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    Quinazoline-2,4-dione derivatives
    1.
    发明授权
    Quinazoline-2,4-dione derivatives 有权
    喹唑啉-2,4-二酮衍生物

    公开(公告)号：US08916573B2

    公开(公告)日：2014-12-23

    申请号：US14238415

    申请日：2012-08-10

    Applicant: Christian Hubschwerlen ,  Georg Rueedi ,  Jean-Philippe Surivet ,  Cornelia Zumbrunn Acklin

    Inventor： Christian Hubschwerlen ,  Georg Rueedi ,  Jean-Philippe Surivet ,  Cornelia Zumbrunn Acklin

    IPC: A01N43/54 ,  A61K31/517 ,  C07D239/72 ,  C07D401/00

    CPC classification number: C07D471/04 ,  C07D413/14 ,  C07D417/14 ,  C07D498/04 ,  C07D513/04

    Abstract: The invention relates to antibacterial compounds of formula (I), wherein R1 is H, halogen, (C1-C3)alkyl or (C1-C3)alkoxy; R2 is H, halogen, (C1-C3)alkyl, (C1-C3)alkoxy or pyrrolidin-1-yl; R3 is H, halogen, (C1-C3)alkyl, (C1-C3)alkoxy, vinyl or 2-methoxycarbonyvinyl or R2 and R3 together with the two carbon atoms which bear them form a phenyl ring; R4 is H, halogen, (C1-C3)alkyl or (C1-C3)alkoxy; and R5 is H, (C1-C3)alkyl or cyclopropyl, or R4 and R5form together a —CH2CH2CH2— group; A is the divalent group —CH2—, —CH2CH2—, #—CH(OH)CH2—*, #—CH2N(R6)—* and —CH2NHCH2—, wherein # indicates the point of attachment to the optionally substituted (quinazoline-2,4-dione-3-yl)methyl residue and * represents the point of attachment to the substituted (oxazolidinon-4-yl)methyl residue; R6 is H or acetyl; Y is CH or N; and Q is O or S; and salts of such compounds.

    Abstract translation: 本发明涉及式（I）的抗菌化合物，其中R1是H，卤素，（C1-C3）烷基或（C1-C3）烷氧基; R2是H，卤素，（C1-C3）烷基，（C1-C3）烷氧基或吡咯烷-1-基; R 3是H，卤素，（C 1 -C 3）烷基，（C 1 -C 3）烷氧基，乙烯基或2-甲氧基羰基乙烯基，或者R 2和R 3与它们的两个碳原子一起形成苯环; R4是H，卤素，（C1-C3）烷基或（C1-C3）烷氧基; 并且R 5是H，（C 1 -C 3）烷基或环丙基，或R 4和R 5一起形成-CH 2 CH 2 CH 2 - 基; A是二价基团-CH 2 - ， - CH 2 CH 2 - ， - CH 2 OH，-CH 2 - ， - CH 2 OH（R ​​6） - *和-CH 2 NHCH 2 - ，其中＃表示与任选取代的（喹唑啉 - 2,4-二酮-3-基）甲基残基，*表示与取代的（恶唑烷酮-4-基）甲基残基的连接点; R6是H或乙酰基; Y是CH或N; Q为O或S; 和这些化合物的盐。

    Spiro antibiotic derivatives
    4.
    发明授权
    Spiro antibiotic derivatives 失效
    螺环类抗生素衍生物

    公开(公告)号：US07999115B2

    公开(公告)日：2011-08-16

    申请号：US12439571

    申请日：2007-08-29

    Applicant: Christian Hubschwerlen ,  Jean-Philippe Surivet ,  Cornelia Zumbrunn-Acklin

    Inventor： Christian Hubschwerlen ,  Jean-Philippe Surivet ,  Cornelia Zumbrunn-Acklin

