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MACROCYCLIC QUINAZOLE DERIVATIVES AND THEIR USE AS MTKI
专利权人:
发明人:
申请号:
HK12108834.9
公开号:
HK1168095B
申请日:
2012.09.10
申请国别(地区):
HK
年份:
2017
代理人:
摘要:
The present Invention relates to compounds of formula forms of N - oxides, salts Addition acceptable for pharmaceutical use and forms of the same estereoquimicamente isomericas, where z represents NH and C3 - 9 represents alkyl, alkyl - C1 - 5 - NR13 - c1-5 alkyl, alkyl - nr14 - C1 - 5 - Co c1-5 alkyl -,Alkyl - C1 - 2 - nr21 - H2 co NH - c1-3 alkyl or alkyl - C1 - 2 - nr23 co cr16r17 - NH -, X1 represents alkyl - or or - or - C1 - 2 - x2 represents a direct Union, alkyl - C1 - 2 - - CO, c1-2 alkyl or alkyl - nr12 c1-2 r1 represents Hydrogen or Halo Halo R2 represents, R3 represents Hydrogen or acetylene or het1 Ciano R4 - alquiloxi AR4 represents c1-4 alquiloxi, c1-4,Alquiloxi c1-4 or alquiloxi c1-4 replaced with one or, where possible, two or more substituents selected from het2, nr7r8,C1 - 4 - hydroxy and alquiloxi alquiloxi c1-4 R7 represents Hydrogen or alkyl c1-4, R8 represents c1-4 alkyl substituted with nr25r26 or alquilsulfonilo c1-4 alkyl represents Hydrogen R12 or R13 represents c1-4, AR6 - sulfonyl or alquiloxicarbonilo C1 - 6 which is optionally substituted phenyl R16 and R17 represents Hydrogen,C1-4 alkyl or R16 and R17 taken together with the carbon Atom to which they are United to form a cycloalkyl C3 - 6 R23 represents c1-4 alkyl and R23 R16 and R17 represents Hydrogen when taken together with the carbon Atom to which they are United to form a cycloalkyl C3 R25, R26, 6R27, R28 each independently represents a hydrogen or alquilcarbonilo c1-4, het1 represents 2 - Bora - 1.3 - dioxolanilo het2 represents piperidinilo, piperazinilo, morfolinilo, tiomorfolinilo or 11 - dioxotiomorfolinilo where the het2 is optionally replaced with alquiloxicarbonilo c1-4 alkyl or nr27r28 c1-4, AR4 and AR5 represents phenyl, phenyl optionally substituted AR6 represents this with nitro.LA PRESENTE INVENCION SE REFIERE A LOS COMPUESTOS DE FORMULA LAS FORMAS DE N-OXIDOS, LAS SALES DE ADICION ACEPTABLES PARA USO FARMACEUTICO Y LAS FORMAS ESTEREOQUIMICAMENTE ISOMERICAS DE LAS M
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