- BICYCLIC COMPOUNDS AS PEST CONTROL AGENTS
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The present application relates to novel bicyclic compounds, to compositions comprising these compounds, to their use for controlling animal pests and to processes and intermediates for their preparation.
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Paragraph 0633; 0634
(2017/09/25)
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- Development of 2, 4-diaminoquinazoline derivatives as potent PAK4 inhibitors by the core refinement strategy
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Upon analysis of the reported crystal structure of PAK4 inhibitor KY04031 (PAK4 IC50?=?0.790?μM) in the active site of PAK4, we investigated the possibility of changing the triazine core of KY04031 to a quinazoline. Using KY04031 as a starting
- Hao, Chenzhou,Huang, Wanxu,Li, Xiaodong,Guo, Jing,Chen, Meng,Yan, Zizheng,Wang, Kai,Jiang, Xiaolin,Song, Shuai,Wang, Jian,Zhao, Dongmei,Li, Feng,Cheng, Maosheng
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- Synthesis of aromatic 13C/2H-α-ketoacid precursors to be used in selective phenylalanine and tyrosine protein labelling
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Recent progress in protein NMR spectroscopy revealed aromatic residues to be valuable information sources for performing structure and motion analysis of high molecular weight proteins. However, the applied NMR experiments require tailored isotope labelling patterns in order to regulate spin-relaxation pathways and optimize magnetization transfer. We introduced a methodology to use α-ketoacids as metabolic amino acid precursors in cell-based overexpression of phenylalanine and/or tyrosine labelled proteins in a recent publication, which we have now developed further by providing synthetic routes to access the corresponding side-chain labelled precursors. The target compounds allow for selective introduction of 13C-1H spin systems in a highly deuterated chemical environment and feature alternating 12C-13C-12C ring-patterns. The resulting isotope distribution is especially suited to render straightforward 13C spin relaxation experiments possible, which provide insight into the dynamic properties of the corresponding labelled proteins.
- Lichtenecker, R. J.
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p. 7551 - 7560
(2015/01/08)
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- NOVEL NICOTINAMIDE DERIVATIVE OR SALT THEREOF
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The object of the present invention is to provide a compound and a pharmaceutical composition having excellent Syk inhibitory activity. According to the present invention, a nicotinamide derivative represented by the following formula (I) or a salt thereof is provided, wherein R1 is a substituent represented by the following formula (II-1), (III-1), or (IV-1) (wherein R3, R4, R5, n, and X1 have the same definitions as those described in the specification), and R2 is a pyridyl, indazolyl, phenyl, pyrazolopyridyl, benzisoxazolyl, pyrimidinyl, or quinolyl group, each of which optionally has at least one substituent.
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Paragraph 0557; 0558; 0559
(2014/10/29)
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- SUBSTITUTED 5-(PYRAZIN-2-YL)-1H-PYRAZOLO [3,4-B] PYRIDINE AND PYRAZOLO [3,4-B] PYRIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS
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Substituted 5-(pyrazin-2-yl)-1H-pyrazolo [3,4-b] pyridine, 5-(pyrazin-2-yl)-1H-pyrrolo[2,3-b]pyridine and pyrazolo [3,4-b] pyridine derivatives according to formula I, II and VII, and methods for making same, which are inhibitors of constitutively activated Tyrosine Kinase-Like (TKL), CMGC protein kinases family members and can be useful in the treatment of Parkinson?s disease, Alzheimer?s disease, Down?s Syndrome, Huntington?s disease, other neurodegenerative and central nervous system disorders, cancer, metabolic disorders and inflammatory diseases. Also disclosed are pharmaceutical compositions including the compounds and methods of inhibiting wild type and/or mutated protein kinase activities of these families and the treatment of disorders associated there with using compounds and pharmaceutical compositions including the compounds.
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Page/Page column 16
(2012/10/18)
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- Synthesis of bi-substrate state mimics of dihydropteroate synthase as potential inhibitors and molecular probes
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The increasing emergence of resistant bacteria drives us to design and develop new antimicrobial agents. Pursuant to that goal, a new targeting approach of the dihydropteroate synthase enzyme, which serves as the site of action for the sulfonamide class o
- Qi, Jianjun,Virga, Kristopher G.,Das, Sourav,Zhao, Ying,Yun, Mi-Kyung,White, Stephen W.,Lee, Richard E.
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experimental part
p. 1298 - 1305
(2011/04/17)
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- HETEROCYCLIC CYTOKINE INHIBITORS
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The present invention provides low molecular weight compounds useful as cytokine inhibitors, and compositions thereof. In particular, compounds of the invention are useful as anti-inflammatory, anti-pain or anti-cancer agents. There are further provided m
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Page/Page column 153
(2010/11/27)
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- Diaminopyrimidines as P2X3 and P2X2/3 modulators
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Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein A, D, E, G, J, X, Y, Z R6, R7 and R8 are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist and methods of making the compounds.
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Page/Page column 25
(2010/11/26)
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- Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same
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Compounds are disclosed that have a formula represented by the following: 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, pain, inflammation, traumatic injury, and others.
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Page/Page column 28
(2010/11/23)
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- Bicyclic heterocycles as cannabinoid receptor modulators
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The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents and methods of treatment using the compounds a
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Page/Page column 10
(2008/06/13)
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- Synthesis, DNA binding, topoisomerases inhibition and cytotoxic properties of 4-arylcarboxamidopyrrolo-2-carboxyanilides
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Three 4-arylcarboxamidopyrrolo-2-carboxyanilides bearing different substituents on the pyrrole nitrogen were synthesized and evaluated for their capacities to bind to specific sequences within the minor groove of DNA and to inhibit human topoisomerases I and II in vitro. The cytotoxicity of the drugs correlates with their DNA binding affinities. The two drugs bearing a N-methyl or N-benzyl pyrrole stabilize topoisomerase I-DNA complexes. (C) 2000 Elsevier Science Ltd. All rights reserved.
- Dudouit, Fabienne,Goossens, Jean-Francois,Houssin, Raymond,Henichart, Jean-Pierre,Colson, Pierre,Houssier, Claude,Gelus, Nathalie,Bailly, Christian
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p. 553 - 557
(2007/10/03)
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