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    • 71. 发明专利
    • DE602004006379T2
    • 2008-01-10
    • DE602004006379
    • 2004-01-27
    • CYCLACEL LTD
    • MCINNES CAMPBELLMEADES CHRISTOPHERMEZNA MOKDADFISCHER PETER
    • A61K31/428A61P35/00C07D277/68
    • The present invention relates to the use of a compound of formula I, or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 , R 3 , and R 4 are each independently H, NO 2 , CF 3 , SCF 3 , CN, halo, OH, OR 6 , NH 2 , NHR 6 , NR 6 R 7 , N + R 6 R 7 R 8 , COOH, COOR 6 , CONH 2 , CONHR 6 , CONR 6 R 7 , COH, COR 6 , SR 6 , SOR 6 , SO 2 R 6 , SO 2 OH, SO 2 OR 6 , SO 2 NH 2 , SO 2 NHR 6 , SO 2 NR 6 R 7 , alkyl, cycloalkyl, cycloheteroalkyl, aryl, or heteroaryl, with the proviso that at least one of R 1 , R 2 , R 3 , and R 4 is other than H; or R 1 and R 2 , R 2 and R 3 , or R 3 and R 4 , may together form part of a fused or unfused saturated or unsaturated ring system, optionally containing up to two heteroatoms selected from N, O, and S; R 5 is OH, OR 9 , CN, CONH 2 , CONHNH 2 , CONHOH, CONHR 9 , CONR 9 R 10 , NH 2 , NHR 9 , or NR 9 R 10 ; each R 6 , R 7 and R 8 is independently hydrocarbyl, or two of R 6 , R 7 and R 8 together form part of a saturated or unsaturated ring system, optionally containing up to two heteroatoms selected from N, O, and S; each R 9 and R 10 is independently hydrocarbyl, or R 9 and R 10 together form part of a saturated or unsaturated ring system, optionally containing up to two heteroatoms selected from N, O, and S; in the preparation of a medicament for treating a proliferative disorder.
    • 75. 发明专利
    • THIAZOLO-, OXAZALO AND IMIDAZOLO-QUINAZOLINE COMPOUNDS CAPABLE OF INHIBITING PROT EIN KINASES
    • CA2530455A1
    • 2005-01-20
    • CA2530455
    • 2004-07-07
    • CYCLACEL LTD
    • MCINTYRE NEILWESTWOOD NICHOLASMCINNES CAMPBELLTHOMAS MARKFISCHER PETERWANG SHUDONG
    • C07D513/04A61K31/519A61P25/00C07D413/04
    • compound of formula (1), or a pharmaceutically acceptable salt thereof, wherein: X is S, 0, or NH; "a" is a single bond; or "a" is a double bond and one of R3 and R4 and one of R5 and R6 are absent; R1 is H; or is selected fr om an alkyl group, a cycloalkyl group, a heteroaryl group, an aralkyl group, CO - alkyl, S02-alkyl, C02R13 and an aryl group, each of which optionally contain s one or more heteroatoms, and is optionally substituted with one or more grou ps selected from R8 and R9; R2 is H, R8 , or an alkyl group optionally substituted with one or more R8 groups; R3 , R4, R5, and R6 are each independently selected from H, R8 , an alkyl group and an alkenyl group, wherein said alkyl and alkenyl groups are optionally substituted with one or more R8 groups; or R3 and R4, and/or R5 and R6 together represent =0; R7 is H, R8, NH(CH2)nR9, CO(CH2)nR9, NHCO(CH2)nR9, O(CH2)nR9, or an alkyl or phenyl group, each of which is optionally substituted with one or more groups selected from R8 and R9; R8is OR10, NR10R11, halogen, CF3, N02, COR10, CN, COOR10, CONR10R11, S02R10 or S02NR10R11; R9 is a saturated or unsaturated 5- or 6-membered cyclic group optionally containing one or more heteroatoms selected from N, 0 and S, and optionally substituted with one or more R8 groups; R10, R11, R12 and R13 are eachindependently H or a hydrocarbyl group ; and n is 0, 1, 2 or 3. Further aspects of the invention relate to pharmaceutical compositions comprising compounds of formula (1), and the therapeutic use thereof in the treatment of proliferative disorders, viral disorders, CNS disorders, diabetes, stroke and cardiovascular disorders.