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1. 发明公开

EP1147084A1 PHENYLSULPHONYL DERIVATIVES AS 5-HT RECEPTOR LIGANDS 有权
标题翻译： PHENYLSULPHONYLDERIVATIVE 5-HT受体配体
公开(公告)号：EP1147084A1
公开(公告)日：2001-10-24
申请号：EP00900723.8
申请日：2000-01-11
申请人： MERCK SHARP & DOHME LTD.
发明人： BLURTON, Peter , BURKAMP, Frank , CHENG, Susan, Koon-Fung , FLETCHER, Stephen, RobertTerlings Park , MACLEOD, Angus, Murray , VAN NIEL, Monique, Bodil , SPINKS, Daniel
IPC分类号： C07D211/54 , C07D401/10 , A61K31/445 , A61P25/00
CPC分类号： C07D231/12 , C07D211/54 , C07D233/56 , C07D249/08 , C07D401/10
摘要： A class of phenylsulphonyl derivatives wherein the sulphonyl moiety is also attached to an N-arylalkyl-substituted azetidine, pyrrolidine or piperidine ring are selective antagonists of the human 5-HT2A receptor and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of adverse conditions of the central nervous system, including schizophrenia and depression.

2. 发明授权

EP1147084B1 PHENYLSULPHONYL DERIVATIVES AS 5-HT RECEPTOR LIGANDS 有权
标题翻译：苯基磺酰基衍生物作为5-HT受体配体
公开(公告)号：EP1147084B1
公开(公告)日：2004-05-19
申请号：EP00900723.8
申请日：2000-01-11
申请人： MERCK SHARP & DOHME LTD.
发明人： BLURTON, Peter , BURKAMP, Frank , CHENG, Susan, Koon-Fung , FLETCHER, Stephen, Robert Terlings Park , MACLEOD, Angus, Murray , VAN NIEL, Monique, Bodil , SPINKS, Daniel
IPC分类号： C07D211/54 , C07D401/10 , A61K31/445 , A61P25/00
CPC分类号： C07D231/12 , C07D211/54 , C07D233/56 , C07D249/08 , C07D401/10
摘要： A class of phenylsulphonyl derivatives wherein the sulphonyl moiety is also attached to an N-arylalkyl-substituted azetidine, pyrrolidine or piperidine ring are selective antagonists of the human 5-HT2A receptor and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of adverse conditions of the central nervous system, including schizophrenia and depression.
摘要翻译：其中磺酰基部分也与N-芳基烷基取代的氮杂环丁烷，吡咯烷或哌啶环连接的一类苯磺酰基衍生物是人5-HT2A受体的选择性拮抗剂，因此可用作药物，特别是在治疗和/或预防中枢神经系统的不良状况，包括精神分裂症和抑郁症。

3. 发明公开

EP1280785A1 PHENYLSULPHONYLPIPERAZINYL DERIVATIVES AS 5-HT RECEPTOR LIGANDS 审中-公开
标题翻译： PHENYLSULPHONYLPIPERAZINYL衍生物作为5-HT受体配体
公开(公告)号：EP1280785A1
公开(公告)日：2003-02-05
申请号：EP01915573.8
申请日：2001-03-30
申请人： MERCK SHARP & DOHME LTD.
发明人： BURKAMP, Frank , CHENG, Susan, Koon-Fung , FLETCHER, Stephen Robert
IPC分类号： C07D295/26 , A61K31/495 , A61P25/18
CPC分类号： C07D295/26
摘要： A class of phenylsulphonyl derivatives of the following formula (I) wherein Z represents halogen, cyano, nitro, trifluoromethyl, trifluoromethoxy, -R?a, -ORa, -SRa, -SORa, -SO¿2Ra, -SO2NR?aRb, -NRaRb, -NRaCORb, -NRaCO¿2R?b; -CORa; -CO¿2Ra or -CONRaRb; or Z represents an optionally substituted five-membered heteroaromatic ring selected from furan, thiophene, pyrrole, oxazole, thiazole, isoxazole, isothiazole, imidazole, pyrazole, oxadiazole, thiadiazole, triazole and tetrazole; or Z represents an optionally substituted six-membered heteroaromatic ring selected from pyridine, pyrazine, pyrimidine and pyridazine; R?a and Rb¿ independently represent hydrogen of C¿1-6? alkyl, or R?a and Rb¿, when linked through a nitrogen atom, together represent the residue of an azetidine, pyrrolidine, piperidine or morpholine ring; E represents a chemical bond or a straight or branched alkylene chain containing from 1 to 4 carbon atoms, optionally incorporating an oxygen atom to form an ether linkage; R1 represents an optionally substituted aryl(C¿2-4?)alkyl group; and R?2¿ represents hydrogen or halogen, which are selective antagonists of the human 5-HT¿2A? receptor and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of adverse conditions of the central nervous system, including schizophrenia and depression.

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