- HPK1 ANTAGONISTS AND USES THEREOF
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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.
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Paragraph 1078; 1079
(2021/03/19)
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- SUBSTITUTED IMIDAZOLES FOR THE INHIBITION OF TGF-BETA AND METHODS OF TREATMENT
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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.
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Paragraph 0071
(2020/03/15)
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- Method for preparing hydrofluoroether through two-step process
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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.
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Paragraph 0058; 0059; 0070; 071
(2019/07/10)
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- Selective 19F-Labeling of Functionalized Carboxylic Acids with Difluoromethyl Diazomethane (CF2HCHN2)
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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.
- Mykhailiuk, Pavel K.,Kishko, Igor,Kubyshkin, Vladimir,Budisa, Nediljko,Cossy, Janine
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supporting information
p. 13279 - 13283
(2017/10/05)
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- METHYL OXAZOLE OREXIN RECEPTOR ANTAGONISTS
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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.
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Page/Page column 33
(2016/06/28)
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- PIPERIDINE ISOXAZOLE AND ISOTHIAZOLE OREXIN RECEPTOR ANTAGONISTS
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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.
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Page/Page column 53
(2016/05/19)
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- 6,5-BICYCLIC OCTAHYDROPYRROLOPYRIDINE OREXIN RECEPTOR ANTAGONISTS
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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.
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Paragraph 42
(2016/07/05)
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- ETHYLDIAMINE OREXIN RECEPTOR ANTAGONISTS
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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.
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Page/Page column 43
(2016/07/05)
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- BRIDGED DIAZEPANE OREXIN RECEPTOR ANTAGONISTS
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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.
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Page/Page column 38; 39
(2016/06/14)
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- GLUCOPYRANOSYL DERIVATIVES AND THEIR USES IN MEDICINE
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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.
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Paragraph 00265
(2015/04/15)
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- DIAZEPANE OREXIN RECEPTOR ANTAGONISTS
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The present invention is directed to diazepane compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the diazepane compounds described herein in the potential treatment or prevention of neurological and psy
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Page/Page column 34
(2015/07/07)
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- TETRACYCLIC HETEROCYCLE COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
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The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
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Paragraph 0744
(2014/08/07)
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- TETRACYCLIC HETEROCYCLE COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
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The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
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Page/Page column 191
(2013/03/26)
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