公开(公告)号：US20180325898A1

公开(公告)日：2018-11-15

申请号：US16042206

申请日：2018-07-23

Applicant: Paul S. Charifson ,  Kevin Michael Cottrell ,  Hongbo Deng ,  John P. Duffy ,  Huai Gao ,  Simon Giroux ,  Jeremy Green ,  Katrina Lee Jackson ,  Joseph M. Kennedy ,  David J. Lauffer ,  Mark Willem Ledeboer ,  Pan Li ,  John Patrick Maxwell ,  Mark A. Morris ,  Albert Charles Pierce ,  Nathan D. Waal ,  Jinwang Xu

Inventor： Paul S. Charifson ,  Kevin Michael Cottrell ,  Hongbo Deng ,  John P. Duffy ,  Huai Gao ,  Simon Giroux ,  Jeremy Green ,  Katrina Lee Jackson ,  Joseph M. Kennedy ,  David J. Lauffer ,  Mark Willem Ledeboer ,  Pan Li ,  John Patrick Maxwell ,  Mark A. Morris ,  Albert Charles Pierce ,  Nathan D. Waal ,  Jinwang Xu

IPC: A61K31/506 ,  A61K9/48 ,  C07D417/10 ,  A61K41/00 ,  C07D521/00 ,  C07D495/04 ,  C07D491/056 ,  C07D491/048 ,  C07D471/04 ,  C07D417/14 ,  C07D417/04 ,  C07D413/10 ,  C07D413/04 ,  C07D409/14 ,  C07D409/04 ,  C07D239/42 ,  C07D403/10 ,  C07D403/04 ,  C07D401/04 ,  C07D413/14 ,  C07D405/14 ,  C07D401/14 ,  A61K47/55 ,  A61K31/53 ,  A61K47/54 ,  A61K31/5377 ,  A61K9/20

CPC classification number: C07D401/14 ,  A61K9/20 ,  A61K9/48 ,  A61K31/506 ,  A61K31/53 ,  A61K31/5377 ,  A61K41/0038 ,  A61K47/545 ,  A61K47/55 ,  C07D239/42 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D413/10 ,  C07D413/14 ,  C07D417/04 ,  C07D417/10 ,  C07D417/14 ,  C07D471/04 ,  C07D491/048 ,  C07D491/056 ,  C07D495/04 ,  C07D521/00

Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

公开(公告)号：US07795245B2

公开(公告)日：2010-09-14

申请号：US12001043

申请日：2007-12-07

Applicant: Christoph Steeneck ,  Christian Gege ,  Frank Richter ,  Heiko Kroth ,  Matthias Hochgurtel ,  Michael Essors ,  Joshua Van Veldhuizen ,  Bert Nolte ,  Brian M. Gallagher, Jr. ,  Tim Feuerstein ,  Matthias Schneider ,  Torsten Arndt ,  Hongbo Deng ,  Ralf Biesinger ,  Xinyuan Wu ,  Harald Bluhm ,  Irving Sucholeiki ,  Arthur G. Taveras

Inventor： Christoph Steeneck ,  Christian Gege ,  Frank Richter ,  Heiko Kroth ,  Matthias Hochgurtel ,  Michael Essors ,  Joshua Van Veldhuizen ,  Bert Nolte ,  Brian M. Gallagher, Jr. ,  Tim Feuerstein ,  Matthias Schneider ,  Torsten Arndt ,  Hongbo Deng ,  Ralf Biesinger ,  Xinyuan Wu ,  Harald Bluhm ,  Irving Sucholeiki ,  Arthur G. Taveras

IPC: A61K31/397 ,  A61K31/519 ,  A61K31/535 ,  A01N43/90 ,  C07D487/00 ,  C07D413/00

CPC classification number: C07D487/04

Abstract: The present invention relates generally to amide group containing pharmaceutical agents, and in particular, to amide containing heterobicyclic metalloprotease inhibitor compounds having the following formulas: wherein R1, R2, R3, and R4 are as defined in the specification. More particularly, the present invention provides a new class of heterobicyclic MMP-13 inhibiting and MMP-3 inhibiting compounds amide containing heterobicyclic compounds, that exhibit an increased potency in relation to currently known MMP-13 and MMP-3 inhibitors.

