Hoechst Celanese Corporation

American Hoechst Corporation

Gensia Pharmaceuticals, Inc.

Gensia, Inc.

Ernest K Metzner

Gerald F Sigler

Harold David

Emily S Winn-Deen

Rodrigo G Chavez

Mark D Erion

Harry E Gruber

Ronald R Tuttle

Bheemarao G Ugarkar

Paul J Marangos

Clinton E Browne

Jack W Reich

The present invention relates generally to methods of diagnosis, evaluation and treatment of coronary artery disease in mammals using substituted catecholamines and compounds therefore. It also relates to the preparation, use and administration of these compounds which are useful in the diagnosis, evaluation and treatment of coronary artery disease by means of a feedback controlled drug delivery system that delivers exercise simulating agents which are capable of eliciting acute responses similar to those elicited by aerobic exercise.

Method and compounds for diagnosing coronary artery disease

AICA riboside and prodrugs of AICA riboside are provided which lower blood glucose for the treatment of various pathologic conditions, including hypoglycemia, insulin deficiency, insulin resistance diabetes and Syndrome X. Prodrugs of AICA riboside provide AICA riboside in an orally bioavailable form. The use of adenosine kinase inhibition and ZMP enhancement for lowering blood glucose are also described.

Method and compounds for aica riboside delivery and for lowering blood

An aromatic substituted glycoside is disclosed of the formula ##STR1## wherein the configuration of the substituted --OR on the anomeric carbon is alpha, n is an integer of 0 or 1, and R is a substituted aromatic radical selected from the group ##STR2## where R.sub.1 through R.sub.6 are independently halogen, NO.sub.2, SO.sub.3 H, COR.sub.7, ##STR3## where R.sub.7 is lower alkyl; and includes its stereoisomers, optical isomers and geometric isomers and mixtures of the foregoing isomers. These substrates are useful as direct substrates for alpha-amylases. A process for the preparation of the substrates and related substances is also described.

Aromatic substituted glycoside

An aromatic substituted glycoside is disclosed of the formula ##STR1## wherein the configuration of the substituted --OR on the anomeric carbon is alpha, n is an integer of 0 or 1, and R is a substituted aromatic radical selected from the group ##STR2## where R.sub.1 through R.sub.6 are independently halogen, NO.sub.2, SO.sub.3 H, ##STR3## where R.sub.7 is lower alkyl; and includes its stereoisomers, optical isomers and geometric isomers and mixtures of the foregoing isomers. These substrates are useful as direct substrates for alpha-amylases. A process for the preparation of the substrates and related substances is also described.

An aromatic substituted glycoside is disclosed of the formula ##STR1## wherein the configuration of the substituted --OR on the anomeric carbon is alpha, n is an integer of 0 to 1, and R is a substituted aromatic radical selected from the group ##STR2## where R.sub.1 through R.sub.6 are independently halogen, NO.sub.2, SO.sub.3 H, ##STR3## where R.sub.7 is lower alkyl; and includes its stereoisomers, optical isomers and geometric isomers and mixtures of the foregoing isomers. These substrates are useful as direct substrates for alpha-amylases. A process for the preparation of the substrates and related substances is also described.

Reagent system for an alpha-amylase assay containing aromatic

.beta.-Hydroxy-.beta.-methylglutaric acid is prepared by treating 3-methyl-1,3,5-pentanetriol in aqueous media with a permanganate salt.

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Del Mar, CA, United States of America

Ernest K Metzner