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    Ethanol or 1,2-Ethanediol Cyclohexyl Antibiotic Derivatives
    42.
    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

    申请人： Christian Hubschwerlen ,  Jean-Philippe Surivet ,  Cornelia Zumbrunn Acklin

    发明人： Christian Hubschwerlen ,  Jean-Philippe Surivet ,  Cornelia Zumbrunn Acklin

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

    CPC分类号： C07D471/04 ,  C07D241/44 ,  C07D513/04

    摘要： 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).

    摘要翻译： 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。

    Derivatives of 3-(2-oxo-[1,3′]bipyrrolidinyl-3-ylidenemethyl)-cephams
    44.
    发明授权
    Derivatives of 3-(2-oxo-[1,3′]bipyrrolidinyl-3-ylidenemethyl)-cephams 有权
    3-（2-氧代 - [1,3']联吡咯烷基-3-亚甲基甲基） - 头孢的衍生物

    公开(公告)号：US06232306B1

    公开(公告)日：2001-05-15

    申请号：US09332811

    申请日：1999-06-14

    申请人： Paul Hebeisen ,  Christian Hubschwerlen ,  Jean-Luc Specklin

    发明人： Paul Hebeisen ,  Christian Hubschwerlen ,  Jean-Luc Specklin

    IPC分类号： C07D50124

    CPC分类号： C07D501/00

    摘要： The present invention provides compounds of formula I wherein R1 is hydrogen, C1-6-alkyl, C1-6-alkyl substituted by fluoro, or C3-6-cycloalkyl; R2 is hydrogen or a substituent selected from the group consisting of —CH2C(═CHR)—COOR, —CH2OCOR, —CH(R)OCOR, —CH(R)OCOOR, —CH(OCOR)OCOR, —CH2COCH2OCOR and R3 is hydrogen or a substituent selected from the group consisting of —CH2C(═CH2)—COOR, —COOCH2C(═CHR)—COOR, —COOCH2OCOR, —COOCH(R)OCOR, —COOCH(R)OCOOR, —COOCH(OCOR)OCOR, —COOCH2COCH2OCOR, and  with the proviso that one of R2 and R3 is hydrogen and the other is not hydrogen, R is hydrogen or C1-6-alkyl; R4 is hydrogen or hydroxy, R5 is hydrogen or &ohgr;-hydroxyalkyl; and X is CH or N, pharmaceutically acceptable salts of the compounds and hydrates of the compounds and of their salts.

    摘要翻译： 本发明提供式I化合物，其中R 1是氢，C 1-6 - 烷基，被氟取代的C 1-6 - 烷基或C 3-6 - 环烷基; R 2是氢或选自-CH 2 C（= CHR ）-COOR，-CH 2 OCOR，-CH（R）OCOR，-CH（R）OCOOR，-CH（OCOR）OCOR，-CH 2 COCH 2 OCOR和R 3是氢或选自-CH 2 C（= CH 2）-COOR ，-COOCH 2 C（= CHR）-COOR，-COOCH 2 OCOR，-COOCH（R）OCOR，-COOCH（R）OCOOR，-COOCH（OCOR）OCOR，-COOCH 2 COCH 2 OCOR，条件是R 2和R 3之一为氢， 另一个不是氢，R是氢或C 1-6 - 烷基; R 4是氢或羟基，R 5是氢或ω-羟基烷基; 和X是CH或N，化合物及其盐的化合物和水合物的药学上可接受的盐。

    QUINAZOLINE-2,4-DIONE DERIVATIVES
    47.
    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

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

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

    IPC分类号： C07D513/04 ,  C07D498/04 ,  C07D471/04 ,  C07D417/14

    CPC分类号： C07D471/04 ,  C07D413/14 ,  C07D417/14 ,  C07D498/04 ,  C07D513/04

    摘要： 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.

    摘要翻译： 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。

    3-UREIDOISOQUINOLIN-8-YL DERIVATIVES
    48.
    发明申请
    3-UREIDOISOQUINOLIN-8-YL DERIVATIVES 有权
    3-UREIDOISOQUINOLIN-8-YL衍生物

