658-98-0

Usage

Chemical Properties

White crystalline powder

Upstream product

• 2994-69-6 2-chloro-4-(chloromethyl)-1-fluorobenzene 
• 151-50-8 potassium cyanide 
• 773837-37-9 sodium cyanide 
• 192702-01-5 3-chloro-4-fluorobenzyl bromide 
• 161446-90-8 3-chloro-4-fluorobenzyl alcohol 
• 7677-24-9 trimethylsilyl cyanide 
• 348-51-6 1-chloro-2-fluorobenzene 

Downstream Products

• 2993-87-5 3-Hydroxy-2-<4-fluor-3-chlor-phenyl>-crotonsaeure-nitril 
• 1231957-81-5 2-(3-chloro-4-fluorophenyl)-4-(tetrahydro-2H-pyran-2-yloxy)butanenitrile 
• 1440519-55-0 N-[2-(3-chloro-4-fluoro-phenyl)-ethyl]-2,2,2-trifluoro-acetamide 
• 1432051-10-9 1-(3-chloro-4-fluorophenyl)-3-hydroxycyclobutanecarbonitrile 
• 1207438-42-3 tert-butyl 4-[(3-chloro-4-fluorophenyl)(cyano)methylidene]piperidine-1-carboxylate 
• 1207436-36-9 4-[(1RS)-1-(3-chloro-4-fluorophenyl)-2-methoxyethyl]piperidine monohydrochloride 
• 1207438-92-3 tert-butyl 4-[(1RS)-1-(3-chloro-4-fluorophenyl)-2-methoxyethyl]piperidine-1-carboxylate 
• 1207438-80-9 tert-butyl 4-[(1RS)-1-(3-chloro-4-fluorophenyl)-2-hydroxyethyl]piperidine-1-carboxylate 
• 1207438-61-6 (2RS)-2-[1-(tert-butoxycarbonyl)piperidin-4-yl]-2-(3-chloro-4-fluorophenyl)ethanoic acid 
• 1207438-49-0 tert-butyl 4-[(RS)-(3-chloro-4-fluorophenyl)(cyano)methyl]piperidine-1-carboxylate 
• 1432097-38-5 3-[(S)-hydroxy(pyridin-2-yl)methyl]-3-[4-(trifluoromethyl)pyridin-2-yl]-cyclobutanone 
• 1432051-34-7 3-(3-chloro-4-fluorophenyl)-3-[(S)-hydroxy(pyridin-2-yl)methyl]-cyclobutanone 
• 1432051-20-1 3-(3-chloro-4-fluorophenyl)-3-[hydroxy(pyridin-2-yl)methyl]-cyclobutanone 
• 1432051-17-6 [2-(3-chloro-4-fluorophenyl)-5,8-dioxaspiro[3.4]octan-2-yl](pyridin-2-yl)-methanone 

Relevant academic research and scientific papers

Discovery of 3-Pyridyl Isoindolin-1-one Derivatives as Potent, Selective, and Orally Active Aldosterone Synthase (CYP11B2) Inhibitors

Aldosterone synthase (CYP11B2) inhibitors have been explored in recent years as an alternative therapeutic option to mineralocorticoid receptor (MR) antagonists to reduce elevated aldosterone levels, which are associated with deleterious effects on various organ systems including the heart, vasculature, kidney, and central nervous system (CNS). A benzamide pyridine hit derived from a focused screen was successfully developed into a series of potent and selective 3-pyridyl isoindolin-1-ones CYP11B2 inhibitors. Our systematic structure-activity relationship study enabled us to identify unique structural features that result in high selectivity against the closely homologous cortisol synthase (CYP11B1). We evaluated advanced lead molecules, exemplified by compound 52, in an in vivo cynomolgus monkey acute adrenocorticotropic hormone (ACTH) challenge model and demonstrated a superior 100-fold in vivo selectivity against CYP11B1.

NEW BICYCLIC DIHYDROISOQUINOLINE-1-ONE DERIVATIVES

The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4? R5, R6, A1, A2, A3, A4, A5 and n are as described herein,compositions including the compounds and methods of using the compounds as aldosterone synthase (CYP11B2 or CYP11B1) inhibitors for the treatment or prophylaxis of chronic kidney disease, congestive heart failure, hypertension, primary aldosteronism and Cushing syndrom.

QUATERNARY PIPERIDINE DERIVATIVES AND USES THEREOF

This invention generally relates to quaternary piperidine compounds, particularly substituted 3-phenylpiperidine compounds and salts thereof. This invention also relates to pharmaceutical compositions comprising such a compound, uses of such a compound (including, for example, treatment methods and medicament preparations), and processes for making such a compound.