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31. 发明申请

WO2003093236A1 1-(PYRID-2-YL)-PIPERAZINE COMPOUNDS AS METABOTROPIC GLUTAMATE RECEPTOR INHIBITOR 审中-公开
标题翻译： 1-（PYRID-2-YL） - 哌嗪化合物作为代谢型谷氨酸受体抑制剂
公开(公告)号：WO2003093236A1
公开(公告)日：2003-11-13
申请号：PCT/US2003/013964
申请日：2003-05-02
申请人： EURO-CELTIQUE, S.A. , GHARAGOZLOO, Parviz , ISLAM, Khondaker , KYLE, Donald, J. , SUN, Qun , TAFESSE, Laykea , WHITEHEAD, John, William, Frank , YANG, Ji , ZHOU, Xiaoming
发明人： GHARAGOZLOO, Parviz , ISLAM, Khondaker , KYLE, Donald, J. , SUN, Qun , TAFESSE, Laykea , WHITEHEAD, John, William, Frank , YANG, Ji , ZHOU, Xiaoming
IPC分类号： C07D213/74
CPC分类号： C07D213/74 , C07D213/80 , C07D213/85 , C07D401/04 , C07D401/14 , C07D405/12
摘要： A compound of formula: (I) (wherein A, R 1 , R 2 , R 6 , m and n are disclosed herein) or a pharmaceutically acceptable salt thereof (a "Piperazine Compound"); pharmaceutical compositions comprising a Piperazine Compound; and methods for treating pain, urinary incontinence (Ul), 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 (ALS), dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia and depression in an animal comprising administering to an animal in need thereof an effective amount of a Piperazine Compound are disclosed.
摘要翻译：式（I）（其中A，R 1，R 2，R 6，m和n在本文中公开）的化合物或其药学上可接受的盐（“哌嗪化合物”）; 包含哌嗪化合物的药物组合物; 治疗疼痛，尿失禁（Ul），成瘾性障碍，帕金森病，帕金森综合征，焦虑症，癫痫，中风，癫痫发作，瘙痒症状，精神病，认知障碍，记忆缺陷，限制性脑功能，亨廷顿氏舞蹈症，肌萎缩性侧索硬化（ALS），痴呆，视网膜病变，肌肉痉挛，偏头痛，呕吐，运动障碍和抑郁症，包括向有需要的动物施用有效量的哌嗪化合物。

32. 发明申请

WO2004002983A2 THERAPEUTIC AGENTS USEFUL FOR TREATING PAIN 审中-公开
标题翻译：治疗药物有用的治疗药物
公开(公告)号：WO2004002983A2
公开(公告)日：2004-01-08
申请号：PCT/US2003/020509
申请日：2003-06-27
申请人： EURO-CELTIQUE, S.A. , 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： C07D401/00
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 3 , R 6 , 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，成瘾性疾病，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。

33. 发明申请

WO2005066130A1 PIPERAZINES USEFUL FOR TREATING PAIN 审中-公开
标题翻译：用于治疗疼痛的PIPERAZINES有用
公开(公告)号：WO2005066130A1
公开(公告)日：2005-07-21
申请号：PCT/US2004/042732
申请日：2004-12-17
申请人： EURO-CELTIQUE S.A. , SUN, Qun , TAFESSE, Laykea
发明人： SUN, Qun , TAFESSE, Laykea
IPC分类号： C07D213/74
CPC分类号： C07D213/74 , C07D237/20
摘要： Compounds of formulae (I) and (II) where Ar 1 , Ar 2 , R 3 , R 4 , 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.
摘要翻译：其中Ar1，Ar2，R3，R4和m在本文中公开的式（I）和（II）的化合物或其药学上可接受的盐（“硝基（氰基）乙烯基哌嗪化合物”）; 包含有效量的硝基（氰基）乙烯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他病症的方法，其包括向有需要的动物施用有效量的硝基（氰基）乙烯基哌嗪化合物。

