Substituted aromatic sulfonamides as antiglaucoma agents

Details Substituted aromatic sulfonamides as antiglaucoma agents Substituted aromatic sulfonamides as antiglaucoma agents

C - Chemistry, Metallurgy

07

D

167/211, 167/242

C07D 495/04 (2006.01) A61K 31/38 (2006.01) A61K 31/395 (2006.01)

Patent

CA 2022119

Carbonic anhydrase inhibitors of the thieno- [2,3-b]thiopyran-2-sulfonamide type with a substituted- alkyl-amino group in the 4-position are topically effective in lowering intraocular pressure; the inhibitors are compounds of formula (I): Image wherein: X is -S-, or -0-; m is 0, 1 or 2 n is 0, 1 or 2 R is hydrogen or R1, R1 is 1) C2-7-alkene, 2) C2-7-alkyne, 3) C1-5 alkyl having 1, 2 or 3 substituents wherein the substituents are independently: a) halogen; b) hydroxy; c) -NR6R7 wherein R6 and R7 are independently: i) hydrogen, ii) C1-3 alkyl, iii) -CO-C1-3 alkyl, or iv) R6 and R7 taken together with the nitrogen to which they are attached represent a saturated heterocycle of 5-7 members which may include a second hetero group selected from 0, S, S0, or S02; d) -S-C1-3-alkyl; (0)n e) -CN; f) C1-3-alkoxy, g) -SH, h) C1-3-alkoxycarbonyl, O " i) -C-C1-3 alkyl, 0 " j) -CNR6r7 or k) C3-6 cycloalkyl; R2 is 1) hydrogen, 2) -CN, 3) phenyl-C1-3 alkyl, wherein the phenyl is either unsubstituted or substituted with one or more of a) hydroxy, b) C1-3-alkoxy, c) R6R7NC1-5-alkyl; or 4) C1-5 alkyl; and R3 and R4 are independently: 1) hydrogen, 2) C1-5 alkyl, either unsubstituted or substituted with one or more of a) halogen, b) hydroxy, c) -NR8R9, wherein R8 and R9 are independently i) hydrogen, ii) C1-5 alkyl, unsubstituted or substituted with phenyl, wherein the phenyl is unsubstituted or substituted with C1-3 alkoxy, halogen, or di(C1-3- alkyl)-amino; d) phenyl, unsubstituted or substituted with one or more of i) hydroxy, ii) C1-3 alkoxy, iii) C1-3 alkyl-NR10R11, wherein R10 and R11 are independently hydrogen or C1-5 alkyl, 3) phenyl, either unsubstituted or substituted with i) hydroxy, ii) C1-3 alkoxy, iii) C1-5 alkyl-NR10R11, iv) halo, 4) aromatic heterocycle of 5 or 6 members unsubstituted or substituted with C1-3 alkyl -NR10R11, R3 and R4 taken together represent methylene: with the proviso that R1 is not 2-hydroxy-2-methyl-1- propyl if R, R2, R3 and R4 are all hydrogen and n is 2.

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