876761-25-0

Upstream product

• 876761-54-5 (S)-4-tert-butoxycarbonylamino-4-cyclohexyl-butyric acid methyl ester 
• 77-92-9 citric acid 
• 70491-05-3 (2R)-[(tert-butoxycarbonyl)-amino](cyclohexyl)ethanoic acid 
• 188348-02-9 tert-butyl (R)-(methoxycarbonyl)(cyclohexyl)methylcarbamate 
• 171560-20-6 (2R)-2-(1,1-dimethylethoxycarbonylamino)-2-cyclohexylethanal 
• 876761-24-9 C₁₇H₂₉NO₄ 

Downstream Products

• 946136-75-0 C₃₆H₅₂N₂O₄ 
• 876761-29-4 4-(2-amino-5-phenoxy-benzylamino)-4,N-dicyclohexyl-N-methyl-butyramide 
• 877032-57-0 4-(2-amino-6-phenoxy-4H-quinazolin-3-yl)-4-(S)-,N-dicyclohexyl-N-methyl-butyramide 
• 1397458-19-3 C₃₆H₄₇N₅O₂S 
• 1397458-21-7 C₃₆H₄₇N₅O₂S 
• 1397458-23-9 C₃₇H₄₉N₅O₂S 
• 1397458-25-1 C₃₆H₄₇N₅O₃S 

Relevant academic research and scientific papers

Synthesis, radiolabeling, and evaluation of a potent β-site APP cleaving enzyme (BACE1) inhibitor for PET imaging of BACE1 in vivo

The β-site APP-cleaving enzyme 1 (BACE1) plays important roles in the proteolytic processing of amyloid precursor protein, and can be regarded as an important target for the diagnosis and treatment of AD. This study aimed to report the synthesis and evaluation of an 18F-labeled 2-amino-3,4-dihydroquinazoline analog as a potential BACE1 radioligand. A fluoropropyl side chain was introduced to the phenyl of this 3,4-dihydroquinazoline scaffold to generate the radioligand. Our preliminary data indicated that although the 2-amino-3,4-dihydroquinazoline scaffold possessed favorable in-vitro properties as a PET ligand, its poor brain uptake hindered the in-vivo imaging of BACE1. Further investigation would be required to optimize the scaffold for the development of a blood-brain-barrier-permeable BACE1-targeted PET ligand.

Structure-based design, synthesis, and biological evaluation of dihydroquinazoline-derived potent β-secretase inhibitors

Structure-based design, synthesis, and biological evaluation of a series of dihydroquinazoline-derived β-secretase inhibitors incorporating thiazole and pyrazole-derived P2-ligands are described. We have identified inhibitor 4f which has shown potent enzyme inhibitory (Ki = 13 nM) and cellular (IC50 = 21 nM in neuroblastoma cells) assays. A model of 4f was created based upon the X-ray structure of 3a-bound β-secretase. The model suggested possible interactions in the active site.

SUBSTITUTED AMINO-BENZIMIDAZOLES, MEDICAMENTS COMPRISING SAID COMPOUND, THEIR USE AND THEIR METHOD OF MANUFACTURE

The present invention relates to substituted amino-benzimidazoles of general formula (1) wherein the groups R1 to R14 and A, are defined as in the specification and claims and the use thereof for the treatment of Alzheimer's disease (AD) and similar diseases.

MACROCYCLE DERIVATIVES USEFUL AS INHIBITORS OF beta-SECRETASE (BACE)

The present invention is directed to macrocycle derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD) and related disorders. The compounds of the invention are inhibitors of β-secretase, also known as β-site cleaving enzyme and BACE, BACE1, Asp2 and memapsin2.

2-Amino-3,4-dihydroquinazolines as inhibitors of BACE-1 (β-site APP cleaving enzyme): Use of structure based design to convert a micromolar hit into a nanomolar lead

A new aspartic protease inhibitory chemotype bearing a 2-amino-3,4- dihydroquinazoline ring was identified by high-throughput screening for the inhibition of BACE-1. X-ray crystallography revealed that the exocyclic amino group participated in a hydrogen

2-AMINO-3,4-DIHYDRO-PYRIDO[3,4-D]PYRIMIDINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE)

The present invention is directed to 2-amino-3,4-dihydro-pyrido[3,4-d]pyrimidine derivatives of formula (I), pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD) and related disorders. The compounds of the invention are inhibitors of β-site cleaving enzyme and BACE, BACE1, Asp2 and memapsin2.