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1. 发明申请

US20110183996A1 THE 1-BUTYL-2-HYDROXYARALKYL PIPERAZINE DERIVATIVES AND THE USES AS ANTI-DEPRESSION MEDICINE THEREOF 有权
标题翻译： 1-丁基-2-羟基甲基哌嗪衍生物及其作为抗抑郁药物的用途
公开(公告)号：US20110183996A1
公开(公告)日：2011-07-28
申请号：US13122691
申请日：2009-09-29
申请人： Jianqi Li , Na Lv , Hua Jin , Zhijie Weng , Yongyong Zheng
发明人： Jianqi Li , Na Lv , Hua Jin , Zhijie Weng , Yongyong Zheng
IPC分类号： A61K31/495 , C07D295/096 , A61P25/24
CPC分类号： A61K31/495 , C07D295/088 , C07D295/092
摘要： The invention discloses 1-butyl-2-hydroxyl aralkyl piperazine derivatives and their use as antidepressants. The derivatives of the present invention have triple inhibition effect on the reuptake of 5-HT, NA and DA, and can be administrated to the patients in need thereof in form of composition by route of oral administration, injection and the like. Compared with clinically currently used dual targets antidepressants (such as venlafaxine), said derivatives may have stronger antidepression effect, broader indications, faster onset and lower neurotoxicity and side reaction; and said derivatives have stronger antidepression activity, lower toxicity, higher bioavailability, longer half life and better druggablity, compared with aryl alkanol piperazine derivatives and optical isomers thereof disclosed in prior art. The 1-butyl-2-hydroxyl aralkyl piperazine derivative is the free alkali or its salt of a compound of formula below:
摘要翻译：本发明公开了1-丁基-2-羟基芳烷基哌嗪衍生物及其作为抗抑郁药的用途。本发明的衍生物对5-HT，NA和DA的再摄取具有三重抑制作用，并且可以通过口服给药，注射等途径以组合物的形式施用于有需要的患者。与临床目前使用的双抗抑郁药（如文拉法辛）相比，所述衍生物可能具有更强的抗抑郁作用，适应症广，发病更快，神经毒性和副反应降低; 与现有技术中公开的芳基链烷醇哌嗪衍生物及其旋光异构体相比，所述衍生物具有更强的抗抑郁活性，更低的毒性，更高的生物利用度，更长的半衰期和更好的药物可用性。 1-丁基-2-羟基芳烷基哌嗪衍生物是下式化合物的游离碱或其盐：

2. 发明授权

US08252796B2 1-butyl-2-hydroxyaralkyl piperazine derivatives and the uses as anti-depression medicine thereof 有权
标题翻译： 1-丁基-2-羟基烷基哌嗪衍生物及其作为抗抑郁药的用途
公开(公告)号：US08252796B2
公开(公告)日：2012-08-28
申请号：US13122691
申请日：2009-09-29
申请人： Jianqi Li , Na Lv , Hua Jin , Zhijie Weng , Yongyong Zheng
发明人： Jianqi Li , Na Lv , Hua Jin , Zhijie Weng , Yongyong Zheng
IPC分类号： A61K31/495 , C07D241/04
CPC分类号： A61K31/495 , C07D295/088 , C07D295/092
摘要： The invention discloses 1-butyl-2-hydroxyl aralkyl piperazine derivatives and their use as antidepressants. The derivatives of the present invention have triple inhibition effect on the reuptake of 5-HT, NA and DA, and can be administrated to the patients in need thereof in form of composition by route of oral administration, injection and the like. Compared with clinically currently used dual targets antidepressants (such as venlafaxine), said derivatives may have stronger antidepression effect, broader indications, faster onset and lower neurotoxicity and side reaction; and said derivatives have stronger antidepression activity, lower toxicity, higher bioavailability, longer half life and better druggablity, compared with aryl alkanol piperazine derivatives and optical isomers thereof disclosed in prior art. The 1-butyl-2-hydroxyl aralkyl piperazine derivative is the free alkali or its salt of a compound of formula below:
摘要翻译：本发明公开了1-丁基-2-羟基芳烷基哌嗪衍生物及其作为抗抑郁药的用途。本发明的衍生物对5-HT，NA和DA的再摄取具有三重抑制作用，并且可以通过口服给药，注射等途径以组合物的形式施用于有需要的患者。与临床目前使用的双抗抑郁药（如文拉法辛）相比，所述衍生物可能具有更强的抗抑郁作用，适应症广，发病更快，神经毒性和副反应降低; 与现有技术中公开的芳基链烷醇哌嗪衍生物及其旋光异构体相比，所述衍生物具有更强的抗抑郁活性，更低的毒性，更高的生物利用度，更长的半衰期和更好的药物可用性。 1-丁基-2-羟基芳烷基哌嗪衍生物是下式化合物的游离碱或其盐：

