1-oxa-3,9-diaza-spiro [5,5] undecan-2-ones derivatives and its use as antagonist of the neurikinin receptor

本发明涉及通式(I)的化合物及其药学上可接受的酸加成盐：其中(R#+[1])#-[n]各自独立为卤素、低级烷基或低级烷氧基；R#+[2]为氢、低级烷基、低级卤素-烷基、-(CH#-[2])#-[m]-OH、-(CH#-[2])#-[m]-NR#-[2]、-(CH#-[2])#-[m]O-低级烷基、-(CH#-[2])#-[m]-C(O)-NR#-[2]，或者为任选被一个或多个低级烷氧基取代的-(CH#-[2])#-[m]-6-元杂芳基、任选被羟基或低级烷基取代的-(CH#-[2])#-[m]-5元或6-元非芳族杂环基；R为氢或低级烷基并且在R#+[2]时可以相同或不同；n为0、1或2；m为0、...

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Bibliographische Detailangaben
Hauptverfasser:	CAI HAIYING, M.P. DILLON, G. GALLEY
Format:	Patent
Sprache:	chi ; eng
Schlagworte:	CHEMISTRY HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Beschreibung
Zusammenfassung:	本发明涉及通式(I)的化合物及其药学上可接受的酸加成盐：其中(R#+[1])#-[n]各自独立为卤素、低级烷基或低级烷氧基；R#+[2]为氢、低级烷基、低级卤素-烷基、-(CH#-[2])#-[m]-OH、-(CH#-[2])#-[m]-NR#-[2]、-(CH#-[2])#-[m]O-低级烷基、-(CH#-[2])#-[m]-C(O)-NR#-[2]，或者为任选被一个或多个低级烷氧基取代的-(CH#-[2])#-[m]-6-元杂芳基、任选被羟基或低级烷基取代的-(CH#-[2])#-[m]-5元或6-元非芳族杂环基；R为氢或低级烷基并且在R#+[2]时可以相同或不同；n为0、1或2；m为0、1、2、3或4。上述化合物对NK-1受体有良好的亲合力，因此它们适合用于治疗与NK-1受体有关的疾病。 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.