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1.发明授权
公开(公告)号：EP2376497B1
公开(公告)日：2013-09-18
申请号：EP09796819.2
申请日：2009-12-11
IPC分类号： C07D491/056 , C07D497/04 , C07D519/00 , A61K31/4375 , A61K31/498 , A61P31/04
CPC分类号： C07D519/00 , C07D491/056 , C07D497/04
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公开(公告)号：EP2376497A1
公开(公告)日：2011-10-19
申请号：EP09796819.2
申请日：2009-12-11
IPC分类号： C07D491/056 , C07D497/04 , C07D519/00 , A61K31/4375 , A61K31/498 , A61P31/04
CPC分类号： C07D519/00 , C07D491/056 , C07D497/04
摘要： The invention relates to antibacterial compounds of formula I wherein R
1 represents alkoxy (notably methoxy); R
2 represents H or F; each of R
3 , R
4 , R
5 and R
6 represents independently H or D; V represents CH and W represents CH or N or V represents N and W represents CH; Y represents CH or N; Z represents O, S or CH
2 ; and A represents CH
2 , CH
2 CH
2 or CD
2 CD
2 ; and salts of such compounds.-
公开(公告)号：EP2257551A2
公开(公告)日：2010-12-08
申请号：EP09712156.0
申请日：2009-02-19
IPC分类号： C07D471/16 , C07D498/16 , C07D519/00 , A61P31/04 , A61K31/5415 , A61K31/538 , A61K31/4745 , A61K31/4375 , A61K31/437 , C07D455/04
CPC分类号： C07D498/16 , C07D455/04 , C07D471/16 , C07D519/00
摘要： The invention relates to antibacterial compounds of formula I (I) wherein n is 0 or 1; R
1 represents H or F; U represents CH
2 or, provided n is 1, O or NH; "---- " is a bond or is absent; V represents CH or N when "---- " is a bond, or CH
2 or NH when "---- " is absent; W represents CH or N; A represents -(CH
2 )
p -NH-(CH
2 )
q - wherein p is 1 and q is 1 or 2 or, provided U represents CH
2 and n is 1, p may also be 0 and q is then 2; G represents one of the groups (II) (III) wherein Z represents N or CH and Q represents O or S; and Z
0 , Z
1 and Z
2 each represent CH, or Z
0 and Z
1 each represent CH and Z
2 represents N, or Z
0 represents CH, Z
1 represents N and Z
2 represents CH or N, or Z
0 represents N and Z
1 and Z
2 each represent CH; and to salts of such compounds-
4.发明授权
公开(公告)号：EP2001478B1
公开(公告)日：2010-06-02
申请号：EP07735216.9
申请日：2007-03-22
IPC分类号： A61K31/517 , C07D401/00 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/12 , C07D409/14 , C07D411/06 , C07D411/12 , C07D411/14 , C07D413/06
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 carboxamide 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 a naturally occurring amino acid or dimethylaminoglycine; and to salts of such compounds of formula (I).
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5.发明公开
公开(公告)号：EP2167494A1
公开(公告)日：2010-03-31
申请号：EP08763320.2
申请日：2008-06-13
IPC分类号： C07D405/06 , C07D413/14 , C07D471/04 , C07D498/04 , C07D513/04 , C07D519/00 , A61K31/4375 , A61K31/4709 , A61P31/04
CPC分类号： C07D498/04 , C07D405/06 , C07D413/14 , C07D471/04 , C07D513/04 , C07D519/00
摘要： The invention relates to antibacterial compounds of formula I wherein R1 represents halogen or alkoxy; U and W each represent N, V represents CH and R2 represents H or F, or U and V each represent CH, W represents N and R2 represents H or F, or U represents N, V represents CH, W represents CH or CRa and R2 represents H, or also, when W represents CH, may represent F; Ra represents CH2OH or alkoxycarbonyl; A represents the group CH=CH-B, a binuclear heterocyclic system D, a phenyl group which is mono substituted in position 4 by alkyl, or a phenyl group which is disubstituted in positions 3 and 4, wherein each of the substituents is independently selected from alkyl and halogen, B representing a mono- or di-substituted phenyl group wherein each substituent is a halogen atom and D representing the group wherein Z represents CH or N, and Q represents O or S; and to salts of such compounds.
