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1. 发明申请

US20140315786A1 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：US20140315786A1
公开(公告)日：2014-10-23
申请号：US14006037
申请日：2012-03-16
申请人： Michael R. Jirousek , Jill C. Milne , David Carney , Jean E. Bemis , Chi B. Vu
发明人： Michael R. Jirousek , Jill C. Milne , David Carney , Jean E. Bemis , Chi B. Vu
IPC分类号： A61K47/48 , A61K31/194 , A61K31/198 , A61K31/618 , A61K31/202 , A61K31/455
CPC分类号： A61K31/194 , A61K31/198 , A61K31/202 , A61K31/455 , A61K31/60 , A61K31/618 , A61K45/06 , A61K47/542 , A61K47/55 , A61K47/65 , Y02A50/422 , 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。

2. 发明申请

US20130190327A1 BIS-FATTY ACID CONJUGATES AND THEIR USES 审中-公开
标题翻译： BIS脂肪酸结合物及其用途
公开(公告)号：US20130190327A1
公开(公告)日：2013-07-25
申请号：US13581392
申请日：2011-02-25
申请人： Jill C. Milne , Michael R. Jirousek , Jean E. Bemis , Chi B. Vu
发明人： Jill C. Milne , Michael R. Jirousek , Jean E. Bemis , Chi B. Vu
IPC分类号： C07C233/49 , C07D295/195 , C07D339/04
CPC分类号： C07C233/49 , A61K31/16 , A61K31/495 , C07C233/20 , C07C233/38 , C07D295/185 , C07D295/195 , C07D339/04
摘要： The invention relates to bis-fatty acid conjugates; compositions comprising an effective amount of a bis-fatty acid conjugate; and methods for treating or preventing cancer, a metabolic disease or a neurodegenerative disease comprising the administration of an effective amount of a bis-fatty acid conjugate.
摘要翻译：本发明涉及双脂肪酸共轭物; 包含有效量的双 - 脂肪酸缀合物的组合物; 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双脂肪酸缀合物。

3. 发明申请

US20130190309A1 PHTHALAZINONE AND RELATED ANALOGS AS SIRTUIN MODULATORS 审中-公开
标题翻译：苯达嗪和相关模拟物作为SIRTUIN调节剂
公开(公告)号：US20130190309A1
公开(公告)日：2013-07-25
申请号：US13139965
申请日：2009-12-16
申请人： Chi B. Vu
发明人： Chi B. Vu
IPC分类号： C07D401/12 , C07D417/12 , C07D405/12 , C07D403/12
CPC分类号： C07D401/12 , C07D403/12 , C07D405/12 , C07D417/12
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。

4. 发明申请

US20130065909A1 FATTY ACID FUMARATE DERIVATIVES AND THEIR USES 有权
公开(公告)号：US20130065909A1
公开(公告)日：2013-03-14
申请号：US13673588
申请日：2012-11-09
申请人： Jill C. Milne , Michael R. Jirousek , Jean E. Bemis , Chi B. Vu
发明人： Jill C. Milne , Michael R. Jirousek , Jean E. Bemis , Chi B. Vu
IPC分类号： C07C235/76 , A61K31/22 , C07D339/04 , A61K31/385 , C07D241/04 , A61K31/495 , C07D207/416 , A61K31/4015 , C07D295/185 , A61K31/194 , A61P29/00 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/28 , A61P9/00 , A61P3/10 , A61P3/06 , A61P13/12 , A61P27/02 , A61P9/06 , C07C323/41
CPC分类号： C07C235/76 , A61K31/195 , A61K31/197 , A61K31/221 , A61K31/225 , A61K31/385 , A61K31/4015 , A61K31/495 , A61K47/55 , C07C233/20 , C07C233/38 , C07C233/49 , C07C323/41 , C07D207/14 , C07D207/40 , C07D207/416 , C07D241/04 , C07D295/18 , C07D339/04
摘要： The invention relates to Fatty Acid Fumarate Derivatives; compositions comprising an effective amount of a Fatty Acid Fumarate Derivative; and methods for treating or preventing cancer, a metabolic disorder or neurodegenerative disorder comprising the administration of an effective amount of a Fatty Acid Fumarate Derivative.

