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1. 发明授权

EP1631285B1 THERAPEUTIC AGENTS USEFUL FOR TREATING PAIN 无效
标题翻译：疼痛合适的治疗剂的治疗
公开(公告)号：EP1631285B1
公开(公告)日：2007-08-08
申请号：EP04776652.2
申请日：2004-06-14
申请人： Euro-Celtique S.A.
发明人： KYLE, Donald, J. , SUN, Qun , TAFESSE, Laykea
IPC分类号： A61K31/44 , A61K31/495 , C07D213/02 , C07D401/02 , A61P25/00
CPC分类号： C07D211/78 , C07D213/02 , C07D401/02 , C07D401/04 , C07D401/14 , C07D405/12 , C07D405/14 , C07D413/14 , C07D417/04 , C07D417/14
摘要： A compound of formula: wherein Ar1, Ar2, V, X, R3, R4, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a 'Cyclo(hetero)alkenyl Compound'); compositions comprising an effective amount of a Cyclo(hetero)alkenyl Compound; and methods for treating or preventing, e.g., pain, UI, an ulcer, IBD, or IBS in an animal, comprising administering to an animal in need thereof an effective amount of a Cyclo(hetero)alkenyl Compound are disclosed herein.

2. 发明公开

EP1583763A1 BENZOAZOLYPIPERAZINE DERIVATIVES HAVING MGLUR1- AND MGLUR5-ANTAGONISTIC ACTIVITY 有权
标题翻译：具有MGLUR1-和MGLUR5-拮抗活性的苯并氮杂哌嗪衍生物
公开(公告)号：EP1583763A1
公开(公告)日：2005-10-12
申请号：EP03814351.7
申请日：2003-12-22
申请人： Euro-Celtique S.A.
发明人： SUN, Qun , TAFESSE, Laykea , VICTORY, Sam
IPC分类号： C07D417/12 , C07D413/12 , C07D403/12 , C07D401/12 , A61K31/495 , A61P29/00 , A61P13/00
CPC分类号： C07D417/12 , A61K31/495 , C07D401/12 , C07D403/12 , C07D413/12
摘要： A compound of formula (I) wherein Ar1, A, R3, x, and m are as disclosed herein and Ar2 is a benzothiazolyl, benzooxazolyl, or benzoimidazolyl group or a pharmaceutically acceptable salt thereof (a “Benzoazolylpiperazine Compound”), compositions comprising a Benzoazolylpiperazine 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, retricted 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 Benzoazolylpiperazine Compound are disclosed.
摘要翻译：其中Ar 1，A，R 3，x和m如本文所公开且Ar 2为苯并噻唑基，苯并恶唑基或苯并咪唑基或其药学上可接受的盐（“苯并唑基哌嗪化合物”）的组合物，苯并唑基哌嗪化合物，以及治疗或预防疼痛，UI，溃疡，IBD，IBS，成瘾性病症，帕金森病，帕金森病，焦虑症，癫痫症，中风，惊厥，瘙痒症状，精神病，认知障碍，记忆公开了在动物中施用有效量的苯并唑基哌嗪化合物，包括向有需要的动物给药，包括给予有效量的苯并唑基哌嗪化合物，其中所述化合物包含有效量的苯并咪唑基哌嗪化合物或其药学可接受的盐。

3. 发明公开

EP1814851A2 4-PHENYLSULFONAMIDOPIPERIDINES AS CALCIUM CHANNEL BLOCKERS 有权
标题翻译： 4-苯磺酰氨基哌啶作为钙通道阻断剂
公开(公告)号：EP1814851A2
公开(公告)日：2007-08-08
申请号：EP05800452.4
申请日：2005-10-14
申请人： EURO-CELTIQUE S.A.
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 , C07D401/06 , C07D211/98 , A61K31/4468 , A61P29/02
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 R1-R3 and Z are defined as set forth in the specification. The invention is also directed to an assay useful for identifying such compounds as N-type calcium channel modulators or blockers. The invention is also directed to the compounds of Formula (I) and compounds identified by the above assay, and the use of such compounds to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
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，前药或溶剂化物，其中R 1 -R 3和Z如说明书中所定义。本发明还涉及用于鉴定诸如N-型钙通道调节剂或阻断剂的化合物的测定法。本发明还涉及式（I）化合物和通过上述测定法鉴定的化合物，以及这些化合物用于治疗，预防或改善响应于钙通道阻断的病症，特别是N-型钙通道。本发明的化合物对于治疗疼痛特别有用。

