209959-26-2

Upstream product

• 209959-25-1 tert-butyl 4-(4-nitrophenyl)-1H-pyrazole-1-carboxylate 
• 552846-17-0 tert-butyl 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyrazole-1-carboxylate 
• 321-23-3 4-bromo-2-fluoronitrobenzene 
• 24424-99-5 di-tert-butyl dicarbonate 
• 114474-26-9 4-(4-nitrophenyl)-1H-pyrazole 
• 586-78-7 para-nitrophenyl bromide 

Downstream Products

• 1610874-68-4 N-(4-(1H-pyrazol-4-yl)phenyl)-3-(2-chlorophenyl)propanamide 
• 1610875-33-6 tert-butyl 4-(4-(3-(2-chlorophenyl)propanamido)phenyl)-1H-pyrazole-1-carboxylate 

Relevant academic research and scientific papers

ROCK INHIBITOR, AND PREPARATION METHOD THEREFOR AND USE THEREOF

The invention relates to a ROCK inhibitor represented by formula (I), its preparation method and its use. The ROCK inhibitor has excellent ROCK inhibition activity, in particular good selective inhibition on ROCK2 kinase, has good safety and metabolic stability, and has high bioavailability. The process of preparing the ROCK inhibitor is simple, and the ROCK inhibitor is easy to purify, and therefore offers good prospects for application.

CYCLIN-DEPENDENT KINASE INHIBITORS

Described herein are compounds and their pharmaceutically acceptable salts, pharmaceutical compositions thereof, methods of treatment, and medical uses. The compounds described herein are modulators of cyclin-dependent kinases, and are useful in the treatment or alleviation of protein kinase associated disorders, including cancer, infectious diseases, autoimmune diseases, or cardiovascular diseases.

CYCLIN-DEPENDENT KINASE INHIBITORS

Described herein are compounds and their pharmaceutically acceptable salts, pharmaceutical compositions thereof, methods of treatment, and medical uses. The compounds described herein are modulators of cyclin-dependent kinases, and are useful in the treatment or alleviation of protein kinase associated disorders, including cancer, infectious diseases, autoimmune diseases, or cardiovascular diseases.

CYCLIN-DEPENDENT KINASE INHIBITORS

Described herein are compounds and their pharmaceutically acceptable salts, pharmaceutical compositions thereof, methods of treatment, and medical uses. The compounds described herein are modulators of cyclin-dependent kinases, and are useful in the treatment or alleviation of protein kinase associated disorders, including cancer, infectious diseases, autoimmune diseases, or cardiovascular diseases.

RHO-ASSOCIATED PROTEIN KINASE INHIBITOR, PHARMACEUTICAL COMPOSITION COMPRISING THE SAME, AS WELL AS PREPARATION METHOD AND USE THEREOF

The present invention relates to a Rho-associated protein kinase inhibitor of Formula (I), a pharmaceutical composition comprising the same, a preparation method thereof, and use thereof for the prevention or treatment of a disease mediated by the Rho-associated protein kinase (ROCK).

RHO-ASSOCIATED PROTEIN KINASE INHIBITOR, PHARMACEUTICAL COMPOSITION COMPRISING THE SAME, AS WELL AS PREPARATION METHOD AND USE THEREOF

The present invention relates to a Rho-associated protein kinase inhibitor of Formula (I), a pharmaceutical composition comprising the same, a preparation method thereof, and use thereof for the prevention or treatment of a disease mediated by the Rho-associated protein kinase (ROCK).

LACTAMS AS INHIBITORS OF ROCK

The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.

Discovery of lipoic acid-4-phenyl-1: H -pyrazole hybrids as novel bifunctional ROCK inhibitors with antioxidant activity

A series of lipoic acid (LA) and 4-phenyl-1H-pyrazole hybrids as bifunctional Rho-associated kinase (ROCK) inhibitors were designed, synthesized and evaluated. Compound 15 is identified to be a novel potent bifunctional ROCK inhibitor with antioxidant activity and neuroprotection.

Compounds for treating degenerative disease of central nervous system and application of compounds

The invention relates to compounds for treating degenerative disease of a central nervous system, pharmaceutical composition and an application of the compounds. The compounds have a structure shown in a formula (I) and can be used as a ROCK inhibitor, and appropriate pharmaceutical dosage forms prepared from the compounds are used for treating the neurodegenerative disease.

PHENYLPYRAZOLE DERIVATIVES AS POTENT ROCK1 AND ROCK2 INHIBITORS

The present invention provides compounds of Formula (I): (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.