Merrell Dow Pharmaceuticals

Mohinder S Kang

Paul S Liu

Norton P Peet

Sai P Sunkara

Robert A Farr

Barry L Rhinehart

Roland S Rogers

[4S-(4.alpha.,4a.beta.,5.beta.,6.alpha.,7.alpha.,7a.alpha.)]-Octahydro-1H-1 -pyrindine-4,5,6,7-tetrols and [4R-(4.alpha.,4a.alpha.,5.alpha.,6.beta.,7.beta.,7a.beta.)]-octahydro-1H-1 -pyrindine-4,5,6,7-tetrols are useful as inhibitors of alpha-mannosidase and are useful immunostimulants, chemoprotective and radioprotective agents and antimetastatic agents.

.alpha.-mannosidase inhibitors

Amide and ester derivatives of 6-amino-octahydro-1,7,8-indolizinetriol are described herein. The compounds are prepared from castanospermine by replacing the appropriate hydroxy function with an amino function while protecting the other hydroxy groups in the meantime. The compounds are useful as hexosaminidase inhibitors.

Derivatives of 6-aminooctahydroindolizinetriol

The present invention describes a group of polyhydroxylated indolizidines and quinolizidines and their esters. These compounds are prepared starting from 2,6-dideoxy-2,6-dideoxy-2,6-imino-1,3,4,5-tetrakis-O- (phenylmethyl)-D-glycero-L-gulo-heptitol or a corresponding N-substituted compound. The compounds are useful in the treatment of diabetes and as .alpha.-glucosidase I inhibitors.

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Cincinnati, OH, United States of America

Mohinder S Kang