公开(公告)号：US07772238B2

公开(公告)日：2010-08-10

申请号：US11918912

申请日：2006-04-14

申请人： Jed Lee Hubbs ,  Sam Kattar ,  Joey Methot ,  Thomas Miller ,  Phieng Siliphaivanh ,  Matthew Stanton ,  Kevin Wilson ,  David J. Witter

发明人： Jed Lee Hubbs ,  Sam Kattar ,  Joey Methot ,  Thomas Miller ,  Phieng Siliphaivanh ,  Matthew Stanton ,  Kevin Wilson ,  David J. Witter

IPC分类号： A61K31/496 ,  A61K31/381 ,  C07D405/04 ,  C07D333/56

CPC分类号： C07D333/70 ,  A61K31/38 ,  A61K31/381 ,  A61K31/41

摘要： The present invention relates to a novel class of hydroxamic acid derivatives. The hydroxamic acid compounds can be used to treat cancer. The hydroxamic acid compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention are also useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the hydroxamic acid derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the hydroxamic acid derivatives in vivo.

摘要翻译： 本发明涉及一类新型异羟肟酸衍生物。 异羟肟酸化合物可用于治疗癌症。 异羟肟酸化合物也可以抑制组蛋白脱乙酰酶，适用于选择性诱导终末分化，阻止肿瘤细胞的细胞生长和/或凋亡，从而抑制这些细胞的增殖。 因此，本发明的化合物可用于治疗具有以肿瘤细胞增殖为特征的肿瘤的患者。 本发明的化合物还可用于预防和治疗TRX介导的疾病，例如自身免疫性，过敏性和炎性疾病，以及预防和/或治疗中枢神经系统（CNS）的疾病，例如神经变性 疾病 本发明进一步提供包含异羟肟酸衍生物和这些药物组合物的安全投药方案的药物组合物，它们易于遵循，并且其在体内导致治疗有效量的异羟肟酸衍生物。

公开(公告)号：US20090069391A1

公开(公告)日：2009-03-12

申请号：US11918912

申请日：2006-04-14

申请人： Jed Lee Hubbs ,  Sam Kattar ,  Joey Methot ,  Thomas Miller ,  Phieng Siliphaivanh ,  Matthew Stanton ,  Kevin Wilson ,  David J. Witter

发明人： Jed Lee Hubbs ,  Sam Kattar ,  Joey Methot ,  Thomas Miller ,  Phieng Siliphaivanh ,  Matthew Stanton ,  Kevin Wilson ,  David J. Witter

IPC分类号： A61K31/381 ,  C07D333/52 ,  A61K31/4245 ,  A61P25/00 ,  A61P35/00 ,  C07D271/10

CPC分类号： C07D333/70 ,  A61K31/38 ,  A61K31/381 ,  A61K31/41

摘要： The present invention relates to a novel class of hydroxamic acid derivatives. The hydroxamic acid compounds can be used to treat cancer. The hydroxamic acid compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention are also useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the hydroxamic acid derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the hydroxamic acid derivatives in vivo.

摘要翻译： 本发明涉及一类新型异羟肟酸衍生物。 异羟肟酸化合物可用于治疗癌症。 异羟肟酸化合物也可以抑制组蛋白脱乙酰酶，适用于选择性诱导终末分化，阻止肿瘤细胞的细胞生长和/或凋亡，从而抑制这些细胞的增殖。 因此，本发明的化合物可用于治疗具有以肿瘤细胞增殖为特征的肿瘤的患者。 本发明的化合物还可用于预防和治疗TRX介导的疾病，例如自身免疫性，过敏性和炎性疾病，以及预防和/或治疗中枢神经系统（CNS）的疾病，例如神经变性 疾病 本发明进一步提供包含异羟肟酸衍生物和这些药物组合物的安全投药方案的药物组合物，它们易于遵循，并且其在体内导致治疗有效量的异羟肟酸衍生物。

公开(公告)号：US20120022044A1

公开(公告)日：2012-01-26

申请号：US13139830

申请日：2009-12-07

申请人： Christian Fischer ,  Joey Methot ,  Hua Zhou ,  Adam J. Schell ,  Benito Munoz ,  Alexey A. Rivkin ,  Sean P. Ahearn ,  Stephanie Chichetti ,  Rachel N. MacCoss ,  Sam Kattar ,  Matthew Christopher ,  Chaomin Li ,  Andrew Rosenau ,  William Colby Brown

