- AZOLOPYRIDINE AND AZOLOPYRIMIDINE COMPOUNDS AND METHODS OF USE THEREOF
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Provided herein are azolopyridine and azolopyrimidine compounds for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
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Page/Page column 147
(2012/03/26)
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- New application of heterocyclic diazonium salts. Synthesis of pyrazolo[3,4-d][1,2,3]triazin-4-ones and imidazo[4,5-d][1,2,3]triazin-4-ones
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The pyrazolo[3,4-d][1,2,3]triazin-4-ones 3 and imidazo[4,5-d][1,2,3] triazin-4-ones 4 are analogs structurally related to purines that have showed a wide and significant variety of biological activity. These compounds were synthesized by one-pot diazotization of 5-amino-1H-pyrazole-4-carbonitriles 1 and 5-amino-1H-imidazole-4-carbonitriles 2, respectively.
- Colomer, Juan Pablo,Moyano, Elizabeth Laura
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supporting information; scheme or table
p. 1561 - 1565
(2011/05/05)
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- Adenosine A3 receptor modulators
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The compounds of the following formula: wherein R, R2, R3 and A have the meanings given in the specification, are endowed with selective A3 adenosine receptor antagonist activity. These compounds can be used in a pharmaceu
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- Novel, highly potent adenosine deaminase inhibitors containing the pyrazolo[3,4-d]pyrimidine ring system. Synthesis, structure-activity relationships, and molecular modeling studies
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This study reports the synthesis of a number of 1- and 2-alkyl derivatives of the 4-aminopyrazolo[3,4-d]pyrimidine (APP) nucleus and their evaluation as inhibitors of ADA from bovine spleen. The 2-substituted aminopyrazolopyrimidines proved to be potent inhibitors, most of them exhibiting Ki values in the nanomolar/subnanomolar range. In this series the inhibitory activity is enhanced with the increase in length of the alkyl chain, reaching a maximum with the n-decyl substituent. Insertion of a 2′-hydroxy group in the ra-decyl chain gave 3k, whose (R)-isomer displayed the highest inhibitory potency of the series (Ki 0.053 nM), showing an activity 2 orders of magnitude higher than that of (+)-EHNA (Ki 1.14 nM), which was taken as the reference standard. Docking simulations of aminopyrazolopyrimidines into the ADA binding site were also performed, to rationalize the structure-activity relationships of this class of inhibitors.
- Da Settimo, Federico,Primofiore, Giampaolo,La Motta, Concettina,Taliani, Sabrina,Simorini, Francesca,Marini, Anna Maria,Mugnaini, Laura,Lavecchia, Antonio,Novellino, Ettore,Tuscano, Daniela,Martini, Claudia
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p. 5162 - 5174
(2007/10/03)
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- Adenosine A3 receptor modulators
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The compounds of the following formula: wherein R, R2, R3 and A have the meanings given in the specification, are endowed with selective A3 adenosine receptor antagonist activity. These compounds can be used in a pharmaceu
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- Adenosine A3 receptor modulators
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The compounds of the following formula: wherein R, R1, R2R3and A have the meanings given in the specification, are endowed with selective A3adenosine receptor agonist activity. These compounds can be used in a p
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- Synthesis and Pharmacological Evaluation of a Series of 4-Piperazinylpyrazolo- and -benzodiazepines as Potential Anxiolytics
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The synthesis and pharmacological evaluation of a series of pyrazolobenzodiazepines are described.Some of the 4-piperazinyl-2,10-dihydropyrazolobenzodiazepine derivatives demonstrated potent anxiolytic activity in the three-part operan
- Chakrabarti, Jiban K.,Hotten, Terrence M.,Pullar, Ian A.,Tye, Nicholas C.
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p. 2573 - 2582
(2007/10/02)
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