公开(公告)号：US08148376B2

公开(公告)日：2012-04-03

申请号：US12767515

申请日：2010-04-26

申请人： Jeffrey Chisholm ,  Dmitry Koltun ,  Jeff Zablocki ,  Eric Parkhill ,  Andrey Glushkov ,  Natalya Vasilevich ,  Timur Zilbershtein ,  Alexey Ivanov

发明人： Jeffrey Chisholm ,  Dmitry Koltun ,  Jeff Zablocki ,  Eric Parkhill ,  Andrey Glushkov ,  Natalya Vasilevich ,  Timur Zilbershtein ,  Alexey Ivanov

IPC分类号： A61K31/495

CPC分类号： C07D471/04 ,  C07D241/44 ,  C07D401/04

摘要： The present invention discloses 3,4-dihydroquinoxalin-2(1H)-ones for use as inhibitors of stearoyl-CoA desaturase. The compounds are useful in treating and/or preventing various human diseases, mediated by stearoyl-CoA desaturase (SCD) enzymes, especially diseases related to abnormal lipid levels, cardiovascular disease, diabetes, obesity, oily skin conditions, metabolic syndrome, and the like.

摘要翻译： 本发明公开了用作硬脂酰辅酶A去饱和酶抑制剂的3,4-二氢喹喔啉-2（1H） - 酮。 该化合物可用于治疗和/或预防由硬脂酰辅酶A去饱和酶（SCD）酶介导的各种人类疾病，特别是与异常脂质水平，心血管疾病，糖尿病，肥胖，油性皮肤病症，代谢综合征等有关的疾病 。

公开(公告)号：US20100204238A1

公开(公告)日：2010-08-12

申请号：US12767515

申请日：2010-04-26

申请人： Jeffrey Chisholm ,  Dmitry Koltun ,  Jeff Zablocki ,  Eric Parkhill ,  Andrey Glushkov ,  Natalya Vasilevich ,  Timur Zilbershtein ,  Alexey Ivanov

发明人： Jeffrey Chisholm ,  Dmitry Koltun ,  Jeff Zablocki ,  Eric Parkhill ,  Andrey Glushkov ,  Natalya Vasilevich ,  Timur Zilbershtein ,  Alexey Ivanov

IPC分类号： A61K31/4985 ,  C07D471/04 ,  A61P35/00 ,  A61P3/10 ,  A61P3/04 ,  A61P9/00 ,  A61P3/00

CPC分类号： C07D471/04 ,  C07D241/44 ,  C07D401/04

摘要： The present invention discloses bicyclic nitrogen-containing heterocyclic compounds for use as inhibitors of stearoyl-CoA desaturase. The compounds are useful in treating and/or preventing various human diseases, mediated by stearoyl-CoA desaturase (SCD) enzymes, especially diseases related to abnormal lipid levels, cardiovascular disease, diabetes, obesity, oily skin conditions, metabolic syndrome, and the like.

摘要翻译： 本发明公开了用作硬脂酰辅酶A去饱和酶抑制剂的双环含氮杂环化合物。 该化合物可用于治疗和/或预防由硬脂酰辅酶A去饱和酶（SCD）酶介导的各种人类疾病，特别是与异常脂质水平，心血管疾病，糖尿病，肥胖，油性皮肤病症，代谢综合征等有关的疾病 。

公开(公告)号：US20080139570A1

公开(公告)日：2008-06-12

申请号：US11868386

申请日：2007-10-05

申请人： Jeffrey Chisholm ,  Dmitry Koltun ,  Jeff Zablocki ,  Eric Parkhill ,  Andrey Glushkov ,  Natalya Vasilevich ,  Timur Zilbershtein ,  Alexey Ivanov

发明人： Jeffrey Chisholm ,  Dmitry Koltun ,  Jeff Zablocki ,  Eric Parkhill ,  Andrey Glushkov ,  Natalya Vasilevich ,  Timur Zilbershtein ,  Alexey Ivanov

IPC分类号： A61K31/4985 ,  C07D241/36 ,  A61P9/00 ,  A61P35/00 ,  A61P3/00

CPC分类号： C07D471/04 ,  C07D241/44 ,  C07D401/04

摘要： The present invention discloses bicyclic nitrogen-containing heterocyclic compounds for use as inhibitors of stearoyl-CoA desaturase. The compounds are useful in treating and/or preventing various human diseases, mediated by stearoyl-CoA desaturase (SCD) enzymes, especially diseases related to abnormal lipid levels, cardiovascular disease, diabetes, obesity, oily skin conditions, metabolic syndrome, and the like.

