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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.
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![Substituted pyrrolo[3,2-c]pyridines as TrkA kinase inhibitors](/abs-image/US/2015/08/11/US09102673B2/abs.jpg.150x150.jpg)
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。
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3.发明授权Spiropyrrolidine beta-secretase inhibitors for the treatment of alzheimer'S disease 有权Spiropyrrolidineβ-分泌酶抑制剂用于治疗阿尔茨海默氏病公开(公告)号：US08865701B2
公开(公告)日：2014-10-21
申请号：US13201570
申请日：2010-02-20
申请人： Kun Liu , Shawn J. Stachel , Craig A. Coburn , Thomas G. Steele , Richard Soll , Hao Wu , Xuanjin Peng , Yaxian Cai , Xiaoxiang Du , Jian Li
发明人： Kun Liu , Shawn J. Stachel , Craig A. Coburn , Thomas G. Steele , Richard Soll , Hao Wu , Xuanjin Peng , Yaxian Cai , Xiaoxiang Du , Jian Li
IPC分类号： A61K31/55 , C07D513/20 , A61K31/438 , A61K31/445 , A61P25/28 , C07D405/14 , C07D413/14 , C07D495/10 , C07D491/20 , C07D209/96 , C07D491/10 , C07D471/20 , C07D513/10 , C07D471/10
CPC分类号： C07D401/06 , C07D209/96 , C07D471/10 , C07D471/20 , C07D491/10 , C07D491/107 , C07D491/20 , C07D495/10 , C07D513/10 , C07D513/20
摘要： The present invention is directed to spiropyrrolidine compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
摘要翻译： 本发明涉及作为β-分泌酶的抑制剂并可用于治疗其中涉及β-分泌酶的疾病如阿尔茨海默氏病的式（I）的螺吡咯烷化合物。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗涉及β-分泌酶的疾病中的用途。
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4.发明授权3,4-substituted pyrrolidine beta-secretase inhibitors for the treatment of alzheimer's disease 有权用于治疗阿尔茨海默病的3,4-取代吡咯烷β-分泌酶抑制剂公开(公告)号：US08354545B2
公开(公告)日：2013-01-15
申请号：US12747605
申请日：2008-12-10
IPC分类号： C07D401/06 , C07D207/06 , C07D403/14 , C07D413/06 , A61K31/535 , A61K31/445 , A61K31/415 , A61K31/4025
CPC分类号： C07D413/06 , C07D401/06 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D491/04 , C07D491/10
摘要： The present invention is directed to 3,4-substituted pyrrolidine compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
摘要翻译： 本发明涉及作为β-分泌酶的抑制剂的式（I）的3,4-取代吡咯烷化合物，其可用于治疗其中涉及β-分泌酶的疾病，例如阿尔茨海默病 。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗涉及β-分泌酶的疾病中的用途。
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5.发明授权2,4,6-substituted pyridyl derivative compounds useful as beta-secretase inhibitors for the treatment of Alzheimer's Disease 有权用作治疗阿尔茨海默病的β-分泌酶抑制剂的2,4,6-取代的吡啶基衍生物化合物公开(公告)号：US07968571B2
公开(公告)日：2011-06-28
申请号：US11547994
申请日：2005-04-20
申请人： James C. Barrow , Georgia B. McGaughey , Philippe G. Nantermet , Hemaka A. Rajapakse , Harold G. Selnick , Shaun R. Stauffer , Joseph P. Vacca , Shawn J. Stachel , Craig A. Coburn , Matthew G. Stanton
发明人： James C. Barrow , Georgia B. McGaughey , Philippe G. Nantermet , Hemaka A. Rajapakse , Harold G. Selnick , Shaun R. Stauffer , Joseph P. Vacca , Shawn J. Stachel , Craig A. Coburn , Matthew G. Stanton
IPC分类号： A61K31/443 , C07D413/04
CPC分类号： C07D413/04 , C07D401/04 , C07D413/14 , C07D417/04 , C07D417/14
摘要： The present invention is directed to 2,4,6-substituted pyridyl derivative compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
摘要翻译： 本发明涉及作为β-分泌酶的抑制剂并可用于治疗其中涉及β-分泌酶的疾病如阿尔茨海默氏病的2,4,6-取代的吡啶衍生物化合物。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗涉及β-分泌酶的疾病中的用途。
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6.发明授权N-alkyl phenylcarboxamide beta-secretase inhibitors for the treatment of Alzheimer's disease 有权用于治疗阿尔茨海默氏病的N-烷基苯基卡巴酰胺β-分泌酶抑制剂公开(公告)号：US07291620B2
公开(公告)日：2007-11-06
申请号：US10563538
申请日：2004-06-25
IPC分类号： A61K31/4965 , A61K31/445 , A61K31/40 , A61K31/279 , A61K31/16
CPC分类号： C07C237/10 , C07C255/57 , C07C311/08 , C07C2601/02 , C07D207/06 , C07D207/08 , C07D207/10 , C07D207/14 , C07D211/38 , C07D295/084 , C07D295/185
摘要： The present invention is directed to compounds which are inhibitors of the beta-secretase enzyme and which are useful in the treatment or prevention of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
摘要翻译： 本发明涉及作为β-分泌酶的抑制剂并且可用于治疗或预防涉及β-分泌酶的疾病如阿尔茨海默氏病的化合物。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗涉及β-分泌酶的疾病中的用途。
