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1. 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。

2. 发明申请

WO2020033520A1 INDOLE AND AZAINDOLE INHIBITORS OF PAD ENZYMES 审中-公开
公开(公告)号：WO2020033520A1
公开(公告)日：2020-02-13
申请号：PCT/US2019/045466
申请日：2019-08-07
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： SRIVASTAVA, Anurag S. , CHERNEY, Robert J. , NGU, Khehyong
IPC分类号： A61P35/00 , A61K31/437 , C07D403/14 , C07D407/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/08
摘要： The present invention provides compounds of Formula (I) useful as inhibitors of PAD4, compositions thereof, and methods of treating PAD4-related disorders, wherein each of Ring A, L, Q, R1, R2, R3, R4, R7, and R8 along with other variables are as defined herein.

3. 发明申请

WO2005051386A1 HMG-COA REDUCTASE INHIBITORS AND METHOD 审中-公开
标题翻译： HMG-COA还原酶抑制剂和方法
公开(公告)号：WO2005051386A1
公开(公告)日：2005-06-09
申请号：PCT/US2004/039051
申请日：2004-11-19
申请人： BRISTOL-MYERS SQUIBB COMPANY , O'CONNOR, Stephen P. , ROBL, Jeffrey , AHMAD, Saleem , BISAHA, Sharon , MURUGESAN, Natesan , NGU, Khehyong , SHI, Yan , STEIN, Philip D. , SOUNDARARAJAN, Nachimuthu , NATALIE, Kenneth J. Jr. , KOLLA, Laxma R. , SAUSKER, Justin , QUINLAN, Sandra L. , FAN, Junying , PETSCH, Dejah , GUO, Zhenrong
发明人： O'CONNOR, Stephen P. , ROBL, Jeffrey , AHMAD, Saleem , BISAHA, Sharon , MURUGESAN, Natesan , NGU, Khehyong , SHI, Yan , STEIN, Philip D. , SOUNDARARAJAN, Nachimuthu , NATALIE, Kenneth J. Jr. , KOLLA, Laxma R. , SAUSKER, Justin , QUINLAN, Sandra L. , FAN, Junying , PETSCH, Dejah , GUO, Zhenrong
IPC分类号： A61K31/435
CPC分类号： C07D213/80 , C07D211/76 , C07D401/14 , C07D471/04 , C07D491/04 , C07D498/04 , C07D513/04
摘要： Compounds are provided having the following structure (I) and pharmaceutically acceptable salts thereof, A is (II) or (III); wherein R 1 , R 2 , R 3 , R 4 , U, V, W, Y, and n are as defined above, which compounds are HMG CoA reductase inhibitors and thus are active in inhibiting cholesterol biosynthesis, modulating blood serum lipids, for example, lowering LDL cholesterol and/or increasing HDL cholesterol, and treating hyperlipidemia, dyslipidemia, hypercholesterolemia, hypertriglyceridemia and atherosclerosis as well as Alzheimer's disease and osteoporosis and may be employed as hormone replacement therapy. A method for treating the above diseases employing the above compounds is also provided.
摘要翻译：提供具有以下结构（I）的化合物及其药学上可接受的盐，A是（II）或（III）; 其中R1，R2，R3，R4，U，V，W，Y和n如上所定义，这些化合物是HMG CoA还原酶抑制剂，因此具有抑制胆固醇生物合成，调节血清脂质的作用，例如降低LDL 胆固醇和/或增加HDL胆固醇，以及治疗高脂血症，血脂异常，高胆固醇血症，高甘油三酯血症和动脉粥样硬化以及阿尔茨海默病和骨质疏松症，并且可用作激素替代疗法。还提供了使用上述化合物治疗上述疾病的方法。

4. 发明申请

WO2020033514A1 BENZIMIDAZOLE INHIBITORS OF PAD ENZYMES 审中-公开
公开(公告)号：WO2020033514A1
公开(公告)日：2020-02-13
申请号：PCT/US2019/045459
申请日：2019-08-07
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： NGU, Khehyong
IPC分类号： A61P35/00 , C07D401/14 , C07D403/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , A61K31/4184
摘要： The present invention provides compounds of Formula (I): or a pharmaceutically acceptable salt thereof, useful as inhibitors of PAD4, compositions thereof, and methods of treating PAD4-related disorders. Variables rings A, B, R 1 , R 3 , R 8 , and other variables are as defined herein.

5. 发明申请

WO2009009501A4 NON-BASIC MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS AND METHODS 审中-公开
公开(公告)号：WO2009009501A4
公开(公告)日：2009-01-15
申请号：PCT/US2008/069361
申请日：2008-07-07
申请人： BRISTOL-MYERS SQUIBB COMPANY , STEIN, Philip, D. , BISAHA, Sharon, N. , AHMAD, Saleem , NGU, Khehyong , WASHBURN, William, N.
发明人： STEIN, Philip, D. , BISAHA, Sharon, N. , AHMAD, Saleem , NGU, Khehyong , WASHBURN, William, N.
IPC分类号： C07D241/18 , C07D401/12
摘要： The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I, wherein, R1, R2, R3, R8, and R9 are defined herein. 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-1 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.