摘要翻译： 本发明公开了用作硬脂酰辅酶A去饱和酶抑制剂的双环含氮杂环化合物。 该化合物可用于治疗和/或预防由硬脂酰辅酶A去饱和酶（SCD）酶介导的各种人类疾病，特别是与异常脂质水平，心血管疾病，糖尿病，肥胖，油性皮肤病症，代谢综合征等有关的疾病 。

公开(公告)号：US07732453B2

公开(公告)日：2010-06-08

申请号：US11868386

申请日：2007-10-05

申请人： Dmitry Koltun ,  Jeff Zablocki ,  Eric Parkhill ,  Andrey Glushkov ,  Natalya Vasilevich ,  Timur Zilbershtein ,  Alexey Ivanov

发明人： Dmitry Koltun ,  Jeff Zablocki ,  Eric Parkhill ,  Andrey Glushkov ,  Natalya Vasilevich ,  Timur Zilbershtein ,  Alexey Ivanov

IPC分类号： A61K31/4965

CPC分类号： C07D471/04 ,  C07D241/44 ,  C07D401/04

摘要： The present invention discloses pyrido[2,3-B]pyrazin-3(4h)-ones for use as inhibitors of stearoyl-CoA desaturase. The compounds are useful in treating and/or preventing various human diseases, mediated by stearoyl-CoA desaturase (SCD) enzymes, especially diseases related to abnormal lipid levels, cardiovascular disease, diabetes, obesity, oily skin conditions, metabolic syndrome, and the like.

摘要翻译： 本发明公开了用作硬脂酰CoA去饱和酶抑制剂的吡啶并[2,3-B]吡嗪-3（4h）酮。 该化合物可用于治疗和/或预防由硬脂酰辅酶A去饱和酶（SCD）酶介导的各种人类疾病，特别是与异常脂质水平，心血管疾病，糖尿病，肥胖，油性皮肤病症，代谢综合征等有关的疾病 。

公开(公告)号：US20100113463A1

公开(公告)日：2010-05-06

申请号：US12684007

申请日：2010-01-07

申请人： Jeffrey Chisholm ,  Dmitry Koltun ,  Jeff Zablocki ,  Eric Parkhill ,  Andrey Glushkov ,  Natalya Vasilevich ,  Timur Zilbershtein ,  Andrew Cole ,  Tsung Lin ,  Ian Henderson

发明人： Jeffrey Chisholm ,  Dmitry Koltun ,  Jeff Zablocki ,  Eric Parkhill ,  Andrey Glushkov ,  Natalya Vasilevich ,  Timur Zilbershtein ,  Andrew Cole ,  Tsung Lin ,  Ian Henderson

IPC分类号： A61K31/519 ,  C07D475/00 ,  A61P9/12 ,  A61P9/10 ,  A61P35/00 ,  A61P3/04 ,  A61P3/10

CPC分类号： C07D487/04

摘要： The present invention discloses pteridinone derivatives for use as inhibitors of stearoyl-CoA desaturase having the structure of Formula I: The compounds are useful in treating and/or preventing various human diseases, mediated by stearoyl-CoA desaturase (SCD) enzymes, especially diseases related to abnormal lipid levels, cardiovascular disease, diabetes, obesity, metabolic syndrome and the like.

