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81. 发明公开

EP2086968A1 5-HYDROXYMETHYL-OXAZOLIDIN-2-ONE DERIVATIVES 有权
标题翻译： 5-羟甲基-2-酮衍生物
公开(公告)号：EP2086968A1
公开(公告)日：2009-08-12
申请号：EP07827038.6
申请日：2007-11-09
申请人： Actelion Pharmaceuticals Ltd.
发明人： HUBSCHWERLEN, Christian , PANCHAUD, Philippe , SPECKLIN, Jean-Luc
IPC分类号： C07D413/14 , C07D471/04 , A61K31/4375 , A61K31/4709 , A61P31/00
CPC分类号： C07D413/14 , C07D471/04
摘要： The invention relates to novel chimeric antibiotics of formula (I) wherein R1 represents OH, OPO3H2 or OCOR5; R2 represents H, OH or OPO3H2; A represents N or CR6; R3 represents H or fluorine; R4 is H, (C1-C3) alkyl, or cycloalkyl; R5 is the residue of a naturally occurring amino acid, of the enantiomer of a naturally occurring amino acid or of dimethylaminoglycine; R6 represents H, alkoxy or halogen; and n is O or 1; and to salts (in particular pharmaceutically acceptable salts) of compounds of formula (I). These chimeric compounds are useful in the manufacture of medicaments for the treatment of infections (e.g. bacterial infections).

82. 发明公开

EP2991992A1 QUINOLONE DERIVATIVES 有权
标题翻译： CHINOLONDERIVATE
公开(公告)号：EP2991992A1
公开(公告)日：2016-03-09
申请号：EP14726420.4
申请日：2014-04-30
申请人： Actelion Pharmaceuticals Ltd.
发明人： ENDERLIN-PAPUT, Stephanie , HUBSCHWERLEN, Christian , RUEEDI, Georg , ZUMBRUNN, Cornelia
IPC分类号： C07D498/04 , C07D513/04 , C07D519/00 , A61K31/424 , A61K31/429 , A61K31/4353 , A61P31/04
CPC分类号： C07D519/00 , C07D498/04 , C07D513/04
摘要： The invention relates to antibacterial compounds of formula I wherein R1, U, V and A are as defined in the description, to pharmaceutical compositions containing them and uses of these compounds in the manufacture of medicaments for the treatment of bacterial infections.
摘要翻译：本发明涉及式I的抗菌化合物，其中R1，U，V和A如说明书中所定义，含有它们的药物组合物和这些化合物在制备用于治疗细菌感染的药物中的用途。

83. 发明授权

EP2146987B1 OXAZOLIDINONE ANTIBIOTIC DERIVATIVES 失效转让
标题翻译：抗生素恶唑烷酮衍生物
公开(公告)号：EP2146987B1
公开(公告)日：2015-12-02
申请号：EP08737784.2
申请日：2008-04-10
申请人： Actelion Pharmaceuticals Ltd.
发明人： GUDE, Markus , HUBSCHWERLEN, Christian , RUEEDI, Georg , SURIVET, Jean-Philippe , ZUMBRUNN ACKLIN, Cornelia
IPC分类号： C07D471/04 , C07D413/14 , C07D417/14 , A61K31/4375 , A61P31/04
CPC分类号： C07D471/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14

84. 发明授权

EP2144910B1 OXAZOLIDINONE ANTIBIOTICS 失效转让
标题翻译：恶唑烷酮抗生素
公开(公告)号：EP2144910B1
公开(公告)日：2015-10-28
申请号：EP08737800.6
申请日：2008-04-11
申请人： Actelion Pharmaceuticals Ltd.
发明人： BUR, Daniel , HUBSCHWERLEN, Christian , RUEEDI, Georg , SURIVET, Jean-Philippe , ZUMBRUNN ACKLIN, Cornelia
IPC分类号： C07D471/04 , A61K31/435 , A61P31/00 , C07D519/00
CPC分类号： C07D413/14 , C07D471/04 , C07D519/00

85. 发明公开

EP2742042A1 QUINAZOLINE-2,4-DIONE DERIVATIVES 审中-公开
标题翻译： CHINAZOLIN -2,4-二酮衍生物
公开(公告)号：EP2742042A1
公开(公告)日：2014-06-18
申请号：EP12770233.0
申请日：2012-08-10
申请人： Actelion Pharmaceuticals Ltd.
发明人： HUBSCHWERLEN, Christian , SURIVET, Jean-Philippe , RUEEDI, Georg , ZUMBRUNN ACKLIN, Cornelia
IPC分类号： C07D413/14 , C07D417/14 , C07D498/04 , C07D513/04 , A61K31/538 , A61K31/5383 , A61K31/5415 , A61K31/542 , A61P31/04 , A61P31/06 , A61P33/02
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 R
1 is H, halogen, (C
1 -C
3 )alkyl or (C
1 -C
3 )alkoxy; R
2 is H, halogen, (C
1 -C
3 )alkyl, (C
1 -C
3 )alkoxy or pyrrolidin-l-yl; R
3 is H, halogen, (C
1 -C
3 )alkyl, (C
1 -C
3 )alkoxy, vinyl or 2-methoxycarbonylvinyl or R
2 and R
3 together with the two carbon atoms which bear them form a phenyl ring; R
4 is H, halogen, (C
1 -C
3 )alkyl or (C
1 -C
3 )alkoxy and R5 is H, (C1-C3)alkyl or cyclopropyl, or R
4 and R
5 form together a -CH
2 CH
2 CH
2 - group; A is the divalent group -CH
2 -, -CH
2 CH
2 -, #-CH(OH)CH
2 -*, #-CH
2 N(R
6 )-* or -CH
2 NHCH
2 -, 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; R
6 is H or acetyl; Y is CH or N; and Q is O or S; and salts of such compounds.