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公开(公告)号：EP2986607A1
公开(公告)日：2016-02-24
申请号：EP14721539.6
申请日：2014-04-15
发明人： CREN, Sylvaine , FRIEDLI, Astrid , HUBSCHWERLEN, Christian , RUEEDI, Georg , ZUMBRUNN, Cornelia
IPC分类号： C07D413/14 , A61K31/538 , A61K31/5383 , A61K31/5415 , A61K31/542 , C07D413/04 , C07D417/04 , C07D417/14 , C07D498/04 , C07D513/04 , A61P31/00
CPC分类号： C07D513/04 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D498/04
摘要： The invention relates to antibacterial compounds of formula I (I) wherein R is H, cyano, alkoxy, cyanomethoxy, cycloalkylmethoxy, hydroxyalkoxy, alkoxyalkoxy, alkoxycarbonyl, 2-ethoxy-2-oxoethoxy, 2-(methylamino)-2-oxoethoxy, (l-cyanocyclobutyl)methoxy, 3-hydroxy-pyrrolidin-l-yl or 3,4-dihydroxycyclopentyl)methoxy; U
1 is N or CR
1 , U
2 is N or CR
2 , U
3 is N or CR
3 and U
4 is N or CR
4 , it being understood that at most three of U
1 , U
2 , U
3 and U
4 can be N at the same time; V
1 is N or CR
5 , V
2 is N or CR
6 , V
3 is N or CR
7 and V
4 is N or CH, it being understood that at most two of V
1 , V
2 , V
3 and V4 can be N at the same time; R1 is H, cyano, hydroxy or alkoxy; R2 is H, hydroxy or alkoxy; R
3 is H, cyano, hydroxy, alkoxy or carboxamido; R
4 is H or alkoxy; R
5 is H, hydroxy or halogen; R
6 is H, hydroxy or halogen; R
7 is H; the dotted line "_____ " represents a bond or is absent; W represents CH or N when the dotted line "_____ " is a bond, or W represents CH
2 when the dotted line "_____ " is absent; X represents CH or N; and Q represents O or S; and salts thereof.-
公开(公告)号：EP2776431A1
公开(公告)日：2014-09-17
申请号：EP12791863.9
申请日：2012-11-07
IPC分类号： C07D413/14 , A61K31/501
CPC分类号： C07D513/04 , C07D413/14 , C07D417/14 , C07D498/04
摘要： The invention relates to antibacterial compounds of formula I (Fornula I) (I) wherein R
1a represents H or carboxy and R
1b represents H, or R
1a and R
1b represent together either the group *-C(0)-NH-S-
# or the group *-C(OH)=N-S-
# wherein "*" represents the point of attachment of R
1a and
"#" represents the point of attachment of R
1b ; R
2 represents H, (C
1 -C
3 )alkyl, hydroxy-(C
1 C
3 )alkyl, benzyl or (C
3 -C
5 )cycloalkyl; R
3 represents H or halogen; U represents N or CR
4 ; wherein R
4 is H or (C
1 -C
3 )alkoxy; A represents CH, B represents NH and m represents 1 or 2 and n represents 1 or 2; or A represents N, B is absent, m represents 2 and n represents 2; Y represents CH or N; and Q represents O or S; and salts of such compounds.-
8.发明授权2-HYDROXYETHYL-1H-QUINOLIN-2-ONE DERIVATIVES AND THEIR AZAISOSTERIC ANALOGUES WITH ANTIBACTERIAL ACTIVITY 有权2-羟基乙基-1H-喹啉-2-酮衍生物及其ANALOG AZAISOSTEREN具有抗菌作用的
公开(公告)号：EP2417141B1
公开(公告)日：2013-10-16
申请号：EP10714481.8
申请日：2010-04-08
IPC分类号： C07D491/056 , C07D497/04 , A61K31/436 , A61K31/4365 , A61K31/498 , A61P31/04
CPC分类号： C07D491/056 , C07D497/04
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公开(公告)号：EP2245028B1
公开(公告)日：2012-02-22
申请号：EP08861657.8
申请日：2008-12-17
IPC分类号： C07D413/14 , C07D417/14 , C07D471/04 , A61K31/5415 , A61K31/536 , A61K31/517 , A61K31/4375 , A61K31/435 , A61P31/00
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 O or 1 and n is O or 1; and G is as defined in the description; and to salts of such compounds.
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公开(公告)号：EP2254887A1
公开(公告)日：2010-12-01
申请号：EP09711588.5
申请日：2009-02-20
IPC分类号： C07D413/14 , C07D417/14 , C07D417/04 , C07D519/00 , A61K31/536 , A61K31/4704 , A61K31/498 , A61K31/4985 , A61P31/00
CPC分类号： C07D417/14 , C07D413/14 , C07D471/04 , C07D519/00
摘要： The invention relates to compounds of Formula (I) wherein U, V, W, R
1 , R
1b , A and G are as defined in the description, to pharmaceutically acceptable salts of such compounds and to the use of these compounds in the manufacture of a medicament for the prevention or treatment of a bacterial infection.
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