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1. 发明授权

US06605607B1 Tetrahydrobenzazepine derivatives useful as modulators of dopamine D3 receptors (antipsychotic agents) 失效
标题翻译：可用作多巴胺D3受体调节剂的四氢苯并吖庚因衍生物（抗精神病药）
公开(公告)号：US06605607B1
公开(公告)日：2003-08-12
申请号：US09806902
申请日：2001-07-16
申请人： Michael Stewart Hadley , Christopher Norbert Johnson , Gregor James MacDonald , Geoffrey Stemp , Antonio Kuok Keong Vong
发明人： Michael Stewart Hadley , Christopher Norbert Johnson , Gregor James MacDonald , Geoffrey Stemp , Antonio Kuok Keong Vong
IPC分类号： A61K3155
CPC分类号： C07D223/16 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04
摘要： Compounds of Formula I and their salts having affinity for dopamine receptors, in particular the D3 Receptor, and thus potential in the treatment of conditions wherein modulation of the D3 receptor is beneficial, e.g., as antipsychotic agents.
摘要翻译：式I化合物及其对多巴胺受体，特别是D3受体具有亲和性的盐，因此治疗其中D3受体的调节是有益的，例如作为抗精神病药的潜力。

2. 发明授权

US5688790A Phenylpyrrole derivatives and their use as antipsychotic agents 失效
标题翻译：苯基吡咯衍生物及其作为抗精神病药的用途
公开(公告)号：US5688790A
公开(公告)日：1997-11-18
申请号：US532548
申请日：1995-09-28
申请人： Michael Stewart Hadley , Christopher Norbert Johnson , Geoffrey Stemp
发明人： Michael Stewart Hadley , Christopher Norbert Johnson , Geoffrey Stemp
IPC分类号： A61K31/435 , A61P25/18 , C07D455/02 , C07D471/04
CPC分类号： C07D471/04 , C07D455/02
摘要： This invention relates to compounds of formula (I): ##STR1## wherein R.sup.1 represents C.sub.1-4 alkyl; and R.sup.2, R.sup.3, R.sup.4 and R.sup.5 each independently represent hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkoxyC.sub.1-4 alkyl, C.sub.1-4 alkylsulphonyl, trifluoromethylsulphonyl; optionally substituted arylsulphonyl, optionally substituted heteroarylsulphonyl, optionally substituted aralkylsulphonyl, optionally substituted heteroaralkylsulphonyl, nitro, cyano, amino, mono- or di-alkylamino, trifluoromethyl, trifluoromethoxy, hydroxyl, hydroxyC.sub.1-4 alkyl, C.sub.1-4 alkylthio, C.sub.1-4 alkanoyl, C.sub.1-4 alkoxycarbonyl, aminosulphonyl, or mono- or diC.sub.1-4 alkylaminosulphonyl; or R.sup.1 and R.sup.2 together form a linking chain --(CH.sub.2).sub.m Op; (wherein m is 2 to 4 and p is zero or 1) which chain may be optionally substituted by one or two C.sub.1-4 alkyl groups; and Y represents a group of formula (.alpha.): ##STR2## wherein each of n and m independently represent an integer from 1 to 3; and salts thereof, having activity at dopamine receptors and potential utility in the treatment of psychoses such as schizophrenia.
摘要翻译： PCT No.PCT / EP94 / 00992 Sec。 371 1995年9月28日第 102（e）日期1995年9月28日PCT 1994年3月29日PCT公布。公开号WO94 / 24129 日本公开专利文献1：日本专利公开公报发明内容本发明涉及式（I）的化合物：其中R 1表示C 1-4烷基的式（I）并且R 2，R 3，R 4和R 5各自独立地表示氢，卤素，C 1-4烷基，C 1-4烷氧基，C 1-4烷氧基C 1-4烷基，C 1-4烷基磺酰基，三氟甲基磺酰基; 任选取代的芳基磺酰基，任选取代的芳基磺酰基，任选取代的芳烷基磺酰基，任选取代的杂芳烷基磺酰基，硝基，氰基，氨基，一或二 - 烷基氨基，三氟甲基，三氟甲氧基，羟基，羟基C 1-4烷基，C 1-4烷硫基，C 1-4烷酰基，C 1-4烷氧基羰基，氨基磺酰基，或单或二C 1-4烷基氨基磺酰基; 或R 1和R 2一起形成连接链 - （CH 2）mOp; （其中m为2〜4，p为0或1），该链可以任选被一个或两个C 1-4烷基取代; 并且Y表示式（α）的基团：其中n和m各自独立地表示1至3的整数; 及其盐，其在多巴胺受体上具有活性，在治疗精神病如精神分裂症中具有潜在的用途。