3. 发明授权

US07326710B2 Aralkyl formyl-alkyl piperazine derivatives and their uses as a cerebral nerve protective agent 有权
标题翻译：芳烷基 - 烷基哌嗪衍生物及其作为脑神经保护剂的用途
公开(公告)号：US07326710B2
公开(公告)日：2008-02-05
申请号：US10513699
申请日：2003-04-16
申请人： Jianqi Li , Liying Huang , Yang Min , Zhijie Weng , Chunnian Zhang
发明人： Jianqi Li , Liying Huang , Yang Min , Zhijie Weng , Chunnian Zhang
IPC分类号： A61K31/497 , A61K31/4965 , C07D241/04 , C07D295/00 , C07D401/00 , C07D405/00
CPC分类号： C07D295/192 , A61K31/495 , C07D317/54
摘要： Aralkyl formyl alkyl piperazine derivatives Pharmaceutical compositions comprising the same, and methods of using them as a neuroprotective agent. Pharmaceutical results indicate that these compounds have excellent neuroprotective activities and fewer side effects.
摘要翻译：芳烷基甲酰基烷基哌嗪衍生物包含其的药物组合物及其用作神经保护剂的方法。药物结果表明，这些化合物具有优异的神经保护活性和较少的副作用。

4. 发明申请

US20050153981A1 Aralkyl formly-alkyl piperazine derivatives and their uses as a cerebral nerve protective agent 有权
标题翻译：芳基烷基哌嗪衍生物及其作为脑神经保护剂的用途
公开(公告)号：US20050153981A1
公开(公告)日：2005-07-14
申请号：US10513699
申请日：2003-04-16
申请人： Jianqi Li , Yang Min , Zhijie Weng , Chunnian Zhang
发明人： Jianqi Li , Yang Min , Zhijie Weng , Chunnian Zhang
IPC分类号： A61K31/495 , A61P25/24 , C07D295/192 , C07D317/54 , C07D241/04
CPC分类号： C07D295/192 , A61K31/495 , C07D317/54
摘要： Aralkyl formyl alkyl piperazine derivatives Pharmaceutical compositions comprising the same, and methods of using them as a neuroprotective agent. Pharmaceutical results indicate that these compounds have excellent neuroprotective activities and fewer side effects.
摘要翻译：芳烷基甲酰基烷基哌嗪衍生物包含其的药物组合物及其用作神经保护剂的方法。药物结果表明，这些化合物具有优异的神经保护活性和较少的副作用。

5. 发明授权

US08962621B2 Aralkyl diamine derivatives and uses thereof as antidepressants 有权
标题翻译：芳烷基二胺衍生物及其作为抗抑郁药的用途
公开(公告)号：US08962621B2
公开(公告)日：2015-02-24
申请号：US13697389
申请日：2011-05-13
申请人： Jianqi Li , Yongyong Zheng , Yunfeng Liao , Yali Li
发明人： Jianqi Li , Yongyong Zheng , Yunfeng Liao , Yali Li
IPC分类号： C07D413/06 , C07D209/14 , C07D295/02 , C07D295/073 , C07D295/13 , C07D307/81 , C07D317/58 , C07D333/20 , C07D333/58 , C07D207/06 , C07D241/04 , C07D265/30
CPC分类号： C07D413/06 , C07D207/06 , C07D209/14 , C07D241/04 , C07D265/30 , C07D295/02 , C07D295/073 , C07D295/13 , C07D307/81 , C07D317/58 , C07D333/20 , C07D333/58
摘要： Aralkyl diamine derivative of the following formula, pharmaceutically acceptable salts or uses thereof as antidepressants. The derivatives have triplex inhibiting activities of the reuptake of 5-HT, dopamine and noradrenalin, which can be administered to the patients in need of such treatment in the form of compositions orally or injectedly et al.
摘要翻译：下式的芳烷基二胺衍生物，其药学上可接受的盐或其用途作为抗抑郁药。该衍生物具有三重抑制5-HT，多巴胺和去甲肾上腺素再摄取的活性，其可以以口服或注射等的组合物的形式施用于需要这种治疗的患者。

