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1. 发明申请

WO2006019886A3 PYRROLO(OXO)ISOQUINOLINES AS 5HT LIGANDS 审中-公开
公开(公告)号：WO2006019886A3
公开(公告)日：2006-02-23
申请号：PCT/US2005/024953
申请日：2005-07-14
申请人： BRISTOL-MYERS SQUIBB COMPANY , FEVIG, John, M. , FENG, Jianxin , AHMAD, Saleem
发明人： FEVIG, John, M. , FENG, Jianxin , AHMAD, Saleem
IPC分类号： A61K31/437 , C07D471/04 , C07D471/12
摘要： The present application describes compounds 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 or pharmaceutically acceptable salt forms thereof, wherein A, B, D, E, m, n, R3, R7, R8, R9, R10, R11 and X are described herein.

2. 发明申请

WO2006019940A2 PYRROLO(OXO)QUINOLINES AS 5HT LIGANDS 审中-公开
标题翻译：吡咯（OXO）喹啉作为5HT配体
公开(公告)号：WO2006019940A2
公开(公告)日：2006-02-23
申请号：PCT/US2005/025038
申请日：2005-07-14
申请人： BRISTOL-MYERS SQUIBB COMPANY , FEVIG, John, M. , FENG, Jianxin , AHMAD, Saleem
发明人： FEVIG, John, M. , FENG, Jianxin , AHMAD, Saleem
IPC分类号： A61K31/4745 , C07D471/02
CPC分类号： C07D471/04
摘要： The present application provides pyrrolo (oxo) isoquinolines as modulators of serotonin receptors, pharmaceutical compositions containing such modulators and methods for 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 such compounds and compositions.
摘要翻译：本申请提供吡咯并（氧代）异喹啉作为5-羟色胺受体调节剂，含有此类调节剂的药物组合物以及治疗与血清素受体调节有关的各种疾病，病症和病症的方法，例如：代谢疾病，其包括但不限于肥胖症，糖尿病，糖尿病并发症，动脉粥样硬化，葡萄糖耐量降低和血脂异常; 包括但不限于焦虑症，抑郁症，强迫症，恐慌症，精神病，精神分裂症，睡眠障碍，性障碍和社交恐怖症的中枢神经系统疾病; 头痛; 偏头痛; 和使用这种化合物和组合物的胃肠疾病。

3. 发明申请

WO2006019886A2 PYRROLO(OXO)ISOQUINOLINES AS 5HT LIGANDS 审中-公开
标题翻译： PYRROLO（OXO）ISOQUINOLINES作为5HT配置
公开(公告)号：WO2006019886A2
公开(公告)日：2006-02-23
申请号：PCT/US2005024953
申请日：2005-07-14
申请人： SQUIBB BRISTOL MYERS CO , FEVIG JOHN M , FENG JIANXIN , AHMAD SALEEM
发明人： FEVIG JOHN M , FENG JIANXIN , AHMAD SALEEM
IPC分类号： A61K31/4745 , C07D471/02
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 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 or pharmaceutically acceptable salt forms thereof, wherein A, B, D, E, m, n, R3, R7, R8, R9, R10, R11 and X are described herein.
摘要翻译：本申请描述了根据式I的化合物，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和治疗与调节血清素受体相关的各种疾病，病症和病症的方法，例如糖尿病并发症，动脉粥样硬化，葡萄糖耐量异常和血脂异常等代谢疾病，包括但不限于肥胖，糖尿病，糖尿病并发症，动脉粥样硬化，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的化合物或其药学上可接受的盐形式的胃肠道疾病，其中A，B，D，E，m，n，R 3，R 7，R 8，R 9，R 10，R 11和X在本文中描述。

4. 发明申请

WO2006127287A3 PYRROLOPYRIDINE-BASED INHIBITORS OF DIPEPTIDYL PEPTIDASE IV AND METHODS 审中-公开
标题翻译：基于吡咯基吡啶的DIPEPTIDYL PEPTIDASE IV和方法的抑制剂
公开(公告)号：WO2006127287A3
公开(公告)日：2007-06-07
申请号：PCT/US2006018185
申请日：2006-05-11
申请人： SQUIBB BRISTOL MYERS CO , DEVASTHALE PRATIK , WANG WEI , HAMANN LAWRENCE G , O'CONNOR STEPHEN P , FEVIG JOHN M
发明人： DEVASTHALE PRATIK , WANG WEI , HAMANN LAWRENCE G , O'CONNOR STEPHEN P , FEVIG JOHN M
IPC分类号： C07D487/04 , A61K31/407
CPC分类号： C07D471/04
摘要： Compounds are provided having the formula (I): wherein R, X, Y, Z, A and n are as defined herein, which are inhibitors of dipeptidyl peptidase IV and thus are useful in treating diabetes and related diseases.
摘要翻译：提供具有式（I）的化合物：其中R，X，Y，Z，A和n如本文所定义，其是二肽基肽酶IV的抑制剂，因此可用于治疗糖尿病和相关疾病。

