公开(公告)号：US08268873B2

公开(公告)日：2012-09-18

申请号：US12221921

申请日：2008-08-07

申请人： Dean Stamos ,  Martin Trudeau ,  Randy S. Bethiel ,  Steven M. Ronkin ,  Michael C. Badia ,  Jeffrey O. Saunders

发明人： Dean Stamos ,  Martin Trudeau ,  Randy S. Bethiel ,  Steven M. Ronkin ,  Michael C. Badia ,  Jeffrey O. Saunders

IPC分类号： A61K31/42 ,  A61K31/27 ,  C07D263/14 ,  C07D207/00

CPC分类号： C07C275/40 ,  C07B2200/07 ,  C07C275/42 ,  C07D263/32 ,  C07F9/653

摘要： The present invention relates to compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH-mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.

摘要翻译： 本发明涉及抑制IMPDH的化合物。 本发明还涉及包含这些化合物的药物组合物。 本发明的化合物和药物组合物特别适用于抑制IMPDH酶活性，因此可有利地用作IMPDH介导的方法的治疗剂。 本发明还涉及使用本发明化合物和相关化合物抑制IMPDH活性的方法。

公开(公告)号：US07989498B2

公开(公告)日：2011-08-02

申请号：US10671967

申请日：2003-09-25

申请人： Jeffrey O Saunders ,  Daniel Elbaum ,  Perry M Novak ,  Douglas Naegele ,  Randy S Bethiel ,  Steven M Ronkin ,  Michael C Badia ,  Catharine Frank ,  Dean P Stamos ,  William Walters ,  David Pearlman

发明人： Jeffrey O Saunders ,  Daniel Elbaum ,  Perry M Novak ,  Douglas Naegele ,  Randy S Bethiel ,  Steven M Ronkin ,  Michael C Badia ,  Catharine Frank ,  Dean P Stamos ,  William Walters ,  David Pearlman

IPC分类号： A61K31/165 ,  A61K31/16

CPC分类号： C07D213/75 ,  A61K31/4965 ,  A61K31/53 ,  C07C217/84 ,  C07C235/64 ,  C07C311/21 ,  C07C311/29 ,  C07C317/40 ,  C07C323/42 ,  C07C333/08 ,  C07D263/32 ,  C07D271/06 ,  C07D307/91 ,  C07D317/68 ,  C07D413/12

摘要： The present invention relates to compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.

摘要翻译： 本发明涉及抑制IMPDH的化合物。 本发明还涉及包含这些化合物的药物组合物。 本发明的化合物和药物组合物特别适用于抑制IMPDH酶活性，因此可有利地用作IMPDH介导的过程的治疗剂。 本发明还涉及使用本发明化合物和相关化合物抑制IMPDH活性的方法。

公开(公告)号：US07582641B2

公开(公告)日：2009-09-01

申请号：US10986569

申请日：2004-11-11

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

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

IPC分类号： A61K31/506 ,  C07D239/26

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

摘要： 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.

摘要翻译： 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：US6054472A

公开(公告)日：2000-04-25

申请号：US832165

申请日：1997-04-02

申请人： David M. Armistead ,  Michael C. Badia ,  Guy W. Bemis ,  Randy S. Bethiel ,  Catharine A. Frank ,  Perry M. Novak ,  Steven M. Ronkin ,  Jeffrey O. Saunders

发明人： David M. Armistead ,  Michael C. Badia ,  Guy W. Bemis ,  Randy S. Bethiel ,  Catharine A. Frank ,  Perry M. Novak ,  Steven M. Ronkin ,  Jeffrey O. Saunders

IPC分类号： A61K31/404 ,  A61K31/42 ,  A61K31/422 ,  C07C275/42 ,  C07D263/32 ,  C07D413/12 ,  A01N43/76 ,  C07D263/02 ,  C07D263/34

CPC分类号： C07D413/12 ,  A61K31/404 ,  A61K31/42 ,  A61K31/422 ,  C07C275/42 ,  C07D263/32

摘要： The present invention relates to a novel class of compounds which are IMPDH inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.

公开(公告)号：US5807876A

公开(公告)日：1998-09-15

申请号：US636361

申请日：1996-04-23

申请人： David M. Armistead ,  Michael C. Badia ,  Guy W. Bemis ,  Randy S. Bethiel ,  Catharine A. Frank ,  Perry M. Novak ,  Steven M. Ronkin ,  Jeffrey O. Saunders

发明人： David M. Armistead ,  Michael C. Badia ,  Guy W. Bemis ,  Randy S. Bethiel ,  Catharine A. Frank ,  Perry M. Novak ,  Steven M. Ronkin ,  Jeffrey O. Saunders

IPC分类号： A61K31/17 ,  A61K31/18 ,  A61K31/404 ,  A61K31/42 ,  A61K31/421 ,  A61K31/422 ,  A61P9/14 ,  A61P29/00 ,  A61P31/12 ,  A61P35/00 ,  A61P37/06 ,  A61P43/00 ,  C07C275/42 ,  C07D263/18 ,  C07D263/32 ,  C07D277/18 ,  C07D413/12 ,  C07D263/34 ,  C07D413/00

CPC分类号： C07D413/12 ,  A61K31/404 ,  A61K31/42 ,  A61K31/422 ,  C07C275/42 ,  C07D263/32

摘要： The present invention relates to a novel class of compounds which are IMPDH inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as agents for immunosuppression. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.

