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    5-AMINOCYCLYLMETHYL-OXAZOLIDIN-2-ONE DERIVATIVES
    12.
    发明申请
    5-AMINOCYCLYLMETHYL-OXAZOLIDIN-2-ONE DERIVATIVES 有权
    5-氨基环戊基 - 氧杂环丁烷-2-酮衍生物

    公开(公告)号：US20110003789A1

    公开(公告)日：2011-01-06

    申请号：US12809555

    申请日：2008-12-17

    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 ,  C07D471/04 ,  C07D417/14 ,  C07D413/14 ,  C07D498/04 ,  A61K31/517 ,  A61K31/538 ,  A61K31/5395 ,  A61P31/04

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

    Abstract: The invention relates to antibacterial compounds of formula I wherein one or two of U, V, W, and X represent N, the rest represent CH or, in the case of X, may also represent CRa wherein Ra is fluorine; R1 represents alkoxy, halogen or cyano; R2 represents H, CH2OH, CH2N3, CH2NH2, alkylcarbonylaminomethyl or triazol-1-ylmethyl; R3 represents H, or, when n is 1, R3 may also represent OH, NH2, NHCOR6 or triazol-1-yl; A represents CR4; K represents O, NH, OCH2, NHCO, NHCH2, CH2NH, CH2CH2, CH═CH, CHOHCHOH or CHR5; R4 represents H or together with R5 forms a bond, or also R4 can represent OH when K is not O, NH, OCH2 or NHCO; R5 represents OH or together with R4 forms a bond; R6 represents alkyl; m is 0 or 1 and n is 0 or 1; and G is as defined in the description; and to salts of such compounds.

    Abstract translation: 本发明涉及式I的抗菌化合物，其中U，V，W和X中的一个或两个表示N，其余表示CH，或在X的情况下，也可以表示其中Ra为氟的CRa; R 1表示烷氧基，卤素或氰基; R 2表示H，CH 2 OH，CH 2 N 3，CH 2 NH 2，烷基羰基氨基甲基或三唑-1-基甲基; R3表示H，或当n为1时，R3也可以表示OH，NH2，NHCOR6或三唑-1-基; A代表CR4; K表示O，NH，OCH 2，NHCO，NHCH 2，CH 2 NH，CH 2 CH 2，CH = CH，CHOHCHOH或CHR 5; R 4表示H或与R 5一起形成键，或者当K不是O，NH，OCH 2或NHCO时，R 4可以表示OH; R5表示OH或与R4一起形成键; R6代表烷基; m为0或1，n为0或1; 并且G如说明书中所定义; 和这些化合物的盐。

    Ethanol or 1,2-ethanediol cyclohexyl antibiotic derivatives
    13.
    发明授权
    Ethanol or 1,2-ethanediol cyclohexyl antibiotic derivatives 有权
    乙醇或1,2-乙二醇环己基抗生素衍生物

    公开(公告)号：US07820655B2

    公开(公告)日：2010-10-26

    申请号：US12279329

    申请日：2007-02-14

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

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

    IPC: C07D498/04 ,  A61K31/542 ,  A61K31/5383

    CPC classification number: C07D471/04 ,  C07D241/44 ,  C07D513/04

    Abstract: The invention relates to antibiotic ethanol or 1,2-ethanediol cyclohexyl derivatives of formula (I) wherein R1 represents (C1-C4)alkoxy; one or two of U, V, W and X represents) N and the remaining represent each independently CH or, in the case of V or X, may also represent CRa; Ra represents halogen; R2 represents H or OH; A represents CH2, CO, CH2CH═CH or COCH═CH; D represents a phenyl group optionally substituted one or two times by halogen atoms, or D represents a group of the formula (II) in which Q is oxygen or sulphur; and to salts of these derivatives of formula (I).

