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1. 发明申请

WO2007019344A1 IMIDAZO [2,1-B] THIAYOLE DERIVATIVES AS SIRTUIN MODULATING COMPOUNDS 审中-公开
标题翻译：咪唑并[2,1-B]噻吩衍生物作为SIRTUIN调节化合物
公开(公告)号：WO2007019344A1
公开(公告)日：2007-02-15
申请号：PCT/US2006030510
申请日：2006-08-04
申请人： SIRTRIS PHARMACEUTICALS INC , NUNES JOSEPH J , MILNE JILL , BEMIS JEAN , XIE ROGER , VU CHI B , NG PUI YEE , DISCH JEREMY S
发明人： NUNES JOSEPH J , MILNE JILL , BEMIS JEAN , XIE ROGER , VU CHI B , NG PUI YEE , DISCH JEREMY S
IPC分类号： C07D513/04 , A61K31/41 , A61P3/00 , A61P7/00 , A61P21/00 , A61P25/00 , A61P27/00 , A61P39/00
CPC分类号： C07D235/18 , C07D401/12 , C07D403/12 , C07D513/04
摘要： Provided herein are novel sirtuin-modulating compounds 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 benfit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
摘要翻译：本文提供了新的沉默调节蛋白的调节化合物及其使用方法。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/或预防多种疾病和病症，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，凝血障碍，炎症，癌症和/或潮红以及由线粒体活性增加所致的疾病或病症。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。

2. 发明申请

WO2008156869A3 SIRTUIN MODULATING THIAZOLOPYRIDINE COMPOUNDS 审中-公开
标题翻译： SIRTUIN调节噻唑吡啶化合物
公开(公告)号：WO2008156869A3
公开(公告)日：2009-05-14
申请号：PCT/US2008007776
申请日：2008-06-20
申请人： SIRTRIS PHARMACEUTICALS INC , BEMIS JEAN , DISCH JEREMY S , NG PUI YEE , OALMANN CHRISTOPHER , PERNI ROBERT B , VU CHI B
发明人： BEMIS JEAN , DISCH JEREMY S , NG PUI YEE , OALMANN CHRISTOPHER , PERNI ROBERT B , VU CHI B
IPC分类号： C07D513/04 , A61K31/437 , A61P3/10
CPC分类号： C07D513/04
摘要： Provided herein are novel sirtuin-modulating compounds 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：本文提供了新的沉默调节蛋白的调节化合物及其使用方法。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。还提供了包含沉默调节蛋白的调节性化合物与另一种治疗剂组合的组合物。

3. 发明申请

WO2008073451A8 BENZOIMIDAZOLE DERIVATIVES AS SIRTUIN (SIR) MODULATING COMPOUNDS 审中-公开
标题翻译：苯并咪唑衍生物作为SIRTUIN（SIR）调节化合物
公开(公告)号：WO2008073451A8
公开(公告)日：2008-12-11
申请号：PCT/US2007025391
申请日：2007-12-11
申请人： SIRTRIS PHARMACEUTICALS INC , BEMIS JEAN , VU CHI B , NUNES JOSEPH J , ARMISTEAD DAVID
发明人： BEMIS JEAN , VU CHI B , NUNES JOSEPH J , ARMISTEAD DAVID
IPC分类号： C07D417/14 , A61K31/429 , C07D417/04
CPC分类号： C07D513/04
摘要： A. Provided herein are novel sirtuin-modulating compounds of formula (I) 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 ( I ), wherein: one of R1 R2 R3 or R4 is selected from a 5- to 6-membered heteroaryl comprising 1 to 3 heteroatoms 'independently selected from N, O or S, wherein said heteroaryl is optionally benzofused or optionally fused to a second 5- to 6-membered heteroaryl comprising 1 to 3 heteroatoms independently selected from N, O or S and is bound to the rest of the compound via a carbon ring atom, wherein said heteroaryl is optionally substituted on a single carbon ring atom with a substituent selected from a solubilizing group, or a C1-C4 straight or branched alkyl.
摘要翻译： A.本文提供的是式（I）的新型沉默调节蛋白的调节性化合物及其使用方法。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（I）组合的沉默调节蛋白的调节性化合物的组合物，其中：R 1 R 2 R 3或R 4中的一个选自包含1至3个独立地选自N ，O或S，其中所述杂芳基任选地被苯并稠合或任选地与包含1至3个独立地选自N，O或S的杂原子的第二个5-至6-元杂芳基稠合，并且经由碳环与化合物的其余部分结合原子，其中所述杂芳基任选地在单个碳环原子上具有选自增溶基团或C 1 -C 4直链或支链烷基的取代基取代。