86. 发明公开

EP2691373A1 3-UREIDOISOQUINOLIN-8-YL DERIVATIVES 审中-公开
标题翻译： 3-十一烷基喹啉-8-基衍生物
公开(公告)号：EP2691373A1
公开(公告)日：2014-02-05
申请号：EP12715438.3
申请日：2012-03-28
申请人： Actelion Pharmaceuticals Ltd.
发明人： GUDE, Markus , HUBSCHWERLEN, Christian , PANCHAUD, Philippe
IPC分类号： C07D217/22 , C07D401/04 , C07D401/12 , C07D401/14 , A61K31/472 , A61K31/4725 , A61P31/04
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 I wherein R is alkyl, haloalkyl or cyclopropyl; R 2 is H, halogen, pyridazin-4-yl, pyrimidin-5-yl or an optionally substituted pyridin-3-yl, pyridin-4-yl or phenyl group; R 3 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, -CH 2 R a, -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 )C(O)O-R d, -(CH 2 ) n -R e or -O-(CH 2 ) n -R e; R a is cyano, acetylamino or N,N-dimethylamino; R b is cyano or carbamoyl; R c is H or methyl; R d is alkyl; R e 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; R 4 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为烷基，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; （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 R a，-CH 2 CH 2 R b， - （CH 2）n -C（O）OR d， - （CH 2）n -N（R c）C（O）OR d，-O- CH 2）n -N（R c）C（O）OR d， - （CH 2）n -R e或-O-（CH 2）n -R e; R a是氰基，乙酰氨基或N，N-二甲氨基; R b是氰基或氨基甲酰基; R c是H或甲基; R d是烷基; R e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 4-氧代咪唑烷-1-基，4-（叔丁氧基羰基）哌嗪-1-基，4-（氨基甲基）环己基或杂芳基; R 4是H或甲基; 并涉及这些化合物的盐。这些化合物可用于预防或治疗细菌感染。

87. 发明授权

EP2297107B1 [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] - 甲胺和[6-（1-氨基 - 乙基） - 四氢 - 吡喃-3-基] -METHYLAMINDERIVATE作为抗菌剂
公开(公告)号：EP2297107B1
公开(公告)日：2013-11-13
申请号：EP09757966.8
申请日：2009-06-02
申请人： Actelion Pharmaceuticals Ltd.
发明人： HUBSCHWERLEN, Christian , RUEEDI, Georg , SURIVET, Jean-Philippe , ZUMBRUNN ACKLIN, Cornelia
IPC分类号： C07D215/22 , C07D407/06 , C07D471/04 , C07D491/04 , C07D498/04 , C07D513/04 , A61K31/4709 , A61K31/47 , A61K31/4375 , A61P31/00
CPC分类号： C07D215/22 , C07D405/06 , C07D417/14 , C07D471/04 , C07D498/04 , C07D513/04 , C07D519/00

88. 发明授权

EP2254887B9 OXAZOLIDINONE DERIVATIVES 有权
标题翻译： OXAZOLIDINONDERIVATE
公开(公告)号：EP2254887B9
公开(公告)日：2013-05-29
申请号：EP09711588.5
申请日：2009-02-20
申请人： Actelion Pharmaceuticals Ltd.
发明人： HUBSCHWERLEN, Christian , RUEEDI, Georg , SURIVET, Jean-Philippe , ZUMBRUNN ACKLIN, Cornelia
IPC分类号： C07D471/04 , C07D413/14 , C07D417/14 , C07D519/00 , A61K31/536 , A61K31/4704 , A61K31/498 , A61K31/4985 , A61P31/00
CPC分类号： C07D417/14 , C07D413/14 , C07D471/04 , C07D519/00

89. 发明授权

EP2254887B1 OXAZOLIDINONE DERIVATIVES 有权
标题翻译：恶唑烷酮衍生物
公开(公告)号：EP2254887B1
公开(公告)日：2012-12-19
申请号：EP09711588.5
申请日：2009-02-20
申请人： Actelion Pharmaceuticals Ltd.
发明人： HUBSCHWERLEN, Christian , RUEEDI, Georg , SURIVET, Jean-Philippe , ZUMBRUNN ACKLIN, Cornelia
IPC分类号： C07D471/04 , C07D413/14 , C07D417/14 , C07D519/00 , A61K31/536 , A61K31/4704 , A61K31/498 , A61K31/4985 , A61P31/00
CPC分类号： C07D417/14 , C07D413/14 , C07D471/04 , C07D519/00

90. 发明公开

EP2297107A1 Ý4-(1-AMINO-ETHYL) -CYCLOHEXYL¨-METHYL-AMINE AND Ý6-(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] - 甲基氨基甲酸[6-（1-氨基 - 乙基） - 羟基 - 吡喃-3-基] - 甲基氨基甲酸酯
公开(公告)号：EP2297107A1
公开(公告)日：2011-03-23
申请号：EP09757966.8
申请日：2009-06-02
申请人： Actelion Pharmaceuticals Ltd.
发明人： HUBSCHWERLEN, Christian , RUEEDI, Georg , SURIVET, Jean-Philippe , ZUMBRUNN ACKLIN, Cornelia
IPC分类号： C07D215/22 , C07D407/06 , C07D471/04 , C07D491/04 , C07D498/04 , C07D513/04 , A61K31/4709 , A61K31/47 , A61K31/4375 , A61P31/00
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 R
1 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 CH
2 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 (II), (III) hereafter wherein Z represent CH or N, Q represents O or S and K represents O or S; and salts of such compounds.

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