专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2016081692A2 SUBSTITUTED BRIDGED UREA ANALOGS AS SIRTUIN MODULATORS 审中-公开
标题翻译：替代桥联尿素模拟物作为SIRTUIN调节剂
公开(公告)号：WO2016081692A2
公开(公告)日：2016-05-26
申请号：PCT/US2015/061501
申请日：2015-11-19
申请人： GLAXOSMITHKLINE LLC
发明人： BLUM, Charles, A. , CALDWELL, Richard Dana , CASAUBON, Rebecca , DISCH, Jeremy S. , FOX, Ryan, Michael , KOPPETSCH, Karsten , MILLER, William, Henry , NG, Pui, Yee , OALMANN, Christopher , PERNI, Robert, B. , SZCZEPANKIEWICZ, Bruce G. , WHITE, Brian H.
IPC分类号： C07D471/18 , A61K31/4995
CPC分类号： A61K45/06 , C07D471/18 , C07D513/18 , C07D519/00
摘要： The present invention relates to novel substituted bridged urea compounds, corresponding related analogs, pharmaceutical compositions and methods of use thereof. Sirtuin-modulating compounds of the present invention may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders, which include, but are not limited to, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. The present invention also related to compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
摘要翻译：本发明涉及新的取代桥联脲化合物，相应的相关类似物，药物组合物及其使用方法。本发明的沉默调节蛋白的调节性化合物可用于增加细胞的寿命，以及治疗和/或预防各种各样的疾病和病症，其包括但不限于例如与衰老或压力，糖尿病，肥胖症，神经变性疾病，心血管疾病，凝血障碍，炎症，癌症和/或潮红以及可能从线粒体活性增加中受益的疾病或病症。本发明还涉及包含与另一种治疗剂组合的沉默调节蛋白的调节化合物的组合物。

2. 发明申请

WO2015200324A1 PHARMACEUTICAL COMPOSITIONS 审中-公开
标题翻译：药物组合物
公开(公告)号：WO2015200324A1
公开(公告)日：2015-12-30
申请号：PCT/US2015/037183
申请日：2015-06-23
申请人： GLAXOSMITHKLINE LLC
发明人： CHANG, Liuquan , DOUCET, Dany , NESTA, Douglas, P.
IPC分类号： A61K38/26 , A61K38/00 , A61K38/16 , C07K14/00
CPC分类号： A61K38/26 , A61K9/0019 , A61K9/08 , A61K47/12 , A61K47/183 , A61K47/22 , A61K47/26 , C07K14/605 , C07K14/76 , C07K19/00 , C07K2319/00
摘要： The present invention provides liquid compositions comprising albiglutide or a variant thereof, a buffering agent, at least one saccharide and/or at least one polyol, at least one stabilizing agent and optionally a surfactant wherein said albiglutide remains stable in said liquid composition. Albiglutide or a variant thereof can be considered to remain stable in liquid if at least about ≥96% of said albiglutide or a variant thereof remains as a monomer in the liquid composition over a period of at least one week.
摘要翻译：本发明提供了包含阿奇格肽或其变体，缓冲剂，至少一种糖和/或至少一种多元醇，至少一种稳定剂和任选的表面活性剂的液体组合物，其中所述白化素在所述液体组合物中保持稳定。如果在至少一周的时间内，如果至少约百分之九十六的所述白化或其变体在液体组合物中作为单体保留，则阿奇格列或其变体可以被认为在液体中保持稳定。

3. 发明申请

WO2015089260A3 METERED DOSE CONTAINER 审中-公开
标题翻译：计量剂量容器
公开(公告)号：WO2015089260A3
公开(公告)日：2015-11-12
申请号：PCT/US2014069685
申请日：2014-12-11
申请人： GLAXOSMITHKLINE LLC
发明人： SABHARWAL AMIT , SAINI SUKHDEV SINGH
IPC分类号： G01F11/12
CPC分类号： A61J7/0076 , A61J1/00 , G01F11/34
摘要： Aspects of the present invention are directed to a metered dose container. The container may comprise a body; a first barrier in contact with a base of the container and extending partially along the vertical axis of the body; a second barrier in contact with a top of the container and extending partially along with vertical axis of the body. The space between the first barrier and the second barrier defines a loading chamber, the space between the second barrier and a front wall of the container defines a dispensing chamber, and the space between a rear wall of the container and the first barrier defines a storage chamber. The base also comprises a depressible portion that can convert the container from a transit mode to a dispensing mode.
摘要翻译：本发明的各方面涉及计量剂量容器。该容器可以包括一个主体; 与容器的基部接触并且部分地沿着主体的竖直轴线延伸的第一屏障; 与容器的顶部接触并且部分地沿着主体的竖直轴线延伸的第二屏障。第一屏障和第二屏障之间的空间限定加载室，第二屏障和容器前壁之间的空间限定分配室，并且容器的后壁和第一屏障之间的空间限定存储器室。基座还包括可按压部分，其可将容器从运输模式转换为分配模式。

