Gensia Pharmaceuticals, Inc.

Gensia, Inc.

Metabasis Therapeutics, Inc.

Clinton E Browne

Ronald R Tuttle

Bheemarao G Ugarkar

Harry E Gruber

Mark D Erion

Angelo J Castellino

David A Bullough

Kevin M Mullane

Jorge E Gomez Galeno

Jack W Reich

Paul J Marangos

Ernest K Metzner

Gary S Firestein

Leonard P Miller

Bheemaro G Vgarkar

Ernest K Metzker

Novel compounds which selectively inhibit adenosine kinase and methods of preparing adenosine kinase inhibitors are provided. Also provided are methods of treating various conditions which may be ameliorated by increased local concentrations of adenosine using adenosine kinase inhibitors.

Adenosine kinase inhibitors

Analogs of 5-amino-1-beta-D-ribofuranosylimidazole-4-carboxamide (AICA riboside) are provided which are useful in increasing extracellular levels of adenosine.

AICA riboside analogs

This invention relates to adenosine kinase inhibitors and to nucleoside analogs, specifically to orally active, substituted 5-aryl pyrrolo�2,3-d! pyrimidine and 3-aryl pyrazolo�3,4-d! pyrimidine nucleoside analogs having activity as adenosine kinase inhibitors. The invention also relates to the preparation and use of these and other adenosine kinase inhibitors in the treatment of cardiovascular and cerebrovascular diseases, inflammation and other diseases which can be regulated by increasing the local concentration of adenosine.

Orally active adenosine kinase inhibitors

This invention relates to adenosine kinase inhibitors and to nucleoside analogs, specifically to orally active, substituted 5-aryl pyrrolo�2,3-d!pyrimidine and 3-aryl pyrazolo�3,4-d! pyrimidine nucleoside analogs having activity as adenosine kinase inhibitors. The invention also relates to the preparation and use of these and other adenosine kinase inhibitors in the treatment of cardiovascular and cerebrovascular diseases, inflammation and other diseases which can be regulated by increasing the local concentration of adenosine.

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

Novel compounds which selectively inhibit adenosine kinase and methods of preparing adenosine kinase inhibitors are provided. Also provided are methods of treating various inflammatory conditions, including arthritis and SIRS, which may be ameliorated by increased local concentrations of adenosine using adenosine kinase inhibitors.

Methods for treating adenosine kinase related conditions

Methods and devices for the diagnosis, evaluation and treatment of coronary artery disease (CAD) by means of a closed-loop drug delivery system that delivers an exercise simulating agent, including novel exercise simulating agents which elicit both acute and adaptive cardiovascular responses similar to those elicited by aerobic activity are provided. The acute responses to the exercise simulating agent are used to diagnose and evaluate CAD in lieu of the acute responses to aerobic exercise. Due to their adaptive responses these compounds may be used to treat CAD in lieu of the adaptive responses caused by aerobic exercise training or to treat other conditions where the adaptive responses caused by aerobic exercise are desirable.

Diagnosis, evaluation and treatment of coronary artery disease by

1-(3,4-dihydroxyphenyl)-2-(4-(4-hydroxyphenyl)butaylamino)ethanol

Prodrugs of AICA riboside are provided which increase the bioavailability of AICA riboside and thereby increase extracellular concentrations of the prophylactic and affirmative treatment of various pathologic conditions, including ischemia. Also provided are methods of using AICA riboside prodrugs in treating such conditions.

Growing community of inventors

Oceanside, CA, United States of America

Clinton E Browne