64834-62-4

Usage

Type of compound

Ethanolamine derivative

Contains

An amino group and an alcohol group

Molecular weight

181.23 g/mol

Melting point

68-70 °C

Physical state at room temperature

Colorless to pale yellow liquid

Solubility

Soluble in water and ethanol

Uses

Intermediate or building block in the synthesis of pharmaceuticals and agrochemicals, solvent or reagent in organic synthesis.

Upstream product

• 141-43-5 ethanolamine 
• 591-31-1 3-methoxy-benzaldehyde 
• 70365-15-0 C₁₀H₁₃NO₂ 

Downstream Products

• 1219729-13-1 3-(4-bromophenyl)-1-(2-hydroxyethyl)-1-(3-methoxybenzyl)urea 
• 1219722-73-2 3-(2-(2-hydroxyethoxy)-4-(1H-pyrazol-4-yl)phenyl)-1-(2-hydroxyethyl)-1-(3-methoxybenzyl)urea 
• 1219729-18-6 C₁₉H₂₃BrN₂O₅ 
• 1219722-68-5 1-(2-hydroxyethyl)-1-(3-methoxybenzyl)-3-[4-(1H-pyrazol-4-yl)phenyl]urea 

Relevant academic research and scientific papers

Biphenyl formamide urea compound, and preparation method and application thereof

The invention belongs to the technical field of medicines, particularly relates to the field of treatment of tumor-related diseases, and relates to a biphenyl formamide urea compound, and a preparation method and application thereof. In order to solve the problem that the effect of a ROCK inhibitor in the prior art still needs to be improved, the invention provides the biphenyl formamide urea compound represented by formula (I) shown in the specification. The novel biphenyl formamide urea ROCKI inhibitor is prepared through a dominant fragment heterozygosis design strategy, so that the novel biphenyl formamide urea ROCKI inhibitor can simultaneously extend into target key binding regions (a pocket A and a pocket D) to improve the target affinity with the ROCKI inhibitor; further, the ROCK inhibition effect and the anti-tumor effect are improved.

DRUGS AND COMPOSITIONS FOR THE TREATMENT OF OCULAR DISORDERS

The present invention provides new prodrugs of therapeutically active compounds, including oligomeric prodrugs, and compositions to treat medical disorders, for example glaucoma, a disorder or abnormality related to an increase in intraocular pressure (IOP), a disorder requiring neuroprotection, age-related macular degeneration, or diabetic retinopathy.

Synthesis and biological evaluation of urea derivatives as highly potent and selective rho kinase inhibitors

RhoA and its downstream effector ROCK mediate stress fiber formation and cell contraction through their effects on the phosphorylation of myosin light chain (MLC). Inhibition of the RhoA/ROCK pathway has proven to be a promising strategy for several indications such as cardiovascular disease, glaucoma, and inflammatory disease. In 2010, our group reported urea-based ROCK inhibitors as potential antiglaucoma agents. These compounds showed potent IC50 values in enzymatic and cell-based assays and significant intraocular pressure (IOP)-lowering effects in rats (～7 mmHg).(22) To develop more advanced ROCK inhibitors targeting various potential applications (such as myocardial infarction, erectile dysfunction, multiple sclerosis, etc.) in addition to glaucoma, a thorough SAR for this urea-based scaffold was studied. The detailed optimization process, counter-screening, and in vitro and in vivo DMPK studies are discussed. Potent and selective ROCK inhibitors with various in vivo pharmacokinetic properties were discovered.