59023-32-4

Upstream product

• 78208-58-9 1,3-dimethyl-4-nitropyrazole-5-carboxamide 
• 3920-37-4 1,3-dimethyl-4-nitro-1H-pyrazole-5-carboxylic acid 
• 37141-71-2 1,3-dimethyl-4-nitro-1H-pyrazole-5-carbonyl chloride 
• 5744-56-9 1,3-dimethylpyrazol-5-carboxylic acid 

Downstream Products

• 104393-48-8 4-(4-Chloro-benzoylamino)-2,5-dimethyl-2H-pyrazole-3-carboxylic acid amide 
• 104393-52-4 4-(3,5-Dimethoxy-benzoylamino)-2,5-dimethyl-2H-pyrazole-3-carboxylic acid amide 
• 104393-46-6 2,5-Dimethyl-4-phenylacetylamino-2H-pyrazole-3-carboxylic acid amide 
• 59023-41-5 5-(4-chloro-phenoxymethyl)-1,3-dimethyl-1,6-dihydro-pyrazolo[4,3-d]pyrimidin-7-one 
• 1285500-15-3 (S)-1-ethyl-3-(4-(7-(3-ethylmorpholino)-1,3-dimethyl-1H-pyrazolo[4,3-d]pyrimidin-5-yl)phenyl)urea 
• 104393-45-5 4-(1,3-dimethyl-7-oxopyrazolo<4,3-d>pyrimidin-5-yl)-N-<2-(dimethylamino)ethyl>benzenesulfonamide 
• 104393-27-3 5-(3,5-Dimethoxy-phenyl)-1,3-dimethyl-1,6-dihydro-pyrazolo[4,3-d]pyrimidin-7-one 
• 104393-41-1 5-(2-Amino-4-chloro-phenyl)-1,3-dimethyl-1,6-dihydro-pyrazolo[4,3-d]pyrimidin-7-one 
• 104393-25-1 5-(2-Methoxy-phenyl)-1,3-dimethyl-1,6-dihydro-pyrazolo[4,3-d]pyrimidin-7-one 
• 104393-26-2 5-(3,4-Dichloro-phenyl)-1,3-dimethyl-1,6-dihydro-pyrazolo[4,3-d]pyrimidin-7-one 
• 104393-23-9 5-(4-Chloro-phenyl)-1,3-dimethyl-1,6-dihydro-pyrazolo[4,3-d]pyrimidin-7-one 
• 104393-21-7 5-Benzyl-1,3-dimethyl-1,6-dihydro-pyrazolo[4,3-d]pyrimidin-7-one 
• 104393-24-0 1,3-Dimethyl-5-p-tolyl-1,6-dihydro-pyrazolo[4,3-d]pyrimidin-7-one 

Relevant academic research and scientific papers

A hit to lead discovery of novel N-methylated imidazolo-, pyrrolo-, and pyrazolo-pyrimidines as potent and selective mTOR inhibitors

A series of N-7-methyl-imidazolopyrimidine inhibitors of the mTOR kinase have been designed and prepared, based on the hypothesis that the N-7-methyl substituent on imidazolopyrimidine would impart selectivity for mTOR over the related PI3Kα and δ kinases. The corresponding N-Me substituted pyrrolo[3,2-d]pyrimidines and pyrazolo[4,3-d]pyrimidines also show potent mTOR inhibition with selectivity toward both PI3α and δ kinases. The most potent compound synthesized is pyrazolo[4,3-d]pyrimidine 21c. Compound 21c shows a Ki of 2 nM against mTOR inhibition, remarkable selectivity (>2900×) over PI3 kinases, and excellent potency in cell-based assays.

N-7 SUBSTITUTED PURINE AND PYRAZOLOPYRIMINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE

The present invention relates to compounds of Formula I: wherein R1, R2, R3, A1, A2, A3, A4, Y1 and Y2 and D have the meaning described herein. The present invention also relates to pharmaceutical compositions comprising such compounds and therapeutic uses thereof.

Sildenafil (Viagra(TM)), a potent and selective inhibitor of type 5 CGMP phosphodiesterase with utility for the treatment of male erectile dysfunction

5-(2'-Alkoxyphenyl)pyrazolo[4,3-d]pyrimidin-7-ones, and in particular our preferred compound, sildenafil (VIAGRA(TM)), discovered through a rational drug design programme, are potent and selective inhibitors of the type 5 cGMP phosphodiesterase from both rabbit platelets and human corpus cavernosum. Sildenafil is currently in the clinic for the oral treatment of male erectile dysfunction.

Synthesis and potential antipsychotic activity of 1H-imidazo[1,2-c]pyrazolo[3,4-e]pyrimidines

The synthesis of a series of 1H-imidazo[1,2-c]pyrazolo[3,4-e]pyrimidines is reported along with the effects of these compounds in preclinical tests for antipsychotic activity. Certain of these compounds displayed antipsychotic-like effects in conditioned

PYRAZOLO[4,3-D]PYRIMIDINE-5,7-(4H,6H)DIONE OR -5-THIONE-7-ONE ANALOGS

Various novel analogs of pyrazolo 4,3d!pyrimidine-5,7-(4H,6H) diones and also 5-thione-7-ones, novel methods of synthesis therefor, compositions and uses are the present invention. For example, the novel 5, 7-diones and 5-thione-7-ones are useful for stimulating the central nervous system reversing bronchoconstriction, and as cardiac stimulants cardiotonic agents.

5-Substituted pyrazolo[4,3-d]pyrimidine-7-ones and methods of use

The present invention relates to novel 5-substituted pyrazolo[4,3-d]pyrimidine-7-one compounds, and compositions, methods of use and processes to make therefor. The novel compounds are useful in the treatment of cardiovascular disorders, such as heart failure or cardiac insufficiency. The novel compounds bind adenosine receptors and selectively inhibit phosphodiesterase.

Synthesis and Structure-Activity Relationships of Pyrazolopyrimidin-7-ones as Adenosine Receptor Antagonists

A series of 21 1,3-dialkylpyrazolopyrimidin-7-ones substituted in the 5-position with various phenyl substituents has been synthesized and found to have affinity for the adenosine A1 receptor.The potency pattern due to substituents of the phenyl ring was found to parallel that found in a previously reported 1,3-dialkyl-8-phenylxanthine series.A quantitative structure-activity relationship was developed between these two series that correctly predicted the potencies of six additional 5-substituted pyrazolopyrimidines that were synthesized during the course of the analysis.With use of the correlation as a guide, one additional 5-phenylpyrazolopyrimidine containing a 4amino>sulfonyl substituent to improve aqueous solubility was prepared.On the basis of the high correlation between adenosine binding affinities of analogously substituted xanthines and pyrazolopyrimidines and the close superposition of the heterocyclic rings and substituents that is apparent from molecular models of these two series (Figure 2), it is hypothesized they fit the receptor in an analogous fashion.

Pyrazolobenzodiazepinones, their intermediates, their compositions and their use

1-(Lower)alkyl-4-(substituted)aminoalkylcarbonyl-1,4,9,10-tetrahydropyrazolo[4,3-b][1,5]benzodiazepin-10-ones are useful, e.g., to protect warm blooded animals against the formation of gastric ulcers. They are active ingredients in otherwise conventional medicament compositions administered enterally or parenterally in standard dosage forms. Their synthesis, their novel intermediates and their acid-addition salts are described.