1056675-35-4

Upstream product

• 14470-28-1 mono-4-methoxytrityl chloride 
• 874-97-5 3-(hydroxymethyl)benzonitrile 
• 1056675-27-4 3-(4-methoxytrityloxymethyl)benzonitrile 
• 75-16-1 methylmagnesium bromide 

Downstream Products

• 1056675-31-0 (1R,S)-1-(t-butoxycarbonylamino)-1-(3-(4-methoxytrityloxymethyl)phenyl) ethane 
• 1079398-50-7 N-{4R-(1S-benzylcarbamoyl-2-methylpropylcarbamoyl)-1S-[3-(1R/S-tert-butoxycarbonyl-aminoethyl)-benzyloxymethyl]-2S-hydroxy-4R-methoxybutyl}-5-(methanesulphonylmethylamino)isophthalamic acid tert-butyl ester 
• 1079398-47-2 (1R/S-{3-[2S-amino-5R-(1S-benzylcarbamoyl-2-methylpropylcarbamoyl)-3S-hydroxy-5R-methoxypentyloxymethyl]-phenyl}-ethyl) carbamic acid tert-butyl ester 
• 1079398-45-0 (1R/S-{3-[2R-hydroxy-2R-(4R-methoxy-5-oxotetrahydrofuran-2S-yl)ethoxymethy]-phenyl}-ethyl)carbamic acid-tert-butylester 
• 1079398-46-1 (1R/S-{3-[2S-azido-2S-(4R-methoxy-5-oxotetrahvdrofuran-2S-yl)ethoxymethyl]-phenyl} - ethyl)-carbamic acid-tert-butylester 
• 1056675-55-8 (2S,4S,5S)-5-azido-6-(3-((1RS)-1-(t-butoxycarbonylamino)ethyl)benzyloxy)-4-hydroxy-2-isopropyl-hexanoic acid ((S)-1-benzylcarbamoyl-2-methyl-propyl)-amide 
• 1056671-27-2 (2S,4S,5S)-5-amino-6-(3-(1-(t-butoxycarbonylamino)ethyl)benzyloxy)-4-hydroxy-2-isopropyl-hexanoic acid ((S)-1-benzylcarbamoyl-2-methyl-propyl)-amide 
• 1056675-47-8 2,3-dideoxy-6-O-(3-(((1R,S)-1-tert-butoxycarbonylamino)ethyl)benzyl)-2-isopropyl-D-glucono-1,4-lactone 
• 1056675-43-4 (1R,S)-1-(3-(bromomethyl)phenyl)-1-(t-butoxycarbonylamino)ethane 
• 1056675-39-8 (1R,S)-1-(tert-butoxycarbonylamino )-1-(3-(hydroxymethyl)pheny)ethane 

Relevant academic research and scientific papers

Design and synthesis of potent macrocyclic renin inhibitors

Two types of P1-P3-linked macrocyclic renin inhibitors containing the hydroxyethylene isostere (HE) scaffold just outside the macrocyclic ring have been synthesized. An aromatic or aliphatic substituent (P3sp) was introduced in the macrocyclic ring aiming

NEW COMPOUNDS

The invention provides compounds of the formula I wherein Q is aryl or heterocyclyl any of which is optionally substituted; Z is O, S, NRa or S(=O)p; Y is NH, NHNH, CH2NH, O, S or S(=O)p; n is 0, 1, 2 or 3; m is 0, 1 or 2; p is 1 or 2; Ra is H or C1-C4alkyl; R1 is hydrogen, C1-C6alkyl, C0-C3alkanediylC3-C7cycloalkyl, C0-C3alkanediylaryl or C0- C3alkanediylheterocyclyl; R2 is hydrogen or C1-C6alkyl; X' is hydrogen, fluoro, hydroxy, amino or C1-C6alkoxy; X" is hydrogen, or when X' is fluoro, then X" may also be fluoro; R3is C1-C6alkyl; R4' is C1-C6alkyl; R4" is H or C1-C6alkyl; or R4' and R4" together with the carbon atom to which they are attached define a C3-C6cycloalkyl; W is C1-C6alkyl, C3-C7cycloalkyl, aryl or heterocyclyl any of which is optionally substituted; or a pharmaceutically acceptable salt, hydrate or N-oxide thereof. The compounds of the invention are inhibitors of aspartyl proteases such as renin and are among other things useful for the treatment of conditions associated with activities of the RAS, such as hypertension, heart failure and renal insufficiency.

ASPARTYL PROTEASE INHIBITORS

The invention provides compounds of the formula (I) N-oxides, addition salts, quaternary amines, metal complexes, stereochemically isomeric forms and metabolites thereof, wherein G is-O-, -S(=O)r-, -CRdRd or -NRa-; W is H, C1-C6