183180-53-2

Upstream product

• 38411-41-5 (3-nitrophenyl)acetyl chloride 
• 591-19-5 m-Bromoaniline 
• 161608-46-4 3-amino-1-ethoxycarbonylmethyl-5-phenyl-2,3-dihydro-1H-1-benzazepin-2-one 
• 1877-73-2 3-nitro-benzeneacetic acid 
• 180150-74-7 3-nitrophenylacetic acid t-butyl ester 

Downstream Products

• 847834-87-1 3-nitrosophenylacetic acid tert-butyl ester 
• 183175-93-1 tert-Butyl 2-[3-[3-[N-[3-[N-ethyl-N-(3,5-dimethylphenyl)carbamoylmethyloxy]phenyl]-N-(N-methyl-N-phenylcarbamoylmethyl)carbamoylmethyl]ureido]phenyl] acetate 

Relevant academic research and scientific papers

Photocontrolled DNA minor groove interactions of imidazole/pyrrole polyamides

Azobenzenes are photoswitchable molecules capable of generating significant structural changes upon E-to-Z photoisomerization in peptides or small molecules, thereby controlling geometry and functionality. E-to-Z photoisomerization usually is achieved upo

COMPOUND, CURED PRODUCT, POLYMER, PHOTO-ALIGNMENT FILM, OPTICALLY ANISOTROPIC BODY AND LIQUID CRYSTAL DISPLAY ELEMENT

A compound and a polymer which can each form a photo-alignment film having excellent ability of controlling alignment, a photo-alignment film obtained using the polymer and an optically anisotropic body and a liquid crystal display element each having the photo-alignment film are provided. A compound represented by the general formula (1). In the formula, P represents a polymerizable group, Z and Z1 represent divalent linking groups, A and A1 represent divalent cyclic groups, and X1 to X5 each independently represent a hydrogen atom, a fluorine atom, a chlorine atom, a hydroxy group, a nitro group, a cyano group or an alkyl group having 1 to 40 carbon atoms which may have a substituent, provided that X1, X2, X4 and X5 are not simultaneously hydrogen atoms.

SYMMETRICAL TRIS-ARYL-AMIDE DERIVATIVES AND THEIR USE AS ANTI-HEPARANASE

The present invention relates to tris-aryl-amide derivatives having an anti-heparanase activity, in particular it relates to ureido/thioureido/ether tris-aryl-amide derivatives of formula The invention also relates to the use of such compounds as a medica

Palladium-catalyzed α-arylation of zinc enolates of esters: Reaction conditions and substrate scope

The intermolecular α-arylation of esters by palladium-catalyzed coupling of aryl bromides with zinc enolates of esters is reported. Reactions of three different types of zinc enolates have been developed. α-Arylation of esters occurs in high yields with i

Aminophenol derivatives

Aminophenol derivatives represented by the following formula (1): STR1 wherein X is O or S; A is alkylene, R 1 is phenyl, etc., R 2 and R 3 are H or alkyl; R 4 is substituted carbamoylalkyl, etc.; R 5 is substituted amino, etc.; their salts, and optical i

N-phenylamidines as selective inhibitors of human neuronal nitric oxide synthase: Structure-activity studies and demonstration of in vivo activity

Selective inhibition of the neuronal isoform of nitric oxide synthase (NOS) compared to the endothelial and inducible isoforms may be required for treatment of neurological disorders caused by excessive production of nitric oxide. Recently, we described N-(3-(aminomethyl)benzyl)acetamidine (13) as a slow, tight-binding inhibitor, highly selective for human inducible nitric oxide synthase (iNOS). Removal of a single methylene bridge between the amidine nitrogen and phenyl ring to give N-(3- (aminomethyl)phenyl)acetamidine (14) dramatically altered the selectivity to give a neuronal selective nitric oxide synthase (nNOS) inhibitor. Part of this large shift in selectivity was due to 14 being a rapidly reversible inhibitor of iNOS in contrast to the essentially irreversible inhibition of iNOS observed with 13. Structure-activity studies revealed that a basic amine functionality tethered to an aromatic ring and a sterically compact amidine are key pharmacophores for this class of NOS inhibitors. Maximal nNOS inhibition potency was achieved with N-(3-(aminomethyl)phenyl)-2- furanylamidine (77) (K(i-nNOS) = 0.006 μM; K(i-eNOS) = 0.35 μM; K(i-iNOS) = 0.16 μM). Finally, α-fluoro-N-(3-(aminomethyl)phenyl)acetamidine (74) (K(i- nNOS) = 0.011 μM; K(i-eNOS) = 1.1 μM; K(i-iNOS) = 0.48 μM) had excellent brain penetration and inhibited nNOS in a rat brain slice assay as well as in the rat brain (cerebellum) in vivo. Thus, N-phenylamidines should be useful in validating the role of nNOS in neurological disorders.

3-AMINOAZEPINE COMPOUND AND PHARMACEUTICAL USE THEREOF

A 3-aminoazepine compound represented by general formula (I), an optically active isomer thereof, or a pharmaceutically acceptable salt thereof, wherein Ar represents phenyl, etc.; R1 represents hydrogen, alkyl, etc.; R2 and R3 represent each independently hydrogen, alkyl,-CO-R? (wherein R? represents heteroaryl, etc.),-CONH-R? (wherein R? represents phenyl, etc.), etc.; R? represents hydrogen, alkyl, etc.; X represents oxygen or sulfur, provided R? and X may be combined together to form-C(R1?)=N-N= (wherein R1? represents hydrogen, alkyl, etc.). This compound has CCK and gastrin antagonisms and is useful as a remedy for central nervous system diseases such as anxiety and depression and as a preventive or a remedy for pancreatic diseases and gastrointestinal ulcer.