939979-32-5

Upstream product

• 83824-38-8 1-methyl-1H-pyrazolo[4,3-d]pyrimidine-5,7-(4H,6H)-dione 
• 92534-73-1 4-amino-1-methyl-1H-pyrazole-5-carboxamide 
• 92534-72-0 1-methyl-4-nitro-1H-pyrazole-5-carboxamide 
• 16034-46-1 1-methyl-1H-pyrazole-5-carboxylic acid 
• 1006962-20-4 1-methyl-4-nitro-1H-pyrazole-5-carbonyl chloride 
• 92534-69-5 1-methyl-4-nitro-1H-pyrazole-5-carboxylic acid 
• 83824-38-8 1-methylpyrazolo[4,3-d]pyrimidine-5,7-diol 
• 309740-49-6 methyl 1-methyl-4-nitro-1H-pyrazole-5-carboxylate 
• 923283-54-9 methyl 4-amino-1-methyl-1H-pyrazole-5-carboxylate 
• 530-62-1 1,1'-carbonyldiimidazole 

Downstream Products

• 939979-33-6 C₁₃H₁₀Cl₃N₅ 
• 1285500-09-5 (S)-1-ethyl-3-(4-(1-methyl-7-(3-methylmorpholino)-1H-pyrazolo[4,3-d]pyrimidin-5-yl)phenyl)urea 
• 1285500-13-1 (S)-1-ethyl-3-(4-(7-(3-ethylmorpholino)-1-methyl-1H-pyrazolo[4,3-d]pyrimidin-5-yl)phenyl)urea 
• 1285500-14-2 1-(4-(7-((1S,4S)-2-oxa-5-azabicyclo[2.2.1]heptan-5-yl)-1-methyl-1H-pyrazolo[4,3-d]pyrimidin-5-yl)phenyl)-3-ethylurea 
• 1357086-91-9 8-(furan-2-yl)-1-methyl-5-(4-phenylpiperazin-1-yl)-1H-pyrazolo[3,4-e][1,2,4]triazolo[1,5-c]pyrimidine 
• 1357086-88-4 5-cyclohexylamino-8-(furan-2-yl)-1-methyl-1H-pyrazolo[3,4-e][1,2,4]triazolo[1,5-c]pyrimidine 
• 1357086-75-9 5-{[(4-methoxy-phenyl)carbamoyl]amino}-8-(furan-2-yl)-1-methyl-1H-pyrazolo[3,4-e][1,2,4]triazolo[1,5-c]pyrimidine 

Relevant academic research and scientific papers

Novel pyrazolo[4,3-d]pyrimidine microtubule targeting agents (MTAs): Synthesis, structure–activity relationship, in vitro and in vivo evaluation as antitumor agents

The design, synthesis, and biological evaluation of a series novel N1?methyl pyrazolo[4,3-d]pyrimidines as inhibitors of tubulin polymerization and colchicine binding were described here. Synthesis of target compounds involved alkylation of the pyrazolo scaffold, which afforded two regioisomers. These were separated, characterized and identified with 1H NMR and NOESY spectroscopy. All compounds, except 10, inhibited [3H]colchicine binding to tubulin, and the potent inhibition was similar to that obtained with CA-4. Compounds 9 and 11–13 strongly inhibited the polymerization of tubulin, with IC50 values of 0.45, 0.42, 0.49 and 0.42 μM, respectively. Compounds 14–16 inhibited the polymerization of tubulin with IC50s near ～1 μM. Compounds 9, 12, 13 and 16 inhibited MCF-7 breast cancer cell lines and circumvented βIII-tubulin mediated cancer cell resistance to taxanes and other MTAs, and compounds 9–17 circumvented Pgp-mediated drug resistance. In the standard NCI testing protocol, compound 9 exhibited excellent potency with low to sub nanomolar GI50 values (≤10 nM) against most tumor cell lines, including several multidrug resistant phenotypes. Compound 9 was significantly (P 0.0001) better than paclitaxel at reducing MCF-7 TUBB3 (βIII-tubulin overexpressing) tumors in a mouse xenograft model. Collectively, these studies support the further preclinical development of the pyrazolo[4,3-d]pyrimidine scaffold as a new generation of tubulin inhibitors and 9 as an anticancer agent with advantages over paclitaxel.

DNA POLYMERASE IIIC INHIBITORS AND USE THEREOF

The present invention relates to compounds and methods useful for inhibiting the DNA polymerase IIIC enzyme. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of Gram-positive bacterial infections.

IRAK DEGRADERS AND USES THEREOF

The present invention provides compounds, compositions thereof, and methods of using the same.

Pyrazolo[4,3-d]pyrimidines as Antitumor Agents

A compound of Formula I, or optionally a salt or a hydrate of the compound of Formula I is provided: wherein X is one selected from the group consisting of wherein R is an alkyl group having from one to six carbon atoms, and wherein R2 is a halogen atom. A pharmaceutical composition comprising a compound of Formula I, or optionally a salt or a hydrate of the compound of Formula I, and a pharmaceutically acceptable carrier, is provided. A method of treating a patient with cancer is set forth including administering a therapeutically acceptable amount of the compound of Formula I, or a salt or a hydrate of the compound of Formula I, or a pharmaceutical composition comprising a compound of Formula I.

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.

Pyrrolo- and pyrazolo-[3,4-e][1,2,4]triazolo[1,5-c]pyrimidines as adenosine receptor antagonists

The discovery and development of adenosine receptor antagonists have represented for years an attractive field of research from the perspective of identifying new drugs for the treatment of widespread disorders such as inflammation, asthma and Parkinson's

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.

ALICYCLIC HETEROCYCLIC COMPOUND

An alicyclic heterocyclic compound represented by the following formula or a pharmaceutically acceptable salt thereof: wherein ring A is a heterocyclic ring, ring B is a carbocyclic ring, a heterocyclic ring etc., P1 and P2 are CH or N, q and r are 0 to 2, X is -NH-, -O-, -CH2-, etc., Y is -CH2-, -CO-, -SO2-, etc., Z is -CO-, -SO2-, etc., and R3 is carbocyclic group, heterocyclic group, hydroxyl, alkoxy or amino, is useful as a controlling agent of the function of CCR4 useful for the prevention or treatment for bronchial asthma, atopic dermatitis, etc.

AROMATIC COMPOUND

An aromatic compound represented by the following formula or a pharmaceutically acceptable salt thereof: , wherein ring A is a heterocyclic ring, ring B is a carbocyclic ring, a heterocyclic ring etc., G1, G2, G3, G4 and G5 are CH or N, X is -NH-, -O-, -CH2-, etc., Y is - CH2-,-CO-,-SO2- etc., Z is a single bond, -CO-, -SO2-, -NH-, -O-, -S-, -CONH-,-SO2NH-, etc., R2 is hydrogen, alkyl, alkoxy, halogen, etc., and R3 is carbocyclic group, heterocyclic group, alkyl, etc., is useful as a controlling agent of the function of CCR4 useful for the treatment or therapy for bronchial asthma, atopic dermatitis, etc.