Abstract: Novel indole and azaindole compounds of the following structure and their use as fructose-1,6-bisphosphatase inhibitors is described: ##STR1## and pharmaceutically acceptable prodrugs and salts thereof.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: Novel diazepine derivatives which selectively inhibit adenosine monophosphate deaminase and methods of preparing these compounds are provided. These compounds are useful in treating certain conditions in vivo which may be ameliorated by increased local concentrations of adenosine.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: The specification discloses the compounds of formula I ##STR1## wherein (a) --CH.sub.2 Ar represents ##STR2## in which R.sub.1 represents hydrogen, halogen, C.sub.1 -C.sub.3 -alkyl, C.sub.1 -C.sub.3 -alkoxy, benzyloxy, hydroxy or trifluoromethyl; and R.sub.2 represents hydrogen, halogen, C.sub.1 -C.sub.3 -alkyl, C.sub.1 -C.sub.3 -alkoxy, benzyloxy, hydroxy or trifluoromethyl; provided that R.sub.2 represents hydrogen or C.sub.1 -C.sub.3 -alkyl if R.sub.1 represents trifluoromethyl, or that R.sub.1 represents hydrogen or C.sub.1 -C.sub.3 -alkyl if R.sub.2 represents trifluoromethyl; or(b) --CH.sub.2 Ar represents ##STR3## in which X represents sulfur or oxygen and in which attachment to the thiophene or furan ring is at the 2- or 3-position; and tautomers thereof; as purine nucleoside phosphorylase inhibitors.

Abstract: Novel lyxose derivatives which selectively inhibit adenosine kinase and methods of preparing these compounds are provided. These compounds are useful in treating certain conditions in vivo which may be ameliorated by increased local concentrations of adenosine.

Abstract: The invention relates to the N-phosphonomethyl-biaryl substituted dipeptide derivatives of formula I ##STR1## and tetrazole derivatives of the formula Ia ##STR2## wherein A represents a direct bond, lower alkylene, phenylene or cyclohexylene; m represents 1 or zero, provided that m represents 1 when A is a direct bond; R.sub.2 represents hydrogen, hydroxy, lower alkyl, aryl-lower alkyl, C.sub.5 -C.sub.

Abstract: Disclosed is a compound of the formula ##STR1## wherein R.sup.1 is H, NH.sub.2, or OCH.sub.3, R.sup.2 is an optionally substituted cyclic group optionally containing one or more heteroatoms, R.sup.3 and R.sup.4 are independently H or C.sub.1-4 alkyl, m is 0-4, n is 0-6, p is 0.1, X is CN, CSNH.sub.2, PO(OH).sub.2, COOH, SO.sub.2 NH.sub.2, NH.sub.2, OH, CNHNH.sub.2, tetrazole, triazole, or COR.sup.5 where R.sup.5 is C.sub.1-4 alkyl, CF.sub.3, NH.sub.2, or OC.sub.1-4 alkyl, and Y is O or NH that is useful as a pharmaceutical.

Abstract: The invention relates to the N-phosphonomethyl-biaryl substituted dipeptide derivatives of formula I ##STR1## wherein A represents a direct bond, lower alkylene, phenylene or cyclohexylene; m represents 1 or zero, provided that m represents 1 when A is a direct bond; R.sub.2 represents hydrogen, hydroxy, lower alkyl, aryl-lower alkyl, C.sub.5 -C.sub.

Abstract: Disclosed is a compound containing a 2-amino-7-(substituted methyl)-3H,5H-pyrrolo[3,2-d]pyrimidin-4-one wherein substituted methyl is --CH.sub.2 --R wherein R is an optionally substituted alicyclic group, a pharmaceutical composition containing the compound, and a method for the selective suppression of mammalian T-cell function without diminished effect on humoral immunity which involves administering the composition to a mammal.

Abstract: Disclosed is a compound containing a 2-amino-7-(substituted methyl)-3H,5H-pyrrolo[3,2-d]pyrimidin-4-one wherein substituted methyl is --CH.sub.2 --R wherein R is an optionally substituted heteroalicyclic group, a pharmaceutical composition containing the compound, and a method for the selective suppression of mammalian T-cell function without diminished effect on humoral immunity which involves administering the composition to a mammal.

Abstract: Disclosed is a compound containing 2-amino-7-(R)-3H,5H-pyrrolo[3,2-d]pyrimidin-4-one wherein R is optionally substituted cyclohexenyl or cyclohexyl, a pharmaceutical composition containing the compound, and a method for the selective suppresion of mammalian T-cell function without diminished effect on humoral immunity which involves administering the composition to a mammal.

Abstract: Disclosed is a compound containing a 2-amino-7-(substituted methyl)-3H,5H-pyrrolo[3,2-d]pyrimidin-4-one wherein substituted methyl is --CH.sub.2 --R wherein R is optionally substituted pyridinyl, a pharmaceutical composition containing the compound, and a method for the selective suppression of mammalian T-cell function without diminished effect on humoral immunity which involves administering the composition to a mammal.