354575-15-8

Upstream product

• 41490-13-5 4-(benzyloxy)-3,5-dichlorobenzoicacid 
• 97888-80-7 3,5-dimethyl-4-benzyloxy-benzoic acid 
• 79-37-8 oxalyl dichloride 
• 536974-83-1 4-benzyloxy-3,5-dichlorobenzoic acid methyl ester 
• 17302-82-8 ethyl 3,5-dichloro-4-hydroxybenzoate 
• 40689-39-2 ethyl 3,5-dichloro-4-(benzyloxy)benzoate 
• 3337-59-5 methyl 3,5-dichloro-4-hydroxybenzoate 
• 100-39-0 benzyl bromide 

Downstream Products

• 27163-99-1 1-(4-Benzyloxy-3,5-dichloro-phenyl)-2-diazo-ethanone 
• 888731-52-0 (4-benzyloxy-3,5-dichlorophenyl)-(2,3-dihydrobenzo[1,4]thiazin-4-yl)-methanone 
• 888731-77-9 (4-benzyloxy-3,5-dichlorophenyl)-(3,4-dihydro-2H-quinoxalin-1-yl)-methanone 
• 888731-62-2 4-benzyloxy-3,5-dichloro-N-(5-diethylsulfamoyl-2-hydroxyphenyl)-benzamide 
• 888731-70-2 4-benzyloxy-3,5-dichloro-N-[2-hydroxy-5-(pyrrolidine-1-sulfonyl)phenyl]benzamide 
• 888731-94-0 (4-benzyloxy-3,5-dichlorophenyl)-[8-(tert-butyldimethylsilyloxy)-2,3-dihydrobenzo[1,4]oxazin-4-yl]-methanone 
• 888731-97-3 4-benzyloxy-N-{2-[3-(tert-butyldimethylsilyloxy)propoxy]phenyl}-3,5-dichlorobenzamide 
• 888731-81-5 (4-benzyloxy-3,5-dichlorophenyl)-(5-nitro-2,3-dihydroindol-1-yl)-methanone 
• 1272528-06-9 methyl 4-(4-(benzyloxy)-3,5-dichlorobenzamido)benzoate 

Relevant academic research and scientific papers

Design and synthesis of a potent, highly selective, orally bioavailable, retinoic acid receptor alpha agonist

A ligand-based virtual screening exercise examining likely bioactive conformations of AM 580 (2) and AGN 193836 (3) was used to identify the novel, less lipophilic RARα agonist 4-(3,5-dichloro-4-ethoxybenzamido)benzoic acid 5, which has good selectivity over the RARβ and RARγ receptors. Analysis of the medicinal chemistry parameters of the 3,5-substituents of derivatives of template 5 enabled us to design a class of drug-like molecules with lower intrinsic clearance and higher oral bioavailability which led to the novel RARα agonist 4-(3-chloro-4-ethoxy-5-isopropoxybenzamido)-2-methylbenzoic acid 56 that has high RARα potency and excellent selectivity versus RARβ (2 orders of magnitude) and RARγ (4 orders of magnitude) at both the human and mouse RAR receptors with improved drug-like properties. This RARα specific agonist 56 has high oral bioavailability (>80%) in both mice and dogs with a good PK profile and was shown to be inactive in cytotoxicity and genotoxicity screens.

A concise [C+NC+CC] coupling-enabled synthesis of kaitocephalin

A 15-step synthesis of the iGluR antagonist kaitocephalin from aspartic acid is reported. The linchpin pyrrolidine ring of the target molecule is efficiently assembled with in a single operation via an asymmetric [C+NC+CC] reaction.

Pharmaceutical Compositions Comprising Nitrogen-Containing Fused Ring Coumpounds

[Problems] The present invention provides pharmaceutical composition which is effective for the prophylaxis or treatment of pathology showing involvement of uric acid (hyperuricemia, gouty tophus, acute gout arthritis, chronic gout arthritis, gouty kidney, urolithiasis, renal function disorder, coronary arterial disease, ischemic heart disease and the like) and the like, and is superior in the time-course stability and dissolution property (disintegration property). [Solving Means] The pharmaceutical composition of the present invention is a pharmaceutical composition comprising a nitrogen-containing fused ring compound represented by the following formula [1] or a pharmaceutically acceptable salt thereof, and one or more pharmaceutically acceptable additives, wherein the nitrogen-containing fused ring compound or a pharmaceutically acceptable salt thereof is not in contact with a basic additive: wherein each symbol is as described in the specification.

Production Method of Nitrogen-Containing Fused Ring Compounds

[Problems] The present invention provides a superior production method and a superior purification method of compounds effective for the treatment or prophylaxis of pathology showing involvement of uric acid, such as hyperuricemia, gouty tophus, acute gouty arthritis, chronic gouty arthritis, gouty kidney, urolithiasis, renal function disorder, coronary artery disease, ischemic heart disease and the like. [Means] A compound represented by the following formula [2] or a pharmaceutically acceptable salt thereof can be produced by reacting a compound represented by the following formula [3] or a salt thereof with a compound represented by the following formula [4], a salt thereof or a reactive derivative thereof. Moreover, crystallization of a compound represented by the formula [2] can be performed with industrially superior workability, and high quality crystals of a compound represented by the formula [2] can be obtained. wherein each symbol is as defined in the description.

Nitrogen-containing fused ring compounds and use thereof

A URAT1 activity inhibitor containing a nitrogen-containing fused ring compound represented by the following formula [1]: wherein each symbol is as defined in the description. The present invention is useful for the prophylaxis or treatment of pathology showing involvement of uric acid, such as hyperuricemia, gouty tophus, acute gouty arthritis, chronic gouty arthritis, gouty kidney, urolithiasis, renal function disorder, coronary artery disease, ischemic heart disease and the like.

PREVENTIVES/REMEDIES FOR POSTOPERATIVE STRESS

The present invention provides pharmaceutical composition for prophylaxis or/and therapy of a postoperative stress, which comprises a CRF antagonist.