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1. 发明申请

US20080269214A1 Pyrrole Derivatives as Dna Gyrase and Topoisomerase Inhibitors 审中-公开
标题翻译：吡咯衍生物作为Dna促旋酶和拓扑异构酶抑制剂
公开(公告)号：US20080269214A1
公开(公告)日：2008-10-30
申请号：US11817629
申请日：2006-03-02
申请人： Gregory Steven Basarab , Michael Barry Gravestock , Sheila Irene Hauck
发明人： Gregory Steven Basarab , Michael Barry Gravestock , Sheila Irene Hauck
IPC分类号： A61K31/5377 , C07D403/04 , A61K31/4192 , C07D413/14 , A61P31/04 , C07D401/04 , A61K31/455
CPC分类号： C07D471/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： Compounds of formula (I) and their pharmaceutically acceptable salts are described: Formula (I). Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.
摘要翻译：描述式（I）化合物及其药学上可接受的盐：式（I）。还描述了其制备方法，含有它们的药物组合物，其作为药物的用途及其在治疗细菌感染中的用途。

2. 发明申请

US20100179150A1 ANTIBACTERIAL PIPERDINE DERIVATIVES 失效
标题翻译：抗菌素衍生物
公开(公告)号：US20100179150A1
公开(公告)日：2010-07-15
申请号：US11816612
申请日：2006-02-16
申请人： Gregory Basarab , Brian Dangel , Paul Robert Fleming , Michael Barry Gravestock , Oluyinka Green , Sheila Irene Hauck , Pamela Hill , Kenneth Gregory Hull , George Mullen , Brian Sherer , Fei Zhou , Haihong Ni
发明人： Gregory Basarab , Brian Dangel , Paul Robert Fleming , Michael Barry Gravestock , Oluyinka Green , Sheila Irene Hauck , Pamela Hill , Kenneth Gregory Hull , George Mullen , Brian Sherer , Fei Zhou , Haihong Ni
IPC分类号： A61K31/454 , C07D417/14 , C07D401/14 , A61K31/5377 , A61K31/4545 , A61P31/04
CPC分类号： C07D417/14 , C07D401/14 , C07D513/04
摘要： Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.
摘要翻译：描述式（I）化合物及其药学上可接受的盐。还描述了其制备方法，含有它们的药物组合物，其作为药物的用途及其在治疗细菌感染中的用途。

3. 发明授权

US07186738B2 Antibacterial oxalidinones 失效
标题翻译：抗菌草甘膦
公开(公告)号：US07186738B2
公开(公告)日：2007-03-06
申请号：US10550038
申请日：2004-03-16
申请人： Michael Barry Gravestock , Neil James Hale , Sheila Irene Hauck
发明人： Michael Barry Gravestock , Neil James Hale , Sheila Irene Hauck
IPC分类号： A01N43/76 , A01N43/72 , A01N43/828 , A01N43/647 , A01N43/56 , C07D261/06 , C07D263/04
CPC分类号： C07D413/14 , C07F9/65583
摘要： Compounds of the formula (I), or a pharmaceutically-acceptable salts, or in-vivo-hydrolysable esters thereo Formula (I): wherein N-HeT is for example triazolyl; Q is for example phenyl or pyridyl, substituted with: T is for example selected from (TAa1 to TAa12) such as (TAa1) and (TAa5): R4h, R5h, R6h are for example selected from hydrogen, (1–4C)alkyl, (1–4C)alkoxy-carbonyl, (1–4C)alkanoyl and carbamoyl; processes for making them, compositions containing them and their use as antibacterial agents are described.
摘要翻译：式（I）化合物或其药学上可接受的盐或体内可水解的酯，其中式（I）：其中N-HeT是例如三唑基; Q为例如苯基或吡啶基，被以下取代：T例如选自（TAa1至TAa12）如（TAa1）和（TAa5）：R 4h，R 5h / （1-4C）烷基，（1-4C）烷氧基 - 羰基，（1-4C）烷酰基和氨基甲酰基; R 1，R 2，R 4，描述了制备它们的方法，含有它们的组合物及其作为抗菌剂的用途。