6. 发明授权

US08618133B2 Aralkyl alcohol pyridine derivative compounds and the use thereof as medicaments for treating depression 失效
标题翻译：芳烷基醇吡啶衍生物化合物及其作为治疗抑郁症的药物的用途
公开(公告)号：US08618133B2
公开(公告)日：2013-12-31
申请号：US12997511
申请日：2009-06-08
申请人： Jianqi Li , Kai Gao , Wangping Cai , Yongyong Zheng
发明人： Jianqi Li , Kai Gao , Wangping Cai , Yongyong Zheng
IPC分类号： A61K31/445 , C07D211/18
CPC分类号： C07D211/18 , C07D211/44 , C07D211/58 , C07D211/70 , C07D211/72 , C07D401/06 , C07D409/06
摘要： The present invention relates to an aralkyl alcohol piperidine derivative and use as antidepressant thereof. The said aralkyl alcohol piperidine derivative has a triple inhibition effect on the reuptaking of 5-HT, NA and DA. The derivative may be administered to the patient in need of such treatment in the form of composition by oral administration, injection and the like. The derivative is a compound having the following general formula or its salt:
摘要翻译：本发明涉及芳烷基醇哌啶衍生物，用作其抗抑郁药。所述芳烷基醇哌啶衍生物对5-HT，NA和DA的再次起始具有三重抑制作用。衍生物可以通过口服给药，注射等方式以组合物的形式施用于需要这种治疗的患者。该衍生物是具有以下通式的化合物或其盐：

7. 发明申请

US20130072488A1 ARALKYL DIAMINE DERIVATIVES AND USES THEREOF AS ANTIDEPRESSANTS 有权
标题翻译： ARALKYL DIAMINE衍生物及其作为抗病毒剂的用途
公开(公告)号：US20130072488A1
公开(公告)日：2013-03-21
申请号：US13697389
申请日：2011-05-13
申请人： Jianqi Li , Yongyong Zheng , Yunfeng Liao , Yali Li
发明人： Jianqi Li , Yongyong Zheng , Yunfeng Liao , Yali Li
IPC分类号： C07D413/06 , C07D241/04 , C07D265/30 , C07D207/06
CPC分类号： C07D413/06 , C07D207/06 , C07D209/14 , C07D241/04 , C07D265/30 , C07D295/02 , C07D295/073 , C07D295/13 , C07D307/81 , C07D317/58 , C07D333/20 , C07D333/58
摘要： Aralkyl diamine derivative of the following formula, pharmaceutically acceptable salts or uses thereof as antidepressants. The derivatives have triplex inhibiting activities of the reuptake of 5-HT, dopamine and noradrenalin, which can be administered to the patients in need of such treatment in the form of compositions orally or injectedly et al.
摘要翻译：下式的芳烷基二胺衍生物，其药学上可接受的盐或其用途作为抗抑郁药。该衍生物具有三重抑制5-HT，多巴胺和去甲肾上腺素再摄取的活性，其可以以口服或注射等的组合物的形式施用于需要这种治疗的患者。

8. 发明申请

US20110160247A1 Aralkyl alcohol piperidine derivative and the use thereof as a medicament for treating depression 失效
标题翻译：芳烷基醇哌啶衍生物及其用作治疗抑郁症的药物的用途
公开(公告)号：US20110160247A1
公开(公告)日：2011-06-30
申请号：US12997511
申请日：2009-06-08
申请人： Jianqi Li , Kai Gao , Wangping Cai , Yongyong Zheng
发明人： Jianqi Li , Kai Gao , Wangping Cai , Yongyong Zheng
IPC分类号： A61K31/4535 , A61K31/44 , A61K31/445 , A61K31/4436 , C07D409/06 , C07D211/14 , C07D211/70 , A61P25/24
CPC分类号： C07D211/18 , C07D211/44 , C07D211/58 , C07D211/70 , C07D211/72 , C07D401/06 , C07D409/06
摘要： The present invention relates to an aralkyl alcohol piperidine derivative and use as antidepressant thereo. The said aralkyl alcohol piperidine derivative has a triple inhibition effect on the reuptaking of 5-HT, NA and DA. The derivative may be administered to the patient in need of such treatment in the form of composition by oral administration, injection and the like. The derivative is a compound having the following general formula or its salt:
摘要翻译：本发明涉及芳烷基醇哌啶衍生物，其用作抗抑郁药。所述芳烷基醇哌啶衍生物对5-HT，NA和DA的再次起始具有三重抑制作用。衍生物可以通过口服给药，注射等方式以组合物的形式施用于需要这种治疗的患者。该衍生物是具有以下通式的化合物或其盐：

