409127-35-1

Upstream product

• 67-56-1 methanol 
• 155891-93-3 (3,5-Dichloro-4-hydroxy-phenyl)-carbamic acid tert-butyl ester 
• 201230-82-2 carbon monoxide 
• 68-12-2 N,N-dimethyl-formamide 
• 1940-29-0 4-bromo-3,5-dichloroaniline 
• 626-43-7 3,5-Dichloroaniline 
• 1098619-84-1 trifluoro-methanesulfonic acid 4-tert-butoxycarbonylamino-2,6-dichloro-phenyl ester 
• 124-38-9 carbon dioxide 
• 5930-28-9 4-amino-2,6-dichlorophenol 
• 24424-99-5 di-tert-butyl dicarbonate 
• 264272-64-2 2,6-dichlorobenzene-1,4-dicarboxylic acid,1-methyl ester 

Downstream Products

• 409127-36-2 2,6-dichloro-4-[bis(methanesulfonyl)amino] benzoic acid methylester 
• 1258298-01-9 2,6-dichloro-4-iodo-benzoic acid 
• 1258298-16-6 2,6-dichloro-4-iodo-benzoyl chloride 
• 1426833-40-0 2,6-dichloro-4-iodo-benzoic acid N'-(2-methyl-pyrido[2,3-b]pyrazin-3-yl)-hydrazide 
• 1426833-14-8 1-(2,6-dichloro-4-iodo-phenyl)-4-methyl-2,3,5,9,9b-pentaazacyclopenta[a]naphthalene 
• 1258298-20-2 2,6-dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)-4-formylbenzamide 
• 1258298-19-9 2,6-dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)-4-vinylbenzamide 
• 1258298-18-8 N-(2-bromopyridin-4-yl)-2,6-dichloro-4-vinylbenzamide 
• 1258293-59-2 2,6-dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)-4-(hydroxymethyl)benzamide 
• 1258298-17-7 N-(2-bromopyridin-4-yl)-2,6-dichloro-4-iodobenzamide 
• 1258295-54-3 2,6-dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)-4-(methylsulfonamido)benzamide 
• 1258295-53-2 4-acetamido-2,6-dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide 
• 1258295-55-4 2,6-dichloro-4-(cyclopropanecarboxamido)-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide 
• 1258295-50-9 4-amino-2,6-dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide 

Relevant academic research and scientific papers

Identification of an imidazopyridine scaffold to generate potent and selective TYK2 inhibitors that demonstrate activity in an in vivo psoriasis model

Herein we report identification of an imidazopyridine class of potent and selective TYK2 inhibitors, exemplified by prototype 6, through constraint of the rotatable amide bond connecting the pyridine and aryl rings of compound 1. Further optimization led to generation of compound 30 that potently inhibits the TYK2 enzyme and the IL-23 pathway in cells, exhibits selectivity against cellular JAK2 activity, and has good pharmacokinetic properties. In mice, compound 30 demonstrated dose-dependent reduction of IL-17 production in a PK/PD model as well as in an imiquimod-induced psoriasis model. In this efficacy model, the IL-17 decrease was accompanied by a reduction of ear thickness indicating the potential of TYK2 inhibition as a therapeutic approach for psoriasis patients.

FACTOR IXA INHIBITORS

The present invention provides a compound of Formula I, and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing unstable angina, refractory angina, myocardial infarction, trans

Lead optimization of a 4-aminopyridine benzamide scaffold to identify potent, selective, and orally bioavailable TYK2 inhibitors

Herein we report our lead optimization effort to identify potent, selective, and orally bioavailable TYK2 inhibitors, starting with lead molecule 3. We used structure-based design to discover 2,6-dichloro-4-cyanophenyl and (1R,2R)-2-fluorocyclopropylamide modifications, each of which exhibited improved TYK2 potency and JAK1 and JAK2 selectivity relative to 3. Further optimization eventually led to compound 37 that showed good TYK2 enzyme and interleukin-12 (IL-12) cell potency, as well as acceptable cellular JAK1 and JAK2 selectivity and excellent oral exposure in mice. When tested in a mouse IL-12 PK/PD model, compound 37 showed statistically significant knockdown of cytokine interferon-γ (IFNγ), suggesting that selective inhibition of TYK2 kinase activity might be sufficient to block the IL-12 pathway in vivo.

PYRIDINE COMPOUNDS AND USES THEREOF

The present invention is directed to pyridine compounds of Formula (I). Separate aspects of the invention are directed to pharmaceutical compositions comprising said compounds and uses of the compounds as therapeutic agents treating neurological and psych

IMIDAZOPYRIDINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE

The invention provides compounds of Formulas Ia-Ib, stereoisomers or pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R4, R5 and R16 are defined herein, a pharmaceutical composition that includes a compound of Formulas Ia-Ib and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of using the compound or composition in therapy.

Antagonists for treatment of CD/11CD18 adhesion receptor mediated disorders

Compounds of the general structure D-L-B-(AA), for example (A), that are useful for treating Mac-1 or LFA-1-mediated disorders such as inflammatory disorders, allergies, and autoimmune diseases are provided.

New phenylalanine derivatives

Specific phenylalanine derivatives or pharmaceutically acceptable. salts thereof have an antagonistic effect on the α4 integrins and, therefore, are usable as therapeutic agents or preventive agents for diseases in which α4 integrin-depending adhesion process participates in the pathology, such as inflammatory diseases, rheumatoid arthritis, inflammatory bowel diseases, systemic lupus erythematosus, multiple sclerosis, Sj?gren's syndrome, asthma, psoriasis, allergy, diabetes, cardiovascular diseases, arterial sclerosis, restenosis, tumor proliferation, tumor metastasis and transplantation rejection.