485841-47-2

Upstream product

• 220000-87-3 4-chloro-N-methylpicolinamide 
• 610-81-1 4-hydroxy-2-nitroaniline 
• 485841-45-0 4-(4-amino-3-nitro-phenoxy)-pyridine-2-carboxylic acid methylamide 
• 485841-46-1 4-(4-methylamino-3-nitrophenoxy)-pyridine-2-carboxylic acid methylamide 

Downstream Products

• 611213-97-9 4-({1-methyl-5-[2-(N-methylcarbamoyl)(4-pyridyloxy)]benzimidazol-2-yl}amino)benzoic acid 
• 611224-74-9 4-[2-(4-bromophenyl)-1-methyl-1H-benzimidazol-5-yloxy]-pyridine-2-carboxylic acid methylamide, trifluoroacetic acid salt 
• 611214-71-2 3-{[1-methyl-5-({2-[(methylamino)carbonyl]pyridin-4-yl}-oxy)-1H-benzimidazol-2-yl]amino}benzoic acid 
• 611225-83-3 [4-(2-{[4-(chloromethyl)phenyl]carbonylamino}-1-methylbenzimidazol-5-yloxy)(2-pyridyl)]-N-methylcarboxamide 
• 611220-19-0 (4-{2-[(4-bromophenyl)methyl]-1-methylbenzimidazol-5-yloxy}-(2-pyridyl))-N-methylcarboxamide 
• 611214-99-4 4-{[2-({4-[(4-ethylpiperazin-1-yl)methyl]phenyl}amino)-1-methyl-1H-benzimidazol-5-yl]oxy}-N-methylpyridine-2-carboxamide 
• 611220-10-1 [4-(2-{[4-(4-ethylpiperazin-1-yl)phenyl]amino}-1-methyl-benzimidazol-5-yloxy)(2-pyridyl)]-N-methylcarboxamide 
• 611220-12-3 N-methyl [4-(1-methyl-2-{[4-(2-morpholin-4-ylethyl)phenyl]-amino}-benzimidazol-5-oxy)(2-pyridyl)]carboxamide 
• 611215-13-5 N-methyl-4-({1-methyl-2-[(4-{1-[(phenylmethyl)amino]ethyl}phenyl)amino]-1H-benzimidazol-5-yl}oxy)pyridine-2-carboxamide 
• 611226-08-5 4-({2-[(3-bromo-4-chlorophenyl)amino]-1-methyl-1H-benzirnidazol-5-yl}oxy)-N-methylpyridine-2-carboxamide 
• 611224-71-6 4-[1-Methyl-2-(3-phenoxy-phenylamino)-1H-benzoimidazol-5-yloxy]-pyridine-2-carboxylic acid methylamide 
• 710351-69-2 N-methyl-4-({1-methyl-2-[(4-methyl-3-pyrrolidin-1-ylphenyl)-amino]-1H-benzimidazol-5-yl}oxy)pyridine-2-carboxamide 
• 710351-80-7 N-methyl-4-[(1-methyl-2-{[3-(2-pyrrolidin-1-ylethyl)phenyl]amino}-1H-benzimidazol-5-yl)oxy]pyridine-2-carboxamide 
• 611215-30-6 4-[(2-{[3-(1,1-dimethylethyl)phenyl]amino}-1-methyl-1H-benzimidazol-5-yl)oxy]-N-methylpyridine-2-carboxamide 

Relevant academic research and scientific papers

Design and synthesis of orally bioavailable benzimidazoles as raf kinase inhibitors

A series of arylaminobenzimidazoles was designed and synthesized as Raf kinase inhibitors. Exploration of the structure-activity relationship resulted in compounds that are potent in vitro and show desirable in vivo properties.

Design, synthesis, and evaluation of orally active benzimidazoles and benzoxazoles as vascular endothelial growth factor-2 receptor tyrosine kinase inhibitors

Inhibition of the VEGF signaling pathway has become a valuable approach in the treatment of cancers. Guided by X-ray crystallography and molecular modeling, a series of 2-aminobenzimidazoles and 2-aminobenzoxazoles were identified as potent inhibitors of VEGFR-2 (KDR) in both enzymatic and HUVEC cellular proliferation assays. In this report we describe the synthesis and structure-activity relationship of a series of 2-aminobenzimidazoles and benzoxazoles, culminating in the identification of benzoxazole 22 as a potent and selective VEGFR-2 inhibitor displaying a good pharmacokinetic profile. Compound 22 demonstrated efficacy in both the murine matrigel model for vascular permeability (79% inhibition observed at 100 mg/kg) and the rat corneal angiogenesis model (ED50 = 16.3 mg/kg).

Substituted benzazoles and methods of their use as inhibitors of Raf kinase

New substituted benz-azole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.