- ACID ADDITION SALTS OF PIPERAZINE DERIVATIVES
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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.
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Page/Page column 37
(2017/09/09)
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- GLYCOSIDASE INHIBITORS
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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.
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Page/Page column 101
(2016/03/22)
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- COMPOUNDS AS TRVP1 BLOCKERS, PHARMACEUTICAL COMPOSITIONS AND MEDICAL USES THEREOF
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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
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Page/Page column 25
(2012/07/28)
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- Synthesis and biological evaluation of piperazinyl carbamates and ureas as fatty acid amide hydrolase (FAAH) and transient receptor potential (TRP) channel dual ligands
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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.
- Morera, Enrico,De Petrocellis, Luciano,Morera, Ludovica,Moriello, Aniello Schiano,Ligresti, Alessia,Nalli, Marianna,Woodward, David F.,Di Marzo, Vincenzo,Ortar, Giorgio
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scheme or table
p. 6806 - 6809
(2010/06/12)
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- Piperazine sulfonamides as potent, selective, and orally available 11β-hydroxysteroid dehydrogenase type 1 inhibitors with efficacy in the rat cortisone-induced hyperinsulinemia model
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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.
- 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
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supporting information; experimental part
p. 4068 - 4071
(2009/05/30)
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- Discovery and Initial SAR of Arylsulfonylpiperazine Inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1)
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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).
- 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.
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scheme or table
p. 3513 - 3516
(2009/04/11)
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- 11-BETA HSD1 INHIBITORS
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This invention relates to inhibiting 11βHSD1.
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Page/Page column 95
(2008/06/13)
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- 1,4-DISUBSTITUTED PIPERAZINE AND 1,4-DISUBSTITUTED AZEPANE AS 11 -BETA-HYDROXYSTEROID DEHYDROGENASE 1 INHIBITORS
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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.
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Page/Page column 32-33
(2010/11/29)
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- DIAZA HETEROCYCLIC SULFONAMIDE DERIVATIVES AND THEIR USES
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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.
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Page/Page column 64
(2008/06/13)
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- 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
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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
- 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.
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p. 1857 - 1872
(2007/10/03)
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- PYRIDYL PIPERAZINYL UREAS
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There are disclosed novel pyridyl piperazinyl ureas that are potent antagonists of vanilloid receptor, VR1, and are useful for the treatment and/or prevention of i) acute or chronic pain or itch; ii) inflammation; iii) gastrointestinal and urinary tract disorders; and iv) tracheobronchial and diaphragmatic dysfunction in humans.
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Page/Page column 20
(2008/06/13)
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- Acetamides and benzamides that are useful in treating sexual dysfunction
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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.
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- Acetamides and benzamides that are useful in treating sexual dysfunction
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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.
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- 4-(2-Pyridyl)piperazine-1-carboxamides: Potent vanilloid receptor 1 antagonists
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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).
- 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.
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p. 3611 - 3616
(2007/10/03)
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- 1-indolyalkyl-4-(substituted-pyridinyl)piperazines
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A series of 1,4-disubstituted piperazine derivatives comprised of indol-3-ylalkyl and substituted pyridin-2-yl substituent groups. These compounds are useful as antidepressant agents.
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- Pyridinylpiperazines, a new class of selective α2-adrenoceptor antagonists
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A series of 1-(2-pyridinyl)piperazine derivatives was synthesized and evaluated for adrenergic activity. In vitro activity was assessed through the antagonism of clonidine's effect in the rat, isolated, field-stimulated vas deferens and by the displacemen
- Saari, Walfred S.,Halczenko, Wasyl,King, Stella W.,Huff, Joel R.,Guare, James P.,et al.
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p. 1696 - 1701
(2007/10/02)
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