- 1-PYRAZOLYL, 5-, 6- DISUBSTITUTED INDAZOLE DERIVATIVES AS LRRK2 INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND USES THEREOF
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The present invention is directed to substituted certain 1-pyrazolyl, 5-, 6- disubstituted indazole derivatives of Formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, and ring A are as defined herein, which are potent inhibitors of LRRK2 kinase and may be useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease and other diseases and disorders described herein. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of diseases, such as Parkinson's disease, in which LRRK-2 kinase is involved.
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Page/Page column 53; 54
(2020/12/29)
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- Targeting human La and its precursor compound of the protein in the preparation of anti-hepatitis b virus use in medicine
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The invention belongs to the field of pharmacy and relates to a lead compound of a targeting human La protein and purpose thereof in preparation of a medicament for resisting hepatitis B virus. According to the invention, research on enhancement of HBVRNA stability by the targeting La protein is employed to screen out the lead compound of the targeting human La protein shown as a formula (I), a formula (II) or a formula (III). Tests show that the lead compound has strong antiviral activity and effect of targeting the La protein. The lead compound of the present invention can be further optimized in structure and has good application prospect; and the lead compound and derivatives thereof can be used for preparation of medicament for resisting hepatitis B virus, as well as preparation of medicament targeting the La protein.
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Paragraph 0055; 0059; 0060
(2017/01/12)
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- QUINAZOLINE BASED RESPIRATORY SYNCYTIAL VIRUS INHIBITORS
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Compounds of Formula (I), wherein R1, R2, R3, R4 and n are defined herein, are useful as inhibitors of RSV.
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Page/Page column 49
(2015/05/19)
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- INDOLES AS RESPIRATORY SYNCYTIAL VIRUS ANTIVIRAL AGENTS
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Indoles having inhibitory activity on RSV replication and having the formula I the prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof; compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.
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Paragraph 0092; 0096-0097
(2013/10/22)
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- Non-benzimidazole containing inhibitors of respiratory syncytial virus
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Several non-benzimidazole containing inhibitors of respiratory syncytial virus are described. Core template modification, analysis of antiviral activity, physicochemistry and optimisation of properties led to the thiazole-imidazole 13, that showed a good potency and pharmacokinetic profile in the rat.
- Pryde, David C.,Tran, Thien-Duc,Gardner, Iain,Bright, Helen,Stupple, Paul,Galan, Sebastien,Alsop, Liam,Watson, Lesa,Middleton, Donald S.,Dayal, Satish,Platts, Michelle,Murray, Edward J.,Parkinson, Tanya,Webster, Robert
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supporting information
p. 827 - 833
(2013/03/13)
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- IMIDAZOPYRIDINES AS RESPIRATORY SYNCYTIAL VIRUS ANTIVIRAL AGENTS
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A compound satisfying formula I, a prodrug, N-oxide, addition salt, quaternary amine, metal complex, or a stereochemically isomeric form thereof; compositions contain these compounds as active ingredient and processes for preparing these compounds and compositions.
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Page/Page column 20
(2012/06/30)
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- INDOLES AS RESPIRATORY SYNCYTIAL VIRUS ANTIVIRAL AGENTS
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Indoles having inhibitory activity on RSV replication and having the formula I the prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof, compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.
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Page/Page column 19
(2012/06/30)
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- AZAINDOLES AS RESPIRATORY SYNCYTIAL VIRUS ANTIVIRAL AGENTS
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Azaindoles having inhibitory activity on RSV replication and having the formula (I) compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.
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Page/Page column 19
(2012/06/30)
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- AZABENZIMIDAZOLES AS RESPIRATORY SYNCYTIAL VIRUS ANTIVIRAL AGENTS
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A compound satisfying formula I, a prodrug, N-oxide, addition salt, quaternary metal complex, or a stereochemically isomeric form thereof; (formula I) compositions contain these compounds as active ingredient and processes for preparing these compounds and compositions.
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Page/Page column 22; 23
(2012/06/30)
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- Development of an efficient and scalable process of a respiratory syncytial virus inhibitor
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An improved process has been developed for compound 1, a respiratory syncytial virus (RSV) inhibitor. This improved process is convergent, safe, efficient, and useful to prepare compound 1 in kilogram quantities.
- Provencal, David P.,Gesenberg, Kirsten D.,Wang, Hua,Escobar, Carlos,Wong, Henry,Brown, Matthew A.,Staab, Andrew J.,Pendri, Yadagiri R.
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p. 903 - 908
(2013/09/03)
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- Substituted 2-methyl-benzimidazole respiratory syncytial virus antiviral agents
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The present invention concerns antiviral compounds, their methods of preparation and their compositions, and use in the treatment of viral infections. More particularly, the invention provides heterocyclic substituted 2-methylbenzimidazole derivatives for the treatment of respiratory syncytial virus infection.
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