3. 发明授权

US07977337B2 Quinoline derivatives and their use as 5-HT6 ligands 有权
标题翻译：喹啉衍生物及其作为5-HT6配体的用途
公开(公告)号：US07977337B2
公开(公告)日：2011-07-12
申请号：US12847039
申请日：2010-07-30
申请人： Mahmood Ahmed , Christopher Norbert Johnson , Martin C Jones , Gregor James MacDonald , Stephen Frederick Moss , Mervyn Thompson , Charles Edward Wade , David R Witty
发明人： Mahmood Ahmed , Christopher Norbert Johnson , Martin C Jones , Gregor James MacDonald , Stephen Frederick Moss , Mervyn Thompson , Charles Edward Wade , David R Witty
IPC分类号： A61K31/47 , A61K31/496
CPC分类号： C07D487/04 , C07D215/00 , C07D487/08
摘要： Disclosed are quinoline compounds having affinity for the 5-HT6 receptor and having the formula: where R1, R2, R3, R4, R5, n, m, p and A are defined herein, and salts thereof, compositions containing these compounds and salts and processes for making and using the same.
摘要翻译：公开了对5-HT 6受体具有亲和性并具有下式的喹啉化合物：其中R1，R2，R3，R4，R5，n，m，p和A如本文所定义，及其盐，含有这些化合物和盐的组合物制作和使用相同的过程。

4. 发明授权

US07452888B2 Quinoline derivatives and their use as 5-ht6 ligands 有权
标题翻译：喹啉衍生物及其作为5-ht6配体的用途
公开(公告)号：US07452888B2
公开(公告)日：2008-11-18
申请号：US10509078
申请日：2003-03-25
申请人： Mahmood Ahmed , Christopher Norbert Johnson , Martin C Jones , Gregor James Macdonald , Stephen Frederick Moss , Mervyn Thompson , Charles Edward Wade , David R Witty
发明人： Mahmood Ahmed , Christopher Norbert Johnson , Martin C Jones , Gregor James Macdonald , Stephen Frederick Moss , Mervyn Thompson , Charles Edward Wade , David R Witty
IPC分类号： A61K31/496 , C07D215/40
CPC分类号： C07D487/04 , C07D215/00 , C07D487/08
摘要： Disclosed are novel quinoline compounds of formula (I), processes for their preparation, compositions containing them and their use in the treatment of CNS disorders.
摘要翻译：公开了式（I）的新型喹啉化合物，其制备方法，含有它们的组合物及其在治疗CNS障碍中的用途。

