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1. 发明申请

WO2004002983A3 THERAPEUTIC PIPERAZINE DERIVATIVES USEFUL FOR TREATING PAIN 审中-公开
标题翻译：用于治疗疼痛的治疗药物派尼汀衍生物
公开(公告)号：WO2004002983A3
公开(公告)日：2004-03-18
申请号：PCT/US0320509
申请日：2003-06-27
申请人： EURO CELTIQUE SA , KYLE DONALD J , SUN QUN , TAFESSE LAYKEA , ZHANG CHONGWU , ZHOU XIAOMING
发明人： KYLE DONALD J , SUN QUN , TAFESSE LAYKEA , ZHANG CHONGWU , ZHOU XIAOMING
IPC分类号： A61K31/496 , A61P1/00 , A61P1/04 , A61P1/08 , A61P13/02 , A61P17/04 , A61P21/00 , A61P21/02 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P27/02 , A61P29/00 , A61P43/00 , C07D213/74 , C07D213/85 , C07D237/20 , C07D239/42 , C07D241/20 , C07D285/06 , C07D333/16 , C07D401/04 , A61K31/4965 , A61K31/501 , A61K31/506
CPC分类号： C07D213/74 , C07D213/85 , C07D237/20 , C07D239/42 , C07D241/20 , C07D285/06 , C07D333/16
摘要： A compound of formula (I): wherein A, Ar, R , R , and m are disclosed herein, or a pharmaceutically acceptable salt thereof (a "Cyanoiminopiperazine Compound"), cornposition, comprising an effective amount of a Cyanoiminopiperazine Compound, and methods for treating or preventing pain, urinary incontinence, an ulcer, inflammatory-bowel disease, irritable-bowel syndi oine, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke. a sc z are, a prurifc condition, psychosis, a cognitive disorder;`a memory deficit, restricted brain function. R rnfington's chorea., arsiyotrophic lateral sclerosis, dementia, retinopathy, a muscie ,spasm" a migraine, vomiting, dyskinesia or depression in an animal comprising administek irgT b ati animal in need thereof an effective amount of a Cyanoi:irinopiperazine Compound are disclosed.
摘要翻译：式（I）化合物：其中A，Ar，R 3，R 6和m在本文中公开，或其药学上可接受的盐（“氰基亚氨基哌嗪化合物”），包含有效量氰酰亚哌嗪化合物，以及治疗或预防疼痛，尿失禁，溃疡，炎性肠病，肠易激综合征，成瘾性障碍，帕金森病，帕金森综合征，焦虑症，癫痫，中风的方法。是一种瘙痒症状，精神病，认知障碍，记忆障碍，脑功能受限。 Rnfington的舞蹈病，arsiyotrophial侧索硬化症，痴呆症，视网膜病变，肌肉，痉挛“偏头痛，呕吐，运动障碍或抑郁症包括有需要的有效量的Cyanoi 公开了伊立哌嗪化合物。

2. 发明申请

WO2004011439A3 ARYL SUBSTITUTED BENZIMIDAZOLES AND THEIR USE AS SODIUM CHANNEL BLOCKERS 审中-公开
标题翻译： ARYL取代苯并咪唑及其作为钠通道阻断剂
公开(公告)号：WO2004011439A3
公开(公告)日：2004-04-01
申请号：PCT/US0323828
申请日：2003-07-31
申请人： EURO CELTIQUE SA , SUN QUN , ZHOU XIAOMING , KYLE DONALD J
发明人： SUN QUN , ZHOU XIAOMING , KYLE DONALD J
IPC分类号： C07D235/08 , C07D235/12 , C07D403/06 , C07D235/18 , A61K31/4184
CPC分类号： C07D403/06 , C07D235/08 , C07D235/12
摘要： This invention relates aryl substituted benzimidazoles of Formula (I) or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein R1, R2, R10 and n are defined in the specification. The invention is also directed to the use of compounds of Formula (I) for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.
摘要翻译：本发明涉及式（I）的芳基取代的苯并咪唑或其药学上可接受的盐，前药或溶剂化物，其中R1，R2，R10和n在本说明书中定义。本发明还涉及式（I）化合物用于治疗全身和局部缺血后的神经元损伤，用于治疗或预防神经变性疾病如肌萎缩性侧索硬化（ALS）以及治疗，预防或改善急性或慢性疼痛，作为抗惊厥剂，抗惊厥药，抗抑郁药，作为局部麻醉剂，作为抗心律失常药，以及用于治疗或预防糖尿病性神经病变。