    IPC: C07D263/52 ,  C07D263/58

    CPC classification number: C07D498/10

    Abstract: The invention relates to compounds of formula (I) wherein R1 represents H, alkyl, alkoxy, cyano or halogen; one of U and X represents CH or N and the other represents CH, or, in the case of U, may also represent CRa and, in the case of X, may also represent CRb; Ra represents halogen; Rb represents halogen or alkoxy; B represents N, D represents CH2 and A represents CH(OH)CH2 or CH2CH2, or B represents CH, D represents CH2 or O and A represents OCH2, CH2CH(OH), CH(OH)CH2, CH(OH)CH(OH), CH═CH, CH2CH2 or NHCO, or also B represents C(OH), D represents CH2 and A represents OCH2, CH2CH(OH), CH(OH)CH2, CH(OH)CH(OH), CH═CH, CH2CH2 Or NHCO; R2 represents H, alkyl, alkenyl, hydroxyalkyl or alkoxycarbonylalkyl; and E represents naphthyl or a binuclear heterocyclic group; and to salts of such compounds. These compounds are useful as antimicrobial agents.

    Abstract translation: 本发明涉及式（I）化合物，其中R 1表示H，烷基，烷氧基，氰基或卤素; U和X之一表示CH或N，另一个表示CH，或在U的情况下也可以表示CR a，在X的情况下也可以表示CRb; Ra表示卤素; Rb表示卤素或烷氧基; B表示N，D表示CH 2，A表示CH（OH）CH 2或CH 2 CH 2，或B表示CH，D表示CH 2或O，A表示OCH 2，CH 2 CH（OH），CH（OH）CH 2，CH（OH） OH），CH = CH，CH 2 CH 2或NHCO，或B表示C（OH），D表示CH 2，A表示OCH 2，CH 2 CH（OH），CH（OH）CH 2，CH（OH）CH（OH） CH，CH 2 CH 2或NHCO; R2代表H，烷基，烯基，羟基烷基或烷氧基羰基烷基; E表示萘基或双核杂环基; 和这些化合物的盐。 这些化合物可用作抗微生物剂。

    Antibiotics Derivatives
    7.
    发明申请
    Antibiotics Derivatives 失效

    公开(公告)号：US20080280888A1

    公开(公告)日：2008-11-13

    申请号：US11915179

    申请日：2006-05-24

    Applicant: Daniel Bur ,  Christian Hubschwerlen ,  Jean-Philippe Surivet ,  Cornelia Zumbrunn-Acklin

    Inventor： Daniel Bur ,  Christian Hubschwerlen ,  Jean-Philippe Surivet ,  Cornelia Zumbrunn-Acklin

    IPC: A61K31/5415 ,  C07D417/02 ,  A61K31/538 ,  A61K31/428 ,  A61K31/542 ,  C07D513/04

    CPC classification number: C07D277/64 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D513/04

    Abstract: The invention relates to antibiotic derivatives of formula I wherein: A represents —O—, S, —C(═O)—, —C(═NOR6)—; Z-B represents NCH2CH2, NCOCH2, NCH2CO, NCH2CH(OH), CHN(R8)CH2 or CHN(R8)CO; D represents binuclear heteroaryl; Y1 represents —CR1— or —N—, Y2 represents —CR2— or —N—, Y3 represents —CR3— or —N— and Y4 represents —CR4— or —N—; U represents —NH—, —O— or —S— and V represents —N— or —CH—; W represents —CH2—, —O— or —NR7—; R1 represents H, methyl, ethyl or halogen; R2, R3 and R4 each represent independently H, C1-C4 alkyl, halogen, or C1-C4 alkoxy; R5 represents H, C1-C4 alkyl or fluorine; R6 represents H, C1-C4 alkyl or aryl-C1-C4 alkyl; R7 represents H, C1-C4 alkyl, aryl-C1-C4 alkyl or —CH2—COOH; R8 represents H, C1-C4 alkyl or —CH2—COOH; with the provisos that if Z-B represents NCH2CH2, NCOCH2, NCH2CO or NCH2CH(OH), then W represents —CH2—; if A represents O or S, then W represents —CH2—; and only one or two of Y1, Y2, Y3 and Y4 can represent N at the same time.

