公开(公告)号：US20140155413A1

公开(公告)日：2014-06-05

申请号：US14131861

申请日：2012-07-06

申请人： Barbara Hanney ,  Peter Manley ,  Michael T. Rudd ,  John M. Sanders ,  Shawn J. Stachel ,  Darrell Henze

发明人： Barbara Hanney ,  Peter Manley ,  Michael T. Rudd ,  John M. Sanders ,  Shawn J. Stachel ,  Darrell Henze

IPC分类号： C07D471/04 ,  C07D417/04 ,  C07D401/04 ,  C07D405/04 ,  C07D487/04 ,  C07D403/04

CPC分类号： C07D471/04 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D417/04 ,  C07D487/04

摘要： The present invention is directed to compounds of formula I and 1a: which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.

摘要翻译： 本发明涉及式I和1a的化合物：其是原肌球蛋白相关激酶（Trk）家族蛋白激酶抑制剂，因此可用于治疗疼痛，炎症，癌症，再狭窄，动脉粥样硬化，牛皮癣，血栓形成， 与神经生长因子（NGF）受体TrkA的异常活动相关的疾病，失调，损伤或功能障碍，或与脱髓鞘或脱髓鞘相关的疾病或病症。

公开(公告)号：US09102673B2

公开(公告)日：2015-08-11

申请号：US14131861

申请日：2012-07-06

申请人： Barbara Hanney ,  Peter Manley ,  Michael T. Rudd ,  John M. Sanders ,  Shawn J. Stachel ,  Darrell Henze

发明人： Barbara Hanney ,  Peter Manley ,  Michael T. Rudd ,  John M. Sanders ,  Shawn J. Stachel ,  Darrell Henze

IPC分类号： A61K31/437 ,  C07D471/04 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D417/04 ,  C07D487/04

CPC分类号： C07D471/04 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D417/04 ,  C07D487/04

摘要： The present invention is directed to compounds of formula I and Ia: which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.

摘要翻译： 本发明涉及式I和Ia的化合物：它们是原肌球蛋白相关激酶（Trk）家族蛋白激酶抑制剂，因此可用于治疗疼痛，炎症，癌症，再狭窄，动脉粥样硬化，牛皮癣，血栓形成， 与神经生长因子（NGF）受体TrkA的异常活动相关的疾病，失调，损伤或功能障碍，或与脱髓鞘或脱髓鞘相关的疾病或病症。

公开(公告)号：US20200247754A1

公开(公告)日：2020-08-06

申请号：US16341595

申请日：2017-10-09

申请人： Michael T. RUDD ,  Zhaoyang MENG ,  Jenny WAI ,  David Jonathan BENNETT ,  Edward J. BRNARDIC ,  Nigel J. LIVERTON ,  Shawn J. STACHEL ,  Yongxin HAN ,  Paul TEMPEST ,  Jiuxiang ZHU ,  Xuewang XU ,  Bin ZHU ,  Merck Sharp & Dohme Corp.

发明人： Michael T. Rudd ,  Zhaoyang Meng ,  Jenny Wai ,  David Jonathan Bennett ,  Edward J. Brnardic ,  Nigel J. Liverton ,  Shawn J. Stachel ,  Yongxin Han ,  Paul Tempest ,  Jiuxiang Zhu ,  Xuewang Xu ,  Bin Zhu

IPC分类号： C07D221/20 ,  C07D401/12 ,  C07D417/12 ,  C07D405/12 ,  C07D211/22 ,  C07D401/14 ,  C07D417/14

摘要： In its many embodiments, the present invention provides certain substituted aryl and heteroaryl ether compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, L, R4, L1, Q, and R5 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.

公开(公告)号：US20180327374A1

公开(公告)日：2018-11-15

申请号：US15774157

申请日：2016-11-07

申请人： Michael T. RUDD ,  Edward J. BRNARDIC ,  Yuntae KIM ,  Robert S. MEISSNER ,  Vanessa RADA ,  Shawn J. STACHEL ,  Celina V. ZERBINATTI ,  Merck Sharp & Dohme Corp.