5. 发明授权

US08304552B2 Fatty acid niacin conjugates and their uses 有权
公开(公告)号：US08304552B2
公开(公告)日：2012-11-06
申请号：US13427001
申请日：2012-03-22
申请人： Jill C. Milne , Michael R. Jirousek , Jean E. Bemis , Chi B. Vu
发明人： Jill C. Milne , Michael R. Jirousek , Jean E. Bemis , Chi B. Vu
IPC分类号： C07D211/72 , A61K31/44
CPC分类号： A61K47/542 , A61K31/202 , A61K31/44 , A61K31/4406 , A61K31/455 , A61K41/0038 , A61K47/55 , C07D213/80 , C07D213/82
摘要： The invention relates to fatty acid niacin conjugates; compositions comprising an effective amount of a fatty acid niacin conjugate; and methods for treating or preventing an metabolic disease comprising the administration of an effective amount of a fatty acid niacin conjugate.

6. 发明申请

US20120252850A1 NIACIN CONJUGATED FATTY ACID MIXTURES AND THEIR USES 有权
标题翻译： NIACIN联合脂肪酸混合物及其用途
公开(公告)号：US20120252850A1
公开(公告)日：2012-10-04
申请号：US13437643
申请日：2012-04-02
申请人： Jill C. Milne , Michael R. Jirousek , Jean E. Bemis , Chi B. Vu
发明人： Jill C. Milne , Michael R. Jirousek , Jean E. Bemis , Chi B. Vu
IPC分类号： A61K31/455 , A61P3/04 , A61P9/00 , A61P3/10 , C07D213/82 , A61P3/06
CPC分类号： A61K47/542 , A61K31/202 , A61K31/44 , A61K31/4406 , A61K31/455 , A61K41/0038 , A61K47/55 , C07D213/80 , C07D213/82
摘要： The invention relates to niacin conjugated fatty acid mixtures; compositions comprising an effective amount of a niacin conjugated fatty acid mixture; and methods for treating or preventing an metabolic disorder comprising the administration of an effective amount of a niacin conjugated fatty acid mixture.
摘要翻译：本发明涉及烟酸结合脂肪酸混合物; 包含有效量的烟酸结合脂肪酸混合物的组合物; 以及用于治疗或预防代谢紊乱的方法，包括施用有效量的烟酸结合脂肪酸混合物。

7. 发明申请

US20120184585A1 FATTY ACID NIACIN CONJUGATES AND THEIR USES 有权
标题翻译：脂肪酸的氮芥结合物及其用途
公开(公告)号：US20120184585A1
公开(公告)日：2012-07-19
申请号：US13427001
申请日：2012-03-22
申请人： Jill C. Milne , Michael R. Jirousek , Jean E. Bemis , Chi B. Vu
发明人： Jill C. Milne , Michael R. Jirousek , Jean E. Bemis , Chi B. Vu
IPC分类号： A61K31/4406 , A61P3/00 , A61P7/00 , A61P27/02 , A61P9/10 , A61P9/00 , A61P3/10 , A61P13/12 , C07D213/82 , A61P1/16
CPC分类号： A61K47/542 , A61K31/202 , A61K31/44 , A61K31/4406 , A61K31/455 , A61K41/0038 , A61K47/55 , C07D213/80 , C07D213/82
摘要： The invention relates to fatty acid niacin conjugates; compositions comprising an effective amount of a fatty acid niacin conjugate; and methods for treating or preventing an metabolic disease comprising the administration of an effective amount of a fatty acid niacin conjugate.
摘要翻译：本发明涉及脂肪酸烟酸缀合物; 包含有效量的脂肪酸烟酸缀合物的组合物; 以及用于治疗或预防代谢疾病的方法，包括施用有效量的脂肪酸烟酸缀合物。

