公开(公告)号：US08178536B2

公开(公告)日：2012-05-15

申请号：US12955663

申请日：2010-11-29

Applicant: Joseph J. Nunes ,  Jill Milne ,  Jean Bemis ,  Roger Xie ,  Chi B. Vu ,  Pui Yee Ng ,  Jeremy S. Disch ,  Thomas Salzmann ,  David Armistead

Inventor： Joseph J. Nunes ,  Jill Milne ,  Jean Bemis ,  Roger Xie ,  Chi B. Vu ,  Pui Yee Ng ,  Jeremy S. Disch ,  Thomas Salzmann ,  David Armistead

IPC: A61K31/50 ,  C07D237/26

CPC classification number: 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

Abstract: 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.

公开(公告)号：US20060211864A1

公开(公告)日：2006-09-21

申请号：US11364506

申请日：2006-02-28

Applicant: Brian Aquila ,  Thomas Bannister ,  Gregory Cuny ,  James Hauske ,  Michele Heffernan ,  Michael Hoemann ,  Donald Kessler ,  Liming Shao ,  Xinhe Wu ,  Roger Xie

Inventor： Brian Aquila ,  Thomas Bannister ,  Gregory Cuny ,  James Hauske ,  Michele Heffernan ,  Michael Hoemann ,  Donald Kessler ,  Liming Shao ,  Xinhe Wu ,  Roger Xie

IPC: C07D211/06 ,  C07D211/60 ,  C07D211/26 ,  C07D211/28

CPC classification number: C07D211/22 ,  C07D211/26

Abstract: One aspect of the present invention relates to methods of synthesizing substituted piperidines. A second aspect of the present invention relates to stereoselective methods of synthesizing substituted piperidines. The methods of the present invention will find use in the synthesis of compounds useful for treatment of numerous ailments, conditions and diseases that afflict mammals, including but not limited to addiction and pain. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the substituted piperidines using the methods of the present invention. An additional aspect of the present invention relates to enantiomerically substituted pyrrolidines, piperidines, and azepines.

公开(公告)号：US08044198B2

公开(公告)日：2011-10-25

申请号：US12070350

申请日：2008-02-15

Applicant: Joseph J. Nunes ,  Jill Milne ,  Jean Bemis ,  Roger Xie ,  Chi B. Vu ,  Pui Yee Ng ,  Jeremy S. Disch

Inventor： Joseph J. Nunes ,  Jill Milne ,  Jean Bemis ,  Roger Xie ,  Chi B. Vu ,  Pui Yee Ng ,  Jeremy S. Disch

IPC: C07D237/26 ,  A61K31/50

CPC classification number: C07D235/18 ,  C07D401/12 ,  C07D403/12 ,  C07D513/04

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20090143351A1

公开(公告)日：2009-06-04

申请号：US12359490

申请日：2009-01-26

Applicant: Thomas Bannister ,  Cassandra Celatka ,  Nizal S. Chandrakumar ,  Hongfeng Deng ,  Zihong Guo ,  Lei Jin ,  Tsvetelina Lazarova ,  Jian Lin ,  Scott T. Moe ,  Pamela Nagafuji ,  Manuel Navia ,  Amy Ripka ,  Michael J. Rynkiewicz ,  Kerry L. Spear ,  James E. Stickler ,  Roger Xie

Inventor： Thomas Bannister ,  Cassandra Celatka ,  Nizal S. Chandrakumar ,  Hongfeng Deng ,  Zihong Guo ,  Lei Jin ,  Tsvetelina Lazarova ,  Jian Lin ,  Scott T. Moe ,  Pamela Nagafuji ,  Manuel Navia ,  Amy Ripka ,  Michael J. Rynkiewicz ,  Kerry L. Spear ,  James E. Stickler ,  Roger Xie

IPC: A61K31/397 ,  C07D401/06 ,  C07D205/08 ,  A61P7/00 ,  C07D401/04 ,  A61K31/4427

CPC classification number: C07D405/06 ,  C07D205/08 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/14

Abstract: Compounds are provided which have the structure Wherein A, B, C, D, m, Y, Ra, Rc, Rd, and Rd′ are as described herein, and which are useful as inhibitors of tryptase, thrombin, trypsin, Factor Xa, Factor VIIa, Factor XIa, and urokinase-type plasminogen activator and may be employed in preventing and/or treating asthma, chronic asthma, allergic rhinitis, and thrombotic disorders.

