33360-19-9

Upstream product

• 33360-18-8 2-phenyl-6H-oxazolo[5,4-d]pyrimidin-7-one 
• 33360-18-8 2-phenyloxazolo[5,4-d]pyrimidin-7-ol 
• 5413-85-4 5-amino-4,6-dichloropyridimine 
• 98-88-4 benzoyl chloride 
• 93-97-0 benzoic acid anhydride 
• 5098-18-0 5-amino-2-phenyl[1,3]oxazole-4-carbonitrile 
• 90840-73-6 benzoylamino-malonic acid diamide 

Downstream Products

• 33360-24-6 2-phenyl-7-piperidin-1-yl-oxazolo[5,4-d]pyrimidine 
• 33360-22-4 7-morpholin-4-yl-2-phenyl-oxazolo[5,4-d]pyrimidine 
• 33360-20-2 2-phenyl-6H,7H-[1,3]oxazolo[5,4-d]pyrimidine-7-thione 
• 33360-28-0 7-benzylsulfanyl-2-phenyl-oxazolo[5,4-d]pyrimidine 
• 33360-26-8 7-methylsulfanyl-2-phenyl-oxazolo[5,4-d]pyrimidine 

Relevant academic research and scientific papers

Development of novel oxazolo[5,4-d]pyrimidines as competitive CB2 neutral antagonists based on scaffold hopping

A series of novel oxazolo[5,4-d]pyrimidines was designed via a scaffold hopping strategy and synthesized through a newly developed approach. All these compounds were evaluated for their biological activity toward CB1/CB2 cannabinoid receptors, their metabolic stability in mice liver microsomes and their cytotoxicity against several cell lines. Eight compounds have been identified as CB2 ligands with Ki values less than 1 μM. It is noteworthy that 2-(2-chlorophenyl)-5-methyl-7-(4-methylpiperazin-1-yl) oxazolo[5,4-d]pyrimidine 47 and 2-(2-chlorophenyl)-7-(4-ethylpiperazin-1-yl)- 5-methyloxazolo[5,4-d]pyrimidine 48 showed CB2 binding affinity in the nanomolar range and significant selectivity over CB1 receptors. Interestingly, functionality studies imply that they behave as competitive neutral antagonists. Moreover, all tested compounds are devoid of cytotoxicity toward several cell lines, including Chinese hamster ovary cells (CHO) and human colorectal adenocarcinoma cells HT29.

FUSED MULTICYCLIC COMPOUNDS AS PROTEIN KINASE INHIBITORS

Fused multicyclic compounds of formula (I): wherein R′, R″, X, Y, Z, A, B, C, D, and n are defined herein. Also disclosed are a method for inhibiting protein kinase (e.g., Aurora kinase) activity and a method for treating a protein kinase mediated disorde

N-ARYL-ISOXAZOLOPYRIMIDIN-4-AMINES AND RELATED COMPOUNDS AS ACTIVATORS OF CASPASES AND INDUCERS OF APOPTOSIS AND THE USE THEREOF

Disclosed are N-aryl-isoxazolopyrimidin-4-amines and related compounds thereof, represented by the Formula (I): wherein Ar, R1-R5, A, B, D, E, F and H are defined herein. The present invention relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

Heteroaryl compounds useful as inhibitors of E1 activating enzymes

This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.

Discovery and optimization of 2-aryl oxazolo-pyrimidines as adenosine kinase inhibitors using liquid phase parallel synthesis

Adenosine kinase inhibition is an attractive therapeutic approach for several conditions for example, neurodegeneration, seizures, ischemia, inflammation and pain. Several nucleosidic and non-nucleosidic inhibitors are available. Using a virtual screening approach, we have discovered that 2-aryl oxazolo-pyrimidines are adenosine kinase inhibitors. Subsequent high throughput derivatization enabled the optimization of this new inhibitor chemotype resulting in highly potent derivatives. A variety of analogues were produced by applying liquid phase parallel synthesis to vary the 7-amino residues as well as the 2-aryl moiety.