公开(公告)号：US07199143B2

公开(公告)日：2007-04-03

申请号：US10505902

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

发明人： Michael Barry Gravestock ,  Neil James Hales ,  Folkert Reck ,  Fei Zhou ,  Paul Robert Fleming ,  Daniel Robert Carcanague

IPC分类号： A61K31/442 ,  C07D413/10 ,  C07D263/20

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，

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。

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

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。

公开(公告)号：US20100137313A1

公开(公告)日：2010-06-03

申请号：US12572436

申请日：2009-10-02

申请人： Ann Boriack-Sjodin ,  Daniel Robert Carcanague ,  Daemian David Dussault ,  Holia Hatoum-Mokdad ,  Kenneth Gregory Hull ,  Georgine Ioannidis ,  John Irvin Manchester ,  Helen Maureen McGuire ,  David Charles McKinney ,  Suzanne Stokes

发明人： Ann Boriack-Sjodin ,  Daniel Robert Carcanague ,  Daemian David Dussault ,  Holia Hatoum-Mokdad ,  Kenneth Gregory Hull ,  Georgine Ioannidis ,  John Irvin Manchester ,  Helen Maureen McGuire ,  David Charles McKinney ,  Suzanne Stokes

IPC分类号： A61K31/5377 ,  C07D401/14 ,  A61K31/506 ,  C07D413/14

CPC分类号： C07D239/48 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

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。