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1. 发明申请

WO2010047956A1 AZOLOPYRROLONE MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS 审中-公开
标题翻译：阿莫洛林粉红素浓缩激素受体-1拮抗剂
公开(公告)号：WO2010047956A1
公开(公告)日：2010-04-29
申请号：PCT/US2009/059924
申请日：2009-10-08
申请人： BRISTOL-MYERS SQUIBB COMPANY , DEVASTHALE, Pratik , WASHBURN, William, N. , WANG, Wei , HERNANDEZ, Andres , AHMAD, Saleem , ZHAO, Guohua
发明人： DEVASTHALE, Pratik , WASHBURN, William, N. , WANG, Wei , HERNANDEZ, Andres , AHMAD, Saleem , ZHAO, Guohua
IPC分类号： C07D487/04 , A61K31/4015 , A61P3/00
CPC分类号： C07D487/04
摘要： The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula (I) including all pharmaceutically acceptable salts and stereoisomers thereof: wherein A is a monocyclic aryl or monocyclic heteroaryl; W is a direct bond, -0-, or -N(R 6 )-, provided that if W is a direct bond, D must be a cyclic amine that is attached to A via the nitrogen atom of said cyclic amine; D is a direct bond, substituted or unsubstituted C 1 to C 4 alkyl, substituted or unsubstituted C 3 to C 7 cycloalkyl, cycloalkylalkyl, or a 4 to 6 membered cyclic amine; B and E are independently N or CH provided that both are not CH;
摘要翻译：本申请提供了包括其所有药学上可接受的盐和立体异构体的根据式（I）的所有立体异构体，溶剂化物，前药和药学上可接受的形式的化合物：其中A是单环芳基或单环杂芳基; W是直接键，-O-或-N（R6） - ，条件是如果W是直接键，则D必须是通过所述环胺的氮原子连接到A的环胺; D是直接键，取代或未取代的C1至C4烷基，取代或未取代的C3至C7环烷基，环烷基烷基或4至6元环胺; B和E独立地为N或CH，条件是两者都不是CH;

2. 发明申请

WO2010042674A1 PYRROLONE MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS 审中-公开
标题翻译：吡咯酮梅兰宁浓缩HORMONE RECEPTOR-1 ANTAGONISTS
公开(公告)号：WO2010042674A1
公开(公告)日：2010-04-15
申请号：PCT/US2009/059918
申请日：2009-10-08
申请人： BRISTOL-MYERS SQUIBB COMPANY , ZHAO, Guohua , WASHBURN, William N. , MIGNONE, James
发明人： ZHAO, Guohua , WASHBURN, William N. , MIGNONE, James
IPC分类号： C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04 , A61K31/407 , A61P3/00
CPC分类号： C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04
摘要： The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R 1 , Formula Ia, R 4 , R 5 , Formula Ib, R 3 , R 3a , W, D, R 2a , R 2b and R 2c 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, anxiety or intestinal inflammation, by administration of a therapeutically effective dose of a compound according to Formula I.
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，其中R1，式Ia，R4，R5，式Ib，R3，R3a，W，D，R2a，R2b和R2c被定义于此。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化合物来治疗患有MCHR-1调节的疾病或病症例如肥胖症，糖尿病，抑郁症，焦虑或肠道炎症的患者的方法，一级方程式

3. 发明申请

WO2007092416A2 MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS 审中-公开
标题翻译： MELANIN合成激素受体-1拮抗剂
公开(公告)号：WO2007092416A2
公开(公告)日：2007-08-16
申请号：PCT/US2007/003099
申请日：2007-02-06
申请人： BRISTOL-MYERS SQUIBB COMPANY , ZHAO, Guohua
发明人： ZHAO, Guohua
CPC分类号： C07D487/04
摘要： The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula (I) wherein R 1a , R 1b , R 1c , Q, A, R 3 , W, D and R 2 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.
摘要翻译：本申请提供了根据式（I）的化合物，包括其所有的立体异构体，溶剂化物，前药和药学上可接受的形式，其中R 1，R 2， R 1，R 2，Q，A，R 3，W，D和R 2如本文所定义。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症，糖尿病，抑郁症或焦虑症的患者的方法。 / p>

4. 发明申请

WO2005035533A1 MODULATORS OF SEROTONIN RECEPTORS 审中-公开
标题翻译： SEROTONIN受体的调节剂
公开(公告)号：WO2005035533A1
公开(公告)日：2005-04-21
申请号：PCT/US2004/032849
申请日：2004-10-06
申请人： BRISTOL-MYERS SQUIBB COMPANY , WACKER, Dean A. , ZHAO, Guohua , KWON, Chet , VARNES, Jeffrey G. , STEIN, Philip D.
发明人： WACKER, Dean A. , ZHAO, Guohua , KWON, Chet , VARNES, Jeffrey G. , STEIN, Philip D.
IPC分类号： C07D487/04
CPC分类号： C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention 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：本发明提供5-羟色胺受体的调节剂，含有这样的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症，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，恐慌症，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。

5. 发明申请

WO2002042273A3 ACID DERIVATIVES USEFUL AS SERINE PROTEASE INHIBITORS 审中-公开
公开(公告)号：WO2002042273A3
公开(公告)日：2002-05-30
申请号：PCT/US2001/046884
申请日：2001-11-07
申请人： BRISTOL-MYERS SQUIBB COMPANY , BISACCHI, Gregory, S. , SUTTON, James, C., Jr. , SLUSARCHYK, William, A. , TREUNER, Uwe, D. , ZHAO, Guohua , CHENEY, Daniel, L. , WU, Shung, C. , SHI, Yan
发明人： BISACCHI, Gregory, S. , SUTTON, James, C., Jr. , SLUSARCHYK, William, A. , TREUNER, Uwe, D. , ZHAO, Guohua , CHENEY, Daniel, L. , WU, Shung, C. , SHI, Yan
IPC分类号： C07D401/12
摘要： Compounds having the formula (I), are useful as serine protease inhibitors, more particularly inhibitors of Factors VIIa, Ixa, Xa, and/or Xia, wherein ring B is phenyl or pyridyl, W is preferably C(=O)NR 4 R 5 , L is a linker group, X 2 comprises nitrogen or carbon, Z is an optionally-substituted monocyclic or bicyclic ring system, and R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are as defined in the specification.