4. 发明申请

WO2013177253A3 FATTY ACID SYNTHASE INHIBITORS 审中-公开
标题翻译：脂肪酸合成酶抑制剂
公开(公告)号：WO2013177253A3
公开(公告)日：2015-06-18
申请号：PCT/US2013042173
申请日：2013-05-22
申请人： GLAXOSMITHKLINE LLC
发明人： ADAMS NICHOLAS DAVID , KIESOW TERENCE JOHN , WIGGALL KENNETH
IPC分类号： A61K31/5386 , C07D265/28
CPC分类号： A61K45/06 , C07D498/10
摘要： Disclosed are compounds having Formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, Y, m, and n are defined herein and methods of using the same.
摘要翻译：公开了具有式（I）的化合物，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9，Y，m和n如本文所定义，以及使用该化合物的方法。

5. 发明申请

WO2014066606A8 COMBINATION 审中-公开
标题翻译：组合
公开(公告)号：WO2014066606A8
公开(公告)日：2015-06-04
申请号：PCT/US2013066564
申请日：2013-10-24
申请人： GLAXOSMITHKLINE LLC
发明人： HOOS AXEL , GRESHOCK JOEL
IPC分类号： A61K31/519
CPC分类号： A61K39/3955 , A61K31/506 , A61K31/517 , A61K31/519 , A61K45/06 , A61K2300/00
摘要： A novel combination comprising a B-Raf inhibitor, particularly N-{3-[5-(2-Amino- 4-pyrimidinyl)-2-(l, 1 -dimethylethyl)- 1,3-thiazol-4-yl]-2-fluorophenyl} -2,6- difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, and/or the MEK inhibitor N- {3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)6,8-dimethyl;-2,4,7- trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-l-yl]phenyl}acetamide, or a pharmaceutically acceptable salt or solvate thereof, and an EGFR inhibitor suitably cetuximab (Erbitux) or erlotinib; pharmaceutical compositions comprising the same and methods of using such combinations and compositions in the treatment of conditions in which the inhibition of MEK and/or B-Raf and/or EGFR is beneficial, eg. cancer.
摘要翻译：包含B-Raf抑制剂，特别是N- {3- [5-（2-氨基-4-嘧啶基）-2-（1,1-二甲基乙基）-1,3-噻唑-4-基] - 2-氟苯基} -2,6-二氟苯磺酰胺或其药学上可接受的盐，和/或MEK抑制剂N- {3- [3-环丙基-5-（2-氟-4-碘 - 苯基氨基） -2,4,7-三氧代-3,4,6,7-四氢-2H-吡啶并[4,3-d]嘧啶-1-基]苯基}乙酰胺或其药学上可接受的盐或溶剂化物，和EGFR抑制剂适当地西妥昔单抗（Erbitux）或厄洛替尼; 包含其的药物组合物和使用这些组合和组合物治疗MEK和/或B-Raf和/或EGFR的抑制作用有利的条件的方法，例如，癌症。

6. 发明申请

WO2014186313A1 SUBSTITUTED BRIDGED UREA ANALOGS AS SIRTUIN MODULATORS 审中-公开
标题翻译：作为SIRTUIN调制器的替代桥联尿素模拟物
公开(公告)号：WO2014186313A1
公开(公告)日：2014-11-20
申请号：PCT/US2014/037767
申请日：2014-05-13
申请人： GLAXOSMITHKLINE LLC
发明人： BLUM, Charles, A. , OALMANN, Christopher , SZCZEPANKIEWICZ, Bruce, G. , CALDWELL, Richard, Dana , CASAUBON, Rebecca , WHITE, Brian, H. , PERNI, Robert, B. , KOPPETSCH, Karsten , DISCH, Jeremy, S. , NG, Pui, Yee , FOX, Ryan, Michael
IPC分类号： C07D471/04
CPC分类号： C07D471/18 , A61K31/4995 , A61K31/506 , A61K31/551 , A61K45/06 , A61P17/10 , C07D487/04 , C07D513/18 , C07D519/00
摘要： Provided herein are novel substituted bridged urea and related analogs and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
摘要翻译：本文提供了新的取代的桥连脲和相关的类似物及其使用方法。沉默调节蛋白的调节化合物可用于增加细胞的寿命，以及治疗和/或预防各种各样的疾病和病症，包括例如与老化或紧张相关的疾病或病症，糖尿病，肥胖症，神经变性疾病，心血管疾病，血液凝固障碍，炎症，癌症和/或潮红以及将受益于增加的线粒体活性的疾病或病症。还提供了包含与另一种治疗剂组合的沉默调节蛋白的调节化合物的组合物。