    Tricyclic antibiotics
    9.
    发明授权
    Tricyclic antibiotics 失效
    三环类抗生素

    公开(公告)号：US08012961B2

    公开(公告)日：2011-09-06

    申请号：US12988205

    申请日：2009-04-14

    Applicant: Christian Hubschwerlen ,  Georg Rueedi ,  John-Philippe Surivet ,  Cornelia Zumbrunn-Acklin

    Inventor： Christian Hubschwerlen ,  Georg Rueedi ,  John-Philippe Surivet ,  Cornelia Zumbrunn-Acklin

    IPC: C07D491/048 ,  C07D519/00 ,  A61K31/33

    CPC classification number: C07D491/048 ,  C07D519/00

    Abstract: The invention relates to antibacterial compounds of formula (I) wherein U represents CH or N; W represents CH or N; R1 represents alkoxy, halogen or CN; ring A represents a pyrrolidin-1,3-diyl-, a piperidin-1,3-diyl or a morpholin-2,4-diyl group and B represents CH2; or ring A is selected from the groups drawn below: wherein R2 represents H, F or hydroxymethyl, and B is absent; G represents a group selected from the group consisting of  —CH═CH-E, wherein Y1, Y2, Y3 and Z independently represent CH or N; Q represents O or S; and E represents phenyl which is mono- or di-substituted wherein the substituents are each independently halogen; and to pharmaceutically acceptable salts of such compounds.

    Abstract translation: 本发明涉及式（I）的抗菌化合物，其中U代表CH或N; W表示CH或N; R 1表示烷氧基，卤素或CN; 环A表示吡咯烷-1,3-二基 - 哌啶-1,3-二基或吗啉代-2,4-二基，B表示CH 2; 或环A选自下列基团：其中R2表示H，F或羟甲基，B不存在; G表示选自-CH = CH-E的基团，其中Y1，Y2，Y3和Z独立地表示CH或N; Q表示O或S; 并且E表示被单取代或二取代的苯基，其中取代基各自独立地为卤素; 以及这些化合物的药学上可接受的盐。

    OXAZOLIDINYL ANTIBIOTICS
    10.
    发明申请
    OXAZOLIDINYL ANTIBIOTICS 有权
    奥昔布林抗生素

    公开(公告)号：US20110201595A1

    公开(公告)日：2011-08-18

    申请号：US13123708

    申请日：2009-10-09

    Applicant: Christian Hubschwerlen ,  Georg Rueedi ,  Jean-Philippe Surivet ,  Cornelia Zumbrunn-Acklin

    Inventor： Christian Hubschwerlen ,  Georg Rueedi ,  Jean-Philippe Surivet ,  Cornelia Zumbrunn-Acklin

    IPC: A61K31/5415 ,  A61K31/538 ,  A61K31/4985 ,  A61K31/4704 ,  C07D417/14 ,  C07D413/14 ,  C07D487/04 ,  A61P31/04

    CPC classification number: C07D413/14 ,  C07D413/12 ,  C07D417/14 ,  C07D471/04

    Abstract: The invention relates to antibacterial compounds of formula I wherein R1 is alkoxy or halogen; U and V each independently are CH or N; is a bond or is absent; W is CH or N or, when is absent, W is CH2 or NH, with the proviso that U, V and W are not all N; A is a bond or CH2; R2 is H or, provided A is CH2, may also be OH; m and n each independently are 0 or 1; D is CH2 or a bond; G represents a phenyl group substituted once or twice in the meta and/or para position(s) by substituents selected from alkyl, (C1-C3)alkoxy and halogen, or G is a group G1 or G2 wherein Z1, Z2 and Z3 may each represent CH or N; X is N or CH and Q is O or S; it being understood that if m and n each are 0, then A is CH2; and salts of such compounds.

    Abstract translation: 本发明涉及式I的抗菌化合物，其中R 1是烷氧基或卤素; U和V各自独立地为CH或N; 是债券或不存在; W是CH或N，当不存在时，W是CH 2或NH，条件是U，V和W不全为N; A是键或CH2; R2是H，或者如果A是CH2，也可以是OH; m和n各自独立地为0或1; D是CH 2或键; G表示在间位和/或对位通过选自烷基，（C 1 -C 3）烷氧基和卤素的取代基取代一次或两次的苯基，或G是基团G1或G2，其中Z1，Z2和Z3可以 各自表示CH或N; X为N或CH，Q为O或S; 应理解，如果m和n各自为0，则A为CH 2; 和这些化合物的盐。

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