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1. 发明授权

US6121260A Method of treating conditions susceptible to modulation of NPY receptors with diarylimidazole derivatives 失效
标题翻译：用二芳基咪唑衍生物处理易受NPY受体调节的条件的方法
公开(公告)号：US6121260A
公开(公告)日：2000-09-19
申请号：US109558
申请日：1998-07-02
申请人： Andrew Thurkauf , Jun Yuan , Alan Hutchison , Charles A. Blum , Richard L. Elliot , Marlys Hammond
发明人： Andrew Thurkauf , Jun Yuan , Alan Hutchison , Charles A. Blum , Richard L. Elliot , Marlys Hammond
IPC分类号： A61K31/40 , A61K31/4164 , A61K31/4178 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/495 , A61K31/538 , A61K31/5415 , A61P3/04 , A61P9/00 , A61P43/00 , C07D233/54 , C07D233/64 , C07D401/04 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07D413/04 , C07D417/04 , A61K31/54 , A61K31/4166 , A61K31/5377 , A61K31/541
CPC分类号： C07D233/64 , C07D401/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07D413/04 , C07D417/04
摘要： Certain diaryl imidazoles act as partial agonists or antagonists for NPY receptors, in particular NPY 5 receptors. They are of use, for example in treating loss of appetite. Such compounds bear aryl groups in the 2 position. Many of the compounds are novel.
摘要翻译：某些二芳基咪唑作为NPY受体特别是NPY 5受体的部分激动剂或拮抗剂。它们是有用的，例如用于治疗食欲不振。这种化合物在2位上带有芳基。许多化合物是新颖的。

2. 发明授权

US06515133B1 Pharmaceutical compositions containing certain diarylimidazole derivatives 失效
标题翻译：含有某些二芳基咪唑衍生物的药物组合物
公开(公告)号：US06515133B1
公开(公告)日：2003-02-04
申请号：US09523328
申请日：2000-03-10
申请人： Andrew Thurkauf , Jun Yuan , Alan Hutchison , Charles A. Blum , Richard L. Elliott , Marlys Hammond
发明人： Andrew Thurkauf , Jun Yuan , Alan Hutchison , Charles A. Blum , Richard L. Elliott , Marlys Hammond
IPC分类号： C07D40104
CPC分类号： C07D233/64 , C07D401/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07D413/04 , C07D417/04
摘要： Certain diaryl imidazoles act as partial agonists or antagonists for NPY receptors, in particular NPY 5 receptors. They are of use, for example in treating loss of appetite. Such compounds bear aryl groups in the 2 position. Many of the compounds are novel.
摘要翻译：某些二芳基咪唑作为NPY受体特别是NPY 5受体的部分激动剂或拮抗剂。它们是有用的，例如用于治疗食欲不振。这种化合物在2位上带有芳基。许多化合物是新颖的。

3. 发明授权

US5677454A Certain methylpiperazinyl and methylpiperidinyl substituted biphenyl derivatives; novel dopamine receptor subtype selective ligands 失效
标题翻译：某些甲基哌嗪基和甲基哌啶基取代的联苯衍生物; 新型多巴胺受体亚型选择性配体
公开(公告)号：US5677454A
公开(公告)日：1997-10-14
申请号：US457633
申请日：1995-06-01
申请人： Jun Yuan , Andrew Thurkauf
发明人： Jun Yuan , Andrew Thurkauf
IPC分类号： C07C211/27 , C07D211/14 , C07D211/70 , C07D239/42 , C07D295/096 , C07D401/06 , C07D239/24 , C07D401/04 , C07D403/04
CPC分类号： C07D239/42 , C07C211/27 , C07D211/14 , C07D211/70 , C07D295/096 , C07D401/06
摘要： Disclosed are compounds of the formula: ##STR1## where S and V are various organic or inorganic substituents; G and K are the same or different and represent N or CR' where R' is an organic or inorganic substituent; R is hydrogen or an alkyl group; R.sub.1, X, Y, Z and T are organic or inorganic substituents; and R.sub.2 and R.sub.3 represent hydrogen or organic substituents; or NR.sub.2 R.sub.3 together represents a heterocyclic ring system; and the pharmaceutically acceptable salts thereof; which are highly selective partial agonists or antagonists at brain dopamine receptor subtypes and, thus, are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism.
摘要翻译：公开了下式的化合物：其中S和V是各种有机或无机取代基; G和K相同或不同，表示N或CR'，其中R'是有机或无机取代基; R是氢或烷基; R1，X，Y，Z和T是有机或无机取代基; R2和R3代表氢或有机取代基; 或NR2R3一起表示杂环体系; 及其药学上可接受的盐; 其是脑多巴胺受体亚型的高度选择性部分激动剂或拮抗剂，因此可用于诊断和治疗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。

