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。

公开(公告)号：US06867305B2

公开(公告)日：2005-03-15

申请号：US09796959

申请日：2001-03-01

申请人： Samuel J. Danishefsky ,  Shawn J. Stachel ,  Chul Bom Lee ,  Mark D. Chappell ,  Zhical Wu

发明人： Samuel J. Danishefsky ,  Shawn J. Stachel ,  Chul Bom Lee ,  Mark D. Chappell ,  Zhical Wu

IPC分类号： A61K31/337 ,  A61K31/475 ,  A61K45/06 ,  C07D277/30 ,  C07D417/06 ,  C07D263/32

CPC分类号： C07D417/06 ,  A61K31/337 ,  A61K31/475 ,  A61K45/06 ,  A61K2300/00

摘要： The present invention provides convergent processes for preparing epothilones, desoxyepothilones, and analogues thereof. The present invention further provides novel compositions and methods for the treatment of cancer and additionally provides methods for the treatment of cancer which has developed a multi-drug phenotype.

摘要翻译： 本发明提供用于制备埃坡霉素，脱氧头孢烯酮及其类似物的收敛方法。 本发明还提供了用于治疗癌症的新型组合物和方法，并且另外提供了治疗已发展成多种药物表型的癌症的方法。

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。

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。

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。

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：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：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。

公开(公告)号：US08354545B2

公开(公告)日：2013-01-15

申请号：US12747605

申请日：2008-12-10

申请人： Shawn J. Stachel ,  Thomas Steele ,  Alessia Petrocchi

发明人： Shawn J. Stachel ,  Thomas Steele ,  Alessia Petrocchi

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。

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。