公开(公告)号：US08383643B2

公开(公告)日：2013-02-26

申请号：US13383446

申请日：2010-07-21

申请人： Jean-Philippe Leclerc ,  Chun-Sing Li ,  Oscar Miguel Moradei

发明人： Jean-Philippe Leclerc ,  Chun-Sing Li ,  Oscar Miguel Moradei

IPC分类号： A61K31/438 ,  C07D491/107

CPC分类号： C07D491/107

摘要： Heteroaromatic compounds of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.

公开(公告)号：US20170217986A1

公开(公告)日：2017-08-03

申请号：US15123111

申请日：2015-03-02

申请人： John A. MCCAULEY ,  David Johathan BENNETT ,  Christopher J. BUNGARD ,  Thomas J. GRESHOCK ,  M. Katharine HOLLOWAY ,  Peter D. WILLIAMS ,  Christian BEAULIEU ,  Sheldon CRANE ,  Stephanie LESSARD ,  Daniel MCKAY ,  Carmela MOLINARO ,  Oscar Miguel MORADEI ,  Vijayasaradhi SIVALENKA ,  Vouy Linh TRUONG ,  Satyanarayana TUMMANAPALLI ,  Merck Canada Inc.

发明人： John A. McCauley ,  David Jonathan Bennett ,  Christopher J. Bungard ,  Thomas J. Greshock ,  M. Katharine Holloway ,  Peter D. Williams ,  Christian Beaulieu ,  Sheldon Crane ,  Stephanie Lessard ,  Daniel Mckay ,  Carmela Molinaro ,  Oscar Miguel Moradei ,  Vijayasaradhi Sivalenka ,  Vouy Linh Truong ,  Satyanarayana Tummanapalli

IPC分类号： C07D498/10 ,  A61K31/5375 ,  C07D413/12 ,  A61K31/5377 ,  C07D417/14 ,  A61K45/06 ,  C07D487/04 ,  C07D471/04 ,  C07D413/06 ,  C07D265/36 ,  A61K31/5386 ,  C07D265/30 ,  C07D413/14

CPC分类号： C07D498/10 ,  A61K31/5375 ,  A61K31/5377 ,  A61K31/5386 ,  A61K45/06 ,  C07D265/30 ,  C07D265/36 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04

摘要： The present invention is directed to 2,6-morpholine derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein Z1, Z2, V1, V2, V3, R6, R6A, and X are defined herein. The invention also relates to methods of using the 2,6-morpholine derivatives of the invention for the inhibition of HV protease, the inhibition of HV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

公开(公告)号：US20110312952A1

公开(公告)日：2011-12-22

申请号：US13148985

申请日：2010-02-16

申请人： Nicolas Lachance ,  Jean-Philippe Leclerc ,  Chun Sing Li ,  Oscar Miguel Moradei

发明人： Nicolas Lachance ,  Jean-Philippe Leclerc ,  Chun Sing Li ,  Oscar Miguel Moradei

IPC分类号： A61K31/438 ,  C07D498/10 ,  A61P3/06 ,  C07D417/14 ,  A61P3/10 ,  A61K31/537 ,  C07D491/107

CPC分类号： A61K31/438 ,  C07D491/107

摘要： Heteroaromatic compounds of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.

摘要翻译： 结构式（I）的杂芳族化合物是相对于其他已知的硬脂酰辅酶A去饱和酶的硬脂酰辅酶Aδ-9去饱和酶（SCD1）的选择性抑制剂。 本发明的化合物可用于预防和治疗与脂质合成和代谢异常有关的病症，包括心血管疾病，如动脉粥样硬化; 肥胖; 糖尿病; 神经系统疾病; 代谢综合征; 胰岛素抵抗; 和肝脂肪变性。

公开(公告)号：US09315475B2

公开(公告)日：2016-04-19

申请号：US14021930

申请日：2013-09-09

申请人： Christian Beaulieu ,  David J. Bennett ,  Christopher J. Bungard ,  Ronald K. Chang ,  Sheldon Crane ,  Thomas J. Greshock ,  Li Hao ,  Kate Holloway ,  Jesse J. Manikowski ,  John A. McCauley ,  Daniel McKay ,  Carmela Molinaro ,  Oscar Miguel Moradei ,  Philippe G. Nantermet ,  Christian Nadeau ,  Satyanarayana Tummanapalli ,  William Shipe ,  Sanjay Kumar Singh ,  Vouy Linh Truong ,  Sivalenka Vijayasaradhi ,  Peter D. Williams ,  Catherine M. Wiscount

发明人： Christian Beaulieu ,  David J. Bennett ,  Christopher J. Bungard ,  Ronald K. Chang ,  Sheldon Crane ,  Thomas J. Greshock ,  Li Hao ,  Kate Holloway ,  Jesse J. Manikowski ,  John A. McCauley ,  Daniel McKay ,  Carmela Molinaro ,  Oscar Miguel Moradei ,  Philippe G. Nantermet ,  Christian Nadeau ,  Satyanarayana Tummanapalli ,  William Shipe ,  Sanjay Kumar Singh ,  Vouy Linh Truong ,  Sivalenka Vijayasaradhi ,  Peter D. Williams ,  Catherine M. Wiscount

IPC分类号： C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D265/30 ,  C07D487/04 ,  C07D493/04 ,  A61K31/5375 ,  A61K31/5377 ,  A61K31/695 ,  A61K45/06 ,  C07F7/08

