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发明授权
CN101657418B 作为NK1/NK3受体双重拮抗剂的吡咯烷衍生物 失效 - 权利终止

作为NK1/NK3受体双重拮抗剂的吡咯烷衍生物
摘要：
本发明涉及式(I)的吡咯烷衍生物，其中R1是氢、卤素或低级烷基；R2是氢、卤素、低级烷氧基或被卤素取代的低级烷基；R3是-(CH2)p-杂环基，其任选被低级烷基、卤素、-S(O)2-低级烷基、-C(O)-低级烷基、-C(O)O-低级烷基、羟基、被羟基取代的低级烷基、-(CH2)p-O-低级烷基、-NHCO-低级烷基取代，或者是C3-6-环烷基，其任选被＝O、-(CH2)p-O-低级烷基或低级炔基取代，或者是未被取代的或被取代的芳基或杂芳基，其中取代基选自低级烷基、CN、-S(O)2-低级烷基、卤素、-C(O)-低级烷基、羟基、低级烷氧基或被卤素取代的低级烷氧基；或者是-(CH2)p-NR4R5；R4/R5彼此独立地是氢、低级烷基、被羟基取代的-(CRR’)p-低级烷基、-(CRR’)p-O-低级烷基、-(CRR’)p-S-低级烷基、被羟基取代的-(CRR’)p-O-低级烷基或C3-6-环烷基；R/R’彼此独立地是氢、低级烷基或被羟基取代的低级烷基；n 是1或2；0 是1或2；p 是0、1、2、3或4；或其有药学活性的酸加成盐。
摘要（英）：

The invention relates to pyrrolidine derivatives of formula (I) wherein R<1> is hydrogen, halogen or lower alkyl; R<2> is hydrogen, halogen, lower alkoxy or lower alkyl substituted by halogen; R<3> is -(CH2)p-heterocyclyl optionally substituted by lower alkyl, halogen, -S(O)2-lower alkyl, -C(O)-lower alkyl, -C(O)O-lower alkyl, hydroxy, lower alkyl substituted by hydroxy, -(CH2)p-O-lower alkyl, -NHCO-lower alkyl, or is C3-6-cycloalkyl optionally substituted by =O, -(CH2)p-O-lower alkyl or lower alkinyl, or is unsubstituted or substituted aryl or heteroaryl, wherein the substituents are selected from the group consisting of lower alkyl, CN, -S(O)2-lower alkyl, halogen, -C(O) -lower alkyl, hydroxy, lower alkoxy or lower alkoxy substituted by halogen; or is -(CH2)P-NR<4>R<5>; R<4>/R<5> are independently from each other hydrogen, lower alkyl, -(CRR')p-lower alkyl substituted by hydroxy, -(CRR')p-O-lower alkyl, -(CRR')p-S-lower alkyl, -(CRR')p-O-lower alkyl substituted by hydroxy or C3-6-cycloalkyl; R/R' are independently from each other hydrogen, lower alkyl or lower alkyl substituted by hydroxyl; n is 1 or 2; o is 1 or 2; P is 0, 1, 2, 3 or 4; or to pharmaceutically active acid-addition salts thereof.

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