3. 发明申请

WO2006040181A2 PIPERIDINYL COMPOUNDS AND THE USE THEREOF 审中-公开
标题翻译：哌嗪化合物及其用途
公开(公告)号：WO2006040181A2
公开(公告)日：2006-04-20
申请号：PCT/EP2005011105
申请日：2005-10-14
申请人： EURO CELTIQUE SA , BENJAMIN ELFRIDA R , CHEN ZHENGMING , SHA DEYOU , TAFESSE LAYKEA , VICTORY SAMUEL F , WHITEHEAD JOHN W F , ZHOU XIAOMING
发明人： BENJAMIN ELFRIDA R , CHEN ZHENGMING , SHA DEYOU , TAFESSE LAYKEA , VICTORY SAMUEL F , WHITEHEAD JOHN W F , ZHOU XIAOMING
CPC分类号： C07D401/06 , C07D211/58 , C07D211/96
摘要： The invention relates to piperidinyl compounds of Formula (I): or a pharmaceutically acceptable salt, prodrug, or solvate thereof, wherein R
摘要翻译：本发明涉及式（I）的哌啶基化合物：或其药学上可接受的盐，前药或溶剂合物，其中R

4. 发明申请

WO2012035421A2 PYRIDINE COMPOUNDS AND THE USES THEREOF 审中-公开
标题翻译：吡啶化合物及其用途
公开(公告)号：WO2012035421A2
公开(公告)日：2012-03-22
申请号：PCT/IB2011002172
申请日：2011-09-16
申请人： PURDUE PHARMA LP , NI CHIYOU , SHAO BIN , TAFESSE LAYKEA , YAO JIANGCHAO , YU JIANMING , ZHOU XIAOMING
发明人： NI CHIYOU , SHAO BIN , TAFESSE LAYKEA , YAO JIANGCHAO , YU JIANMING , ZHOU XIAOMING
IPC分类号： C07D213/30 , A61K31/4418 , A61K31/4439 , A61K31/444 , A61P23/00 , C07D213/46 , C07D213/74 , C07D213/79 , C07D213/81 , C07D213/84 , C07D401/04 , C07D401/12 , C07D403/12 , C07D403/14
CPC分类号： C07D213/81 , C07D213/30 , C07D213/46 , C07D213/50 , C07D213/57 , C07D213/58 , C07D213/643 , C07D213/65 , C07D213/74 , C07D213/79 , C07D213/84 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14
摘要： The invention relates to substituted pyridine compounds of Formula (I) and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein R1a, A1, A2, E, G, Z1, and Z2 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.
摘要翻译：本发明涉及式（I）的取代的吡啶化合物及其药学上可接受的盐，前药和溶剂合物，其中R 1a，A 1，A 2，E，G，Z 1和Z 2如说明书中所定义。本发明还涉及式I化合物用于治疗对钠通道阻断有响应的病症的用途。本发明的化合物对于治疗疼痛特别有用。

5. 发明申请

WO2012085648A9 PHOSPHORUS-SUBSTITUTED QUINOXALINE-TYPE PIPERIDINE COMPOUNDS AND USES THEREOF 审中-公开
标题翻译：磷酸替代的喹啉类型哌啶化合物及其用途
公开(公告)号：WO2012085648A9
公开(公告)日：2013-03-21
申请号：PCT/IB2011003132
申请日：2011-12-21
申请人： PURDUE PHARMA LP , TADESSE DAWIT , TAFESSE LAYKEA , ZHOU XIAOMING
发明人： TADESSE DAWIT , TAFESSE LAYKEA , ZHOU XIAOMING
IPC分类号： A61K31/498 , A61P3/02 , A61P23/00 , A61P25/00 , A61P25/16 , A61P25/24 , C07D401/04 , C07D401/14
CPC分类号： C07F9/6561 , C07F9/65583
摘要： The disclosure relates to Phosphorus-Substituted Quinoxaline-Type Piperidine Compounds of Formula (I), and pharmaceutically acceptable derivatives thereof wherein the dashed line, A, B, Q, R1, R2, R3, R4, Y1, Z, and a are as defined herein, compositions comprising an effective amount of a Phosphorus-Substituted Quinoxaline-Type Piperidine Compound, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Phosphorus- Substituted Quinoxaline-Type Piperidine Compound.
摘要翻译：本公开涉及式（I）的磷取代的喹喔啉型哌啶化合物及其药学上可接受的衍生物，其中虚线A，B，Q，R 1，R 2，R 3，R 4，Y 1，Z和a分别为包含有效量的磷取代的喹喔啉型哌啶化合物的组合物，以及治疗或预防诸如疼痛的病症的方法，包括向有需要的动物施用有效量的磷取代的喹喔啉 - 类哌啶化合物。