    Abstract translation: 本发明涉及式（I）的抗生素乙醇或1,2-乙二醇环己基衍生物，其中R1表示（C1-C4）烷氧基; U，V，W和X中的一个或两个表示）N，其余各自独立地表示CH，或者在V或X的情况下也可以表示CRa; Ra表示卤素; R2表示H或OH; A表示CH 2，CO，CH 2 CH = CH或COCH = CH; D表示任选被卤素原子取代一或两次的苯基，或D表示其中Q为氧或硫的式（II）的基团; 和式（I）的这些衍生物的盐。

    OXAZOLIDINONE ANTIBIOTIC DERIVATIVES
    14.
    发明申请
    OXAZOLIDINONE ANTIBIOTIC DERIVATIVES 有权
    奥沙利汀抗生素衍生物

    公开(公告)号：US20100137290A1

    公开(公告)日：2010-06-03

    申请号：US12595711

    申请日：2008-04-10

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

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

    IPC: A61K31/5415 ,  C07D471/02 ,  A61K31/4375 ,  C07D215/00 ,  A61K31/4709 ,  C07D279/16 ,  C07D241/36 ,  A61K31/498 ,  C07D413/14 ,  A61K31/517 ,  C07D265/36 ,  A61K31/536 ,  A61P31/04

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

    Abstract: The invention relates to antibacterial compounds of formula I wherein R1 is hydrogen, halogen, hydroxy, alkoxy or cyano; Y1 and Y2 each represent CH, one or two of U, V, W and X represent(s) N and the remaining each represent CH or, in the case of X, may also represent CRa, Ra being halogen, and, in the case of W, may also represent CRb, or each of U, V, W, X, Y1 and Y2 represents CH, or each of U, V, W, X and Y1 represents CH and Y2 represents N, or also one or, provided R1 is hydrogen, two of U, V, W, X, Y1 and Y2 represent(s) CRC and the remaining each represent CH, Rb being alkoxy, alkoxycarbonyl or alkoxyalkoxy and Rc being, each time it occurs, independently represents hydroxy or alkoxy; A-B-D represents a chain of 4 to 6 atoms, which 4 to 6 atoms are seleted from carbon, oxygen and nitrogen and may be substituted; E is one of the following groups: in which Z is CH or N and Q is O or S, or E is a phenyl group which is substituted once or twice in the meta and/or para position(s); and to salts of such compounds.

    Abstract translation: 本发明涉及式I的抗菌化合物，其中R 1是氢，卤素，羟基，烷氧基或氰基; Y1和Y2各自表示CH，U，V，W和X中的一个或两个表示（s）N，其余各自表示CH，或在X的情况下也可以表示CR a，R a为卤素，并且在 W的情况也可以表示CRb，或者U，V，W，X，Y1，Y2各自表示CH，或U，V，W，X，Y1各自表示CH，Y2表示N， 如果R1是氢，则U，V，W，X，Y1和Y2中的两个表示（s）CRC，其余各自表示CH，Rb是烷氧基，烷氧基羰基或烷氧基烷氧基，Rc每次发生时，独立地表示羟基或 烷氧基 A-B-D表示4至6个原子的链，其中4至6个原子从碳，氧和氮中分离并可以被取代; E是以下组之一：其中Z是CH或N，Q是O或S，或E是在间位和/或对位被取代一次或两次的苯基; 和这些化合物的盐。

    SPIRO ANTIBIOTIC DERIVATIVES
    15.
    发明申请
    SPIRO ANTIBIOTIC DERIVATIVES 失效
    SPIRO抗生素衍生物

    公开(公告)号：US20090270375A1

    公开(公告)日：2009-10-29

    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: A61K31/5415 ,  C07D471/04 ,  A61K31/538 ,  A61K31/4375 ,  A61P31/04

    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。

    Ethanol or 1,2-Ethanediol Cyclohexyl Antibiotic Derivatives
    16.
    发明申请
    Ethanol or 1,2-Ethanediol Cyclohexyl Antibiotic Derivatives 有权
    乙醇或1,2-乙二醇环己基抗生素衍生物

    公开(公告)号：US20090005368A1

    公开(公告)日：2009-01-01

    申请号：US12279329

    申请日：2007-02-14

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

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

    IPC: A61K31/542 ,  C07D513/04 ,  A61K31/5383 ,  A61P31/04 ,  A61P33/02 ,  C07D498/04

    CPC classification number: C07D471/04 ,  C07D241/44 ,  C07D513/04

    Abstract: The invention relates to antibiotic ethanol or 1,2-ethanediol cyclohexyl derivatives of formula (I) wherein R1 represents (C1-C4)alkoxy; one or two of U, V, W and X represents) N and the remaining represent each independently CH or, in the case of V or X, may also represent CRa; Ra represents halogen; R2 represents H or OH; A represents CH2, CO, CH2CH═CH or COCH═CH; D represents a phenyl group optionally substituted one or two times by halogen atoms, or D represents a group of the formula (II) in which Q is oxygen or sulphur; and to salts of these derivatives of formula (I).

