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1. 发明授权

US06441175B1 1-(N'-arylalkylaminoalkyl)aminoisoquinolines: a new class of dopamine receptor subtype 失效
标题翻译： 1-（N'-芳基烷基氨基烷基）氨基异喹啉：新一类多巴胺受体亚型
公开(公告)号：US06441175B1
公开(公告)日：2002-08-27
申请号：US09885847
申请日：2001-06-20
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 , C07D217/22 , C07D403/12
摘要： Disclosed are compounds of the formula or the pharmaceutically acceptable salts thereof wherein the variables R5, R11, R12, R13, R1, R11, Ar, n, m and L are defined herein. These 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 affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism. Furthermore, compounds of this invention may be useful in treating the extrapyramidyl side effects associated with the use of conventional neuroleptic agents. The interaction of 1-(N′-(arylalkylaminoalkyl))aminoisoindole derivatives of the invention with dopamine receptor subtypes is described. This interaction results in the pharmacological activities of these compounds.
摘要翻译：公开了下列化合物或其药学上可接受的盐，其中变量R5，R11，R12，R13，R1，R11，Ar，n，m和L在本文中定义。这些化合物可用于治疗各种神经心理障碍，包括例如，精神分裂症，痴呆，抑郁症，焦虑症，类似帕金森综合征的运动障碍以及与使用精神分裂症药物，情感障碍如精神分裂症和抑郁症以及某些运动障碍如帕金森综合征有关的运动障碍。此外，本发明的化合物可用于治疗与常规精神抑制剂的使用相关的外贴剂副作用。描述了本发明的1-（N' - （芳基烷基氨基烷基））氨基异吲哚衍生物与多巴胺受体亚型的相互作用。这种相互作用导致这些化合物的药理活性。

2. 发明授权

US06252077B1 1-(N′-(arylalkylaminoalkyl) aminoisoquinolines; a new class of dopamine receptor subtype specific ligands 失效
标题翻译： 1-（N' - （芳基烷基氨基烷基）氨基异喹啉;一类新的多巴胺受体亚型特异性配体
公开(公告)号：US06252077B1
公开(公告)日：2001-06-26
申请号：US09470594
申请日：1999-12-22
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： C07D20940
CPC分类号： C07D401/12 , C07D209/44 , C07D217/22 , 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; m represents an integer; n is 0, or an integer; R12 and R13 independently represent lower alkyl; CR′R″ represent a methylene group optionally substituted with lower alkyl; and k is 1, which compounds are useful in treating various neuropsychological 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是碳，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，R11表示电子对; R5是氢或低级烷基; m表示整数; n是0或整数; R12和R13独立地表示低级烷基; CR'R“表示任选的亚甲基被低级烷基取代; andk是1，哪些化合物可用于治疗各种神经心理障碍，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. 发明授权

US5656632A 1-(N'-(arylalkylaminoalkyl)) aminoisoindoles; dopamine receptor subtype specific ligands 失效
标题翻译： 1-（N' - （芳基烷基氨基烷基））氨基异吲哚; 多巴胺受体亚型特异性配体
公开(公告)号：US5656632A
公开(公告)日：1997-08-12
申请号：US463037
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 , C07D217/02 , C07D401/00
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 heteroarylZ 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。

4. 发明授权

US5602168A 1-(N'-(arylalkylaminoalkyl)) aminoisoindoles; dopamine receptor subtype specific ligands 失效
标题翻译： 1-（N' - （芳基烷基氨基烷基））氨基异吲哚; 多巴胺受体亚型特异性配体
公开(公告)号：US5602168A
公开(公告)日：1997-02-11
申请号：US464336
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 , A61K31/40 , A61K31/33 , C07D217/02 , C07D263/16
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 heteroarylZ 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。

5. 发明授权

US06245768B1 1-(N′-(arylalkylaminoalkyl)) aminoisoindoles; a new class of dopamine receptor subtype specific ligands 失效
标题翻译： 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。

6. 发明授权

US5744472A 1-(N'-(arylalkylaminoalkyl)) aminoisoindoles; a new class of dopamine receptor subtype specific ligands 失效
标题翻译： 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。

7. 发明授权

US5932729A 1-(N'-(arylalkylaminoalkyl)) aminoisoindoles; a new class of dopamine receptor subtype specific ligands 失效
标题翻译： 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。

