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11. 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。

12. 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。

13. 发明授权

US07192974B2 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：US07192974B2
公开(公告)日：2007-03-20
申请号：US10546373
申请日：2004-02-24
申请人： Michael Barry Gravestock , Daniel Robert Carcanague , Neil James Hales
发明人： Michael Barry Gravestock , Daniel Robert Carcanague , Neil James Hales
IPC分类号： C07D413/14 , A61K31/4427
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

14. 发明授权

US07141583B2 Oxazolidinone derivatives with antibiotic activity 有权
标题翻译：具有抗菌活性的恶唑烷酮衍生物
公开(公告)号：US07141583B2
公开(公告)日：2006-11-28
申请号：US10258355
申请日：2001-04-23
申请人： Michael Barry Gravestock , Michael John Betts , Ian Richard Matthews , David Alan Griffin
发明人： Michael Barry Gravestock , Michael John Betts , Ian Richard Matthews , David Alan Griffin
IPC分类号： A61K31/4439 , A61K31/454 , C07D401/14
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D413/06 , C07D413/14 , C07D417/14 , C07D491/10
摘要： Compounds of the formula (I), or a pharmaceutically acceptable salt, or an in-vivo-hydrolysable ester thereof, wherein HET is an N-linked 5-membered heteroaryl ring, optionally substituted on a C atom by an oxo or thioxo group; and/or by 1 or 2 (1–4C)alkyl groups; and/or on an available nitrogen atom by (1–4C)alkyl; or HET is an N-linked 6-membered heteroaryl ring containing up to three nitrogen heteroatoms in total, optionally substituted on a C atom as above; Q is selected from, for example, Q1 R2 and R3 are independently hydrogen or fluoro; T is selected from a range of groups, for example, of formula (TC5) wherein Rc is, for example, R13CO—, R13SO2— or R13CS—; wherein R13 is, for example, optionally substituted (1–10C)alkyl or R14C(O)O(1–6C)alkyl wherein R14 is optionally substituted (1–10C)alkyl; 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HET是通过氧代或硫代基团在C原子上取代的N-连接的五元杂芳基环; 和/或1或2（1-4C）烷基; 和/或在可用的氮原子上由（1-4C）烷基取代; 或HET是总共含有多达三个氮杂原子的N-连接的6-元杂芳基环，任选地如上所述在C原子上取代; Q选自例如Q1 R 2和R 3独立地是氢或氟; T选自例如式（TC5）的基团范围，其中R c是例如R 13 CO-，R 13 SO 2 - 或R 13 CS-; 其中R 13为例如任选取代的（1-10C）烷基或R 14 C（O）O（1-6C）烷基，其中R 14 任选取代的（1-10C）烷基; 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。

15. 发明授权

US06617339B1 Oxazolidinone derivatives, process for their preparation and pharmaceutical compositions containing them 失效
标题翻译：恶唑烷酮衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US06617339B1
公开(公告)日：2003-09-09
申请号：US09719012
申请日：2000-12-05
申请人： Michael Barry Gravestock
发明人： Michael Barry Gravestock
IPC分类号： A61K31443
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D451/02 , C07D487/08 , C07F9/59 , C07F9/65583
摘要： Compounds of formula (I) as defined herein, or a pharmaceutically acceptable salt, or an in-vivo-hydrolysable ester thereof, are useful as antibacterial agents. Processes for their manufacture and pharmaceutical compositions containing them are described.
摘要翻译：本文定义的式（I）化合物或其药学上可接受的盐或其体内可水解的酯可用作抗菌剂。描述了其制备方法和含有它们的药物组合物。