6. 发明申请

WO2006086464A2 DIHYDROQUINAZOLINONES AS 5HT MODULATORS 审中-公开
标题翻译：作为5HT调制剂的二氢喹诺酮类
公开(公告)号：WO2006086464A2
公开(公告)日：2006-08-17
申请号：PCT/US2006/004417
申请日：2006-02-09
申请人： BRISTOL-MYERS SQUIBB COMPANY , AHMAD, Saleem , NGU, Khehyong
发明人： AHMAD, Saleem , NGU, Khehyong
IPC分类号： C07D487/04 , A61K31/495 , A61K31/55 , A61P3/04 , A61P3/10 , A61P25/22 , A61P25/24 , A61P25/06 , A61P25/18 , A61P25/20
CPC分类号： C07D487/04
摘要： The present application provides 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

WO2012149236A1 NOVEL BICYCLIC NITROGEN CONTAINING HETEROARYL TGR5 RECEPTOR MODULATORS 审中-公开
标题翻译：新型双相含氮异氰酸酯TGR5受体调节剂
公开(公告)号：WO2012149236A1
公开(公告)日：2012-11-01
申请号：PCT/US2012/035327
申请日：2012-04-27
申请人： BRISTOL-MYERS SQUIBB COMPANY , ROBL, Jeffrey A. , LI, Jun , KENNEDY, Lawrence J. , WALKER, Steven J. , WANG, Haixia , WASHBURN, William N. , AHMAD, Saleem , NGU, Khehyong
发明人： ROBL, Jeffrey A. , LI, Jun , KENNEDY, Lawrence J. , WALKER, Steven J. , WANG, Haixia , WASHBURN, William N. , AHMAD, Saleem , NGU, Khehyong
IPC分类号： C07D215/08 , C07D401/04 , C07D403/04 , C07D413/04 , C07D417/04 , A61K31/4709 , A61K31/553 , A61K31/554 , A61P3/00 , A61P9/00 , C07D401/14 , C07D413/14
CPC分类号： C07D401/04 , A61K31/47 , A61K31/4709 , A61K31/473 , A61K31/4747 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/5415 , A61K31/55 , A61K31/553 , A61K31/554 , A61K31/675 , A61K45/06 , C07D215/08 , C07D221/16 , C07D401/12 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07F9/60
摘要： Novel compounds of Formula I:or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, wherein m, Q, T, U, V, ring A, X, Y, R 3 , R 4 , R 4a , R 5a , R 5b , R 5c , R 5d , R 5e , R 6a , R 6b , and R 6c are defined herein, are provided which are TGR5 G protein-coupled receptor modulators. TGR5 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring TGR5 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the TGR5 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.
摘要翻译：式I的新型化合物或其对映体，非对映体，互变异构体，前药或其盐，其中m，Q，T，U，V，环A，X，Y，R 3，R 4，R 4a，R 5a，R 5b，R 5c，本文定义的R5e，R6a，R6b和R6c是TGR5G蛋白偶联受体调节剂。 TGR5G蛋白偶联受体调节剂可用于治疗，预防或减缓需要TGR5G蛋白偶联受体调节剂治疗的疾病进展。因此，本公开还涉及包含这些新化合物的组合物和通过使用任何这些新化合物或包含任何这些新化合物的组合物来治疗与TGR5G蛋白偶联受体的活性有关的疾病或病症的方法。