5. 发明申请

WO2006127287A2 PYRROLOPYRIDINE-BASED INHIBITORS OF DIPEPTIDYL PEPTIDASE IV AND METHODS 审中-公开
标题翻译：基于吡咯基吡啶的DIPEPTIDYL PEPTIDASE IV和方法的抑制剂
公开(公告)号：WO2006127287A2
公开(公告)日：2006-11-30
申请号：PCT/US2006/018185
申请日：2006-05-11
申请人： BRISTOL-MYERS SQUIBB COMPANY , DEVASTHALE, Pratik , WANG, Wei , HAMANN, Lawrence G. , O'CONNOR, Stephen P. , FEVIG, John M.
发明人： DEVASTHALE, Pratik , WANG, Wei , HAMANN, Lawrence G. , O'CONNOR, Stephen P. , FEVIG, John M.
IPC分类号： C07D487/04 , A61K31/407
CPC分类号： C07D471/04
摘要： Compounds are provided having the formula (I): wherein R, X, Y, Z, A and n are as defined herein, which are inhibitors of dipeptidyl peptidase IV and thus are useful in treating diabetes and related diseases.
摘要翻译：提供具有式（I）的化合物：其中R，X，Y，Z，A和n如本文所定义，其是二肽基肽酶IV的抑制剂，因此可用于治疗糖尿病和相关疾病。

6. 发明申请

WO2006019940A3 PYRROLO(OXO)QUINOLINES AS 5HT LIGANDS 审中-公开
标题翻译： PYRROLO（OXO）QUINOLINES作为5HT配置
公开(公告)号：WO2006019940A3
公开(公告)日：2006-06-08
申请号：PCT/US2005025038
申请日：2005-07-14
申请人： SQUIBB BRISTOL MYERS CO , FEVIG JOHN M , FENG JIANXIN , AHMAD SALEEM
发明人： FEVIG JOHN M , FENG JIANXIN , AHMAD SALEEM
IPC分类号： C07D471/04 , A61K31/437 , C07D487/02
CPC分类号： C07D471/04
摘要： The present application provides pyrrolo (oxo) isoquinolines as modulators of serotonin receptors, pharmaceutical compositions containing such modulators and methods for 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 such compounds and compositions.
摘要翻译：本申请提供吡咯（氧代）异喹啉作为5-羟色胺受体的调节剂，含有这种调节剂的药物组合物和用于治疗与调节血清素受体相关的各种疾病，病症和病症的方法，所述调节剂包括但不限于代谢疾病限于肥胖，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; 和使用这些化合物和组合物的胃肠道疾病。

7. 发明申请

WO2008137436A1 [6,5]-BICYCLIC GPR119 G PROTEIN-COUPLED RECEPTOR AGONISTS 审中-公开
标题翻译： [6,5] -BICYCLIC GPR119 G蛋白偶联受体激动剂
公开(公告)号：WO2008137436A1
公开(公告)日：2008-11-13
申请号：PCT/US2008/061930
申请日：2008-04-30
申请人： BRISTOL-MYERS SQUIBB COMPANY , FEVIG, John M. , WACKER, Dean A.
发明人： FEVIG, John M. , WACKER, Dean A.
IPC分类号： C07D471/04 , C07D473/34 , C07D487/04 , A61K31/4375 , A61K31/52 , A61K31/519 , A61P3/00
CPC分类号： C07D471/04 , C07D473/34 , C07D487/04
摘要： Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure: or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein n2, n3, n4, A, B, D, E, G, J, Y, R 1 and R 2 are defined herein.
摘要翻译：提供了新的化合物，它们是GPR119G蛋白偶联受体调节剂。 GPR119 G蛋白偶联受体调节剂可用于治疗，预防或减缓需要GPR119 G蛋白偶联受体调节剂治疗的疾病进展。这些新化合物具有以下结构：或其立体异构体或前药或其药学上可接受的盐，其中n2，n3，n4，A，B，D，E，G，J，Y，R 1和R SUB> 2 在本文中定义。

