公开(公告)号：US20110021516A1

公开(公告)日：2011-01-27

申请号：US12934208

申请日：2009-03-24

申请人： Harold G. Selnick ,  Ian M. Bell ,  Melody McWherter ,  Donnette D. Staas ,  Shawn J. Stachel ,  Thomas Steele ,  Craig Stump ,  Michael R. Wood ,  C. Blair Zartman

发明人： Harold G. Selnick ,  Ian M. Bell ,  Melody McWherter ,  Donnette D. Staas ,  Shawn J. Stachel ,  Thomas Steele ,  Craig Stump ,  Michael R. Wood ,  C. Blair Zartman

IPC分类号： A61K31/5365 ,  C07D471/04 ,  A61K31/496 ,  A61P25/06

CPC分类号： C07D471/10 ,  C07D403/06 ,  C07D471/20 ,  C07D519/00

摘要： The present invention is directed to compounds of the formula (I): (wherein variables A1, A2, A3, A4, A5, A6, A7, A8, G1, G2, G3, G4, J, Q, Ea, Eb, Ec, R6, R7, RPG and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. 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 CGRP is involved.

摘要翻译： 本发明涉及式（I）的化合物：（其中变量A1，A2，A3，A4，A5，A6，A7，A8，G1，G2，G3，G4，J，Q，Ea，Eb，Ec ，R6，R7，RPG和Y如本文所述），其是CGRP受体的拮抗剂，其可用于治疗或预防涉及CGRP的疾病，例如偏头痛。 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CGRP的疾病中的用途。

公开(公告)号：US07829597B2

公开(公告)日：2010-11-09

申请号：US10573232

申请日：2004-09-29

申请人： Philippe G. Nantermet ,  Hemaka Anthony Rajapakse ,  Harold G. Selnick

发明人： Philippe G. Nantermet ,  Hemaka Anthony Rajapakse ,  Harold G. Selnick

IPC分类号： C07C15/12 ,  C07C13/48 ,  A61K31/135

CPC分类号： C07D213/81 ,  C07C255/57 ,  C07C311/08 ,  C07C2601/02 ,  C07D207/06 ,  C07D207/08 ,  C07D213/76 ,  C07D295/192 ,  C07D333/20 ,  C07D405/04

摘要： The present invention is directed to 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）化合物，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：US20090247514A1

公开(公告)日：2009-10-01

申请号：US12085057

申请日：2006-11-14

申请人： Ian M. Bell ,  Harold G. Selnick ,  Michael R. Wood ,  Cory R. Theberge ,  Craig A. Stump ,  Steven N. Gallicchio ,  C. Blair Zartman

发明人： Ian M. Bell ,  Harold G. Selnick ,  Michael R. Wood ,  Cory R. Theberge ,  Craig A. Stump ,  Steven N. Gallicchio ,  C. Blair Zartman

IPC分类号： A61K31/5377 ,  C07D471/10 ,  A61K31/438 ,  A61K31/497 ,  A61P25/00

CPC分类号： C07D471/20 ,  C07D519/00

摘要： Compounds of formula I: (wherein variables A1, A2, A3, A4, A5, A6, A7, E1, E2, E3, E4, E5, G1, G2, J and K are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 CGRP is involved.

摘要翻译： 式I化合物（其中变量A1，A2，A3，A4，A5，A6，A7，E1，E2，E3，E4，E5，G1，G2，J和K如本文所述），其是CGRP受体的拮抗剂 并且其可用于治疗或预防涉及CGRP的疾病，例如偏头痛。 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CGRP的疾病中的用途。

公开(公告)号：US20080318927A1

公开(公告)日：2008-12-25

申请号：US12214460

申请日：2008-06-19

申请人： Michael R. Wood ,  Steven N. Gallicchio ,  Harold G. Selnick ,  C. Blair Zartman ,  Ian M. Bell ,  Craig A. Stump

发明人： Michael R. Wood ,  Steven N. Gallicchio ,  Harold G. Selnick ,  C. Blair Zartman ,  Ian M. Bell ,  Craig A. Stump

IPC分类号： A61K31/551 ,  A61K31/454 ,  C07D401/12 ,  A61K31/541 ,  A61P25/06 ,  A61K31/501 ,  A61K31/496 ,  C07D417/12 ,  C07D471/04

CPC分类号： C07D401/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D471/20 ,  C07D519/00

摘要： Compounds of formula I: (wherein variables A1, A2, A2, A4, m, n, J, Q, R4, Ea, Eb, Ec, R6, R7, Re, Rf, RPG and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 CGRP is involved.

