1194450-91-3

Upstream product

• 496-15-1 1-indoline 
• 57368-91-9 8-bromo-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one 
• 57369-32-1 pyroquilone 
• 288-32-4 1H-imidazole 
• 1386443-33-9 4-[hydroxy-(4-oxo-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-8-yl)-methyl]-benzonitrile 
• 1386443-21-5 4-(4-oxo-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinoline-8-carbonyl)-benzonitrile 
• 64140-62-1 N-(β-chloropropionyl)-indoline 

Relevant academic research and scientific papers

Novel imidazol-1-ylmethyl substituted 1,2,5,6-tetrahydropyrrolo[3,2,1-ij] quinolin-4-ones as potent and selective cyp11b1 inhibitors for the treatment of cushing's syndrome

CYP11B1 inhibition is a promising therapy for Cushing's syndrome. Starting from etomidate, references I and II, the title compounds were designed and synthesized. Cyclopropyl analogue 4 was identified as a CYP11B1 inhibitor more potent (IC50 = 2.2 nM) than leads and more selective (SF = 11) than I and metyrapone. Since it also showed potent inhibition of rat CYP11B1 and good selectivity over human CYP17 and CYP19, it is a promising candidate for further development.

Inhibitors of the Human Aldosterone Sythase CYP11B2

The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and a method of treating of hyperaldosteronism and/or disorders or diseases that are mediated by 11β-hydroxylase (CYP11B1) with these compounds.

6-PYRIDIN-3-YL-3,4-DIHYDRO-1H-QUINOLIN-2-ONE DERIVATIVES AND RELATED COMPOUNDS AS INHIBITORS OF THE HUMAN ALDOSTERONE SYNTHASE CYP11B2

The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and the use of these compounds and other heteroaryl substituted quinolinone derivatives for the treatment of hyperaldosteronism and/or disorders or diseases that are mediated by 11 β-hydroxylase (CYP11 B1 ).