9. 发明授权

US08680097B2 Benzothiophene alkanol piperazine derivatives and their use as antidepressant 失效
标题翻译：苯并噻吩烷醇哌嗪衍生物及其用作抗抑郁药
公开(公告)号：US08680097B2
公开(公告)日：2014-03-25
申请号：US13001998
申请日：2009-06-30
申请人： Jianqi Li , Kai Gao , Na Lv
发明人： Jianqi Li , Kai Gao , Na Lv
IPC分类号： A61K31/496 , A61K31/5377 , C07D333/58 , C07D409/12 , C07D413/12
CPC分类号： C07D409/06 , C07D409/14
摘要： The invention discloses benzothiophene alkanol piperazine derivatives and their use as antidepressants. The invention discloses the said benzothiophene alkanol piperazine derivative having triple inhibition effect on the reuptake of 5-HT, NA and DA. Compared with clinical used antidepressants so far having single target, e.g. desipramine and fluoxetine, and clinical used antidepressants so far having double targets, e.g venlafaxine and duloxetine, the said benzothiophene alkanol piperazine derivatives of the present invention may have a broader indication range and less toxic and side effects to nervous system. The benzothiophene alkanol piperazine derivatives are the compounds with the following formula or their pharmaceutically acceptable salts, wherein Ar1, R1-R4, X, Y, m and n have the same definition as defined in claim 1.
摘要翻译：本发明公开了苯并噻吩烷醇哌嗪衍生物及其作为抗抑郁药的用途。本发明公开了对5-HT，NA和DA的再摄取具有三重抑制作用的所述苯并噻吩烷醇哌嗪衍生物。与迄今为止具有单一目标的临床使用的抗抑郁药相比，本发明的所述苯并噻吩烷醇哌嗪衍生物可能具有更广泛的适应范围和对神经系统的毒副作用较小的临床用途的抗抑郁药，目前为止具有双重目标，例如文拉法辛和度洛西汀。苯并噻吩烷醇哌嗪衍生物是具有下式的化合物或其药学上可接受的盐，其中Ar1，R1-R4，X，Y，m和n具有与权利要求1中所定义的相同的定义。

10. 发明申请

US20110306638A1 BENZISOXAZOLE PIPERIDINYL DERIVATIVES, PHARMACEUTICAL COMPOSITIONS COMPRISING THE DERIVATIVES AND THEIR USE 审中-公开
标题翻译：苯并噻唑苯哌啶衍生物，包含衍生物及其用途的药物组合物
公开(公告)号：US20110306638A1
公开(公告)日：2011-12-15
申请号：US13141811
申请日：2009-12-22
申请人： Jianqi Li , Guan Wang , Guisen Zhang , Na Lv , Guangjun Jiao , Shicheng Liu , Shixia Zhou
发明人： Jianqi Li , Guan Wang , Guisen Zhang , Na Lv , Guangjun Jiao , Shicheng Liu , Shixia Zhou
IPC分类号： A61K31/454 , A61P25/20 , A61P25/04 , C07D413/14 , A61P29/00
CPC分类号： C07D413/14
摘要： The invention relates to a benzisoxazolyl piperidine derivative having the following general formula, a salt or a hydrate thereof, wherein R, X, Y, R′ and T are defined as in the specification. Such compounds have serotonin system modulating effects such as antagonizing effect on 5-HT2A and inhibitory effect on 5-HT reuptake. The compounds have good analgesic and sedative activities with mild toxic and side effects. The invention also relates to a composition comprising said derivative and the use thereof.
摘要翻译：本发明涉及具有以下通式的苯并异恶唑基哌啶衍生物，其盐或其水合物，其中R，X，Y，R'和T如说明书中所定义。这些化合物具有5-羟色胺系统调节作用，如对5-HT2A的拮抗作用和对5-HT再摄取的抑制作用。该化合物具有良好的止痛和镇静作用，具有轻度毒副作用。本发明还涉及包含所述衍生物及其用途的组合物。

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