8. 发明授权

US08178536B2 Sirtuin modulating compounds 有权
公开(公告)号：US08178536B2
公开(公告)日：2012-05-15
申请号：US12955663
申请日：2010-11-29
申请人： Joseph J. Nunes , Jill Milne , Jean Bemis , Roger Xie , Chi B. Vu , Pui Yee Ng , Jeremy S. Disch , Thomas Salzmann , David Armistead
发明人： Joseph J. Nunes , Jill Milne , Jean Bemis , Roger Xie , Chi B. Vu , Pui Yee Ng , Jeremy S. Disch , Thomas Salzmann , David Armistead
IPC分类号： A61K31/50 , C07D237/26
CPC分类号： C07D209/80 , C07C233/81 , C07C235/56 , C07C237/42 , C07D209/14 , C07D213/40 , C07D215/12 , C07D231/12 , C07D235/18 , C07D241/42 , C07D243/08 , C07D249/08 , C07D263/57 , C07D265/14 , C07D271/107 , C07D277/26 , C07D277/28 , C07D277/66 , C07D307/68 , C07D333/20 , C07D401/12 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/12 , C07D471/04 , C07D487/04 , C07D491/04 , 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.

9. 发明申请

US20110172240A1 FATTY ACID FUMARATE DERIVATIVES AND THEIR USES 审中-公开
标题翻译：脂肪酸的FUMARATE衍生物及其用途
公开(公告)号：US20110172240A1
公开(公告)日：2011-07-14
申请号：US12986713
申请日：2011-01-07
申请人： Jill C. Milne , Michael R. Jirousek , Jean E. Bemis , Chi B. Vu
发明人： Jill C. Milne , Michael R. Jirousek , Jean E. Bemis , Chi B. Vu
IPC分类号： A61K31/495 , C07C229/38 , C07D241/04 , C07D207/02 , C07D339/04 , A61K31/225 , A61K31/221 , A61K31/4015 , A61K31/385 , A61P25/28 , A61P37/00 , A61P25/16 , A61P25/00
CPC分类号： C07C235/76 , A61K31/195 , A61K31/197 , A61K31/221 , A61K31/225 , A61K31/385 , A61K31/4015 , A61K31/495 , A61K47/55 , C07C233/20 , C07C233/38 , C07C233/49 , C07C323/41 , C07D207/14 , C07D207/40 , C07D207/416 , C07D241/04 , C07D295/18 , C07D339/04
摘要： The invention relates to Fatty Acid Fumarate Derivatives; compositions comprising an effective amount of a Fatty Acid Fumarate Derivative; and methods for treating or preventing cancer, a metabolic disorder or neurodegenerative disorder comprising the administration of an effective amount of a Fatty Acid Fumarate Derivative.
摘要翻译：本发明涉及富马酸脂肪酸衍生物; 包含有效量的富马酸脂肪酸衍生物的组合物; 以及用于治疗或预防癌症，代谢紊乱或神经变性疾病的方法，包括施用有效量的富马酸脂肪酸衍生物。

10. 发明申请

US20110082156A1 FATTY ACID ACIPIMOX DERIVATIVES AND THEIR USES 审中-公开
标题翻译：脂肪酸ACIPIMOX衍生物及其用途
公开(公告)号：US20110082156A1
公开(公告)日：2011-04-07
申请号：US12898443
申请日：2010-10-05
申请人： Jill C. Milne , Michael R. Jirousek , Jean E. Bemis , Chi B. Vu
发明人： Jill C. Milne , Michael R. Jirousek , Jean E. Bemis , Chi B. Vu
IPC分类号： A61K31/4965 , C07D241/24 , A61P3/10 , A61P3/06 , A61P9/10
CPC分类号： A61K31/4965 , C07D241/24
摘要： The invention relates to fatty acid acipimox derivatives; compositions comprising an effective amount of a fatty acid acipimox derivative; and methods for treating or preventing an metabolic disease comprising the administration of an effective amount of a fatty acid acipimox derivative.
摘要翻译：本发明涉及脂肪酸acipimox衍生物; 包含有效量的脂肪酸丙酰氧基衍生物的组合物; 以及用于治疗或预防代谢疾病的方法，包括施用有效量的脂肪酸阿昔莫司衍生物。

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