group substituted with 1-3 substituents selected from (C1-C4) alkyl, (C1-C4) alkoxy, hydroxy, nitro, cyano, halo, trifluoromethyl, carboxyl, tetrazolyl and -CONH2, and containing from 5 to 30 carbon atoms, and R3, R4 and R5 are each selected from hydrogen, carboxyl, (C2-C5) alkoxycarbonyl, (C1-C4) alkyl, (C1-C4) alkoxy, hydroxyl, optionally protected tetrazolyl, halo, trifluoromethyl, nitrile, nitro and CONR?10 where each R10 is hydrogen or (C1-C4) alkyl.

615758

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