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1. 发明申请

WO2004056324A2 SUBSTITUTED TRICYCLIC GAMMA-CARBOLINES AS SEROTONIN RECEPTOR AGONISTS AND ANTAGONISTS 审中-公开
标题翻译：作为丝氨酸蛋白酶受体激动剂和拮抗剂的取代三聚氰胺
公开(公告)号：WO2004056324A2
公开(公告)日：2004-07-08
申请号：PCT/US2003/041447
申请日：2003-12-19
申请人： BRISTOL-MYERS SQUIBB COMPANY , LEE, Taekyu , CHEN, Wenting , DENG, Wei , ROBICHAUD, Albert , WEXLER, Ruth
发明人： LEE, Taekyu , CHEN, Wenting , DENG, Wei , ROBICHAUD, Albert , WEXLER, Ruth
IPC分类号： A61K
CPC分类号： C07D471/04
摘要： The present invention is directed to novel compounds represented by structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein R 1 , R 4a , R 5 , R 6 , R 7 , R 8 , R 9 , and m, are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain central nervous system disorders. The compounds of this invention are serotonin receptor modulators, in particular 5HT 2C receptor agonists and antagonists, and are useful in the control or prevention of central nervous system disorders including obesity, anorexia, bulemia, depression, anxiety, psychosis, schizophrenia, migraine, addictive behavior, obsessive-compulsive disorder, and sexual disorders.
摘要翻译：本发明涉及由结构式（I）表示的新化合物：或其药学上可接受的盐，其中R 1，R 4，R 5，R 6，R 7，R 7， <8>，R 9和m在本文中定义。本发明还涉及包含这些新化合物作为活性成分的药物制剂以及新型化合物及其制剂在治疗某些中枢神经系统疾病中的用途。本发明的化合物是5-羟色胺受体调节剂，特别是5HT 2C受体激动剂和拮抗剂，并且可用于控制或预防中枢神经系统疾病，包括肥胖症，厌食症，血友病，抑郁症，焦虑症，精神病，精神分裂症，偏头痛，成瘾行为，强迫症，强迫症和性功能障碍。

2. 发明申请

WO2005105082A1 SUBSTITUTED HEXAHYDRO-PYRIDOINDOLE DERIVATIVES AS SEROTONIN RECEPTOR AGONISTS AND ANTAGONISTS 审中-公开
标题翻译：作为丝氨酸受体激动剂和拮抗剂的取代的十六氢吡啶衍生物
公开(公告)号：WO2005105082A1
公开(公告)日：2005-11-10
申请号：PCT/US2005/012546
申请日：2005-04-14
申请人： BRISTOL-MYERS SQUIBB COMPANY , LEE, Taekyu , DENG, Wei , ROBICHAUD, Albert J.
发明人： LEE, Taekyu , DENG, Wei , ROBICHAUD, Albert J.
IPC分类号： A61K31/437
CPC分类号： C07D471/04
摘要： The present application provides novel compounds according to Formula (I): including all stereoisomers, solvates, prodrug esters and pharmaceutically acceptable salt forms thereof, wherein R 1 , R 4a , R 5 , R 6 , R 7 , R 8 , R 9 , m, and X are described herein. Additionally, the present application provides novel pharmaceutical compositions comprising at least one compound according to Formula (I). Further, the present application provides methods of treating a patient in need comprising administering a therapeutically effective amount of at least one compound according to Formula (I).
摘要翻译：本申请提供了根据式（I）的新化合物：包括所有立体异构体，溶剂合物，前药酯及其药学上可接受的盐形式，其中R 1，R 4a，R 5，R 6，R 本文描述了R 8，R 8，R 9，m和X。另外，本申请提供了包含至少一种根据式（I）的化合物的新型药物组合物。此外，本申请提供了治疗需要的患者的方法，其包括施用治疗有效量的至少一种根据式（I）的化合物。

3. 发明申请

WO2006138695A1 TRIAZOLOPYRIDINE DERIVATIVES AS CANNABINOID RECEPTOR 1 ANTAGONISTS 审中-公开
标题翻译：作为CANNABINOID受体1拮抗剂的三唑吡啶衍生物
公开(公告)号：WO2006138695A1
公开(公告)日：2006-12-28
申请号：PCT/US2006/023716
申请日：2006-06-19
申请人： BRISTOL-MYERS SQUIBB COMPANY , SUN, Chongqing , SHER, Philip M. , WU, Gang , EWING, William R. , HUANG, Yanting , LEE, Taekyu , MURUGESAN, Natesan , SULSKY, Richard B.
发明人： SUN, Chongqing , SHER, Philip M. , WU, Gang , EWING, William R. , HUANG, Yanting , LEE, Taekyu , MURUGESAN, Natesan , SULSKY, Richard B.
IPC分类号： C07D471/04 , A61K31/435 , A61P25/00 , A61P37/00
CPC分类号： C07D471/04
摘要： The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents, and methods of treatment using the compounds according to Formula I both alone and in combination with one or more additional therapeutic agents. The compounds have the following general formula I including all solvates, pharmaceutically acceptable salts and stereoisomers, wherein R 1 , R 2 , R 3 , R 4 and R 5 are described herein. '
摘要翻译：本申请描述了根据式I的化合物，包含至少一种根据式I的化合物和任选的一种或多种另外的治疗剂的药物组合物，以及使用式I化合物单独和与一种或多种其他治疗剂。所述化合物具有以下通式I，其包括所有溶剂合物，药学上可接受的盐和立体异构体，其中R 1，R 2，R 3，R 3，本文描述了第4和第5和第5。 “