摘要翻译： 式I化合物（其中变量A1，A2，A2，A4，m，n，J，Q，R4，Ea，Eb，Ec，R6，R7，Re，Rf，RPG和Y如本文所述） CGRP受体的拮抗剂，其可用于治疗或预防涉及CGRP的疾病，例如偏头痛。 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CGRP的疾病中的用途。

公开(公告)号：US20080269302A1

公开(公告)日：2008-10-30

申请号：US11667913

申请日：2005-11-14

申请人： Philippe G. Nantermet ,  Hemaka A. Rajapakse ,  Harold G. Selnick ,  Stacey Lindsley ,  Keith P. Moore ,  Shawn J. Stachel

发明人： Philippe G. Nantermet ,  Hemaka A. Rajapakse ,  Harold G. Selnick ,  Stacey Lindsley ,  Keith P. Moore ,  Shawn J. Stachel

IPC分类号： A61K31/365 ,  C07D267/00 ,  C07D313/00 ,  A61K31/395 ,  A61P25/28 ,  C07D498/00 ,  C07D321/00

CPC分类号： C07D273/01 ,  C07D267/00 ,  C07D313/00 ,  C07D321/00 ,  C07D323/00 ,  C07D413/04 ,  C07D498/08

摘要： The present invention is directed to macrocyclic tertiary amine compounds represented by general 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： 本发明涉及由通式（I）表示的大环叔胺化合物，其为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：US20080153846A1

公开(公告)日：2008-06-26

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： A61K31/496 ,  C07C211/00 ,  A61K31/13 ,  A61K31/4245 ,  A61P25/28 ,  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：US07084134B2

公开(公告)日：2006-08-01

申请号：US10427435

申请日：2003-05-01

申请人： James C. Barrow ,  Philippe G. Nantermet ,  Harold G. Selnick

发明人： James C. Barrow ,  Philippe G. Nantermet ,  Harold G. Selnick

IPC分类号： A61K38/00

CPC分类号： C07K5/12 ,  A61K38/00 ,  A61K38/55

摘要： Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof.

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：US06462050B1

公开(公告)日：2002-10-08

申请号：US09916745

申请日：2001-07-27

申请人： Richard C. Isaacs ,  Kellie Cutrona ,  James C. Barrow ,  Harold G. Selnick

发明人： Richard C. Isaacs ,  Kellie Cutrona ,  James C. Barrow ,  Harold G. Selnick

IPC分类号： A61K31497

CPC分类号： C07D401/12 ,  A61K38/00 ,  C07D401/14 ,  C07K5/06191

摘要： Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure:

公开(公告)号：US09701693B2

公开(公告)日：2017-07-11

申请号：US14129169

申请日：2012-06-27

申请人： Tong-Shuang Li ,  Ernest J. Mceachern ,  David J. Vocadlo ,  Yuanxi Zhou ,  Yongbao Zhu ,  Harold G. Selnick

发明人： Tong-Shuang Li ,  Ernest J. Mceachern ,  David J. Vocadlo ,  Yuanxi Zhou ,  Yongbao Zhu ,  Harold G. Selnick

IPC分类号： C07D513/00 ,  C07D513/04 ,  C07H9/06 ,  C12Q1/37 ,  C12Q1/34

CPC分类号： C07D513/04 ,  C07H9/06 ,  C12Q1/34 ,  C12Q1/37 ,  G01N2333/924 ,  G01N2500/04

摘要： The invention provides compounds for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.