923359-38-0

Basic information

• Product Name: SAR407899
• Synonyms: 6-(piperidin-4-yloxy)isoquinolin-1(2H)-one;-6-(piperidin-4-yloxy)-2H-isoquinolin-1-one;SAR407899 free base
• CAS NO: 923359-38-0
• Molecular Formula: C₁₄H₁₆N₂O₂
• Molecular Weight: 244.28904
• Mol File: 923359-38-0.mol
• Article Data: 3

Chemical Properties

• Boiling Point: 517.8±50.0 °C(Predicted)
• Appearance: /
• Density: 1.193±0.06 g/cm3(Predicted)
• PKA: 12.79±0.20(Predicted)
• CAS DataBase Reference: SAR407899(CAS DataBase Reference)
• NIST Chemistry Reference: SAR407899(923359-38-0)
• EPA Substance Registry System: SAR407899(923359-38-0)

Safety Data

• Hazardous Substances Data: 923359-38-0(Hazardous Substances Data)

Usage

General Description

SAR407899 is a chemical compound that belongs to the category of adenosine A2a receptor antagonists, which are commonly used in the treatment of Parkinson's disease. It acts by inhibiting the activity of the adenosine A2a receptor, which plays a role in the regulation of dopamine release in the brain. By blocking this receptor, SAR407899 helps to restore the balance of dopamine levels in the brain, which can alleviate some of the symptoms associated with Parkinson's disease, such as tremors and muscle rigidity. Research has shown that SAR407899 may have potential as a therapeutic agent for the management of Parkinson's disease and other related neurological disorders. However, further studies are needed to fully understand its effectiveness and safety profile.

Upstream product

• 252061-78-2 6-hydroxyisoquinolin-1(2H)-one 
• 591-31-1 3-methoxy-benzaldehyde 
• 24186-48-9 1-((E)-2-Isocyanato-vinyl)-3-methoxy-benzene 
• 15854-56-5 3-methoxy-cinnamic acid methyl ester 
• 6099-04-3 3-methoxycinnamic acid 
• 26829-43-6 6-methoxy-2H-isoquinolin-1-one 

Relevant articles and documents

Optimisation of 6-substituted isoquinolin-1-amine based ROCK-I inhibitors

Rho kinase is an important target implicated in a variety of cardiovascular diseases. Herein, we report the optimisation of the fragment derived ATP-competitive ROCK inhibitors 1 and 2 into lead compound 14A. The initial goal of improving ROCK-I potency relative to 1, whilst maintaining a good PK profile, was achieved through removal of the aminoisoquinoline basic centre. Lead 14A was equipotent against both ROCK-I and ROCK-II, showed good in vivo efficacy in the spontaneous hypertensive rat model, and was further optimised to demonstrate the scope for improving selectivity over PKA versus hydroxy Fasudil 3.

ISOQUINOLINE DERIVATIVES

The invention relates to isoquinoline derivatives having the general Formula (I) wherein X is O, S or NH; Y is OH or NH2; m is 0, 1 or 2; n is 1 or 2; R1 is H, when Y is NH2; or R1 is H, (C1-4)alkyl or halogen, when Y is OH; R2 and R3 are independently H, (C1-4)alkyl or halogen; R is H or (C1-6)alkyl, optionally substituted with OH, (C1-4)- alkyloxy, (C1-4)alkyloxycarbonyl, (C3-7)cycloalkyl, which may optionally comprise a heteroatom selected from O and S, (C6-10)aryl, (C6-10)aryloxy or a 5- or 6-membered heteroaryl group comprising 1-3 heteroatoms independently selected from O, N and S, each aryl or heteroaryl group being optionally substituted with 1-3 substituents independently selected from (C1-4)alkyl, (C1-4)alkyloxy, (C1-4)alkylsulfonyl and halogen; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same as well as to the use of the isoquinoline derivatives in the treatment of ROCK-I related disorders such as hypertension, atherosclerosis and glaucoma.