C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/328.2, 260/3
C07D 333/34 (2006.01) A61K 31/38 (2006.01) C07D 333/28 (2006.01) C07D 409/12 (2006.01) C07D 417/12 (2006.01)
Patent
CA 1219867
ABSTRACT OF THE DISCLOSURE The invention relates to novel derivatives of [phenylsulfonyl(or sulfinyl or carbonyl)]thiophene- sulfonamide having the structural formula: Image wherein R is 1) C1-18alkyl, either straight or branched chain, 2) C1-18 haloalkyl, wherein halo is chloro, bromo, or fluoro, 3) R1, R2N-C1-5alkyl, wherein R1 and R2 are independently hydrogen or C1-3alkyl, or R1 and R2 are joined together to form a heterocycle selected from piperidinyl, morpholinyl, or pyrrolidinyl, 4) C1-3- alkoxycarbonyl-C1-5alkyl, 5) C3-6cycloalkyl, 6) C3-6- cycloalkyl-C1-3alkyl, 7) C1-3alkyl-C3-6cycloalkyl, 8) aryl, wherein aryl is a carbocycle or heterocycle selected from phenyl, naphthyl, pyridinyl, furanyl, thienyl, or the like, either unsubstituted or substi- tuted with one or more of C1-3alkyl, halo or C1-3alkoxy, 9) aryl-C1-3alkyl, either unsubstituted or substituted with one or more of halo, C1-3alkyl or C1-3alkoxy, 10) C2-6alkenyl, 11) C2-6alkynyl, 12) aryl-C2-6- alkenyl, 13) NR3-piperidinyl, wherein R3 is C1-3alkyl or C2-5alkanoyl, or 14) C1-3alkoxy-C1-5alkyl; X is Image These compounds are useful for the topical treatment of elevated intraocular pressure in ophthalmic compositions including drops and inserts.
456792
Goudreau Gage Dubuc
Merck & Co. Inc.
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