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11. 发明申请

WO2003050261A3 (1-PHENYL-2-HETEROARYL)ETHYL-GUANIDINE COMPOUNDS AS INHIBITORS OF MITOCHONDRIAL F1F0 ATP HYDROLASE 审中-公开
公开(公告)号：WO2003050261A3
公开(公告)日：2003-06-19
申请号：PCT/US2002/039478
申请日：2002-12-10
申请人： BRISTOL-MYERS SQUIBB COMPANY , ATWAL, Karnail S, , GROVER, Gary J, , DING, Charles Z, , STEIN, Philip D, , LLOYD, John , AHMAD, Saleem , HAMANN, Lawrence G, , GREEN, David , FERRARA, Francis N,
发明人： ATWAL, Karnail S, , GROVER, Gary J, , DING, Charles Z, , STEIN, Philip D, , LLOYD, John , AHMAD, Saleem , HAMANN, Lawrence G, , GREEN, David , FERRARA, Francis N,
IPC分类号： A61P9/00
摘要： Compounds having formula (I), and pharmaceutically acceptable salts thereof, are useful for modulating mitochondrial F 1 F 0 ATPase activity and treating ischemic conditions including myocardial infarction, congestive heart failure, and cardiac arrhythmias.

12. 发明申请

WO2010104818A1 AZA PYRIDONE ANALOGS USEFUL AS MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS 审中-公开
标题翻译： AZA PYRIDONE ANALOGS有益于MELANIN浓缩HORMONE RECEPTOR-1 ANTAGONISTS
公开(公告)号：WO2010104818A1
公开(公告)日：2010-09-16
申请号：PCT/US2010/026604
申请日：2010-03-09
申请人： BRISTOL-MYERS SQUIBB COMPANY , AHMAD, Saleem
发明人： AHMAD, Saleem
IPC分类号： C07D239/36 , C07D239/47 , C07D239/54 , C07D239/56
CPC分类号： C07D239/36 , C07D239/47 , C07D239/54 , C07D239/56
摘要： MCHR1 antagonists are provided having the following Formula (I): A 1 and A 2 are independently C or N; E is C or N; Q 1 , Q 2 , and Q 3 are independently C or N provided that at least one of Q 1 , Q 2 , and Q 3 is N but not more than one of Q 1 , Q 2 , and Q 3 is N; D 1 is a bond, -CR 8 R 9 X-, -XCR 8 R 9 -, -CHR 8 CHR 9 -, -CR 10 =CR 10' -, -C≡C-, or 1,2-cyclopropyl; X is O, S or NR 11 ; R 1 , R 2 , and R 3 are independently selected from the group consisting of hydrogen, halogen, lower alkyl, lower cycloalkyl, -CF 3 , -OCF 3 , -OR 12 and -SR 12 ; G is O, S or -NR 15 ; D 2 is lower alkyl, lower cycloalkyl, lower alkylcycloalkyl, lower cycloalkylalkyl, lower cycloalkoxyalkyl or lower alkylcycloalkoxy or when G is NR 15 , G and D 2 together may optionally form an azetidine, pyrrolidine or piperidine ring; Z 1 and Z 2 are independently hydrogen, lower alkyl, lower cycloalkyl, lower alkoxy, lower cycloalkoxy, halo, -CF 3 , -OCONR 14 R 14' , -CN, -CONR 14 R 14' , -SOR 12 , -SO 2 R 12 , -NR 14 COR 14' , -NR 14 CO 2 R 14' , -CO 2 R 12 , NR 14 SO 2 R 12 or COR 12 ; R 5 , R 6 , and R 7 are independently selected from the group consisting of hydrogen lower alkyl, lower cycloalkyl, -CF 3 , -SR 12 , lower alkoxy, lower cycloalkoxy, -CN, -CONR 14 R 14' , SOR 12 , SO 2 R 12 , NR 14 COR 14' , NR 14 CO 2 R 12 , CO 2 R 12 , NR 14 SO 2 R 12 and -COR 12 ; R 8 , R 9 , R 10 , R 10' , R 11 are independently hydrogen or lower alkyl; R 12 is lower alkyl or lower cycloalkyl; R 14 and R 14' are independently H, lower alkyl, lower cycloalkyl or R 14 and R 14' together with the N to which they are attached form a ring having 4 to 7 atoms; and R 15 is independently selected from the group consisting of hydrogen and lower alkyl. Such compounds are useful for the treatment of MCHR1 mediated diseases, such as obesity, diabetes, IBD, depression, and anxiety.
摘要翻译：提供具有下式（I）的MCHR1拮抗剂：A1和A2独立地为C或N; E为C或N; Q1，Q2和Q3独立地为C或N，条件是Q1，Q2和Q3中的至少一个为N但不大于Q1，Q2和Q3中的一个为N; D1是键，-CR8R9X，-XCR8R9-，-CHR8CHR9-，-CR10 = CR10'-，-C = C-或1,2-环丙基; X是O，S或NR11; R 1，R 2和R 3独立地选自氢，卤素，低级烷基，低级环烷基，-CF 3，-OCF 3，-OR 12和-SR 12; G是O，S或-NR 15; D2是低级烷基，低级环烷基，低级烷基环烷基，低级环烷基烷基，低级环烷氧基烷基或低级烷基环烷氧基，或当G是NR15时，G和D2可一起形成氮杂环丁烷，吡咯烷或哌啶环; Z1和Z2独立地是氢，低级烷基，低级环烷基，低级烷氧基，低级环烷氧基，卤素，-CF3，-OCONR14R14'，-CN，-CONR14R14'，-SOR12，-SO2R12，-NR14COR14'，-NR14CO2R14' CO 2 R 12，NR 14 SO 2 R 12或COR 12; R5，R6和R7独立地选自氢低级烷基，低级环烷基，-CF3，-SR12，低级烷氧基，低级环烷氧基，-CN，-CONR14R14'，SOR12，SO2R12，NR14COR14'，NR14CO2R12，CO2R12 ，NR14SO2R12和-COR12; R8，R9，R10，R10'，R11独立地为氢或低级烷基; R12是低级烷基或低级环烷基; R 14和R 14'独立地是H，低级烷基，低级环烷基或R 14和R 14'与它们所连接的N一起形成具有4至7个原子的环; R 15独立地选自氢和低级烷基。这些化合物可用于治疗MCHR1介导的疾病，例如肥胖症，糖尿病，IBD，抑郁症和焦虑症。

