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12 条记录 (耗时 0.053 秒)

    Oxazolidinone And/Or Isoxazoline As Antibacterial Agents
    3.
    发明申请
    Oxazolidinone And/Or Isoxazoline As Antibacterial Agents 审中-公开
    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。

    Phenanthroline derivatives
    4.
    发明授权
    Phenanthroline derivatives 失效
    菲咯啉衍生物

    公开(公告)号：US5916898A

    公开(公告)日：1999-06-29

    申请号：US957450

    申请日：1997-10-24

    申请人： Philip Neil Edwards ,  Michael Stewart Large ,  Neil James Hales

    发明人： Philip Neil Edwards ,  Michael Stewart Large ,  Neil James Hales

    IPC分类号： A61K31/4745 ,  C07D471/04 ,  A61K31/435 ,  C07D471/18

    CPC分类号： C07D471/04 ,  A61K31/4745

    摘要： The present invention provides a phenanthroline derivative of formula (I) ##STR1## wherein, for example, R.sup.1 is hydrogen, carboxy, cyano, nitro, (1-4C)alkyl, (1-6C)alkoxycarbonyl, (1-4C)alkylamino, (2-4C)alkanoyl, (1-4C)alkoxy-(2-4C)alkoxy-(2-4C)alkoxycarbonyl or N-�amino-(2-8C)alkyl!carbamoyl;R.sup.2 is, for example, hydrogen, carboxy, (1-6C)alkoxycarbonyl, carbamoyl, N-(1-8C)alkylcarbamoyl, N,N-di-(1-8C)alkylcarbamoyl, N-(1-4C)alkylcyclohexylcarbamoyl, 1,2,3,4-tetrahydro-isoquinolin-2-ylcarbonyl or N,N-�di-(1-4C)alkyl!thiocarbamoyl;R.sup.3 and R.sup.4, which may be the same or different, are, for example, hydrogen or halo; andR.sup.5 is, for example, hydrogen, di-(1-4C)alkylamino or halo; or a pharmaceutically-acceptable salt thereof.The invention further provides pharmaceutical compositions comprising phenanthroline derivatives, processes for making the same and their use in producing an anti-fibroproliferative effect.

    摘要翻译： 本发明提供式（I）的菲咯啉衍生物，其中例如R 1是氢，羧基，氰基，硝基，（1-4C）烷基，（1-6C）烷氧基羰基，（1-4C）烷基氨基，（2 -4C）烷酰基，（1-4C）烷氧基 - （2-4C）烷氧基 - （2-4C）烷氧基羰基或+ E，未N + EE- [氨基 - （2-8C）烷基]氨基甲酰基; R2是例如氢，羧基，（1-6C）烷氧基羰基，氨基甲酰基，+ E，不为N + EE-（1-8C）烷基氨基甲酰基，+ E，非N + EE，+ E， （1-8C）烷基氨基甲酰基，+ E，N + EE - （1-4C）烷基环己基氨基甲酰基，1,2,3,4-四氢 - 异喹啉-2-基羰基或+ E，不N + EE，+ E ，N + EE - [二（1-4C）烷基]硫代氨基甲酰基; R 3和R 4可以相同或不同，例如是氢或卤素; 和R5是例如氢，二 - （1-4C）烷基氨基或卤素; 或其药学上可接受的盐。 本发明还提供了包含菲咯啉衍生物的药物组合物，其制备方法及其在产生抗纤维增生作用中的用途。

    Oxazolidinones as antibacterial agents
    6.
    发明授权
    Oxazolidinones as antibacterial agents 失效
    恶唑烷酮作为抗菌剂

    公开(公告)号：US07498350B2

    公开(公告)日：2009-03-03

    申请号：US10536687

    申请日：2003-11-24

    申请人： Michael Barry Gravestock ,  Neil James Hales ,  Folkert Reck ,  Fei Zhou

    发明人： Michael Barry Gravestock ,  Neil James Hales ,  Folkert Reck ,  Fei Zhou

    IPC分类号： A61K31/44 ,  C07D413/00

    CPC分类号： C07D413/14

    摘要： A compound of the formula (I), or a pharmaceutically-acceptable salt, or in-vivo hydrolysable ester thereof: Wherein C is selected from (D) and (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 optionally substituted diazolyl, triazolyl or tetrazolyl; 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：其中C选自（D）和（E），R 2a，R 6a和R 3a独立地选自例如H ，CF3，Me和Et; R2b和R6b独立地选自H，F，CF3，Me和Et; R 1b是例如任选取代的二唑基，三唑基或四唑基; R4是例如任选取代的5元或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。

    Oxazolidinone and/or isoxazoline as antibacterial agents
    8.
    发明授权
    Oxazolidinone and/or isoxazoline as antibacterial agents 失效
    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。

    Hydroxymethyl substituted dihydroisoxazole derivatives useful as antibiotic agents
    9.
    发明授权
    Hydroxymethyl substituted dihydroisoxazole derivatives useful as antibiotic agents 失效
    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