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1. 发明申请

US20050119292A1 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5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：US20050119292A1
公开(公告)日：2005-06-02
申请号：US10506020
申请日：2003-02-25
申请人： Michael Gravestock , Neil Hales , Folkert Reck , Fei Zhou , Paul Fleming , Daniel Carcanague , Marc Girardot
发明人： Michael Gravestock , Neil Hales , Folkert Reck , Fei Zhou , Paul Fleming , Daniel Carcanague , Marc Girardot
IPC分类号： C07D413/14 , A61K31/422 , A61K31/454 , A61K31/541 , A61P31/04 , C07D413/06 , C07D413/10 , C07D417/14 , C07D521/00 , A61K31/4439 , A61K31/4747
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：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-N-HET是例如（Ic）或（If）其中R1是（1-4C）烷基; Q选自例如其中R 2和R 3独立地为氢或氟的Q1; 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。

2. 发明申请

US20050182112A1 Chemical compounds 失效
标题翻译：化合物
公开(公告)号：US20050182112A1
公开(公告)日：2005-08-18
申请号：US10505902
申请日：2003-02-25
申请人： Michael Gravestock , Neil Hales , Folkert Reck , Fei Zhou , Paul Fleming , Daniel Carcanague
发明人： Michael Gravestock , Neil Hales , Folkert Reck , Fei Zhou , Paul Fleming , Daniel Carcanague
IPC分类号： C07D413/14 , A61K20060101 , A61K31/422 , A61K31/5377 , A61K31/661 , A61P20060101 , A61P31/04 , A61P43/00 , C07B53/00 , C07D20060101 , C07D413/04 , C07F9/6558
CPC分类号： 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, for example, halogen or a (1-4C)alkyl group which is substituted by one substituent selected from, for example, hydroxy, (1-4C)alkoxy, amino, cyano or azido; 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：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-N-HET是例如（Ic）或（If），其中R 1是例如卤素或被选自例如羟基，（1-4C）烷氧基，氨基，氰基或叠氮基的一个取代基取代的（1-4C）烷基; Q选自例如其中R 2和R 3独立地为氢或氟的Q1; 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。

3. 发明申请

US20060052399A1 Oxazolidinone derivatives as antibacterial agents 审中-公开
标题翻译：恶唑烷酮衍生物作为抗菌剂
公开(公告)号：US20060052399A1
公开(公告)日：2006-03-09
申请号：US10539486
申请日：2003-12-15
申请人： Michael Gravestock , Folkert Reck , Fei Zhou , Neil Hales
发明人： Michael Gravestock , Folkert Reck , Fei Zhou , Neil Hales
IPC分类号： A61K31/506 , A61K31/4439 , C07D413/02
CPC分类号： C07D413/14 , C07D413/10
摘要： A compound of the formula (I), or a pharmaceutically-acceptable salt, or in-vivo hydsolysable ester thereof: formula (I) wherein C is selected from D and E, formula (D), formula (E) R2a, R6a, and R3a are independently selected from for example H, CF3, Me and Et; R2b and R6b are independently selected from for example H, F, CF3, Me and Et; R1b is for example acetamido; R4 is for example an optionally substituted 5- or 6-membered heterocyclic ring system. Methods for making compounds of the 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其体内可水解的酯：式（I）其中C选自D和E，式（D），式（E） 2个a，R 6 a和R 3 a独立地选自例如H，CF 3，Me和Et ; R 2 b和R 6 b独立地选自例如H，F，CF 3，Me和Et; R 1是例如乙酰氨基; R 4是例如任选取代的5或6元杂环系。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。

4. 发明申请

US20080021071A1 3-{4-(Pyridin-3-Yl) 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-（吡啶-3-基）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：US20080021071A1
公开(公告)日：2008-01-24
申请号：US11569208
申请日：2005-05-24
申请人： Michael Gravestock , Folkert Reck , Fei Zhou
发明人： Michael Gravestock , Folkert Reck , Fei Zhou
IPC分类号： A61K31/4439 , A61K31/443 , A61P31/04 , C07D413/14
CPC分类号： C07D413/14
摘要： Compounds of formula (I), as well as pharmaceutically-acceptable salts and pro-drugs thereof, are disclosed wherein R1, R2, R3, and R4 are defined herein. Also disclosed are processes for making compounds of formula (I) as well as methods of using compounds of formula (I) for treating bacterial infections.
摘要翻译：公开了式（I）化合物及其药学上可接受的盐和前药，其中R 1，R 2，R 3， SUP>和R 4在本文中定义。还公开了制备式（I）化合物的方法以及使用式（I）化合物治疗细菌感染的方法。

