公开(公告)号：US20100298342A1

公开(公告)日：2010-11-25

申请号：US12310573

申请日：2007-09-04

申请人： Melissa S. Egbertson ,  Shaun R. Stauffer ,  Craig A. Coburn ,  James C. Barrow ,  Lou Anne Neilson ,  Jenny M. Wai ,  Wenjin Yang ,  Wanli Lu ,  Bruce Fahr

发明人： Melissa S. Egbertson ,  Shaun R. Stauffer ,  Craig A. Coburn ,  James C. Barrow ,  Lou Anne Neilson ,  Jenny M. Wai ,  Wenjin Yang ,  Wanli Lu ,  Bruce Fahr

IPC分类号： A61K31/438 ,  C07D471/10 ,  A61K31/497 ,  A61P25/28

CPC分类号： C07D471/10 ,  C07D498/10

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：US07550481B2

公开(公告)日：2009-06-23

申请号：US10582856

申请日：2004-12-15

申请人： James C. Barrow ,  Craig A. Coburn ,  Philippe G. Nantermet ,  Harold G. Selnick ,  Shawn J. Stachel ,  Matthew G. Stanton ,  Shaun R. Stauffer ,  Linghang Zhuang ,  Jennifer R. Davis

发明人： James C. Barrow ,  Craig A. Coburn ,  Philippe G. Nantermet ,  Harold G. Selnick ,  Shawn J. Stachel ,  Matthew G. Stanton ,  Shaun R. Stauffer ,  Linghang Zhuang ,  Jennifer R. Davis

IPC分类号： C07D401/02 ,  A61K31/44

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：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。

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：US20100093811A1

公开(公告)日：2010-04-15

申请号：US12523200

申请日：2008-09-22

申请人： Craig A. Coburn ,  Joseph P. Vacca ,  Hemaka A. Rajapakse ,  Kristen L.G. Jones ,  Philippe Nantermet ,  James C. Barrow ,  Keith P. Moore ,  Steven S. Sharik ,  Cory Theberge ,  Abbas M. Walji

发明人： Craig A. Coburn ,  Joseph P. Vacca ,  Hemaka A. Rajapakse ,  Kristen L.G. Jones ,  Philippe Nantermet ,  James C. Barrow ,  Keith P. Moore ,  Steven S. Sharik ,  Cory Theberge ,  Abbas M. Walji

IPC分类号： A61K31/44 ,  C07C311/15 ,  A61K31/18 ,  C07C271/06 ,  A61K31/27 ,  C07D277/62 ,  A61K31/426 ,  C07D213/55 ,  A61P31/18

CPC分类号： C07C311/41 ,  C07C311/18 ,  C07C311/29 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2603/32 ,  C07D213/30 ,  C07D277/64

摘要： Compounds of Formula I are disclosed: (I), wherein XA, k, R1, R2, R3, R4, R5, R5A, R6, R6A, R7 and R8 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

摘要翻译： 公开了式I的化合物：其中XA，k，R1，R2，R3，R4，R5，R5A，R6，R6A，R7和R8如本文所定义。 式I所包括的化合物包括可以在体内代谢为HIV蛋白酶抑制剂的HIV蛋白酶抑制剂和其它化合物的化合物。 化合物及其药学上可接受的盐可用于预防或治疗HIV感染以及预防，治疗或延迟艾滋病的发病。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。

公开(公告)号：US08389720B2

公开(公告)日：2013-03-05

申请号：US13127898

申请日：2009-11-03

申请人： James C. Barrow ,  Mark T. Bilodeau ,  Christopher D. Cox ,  John C. Hartnett ,  Nathan R. Kett ,  Yiwei Li ,  Peter J. Manley ,  Jeffrey Melamed ,  William D. Shipe ,  B. Wesley Trotter ,  Amy Zartman

发明人： James C. Barrow ,  Mark T. Bilodeau ,  Christopher D. Cox ,  John C. Hartnett ,  Nathan R. Kett ,  Yiwei Li ,  Peter J. Manley ,  Jeffrey Melamed ,  William D. Shipe ,  B. Wesley Trotter ,  Amy Zartman

IPC分类号： A61K31/551 ,  A61K31/5355 ,  A61K31/497 ,  A61K31/519 ,  A61K31/4412 ,  A61K31/4704 ,  C07D243/08 ,  C07D413/14 ,  C07D471/04 ,  C07D401/14 ,  C07D401/12 ,  C07D405/14

CPC分类号： A61K31/47 ,  C07D401/12 ,  C07D405/12

摘要： The present invention is directed to quinolone compounds which are antagonists of neuropeptide S receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which the neuropeptide S receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the neuropeptide S receptor is involved.

摘要翻译： 本发明涉及作为神经肽S受体的拮抗剂的喹诺酮化合物，其可用于治疗或预防神经和精神疾病以及涉及神经肽S受体的疾病。 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预防或治疗涉及神经肽S受体的疾病中的用途。

公开(公告)号：US20110212946A1

公开(公告)日：2011-09-01

申请号：US13127898

申请日：2009-11-03

申请人： James C. Barrow ,  Mark T. Bilodeau ,  Christopher D. Cox ,  John C. Hartnett ,  Nathan R. Kett ,  Yiwei Li ,  Peter J. Manley ,  Jeffrey Melamed ,  William D. Shipe ,  B. Wesley Trotter ,  Amy Zartman

发明人： James C. Barrow ,  Mark T. Bilodeau ,  Christopher D. Cox ,  John C. Hartnett ,  Nathan R. Kett ,  Yiwei Li ,  Peter J. Manley ,  Jeffrey Melamed ,  William D. Shipe ,  B. Wesley Trotter ,  Amy Zartman

IPC分类号： A61K31/4704 ,  C07D405/14 ,  A61K31/496 ,  A61K31/55 ,  C07D401/12 ,  A61K31/4709 ,  C07D413/12 ,  A61K31/5377 ,  C07D215/227 ,  A61P25/00

CPC分类号： A61K31/47 ,  C07D401/12 ,  C07D405/12

摘要： The present invention is directed to quinolone compounds which are antagonists of neuropeptide S receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which the neuropeptide S receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the neuropeptide S receptor is involved.

摘要翻译： 本发明涉及作为神经肽S受体的拮抗剂的喹诺酮化合物，其可用于治疗或预防神经和精神疾病以及涉及神经肽S受体的疾病。 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预防或治疗涉及神经肽S受体的疾病中的用途。

公开(公告)号：US08003653B2

公开(公告)日：2011-08-23

申请号：US12085174

申请日：2006-11-10

申请人： James C. Barrow ,  Kenneth E. Rittle ,  Phung Le Bondiskey

发明人： James C. Barrow ,  Kenneth E. Rittle ,  Phung Le Bondiskey

IPC分类号： A61K31/496 ,  A61K31/4439 ,  A61K31/4166 ,  C07D403/12 ,  C07D401/12 ,  C07D235/02 ,  C07D233/32

CPC分类号： C07D233/32 ,  C07D401/12 ,  C07D403/12 ,  C07D405/06 ,  C07D491/107

摘要： The present invention is directed to imidazolidinone 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其中涉及β-分泌酶的疾病如阿尔茨海默氏病的咪唑啉酮化合物。 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。