143935-49-3

Upstream product

• 60-29-7 diethyl ether 
• 105-36-2 ethyl bromoacetate 
• 121-44-8 triethylamine 
• 3218-02-8 cyclohexylmethylamine 
• 24424-99-5 di-tert-butyl dicarbonate 
• 65940-28-5 N-cyclohexanemethylglycine benzyl ester 
• 144006-28-0 ethyl 2-<(cyclohexylmethyl)amino>acetate 
• 225377-11-7 1,1-dimethylethyl N-(cyclohexylmethyl)-N-(2-ethoxy-2-oxoethyl)carbamate 
• 172834-26-3 (tert-Butoxycarbonyl-cyclohexylmethyl-amino)-acetic acid benzyl ester 

Downstream Products

• 225377-22-0 1,1-dimethylethyl N-(cyclohexyl)-N-<2-amino>-2-oxoethyl>carbamate 
• 245756-18-7 2-(2-chloro-allyl)-N¹-[2-cyclohexyl-1-(5-isobutyl-2,2-dimethyl-[1,3]dioxolan-4-yl)-ethyl]-N⁴-cyclohexylmethyl-N⁴-{[methyl-(2-pyridin-2-yl-ethyl)-carbamoyl]-methyl}-succinamide 
• 245756-11-0 2-(2-chloro-allyl)-N⁴-cyclohexylmethyl-N¹-(1-cyclohexylmethyl-2,3-dihydroxy-5-methyl-hexyl)-N⁴-{[methyl-(2-pyridin-2-yl-ethyl)-carbamoyl]-methyl}-succinamide 
• 245756-15-4 2-(2-chloro-allyl)-N⁴-cyclohexylmethyl-N¹-(1-cyclohexylmethyl-5-methyl-hex-2-enyl)-N⁴-{[methyl-(2-pyridin-2-yl-ethyl)-carbamoyl]-methyl}-succinamide 
• 192516-55-5 4-chloro-2-[(cyclohexylmethyl-{[methyl-(2-pyridin-2-yl-ethyl)-carbamoyl]-methyl}-carbamoyl)-methyl]-pent-4-enoic acid methyl ester 
• 294856-63-6 2-(2-bromo-allyl)-N¹-[2-cyclohexyl-1-(5-isobutyl-2,2-dimethyl-[1,3]dioxolan-4-yl)-ethyl]-N⁴-cyclohexylmethyl-N⁴-{[methyl-(2-pyridin-2-yl-ethyl)-carbamoyl]-methyl}-succinamide 
• 294856-61-4 N⁴-(cyclohexylmethyl)-N⁴-[2-[methyl[2-(2-pyridinyl)ethyl]amino]-2-oxoethyl]-N¹-[1(S)-(cyclohexylmethyl)-2(R),3(S)-dihydroxy-5-methylhexyl]-2(S)-(2-bromo-2-propenyl)butanediamide 
• 294856-57-8 3-[4-bromo-2(S)-[2-[(cyclohexylmethyl)[2-[methyl[2-(2-pyridinyl)ethyl]amino]-2-oxoethyl]amino]-2-oxoethyl]-1-oxo-4-pentenyl]-4(S)-(1-methylethyl)-2-oxazolidinone 
• 294856-58-9 2(S)-(2-bromo-2-propenyl)-4-[(cyclohexylmethyl)[2-[methyl[2-(2-pyridinyl)ethyl]amino]-2-oxo-ethyl]amino]-4-oxobutanoic acid 
• 192516-54-4 2-<(cyclohexylmethyl)amino>-N-methyl-N-<2-(2-pyridinyl)ethyl>acetamide 
• 160937-56-4 BILA 2157 BS 

Relevant academic research and scientific papers

Stereoselective synthesis of renin inhibitor BILA 2157 BS

We have developed a convergent and stereoselective synthesis of orally active renin inhibitor BILA 2157 BS. Three building blocks were used to generate the basic skeleton of the inhibitor. The key feature consisted of the late elaboration of the 2-amino-4-thiazolyl heterocycle from a vinylbromide precursor. The synthetic sequence, which required a total of 22 chemical steps, provided 0.6 kg of BILA 2157 BS in 7.3% overall yield.

Antiherpes virus compounds and methods for their preparation and use

This invention relates to methods for inhibiting herpes replication and for treating herpes infection in a mammal by inhibiting the herpes helicase-primase enzyme complex. This invention also relates to thiazolyphenyl derivatives that inhibit the herpes helicase-primase and to pharmaceutical compositions comprising the thiazolylphenyl derivatives, to methods of using and methods of producing the thiazolylphenyl derivatives

Anti-herpesvirus compounds and methods for identifying, making and using same

This invention relates to methods for inhibiting herpes replication and for treating herpes infection in a mammal by inhibiting the herpes helicase-primase enzyme complex. This invention also relates to thiazolyphenyl derivatives that inhibit the herpes helicase-primase and to pharmaceutical compositions comprising the thiazolylphenyl derivatives, to methods of using and methods of producing the thiazolylphenyl derivatives.

Discovery of non-peptidic P2-P3 butanediamide renin inhibitors with high oral efficacy

A new series of non-peptidic renin inhibitors having a 2-substituted butanediamide moiety at the P2 and P3 positions has been identified. The optimized inhibitors have IC50 values of 0.8 to 1.4nM and 2.5 to 7.6nM in plasma renin assays at pH 6.0 and 7.4, respectively. When evaluated in the normotensive cynomolgus monkey model, two of the most potent inhibitors were orally active at a dose as low as 3mg/kg. These potent renin inhibitors are characterized by oral bioavailabilities of 40 and 89% in the cynomolgus monkey. Inhibitor 3z (BILA 2157 BS) was selected as candidate for pre-development. Copyright (C) 1999 Elsevier Science Ltd.

Bradykinin receptor antagonists containing N-substituted amino acids: In vitro and in vivo B2 and B1 receptor antagonist activity

We report a systematic probing of the structural requirements of the bradykinin (BK) type 2 (B2) receptor for antagonist activity by incorporating N-alkyl-amino acid residues at positions 7 and 8 of a potent antagonist sequence. Compound 1 (D-A