发明人： Michael T. Rudd ,  Edward J. Brnardic ,  Yuntae Kim ,  Robert S. Meissner ,  Vanessa L. Rada ,  Shawn J. Stachel ,  Celina V. Zerbinatti

IPC分类号： C07D295/16 ,  C07D243/08 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/08 ,  C07D487/08 ,  C07D513/04 ,  A61P25/28 ,  A61P25/18 ,  A61P25/16 ,  A61P3/10

CPC分类号： C07D295/16 ,  A61K31/496 ,  A61P3/10 ,  A61P25/16 ,  A61P25/18 ,  A61P25/28 ,  C07D213/74 ,  C07D213/85 ,  C07D243/08 ,  C07D295/192 ,  C07D295/205 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/08 ,  C07D487/08 ,  C07D487/18 ,  C07D513/04 ,  C07D515/04

摘要： In its many embodiments, the present invention provides substituted cyanopyridine containing compounds of the Formula (I): and acceptable salts thereof, wherein R1, R2, R3, R4, R5, X, Y, Q, and the moiety are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.

公开(公告)号：US11655216B2

公开(公告)日：2023-05-23

申请号：US16341595

申请日：2017-10-09

申请人： Merck Sharp & Dohme Corp. ,  Michael T. Rudd ,  Zhaoyang Meng ,  Jenny Wai ,  David Jonathan Bennett ,  Edward J. Brnardic ,  Nigel J. Liverton ,  Shawn J. Stachel ,  Yongxin Han ,  Paul Tempest ,  Jiuxiang Zhu ,  Xuewang Xu ,  Bin Zhu

发明人： Michael T. Rudd ,  Zhaoyang Meng ,  Jenny Wai ,  David Jonathan Bennett ,  Edward J. Brnardic ,  Nigel J. Liverton ,  Shawn J. Stachel ,  Yongxin Han ,  Paul Tempest ,  Jiuxiang Zhu ,  Xuewang Xu ,  Bin Zhu

IPC分类号： C07D221/20 ,  C07D401/12 ,  C07D417/12 ,  C07D405/12 ,  C07D211/22 ,  C07D401/14 ,  C07D417/14

CPC分类号： C07D221/20 ,  C07D211/22 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D417/12 ,  C07D417/14

摘要： In its many embodiments, the present invention provides certain substituted aryl and heteroaryl ether compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, L, R4, L1, Q, and R5 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.

公开(公告)号：US10894775B2

公开(公告)日：2021-01-19

申请号：US16341591

申请日：2017-10-09

申请人： Merck Sharp & Dohme Corp. ,  Michael T. Rudd ,  Zhaoyang Meng ,  Jenny Wai ,  David Jonathan Bennett ,  Edward J. Brnardic ,  Nigel J. Liverton ,  Shawn J. Stachel ,  Yongxin Han ,  Paul Tempest ,  Jiuxiang Zhu ,  Xuewang Xu ,  Bin Zhu ,  Chuanman Huang

发明人： Michael T. Rudd ,  Zhaoyang Meng ,  Jenny Wai ,  David Jonathan Bennett ,  Edward J. Brnardic ,  Nigel J. Liverton ,  Shawn J. Stachel ,  Yongxin Han ,  Paul Tempest ,  Jiuxiang Zhu ,  Xuewang Xu ,  Bin Zhu ,  Chuanman Huang

IPC分类号： C07D221/20 ,  C07D211/16 ,  C07D211/96

摘要： In its many embodiments, the present invention provides certain piperidine compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein X, Y, R1, R2, R3, L, R4, L1, Q, and R5 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.

公开(公告)号：US10239849B2

公开(公告)日：2019-03-26

申请号：US15774157

申请日：2016-11-07

申请人： Merck Sharp & Dohme Corp. ,  Michael T. Rudd ,  Edward J. Brnardic ,  Yuntae Kim ,  Robert S. Meissner ,  Vanessa L. Rada ,  Shawn J. Stachel ,  Celina V. Zerbinatti

发明人： Michael T. Rudd ,  Edward J. Brnardic ,  Yuntae Kim ,  Robert S. Meissner ,  Vanessa L. Rada ,  Shawn J. Stachel ,  Celina V. Zerbinatti

IPC分类号： C07D243/08 ,  C07D295/16 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/08 ,  C07D487/08 ,  C07D513/04 ,  A61P25/18 ,  A61P25/16 ,  A61P25/28 ,  A61P3/10

摘要： In its many embodiments, the present invention provides substituted cyanopyridine containing compounds of the Formula (I): and acceptable salts thereof, wherein R1, R2, R3, R4, R5, X, Y, Q, and the moiety are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.

