253449-32-0

Upstream product

• 103322-56-1 tert-butyl [(1S)-2-cyclohexyl-1-(hydroxymethyl)ethyl]carbamate 
• 124-63-0 methanesulfonyl chloride 
• 24424-99-5 di-tert-butyl dicarbonate 
• 117160-99-3 (2S)-2-amino-3-cyclohexylpropan-1-ol hydrochloride 

Downstream Products

• 1026848-32-7 (2-cyclohexyl-1-cyclohexylsulfanylmethyl-ethyl)-carbamic acid tert-butyl ester 
• 253449-33-1 2(S)-N-tert-butoxycarbonyl-3-cyclohexyl-1-ethylthio-2-propylamine 
• 1026461-29-9 (1-tert-butylsulfanylmethyl-2-cyclohexyl-ethyl)-carbamic acid tert-butyl ester 
• 884511-15-3 (S)-tert-butyl 1-cyclohexyl-3-(methylamino)propan-2-ylcarbamate 
• 884511-11-9 (S)-tert-butyl (1-azido-3-cyclohexylpropan-2-yl)carbamate 
• 1093865-10-1 1,1-dimethylethyl [(1S)-2-azido-1-(cyclohexylmethyl)ethyl]methylcarbamate 
• 884511-41-5 (S)-tert-butyl (1-amino-3-cyclohexylpropan-2-yl)(methyl)carbamate 
• 149423-46-1 (S)-tert-butyl (1-amino-3-cyclohexylpropan-2-yl)carbamate 
• 884513-80-8 (S)-tert-butyl 1-(p-nitrophenoxycarbonylamino)-3-cyclohexylpropan-2-ylcarbamate 
• 884511-14-2 (S)-2-(trimethylsilyl)ethyl 2-amino-3-cyclohexylpropyl(methyl)carbamate 
• 884511-16-4 (S)-tert-butyl 1-cyclohexyl-3-(N-methyl-N-(2-(trimethylsilyl)ethoxycarbonyl)amino)propan-2-ylcarbamate 
• 942143-51-3 C₁₆H₃₂N₂O₂ 

Relevant academic research and scientific papers

Discovery of VTP-27999, an alkyl amine renin inhibitor with potential for clinical utility

Structure guided optimization of a series of nonpeptidic alkyl amine renin inhibitors allowed the rational incorporation of additional polar functionality. Replacement of the cyclohexylmethyl group occupying the S1 pocket with a (R)-(tetrahydropyran-3-yl)

Optimization of orally bioavailable alkyl amine renin inhibitors

Structure-guided drug design led to new alkylamine renin inhibitors with improved in vitro and in vivo potency. Lead compound 21a, has an IC50 of 0.83 nM for the inhibition of human renin in plasma (PRA). Oral administration of 21a at 10 mg/kg

RENIN INHIBITORS AND METHOD OF USE THEREOF

Disclosed are aspartic protease inhibitors represented by the following Formula: wherein R1 , R2, R3, R4, R5, R6, R7a, R7b and n are as defined herein, or a pharmaceut

Design and optimization of renin inhibitors: Orally bioavailable alkyl amines

Structure-based drug design led to the identification of a novel class of potent, low MW alkylamine renin inhibitors. Oral administration of lead compound 21l, with MW of 508 and IC50 of 0.47 nM, caused a sustained reduction in mean arterial bl

RENIN INHIBITORS

Described are compounds that bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also described are methods of use of the compounds described herein in ameliorating or treating aspartic protease related disorders in a subject in need thereof.

ASPARTIC PROTEASE INHIBITORS

The present invention is directed to aspartic protease inhibitors. Certain aspartic protease inhibitors of the invention can be represented by the following structural formula or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.

Discovery of a series of cyclohexylethylamine-containing protein farnesyltransferase inhibitors exhibiting potent cellular activity

Synthesis of a library of secondary benzylic amines based on the Sebti- Hamilton type peptidomimetic farnesyltransferase (FTase) inhibitor FTI-276 (1) led to the identification of 6 as a potent enzyme inhibitor (IC50 of 8 nM) which lacked the p