公开(公告)号：US08481538B2

公开(公告)日：2013-07-09

申请号：US12441187

申请日：2007-09-18

Applicant: Alexander Aronov ,  Jon Come ,  John Court ,  David Deininger ,  David Lauffer ,  Pan Li ,  Kira McGinty ,  Suganthini Nanthakumar ,  Dean Stamos ,  Kirk Tanner

Inventor： Alexander Aronov ,  Jon Come ,  John Court ,  David Deininger ,  David Lauffer ,  Pan Li ,  Kira McGinty ,  Suganthini Nanthakumar ,  Dean Stamos ,  Kirk Tanner

IPC: A61K31/5025 ,  C07D487/04 ,  A61P35/00 ,  A61P9/10

CPC classification number: C07D497/04 ,  C07D513/04

Abstract: The present invention provides compounds useful as inhibitors of c-Met tyrosine kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various proliferative disorders.

Abstract translation: 本发明提供了可用作c-Met酪氨酸激酶抑制剂的化合物。 本发明还提供包含本发明化合物的药学上可接受的组合物和使用该组合物治疗各种增殖性疾病的方法。

公开(公告)号：US20130030004A1

公开(公告)日：2013-01-31

申请号：US11593418

申请日：2006-11-06

Applicant: Paul Charifson ,  David Deininger ,  Joseph Drumm ,  Anne-Laure Grillot ,  Arnaud LeTiran ,  Yusheng Liao ,  Emanuele Perola ,  Steven Ronkin ,  Dean Stamos ,  Tiansheng Wang

Inventor： Paul Charifson ,  David Deininger ,  Joseph Drumm ,  Anne-Laure Grillot ,  Arnaud LeTiran ,  Yusheng Liao ,  Emanuele Perola ,  Steven Ronkin ,  Dean Stamos ,  Tiansheng Wang

IPC: A61K31/506 ,  C07D403/10 ,  A61K31/4184 ,  A61P31/04 ,  A61K31/4439 ,  C07D401/14 ,  A61K31/4545 ,  C07D403/14 ,  C07D401/10

CPC classification number: C07D403/04 ,  C07D401/04 ,  C07D403/14

Abstract: The present invention relates to compounds of formula I: or a pharmaceutically acceptable salt thereof, that inhibit bacterial gyrase and/or TopoIV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals.

Abstract translation: 本发明涉及抑制细菌促旋酶和/或TopoIV的式I化合物或其药学上可接受的盐以及包含所述化合物的药学上可接受的组合物。 这些化合物及其组合物可用于治疗细菌感染。 因此，本发明还涉及用于治疗哺乳动物细菌感染的方法。

公开(公告)号：US20110104207A1

公开(公告)日：2011-05-05

申请号：US12761576

申请日：2010-04-16

Applicant: Paul CHARIFSON ,  David DEININGER ,  Joseph DRUMM ,  Anne-Laure GRILLOT ,  Yusheng LIAO ,  Patricia OLIVER-SHAFFER ,  Dean STAMOS

Inventor： Paul CHARIFSON ,  David DEININGER ,  Joseph DRUMM ,  Anne-Laure GRILLOT ,  Yusheng LIAO ,  Patricia OLIVER-SHAFFER ,  Dean STAMOS

IPC: A61K39/085 ,  C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  A61K31/513 ,  A61K31/506 ,  A61K31/4545 ,  A61K31/4439 ,  A61K31/444 ,  A61K38/18 ,  C12N9/99 ,  A61K39/09 ,  A61K39/108 ,  A61K39/02 ,  A61K39/07 ,  A61K39/102 ,  A61K39/118 ,  C07C255/24 ,  A61P29/00 ,  A61P37/06 ,  A61P37/02 ,  A61P35/00 ,  A61P31/12 ,  A61P31/04

CPC classification number: C07D401/04 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/506 ,  A61K45/06 ,  C07C275/06 ,  C07D401/14 ,  C07D403/04 ,  Y02A50/473 ,  Y02A50/478 ,  A61K2300/00

Abstract: The present invention relates to compounds which inhibit bacterial gyrase and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals. The present invention also relates to a method for preparing these compounds.