Abstract translation: 提供具有其中A，B，C，D，m，Y，Ra，Rc，Rd和Rd'如本文所述的结构的化合物，其可用作类胰蛋白酶，凝血酶，胰蛋白酶，因子Xa， 因子VIIa，因子XIa和尿激酶型纤溶酶原激活剂，可用于预防和/或治疗哮喘，慢性哮喘，过敏性鼻炎和血栓形成障碍。

公开(公告)号：US20090099170A1

公开(公告)日：2009-04-16

申请号：US12070350

申请日：2008-02-15

Applicant: Joseph J. Nunes ,  Jill Milne ,  Jean Bemis ,  Roger Xie ,  Chi B. Vu ,  Pui Yee Ng ,  Jeremy S. Disch

Inventor： Joseph J. Nunes ,  Jill Milne ,  Jean Bemis ,  Roger Xie ,  Chi B. Vu ,  Pui Yee Ng ,  Jeremy S. Disch

IPC: A61K31/5377 ,  C07D471/04 ,  C07D401/10 ,  C07D413/14 ,  A61K31/437 ,  A61K31/497 ,  A61P3/00

CPC classification number: C07D235/18 ,  C07D401/12 ,  C07D403/12 ,  C07D513/04

Abstract: 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.

公开(公告)号：US20120197013A1

公开(公告)日：2012-08-02

申请号：US13442630

申请日：2012-04-09

Applicant: Joseph J. Nunes ,  Jill Milne ,  Jean Bemis ,  Roger Xie ,  Chi B. Vu ,  Pui Yee Ng ,  Jeremy S. Disch

Inventor： Joseph J. Nunes ,  Jill Milne ,  Jean Bemis ,  Roger Xie ,  Chi B. Vu ,  Pui Yee Ng ,  Jeremy S. Disch

IPC: C07D513/04 ,  C07F5/02

CPC classification number: C07D235/18 ,  C07D401/12 ,  C07D403/12 ,  C07D513/04

Abstract: 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.

公开(公告)号：US08093401B2

公开(公告)日：2012-01-10

申请号：US11499239

申请日：2006-08-04

Applicant: Joseph J. Nunes ,  Jill Milne ,  Jean Bemis ,  Roger Xie ,  Chi B. Vu ,  Pui Yee Ng ,  Jeremy S. Disch

Inventor： Joseph J. Nunes ,  Jill Milne ,  Jean Bemis ,  Roger Xie ,  Chi B. Vu ,  Pui Yee Ng ,  Jeremy S. Disch

IPC: C07D235/04 ,  A61K31/415

CPC classification number: C07D471/04

Abstract: 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.

公开(公告)号：US20100144698A1

公开(公告)日：2010-06-10

申请号：US12703610

申请日：2010-02-10

Applicant: Thomas Bannister ,  Cassandra Celatka ,  Nizal S. Chandrakumar ,  Hongfeng Deng ,  Zihong Guo ,  Lei Jin ,  Tsveltelina Lazarova ,  Jian Lin ,  Scott T. Moe ,  Pamela Nagafuji ,  Manuel Navia ,  Amy Ripka ,  Michael J. Rynkiewicz ,  Kerry L. Spear ,  James E. Stickler ,  Roger Xie

Inventor： Thomas Bannister ,  Cassandra Celatka ,  Nizal S. Chandrakumar ,  Hongfeng Deng ,  Zihong Guo ,  Lei Jin ,  Tsveltelina Lazarova ,  Jian Lin ,  Scott T. Moe ,  Pamela Nagafuji ,  Manuel Navia ,  Amy Ripka ,  Michael J. Rynkiewicz ,  Kerry L. Spear ,  James E. Stickler ,  Roger Xie

IPC: A61K31/397 ,  C07D205/04 ,  A61P9/00 ,  A61P7/00

CPC classification number: C07D405/06 ,  C07D205/08 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/14

Abstract: Compounds are provided which have the structure Wherein A, B, C, D, m, Y, Ra, Rc, Rd, and Rd′ are as described herein, and which are useful as inhibitors of tryptase, thrombin, trypsin, Factor Xa, Factor VIIa, Factor XIa, and urokinase-type plasminogen activator and may be employed in preventing and/or treating asthma, chronic asthma, allergic rhinitis, and thrombotic disorders.

