公开(公告)号：US20080015233A1

公开(公告)日：2008-01-17

申请号：US11547994

申请日：2005-04-20

申请人： James Barrow ,  Georgia McGaughey ,  Philippe Nantermet ,  Hemaka Rajapakse ,  Harold Selnick ,  Shaun Stauffer ,  Joseph Vacca ,  Shawn Stachel ,  Craig Coburn ,  Matthew Stanton

发明人： James Barrow ,  Georgia McGaughey ,  Philippe Nantermet ,  Hemaka Rajapakse ,  Harold Selnick ,  Shaun Stauffer ,  Joseph Vacca ,  Shawn Stachel ,  Craig Coburn ,  Matthew Stanton

IPC分类号： A61K31/4439 ,  A61P25/28 ,  C07D401/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04

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。

公开(公告)号：US20070244119A1

公开(公告)日：2007-10-18

申请号：US11578559

申请日：2005-04-15

申请人： James Barrow ,  Georgia McGaughey ,  Philippe Nantermet ,  Hemaka Rajapakse ,  Harold Selnick ,  Shaun Stauffer ,  Craig Coburn

发明人： James Barrow ,  Georgia McGaughey ,  Philippe Nantermet ,  Hemaka Rajapakse ,  Harold Selnick ,  Shaun Stauffer ,  Craig Coburn

IPC分类号： A61K31/4245 ,  A61K31/341 ,  A61K31/433 ,  A61K31/5377 ,  C07D263/30 ,  C07D285/12 ,  C07D413/04 ,  C07D307/02 ,  C07D271/10 ,  C07D253/02 ,  A61K31/4418 ,  A61K31/421

CPC分类号： C07D271/10 ,  C07D249/06 ,  C07D249/08 ,  C07D263/32 ,  C07D263/62 ,  C07D271/06 ,  C07D285/12 ,  C07D307/14 ,  C07D307/42 ,  C07D307/44 ,  C07D307/52 ,  C07D307/54 ,  C07D413/04 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14

摘要： The present invention is directed to 1,3,5-phenyl substituted 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1,3,5-苯基取代的衍生物化合物。 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。

公开(公告)号：US20070021454A1

公开(公告)日：2007-01-25

申请号：US11487229

申请日：2006-07-14

申请人： Craig Coburn ,  Melissa Egbertson ,  Samuel Graham ,  Georgia McGaughey ,  Shaun Stauffer ,  Hemaka Rajapakse ,  Philippe Nantermet ,  Shawn Stachel ,  Wenjin Yang ,  Wanli Lu ,  Bruce Fahr

发明人： Craig Coburn ,  Melissa Egbertson ,  Samuel Graham ,  Georgia McGaughey ,  Shaun Stauffer ,  Hemaka Rajapakse ,  Philippe Nantermet ,  Shawn Stachel ,  Wenjin Yang ,  Wanli Lu ,  Bruce Fahr

IPC分类号： A61K31/4747 ,  C07D471/10

CPC分类号： C07D471/10

摘要： The present invention is directed to spiropiperidine compounds of formula (I) and tautomers thereof, 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： 本发明涉及式（I）的螺哌啶化合物及其互变异构体，其是β-分泌酶的抑制剂，并且其可用于治疗涉及β-分泌酶的疾病，例如阿尔茨海默氏病。 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：US20070197571A1

公开(公告)日：2007-08-23

申请号：US11663388

申请日：2005-10-12

申请人： James Barrow ,  Craig Coburn ,  Melissa Egbertson ,  Georgia McGaughey ,  Melody McWherter ,  Lou Neilson ,  Kenneth Rittle ,  Harold Selnick ,  Shaun Stauffer ,  Zhi-Qiang Yang ,  Wenjin Yang ,  Wanli Lu ,  Bruce Fahr

发明人： James Barrow ,  Craig Coburn ,  Melissa Egbertson ,  Georgia McGaughey ,  Melody McWherter ,  Lou Neilson ,  Kenneth Rittle ,  Harold Selnick ,  Shaun Stauffer ,  Zhi-Qiang Yang ,  Wenjin Yang ,  Wanli Lu ,  Bruce Fahr

IPC分类号： A61K31/4747 ,  C07D471/10

CPC分类号： C07D471/10

摘要： The present invention is directed to spiropiperidine 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-分泌酶的抑制剂并且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）的哌啶哌啶化合物。 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：US20070142634A1

公开(公告)日：2007-06-21

申请号：US10582856

申请日：2004-12-15

申请人： James Barrow ,  Craig Coburn ,  Philippe Nantermet ,  Harold Selnick ,  Shawn Stachel ,  Matthew Stanton ,  Shaun Stauffer ,  Linghang Zhuang ,  Jennifer Davis

发明人： James Barrow ,  Craig Coburn ,  Philippe Nantermet ,  Harold Selnick ,  Shawn Stachel ,  Matthew Stanton ,  Shaun Stauffer ,  Linghang Zhuang ,  Jennifer Davis

IPC分类号： A61K31/5377 ,  C07D417/02 ,  C07D413/02 ,  C07D403/02 ,  C07D213/72

CPC分类号： C07D213/81 ,  C07D213/75 ,  C07D257/04 ,  C07D401/04 ,  C07D409/12 ,  C07D413/12

摘要： The present invention is directed to phenylamide and pyridylamide derivative compounds of 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： 本发明涉及苯酰胺和吡啶酰胺衍生物化合物，其是β-分泌酶的抑制剂，可用于治疗其中涉及β-分泌酶的疾病，例如阿尔茨海默氏病。 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：US20170217940A1

公开(公告)日：2017-08-03

申请号：US15104584

申请日：2014-12-15

申请人： Joseph KOZLOWSKI ,  Craig COBURN ,  Wensheng YU ,  Bin HU ,  Bin ZHONG ,  Jinglai HAO ,  Dahai WANG ,  Tao JI ,  MERCL SHARP & DOHME CORP.

