- COMPOUNDS FOR THE TREATMENT OF INFLAMMATORY DISORDERS
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This invention relates to compounds of the Formula (I)-(IX):, as defined herein, or a pharmaceutically acceptable salt, solvate or ester thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, T
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- A photocaged, cyclopropene-containing analog of the amino acid neurotransmitter glutamate
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Substituted cyclopropenes serve as compact biorthogonal appendages that enable analysis of biomolecules in complex systems. Neurotransmitters, a chemically diverse group of biomolecules that control neuron excitation and inhibition, are not among the systems that have been studied using biorthogonal chemistry. Here we describe the synthesis of cyclopropene-containing analogs of the excitatory amino acid neurotransmitter glutamate starting from a Garner's aldehyde-derived alkyne. The deprotected cyclopropene glutamate was stable in solution but decomposed upon concentration. Appending a light-cleavable group improved the stability of the cyclopropene while simultaneously caging the neurotransmitter. This strategy has the potential to permit deployment of cyclopropene-modified glutamate as a bioorthogonal probe of the neurotransmitter glutamate in vivo with spatiotemporal precision.
- Kumar, Pratik,Shukhman, David,Laughlin, Scott T.
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p. 5750 - 5752
(2016/12/03)
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- COMPOUNDS FOR THE TREATMENT OF INFLAMMATORY DISORDERS
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This invention relates to compounds of the Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.
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Page/Page column 102-103
(2010/06/11)
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- Novel TNF-α converting enzyme (TACE) inhibitors as potential treatment for inflammatory diseases
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Our research on hydantoin based TNF-α converting enzyme (TACE) inhibitors has led to an acetylene containing series that demonstrates sub-nanomolar potency (Ki) as well as excellent activity in human whole blood. These studies led to the discov
- Girijavallabhan, Vinay M.,Chen, Lei,Dai, Chaoyang,Feltz, Robert J.,Firmansjah, Luke,Li, Dansu,Kim, Seong Heon,Kozlowski, Joseph A.,Lavey, Brian J.,Kosinski, Aneta,Piwinski, John J.,Popovici-Muller, Janeta,Rizvi, Razia,Rosner, Kristin E.,Shankar, Banderpalle B.,Shih, Neng-Yang,Siddiqui, M. Arshad,Tong, Ling,Wong, Michael K.C.,Yang, De-Yi,Yang, Liping,Yu, Wensheng,Zhou, Guowei,Guo, Zhuyan,Orth, Peter,Madison, Vincent,Bian, Hong,Lundell, Daniel,Niu, Xiaoda,Shah, Himanshu,Sun, Jing,Umland, Shelby
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scheme or table
p. 7283 - 7287
(2011/02/21)
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- HYDANTOIN DERIVATIVES FOR THE TREATMENT OF INFLAMMATORY DISORDERS
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This invention relates to compounds of the Formula: (I); or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF-α or combinations thereof.
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