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    AZATRICYCLIC ANTIBIOTIC COMPOUNDS
    21.
    发明申请
    AZATRICYCLIC ANTIBIOTIC COMPOUNDS 有权
    亚胺基抗生素化合物

    公开(公告)号：US20100331318A1

    公开(公告)日：2010-12-30

    申请号：US12918749

    申请日：2009-02-19

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

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

    IPC: A61K31/5415 ,  C07D413/14 ,  C07D471/06 ,  A61K31/538 ,  A61K31/4375 ,  A61P31/04

    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 —(CH—)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 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“-----”是键时，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-）p-NH-（CH 2）q-，其中p为1且q为1或2，或者，假设U表示CH 2且n为1，p也可以为0，q为2; G表示其中Z表示N或CH并且Q表示O或S的基团之一; 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。

    CYCLOHEXYL OR PIPERIDINYL CARBOXAMIDE ANTIBIOTIC DERIVATIVES
    23.
    发明申请
    CYCLOHEXYL OR PIPERIDINYL CARBOXAMIDE ANTIBIOTIC DERIVATIVES 失效
    环己基或哌啶甲酰胺抗生素衍生物

    公开(公告)号：US20090105232A1

    公开(公告)日：2009-04-23

    申请号：US12294163

    申请日：2007-03-22

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

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

    IPC: A61K31/47 ,  C07D215/00 ,  C07D239/72 ,  A61K31/541 ,  A61P31/04 ,  A61K31/517 ,  C07D279/12

    CPC classification number: C07D405/12 ,  C07D215/20 ,  C07D401/06 ,  C07D405/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

    Abstract: The invention relates to antibiotic cyclohexyl or piperidinyl carboximide derivatives of formula (I) wherein R1 represents hydrogen, halogen, (C1-C4)alkyl, (C1-C4)alkoxy, cyano or COOR2, R2 being (C1-C4)alkyl; one or two of U, V, W and X represent(s) N and the remaining represent each CH, or, in the case of X, may also represent CRX, RX being a halogen atom; either B represents N and A represents CH2CH2 or CH(OR3)CH2, or B represents CH or C(OR4) and A represents OCH2, CH2CH(OR5), CH(OR6)CH2, CH(OR7)CH(OR8), CH═CH or CH2CH2; each of R3, R4, R5, R6, R7, and R8 represents independently hydrogen, SO3H, PO3H2, CH2OPO3H2 or COR9, R9 being either CH2CH2COOH or such that R9—COOH is naturally occurring amino acid or dimethylaminoglycine; and to salts of such compounds of formula (I).

    Abstract translation: 本发明涉及式（I）的抗生素环己基或哌啶基甲酰亚胺衍生物，其中R1表示氢，卤素，（C1-C4）烷基，（C1-C4）烷氧基，氰基或COOR2，R2是（C1-C4）烷基; U，V，W和X中的一个或两个表示（s）N，其余表示每个CH，或者在X的情况下也可以表示CRX，RX表示卤素原子; B表示N，A表示CH 2 CH 2或CH（OR 3）CH 2，或B表示CH或C（OR 4），A表示OCH 2，CH 2 CH（OR 5），CH（OR 6）CH 2，CH（OR 7）CH（OR 8） -CH或CH 2 CH 2; R 3，R 4，R 5，R 6，R 7和R 8各自独立地表示氢，SO 3 H，PO 3 H 2，CH 2 OPO 3 H 2或COR 9，R 9是CH 2 CH 2 COOH或使得R 9 -COOH是天然存在的氨基酸或二甲基氨基甘氨酸; 和式（I）化合物的盐。

    QUINAZOLINE-2,4-DIONE DERIVATIVES
    25.
    发明申请
    QUINAZOLINE-2,4-DIONE DERIVATIVES 有权
    喹唑啉-2,4-二酮衍生物

    公开(公告)号：US20140171425A1

    公开(公告)日：2014-06-19

    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: C07D513/04 ,  C07D498/04 ,  C07D471/04 ,  C07D417/14

    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 R5 form 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; 和R 5是H，（C 1 -C 3）烷基或环丙基，或者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。

    Tricyclic oxazolidinone antibiotic compounds
    26.
    发明授权
    Tricyclic oxazolidinone antibiotic compounds 有权
    三环恶唑烷酮抗生素化合物

    公开(公告)号：US08618092B2

    公开(公告)日：2013-12-31

    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: A61K31/54 ,  A61K31/535

    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，烷基或羟基烷基; 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。

    Oxazolidinyl antibiotics
    27.
    发明授权
    Oxazolidinyl antibiotics 有权
    恶唑烷基抗生素

    公开(公告)号：US08507478B2

    公开(公告)日：2013-08-13

    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 ,  A61K31/498 ,  A61K31/4985 ,  A61K31/4704

    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。

    4-(1-amino-ethyl)-cyclohexylamine derivatives
    29.
    发明授权
    4-(1-amino-ethyl)-cyclohexylamine derivatives 有权
    4-（1-氨基 - 乙基） - 环己胺衍生物

    公开(公告)号：US08044044B2

    公开(公告)日：2011-10-25

    申请号：US12520580

    申请日：2007-12-21

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

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

    IPC: A61K31/542 ,  A61K31/5415

    CPC classification number: C07D215/20 ,  C07D215/227 ,  C07D215/48 ,  C07D413/12 ,  C07D471/04 ,  C07D513/04

    Abstract: The invention relates to compounds of formula (I) wherein R0 represents H or OH; R1 represents alkoxy; U and W represent N, V represents CH and R2 represents H or F, or U and V represent CH, W represents N and R2 represents H or F, or U and V represent N, W represents CH and R2 represents H, or U represents N, V represents CH, W represents CRa and R2 represents H; Ra represents CH2OH or alkoxycarbonyl; A represents the group CH═CH—B or a binuclear heterocyclic system D, B representing a mono- or di-substituted phenyl group wherein the substituents are halogen atoms and D representing one of the following groups wherein Z represents CH or N, and Q represents O or S; and to salts of such compounds. These compounds are useful as antibacterial agents.

    Abstract translation: 本发明涉及式（I）化合物，其中R 0表示H或OH; R1代表烷氧基; U和W表示N，V表示CH，R2表示H或F，或U表示CH，W表示N，R2表示H或F，或U表示N，W表示CH，R2表示H或U 表示N，V表示CH，W表示CRa，R2表示H; Ra表示CH 2 OH或烷氧基羰基; A表示基团CH = CH-B或双核杂环体系D，B表示一或二取代苯基，其中取代基为卤素原子，D表示以下基团之一，其中Z表示CH或N，Q表示 表示O或S; 和这些化合物的盐。 这些化合物可用作抗菌剂。

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