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11. 发明授权

US08193179B2 3-amino-6-(1-amino-ethyl)-tetrahydropyran derivatives 有权
标题翻译： 3-氨基-6-（1-氨基 - 乙基） - 四氢吡喃衍生物
公开(公告)号：US08193179B2
公开(公告)日：2012-06-05
申请号：US12664828
申请日：2008-06-13
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： A61K31/542 , A61K31/5365 , A61K31/4353 , A61K31/47 , C07D279/10 , C07D265/28 , C07D471/04 , C07D471/00
CPC分类号： C07D498/04 , C07D405/06 , C07D413/14 , C07D471/04 , C07D513/04 , C07D519/00
摘要： Antibacterial compounds including 3-amino-6-(1-amino-ethyl)-tetrahydropyran derivatives are provided, and methods of treatment or prevention of bacterial infection with such compounds are provided.
摘要翻译：提供了包括3-氨基-6-（1-氨基 - 乙基） - 四氢吡喃衍生物的抗菌化合物，并且提供了用这些化合物治疗或预防细菌感染的方法。

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

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。

14. 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。

15. 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。

16. 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。

17. 发明授权

US08349829B2 [4-(1-amino-ethyl)-cyclohexyl]-methyl-amine and [6-(1-amino-ethyl)-tetrahydro-pyran-3-yl]-methyl-amine derivatives as antibacterials 有权
标题翻译： [4-（1-氨基 - 乙基） - 环己基] - 甲基胺和[6-（1-氨基 - 乙基） - 四氢 - 吡喃-3-基] - 甲基 - 胺衍生物作为抗菌剂
公开(公告)号：US08349829B2
公开(公告)日：2013-01-08
申请号：US12996360
申请日：2009-06-02
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 , C07D405/06 , A61K31/542 , A61K31/5383 , A61K31/4709
CPC分类号： C07D215/22 , C07D405/06 , C07D417/14 , C07D471/04 , C07D498/04 , C07D513/04 , C07D519/00
摘要： The invention relates to antibacterial compounds of formula I wherein R1 represents alkoxy or halogen; U, V and W each represent CH, or one of U, V and W represents N and the others each represent CH; A represents CH2 or O; G is CH═CH-E wherein E represents a phenyl group mono- or di-substituted with halogen, or G is a group of one of the formulae hereafter wherein Z represent CH or N, Q represents O or S and K represents 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代表烷氧基或卤素; U，V和W各自表示CH，或U，V和W之一表示N，其余各自表示CH; A表示CH 2或O; G是CH = CH-E，其中E表示被卤素单取代或二取代的苯基，或G是下式之一的基团，其中Z表示CH或N，Q表示O或S，K表示O或 S; 和这些化合物的盐。

18. 发明授权

US08217029B2 Oxazolidinone antibiotics 有权
标题翻译：恶唑烷酮类抗生素
公开(公告)号：US08217029B2
公开(公告)日：2012-07-10
申请号：US12595720
申请日：2008-04-11
申请人： Daniel Bur , Christian Hubschwerlen , Georg Rueedi , Jean-Philippe Surivet , Cornelia Zumbrunn-Acklin
发明人： Daniel Bur , Christian Hubschwerlen , Georg Rueedi , Jean-Philippe Surivet , Cornelia Zumbrunn-Acklin
IPC分类号： A61K31/397 , A61K31/55 , A61K31/54 , A61K31/50 , A61K31/497 , A61K31/44 , C07D243/08 , C07D279/10 , C07D237/26 , C07D401/14 , C07D239/72 , C07D471/12 , C07D471/22 , C07D215/00
CPC分类号： C07D413/14 , C07D471/04 , C07D519/00
摘要： The invention relates to compounds of formula (I) wherein U, V, W, X, R1, R2, R3, R4, R5, R6, A, B, D, E, G, m, and n are as defined in the description, to pharmaceutically acceptable salts of such compounds for use in the manufacture of a medicament for the prevention or treatment of a bacterial infection. Certain compounds of formula (I) are new and are also part of this invention.
摘要翻译：本发明涉及式（I）化合物，其中U，V，W，X，R 1，R 2，R 3，R 4，R 5，R 6，A，B，D，E，G，m和n如描述了用于制备用于预防或治疗细菌感染的药物的这些化合物的药学上可接受的盐。某些式（I）化合物是新的，也是本发明的一部分。

19. 发明授权

US08114867B2 Oxazolidinone antibiotic derivatives 有权
标题翻译：恶唑烷酮类抗生素衍生物
公开(公告)号：US08114867B2
公开(公告)日：2012-02-14
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： C07D471/04 , C07D413/14 , C07D417/14 , A61K31/4375
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 selected 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个原子选自碳，氧和氮并且可以被取代; 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。

20. 发明授权

US08618092B2 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：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。

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