公开(公告)号：US20110028494A1

公开(公告)日：2011-02-03

申请号：US11989886

申请日：2006-07-28

申请人： M. Katharine Holloway ,  Nigel J. Liverton ,  John A. McCauley ,  Michael T. Rudd ,  Joseph P. Vacca ,  Steven W. Ludmerer ,  David B. Olsen

发明人： M. Katharine Holloway ,  Nigel J. Liverton ,  John A. McCauley ,  Michael T. Rudd ,  Joseph P. Vacca ,  Steven W. Ludmerer ,  David B. Olsen

IPC分类号： A61K31/437 ,  C07D498/14 ,  A61P31/12

CPC分类号： C07K5/0812 ,  A61K38/00 ,  C07K5/0827

摘要： The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.

摘要翻译： 本发明涉及可用作丙型肝炎病毒（HCV）NS3蛋白酶抑制剂及其合成及其用于治疗或预防HCV感染的用途的式（I）的大环化合物。

公开(公告)号：US20100099695A1

公开(公告)日：2010-04-22

申请号：US12447342

申请日：2007-10-23

申请人： Nigel J. Liverton ,  Vincenzo Summa ,  Maria Emilia Di Francesco ,  Marco Ferrara ,  Kevin F. Gilbert ,  Steven Harper ,  John A. McCauley ,  Charles A. McIntyre ,  Alessia Petrocchi ,  Marco Pompei ,  Joseph J. Romano ,  Michael T. Rudd ,  John W. Butcher ,  M. Katharine Holloway

发明人： Nigel J. Liverton ,  Vincenzo Summa ,  Maria Emilia Di Francesco ,  Marco Ferrara ,  Kevin F. Gilbert ,  Steven Harper ,  John A. McCauley ,  Charles A. McIntyre ,  Alessia Petrocchi ,  Marco Pompei ,  Joseph J. Romano ,  Michael T. Rudd ,  John W. Butcher ,  M. Katharine Holloway

IPC分类号： A61K31/439 ,  C07D513/18 ,  C07D513/08 ,  A61K31/407 ,  A61K31/4748 ,  A61P31/12

CPC分类号： C07D498/22 ,  A61K31/407 ,  A61K31/4192 ,  A61K31/437 ,  A61K31/439 ,  A61K38/00 ,  A61K45/06 ,  C07D498/08 ,  C07D498/18 ,  C07K5/0804 ,  C07K5/0806 ,  C07K5/0808 ,  C07K5/0812

摘要： The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.

摘要翻译： 本发明涉及可用作丙型肝炎病毒（HCV）NS3蛋白酶抑制剂及其合成及其用于治疗或预防HCV感染的用途的式（I）的大环化合物。

公开(公告)号：US20090075869A1

公开(公告)日：2009-03-19

申请号：US11919783

申请日：2006-04-28

申请人： M. Katharine Holloway ,  Nigel J. Liverton ,  Steven W. Ludmerer ,  John A. McCauley ,  David Olsen ,  Michael T. Rudd ,  Joseph P. Vacca

发明人： M. Katharine Holloway ,  Nigel J. Liverton ,  Steven W. Ludmerer ,  John A. McCauley ,  David Olsen ,  Michael T. Rudd ,  Joseph P. Vacca

IPC分类号： A61K38/12 ,  C07D498/04 ,  C07K5/12

CPC分类号： C07K5/0808 ,  C07K5/0806 ,  C07K5/0812 ,  C07K5/0815 ,  C07K5/0821

摘要： The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.

摘要翻译： 本发明涉及可用作丙型肝炎病毒（HCV）NS3蛋白酶抑制剂及其合成及其用于治疗或预防HCV感染的用途的式（I）的大环化合物。