887913-52-2

Upstream product

• 4248-19-5 tert-butyl carbazate 
• 556-61-6 methyl thioisocyanate 
• 624-83-9 methyl isocyanate 
• 24424-99-5 di-tert-butyl dicarbonate 
• 598-52-7 1-(methyl)-thiourea 

Downstream Products

• 1254199-70-6 (S)-tert-butyl 4-(5-amino-2-fluorophenyl)-1,4-dimethyl-6-oxotetrahydropyrimidin-2(1H)-ylidenecarbamate 
• 1286278-36-1 (S)-tert-butyl 4-(5-bromo-2-fluorophenyl)-1,4-dimethyl-6-oxotetrahydropyrimidin-2(1H)-ylidenecarbamate 
• 1254199-54-6 (S)-tert-butyl 4-(2-fluoro-5-nitrophenyl)-1,4-dimethyl-6-oxotetrahydropyrimidin-2(1H)-ylidenecarbamate 
• 1125407-02-4 C₁₈H₂₂BrN₃O₃ 
• 1192479-41-6 C₂₃H₂₇BrN₄O₃S 
• 1254199-66-0 [(S)-4-(3-amino-phenyl)-1,4-dimethyl-6-oxo-1,4,5,6-tetrahydro-pyrimidin-2-yl]-carbamic acid tert-butyl ester 

Relevant academic research and scientific papers

COMPOUNDS AND THEIR USE AS BACE1 INHIBITORS

The present invention relates to compounds of Formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein X, Y, Z, Q, W, m, u, ring (A), R2, R3, R4, R5 and R6, are as defined in the specification and claims. The present invention provides a pharmaceutical composition containing the compounds of Formula (I) and a therapeutic method of treating and/or preventing Downs syndrome, β-amyloid angiopathy, disorders associated with cognitive impairment, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegenerative diseases, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, Alzheimer's disease and/or Down syndrome, age-related macular degeneration (AMD), glaucoma, olfactory function impairment, traumatic brain injury, progressive muscle diseases, Type II diabetes mellitus and cardiovascular diseases (stroke).

Discovery of an orally available, brain penetrant BACE1 inhibitor that affords robust CNS Aβ reduction

Inhibition of BACE1 to prevent brain Aβ peptide formation is a potential disease-modifying approach to the treatment of Alzheimer's disease. Despite over a decade of drug discovery efforts, the identification of brain-penetrant BACE1 inhibitors that substantially lower CNS Aβ levels following systemic administration remains challenging. In this report we describe structure-based optimization of a series of brain-penetrant BACE1 inhibitors derived from an iminopyrimidinone scaffold. Application of structure-based design in tandem with control of physicochemical properties culminated in the discovery of compound 16, which potently reduced cortex and CSF Aβ40 levels when administered orally to rats.

1,4,5,6-TETRAHYDRO-PYRIMIDIN-2-YLAMINE COMPOUNDS

This invention relates to compounds of the formula wherein R1 to R9 are as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the therapeutic and/

1,4,5,6-TETRAHYDRO-PYRIMIDIN-2-YLAMINE COMPOUNDS

This invention relates to compounds of the formula wherein R1 to R9 are as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the therapeutic and/

PENTAFLUOROSULFUR IMINO HETEROCYCLIC COMPOUNDS AS BACE-1 INHIBITORS, COMPOSITIONS, AND THEIR USE

In its many embodiments, the present invention provides provides certain pentafluorosulfur imino heterocyclic compounds, including compounds Formula (I): and tautomers thereof, and solvates, prodrugs, esters, and deuterates of said compounds and said tautomers, and pharmaceutically acceptable salts of said compounds, tautomers, solvates, prodrugs, esters, and deuterates, wherein each of R1, R2, R3, R4, R5, R9, R11, ring A, ring B, m, n, p, q, r, -L1-,L2-, and L3- is selected independently and as defined herein. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (Aβ) protein, including Alzheimers Disease, are also disclosed.

DIHYDROPYRIMIDINONES FOR USE AS BACE2 INHIBITORS

This invention relates to dihydropyrimidinones of the formula (I), wherein X and R1 to R7 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors

One-step synthesis and isolation of N-(tert-butoxycarbonyl)-N′- methylthiourea on a large scale

Simple preparation and isolation of N-(tert-butoxycarbonyl)-N′- methylthiourea on a large scale are described. Copyright Taylor & Francis Group, LLC.

Unexpected reactivity of the 9-aminoacridine chromophore in guanidylation reactions

(Chemical Equation Presented) The 9-aminoacridine chromophore is an important building block of DNA-targeted chemotherapeutic agents. The success of 1-[2-(acridin-9-ylamino)ethyl]-1,3-dimethylthiourea as a carrier group in cytotoxic platinum-intercalator conjugates prompted us to explore the synthesis of an analogous guanidine-functionalized acridine. In a successful effort to generate such a derivative, various methods of guanidylation were employed, which demonstrate that the acridine C9-N9 linkage is highly susceptible to electrophilic and nucleophilic attack. The newly established reactivities provide efficient pathways to novel cyclic and spirocyclic acridine derivatives.