Srs-a antagonists

Details Srs-a antagonists Srs-a antagonists

C - Chemistry, Metallurgy

07

D

260/477, 260/514

C07D 309/28 (2006.01) C07B 45/04 (2006.01) C07C 317/46 (2006.01) C07C 323/22 (2006.01) C07C 323/56 (2006.01) C07C 323/58 (2006.01) C07D 303/40 (2006.01) C07D 303/42 (2006.01) C07D 307/38 (2006.01) C07D 309/12 (2006.01) C07D 309/30 (2006.01) C07D 313/04 (2006.01) C07F 9/53 (2006.01) C07K 5/06 (2006.01)

Patent

CA 1224795

ABSTRACT OF THE INVENTION There are described pharmacologically active compounds, useful in the treatment of allergic/inflammatory disorders involving SRS-A as causal mediator and which, in free acid form, are of formula I, Image in which R1 is an aliphatic, saturated or unsaturated hydrocarbyl radical of up to 20 carbon atoms, unsubstituted or substituted by at least one substituent selected from halogen, hydroxy, C3-6 alkoxy, C3-6 cycloalkyl, aryl or heteroaryl, the cyclo- alkyl, aryl or heteroaryl being unsubstituted or substituted by at least one substituent selected from hydroxy, halogen and alkyl, alkenyl or alkynyl of up to 10 carbon atoms, cycloalkyl of 3 to 8 carbon atoms unsubstituted or substituted by alkyl, alkenyl or alkynyl of up to 16 carbon atoms, or aryl or heteroaryl, unsubstituted or substituted by hydroxyl, C1-4 alkoxy, halogen or alkyl, alkenyl or alkynyl of up to 16 carbon atoms; and R2 is alkyl, cycloalkyl or alkenyl of up to 10 carbon atoms, unsubstituted or substituted by one or more substituents selected from aryl, cycloalkyl, halogen, hydroxy, NHR3 and COX, where R3 is H, C1-4 alkyl, aryl or an amino acid residue or COX, and X is OH, C1-4 alkyl, NH2 or an amino acid residue, or (ii) aryl or heteroaryl, unsubstituted or substituted by one or more substituents selected from C1-4 alkyl, C1-4 alkoxy, C2-5 acyl, halogen, hydroxy, carboxy, nitro, trihalomehtyl, phenyl, C1-4 acylamino and NHR4, where R4 is hydrogen r C1-4 alkyl; and Y is -S-, -SO- or -SO2_, with the proviso that when -YR2 is glutathionyl, cysteinyl or cysteinylglycinyl, then R1 is other than an unsubstituted alka- tetraenyl or alkapentaenyl radical of 12 to 16 carbon atoms.

405382

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