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US 6,331,640 B1Granted
Diaminopropionic acid derivatives
AssigneeHoffmann-La Roche Inc.
InventorsNader Fotouhi, Paul Gillespie, Robert William Guthrie, Sherrie Lynn Pietranico-Cole, Weiya Yun
Life of this patent
Estimating the term…
Abstract
A compound of formula 1a which is useful for treating reperfusion injury, and salts, prodrugs, and related compounds.
Claims32
A compound of formula 1h
- wherein
- U, V, and W are independently selected from the group consisting of halogen, hydrogen and methyl, provided U and V are not both hydrogen;
- X is carbonyl or sulfonyl;
- Y is methylene;
- R3 is hydrogen or lower alkyl;
- k is 0 or 1;
- when k is 1, Z is hydrogen, lower alkylthio, —COOH, —CONH2—, amino, 1-adamantyl, diphenylmethyl, 3-[[(5-chloropyridin-2-yl)amino]carbonyl]pyrazin-2-yl, or Z is one of the following:
- cycloalkyl or aryl containing 0 to 3 heteroatoms which may be the same or different, or a fused ring system containing two or three rings which rings are independently cycloalkyl or aryl containing 0 to 3 heteroatoms which may be the same or different, any of which rings may be unsubstituted, or substituted with at least one of:
- halogen, cyano, amino, substituted amino, aminosulfonyl, nitro, oxo, hydroxy, aryl, aryloxy, unsubstituted lower alkyl, halogen-substituted lower alkyl, lower alkoxy-substituted lower alkyl, lower alkoxy, lower alkanesulfonyl, lower alkylthio, acetyl, aminocarbonyl, hydrazino, carboxy, lower alkoxycarbonyl, or acetoxy;
- and
- when k is 0, Z is 1-adamantyl, diphenylmethyl, 3-[[(5-chloropyridin-2-yl)amino]carbonyl]pyrazin-2-yl, or Z is one of the following:
- cycloalkyl or aryl containing 0 to 3 heteroatoms which may be the same or different, or a fused ring system containing two or three rings which rings are independently cycloalkyl or aryl containing 0 to 3 heteroatoms which may be the same or different, any of which rings may be unsubstituted, or substituted with at least one of:
- halogen, cyano, amino, substituted amino, aminosulfonyl, nitro, oxo, hydroxy, aryl, aryloxy, unsubstituted lower alkyl, halogen-substituted lower alkyl, lower alkoxy-substituted lower alkyl, lower alkoxy, lower alkanesulfonyl, lower alkylthio, acetyl, aminocarbonyl, hydrazino, carboxy, lower alkoxycarbonyl, or acetoxy;
- and pharmaceutically acceptable salts and esters thereof.
11 more elements
Dependencies are inferred from the claim text.