4. 发明授权

US07396847B2 Oxazolidinone and/or isoxazoline as antibacterial agents 失效
标题翻译：恶唑烷酮和/或异恶唑啉作为抗菌剂
公开(公告)号：US07396847B2
公开(公告)日：2008-07-08
申请号：US10489266
申请日：2002-09-09
申请人： Michael Barry Gravestock , Neil James Hales , Michael Lingard Swain , Sheila Irene Hauck , Stuart Dennett Mills
发明人： Michael Barry Gravestock , Neil James Hales , Michael Lingard Swain , Sheila Irene Hauck , Stuart Dennett Mills
IPC分类号： A61K31/42 , C07D263/02 , C07D263/00 , C07D261/02
CPC分类号： C07D263/20 , C07D413/10 , C07D413/14
摘要： Compounds of the formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, and compounds as shown in (I) wherein C is for example wherein A and B are independently selected from R2a to R3b are independently selected from hydrogen and fluorine; R1a and R1b are independently selected from, for example, hydroxy, —NHC(═W)R4, wherein W is O or S; R4 is, for example, hydrogen, amino, (1-4C)alkyl; HET-1 is, for example, a C-linked 5-membered heteroaryl ring; HET-2 is, for example, an N-linked 5-membered, fully or partially unsaturated heterocyclic ring; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are described.
摘要翻译：式（I）化合物或其药学上可接受的盐或其体内可水解的酯，和（I）所示的化合物，其中C为例如其中A和B独立地选自R 1， 2 a至R 3 b独立地选自氢和氟; R 1 a和R 1 b独立地选自，例如羟基，-NHC（-W）R 4，其中W是 O或S; R 4是例如氢，氨基，（1-4C）烷基; HET-1是例如C连接的5元杂芳基环; HET-2是例如N-连接的5元全部或部分不饱和杂环; 作为抗菌剂是有用的; 并描述了其制造方法和含有它们的药物组合物。

5. 发明申请

US20100137243A1 Oxazolidinone And/Or Isoxazoline As Antibacterial Agents 审中-公开
标题翻译：恶唑烷酮和/或异恶唑啉作为抗菌剂
公开(公告)号：US20100137243A1
公开(公告)日：2010-06-03
申请号：US12128135
申请日：2008-05-28
申请人： Michael Barry Gravestock , Neil James Hales , Michael Lingrad Swaim , Sheila Irene Hauck , Stuart Dennett Mills
发明人： Michael Barry Gravestock , Neil James Hales , Michael Lingrad Swaim , Sheila Irene Hauck , Stuart Dennett Mills
IPC分类号： A61K31/695 , A61K31/4439 , C07D413/14 , A61K31/422 , C07F9/06 , A61K31/675 , C07F7/02
CPC分类号： C07D263/20 , C07D413/10 , C07D413/14
摘要： Compounds of Formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, and compounds as shown in Formula (I) wherein C is for example (D), (E), (F); wherein A and B are independently selected from (i) and (ii); R2a to R3b are independently selected from hydrogen and fluorine; R1a and R1b are independently selected from, for example, hydroxy, —NHC(═W)R4, (a) and (b); wherein W is O or S; R4 is, for example, hydrogen, amino, (1-4C)alkyl; HET-1 is, for example, a C-linked 5-membered heteroaryl ring; HET-2 is, for example, an N-linked 5-membered, fully or partially unsaturated heterocyclic ring; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are described.
摘要翻译：式（I）化合物或其药学上可接受的盐或其体内可水解的酯，以及其中C为（D），（E），（F）的式（I）所示的化合物。其中A和B独立地选自（i）和（ii）; R2a至R3b独立地选自氢和氟; R1a和R1b独立地选自例如羟基，-NHC（= W）R4，（a）和（b）; 其中W是O或S; R4是例如氢，氨基，（1-4C）烷基; HET-1是例如C连接的5元杂芳基环; HET-2是例如N-连接的5元全部或部分不饱和杂环; 作为抗菌剂是有用的; 并描述了其制造方法和含有它们的药物组合物。