13. 发明申请

WO2008134480A1 NON-BASIC MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS 审中-公开
标题翻译：非基础麦芽宁浓缩激素受体-1拮抗剂
公开(公告)号：WO2008134480A1
公开(公告)日：2008-11-06
申请号：PCT/US2008/061519
申请日：2008-04-25
申请人： BRISTOL-MYERS SQUIBB COMPANY , WASHBURN, William N. , AHMAD, Saleem , HERNANDEZ, Andres S.
发明人： WASHBURN, William N. , AHMAD, Saleem , HERNANDEZ, Andres S.
IPC分类号： C07D495/04 , A61K31/5025 , A61K31/53 , A61K31/381 , A61P25/24
CPC分类号： C07D495/04
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 MCHR-I modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula (I) where R 1 , R 1a , R 1b , A, R 3 , R 4 , R 5 , R5 b and R 6 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。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MCHR-1调节的疾病或病症例如肥胖，糖尿病，抑郁或焦虑的患者的方法，其中R 1，R 1a，R 1b，A，R 3，R 4， R 5，R 5，R 6和R 6如本文所定义。

14. 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。

15. 发明申请

WO2014193884A1 DIHYDROPYRIDINONE MGAT2 INHIBITORS 审中-公开
标题翻译： DIHYDROPYRIDINONE MGAT2抑制剂
公开(公告)号：WO2014193884A1
公开(公告)日：2014-12-04
申请号：PCT/US2014/039661
申请日：2014-05-28
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： AHMAD, Saleem , NEGASH, Lidet, A.
IPC分类号： C07D211/86 , C07D211/90 , A61K31/44 , A61P3/00
CPC分类号： C07D211/90 , A61K31/4412 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K45/06 , C07D211/78 , C07D211/86 , C07D401/04 , C07D409/04 , C07D409/14 , C07D417/04
摘要： The present invention provides compounds of Formula (I): Formula (I)or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.
摘要翻译：本发明提供式（I）的化合物：式（I）或其立体异构体或其药学上可接受的盐，其中所有变量如本文所定义。这些化合物是可用作药物的单酰甘油酰基转移酶2型（MGAT2）抑制剂。

16. 发明申请

WO2013082345A1 ARYL DIHYDROPYRIDINONE AND PIPERIDINONE AS MGAT2 INHIBITORS 审中-公开
标题翻译： ARYL DIHYDROPRIDINONE和PIPERIDINONE作为MGAT2抑制剂
公开(公告)号：WO2013082345A1
公开(公告)日：2013-06-06
申请号：PCT/US2012/067173
申请日：2012-11-30
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： TURDI, Huji , HANGELAND, Jon J. , LAWRENCE, R. Michael , CHENG, Dong , AHMAD, Saleem , MENG, Wei , BRIGANCE, Robert Paul , DEVASTHALE, Pratik
IPC分类号： C07D211/86 , C07D211/90 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D407/14 , C07D413/04 , C07D413/12 , C07D417/04 , C07D417/14 , C07F9/40 , A61K31/4418 , A61K31/4427 , A61P3/00
CPC分类号： A61K31/438 , A61K31/4418 , A61K31/4439 , A61K31/5377 , A61K31/675 , A61K45/06 , C07D211/86 , C07D211/90 , C07D221/20 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/14 , C07D407/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/14 , C07F9/4006 , C07F9/5352 , C07F9/598
摘要： The present invention provides compounds of Formula (I), or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.
摘要翻译：本发明提供式（I）化合物或其立体异构体或其药学上可接受的盐，其中所有变量如本文所定义。这些化合物是可用作药物的单酰基甘油酰基转移酶2型（MGAT2）抑制剂。