    Abstract translation: 本发明涉及式（I）的抗生素乙醇或1,2-乙二醇环己基衍生物，其中R1表示（C1-C4）烷氧基; U，V，W和X中的一个或两个表示）N，其余各自独立地表示CH，或者在V或X的情况下也可以表示CRa; Ra表示卤素; R2表示H或OH; A表示CH 2，CO，CH 2 CH-CH或COCH-CH; D表示任选被卤素原子取代一或两次的苯基，或D表示其中Q为氧或硫的式（II）的基团; 和式（I）的这些衍生物的盐。

    Azatricyclic antibiotic compounds
    17.
    发明授权
    Azatricyclic antibiotic compounds 有权
    抗生素化合物

    公开(公告)号：US08349828B2

    公开(公告)日：2013-01-08

    申请号：US12918749

    申请日：2009-02-19

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

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

    IPC: A61K31/54 ,  C07D279/16

    CPC classification number: C07D498/16 ,  C07D455/04 ,  C07D471/16 ,  C07D519/00

    Abstract: The invention relates to antibacterial compounds of formula I wherein n is 0 or 1; R1 represents H or F; U represents CH2 or, provided n is 1, O or NH; “-----” is a bond or is absent; V represents CH or N when “-----” is a bond, or CH2 or NH when “-----” is absent; W represents CH or N; A represents —(CH2)p—NH—(CH2)q— wherein p is 1 and q is 1 or 2 or, provided U represents CH2 and n is 1, p may also be 0 and q is then 2; G represents one of the groups 1 wherein Z represents N or CH and Q represents O or S; and Z0, Z1 and Z2 each represent CH, or Z0 and Z1 each represent CH and Z2 represents N, or Z0 represents CH, Z1 represents N and Z2 represents CH or N, or Z0 represents N and Z1 and Z2 each represent CH; and to salts of such compounds.

    Abstract translation: 本发明涉及式I的抗菌化合物，其中n为0或1; R1表示H或F; U表示CH 2，或者n为1，O或NH; -----是债券或不存在; 当-----为键时，V表示CH或N，当不存在时，表示CH2或NH; W表示CH或N; A表示 - （CH 2）p -NH-（CH 2）q - ，其中p为1且q为1或2，或者，如果U表示CH 2且n为1，p也可以为0，q为2; G表示1组，其中Z表示N或CH，Q表示O或S; Z0，Z1和Z2各自表示CH，Z0和Z1各自表示CH，Z2表示N，Z0表示CH，Z1表示N，Z2表示CH或N，Z0表示N，Z1和Z2表示CH; 和这些化合物的盐。

    TRICYCLIC OXAZOLIDINONE ANTIBIOTIC COMPOUNDS
    18.
    发明申请
    TRICYCLIC OXAZOLIDINONE ANTIBIOTIC COMPOUNDS 有权
    三氧化二氮唑酮类抗生素化合物

