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:US5932729A

    公开(公告)日:1999-08-03

    申请号:US907402

    申请日:1997-08-07

    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 thatwhere 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; andwhere 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; andk 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: 公开了下式的化合物或其药学上可接受的盐,其中6元环可以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的基团取代的苯基 ; 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; 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。

    3-aminoalkylamino-2H-1,4-benzoxazines and 3-aminoalkylamino-2H-1,4-benzothiazines: dopamine receptor subtype specific ligands
    8.
    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

    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
    9.
    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

    IPC分类号: C07D40112

    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
    10.
    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

    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。