4. 发明申请

WO2008073451A3 BENZOIMDAZOLE DERIVATIVES AS SIRTUIN (SIR) MODULATING COMPOUNDS 审中-公开
标题翻译：苯并咪唑衍生物作为SIRTUIN（SIR）调节化合物
公开(公告)号：WO2008073451A3
公开(公告)日：2008-09-12
申请号：PCT/US2007025391
申请日：2007-12-11
申请人： SIRTRIS PHARMACEUTICALS INC , BEMIS JEAN , VU CHI B , NUNES JOSEPH J , ARMISTEAD DAVID
发明人： BEMIS JEAN , VU CHI B , NUNES JOSEPH J , ARMISTEAD DAVID
IPC分类号： C07D417/14 , A61K31/429 , C07D417/04
CPC分类号： C07D513/04
摘要： Provided herein are novel sirtuin-modulating compounds of formula (VI) 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 benfit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
摘要翻译：本文提供了式（VI）的新型沉默调节蛋白的调节性化合物及其使用方法。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，凝血障碍，炎症，癌症和/或潮红以及由线粒体活性增加所致的疾病或病症。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。

5. 发明申请

WO2009134973A1 QUENOLINES AND RELATED ANALOGS AS SIRTUIN MODULATORS 审中-公开
标题翻译：槲皮素和相关模拟物作为SIRTUIN调节剂
公开(公告)号：WO2009134973A1
公开(公告)日：2009-11-05
申请号：PCT/US2009042255
申请日：2009-04-30
申请人： SIRTRIS PHARMACEUTICALS INC , VU CHI B , DISCH JEREMY S , SPRINGER STEPHANIE K , BLUM CHARLES A , PERNI ROBERT B
发明人： VU CHI B , DISCH JEREMY S , SPRINGER STEPHANIE K , BLUM CHARLES A , PERNI ROBERT B
IPC分类号： A61K31/535
CPC分类号： C07D401/12 , C07D215/12 , C07D215/40 , C07D215/48 , C07D401/04 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D453/02 , C07D471/04
摘要： Provided herein are novel sirtuin-modulating compounds 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：本文提供了新的沉默调节蛋白的调节化合物及其使用方法。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。

6. 发明申请

WO2009061453A1 SOLUBILIZED THIAZOLOPYRIDINES 审中-公开
标题翻译：溶解的噻唑啉
公开(公告)号：WO2009061453A1
公开(公告)日：2009-05-14
申请号：PCT/US2008012548
申请日：2008-11-07
申请人： SIRTRIS PHARMACEUTICALS INC , VU CHI B , AOLMANN CHRISTOPHER , PERNI ROBERT B , DISCH JEREMY S , SZCZEPANKIEWICZ BRUCE , GUALTIERI GIOVANNA , CASAUBON REBECCA L
发明人： VU CHI B , AOLMANN CHRISTOPHER , PERNI ROBERT B , DISCH JEREMY S , SZCZEPANKIEWICZ BRUCE , GUALTIERI GIOVANNA , CASAUBON REBECCA L
IPC分类号： C07D513/04 , A61K31/437 , A61P3/00 , C07D519/00
CPC分类号： C07D513/04 , C07D519/00
摘要： Provided herein are novel sirtuin-modulating compounds Structural Formula (I): 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 benfit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
摘要翻译：本文提供了新的沉默调节蛋白的调节性化合物结构式（I）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，凝血障碍，炎症，癌症和/或潮红以及由线粒体活性增加所致的疾病或病症。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

WO2012129112A2 USE OF INTRACELLULAR ENZYMES FOR THE RELEASE OF COVALENTLY LINKED BIOACTIVES 审中-公开
标题翻译：用于释放共连接生物活性的细胞内酶的使用
公开(公告)号：WO2012129112A2
公开(公告)日：2012-09-27
申请号：PCT/US2012029504
申请日：2012-03-16
申请人： CATABASIS PHARMACEUTICALS INC , JIROUSEK MICHAEL R , MILNE JILL C , CARNEY DAVID , BEMIS JEAN E , VU CHI B
发明人： JIROUSEK MICHAEL R , MILNE JILL C , CARNEY DAVID , BEMIS JEAN E , VU CHI B
IPC分类号： A61K31/455
CPC分类号： A61K47/48338 , A61K31/194 , A61K31/198 , A61K31/202 , A61K31/455 , A61K31/60 , A61K31/618 , A61K45/06 , A61K47/542 , A61K47/55 , A61K47/65 , A61K2300/00
摘要： The present invention relates to targeting an intracellular enzyme for release of covalently linked bioactives which results in a synergistic effect between the bioactives. The present invention relates to the use of bioactives that are directly connected covalently or through a covalent molecular linker which have increased therapeutic activity when released as the free bioactives by intracellular enzymes as compared to when the bioactives are administered individually (i.e. not covalently linked). Further, methods are described of administering to patients in need thereof, bioactives as linked bioactives having increased therapeutic activity. Accordingly, this invention also relates to methods of treating patients for certain diseases.
摘要翻译：本发明涉及靶向细胞内酶以释放共价连接的生物活性物质，其导致生物活性物之间的协同作用。本发明涉及当与单独施用生物活性（即不共价连接）相比时，通过共价直接连接或通过共价分子接头直接连接的生物活性物质，其通过细胞内酶释放作为游离生物活性时具有增加的治疗活性。此外，描述了向有需要的患者施用作为具有增加的治疗活性的相关生物活性物的生物活性物质的方法。因此，本发明还涉及治疗患者某些疾病的方法。