5. 发明申请

US20080021012A1 3-[4-{6-Substituted Alkanoyl 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-取代的烷酰基吡啶-3-基] -3-苯基] -5-（1H-1,2,3-三唑-1-基甲基）-1,3-恶唑烷-2-酮抗菌剂
公开(公告)号：US20080021012A1
公开(公告)日：2008-01-24
申请号：US11569408
申请日：2005-05-24
申请人： Michael Gravestock , Folkert Reck , Fei Zhou
发明人： Michael Gravestock , Folkert Reck , Fei Zhou
IPC分类号： A61K31/397 , A61K31/4439 , A61K31/4523 , A61K31/5377 , A61P31/04 , C07D205/02 , C07D213/02 , C07D221/00 , C07D295/00
CPC分类号： C07D413/14
摘要： Compounds of formula (I) as well as pharmaceutically-acceptable salts and pro-drugs thereof are disclosed wherein R1, R2, R3, and R4 are defined herein. Also disclosed are processes for making compounds of formula (I) as well as methods of using compounds of formula (I) for treating bacterial infections.
摘要翻译：公开了式（I）化合物及其药学上可接受的盐和前药，其中R 1，R 2，R 3，和R 4在本文中定义。还公开了制备式（I）化合物的方法以及使用式（I）化合物治疗细菌感染的方法。

6. 发明申请

US20060116400A1 Oxazolidinone and/or isoxazoline derivatives as antibacterial agents 审中-公开
标题翻译：恶唑烷酮和/或异恶唑啉衍生物作为抗菌剂
公开(公告)号：US20060116400A1
公开(公告)日：2006-06-01
申请号：US10536686
申请日：2003-11-24
申请人： Daniel Carcanague , Michael Gravestock , Sheila Hauck , Thomas Weber , Neil Hales
发明人： Daniel Carcanague , Michael Gravestock , Sheila Hauck , Thomas Weber , Neil Hales
IPC分类号： A61K31/444 , A61K31/4439 , A61K31/422 , A61K31/42 , C07D413/14 , C07D413/02
CPC分类号： C07D413/14 , C07D413/10 , C07D417/14 , C07F9/653 , C07F9/65583
摘要： A compound of the formula (I), or a pharmaceutically-acceptable salt, or in-vivo hydrolysable ester thereof formula (I) wherein in (I) C is for example formula (D), formula (E), formula (H) wherein A and B are independently selected from (i) formula (J) and (ii) formula (K) m is 1 or 2; R2b and R6b, R2a and R6a, R3a and R5a, are for example selected from H, F, OMe and Me; R2b′ and R6b′, R2a′ and R6a′, R3a′, R5a′ are for example selected from H, OMe and Me; R1a is for example optionally substituted (1-10C)alkyl; R1b is for example selected from —NR5C(═W)R4, formula (a), or formula (b) wherein HET-1 is for example isoxazolyl and HET-2 is for example triazolyl or tetrazolyl. Methods for making compounds of the 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其体内可水解的酯（I）其中（I）中的C为例如式（D），式（E），式（H）其中A和B独立地选自（i）式（J）和（ⅱ）式（K）中m是1或2; R 2 b和R 6 b，R 2 a和R 6 a，R 3， a和R 5 a，例如选自H，F，OMe和Me; R 2'b'和R 6'b'，R 2'a'和R 6 a'，R“ 例如，从H，OMe和Me中选择a，b，b， R 1是例如任选取代的（1-10C）烷基; R 1是例如选自-NR 5 C（-W）R 4，式（a）或式（b）其中HET-1是例如异恶唑基，HET-2是例如三唑基或四唑基。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。

7. 发明申请

US20060270637A1 Hydroxymethyl substituted dihydroisoxazole derivatives useful as antibiotic agents 失效
标题翻译：用作抗生素的羟甲基取代的二氢异恶唑衍生物
公开(公告)号：US20060270637A1
公开(公告)日：2006-11-30
申请号：US10546373
申请日：2004-02-24
申请人： Michael Gravestock , Daniel Carcanague , Neil Hales
发明人： Michael Gravestock , Daniel Carcanague , Neil Hales
IPC分类号： A61K31/4439 , C07D413/14 , A61K31/655
CPC分类号： C07D413/14
摘要： Compounds of the formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, (I) R1a is NH(C═W)R5 or (a); W is O or S; R2 and R3 are for example H or F; R1 is for example hydrogen, or halogen; R5 is selected from hydrogen, (2-6C)alkyl (optionally substituted); R6 and R7 are independently selected from hydrogen, and (1-4C)alkyl (optionally substituted); wherein R4 is either a hydroxymethyl substituent on C-4′ of the isoxazoline ring; or R4 is a hydroxymethyl substituent on C-5′ of the isoxazoline ring and the stereochemistry at C-5′ of the isoxazoline ring and at C-5 of the oxazolidinone ring is selected, such that the compound of formula (I) is a single diastereomer; 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，（I）R 1a是NH（C-W）R 5或（a）; W为O或S; R 2和R 3是例如H或F; R 1是例如氢或卤素; R 5选自氢，（2-6C）烷基（任选取代的）; R 6和R 7独立地选自氢和（1-4C）烷基（任选取代的）; 其中R 4是异恶唑啉环的C-4'上的羟甲基取代基; 或R 4是异恶唑啉环的C-5'上的羟甲基取代基，并且选择异恶唑啉环的C-5'和恶唑烷酮环的C-5的立体化学，使得式（I）化合物是单一非对映异构体; 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。

