845543-89-7

Upstream product

• 845543-86-4 (2S,3S)-2-(3,5-difluorobenzyl)-3-((R)-2-(tert-butoxycarbonyl)-1,2,3,4-tetrahydroisoquinolin-3-yl)-3-hydroxypropanoic acid 
• 877078-49-4 (S)-4-benzyl-3-(3-(3,5-difluorophenyl)propanoyl)oxazolidin-2-one 
• 1034606-46-6 (R)-tert-butyl 3-((1S,2S)-2-(3,5-difluorobenzyl)-3-((S)-4-benzyl-2-oxooxazolidin-3-yl)-1-hydroxy-3-oxopropyl)-3,4-dihydro-isoquinoline-2(1H)-carboxylate 
• 845543-81-9 tert-butyl (3R)-3-(hydroxymethyl)-3,4-dihydroisoquinoline-2(1H)-carboxylate 
• 312639-49-9 N-Boc-(D)-Tic methyl ester 
• 78879-20-6 D-N-tert-butoxycarbonyl-1,2,3,4-tetrahydroisoquinolinoline-3-carboxylic acid 
• 845543-84-2 C₃₀H₃₆F₂N₂O₆ 
• 444583-19-1 tert-butyl (3R)-3-formyl-3,4-dihydroisoquinoline-2(1H)-carboxylate 

Downstream Products

• 845543-91-1 C₂₃H₂₈F₂N₂O₃ 
• 1034606-50-2 (4S,5R)-4-(3,5-difluorobenzyl)-5-((R)-1,2,3,4-tetrahydroisoquinolin-3-yl)oxazolidin-2-one 
• 845972-71-6 C₃₈H₄₇F₂N₃O₅ 
• 1034607-32-3 C₃₇H₄₅F₂N₃O₄ 
• 1034607-30-1 C₄₄H₅₁F₂N₃O₄ 
• 1034607-41-4 C₄₀H₄₃F₂N₅O₄ 
• 1345968-31-1 C₄₆H₅₄F₂N₄O₅ 
• 1034606-52-4 (4S,5S)-4-(3,5-difluorobenzyl)-5-((R)-2-(4-methoxybenzyl)-1,2,3,4-tetrahydroisoquinolin-3-yl)oxazolidin-2-one 
• 1034606-33-1 (S)-2-((S)-3-butyl-2-oxopyrrolidin-1-yl)-N-((1R,2S)-3-(3,5-difluorophenyl)-1-hydroxy-1-((R)-1,2,3,4-tetrahydroisoquinolin-3-yl)propan-2-yl)propanamide 
• 1034606-31-9 C₃₆H₄₃F₂N₃O₃ 
• 1034606-39-7 C₃₂H₃₅F₂N₅O₃ 
• 1345968-38-8 C₃₂H₃₇F₂N₃O₃ 
• 1034606-35-3 (S)-2-((R)-3-acetamido-3-isobutyl-2-oxopyrrolidin-1-yl)-N-((1R,2S)-3-(3,5-difluorophenyl)-1-hydroxy-1-((R)-1,2,3,4-tetrahydroisoquinolin-3-yl)propan-2-yl)-4-phenylbutanamide 
• 1034606-41-1 (1S,2S)-1-((R)-2-(4-methoxybenzyl)-1,2,3,4-tetrahydroisoquinolin-3-yl)-2-amino-3-(3,5-difluorophenyl)propan-1-ol 

Relevant academic research and scientific papers

Synthesis and in vivo evaluation of cyclic diaminopropane BACE-1 inhibitors

The synthesis, evaluation, and structure-activity relationships of a set of related constrained diaminopropane inhibitors of BACE-1 are described. The full in vivo profile of an optimized inhibitor in both normal and P-gp deficient mice is compared with data generated in normal rats.

Substituted Tetrahydroisoquinolines as Beta-secretase Inhibitors

There is provided a series of tetrahydroisoquinoline diaminopropane compounds of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R, R8 and R9 are as defined herein, their pharmaceutical compositi

CYCLIC AMINE BASE-1 INHIBITORS HAVING A HETEROCYCLIC SUBSTITUENT

Disclosed are novel compounds of the formula (I)or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is formula (I) X is -0-, -C(R14)2- or -N(R)-; Z is -C(R14)2- or -N(R)-; t is 0, 1, 2 or 3; each R and R2 is independently H, alkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, alkenyl or alkynyl; each R14 is H, alkyl, alkenyl, alkynyl, halo, -CN, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, -OR35, -N(R24)(R25)or -SR35; R41 is alkyl, cycloalkyl, -S02(alkyl), -C(O)-alkyl, -C(O)-cycloalkyl or -alkyl-NH-C(O)CH3; and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I and methods of treating cognitive or neurodegenerative diseases with compounds of formula (I). Also disclosed are pharmaceutical compositions and methods of treatment comprising compounds of formula I in combination with other agents useful in treating cognitive or neurodegenerative diseases.

CYCLIC AMINE BACE-1 INHIBITORS HAVING A BENZAMIDE SUBSTITUENT

Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R is-C(O)-N(R27)(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer’s disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a β-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, and N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.