发明名称 Dihydrothiazine prodrugs of thiazolium agents
摘要 Provided are compounds of the formula (and pharmaceutically acceptable salts thereof): wherein: R is hydrogen, methyl, hydroxymethyl or alpha-hydroxyethyl; R<1 >and R<2 >are independently selected from hydrogen, C1-C6 alkyl, C1-C6 hydroxyalkyl, C3-C8 cycloalkyl, C1-C6 alkenyl, C1-C6 alkynyl, amino, monoalkylamino, dialkylaminoalkyl, and pyrrolidin-1-ylalkyl; and Y is selected from the group consisting of C1-C6 alkyl, substituted and unsubstituted aryl; with the provisos that: (a) if Y is aryl, then at least one of R<1 >and R<2 >is other than hydrogen, and (b) if R<2 >is hydrogen R<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.
申请公布号 US2005014747(A1) 申请公布日期 2005.01.20
申请号 US20040824848 申请日期 2004.04.15
申请人 REINHARD EMILY;KATTEN ELLIOT 发明人 REINHARD EMILY;KATTEN ELLIOT
分类号 A61P9/00;A61P9/10;A61P9/12;A61P9/14;C07D279/12;(IPC1-7):C07D279/12;A61K31/54;A61K31/541 主分类号 A61P9/00
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