937057-48-2

Upstream product

• 696-59-3 cis,trans-2,5-dimethoxytetrahydrofuran 
• 152911-43-8 (2-amino-5-chlorophenyl)(2,3-dimethoxyphenyl)methanone 

Downstream Products

• 937057-49-3 1-[4-chloro-2-(2,3-dimethoxybenzoyl)phenyl]-1H-pyrrole-2-carbaldehyde 
• 937057-50-6 1-(4-chloro-2-(2,3-dimethoxybenzoyl)phenyl)-1H-pyrrolo-3-carbaldehyde 
• 937057-99-3 2-(1-{2-[(4R,6S)-8-chloro-6-(2,3-dimethoxyphenyl)-4H,6H-pyrrolo[1,2-a][4,1]benzoxazepin-4-yl]ethyl}-1H-pyrazol-5-yl)acetonitrile 
• 937055-79-3 2-(1-{2-[(4R,6S)-8-chloro-6-(2,3-dimethoxyphenyl)-4H,6H-pyrrolo[1,2-a][4,1]benzoxazepin-4-yl]ethyl}-1H-pyrazol-5-yl)acetic acid 
• 937060-68-9 ethyl 1-{2-[(4R,6S)-8-chloro-6-(2,3-dimethoxyphenyl)-4H,6H-pyrrolo[1,2-a][4,1]benzoxazepin-4-yl]ethyl}-1H-pyrazole-4-carboxylate 
• 937060-70-3 1-{2-[(4R,6S)-8-chloro-6-(2,3-dimethoxyphenyl)-4H,6H-pyrrolo[1,2-a][4,1]benzoxazepin-4-yl]ethyl}-1H-pyrazole-4-carboxylic acid 
• 937063-56-4 (1-{2-[(4R,6S)-8-chloro-6-(2,3-dimethoxyphenyl)-4H,6H-pyrrolo[1,2-a][4,1]benzoxazepin-4-yl]ethyl}-1H-pyrazol-4-yl)methanol 
• 937063-57-5 2-(1-{2-[(4R,6S)-8-chloro-6-(2,3-dimethoxyphenyl)-4H,6H-pyrrolo[1,2-a][4,1]benzoxazepin-4-yl]ethyl}-1H-pyrazol-4-yl)acetonitrile 
• 937060-69-0 2-(1-{2-[(4R,6S)-8-chloro-6-(2,3-dimethoxyphenyl)-4H,6H-pyrrolo[1,2-a][4,1]benzoxazepin-4-yl]ethyl}-1H-pyrazol-4-yl)acetic acid 
• 937055-60-2 ethyl 1-{2-[(4R,6S)-8-chloro-6-(2,3-dimethoxyphenyl)-4H,6H-pyrrolo[1,2-a][4,1]benzoxazepin-4-yl]ethyl}-1H-1,2,3,4-tetrazole-5-carboxylate 
• 937055-59-9 ethyl 2-{2-[(4R,6S)-8-chloro-6-(2,3-dimethoxyphenyl)-4H,6H-pyrrolo[1,2-a][4,1]benzoxazepin-4-yl]ethyl}-2H-1,2,3,4-tetrazole-5-carboxylate 
• 937055-71-5 2-{2-[(4R,6S)-8-chloro-6-(2,3-dimethoxyphenyl)-4H,6H-pyrrolo[1,2-a][4,1]benzoxazepin-4-yl]ethyl}-2H-1,2,3,4-tetrazole-5-carboxylic acid 
• 937054-67-6 methyl 2-[1,8-dichloro-6-(2,3-dimethoxyphenyl)-4H,6H-pyrrolo[1,2-a][4,1]benzoxazepin-4-yl]acetate 
• 937055-55-5 ethyl 2-(2-{2-[(4R,6S)-8-chloro-6-(2,3-dimethoxyphenyl)-4H,6H-pyrrolo[1,2-a][4,1]benzoxazepin-4-yl]ethyl}-2H-1,2,3,4-tetrazol-5-yl)acetate 

Relevant academic research and scientific papers

Discovery of novel tricyclic compounds as squalene synthase inhibitors

In the present article, we have reported the design, synthesis, and identification of highly potent benzhydrol derivatives as squalene synthase inhibitors (compound 1). Unfortunately, the in vivo efficacies of the compounds were not enough for acquiring the clinical candidate. We continued our investigation to obtain a more in vivo efficacious template than the benzhydrol template. In our effort, we focused on a benzoxazepine ring and designed a new tricyclic scaffold by the incorporation of heterocycle into it. Prepared pyrrolobenzoxazepine derivatives showed further efficient in vitro and in vivo activities.

TRICYCLIC COMPOUND

The present invention relates to tricyclic compounds each represented by the following formula (I): (wherein, R1, R2, R2', R3, R4, X, Y and Z have the same meanings as defined in the specification); and a drug containing the compound. Since the compounds according to the present invention exhibit an excellent squalene synthetase inhibitory effect and cholesterol synthesis inhibitory effect so that they are useful as a drug such as preventive and/or remedy for diseases in mammals including humans such as hyperlipemia, e.g., hypercholesterolemia, hypertriglyceridemia, and low HDL cholesterolemia and/or arteriosclerosis.