- PROTECTIVE GROUPS AND METHODS FOR PROTECTING BENZOXABOROLES OR OXABOROLES
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The present invention relates in part protective groups that can be used to reversibly protect benzoxaboroles and/or oxaboroles and yield the corresponding protected complexes. The invention further relates to the use of these protective groups to protect benzoxaboroles and/or oxaboroles.
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Page/Page column 35; 36
(2019/10/01)
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- Protection of the Benzoxaborole Moiety: Synthesis and Functionalization of Zwitterionic Benzoxaborole Complexes
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The synthesis and utility of three benzoxaborole protecting groups are reported. These protecting groups improve organic solubility and allow otherwise incompatible reactions (oxidations, substitutions, and mild reductions) to be achieved in the presence of the benzoxaborole moiety. 3-(N,N-Dimethylamino)-1-propanol was determined to be useful in one-step sequences and is readily cleaved upon workup. Two other groups, N-methylsalicylidenimine and 2-[1-(methylimino)ethyl]phenol, are suitable for multistep syntheses. Deprotection with mild aqueous acid allows for chromatography-free isolation of the benzoxaborole in high yields.
- Gamrat, James M.,Mancini, Giulia,Burke, Sarah J.,Colandrea, Rebecca C.,Sadowski, Nicholas R.,Figula, Bryan C.,Tomsho, John W.
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supporting information
p. 6193 - 6201
(2018/05/15)
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- A general method for selective recognition of monosaccharides and oligosaccharides in water
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Molecular recognition of carbohydrates plays vital roles in biology but has been difficult to achieve with synthetic receptors. Through covalent imprinting of carbohydrates in boroxole-functionalized cross-linked micelles, we prepared nanoparticle receptors for a wide variety of mono- and oligosaccharides. The boroxole functional monomer bound the sugar templates through cis-1,2-diol, cis-3,4-diol, and trans-4,6-diol. The protein-sized nanoparticles showed excellent selectivity for daldohexoses in water with submillimolar binding affinities and completely distinguished the three biologically important hexoses (glucose, mannose, and galactose). Glycosides with nonpolar aglycon showed stronger binding due to enhanced hydrophobic interactions. Oligosaccharides were distinguished on the basis of their monosaccharide building blocks, glycosidic linkages, chain length, as well as additional functional groups that could interact with the nanoparticles.
- Gunasekara, Roshan W.,Zhao, Yan
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p. 829 - 835
(2017/05/17)
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- IMMUNE ADJUSTMENT COMPOUND, USE THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
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The present invention provides a compound represented by formula I, wherein R is a halogen element or a C1-C6 alkyl group. The compound has S1 P1 receptor agonist activity and selective specificity and has obviously-shortened half-life in-vivo, and therefore the compound is a high-quality second-generation S1P1 receptor agonist. The present invention also provides a use of the compound in preparing medicine for treating diseases or symptoms mediated by an S1P1 receptor, a pharmaceutical composition comprising the compound, and uses of the compound and the pharmaceutical composition in treating diseases or symptoms mediated by the S1 P1 receptor.
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Paragraph 0081; 0082
(2016/08/29)
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- 2-ARYL SELENAZOLE COMPOUND AND PHARMACEUTICAL COMPOSITION THEREOF
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Disclosed are a 2-aryl selenazole compound and a pharmaceutical composition thereof, where the 2-aryl selenazole compound is a compound represented by formula (I) or a pharmaceutically acceptable salt thereof. The 2-aryl selenazole compound has the activi
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- COMPOSITIONS, METHODS, AND SYSTEMS FOR THE SYNTHESIS AND USE OF IMAGING AGENTS
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The present invention relates to systems, compositions, and methods for the synthesis and use of imaging agents, or precursors thereof. An imaging agent precursor may be converted to an imaging agent using the methods described herein. In some cases, the
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- Monosaccharide-responsive release of insulin from polymersomes of polyboroxole block copolymers at neutral pH
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We synthesized a boroxole-containing styrenic monomer that can be polymerized by the reversible addition-fragmentation and chain transfer (RAFT) method. Poly(styreneboroxole) (PBOx) and its block copolymers with a poly(ethylene glycol) (PEG) as a hydrophi
- Kim, Hyunkyu,Kang, Young Ji,Kang, Sebyung,Kim, Kyoung Taek
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supporting information; experimental part
p. 4030 - 4033
(2012/04/10)
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- BORON-CONTAINING SMALL MOLECULES AS ANTIPROTOZOAL AGENTS
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This invention provides novel compounds of the following formula useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.
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Page/Page column 102
(2011/04/13)
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- Synthesis and biological evaluations of P4-benzoxaborole-substituted macrocyclic inhibitors of HCV NS3 protease
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We disclose here a series of P4-benzoxaborole-substituted macrocyclic HCV protease inhibitors. These inhibitors are potent against HCV NS3 protease, their anti-HCV replicon potencies are largely impacted by substitutions on benzoxaborole ring system and P2 groups. P2 2-thiazole-isoquinoline provides best replicon potency. The in vitro SAR studies and in vivo PK evaluations of selected compounds are described herein.
- Ding, Charles Z.,Zhang, Yong-Kang,Li, Xianfeng,Liu, Yang,Zhang, Suoming,Zhou, Yasheen,Plattner, Jacob J.,Baker, Stephen J.,Liu, Liang,Duan, Maosheng,Jarvest, Richard L.,Ji, Jingjing,Kazmierski, Wieslaw M.,Tallant, Matthew D.,Wright, Lois L.,Smith, Gary K.,Crosby, Renae M.,Wang, Amy A.,Ni, Zhi-Jie,Zou, Wuxin,Wright, Jon
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scheme or table
p. 7317 - 7322
(2011/01/12)
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- BORON-CONTAINING SMALL MOLECULES AS ANTI-PROTOZOAL AGENTS
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This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.
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Page/Page column 134
(2010/04/30)
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