公开(公告)号：US07820674B2

公开(公告)日：2010-10-26

申请号：US11795283

申请日：2006-01-13

申请人： Craig A. Coburn ,  Philippe G. Nantermet ,  Hemaka A. Rajapakse ,  Harold G. Selnick ,  Shaun R. Stauffer

发明人： Craig A. Coburn ,  Philippe G. Nantermet ,  Hemaka A. Rajapakse ,  Harold G. Selnick ,  Shaun R. Stauffer

IPC分类号： A61K31/4245 ,  A61K31/496 ,  A61K31/454 ,  A61K31/5377 ,  C07D271/10 ,  C07D271/00 ,  C07D271/06 ,  C07D413/06

CPC分类号： C07D413/06 ,  C07D271/10

摘要： The present invention is directed to aminomethyl 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涉及β-分泌酶的疾病如阿尔茨海默氏病的氨基甲基化合物。 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：US20160297792A1

公开(公告)日：2016-10-13

申请号：US15036268

申请日：2014-11-07

申请人： Craig A. Coburn ,  Milana M. Maletic ,  Yunfu Luo ,  Zhiqi Qi ,  Tingting Yu ,  Richard Soll

发明人： Craig A. Coburn ,  Milana M. Maletic ,  Yunfu Luo ,  Zhiqi Qi ,  Tingting Yu ,  Richard Soll

IPC分类号： C07D401/06 ,  C07D417/14 ,  C07D405/14 ,  C07D413/14 ,  A61K31/4545 ,  A61K45/06 ,  A61K31/4178 ,  C07D403/06 ,  A61K31/551 ,  C07D471/10 ,  A61K31/541 ,  A61K31/454 ,  C07D401/14

摘要： The present invention relates to piperidine or piperazine linked imidazole and triazole derivatives, compositions comprising said compounds, alone or in combination with other drugs, and methods of using the compounds for improving the pharmacokinetics of a drug. The compounds of the invention are useful in human and veterinary medicine for inhibiting CYP3A4 and for improving the pharmacokinetics of a therapeutic compound that is metabolized by CYP3A4.

摘要翻译： 本发明涉及哌啶或哌嗪连接的咪唑和三唑衍生物，包含所述化合物单独或与其它药物组合的组合物，以及使用该化合物改善药物药代动力学的方法。 本发明的化合物可用于抑制CYP3A4的人和兽医药物，并且用于改善由CYP3A4代谢的治疗化合物的药代动力学。

公开(公告)号：US08211904B2

公开(公告)日：2012-07-03

申请号：US11487229

申请日：2006-07-14

申请人： Craig A. Coburn ,  Melissa S. Egbertson ,  Samuel L. Graham ,  Georgia B. McGaughey ,  Shaun R. Stauffer ,  Hemaka A. Rajapakse ,  Philippe G. Nantermet ,  Shawn J. Stachel ,  Wenjin Yang ,  Wanli Lu ,  Bruce Fahr

发明人： Craig A. Coburn ,  Melissa S. Egbertson ,  Samuel L. Graham ,  Georgia B. McGaughey ,  Shaun R. Stauffer ,  Hemaka A. Rajapakse ,  Philippe G. Nantermet ,  Shawn J. Stachel ,  Wenjin Yang ,  Wanli Lu ,  Bruce Fahr

IPC分类号： A61K31/438 ,  C07D401/04 ,  C07D403/04

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：US08114887B2

公开(公告)日：2012-02-14

申请号：US11663388

申请日：2005-10-12

申请人： James C. Barrow ,  Craig A. Coburn ,  Melissa S. Egbertson ,  Georgia B. McGaughey ,  Melody A. McWherter ,  Lou Anne Neilson ,  Kenneth E. Rittle ,  Harold G. Selnick ,  Shaun R. Stauffer ,  Zhi-Qiang Yang ,  Wenjin Yang ,  Wanli Lu ,  Bruce Fahr

发明人： James C. Barrow ,  Craig A. Coburn ,  Melissa S. Egbertson ,  Georgia B. McGaughey ,  Melody A. McWherter ,  Lou Anne Neilson ,  Kenneth E. Rittle ,  Harold G. Selnick ,  Shaun R. Stauffer ,  Zhi-Qiang Yang ,  Wenjin Yang ,  Wanli Lu ,  Bruce Fahr

IPC分类号： A61K31/438 ,  C07D411/02

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：US07847100B2

公开(公告)日：2010-12-07

申请号：US11578559

申请日：2005-04-15

申请人： James C. Barrow ,  Georgia B. McGaughey ,  Philippe G. Nantermet ,  Hemaka A. Rajapakse ,  Harold G. Selnick ,  Shaun R. Stauffer ,  Craig A. Coburn

发明人： James C. Barrow ,  Georgia B. McGaughey ,  Philippe G. Nantermet ,  Hemaka A. Rajapakse ,  Harold G. Selnick ,  Shaun R. Stauffer ,  Craig A. Coburn

IPC分类号： A61K31/4245 ,  C07D271/10 ,  C07D271/06

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：US07714021B2

公开(公告)日：2010-05-11

申请号：US11629209

申请日：2005-06-10

申请人： Craig A. Coburn

发明人： Craig A. Coburn

IPC分类号： A61K31/4025 ,  A61K31/40 ,  C07D207/14

CPC分类号： C07D207/14

摘要： The present invention is directed to pyrrolidin-3-yl 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-分泌酶的抑制剂并且可用于治疗涉及β-分泌酶的疾病如阿尔茨海默氏病的吡咯烷-3-基衍生物化合物。 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：US20080161363A1

公开(公告)日：2008-07-03

申请号：US11666942

申请日：2005-10-25

申请人： Craig A. Coburn ,  M. Katharine Holloway ,  Shawn J. Stachel

发明人： Craig A. Coburn ,  M. Katharine Holloway ,  Shawn J. Stachel

IPC分类号： A61K31/4965 ,  A61K31/501

CPC分类号： C07D213/73

摘要： The present invention is directed to 2-aminopyridine 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-氨基吡啶化合物。 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：US5846978A

公开(公告)日：1998-12-08

申请号：US850359

申请日：1997-05-02

申请人： Craig A. Coburn ,  Mark E. Fraley ,  M. Katharine Holloway ,  Randall W. Hungate ,  Kristine Prendergast

发明人： Craig A. Coburn ,  Mark E. Fraley ,  M. Katharine Holloway ,  Randall W. Hungate ,  Kristine Prendergast

IPC分类号： A61K45/06 ,  A61K31/435 ,  C07D221/22

CPC分类号： A61K45/06

摘要： Compounds such as ##STR1## or pharmaceutically acceptable salts thereof, are HIV protease inhibitors. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.