6. 发明授权

US07157482B2 Antibacterial 1,3-oxazolidin-2-one derivatives 失效
标题翻译：抗菌1,3-恶唑烷-2-酮衍生物
公开(公告)号：US07157482B2
公开(公告)日：2007-01-02
申请号：US10550039
申请日：2004-03-16
申请人： Michael Barry Gravestock , Neil James Hale , Sheila Irene Hauck
发明人： Michael Barry Gravestock , Neil James Hale , Sheila Irene Hauck
IPC分类号： A01N43/76 , A01N43/72 , A01N43/828 , A01N43/647 , A01N43/56 , C07D261/06 , C07D263/04
CPC分类号： C07D413/14
摘要： Compounds of the formula (I), or a pharmaceutically-acceptable salts, or in-vivo-hydrolysable esters thereof, wherein: N—HET is for example triazolyl substituted with R1; R1 is for example optionally substituted (1-4C)alkyl; Q is for example phenyl or pyridyl, substituted with T; T is for example selected from (TAa1 to TAa12) such as (TAa1 and TAa5); formula (II): R4h, R5h, R6h are for example selected from hydrogen, (1-4C)alkyl, (1-4C)alkoxycarbonyl, (1-4C)alkanoyl and carbamoyl; processes for making them, compositions containing them and their use as antibacterial agents are described.
摘要翻译：式（I）化合物或其药学上可接受的盐或体内可水解的酯，其中：N-HET例如被R 1取代的三唑基; R 1是例如任选取代的（1-4C）烷基; Q为例如苯基或吡啶基，被T取代; T例如选自（TAa1〜TAa12），例如（TAa1和TAa5）; 式（II）：R 4h，R 5h，R 6h是例如选自氢，（1-4C）烷基，（1 -4C）烷氧基羰基，（1-4C）烷酰基和氨基甲酰基; 描述了制备它们的方法，含有它们的组合物及其作为抗菌剂的用途。

7. 发明授权

US08399489B2 Antibacterial piperdine derivatives 失效
标题翻译：抗菌哌啶衍生物
公开(公告)号：US08399489B2
公开(公告)日：2013-03-19
申请号：US11816612
申请日：2006-02-16
申请人： Gregory Basarab , Brian Dangel , Paul Robert Fleming , Michael Barry Gravestock , Oluyinka Green , Sheila Irene Hauck , Pamela Hill , Kenneth Gregory Hull , George Mullen , Haihong Ni , Brian Sherer , Fei Zhou
发明人： Gregory Basarab , Brian Dangel , Paul Robert Fleming , Michael Barry Gravestock , Oluyinka Green , Sheila Irene Hauck , Pamela Hill , Kenneth Gregory Hull , George Mullen , Haihong Ni , Brian Sherer , Fei Zhou
IPC分类号： A61K31/454 , C07D401/14
CPC分类号： C07D417/14 , C07D401/14 , C07D513/04
摘要： Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.
摘要翻译：描述式（I）化合物及其药学上可接受的盐。还描述了其制备方法，含有它们的药物组合物，其作为药物的用途及其在治疗细菌感染中的用途。

8. 发明授权

US07473699B2 3-cyclyl-5-(nitrogen-containing 5-membered ring)methyl-oxazolidinone derivatives and their use as antibacterial agents 失效
标题翻译： 3-环-5-（含氮五元环）甲基恶唑烷酮衍生物及其作为抗菌剂的用途
公开(公告)号：US07473699B2
公开(公告)日：2009-01-06
申请号：US10506020
申请日：2003-02-25
申请人： Michael Barry Gravestock , Neil James Hales , Folkert Reck , Fei Zhou , Paul Robert Fleming , Daniel Robert Carcanague , Marc Michel Girardot
发明人： Michael Barry Gravestock , Neil James Hales , Folkert Reck , Fei Zhou , Paul Robert Fleming , Daniel Robert Carcanague , Marc Michel Girardot
IPC分类号： A61K31/42 , C07D263/00
CPC分类号： C07D233/56 , C07D231/12 , C07D249/08 , C07D413/06 , C07D413/10 , C07D413/14
摘要： Compounds of the formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, wherein —N-HET is, for example, (Ic) or (If) wherein R1 is (1-4C)alkyl; Q is selected from, for example, Q1 wherein R2 and R3 are independently hydrogen or fluoro; T is selected from a range of groups, for example, wherein m is 0, 1 or 2; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are described.
摘要翻译：其中-N-HET是例如（Ic）或（If）的式（I）化合物或其药学上可接受的盐或其体内可水解的酯，其中R1是（1-4C）烷基; Q选自例如Q1，其中R2和R3独立地是氢或氟; T选自一组基团，例如其中m为0,1或2; 作为抗菌剂是有用的; 并描述了其制造方法和含有它们的药物组合物。

