67092-18-6Relevant academic research and scientific papers
OCTAHYDROPYRROLO [3, 4-c] PYRROLE DERIVATIVES AND USES THEREOF
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Paragraph 00215; 00221, (2017/07/04)
The invention relates to octahydropyrrolo [3, 4-c] pyrrole derivatives and uses thereof. Compounds and pharmaceutical compositions comprising the compounds provided herein are used for antagonizing orexin receptors. The invention also relates to processes for preparing the compounds and pharmaceutical compositions, and uses thereof in treating or preventing a disease related to orexin receptors.
Substituted piperazine compounds, application method and applications thereof
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Paragraph 0206; 0207; 0208; 0209; 0277; 0278; 0279, (2016/10/09)
The invention discloses substituted piperazine compounds, an application method and applications thereof. Specifically, the invention relates to piperazine compounds and pharmaceutical compositions thereof for inhibiting reuptake of 5-hydroxytryptamine and/or stimulation of 5-HT1A acceptor. The invention also relates to a preparation method of the compounds and pharmaceutical compositions thereof, and an application of the compounds and pharmaceutical compositions thereof in the treatment of central nervous system dysfunction.
Design, synthesis, and structure-activity relationships of highly potent 5-HT3 receptor ligands
Verheij, Mark H. P.,Thompson, Andrew J.,Van Muijlwijk-Koezen, Jacqueline E.,Lummis, Sarah C. R.,Leurs, Rob,De Esch, Iwan J. P.
, p. 8603 - 8614 (2013/01/15)
The 5-HT3 receptor, a pentameric ligand-gated ion channel (pLGIC), is an important therapeutic target. During a recent fragment screen, 6-chloro-N-methyl-2-(4-methyl-1,4-diazepan-1-yl)quinazolin-4-amine (1) was identified as a 5-HT3R hit fragment. Here we describe the synthesis and structure-activity relationships (SAR) of a series of (iso)quinoline and quinazoline compounds that were synthesized and screened for 5-HT3R affinity using a [3H]granisetron displacement assay. These studies resulted in the discovery of several high affinity ligands of which compound 22 showed the highest affinity (pKi > 10) for the 5-HT3 receptor. The observed SAR is in agreement with established pharmacophore models for 5-HT3 ligands and is used for ligand-receptor binding mode prediction using homology modeling and in silico docking approaches.
NITROGEN HETEROCYCLIC COMPOUNDS USEFUL AS PDE10 INHIBITORS
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Page/Page column 185, (2011/12/02)
Unsaturated nitrogen heterocyclic compounds of formula (I): (I), as defined in the specification, compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, Huntington's Disease, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
Pyri(mi)dyl-oxy-and -thio-benzoic acid derivatives useful as herbicides and plant growth regulants
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, (2008/06/13)
New pyri(mi)dyl-oxy- or -thio-benzoic acid derivatives of the formula STR1 are taught which have herbicidal and plant growth regulating activity. In the formula Z can be Ch or N, X is oxygen or sulphur, A is oxygen, sulphur, a radical R5 --N=or a radical R6 O--N=and B is oxygen, sulphur, a radical STR2 with the proviso that at least one of the radicals R1, R2 or R3 represents alkyl or a part of a 3- to 6-membered fused carbocyclic ring.
Heterocyclic compounds
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, (2008/06/13)
The use of compounds of formula (IIA) where R3 is halogen, CF3 or methyl, R4′is methyl or ethyl; and, R5′is OR6 or -NHSO2R7 wherein R6 is hydrogen, optionally substituted C1