34. 发明申请

WO2004029044A1 PYRIMIDINE COMPOUNDS AS THERAPEUTIC AGENTS 审中-公开
标题翻译：吡嗪类化合物作为治疗药物
公开(公告)号：WO2004029044A1
公开(公告)日：2004-04-08
申请号：PCT/US2003/030187
申请日：2003-09-24
申请人： EURO-CELTIQUE, S.A. , CHEN, Zhengming , TAFESSE, Laykea
发明人： CHEN, Zhengming , TAFESSE, Laykea
IPC分类号： C07D403/04
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 R 1 , R 2 , R 3 , 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.
摘要翻译：本发明提供其中R1，R2，R3，A，n和p在本文中公开的式（I）化合物或其药学上可接受的盐（“2-嘧啶基哌嗪化合物”）; 包含有效量的2-嘧啶基哌嗪化合物的药物组合物; 治疗或预防诸如疼痛，尿失禁，成瘾性障碍，帕金森病，帕金森综合征，焦虑症，癫痫，中风，癫痫发作，瘙痒症状，精神病，认知障碍，记忆缺陷，限制性脑功能等疾病的方法亨廷顿舞蹈病，肌萎缩性侧索硬化症，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，包括向有需要的动物施用有效量的2-嘧啶基哌嗪化合物。

35. 发明申请

WO2007057229A1 4-OXADIAZOLYL-PIPERIDINE COMPOUNDS AND USE THEREOF 审中-公开
标题翻译： 4-氧杂双环哌啶化合物及其用途
公开(公告)号：WO2007057229A1
公开(公告)日：2007-05-24
申请号：PCT/EP2006/011150
申请日：2006-11-21
申请人： EURO-CELTIQUE S.A. , TAFESSE, Laykea
发明人： TAFESSE, Laykea
IPC分类号： C07D413/04 , C07D413/14 , A61K31/454 , A61P25/00
CPC分类号： C07D413/04 , C07D413/14
摘要： 4-Oxadiazolyl-piperidine compounds of formula (I) and (II), their compositions and use for the treatment of pain and diarrhoea.
摘要翻译：式（I）和（II）的4-恶二唑基 - 哌啶化合物，其组合物和用于治疗疼痛和腹泻的用途。

36. 发明申请

WO2006040181A3 4-PHENYLSULFONAMIDOPIPERIDINES AS CALCIUM CHANNEL BLOCKERS 审中-公开
公开(公告)号：WO2006040181A3
公开(公告)日：2006-04-20
申请号：PCT/EP2005/011105
申请日：2005-10-14
申请人： EURO-CELTIQUE S.A. , 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
IPC分类号： C07D211/58 , C07D401/06 , C07D211/98 , A61K31/4468 , A61P29/02
摘要： The invention relates to piperidinyl compounds of Formula (I): or a pharmaceutically acceptable salt, prodrug, or solvate thereof, wherein R 1 -R 3 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.

37. 发明申请

WO2004058754A1 BENZOAZOLYPIPERAZINE DERIVATIVES HAVING MGLUR1- AND MGLUR5-ANTAGONISTIC ACTIVITY 审中-公开
标题翻译：具有MGLUR1和MGLUR5拮抗活性的苯并唑啉嘌呤衍生物
公开(公告)号：WO2004058754A1
公开(公告)日：2004-07-15
申请号：PCT/US2003/041100
申请日：2003-12-22
申请人： EURO-CELTIQUE S.A. , SUN, Qun , TAFESSE, Laykea , VICTORY, Sam
发明人： SUN, Qun , TAFESSE, Laykea , VICTORY, Sam
IPC分类号： C07D417/12
CPC分类号： C07D417/12 , A61K31/495 , C07D401/12 , C07D403/12 , C07D413/12
摘要： A compound of formula (I) wherein Ar 1 , A, R 3 , x, and m are as disclosed herein and Ar 2 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Ar1，A，R3，x和m如本文所公开的式（I）化合物，Ar 2是苯并噻唑基，苯并恶唑基或苯并咪唑基或其药学上可接受的盐（“苯并恶唑基哌嗪化合物”），苯并唑基哌嗪化合物，治疗或预防疼痛的方法，UI，溃疡，IBD，IBS，成瘾性障碍，帕金森病，帕金森综合征，焦虑症，癫痫，中风，癫痫发作，瘙痒症状，精神病，认知障碍，记忆包括对有需要的动物施用有效量的苯并恶唑基哌嗪化合物，其中所述方法包括给予有需要的动物，苯并恶唑基哌嗪化合物。

