.gamma.-allenyl-.gamma.-aminobutyric acids

Details .gamma.-allenyl-.gamma.-aminobutyric acids .gamma.-allenyl-.gamma.-aminobutyric acids

C - Chemistry, Metallurgy

07

D

167/246, 260/520

C07D 207/26 (2006.01) C07D 207/267 (2006.01) C07D 207/273 (2006.01) C07D 207/28 (2006.01) C07D 207/404 (2006.01)

Patent

CA 1252477

ABSTRACT OF THE DISCLOSURE: This invention is for ?-allenyl-?-aminobutyric acid derivatives of the formula: (I) Image 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 sulfonyl- or 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 Image ( II ) - 2 - 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) Image wherein R7 is hydrogen, alkyl of 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; A is -CH=CH- or Formula IV Image (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.

458364

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