摘要翻译： 本发明公开了用作具有式I结构的硬脂酰CoA去饱和酶抑制剂的蝶啶酮衍生物：该化合物可用于治疗和/或预防由硬脂酰辅酶A去饱和酶（SCD）酶介导的各种人类疾病，特别是疾病相关 心血管疾病，糖尿病，肥胖症，代谢综合症等。

公开(公告)号：US07662819B2

公开(公告)日：2010-02-16

申请号：US11868407

申请日：2007-10-05

申请人： Jeffrey Chisholm ,  Dmitry Koltun ,  Jeff Zablocki ,  Eric Parkhill ,  Andrey Glushkov ,  Natalya Vasilevich ,  Timur Zilbershtein ,  Andrew Cole ,  Tsung Lin ,  Ian Henderson

发明人： Jeffrey Chisholm ,  Dmitry Koltun ,  Jeff Zablocki ,  Eric Parkhill ,  Andrey Glushkov ,  Natalya Vasilevich ,  Timur Zilbershtein ,  Andrew Cole ,  Tsung Lin ,  Ian Henderson

IPC分类号： A61K31/519 ,  C07D475/00 ,  A61P35/00 ,  A61P3/10 ,  A61P9/00

CPC分类号： C07D487/04

摘要： The present invention discloses pteridinone derivatives for use as inhibitors of stearoyl-CoA desaturase having the structure of Formula I: The compounds are useful in treating and/or preventing various human diseases, mediated by stearoyl-CoA desaturase (SCD) enzymes, especially diseases related to abnormal lipid levels, cardiovascular disease, diabetes, obesity, metabolic syndrome and the like.

摘要翻译： 本发明公开了用作具有式I结构的硬脂酰CoA去饱和酶抑制剂的蝶啶酮衍生物：该化合物可用于治疗和/或预防由硬脂酰辅酶A去饱和酶（SCD）酶介导的各种人类疾病，特别是疾病相关 心血管疾病，糖尿病，肥胖症，代谢综合症等。

公开(公告)号：US20080249100A1

公开(公告)日：2008-10-09

申请号：US11868407

申请日：2007-10-05

申请人： Jeffrey Chisholm ,  Dmitry Koltun ,  Jeff Zablocki ,  Eric Parkhill ,  Andrey Glushkov ,  Natalya Vasilevich ,  Timur Zilbershtein ,  Andrew Cole ,  Tsung Lin ,  Ian Henderson

发明人： Jeffrey Chisholm ,  Dmitry Koltun ,  Jeff Zablocki ,  Eric Parkhill ,  Andrey Glushkov ,  Natalya Vasilevich ,  Timur Zilbershtein ,  Andrew Cole ,  Tsung Lin ,  Ian Henderson

IPC分类号： A61K31/519 ,  A61P9/00 ,  A61P25/00 ,  A61P35/00 ,  A61P3/00 ,  C07D487/04

CPC分类号： C07D487/04

摘要： The present invention discloses pteridinone derivatives for use as inhibitors of stearoyl-CoA desaturase having the structure of Formula I: The compounds are useful in treating and/or preventing various human diseases, mediated by stearoyl-CoA desaturase (SCD) enzymes, especially diseases related to abnormal lipid levels, cardiovascular disease, diabetes, obesity, metabolic syndrome and the like.

摘要翻译： 本发明公开了用作具有式I结构的硬脂酰CoA去饱和酶抑制剂的蝶啶酮衍生物：该化合物可用于治疗和/或预防由硬脂酰辅酶A去饱和酶（SCD）酶介导的各种人类疾病，特别是疾病相关 心血管疾病，糖尿病，肥胖症，代谢综合症等。

公开(公告)号：US20080255130A1

公开(公告)日：2008-10-16

申请号：US12082332

申请日：2008-04-09

申请人： Dmitry Koltun ,  Jeff Zablocki ,  Eric Parkhill ,  Andrei Glushkov ,  Natalya Vasilevich ,  Timur Zilbershtein ,  Alexey Ivanov ,  Jeffrey Chisholm

发明人： Dmitry Koltun ,  Jeff Zablocki ,  Eric Parkhill ,  Andrei Glushkov ,  Natalya Vasilevich ,  Timur Zilbershtein ,  Alexey Ivanov ,  Jeffrey Chisholm

IPC分类号： A61K31/4985 ,  C07D471/04 ,  C07D241/52

CPC分类号： C07D241/44 ,  C07D401/04 ,  C07D471/04

摘要： The present invention discloses bicyclic nitrogen-containing heterocyclic compounds for use as inhibitors of stearoyl-CoA desaturase. The compounds are useful in treating and/or preventing various human diseases, mediated by stearoyl-CoA desaturase (SCD) enzymes, especially diseases related to abnormal lipid levels, cardiovascular disease, diabetes, obesity, oily skin conditions, metabolic syndrome, and the like.