7. 发明申请

WO2014074761A3 NOVEL COMPOUNDS AS DIACYLGLYCEROL ACYLTRANSFERASE INHIBITORS 审中-公开
标题翻译：新型化合物作为二乙酰胆碱酯酶抑制剂
公开(公告)号：WO2014074761A3
公开(公告)日：2014-10-23
申请号：PCT/US2013069024
申请日：2013-11-08
申请人： GLAXOSMITHKLINE LLC
发明人： CHEUNG MUI , TANGIRALA RAGHURAM S
IPC分类号： A61K31/501
CPC分类号： C07D213/72 , A61K31/122 , A61K31/50 , C07D213/74 , C07D237/20 , C07D277/42 , C07D401/12 , C07D405/12 , C07D417/12
摘要： This invention relates to novel compounds which are inhibitors of acyl coenzyme A: diacylglycerol acyl transferase 1 (DGAT-1), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination with other triglyceride lowering therapies for the prevention or treatment of diseases related to DGAT-1 dysfunction or where modulation of DGAT-1 activity may have therapeutic benefit including but not limited to obesity, obesity related disorders, genetic (Type 1, Type 5 hyperlipidemia) and acquired forms of hypertriglyceridemia or hyperlipoproteinemia related disorders, caused by but not limited to lipodystrophy, hypothyroidism, medications (beta blockers, thiazides, estrogen, glucocorticoids, transplant) and other factors (pregnancy, alcohol intake), hyperlipoproteinemia, chylomicronemia, dyslipidemia, non-alcoholic steatohepatitis, diabetes, insulin resistance, metabolic syndrome, cardiovascular outcomes, angina, excess hair growth (including syndromes associated with hirsutism), nephrotic syndrome, fibrosis such as mycocardial, renal and liver fibrosis, hepatitis C virus infection and acne or other skin disorders.
摘要翻译：本发明涉及作为酰基辅酶A：二酰基甘油酰基转移酶1（DGAT-1）的抑制剂的新化合物，含有它们的药物组合物，其制备方法及其在治疗中的用途，单独或与其它甘油三酯组合降低用于预防或治疗与DGAT-1功能障碍有关的疾病或DGAT-1活性调节可能具有治疗益处的疗法，包括但不限于肥胖症，肥胖相关疾病，遗传（1型，5型高脂血症）和获得性形式高甘油三酯血症或高脂蛋白血症相关疾病，由但不限于脂肪营养不良，甲状腺功能减退，药物（β受体阻滞剂，噻嗪类，雌激素，糖皮质激素，移植物）等因素（怀孕，酒精摄入），高脂蛋白血症，乳糜微粒血症，血脂异常，非酒精性脂肪性肝炎，糖尿病，胰岛素抵抗，代谢综合征，心血管结局，心绞痛，过量的h 空气生长（包括与多毛症相关的综合征），肾病综合征，纤维化如心肌炎，肾和肝纤维化，丙型肝炎病毒感染和痤疮或其他皮肤病。

