913613-99-7Relevant academic research and scientific papers
Preparation method of amide-like derivative and intermediate thereof
-
, (2020/07/12)
The invention discloses a preparation method of an amide-like derivative and an intermediate thereof. The invention provides a preparation method of a compound as shown in a formula VI and an intermediate thereof, the compound as shown in the formula VI c
Amide-like derivative impurity and application thereof
-
, (2020/07/12)
The invention relates to an amide-like derivative impurity and application thereof. The invention belongs to the field of medical chemistry, and particularly relates to an impurity A, an impurity B, an impurity G, a preparation method thereof, and applica
Isoquinolinone derivatives as potent CNS multi-receptor D2/5-HT1A/5-HT2A/5-HT6/5-HT7 agents: Synthesis and pharmacological evaluation
Cao, Xudong,Chen, Yin,Dou, Fei,Gao, Lanchang,Hao, Chao,Jin, Jian,Liu, Bi-Feng,Liu, Xin,Xiong, Jiaying,Zhang, Guisen,Zhang, Kunxiao,Zhang, Yifang
, (2020/09/02)
In this study, a series of novel Isoquinolinone derivatives were synthesized as potential multi-target antipsychotics. Among these, compound 13 showed high affinity for dopamine D2 and serotonin 5-HT1A, 5-HT2A, 5-HT6, and 5-HT7 receptors, showed low affinity for off-target receptors (5-HT2C, H1, and α1), and negligible effects on ether-a-gogo-related gene (hERG; i.e., reduced QT interval prolongation). An animal behavioral study revealed that compound 13 reversed APO-induced hyperlocomotion, MK-801-induced hyperactivity, and DOI-induced head twitch. Moreover, compound 13 exhibited a high threshold for acute toxicity, a lack of tendency to induce catalepsy, and did not cause prolactin secretion or weight gain when compared to risperidone. Furthermore, in the forced swim test, tail suspension test, and novel object recognition test, treatment with compound 13 resulted in improvements in depression and cognitive impairment. In addition, compound 13 had a favorable pharmacokinetic profile in rats. Thus, the antipsychotic drug-like effects of compound 13 indicate that it may be useful for developing a novel class of drugs for the treatment of schizophrenia.
Synthesis and evaluation of histamine H3 receptor ligand based on lactam scaffold as agents for treating neuropathic pain
Dou, Fei,Cao, Xudong,Jing, Peng,Wu, Chunyan,Zhang, Yuxin,Chen, Yin,Zhang, Guisen
, p. 1492 - 1496 (2019/04/14)
The synthesis and H3 receptor ligand of a new series of lactam derivatives are reported. The new compounds were evaluated in vitro in H3 and H1 receptor-binding assays. The structure-activity relationship led us to the pro
LACTAM COMPOUND DERIVATIVE AND APPLICATION THEREOF
-
, (2018/10/15)
The present invention relates to a lactam compound derivative, a medicine composition comprising the lactam compound derivative, and uses of the composition and the lactam compound derivative in preparation of a medicine for preventing or treating schizop
Lactam derivative and application thereof
-
, (2017/09/01)
The invention relates to a lactam derivative and application thereof. Particularly, a related lactam compound can act on an H3 receptor for treating diseases such as epilepsy, schizophrenia, senile dementia, sleep disorders, obesity, neuralgia and attenti
NOVEL MONOAMINE RE-UPTAKE INHIBITOR
-
, (2009/10/22)
The present invention relates to novel compounds of Formula (I), their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers including R and S isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also rel
PIPERAZINE-SUBSTITUTED BENZOTHIOPHENES FOR TREATMENT OF MENTAL DISORDERS
-
Page/Page column 58, (2010/11/24)
The present invention provides a heterocyclic compound represented by the general formula (1): The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.