Abstract translation: 本发明一般涉及含酰胺基的药剂，特别涉及具有下式的含酰胺的杂双环金属蛋白酶抑制剂化合物：其中R1，R2，R3和R4如说明书中所定义。 更具体地，本发明提供了一类新型的杂双环MMP-13抑制和MMP-3抑制化合物，其含有杂双环化合物的酰胺，其与当前已知的MMP-13和MMP-3抑制剂相比具有增强的效力。

公开(公告)号：US20080207607A1

公开(公告)日：2008-08-28

申请号：US11986603

申请日：2007-11-20

Applicant: Christian Gege ,  Carine Chevrier ,  Matthias Schneider ,  Harald Bluhm ,  Matthias Hochgurtel ,  Hongbo Deng ,  Brian M. Gallagher ,  Irving Sucholeiki ,  Arthur Taveras

Inventor： Christian Gege ,  Carine Chevrier ,  Matthias Schneider ,  Harald Bluhm ,  Matthias Hochgurtel ,  Hongbo Deng ,  Brian M. Gallagher ,  Irving Sucholeiki ,  Arthur Taveras

IPC: A61K31/538 ,  C07D265/36 ,  C07D217/00 ,  A61K31/4725 ,  A61K31/541 ,  A61P29/00 ,  A61K31/519 ,  C07D239/00 ,  C07D417/14

CPC classification number: C07D495/04 ,  C07D239/88 ,  C07D401/12 ,  C07D413/12 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D495/14 ,  C07D495/22 ,  C07D498/04 ,  C07D513/04

Abstract: The present invention relates generally to azatriocyclic containing pharmaceutical agents, and in particular, to azatricyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of azatricyclic MMP-3, MMP-8 and/or MMP-13 inhibiting compounds, that exhibit an increased potency and selectivity in relation to currently known MMP-13, MMP-8 and MMP-3 inhibitors.

Abstract translation: 本发明一般涉及含有三氮杂环的药物，尤其涉及氮杂三环金属蛋白酶抑制化合物。 更具体地说，本发明提供了一类新型的azatricyclic MMP-3，MMP-8和/或MMP-13抑制化合物，其与当前已知的MMP-13，MMP-8和MMP- 3抑制剂。

公开(公告)号：US20120015920A1

公开(公告)日：2012-01-19

申请号：US13163457

申请日：2011-06-17

Applicant: Christoph Steeneck ,  Christian Gege ,  Frank Richter ,  Heiko Kroth ,  Matthias Hochgürtel ,  Michael Essers ,  Joshua van Veldhuizen ,  Bert Nolte ,  Brian M. Gallagher, JR. ,  Tim Feuerstein ,  Matthias Schneider ,  Torsten Arndt ,  Hongbo Deng ,  Ralf Biesinger ,  Xinyuan Wu ,  Harald Bluhm ,  Irving Sucholeiki ,  Arthur G. Taveras

Inventor： Christoph Steeneck ,  Christian Gege ,  Frank Richter ,  Heiko Kroth ,  Matthias Hochgürtel ,  Michael Essers ,  Joshua van Veldhuizen ,  Bert Nolte ,  Brian M. Gallagher, JR. ,  Tim Feuerstein ,  Matthias Schneider ,  Torsten Arndt ,  Hongbo Deng ,  Ralf Biesinger ,  Xinyuan Wu ,  Harald Bluhm ,  Irving Sucholeiki ,  Arthur G. Taveras

IPC: A61K31/56 ,  A61K31/519 ,  A61K31/538 ,  A61P29/00 ,  A61P19/02 ,  A61P35/00 ,  A61P9/10 ,  A61P11/00 ,  A61P25/00 ,  A61P27/02 ,  A61P31/04 ,  A61P7/02 ,  A61P25/16 ,  A61P25/28 ,  A61P31/18 ,  C12N9/99 ,  C07D487/04

CPC classification number: C07D487/04

Abstract: The present invention relates generally to amide group containing pharmaceutical agents, and in particular, to amide containing heterobicyclic metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of heterobicyclic MMP-13 inhibiting and MMP-3 inhibiting compounds, that exhibit an increased potency in relation to currently known MMP-13 and MMP-3 inhibitors.

Abstract translation: 本发明一般涉及含酰胺基的药剂，特别涉及含酰胺的杂双环金属蛋白酶抑制剂化合物。 更具体地，本发明提供了一类新型的杂双环MMP-13抑制和MMP-3抑制化合物，其与当前已知的MMP-13和MMP-3抑制剂相比具有增强的效力。

公开(公告)号：US20080261968A1

公开(公告)日：2008-10-23

申请号：US11986626

申请日：2007-11-20

Applicant: Christian Gege ,  Matthias Schneider ,  Carine Chevrier ,  Hongbo Deng ,  Irving Sucholeiki ,  Brian M. Gallagher ,  Michael Bosies ,  Christoph Steeneck ,  Xinyuan Wu ,  Matthias Hochgurtel ,  Bert Nolte ,  Arthur Taveras

Inventor： Christian Gege ,  Matthias Schneider ,  Carine Chevrier ,  Hongbo Deng ,  Irving Sucholeiki ,  Brian M. Gallagher ,  Michael Bosies ,  Christoph Steeneck ,  Xinyuan Wu ,  Matthias Hochgurtel ,  Bert Nolte ,  Arthur Taveras