摘要翻译： 本发明公开了用作硬脂酰辅酶A去饱和酶抑制剂的双环含氮杂环化合物。 该化合物可用于治疗和/或预防由硬脂酰辅酶A去饱和酶（SCD）酶介导的各种人类疾病，特别是与异常脂质水平，心血管疾病，糖尿病，肥胖，油性皮肤病症，代谢综合征等有关的疾病 。

公开(公告)号：US07893066B2

公开(公告)日：2011-02-22

申请号：US12082332

申请日：2008-04-09

申请人： Dmitry Koltun ,  Jeff Zablocki ,  Eric Parkhill ,  Andrei Glushkov ,  Natalya Vasilevich ,  Timur Zilbershtein ,  Alexey Ivanov ,  Jeffrey Chisholm

发明人： Dmitry Koltun ,  Jeff Zablocki ,  Eric Parkhill ,  Andrei Glushkov ,  Natalya Vasilevich ,  Timur Zilbershtein ,  Alexey Ivanov ,  Jeffrey Chisholm

IPC分类号： A61K31/495

CPC分类号： C07D241/44 ,  C07D401/04 ,  C07D471/04

摘要： The present invention discloses pyrido[2,3-B]pyrazinones having the structure of Formula I for use as inhibitors of stearoyl-CoA desaturase. The compounds are useful in treating and/or preventing various human diseases, mediated by stearoyl-CoA desaturase (SCD) enzymes, especially diseases related to abnormal lipid levels, cardiovascular disease, diabetes, obesity, oily skin conditions, metabolic syndrome, and the like.

摘要翻译： 本发明公开了具有式I结构的吡啶并[2,3-B]吡嗪酮，用作硬脂酰辅酶A去饱和酶的抑制剂。 该化合物可用于治疗和/或预防由硬脂酰辅酶A去饱和酶（SCD）酶介导的各种人类疾病，特别是与异常脂质水平，心血管疾病，糖尿病，肥胖，油性皮肤病症，代谢综合征等有关的疾病 。

公开(公告)号：US20090105283A1

公开(公告)日：2009-04-23

申请号：US12252057

申请日：2008-10-15

申请人： Dmitry Koltun ,  Eric Parkhill ,  Melanie Boze ,  Jeff Zablocki ,  Natalya Vasilevich ,  Elena Mayboroda ,  Andrei Glushkov ,  Andrew G. Cole ,  Jeffrey Chisholm

发明人： Dmitry Koltun ,  Eric Parkhill ,  Melanie Boze ,  Jeff Zablocki ,  Natalya Vasilevich ,  Elena Mayboroda ,  Andrei Glushkov ,  Andrew G. Cole ,  Jeffrey Chisholm

IPC分类号： A61K31/519 ,  C07D239/72 ,  C07D471/04 ,  A61K31/517

CPC分类号： C07D239/91 ,  C07D471/04

摘要： The present invention discloses 3-hydroquinazolin-4-one derivatives for use as inhibitors of stearoyl-CoA desaturase. The compounds are useful in treating and/or preventing various human diseases, mediated by stearoyl-CoA desaturase (SCD) enzymes, especially diseases related to abnormal lipid levels, cancer, cardiovascular disease, diabetes, obesity, metabolic syndrome and the like.

摘要翻译： 本发明公开了用作硬脂酰辅酶A去饱和酶抑制剂的3-氢喹唑啉-4-酮衍生物。 该化合物可用于治疗和/或预防由硬脂酰辅酶A去饱和酶（SCD）酶介导的各种人类疾病，特别是与异常脂质水平，癌症，心血管疾病，糖尿病，肥胖症，代谢综合征等相关的疾病。