- 1- [4- (SULFONYL) -PHENYL] -5- (BENZYL) -IH-I, 2, 4-TRIAZOL DERIVATIVES AS INHIBITORS OF CARBONIC ANHYDRASE FOR TREATING GLAUCOMA OR OCULAR HYPERTENSION
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The invention relates to compounds of formula (I) and to pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4 and RA through RE are as defined herein. The invention also relates to methods of treating glaucoma, ocular hypertension, age-related macular degeneration, diabetic macular edema, diabetic retinopathy, hypertensive retinopathy, retinal vasculopathies and intraocular pressure in mammals by administering the compounds of formula I, and to pharmaceutical compositions which contain the compounds of formula I for such treatments. The invention also relates to methods of preparing the compounds of formula (I).
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Page/Page column 33; 34
(2008/12/06)
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- Synthesis and cyclooxygenase-2 inhibiting property of 1,5-diarylpyrazoles with substituted benzenesulfonamide moiety as pharmacophore: Preparation of sodium salt for injectable formulation
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A series of 1,5-diarylpyrazoles having a substituted benzenesulfonamide moiety as pharmacophore was synthesized and evaluated for cyclooxygenase (COX-1/COX-2) inhibitory activities. Through SAR and molecular modeling, it was found that fluorine substituti
- Pal, Manojit,Madan, Manjula,Padakanti, Srinivas,Pattabiraman, Vijaya R.,Kalleda, Srinivas,Vanguri, Akhila,Mullangi, Ramesh,Mamidi, N. V. S. Rao,Casturi, Seshagiri R.,Malde, Alpeshkumar,Gopalakrishnan,Yeleswarapu, Koteswar R.
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p. 3975 - 3984
(2007/10/03)
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- Topically active carbonic anhydrase inhibitors. 4. [(hydroxyalkyl)sulfonyl]benzene and [(hydroxyalkyl)sulfonyl]thiophenesulfonamides
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For several decades a tantalizing goal for the treatment of primary open-angle glaucoma has been the development of a topically active carbonic anhydrase inhibitor. Recent results from several research groups indicate that considerable progress has been made toward this objective. In this report, we present the design and synthesis of (hydroxyalkyl)sulfonyl-substituted benzene- and thiophenesulfonamides. These compounds exhibit inhibition of carbonic anhydrase II in the nanomolar range and lower intraocular pressure in the α-chymotrypsinized rabbit model of ocular hypertension after topical instillation.
- Shepard,Graham,Hudcosky,Michelson,Scholz,Schwam,Smith,Sondey,Strohmaier,Smith,Sugrue
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p. 3098 - 3105
(2007/10/02)
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- Substituted benzenesulfonamides
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Benzenesulfonamides with a substituted-alkyl-S(O)n -substituent are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.
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