4. 发明授权

US06211366B1 Bridged 4-phenyl-2-aminomethylimidazoles 失效
标题翻译：桥接的4-苯基-2-氨基甲基咪唑
公开(公告)号：US06211366B1
公开(公告)日：2001-04-03
申请号：US09371066
申请日：1999-08-09
申请人： Jun Yuan , Andrew Thurkauf
发明人： Jun Yuan , Andrew Thurkauf
IPC分类号： C07D40314
CPC分类号： C07D235/02 , C07D403/12 , C07D491/04
摘要： Disclosed are compounds encompassed by general formula (I), wherein, A represents ethenylene, or A represents —X—CH2—; where X is CH2 or oxygen, provided that when X is oxygen, the oxygen is adjacent the 6-membered ring; R1, R2, R3 and R4 are inorganic or organic substituents; and R5 and R6 are optionally substituted organic substituents; or NR5R6 represents a carbocyclic or heterocyclic six-membered ring optionally substituted with various organic or inorganic groups, which compounds can be used in treatment of neuropsychological disorders.
摘要翻译：公开了通式（I）所包括的化合物，其中A表示亚乙烯基，或A表示-X-CH 2 - ; 其中X是CH 2或氧，条件是当X是氧时，氧与6元环相邻; R1，R2，R3和R4是无机或有机取代基; 并且R 5和R 6是任选取代的有机取代基; 或NR 5 R 6表示任选被各种有机或无机基团取代的碳环或杂环六元环，所述化合物可用于治疗神经心理障碍。

5. 发明授权

US5948912A Certain bridged 4-phenyl-2-aminomethylimidazoles; new dopamine receptor subtype specific ligands 失效
标题翻译：某些桥接的4-苯基-2-氨基甲基咪唑; 新的多巴胺受体亚型特异性配体
公开(公告)号：US5948912A
公开(公告)日：1999-09-07
申请号：US913116
申请日：1998-01-20
申请人： Jun Yuan , Andrew Thurkauf
发明人： Jun Yuan , Andrew Thurkauf
IPC分类号： C07D235/02 , C07D403/12 , C07D491/04 , C07D403/14 , A61K31/44 , C07D401/06 , C07D401/14 , C07D403/06
CPC分类号： C07D235/02 , C07D403/12 , C07D491/04
摘要： Disclosed are compounds encompassed by general formula (I), wherein, A represents ethenylene, or A represents --X--CH.sub.2 --; where X is carbon or oxygen, provided that when X is oxygen, the oxygen is adjacent the 6-membered ring; R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are inorganic or organic substituents; and R.sub.5 and R.sub.6 are optionally substituted organic substituents; or NR.sub.5 R.sub.6 represents a carbocyclic or heterocyclic six-membered ring optionally substituted with various organic or inorganic groups, which compounds can be used in the treatment of neuropsychological disorders. ##STR1##
摘要翻译： PCT No.PCT / US96 / 01906 Sec。 371日期1998年1月20日 102（e）1998年1月20日PCT PCT 1996年2月14日PCT公布。公开号WO96 / 25411 PCT 日期1996年8月22日公开是通式（I）所包含的化合物，其中A表示亚乙烯基，或A表示-X-CH2-; 其中X是碳或氧，条件是当X是氧时，氧与6元环相邻; R1，R2，R3和R4是无机或有机取代基; 并且R 5和R 6是任选取代的有机取代基; 或NR 5 R 6表示任选被各种有机或无机基团取代的碳环或杂环六元环，所述化合物可用于治疗神经心理障碍。

