Amino acid analogs as cck-antagonists

Details Amino acid analogs as cck-antagonists Amino acid analogs as cck-antagonists

C - Chemistry, Metallurgy

07

D

167/240, 260/319

C07D 209/20 (2006.01) A61K 31/40 (2006.01) C07C 275/30 (2006.01) C07D 209/42 (2006.01) C07K 5/078 (2006.01)

Patent

CA 1298842

2315S/1172A 17428 TITLE OF THE INVENTION AMINO ACID ANALOGS AS CCK-ANTAGONISTS ABSTRACT OF THE DISCLOSURE Analogs of glutamic acid and related amino acids and pharmaceutically-acceptable salts thereof which antagonize the function of cholecystokinins and gastrin disease states in animals and compositions for and methods of preventing or treating disorders of the gastrointestinal, central nervous and appetite regulatory systems of mammals, especially of humans. The compounds of the present invention are represented by the following formula: Image (I) wherein: R1 is (CH2)m-R5 or X1-(CH2)m-R6; R2 and R3 are independently selected from H; C1-C8-straight- or branched-chain-alkyl; C3-C8-cycloalkyl; with the proviso that R2 and R3 cannot both be H concurrently; R4 is ON; C1-C4-straight- or branched-chain- alkoxy; C3-C6-cycloalkoxy; OCH2 phenyl; amino-mono- or di-C1-C4-straight- or branched-chain-alkyl; amino-mono- or di-C3-C6-cycloalkyl: NH-CH2-phenyl; R5 is or Image ; R6 is Image ; R7 is H; C1-C4-straight- or branched-chain-alkyl; X1 is O or NH; X2 and X3 are independently H; OH; NO2; halo; C1-C4- straight- or branched-chain-alkyl; C1-C4- straight- or branched-chain-alkylthio; or C1-C4-straight- or branched-chain-alkoxy; X4 is O or NH; Y is NR7; n is 1-to-3; m is 0-to-4; and halo is F, Cl, Br, or I; or pharmaceutically-acceptable salts of these compounds.

539628

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