38. 发明申请

WO2017210616A1 TRACE AMINE ASSOCIATED RECEPTOR 1 AGONISTS AND PARTIAL AGONISTS FOR PAIN TREATMENT 审中-公开
标题翻译： TRAIL胺相关受体1激动剂和部分激动剂治疗疼痛
公开(公告)号：WO2017210616A1
公开(公告)日：2017-12-07
申请号：PCT/US2017/035776
申请日：2017-06-02
申请人： PURDUE PHARMA L.P.
发明人： HUMMEL, Michele , TAFESSE, Laykea , KYLE, Donald J. , WHITESIDE, Garth
IPC分类号： A61K31/455 , A61K9/48
CPC分类号： A61K31/5386 , A61K9/0019 , A61K9/0053 , A61K31/402 , A61K31/4164 , A61K31/4174 , A61K31/421 , A61K31/44 , A61K31/4439 , A61K31/455 , A61K31/485 , A61K31/5377 , A61P25/02
摘要： This application relates to using trace amine associated receptor 1 (TAAR1) agonists and/or partial agonists for treating or preventing pain, especially neuropathic pain.
摘要翻译：本申请涉及使用痕量胺相关受体1（TAAR1）激动剂和/或部分激动剂来治疗或预防疼痛，特别是神经性疼痛。

39. 发明申请

WO2015171553A1 BENZOMORPHAN ANALOGS AND USE THEREOF 审中-公开
标题翻译：苯并吡喃类似物及其用途
公开(公告)号：WO2015171553A1
公开(公告)日：2015-11-12
申请号：PCT/US2015/029161
申请日：2015-05-05
申请人： PURDUE PHARMA L.P.
发明人： TAFESSE, Laykea , YAO, Jiangchao , YU, Jianming , GOEHRING, R. Richard
IPC分类号： A61K31/439 , A61K31/485 , A61P29/00
CPC分类号： C07D221/26 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The invention provides compounds as represented by Formula I or I' and pharmaceutically acceptable salts, solvates, and diastereomers thereof: Wherein R 1 , R 2 , R 2a , R 3 , and R 4 are defined in the disclosure. The invention also provides compounds of Formulae II, III, and A-H, and pharmaceutically acceptable salts, solvates, and diastereomers thereof. In certain embodiments, Compounds of the Invention are useful for treating pain, constipation, and other conditions as delineated in the disclosure. Without wishing to be bound by any theory, it is believed that Compounds of the Invention are effective in treating conditions that are modulated by activity of opioid and/or ORL-1 receptors.
摘要翻译：本发明提供由式I或I'表示的化合物及其药学上可接受的盐，溶剂合物和非对映异构体：其中R1，R2，R2a，R3和R4在本公开内容中定义。本发明还提供式II，III和A-H的化合物及其药学上可接受的盐，溶剂化物和非对映异构体。在某些实施方案中，本发明的化合物可用于治疗本发明所描述的疼痛，便秘和其它病症。不希望受任何理论的约束，相信本发明的化合物在治疗由阿片样物质和/或ORL-1受体的活性调节的病症中是有效的。

40. 发明申请

WO2015099863A1 6-SUBSTITUTED AND 7-SUBSTITUTED MORPHINAN ANALOGS AND THE USE THEREOF 审中-公开
标题翻译： 6-取代和7-取代的吗啉类似物及其用途
公开(公告)号：WO2015099863A1
公开(公告)日：2015-07-02
申请号：PCT/US2014/060113
申请日：2014-10-10
申请人： PURDUE PHARMA L.P.
发明人： LOCKMAN, Jeffrey , TAFESSE, Laykea , PARK, Jae, Hyun , YOUNGMAN, Mark
IPC分类号： A61K31/485 , C07D221/08 , C07D471/08
CPC分类号： C07D221/28 , C07C53/18 , C07D221/08 , C07D471/08 , C07D491/18
摘要： The application is directed to compounds of Formula I or II: and pharmaceutically acceptable salts and solvates thereof, wherein R', R", R"' R 1 , R 2 , R 3 , R 4 , R 4a , and R 20 are defined as set forth in the specification. The invention is also directed to use of compounds of Formula I or II and the pharmaceutically acceptable salts and solvates thereof to treat disorders responsive to the modulation of one or more opioid receptors. Certain compounds of the invention are especially useful for treating pain.
摘要翻译：本发明涉及式I或II化合物及其药学上可接受的盐和溶剂化物，其中R'，R“，R”'R 1，R 2，R 3，R 4，R 4a和R 20定义如说明书。本发明还涉及使用式I或II的化合物及其药学上可接受的盐和溶剂化物来治疗对一种或多种阿片受体调节作用的病症。本发明的某些化合物特别适用于治疗疼痛。

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