| 摘要 |
<p>The invention relates to novel 2-sulfamoyl-benzo¢b!thiophenes which are useful in the reduction of elevated intraocular pressure and having the formula: wherein X is hydrogen, halo, such as chloro, bromo or fluoro, C1-3 alkyl, hydroxy or C1-3 alkoxy; and R is 1) hydroxY, 2) R1 wherein R? is a) C1-18 alkyl either straight or branched chain substituted with one or more of i) C3-6 cycloalkyl, ii) halo, such as chloro, bromo or fluoro, iii) aryl, wherein the aryl group is carbocyclic such as phenyl or naphthyl, or heterocyclic such as pyridinyl, furanyl, pyrazinyl, morpholinyl, oxazolinyl, dioxolinonyl, imidazolyl, thienyl or the like and wherein the aryl group can be substituted with one or more of C1-10 alkyl, halo, C1-4 alkoxy, C2-5 alkanoyl, or trifluoromethyl, iv) hydroxy, v) C1-3 alkoxy, vi) aryl-C1-3 alkoxy, vii) C1-4 alkoxy-C1-3 alkoxy, viii) amino, ix) (C1-3 alkyl)amino, x) di(C1-3 alkyl)amino, xi) R2-?-, wherein R2 is 1) HO-, 2) M+O-, wherein M+ is a pharmaceutically acceptable cation such as that from an alkali metal, or an ammonium, 3) C1-10 alkoxy, 4) R3R4N- wherein R3 and R4 are independently hydrogen, hydroxy, C1-15 alkyl, or taken together form a 3-7 membered heterocycle with the nitrogen to which they are attached such as piperidino or pyrrolidino, or xii) C2-5 alkanoyl; b) C3-6 cycloalkyl, c) C1-18 alkyl-C3-6 cycloalkyl, d) aryl as previously defined, e) R3R4N-, f) C2-6 alkenyl, g) aryl-C2-6 alkenyl, h) C2-6 alkynyl, or i) heterocyclyl of 5 or 6 members with one or two heteroatoms selected from O, N and S, such as tetrahydropyrrolyl, tetrahydrofuranyl, or imidazolidinyl, 3) R?-O-, 4) R1-?-, wherein R1 is R? or C1-18 alkyl, 5) R1-?-O-, 6) R1-O-?-O, 7) wherein x is 0-2; y is 0-3; z is 0 or 1; and A is a heteroatom such as S, O or N, 8) where R5 and R6 are independently: a) hydrogen, b) C1-18 alkyl, either straight or branched chain, c) C3-6 cycloalkyl, d) C3-6 cycloalkyl-C1-3 alkyl, e) aryl-C1-3 alkyl wherein the aryl group is either unsubstituted or substituted with one or more of chloro, bromo, fluoro, C1-3 alkyl or C1-3 alkoxy, f) R7?-, or R7O?- wherein R7 is i) C1-18 alkyl, either straight or branched chain, ii) aryl, either unsubstituted or substituted with one or more of chloro, bromo, fluoro, C1-3 alkyl, or C1-3 alkoxy, iii) aryl-C1-3 alkyl wherein the aryl group is either unsubstituted or substituted with one or more of chloro, bromo, fluoro, C1-3 alkyl or C1-3 alkoxy, iv) amino-C1-18 alkyl either straight or branched chain; or g) R5 and R6 if lower alkyl, are joined together directly or through a heteroatom selected from O or N to form a 5 or 6 membered heterocycle with the nitrogen to which they are attached such as pyrrolidine, piperidine, morpholine, or piperazine, 9) , wherein ? is an ophthalmologically acceptable cation selected from sodium, potassium, ammonium, tetra(C1-4 alkyl)ammonium, pyridinium, imidazolium, pralidoxime, and thiamine, 10) wherein ? is as previously defined; 11) , wherein R8 is C1-3 alkyl or phenyl-C1-3 alkyl; or 12) (R8O)2 ?-O-, wherein R8 is as previously defined, and the two may be the same or different; and R and X, joined together, represent methylenedioxy, as well as the pharmaceutically and ophthalmologically acceptable salts thereof.</p> |
