- TYK2 INHIBITORS AND USES THEREOF
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Described herein are compounds that are useful in treating a TYK2-mediated disorder. In some embodiments, the TYK2-mediated disorder is an autoimmune disorder, an inflammatory disorder, a proliferative disorder, an endocrine disorder, a neurological disorder, or a disorder associated with transplantation.
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- Efficient synthesis of NIR emitting bis[2-(2′-hydroxylphenyl)benzoxazole] derivative and its potential for imaging applications
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Unassymetric bis[2-(2′-hydroxyphenylbenzoxole)] bis(HBO) derivatives with a DPA functionality for zinc binding have been developed with an efficient synthetic route, using the retrosynthetic analysis. Comparison of bis(HBO) derivatives with different substitution patterns allows us to verify and optimize their unique fluorescence properties. Upon binding zinc cation, bis(HBO) derivatives give a large fluorescence turn-on in both visible (λem ≈ 536 nm) and near-infrared (NIR) window (λem ≈ 746 nm). The probes are readily excitable by a 488 nm laser, making this series of compounds a suitable imaging tool for in vitro and in vivo study on a confocal microscope. The application of zinc binding-induced fluorescence turn-on is successfully demonstrated in cellular environments and thrombus imaging.
- Wang, Junfeng,Baumann, Hannah,Bi, Xiaoman,Shriver, Leah P.,Zhang, Zhaoda,Pang, Yi
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supporting information
(2020/01/25)
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- CLASS OF NEAR INFRARED MOLECULAR PROBES FOR BIOLOGICAL APPLICATIONS
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Methods for preparing 2,5-Bis(benzoxazol-2′-yl)benzene-1,4-diol derivatives (Zinhbo derivatives) are provided. Zinhbo derivatives are used to detect zinc ions and have particular application in vivo and in vitro. Zinhbo derivatives upon excitation give a florescence response emission that can be used to determine the presence of zinc cation in solution. Zinhbo derivatives complexed with zinc cations upon excitation can produce a florescence response emission in the visible and near infrared range. Zinhbo derivatives complexed with zinc cations exhibit a large stoke shift between the excitation and emission wavelengths.
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Paragraph 0088
(2014/10/16)
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- Rh2(II)-catalyzed selective aminomethylene migration from styryl azides
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Rh2(II)-Carboxylate complexes were discovered to promote the selective migration of aminomethylenes in β,β-disubstituted styryl azides to form 2,3-disubstituted indoles. Mechanistic data are also presented that suggest that the migration occurs stepwise before diffusion of the iminium ion.
- Kong, Chen,Jana, Navendu,Driver, Tom G.
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p. 824 - 827
(2013/03/29)
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- Discovery of novel phosphonic acid derivatives as new chemical leads for inhibitors of TNF-α production
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2-(Acylamino)benzylphosphonic acid 6 derived from an artificial substrate of sphingomyelinase was found to show inhibitory activity of TNF-α production. Structural optimization was started with the chemical modification of 6. The discovery of another chem
- Matsui, Toshiaki,Takahashi, Shinya,Matsunaga, Naoki,Nakamura, Kazunori,Omawari, Nagashige,Sakai, Masaru,Kamoshima, Wataru,Terai, Kouichiro,Ohno, Hiroyuki,Obata, Takaaki,Nakai, Hisao,Toda, Masaaki
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p. 3807 - 3815
(2007/10/03)
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- Structure-activity relationship of a series of phenylureas linked to 4- phenylimidazole. Novel potent inhibitors of acyl-CoA:cholesterol O- acyltransferase with antiatherosclerotic activity. 2
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In our continuing search to find systemically bioavailable ACAT (acyl- CoA:cholesterol O-acyl-transferase) inhibitors with more potent antiatherosclerotic effect than N-[2-(dimethylamino)-6-[3-(5-methyl-4- phenyl-1H-imidazol-1-yl)propoxy]phenyl]-N'-pentyl
- Kimura,Watanabe,Matsui,Hayashi,Tanaka,Ohtsuka,Saeki,Kogushi,Kabayashi,Akasaka,Yamagishi,Saitou,Yamatsu
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p. 1641 - 1653
(2007/10/02)
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