1186229-95-7

Basic information

• Product Name: Lu AE₅₁₀₉₀
• Synonyms: Lu AE₅₁₀₉₀
• CAS NO: 1186229-95-7
• Molecular Weight: 407.513
• Mol File: 1186229-95-7.mol

Chemical Properties

• CAS DataBase Reference: Lu AE₅₁₀₉₀(CAS DataBase Reference)
• NIST Chemistry Reference: Lu AE₅₁₀₉₀(1186229-95-7)
• EPA Substance Registry System: Lu AE₅₁₀₉₀(1186229-95-7)

Safety Data

• Hazardous Substances Data: 1186229-95-7(Hazardous Substances Data)

Upstream product

• 1094435-32-1 4-(3-bromopropyl)-2H-benzo[b][1,4]oxazin-3(4H)-one 
• 73874-95-0 (piperidin-4-yl)carbamic acid tert-butyl ester 
• 5466-88-6 3,4-dihydro-3-oxo-2H-1,4-benzoxazine 
• 1186230-36-3 4-(3-(4-aminopiperidin-1-yl)propyl)-2H-benzo[b][1,4]oxazin-3(4H)-one 
• 103-80-0 phenylacetyl chloride 

Relevant articles and documents

Proof of concept study for designed multiple ligands targeting the dopamine D2, serotonin 5-HT2A, and muscarinic M1 acetylcholine receptors

Herein we describe the hybridization of a benzoxazinone M1 scaffold with D2 privileged structures derived from putative and clinically relevant antipsychotics to develop designed multiple ligands. The M1 mAChR is an attractive target for the cognitive deficits in key CNS disorders. Moreover, activity at D2 and 5-HT2A receptors has proven useful for antipsychotic efficacy. We identified 9 which retained functional activity at the target M1 mAChR and D2R and demonstrated high affinity for the 5-HT2AR.

Discovery of N-{1-[3-(3-Oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl] piperidin-4-yl}-2-phenylacetamide (Lu AE51090): An allosteric muscarinic M 1 receptor agonist with unprecedented selectivity and procognitive potential

The discovery and Structure-activity relationship (SAR) of a series of allosteric muscarinic M1 receptor agonists are described. Compound 17 (Lu AE51090) was identified as a representative compound from the series, based on its high selectivity as an agonist at the muscarinic M1 receptor across a panel of muscarinic receptor subtypes. Furthermore, 17 displayed a high degree of selectivity when tested in a broad panel of G-protein-coupled receptors, ion channels, transporters, and enzymes, and 17 showed an acceptable pharmacokinetic profile and sufficient brain exposure in rodents in order to characterize the compound in vivo. Hence, in a rodent model of learning and memory, 17 reversed delay-induced natural forgetting, suggesting a procognitive potential of 17.

NOVEL HETEROCYCLIC CARBOXAMIDES AS M1 AGONISTS

The present invention relates to novel M1 agonistic compounds of formula (I) and their use in the treatment of cognitive impairment associated i.a. with schizophrenia and in the treatment of other diseases mediated by the muscarinic M1 receptor.