CPC分类号： C07D265/30 ,  A61K31/5375 ,  A61K31/5377 ,  A61K31/695 ,  A61K45/06 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D487/04 ,  C07D493/04 ,  C07F7/0814

摘要： The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

摘要翻译： 式I所包括的化合物包括可以在体内代谢为HIV蛋白酶抑制剂的HIV蛋白酶抑制剂和其它化合物的化合物。 化合物及其药学上可接受的盐可用于预防或治疗HIV感染以及预防，治疗或延迟艾滋病的发病。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。

公开(公告)号：US09168248B2

公开(公告)日：2015-10-27

申请号：US13148985

申请日：2010-02-16

申请人： Nicolas Lachance ,  Jean-Philippe Leclerc ,  Chun Sing Li ,  Oscar Miguel Moradei

发明人： Nicolas Lachance ,  Jean-Philippe Leclerc ,  Chun Sing Li ,  Oscar Miguel Moradei

IPC分类号： C07D471/00 ,  C07D491/10 ,  A61K31/44 ,  A61K31/438 ,  C07D491/107

CPC分类号： A61K31/438 ,  C07D491/107

摘要： Heteroaromatic compounds of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.

摘要翻译： 结构式（I）的杂芳族化合物是相对于其他已知的硬脂酰辅酶A去饱和酶的硬脂酰辅酶Aδ-9去饱和酶（SCD1）的选择性抑制剂。 本发明的化合物可用于预防和治疗与脂质合成和代谢异常有关的病症，包括心血管疾病，如动脉粥样硬化; 肥胖; 糖尿病; 神经系统疾病; 代谢综合征; 胰岛素抵抗; 和肝脂肪变性。

公开(公告)号：US20120122912A1

公开(公告)日：2012-05-17

申请号：US13383446

申请日：2010-07-21

申请人： Jean-Philippe Leclerc ,  Chun-Sing Li ,  Oscar Miguel Moradei

发明人： Jean-Philippe Leclerc ,  Chun-Sing Li ,  Oscar Miguel Moradei

IPC分类号： A61K31/438 ,  A61P7/00 ,  A61P5/48 ,  A61P3/06 ,  C07D491/107 ,  A61P3/10

CPC分类号： C07D491/107

摘要： Heteroaromatic compounds of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.

摘要翻译： 结构式（I）的杂芳族化合物是相对于其他已知的硬脂酰辅酶A去饱和酶的硬脂酰辅酶Aδ-9去饱和酶（SCD1）的选择性抑制剂。 本发明的化合物可用于预防和治疗与脂质合成和代谢异常有关的病症，包括心血管疾病，如动脉粥样硬化; 肥胖; 糖尿病; 神经系统疾病; 代谢综合征; 胰岛素抵抗; 和肝脂肪变性。

公开(公告)号：US20140200197A1

公开(公告)日：2014-07-17

申请号：US14021930

申请日：2013-09-09

申请人： JOHN A. MCCAULEY ,  CHRISTIAN BEAULIEU ,  DAVID J. BENNETT ,  CHRISTOPHER J. BUNGARD ,  RONALD K. CHANG ,  SHELDON CRANE ,  THOMAS J. GRESHOCK ,  LI HAO ,  KATE HOLLOWAY ,  JESSE J. MANIKOWSKI ,  DANIEL MCKAY ,  CARMELA MOLINARO ,  OSCAR MIGUEL MORADEI ,  PHILIPPE G. NANTERMET ,  CHRISTIAN NADEAU ,  TUMMANAPALLI SATYANARAYANA ,  WILLIAM SHIPE ,  SANJAY KUMAR SINGH ,  VOUY LINH TRUONG ,  SIVALENKA VIJAYARADHI ,  PETER D. WILLIAMS ,  CATHERINE M. WISCOUNT

发明人： JOHN A. MCCAULEY ,  CHRISTIAN BEAULIEU ,  DAVID J. BENNETT ,  CHRISTOPHER J. BUNGARD ,  RONALD K. CHANG ,  SHELDON CRANE ,  THOMAS J. GRESHOCK ,  LI HAO ,  KATE HOLLOWAY ,  JESSE J. MANIKOWSKI ,  DANIEL MCKAY ,  CARMELA MOLINARO ,  OSCAR MIGUEL MORADEI ,  PHILIPPE G. NANTERMET ,  CHRISTIAN NADEAU ,  TUMMANAPALLI SATYANARAYANA ,  WILLIAM SHIPE ,  SANJAY KUMAR SINGH ,  VOUY LINH TRUONG ,  SIVALENKA VIJAYARADHI ,  PETER D. WILLIAMS ,  CATHERINE M. WISCOUNT

IPC分类号： C07D265/30 ,  A61K45/06 ,  C07D413/12 ,  A61K31/695 ,  C07D413/06 ,  C07D417/12 ,  C07D487/04 ,  C07F7/08 ,  A61K31/5375 ,  A61K31/5377

CPC分类号： C07D265/30 ,  A61K31/5375 ,  A61K31/5377 ,  A61K31/695 ,  A61K45/06 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D487/04 ,  C07D493/04 ,  C07F7/0814

摘要： The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

摘要翻译： 式I所包括的化合物包括可以在体内代谢为HIV蛋白酶抑制剂的HIV蛋白酶抑制剂和其它化合物的化合物。 化合物及其药学上可接受的盐可用于预防或治疗HIV感染以及预防，治疗或延迟艾滋病的发病。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。