9. 发明授权

US06638955B2 Antibiotic oxazolidinone derivatives 失效
标题翻译：抗生素恶唑烷酮衍生物
公开(公告)号：US06638955B2
公开(公告)日：2003-10-28
申请号：US10032584
申请日：2001-12-21
申请人： Michael Barry Gravestock
发明人： Michael Barry Gravestock
IPC分类号： C07D41310
CPC分类号： C07D413/10 , C07D413/14 , C07D513/04
摘要： The present application discloses a class of antibiotic compounds containing an oxazolidinone ring. These compounds have useful activity against Gram-positive pathogens including MRSA and MRCNS and, in particular, against various strains exhibiting resistance to vancomycin and against E. faecium strains resistant to both aminoglycosides and clinically used &bgr;-lactams. The compounds also possess a favorable toxicological profile. This invention further relates to processes for their preparation, to intermediates useful in their preparation, to their use as therapeutic agents and to pharmaceutical compositions containing them.
摘要翻译：本申请公开了一类含有恶唑烷酮环的抗生素化合物。这些化合物对包括MRSA和MRCNS在内的革兰氏阳性病原体具有有效的活性，特别是针对对万古霉素和对两种氨基糖苷类和临床使用的β-内酰胺均有抗性的屎肠球菌菌株具有抗性的各种菌株。这些化合物也具有良好的毒理学特征。本发明还涉及其制备方法，可用于其制备的中间体，其用作治疗剂和含有它们的药物组合物。

10. 发明申请

US20080064689A1 3-[4-(6-Pyridin-3-Yl)-3-Phenyl] -5-(1H-1,2,3-Triazol-1-Ylmethyl)-1,3-Oxazolidin-2-Ones as Antibacterial Agents 审中-公开
标题翻译： 3- [4-（6-吡啶-3-基）-3-苯基] -5-（1H-1,2,3-三唑-1-基甲基）-1,3-恶唑烷-2-酮作为抗菌剂
公开(公告)号：US20080064689A1
公开(公告)日：2008-03-13
申请号：US11569148
申请日：2004-05-24
申请人： Daniel Robert Carcanague , Michael Barry Gravestock
发明人： Daniel Robert Carcanague , Michael Barry Gravestock
IPC分类号： A61K31/4418 , A61K31/445 , A61K31/497 , A61K31/535 , A61K31/54 , C07D413/04 , C07D413/14
CPC分类号： C07D413/14
摘要： Compounds of the formula (I): or a pharmaceutically-acceptable salt or pro-drug thereof: wherein R1 is selected for example from hydrogen, halogen, optionally substituted methyl; R2 and R3 are independently selected from hydrogen, fluoro, chloro and trifluoromethyl; R4 and R5 are independently selected, for example, from hydrogen, methyl, optionally substituted (2-4C)alkyl, C(O)R6 or R4 and R5 together with the nitrogen to which they are attached form an optionally substituted 5 or 6 membered, saturated or partially unsaturated heterocyclyl ring or an optionally substituted imidazole ring. Methods for making the compounds of formula (I), compositions containing them and their use as antibacterial agents are also described.
摘要翻译：式（I）化合物或其药学上可接受的盐或前体药物：其中R 1选自例如氢，卤素，任选取代的甲基; R 2和R 3独立地选自氢，氟，氯和三氟甲基; R 4和R 5独立地选自，例如，氢，甲基，任选取代的（2-4C）烷基，C（O）R 6，或者R 4和R 5与它们所连接的氮一起形成任选取代的5或6元饱和或部分不饱和的杂环基环或任选地取代的咪唑环。还描述了制备式（I）化合物，含有它们的组合物及其作为抗菌剂的用途的方法。

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