- ANTI-INFLUENZA VIRUS PYRIMIDINE DERIVATIVE
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The present invention discloses a class of anti-influenza virus compounds, and the use thereof in the preparation of a drug for treating diseases associated with influenza viruses. In particular, the present invention discloses a compound represented by formula (I) and a pharmaceutically acceptable salt thereof.
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- Simple preparation method of 5-halogenated-7-azaindole
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The invention discloses a simple preparation method of 5-halogenated-7-azaindole. The method comprises: carrying out a 1,4-addition reaction on 4,4-dialkoxy n-butyronitrile (II) and 2,3-dihalogenatedacrolein (III) in the presence of a solvent and a catalyst to generate 2,3-dihalogenated-4-cyano-6,6-dialkoxy n-hexanal (IV), and carrying out a cyclization reaction on the 2,3-dihalogenated-4-cyano-6,6-dialkoxy n-hexanal, an alkali, ammonia and an ammonium salt to prepare the 5-halogenated-7-azaindole (I). According to the present invention, the method has characteristics of inexpensive and easily available raw materials, short process route, less wastewater discharge, easy environmental protection, convenient reaction operation, high reaction selectivity, high product purity, high yield andlow cost, and is suitable for the environmentally-friendly industrial production of 5-halogenated-7-azaindole.
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Paragraph 0050-0053
(2019/10/01)
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- PYRROLOPYRIMIDINE DERIVATIVES USEFUL AS INHIBITORS OF INFLUENZA VIRUS REPLICATION
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Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient a safe and effective amount of a compound represented by any of Formulas l-lll, or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a safe and effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.
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- INHIBITORS OF CYCLIN DEPENDNT KINASE 7 (CDK7)
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The present invention provides novel compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of cyclin-dependent kinase 7 (CDK7), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.
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- METHODS OF PREPARING INHIBITORS OF INFLUENZA VIRUSES REPLICATION
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A method of preparing Compound (1) or a pharmaceutically acceptable salt thereof: comprises: (a) reacting Compound (X): a pharmaceutically acceptable salt thereof with Compound (Y): in the presence of a palladium catalyst and a carbonate or phosphate base
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- The optimization of aminooxadiazoles as orally active inhibitors of Cdc7
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A series of aminooxadiazoles was optimized for inhibition of Cdc7. Early lead isoquinoline 1 suffered from modest cell potency (cellular IC50 = 0.71 μM measuring pMCM2), low selectivity against structurally related kinases, and high IV clearance in rats (CL = 18 L/h/kg). Extensive optimization resulted in azaindole 26 (Cdc7 IC50 = 1.1 nM, pMCM2 IC50 = 32 nM) that demonstrated robust lowering of pMCM2 in a mouse pharmacodynamic (PD) model when dosed orally. Modifications to improve the pharmacokinetic profile of this series were guided by trapping experiments with glutathione in rat hepatocytes.
- Harrington, Paul E.,Bourbeau, Matthew P.,Fotsch, Christopher,Frohn, Michael,Pickrell, Alexander J.,Reichelt, Andreas,Sham, Kelvin,Siegmund, Aaron C.,Bailis, Julie M.,Bush, Tammy,Escobar, Sonia,Hickman, Dean,Heller, Scott,Hsieh, Faye,Orf, Jessica N.,Rong, Minqing,San Miguel, Tisha,Tan, Helming,Zalameda, Leeanne,Allen, John G.
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p. 6396 - 6400
(2013/11/19)
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- NEW IMIDAZOLONE DERIVATIVES, PREPARATION THEREOF AS DRUGS, PHARMACEUTICAL COMPOSITIONS, AND USE THEREOF AS PROTEIN KINASE INHIBITORS, IN PARTICULAR CDC7
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The present invention relates to imidazolone derivatives of formula (I) to methods of preparing such derivatives, intermediates thereto, pharmaceutical compositions comprising such derivatives, and methods of inhibiting protein kinase, and methods of treatment comprising administration of such derivatives.
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Page/Page column 42
(2009/10/17)
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- SELECTIVE AZOLE PDE10A INHIBITOR COMPOUNDS
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The invention pertains to heteroaromatic compounds of the formula I, as defined herein, that serve as effective phosphodiesterase (PDE) inhibitors. In particular, the invention relates to said compounds which are selective inhibitors of PDE10. The invention also relates to pharmaceutical compositions comprising said compounds; and the use of said compounds in a method for treating certain central nervous system (CNS) or other disorders.
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- COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR
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Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
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Page/Page column 35
(2008/12/06)
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- Novel Bis-Azaindole Derivatives, Preparation And Pharmaceutical Use Thereof As Kinase Inhibitors
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Disclosed are compounds of formula (I): wherein R1, R2, R3, R4, and R5 have the meanings given in the description, and to salts thereof, pharmaceutical compositions comprising said compounds and the use thereof as protein kinase inhibitors.
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Page/Page column 30
(2010/11/30)
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- Novel pyrrolo (2,3-b)pyridine derivatives, the preparation and the pharmaceutical use thereof in the form of kinase inhibitors
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Novel compounds of formula (I): or pharmaceutically acceptable salts thereof, wherein R, R1, R2, R3, R4, R5, and R6 have the meanings given in the description, pharmaceutical compositions comprising said compounds and use thereof as protein kinase inhibit
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Page/Page column 45; 64-65
(2008/06/13)
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- AZAINDOLES USEFUL AS INHIBITORS OF ROCK AND OTHER PROTEIN KINASES
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The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
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Page/Page column 180-181
(2008/06/13)
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