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1. 发明申请

WO2010041219A1 2-BENZOTHIOPHENYL-AND 2-NAPHTHYL-0XAZ0LIDIN0NES AND THEIR AZAISOSTERE ANALOGUES AS ANTIBACTERIAL AGENTS 审中-公开
标题翻译： 2-苯并噻吩和2-萘基-OXAZ0LIDINONES及其作为抗菌剂的AZAISOSTERE类似物
公开(公告)号：WO2010041219A1
公开(公告)日：2010-04-15
申请号：PCT/IB2009/054434
申请日：2009-10-09
申请人： ACTELION PHARMACEUTICALS LTD , EGGER, Verena , GUDE, Markus , HUBSCHWERLEN, Christian , RUEEDI, Georg , SURIVET, Jean-Philippe , ZUMBRUNN ACKLIN, Cornelia
发明人： EGGER, Verena , GUDE, Markus , HUBSCHWERLEN, Christian , RUEEDI, Georg , SURIVET, Jean-Philippe , ZUMBRUNN ACKLIN, Cornelia
IPC分类号： C07D413/04 , C07D417/04 , C07D417/14 , C07D495/04 , A61K31/422 , A61P31/04
CPC分类号： C07D417/14 , C07D413/14 , C07D417/04 , C07D495/04
摘要： The invention relates to antibacterial compounds of Formula (I) wherein U, V, W, X, R 1 , R 2 , m, A, B 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.
摘要翻译：本发明涉及其中U，V，W，X，R 1，R 2，m，A，B和G如说明书中所定义的式（I）的抗菌化合物与这些化合物的药学上可接受的盐以及使用这些化合物在制备药物中。

2. 发明申请

WO2010041218A2 OXAZOLIDINYL ANTIBIOTICS 审中-公开
标题翻译：奥昔布林抗生素
公开(公告)号：WO2010041218A2
公开(公告)日：2010-04-15
申请号：PCT/IB2009/054433
申请日：2009-10-09
申请人： ACTELION PHARMACEUTICALS LTD , HUBSCHWERLEN, Christian , RUEEDI, Georg , SURIVET, Jean-Philippe , ZUMBRUNN ACKLIN, Cornelia
发明人： HUBSCHWERLEN, Christian , RUEEDI, Georg , SURIVET, Jean-Philippe , ZUMBRUNN ACKLIN, Cornelia
IPC分类号： C07D413/14 , C07D417/14 , C07D471/04 , A61K31/4709 , A61K31/498 , A61K31/4985
CPC分类号： C07D413/14 , C07D413/12 , C07D417/14 , C07D471/04
摘要： The invention relates to antibacterial compounds of Formula (I) wherein R 1 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 CH 2 or NH, with the proviso that U, V and W are not all N; A is a bond or CH 2 ; R 2 is H or, provided A is CH 2 , may also be OH; m and n each independently are 0 or 1; D is CH 2 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, (C 1 -C 3 )alkyl and halogen, or G is a group G 1 or G 2 wherein Z 1 , Z 2 and Z 3 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 CH 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; U和V各自独立地为CH或N; “----”是债券或不存在; W是CH或N，或当“----”不存在时，W是CH2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表示通过选自烷基，（C1-C3）烷基和卤素的取代基在间位和/或对位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。

3. 发明申请

WO2009034546A3 TRANS-DECAHYDROISOQUINOLINE DERIVATIVES 审中-公开
公开(公告)号：WO2009034546A3
公开(公告)日：2009-03-19
申请号：PCT/IB2008/053688
申请日：2008-09-12
申请人： ACTELION PHARMACEUTICALS LTD , HUBSCHWERLEN, Christian , RUEEDI, Georg , SURIVET, Jean-Philippe , ZUMBRUNN ACKLIN, Cornelia
发明人： HUBSCHWERLEN, Christian , RUEEDI, Georg , SURIVET, Jean-Philippe , ZUMBRUNN ACKLIN, Cornelia
IPC分类号： C07D401/04 , C07D471/04 , C07D519/00 , A61K31/4725 , A61K31/04
摘要： The invention relates to antibacterial compounds of formula (I) wherein R 1 is alkoxy, one or two of U, V, W, X represent(s) N, the remaining represents CH, whereby V may also represent CR a, W may also represent CR b and X may also represent CR C , R a is hydroxyalkyl; R b is alkoxycarbonyl, carboxy or hydroxyalkyl; R c is halogen, R 2 is alkoxycarbonyl, carboxy, hydroxyalkyl or aminoalkyl, A is CH 2 B, C(=O)B or CH 2 CH=CHD, B is the group (II) wherein Z is N or CH and the ring P is selected from the formula (III) in which Q is O or S, and D is aryl (e.g. 1,4-difluoro-2 -phenyl).