4. 发明申请

WO2007016353A2 SUBSTITUTED TETRAHYDRO-1H-PYRIDO[4,3,B]INDOLES AS SEROTONIN RECEPTOR AGONISTS AND ANTAGONISTS 审中-公开
标题翻译：取代的四氢-1H-吡唑并[4,3，B]作为丝氨酸受体激动剂和拮抗剂
公开(公告)号：WO2007016353A2
公开(公告)日：2007-02-08
申请号：PCT/US2006/029436
申请日：2006-07-27
申请人： BRISTOL-MYERS SQUIBB COMPANY , LEE, Taekyu
发明人： LEE, Taekyu
IPC分类号： C07D471/04 , A61K31/437 , A61P3/00
CPC分类号： C07D471/04
摘要： The present application describes compounds, including all pharmaceutically acceptable salts, prodrugs, solvates and stereoisomers thereof, according to Formula I, pharmaceutical compositions, comprising at least one compound according to Formula I and optionally at least one additional therapeutic agent and methods of treating various diseases, conditions and disorders associated with modulation of serotonin receptors such as, for example: metabolic diseases, which includes but is not limited to obesity, diabetes, diabetic complications, atherosclerosis, impared glucose tolerance and dyslipidemia; central nervous system diseases which includes but is not limited to, anxiety, depression, obsessive compulsive disorder, panic disorder, psychosis, schizophrenia, sleep disorder, sexual disorder and social phobias; cephalic pain; migraine; and gastrointestinal disorders using compounds according to Formula I
摘要翻译：本申请描述了根据式I的化合物，包括其所有药学上可接受的盐，前药，溶剂化物和立体异构体，药物组合物，其包含至少一种根据式I的化合物和任选的至少一种另外的治疗剂以及治疗各种疾病的方法与调节血清素受体相关的病症和紊乱，例如：代谢疾病，其包括但不限于肥胖，糖尿病，糖尿病并发症，动脉粥样硬化，葡萄糖耐量异常和血脂异常; 包括但不限于焦虑，抑郁，强迫症，惊恐障碍，精神病，精神分裂症，睡眠障碍，性障碍和社交恐惧症的中枢神经系统疾病; 头痛偏头痛; 和使用根据式I的化合物的胃肠道疾病

5. 发明申请

WO2006138657A1 BICYCLIC HETEROCYCLES AS CANNABINOID-1 RECEPTOR MODULATORS 审中-公开
标题翻译：作为CANNABINOID-1受体调节剂的双相异构体
公开(公告)号：WO2006138657A1
公开(公告)日：2006-12-28
申请号：PCT/US2006/023638
申请日：2006-06-19
申请人： BRISTOL-MYERS SQUIBB COMPANY , SUN, Chongqing , HUANG, Yanting , SITKOFF, Doree, F. , LEE, Taekyu , EWING, William, R.
发明人： SUN, Chongqing , HUANG, Yanting , SITKOFF, Doree, F. , LEE, Taekyu , EWING, William, R.
IPC分类号： C07D487/04 , C07D471/04 , A61K31/5025 , A61K31/5377 , A61P3/00 , A61P25/00
CPC分类号： C07D471/04 , C07D487/04
摘要： The present application describes compounds according to Formula (I), pharmaceutical compositions comprising at least one compound according to Formula (I) and optionally one or more additional therapeutic agents and methods of treatment using the compounds according to Formula (I) both alone and in combination with one or more additional therapeutic agents. The compounds have the following general formula (I) including all prodrugs, solvates, pharmaceutically acceptable salts and stereoisomers, wherein A, B, R 1 , R 2 , R 3 and R 8 are described herein.
摘要翻译：本申请描述了根据式（I）的化合物，包含至少一种根据式（I）的化合物和任选的一种或多种另外的治疗剂的药物组合物和使用根据式（I）的化合物单独和与一种或多种另外的治疗剂组合。所述化合物具有以下通式（I），其包括所有前药，溶剂化物，药学上可接受的盐和立体异构体，其中A，B，R 1，R 2，R 2 > 3＆lt; 8＆gt;和＆lt; 8＆gt;。

6. 发明申请

WO2002059124A3 SUBSTITUTED PYRROLOQUINOLINES AND PYRIDOQUINOLINES AS SEROTONIN AGONISTS AND ANTAGONISTS 审中-公开
公开(公告)号：WO2002059124A3
公开(公告)日：2002-08-01
申请号：PCT/US2001/049380
申请日：2001-12-19
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： FEVIG, John, M. , MITCHELL, Ian, S. , LEE, Taekyu , CHEN, Wenting , CACCIOLA, Joseph
IPC分类号： C07D471/16
摘要： The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R 1 , R 6a , R 6b , R 7 , R 8 , R 9 X, b, m, and n are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.

