Abstract: A method for preparing a N-[(aliphatic or aromatic)carbonyl)]-2-aminoacetamide compound, and for preparing a cyclized compound therefrom, as well as novel resin bound intermediate compounds that are useful for preparing such compounds.
Type:
Grant
Filed:
August 4, 1999
Date of Patent:
December 10, 2002
Assignee:
Aventis Pharamaceuticals Inc.
Inventors:
Christopher Hulme, George C. Morton, Joseph M. Salvino, Richard F. Labaudiniere, Helen J. Mason, Matthew M. Morrissette, Liang Ma, Marie-Pierre Cherrier
Abstract: This application relates to compounds of the formula
wherein R1 is hydrogen, (C1-C12)alkylcarbonyl, (C1-C12)alkoxycarbonyl, aryl(C1-C12)alkylaminocarbonyl, mono(C1-C18)alkylaminocarbonyl or di(C1-C8)alkylaminocarbonyl;
R2 is (C1-C12)alkylcarbonyloxy, aryl(C1-C4)alkylcarbonyloxy, (C1-C12)alkoxycarbonyloxy, arylcarbonyloxy, hydroxy, (C1-C6)alkoxycarbonyl(C1-C6)alkoxy or hydroxy(C1-C10)alkoxy;
R3 is hydrogen or halo; and pharmaceutically acceptable addition salts; with the proviso that when R2 is hydroxy, R1 and R3 are not both hydrogen or when R2 is hydroxy and R3 is hydrogen, R1 is not methylcarbonyl;
which compounds are useful for the treatment of memory dysfunction characterized by decreased cholinergic function, pharmaceutical compositions containing the compounds and methods for making and using the compounds.
Type:
Grant
Filed:
October 15, 1993
Date of Patent:
November 13, 2001
Assignee:
Aventis Pharamaceuticals Inc.
Inventors:
Raymond W. Kosley, Jr., Larry Davis, Veronica Taberna