515143-79-0

Upstream product

• 104901-43-1 methyl 3-bromo-4-methylbenzoate 
• 515140-22-4 C₁₃H₁₇BrN₂O₃ 

Downstream Products

• 944535-04-0 C₁₂H₁₃BrN₂O 
• 148672-45-1 C₁₀H₉BrN₂O 
• 944680-70-0 C₁₁H₁₁BrN₂O 
• 1257543-33-1 C₁₀H₁₀BrClN₂O₂ 
• 1373940-07-8 5-(3-(5-aminopyrazin-2-yl)-4-methylphenyl)-3-methyl-1,3,4-oxadiazol-2(3H)-one 
• 1373940-06-7 5-(3-bromo-4-methylphenyl)-3-methyl-1,3,4-oxadiazol-2(3H)-one 
• 1373940-05-6 1-(5-(3-bromo-4-methylphenyl)-2,2-dimethyl-1,3,4-oxadiazol-3(2H)-yl)ethanone 
• 1373939-74-2 N-(2,6-difluorophenyl)-5-(2-methyl-5-(4-methyl-5-oxo-4,5-dihydro-1,3,4-oxadiazol-2-yl)phenyl)thiophene-2-carboxamide 
• 458526-43-7 3-bromo-4-methyl-N'-(propan-2-ylidene)benzohydrazide 
• 671794-35-7 5-(3-bromo-4-methylphenyl)-1,3,4-oxadiazol-2(3H)-one 

Relevant academic research and scientific papers

Discovery of a Novel Potent and Selective Calcium Release-Activated Calcium Channel Inhibitor: 2,6-Difluoro- N-(2′-methyl-3′-(4-methyl-5-oxo-4,5-dihydro-1,3,4-oxadiazol-2-yl)-[1,1′-biphenyl]-4-yl)benzamide. Structure-Activity Relationship and Preclinical Characterization

The role of calcium release-activated calcium (CRAC) channels is well characterized and is of particular importance in T-cell function. CRAC channels are involved in the pathogenesis of several autoimmune diseases, making it an attractive therapeutic target for treating inflammatory diseases, like rheumatoid arthritis (RA). A systematic structure-activity relationship study with the goal of optimizing lipophilicity successfully yielded two lead compounds, 36 and 37. Both compounds showed decent potency and selectivity and a remarkable pharmacokinetic profile. Further characterization in in vivo RA models and subsequent histopathological evaluation of tissues led to the identification of 36 as a clinical candidate. Compound 36 displayed an excellent safety profile and had a sufficient safety margin to qualify it for use in human testing. Oral administration of 36 in Phase 1 clinical study in healthy volunteers established favorable safety, tolerability, and good target engagement as measured by levels of IL-2 and TNF-α.

OXAZOLE AND ISOXAZOLE CRAC MODULATORS

The present invention relates to compounds of Formula (I) along with processes for their preparation that are useful for treating, preventing and/or managing the diseases, disorders, syndromes or conditions associated with the modulation of CRAC. The invention further relates to methods of treating, preventing managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of CRAC of Formula (I).

AZOLE DERIVATIVES AS WTN PATHWAY INHIBITORS

The present invention relates to new compounds of formula I, to processes for their preparation, to pharmaceutical formulations containing such compounds and to their use in therapy. Such compounds find particular use in the treatment and/or prevention of conditions or diseases which are affected by over-activation of signaling in the Wnt pathway. For example, these may be used in preventing and/or retarding proliferation of tumor cells, for example carcinomas such as colon carcinomas.

Biphenyl amide p38 kinase inhibitors 2: Optimisation and SAR

The biphenyl amides are a novel series of p38 MAP kinase inhibitors. Structure-activity relationships of the series against p38α are discussed with reference to the X-ray crystal structure of an example. The series was optimised rapidly to a compound showing oral activity in an in vivo disease model.