8. 发明申请

WO2008137435A1 [6,6] AND [6,7]-BICYCLIC GPR119 G PROTEIN-COUPLED RECEPTOR AGONISTS 审中-公开
标题翻译： [6,6]和[6,7] -BICYCLIC GPR119 G蛋白偶联受体激动剂
公开(公告)号：WO2008137435A1
公开(公告)日：2008-11-13
申请号：PCT/US2008/061928
申请日：2008-04-30
申请人： BRISTOL-MYERS SQUIBB COMPANY , FEVIG, John M. , WACKER, Dean A.
发明人： FEVIG, John M. , WACKER, Dean A.
IPC分类号： C07D413/04 , C07D413/14 , C07D471/04 , C07D498/04 , A61K31/5383 , A61K31/553 , A61K31/522 , A61P3/00
CPC分类号： C07D413/04 , C07D413/14 , C07D471/04 , C07D498/04
摘要： Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure:formule (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein n 1 , n 2 , n 3 , n 4 , A, B, D, E, G, Y, Z, R 1 and R 2 are defined herein.
摘要翻译：提供了新的化合物，它们是GPR119G蛋白偶联受体调节剂。 GPR119 G蛋白偶联受体调节剂可用于治疗，预防或减缓需要GPR119 G蛋白偶联受体调节剂治疗的疾病进展。这些新化合物具有以下结构：式（I）或其立体异构体或前药或其药学上可接受的盐，其中n 1，n 2，n 3， >，n 4，A，B，D，E，G，Y，Z，R 1和R 2在本文中定义。

9. 发明申请

WO2008064107A3 7,8-DIHYDRO-1,6-NAPHTHYRIDIN-5(6H)-ONES AND RELATED BICYCLIC COMPOUNDS AS INHIBITORS OF DIPEPTIDYL PEPTIDASE IV AND METHODS 审中-公开
标题翻译： 7,8-二氢-1,6-萘二酮-5（6H） - 酮和相关双酚化合物作为DIPEPTIDYL PEPTIDASE IV的抑制剂和方法
公开(公告)号：WO2008064107A3
公开(公告)日：2008-07-10
申请号：PCT/US2007084927
申请日：2007-11-16
申请人： SQUIBB BRISTOL MYERS CO , FEVIG JOHN M , FENG JIANXIN
发明人： FEVIG JOHN M , FENG JIANXIN
IPC分类号： C07D471/04 , A61K31/4375 , A61P3/06
CPC分类号： C07D471/04
摘要： The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an DPP4 modulated disease or disorder such as, for example, diabetes, by administration of a therapeutically effective dose of a compound according to Formula I. wherein X, Z, A, R2, Y, R1, n, and b are as defined herein.
摘要翻译：本申请提供化合物，包括根据式I的所有立体异构体，溶剂合物，前药和药学上可接受的形式。另外，本申请提供含有至少一种根据式I的化合物和任选的至少一种另外的治疗剂的药物组合物。最后，本申请提供了通过施用治疗有效剂量的根据式I的化合物治疗患有DPP4调节的疾病或病症例如糖尿病的患者的方法。其中X，Z，A，R 2 ，Y，R 1，n和b如本文所定义。

10. 发明申请

WO2008064107A2 7,8-DIHYDRO-1,6-NAPHTHYRIDIN-5(6H)-ONES AND RELATED BICYCLIC COMPOUNDS AS INHIBITORS OF DIPEPTIDYL PEPTIDASE IV AND METHODS 审中-公开
标题翻译： 7,8-二氢-1,6-萘啶-5（6H） - 酮及相关的双环化合物作为二磷酸肽酶IV的抑制剂和方法
公开(公告)号：WO2008064107A2
公开(公告)日：2008-05-29
申请号：PCT/US2007/084927
申请日：2007-11-16
申请人： BRISTOL-MYERS SQUIBB COMPANY , FEVIG, John M. , FENG, Jianxin
发明人： FEVIG, John M. , FENG, Jianxin
IPC分类号： C07D471/04 , A61K31/4375 , A61P3/06
CPC分类号： C07D471/04
摘要： The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an DPP4 modulated disease or disorder such as, for example, diabetes, by administration of a therapeutically effective dose of a compound according to Formula I. wherein X, Z, A, R2, Y, R1, n, and b are as defined herein.
摘要翻译：本申请提供了包括根据式I的所有立体异构体，溶剂合物，前药和药学上可接受的形式的化合物。此外，本申请提供了药物组合物，其含有至少一种根据式I的化合物和任选地至少一种另外的治疗剂。最后，本申请提供了通过施用治疗有效剂量的根据式I的化合物治疗患有DPP4调节的疾病或病症例如糖尿病的患者的方法，其中X，Z，A，R2 ，Y，R1，n和b如本文所定义。

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