Treatment of glaucoma

Details Treatment of glaucoma Treatment of glaucoma

C - Chemistry, Metallurgy

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C07C 311/46 (2006.01) A61K 31/18 (2006.01) A61K 31/40 (2006.01) A61K 31/63 (2006.01) A61K 38/05 (2006.01) C07C 311/49 (2006.01) C07D 207/16 (2006.01) C07K 5/06 (2006.01)

Patent

CA 2015768

ABSTRACT OF THE DISCLOSURE Method and formulation useful in treatment of glaucoma in a mammal wherein an effective amount of an active water soluble carbonic anhydrase inhibitor is administered, said inhibitor being a compound having the formula Image or a pharmaceutically acceptable salt thereof, wherein R1 is selected from the group consisting of H, NH2CH2-, -CH(Me)NH2, -CH(NH2)CHMe2, -CH(NH2)CH2CHMe2,- CH(NH2)CH(Me)CH2Me, 2-pyrrolidinyl residues wherein the R1CO- constitutes an .alpha.-aminoacyl group, N-acetylaminoacyl derivatives and the corresponding dipeptidyl -radicals wherein R1CO- is a dipeptidyl residue containing two amino acid residues of the formula where R1 is -CHR7NHCOCHR8NH2, R6NHCHR5-, Image , Image ,and R6NHCH2CHR5-; R2 is selected from the group consisting of H, alkyl having from 1 to 6 carbon atoms, alkenyl having from 2 to 6 carbon atoms, and cycloalkyl; R3 is selected from the group consisting of H, Cl, Br, F, -CF3, -OCH3, -NO2, alkyl having from 1 to 6 carbon atoms and alkenyl having from 1 to 6 carbon atoms: R4 is selected from the group consisting of H, -OH, -NH2, -CN and -OCH3; R5 is selected from the group consisting of H, -CH3, -CH(CH3)2, and alpha amino acid side chain moieties; R6 is selected from the group consisting of H, HCO-, CH3CO-, PhCH2OCO- and XCH2CO- wherein Ph is phenyl and X is chlorine or bromine; and R7 and R8 correspond to the alkyl side chains of glycine, alanine, valine, leucine, isoleucine, proline and serine, and stereoisomers thereof.

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