Abstract translation: 提供具有其中A，B，C，D，m，Y，Ra，Rc，Rd和Rd'如本文所述的结构的化合物，其可用作类胰蛋白酶，凝血酶，胰蛋白酶，因子Xa， 因子VIIa，因子XIa和尿激酶型纤溶酶原激活剂，可用于预防和/或治疗哮喘，慢性哮喘，过敏性鼻炎和血栓形成障碍。

公开(公告)号：US20090163476A1

公开(公告)日：2009-06-25

申请号：US11885577

申请日：2006-03-03

Applicant: Michael Milburn ,  Jill Milne ,  Jean Bemis ,  Joseph J. Nunes ,  Roger Xie ,  Karl D. Normington ,  Chi B. Vu

Inventor： Michael Milburn ,  Jill Milne ,  Jean Bemis ,  Joseph J. Nunes ,  Roger Xie ,  Karl D. Normington ,  Chi B. Vu

IPC: A61K31/551 ,  C12N5/02 ,  C07C69/34 ,  A61K31/225 ,  C07C229/00 ,  A61K31/195 ,  C07D243/08

CPC classification number: C07D277/66 ,  C07D235/18 ,  C07D241/42 ,  C07D263/57 ,  C07D265/22 ,  C07D471/04 ,  C07D513/04

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US07501404B2

公开(公告)日：2009-03-10

申请号：US11398438

申请日：2006-04-04

Applicant: Thomas Bannister ,  Cassandra Celatka ,  Nizal S. Chandrakumar ,  Hongfeng Deng ,  Zihong Guo ,  Lei Jin ,  Tsvetelina Lazarova ,  Jian Lin ,  Scott T. Moe ,  Pamela Nagafuji ,  Manuel Navia ,  Amy Ripka ,  Michael J. Rynkiewicz ,  Kerry L. Spear ,  James E. Stickler ,  Roger Xie

Inventor： Thomas Bannister ,  Cassandra Celatka ,  Nizal S. Chandrakumar ,  Hongfeng Deng ,  Zihong Guo ,  Lei Jin ,  Tsvetelina Lazarova ,  Jian Lin ,  Scott T. Moe ,  Pamela Nagafuji ,  Manuel Navia ,  Amy Ripka ,  Michael J. Rynkiewicz ,  Kerry L. Spear ,  James E. Stickler ,  Roger Xie

IPC: C07D205/08 ,  C07D205/085 ,  C07D401/14 ,  C07D401/12 ,  C07D401/06 ,  C07D403/12 ,  C07D403/14 ,  C07D403/04 ,  A61K31/397 ,  A61K31/506 ,  A61K31/4427 ,  A61K31/41

CPC classification number: C07D405/06 ,  C07D205/08 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/14

Abstract: Compounds are provided which have the structure Wherein A, B, C, D, m, Y, Ra, Rc, Rd, and Rd′ are as described herein, and which are useful as inhibitors of tryptase, thrombin, trypsin, Factor Xa, Factor VIIa, Factor XIa, and urokinase-type plasminogen activator and may be employed in preventing and/or treating asthma, chronic asthma, allergic rhinitis, and thrombotic disorders.

Abstract translation: 提供具有其中A，B，C，D，m，Y，Ra，Rc，Rd和Rd'如本文所述的结构的化合物，其可用作类胰蛋白酶，凝血酶，胰蛋白酶，因子Xa， 因子VIIa，因子XIa和尿激酶型纤溶酶原激活剂，可用于预防和/或治疗哮喘，慢性哮喘，过敏性鼻炎和血栓形成障碍。