5. 发明申请

US20090036682A1 Quinoline Derivatives and Their Use as 5-HT6 Ligands 有权
标题翻译：喹啉衍生物及其用作5-HT6配体
公开(公告)号：US20090036682A1
公开(公告)日：2009-02-05
申请号：US12205079
申请日：2008-09-05
申请人： Mahmood AHMED , Christopher Norbert Johnson , Martin C. Jones , Gregor James MacDonald , Stephen Frederick Moss , Mervyn Thompson , Charles Edward Wade , David R. Witty
发明人： Mahmood AHMED , Christopher Norbert Johnson , Martin C. Jones , Gregor James MacDonald , Stephen Frederick Moss , Mervyn Thompson , Charles Edward Wade , David R. Witty
IPC分类号： C07D401/10
CPC分类号： C07D487/04 , C07D215/00 , C07D487/08
摘要： The present invention relates to novel quinoline compounds having pharmacological activity, to processes for their preparation, to compositions containing them and to their use in the treatment of CNS and other disorders.
摘要翻译：本发明涉及具有药理学活性的新喹啉化合物，其制备方法，含有它们的组合物及其在治疗CNS和其它疾病中的用途。

6. 发明申请

US20110237792A1 QUINOLINE DERIVATIVES AND THEIR USE AS 5-HT6 LIGANDS 有权
标题翻译：喹啉衍生物及其作为5-HT6配体使用
公开(公告)号：US20110237792A1
公开(公告)日：2011-09-29
申请号：US13152356
申请日：2011-06-03
申请人： Mahmood AHMED , Christopher Norbert Johnson , Martin C. Johnes , Gregor James MacDonald , Stephen Frederick Moss , Mervyn Thompson , Charles Edward Wade , David R. Witty
发明人： Mahmood AHMED , Christopher Norbert Johnson , Martin C. Johnes , Gregor James MacDonald , Stephen Frederick Moss , Mervyn Thompson , Charles Edward Wade , David R. Witty
IPC分类号： C07D403/10 , C07D401/10 , C07D487/04
CPC分类号： C07D487/04 , C07D215/00 , C07D487/08
摘要： Disclosed are quinoline compounds having affinity for the 5-HT6 receptor and having the formula: where R1, R2, R3, R4, R5, n, m, p and A are defined herein, and salts thereof, compositions containing these compounds and salts and processes for making and using the same.
摘要翻译：公开了对5-HT 6受体具有亲和性并具有下式的喹啉化合物：其中R1，R2，R3，R4，R5，n，m，p和A如本文所定义，及其盐，含有这些化合物和盐的组合物制作和使用相同的过程。

7. 发明申请

US20100305107A1 QUINOLINE DERIVATIVES AND THEIR USE AS 5-HT6 LIGANDS 有权
标题翻译：喹啉衍生物及其作为5-HT6配体使用
公开(公告)号：US20100305107A1
公开(公告)日：2010-12-02
申请号：US12847039
申请日：2010-07-30
申请人： Mahmood AHMED , Christopher Norbert Johnson , Martin C. Jones , Gregor James MacDonald , Stephen Frederick Moss , Mervyn Thompson , Charles Edward Wade , David R. Witty
发明人： Mahmood AHMED , Christopher Norbert Johnson , Martin C. Jones , Gregor James MacDonald , Stephen Frederick Moss , Mervyn Thompson , Charles Edward Wade , David R. Witty
IPC分类号： A61K31/4709 , A61K31/496 , A61K31/551 , A61K31/4985 , A61P25/00 , A61P25/06 , A61P25/16 , A61P25/24 , A61P25/30
CPC分类号： C07D487/04 , C07D215/00 , C07D487/08
摘要： Disclosed are quinoline compounds having affinity for the 5-HT6 receptor and having the formula: where R1, R2, R3, R4, R5, n, m, p and A are defined herein, and salts thereof, compositions containing these compounds and salts and processes for making and using the same.
摘要翻译：公开了对5-HT 6受体具有亲和性并具有下式的喹啉化合物：其中R1，R2，R3，R4，R5，n，m，p和A如本文所定义，及其盐，含有这些化合物和盐的组合物制作和使用相同的过程。

