846057-27-0Relevant articles and documents
PYRAZOLO[1,5-A]PYRIMIDINE DERIVATIVES HAVING MULTIMODAL ACTIVITY AGAINST PAIN
-
Page/Page column 213; 215, (2021/12/08)
The present invention relates to pyrazolopyrimidine derivatives having dual pharmacological activity towards both the α2δ subunit of the voltage-gated calcium channel and the sigma-1 (σ1) receptor, to processes of preparation of such compounds,
N-ACYL-{4-[(4-ARYL-PHENYL)SULFONYLMETHYL]PIPERIDINE} COMPOUNDS AND THEIR THERAPEUTIC USE
-
Page/Page column 83; 84, (2020/10/28)
The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain N-acyl-{4-[(4-aryl- phenyl)sulfonylmethyl]piperidine} compounds of the following formula (collectively referred to
Discovery and SAR of N-(1-((substituted piperidin-4-yl)methyl)-3-methoxypiperidin-4-yl)-2-methoxybenzamide derivatives: 5-Hydroxytryptamine receptor 4 agonist as a potent prokinetic agent
Park, Jung Sang,Im, Weonbin,Choi, Sunghak,Park, Sook Jin,Jung, Jun Min,Baek, Ki Seon,Son, Han Pyo,Sharma, Satyasheel,Kim, In Su,Jung, Young Hoon
, p. 75 - 88 (2016/01/09)
A series of novel benzamide derivatives, altering the 4-fluorophenylalkyl moiety in cisapride, were synthesized as 5-HT4 receptor agonists, and SAR of these analogs was examined on in vitro and in vivo prokinetic activities. These compounds were synthesized for high 5-HT4 receptor binding affinities and low hERG affinities. Several types of analogs were obtained and screened for 5-HT4 binding, hERG blocking, agonism, and gastric emptying assessment. Among the analogues, compound 23g showed promising results compared with the other analogs with respect to gastric emptying rates in rats. Therefore, we suggest that it may be a clinical candidate for the development of a potent prokinetic agent to treat GI disorders.