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发明公开
CN101778837A 作为NK3受体拮抗剂的吡咯烷芳基-醚 无效 - 撤回

作为NK3受体拮抗剂的吡咯烷芳基-醚
摘要：
本发明涉及通式I的化合物，或其药用活性盐，包括式I化合物的所有立体异构形式、单一非对映异构体和对映异构体以及其外消旋和非外消旋混合物，其中：Ar1是芳基或五或六元杂芳基；Ar2是芳基或五或六元杂芳基；R1是氢、卤素、低级烷基、低级烷氧基、卤素取代的低级烷基、卤素取代的低级烷氧基、S-低级烷基、-S(O)2-低级烷基、-S(O)2-二低级烷基氨基、-(CH2)qR、氰基、氨基、单或二低级烷基氨基、NHC(O)-低级烷基、环烷基，或者是任选地被低级烷基取代的五元杂芳基；其中R是氰基、二低级烷基氨基或吡咯烷-1-基；R2是氢、卤素、低级烷基、被卤素或氰基取代的低级烷基；R3是氢或低级烷基或CH2OH；R4是氢、卤素、低级烷基、被卤素或氰基取代的低级烷基；n是1、2或3；当n是2或3时，R1可以相同或不同；o是1、2或3；当o是2或3时，R2可以相同或不同；p是1、2或3；当p是2或3时，R4可以相同或不同；q是1或2。已经发现本发明化合物是高效的NK-3受体拮抗剂，用于治疗抑郁、疼痛、精神病、帕金森病、精神分裂症、焦虑或注意缺陷多动症(ADHD)。
摘要（英）：

The invention relates to a compound of general formula (I) wherein Ar1 is aryl or a five or six membered heteroaryl; Ar2 is aryl or a five or six membered heteroaryl; R1 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, S-lower alkyl, -S(O)2-lower alkyl, -S(O)2-di-lower alkyl amino, -(CH2)qR, cyano, amino, mono or di-lower alkyl amino, NHC(O)-lower alkyl, cycloalkyl or is or a five membered heteroaryl, optionally substituted by lower alkyl; wherein R is cyano, di-lower alkyl amino or pyrrolidin-1-yl; R2 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen or cyano; R3 is hydrogen or lower alkyl or CH2OH; R4 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen or cyano; n is 1, 2 or 3; in case n is 2 or 3, R1 may be the same or different; o is 1, 2 or 3; in case o is 2 or 3, R2 may be the same or different; p is 1, 2 or 3; in case p is 2 or 3, R4 may be the same or different; q is 1 or 2; or to a pharmaceutically active salt thereof, including all stereoisomeric forms, individual diastereoisomers and enantiomers of the compound of formula (I) as well as racemic and non-racemic mixtures thereof. It has been found that the present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).

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