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7.发明授权2,3,4,6-substituted pyridyl derivative compounds useful as beta-secretase inhibitors for the treatment of alzheimer's disease 有权用作治疗阿尔茨海默氏病的β-分泌酶抑制剂的2,3,4,6-取代的吡啶衍生物化合物公开(公告)号：US08394837B2
公开(公告)日：2013-03-12
申请号：US11791204
申请日：2005-11-18
申请人： Philippe G. Nantermet , Hemaka A. Rajapakse , Harold G. Selnick , James C. Barrow , Shaun R. Stauffer , Joseph P. Vacca , Keith P. Moore , Shawn J. Stachel , Mattahew G. Stanton
发明人： Philippe G. Nantermet , Hemaka A. Rajapakse , Harold G. Selnick , James C. Barrow , Shaun R. Stauffer , Joseph P. Vacca , Keith P. Moore , Shawn J. Stachel , Mattahew G. Stanton
IPC分类号： A61K31/4439 , C07D413/04
CPC分类号： C07D413/04 , C07D413/14
摘要： The present invention is directed to 2,3,4,6-substituted pyridyl derivative compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
摘要翻译： 本发明涉及2,3,4,6-取代的吡啶基衍生物化合物，其是β-分泌酶的抑制剂并且可用于治疗涉及β-分泌酶的疾病，例如阿尔茨海默病 。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗涉及β-分泌酶的疾病中的用途。
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8.发明申请SPIROPYRROLIDINE BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE 有权用于治疗阿尔茨海默病的螺旋罗哌啶β-分泌酶抑制剂公开(公告)号：US20110306595A1
公开(公告)日：2011-12-15
申请号：US13201570
申请日：2010-02-20
申请人： Kun Liu , Shawn J. Stachel , Craig A. Coburn , Thomas G. Steele , Richard Soll , Hao Wu , Xuanjin Peng , Yaxian Cai , Xiaoxiang Du , Jian Li
发明人： Kun Liu , Shawn J. Stachel , Craig A. Coburn , Thomas G. Steele , Richard Soll , Hao Wu , Xuanjin Peng , Yaxian Cai , Xiaoxiang Du , Jian Li
IPC分类号： A61K31/55 , C07D513/20 , A61K31/438 , A61K31/445 , A61P25/28 , C07D405/14 , C07D413/14
CPC分类号： C07D401/06 , C07D209/96 , C07D471/10 , C07D471/20 , C07D491/10 , C07D491/107 , C07D491/20 , C07D495/10 , C07D513/10 , C07D513/20
摘要： The present invention is directed to spiropyrrolidine compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
摘要翻译： 本发明涉及作为β-分泌酶的抑制剂并可用于治疗其中涉及β-分泌酶的疾病如阿尔茨海默氏病的式（I）的螺吡咯烷化合物。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗涉及β-分泌酶的疾病中的用途。
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9.发明申请2-AMINOIMIDAZOLE BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE 有权用于治疗阿尔茨海默病的2-氨基咪唑β-分泌酶抑制剂公开(公告)号：US20110034483A1
公开(公告)日：2011-02-10
申请号：US12919277
申请日：2009-02-18
申请人： Ivory D. Hills , Craig A. Coburn , Samuel L. Graham , Keith P. Moore , Philippe G. Nantermet , Hemaka A. Rajapakse , Shawn J. Stachel , Hong Zhu
发明人： Ivory D. Hills , Craig A. Coburn , Samuel L. Graham , Keith P. Moore , Philippe G. Nantermet , Hemaka A. Rajapakse , Shawn J. Stachel , Hong Zhu
IPC分类号： A61K31/506 , C07D233/88 , A61K31/4174 , C07D403/10 , A61K31/4178 , C07D403/06 , C07D413/10 , A61K31/42 , C07D401/10 , A61K31/4439 , A61K31/422 , A61P25/28
CPC分类号： C07D233/88 , C07D401/04 , C07D401/06 , C07D401/08 , C07D401/10 , C07D401/14 , C07D403/06 , C07D403/10 , C07D405/06 , C07D405/10 , C07D409/10 , C07D413/10
摘要： The present invention is directed to 2-aminoimidazole compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
摘要翻译： 本发明涉及作为β-分泌酶的抑制剂并可用于治疗其中涉及β-分泌酶的疾病如阿尔茨海默病的式（I）的2-氨基咪唑化合物。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗涉及β-分泌酶的疾病中的用途。
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公开(公告)号：US07115651B2
公开(公告)日：2006-10-03
申请号：US09938754
申请日：2001-08-24
申请人： Samuel J. Danishefsky , Robert M. Garbaccio , Daniel K. Baeschlin , Shawn J. Stachel , David Solit , Neal Rosen
发明人： Samuel J. Danishefsky , Robert M. Garbaccio , Daniel K. Baeschlin , Shawn J. Stachel , David Solit , Neal Rosen
IPC分类号： A61P7/00 , A61K31/385 , A61K31/335 , C07D339/00 , C07D313/00
CPC分类号： C07D491/04 , C07D225/06 , C07D313/00 , C07D493/04
摘要： The present invention relates to compounds having the structure (and pharmaceutically acceptable derivatives thereof) wherein R0–R4, Z, X, A—B, D—E, G—J, and K—L are as defined herein, the synthesis thereof and the use of these compounds as therapeutic agents.
摘要翻译： 本发明涉及其中R 0〜R 4，Z，X，AB，DE，GJ和KL的结构（及其药学上可接受的衍生物）的化合物是 如本文所定义，其合成和这些化合物作为治疗剂的用途。
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