8. 发明申请

WO2013033602A3 FATTY ACID AMIDES, COMPOSITIONS AND METHODS OF USE 审中-公开
标题翻译：脂肪酸，组合物和使用方法
公开(公告)号：WO2013033602A3
公开(公告)日：2014-05-08
申请号：PCT/US2012053452
申请日：2012-08-31
申请人： MILNE JILL C , JIROUSEK MICHAEL R , BEMIS JEAN E , VU CHI B , TING AMAL
发明人： MILNE JILL C , JIROUSEK MICHAEL R , BEMIS JEAN E , VU CHI B , TING AMAL
IPC分类号： C07C233/20 , A61K31/16 , A61K31/19 , A61K31/397 , A61K31/60 , A61K31/70 , A61P1/00 , A61P1/16 , A61P3/00 , A61P3/06 , A61P3/10 , A61P9/10 , A61P17/06 , A61P19/02 , A61P25/16 , A61P25/28 , A61P29/00 , A61P37/06 , C07C233/46 , C07H5/04
CPC分类号： C07C323/41 , A61K45/06 , C07C233/20 , C07H13/04
摘要： The invention relates to fatty acid amides; compositions comprising an effective amount of a fatty acid amide; and methods for treating or preventing cancer, a metabolic disease or a neurodegenerative disease comprising the administration of an effective amount of a fatty acid amide.
摘要翻译：本发明涉及脂肪酸酰胺; 包含有效量的脂肪酸酰胺的组合物; 以及用于治疗或预防癌症，代谢疾病或神经变性疾病的方法，其包括施用有效量的脂肪酸酰胺。

9. 发明申请

WO2013177536A3 METHODS OF LOWERING PROPROTEIN CONVERTASE SUBTILISIN/KEXIN TYPE 9 (PCSK9) 审中-公开
标题翻译：降低丙氨酸转化酶底物/ KEXIN 9型（PCSK9）的方法
公开(公告)号：WO2013177536A3
公开(公告)日：2014-03-13
申请号：PCT/US2013042693
申请日：2013-05-24
申请人： CATABASIS PHARMACEUTICALS INC , MILNE JILL C , JIROUSEK MICHAEL R , VU CHI B
发明人： MILNE JILL C , JIROUSEK MICHAEL R , VU CHI B
IPC分类号： A61K31/12
CPC分类号： C07D213/82 , A61K31/195 , A61K31/202 , A61K31/216 , A61K31/22 , A61K31/341 , A61K31/366 , A61K31/40 , A61K31/401 , A61K31/4025 , A61K31/403 , A61K31/404 , A61K31/4178 , A61K31/4184 , A61K31/4406 , A61K31/4418 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/455 , A61K31/496 , A61K31/4965 , A61K31/497 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K31/713 , A61K45/06 , C07C233/78 , C07C233/83 , C07C235/20 , C07C323/42 , C07D207/14 , C07D213/56 , C07D213/61 , C07D239/28 , C07D241/24 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/12 , A61K2300/00
摘要： The invention relates to new methods of modulating cholesterol by inhibiting proprotein convertase subtilisin/kexin type 9 (PCSK9) with fatty acid derivatives; and new methods for treating or preventing a metabolic disease comprising the administration of an effective amount of a fatty acid derivative. The present invention is also directed to fatty acid bioative derivatives and their use in the treatment of metabolic diseases.
摘要翻译：本发明涉及通过用脂肪酸衍生物抑制前体蛋白转化酶枯草杆菌蛋白酶/ 9型（PCSK9）来调节胆固醇的新方法。以及用于治疗或预防代谢疾病的新方法，包括施用有效量的脂肪酸衍生物。本发明还涉及脂肪酸生物衍生物及其在治疗代谢性疾病中的应用。

10. 发明申请

WO2013059587A1 SUBSTITUTED BICYCLIC AZA-HETEROCYCLES AND ANALOGUES AS SIRTUIN MODULATORS 审中-公开
标题翻译：作为SIRTUIN调节剂的取代的双环AZA-杂环化合物和类似物
公开(公告)号：WO2013059587A1
公开(公告)日：2013-04-25
申请号：PCT/US2012061015
申请日：2012-10-19
申请人： SIRTRIS PHARMACEUTICALS INC , CASAUBON REBECCA L , NARAYAN RADHA , OALMANN CHRISTOPHER , VU CHI B
发明人： CASAUBON REBECCA L , NARAYAN RADHA , OALMANN CHRISTOPHER , VU CHI B
IPC分类号： A61K31/535
CPC分类号： C07D487/04 , A61K31/5025 , A61K31/506 , A61K31/519 , A61K31/5377 , A61K45/06 , C07D491/107 , C07D495/10 , C07D519/00 , A61K2300/00 , A61K31/56
摘要： Provided herein are novel substituted bicyclic aza-heterocycle sirtuin- modulating compounds 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：本文提供了新型取代的双环氮杂 - 杂环调节蛋白的调节化合物及其使用方法。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。还提供了包含沉默调节蛋白的调节性化合物与另一种治疗剂组合的组合物。

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