- PYRROLO[3,2-D]PYRIMIDINE-2,4(3H,5H)-DIONE DERIVATIVES
-
This invention relates to novel Pyrrolo[3,2-d]pyrimidine-2,4(3H,5H)-dione derivatives of Formula (I), and their use as TRPC5 modulators, pharmaceutical compositions containing the same, and methods of using the same as agents for the treatment of TRPC5 receptor mediated disorders or conditions. R1, R2, R3 R4 and R5 have meanings given in the description.
- -
-
Page/Page column 33
(2016/02/29)
-
- SULFONAMIDE DERIVATIVE AND MEDICINAL USE THEREOF
-
Provided are sulfonamide derivatives of a specific chemical structure in which a sulfonamide group having, as a substituent, a phenyl group or a heterocyclic group having a hetero atom(s) as a constituent element(s) is present at its terminal, and pharmaceutically acceptable salts thereof. These compounds are novel compounds having excellent α4 integrin-inhibitory action.
- -
-
Paragraph 0617-0618
(2015/02/25)
-
- New pyrrolopyrimidin-6-yl benzenesulfonamides: Potent A2B adenosine receptor antagonists
-
A new series of 4-(1,3-dialkyl-2,4-dioxo-2,3,4,5-tetrahydro-1H-pyrrolo[3,2-d]pyrimidin-6 -yl)benzenesulfonamides has been identified as potent A2B adenosine receptor antagonists. The products have been evaluated for their binding affinities for the human A2B, A1 and A3 adenosine receptors. 6-(4-{[4-(4-Bromobenzyl)piperazin-1-yl]sulfonyl}phenyl)-1,3-dimethyl-1H- pyrrolo[3,2-d]pyrimidine-2,4(3H,5H)-dione (16) showed a high affinity for the A2B adenosine receptor (IC50 = 1 nM) and selectivity (A1: 183x; A3: 12660x). Synthesis and SAR of this novel class of compounds showing improved absorption properties is presented herein.
- Esteve, Cristina,Nueda, Arsenio,Diaz, Jose Luis,Beleta, Jorge,Cardenas, Alvaro,Lozoya, Estrella,Cadavid, Maria Isabel,Loza, Maria Isabel,Ryder, Hamish,Vidal, Bernat
-
p. 3642 - 3645
(2008/09/21)
-
- Polyfunctional derivatives of isocytosine. Effect of hydration on prototropic tautomerism of 2-(2-hydroxyethyl)amino-6-methylpyrimidin-4(3H)-one
-
Hydration of 2-(2-hydroxyethyl)amino-6-methylpyrimidin-4(3H)-one forms an equilibrium mixture of 4-oxo-3,4-dihydro and 4-hydroxy tautomers. The intermediate in mutual transitions of these tautomers has a zwitter ionic structure. The equilibrium shifts to the 4-oxo-3,4-dihydro form as the polarity of the medium decreases. 2005 Pleiades Publishing, Inc.
- Erkin,Krutikov
-
p. 639 - 644
(2008/02/01)
-
- Kinetics and Mechanisms of Hydrolytic Reactions of Methylated Cytidines under Acidic and Neutral Conditions
-
First-order constants have been determined for acidic hydrolysis, and for acidic and acid buffer-catalysed, deamination of cytidine and a number of its methylated derivatives.Rate constants for deamination under neutral conditions (frequently referred to as spontaneous deamination) have also been determined.N4-Methyl groups retard both deamination and hydrolysis, the former influence being much larger.A 6-methyl substituent retards deamination even more markedly, but accelerates hydrolysis.The effect of a 5-methyl group on the rates of both reactions is minor.The mechanisms of the deamination reactions under various conditions are discussed on the basis of structural effects, rates of hydrogen exchange at C5 and kinetic α-secondary isotope effects.Relevance of the data to enzyme-catalysed deamination and non-enzymatic deamination of cytosine residues in nucleic acids is briefly discussed.
- Kusmierek, Jaroslav,Kaeppi, Rainer,Neuvonen, Kari,Shugar, David,Loennberg, Harri
-
p. 196 - 202
(2007/10/02)
-