;wherein, generally, ;Q is chemistry chemdraw filechemistry mol file;R1 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-piperidinyl)-1-phenylpropyl) substituted sulfonamides as NK-3 receptor antagonists
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N-(3-(4-substituted-1-piperidinyl)-1-phenylpropyl) substituted sulfonamides as NK-3 receptor antagonists
N-(3-(4-substituted-1-piperidinyl)-1-phenylpropyl) substituted sulfonamides as NK-3 receptor antagonists
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机译:N-(3-(4-取代-1-哌啶基)-1-苯基丙基)取代的磺酰胺类药物作为NK-3受体拮抗剂
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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: chemistry chemdraw filechemistry mol file;wherein, generally, ;Q is chemistry chemdraw filechemistry mol file;R1 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.
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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: <图像文件=“ US20040002504A1-20040101-C00001.GIF” he =“ 44.87805” id =“ EMI-C00001” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 90.72“ /> 化学化学绘图文件 ExternalFileRef> 化学分子文件 ExternalFileRef> Chemistry>;其中,通常,Q为 <图像文件=“ US20040002504A1-20040101-C00002.GIF” he =“ 32.886” id =“ EMI-C00002” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 82.81035“ /> 化学化学绘图文件 ExternalFileRef> 化学mol文件 ExternalFileRef> Chemistry>; R 1 Sup>是苄基,苯基,噻吩或咪唑基,可选地被C 1-4 Sub>烷基或卤素取代,如甲基,氟或溴; ; R 2 Sup>是氢或C 1-4 Sub>烷基,例如甲基; ; R 3 Sup>是苯基; ; R 4 Sup>是氢; ; R 5 Sup>是氢或C 1-6 Sub>烷基羰基,例如甲基羰基; ; X为&mdash; SO 2 Sub>&mdash;或&mdash; C(O)N(R 2 Sup>)SO 2 Sub>&mdash;其中R 2 Sup>优选为氢; ; Y是一个键,CH 2 Sub>或Z 1 Sup>,其中Z 1 Sup>是&ndash; N(R f Sup>) &mdash;其中R f Sup>是C 1-6 Sub>烷基羰基,例如乙基羰基; ; R 6和R 6是任选地被一个或两个选自C 1-6烷基和苄基的基团如甲基,乙基取代的苯基,吡唑基,吡啶基,嘧啶基或苯并咪唑啉基。和苄基; ;或其药学上可接受的盐。
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