- CHEMOKING RECEPTOR ANTAGONISTS
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Disclosed herein are chemokine receptor antagonists of formula (I) wherein G1, X1, X2, and X3 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.
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Page/Page column 220
(2013/03/26)
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- Overcoming hERG activity in the discovery of a series of 4-azetidinyl-1-aryl-cyclohexanes as CCR2 antagonists
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A series of 4-azetidinyl-1-aryl-cyclohexanes as potent CCR2 antagonists with high selectivity over activity for the hERG potassium channel is discovered through divergent SARs of CCR2 and hERG.
- Zhang, Xuqing,Hufnagel, Heather,Markotan, Thomas,Lanter, James,Cai, Chaozhong,Hou, Cuifen,Singer, Monica,Opas, Evan,McKenney, Sandra,Crysler, Carl,Johnson, Dana,Sui, Zhihua
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supporting information; experimental part
p. 5577 - 5582
(2011/10/09)
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- Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2
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Rational design based on a pharmacophore of CCR2 antagonists reported in the literature identified lead compound 9a with potent inhibitory activity against human CCR2 (hCCR2) but moderate activity against murine CCR2 (mCCR2). Modification on 9a led to the
- Xue, Chu-Biao,Wang, Anlai,Meloni, David,Zhang, Ke,Kong, Ling,Feng, Hao,Glenn, Joseph,Huang, Taisheng,Zhang, Yingxin,Cao, Ganfeng,Anand, Rajan,Zheng, Changsheng,Xia, Michael,Han, Qi,Robinson,Storace, Lou,Shao, Lixin,Li, Mei,Brodmerkel, Carrie M.,Covington, Maryanne,Scherle, Peggy,Diamond, Sharon,Yeleswaram, Swamy,Vaddi, Kris,Newton, Robert,Hollis, Greg,Friedman, Steven,Metcalf, Brian
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experimental part
p. 7473 - 7478
(2011/01/12)
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- 4-AZETIDINYL-1-PHENYL-CYCLOHEXANE ANTAGONISTS OF CCR2
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The present invention comprises compounds of Formula (I): wherein: X, R1, R2, R3, and R4 are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).
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Page/Page column 44
(2010/11/03)
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- Development of a presynaptic 5-HT1A antagonist.
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A new 5-HT(1A) silent antagonist 14 (5-HT(1A) IC(50)=2.2 nM) antagonizes the effects of agonists on reciprocal forepaw treading behavior, on neuronal firing in the rat dorsal raphe, and on 5-HT(1A) release in the raphe and hippocampus. While 14 alone was inactive in the social interaction paradigm, it completely reversed the social interaction activity of the serotonergic compounds (buspirone, 1, and 2).
- Mattson, Ronald J,Catt, John D,Sloan, Charles P,Gao,Carter, Richard B,Gentile, Anthony,Mahle, Cathy D,Matos, F Fatima,McGovern, Rachel,VanderMaelen, Cam P,Yocca, Frank D
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p. 285 - 288
(2007/10/03)
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- Piperazinyl-cyclohexanes and cyclohexenes
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Novel non-dopaminergic antiischemic compounds have Formula I: wherein R=R1 and is independently H, C1-4 alky C1-4 alkoxy, C1-4 trihaloalkyl or halogen, or R and R1 may be taken together to form an -O(CH2)mO- (m=1 or 2); X=a 3-indolyl, phenyl, naphthalenyl or 2-benzothiazolyl residue; n=0, 1, 2 or 3; R2=R3 and is independently H or C1-4 alkyl; and R4=phenyl, 2-thienyl, 2-quinolinyl, 4-pyridinyl or substituted phenyl.
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- PIPERAZINYL-AND PIPERIDINYL-CYCLOHEXANOLS
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Novel piperazinyl-and piperidinyl-cyclohexanols of the following formula are useful as anxiolytic agents and have other psychotropic properties STR1
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- AMINOMETHYL-BENZODIOXANE AND BENZOPYRAN SEROTONERGIC AGENTS
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Certain aminomethyl-benzodioxanes and benzopyrans are useful serotonergic agents. They possess anxiolytic properties with few of the side effects often associated with dopaminergic agents.
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