212628-46-1

Upstream product

• 13194-68-8 4-iodo-2-methylaniline 
• 212631-85-1 3-bromo-4,5,6-trifluorobenzoic acid 

Downstream Products

• 219778-43-5 5-bromo-N-cyclohexylmethoxy-3,4-difluoro-2-(4-iodo-2-methyl-phenylamino)-benzamide 
• 219778-40-2 5-bromo-3,4-difluoro-2-(4-iodo-2-methyl-phenylamino)-N-isobutoxy-benzamide 
• 219778-52-6 5-Bromo-N-cyclobutylmethoxy-3,4-difluoro-2-(4-iodo-2-methyl-phenylamino)-benzamide 
• 219778-48-0 5-bromo-N-cyclopentylmethoxy-3,4-difluoro-2-(4-iodo-2-methyl-phenylamino)-benzamide 
• 321438-68-0 5-bromo-3,4-difluoro-2-(4-iodo-2-methyl-phenylamino)-N-methoxy-benzamide 
• 391212-08-1 5-Bromo-3,4-difluoro-2-(4-iodo-2-methyl-phenylamino)-benzoic acid pentafluorophenyl ester 

Relevant academic research and scientific papers

A simple and efficient synthesis of 2-(N-phenylamino)-benzoic acids

A new method for the synthesis of 2-(N-phenylamino)benzoic acids is presented, with 2-fluorobenzoic acids and anilines as starting materials. Several experimental conditions as well as the factors influencing the outcome of the reaction are described.

The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901

A novel series of benzhydroxamate esters derived from their precursor anthranilic acids have been prepared and have been identified as potent MEK inhibitors. 2-(2-Chloro-4-iodo-phenylamino)-N-cyclopropylmethoxy-3,4-difluoro-benzam ide, CI-1040, was the first MEK inhibitor to demonstrate in vivo activity in preclinical animal models and subsequently became the first MEK inhibitor to enter clinical trial. CI-1040 suffered however from poor exposure due to its poor solubility and rapid clearance, and as a result, development of the compound was terminated. Optimization of the diphenylamine core and modification of the hydroxamate side chain for cell potency, solubility, and exposure with oral delivery resulted in the discovery of the clinical candidate N-(2,3-dihydroxy-propoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-b enzamide PD 0325901.

Treatment of asthma with MEK inhibitors

This invention provides a method of preventing or treating asthma by administering to a patient in need of treatment an effective amount of a selective MEK inhibitor, especially a phenyl amine of Formula I and II:

Oxygenated esters of 4-lodo phenylamino benzhydroxamic acids

The present invention relates to oxygenated esters of 4-iodophenylamino benzhydroxamic acid derivatives, pharmaceutical compositions and methods of use thereof. The present invention also relates to crystaline forms of oxygenated esters of 4-iodophenylamino benzhydroxamic acid derivatives, pharmaceutical compositions and methods of use thereof.

Combination chemotherapy

Mitotic inhibitors such as paclitaxel have improved antitumor activity when used in combination with a selective MEK inhibitor, especially a phenyl amine compound of Formula I and II:

4-bromo or 4-iodo phenylamino benzhydroxamic acid derivatives and their use as MEK inhibitors

Phenylamino benzhydroxamic acid derivatives of formula (I) where R1, R2, R3, R4, R5, and R6 are hydrogen or substituent groups such as alkyl, and where R7 is hydrogen or an organic radical, are potent inhibitors of MEK and, as such, are effective in treat

2-(4-bromo or 4-iodo phenylamino) benzoic acid derivatives and their use as MEK inhibitors

Phenylamino benzoic acid, benzamides, and benzyl alcohol derivatives of the formula where R1, R2, R3, R4, R5, and R6are hydrogen or substituent groups such as alkyl, and where R7

Method of treating or preventing septic shock by administering a MEK inhibitor

The present invention provides a method for treating or preventing septic shock. Specifically, the present invention provides a method of treating or preventing septic shock by administering to a patient a MEK inhibitor.