104396-10-3Relevant academic research and scientific papers
Substituted indole compound and method and use thereof
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Paragraph 0327; 0328; 0494; 0496; 0497, (2018/11/03)
The invention provides a new indole compound, pharmaceutically acceptable salts and medicinal preparations thereof, and a use of the new indole compound in selective inhibition of 5-hydroxytryptamine reuptake and /or excitation of a 5-HT1A receptor. The invention also relates to medicinal compositions comprising the compounds, and a method for treating the central nervous system dysfunction of mammals, especially humans by using the medicinal compositions.
COMPOUNDS AS ASIC INHIBITORS AND USES THEREOF
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Paragraph 00240, (2017/04/11)
The present invention relates to compounds, and pharmaceutically acceptable compositions thereof, useful as ASIC inhibitors.
Discovery and Initial SAR of Arylsulfonylpiperazine Inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1)
Sun, Daqing,Wang, Zhulun,Di, Yongmei,Jaen, Juan C.,Labelle, Marc,Ma, Ji,Miao, Shichang,Sudom, Athena,Tang, Liang,Tomooka, Craig S.,Tu, Hua,Ursu, Stefania,Walker, Nigel,Yan, Xuelei,Ye, Qiuping,Powers, Jay P.
scheme or table, p. 3513 - 3516 (2009/04/11)
High-throughput screening of a small-molecule compound library resulted in the identification of a series of arylsulfonylpiperazines that are potent and selective inhibitors of human 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1). Optimization of the initial lead resulted in the discovery of compound (R)-45 (11β-HSD1 IC50 = 3 nM).
Identification and biological evaluation of 4-(3-trifluoromethylpyridin-2- yl)piperazine-1-carboxylic acid (5-trifluoromethylpyridin-2-yl)amide, a high affinity TRPV1 (VR1) vanilloid receptor antagonist
Swanson, Devin M.,Dubin, Adrienne E.,Shah, Chandra,Nasser, Nadia,Chang, Leon,Dax, Scott L.,Jetter, Michele,Breitenbucher, J. Guy,Liu, Changlu,Mazur, Curt,Lord, Brian,Gonzales, Lisa,Hoey, Kenway,Rizzolio, Michele,Bogenstaetter, Michael,Codd, Ellen E.,Lee, Doo H.,Zhang, Sui-Po,Chaplan, Sandra R.,Carruthers, Nicholas I.
, p. 1857 - 1872 (2007/10/03)
High throughput screening using the recombinant human TRPV1 receptor was used to identify a series of pyridinylpiperazine ureas (3) as TRPV1 vanilloid receptor ligands. Exploration of the structure-activity relationships by parallel synthesis identified t
Acetamides and benzamides that are useful in treating sexual dysfunction
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, (2008/06/13)
The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction.
4-(2-Pyridyl)piperazine-1-carboxamides: Potent vanilloid receptor 1 antagonists
Sun, Qun,Tafesse, Laykea,Islam, Khondaker,Zhou, Xiaoming,Victory, Sam F.,Zhang, Chongwu,Hachicha, Mohamed,Schmid, Lori A.,Patel, Aniket,Rotshteyn, Yakov,Valenzano, Kenneth J.,Kyle, Donald J.
, p. 3611 - 3616 (2007/10/03)
A series of 4-(2-pyridyl)piperazine-1-carboxamide analogues based on the lead compound 1 was synthesized and evaluated for VR1 antagonist activity in capsaicin-induced (CAP) and pH (5.5)-induced (pH) FLIPR assays in a rat VR1-expressing HEK293 cell line. Potent VR1 antagonists were identified through SAR studies. From these studies, 18 was found to be very potent in the in vitro assay [IC50=4.8 nM (pH) and 35 nM (CAP)] and orally available in rat (F%=15.1).
Acetamides and benzamides that are useful in treating sexual dysfunction
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Page 98-99, (2008/06/13)
The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction.
Atypical Antipsychotic Agents: Patterns of Activity in a Series of 3-Substituted 2-Pyridinyl-1-piperazine Derivatives
New, James S.,Yevich, Joseph P.,Temple, Davis L.,New, Kimberly B.,Gross, Sharon M.,et al.
, p. 618 - 624 (2007/10/02)
A series of 3-substituted 2-pyridinyl-1-piperazine derivaties have been appended to cyclic imide groups and evaluated for their potential antipsochotic activity.The dopamine receptor affinities of these target molecules, as well as their ability to block apomorphine-induced stereotypy or reverse neuroleptic-induced catalepsy, was dependent on the lipophilic and electronic characteristics of the substituent situated on the pyridine ring.Groups with +? and -? values were most consistent with the desired biological profile of the target molecules, the cyano moiety being the optimum choice.Evaluation of compound 12 in a monkey model of amphetamine psychosis, and the regional selectivity it expresses for the A10 dopaminergic cell bodies in electrophysiological experiments, suggest this compound would be an atypical antipsychotic agent with few side effects.
ANTIPSYCHOTIC CYCLIC IMIDE DERIVATIVES OF 2-(4-BUTYLPIPERAZIN-1-YL) PYRIDINES, COMPOSITIONS AND USE
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, (2008/06/13)
Disubstituted N,N-piperazinyl derivatives are disclosed wherein one substituent is a substituted pyridin-2-yl ring and the second substituent is a butylene chain attached to cyclic imide heterocycles such as azaspiro 4.5!decanedione, dialkylglutarimide, thiazolidinedione, spirocyclopentylthiazolidinedione, or morpholine-2,6-dione. The compounds have psychotropic properties and 2-4-4-(2,4-dioxo-1-thia-3-azaspiro 4. 5!nonane-3-yl)butyl!-1-piperazinyl!-pyridine-3-carboxaldehyde is a typical embodiment having selective antipsychotic activity.
ANTIPSYCHOTIC CYCLIC IMIDE DERIVATIVES OF 2-(4-BUTYLPIPERAZIN-1-YL)PYRIDINES, COMPOSITIONS AND USE
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, (2008/06/13)
Disubstituted N,N-piperazinyl derivatives are disclosed wherein one substituent is a substituted pyridin-2-yl ring and the second substituent is a butylene chain attached to cyclic imide heterocycles such as azaspiro 4.5!decanedione, dialkylglutarimide, thiazolidinedione, spirocyclopentylthiazolidinedione, or morpholine-2,6-dione. The compounds have psychotropic properties and 2-4-4-(2,4-dioxo-1-thia-3-azaspiro 4. 5!nonane-3-yl)butyl!-1-piperazinyl!pyridine-3-carboxaldehyde is a typical embodiment having selective antipsychotic activity.