17. 发明申请

WO2021158495A1 BENZO[5,6][1,4]DIOXINO[2,3-B]PYRIDINE COMPOUNDS USEFUL AS IRAK4 INHIBITORS 审中-公开
公开(公告)号：WO2021158495A1
公开(公告)日：2021-08-12
申请号：PCT/US2021/016123
申请日：2021-02-02
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： NEGASH, Lidet A. , AHMAD, Saleem
IPC分类号： C07D491/056 , A61P29/00 , A61P37/00 , A61P35/00 , A61K31/436
摘要： Disclosed are compounds of Formula (I) or a salt or prodrug thereof, wherein R1, R2, and R3 are defined herein. Also disclosed are methods of using such compounds as modulators of IRAK4, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing inflammatory and autoimmune diseases, or in the treatment of cancer.

18. 发明申请

WO2021030379A1 BICYCLIC HETEROARYL COMPOUNDS USEFUL AS IRAK4 INHIBITORS 审中-公开
公开(公告)号：WO2021030379A1
公开(公告)日：2021-02-18
申请号：PCT/US2020/045831
申请日：2020-08-12
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： AHMAD, Saleem , SARKUNAM, Kandhasamy , LI, Ling , NEGASH, Lidet A. , HYNES, John
IPC分类号： C07D487/04 , A61P35/00 , A61P37/00
摘要： Disclosed are compounds of Formula (I) or a salt or prodrug thereof, wherein: X is C or N; Y is C or N; Z is CR4 or N; provided that when: (i) X is N, then Y is C; and (ii) X is C, then Y is N and Z is N; and wherein R1, R2, R3, and R4 are define herein. Also disclosed are methods of using such compounds as modulators of IRAK4, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing inflammatory and autoimmune diseases, or in the treatment of cancer.

19. 发明申请

WO2016065226A1 INDOLE CARBOXAMIDES COMPOUNDS USEFUL AS KINASE INHOBITORS 审中-公开
标题翻译：吲哚类化合物可用作激酶抑制剂
公开(公告)号：WO2016065226A1
公开(公告)日：2016-04-28
申请号：PCT/US2015/057055
申请日：2015-10-23
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： AHMAD, Saleem , TINO, Joseph A. , MACOR, John E. , TEBBEN, Andrew J. , GONG, Hua , LIU, Qingjie , BATT, Douglas G. , NGU, Khehyong , WATTERSON, Scott Hunter , GUO, Weiwei , BEAUDOIN BERTRAND, Myra
IPC分类号： C07D403/12 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/10 , C07D413/04 , C07D417/04 , C07D471/04 , C07D487/04 , C07D487/10 , C07D209/18 , A61K31/4045 , A61P29/00 , A61P37/00
CPC分类号： C07D401/10 , C07D209/08 , C07D209/18 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/10 , C07D403/12 , C07D413/04 , C07D417/04 , C07D471/04 , C07D487/04 , C07D487/10
摘要： Disclosed are compounds of Formula (I): or a salt thereof, wherein: X is CR 4 or N; R 1 , R 2 , R 3 , R 4 , and A are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bruton's tyrosine kinase (Btk), and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
摘要翻译：公开了式（I）的化合物或其盐，其中：X是CR 4或N; R1，R2，R3，R4和A在本文中定义。还公开了使用这种化合物作为Bruton酪氨酸激酶（Btk）的抑制剂的方法和包含这些化合物的药物组合物。这些化合物可用于治疗，预防或减缓各种治疗领域（例如自身免疫疾病和血管疾病）中的疾病或病症的进展。

20. 发明申请

WO2014039412A1 PYRROLONE OR PYRROLIDINONE MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS 审中-公开
标题翻译：吡咯酮或吡咯烷酮富含浓度的激素受体-1拮抗剂
公开(公告)号：WO2014039412A1
公开(公告)日：2014-03-13
申请号：PCT/US2013/057767
申请日：2013-09-03
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： WASHBURN, William N. , MURUGAIAH SUBBAIAH, Murugaiah Andappan , AHMAD, Saleem
IPC分类号： C07D403/12 , C07D401/14 , C07D401/12 , C07D403/14 , C07D405/12 , C07D413/12 , C07D417/12 , C07D491/10 , C07D295/096 , C07D295/135 , A61K31/4025 , A61K31/402 , A61K31/496 , A61K31/5377 , A61K31/454
CPC分类号： C07D207/273 , A61K31/4025 , A61K31/4178 , A61K31/422 , A61K31/435 , A61K31/445 , A61K31/496 , A61K31/506 , A61K31/5377 , C07D295/096 , C07D295/135 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D413/12 , C07D417/12 , C07D491/10 , C07D491/107
摘要： The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are melanin concentrating hormone receptor-1 (MCHR1) antagonists which may be used as medicaments.
摘要翻译：本发明提供了式（I）化合物：如说明书中所定义和包含任何这些新化合物的组合物。这些化合物是可用作药物的黑色素浓缩激素受体-1（MCHR1）拮抗剂。

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