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11. 发明授权

US08012961B2 Tricyclic antibiotics 失效
标题翻译：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
申请人： Christian Hubschwerlen , Georg Rueedi , John-Philippe Surivet , Cornelia Zumbrunn-Acklin
发明人： Christian Hubschwerlen , Georg Rueedi , John-Philippe Surivet , Cornelia Zumbrunn-Acklin
IPC分类号： C07D491/048 , C07D519/00 , A61K31/33
CPC分类号： C07D491/048 , C07D519/00
摘要： 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.
摘要翻译：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。

12. 发明申请

US20110201595A1 OXAZOLIDINYL ANTIBIOTICS 有权
标题翻译：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
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 , A61K31/4985 , A61K31/4704 , C07D417/14 , C07D413/14 , C07D487/04 , A61P31/04
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。

13. 发明申请

US20110003789A1 5-AMINOCYCLYLMETHYL-OXAZOLIDIN-2-ONE DERIVATIVES 有权
标题翻译： 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
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 , C07D471/04 , C07D417/14 , C07D413/14 , C07D498/04 , A61K31/517 , A61K31/538 , A61K31/5395 , A61P31/04
CPC分类号： C07D471/04 , C07D413/14 , C07D417/14
摘要： 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.
摘要翻译：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。

14. 发明授权

US07820655B2 Ethanol or 1,2-ethanediol cyclohexyl antibiotic derivatives 有权
标题翻译：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
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： C07D498/04 , A61K31/542 , A61K31/5383
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。

15. 发明申请

US20100137290A1 OXAZOLIDINONE ANTIBIOTIC DERIVATIVES 有权
标题翻译：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
申请人： Markus Gude , Christian Hubschwerlen , Georg Rueedi , Jean-Philippe Surivet , Cornelia Zumbrunn-Acklin
发明人： Markus Gude , Christian Hubschwerlen , Georg Rueedi , Jean-Philippe Surivet , Cornelia Zumbrunn-Acklin
IPC分类号： 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分类号： C07D471/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： 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.
摘要翻译：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。

16. 发明申请

US20090270375A1 SPIRO ANTIBIOTIC DERIVATIVES 失效
标题翻译： 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
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： A61K31/5415 , C07D471/04 , A61K31/538 , A61K31/4375 , A61P31/04
CPC分类号： C07D498/10
摘要： 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.
摘要翻译：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。

17. 发明申请

US20090005368A1 Ethanol or 1,2-Ethanediol Cyclohexyl Antibiotic Derivatives 有权
标题翻译：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。

18. 发明授权

US09346804B2 Tricyclic oxazolidinone antibiotic compounds 有权
标题翻译：三环恶唑烷酮抗生素化合物
公开(公告)号：US09346804B2
公开(公告)日：2016-05-24
申请号：US14096419
申请日：2013-12-04
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 , C07D471/06 , C07D471/16 , C07D487/06 , C07D519/00
CPC分类号： C07D471/06 , C07D471/16 , C07D487/06 , C07D519/00
摘要： The present 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 cyano, alkyl, or ethynyl; U is CH or N when “----” is a bond, or, if “----” is absent, U is CH2, NH or NH9; 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是氰基，烷基或乙炔基; 当“----”是键时，U是CH或N，或者如果不存在“----”，则U是CH 2，NH或NH 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是取代的苯基或G1或G2，其中Q是O或S，X是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。

19. 发明授权

US08466168B2 Tricyclic alkylaminomethyloxazolidinone derivatives 失效
标题翻译：三环烷基氨基甲基恶唑烷酮衍生物
公开(公告)号：US08466168B2
公开(公告)日：2013-06-18
申请号：US13057650
申请日：2009-08-03
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： C07D471/04 , C07D491/04
CPC分类号： C07D413/12 , C07D471/04 , C07D491/048 , C07D491/052 , C07D491/147
摘要： The invention relates to antibacterial compounds of formula I wherein R1 is alkoxy or halogen; W is CH or N; A is O or NH; B is CO or (CH2)q; G is a group having one of the three formulae below wherein Q represents O or S, Z represents CH or N, R2 represents halogen and R3 represents alkyl; m is 0 or 1; and n is 1 or 2; p is 0 or 1, provided m and p are not each 0; and q is 1 or 2; 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; W是CH或N; A是O或NH; B是CO或（CH 2）q; G是具有以下三个式之一的基团，其中Q表示O或S，Z表示CH或N，R2表示卤素，R3表示烷基; m为0或1; n为1或2; p为0或1，条件是m和p不是每个0; q为1或2; 和这些化合物的盐。

20. 发明授权

US08415375B2 2-hydroxyethyl-1H-quinolin-2-one derivatives and their azaisosteric analogues with antibacterial activity 有权
标题翻译： 2-羟乙基-1H-喹啉-2-酮衍生物及其具有抗菌活性的azaisosteric类似物
公开(公告)号：US08415375B2
公开(公告)日：2013-04-09
申请号：US13263922
申请日：2010-04-08
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： A01N43/42 , A61K31/47
CPC分类号： C07D491/056 , C07D497/04
摘要： The invention relates to antibacterial compounds of formula I wherein R1 represents alkoxy; each of U and V represents CH and W represents CH or N, or U represents N, V represents CH and W represents N, or each of U and V represents N and W represents CH; R2 represents hydrogen or fluorine when W represents CH or R2 represents hydrogen when W represents N; A represents O or CH2; Y represents CH or N; Q represents O or S; and n represents 0 or 1; 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代表烷氧基; U和V各自表示CH，W表示CH或N，或U表示N，V表示CH，W表示N，或U和V表示N，W表示CH; 当W表示CH时，R2表示氢或氟，当W表示N时，R2表示氢; A表示O或CH 2; Y表示CH或N; Q表示O或S; n表示0或1; 和这些化合物的盐。

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