IPC: A61K31/5375 ,  C07D239/72 ,  A61K31/517 ,  A61K31/52 ,  C07D413/02 ,  A61P19/02 ,  A61K31/519 ,  C07D473/00 ,  C07D495/04

CPC classification number: C07D495/04 ,  C07D239/88 ,  C07D401/12 ,  C07D413/12 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D495/14 ,  C07D495/22 ,  C07D498/04 ,  C07D513/04

Abstract: The present invention relates generally to azabicyclic containing pharmaceutical agents, and in particular, to azabicyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of azabicyclic MMP-3, MMP-8 and/or MMP-13 inhibiting compounds, which exhibit an increased potency and selectivity in relation to currently known MMP-13, MMP-8 and MMP-3 inhibitors.

Abstract translation: 本发明一般涉及含有氮杂双环的药物，特别涉及氮杂双环金属蛋白酶抑制化合物。 更具体地说，本发明提供了一类新的氮杂双环MMP-3，MMP-8和/或MMP-13抑制化合物，其相对于目前已知的MMP-13，MMP-8和MMP- 3抑制剂。

公开(公告)号：US20080161300A1

公开(公告)日：2008-07-03

申请号：US12001041

申请日：2007-12-07

Applicant: Christoph Steeneck ,  Christian Gege ,  Frank Richter ,  Heiko Kroth ,  Matthias Hochgurtel ,  Michael Essers ,  Joshua Van Veldhuizen ,  Bert Nolte ,  Brian Gallagher ,  Tim Feuerstein ,  Matthias Schneider ,  Torsten Arndt ,  Hongbo Deng ,  Ralf Beisinger ,  Xinyuan Wu ,  Harald Bluhm ,  Irving Sucholeiki ,  Arthur Taveras

Inventor： Christoph Steeneck ,  Christian Gege ,  Frank Richter ,  Heiko Kroth ,  Matthias Hochgurtel ,  Michael Essers ,  Joshua Van Veldhuizen ,  Bert Nolte ,  Brian Gallagher ,  Tim Feuerstein ,  Matthias Schneider ,  Torsten Arndt ,  Hongbo Deng ,  Ralf Beisinger ,  Xinyuan Wu ,  Harald Bluhm ,  Irving Sucholeiki ,  Arthur Taveras

IPC: A61K31/536 ,  A61K31/519 ,  C07D265/36 ,  C07D487/04

CPC classification number: C07D487/04

Abstract: The present invention relates generally to amide group containing pharmaceutical agents, and in particular, to amide containing heterobicyclic metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of heterobicyclic MMP-13 inhibiting and MMP-3 inhibiting compounds, that exhibit an increased potency in relation to currently known MMP-13 and MMP-3 inhibitors.

Abstract translation: 本发明一般涉及含酰胺基的药剂，特别涉及含酰胺的杂双环金属蛋白酶抑制剂化合物。 更具体地，本发明提供了一类新型的杂双环MMP-13抑制和MMP-3抑制化合物，其与当前已知的MMP-13和MMP-3抑制剂相比具有增强的效力。

公开(公告)号：US20060173183A1

公开(公告)日：2006-08-03

申请号：US11324037

申请日：2005-12-30

Applicant: Timothy Powers ,  Christoph Steeneck ,  Ralf Biesinger ,  Harald Bluhm ,  Hongbo Deng ,  Rory Dodd ,  Brian Gallagher ,  Christian Gege ,  Matthias Hochgurtel ,  Andrew Kiely ,  Frank Richter ,  Matthias Schneider ,  Irving Sucholeiki ,  Joshua Van Veldhuizen ,  Xinyuan Wu ,  Arthur Taveras

Inventor： Timothy Powers ,  Christoph Steeneck ,  Ralf Biesinger ,  Harald Bluhm ,  Hongbo Deng ,  Rory Dodd ,  Brian Gallagher ,  Christian Gege ,  Matthias Hochgurtel ,  Andrew Kiely ,  Frank Richter ,  Matthias Schneider ,  Irving Sucholeiki ,  Joshua Van Veldhuizen ,  Xinyuan Wu ,  Arthur Taveras

IPC: C07D417/02 ,  C07D403/02 ,  C07D413/02

CPC classification number: C07D239/28 ,  C07D239/30 ,  C07D239/42 ,  C07D239/70 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

Abstract: The present invention relates generally to bis-amide group containing pharmaceutical agents, and in particular, to multicyclic bis-amide MMP-13 inhibitor compounds. More particularly, the present invention provides a new class of MMP-13 inhibiting compounds, containing a pyrimidinyl bis-amide group in combination with a heterocyclic moiety, that exhibit an increased potency and solubility in relation to currently known bis-amide group containing MMP-13 inhibitors.