发明人： Christian Fischer ,  Joey Methot ,  Hua Zhou ,  Adam J. Schell ,  Benito Munoz ,  Alexey A. Rivkin ,  Sean P. Ahearn ,  Stephanie Chichetti ,  Rachel N. MacCoss ,  Sam Kattar ,  Matthew Christopher ,  Chaomin Li ,  Andrew Rosenau ,  William Colby Brown

IPC分类号： A61K31/55 ,  C07D403/04 ,  C07D409/14 ,  A61P25/28 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04 ,  C07D401/14 ,  C07D417/14

CPC分类号： A61K31/41 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

摘要： According to the invention there is provided a compound of formula I or a pharmaceutically acceptable salt or hydrate thereof; wherein the variables are as defined herein. The compounds selectively attenuate the production of Aβ42 and hence are useful in treatment of Alzheimer's disease and related conditions.

摘要翻译： 根据本发明，提供式I化合物或其药学上可接受的盐或水合物; 其中变量如本文所定义。 这些化合物选择性地减弱A＆bgr的产生42，因此可用于治疗阿尔茨海默病和相关病症。

公开(公告)号：US08575150B2

公开(公告)日：2013-11-05

申请号：US13139830

申请日：2009-12-07

申请人： Christian Fischer ,  Joey Methot ,  Hua Zhou ,  Adam J. Schell ,  Benito Munoz ,  Alexey A. Rivkin ,  Sean P. Ahearn ,  Stephanie Chichetti ,  Rachel N. MacCoss ,  Sam Kattar ,  Matthew Christopher ,  Chaomin Li ,  Andrew Rosenau ,  William Colby Brown

发明人： Christian Fischer ,  Joey Methot ,  Hua Zhou ,  Adam J. Schell ,  Benito Munoz ,  Alexey A. Rivkin ,  Sean P. Ahearn ,  Stephanie Chichetti ,  Rachel N. MacCoss ,  Sam Kattar ,  Matthew Christopher ,  Chaomin Li ,  Andrew Rosenau ,  William Colby Brown

IPC分类号： C07D249/14 ,  A61K31/4196

CPC分类号： A61K31/41 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

摘要： According to the invention there is provided a compound of formula I or a pharmaceutically acceptable salt or hydrate thereof; wherein the variables are as defined herein. The compounds selectively attenuate the production of Aβ42 and hence are useful in treatment of Alzheimer's disease and related conditions.

摘要翻译： 根据本发明，提供式I化合物或其药学上可接受的盐或水合物; 其中变量如本文所定义。 这些化合物选择性地减弱Abeta42的产生，因此可用于治疗阿尔茨海默病和相关病症。

公开(公告)号：US20170240567A1

公开(公告)日：2017-08-24

申请号：US15519740

申请日：2015-10-21

申请人： Mark E. Scott ,  David Guerin ,  Danielle Molinari ,  Sam Kattar ,  Peter Fuller ,  Christopher Dinsmore ,  Normon Kong ,  Yunfeng Bai ,  Jianmin FU ,  Yumei Liu ,  Zhixiang Zheng

发明人： Mark E. Scott ,  David Guerin ,  Danielle Molinari ,  Sam Kattar ,  Peter Fuller ,  Christopher Dinsmore ,  Normon Kong ,  Yunfeng Bai ,  Jianmin FU ,  Yumei Liu ,  Zhixiang Zheng

IPC分类号： C07D519/00 ,  A61K31/4545 ,  A61K31/55 ,  A61K31/538 ,  A61K31/541 ,  A61K31/554 ,  A61K31/553 ,  C07D471/04 ,  A61K31/5377

CPC分类号： C07D519/00 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/541 ,  A61K31/55 ,  A61K31/553 ,  A61K31/554 ,  A61P11/06 ,  A61P19/02 ,  A61P35/00 ,  C07D471/04

摘要： The instant invention provides compounds of Formula (I) which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer. The present invention provides novel compounds which are inhibitors of JAKs. The invention also provides a method for the treatment and prevention of JAK-mediated diseases and disorders using the novel compounds, as well as pharmaceutical compositions containing the compounds.