7. 发明申请

WO2002059129A2 SUBSTITUTED PYRIDOINDOLES AS SEROTONIN AGONISTS AND ANTAGONISTS 审中-公开
标题翻译：作为丝氨酸激动剂和拮抗剂的替代吡啶衍生物
公开(公告)号：WO2002059129A2
公开(公告)日：2002-08-01
申请号：PCT/US2001/049371
申请日：2001-12-19
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： ROBICHAUD, Albert, J. , FEVIG, John, M. , MITCHELL, Ian, S. , LEE, Taekyu , CHEN, Wenting , CACCIOLA, Joseph
IPC分类号： C07D513/00
CPC分类号： C07D471/16 , C07D498/16 , C07D513/16
摘要： The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R 1 , R 5 , R 6 , R 7 , R 8 , R 9 , X, b, k, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.
摘要翻译：本发明涉及由结构式（I）表示的某些新化合物或其药学上可接受的盐形式，其中R 1，R 5，R 6，R 7，R 8，R <9>，X，b，k和n，这里描述虚线。本发明还涉及包含这些新化合物作为活性成分的药物制剂，以及新型化合物及其制剂在治疗某些疾病中的用途。本发明的化合物是血清素激动剂和拮抗剂，可用于控制或预防中枢神经系统疾病，包括肥胖症，焦虑症，抑郁症，精神病，精神分裂症，睡眠障碍，性障碍，偏头痛，与头痛相关的病症，社交恐怖症，以及胃肠道疾病如胃肠道运动功能障碍。

8. 发明申请

WO2002059124A2 SUBSTITUTED PYRROLOQUINOLINES AND PYRIDOQUINOLINES AS SEROTONIN AGONISTS AND ANTAGONISTS 审中-公开
标题翻译：取代的吡咯啉和吡咯烷醇作为丝氨酸激素和拮抗剂
公开(公告)号：WO2002059124A2
公开(公告)日：2002-08-01
申请号：PCT/US2001/049380
申请日：2001-12-19
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： FEVIG, John, M. , MITCHELL, Ian, S. , LEE, Taekyu , CHEN, Wenting , CACCIOLA, Joseph
IPC分类号： C07D471/16
CPC分类号： C07D471/16 , C07D498/16
摘要： The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R 1 , R 6a , R 6b , R 7 , R 8 , R 9 X, b, m, and n are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.
摘要翻译：本发明涉及由结构式（I）表示的某些新化合物或其药学上可接受的盐形式，其中R 1，R 6a，R 6b，R 7，R 8，R 8 本文描述了X，b，m和n。本发明还涉及包含这些新化合物作为活性成分的药物制剂，以及新型化合物及其制剂在治疗某些疾病中的用途。本发明的化合物是血清素激动剂和拮抗剂，可用于控制或预防中枢神经系统疾病，包括肥胖症，焦虑症，抑郁症，精神病，精神分裂症，睡眠障碍，性障碍，偏头痛，与头痛相关的病症，社交恐怖症，以及胃肠道疾病如胃肠道运动功能障碍。

9. 发明公开

EP1343791A2 SUBSTITUTED TETRACYCLIC PYRIDOINDOLES AS SEROTONIN AGONISTS AND ANTAGONISTS 审中-公开
标题翻译：取代的环TETRA并吲哚血清素激动剂和拮抗剂
公开(公告)号：EP1343791A2
公开(公告)日：2003-09-17
申请号：EP01994316.6
申请日：2001-12-19
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： ROBICHAUD, Albert, J. , FEVIG, John, M. , MITCHELL, Ian, S. , LEE, Taekyu , CHEN, Wenting , CACCIOLA, Joseph
IPC分类号： C07D513/00
CPC分类号： C07D471/16 , C07D498/16 , C07D513/16
摘要： The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R?1, R5, R6, R7, R8, R9¿, X, b, k, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.

10. 发明授权

EP1399445B9 SUBSTITUTED PYRROLOQUINOLINES AND PYRIDOQUINOLINES AS SEROTONIN AGONISTS AND ANTAGONISTS 有权
标题翻译：取代PYRROLOCHINOLINE和PYRIDOCHINOLINE ALS血清素激动剂和拮抗剂
公开(公告)号：EP1399445B9
公开(公告)日：2010-07-21
申请号：EP01994318.2
申请日：2001-12-19
申请人： Bristol-Myers Squibb Company
发明人： FEVIG, John, M. , MITCHELL, Ian, S. , LEE, Taekyu , CHEN, Wenting , CACCIOLA, Joseph
IPC分类号： C07D471/16 , C07D498/16 , C07D513/16 , A61K31/4375 , A61K31/437 , A61K31/553 , A61P25/00
CPC分类号： C07D471/16 , C07D498/16
摘要： The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R?1, R6a, R6b, R7, R8, R9¿ X, b, m, and n are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.

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