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Pyrazolo-quinazolines as modulators of protein kinase activity
专利权人:
Les Laboratoires Servier
发明人:
CALDARELLI, Marina,ANGIOLINI, Mauro,COLOMBO, Riccardo,DISINGRINI, Teresa,NUVOLONI, Stefano,POSTERI, Helena,SALSA, Matteo,SILVAGNI, Marco
申请号:
ES09769164
公开号:
ES2572360T3
申请日:
2009.06.17
申请国别(地区):
ES
年份:
2016
代理人:
摘要:
Compound of formula (I): ** Formula ** where R1 is an orthosubstituted aryl group or a heterocyclyl or cycloalkyl (C3-C7) group; R2 is a hydrogen atom or a (C1-C6) alkyl, (C2-C6) alkenyl, (C2-C6) alkynyl, (C3-C7) cycloalkyl or straight or branched heterocyclyl group; R3 is aryl; R4 is a hydrogen atom, a hydroxyl or (C1-C6) alkyl group, this group may optionally be cyclized together with one of the atoms in the group that may represent R3 to form a fused cyclic (C4-C7) group; R5 and R6 are in each case, independently of each other, a hydrogen atom, (C1-C6) alkyl, or are optionally cycled together with the carbon atom to which they are attached to form a (C3-C7) cycloalkyl group, being "aryl" an aromatic carbocyclic or heteroaryl group containing 1 to 2 ring units, fused or linked together by simple bonds, at least one of the rings being aromatic; and comprising any aromatic heteroaryl ring (also known as aromatic heterocyclyl group), if present, a 5 to 6 member ring containing 1 to 3 heteroatoms selected from N, O or S; "orthosubstituted aryl" being an aryl group as defined above attached to the -NH- fraction, said aryl being always substituted in an ortho position, that is, on the adjacent ring atom to which it is attached to the -NH- fraction , and which is also optionally substituted in other free positions; "heterocyclyl" (also known as "heterocycloalkyl") being a 3- to 7-membered carbocyclic ring, saturated or partially unsaturated, where one or more carbon atoms have been replaced by heteroatoms such as nitrogen, oxygen and sulfur; being "cycloalkyl (C3-C7)", therefore including cycloalkyl (C4-C7), a monocyclic ring of 3 to 7 members all carbon, which may contain one or more double bonds but does not contain any electron system - fully conjugated ; where "C1-C6) is straight or branched alkyl", therefore including (C1-C4) alkyl, any of the groups such as, for example, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, tert -butyl, sec-butyl, n-pentyl, n-hexy
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