4. 发明申请

WO2014178008A1 QUINOLONE DERIVATIVES 审中-公开
标题翻译：喹诺酮衍生物
公开(公告)号：WO2014178008A1
公开(公告)日：2014-11-06
申请号：PCT/IB2014/061099
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 R 1 , 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。

5. 发明申请

WO2010067332A1 5-AMINO-2-(1-HYDROXY-ETHYL)-TETRAHYDROPYRAN DERIVATIVES 审中-公开
标题翻译： 5-氨基-2-（1-羟基 - 乙基） - 羟基衍生物衍生物
公开(公告)号：WO2010067332A1
公开(公告)日：2010-06-17
申请号：PCT/IB2009/055689
申请日：2009-12-11
申请人： ACTELION PHARMACEUTICALS LTD , HUBSCHWERLEN, Christian , RUEEDI, Georg , SURIVET, Jean-Philippe , ZUMBRUNN ACKLIN, Cornelia
发明人： HUBSCHWERLEN, Christian , RUEEDI, Georg , SURIVET, Jean-Philippe , ZUMBRUNN ACKLIN, Cornelia
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.
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（特别是甲氧基）; R2表示H或F; R 3，R 4，R 5和R 6各自独立地表示H或D; V表示CH且W表示CH或N或V表示N，W表示CH; Y表示CH或N; Z表示O，S或CH 2; A代表CH2，CH2CH2或CD2CD2; 和这些化合物的盐。

6. 发明申请

WO2010041194A1 TRICYCLIC OXAZOLIDINONE ANTIBIOTIC COMPOUNDS 审中-公开
标题翻译：三氧化二氮唑酮类抗生素化合物
公开(公告)号：WO2010041194A1
公开(公告)日：2010-04-15
申请号：PCT/IB2009/054357
申请日：2009-10-06
申请人： ACTELION PHARMACEUTICALS LTD , HUBSCHWERLEN, Christian , RITZ, Daniel , RUEEDI, Georg , SURIVET, Jean-Philippe , ZUMBRUNN ACKLIN, Cornelia
发明人： HUBSCHWERLEN, Christian , RITZ, Daniel , RUEEDI, Georg , SURIVET, Jean-Philippe , ZUMBRUNN ACKLIN, Cornelia
IPC分类号： C07D471/06 , C07D471/16 , C07D487/06 , C07D519/00 , A61K31/437 , A61K31/4375 , A61K31/4985 , A61K31/536 , 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, CR 6 or N; R 0 is H or, if ----- is a bond, may also be alkoxy; R 1 is notably H or halogen; U is CH or N when ----- is a bond, or, if ----- is absent, U is CH 2 , NH or NR 9 ; R 2 is H, alkylcarbonyl or CH 2 -R 3 ; R 3 is H, alkyl or hydroxyalkyl; R 4 is H or, if n is not 0 and R 5 is H, may also be OH; R 5 is H, alkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, carboxy or alkoxycarbonyl; R 6 is hydroxyalkyl, carboxy, alkoxycarbonyl or -(CH 2 ) q -NR 7 R 8 , q being 1, 2 or 3 and each of R 7 and R 8 independently being H or alkyl or R 7 and R 8 forming with the N atom bearing them a ring; R 9 is alkyl or hydroxyalkyl; A is -(CH 2 ) p -, -CH 2 CH 2 CH(OH)- or -COCH 2 CH(OH)-; G is substituted phenyl or G 1 or G 2 , wherein Q is O or S and X is CH or N; and Y 1 , Y 2 and Y 3 may each be CH or N; and n is 0 when A is -CH 2 CH 2 CH(OH)- or -COCH 2 CH(OH)-, and n is 0, 1 or 2 when A is -(CH 2 ) 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Δε- 是一个键或不存在，V是CH，CR 6或N; R 0是H，或者如果Δε- 是一个键，也可以是烷氧基; R 1特别是H或卤素; 当Δε- 是一个债券，或者，如果?? ----- ?? 不存在，U是CH 2，NH或NR 9; R 2是H，烷基羰基或者-CH 2 -R 3; R 3为H，烷基或羟烷基; R 4为H，或者如果n不为0且R 5为H，也可为OH; R 5为H，烷基，羟基烷基，氨基烷基，烷氧基烷基，羧基或烷氧基羰基; R 6是羟基烷基，羧基，烷氧基羰基或 - （CH 2）q -NR 7 R 8，q是1,2或3，R 7和R 8各自独立地是H或烷基或R 7和R 8与 N原子带有一个环; R 9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G 1或G 2，其中Q是O或S，X是CH或N; Y 1，Y 2和Y 3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时，n为0,1或2， 2，3或4，条件是n和p的和为2,3或4; 和这些化合物的盐。

