87394-63-6Relevant academic research and scientific papers
ACID ADDITION SALTS OF PIPERAZINE DERIVATIVES
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Page/Page column 37, (2017/09/09)
The invention relates to acid addition salts of piperazine derivatives, as well as solid forms, such as polymorphic forms, thereof, which are useful as pharmaceutical ingredients and in particular as glycosidase inhibitors.
GLYCOSIDASE INHIBITORS
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Page/Page column 101, (2016/03/22)
Compounds of formula (I) wherein A, R, W, Q, n and m have the meaning according to the claims can be employed, inter alia, for the treatment of tauopathies and Alzheimer's disease.
COMPOUNDS AS TRVP1 BLOCKERS, PHARMACEUTICAL COMPOSITIONS AND MEDICAL USES THEREOF
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Page/Page column 25, (2012/07/28)
A kind of new compounds, and their pharmaceutically acceptable salts, and hydrates are disclosed. The pharmaceutical composition thereof is also provided. And also are the medical uses of the compounds, pharmaceutically acceptable salts, hydrates and the
Synthesis and biological evaluation of piperazinyl carbamates and ureas as fatty acid amide hydrolase (FAAH) and transient receptor potential (TRP) channel dual ligands
Morera, Enrico,De Petrocellis, Luciano,Morera, Ludovica,Moriello, Aniello Schiano,Ligresti, Alessia,Nalli, Marianna,Woodward, David F.,Di Marzo, Vincenzo,Ortar, Giorgio
scheme or table, p. 6806 - 6809 (2010/06/12)
The evaluation of a series of piperazinyl carbamates and ureas, designed on the basis of previously reported TRPV1 antagonists and FAAH inhibitors, led to the identification of some 'dual-action' compounds targeting both FAAH and TRPV1 or TRPA1 receptors.
Piperazine sulfonamides as potent, selective, and orally available 11β-hydroxysteroid dehydrogenase type 1 inhibitors with efficacy in the rat cortisone-induced hyperinsulinemia model
Xiang, Jason,Wan, Zhao-Kui,Li, Huan-Qiu,Ipek, Manus,Binnun, Eva,Nunez, Jill,Chen, Lihren,McKew, John C.,Mansour, Tarek S.,Xu, Xin,Suri, Vipin,Tam, May,Xing, Yuzhe,Li, Xiangping,Hahm, Seung,Tobin, James,Saiah, Eddine
supporting information; experimental part, p. 4068 - 4071 (2009/05/30)
11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) is the enzyme that converts cortisone to cortisol. Evidence suggests that selective inhibition of 11β-HSD1 could treat diabetes and metabolic syndrome. Presented herein are the synthesis, structure-activity relationship, and in vivo evaluation of piperazine sulfonamides as 11β-HSD1 inhibitors. Through modification of our initial lead 5a, we have identified potent and selective 11β-HSD1 inhibitors such as 13q and 13u with good pharmacokinetic properties.
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).
11-BETA HSD1 INHIBITORS
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Page/Page column 95, (2008/06/13)
This invention relates to inhibiting 11βHSD1.
1,4-DISUBSTITUTED PIPERAZINE AND 1,4-DISUBSTITUTED AZEPANE AS 11 -BETA-HYDROXYSTEROID DEHYDROGENASE 1 INHIBITORS
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Page/Page column 32-33, (2010/11/29)
Compounds of formula (I): wherein variable groups are defined within; their use in the inhibition of 11βHSD1, processes for making them and pharmaceutical compositions comprising them are described.
DIAZA HETEROCYCLIC SULFONAMIDE DERIVATIVES AND THEIR USES
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Page/Page column 64, (2008/06/13)
Diaza heterocyclic sulfonamide derivatives according to formula I have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders: I where R7, R8, R9, R10, R11, R12, R13, X, Y1, Y2, m, and n are set forth in the description.
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
