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    3-aminoalkylamino-2H-1,4-benzoxazines and 3-aminoalkylamino-2H-1,4-benzothiazines: dopamine receptor subtype specific ligands
    3.
    发明授权
    3-aminoalkylamino-2H-1,4-benzoxazines and 3-aminoalkylamino-2H-1,4-benzothiazines: dopamine receptor subtype specific ligands 失效
    3-氨基烷基氨基-2H-1,4-苯并恶嗪和3-氨基烷基氨基-2H-1,4-苯并噻嗪类：多巴胺受体亚型特异性配体

    公开(公告)号：US06432946B1

    公开(公告)日：2002-08-13

    申请号：US09633042

    申请日：2000-08-04

    申请人： Xiao-shu He

    发明人： Xiao-shu He

    IPC分类号： A61K3154

    CPC分类号： C07D413/12 ,  C07D265/36 ,  C07D417/12

    摘要： Disclosed are compounds of the formula: or the pharmaceutically acceptable acid addition salts thereof, wherein: Ar represents aryl or heteroaryl; R1 and R2 are the same or different and represent organic or inorganic substituents; R5 is hydrogen or C1-C6 alkyl; W represents CH or nitrogen; X is oxygen or sulfur; and A represents an alkylene group, which compounds bind selectively with high affinity to the dopamine D4 receptor subtype and are therefore of use in treatment of various neuropsychological disorders.

    摘要翻译： 公开了下式的化合物或其药学上可接受的酸加成盐，其中：Ar表示芳基或杂芳基; R 1和R 2相同或不同，表示有机或无机取代基; R 5表示氢或C 1 -C 6烷基; W表示 CH或氮; X为氧或硫; 并且A表示亚烷基，该化合物以高亲和力选择性结合多巴胺D4受体亚型，因此可用于治疗各种神经心理障碍。

    1-(N′-(arylalkylaminoalkyl)) aminoisoindoles; a new class of dopamine receptor subtype specific ligands
    4.
    发明授权
    1-(N′-(arylalkylaminoalkyl)) aminoisoindoles; a new class of dopamine receptor subtype specific ligands 失效
    1-（N' - （芳基烷基氨基烷基））氨基异吲哚; 一类新的多巴胺受体亚型特异性配体

    公开(公告)号：US06245768B1

    公开(公告)日：2001-06-12

    申请号：US09366371

    申请日：1999-08-03

    申请人： Xiao-shu He ,  Brian de Costa ,  Jan W. F. Wasley

    发明人： Xiao-shu He ,  Brian de Costa ,  Jan W. F. Wasley

    IPC分类号： C07D40112

    CPC分类号： C07D401/12 ,  C07D209/44 ,  C07D403/12

    摘要： Disclosed are compounds of the formula or the pharmaceutically acceptable salts thereof wherein the 6-membered A ring may be optionally substituted with up to four groups independently selected from halogen, hydroxy, lower alkyl, or lower alkoxy; Ar represents optionally substituted aryl or heteroaryl Z represents carbon or nitrogen provided that where Z is carbon, R11 represents hydrogen, halogen, hydroxy, lower alkyl, or lower alkoxy, or phenyl optionally substituted with one or two groups selected from hydrogen, halogen, hydroxy, lower alkyl, or lower alkoxy; and where Z is nitrogen, R11 represents an electron pair; R5 is hydrogen or lower alkyl, L and m represent integers; n is 0, or an integer; R12 and R13 independently represent lower alkyl; or together may together form an optionally substituted 5-11 membered ring with the nitrogen atoms to which they are bonded;CR′R″ represents a methylene group optionally substituted with lower alkyl;and k is an integer of from 1 to 3, which compounds are useful in treating various neuropsychochological disorders including, for example, schizophrenia, dementia, depression, anxiety, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents.