16. 发明授权

US06734200B1 Heterocyclylaminomethyloxazolidinones as antibacterials 失效
标题翻译：杂环氨基甲基恶唑烷酮作为抗菌剂
公开(公告)号：US06734200B1
公开(公告)日：2004-05-11
申请号：US09807113
申请日：2001-04-05
申请人： Michael Barry Gravestock
发明人： Michael Barry Gravestock
IPC分类号： C07C41314
CPC分类号： C07D413/12 , C07D413/14 , C07D417/14 , C07F9/65583
摘要： Compounds of formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolyzable ester thereof, wherein, for example, HET is an optionally substituted C-linked 5-membered heteroaryl ring containing 2 to 4 heteroatoms independently selected from N, O and S; Q is selected from, for example, Q1 and Q2: R2 and R3 are independently hydrogen or fluoro; T is selected from a range of groups, for example, an N-linked (fully unsaturated) 5-membered heteroaryl ring system or a group of formula (TC5): wherein Rc is, for example, R13CO—, R13SO2— or R13CS—; wherein R13 is, for example, optionally substituted (1-10C)alkyl or R14C(O)O(1-6C)alkyl wherein R14 is optionally substituted (1-10C)alkyl; 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，其中例如HET是任选取代的C连接的5元杂芳基环，其含有2至4个独立地选自 N，O和S; Q选自例如Q1和Q2：R 2和R 3独立地是氢或氟; T选自一组范围，例如，N-连接的（完全不饱和的）5元杂芳基环系或式（TC5）的基团：其中Rc是例如R 13 CO-，R SO 2 - 或R 13 CS-; 其中R 13为例如任选取代的（1-10C）烷基或R 14 C（O）O（1-6C）烷基，其中R 14为任选取代的（1-10C）烷基; 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。

17. 发明授权

US06365751B1 Antibiotic oxazolidinone derivatives 失效
标题翻译：抗生素恶唑烷酮衍生物
公开(公告)号：US06365751B1
公开(公告)日：2002-04-02
申请号：US09836095
申请日：2001-04-17
申请人： Michael Barry Gravestock
发明人： Michael Barry Gravestock
IPC分类号： C07D26304
CPC分类号： C07D413/10 , C07D413/14 , C07D513/04
摘要： The invention concerns a compound of the formula (I): wherein, for example: R1 is of the formula —NHC(═O)Rb wherein Rb is, for example, (1-4C)alkyl; R2 and R3 are hydrogen or fluoro; R2 and R3 are hydrogen or fluoro; D is O; R4 and R5 are hydrogen, (1-4C)alkyl or AR-oxymethyl; AR is phenyl or phenyl(1-4C)alkyl; R6 is hydrogen; >A—B— is of the formula >C═C(Ra)—, >CHCHRa—, or >C(OH)CHRa— (> represents two single bonds) wherein Ra is hydrogen or (1-4C)alkyl; and pharmaceutically-acceptable salts thereof; processes for their preparation; pharmaceutical compositions containing them and their use as antibacterial agents.
摘要翻译：本发明涉及式（I）化合物：其中，例如：R 1为式-NHC（= O）Rb，其中R b为例如（1-4C）烷基; R 2和R 3为氢或氟 ; R 2和R 3为氢或氟; D为O; R 4和R 5为氢，（1-4C）烷基或AR-氧甲基; AR为苯基或苯基（1-4C）烷基; R6为氢;> AB-为其中R a是氢或（1-4C）烷基;及其药学上可接受的盐;式C = C（R a） - ，> CHCHRa-或> C（OH）CHRA- 其准备过程; 含有它们的药物组合物及其作为抗菌剂的用途。

18. 发明授权

US07087629B2 Heterocyclylaminomethyloxazolidinones as antibacterials 失效
标题翻译：杂环氨基甲基恶唑烷酮作为抗菌剂
公开(公告)号：US07087629B2
公开(公告)日：2006-08-08
申请号：US10382396
申请日：2003-03-06
申请人： Michael Barry Gravestock
发明人： Michael Barry Gravestock
IPC分类号： A61K31/422 , C07D413/12 , C07D417/12
CPC分类号： C07D413/12 , C07D413/14 , C07D417/14 , C07F9/65583
摘要： Compounds of formula (I) or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, wherein, for example, HET is an optionally substituted C-linked 5-membered heteroaryl ring containing 2 to 4 heteroatoms independently selected from N, O and S; Q is selected from, for example, Q3 and Q5; R2 and R3 are independently hydrogen or fluoro; T is selected from a range of groups, for example, an N-linked (fully unsaturated) 5-membered heteroaryl ring system or a group of formula (TC5): wherein Rc is, for example, R13CO—, R13SO2— or R13CS—; wherein R13 is, for example, optionally substituted (1–10C)alkyl or R14C(O)O(1–6C)alkyl wherein R14 is optionally substituted (1–10C)alkyl; 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，其中例如HET是任选取代的C连接的5元杂芳基环，其含有2至4个独立地选自N ，O和S; Q选自例如Q3和Q5; R 2和R 3独立地是氢或氟; T选自一组范围，例如，N-连接的（完全不饱和的）5元杂芳基环系或式（TC5）的基团：其中Rc是例如R 13 CO-，R 13 SO 2 - 或R 13 CS-; 其中R 13为例如任选取代的（1-10C）烷基或R 14 C（O）O（1-6C）烷基，其中R 14 任选取代的（1-10C）烷基; 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。