6. 发明申请

WO2004029031A3 THERAPEUTIC PIPERAZINE COMPOUNDS 审中-公开
标题翻译：治疗哌嗪化合物
公开(公告)号：WO2004029031A3
公开(公告)日：2004-08-05
申请号：PCT/US0330185
申请日：2003-09-24
申请人： EURO CELTQUE S A , SUN QUN , ZHOU XIAOMING
发明人： SUN QUN , ZHOU XIAOMING
IPC分类号： A61P29/00 , C07D401/04 , C07D403/04 , C07D417/04 , A61K31/496 , C07D213/74 , C07D237/20 , C07D239/42 , C07D241/20 , C07D285/10
CPC分类号： C07D401/04 , C07D403/04 , C07D417/04
摘要： A compound of formula: wherein Ar, Ar1, Ar2, R3-R6, R13, m, and t are disclosed herein, or a pharmaceutically acceptable salt thereof (a "Hydroxyiminopiperazine Compound"); compositions comprising an effective amount of a Hydroxyiminopiperazine Compound; and methods for treating or preventing pain and other conditions in an animal comprising administering to an animal in need thereof an effective amount of a Hydroxyiminopiperazine Compound are disclosed.
摘要翻译：式中的化合物：其中Ar，Ar1，Ar2，R3-R6，R13，m和t在本文中公开，或其药学上可接受的盐（“羟基亚氨基哌嗪化合物”）; 包含有效量的羟基亚氨基哌嗪化合物的组合物; 以及用于治疗或预防动物中的疼痛和其它病症的方法，包括向有需要的动物施用有效量的羟基亚氨基哌嗪化合物。

7. 发明专利

JP2014065720A 4-phenylsulfonamidopiperidine as calcium channel blocker 审中-公开
标题翻译： 4-PHENYLSULFONAMIDOPIPERIDINE AS CALCIUM CHANNEL BLOCKER
公开(公告)号：JP2014065720A
公开(公告)日：2014-04-17
申请号：JP2013241194
申请日：2013-11-21
申请人： Euro-Celtique Sa , ユーロ−セルティークエス.エイ.
发明人： BENJAMIN ELFRIDA R , CHEN ZHENGMING , SHA DEYOU , TAFESSE LAYKEA , VICTORY SAMUEL F , WHITEHEAD JOHN W F , ZHOU XIAOMING
IPC分类号： A61K31/451 , A61K31/454 , A61K31/4725 , A61P9/06 , A61P9/10 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/22 , A61P25/24
CPC分类号： C07D401/06 , C07D211/58 , C07D211/96
摘要： PROBLEM TO BE SOLVED: To provide compounds that modulate or block the movement of calcium ions through voltage-gated calcium channels including N-type calcium channels.SOLUTION: The invention relates to piperidinyl compounds of formula (I) or salts thereof.
摘要翻译：要解决的问题：提供通过包括N型钙通道的电压门控钙通道调节或阻断钙离子运动的化合物。解决方案：本发明涉及式（I）的哌啶基化合物或其盐。

