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2, 4 -DIAMINO PYRIMIDINE EN TANT QU'INHIBITEURS DE KINASES DU CYCLE CELLULAIRE
专利权人:
BOEHRINGER INGELHEIM INTERNATIONAL GMBH
发明人:
ZAHN, STEPHAN KARL,BISTER, BOJAN,BOEHMELT, GUIDO,GUERTLER, ULRICH,MANTOULIDIS, ANDREAS,REISER, ULRICH,SCHOOP, ANDREAS,SOLCA, FLAVIO,TONTSCH-GRUNT, ULRIKE,TREU, MATTHIAS
申请号:
EP07729171.4
公开号:
EP2027107B1
申请日:
2007.05.15
申请国别(地区):
EP
年份:
2012
代理人:
摘要:
Die vorliegende Erfindung umfasst Verbindungen der allgemeinen Formel (1) worin R1, R2, R4, Rg, X, m, n und p wie in Anspruch 1 definiert sind, welche zur Behandlung von Krankheiten, die durch exzessive oder anomale Zellproliferation charakterisiert sind, geeignet sind, sowie deren Verwendung zur Herstellung eines Arzneimittels mit den vorstehend genannten Eigenschaften.2,4-Diamino pyrimidine compounds (I) and their tautomers, racemates, enantiomers and/or diastereomers, and optionally their acid addition salts, are new. 2,4-Diamino pyrimidine compounds of formula (I) and their tautomers, racemates, enantiomers and/or diastereomers, and optionally their acid addition salts, are new. X : N or CH; R 1>;3-10C cycloalkyl (substituted with R 3>; and optionally with one or more R 4>;); R 2>;H, halo, -CN, -NO 2, 1-4C (halo)alkyl, 3-10C cycloalkyl, 4-16C cycloalkylalkyl or 7-16C arylalkyl; R 3>;-C(O)Rc, -C(O)ORC, -C(O)NRCRC, -S(O)2RC, -N(Rf)S(O)2Rc, -N(Rf)C(O)Rc, -N(Rf)C(O)ORc or -N(Rf)C(O)NRcRc; R 4>;Ra or Rb (where Ra is substituted by Rc and/or Rb); Ra : 1-6C alkyl, 3-10C cycloalkyl, 4-16C cycloalkylalkyl, 6-10C aryl, 7-16C arylalkyl, 2-6 membered heteroalkyl, 3-8 membered heterocycloalkyl, 4-14 membered heterocycloalkylalkyl, 5-12 membered heteroaryl or 6-18 membered heteroarylalkyl; Rb : O=, -ORc, 1-3C haloalkyloxy, -OCF 3, =S, -SRc, =NRc, =NORc, -NRcRc, halo, -CF 3, -CN, -NC, -OCN, -SCN, -NO 2, -S(O)Rc, -S(O) 2Rc, -S(O) 2ORc, -S(O)NRcRc, -S(O) 2NRcRc, -OS(O)Rc, -OS(O) 2Rc, -OS(O) 2ORc, -OS(O) 2NRcRc, -C(O)Rc, -C(O)ORc, -C(O)NRcRc, -CN(Rf)NRcRc, -CN(OH)Rc, -CN(OH)NRcRc, -OC(O)Rc, -OC(O)ORc, -OC(O)NRcRc, -OCN(Rf)NRcRc, -N(Rf)C(O)Rc, -N(Rf)C(S)Rc, -N(Rf)S(O) 2Rc, -N(Rf)C(O)ORc, -N(Rf)C(O)NRcRc, -[N(Rf)C(O)] 2Rc, -N[C(O)] 2Rc, -N[C(O)] 2ORc, -[N(Rf)C(O)] 2ORc or -N(Rf)CN(Rf)NRcRc; Rc : H or optionally Rd and/or Re substituted 1-6C alkyl, 3-10C cycloalkyl, 4-11C cycloalkylalkyl, 6-10C aryl, 7-16C arylalkyl, 2-6 membered heteroalkyl, 3-8 membered heterocycloalky
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