    摘要翻译： 公开的是式的化合物或其药学上可接受的盐，其中6元环可任选被至多四个独立地选自卤素，羟基，低级烷基或低级烷氧基的基团取代; Ar表示任选取代的芳基或杂芳基Z表示碳或 氮，其中Z为碳，R 11表示氢，卤素，羟基，低级烷基或低级烷氧基，或任选被一个或两个选自氢，卤素，羟基，低级烷基或低级烷氧基的基团取代的苯基; 并且其中Z是氮，R 11表示电子对; R 5是氢或低级烷基，L和m表示整数; n是0或整数; R 12和R 13独立地代表低级烷基; 或者一起可以与它们所键合的氮原子一起形成任选取代的5-11元环; CR'R“表示任选被低级烷基取代的亚甲基;并且k是1至3的整数，其中 化合物可用于治疗各种神经精神障碍，包括例如精神分裂症，痴呆，抑郁症，焦虑症，帕金森样运动障碍和与使用神经安定药相关的运动障碍。

    3-aminoalkylamino-2H-1,4-benzoxazines and 3-aminoalkylamino-2H-1,4-benzothiazines: dopamine receptor subtype specific ligands
    5.
    发明授权
    3-aminoalkylamino-2H-1,4-benzoxazines and 3-aminoalkylamino-2H-1,4-benzothiazines: dopamine receptor subtype specific ligands 失效
    3-氨基烷基氨基-2H-1,4-苯并恶嗪和3-氨基烷基氨基-2H-1,4-苯并噻嗪类：多巴胺受体亚型特异性配体

    公开(公告)号：US6100255A

    公开(公告)日：2000-08-08

    申请号：US181624

    申请日：1998-10-28

    申请人： Xiao-shu He

    发明人： Xiao-shu He

    IPC分类号： C07D265/36 ,  C07D413/12 ,  C07D417/12 ,  A61K31/496 ,  A61K31/5355

    CPC分类号： C07D413/12 ,  C07D265/36 ,  C07D417/12

    摘要： Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof, wherein:Ar represents aryl or heteroaryl;R.sub.1 and R.sub.2 are the same or different and represent organic or inorganic substituents;R.sub.5 is hydrogen or C.sub.1 -C.sub.6 alkyl;W represents CH or nitrogen;X is oxygen or sulfur; andA represents an alkylene group,which compounds bind selectively with high affinity to the dopamine D.sub.4 receptor subtype and are therefore of use in treatment of various neuropsychological disorders.

    摘要翻译： 公开了下式的化合物或其药学上可接受的酸加成盐，其中：Ar表示芳基或杂芳基; R1和R2相同或不同，代表有机或无机取代基; R5是氢或C1-C6烷基; W表示CH或氮; X是氧或硫; 并且A表示亚烷基，该化合物以高亲和力选择性结合多巴胺D4受体亚型，因此可用于治疗各种神经心理障碍。

    1-(N'-(arylalkylaminoalkyl)) aminoisoindoles; a new class of dopamine receptor subtype specific ligands
    6.
    发明授权
    1-(N'-(arylalkylaminoalkyl)) aminoisoindoles; a new class of dopamine receptor subtype specific ligands 失效
    1-（N' - （芳基烷基氨基烷基））氨基异吲哚; 一类新的多巴胺受体亚型特异性配体