    公开(公告)号：US20140038961A1

    公开(公告)日：2014-02-06

    申请号：US14009093

    申请日：2012-03-28

    申请人： Markus Gude ,  Christian Hubschwerlen ,  Philippe Panchaud

    发明人： Markus Gude ,  Christian Hubschwerlen ,  Philippe Panchaud

    IPC分类号： C07D217/22 ,  C07D401/14 ,  C07D401/04 ,  C07D401/12

    CPC分类号： C07D217/22 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14

    摘要： The invention relates to 3-ureidoisoquinolin-8-yl derivatives of formula I wherein R1 is alkyl, haloalkyl or cyclopropyl; R2 is H, halogen, pyridazin-4-yl, pyrimidin-5-yl or an optionally substituted pyridin-3-yl, pyridin-4-yl or phenyl group; R3 is alkyl, alkynyl, aminoalkyl, carbamoylalkyl, methylcarbamoylalkyl, alkoxy, haloalkoxy, alkynyloxy, (4-hydroxybut-2-yn-1-yl)oxy, (4-aminobut-2-yn-1-yl)oxy, dimethylaminoalkoxy, carbamoylalkoxy, alkylamino, cycloalkyl, cycloalkylalkyl, cycloalkylalkoxy, hydroxyalkyl, hydroxyalkoxy, alkoxyalkyl, alkoxyalkoxy, carboxyalkyl, carboxyalkoxy, alkoxycarbonylalkoxy, aryl, heteroaryl, benzyl, benzyloxy, 2-cyanoethoxy, 2,3-dihydroxypropoxy, 3,4-dihydroxybutoxy, —CH2Ra, —CH2CH2Rb, —(CH2)n—C(O)O—Rd, —(CH2)n—N(Rc)C(O)O—Rd, —O—(CH2)n—N(Rc)C(O)O—Rd, —(CH2)n—Re or —O—(CH2)n—Re; Ra is cyano, acetylamino or N,N-dimethylamino; Rb is cyano or carbamoyl; Rc is H or methyl; Rd is alkyl; Re is pyrrolidin-1-yl, piperidin-1-yl, piperidin-3-yl, morpholin-1-yl, 2-oxopyrrolidin-1-yl, 5-oxopyrrolidin-2-yl, 2,5-dioxopyrrolidin-1-yl, 2-oxoimidazolidin-1-yl, 4-(tert-butoxycarbonyl)piperazin-1-yl, 4-(aminomethyl)cyclohexyl or heteroaryl; R4 is H or methyl; and to the salts of such compounds. These compounds are useful for the prevention or the treatment of bacterial infections.

    摘要翻译： 本发明涉及式I的3-脲基异喹啉-8-基衍生物，其中R 1是烷基，卤代烷基或环丙基; R 2是H，卤素，哒嗪-4-基，嘧啶-5-基或任选取代的吡啶-3-基，吡啶-4-基或苯基; R3是烷基，炔基，氨基烷基，氨甲酰基烷基，甲基氨基甲酰基烷基，烷氧基，卤代烷氧基，炔氧基，（4-羟基丁-2-炔-1-基）氧基，（4-氨基丁-2-炔-1-基）氧基，二甲基氨基烷氧基， 氨基甲酰基烷氧基，烷基氨基，环烷基，环烷基烷基，环烷基烷氧基，羟基烷基，羟基烷氧基，烷氧基烷基，烷氧基烷氧基，羧基烷基，羧基烷氧基，烷氧基羰基烷氧基，芳基，杂芳基，苄基，苄氧基，2-氰基乙氧基，2,3-二羟基丙氧基，3,4-二羟基丁氧基， ，-CH 2 CH 2 R b， - （CH 2）n C（O）O-R d， - （CH 2）n N（R c）C（O）O-R d，-O-（CH 2）n N（R c） - （CH 2）n -R e或-O-（CH 2）n -R e; R a是氰基，乙酰氨基或N，N-二甲基氨基; Rb是氰基或氨基甲酰基; Rc是H或甲基; Rd为烷基; Re是吡咯烷-1-基，哌啶-1-基，哌啶-3-基，吗啉-1-基，2-氧代吡咯烷-1-基，5-氧代吡咯烷-2-基，2,5-二氧代吡咯烷-1-基， 哌啶-1-基，4-（氨基甲基）环己基或杂芳基; R4是H或甲基; 和这些化合物的盐。 这些化合物可用于预防或治疗细菌感染。

    Tricyclic oxazolidinone antibiotic compounds
    49.
    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

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

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

    IPC分类号： A61K31/54 ,  A61K31/535

    CPC分类号： C07D471/06 ,  C07D471/16 ,  C07D487/06 ,  C07D519/00

    摘要： 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.

    摘要翻译： 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
    50.
    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

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

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

    IPC分类号： A61K31/5415 ,  A61K31/538 ,  A61K31/498 ,  A61K31/4985 ,  A61K31/4704

    CPC分类号： C07D413/14 ,  C07D413/12 ,  C07D417/14 ,  C07D471/04

    摘要： 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.

    摘要翻译： 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。