- 2, 4 -DIAMINOPYRIMIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS
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The present invention relates to novel pyrimide derivatives of formula (I): that are useful as kinase inhibitors. More particularly, the present invention relates to novel pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders.
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Page/Page column 132-133
(2012/05/20)
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- Pharmaceutically active benzoquinazoline compounds
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Compounds of formula (I) or salts thereof, wherein the dotted line represents a single or double bond, R1is alkyl or amino optionally substituted by alkyl, alkanoyl or benzyl group; R2, R3, R4and R5are the same or different and each is selected from hydrogen, phenyl, halo, nitro, a group S(O)nR8wherein n is the integer 0, 1 or 2 and R8is halo or alkyl or a group NR9R10wherein R9and R10are both hydrogen, a group NR11R12wherein R11and R12are the same or different and each is hydrogen or alkyl, a group OR13wherein R13is hydrogen or C1-4alkyl optionally substituted by halo; a C1-4aliphatic group optionally substituted by a group OR14or NR14R15wherein R14and R15are the same or different and each is hydrogen or alkyl; or two of R2to R5are linked together to form a benzo group, or one of R2to R5is a group -X-Y-R16wherein X is CH2, NR17, CO or S(O)m, and Y is CH2, NR17, O, or S(O)m, or -X-Y- is a group -O-, -NR17-, -CH=CH- or -N=N-, are disclosed as pharmacological agents useful in the treatment of tumours. Pharmaceutical compositions and methods for the preparation of compounds of formula (I) are also described.
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- N-[hydroxy(amino)alkyl]amides of amino(nitro)benzoic acids
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2-Aminoethanol and 3-amino-1-propanol react with methyl 3-nitro-and 4-nitrobenzoates in boiling toluene to afford the corresponding ethyl N-(hydroxyalkyl)nitrobenzoates. The reaction of methyl 3-nitro-and 4-nitrobenzoates with bis(2-hydroxyethyl)amine yie
- Bagrov,Vasil'ev,Efimov,Kol'tsov
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p. 674 - 678
(2007/10/03)
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- Synthesis of oligonucleotides containing a new azobenzene fragment with efficient photoisomerizability
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The azobenzene derivatives possessing substituents of ROCH2CH2O- and-CH2CH2OR' or -CONHCH2CH2OR' at p,p'-positions, where R and R' are 4,4'-dimethoxytrityl and 2-cyanoethyl-N,N'-diisopropylphophoramidite, have been synthesized for linking two oligonucelotide segments. It has been found that the azobenzene linkers efficiently undergo trans-cis isomerization by exposing to UV light. The conversion efficiency showed slight dependence on structure or conformation of oligonucleotides attached to the azobenzene chromophore. The cis-form of the azobenzene in oligonucleotides was sufficiently stable at low temperature under dark. The present findings would open the way for light switch of nucleic acid structures. Copyright (C) 1999 Elsevier Science Ltd.
- Yamana, Kazushige,Kan, Katsushi,Nakano, Hidehiko
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p. 2977 - 2983
(2007/10/03)
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