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1-oxa-3,9-diaza-spiro '5.5 undecan-2-one derivatives and their use as a neurokinin receptor antagonist

机译:1-oxa-3,9-diaza-spiro'5.5]十一烷-2-酮衍生物及其作为神经激肽受体拮抗剂的用途

摘要

The invention relates to compounds of the general formulawherein(R1)n is independently from from each other halogen, lower alkyl or lower alkoxy;R2 is hydrogen, lower alkyl, lower halogen-alkyl, -(CH2)m-OH, -(CH2)m-NR2, -(CH2)mO-lower alkyl, -(CH2)m-C(O)-NR2, or is -(CH2)m-6-membered heteroaryl, optionally substituted by one or more lower alkoxy, -(CH2)m-5 or 6-membered not aromatic heterocyclyl, optionally substituted by hydroxy or lower alkyl;R is hydrogen or lower alkyl and may be the same or different in case of R2;n is 0, 1, or 2;m is 0, 1, 2, 3 or 4;and pharmaceutically acceptable acid addition salts thereof. These compounds have a good affinity to the NK-1 receptor and they are therefore suitable for the treatment of diseases, related to this receptor.
机译:本发明涉及通式化合物,其中(R1)n彼此独立地是卤素,低级烷基或低级烷氧基; R2是氢,低级烷基,低级卤代烷基,-(CH2)m-OH,-(CH2 )m-NR2,-(CH2)mO-低级烷基,-(CH2)mC(O)-NR2或为-(CH2)m-6元杂芳基,可选地被一个或多个低级烷氧基-(CH2 )m-5或6元非芳族杂环基,可选地被羟基或低级烷基取代; R为氢或低级烷基,在R2的情况下可以相同或不同; n为0、1或2; m为0 ,1、2、3或4;及其药学上可接受的酸加成盐。这些化合物对NK-1受体具有良好的亲和力,因此适合与该受体有关的疾病的治疗。

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