embedded imagewherein, generally, Q is embedded imageR1 is benzyl, phenyl, thiophene or imidazolyl optionally substituted with C1-4alkyl or halogen, such as methyl, fluorine or bromine; R2 is hydrogen or C1-4alkyl such as methyl; R3 is phenyl; R4 is hydrogen; R5 is hydrogen or C1-6alkylcarbonyl such as methylcarbonyl; X is —SO2— or —C(O)N(R2)SO2— where R2 is preferably hydrogen; Y is a bond, CH2 or Z1 where Z1 is —N(Rf)— in which Rf is C1-6alkylcarbonyl such as ethylcarbonyl; and R6 is phenyl, pyrazolyl, pyridyl, pyrimidinyl or benzimidazolonyl optionally substituted with one or two groups chosen from C1-6alkyl and benzyl, such as methyl, ethyl and benzyl; or a pharmaceutically acceptable salt thereof. "/> N-(3-(4-Substituted-1-piperiding1)-1-phenylpropyl) substituted sulfonamides as NK-3 receptor antagonists
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N-(3-(4-Substituted-1-piperiding1)-1-phenylpropyl) substituted sulfonamides as NK-3 receptor antagonists

机译:N-(3-(4-取代的1-哌啶基1)-1-苯丙基)取代的磺酰胺类药物作为NK-3受体拮抗剂

摘要

The present invention provides a method of treatment of a subject suffering from a disease, such as schizophrenia, for which the administration of an NK-3 antagonist is indicated which comprises administering to that subject a therapeutically effective amount of a compound of formula I: embedded imagewherein, generally, Q is embedded imageR1 is benzyl, phenyl, thiophene or imidazolyl optionally substituted with C1-4alkyl or halogen, such as methyl, fluorine or bromine; R2 is hydrogen or C1-4alkyl such as methyl; R3 is phenyl; R4 is hydrogen; R5 is hydrogen or C1-6alkylcarbonyl such as methylcarbonyl; X is —SO2— or —C(O)N(R2)SO2— where R2 is preferably hydrogen; Y is a bond, CH2 or Z1 where Z1 is —N(Rf)— in which Rf is C1-6alkylcarbonyl such as ethylcarbonyl; and R6 is phenyl, pyrazolyl, pyridyl, pyrimidinyl or benzimidazolonyl optionally substituted with one or two groups chosen from C1-6alkyl and benzyl, such as methyl, ethyl and benzyl; or a pharmaceutically acceptable salt thereof.
机译:本发明提供了一种治疗患有疾病如精神分裂症的对象的方法,针对该对象指示给予NK-3拮抗剂,该方法包括向该对象给予治疗有效量的式I化合物: “嵌入式图像” 其中,通常Q是 <图像alt =“嵌入式图像” file =“ US20070117847A1-20070524-C00002.GIF” he =“ 11.60mm” id =“ EMI-C00002” imgContent =“ chem” imgFormat =“ GIF” wi =“ 29.29mm” /> R 1 是苄基,苯基,噻吩或咪唑基,可选地被C 1-4 <烷基或卤素,例如甲基,氟或溴; R 2 是氢或C 1-4 烷基,例如甲基; R 3 是苯基; R 4 是氢; R 5 是氢或C 1-6 烷基羰基,例如甲基羰基; X是-SO 2 -或-C(O)N(R 2 ) SO 2 -其中R 2 优选为氢; Y是一个键,CH 2 或Z 1 其中Z 1 < / Sup>为–N(R f )-,其中R f 为C 1-6 烷基羰基,例如乙基羰基; R 6 是苯基,吡唑基,吡啶基,嘧啶基或苯并咪唑啉基,可选地被一个或两个选自C < Sub> 1-6 烷基和苄基,例如甲基,乙基和苄基;或其药学上可接受的盐。

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