73721-17-2

Upstream product

• 594-27-4 tetramethylstannane 
• 948-03-8 1-hydroxy-naphthalene-2-carboxylic acid methyl ester 
• 917-64-6 methyl magnesium iodide 
• 6039-59-4 methyl 1-methoxy-2-naphthoate 
• 134391-10-9 methyl 2-methyl-5-phenyl-4,5-dihydrofuran-3-carboxylate 
• 144465-33-8 methyl 1-acetyl-2-phenylcyclopropanecarboxylate 
• 86-48-6 1-hydroxy-2-naphthoic acid 

Downstream Products

• 1354035-50-9 5-bromo-2-[(1S, 2S)-2-hydroxycyclohexyl]-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 
• 1414367-68-2 5-bromo-2-[(1S,2S)-2-{[tert-butyl(dimethyl)silyl]oxy}cyclohexyl]-1,2-dihydro-3H-benzo[e]isoindol-3-one 
• 1354035-55-4 C₁₈H₁₁BrFNO 
• 1569272-99-6 C₁₈H₁₈BrNO₂ 
• 1569273-00-2 C₁₈H₁₈BrNO₂ 
• 1569273-07-9 C₂₀H₁₄FNO 
• 1569273-11-5 C₂₀H₂₁NO₂ 
• 1569273-12-6 C₂₀H₂₁NO₂ 
• 1569273-01-3 C₁₉H₁₂FNO₂ 
• 1569273-04-6 C₁₉H₁₉NO₃ 
• 1569273-05-7 C₁₉H₁₉NO₃ 

Relevant academic research and scientific papers

BENZOISOQUINOLINONE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS

The present invention is directed to substituted benzoisoquinolinone compounds, their salts, pharmaceutical compositions comprising them and their use in therapy. In particular, the invention is directed substituted benzoisoquinolinone compounds which are muscarinic M1 receptor positive allosteric modulators. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M1 receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M1 receptors are involved.

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.

3,4,5-Trimethylphenol and Lewis Acid Dual-Catalyzed Cascade Ring-Opening/Cyclization: Direct Synthesis of Naphthalenes

A 3,4,5-trimethylphenol and Lewis acid dual-catalyzed cascade reaction of donor-acceptor (D-A) cyclopropanes via ring-opening and cyclization is developed. In this reaction, a phenolic compound was used as a covalent catalyst for the first time. Additiona

M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS AND METHODS OF USE THEREOF

The present invention is directed to compounds of general formula (I) or pharmaceutically acceptable salts thereof, 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, or pharmaceutically acceptable salts thereof, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.

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.

Mechanism of alkoxy groups substitution by Grignard reagents on aromatic rings and experimental verification of theoretical predictions of anomalous reactions

The mechanism of direct displacement of alkoxy groups in vinylogous and aromatic esters by Grignard reagents, a reaction that is not observed with expectedly better tosyloxy leaving groups, is elucidated computationally. The mechanism of this reaction has been determined to proceed through the inner-sphere attack of nucleophilic alkyl groups from magnesium to the reacting carbons via a metalaoxetane transition state. The formation of a strong magnesium chelate with the reacting alkoxy and carbonyl groups dictates the observed reactivity and selectivity. The influence of ester, ketone, and aldehyde substituents was investigated. In some cases, the calculations predicted the formation of products different than those previously reported; these predictions were then verified experimentally. The importance of studying the actual system, and not simplified models as computational systems, is demonstrated.

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.