Metabasis Therapeutics, Inc.

Gensia, Inc.

Gensia Pharmaceuticals, Inc.

Bheemarao G Ugarkar

Mark D Erion

K Raja Reddy

Clinton E Browne

Angelo J Castellino

Harry E Gruber

Serge H Boyer

Jorge E Gomez Galeno

Edward D Robinson

David A Bullough

Zhili Sun

William Craigo

Kevin M Mullane

Ronald R Tuttle

Paul J Marangos

Ernest K Metzner

Gary S Firestein

Michael Matelich

Leonard P Miller

Joseph J Kopcho

Jack W Reich

Ernest K Metzker

Michael C Matelich

Compounds of Formula I, their preparation and synthetic intermediates, and their use in the synthesis of prodrugs: 

Cyclic phosphate diesters of 1,3-propane-1-aryl diols and their use in preparing prodrugs

Prodrugs of formula I, their uses, their intermediates, and their method of manufacture are described: 

Prodrugs for phosphorus-containing compounds

The method of preparing compounds of Formula I is described: wherein: Additionally, methods and salt forms are described that enable isolation and purification of the desired isomer.

Process for preparation of cyclic prodrugs of PMEA and PMPA

Compounds of Formula I, their preparation and synthetic intermediates, and their use in the synthesis of prodrugs:  wherein:

Prodrugs of formula I, their uses, their intermediates, and their method of manufacturing are described:and pharmaceutically acceptable prodrugs and salts thereof.

Prodrugs of formula I, their uses, their intermediates, and their method of manufacture are described:

Prodrugs phosphorus-containing compounds

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

This invention relates to adenosine kinase inhibitors and to nucleoside analogs, specifically to water soluble, aryl substituted 4-amino pyrrolo�2,3-d! pyrimidine and pyrazolo�3,4-d! pyrimidine nucleoside analogs having activity as adenosine kinase inhibitors The invention also relates to the preparation and use of these 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.

Water soluble 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, C-4' modified pyrrolo�2,3-d!pyrimidine and pyrazolo�3,4-d!pyrimidine nucleoside analogs having activity as adenosine kinase inhibitors. The invention relates to nucleoside analogs of this kind, having zero substitutions or two substitutions at the C-4' position of the furanose (sugar) moiety. The invention also relates to the preparation and use of these 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.

C-4' modified 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.

Orally active adenosine kinase inhibitors

This invention relates to adenosine kinase inhibitors and to nucleoside analogs, specifically to water soluble, aryl substituted 4-amino pyrrolo�2,3-d! pyrimidine and pyrazolo�3,4-d! pyrimidine nucleoside analogs having activity as adenosine kinase inhibitors. The invention also relates to the preparation and use of these 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.

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.

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Escondido, CA, United States of America

Bheemarao G Ugarkar