8. 发明申请

US20070208062A1 3-(4-(2-DIHYDROISOXAZOL-3-YLPYRIDIN-5-YL)PHENYL)-5-TRIAZOL-1-YLMETHYLOXAZOLIDIN-2-ONE DERIVATIVES AS MAO INHIBITORS FOR THE TREATMENT OF BACTERIAL INFECTIONS 审中-公开
标题翻译： 3-（4-（2-二氢吲哚-3-基）吡啶-5-基）苯基）-5-三唑-1-基]甲氧基]苯甲酰胺-2-酮衍生物作为治疗细菌感染的抑制剂
公开(公告)号：US20070208062A1
公开(公告)日：2007-09-06
申请号：US11569150
申请日：2005-05-24
申请人： Daniel Carcanague , Michael Gravestock
发明人： Daniel Carcanague , Michael Gravestock
IPC分类号： A61K31/4439 , C07D413/14
CPC分类号： C07D413/14
摘要： Compounds of formula (I) as well as pharmaceutically-acceptable salts and pro-drugs thereof are disclosed wherein R1, R2, R3, and R4 are defined herein. Also disclosed are processes for making compounds of formula (I) as well as methods of using compounds of formula (I) for treating bacterial infections.
摘要翻译：公开了式（I）化合物及其药学上可接受的盐和前药，其中R 1，R 2，R 3，和R 4在本文中定义。还公开了制备式（I）化合物的方法以及使用式（I）化合物治疗细菌感染的方法。

9. 发明申请

US20060079695A1 Antibacterial oxalidinones 失效
标题翻译：抗菌草甘膦
公开(公告)号：US20060079695A1
公开(公告)日：2006-04-13
申请号：US10550038
申请日：2004-03-16
申请人： Michael Gravestock , Neil Hales , Sheila Hauck
发明人： Michael Gravestock , Neil Hales , Sheila Hauck
IPC分类号： C07D413/02
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 (1): wherein N-HeT is for example triazolyl; Q is for example phenyl or pyridyl, substituted withr; 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（1）：其中N-HeT是例如三唑基; Q是例如苯基或吡啶基，被 T例如选自（TAa1至TAa12），例如（TAa1）和（TAa5）：R 4h，R 5h，R 6h，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。

10. 发明申请

US20060116401A1 Antibacterial compounds 审中-公开
标题翻译：抗菌化合物
公开(公告)号：US20060116401A1
公开(公告)日：2006-06-01
申请号：US10536729
申请日：2003-11-24
申请人： Michael Gravestock , Neil Hales
发明人： Michael Gravestock , Neil Hales
IPC分类号： A61K31/444 , A61K31/4439 , A61K31/422 , C07D413/14
CPC分类号： C07D413/14 , C07F7/1804
摘要： A compound of the formula (I), or a pharmaceutically-acceptable salt, or in-vivo hydrolysable ester thereof wherein in (I) C is for example formula (D), (E), (H) wherein A and B are independently selected from formulae (i) and (ii) and R2b and R6b, R2b and R6a, R3a and R5a, are for example selected from H, F, OMe and Me; R2b′ and R6b′, R2a′ and R6a′, R3a′, R5a′ are for example selected from H, OMe and Me; R1a and R1b are for example selected from hydroxy, —OSi(tri-(1-6C)alkyl), NR5C(═W) R4, formla (a), formula (b) wherein HET-1 is for example isoxazolyl and HET-2 is for example triazolyl or tetrazolyl. Methods for making compounds of the 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其体内可水解的酯，其中在（I）中，C为例如式（D），（E），（H）其中A和B独立地为选自式（i）和（ii）和R 2 b和R 6 b，R 2 b和R 6， a，R 3 a和R 5 a，例如选自H，F，OMe和Me; R 2'b'和R 6'b'，R 2'a'和R 6 a'，R“ 例如，从H，OMe和Me中选择a，b，b， R 1 a和R 1 b是例如选自羟基，-OSi（三 - （1-6C）烷基），NR 5 C（-W）R 4，式（a），式（b）其中HET-1是例如异恶唑基，HET-2是例如三唑基或四唑基。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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