- Small-compound enhancers for functional O-mannosylation of alpha-dystroglycan, and uses thereof
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The present invention provides compounds that can enhance functional O-mannosylation of proteins including alpha-dystroglycan. Also provided are methods of preparation of the compounds defined by the formula I. Also provided are the methods of using the compounds or the pharmaceutical acceptable salts or prodrugs thereof in treating and preventing subjects suffering from the diseases including muscular dystrophies and cancers.
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Page/Page column 22
(2019/03/14)
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- Nitrogen Oxides and Nitric Acid Enable the Sustainable Hydroxylation and Nitrohydroxylation of Benzenes under Visible Light Irradiation
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A new type of waste recycling strategy is described in which nitrogen oxides or nitric acid are directly employed in photocatalyzed hydroxylations and nitrohydroxylations of benzenes. Through these transformations, otherwise costly denitrification can be combined with the synthesis of valuable compounds for various applications.
- Hofmann, Laura Elena,Mach, Leonard,Heinrich, Markus R.
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supporting information
p. 431 - 436
(2017/12/15)
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- FACTOR XIa INHIBITORS
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The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma Kallikrein.
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Page/Page column 70
(2017/05/21)
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- A Synthetic Pathway to Substituted Benzofuroxans through the Intermediacy of Sulfonates: The Case Example of Fluoro-Nitrobenzofuroxans
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Benzofuroxans are well known compounds that continue to attract particular attention since the discovery of 4,6-dinitrobenzofuroxan (DNBF) back in 1899. It has been shown that these compounds possess biological activities that are related to their electro
- Jovené, Cyril,Marrot, Jérome,Jasmin, Jean-Philippe,Chugunova, Elena,Goumont, Régis
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p. 4084 - 4092
(2016/08/24)
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- Small molecules enhance functional O-mannosylation of Alpha-dystroglycan
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Alpha-dystroglycan (α-DG), a highly glycosylated receptor for extracellular matrix proteins, plays a critical role in many biological processes. Hypoglycosylation of α-DG results in various types of muscular dystrophies and is also highly associated with progression of majority of cancers. Currently, there are no effective treatments for those devastating diseases. Enhancing functional O-mannosyl glycans (FOG) of α-DG on the cell surfaces is a potential approach to address this unmet challenge. Based on the hypothesis that the cells can up-regulate FOG of α-DG in response to certain chemical stimuli, we developed a cell-based high-throughput screening (HTS) platform for searching chemical enhancers of FOG of α-DG from a large chemical library with 364,168 compounds. Sequential validation of the hits from a primary screening campaign and chemical works led to identification of a cluster of compounds that positively modulate FOG of α-DG on various cell surfaces including patient-derived myoblasts. These compounds enhance FOG of α-DG by almost ten folds, which provide us powerful tools for O-mannosylation studies and potential starting points for the development of drug to treat dystroglycanopathy.
- Lv, Fengping,Li, Zhi-Fang,Hu, Wenhao,Wu, Xiaohua
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supporting information
p. 7661 - 7670
(2015/12/18)
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- PROTEIN KINASE C INHIBITORS AND USES THEREOF
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This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
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Page/Page column 36
(2012/02/03)
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- PROTEIN KINASE C INHIBITORS AND USES THEREOF
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This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
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Page/Page column 83
(2011/06/23)
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- Alpha2C adrenoreceptor agonists
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In its many embodiments, the present invention relates to a novel class of phenylmorpholine and phenylthiomorpholine compounds useful as α2C adrenergic receptor agonists, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the α2C adrenergic receptor agonists using such compounds or pharmaceutical compositions.
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Page/Page column 31
(2010/11/26)
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- FLUORINATION OF ANIONIC ?-COMPLEXES BY CESIUM FLUOROXYSULFATE
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Anionic ?-complexes and related structures react with cesium fluoroxysulfate to give predominantly the C-fluoro derivatives: fluoronitrocyclohexadienes or substituted fluoronitrobenzenes.Oxidation or degradation of a complex to form substituted nitrobenzenes is also possible.The balance between all these processes is determined by the structure of the original complex.
- Gakh, A. A.,Romaniko, S. V.,Ugrak, B. I.,Fainzil'berg, A. A.
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p. 1432 - 1436
(2007/10/02)
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- Formation of 4-Halo-4-nitrocyclohexa-2,5-dienones on Nitration of p-Halophenols and p-Halophenyl Acetates.
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Nitration of p-chloro-, p-fluoro-, and p-bromo-phenol or the corresponding p-halophenyl acetates at -40 deg C and below gives the 4-halo-4-nitrocyclohexa-2,5-dienones in addition to the 4-halo-2-nitrophenols.The dienones isomerize to the nitrophenols at temperatures between -40 deg C and 0 deg C.Nitration of 4-chloro-2-methylphenol or its acetate gives both 4-chloro-2-methyl-4-nitrocyclohexa-2,5-dienone and 4-chloro-6-methyl-6-nitrocyclohexa-2,4-dienone. 4-Chloro-3-methylphenol and its acetate give 4-chloro-3-methyl-4-nitrocyclohexa-2,5-dienone.
- Clewley, Robin G.,Cross, Gordon G.,Fischer, Alfred,Henderson, George N.
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p. 1299 - 1310
(2007/10/02)
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