摘要翻译： 本发明涉及一类新颖的IMPDH抑制剂。 本发明还涉及包含这些化合物的药物组合物。 本发明的化合物和药物组合物特别适用于抑制IMPDH酶活性，因此可有利地用作免疫抑制剂。 本发明还涉及使用本发明化合物和相关化合物抑制IMPDH活性的方法。

公开(公告)号：US07569591B2

公开(公告)日：2009-08-04

申请号：US10901928

申请日：2004-07-29

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

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

IPC分类号： A61K31/4439 ,  C07D401/00

CPC分类号： C07D403/04 ,  C07D401/14 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04

摘要： 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：US07432290B2

公开(公告)日：2008-10-07

申请号：US10997810

申请日：2004-11-24

申请人： Dean Stamos ,  Martin Trudeau ,  Randy S. Bethiel ,  Steven M. Ronkin ,  Michael C. Badia ,  Jeffrey O. Saunders

发明人： Dean Stamos ,  Martin Trudeau ,  Randy S. Bethiel ,  Steven M. Ronkin ,  Michael C. Badia ,  Jeffrey O. Saunders

IPC分类号： A61K31/41 ,  A61K31/425 ,  C07D263/00 ,  C07D263/02

CPC分类号： C07C275/40 ,  C07B2200/07 ,  C07C275/42 ,  C07D263/32 ,  C07F9/653

摘要： The present invention relates to compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH-mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.

摘要翻译： 本发明涉及抑制IMPDH的化合物。 本发明还涉及包含这些化合物的药物组合物。 本发明的化合物和药物组合物特别适用于抑制IMPDH酶活性，因此可有利地用作IMPDH介导的方法的治疗剂。 本发明还涉及使用本发明化合物和相关化合物抑制IMPDH活性的方法。

公开(公告)号：US06653309B1

公开(公告)日：2003-11-25

申请号：US09702991

申请日：2000-10-30

申请人： Jeffrey O. Saunders ,  Daniel Elbaum ,  Perry M. Novak ,  Douglas Naegele ,  Randy S. Bethiel ,  Steven M. Ronkin ,  Michael C. Badia ,  Catharine Frank ,  Dean P. Stamos ,  William Walters ,  David Pearlman

发明人： Jeffrey O. Saunders ,  Daniel Elbaum ,  Perry M. Novak ,  Douglas Naegele ,  Randy S. Bethiel ,  Steven M. Ronkin ,  Michael C. Badia ,  Catharine Frank ,  Dean P. Stamos ,  William Walters ,  David Pearlman

IPC分类号： C07D25102

CPC分类号： C07D213/75 ,  A61K31/4965 ,  A61K31/53 ,  C07C217/84 ,  C07C235/64 ,  C07C311/21 ,  C07C311/29 ,  C07C317/40 ,  C07C323/42 ,  C07C333/08 ,  C07D263/32 ,  C07D271/06 ,  C07D307/91 ,  C07D317/68 ,  C07D413/12

摘要： The present invention relates to compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well-suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.

摘要翻译： 本发明涉及抑制IMPDH的化合物。 本发明还涉及包含这些化合物的药物组合物。 本发明的化合物和药物组合物特别适合于抑制IMPDH酶活性，因此可有利地用作IMPDH介导的方法的治疗剂。 本发明还涉及使用本发明化合物和相关化合物抑制IMPDH活性的方法。

公开(公告)号：US07618974B2

公开(公告)日：2009-11-17

申请号：US10971573

申请日：2004-10-21

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

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

IPC分类号： A61K31/506 ,  C07D403/04

CPC分类号： C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04

摘要： 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.

摘要翻译： 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：US06541496B1

公开(公告)日：2003-04-01

申请号：US09556253

申请日：2000-04-24

申请人： David M. Armistead ,  Michael C. Badia ,  Guy W. Bemis ,  Randy S. Bethiel ,  Catharine A. Frank ,  Perry M. Novak ,  Steven M. Ronkin ,  Jeffrey O. Saunders

发明人： David M. Armistead ,  Michael C. Badia ,  Guy W. Bemis ,  Randy S. Bethiel ,  Catharine A. Frank ,  Perry M. Novak ,  Steven M. Ronkin ,  Jeffrey O. Saunders

IPC分类号： A61K3142

CPC分类号： C07D413/12 ,  A61K31/404 ,  A61K31/42 ,  A61K31/422 ,  C07C275/42 ,  C07D263/32 ,  Y02P20/55

摘要： The present invention relates to a novel class of compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.

摘要翻译： 本发明涉及抑制IMPDH的新一类化合物。 本发明还涉及包含这些化合物的药物组合物。 本发明的化合物和药物组合物特别适用于抑制IMPDH酶活性，因此可有利地用作IMPDH介导的过程的治疗剂。 本发明还涉及使用本发明化合物和相关化合物抑制IMPDH活性的方法。