135206-84-7Relevant academic research and scientific papers
HPK1 ANTAGONISTS AND USES THEREOF
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Paragraph 1078; 1079, (2021/03/19)
The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of HPK1, and the treatment of HPK1-mediated disorders.
SUBSTITUTED IMIDAZOLES FOR THE INHIBITION OF TGF-BETA AND METHODS OF TREATMENT
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Paragraph 0071, (2020/03/15)
This disclosure relates to low molecular weight substituted imidazoles that inhibit the TGF-b signaling pathway. More specifically, this disclosure relates to methods of using said imidazoles for the treatment of diseases related to the TGF-b signaling pathways including, but not limited to, atherosclerosis, Marfan syndrome, Loeys-Dietz syndrome, obesity, diabetes, multiple sclerosis, keratoconus, idiopathic pulmonary fibrosis, Alzheimer's Disease, chronic kidney disease, and scleroderma.
Method for preparing hydrofluoroether through two-step process
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Paragraph 0058; 0059; 0070; 071, (2019/07/10)
The invention discloses a method for preparing hydrofluoroether through a two-step process. With the method provided by the invention, p-toluensulfonyl chloride and fluorine-containing alcohol are subjected to a reaction to obtain p-toluenesulfonate, and the p-toluenesulfonate and sodium alkoxide are subjected to a Williamson ether synthetic reaction to obtain the hydrofluoroether. The method disclosed by the invention has the advantages of cheap and low-toxicity raw materials, mild and controllable reaction conditions, and high yield.
Selective 19F-Labeling of Functionalized Carboxylic Acids with Difluoromethyl Diazomethane (CF2HCHN2)
Mykhailiuk, Pavel K.,Kishko, Igor,Kubyshkin, Vladimir,Budisa, Nediljko,Cossy, Janine
supporting information, p. 13279 - 13283 (2017/10/05)
The incorporation of fluorinated moieties into organic structures is a particularly powerful approach for generating compounds with useful biological applications in industry, pharmacology, and agriculture. Here, the recently developed reagent—CF2HCHN2—selectively esterifies carboxyl groups on organic molecules in the presence of other polar functional groups. The reaction is remarkably simple, proceeding at room temperature in chloroform without addition of a catalyst. The procedure allows “last-step” incorporation of a fluorinated ester moiety into organic structures, including bioorganic molecules such as peptides and proteins. The fluorinated ester can subsequently function as a 19F-probe in biomolecules, thereby enabling molecular size determination by diffusion 19F NMR experiments.
METHYL OXAZOLE OREXIN RECEPTOR ANTAGONISTS
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Page/Page column 33, (2016/06/28)
The present invention is directed to methyl oxazole compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.
PIPERIDINE ISOXAZOLE AND ISOTHIAZOLE OREXIN RECEPTOR ANTAGONISTS
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Page/Page column 53, (2016/05/19)
The present invention is directed to piperidine isoxazole and isothiazole orexin compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
6,5-BICYCLIC OCTAHYDROPYRROLOPYRIDINE OREXIN RECEPTOR ANTAGONISTS
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Paragraph 42, (2016/07/05)
The present invention is directed to 6,5-bicyclic octahydropyrrolopyridine compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.
ETHYLDIAMINE OREXIN RECEPTOR ANTAGONISTS
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Page/Page column 43, (2016/07/05)
The present invention is directed to ethyldiamne compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.
BRIDGED DIAZEPANE OREXIN RECEPTOR ANTAGONISTS
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Page/Page column 38; 39, (2016/06/14)
The present invention is directed to bridged diazepane compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.
GLUCOPYRANOSYL DERIVATIVES AND THEIR USES IN MEDICINE
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Paragraph 00265, (2015/04/15)
Disclosed are glucopyranosyl derivatives used as sodium dependent glucose cotransporters (SGLTs) inhibitors, intermediates or preparation processes thereof, and pharmaceutical uses thereof, especially glucopyranosyl derivatives represented by Formula (I), or pharmaceutically acceptable salts or all stereoisomers thereof, pharmaceutical compositions containing these derivatives and their uses for treatment of diabetes and diabetes-related diseases.