6. 发明申请

WO2014039411A1 PYRROLONE OR PYRROLIDINONE MELANIN CONCENTRATING HORMORE RECEPTOR-1 ANTAGONISTS 审中-公开
标题翻译：吡咯酮或吡咯烷酮富含浓度的受体1拮抗剂
公开(公告)号：WO2014039411A1
公开(公告)日：2014-03-13
申请号：PCT/US2013/057766
申请日：2013-09-03
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： AHMAD, Saleem , ZHAO, Guohua , WASHBURN, William N.
IPC分类号： C07D403/12 , C07D401/12 , C07D409/12 , C07D207/27 , A61K31/402 , A61K31/4439 , A61P3/04 , A61P3/10 , A61P17/00 , A61P25/18 , A61P25/24
CPC分类号： C07D207/273 , C07D207/27 , C07D207/327 , C07D401/12 , C07D403/12 , C07D409/12
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。

7. 发明申请

WO2019094319A1 PYRROLOPYRAZINE DERIVATIVES AS ALPHA V INTEGRIN INHIBITORS 审中-公开
公开(公告)号：WO2019094319A1
公开(公告)日：2019-05-16
申请号：PCT/US2018/059157
申请日：2018-11-05
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： ZHAO, Guohua , MIGNONE, James
IPC分类号： C07D487/04 , A61P35/00 , A61K31/00
CPC分类号： C07D487/04 , A61P35/00
摘要： The disclosure relates to compounds of formula I: Formula I which inhibit α v-containing integrins, and includes pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with dysregulation of α V-containing integrins, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders.

8. 发明申请

WO2019089667A1 BRIDGED BICYCLIC COMPOUNDS AS FARNESOID X RECEPTOR MODULATORS 审中-公开
公开(公告)号：WO2019089667A1
公开(公告)日：2019-05-09
申请号：PCT/US2018/058315
申请日：2018-10-31
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： YOON, David S. , ANUMULA, Rushith Kumar , CHERUKU, Srinivas , HUANG, Yanting , JURICA, Elizabeth Anne , MENG, Wei , NARA, Susheel Jethanand , NARAYAN, Rishikesh , SISTLA, Ramesh Kumar , WU, Ximao , ZHAO, Guohua
IPC分类号： C07D413/14 , C07D413/04 , A61K31/422 , A61K31/4245 , A61K31/428 , A61K31/429 , C07D417/12 , C07D417/14 , C07D471/04 , C07D261/08
摘要： The present invention provides compounds of Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds modulate the activity of farnesoid X receptor (FXR), for example, as agonists. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.

9. 发明申请

WO2018089360A1 PYRROLE AMIDES AS ALPHA V INTEGRIN INHIBITORS 审中-公开
标题翻译：吡咯酰胺作为ALPHA V INTEGRIN抑制剂
公开(公告)号：WO2018089360A1
公开(公告)日：2018-05-17
申请号：PCT/US2017/060392
申请日：2017-11-07
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： ZHAO, Guohua , MIGNONE, James
IPC分类号： C07D471/04 , A61K31/4375 , A61P11/00
摘要： The present invention provides compounds of Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds are inhibitors to α v -containing integrins. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with dysregulation of αv-containing integrins, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
摘要翻译：本发明提供式（I）的化合物或其立体异构体，互变异构体或药学上可接受的盐或溶剂合物，其中所有变量如本文所定义。这些化合物是含有αvβ1整联蛋白的抑制剂。本发明还涉及包含这些化合物的药物组合物以及通过使用所述化合物治疗与包含αv的整联蛋白失调相关的疾病，病症或病症（例如病理性纤维化，移植排斥，癌症，骨质疏松症和炎性病症）的方法和药物组合物。

10. 发明申请

WO2018089353A1 3-SUBSTITUTED PROPIONIC ACIDS AS ALPHA V INTEGRIN INHIBITORS 审中-公开
标题翻译： 3-取代丙酸作为αV整合蛋白抑制剂
公开(公告)号：WO2018089353A1
公开(公告)日：2018-05-17
申请号：PCT/US2017/060376
申请日：2017-11-07
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： ZHAO, Guohua , DEVASTHALE, Pratik , YE, Xiang-Yang , SELVAKUMAR, Kumaravel , DHANUSU, Suresh , BALASUBRAMANIAN, Palanikumar , GUERNON, Leatte R. , CIVIELLO, Rita , HAN, Xiaojun , PARKER, Michael F. , JACUTIN-PORTE, Swanee E.
IPC分类号： C07D471/04 , C07D491/04 , A61K31/4375 , A61P11/00
摘要： The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds are antagonists to α ν - containing integrins. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with dysregulation of ay- containing integrins, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
摘要翻译：本发明提供式（I）的化合物：或其立体异构体，互变异构体或药学上可接受的盐或溶剂合物，其中所有变量如本文所定义。这些化合物是含有αvβ的整联蛋白的拮抗剂。本发明还涉及包含这些化合物的药物组合物以及通过使用所述化合物治疗与含有ay的整联蛋白失调相关的疾病，病症或病症（例如病理性纤维化，移植排斥，癌症，骨质疏松症和炎性病症）的方法和药物组合物。

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