692884-29-0

Upstream product

• 692883-31-1 2-(3-(3-(piperidin-4-yl)-propoxy)-phenyl)-N-(4-pyridin-4-yl-thiazol-2-yl)-acetamide 
• 50-00-0 formaldehyd 
• 42058-59-3 3-hydroxy-benzeneacetic acid, methyl ester 
• 156185-63-6 N-Boc-piperidin-4-yl-propanol 
• 692890-07-6 methyl 3-(3-(N-Boc-piperidin-4-yl)-propoxy)-phenylacetate 
• 692890-13-4 3-(3-(N-Boc-piperidin-4-yl)-propoxy)-phenylacetic acid 
• 692891-81-9 2-(3-(3-(N-Boc-piperidin-4-yl)-propoxy)-phenyl)-N-(4-pyridin-4-yl-thiazol-2-yl)-acetamide 

Relevant academic research and scientific papers

ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups

Solubilizing groups have been frequently appended to kinase inhibitor drug molecules when solubility is insufficient for pharmaceutical development. Such groups are usually located at substitution sites that have minimal impact on target activity. In this report we describe the incorporation of solubilizing groups in a class of Rho kinase (ROCK) inhibitors that not only confer improved solubility, but also enhance target potency and selectivity against a closely related kinase, PKA.

COMPOSITIONS USEFUL AS INHIBITORS OF ROCK AND OTHER PROTEIN KINASES

The present invention relates to substitute thiazole and thiophene derivatives useful as inhibitors of rock and other protein kinaeses. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders, including proliferative, cardiac and neurodegenerative diseases.