216059-91-5

Upstream product

• 22282-99-1 4-bromo-2-methylpyridine 
• 214360-73-3 4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)aniline 
• 1115492-92-6 2-methyl-4-pyridylzinc bromide 
• 540-37-4 p-aminoiodobenzene 
• 106-40-1 4-bromo-aniline 
• 579476-63-4 2-methylpyridine-4-boronic acid 
• 586-78-7 para-nitrophenyl bromide 
• 660867-80-1 2-methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine 
• 55218-69-4 2-methyl-4-(4-nitrophenyl)pyridine 
• 636-98-6 p-nitrobenzene iodide 

Downstream Products

• 1161361-81-4 2-(7-bromo-3,4-dihydroisoquinolin-2(1H)-yl)-N-(4-(2-methylpyridin-4-yl)-phenyl)propanamide 
• 1161361-78-9 (S)-2-(6-methoxynaphthalen-2-yl)-N-(4-(2-methylpyridin-4-yl)phenyl)propanamide trifluoroacetate 
• 1161355-29-8 2-(3,5-bis(trifluoromethyl)phenyl)-N-(4-(2-methylpyridin-4-yl)phenyl)propanamide 
• 1161362-12-4 N-(4-(2-methylpyridin-4-yl)phenyl)-2-(4-nitrophenyl)propanamide 
• 1161360-61-7 2-(6-chloropyridin-3-yl)-N-(4-(2-methylpyridin-4-yl)phenyl)propanamide 
• 1161360-79-7 3-cyclopropyl-2-(5-(isopropylamino)pyridin-2-yl)-N-(4-(2-methylpyridin-4-yl)phenyl)-propanamide 
• 1161361-83-6 2-(2-bromophenylamino)-4-methyl-N-(4-(2-methylpyridin-4-yl)phenyl)pentanamide 
• 1161359-46-1 2-(6-fluoropyridin-2-yl)-N-(4-(2-methylpyridin-4-yl)phenyl)propanamide 
• 1161355-45-8 2-(6-chloropyridin-2-yl)-N-(4-(2-methylpyridin-4-yl)phenyl)propanamide 
• 1161359-69-8 2-(2-chloropyridin-4-yl)-N-(4-(2-methylpyridin-4-yl)phenyl)-propanamide 
• 1161358-40-2 2-(4-chloropyridin-2-yl)-N-(4-(2-methylpyridin-4-yl)phenyl)propanamide 
• 1161360-68-4 2-(6-bromopyridin-2-yl)-4-methyl-N-(4-(2-methylpyridin-4-yl)phenyl)-pentanamide 
• 1161361-84-7 6-bromo-2,2-dimethyl-N-(4-(2-methylpyridin-4-yl)phenyl)-3,4-dihydro-2H-chromene-4-carboxamide 
• 1161359-32-5 2-(1H-indol-1-yl)-N-(4-(2-methylpyridin-4-yl)phenyl)propanamide 

Relevant academic research and scientific papers

Triazole naphthoquinone connected aromatic (heterocyclic) ring derivative

The invention belongs to the field of chemical medicine, particularly relates to a micromolecule capable of resisting malignant tumor, acute leukemia and arthritis, multiple sclerosis and immunological rejection and a preparation and application of the mi

Wnt signal pathway inhibitor and use thereof

The invention relates to heterocyclic compounds with Wnt signal channel inhibition activity, particularly including compounds, pharmaceutically acceptable salts, various isotopes, various isomers or various crystal structures thereof having a structure represented by a general formula I (shown in the specification). By the compounds and a composition of the compounds, a Wnt signal channel can be effectively inhibited and diseases related to the Wnt signal channel can be treated or prevented.

FUSED MORPHOLINOPYRIMIDINES AND METHODS OF USE THEREOF

The present disclosure relates to Fused Morpholinopyrimidines, pharmaceutical compositions comprising an effective amount of a Fused Morpholinopyrimidine and methods for using a Fused Morpholinopyrimidine in the treatment of a neurodegenerative disease, comprising administering to a subject in need thereof an effective amount of a Fused Morpholinopyrimidine.

Synthesis and characterization of the first inhibitor of: N -acylphosphatidylethanolamine phospholipase D (NAPE-PLD)

N-Acylphosphatidylethanolamine phospholipase D (NAPE-PLD) is a membrane-associated zinc enzyme that catalyzes the hydrolysis of N-acylphosphatidylethanolamines (NAPEs) into fatty acid ethanolamides (FAEs). Here, we describe the identification of the first small-molecule NAPE-PLD inhibitor, the quinazoline sulfonamide derivative 2,4-dioxo-N-[4-(4-pyridyl)phenyl]-1H-quinazoline-6-sulfonamide, ARN19874.

Exploration of the linkage elements of porcupine antagonists led to potent Wnt signaling pathway inhibitors

The Wnt signaling pathway is a pivotal developmental pathway. It operates through control of cellular functions such as proliferation, differentiation, migration and polarity. Aberrant Wnt signaling has been implicated in the formation and metastasis of tumors. Porcupine is a component of the Wnt signaling pathway. It is a member of the membrane-bound O-acyltransferase family of proteins. Porcupine catalyzes the palmitoylation of Wnt proteins, a process which is essential to their secretion and activity. Here we report a novel series of compounds obtained by a scaffold hybridization strategy from two known porcupine inhibitor classes. The leading compound 62 demonstrated subnanomolar (IC50 0.11 nM) inhibition of Wnt signaling in a paracrine cellular reporter gene assay. Compound 62 also potently inhibited Wnt secretion into culture medium, an indication of direct inhibition of the porcupine protein. Furthermore, compound 62 showed excellent chemical, plasma and liver microsomal stabilities. Collectively, these results strongly support further optimization of this novel scaffold to develop better Wnt pathway inhibitors.

FUSED MORPHOLINOPYRIMIDINES AND METHODS OF USE THEREOF

The present invention relates to Fused Morpholinopyrimidines, pharmaceutical compositions comprising an effective amount of a Fused Morpholinopyrimidine and methods for using a Fused Morpholinopyrimidine in the treatment of a neurodegenerative disease, comprising administering to a subject in need thereof an effective amount of a Fused Morpholinopyrimidine.

FUSED MORPHOLINOPYRIMIDINES AND METHODS OF USE THEREOF

The present disclosure relates to Fused Morpholinopyrimidines, pharmaceutical compositions comprising an effective amount of a Fused Morpholinopyrimidine and methods for using a Fused Morpholinopyrimidine in the treatment of a neurodegenerative disease, comprising administering to a subject in need thereof an effective amount of a Fused Morpholinopyrimidine.

Discovery of 2-methylpyridine-based biaryl amides as γ-secretase modulators for the treatment of Alzheimer's disease

γ-Secretase modulators (GSMs) are potentially disease-modifying treatments for Alzheimer's disease. They selectively lower pathogenic Aβ42 levels by shifting the enzyme cleavage sites without inhibiting γ-secretase activity, possibly avoiding known adverse effects observed with complete inhibition of the enzyme complex. A cell-based HTS effort identified the sulfonamide 1 as a GSM lead. Lead optimization studies identified compound 25 with improved cell potency, PKDM properties, and it lowered Aβ42 levels in the cerebrospinal fluid (CSF) of Sprague-Dawley rats following oral administration. Further optimization of 25 to improve cellular potency is described.

NOVEL SUBSTITUTED TRIAZOLE DERIVATIVES AS GAMMA SECRETASE MODULATORS

The present invention is concerned with novel substituted triazole derivatives of Formula (I) wherein Het1, R1, R2, A1, A2, A3, A4, L1, and L2 have the mean