| 摘要 |
<p>This invention is for ?-allenyl-?-aminobutyric acid derivatives of the formula: (I) and the pharmaceutically acceptable salts thereof wherein: R1 is hydrogen, halo, alkyl of 1 to 4 carbons, alkyl phenyl of 7 to 9 carbon atoms or substituted phenyl or alkyl phenyl of 7 to 9 carbon atoms wherein the substituents are halo, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, thioalkyl of 1 to 4 carbon atoms or amino alkyl of 1 to 4 carbon atoms, or sulfonylor sulfoxylalkyl of 1 to 4 carbon atoms, sulfonyl- or sulfoxylaryl, or sulfonyl- or sulfoxylhaloalkyl of 1 to 4 carbon atoms; R2 and R3 are independently hydrogen, halo, alkyl of 1 to 4 carbons, alkyl phenyl of 7 to 9 carbon atoms or substituted phenyl or alkyl phenyl of 7 to 9 carbon atoms wherein the substituents are halo, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, thioalkyl of 1 to 4 carbon atoms, or amino alkyl of 1 to 4 carbon atoms; R4 is hydrogen, alkyl carbonyl wherein the alkyl moiety contains from 1 to 22 carbon atoms, alkoxy carbonyl wherein the alkoxy moiety contains from 1 to 22 carbon atoms or Formula II ( II ) wherein R6 is hydrogen, alkyl of 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; R5 is hydroxyl, alkoxy of 1 to 22 carbons, alkyl amino of 1 to 22 carbon atoms or Formula III (III) wherein R7 is hydrogen, alkyl of 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; A is -CH=CH- or Formula IV (IV) wherein R8, R8' and R8" are independently hydrogen, alkyl of 1 to 4 carbon atoms, phenyl or substituted phenyl wherein the substituents are halo or alkoxy of 1 to 4 carbon atoms and n is the integer 0 or 1. These derivatives are ?-aminobutyric acid transaminase inhibitors.</p> |
