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公开(公告)号:US07981886B2
公开(公告)日:2011-07-19
申请号:US11915179
申请日:2006-05-24
IPC分类号: C07D417/12 , C07D413/12 , C07D409/12 , A61K31/5415 , A61K31/538
CPC分类号: C07D277/64 , C07D409/12 , C07D413/12 , C07D417/12 , C07D513/04
摘要: 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.
摘要翻译: 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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公开(公告)号:US20110039823A1
公开(公告)日:2011-02-17
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: A61K31/4375 , C07D471/04 , C07D413/14 , A61K31/517 , C07D417/14 , A61K31/4709 , A61K31/5415 , A61K31/496 , A61K31/551 , C07D491/056 , A61K31/5025 , A61P31/04
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可接受的盐。 某些式(I)化合物是新的,也是本发明的一部分。
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公开(公告)号:US20080280888A1
公开(公告)日:2008-11-13
申请号:US11915179
申请日:2006-05-24
IPC分类号: A61K31/5415 , C07D417/02 , A61K31/538 , A61K31/428 , A61K31/542 , C07D513/04
CPC分类号: C07D277/64 , C07D409/12 , C07D413/12 , C07D417/12 , C07D513/04
摘要: 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.
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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。
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公开(公告)号:US08349828B2
公开(公告)日:2013-01-08
申请号:US12918749
申请日:2009-02-19
IPC分类号: A61K31/54 , C07D279/16
CPC分类号: C07D498/16 , C07D455/04 , C07D471/16 , C07D519/00
摘要: 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.
摘要翻译: 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。
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公开(公告)号:US20110195961A1
公开(公告)日:2011-08-11
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: A61K31/5415 , C07D413/14 , A61K31/538 , C07D417/14 , C07D471/06 , A61K31/437 , A61K31/5383 , A61P31/04
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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公开(公告)号:US20090105232A1
公开(公告)日:2009-04-23
申请号:US12294163
申请日:2007-03-22
IPC分类号: A61K31/47 , C07D215/00 , C07D239/72 , A61K31/541 , A61P31/04 , A61K31/517 , C07D279/12
CPC分类号: C07D405/12 , C07D215/20 , C07D401/06 , C07D405/14 , C07D417/12 , C07D417/14 , C07D471/04
摘要: 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).
摘要翻译: 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。
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公开(公告)号:US08193179B2
公开(公告)日:2012-06-05
申请号:US12664828
申请日:2008-06-13
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。
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公开(公告)号:US20110201595A1
公开(公告)日:2011-08-18
申请号:US13123708
申请日:2009-10-09
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。
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公开(公告)号:US20110003789A1
公开(公告)日:2011-01-06
申请号:US12809555
申请日:2008-12-17
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。
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