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1. 发明申请

WO2008073142A3 NOVEL INHIBITORS OF BETA-LACTAMASE 审中-公开
标题翻译： β-LACTAMASE的新型抑制剂
公开(公告)号：WO2008073142A3
公开(公告)日：2008-10-02
申请号：PCT/US2007011979
申请日：2007-05-21
申请人： MERCK & CO INC , METHLGENE INC , DININNO FRANK , HAMMOND MILTON L , DYKSTRA KEVIN , KIM SEONGKON , TAN QIANG , YOUNG KATHERINE , HERMES JEFFREY DONALD , CHEN HELEN , RAEPPEL STEPHANE , MANNION MICHAEL , GAUDETTE FREDERIC , VAISBURG ARKADII , RAHL JUBRAIL , GEORGOPAPADAKOU NAFSIKA , ZHOU NANCY Z
发明人： DININNO FRANK , HAMMOND MILTON L , DYKSTRA KEVIN , KIM SEONGKON , TAN QIANG , YOUNG KATHERINE , HERMES JEFFREY DONALD , CHEN HELEN , RAEPPEL STEPHANE , MANNION MICHAEL , GAUDETTE FREDERIC , VAISBURG ARKADII , RAHL JUBRAIL , GEORGOPAPADAKOU NAFSIKA , ZHOU NANCY Z
IPC分类号： A61P31/04 , A61K31/67 , A61K31/675 , C07F9/6539 , C07F9/6541 , C07F9/6553 , C07F9/6558 , C07F9/6561
CPC分类号： C07F9/655354 , C07F9/65395 , C07F9/6541 , C07F9/6553 , C07F9/6558 , C07F9/6561
摘要： This invention provides novel ß-lactamase inhibitors of the aryl-and heteroarylsulfonarnidomethylphosphonate monoester class having nitrogen-based cations or quarternary ammomium groups. The compounds inhibit three classes of ß-lactamases and synergize the antibacterial effects of ß-lactam antibiotics (e.g., imipenem and ceftazimdime) against those micro-organisms normally resistant to the ß-lactam antibiotics as a result of the presence of the ß-lactamases. Formula (I) or pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供了具有氮基阳离子或季铵基团的芳基和杂芳基磺酰基甲基膦酸酯单酯类的新型β-内酰胺酶抑制剂。该化合物抑制三种类型的β-内酰胺酶，并且与β-内酰胺类抗生素（例如，亚胺培南和头孢他啶的抗菌作用）对抗β-内酰胺抗生素通常具有抗ß-内酰胺抗生素的微生物的协同作用是由于存在β-内酰胺酶。式（I）或其药学上可接受的盐。

2. 发明申请

WO2008073142A8 NOVEL INHIBITORS OF BETA-LACTAMASE 审中-公开
标题翻译： β-LACTAMASE的新型抑制剂
公开(公告)号：WO2008073142A8
公开(公告)日：2009-01-29
申请号：PCT/US2007011979
申请日：2007-05-21
申请人： MERCK & CO INC , METHYLGENE INC , DININNO FRANK , HAMMOND MILTON L , DYKSTRA KEVIN , KIM SEONGKON , TAN QIANG , YOUNG KATHERINE , HERMES JEFFREY DONALD , CHEN HELEN , RAEPPEL STEPHANE , MANNION MICHAEL , GAUDETTE FREDERIC , VAISBURG ARKADII , RAHL JUBRAIL , GEORGOPAPADAKOU NAFSIKA , ZHOU NANCY Z
发明人： DININNO FRANK , HAMMOND MILTON L , DYKSTRA KEVIN , KIM SEONGKON , TAN QIANG , YOUNG KATHERINE , HERMES JEFFREY DONALD , CHEN HELEN , RAEPPEL STEPHANE , MANNION MICHAEL , GAUDETTE FREDERIC , VAISBURG ARKADII , RAHL JUBRAIL , GEORGOPAPADAKOU NAFSIKA , ZHOU NANCY Z
IPC分类号： A61P31/04 , A61K31/67 , A61K31/675 , C07F9/6539 , C07F9/6541 , C07F9/6553 , C07F9/6558 , C07F9/6561
CPC分类号： C07F9/655354 , C07F9/65395 , C07F9/6541 , C07F9/6553 , C07F9/6558 , C07F9/6561
摘要： This invention provides novel ß-lactamase inhibitors of the aryl-and heteroarylsulfonarnidomethylphosphonate monoester class having nitrogen-based cations or quarternary ammomium groups. The compounds inhibit three classes of ß-lactamases and synergize the antibacterial effects of ß-lactam antibiotics (e.g., imipenem and ceftazimdime) against those micro-organisms normally resistant to the ß-lactam antibiotics as a result of the presence of the ß-lactamases. Formula (I) or pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供了具有氮基阳离子或季铵基团的芳基和杂芳基磺酰基甲基膦酸酯单酯类的新型β-内酰胺酶抑制剂。该化合物抑制三种类型的β-内酰胺酶，并且与β-内酰胺类抗生素（例如，亚胺培南和头孢他啶的抗菌作用）对抗β-内酰胺抗生素通常具有抗ß-内酰胺抗生素的微生物的协同作用是由于存在β-内酰胺酶。式（I）或其药学上可接受的盐。

