43024-70-0Relevant articles and documents
CHEMOKINE RECEPTOR ACTIVITY REGULATOR
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Paragraph 0243, (2014/08/19)
The invention provides a chemokine receptor activity modulator containing a pyrazolopyrimidine derivative represented by the formula (I) wherein R1, R2, R3, and R4 are as described herein.
PYRAZOLOPYRIMIDINE DERIVATIVE
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Paragraph 0169, (2013/03/26)
The present invention provides a pyrazolopyrimidine derivative represented by formula (I) {wherein R1 represents -NR1aR1b (wherein R1a and R1b are the same or different and each is a hydrogen atom, ar
3-Aminocarbonyl-substituted fused pyrazolo-derivatives as protein kinase modulators
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Page/Page column 22, (2008/12/04)
The present invention relates to pyrazolo[1,5-a]pyrimidine-3-carboxylic acid compounds of formula I or pharmaceutically acceptable salts thereof and their use for the treatment of protein kinase modulation responsive diseases.
N-Arylpiperazinyl-N'-propylamino derivatives of heteroaryl amides as functional uroselective α1-adrenoceptor antagonists
Elworthy, Todd R.,Ford, Anthony P. D. W.,Bantle, Gary W.,Morgans Jr., David J.,Ozer, Rachel S.,Palmer, Wylie S.,Repke, David B.,Romero, Magarita,Sandoval, Leticia,Sjogren, Eric B.,Talamás, Francisco X.,Vazquez, Alfredo,Wu, Helen,Arredondo, Nicolas F.,Blue Jr., David R.,DeSousa, Andrea,Gross, Lisa M.,Kava, M. Shannon,Lesnick, John D.,Vimont, Rachel L.,Williams, Timothy J.,Zhu, Quan-Ming,Pfister, Jürg R.,Clarke, David E.
, p. 2674 - 2687 (2007/10/03)
Novel arylpiperazines were identified as α1-adrenoceptor (AR) subtype- selective antagonists by functional in vitro screening. 3-[4-(ortho- Substituted phenyl)piperazin-1:yl]propylamines were derivatized with N,N- dimethyl anthranilamides, nicotinamides, as well as carboxamides of quinoline, 1,8-naphthyridine, pyrazolo[3,4-b]pyridine, isoxazolo[3,4- b]pyridine, imidazo[4,5-b]pyridine, and pyrazolo[1,5-a]pyrimidines. Strips of rabbit bladder neck were employed as a predictive assay for antagonism in the human lower tract. Rings of rat aorta were used as a 'negative screen' for the test antagonists. Binding to α1-ARs was relatively sensitive to size and electronic features of the arylpiperazine portion of the antagonists and permissive to these features on the heteroaryl carboxamide side. These structure-affinity findings were exploited to produce nicotinamides (e.g. 13ii and 25x) and pyrazolo[3,4-b]pyridines (e.g. 37f and 37y) ligands with nanomolar affinity at the α1-AR subtype prevalent in the human lower urinary tract (pA2 values: 8.8, 10.7, 9.3, and 9.9, respectively) and displaying 2-3 orders of magnitude selectivity over the α(1D)-AR.
Synthesis and Enzymic Activity of 6-Carbethoxy- and 6-Ethoxy-3,7-disubstituted-pyrazolopyrimidines and Related Derivatives as Adenosine Cyclic 3',5'-Phosphate Phosphodiesterase Inhibitors
Springer, Robert H.,Scholten, M. B.,O'Brien, Darrell E.,Novinson, Thomas,Miller, Jon P.,Robins, Roland K.
, p. 235 - 242 (2007/10/02)
A number of 3,7-disubstituted 6-carbethoxypyrazolopyrimidines and 3,7-disubstituted 6-ethoxypyrazolopyrimidines have been prepared and evaluated as adenosine cyclic 3',5'-phosphate (cAMP) phosphodiesterase (PDE) inhibitors vs. the low Km enzyme isolated from beef heart, rabbit lung, and kidney preparations.The results were found to be between 0.5 to 13 times as potent as theophylline as inhibitors of PDE, depending on the tissue source.A number of these PDE inhibitors exhibited significant physiological effects in different animal systems, suggesting it should be possible to obtain selective PDE inhibition in various tissues.Several of these heterocycles were found superior to adenosine in inhibiting ADP-induced platelet aggregation in vitro.