Abstract translation: 本发明涉及抑制细菌促旋酶的化合物和包含所述化合物的药学上可接受的组合物。 这些化合物及其组合物可用于治疗细菌感染。 因此，本发明还涉及用于治疗哺乳动物细菌感染的方法。 本发明还涉及一种制备这些化合物的方法。

公开(公告)号：US20090325955A1

公开(公告)日：2009-12-31

申请号：US12483312

申请日：2009-06-12

Applicant: PAUL Charifson ,  David Deininger ,  Anne-Laure Grillot ,  Yusheng Liao ,  Steven Ronkin ,  Dean Stamos ,  Emanuele Perola ,  Tiansheng Wang ,  Arnaud Le Tiran ,  Joseph Drumm

Inventor： PAUL Charifson ,  David Deininger ,  Anne-Laure Grillot ,  Yusheng Liao ,  Steven Ronkin ,  Dean Stamos ,  Emanuele Perola ,  Tiansheng Wang ,  Arnaud Le Tiran ,  Joseph Drumm

IPC: A61K31/506 ,  A61K31/5377 ,  A61P31/04 ,  A61K31/519 ,  A61K31/4439 ,  A61K31/4184

CPC classification number: A61K31/4439 ,  A61K31/506 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04

Abstract: The present invention relates to methods of treating, preventing, or lessening the severity of resistant bacterial infections in mammals, utilizing compounds of formula I or formula VII or pharmaceutically salts thereof. The present invention also relates to methods of using compounds of formula I or formula VII in combination with one or more additional antibacterial agents and/or one or more additional therapeutic agents that increase the susceptibility of bacterial organisms to antibiotics.

Abstract translation: 本发明涉及使用式I或式VII化合物或其药学上可接受的方法治疗，预防或减轻哺乳动物中抗性细菌感染的严重性。 本发明还涉及使用式I或式VII化合物与一种或多种另外的抗菌剂和/或一种或多种增加细菌生物体对抗生素敏感性的其它治疗剂的组合的方法。

公开(公告)号：US07618974B2

公开(公告)日：2009-11-17

申请号：US10971573

申请日：2004-10-21

Applicant: Paul Charifson ,  David Deininger ,  Anne-Laure Grillot ,  Yusheng Liao ,  Steven M. Ronkin ,  Dean P. Stamos ,  Emanuele Perola ,  Tiansheng Wang ,  Arnaud LeTiran ,  Joseph Drumm

Inventor： Paul Charifson ,  David Deininger ,  Anne-Laure Grillot ,  Yusheng Liao ,  Steven M. Ronkin ,  Dean P. Stamos ,  Emanuele Perola ,  Tiansheng Wang ,  Arnaud LeTiran ,  Joseph Drumm

IPC: A61K31/506 ,  C07D403/04

CPC classification number: C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04

Abstract: The present invention relates to compounds that inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals.

Abstract translation: 本发明涉及抑制细菌回旋酶和/或Topo IV的化合物和包含所述化合物的药学上可接受的组合物。 这些化合物及其组合物可用于治疗细菌感染。 因此，本发明还涉及用于治疗哺乳动物细菌感染的方法。

公开(公告)号：US20070191369A1

公开(公告)日：2007-08-16

申请号：US11606524

申请日：2006-11-30

Applicant: David Lauffer ,  Alexander Aronov ,  Pan Li ,  David Deininger ,  Kira McGinty ,  Dean Stamos ,  Jon Come ,  Michelle Stewart

Inventor： David Lauffer ,  Alexander Aronov ,  Pan Li ,  David Deininger ,  Kira McGinty ,  Dean Stamos ,  Jon Come ,  Michelle Stewart

IPC: A61K31/53 ,  A61K31/497 ,  A61K31/506 ,  A61K31/501 ,  A61K31/4439 ,  A61K31/433 ,  C07D498/04

CPC classification number: C07D498/04 ,  C07D487/04 ,  C07D513/04

Abstract: The present invention provides compounds useful as inhibitors of c-Met tyrosine kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various proliferative disorders.

Abstract translation: 本发明提供了可用作c-Met酪氨酸激酶抑制剂的化合物。 本发明还提供包含本发明化合物的药学上可接受的组合物和使用该组合物治疗各种增殖性疾病的方法。

公开(公告)号：US20060122196A9

公开(公告)日：2006-06-08

申请号：US10971573

申请日：2004-10-21

Applicant: Paul Charifson ,  David Deininger ,  Anne-Laure Grillot ,  Yusheng Liao ,  Steven Ronkin ,  Dean Stamos ,  Emanuele Perola ,  Tiansheng Wang ,  Arnaud LeTiran ,  Joseph Drumm

Inventor： Paul Charifson ,  David Deininger ,  Anne-Laure Grillot ,  Yusheng Liao ,  Steven Ronkin ,  Dean Stamos ,  Emanuele Perola ,  Tiansheng Wang ,  Arnaud LeTiran ,  Joseph Drumm

IPC: A61K31/506 ,  C07D403/14

CPC classification number: C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04

Abstract: The present invention relates to compounds that inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals.