    公开(公告)号：US5744472A

    公开(公告)日：1998-04-28

    申请号：US463430

    申请日：1995-06-05

    申请人： Xiao-shu He ,  Brian de Costa ,  Jan W. F. Wasley

    发明人： Xiao-shu He ,  Brian de Costa ,  Jan W. F. Wasley

    IPC分类号： C07D209/44 ,  C07D401/12 ,  C07D403/12 ,  A61K31/495 ,  A61K31/50 ,  C07D401/02 ,  C07D403/02

    CPC分类号： C07D401/12 ,  C07D209/44 ,  C07D403/12

    摘要： Disclosed are compounds of the formula ##STR1## or the pharmaceutically acceptable salts thereof wherein the 6-membered A ring may be optionally substituted with up to four groups independently selected from halogen, hydroxy, lower alkyl, or lower alkoxy; Ar represents optionally substituted aryl or heteroaryl Z represents carbon or nitrogen provided that where Z is carbon, R.sub.11 represents hydrogen, halogen, hydroxy, lower alkyl, or lower alkoxy, or phenyl optionally substituted with one or two groups selected from hydrogen, halogen, hydroxy, lower alkyl, or lower alkoxy; and where Z is nitrogen, R.sub.11 represents an electron pair; R.sub.5 is hydrogen or lower alkyl; L and m represent integers; n is 0, or an integer; R.sub.12 and R.sub.13 independently represent lower alkyl; or together may together form an optionally substituted 5-11 membered ring with the nitrogen atoms to which they are bonded;CR'R" represents a methylene group optionally substituted with lower alkyl; and k is an integer of from 1 to 3, which compounds are useful in treating various neuropsychochological disorders including, for example, schizophrenia, dementia, depression, anxiety, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents.

    摘要翻译： 公开了式IMA的化合物或其药学上可接受的盐，其中6元环可任选被至多四个独立地选自卤素，羟基，低级烷基或低级烷氧基的基团取代; Ar表示任选取代的芳基或杂芳基Z表示碳或氮，条件是其中Z为碳，R11表示氢，卤素，羟基，低级烷基或低级烷氧基，或任选被一个或两个选自氢，卤素，羟基 ，低级烷基或低级烷氧基; 并且其中Z是氮，R11表示电子对; R5是氢或低级烷基; L和m表示整数; n为0，或整数; R 12和R 13独立地表示低级烷基; 或一起可以一起形成与它们所键合的氮原子的任选取代的5-11元环; CR'R“表示任选被低级烷基取代的亚甲基; k为1〜3的整数，该化合物可用于治疗各种神经精神障碍，包括精神分裂症，痴呆，抑郁症，焦虑症，帕金森样运动障碍以及与使用精神抑制药有关的运动障碍。

    2-piperazinoalkylaminobenzoazole derivatives: dopamine receptor subtype specific ligands
    9.
    发明授权
    2-piperazinoalkylaminobenzoazole derivatives: dopamine receptor subtype specific ligands 失效
    2-哌嗪基烷基氨基苯并唑衍生物：多巴胺受体亚型特异性配体

    公开(公告)号：US06432958B1

    公开(公告)日：2002-08-13

    申请号：US09942219

    申请日：2001-08-29

    申请人： Xiao Shu He

    发明人： Xiao Shu He

    IPC分类号： A61K31496

    CPC分类号： C07D263/58 ,  C07D235/30 ,  C07D277/82 ,  C07D413/12 ,  C07D417/12

    摘要： Disclosed are compounds of the formula: or pharmaceutically acceptable salts thereof, wherein: A is (un)substituted alkylene; R1 and R2 are the same or different and represent hydrogen, halogen, alkyl, alkoxy, alkylthio, hydroxy, (un)substituted amino, cyano, nitro, sulfonamide, trifluoromethyl or trifluoromethoxy; R3, R4, R5, R6, and R8 are independently hydrogen or alkyl; and X is sulfur, oxygen or NR7 where R8 is defined herein; m is an integer chosen from 0, 1 or 2; and Ar is an aryl or heteroaryl group as further defined herein, which compounds are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents.

    摘要翻译： 公开了下式的化合物或其药学上可接受的盐，其中：A是（未）取代的亚烷基; R 1和R 2相同或不同，表示氢，卤素，烷基，烷氧基，烷硫基，羟基，（取代的）取代的氨基 氰基，硝基，磺酰胺，三氟甲基或三氟甲氧基; R3，R4，R5，R6和R8独立地为氢或烷基; 并且X是硫，氧或NR 7，其中R 8在本文中定义; m是选自0,1或2的整数; 并且Ar是本文进一步定义的芳基或杂芳基，所述化合物可用于治疗和/或预防神经心理障碍，包括但不限于精神分裂症，躁狂症，痴呆，抑郁症，焦虑症，强迫行为，药物滥用，帕金森病 类运动障碍和与使用精神安定药有关的运动障碍。