3. 发明申请

WO2009091856A3 BETA-LACTAMASE INHIBITORS 审中-公开
标题翻译： BETA-LACTAMASE抑制剂
公开(公告)号：WO2009091856A3
公开(公告)日：2009-12-03
申请号：PCT/US2009031047
申请日：2009-01-15
申请人： MERCK & CO INC , BLIZZARD TIMOTHY A , CHEN HELEN , GUDE CANDIDO , HERMES JEFFREY D , IMBRIGLIO JASON E , KIM SEONGKON , WU JANE Y , HA SOOKHEE , MORTKO CHRISTOPHER J , MANGION IAN , RIVERA NELO , RUCK REBECCA T , SHEVLIN MICHAEL
发明人： BLIZZARD TIMOTHY A , CHEN HELEN , GUDE CANDIDO , HERMES JEFFREY D , IMBRIGLIO JASON E , KIM SEONGKON , WU JANE Y , HA SOOKHEE , MORTKO CHRISTOPHER J , MANGION IAN , RIVERA NELO , RUCK REBECCA T , SHEVLIN MICHAEL
IPC分类号： C07D471/08 , A61K31/529 , A61K31/535 , A61P31/04 , C07D487/08 , C07D519/00
CPC分类号： C07D471/08 , C07D211/58 , C07D211/60 , C07D211/78 , C07D487/08 , C07D519/00
摘要： Substituted bicyclic beta-lactams of Formula I: (I), are ß-lactamase inhibitors, wherein a, X, R1 and R2 are defined herein. The compounds and pharmaceutically acceptable salts thereof are useful in the treatment of bacterial infections in combination with ß-lactam antibiotics. In particular, the compounds can be employed with a ß-lactam antibiotics (e.g., imipenem, piperacillin, or ceftazidime) against microorganisms resistant to ß-lactam antibiotics due to the presence of the ß-lactamases.
摘要翻译：式I的取代的双环β-内酰胺：（I）是β-内酰胺酶抑制剂，其中a，X，R 1和R 2在本文中定义。化合物及其药学上可接受的盐可用于治疗细菌感染与β-内酰胺抗生素的组合。特别地，由于β-内酰胺酶的存在，这些化合物可以与β-内酰胺抗生素（例如亚胺培南，哌拉西林或头孢他啶）一起用于抗β-内酰胺抗生素的微生物。

4. 发明专利

AU2007332968A1 Novel inhibitors of beta-lactamase 未知
公开(公告)号：AU2007332968A1
公开(公告)日：2008-06-19
申请号：AU2007332968
申请日：2007-05-21
申请人： METHLGENE INC , MERCK & CO INC
发明人： HAMMOND MILTON L , MANNION MICHAEL , CHEN HELEN , HERMES JEFFREY DONALD , GEORGOPAPADAKOU NAFSIKA , ZHOU NANCY Z , VAISBURG ARKADII , GAUDETTE FREDERIC , YOUNG KATHERINE , RAHL JUBRAIL , DININNO FRANK , KIM SEONGKON , DYKSTRA KEVIN , RAEPPEL STEPHANE , TAN QIANG
IPC分类号： A61P31/04 , A61K31/67 , A61K31/675 , C07F9/6539 , C07F9/6541 , C07F9/6553 , C07F9/6558 , C07F9/6561
摘要： This invention provides novel beta-lactamase inhibitors of the aryl- and heteroaryl-sulfonamidomethylphosphonate monoester class having nitrogen-based cations or quarternary ammomium groups. The compounds inhibit three classes of beta-lactamases and synergize the antibacterial effects of beta-lactam antibiotics (e.g., imipenem and ceftazimdime) against those micro-organisms normally resistant to the beta-lactam antibiotics as a result of the presence of the beta-lactamases.

5. 发明专利

CA2582093A1 BODY ELONGATOR 未知
公开(公告)号：CA2582093A1
公开(公告)日：2008-04-24
申请号：CA2582093
申请日：2007-02-15
申请人： CHEN HELEN , LEE JAY
发明人： CHEN HELEN , LEE JAY
IPC分类号： A61H1/02
摘要： A body elongator includes a container in which a heel elongator and a calf stretcher are fixed. The heel elongator has a leg support slide selectively movable for a predetermined distance by a driving mechanism for elongating a user's heels secured to the leg support slide. The calf stretcher has a toe bar supported between and by two carrier posts. The carrier posts, along with th e toe bar, can be rotated from a horizontal position to a vertical position wi th respect to the frame body. When the user's toes are leaned tightly against the toe bar, with heels secured to the leg support slide, making the feet plantar flexion along the movement direction of the leg support slide, the Achilles tendon and the calf muscles groups can be stretched when the leg support slide is driven to move into the container.

