- Synthesis method of aminopyridine compounds
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The invention provides a synthesis method of aminopyridine compounds. The synthesis method of the aminopyridine compounds comprises the following steps: under a heating condition, halogenated pyridineorganic matters and an ammoniation reagent are subjected to an ammoniation reaction to obtain an ammoniated product system, wherein in the ammoniation reaction, the temperature of the ammoniation reaction is 200-240 DEG C, and the ammoniation reagent is in a solid state and can be decomposed to generate ammonia gas; and the ammoniated product system is sequentially purified and salified to obtainthe aminopyridine compounds. The synthesis method does not need to add a solvent, so that the yield of three wastes can be greatly reduced; the type of the ammonification reagent and the ammonification reaction temperature are limited during the reaction process, such that the high reaction rate and the high conversion rate can be obtained without the addition of the catalyst, and the purification and salification process after the ammonification reaction is simple and has the good separation effect so as to substantially reduce the production cost and improve the product yield and the product purity. In addition, the synthesis method also has the advantages of good repeatability and the like.
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Paragraph 0063-0064
(2020/10/14)
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- Alkoxy pyridone compound as well as preparation method and application thereof
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The invention belongs to the field of medicinal chemistry, specifically, the invention relates to a series of inhibitors of factor XIa (FXIa for short) with a novel structure as well as a preparationmethod and an application thereof. The structure is shown as the following general formula (I). These compounds or stereoisomers, racemates, geometric isomers, tautomers, prodrugs, hydrates, solvatesor pharmaceutically acceptable salts and pharmaceutical compositions thereof can be used to treat or/and prevent related diseases mediated by factor XIa (FXIa for short).
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Paragraph 0175-0177
(2020/12/15)
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- QUINOLINE COMPOUNDS AS MODULATORS OF RAGE ACTIVITY AND USES THEREOF
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Quinoline compounds are disclosed that have a formula represented by the following: and wherein Cy, R1, R4a, R4b, and n are as described herein. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, diabetes complications, inflammation, and neurodegeneration, obesity, cancer, ischemia/reperfusion injury, cardiovascular disease and other diseases related to RAGE activity.
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Paragraph 00379
(2017/11/15)
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- Pyrimidinone Derivatives as Antimalarial Agents
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The invention relates to novel pyrimidinone-based heterocyclic compounds which are parasite growth inhibitors, having the general formula (I) in which Y is a morpholine chosen from three bridged morpholines, L is a bond or a linker, n=0 or 1 and R2 is a methyl group when n=0 and a hydrogen atom when n=1. Process for the preparation thereof and therapeutic use thereof.
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Paragraph 0832; 0833; 0834
(2015/07/15)
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- PYRIMIDINONE DERIVATIVES AS ANTIMALARIAL AGENTS
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The invention relates to novel pyrimidinone-based heterocyclic compounds which are parasite growth inhibitors, having the general formula (I) in which Y is a morpholine chosen from three bridged morpholines, L is a bond or a linker, n = 0 or 1 and R2 is a methyl group when n = 0 and a hydrogen atom when n = 1. Process for the preparation thereof and therapeutic use thereof.
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Page/Page column 90; 91
(2014/01/09)
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- Identification of KD5170: A novel mercaptoketone-based histone deacetylase inhibitor
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We report the identification of KD5170, a potent mercaptoketone-based Class I and II-histone deacetylase inhibitor that demonstrates broad spectrum cytotoxic activity against a range of human tumor-derived cell lines. KD5170 exhibits robust and sustained histone H3 hyperacetylation in HCT-116 xenograft tumors following single oral or iv dose and inhibition of tumor growth following chronic dosing.
- Payne, Joseph E.,Bonnefous, Celine,Hassig, Christian A.,Symons, Kent T.,Guo, Xin,Nguyen, Phan-Manh,Annable, Tami,Wash, Paul L.,Hoffman, Timothy Z.,Rao, Tadimeti S.,Shiau, Andrew K.,Malecha, James W.,Noble, Stewart A.,Hager, Jeffrey H.,Smith, Nicholas D.
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scheme or table
p. 6093 - 6096
(2009/07/18)
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- α-Mercaptoketone based histone deacetylase inhibitors
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In an effort to discover novel non-hydroxamic acid histone deacetylase (HDAC) inhibitors, a novel α-mercaptoketone was identified in a high-throughput screen. Lead optimization of the screening hit, led to a number of potent HDAC inhibitors. In particular, α-mercaptoketone 19y (KD5150) exhibited nanomolar in vitro activity and inhibition of tumor growth in vivo.
- Wash, Paul L.,Hoffman, Timothy Z.,Wiley, Brandon M.,Bonnefous, Celine,Smith, Nicholas D.,Sertic, Michael S.,Lawrence, Charles M.,Symons, Kent T.,Nguyen, Phan-Manh,Lustig, Kevin D.,Guo, Xin,Annable, Tami,Noble, Stewart A.,Hager, Jeffrey H.,Hassig, Christian A.,Malecha, James W.
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scheme or table
p. 6482 - 6485
(2009/10/01)
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- Multicyclic sulfonamide compounds as inhibitors of histone deacetylase for the treatment of disease
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Disclosed herein are sulfonamide compounds of Formula VII as described herein. Methods and compositions are disclosed for treating disease states including, but not limited to cancers, autoimmune diseases, tissue damage, central nervous system disorders, neurodegenerative disorders, fibrosis, bone disorders, polyglutamine-repeat disorders, anemias, thalassemias, inflammatory conditions, cardiovascular conditions, and disorders in which angiogenesis play a role in pathogenesis, using the compounds of the invention. In addition, methods of modulating the activity of histone deacetylase (HDAC) are also disclosed.
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Page/Page column 17; 19
(2010/11/25)
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- Substituted Dihydroisoindolones As Allosteric Modulators of Glucokinase
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The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating glucokinase mediated disorders. More particularly, the compounds of the present invention are glucokinase modulators useful for treating disorders including, but not limited to, type II diabetes.
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Page/Page column 45
(2010/11/27)
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