8. 发明专利

JP2011173897A 4-phenylsulfonamidopiperidine as calcium channel blocker 有权
标题翻译： 4-PHENYLSULFONAMIDOPIPERIDINE AS CALCIUM CHANNEL BLOCKER
公开(公告)号：JP2011173897A
公开(公告)日：2011-09-08
申请号：JP2011084148
申请日：2011-04-06
申请人： Euro-Celtique Sa , ユーロ−セルティークエス.エイ.
发明人： BENJAMIN ELFRIDA R , CHEN ZHENGMING , SHA DEYOU , TAFESSE LAYKEA , VICTORY SAMUEL F , WHITEHEAD JOHN W F , ZHOU XIAOMING
IPC分类号： C07D211/58 , A61K31/4468 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/541 , A61P9/00 , A61P9/10 , A61P9/12 , A61P17/02 , A61P25/00 , A61P25/06 , A61P25/08 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P29/00 , C07D401/06 , C07D401/12
CPC分类号： C07D401/06 , C07D211/58 , C07D211/96
摘要： PROBLEM TO BE SOLVED: To provide a new piperidinyl compound which acts as a blocker of a calcium (Ca 2+ ) channel. SOLUTION: The piperidinyl compound is a compound of formula I or its derivative. In the formula, R 1 -R 3 , and Z are each a specific group. The compound is useful to treat sharp pain and a disorder responsive to the blockade of calcium channels. COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：要解决的问题：提供作为钙（Ca 2 + ）通道阻滞剂的新的哌啶基化合物。哌啶基化合物是式I化合物或其衍生物。在该式中，R 1 -R 3 和Z各自为特定基团。该化合物可用于治疗急性疼痛和对钙通道阻断作出反应的病症。版权所有（C）2011，JPO＆INPIT

9. 发明专利

AU2004259357B2 Piperidine compounds and pharmaceutical compositions containing them 未知
公开(公告)号：AU2004259357B2
公开(公告)日：2010-02-18
申请号：AU2004259357
申请日：2004-07-23
申请人： EURO CELTIQUE SA
发明人： WEN XIN , ZHOU XIAOMING , SUN QUN
IPC分类号： A61P29/00 , A61K31/4545 , C07D401/04 , C07D417/14
摘要： Piperidine Compounds; compositions comprising a Piperidine Compound; and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Piperidine Compound are disclosed. In embodiment, the Piperidine Compound has the formula: and pharmaceutically acceptable salts thereof, wherein Ar 1 , Ar 2 , X, R 3 , R 4 , and m are as disclosed herein.

