- Azacyclo diketone compound and preparation method thereof
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The invention provides an azacyclo diketone compound, which is a compound represented by the following structure defined in the specification, or a pharmaceutically acceptable salt thereof. The invention provides a compound having an inhibitory activity on influenza (flu) virus proliferation, particularly on influenza-related cap-dependent endonuclease to inhibit influenza virus proliferation so as to treat or prevent influenza. The present invention relates to a substituted azacyclo diketone compound having inhibitory activity on cap-dependent endonuclease, and a pharmaceutical composition containing the substituted azacyclo diketone compound.
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Paragraph 0876-0881
(2020/06/17)
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- Azacycle diketone compound and preparation method thereof (by machine translation)
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The invention provides a azacyclodiketone compound which is characterized by being a compound represented by the following structure. The compound has inhibitory activity on cap-dependent endonuclease. (by machine translation)
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Paragraph 0628-0633
(2020/09/12)
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- Novel M2-selective, Gi-biased agonists of muscarinic acetylcholine receptors
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Background and Purpose: More than 30% of currently marketed medications act via GPCRs. Thus, GPCRs represent one of the most important pharmacotherapeutic targets. In contrast to traditional agonists activating multiple signalling pathways, agonists activating a single signalling pathway represent a new generation of drugs with increased specificity and fewer adverse effects. Experimental Approach: We have synthesized novel agonists of muscarinic ACh receptors and tested their binding and function (on levels of cAMP and inositol phosphates) in CHO cells expressing individual subtypes of muscarinic receptors, primary cultures of rat aortic smooth muscle cells and suspensions of digested native tissues from rats. Binding of the novel compounds to M2 receptors was modelled in silico. Key Results: Two of the tested new compounds (1-(thiophen-2-ylmethyl)-3,6-dihydro-2H-pyridinium and 1-methyl-1-(thiophen-2-ylmethyl)-3,6-dihydro-2H-pyridinium) only inhibited cAMP synthesis in CHO cells, primary cultures, and native tissues, with selectivity for M2 muscarinic receptors and displaying bias towards the Gi signalling pathway at all subtypes of muscarinic receptors. Molecular modelling revealed interactions with the orthosteric binding site in a way specific for a given agonist followed by agonist-specific changes in the conformation of the receptor. Conclusions and Implications: The identified compounds may serve as lead structures in the search for novel non-steroidal and non-opioid analgesics acting via M2 and M4 muscarinic receptors with reduced side effects associated with activation of the phospholipase C signalling pathway.
- Randáková, Alena,Nelic, Dominik,Ungerová, Dana,Nwokoye, Peter,Su, Qiwen,Dole?al, Vladimír,El-Fakahany, Esam E.,Boulos, John,Jakubík, Jan
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supporting information
p. 2073 - 2089
(2020/02/18)
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- MUSCARINIC AGONISTS AS NON-STEROIDAL AND NON-OPIOID ANALGESICS AND METHODS OF USE THEREOF
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Novel Gi/o-biased muscarinic agonists selectively activate only one specific signaling pathway and are novel pharmacophores for development of new painkillers (analgesics). Methods of making and using these agonists are also described.
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Paragraph 0060; 0073; 0076; 00106
(2020/09/19)
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- Benzoxazine compound and its preparation methods and application
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The invention relates to a benzoxazine compound represented in the following formula 1. The benzoxazine compound can serve as a beta 2 receptor agonist. The formula can be seen from the description.
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Paragraph 0113; 0114; 0115
(2017/10/07)
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- PLATELET ADP RECEPTOR INHIBITORS
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Compounds are provided which are useful as platelet ADP receptor inhibitors, for treating thrombosis and for reducing the likelihood and/or severity of a secondary ischemic event in a patient.
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Page/Page column 34
(2008/06/13)
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- HETEROCYCLIC COMPOUNDS AND THEIR USE IN THE TREATMENT OF CARDIOVASCULAR DISEASE
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Heterocyclic compounds of the formula (I) are provided: wherein ring A, ring B, R1, R2, R3, R4, Y, m, n and q are as defined herein. R1 is in particular amidino. The invention further provides particular benzothiophene compounds. Compounds of the invention may be useful as inhibitors of Factor IXa and in the therapy of cardiovascular conditions and diseases, e.g. thrombosis.
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Page/Page column 236
(2008/06/13)
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- TETRAHYDROCARBAZOLE DERIVATIVES USEFUL AS ANDROGEN RECEPTOR MODULATORS
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The present invention provides a compound of the formula: Formula I or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising an effective amount of a compound of Formula I in combination with a suitable carrier, diluent, or ex
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Page/Page column 135-136
(2010/11/25)
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- Substituted oxoazaheterocyclyl compounds
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This invention is directed to oxoazaheterocycyl compounds which inhibit Factor Xa, to oxoazaheterocycyl compounds which inhibit both Factor Xa and Factor IIa, to pharmaceutical compositions comprising these compounds, to intermediates useful for preparing these compounds, to a method of directly inhibiting Factor Xa and to a method of simultaneously directly inhibiting Factor Xa and Factor IIa..
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Page/Page column 111
(2008/06/13)
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