公开(公告)号：US20050038247A1

公开(公告)日：2005-02-17

申请号：US10901928

申请日：2004-07-29

Applicant: Paul Charifson ,  David Deininger ,  Anne-Laure Grillot ,  Yusheng Liao ,  Steven Ronkin ,  Dean Stamos ,  Emanuele Perola ,  Tiansheng Wang ,  Arnaud LeTiran ,  Joseph Drumm

Inventor： Paul Charifson ,  David Deininger ,  Anne-Laure Grillot ,  Yusheng Liao ,  Steven Ronkin ,  Dean Stamos ,  Emanuele Perola ,  Tiansheng Wang ,  Arnaud LeTiran ,  Joseph Drumm

IPC: A61K31/4439 ,  A61K31/506 ,  A61P31/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D43/14

CPC classification number: C07D403/04 ,  C07D401/14 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04

Abstract: The present invention relates to compounds that inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals.

Abstract translation: 本发明涉及抑制细菌回旋酶和/或Topo IV的化合物和包含所述化合物的药学上可接受的组合物。 这些化合物及其组合物可用于治疗细菌感染。 因此，本发明还涉及用于治疗哺乳动物细菌感染的方法。

公开(公告)号：US08536136B2

公开(公告)日：2013-09-17

申请号：US12639162

申请日：2009-12-16

Applicant: David Deininger ,  John Court ,  Luc Farmer ,  Janos Pitlik ,  Kevin Cottrell ,  Robert B. Perni

Inventor： David Deininger ,  John Court ,  Luc Farmer ,  Janos Pitlik ,  Kevin Cottrell ,  Robert B. Perni

IPC: A61K38/06 ,  A61K39/42 ,  A61P31/12 ,  A61P1/16 ,  C07K14/81

CPC classification number: C07K5/10 ,  A61K38/00 ,  A61K38/07 ,  A61K45/06 ,  C07K5/0202 ,  C07K7/02 ,  C07K14/005 ,  C12N2770/24222

Abstract: The present invention relates to compounds of formula I: or a pharmaceutically acceptable salt or mixtures thereof that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection and to processes for preparing the compounds. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention. The invention further relates to processes for preparing these compounds.

Abstract translation: 本发明涉及抑制丝氨酸蛋白酶活性，特别是丙型肝炎病毒NS3-NS4A蛋白酶活性的式I化合物或其药学上可接受的盐或混合物。 因此，它们通过干扰丙型肝炎病毒的生命周期起作用，也可用作抗病毒剂。 本发明还涉及包含用于离体使用或用于给予HCV感染患者的这些化合物的组合物和制备该化合物的方法。 本发明还涉及通过施用包含本发明化合物的组合物来治疗患者HCV感染的方法。 本发明还涉及制备这些化合物的方法。

公开(公告)号：US08188095B2

公开(公告)日：2012-05-29

申请号：US12246778

申请日：2008-10-07

Applicant: Paul Charifson ,  David Deininger ,  Anne-Laure Grillot ,  Yusheng Liao ,  Steven Ronkin ,  Dean Stamos ,  Emanuele Perola ,  Tiansheng Wang ,  Arnaud Le Tiran ,  Joseph Drumm

Inventor： Paul Charifson ,  David Deininger ,  Anne-Laure Grillot ,  Yusheng Liao ,  Steven Ronkin ,  Dean Stamos ,  Emanuele Perola ,  Tiansheng Wang ,  Arnaud Le Tiran ,  Joseph Drumm

IPC: A61K31/44 ,  C07D401/04 ,  C07D401/14

CPC classification number: C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04

Abstract: The present invention relates to compounds which inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals.

Abstract translation: 本发明涉及抑制细菌促旋酶和/或Topo IV的化合物和包含所述化合物的药学上可接受的组合物。 这些化合物及其组合物可用于治疗细菌感染。 因此，本发明还涉及用于治疗哺乳动物细菌感染的方法。