8. 发明申请

WO2014138562A1 THIENO[3,2-D]PYRIMIDINE-6-CARBOXAMIDES AND ANALOGUES AS SIRTUIN MODULATORS 审中-公开
标题翻译：噻吩并[3,2-D]嘧啶-6-羧酸和类似物作为SIRTUIN调节剂
公开(公告)号：WO2014138562A1
公开(公告)日：2014-09-12
申请号：PCT/US2014/021683
申请日：2014-03-07
申请人： GLAXOSMITHKLINE LLC
发明人： BLUM, Charles, A. , DISCH, Jeremy, S. , EVINDAR, Ghotas , PERNI, Robert, B.
IPC分类号： C07D495/04
CPC分类号： C07F9/65616 , C07D491/048 , C07D495/04 , C07D519/00 , C12Q1/34
摘要： Provided herein are novel substituted thieno[3,2- d ]pyrimidine-6-carboxamide sirtuin inhibitors and methods of use thereof. The sirtuin inhibitors may be used for inhibiting a sirtuin-mediated biological process, and, e.g. for treating and/or preventing diseases and disorders including, but not limited to cancer, neurodegenerative disease and inflammation. Also provided herein are pharmaceutical compositions comprising these sirtuin inhibitors and compositions comprising a sirtuin inhibitor in combination with another therapeutic agent.
摘要翻译：本文提供新的取代的噻吩并[3,2-d]嘧啶-6-甲酰胺沉默调节蛋白抑制剂及其使用方法。沉默调节蛋白抑制剂可用于抑制沉默调节蛋白的介导的生物学过程，用于治疗和/或预防疾病和病症，包括但不限于癌症，神经变性疾病和炎症。本文还提供了包含这些沉默调节蛋白抑制剂和包含沉默调节蛋白抑制剂与另一种治疗剂组合的组合物的药物组合物。

9. 发明申请

WO2014066606A3 COMBINATION 审中-公开
标题翻译：组合
公开(公告)号：WO2014066606A3
公开(公告)日：2014-07-10
申请号：PCT/US2013066564
申请日：2013-10-24
申请人： GLAXOSMITHKLINE LLC
发明人： HOOS AXEL , GRESHOCK JOEL
IPC分类号： A61K31/519
CPC分类号： A61K39/3955 , A61K31/506 , A61K31/517 , A61K31/519 , A61K45/06 , A61K2300/00
摘要： A novel combination comprising a B-Raf inhibitor, particularly N-{3-[5-(2-Amino- 4-pyrimidinyl)-2-(l, 1 -dimethylethyl)- 1,3-thiazol-4-yl]-2-fluorophenyl} -2,6- difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, and/or the MEK inhibitor N- {3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)6,8-dimethyl;-2,4,7- trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-l-yl]phenyl}acetamide, or a pharmaceutically acceptable salt or solvate thereof, and an EGFR inhibitor suitably cetuximab (Erbitux) or erlotinib; pharmaceutical compositions comprising the same and methods of using such combinations and compositions in the treatment of conditions in which the inhibition of MEK and/or B-Raf and/or EGFR is beneficial, eg. cancer.
摘要翻译：包含B-Raf抑制剂，特别是N- {3- [5-（2-氨基-4-嘧啶基）-2-（1,1-二甲基乙基）-1,3-噻唑-4-基] - 2-氟苯基} -2,6-二氟苯磺酰胺或其药学上可接受的盐和/或MEK抑制剂N- {3- [3-环丙基-5-（2-氟-4-碘 - 苯基氨基） -2,4,7-三氧代-3,4,6,7-四氢-2H-吡啶并[4,3-d]嘧啶-1-基]苯基}乙酰胺或其药学上可接受的盐或溶剂合物，和适宜的西妥昔单抗（爱必妥）或厄洛替尼的EGFR抑制剂; 包含该组合物的药物组合物以及使用这些组合和组合物治疗其中抑制MEK和/或B-Raf和/或EGFR是有益的病症的方法，癌症。

10. 发明申请

WO2014081996A1 NOVEL COMPOUNDS AS DIACYLGLYCEROL ACYLTRANSFERASE INHIBITORS 审中-公开
标题翻译：新型化合物作为二乙酰胆碱酯酶抑制剂
公开(公告)号：WO2014081996A1
公开(公告)日：2014-05-30
申请号：PCT/US2013/071380
申请日：2013-11-22
申请人： GLAXOSMITHKLINE LLC
发明人： CHEUNG, Mui , TANGIRALA, Raghuram, S.
IPC分类号： A61K31/519
CPC分类号： A61K31/519
摘要： This invention relates to novel compounds which are inhibitors of acyl coenzyme A: diacylglycerol acyltransferase 1 (DGAT-1 ), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination with weight management therapies or other triglyceride lowering therapy for the prevention or treatment of diseases related to DGAT-1 dysfunction or where modulation of DGA T-1 activity may have therapeutic benefit.
摘要翻译：本发明涉及作为酰基辅酶A：二酰基甘油酰基转移酶1（DGAT-1）的抑制剂的新化合物，含有它们的药物组合物，其制备方法及其在治疗中的用途，单独使用或与体重管理疗法组合或其他甘油三酸酯降低治疗用于预防或治疗与DGAT-1功能障碍相关的疾病或其中DGA T-1活性的调节可具有治疗益处。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式