Merrell Dow Pharmaceuticals

Merrell Pharmaceuticals, Inc.

Aventis Pharma Limited

Barry L Rhinehart

Paul S Liu

Sai P Sunkara

John K Daniel

Mohinder S Kang

Roland S Rogers

Liu,paul S

A method for inhibiting the formation of glucose by the administration of castanospermine is described herein. In addition, a new process for the isolation of castanospermine from Castanospermum australe is also described.

Isolation of castanospermine and its use as an antidiabetic agent

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.

Hydroxymethyl-indolizidines and quinolizidines and their use as

Castanospermine mono- and di-esters and glycosides active as inhibitors of carbohydrate digestive enzymes and useful in treating diabetes are described herein. The compounds are prepared by the reaction of castanospermine with an appropriate acid halide or anhydride or with an appropriate glycosyl halide or glycosyl acetimidate under conditions which would favor the isolation of the mono- and di-esterified and glycosylated products. Various blocking groups, which can be selectively removed under mild conditions, can also be used to favor the formation of certain isomers.

Castanospermine esters and glycosides

A method for the inhibition of tumor metastases is described herein. The method makes use of the administration of castanospermine.

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Cincinnati, OH, United States of America

Barry L Rhinehart