952151-39-2Relevant articles and documents
Heterocyclic Compound
-
Paragraph 1953; 1954, (2018/06/15)
The present invention provide a compound having an orexin receptor antagonistic activity, which is expected to be useful as medicaments such as agents for the prophylaxis or treatment of sleep disorder, depression, anxiety disorder, panic disorder, schizophrenia, drug dependence, Alzheimer's disease and the like. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.
Synthesis and application of [1,2,5]triazepane and [1,2,5]oxadiazepane as versatile structural units for drug discovery
Suzuki, Hideyuki,Utsunomiya, Iwao,Shudo, Koichi
scheme or table, p. 1001 - 1002 (2010/09/17)
Seven-membered heterocyclic [1,2,5]triazepane and [1,2,5]-oxadiazepane derivatives were synthesized as candidate structures for application in drug discovery in place of conventional piperazine or morpholine moieties, offering multiple sites for modification with functional groups. We first synthesized the Nprotected heterocycles, and then confirmed their utility by synthesizing analogues of the oxazolidinone antibacterial agent linezolid. The analogues exhibited potent in vitro and in vivo antibacterial activity. In particular, compound 10a exhibited good in vivo efficacy when administered intravenously in a murine model of systemic infection with methicillin-resistant Staphylococcus aureus SR3637. These seven-membered heterocycles are expected to be versatile structural units for drug discovery.