17607-79-3

Upstream product

• 100-39-0 benzyl bromide 
• 4027-57-0 ethyl 5-methyl-2H-pyrazole-3-carboxylate 
• 100-44-7 benzyl chloride 
• 615-79-2 ethyl 2,4-diketopentanoate 
• 555-96-4 Benzylhydrazine 
• 20570-96-1 benzylhydrazine dihydrochloride 

Downstream Products

• 1608125-57-0 1-benzyl-3-methyl-5-((3-methyl-1-phenyl-1H-pyrazol-5-yloxy)methyl)-1H-pyrazole 
• 916737-67-2 C₁₉H₂₀N₂O₃S 
• 916737-66-1 4-[(1-benzyl-3-methylpyrazol-5-yl)methyleneoxy]nitrobenzene 
• 174180-85-9 (1-benzyl-3-methyl-1H-pyrazol-5-yl)methanol 
• 17607-80-6 1-benzyl-5-methyl-1H-pyrazole-3-carboxylic acid 
• 1141-70-4 1-benzyl-3-methyl-1H-pyrazole-5-carboxylic acid 

Relevant academic research and scientific papers

Structure-activity relationships of pyrazole derivatives as potential therapeutics for immune thrombocytopenias

Idiopathic or immune thrombocytopenia (ITP) is a serious clinical disorder involving the destruction of platelets by macrophages. Small molecule therapeutics are highly sought after to ease the burden on current therapies derived from human sources. Earlier, we discovered that dimers of five-membered heterocycles exhibited potential to inhibit phagocytosis of human RBCs by macrophages. Here, we reveal a structure-activity relationship of the bis-pyrazole class of molecules with -C-C-, -C-N- and -C-O- linkers, and their evaluation as inhibitors of phagocytosis of antibody-opsonized human RBCs as potential therapeutics for ITP. We have uncovered three potential candidates, 37, 47 and 50, all carrying a different linker connecting the two pyrazole moieties. Among these compounds, hydroxypyrazole derivative 50 is the most potent compound with an IC50 of 14 ± 9 μM for inhibiting the phagocytosis of antibody-opsonized human RBCs by macrophages. None of the compounds exhibited significant potential to induce apoptosis in peripheral blood mononuclear cells (PBMCs). Current study has revealed specific functional features, such as up to 2-atom spacer arm and alkyl substitution at one of the N1 positions of the bivalent pyrazole core to be important for the inhibitory activity.

PYRAZOLE DERIVATIVES AND THEIR USES THEREOF

The present disclosure relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof; wherein U, R1, R2, R3 and Q are as defined herein. The disclosure also provides a method for treating or preventing a method for the prevention, treatment and/or alleviation of one or more autoimmune or alloimmune disease, pharmaceutical compositions and combination comprising a therapeutically effective amount of a compound, as defined herein.

TRICYCLIC FUSED INDOLE DERIVATIVES AND THEIR USE AS AURORA KINASE INHIBITORS

Objects of the present invention are the compounds of formula (I) their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, pharmaceutical compositions containing them an

COMPOSITIONS AND METHODS FOR INHIBITION OF THE JAK PATHWAY

The invention encompasses compounds having formula (I-V) and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, may be therapeutically useful.

Pyrazolecarboxamide human neuropeptide Y5 receptor ligands with in vivo antifeedant activity

1-Aryl-3-carboxamido-5-alkylpyrazoles were prepared based on a hit found in high-throughput screening of our corporate compound library in an assay measuring affinity for the human neuropeptide Y5 receptor. 1-(3-Trifluoromethylphenyl)-3-[N-(5-quinolinyl)carboxamido]-5-methylpyrazole (31) bound to the human neuropeptide Y5 receptor with a 80 nM IC50and was shown to inhibit cumulative food consumption 43.2% 2-6 h after ip dosing in a fasting-induced feeding model in rats.

Orientation de la reaction d'alkylation des pyrazoles dans des conditions neutres et en catalyse par transfert de phase

The N-butylation and N-benzylation of nine pyrazoles bearing different substituents in positions 3 and 5 have been studied in neutral and basic medium (phase transfer catalysis).The orientation of the reaction depends strongly on the method used when the