Abstract: The invention relates to a novel highly selective and potent NPP1 inhibitors, compositions comprising such, and their use as pharmaceuticals.

Abstract: The present invention is directed to styryl quinolinium compounds, a process for their synthesis and their use for selective nucleoli staining in cells, preferably in living cells and for imaging rRNA.

Abstract: The disclosure provides particular uridine di- and tri-phosphate compounds of Formula I, and pharmaceutical compositions thereof. The definitions of variables such as R, Y, B, m, Z1, Z2, and Z3 are as provided in the disclosure. These compounds are useful for treatment of diseases, disorders and conditions modulated by P2Y6 receptors, and particularly for lowering intraocular pressure and thereby treating ocular hypertension and/or glaucoma.

Abstract: Particular nucleoside 5?-phosphorothioate analogues, such as, adenosine or uridine 5?-di- or tri-phosphorothioate analogues in which at least one of the bridging oxygen atoms of the phosphorothioate is replaced by a group such as —CH2— or —CCl2—, and at least one of the non-bridging atoms or negatively-charged atoms of the phosphorothioate is either a sulfur atom or a sulfur ion can be formulated into pharmaceutical compositions. These compounds are useful for treatment of osteoarthritis/calcium pyrophosphate dihydrate (CPPD) deposition disease.

Abstract: The invention provides particular uridine di- and tri-phosphate derivatives, and pharmaceutical compositions thereof. These compounds are useful for treatment of diseases, disorders and conditions modulated by P2Y6 receptors, and particularly for lowering intraocular pressure and thereby treating ocular hypertension and/or glaucoma.

Abstract: The invention provides non-hydrolyzable nucleoside polyphosphate derivatives, e.g., 2MeS-adenosine-?,?-CH2-5?-O-(1-boranotriphosphate), 2MeS-adenosine-?,?-CCl2-5?-O-(1-boranotriphosphate), 2-MeS-adenosine-5?-dichloro methylene-diphosphate, 2-MeS-adenosine-5?-difluoromethylene-diphosphate and 2MeS-adenosine-5?-O-(1-boranodiphosphate), as well as pharmaceutical compositions thereof. These compounds are useful for prevention or treatment of diseases or disorders modulated by P2Y-receptors such as type 2 diabetes, and for pain control.

Abstract: The invention relates to fluorescent N2,N3-etheno-purine (2?-deoxy) riboside derivatives and fluorescent oligonucleotide probes comprising one or more moieties thereof, their preparation and uses thereof for staining DNA/RNA and for detection and quantitation of genetic material.

Abstract: The present invention provides dinucleoside boranophosphate derivatives of the general formula I: wherein X and X? each independently is an unsubstituted or substituted purine or pyrimidine residue; Y and Y? each independently is H or OH; Z1 to Z5 each independently is O? or BH3?, but excluding the compounds wherein Z1 to Z5 are each O?; W1 to W4 each independently is O, CH2, NH or C(Halogen)2; n and n? each independently is 0 or 1; m is 3, 4 or 5; and M+ represents a pharmaceutically acceptable cation, and to pharmaceutical compositions thereof. These dinucleoside boranophosphates are useful for prevention or treatment of diseases or disorders modulated by P2Y receptors such as type 2 diabetes, cystic fibrosis and cancer.

Abstract: The invention provides novel inorganic boranophosphate salts that can be used as fertilizers, in detergent formulations, as additive in melts for the glass industry, in boron neutron-capture therapy of cancer, and as synthetic building blocks in the synthesis of boranonucleotides of various lengths.

Abstract: 2-Substituted-5?-O-(1-boranotriphosphate)adenosine derivatives having at position 2 a radical R1 selected from the group consisting of H; halogen; O-hydrocarbyl; S-hydrocarbyl; NR3R4; and hydrocarbyl optionally substituted by halogen, CN, SCN, NO2, OR3, SR3 or NR3R4; wherein R3 and R4 are each independently H or hydrocarbyl or R3 and R4 together with the nitrogen atom to which they are attached form a saturated or unsaturated heterocyclic ring optionally containing 1-2 further heteroatoms selected from oxygen, nitrogen and sulfur, and pharmaceutically acceptable salts or diastereoisomers thereof or a mixture of diastereoisomers, are useful for treatment of type 2 diabetes.

Abstract: The invention provides novel inorganic boranophosphate salts that can be used as fertilizers, in detergent formulations, as additive in melts for the glass industry, in boron neutron-capture therapy of cancer, and as synthetic building blocks in the synthesis of boranonucleotides of various lengths.

