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NEW AMINOPYRIMIDINE DERIVATIVES AS PLK1 INHIBITORS
专利权人:
MSD K.K.
发明人:
KhASIKhAJaTA Takasi (JP),ХАСИХАЯТА Такаси (JP),KAVAMURA Mikako (JP),КАВАМУРА Микако (JP),MITsUJa Morikhiro (JP),МИЦУЯ Морихиро (JP),SATOKh Josijuki (JP),САТОХ Йосиюки (JP),KHASIKHAJATA TAKASI,KAVAMURA MIKAKO,MITSUJA MORIKHIRO,SATOKH JOSIJUKI
申请号:
RU2009128966/04
公开号:
RU0002458062C2
申请日:
2007.12.20
申请国别(地区):
RU
年份:
2012
代理人:
摘要:
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to to new compounds of formula (1) or their pharmaceutically acceptable salts, optionally in the form of (1S)-isomers showing the properties of polo-like kinase (serine-threonine kinase) PLK1 inhibitor. In the compounds of formula (1) , R1 represents a halogen atom; a lower alkyl group having 1-2 carbon atoms, which can be substituted by 3 fluorine atoms; or a cyclopropyl group; R2 represents a hydrogen atom; one of R3 and R4 represents a hydrogen atom while the other one of R3 and R4 represents: a) a lower alkyl group substituted by NRaRb wherein each Ra and Rb, which can be identical or different, represent a lower alkyl group, or each Ra and Rb, which can be different, represent a hydrogen atom, a lower alkyl group or a cycloalkyl group having 3-6 carbon atoms wherein a cycloalkyl group can be substituted by one ore more substitutes which can be identical or different and specified in a group 1): a lower alkyl; b) a 4-6-member aliphatic heterocyclic group specified in an azetidinyl group, a pyrrolidinyl group and a piperidinyl group; c) a lower alkyl group substituted by a 4-6-member aliphatic heterocyclic group specified in an azetidinyl group, a pyrrolidinyl group and a piperidinyl group; d) a 6-member aromatic heterocyclic group specified in a pyridyl group wherein each of an aliphatic heterocyclic group and an aromatic heterocyclic group can be substituted by substitutes specified in a group 1) described above; R5 represents a hydrogen atom, a cyano group, a halogen atom or a lower alkyl group.EFFECT: compounds can find application in treating oncological diseases.10 cl, 4 dwg, 8 tbl, 42 exИзобретение относится к новым соединениям формулы (I) или их фармацевтически приемлемым солям, возможно в виде (1S)-изомеров, обладающих свойствами ингибитора семейства поло-подобных киназ(серино-треониновых киназ) PLK1. Соединения могут найти применение при лечении опухолевых заболеваний. В соединениях формулы (I
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