6. 发明授权

US5646281A Certain 4-piperidino- and piperazinomethyl-2-phenyl imidazole derivatives; dopamine receptor subtype specific ligands 失效
标题翻译：某些4-哌啶子基和哌嗪基甲基-2-苯基咪唑衍生物; 多巴胺受体亚型特异性配体
公开(公告)号：US5646281A
公开(公告)日：1997-07-08
申请号：US461135
申请日：1995-06-05
申请人： Andrew Thurkauf , Raymond F. Horvath , Jun Yuan , John M. Peterson
发明人： Andrew Thurkauf , Raymond F. Horvath , Jun Yuan , John M. Peterson
IPC分类号： C07D233/54 , C07D233/64 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/06 , A61K31/415 , C07D403/04
CPC分类号： C07D233/64 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12
摘要： Disclosed are compounds of the formula: ##STR1## wherein R.sub.1 represents optionally substituted aryl, heteroaryl, arylalkyl, or cycloalkyl groups; X, Z, and Y are optionally substituted nitrogen or carbon atoms; R.sub.3 and R.sub.4 are organic or inorganic substituents which may together form ring structures; m is zero, one or two; and R.sub.5 and R.sub.6 are are organic or inorganic substituents;and the pharmaceutically acceptable addition salts thereof, which compounds are highly selective partial agonists or antagonists at brain dopamine receptor subtypes or prodrugs thereof and are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism.
摘要翻译：公开了下式的化合物：其中R 1表示任选取代的芳基，杂芳基，芳烷基或环烷基; X，Z和Y任选被取代的氮或碳原子; R3和R4是可以一起形成环结构的有机或无机取代基; m为零，一或二; R5和R6是有机或无机取代基; 和其药学上可接受的加成盐，该化合物是脑多巴胺受体亚型或其前药的高选择性部分激动剂或拮抗剂，并且可用于诊断和治疗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。

7. 发明授权

US5633377A 4-piperidino- and piperazinomethyl-2-cyclohexyl imidazole derivatives; dopamine receptor subtype specific ligands 失效
标题翻译： 4-哌啶子基和哌嗪基甲基-2-环己基咪唑衍生物; 多巴胺受体亚型特异性配体
公开(公告)号：US5633377A
公开(公告)日：1997-05-27
申请号：US462833
申请日：1995-06-05
申请人： Andrew Thurkauf , Raymond F. Horvath , Jun Yuan , John M. Peterson
发明人： Andrew Thurkauf , Raymond F. Horvath , Jun Yuan , John M. Peterson
IPC分类号： C07D233/54 , C07D233/64 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/06 , C07D403/04
CPC分类号： C07D233/64 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12
摘要： Disclosed are compounds of the formula: ##STR1## wherein R.sub.1 represents optionally substituted aryl, heteroaryl, arylalkyl, or cycloalkyl groups; X, Z, and Y are optionally substituted nitrogen or carbon atoms; R.sub.3 and R.sub.4 are organic or inorganic substitutents which may together form ring structures; m is zero, one or two; and R.sub.5 and R.sub.6 are are organic or inorganic substituents;and the pharmaceutically acceptable addition salts thereof,which compounds are highly selective partial agonists or antagonists at brain dopamine receptor subtypes or prodrugs thereof and are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism.
摘要翻译：公开了下式的化合物：其中R 1表示任选取代的芳基，杂芳基，芳烷基或环烷基; X，Z和Y任选被取代的氮或碳原子; R3和R4是可以一起形成环结构的有机或无机取代基; m为零，一或二; R5和R6是有机或无机取代基; 和其药学上可接受的加成盐，该化合物是脑多巴胺受体亚型或其前药的高选择性部分激动剂或拮抗剂，并且可用于诊断和治疗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。

8. 发明授权

US06281359B1 Aminomethyl phenyl pyridine derivatives 失效
标题翻译：氨基甲基苯基吡啶衍生物
公开(公告)号：US06281359B1
公开(公告)日：2001-08-28
申请号：US08457409
申请日：1995-06-01
申请人： Jun Yuan , Andrew Thurkauf
发明人： Jun Yuan , Andrew Thurkauf
IPC分类号： C07D40106
CPC分类号： C07D239/42 , C07C211/27 , C07D211/14 , C07D211/70 , C07D295/096 , C07D401/06
摘要： Disclosed are compounds of the formula: where S and V are various organic or inorganic substituents; G and K are the same or different and represent N or CR′ where R′ is an organic or inorganic substituent; R is hydrogen or an alkyl group; R1, X, Y, Z and T are organic or inorganic substituents; and R2 and R3 represent hydrogen or organic substituents; or NR2R3 together represents a heterocyclic ring system; and the pharmaceutically acceptable salts thereof; which are highly selective partial agonists or antagonists at brain dopamine receptor subtypes and, thus, are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism.
摘要翻译：公开了下式的化合物：其中S和V是各种有机或无机取代基; G和K相同或不同，表示N或CR'，其中R'是有机或无机取代基; R是氢或烷基; R 1 X，Y，Z和T是有机或无机取代基; 且R 2和R 3表示氢或有机取代基; 或NRR2R3一起表示杂环系统;及其药学上可接受的盐; 其是脑多巴胺受体亚型的高度选择性部分激动剂或拮抗剂，因此可用于诊断和治疗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。