Abstract: Dinucleoside poly(borano)phosphates are provided that can be useful for prevention or treatment of diseases or disorders modulated by P2Y receptors such as type 2 diabetes, cystic fibtosis and cancer.

Abstract: The invention relates to fluorescent N2,N3-etheno-purine (2?-deoxy) riboside derivatives and fluorescent oligonucleotide probes comprising one or more moieties thereof, their preparation and uses thereof for staining DNA/RNA and for detection and quantitation of genetic material.

Abstract: 2-Substituted-5?-O-(1-boranotriphosphate)adenosine derivatives having at position 2 a radical R1 selected from the group consisting of H; halogen; O-hydrocarbyl; S-hydrocarbyl; NR3R4; and hydrocarbyl optionally substituted by halogen, CN, SCN, NO2, OR3, SR3 or NR3R4; wherein R3 and R4 are each independently H or hydrocarbyl or R3 and R4 together with the nitrogen atom to which they are attached form a saturated or unsaturated heterocyclic ring optionally containing 1-2 further heteroatoms selected from oxygen, nitrogen and sulfur, and pharmaceutically acceptable salts or diastereoisomers thereof or a mixture of diastereoisomers, are useful for treatment of type 2 diabetes.

Abstract: Ectonucleoside triphosphate diphosphohydrolases [NTPDases; EC 3.6.1.5] constitute a family of enzymes which are involved in the metabolism of extracellular nucleotides, catalysing the hydrolysis of the gamma and beta phosphate bonds of triphospho- and diphosphonucleosides (whereas 5′nucleotidases [EC 3.1.3.5] catalyse the hydrolysis of alpha phosphate bond of monophosphonucleosides). These extracellular nucleotides interact with endothelial, epithelial and smooth muscle cells, as well as blood cells and lymphoid cells, to influence the different physiological systems of vertebrates.

Abstract: C8-substituted purine nucleotide analogs, such as ATP analogs, and their use is described, including their use as inhibitors of NTPDases and thereby as tools to modulate the conversion of nucleotides into nucleoside derivatives, and thus modulate the levels of these compounds. Such modulation further provides for the modulation of the activity and function of many processes which are affected by these compounds.

Abstract: The present invention provides 8-substituted 1,3,7-trialkylxanthines useful as A.sub.2 -selective adenosine receptor antagonists and compositions comprising such compounds. Examples of the 8-substituted 1,3,7-trialkyl xanthines include: ##STR1## In compound (a), R.sub.1, R.sub.3, and R.sub.7 are methyl and X is one to three substituents, which may be the same or different and selected from the group consisting of amino, C.sub.1 -C.sub.4 alkylcarbonylamino, carboxy C.sub.2 -C.sub.4 alkylcarbonylamino, halo, C.sub.1 -C.sub.3 alkyloxy, amino C.sub.1 -C.sub.4 alkyloxy, C.sub.1 -C.sub.4 alkyloxy carbonylamino, amino C.sub.1 -C.sub.4 alkenyloxy, isothiocyanato, and diazonium tetrafluoroborate. In compound (b), R.sub.1, R.sub.3, and R.sub.7 are methyl, R.sub..beta. is hydrogen or methyl, and X is selected from the group consisting of R, C(.dbd.O)OR, and C(.dbd.O)NH--R, wherein R is a C.sub.1 -C.sub.6 alkyl.

Abstract: The present invention provides certain novel adenosine triphosphate (ATP) analogs, pharmaceutical compositions, and methods of using such analogs in the treatment of septic shock and other disease conditions. Examples of the ATP analogs include the mono-, di- and triphosphates of adenosines with various selected substituents at the 2, 6, 8, and 9-positions, such as alkyl, alkylphenyl, phenylalkyl, S-alkyl, S-alkenyl, S-alkylcyano, S-phenyl, S-alkylphenyl, S-alkylamino, S-alkylthioalkyl, S-alkylthiocyanato, S-alkylaminophenyl, S-alkylnitrophenyl, hydroxy, bromo, fluoro, chloro, and aminoalkylamino. The present invention also provides pharmaceutical compositions of and methods of using certain xanthine and uracil derivatives for the above disease conditions. Examples of the xanthine derivatives include xanthines having alkyl or alkyltriphosphate substituents at the 1, 3, and 7-positions. Examples of the uracil derivatives include 5-fluoro- and 5-bromo uracil triphosphates.