19. 发明授权

US06605630B1 Antibiotic oxazolidinone derivatives 失效
标题翻译：抗生素恶唑烷酮衍生物
公开(公告)号：US06605630B1
公开(公告)日：2003-08-12
申请号：US09486092
申请日：2000-02-18
申请人： Michael Barry Gravestock
发明人： Michael Barry Gravestock
IPC分类号： A61K3142
CPC分类号： C07D413/10 , C07D413/14 , C07D471/04
摘要： The invention concerns a compound of the formula (I): wherein, for example: T is of the formula (IA), (IB), or (IC); R1 is of the formula —NHC(═O)Rb wherein Rb is (1-4C)alkyl; R2 and R3 are hydrogen or fluoro; >A—B— is >C═CH— (but not when T is (IA)) or >CH—CH2—; wherein when T is of the formula (IA) or (IB); R6 is, for example, (1-4C)alkyl; R5 is hydrogen, R10CO—, R10SO2— or R10CS— wherein R10 is, for example, optionally substituted phenyl, or (1-10C)alkyl, or when T is of the formula (IA), (IB); or (IC): R5 and R6 are linked to give a 5- or 6-membered ring which is fused to the ring shown in (IA), (IB), or (IC) so as to give an optionally substituted bicyclic ring; and pharmaceutically acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them, and their use as antibacterial agents.
摘要翻译：本发明涉及式（I）化合物：其中，例如：T为式（IA），（IB）或（IC）; R1为式-NHC（= O）Rb，其中Rb为（1-4C）烷基; R2和R3是氢或氟;> AB-是> C = CH-（但不是当T是（IA））或> CH-CH 2 - 时;其中当T是式）或（IB）; R6是例如（1-4C）烷基; R 5为氢，R 10 CO-，R 10 SO 2 - 或R 10 CS-，其中R 10为例如任选取代的苯基或（1-10C）烷基，或当T为式（IA），（IB））时。或（IC）：R5和R6连接，得到与（IA），（IB）或（IC）所示的环稠合的5-或6-元环，得到任选取代的双环; 及其药学上可接受的盐，其制备方法，含有它们的药物组合物及其作为抗菌剂的用途。

20. 发明授权

US06350775B1 3-phenyl-furan-(5H)-2-one and dihydrofuran-2-one derivatives as antibacterial agents 失效
标题翻译： 3-苯基 - 呋喃 - （5H）-2-酮和二氢呋喃-2-酮衍生物作为抗菌剂
公开(公告)号：US06350775B1
公开(公告)日：2002-02-26
申请号：US09621949
申请日：2000-07-24
申请人： Michael Barry Gravestock
发明人： Michael Barry Gravestock
IPC分类号： A61K31341
CPC分类号： C07D405/10 , C07D405/12 , C07D407/10 , C07D409/10
摘要： A compound of formula (I): wherein R1 is hydroxy or of the formula —NHC(═O)(1-4C)alkyl or —NHS(O)n(1-4C)alkyl wherein n is 0, 1 or 2; R2 and R3 are independently hydrogen or fluoro; R4 and R5 are independently hydrogen or methyl; >A—B— is of the formula >C═CH—, or >C(OH)CH2—; >X—Y— is of the formula >C=CH—, or >CHCH2—; and D is S, SO, or SO2; or a pharmaceutically-acceptable salt thereof.
摘要翻译：式（I）化合物：其中R1是羟基或式-NHC（= O）（1-4C）烷基或-NHS（O）n（1-4C）烷基，其中n是0,1或2; R2 并且R 3独立地是氢或氟; R 4和R 5独立地是氢或甲基;> AB-是下式：C = CH-或> C（OH）CH 2 - ;> XY-是式C = CH - 或> CHCH2-; 和D是S，SO或SO 2;或其药学上可接受的盐。

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