8. 发明申请

WO2010104830A1 PYRIDONE ANALOGS USEFUL AS MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS 审中-公开
标题翻译：吡咯烷酮类似物有效用于浓缩HORMONE受体-1拮抗剂的MELANIN
公开(公告)号：WO2010104830A1
公开(公告)日：2010-09-16
申请号：PCT/US2010/026626
申请日：2010-03-09
申请人： BRISTOL-MYERS SQUIBB COMPANY , AHMAD, Saleem , WASHBURN, William, N. , HERNANDEZ, Andres, S. , ROBL, Jeffrey, A. , NGU, Khehyong , WANG, Zhenghua
发明人： AHMAD, Saleem , WASHBURN, William, N. , HERNANDEZ, Andres, S. , ROBL, Jeffrey, A. , NGU, Khehyong , WANG, Zhenghua
IPC分类号： A61K31/4412 , A61P3/04 , C07D213/38 , C07D213/74 , C07D213/30 , C07D213/32 , C07D213/26 , C07D213/68 , C07D401/04 , A61K31/4409 , A61K31/4427
CPC分类号： C07D213/38 , A61K31/4412 , A61K31/4427 , C07D213/26 , C07D213/30 , C07D213/32 , C07D213/68 , C07D401/04
摘要： MCHR1 antagonists are provided having the following Formula I: wherein A 1 and A 2 are independently C or N; E is C or 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, lower cycloalkoxy, -CF 3 , -OCF 3 , -OR 12 and -SR 12 ; G is O or S; D 2 is lower alkyl, lower cycloalkyl, lower alkylcycloalkyl, lower cycloalkylalkyl, lower cycloalkoxyalkyl or lower alkycycloalkoxy; Z 1 and Z 2 are independently hydrogen, halogen, 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 provided that if Z 1 is -CH 3 and one of R 1 , R 2 , or R 3 is F, then Z 2 cannot be H;; R 5 , R 6 , and R 7 are independently selected from the group consisting of hydrogen, halogen, lower alkyl, lower cycloalkyl, -CF 3 , -SR 12 , lower alkoxy, lower cycloalkoxy, -OCH 2 OMe, -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; and 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. 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：其中A1和A2独立地为C或N; E为C或N; D1是键，-CR8R9X-，-XCR8R9-，-CHR8CHR9-，-CR10 = CR10'-，-C = C-或1,2-环丙基; X是O，S或-NR 11; R 1，R 2和R 3独立地选自氢，卤素，低级烷基，低级环烷基，低级环烷氧基，-CF 3，-OCF 3，-OR 12和-SR 12; G为O或S; 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; Z1和Z2独立地是氢，卤素，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，条件是如果Z 1是-CH 3并且R 1，R 2或R 3中的一个是F，则Z 2不能是H。 R5，R6和R7独立地选自氢，卤素，低级烷基，低级环烷基，-CF3，-SR12，低级烷氧基，低级环烷氧基，-OCH2OMe，-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; 并且R 14和R 14'独立地为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。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。

9. 发明申请

WO2007050723A1 THIENOPYRIMIDINONE DERIVATIVES AS MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS 审中-公开
标题翻译：作为MELANIN浓缩激素受体-1拮抗剂的三烯酰基嘧啶衍生物
公开(公告)号：WO2007050723A1
公开(公告)日：2007-05-03
申请号：PCT/US2006/041720
申请日：2006-10-26
申请人： BRISTOL-MYERS SQUIBB COMPANY , WASHBURN, William N. , AHMAD, Saleem , NGU, Khehyong
发明人： WASHBURN, William N. , AHMAD, Saleem , NGU, Khehyong
IPC分类号： C07D495/04 , A61K31/522 , A61P5/00 , A61P25/00
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-1 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).
摘要翻译：本申请提供根据式（I）的化合物，包括所有立体异构体，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，。

10. 发明申请

WO2005030758A1 PYRIMIDINE AND PYRIDINE DERIVATIVES USEFUL AS HMG-COA REDUCTASE INHIBITORS AND METHOD OF PREPARATION THEREOF 审中-公开
标题翻译：用作HMG-COA还原酶抑制剂的吡嗪和吡啶衍生物及其制备方法
公开(公告)号：WO2005030758A1
公开(公告)日：2005-04-07
申请号：PCT/US2004/031212
申请日：2004-09-22
申请人： BRISTOL-MYERS SQUIBB COMPANY , AHMAD, Saleem , ROBL, Jeffrey, A. , NGU, Khehyong
发明人： AHMAD, Saleem , ROBL, Jeffrey, A. , NGU, Khehyong
IPC分类号： C07D403/12
CPC分类号： C07D213/74 , C04B35/632 , C07D239/42 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12
摘要： Compounds are provided having the following structure which are HMG CoA reductase inhibitors and thus are active in inhibiting cholesterol biosynthesis, modulating blood serum lipids, for example, lowering LDL cholesterol and/or increasing HDL cholesterol, and treating hyperlipidemia, dyslipidemia, hormone replacement therapy, hypercholsterolemia, hypertriglyceridemia and atherosclerosis as well as Alzheimer's disease and osteoporosis identified in Formula (I) wherein X is N or CR 5 ; and pharmaceutically acceptable salts thereof, Z is identified in Formula (II) or in Formula (III) ; wherein R 1 to R 7 are as defined herein. A method for treating the above diseases employing the above compounds is also provided.
摘要翻译：提供具有以下结构的化合物，其为HMG CoA还原酶抑制剂，因此具有抑制胆固醇生物合成，调节血清脂质，例如降低LDL胆固醇和/或增加HDL胆固醇，以及治疗高脂血症，血脂异常，激素替代疗法，高胆固醇血症，高甘油三酯血症和动脉粥样硬化以及式（I）中鉴定的阿尔茨海默病和骨质疏松症，其中X是N或CR5; Z在式（II）或式（III）中鉴定; 其中R 1至R 7如本文所定义。还提供了使用上述化合物治疗上述疾病的方法。

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