9. 发明授权

US5773616A Certain bridged 4-phenyl-2-aminomethylimidazoles; new dopamine receptor subtype specific ligands 失效
标题翻译：某些桥接的4-苯基-2-氨基甲基咪唑; 新的多巴胺受体亚型特异性配体
公开(公告)号：US5773616A
公开(公告)日：1998-06-30
申请号：US463759
申请日：1995-06-05
申请人： Jun Yuan , Andrew Thurkauf
发明人： Jun Yuan , Andrew Thurkauf
IPC分类号： C07D235/02 , C07D403/12 , C07D491/04 , C07D403/14 , C07D401/14
CPC分类号： C07D235/02 , C07D403/12 , C07D491/04
摘要： Disclosed are compounds encompassed by the following general formula: ##STR1## wherein, A represents ethenylene, or A represents --X--CH.sub.2 --; where X is carbon or oxygen, provided that when X is oxygen, the oxygen is adjacent the 6-membered ring; R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are inorganic or organic substituents; and R.sub.5 and R.sub.6 is are optionally substituted organic substituents; or NR.sub.5 R.sub.6 represents a carbocyclic or heterocyclic six membered ring optionally substituted with various orgainic or inorganic groups, which compounds can be used in the treatment of neuropsychological disorders.
摘要翻译：公开的是由以下通式包括的化合物：其中A表示亚乙烯基，或A表示-X-CH2-; 其中X是碳或氧，条件是当X是氧时，氧与6元环相邻; R1，R2，R3和R4是无机或有机取代基; 并且R 5和R 6是任选取代的有机取代基; 或NR 5 R 6表示任选被各种有机或无机基团取代的碳环或杂环六元环，该化合物可用于治疗神经心理障碍。

10. 发明授权

US5712392A Certain 4-piperidine- and piperazinoalkyl-2-phenyl imidazole derivatives; dopamine receptor subtype specific ligands 失效
标题翻译：某些4-哌啶和哌嗪基烷基-2-苯基咪唑衍生物; 多巴胺受体亚型特异性配体
公开(公告)号：US5712392A
公开(公告)日：1998-01-27
申请号：US464548
申请日：1995-06-05
申请人： Andrew Thurkauf , Raymond F. Horvath , Jun Yuan , John M. Peterson
发明人： Andrew Thurkauf , Raymond F. Horvath , Jun Yuan , John M. Peterson
IPC分类号： C07D233/54 , C07D233/64 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/04 , A61K31/415 , C07D403/06
CPC分类号： C07D233/64 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12
摘要： Disclosed are compounds of the formula ##STR1## wherein R.sub.1 represents optionally substituted aryl, heteroaryl, arylalkyl, or cycloalkyl groups; X, Z, and Y are optionally substituted nitrogen or carbon atoms; R.sub.3 and R.sub.4 are organic or inorganic substituents which may together form ring structures; m is zero, one or two; and R.sub.5 and R.sub.6 are are organic or inorganic substituents; and the pharmaceutically acceptable addition salts thereof, which compounds are highly selective partial agonists or antagonists at brain dopamine receptor subtypes or prodrugs thereof and are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism.
摘要翻译：公开了式IMA的化合物，其中R 1表示任选取代的芳基，杂芳基，芳基烷基或环烷基; X，Z和Y是任选取代的氮或碳原子; R3和R4是可以一起形成环结构的有机或无机取代基; m为零，一或二; R5和R6是有机或无机取代基; 和其药学上可接受的加成盐，该化合物是脑多巴胺受体亚型或其前药的高选择性部分激动剂或拮抗剂，并且可用于诊断和治疗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。

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