7. 发明申请

WO2009147616A1 [4-(1-AMINO-ETHYL) -CYCLOHEXYL] -METHYL-AMINE AND [6-(1-AMINO-ETHYL) -TETRAHYDRO- PYRAN-3-YL] -METHYL-AMINE DERIVATIVES AS ANTIBACTERIALS 审中-公开
标题翻译： [4-（1-氨基 - 乙基） - 环己基] - 甲基 - 胺和[6-（1-氨基 - 乙基） - 羟基 - 吡喃-3-基] - 甲基胺衍生物作为抗生素
公开(公告)号：WO2009147616A1
公开(公告)日：2009-12-10
申请号：PCT/IB2009/052307
申请日：2009-06-02
申请人： ACTELION PHARMACEUTICALS LTD , HUBSCHWERLEN, Christian , RUEEDI, Georg , SURIVET, Jean-Philippe , ZUMBRUNN ACKLIN, Cornelia
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.
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（II），（III）之一的基团，其中Z表示CH或N，Q表示O 或S和K表示O或S; 和这些化合物的盐。

8. 发明申请

WO2017179002A1 ANTIBACTERIAL BIAROMATIC DERIVATIVES WITH OXETANE-3-YLOXY SUBSTITUTION 审中-公开
标题翻译：具有OXETANE-3-YLOXY取代基的抗菌BIAROMATIC衍生物
公开(公告)号：WO2017179002A1
公开(公告)日：2017-10-19
申请号：PCT/IB2017/052133
申请日：2017-04-13
申请人： ACTELION PHARMACEUTICALS LTD
发明人： CREN, Sylvaine , RUEEDI, Georg , ZUMBRUNN, Cornelia
IPC分类号： C07D417/14 , C07D498/04 , A61P31/04 , A61K31/5383 , A61K31/542
摘要： The invention relates to antibacterial compounds of formula (I), wherein U 1 represents N or CH, U 2 represents N or CH, U 3 represents N or CH, it being understood that at most two of U 1 , U 2 , U 3 can represent N at the same time; V 1 represents N or CH, V 2 represents N, CH or C(OH) and V 3 represents N, CH or C(OH), it being understood that at most two of V 1 , V 2 and V 3 can represent N at the same time; the dotted line "----- " represents a bond or is absent; X represents CH or N; and Q represents O or S. It further relates pharmaceutical compositions containing these compounds and the uses of these compounds in the manufacture of medicaments for the treatment of bacterial infections. These compounds are useful antimicrobial agents effective against a variety of human and veterinary pathogens including among others Gram-positive and Gram-negative aerobic and anaerobic bacteria.
摘要翻译：本发明涉及式（I）的抗菌化合物，其中U 1代表N或CH，U 2代表N或CH，U 3表示N或CH，应该理解的是，U 1，U 2，U 3中至多两个，可以同时代表N; V 1表示N或CH，V 2表示N，CH或C（OH），并且V 3表示N，CH或C（OH）），应该理解，V 1，V 2和V 3中的至多两个可以同时表示N; 虚线“-----” 代表债券或不存在; X代表CH或N; Q代表O或S.它进一步涉及含有这些化合物的药物组合物以及这些化合物在制备用于治疗细菌感染的药物中的用途。这些化合物是有效对抗各种人类和兽医病原体的有用的抗微生物剂，其中包括革兰氏阳性和革兰氏阴性好氧和厌氧细菌。

