- ANTIVIRAL COMPOUNDS
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The invention is provides novel antiviral compounds, as well as derivatives thereof. The compounds of the invention are preferably formulated as pharmaceuticals. The invention provides the compounds for use in the prevention and treatment of infectious diseases, in particular viral diseases. In some aspects the invention is based on the antiviral activity of the provided compounds against the Chikungunya virus, and hence, their application in the treatment or prevention of any physiological manifestation of such viral infection.
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Paragraph 90-94; 129-132
(2020/11/12)
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- Substituted p-chlorophenyl acetylpiperazine-containing compound as well as preparation method and application thereof
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The application provides a substituted p-chlorophenyl acetylpiperazine-containing compound as well as a preparation method and application of the substituted p-chlorophenyl acetylpiperazine-containingcompound. The compound has the structure shown in the formula (I), and has better Akt1 inhibitory activity or growth inhibitory activity to MCL cell lines.
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Paragraph 0116; 0139; 0200-0202; 0204
(2019/01/06)
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- NEW TRPA1 ANTAGONISTS
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The present invention relates to compounds of Formula (I), to the process for preparing such compounds and to their use in the treatment of a pathological condition or disease susceptible to amelioration by TRPA1 channel inhibition or antagonism.
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Page/Page column 62; 63; 129
(2017/08/01)
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- Substituted pyrimidine derivatives with Akt inhibiting activity, and preparation method and application thereof
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The invention relates to novel substituted pyrimidine derivatives with Akt inhibiting activity and a preparation method thereof, a pharmaceutical composition comprising the substituted pyrimidine derivatives and salts thereof, and application of the substituted pyrimidine derivatives and salts thereof in preparing drugs for preventing and/or treating tumors. The structural formula of the compounds is disclosed as Formula (I) or Formula (II). The compounds have the advantages of novel structure, outstanding Akt inhibiting activity, high safety and low preparation cost, and have favorable application prospects in preparing antineoplastic drugs.
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Paragraph 0093; 0094; 0095; 0097
(2016/12/16)
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- Chemoselective reactions of 4,6-dichloro-2-(methylsulfonyl)pyrimidine and related electrophiles with amines
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Chemoselective SNAr reactions of 4,6-dichloro-2-(methylsulfonyl) pyrimidine and several related electrophiles with amines and their derivatives are described. In the presence of weak bases anilines and secondary aliphatic amines selectively displace the chloride group. Deprotonated anilines and their carbonyl derivatives displace the sulfone group. Sterically and electronically unbiased primary aliphatic amines selectively displace the sulfone group in 4,6-dichloro-2-(methylsulfonyl)pyrimidine; however, their reactions with other electrophiles generally are less selective. Steric-driven selectivity explanation was proposed. Georg Thieme Verlag Stuttgart. New York.
- Baiazitov, Ramil,Du, Wu,Lee, Chang-Sun,Hwang, Seongwoo,Almstead, Neil G.,Moon, Young-Choon
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p. 1764 - 1784
(2013/07/26)
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- Discovery of 3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl- piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), A potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase
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A novel series of N-aryl-N′-pyrimidin-4-yl ureas has been optimized to afford potent and selective inhibitors of the fibroblast growth factor receptor tyrosine kinases 1, 2, and 3 by rationally designing the substitution pattern of the aryl ring. On the b
- Guagnano, Vito,Furet, Pascal,Spanka, Carsten,Bordas, Vincent,Le Douget, Micka?l,Stamm, Christelle,Brueggen, Josef,Jensen, Michael R.,Schnell, Christian,Schmid, Herbert,Wartmann, Markus,Berghausen, Joerg,Drueckes, Peter,Zimmerlin, Alfred,Bussiere, Dirksen,Murray, Jeremy,Graus Porta, Diana
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supporting information; experimental part
p. 7066 - 7083
(2011/12/04)
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- PYRIMIDINE UREA DERIVATIVES AS KINASE INHIBITORS
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The invention relates to compounds of formula (I) wherein the substituents X1, R1, R2, R3 and R4 have the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, and a method for the treatment of such a disease.
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Page/Page column 208
(2008/06/13)
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