申请人:ALMIRALL SA
公开号:WO2011113578A1
公开(公告)日:2011-09-22
The present invention relates to an oxadiazole derivative of formula (I)1 or a pharmaceutically acceptable salt or N-oxide thereof: wherein, R1 represents a hydrogen atom, a C1-2 alkyl group or a C3-4 cycloalkyl-C1-2 alkyl group, both R2 and R3 represent a C1-2 alkyl group; Ra represents a hydrogen atom or a C1-2 alkyl group; Rb represents a hydrogen atom, a C1-2 alkyl group, a C3-4, cycloalkyl group, a carboxy group, a carbamoyl group or a -CF3 group; Rc represents a linear or branched C2.5 alkyl group substituted with one substituent selected from a hydroxy group, a triazolyl group and a -P(O)(OH)2 group; a -(CH2)(1-2)-C(O)OR' group; a -NR'R" group; a -(CH2)(1-2NR'R" group; a -(CH2)(1-2)-NHC(O)R" group; a -(CH2)(2-4)NH-(CH2)(1-3)-NR'R" group; or a -O-(CH2)(2-3)NR'R" group, wherein: R' represents a hydrogen atom or a C1-2 alkyl group, R" represents a hydrogen atom; a C5-6 cycloalkyl group substituted with a carboxy group; a 5- to 6-membered saturated heterocyclic ring containing one nitrogen atom and substituted with a carboxy(C1-2alkyl) group; or a C1-2 alkyl group optionally substituted by one or more substituents selected from halogen atoms, hydroxy groups, methyl groups, amino groups, carbamoyl groups and carboxy groups; or R' and R" together with the nitrogen atom to which they are attached form (a) a 4 to 6 membered saturated or unsaturated heterocyclic group, which contains, as heteroatom, one N atom and, optionally, one further N atom and which heterocyclic group is substituted with one or more substituents selected from a halogen atom, a hydroxy group, a methyl group, an oxy group and a carboxy group, or (b) a 5 membered heteroaryl group which contains, as heteroatom, one N atom and, optionally, one or more further N atoms and which heteroaryl group is optionally substituted with one substituent selected from an amino group and a carboxy group.
本发明涉及式(I)1的噁二唑衍生物或其药用盐或N-氧化物:其中,R1表示氢原子,C1-2烷基或C3-4环烷基-C1-2烷基;R2和R3都表示C1-2烷基;Ra表示氢原子或C1-2烷基;Rb表示氢原子,C1-2烷基,C3-4环烷基,羧基,脒基或- CF3基;Rc表示用羟基,三唑基和-O-(OH)2基中选择的一个取代基取代的直链或支链C2.5烷基;-(CH2)(1-2)-C(O)OR'基;-NR'R"基;-(CH2)(1-2)NR'R"基;-(CH2)(1-2)-NHC(O)R"基;-(CH2)(2-4)NH-(CH2)(1-3)-NR'R"基;或-O-(CH2)(2-3)NR'R"基,其中:R'表示氢原子或C1-2烷基,R"表示氢原子;用羧基取代的C5-6环烷基;含有一个氮原子并用羧基(C1-2烷基)基团取代的5至6元饱和杂环;或用卤素原子,羟基,甲基,氨基,脒基和羧基中选择的一个或多个取代基取代的C1-2烷基;或R'和R"与它们连接的氮原子一起形成(a)含有一个N原子和一个或多个N原子的4至6元饱和或非饱和杂环,该杂环被卤素原子,羟基,甲基,氧基和羧基中的一个或多个取代基取代,或(b)含有一个N原子和一个或多个N原子的5元杂芳基,该杂芳基可被氨基和羧基中的一个取代基取代。