- Circumventing seizure activity in a series of G protein coupled receptor 119 (GPR119) agonists
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Agonism of GPR119 is viewed as a potential therapeutic approach for the treatment of type II diabetes and other elements of metabolic syndrome. During progression of a previously disclosed candidate 1 through mice toxicity studies, we observed tonic-cloni
- Scott, James S.,Bowker, Suzanne S.,Brocklehurst, Katy J.,Brown, Hayley S.,Clarke, David S.,Easter, Alison,Ertan, Anne,Goldberg, Kristin,Hudson, Julian A.,Kavanagh, Stefan,Laber, David,Leach, Andrew G.,Macfaul, Philip A.,Martin, Elizabeth A.,McKerrecher, Darren,Schofield, Paul,Svensson, Per H.,Teague, Joanne
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supporting information
p. 8984 - 8998
(2015/03/14)
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- Synthesis and Structure-Activity Relationship Studies of Derivatives of the Dual Aromatase-Sulfatase Inhibitor 4-{[(4-Cyanophenyl)(4H-1,2,4-triazol-4-yl)amino]methyl}phenyl sulfamate
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4-{[(4-Cyanophenyl)(4H-1,2,4-triazol-4-yl)amino]methyl}phenyl sulfamate and its ortho-halogenated (F, Cl, Br) derivatives are first-generation dual aromatase and sulfatase inhibitors (DASIs). Structure-activity relationship studies were performed on these
- Woo, L. W. Lawrence,Wood, Paul M.,Bubert, Christian,Thomas, Mark P.,Purohit, Atul,Potter, Barry V. L.
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p. 779 - 799
(2013/08/25)
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- SUBSTITUTED PIPERIDINE DERIVATIVES AND METHODS FOR PREPARING THE SAME
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The present invention relates to a novel compound or a pharmaceutically acceptable salt thereof, a preparation method thereof and a pharmaceutical composition for treating metabolism-related disorder containing the same. Specifically, the present invention relates to a compound of the formula 1, which can activate GPR119 to treat metabolism-related disorders, including diabetes and related diseases, diabetes-related microvascular complications, diabetes-related macrovascular complications, cardiovascular abnormalities, metabolic syndrome and its constituent diseases, and obesity.
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Paragraph 112; 113; 114; 115; 116
(2013/07/25)
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- Electronically modified polymer-supported cinchona phase-transfer catalysts for asymmetric synthesis of α-alkyl-α-amino acid derivatives
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Merrifield resin-supported hydrocinchonidinium salts containing particular functional groups that can participate in hydrogen bonding were prepared and evaluated as chiral phase-transfer catalysts using the asymmetric benzylation of glycine imine ester. These electronically modified Merrifield resin-supported phase-transfer catalysts generally provided better enantioselectivities compared to the unmodified ones. Copyright
- Shi, Qinghua,Lee, Yeon-Ju,Song, Hongrui,Cheng, Maosheng,Jew, Sang-Sup,Park, Hyeung-Geun,Jeong, Byeong-Seon
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p. 436 - 437
(2008/09/20)
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- Fluorinated linkers for monitoring solid-phase synthesis using gel- phase 19F NMR spectroscopy
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Three fluorinated linkers which are analogues of linkers commonly used in solid-phase peptide synthesis have been prepared. Using 19F NMR spectroscopy, the fluorine atom of the linker allowed monitoring of several transformations in the solid-phase synthesis of a peptoid having a coumarin moiety. Especially, attachment of the linker to the solid phase, coupling of the first building block to the linker and cleavage of the product were efficiently monitored and optimised.
- Svensson, Anette,Bergquist, Karl-Erik,Fex, Tomas,Kihlberg, Jan
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p. 7193 - 7196
(2007/10/03)
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