4. 发明公开

EP1727801A1 PIPERAZINES USEFUL FOR TREATING PAIN 有权
标题翻译：疼痛SUITABLE哌嗪的治疗
公开(公告)号：EP1727801A1
公开(公告)日：2006-12-06
申请号：EP04814866.2
申请日：2004-12-17
申请人： EURO-CELTIQUE S.A.
发明人： SUN, Qun , TAFESSE, Laykea
IPC分类号： C07D213/74 , A61K31/435 , A61K31/495 , A61P1/00 , A61P17/00 , A61P25/00 , A61P29/00
CPC分类号： C07D213/74 , C07D237/20
摘要： Compounds of formulae (I) and (II) where Ar1, Ar2, R3, R4, and m, are disclosed herein, or a pharmaceutically acceptable salt thereof (a 'Nitro(cyano)vinylpiperazine Compound'); compositions comprising an effective amount of a Nitro(cyano)vinylpiperazine 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 Nitro(cyano)vinylpiperazine Compound are disclosed.

5. 发明公开

EP1542991A1 PYRIMIDINE COMPOUNDS AS THERAPEUTIC AGENTS 审中-公开
标题翻译：嘧啶类化合物作为治疗剂
公开(公告)号：EP1542991A1
公开(公告)日：2005-06-22
申请号：EP03798728.6
申请日：2003-09-24
申请人： Euro-Celtique, S.A.
发明人： CHEN, Zhengming , TAFESSE, Laykea
IPC分类号： C07D403/04 , C07D239/42 , C07D239/46 , C07D401/12 , C07D401/14 , A61K31/506 , A61P25/22
CPC分类号： C07D239/42 , C07D239/47 , C07D401/12 , C07D401/14 , C07D403/04
摘要： The invention provides a compound of formula (I) where R1, R2, R3, A, n, and p are disclosed herein) or a pharmaceutically acceptable salt thereof (a '2-Pyrimidinylpiperazine Compound'); pharmaceutical compositions comprising an effective amount of a 2-Pyrimidinylpiperazine Compound; and methods for treating or preventing a condition such as pain, urinary incontinence, 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 2-Pyrimidinylpiperazine Compound.

6. 发明授权

EP1727801B1 PIPERAZINES USEFUL FOR TREATING PAIN 有权
标题翻译：疼痛SUITABLE哌嗪的治疗
公开(公告)号：EP1727801B1
公开(公告)日：2009-02-18
申请号：EP04814866.2
申请日：2004-12-17
申请人： EURO-CELTIQUE S.A.
发明人： SUN, Qun , TAFESSE, Laykea
IPC分类号： C07D213/74 , A61K31/435 , A61K31/495 , A61P1/00 , A61P17/00 , A61P25/00 , A61P29/00
CPC分类号： C07D213/74 , C07D237/20
摘要： Compounds of formulae (I) and (II) where Ar1, Ar2, R3, R4, and m, are disclosed herein, or a pharmaceutically acceptable salt thereof (a 'Nitro(cyano)vinylpiperazine Compound'); compositions comprising an effective amount of a Nitro(cyano)vinylpiperazine 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 Nitro(cyano)vinylpiperazine Compound are disclosed.

7. 发明公开

EP1631285A1 THERAPEUTIC AGENTS USEFUL FOR TREATING PAIN 无效
标题翻译：治疗疼痛的治疗药物
公开(公告)号：EP1631285A1
公开(公告)日：2006-03-08
申请号：EP04776652.2
申请日：2004-06-14
申请人： Euro-Celtique, S.A.
发明人： KYLE, Donald, J. , SUN, Qun , TAFESSE, Laykea
IPC分类号： A61K31/44 , A61K31/495 , C07D213/02 , C07D401/02
CPC分类号： C07D211/78 , C07D213/02 , C07D401/02 , C07D401/04 , C07D401/14 , C07D405/12 , C07D405/14 , C07D413/14 , C07D417/04 , C07D417/14
摘要： A compound of formula: wherein Ar1, Ar2, V, X, R3, R4, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a 'Cyclo(hetero)alkenyl Compound'); compositions comprising an effective amount of a Cyclo(hetero)alkenyl Compound; and methods for treating or preventing, e.g., pain, UI, an ulcer, IBD, or IBS in an animal, comprising administering to an animal in need thereof an effective amount of a Cyclo(hetero)alkenyl Compound are disclosed herein.
摘要翻译：具有下式的化合物：其中Ar 1，Ar 2，V，X，R 3，R 4和m如本文所公开的或其药学上可接受的盐（'环（杂）烯基化合物'）; 包含有效量的环（杂）烯基化合物的组合物; 和用于治疗或预防例如动物中的疼痛，UI，溃疡，IBD或IBS的方法，其包括向有需要的动物施用有效量的环（杂）烯基化合物。