8. 发明授权

US07799774B2 Quinoline derivatives and their use as 5-HT6 ligands 有权
标题翻译：喹啉衍生物及其作为5-HT6配体的用途
公开(公告)号：US07799774B2
公开(公告)日：2010-09-21
申请号：US12541456
申请日：2009-08-14
申请人： Mahmood Ahmed , Christopher Norbert Johnson , Martin C Jones , Gregor James MacDonald , Stephen Frederick Moss , Mervyn Thompson , Charles Edward Wade , David R Witty
发明人： Mahmood Ahmed , Christopher Norbert Johnson , Martin C Jones , Gregor James MacDonald , Stephen Frederick Moss , Mervyn Thompson , Charles Edward Wade , David R Witty
IPC分类号： A61K31/496 , A61K31/47 , C07D215/40 , C07D471/04 , C07D487/08
CPC分类号： C07D487/04 , C07D215/00 , C07D487/08
摘要： Disclosed are quinoline compounds having affinity for the 5-HT6 receptor and having the formula: where R1, R2, R3, R4, R5, n, m, p and A are defined herein, and salts thereof, compositions containing these compounds and salts and processes for making and using the same.
摘要翻译：公开了对5-HT 6受体具有亲和性并具有下式的喹啉化合物：其中R1，R2，R3，R4，R5，n，m，p和A如本文所定义，及其盐，含有这些化合物和盐的组合物制作和使用相同的过程。

9. 发明授权

US08236947B2 Quinoline derivatives and their use as 5-HT6 ligands 有权
标题翻译：喹啉衍生物及其作为5-HT6配体的用途
公开(公告)号：US08236947B2
公开(公告)日：2012-08-07
申请号：US13152356
申请日：2011-06-03
申请人： Mahmood Ahmed , Christopher Norbert Johnson , Martin C Jones , Gregor James MacDonald , Stephen Frederick Moss , Mervyn Thompson , Charles Edward Wade , David R Witty
发明人： Mahmood Ahmed , Christopher Norbert Johnson , Martin C Jones , Gregor James MacDonald , Stephen Frederick Moss , Mervyn Thompson , Charles Edward Wade , David R Witty
IPC分类号： A61K31/496 , A61K31/551 , C07D401/04 , C07D487/08
CPC分类号： C07D487/04 , C07D215/00 , C07D487/08
摘要： Disclosed are quinoline compounds having affinity for the 5-HT6 receptor and having the formula: where R1, R2, R3, R4, R5, n, m, p and A are defined herein, and salts thereof, compositions containing these compounds and salts and processes for making and using the same.
摘要翻译：公开了对5-HT 6受体具有亲和性并具有下式的喹啉化合物：其中R1，R2，R3，R4，R5，n，m，p和A如本文所定义，及其盐，含有这些化合物和盐的组合物制作和使用相同的过程。

10. 发明申请

US20090298841A1 QUINOLINE DERIVATIVES AND THEIR USE AS 5-HT6 LIGANDS 有权
标题翻译：喹啉衍生物及其作为5-HT6配体使用
公开(公告)号：US20090298841A1
公开(公告)日：2009-12-03
申请号：US12541456
申请日：2009-08-14
申请人： Mahmood Ahmed , Christopher Norbert Johnson , Martin C. Jones , Gregor James MacDonald , Stephen Frederick Moss , Mervyn Thompson , Charles Edward Wade , David R. Witty
发明人： Mahmood Ahmed , Christopher Norbert Johnson , Martin C. Jones , Gregor James MacDonald , Stephen Frederick Moss , Mervyn Thompson , Charles Edward Wade , David R. Witty
IPC分类号： A61K31/4985 , C07D401/10 , C07D487/04 , A61K31/496 , A61P25/00 , A61P3/04
CPC分类号： C07D487/04 , C07D215/00 , C07D487/08
摘要： The present invention relates to novel quinoline compounds having pharmacological activity, to processes for their preparation, to compositions containing them and to their use in the treatment of CNS and other disorders.
摘要翻译：本发明涉及具有药理学活性的新喹啉化合物，其制备方法，含有它们的组合物及其在治疗CNS和其它疾病中的用途。

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