10. 发明专利

ES2326979T3 COMPUESTOS DE PIPERIDINA Y COMPOSICIONES FARMACEUTICAS QUE CONTIENEN A LOS MISMOS. 未知
公开(公告)号：ES2326979T3
公开(公告)日：2009-10-22
申请号：ES04779120
申请日：2004-07-23
申请人： EURO CELTIQUE SA
发明人： SUN QUN , WEN KATE , ZHOU XIAOMING
IPC分类号： C07D401/04 , A61K31/4545 , A61P29/00 , C07D417/14
摘要： Compuesto de fórmula (I): **ver fórmula** o una sal farmacéuticamente aceptable del mismo, en los que Ar1 es o una sal farmacéuticamente aceptable del mismo, en los que Ar1 es ** ver fórmula** Ar2 es ** ver fórmula** X es O, S, N-CN, N-OH, ó N-OR 10; R1 es -H, -halo, -CH3, -NO2, -CN, -OH, -OCH3, -NH2, C(halo)3, -CH(halo)2, ó -CH2(halo); cada R2 es independientemente: (a) -halo, -OH, -CN, NO 2, ó -NH 2; (b) -(C1-C10)alquilo, -(C2-C10)alquenilo, -(C2-C10)alquinilo, -(C3-C10)cicloalquilo, -(C8-C14)bicicloalquilo, -(C8- C 14)tricicloalquilo, -(C 5-C 10)cicloalquenilo, -(C 8-C 14)bicicloalquenilo, -(C 8-C 14)tricicloalquenilo, -(3 a 7 miembros) heterociclo, o -(7 a 10 miembros)bicicloheterociclo, cada uno de los cuales es no sustituido o está sustituido con uno o más grupos R5; o (c) -fenilo, -naftilo, -(C14)arilo o -(5 a 10 miembros)heteroarilo, cada uno de los cuales es no sustituido o está sustituido con uno o más grupos R 6; cada R3 es independientemente: (a) -halo, -CN, -OH, -NO 2, ó -NH 2; (b) -(C1-C10)alquilo, -(C2-C10)alquenilo, -(C2-C10)alquinilo, -(C3-C10)cicloalquilo, -(C8-C14)bicicloalquilo, -(C8- C14)tricicloalquilo, -(C5-C10)cicloalquenilo, -(C8-C14)bicicloalquenilo, -(C8-C14)tricicloalquenilo, -(3 a 7 miembros) heterociclo, o -(7 a 10 miembros)bicicloheterociclo, cada uno de los cuales es no sustituido o está sustituido con uno o más grupos R 5; o (c) -fenilo, -naftilo, -(C14)arilo o -(5 a 10 miembros)heteroarilo, cada uno de los cuales es no sustituido o está sustituido con uno o más grupos R6; R 4 es -OH, -OCF 3, -halo, -(C 1-C 6)alquilo, -CH 2OH, -CH 2Cl, -CH 2Br, -CH 2I, -CH 2F, -CH(halo) 2, -CF 3, -OR 10, -SR13, -COOH, -COOR10, -C(O)R10, -C(O)H, -OC(O)R10, -OC(O)NHR10, -NHC(O)R13, -CON(R13)2, -SO2R10, ó NO2; cada R5 es independientemente -CN, -OH, -(C1-C6)alquilo, -(C2-C6)alquenilo, -halo, -N3, -NO2, -N(R7)2, -CH=NR7, -NR 7OH, -OR 7, -COR 7, -C(O)OR 7, -OC(O)R 7, u -OC(O)OR 7; cada R6 es independientemente -(C1-C6)alquilo, -(C2-C6)alquenilo, -(C2-C6)alquinilo, -(C3-C8)cicloalquilo, -(C5- C8)cicloalquenilo, -fenilo, -(3 a 5 miembros)heterociclo, -C(halo)3, -CH(halo)2, -CH2(halo), -CN, -OH, -halo, -N3, -NO2, -CH=NR7, -NR7OH, -OR7, -COR7, -C(O)OR7, -OC(O)R7, -OC(O)OR7, -SR7, -S(O)R7, ó -S(O)2R7; cada R 7 es independientemente -H, -(C 1-C 6)alquilo, -(C 2-C 6)alquenilo, -(C 2-C 6)alquinilo, -(C 3-C 8)cicloalquilo, -(C5-C8)cicloalquenilo, -fenilo, -(3 a 5 miembros)heterociclo, -C(halo)3, -CH(halo)2, ó CH2(halo); cada R8 y R9 son independientemente -H, -(C1-C6)alquilo, -(C2-C6)alquenilo, -(C2-C6)alquinilo, -(C3-C8)cicloalquilo, -(C 5-C 8)cicloalquenilo, -fenilo, -(3 a 5 miembros)heterociclo, -CH 2C(halo) 3 -C(halo) 3, -CH(halo) 2, -CH 2(halo), -CN, -OH, -halo, -N 3, -NO 2, -CH=NR 7, -NR 7OH, -OR 7, -COR 7, -C(O)OR 7, -OC(O)R 7, -OC(O)OR 7, -SR 7, -S(O)R 7, o -S(O)2R7; R10 es -(C1-C4)alquilo; cada R13 es independientemente: (a) -H, ó -(C1-C4)alquilo; o (b) -fenilo o -(3 a 5 miembros)heteroarilo cada uno de los cuales es no sustituido o está sustituido con uno o más grupos R6; cada R14 es independientemente -(C1-C6)alquilo, -(C2-C6)alquenilo, -(C2-C6)alquinilo, -(C3-C8)cicloalquilo, -(C5- C 8)cicloalquenilo, -fenilo, -(3 a 5 miembros)heterociclo, -CH 2C(halo) 3, -C(halo) 3, -CH(halo) 2, -CH 2(halo), -CN, -OH, -halo, -N 3, -NO 2, -CH=NR 7, -NR 7OH, -OR 7, -COR 7, -C(O)OR 7, -OC(O)R 7, -OC(O)OR 7, -SR 7, -S(O)R 7, ó -S(O) 2R 7; cada halo es independientemente -F, -Cl, -Br, ó -I; n es un entero en un intervalo desde 0 a 3; p es un entero en un intervalo desde 0 a 2; q es un entero en un intervalo desde 0 a 4; y m es 0 ó 1.

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