Dihydrothiazine prodrugs of thiazolium agents

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United States of America Patent

APP PUB NO 20050014747A1
SERIAL NO

10824848

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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Provided are compounds of the formula (and pharmaceutically acceptable salts thereof): 1 wherein: R is hydrogen, methyl, hydroxymethyl or .alpha.-hydroxyethyl; R.sup.1 and R.sup.2 are independently selected from hydrogen, C.sub.1-C.sub.6 alkyl, C.sub.1-C.sub.6 hydroxyalkyl, C.sub.3-C.sub.8 cycloalkyl, C.sub.1-C.sub.6 alkenyl, C.sub.1-C.sub.6 alkynyl, amino, monoalkylamino, dialkylaminoalkyl, and pyrrolidin-1-ylalkyl; and Y is selected from the group consisting of C.sub.1-C.sub.6 alkyl, substituted and unsubstituted aryl; with the provisos that: (a) if Y is aryl, then at least one of R.sup.1 and R.sup.2 is other than hydrogen, and (b) if R.sup.2 is hydrogen R.sup.1 is other than methyl. Also provided are pharmaceutical compositions containing the compounds, and methods for the preparation of the compounds. The compounds are useful, among other things, as prodrugs which can be converted under acidic conditions to thiazolium agents. The compounds can be administered to mammals, including humans, for treatment of various indications.

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Patent Owner(s)

Patent OwnerAddress
ALTEON INC165 LUDLOW AVENUE NORTHVALE NEW JERSEY 07647

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Katten, Elliot Flushing, NY 2 4
Reinhard, Emily Ridgewood, NJ 4 12

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