1354035-50-9

Upstream product

• 1354035-48-5 methyl 4-bromo-1-methyl-2-naphthoate 
• 73721-17-2 methyl 1-methyl-2-naphthoate 
• 948-03-8 1-hydroxy-naphthalene-2-carboxylic acid methyl ester 
• 1354035-49-6 methyl 4-bromo-1-(bromomethyl)-2-naphthoate 
• 931-15-7 (1S,2S)-trans-2-aminocyclohexanol 

Downstream Products

• 1414367-68-2 5-bromo-2-[(1S,2S)-2-{[tert-butyl(dimethyl)silyl]oxy}cyclohexyl]-1,2-dihydro-3H-benzo[e]isoindol-3-one 
• 1414367-71-7 5-ethenyl-2-[(1S,2S)-2-hydroxycyclohexyl]-1,2-dihydro-3H-benzo[e]isoindol-3-one 
• 1414367-72-8 2-[(1S,2S)-2-hydroxycyclohexyl]-3-oxo-2,3-dihydro-1H-benzo[e]isoindole-5-carbaldehyde 
• 1414365-97-1 1-({2-[(1S,2S)-2-hydroxycyclohexyl]-3-oxo-2,3-dihydro-1H-benzo[e]isoindol-5-yl}methyl)-4-(pyridine-2-yl)piperidine-4-carbonitrile 
• 1414366-58-7 1-({2-[(1S,2S)-2-hydroxycyclohexyl]-3-oxo-2,3-dihydro-1H-benzo[e]isoindol-5-yl}methyl)-4-pyridin-4-ylpiperidine-4-carbonitrile 
• 1414366-57-6 1-({2-[(1S,2S)-2-hydroxycyclohexyl]-3-oxo-2,3-dihydro-1H-benzo[e]isoindol-5-yl}methyl)-4-pyridin-3-ylpiperidine-4-carbonitrile 
• 1414366-51-0 1-({2-[(1S,2S)-2-hydroxycyclohexyl]-3-oxo-2,3-dihydro-1H-benzo[e]isoindol-5-yl}methyl)-4-(pyridimin-4-yl)piperidine-4-carbonitrile 
• 1414366-50-9 1-({2-[(1S,2S)-2-hydroxycyclohexyl]-3-oxo-2,3-dihydro-1H-benzo[e]isoindol-5-yl}methyl)-4-(pyrazin-2-yl)piperidine-4-carbonitrile 
• 1414366-52-1 1-({2-[(1S,2S)-2-hydroxycyclohexyl]-3-oxo-2,3-dihydro-1H-benzo[e]isoindol-5-yl}methyl)-4-(pyridazin-3-yl)piperidine-4-carbonitrile 
• 1414366-00-9 1-({2-[(1S,2S)-2-hydroxycyclohexyl]-3-oxo-2,3-dihydro-1H-benzo[e]isoindol-5-yl}methyl)-4-(6-methylpyridin-2-yl)piperidine-4-carbonitrile 
• 1414366-65-6 1-({2-[(1S,2S)-2-hydroxycyclohexyl]-3-oxo-2,3-dihydro-1H-benzo[e]isoindol-5-yl}methyl)-4-(4-methylpyridin-2-yl)piperidine-4-carbonitrile 
• 1414366-56-5 1-({2-[(1S,2S)-2-hydroxycyclohexyl]-3-oxo-2,3-dihydro-1H-benzo[e]isoindol-5-yl}methyl)-4-phenylpiperidine-4-carbonitrile 
• 1414365-98-2 5-{[4-fluoro-4-(pyridine-2-yl)piperidine-1-yl]methyl}-2-[(1S,2S)-2-hydroxycyclohexyl]-1,2-dihydro-3H-benzo[e]isoindol-3-one 
• 1414365-99-3 1-({2-[(1S,2S)-2-hydroxycyclohexyl]-1-methyl-3-oxo-2,3-dihydro-1H-benzo[e]isoindol-5-yl}methyl)-4-(pyridine-2-yl)piperidine-4-carbonitrile 

Relevant academic research and scientific papers

MK-7622: A First-in-Class M1 Positive Allosteric Modulator Development Candidate

Identification of ligands that selectively activate the M1 muscarinic signaling pathway has been sought for decades to treat a range of neurological and cognitive disorders. Herein, we describe the optimization efforts focused on addressing key physicochemical and safety properties, ultimately leading to the clinical candidate MK-7622, a highly selective positive allosteric modulator of the M1 muscarinic receptor that has entered Phase II studies in patients with Alzheimer's disease.

Discovery of naphthyl-fused 5-membered lactams as a new class of M 1 positive allosteric modulators

Selective activation of the M1 muscarinic receptor via positive allosteric modulation represents an original approach to treat the cognitive decline in patients with Alzheimer's disease. A series of naphthyl-fused 5-membered lactams were identified as a new class of M1 positive allosteric modulators and were found to possess good potency and in vivo efficacy.

N-LINKED LACTAM M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS

The present invention is directed to N-linked lactam compounds of general formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.