928136-82-7

Basic information

• Product Name: 4-(2-(tert-butyldiMethylsilyloxy)ethyl)-1-trityl-1H-iMidazole
• Synonyms: 4-(2-(tert-butyldiMethylsilyloxy)ethyl)-1-trityl-1H-iMidazole
• CAS NO: 928136-82-7
• Molecular Formula: C₃₀H₃₆N₂OSi
• Molecular Weight: 468.70514
• Mol File: 928136-82-7.mol

Chemical Properties

• Appearance: /
• CAS DataBase Reference: 4-(2-(tert-butyldiMethylsilyloxy)ethyl)-1-trityl-1H-iMidazole(CAS DataBase Reference)
• NIST Chemistry Reference: 4-(2-(tert-butyldiMethylsilyloxy)ethyl)-1-trityl-1H-iMidazole(928136-82-7)
• EPA Substance Registry System: 4-(2-(tert-butyldiMethylsilyloxy)ethyl)-1-trityl-1H-iMidazole(928136-82-7)

Safety Data

• Hazardous Substances Data: 928136-82-7(Hazardous Substances Data)

Upstream product

• 3251-69-2 imidazole-4-acetic acid hydrochloride 
• 76-83-5 trityl chloride 
• 168632-03-9 1-triphenylmethyl-4-imidazolyl-acetic acid 
• 18162-48-6 tert-butyldimethylsilyl chloride 
• 127607-62-9 1-triphenylmethyl-4-(2-hydroxyethyl)-1H-imidazole 

Downstream Products

• 1202709-86-1 5-(2-chloroethyl)-1-(4'-fluorobiphenyl-2-ylmethyl)-1H-imidazole 
• 928134-47-8 3-bromo-4-(6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-5-yl)benzonitrile 
• 928136-89-4 {5-[2-(tert-butyldimethylsilanyloxy)ethyl]imidazol-1-yl}-(2-chloro-4-cyanophenyl)acetic acid methyl ester 
• 928136-90-7 (2-chloro-4-cyanophenyl)-[5-(2-hydroxyethyl)imidazol-1-yl]-acetic acid methyl ester 
• 928136-91-8 (2-chloro-4-cyanophenyl)-[5-(2-methanesulfonyloxyethyl)imidazol-1-yl]-acetic acid methyl ester 

Relevant articles and documents

3-FLUORO-BENZONITRILE INHIBITORS OF 11-BETA-HYDROXYLASE

The present invention relates to new 3-fluoro-benzonitrile modulators of 11-β- hydroxylase, pharmaceutical compositions thereof, and methods of use thereof.

Discovery and in vivo evaluation of potent dual CYP11B2 (aldosterone synthase) and CYP11B1 inhibitors

Aldosterone is a key signaling component of the renin-angiotensin- aldosterone system and as such has been shown to contribute to cardiovascular pathology such as hypertension and heart failure. Aldosterone synthase (CYP11B2) is responsible for the final three steps of aldosterone synthesis and thus is a viable therapeutic target. A series of imidazole derived inhibitors, including clinical candidate 7n, have been identified through design and structure-activity relationship studies both in vitro and in vivo. Compound 7n was also found to be a potent inhibitor of 11β-hydroxylase (CYP11B1), which is responsible for cortisol production. Inhibition of CYP11B1 is being evaluated in the clinic for potential treatment of hypercortisol diseases such as Cushing's syndrome.

Organic compounds

The present invention provides a compound of formula I: Said compound is inhibitor of aldosterone synthase and aromatase, and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase or aromatase. Accordingly, the compound of formula I can be used in treatment of hypokalemia, hypertension, congestive heart failure, atrial fibrillation, renal failure, in particular, chronic renal failure, restenosis, atherosclerosis, syndrome X, obesity, nephropathy, post-myocardial infarction, coronary heart diseases, inflammation, increased formation of collagen, fibrosis such as cardiac or myocardiac fibrosis and remodeling following hypertension and endothelial dysfunction, gynecomastia, osteoporosis, prostate cancer, endometriosis, uterine fibroids, dysfunctional uterine bleeding, endometrial hyperplasia, polycystic ovarian disease, infertility, fibrocystic breast disease, breast cancer and fibrocystic mastopathy. Finally, the present invention also provides a pharmaceutical composition.

ORGANIC COMPOUNDS

The present invention provides a compound of formula (I):said compound is inhibitor of aldosterone synthase, and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase. Accordingly, the compound of formula I can be used in treatment of hypokalemia, hypertension, congestive heart failure, renal failure, in particular, chronic renal failure, restenosis, atherosclerosis, syndrome X, obesity, nephropathy, post-myocardial infarction, coronary heart diseases, increased formation of collagen, cardiac fibrosis and remodeling following hypertension and endothelial dysfunction. Finally, the present invention also provides a pharmaceutical composition.

ALDOSTERONE SYNTHASE AND/OR 11β-HYDROXYLASE INHIBITORS

The present invention provides a compound of formula (I). Said compound is inhibitor of CYP11B2 and/or CYP11B1, and thus can be employed for the treatment of a disorder or disease mediated by CYP11B2 and/or CYP11B1.