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21 条记录 (耗时 0.037 秒)

    Substituted phenserines as specific inhibitors of acetylcholinesterase
    2.
    发明授权
    Substituted phenserines as specific inhibitors of acetylcholinesterase 失效
    取代的苯西林作为乙酰胆碱酯酶的特异性抑制剂

    公开(公告)号：US5171750A

    公开(公告)日：1992-12-15

    申请号：US765746

    申请日：1991-09-26

    申请人： Arnold Brossi ,  Malgarzota Brzostowska ,  Stanley I. Rapoport ,  Nigel Greig ,  Xiao-shu He

    发明人： Arnold Brossi ,  Malgarzota Brzostowska ,  Stanley I. Rapoport ,  Nigel Greig ,  Xiao-shu He

    IPC分类号： C07D487/04 ,  C07D491/04 ,  C07D491/048

    CPC分类号： C07D487/04 ,  C07D491/04

    摘要： The present invention relates to substituted phenylcarbamate or naphthylcarbamate tricyclic compounds which provide highly potent and selective cholinergic agonist and blocking activity and their use as pharmaceutical agents. The invention further relates to improvements in therapy relative to cholinergic diseases such as glacuoma, Myasthenia Gravis, Alzheimer's disease and to improvements in therapy and organophosphate poisoning. The invention further provides for a selective acetylcholinesterase and butyrylcholinesterase agents and a method for inhibiting these esterases.

    摘要翻译： 本发明涉及提供高效和选择性胆碱能激动剂和阻断活性的取代的苯基氨基甲酸酯或萘基氨基甲酸三环化合物及其作为药剂的用途。 本发明还涉及治疗相对于胆碱能疾病如冰川，重症肌无力，阿尔茨海默病以及治疗和有机磷酸盐中毒方面的改进。 本发明进一步提供选择性乙酰胆碱酯酶和丁酰胆碱酯酶及其抑制这些酯酶的方法。

    1-(N'-(arylalkylaminoalkyl)) aminoisoindoles; a new class of dopamine receptor subtype specific ligands
    3.
    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

    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 ,  C07D401/14 ,  C07D403/14

    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 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
    6.
    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
    7.
    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
    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：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
    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：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。