Abstract translation: 本发明一般涉及含有双酰胺基团的药物，特别涉及多元双酰胺MMP-13抑制剂化合物。 更具体地，本发明提供了一类新的MMP-13抑制化合物，其包含与杂环部分组合的嘧啶基双酰胺基团，其相对于目前已知的含有MMP-1的双酰胺基团显示增加的效力和溶解度， 13抑制剂。

公开(公告)号：US20100249102A1

公开(公告)日：2010-09-30

申请号：US12755326

申请日：2010-04-06

Applicant: Christian Gege ,  Carine Chevrier ,  Matthias Schneider ,  Harald Bluhm ,  Matthias Hochgürtel ,  Hongbo Deng ,  Brian M. Gallagher, JR. ,  Irving Sucholeiki ,  Arthur Taveras

Inventor： Christian Gege ,  Carine Chevrier ,  Matthias Schneider ,  Harald Bluhm ,  Matthias Hochgürtel ,  Hongbo Deng ,  Brian M. Gallagher, JR. ,  Irving Sucholeiki ,  Arthur Taveras

IPC: A61K31/519 ,  A61K31/55 ,  A61K31/538 ,  C07D495/14 ,  C07D495/04 ,  C07D495/22 ,  A61P9/10 ,  A61P19/02 ,  A61P29/00

CPC classification number: C07D495/04 ,  C07D239/88 ,  C07D401/12 ,  C07D413/12 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D495/14 ,  C07D495/22 ,  C07D498/04 ,  C07D513/04

Abstract: The present invention relates generally to azatriocyclic containing pharmaceutical agents, and in particular, to azatricyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of azatricyclic MMP-3, MMP-8 and/or MMP-13 inhibiting compounds, that exhibit an increased potency and selectivity in relation to currently known MMP-13, MMP-8 and MMP-3 inhibitors.

公开(公告)号：US20080176870A1

公开(公告)日：2008-07-24

申请号：US11986622

申请日：2007-11-20

Applicant: Bert Nolte ,  Irving Sucholeiki ,  Tim Feuerstein ,  Brian M. Gallagher ,  Xinyuan Wu ,  Christoph Steeneck ,  Christian Gege ,  Hongbo Deng ,  Joshua Van Veldhuizen ,  Arthur Taveras

Inventor： Bert Nolte ,  Irving Sucholeiki ,  Tim Feuerstein ,  Brian M. Gallagher ,  Xinyuan Wu ,  Christoph Steeneck ,  Christian Gege ,  Hongbo Deng ,  Joshua Van Veldhuizen ,  Arthur Taveras

IPC: A61K31/495 ,  C07D487/04 ,  A61P19/02 ,  A61P29/00 ,  A61P9/10

CPC classification number: C07D487/04

Abstract: The present invention relates generally to heterobicyclic containing pharmaceutical agents, and in particular, to heterobicyclic metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of heterobicyclic metalloprotease inhibiting compounds that exhibit an increased potency in relation to currently known metalloprotease inhibitors.

Abstract translation: 本发明一般涉及含杂环的药物，特别是涉及杂双环金属蛋白酶抑制剂化合物。 更具体地，本发明提供了一类新型的杂双环金属蛋白酶抑制化合物，其与当前已知的金属蛋白酶抑制剂相比表现出增加的效力。

公开(公告)号：US20210040092A1

公开(公告)日：2021-02-11

申请号：US17083569

申请日：2020-10-29

Applicant: Paul S. Charifson ,  Michael P. Clark ,  Upal K. Bandarage ,  Randy S. Bethiel ,  Michael J. Boyd ,  Ioana Davies ,  Hongbo Deng ,  John P. Duffy ,  Luc J. Farmer ,  Huai Gao ,  Wenxin Gu ,  Joseph M. Kennedy ,  Brain Ledford ,  Mark W. Ledeboer ,  Francois Maltais ,  Emanuele Perola ,  Tiansheng Wang

Inventor： Paul S. Charifson ,  Michael P. Clark ,  Upal K. Bandarage ,  Randy S. Bethiel ,  Michael J. Boyd ,  Ioana Davies ,  Hongbo Deng ,  John P. Duffy ,  Luc J. Farmer ,  Huai Gao ,  Wenxin Gu ,  Joseph M. Kennedy ,  Brain Ledford ,  Mark W. Ledeboer ,  Francois Maltais ,  Emanuele Perola ,  Tiansheng Wang

IPC: C07D471/04 ,  A61K31/506 ,  A61K45/06 ,  C07F9/6561 ,  A61K31/215 ,  A61K31/351 ,  A61K31/444 ,  A61K31/497

Abstract: Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.