    公开(公告)号：US20110195961A1

    公开(公告)日：2011-08-11

    申请号：US13123218

    申请日：2009-10-06

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

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

    IPC: A61K31/5415 ,  C07D413/14 ,  A61K31/538 ,  C07D417/14 ,  C07D471/06 ,  A61K31/437 ,  A61K31/5383 ,  A61P31/04

    CPC classification number: C07D471/06 ,  C07D471/16 ,  C07D487/06 ,  C07D519/00

    Abstract: The invention relates to antibacterial compounds of formula I wherein is a bond or is absent, V is CH, CR6 or N; R0 is H or, if is a bond, may also be alkoxy; R1 is notably H or halogen; U is CH or N when is a bond, or, if is absent, U is CH2, NH or NR9; R2 is H, alkylcarbonyl or —CH2—R3; R3 is H, alkyl or hydroxyalkyl; R4 is H or, if n is not 0 and R5 is H, may also be OH; R5 is H, alkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, carboxy or alkoxycarbonyl; R6 is hydroxyalkyl, carboxy, alkoxycarbonyl or —(CH2)q—NR7R8, q being 1, 2 or 3 and each of R7 and R8 independently being H or alkyl or R7 and R8 forming with the N atom bearing them a ring; R9 is alkyl or hydroxyalkyl; A is —(CH2)p—, —CH2CH2CH(OH)— or —COCH2CH(OH)—; G is substituted phenyl or G1 or G2 wherein Q is O or S and X is CH or N; and Y1, Y2 and Y3 may each be CH or N; and n is 0 when A is —CH2CH2CH(OH)— or —COCH2CH(OH)—, and n is 0, 1 or 2 when A is —(CH2)p—, p being 1, 2, 3 or 4, with the proviso that the sum of n and p is then 2, 3 or 4; and to salts of such compounds.

    Abstract translation: 本发明涉及式I的抗菌化合物，其中是一个键或不存在，V是CH，CR 6或N; R 0是H，或者如果是键，也可以是烷氧基; R1特别是H或卤素; U是CH或N，当是键时，或如果不存在，U是CH 2，NH或NR 9; R2是H，烷基羰基或-CH2-R3; R3是H，烷基或羟烷基; R4是H或如果n不为0且R5是H，也可以是OH; R5是H，烷基，羟基烷基，氨基烷基，烷氧基烷基，羧基或烷氧基羰基; R6是羟基烷基，羧基，烷氧基羰基或 - （CH2）q-NR7R8，q是1,2或3，R7和R8各自独立地是H或烷基或R7和R8与带有它们的N原子形成环; R9是烷基或羟烷基; A是 - （CH 2）p - ， - CH 2 CH 2 CH（OH） - 或-COCH 2 CH（OH） - ; G为取代苯基或G1或G2，其中Q为O或S，X为CH或N; Y1，Y2和Y3各自为CH或N; 当A为-CH 2 CH 2 CH（OH） - 或-COCH 2 CH（OH） - 时，n为0，当A为 - （CH 2）p - ，p为1,2,3或4时，n为0,1或2， 条件是n和p之和为2,3或4; 和这些化合物的盐。

    Antibiotics derivatives
    19.
    发明授权
    Antibiotics derivatives 失效
    抗生素衍生物

    公开(公告)号：US07981886B2

    公开(公告)日：2011-07-19

    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: C07D417/12 ,  C07D413/12 ,  C07D409/12 ,  A61K31/5415 ,  A61K31/538

    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.

    Abstract translation: 本发明涉及式I的抗生素衍生物，其中：A表示-O-，S，-C（= O） - ， - C（= NOR 6） - ; Z-B表示NCH2CH2，NCOCH2，NCH2CO，NCH2CH（OH），CHN（R8）CH2或CHN（R8）CO; D表示双核杂芳基; Y1表示-CR1-或-N-，Y2表示-CR2-或-N-，Y3表示-CR3-或-N-，Y4表示-CR4-或-N-; U表示-NH-，-O-或-S-，V表示-N-或-CH-; W表示-CH 2 - ， - O-或-NR 7 - ; R1代表H，甲基，乙基或卤素; R2，R3和R4各自独立地表示H，C1-C4烷基，卤素或C1-C4烷氧基; R5表示H，C1-C4烷基或氟; R6表示H，C1-C4烷基或芳基-C1-C4烷基; R 7表示H，C 1 -C 4烷基，芳基-C 1 -C 4烷基或-CH 2 -COOH; R8表示H，C1-C4烷基或-CH2-COOH; 条件是如果Z-B表示NCH 2 CH 2，NCOCH 2，NCH 2 CO或NCH 2 CH（OH），则W表示-CH 2 - ; 如果A表示O或S，则W表示-CH 2 - ; Y1，Y2，Y3和Y4中只有一个可以同时表示N个。

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