9. 发明申请

WO2014108836A1 ANTIBACTERIAL OXADIAZOLONE DERIVATIVES 审中-公开
标题翻译：抗氧化亚油酸衍生物
公开(公告)号：WO2014108836A1
公开(公告)日：2014-07-17
申请号：PCT/IB2014/058123
申请日：2014-01-08
申请人： ACTELION PHARMACEUTICALS LTD
发明人： HUBSCHWERLEN, Christian , RUEEDI, Georg , ZUMBRUNN, Cornelia
IPC分类号： C07D471/06 , C07D471/16 , C07D487/06 , C07D519/00 , A61K31/437 , A61K31/4375 , A61K31/4985 , A61K31/536 , A61P31/04
CPC分类号： C07D471/06 , A61K31/4245 , A61K31/4375 , C07D471/16 , C07D487/06 , C07D519/00 , Y02A50/401
摘要： The invention relates to antibacterial compounds of formula (I) wherein U represents CH or N; V represents CH or N, provided that at least one of U and V does not represent N; R represents H, halogen, methyl, methoxy, cyano or ethynyl; either W represents a phenyl group substituted in para position with (C 1 -C 3 )alkyl, (C 1 -C 3 )alkoxy or (C 1 -C 3 )thioalkoxy and optionally in meta position with halogen, or W is a group having one of the formulae W 1 and W 2 below wherein Q is O or S and X is CH or N; and 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; V表示CH或N，条件是U和V中的至少一个不表示N; R代表H，卤素，甲基，甲氧基，氰基或乙炔基; W表示在对位被（C1-C3）烷基，（C1-C3）烷氧基或（C1-C3）硫代烷氧基取代的苯基，并且任选地在与卤素的间位置，或W是具有式W1之一的基团和W2，其中Q是O或S，X是CH或N; 和这些化合物的盐。

10. 发明申请

WO2013021363A1 QUINAZOLINE-2,4-DIONE DERIVATIVES 审中-公开
标题翻译：喹唑啉-2,4-二酮衍生物
公开(公告)号：WO2013021363A1
公开(公告)日：2013-02-14
申请号：PCT/IB2012/054080
申请日：2012-08-10
申请人： ACTELION PHARMACEUTICALS LTD , HUBSCHWERLEN, Christian , SURIVET, Jean-Philippe , RUEEDI, Georg , ZUMBRUNN ACKLIN, Cornelia
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.
摘要翻译：本发明涉及式（I）的抗菌化合物，其中R1是H，卤素，（C1-C3）烷基或（C1-C3）烷氧基; R2是H，卤素，（C1-C3）烷基，（C1-C3）烷氧基或吡咯烷-1-基; R3是H，卤素，（C1-C3）烷基，（C1-C3）烷氧基，乙烯基或2-甲氧基羰基乙烯基或R2和R3与它们携带的两个碳原子形成苯环; R4是H，卤素，（C1-C3）烷基或（C1-C3）烷氧基，R5是H，（C1-C3）烷基或环丙基，或R4和R5一起形成-CH2CH2CH2-基团; A是二价基团-CH 2 - ， - CH 2 CH 2 - ， - CH 2 OH，CH 2 - ， - CH 2 OH（R 6） - 或-CH 2 NHCH 2 - ，其中＃表示与任选取代的（喹唑啉 - 2,4-二酮-3-基）甲基残基，*表示与取代的（恶唑烷酮-4-基）甲基残基的连接点; R6是H或乙酰基; Y是CH或N; Q为O或S; 和这些化合物的盐。

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