8. 发明授权

EP1814851B1 4-PHENYLSULFONAMIDOPIPERIDINES AS CALCIUM CHANNEL BLOCKERS 有权
标题翻译： 4-苯磺酰氨基哌啶作为钙通道阻断剂
公开(公告)号：EP1814851B1
公开(公告)日：2013-06-05
申请号：EP05800452.4
申请日：2005-10-14
申请人： EURO-CELTIQUE S.A.
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： C07D211/96 , C07D211/58 , C07D401/06 , C07D211/98 , A61K31/4468
CPC分类号： C07D401/06 , C07D211/58 , C07D211/96

9. 发明公开

EP1943250A1 FUSED AND SPIROCYCLE COMPOUNDS AND THE USE THEREOF 审中-公开
标题翻译：简明和螺环化合物及其用途
公开(公告)号：EP1943250A1
公开(公告)日：2008-07-16
申请号：EP06777176.6
申请日：2006-09-08
申请人： EURO-CELTIQUE S.A.
发明人： CHEN, Zhengming , TAFESSE, Laykea , YAO, Jiangchao , ISLAM, Khondaker
IPC分类号： C07D471/10 , C07D221/20 , A61K31/438 , A61P25/04
CPC分类号： C07D491/107 , C07D221/20 , C07D471/10 , G01N33/566
摘要： The invention relates to fused and spirocycle compounds of Formula (I), or a pharmaceutically acceptable salt, prodrug, or solvate thereof, wherein R1, R2, Q1-Q3, and Z are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula (I) to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.

10. 发明授权

EP1583763B1 BENZOAZOLYLPIPERAZINE DERIVATIVES HAVING VR1-ANTAGONIST ACTIVITY 有权
标题翻译：具有VR1拮抗剂活性的苯并唑基哌嗪衍生物
公开(公告)号：EP1583763B1
公开(公告)日：2008-03-26
申请号：EP03814351.7
申请日：2003-12-22
申请人： Euro-Celtique S.A.
发明人： SUN, Qun , TAFESSE, Laykea , VICTORY, Sam
IPC分类号： C07D417/12 , C07D413/12 , C07D403/12 , C07D401/12 , A61K31/495 , A61P29/00 , A61P13/00
CPC分类号： C07D417/12 , A61K31/495 , C07D401/12 , C07D403/12 , C07D413/12
摘要： A compound of formula (I) wherein Ar1, A, R3, x, and m are as disclosed herein and Ar2 is a benzothiazolyl, benzooxazolyl, or benzoimidazolyl group or a pharmaceutically acceptable salt thereof (a “Benzoazolylpiperazine Compound”), compositions comprising a Benzoazolylpiperazine 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, retricted 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 Benzoazolylpiperazine Compound are disclosed.
摘要翻译：其中Ar 1，A，R 3，x和m如本文所公开且Ar 2为苯并噻唑基，苯并恶唑基或苯并咪唑基或其药学上可接受的盐（“苯并唑基哌嗪化合物”）的组合物，苯并唑基哌嗪化合物，以及治疗或预防疼痛，UI，溃疡，IBD，IBS，成瘾性病症，帕金森病，帕金森病，焦虑症，癫痫症，中风，惊厥，瘙痒症状，精神病，认知障碍，记忆公开了在动物中施用有效量的苯并唑基哌嗪化合物，包括向有需要的动物给药，包括给予有效量的苯并唑基哌嗪化合物，其中所述化合物包含有效量的苯并咪唑基哌嗪化合物或其药学可接受的盐。

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