8. 发明授权

US06384224B2 Certain 1-(2-naphthyl) and 1-(2-azanaphthyl)-4-(1-phenylmethyl) piperazines; dopamine receptor subtype specific ligands 失效
标题翻译：某些1-（2-萘基）和1-（2-氮杂萘基）-4-（1-苯基甲基）哌嗪; 多巴胺受体亚型特异性配体
公开(公告)号：US06384224B2
公开(公告)日：2002-05-07
申请号：US09897352
申请日：2001-07-02
申请人： William Greenlee , Ashit Gangly , Jan W. F. Wasley
发明人： William Greenlee , Ashit Gangly , Jan W. F. Wasley
IPC分类号： C07D40304
CPC分类号： C07D215/38 , C07D239/74 , C07D239/84 , C07D241/44 , C07D295/03 , C07D295/073 , C07D405/12
摘要： Disclosed are compounds of the formula: or pharmaceutically acceptable addition salts thereof, wherein: X, Y and Z are the same or different and represent optionally substituted carbon or nitrogen; R1 and R2 independently represent organic or inorganic substituents; R3 and R4 are variables independently representing inorganic or organic substituents; A represents C1-C4 alkylene; and R5, R6, and R7 independently represent hydrogen or C1-C6 alkyl, 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加成盐，其中：X，Y和Z相同或不同，表示任选取代的碳或氮; R 1和R 2独立地表示有机或无机取代基; R 3和R 4独立地是变量代表无机或有机取代基; A代表C1-C4亚烷基; R 5，R 6和R 7独立地表示氢或C 1 -C 6烷基，该化合物以高亲和力与多巴胺D4受体亚型选择性结合，因此可用于治疗各种神经心理障碍。

9. 发明授权

US06331629B1 Certain 1-(2-naphthyl) and 1-(2-azanaphthyl)-4-(1-phenylmethyl)piperazines; dopamine receptor subtype specific ligands 失效
标题翻译：某些1-（2-萘基）和1-（2-氮杂萘基）-4-（1-苯基甲基）哌嗪; 多巴胺受体亚型特异性配体
公开(公告)号：US06331629B1
公开(公告)日：2001-12-18
申请号：US09522139
申请日：2000-03-09
申请人： William Greenlee , Ashit Gangly , Jan W. F. Wasley
发明人： William Greenlee , Ashit Gangly , Jan W. F. Wasley
IPC分类号： C07D295096
CPC分类号： C07D215/38 , C07D239/74 , C07D239/84 , C07D241/44 , C07D295/03 , C07D295/073 , C07D405/12
摘要： Disclosed are compounds of the formula: or pharmaceutically acceptable addition salts thereof, wherein: X, Y and Z are the same or different and represent optionally substituted carbon or nitrogen; R1 and R2 independently represent organic or inorganic substituents; R3 and R4 are variables independently representing inorganic or organic substituents; A represents C1-C4 alkylene; and R5, R6, and R7 independently represent hydrogen or C1-C6 alkyl, 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加成盐，其中：X，Y和Z相同或不同，表示任选取代的碳或氮; R 1和R 2独立地表示有机或无机取代基; R 3和R 4独立地是变量代表无机或有机取代基; A代表C1-C4亚烷基; R 5，R 6和R 7独立地表示氢或C 1 -C 6烷基，该化合物以高亲和力与多巴胺D4受体亚型选择性结合，因此可用于治疗各种神经心理障碍。

10. 发明授权

US5478934A Certain 1-substituted aminomethyl imidazole and pyrrole derivatives: novel dopamine receptor subtype specific ligands 失效
标题翻译：某些1-取代氨基甲基咪唑和吡咯衍生物：新型多巴胺受体亚型特异性配体
公开(公告)号：US5478934A
公开(公告)日：1995-12-26
申请号：US344498
申请日：1994-11-23
申请人： Jun Yuan , Jan W. F. Wasley
发明人： Jun Yuan , Jan W. F. Wasley
IPC分类号： C07D233/54 , C07D401/06 , C07D403/12 , C07D498/04 , C07D401/14 , C07D403/06
CPC分类号： C07D233/64 , C07D401/06 , C07D403/12
摘要： Disclosed are compounds of the formula: ##STR1## wherein: A represents arylalkyl, aryl or heteroaryl; X is nitrogen or CH; and R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent organic or inorganic substituents;and the pharmaceutically acceptable salts thereof; useful for treating disorders of the central nervous system.
摘要翻译：公开了下式的化合物：其中：A表示芳烷基，芳基或杂芳基; X是氮或CH; R2，R3，R4和R5代表有机或无机取代基; 及其药学上可接受的盐; 可用于治疗中枢神经系统疾病。

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