- NEW COMPOUNDS FOR TREATMENT OF DISEASES RELATED TO DUX4 EXPRESSION
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The present invention relates to compounds for the treatment of diseases related to DUX4 expression, such as muscular dystrophies. It also relates to use of such compounds, or to methods of use of such compounds.
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Page/Page column 58; 68
(2021/06/04)
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- NOVEL COMPOUNDS FOR TREATMENT OF DISEASES RELATED TO DUX4 EXPRESSION
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The present invention relates to compounds that act as DUX4 repressors, suitable for the treatment of diseases related to DUX4 expression, such as muscular dystrophies. It also relates to use of such compounds, or to methods of use of such compounds.
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Page/Page column 95
(2021/06/04)
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- Design, synthesis, and structure-activity-relationship of a novel series of CXCR4 antagonists
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The important roles of the CXCL12/CXCR4 axis in numerous pathogenic pathways involving HIV infection and cancer metastasis make the CXCR4 receptor an attractive target for the development of therapeutic agents. Through scaffold hybridization of a few known CXCR4 antagonists, a series of novel aminopyrimidine derivatives was developed. Compound 3 from this new scaffold demonstrates excellent binding affinity with CXCR4 receptor (IC50 = 54 nM) and inhibits CXCL12 induced cytosolic calcium increase (IC50 = 2.3 nM). Furthermore, compound 3 possesses good physicochemical properties (MW 353, clogP 2.0, PSA 48, pKa 6.7) and exhibits minimal hERG and CYP isozyme (e.g. 3A4, 2D6) inhibition. Collectively, these results strongly support further optimization of this novel scaffold to develop better CXCR4 antagonists.
- Li, Zhanhui,Wang, Yujie,Fu, Chunyan,Wang, Xu,Wang, Jun Jun,Zhang, Yi,Zhou, Dongping,Zhao, Yuan,Luo, Lusong,Ma, Haikuo,Lu, Wenfeng,Zheng, Jiyue,Zhang, Xiaohu
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- TRPV4 ANTAGONISTS
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The present invention relates to spirocarbamate compounds of Formula (I) in which R1, (R2)Y, R3, R4, X and A have the meanings given in the specification. The invention further provides pharmaceutical compositions containing the compounds or pharmaceutically acceptable salts thereof and relates to their use of these compounds as TRPV4 antagonists in treating or preventing conditions associated with TRPV4 imbalance.
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Page/Page column 127
(2013/03/26)
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- ANTIMICROBIAL AGENTS
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The invention provides methods of treating a bacterial infection in a mammal comprising administering to the mammal a compound of formula I: [formula should be inserted here] wherein A, B, and X have any of the meanings defined in the specification; or a pharmaceutically acceptable salt thereof, as well as novel compounds of formula I and salts thereof and pharmaceutical compositions comprising a compound of formula I or a pharmaceutically acceptable salt thereof.
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Page/Page column 45
(2013/07/25)
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- AMINOPYRAZINE COMPOUNDS USEFUL AS INHIBITORS OF TRA KINASE
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The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula (I): wherein the variables are as defined herein.
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Page/Page column 90-91
(2012/10/18)
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- GLUCOCORTICOID MIMETICS, METHODS OF MAKING THEM, PHARMACEUTICAL COMPOSITIONS, AND USES THEREOF
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Compounds of Formula (IA) (IA), and Formula (IB) (IB), wherein R1, R2, R3, A, B, C, D, E, G, X, Y, and Z are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
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Page/Page column 163
(2008/12/06)
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