388071-74-7

Upstream product

• 2740-83-2 3-(TRIFLUOROMETHYL)BENZYLAMINE 
• 98760-08-8 (1-oxiranyl-2-phenylethyl)carbamic acid tert-butyl ester 

Downstream Products

• 1463439-29-3 C₃₄H₃₇F₃N₄O₄S 
• 388074-61-1 (2R,3S)-3-amino-4-phenyl-1-((3-(trifluoromethyl)benzyl)amino)butan-2-ol 
• 1108698-65-2 (2R,3S)-3-amino-4-phenyl-1-{[3-(trifluoromethyl)benzyl]amino}butan-2-ol hemi-hydrochloride 

Relevant academic research and scientific papers

Discovery of multifunctional anti-Alzheimer's agents with a unique mechanism of action including inhibition of the enzyme butyrylcholinesterase and γ-aminobutyric acid transporters

Looking for an effective anti-Alzheimer's agent is very challenging; however, a multifunctional ligand strategy may be a promising solution for the treatment of this complex disease. We herein present the design, synthesis and biological evaluation of novel hydroxyethylamine derivatives displaying unique, multiple properties that have not been previously reported. The original mechanism of action combines inhibitory activity against disease-modifying targets: β-secretase enzyme (BACE1) and amyloid β (Aβ) aggregation, along with an effect on targets associated with symptom relief - inhibition of butyrylcholinesterase (BuChE) and γ-aminobutyric acid transporters (GATs). Among the obtained molecules, compound 36 exhibited the most balanced and broad activity profile (eeAChE IC50 = 2.86 μM; eqBuChE IC50 = 60 nM; hBuChE IC50 = 20 nM; hBACE1 IC50 = 5.9 μM; inhibition of Aβ aggregation = 57.9% at 10 μM; mGAT1 IC50 = 10.96 μM; and mGAT2 IC50 = 19.05 μM). Moreover, we also identified 31 as the most potent mGAT4 and hGAT3 inhibitor (IC50 = 5.01 μM and IC50 = 2.95 μM, respectively), with high selectivity over other subtypes. Compounds 36 and 31 represent new anti-Alzheimer agents that can ameliorate cognitive decline and modify the progress of disease.

INHIBITION OF MEMAPSIN 1 CLEAVAGE IN THE TREATMENT OF DIABETES

Proteases such as memapsin-1 are import enzymes, playing roles in a variety o f diseases including diabetes. The in-ventors have developed inhibitors of memapsin 1 and methods of use therefore in the treatment of disease

BACE 2 INHIBITORS

The present invention relates to N-1-Benzyl-2-hydroxy-3-(hetero)arylamino-propyl)-isophthalamides of formula I having BACE2 inhibitory activity and their use as therapeutically active substances, their manufacture and pharmaceutical compositions. The acti

BACE INHIBITORS FOR USE IN THE TREATMENT OF DIABETES

The present invention relates to N-1-Benzyl-2-hydroxy-3-(hetero)arylamino-propyl)-isophthalamides of formula (I) having BACE2 inhibitory activity and their use as therapeutically active substances, their manufacture and pharmaceutical compositions. The ac

1,2,3,4-TETRAHYDROPYRROLO[1,2-A]PYRAZINE-6-CARBOXAMIDE AND 2,3,4,5-TETRAHYDROPYRROLO[1,2-a][1,4]-DIAZEPINE-7-CARBOXAMIDE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF

The present invention relates to derivatives of 1,2,3,4-tetrahydropyrrolo-[1,2-a]pyrazine-6-carboxamides and of 2,3,4,5-tetrahydropyrrolo[1,2-a][1,4]diazepine-7-carboxamides, to the preparation thereof and to the therapeutic use thereof.

Second generation of hydroxyethylamine BACE-1 inhibitors: Optimizing potency and oral bioavailability

BACE-1 inhibition has the potential to provide a disease-modifying therapy for the treatment of Alzheimer's disease. Optimization of a first generation of BACE-1 inhibitors led to the discovery of novel hydroxyethylamines (HEAs) bearing a tricyclic nonprime side. These derivatives have nanomolar cell potency and are orally bioavailable.