Oculoselective Drugs and Prodrugs

Number of patents in Portfolio can not be more than 2000

United States of America Patent

APP PUB NO 20070254950A1
SERIAL NO

11597070

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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Compounds of the following formula are disclosed: wherein R.sup.1 and R.sup.2 are each independently H, W, or a phenoxyl protecting group; and R.sup.4 is H or W, provided that at least one of R.sup.1, R.sup.2, and R.sup.4 is W; R.sup.3 is hydrogen, straight chain or branched C.sub.1-C.sub.10 alkyl, cycloalkyl, amino, C.sub.1-C.sub.10 alkoxy, --NHC(.dbd.O)Ra, or --C(.dbd.O)N(H)R.sup.a; R.sup.a is alkyl, aryl, or heterocyclyl; Z is -0-, --O(C.dbd.O)--, or NH(C.dbd.O)--, wherein when Z is -0-, R.sup.5 is H, straight chain or branched C.sub.1-C.sub.10 alkyl, cycloalkyl, cycloalkyl substituted with at least one straight or branched C.sub.1-C.sub.10 alkyl, CI--Clo alkoxyalkyl, amino, benzyl, tetrahydrofuranyl, dihydrofuranyl, furanyl, morpholinyl, piperidinyl, tetrahydropyranyl, dioxolanyl, 2,2-dimethyl dioxolanyl, dioxanyl, pyrrolyl, pyrrolsdinyl, tetrahydrooxazolyl, dihydrooxazolyl, phenyl, or phenyl substituted with CI--Clo alkyl, C.sub.1-C.sub.10 alkoxy, or halo; and W is: wherein each R.sup.6 is independently H, straight chain or branched C.sub.1-C.sub.10 alkyl, or straight chain or branched C.sub.1-C.sub.10 alkoxyalkyl; and R.sup.7 is alkyl, cycloalkyl, aryl, or aralkyl; and wherein when Z is --O(C.dbd.O)--, R.sup.5 is straight chain or branched C.sub.1-C.sub.10 alkyl, cycloalkyl, cycloalkyl substituted with at least one straight or branched C.sub.1-C.sub.10 alkyl, CI--CIO alkoxyalkyl, amino, benzyl, tetrahydrofuranyl, dihydrofuranyl, furanyl, morpholinyl, piperidinyl, tetrahydropyranyl, dioxolanyl, 2,2-dimethyl dioxolanyl, dioxanyl, pyrrolyl, pyrrolidinyl, tetrahydrooxazolyl, dihydrooxazolyl, phenyl, or phenyl substituted with C.sub.1-C.sub.10 alkyl, C.sub.1-C.sub.10 alkoxy, or halo; and W is:, wherein each R6 is independently H, straight chain or branched CI--C to alkyl, or straight chain or branched C,--C to alkoxyalkyl; and R7 is alkyl, cycloalkyl, aryl, or aralkyl; and wherein when Z is --NH(C.dbd.O)--, R5 is straight chain or branched C.sub.1-C.sub.10 alkyl, cycloalkyl, cycloalkyl substituted with at least one straight or branched C.sub.1-C.sub.10 alkyl, CI--CIO alkoxyalkyl, amino, benzyl, tetrahydrofuranyl, dihydrofuranyl, furanyl, morpholinyl, piperidinyl, tetrahydropyranyl, & oxolanyl, 2,2-dimethyl dioxolanyl, dioxanyl, pyrrolyl, pyrrolidinyl, tetrahydrooxazolyl, dihydrooxazolyl, phenyl, or phenyl substituted with C.sub.1-C.sub.10 alkyl, C.sub.1-C.sub.10 alkoxy, or halo; and W is: wherein each R6 is independently H, straight chain or branched C1-C to alkyl, or straight chain or branched C,--Clo alkoxyalkyl. Methods of preparing the compounds, pharmaceutical compositions comprising the compounds, and methods of treating patients by administration of the pharmaceutical compositions, are also disclosed.

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First Claim

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Patent Owner(s)

Patent OwnerAddress
QLT INCORPORATED887 GREAT NORTHERN WAY VANCOUVER BRITISH COLUMBIA V7C 3L1

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Matier, William L Hockessin, DE 55 314
Patil, Ghanshyam Lincoln University, PA 30 176

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