6. 发明专利

CA2582093C BODY ELONGATOR 未知
公开(公告)号：CA2582093C
公开(公告)日：2009-07-21
申请号：CA2582093
申请日：2007-02-15
申请人： CHEN HELEN , LEE JAY
发明人： CHEN HELEN , LEE JAY
IPC分类号： A61H1/02
摘要： A body elongator includes a container in which a heel elongator and a calf stretcher are fixed. The heel elongator has a leg support slide selectively movable for a predetermined distance by a driving mechanism for elongating a user's heels secured to the leg support slide. The calf stretcher has a toe bar supported between and by two carrier posts. The carrier posts, along with th e toe bar, can be rotated from a horizontal position to a vertical position wi th respect to the frame body. When the user's toes are leaned tightly against the toe bar, with heels secured to the leg support slide, making the feet plantar flexion along the movement direction of the leg support slide, the Achilles tendon and the calf muscles groups can be stretched when the leg support slide is driven to move into the container.

7. 发明公开

EP1023293A4 ARYLOXYMETHYL CARBAPENEM ANTIBACTERIALS 审中-公开
标题翻译：抗老化剂ARYLOXYMETHYLCARBAPENEM
公开(公告)号：EP1023293A4
公开(公告)日：2002-11-20
申请号：EP98951912
申请日：1998-09-14
申请人： MERCK & CO INC
发明人： DININNO FRANK P , CHEN HELEN
IPC分类号： C07D477/00 , A61K31/397 , A61K31/407 , A61K31/4995 , A61P31/04 , C07D477/14 , C07D519/00 , C07D519/06 , C07D521/00 , A61K31/40
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D477/14

8. 发明专利

CA2652995A1 NOVEL INHIBITORS OF BETA-LACTAMASE 未知
公开(公告)号：CA2652995A1
公开(公告)日：2008-06-19
申请号：CA2652995
申请日：2007-05-21
申请人： MERCK & CO INC , METHYLGENE INC
发明人： KIM SEONGKON , DYKSTRA KEVIN , DININNO FRANK , HAMMOND MILTON L , GEORGOPAPADAKOU NAFSIKA , RAHL JUBRAIL , VAISBURG ARKADII , MANNION MICHAEL , GAUDETTE FREDERIC , CHEN HELEN , HERMES JEFFREY DONALD , TAN QIANG , YOUNG KATHERINE , ZHOU NANCY Z , RAEPPEL STEPHANE
IPC分类号： A61P31/04 , A61K31/67 , A61K31/675 , C07F9/6539 , C07F9/6541 , C07F9/6553 , C07F9/6558 , C07F9/6561
摘要： This invention provides novel .beta.-lactamase inhibitors of the aryl-and heteroarylsulfonarnidomethylphosphonate monoester class having nitrogen-bas ed cations or quarternary ammomium groups. The compounds inhibit three class es of .beta.-lactamases and synergize the antibacterial effects of .beta.-la ctam antibiotics (e.g., imipenem and ceftazimdime) against those micro-organ isms normally resistant to the .beta.-lactam antibiotics as a result of the presence of the .beta.-lactamases. Formula (I) or pharmaceutically acceptabl e salt thereof.

9. 发明专利

CA2304267A1 ARYLOXYMETHYL CARBAPENEM ANTIBACTERIALS 未知
公开(公告)号：CA2304267A1
公开(公告)日：1999-03-25
申请号：CA2304267
申请日：1998-09-14
申请人： MERCK & CO INC
发明人： CHEN HELEN , DININNO FRANK P
IPC分类号： C07D477/00 , A61K31/397 , A61K31/407 , A61K31/4995 , A61P31/04 , C07D477/14 , C07D519/00 , C07D519/06 , C07D521/00 , A61K31/40
摘要： The present invention relates to carbapenem antibacterial agents of formula(I), as well as salts and hydrates thereof. Pharmaceutical compositions and methods of treatment are also included.

10. 发明专利

AU9774298A Aryloxymethyl carbapenem antibacterials 未知
公开(公告)号：AU9774298A
公开(公告)日：1999-04-05
申请号：AU9774298
申请日：1998-09-14
申请人： MERCK & CO INC
发明人： DININNO FRANK P , CHEN HELEN
IPC分类号： C07D477/00 , A61K31/397 , A61K31/407 , A61K31/4995 , A61P31/04 , C07D477/14 , C07D519/00 , C07D519/06 , C07D521/00 , A61K31/40

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