发明人： Joseph Kozlowski ,  Craig Coburn ,  Wensheng Yu ,  Ling Tong ,  Bin Hu ,  Bin Zhong ,  Jinglai Hao ,  Dahai Wang ,  Tao Ji

IPC分类号： C07D405/14 ,  A61K31/4178 ,  A61K31/7072 ,  A61K45/06 ,  A61K31/4985

CPC分类号： C07D405/14 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/4985 ,  A61K31/7072 ,  A61K45/06 ,  C07D493/04 ,  A61K2300/00

摘要： The present invention relates to novel Fused Tetracyclic Heterocyclic Compounds of Formula I: (I), wherein A, A′, R2A, R2B, R7, R8, R9, and R10 are defined herein. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HCV and the prophylaxis, treatment, or delay in the onset of disease caused by HCV. The present invention also relates to pharmaceutical compositions comprising at least one Fused Tetracyclic Heterocyclic Compound, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines, and methods of using the Fused Tetracyclic Heterocyclic Compounds for treating or preventing HCV infection in a patient.

公开(公告)号：US20060052615A1

公开(公告)日：2006-03-09

申请号：US10534291

申请日：2003-11-06

申请人： Craig Coburn ,  Shawn Stachel ,  Joseph Vacca

发明人： Craig Coburn ,  Shawn Stachel ,  Joseph Vacca

IPC分类号： C07D403/02 ,  C07C255/45

CPC分类号： C07D207/08 ,  C07C255/46 ,  C07C255/57 ,  C07C311/08 ,  C07C2601/02 ,  C07C2601/08 ,  C07D211/22 ,  C07D211/32 ,  C07D211/44 ,  C07D211/46 ,  C07D211/74 ,  C07D491/10

摘要： Disclosed are compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment or prevention of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease and pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the beta-secretase enzyme is involved.

摘要翻译： 公开了式（I）的化合物，

公开(公告)号：US06610701B2

公开(公告)日：2003-08-26

申请号：US10071422

申请日：2002-02-08

申请人： James C. Barrow ,  Craig Coburn ,  Harold G. Selnick ,  Phung L. Ngo

发明人： James C. Barrow ,  Craig Coburn ,  Harold G. Selnick ,  Phung L. Ngo

IPC分类号： A61K314375

CPC分类号： C07D213/75 ,  C07D213/26 ,  C07D213/89 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/14 ,  C07D471/04

摘要： Compounds of the invention are useful in inhibiting thrombin and treating blood coagulation and cardiovascular disorders and have the following structure: wherein R3 is hydrogen or halogen, and u is N or CH.

摘要翻译： 本发明化合物可用于抑制凝血酶和治疗凝血和心血管疾病，并具有以下结构：其中R 3为氢或卤素，u为N或CH。

公开(公告)号：US6133297A

公开(公告)日：2000-10-17

申请号：US162752

申请日：1998-09-29

申请人： Craig Coburn ,  Adel M. Naylor-Olsen

发明人： Craig Coburn ,  Adel M. Naylor-Olsen

IPC分类号： C07D213/74 ,  A61K31/44 ,  C07D211/72

CPC分类号： C07D213/74

摘要： A compound which inhibits human thrombin and which has the general structure ##STR1## such as ##STR2##

摘要翻译： 抑制人凝血酶的具有一般结构的化合物

公开(公告)号：US20070202547A1

公开(公告)日：2007-08-30

申请号：US10594835

申请日：2005-03-29

申请人： Craig Coburn ,  Amy Espeseth ,  Daria Hazuda

发明人： Craig Coburn ,  Amy Espeseth ,  Daria Hazuda

IPC分类号： G01N33/542

CPC分类号： G01N33/6896 ,  C07D307/79 ,  C07D405/12 ,  G01N2333/4709 ,  G01N2500/00

摘要： Disclosed are methods for identifying and evaluating the binding properties of substances to the amyoid precursor protein (APP) or to β-amyloid (Aβ fragments of APP. Also disclosed is a class of benzofuran derivatives of formula (I), which interact specifically with APP or Aβ, and block interaction of APP or Aβ with secreatase or APP or Aβ binding antibodies.

摘要翻译： 公开了用于鉴定和评价物质与淀粉样前体蛋白（APP）或β-淀粉样蛋白（APP的Aβ片段）的结合性质的方法。还公开了一类与APP特异性相互作用的式（I）的苯并呋喃衍生物 或Abeta，并阻断APP或Abeta与分泌或APP或Abeta结合抗体的相互作用。