C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
167/207, 260/319
C07D 307/81 (2006.01) A61K 31/33 (2006.01) C07D 209/14 (2006.01) C07D 333/58 (2006.01) C07D 333/60 (2006.01)
Patent
CA 1306744
4471 INDOLE BENZOFURAN, BENZOTHIOPHENE CONTAINING LIPOXYGENASE INHIBITING COMPOUNDS Compounds of the formula: Image wherein R1 is (1) hydrogen, (2) C1 to C4 alkyl, (3) C2 to C4 alkenyl, or (4) NR2R3, wherein R2 and R3 are independently selected from (1) hydrogen, (2) C1 to C4 alkyl and (3) hydroxyl, but R2 and R3 are not simultaneously hydroxyl; wherein X is oxygen, sulfur, SO2, or NR4, wherein R4 is (1) hydrogen, (2) C1 to C6 alkyl, (3) C1 to C6 alkoyl, (4) aroyl, or (5) alkylsulfonyl; A is selected from C1 to C6 alkylene and C2 to C6 alkenylene; n is 1-5; Y is selected independently at each occurrence from (1) hydrogen, (2) halogen, (3) hydroxy, (4) cyano, (5) halosubstituted alkyl, (6) C1 to C12 alkyl, (7) C2 to C12 alkenyl, (8) C1 to C12 alkyoxy, (9) C3 to C8 cycloalkyl, (10) C1-C8 thioalkyl, (11) aryl, (12) aryloxy, (13) aroyl, (14) C1 to C12 arylalkyl, (15) C2 to C12 arylalkenyl, (16) C1 to C12 arylalkoxy, (17) C1 to C12 arylthioalkoxy, and substituted derivatives of (18) aryl, (19) aryloxy, (20) aroyl, (21) C1 to C12 arylalkyl, (22) C2 to C12 arylalkenyl, (23) C1 to C12 arylalkoxy, or (24) C1 to C12 arylthioalkoxy, wherein substituents are selected from halo, nitro, cyano, C1 to C12 alkyl, alkoxy, and halosubstituted alkyl; Z is oxygen or sulfur; and M is hydrogen, a pharmaceutically acceptable cation, aroyl, or C1 to C12 alkoyl, are potent inhibitors of 5- and/or 12-lipoxygenase enzymes.Also disclosed are lipoxygenase inhibiting compositions and a method for inhibiting lipoxygenase activity.
558457
Brooks Dee W.
Gunn Bruce P.
Summers James B. Jr.
Abbott Laboratories
Goudreau Gage Dubuc
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