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1. 发明公开

EP2721034A1 TRICYCLIC ANTIBIOTICS 有权
标题翻译：三环类抗生素
公开(公告)号：EP2721034A1
公开(公告)日：2014-04-23
申请号：EP12728438.8
申请日：2012-06-11
申请人： Basilea Pharmaceutica AG
发明人： GAUCHER, Bérangère , DANEL, Franck Hubert , XIE, Tong , XU, Lin
IPC分类号： C07D491/14 , C07D491/147
CPC分类号： C07D498/04 , C07D491/052 , C07D491/14 , C07D491/147 , C07D495/04
摘要： Compounds of formula (I), wherein A1 represents -0-, -S- or -CH
2 -; A2 represents -CH
2 - or -0-; A3 represents C
3 -C
8 cycloalkylene; saturated or unsaturated 4 to 8-membered heterocyclodiyl with 1, 2 or 3 heteroatoms selected from nitrogen or oxygen, which group A3 is unsubstituted or substituted; A4 represents C
1 -C
4 alkylene, -C(=0)-; G represents aryl or heteroaryl, which is unsubstituted or substituted; X1 represents a nitrogen atom or CR1; R1 represents a hydrogen atom or a halogen atom; R2 represents a hydrogen atom; m is 0 or 1; n is 1; the -(CH
2 )
n - group is unsubstituted or substituted; p is 0 or 1; or pharmaceutically acceptable salts thereof are valuable for use as a medicament for the treatment of bacterial infections.
摘要翻译：式（I）化合物，其中A 1表示-O - ， - S-或-CH 2 - A2代表-CH 2或-O-; A3代表C 3 -C 8亚环烷基; 具有1,2或3个选自氮或氧的杂原子的饱和或不饱和的4至8元杂环二基，该基团A3是未取代的或取代的; A4代表C 1 -C 4亚烷基，-C（= O） - ; G代表未经取代或经取代的芳基或杂芳基; X1代表氮原子或CR1; R1代表氢原子或卤素原子; R2代表氢原子; m是0或1; n是1; - （CH 2）n - 基团是未取代的或取代的; p是0或1; 或其药学上可接受的盐对于用作治疗细菌感染的药物有价值。

2. 发明公开

EP1965798A2 USEFUL COMBINATIONS OF MONOBACTAM ANTIBIOTICS WITH BETA-LACTAMASE INHIBITORS 有权
标题翻译：有用的单环内酰胺抗生素
公开(公告)号：EP1965798A2
公开(公告)日：2008-09-10
申请号：EP06817737.7
申请日：2006-12-07
申请人： Basilea Pharmaceutica AG
发明人： DESARBRE, Eric , GAUCHER, Bérangère , PAGE, Malcolm, G.,P. , ROUSSEL, Patrick
IPC分类号： A61K31/4436 , A61K31/427 , A61K31/407 , A61K31/43 , A61K31/545 , A61K31/69 , A61K31/662 , C07D417/14 , C07D487/04
CPC分类号： C07D417/14 , A61K31/407 , A61K31/41 , A61K31/427 , A61K31/43 , A61K31/433 , A61K31/4375 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4725 , A61K31/496 , A61K31/506 , A61K31/545 , A61K31/662 , A61K31/69 , A61K45/06 , C07D401/14 , C07D403/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D487/04 , Y02A50/473
摘要： Compounds of the formula II: in which R8 is of the formula Q-(X) r -CO- wherein either a) X = - CH 2 -, r = 1, Q is a pyridinium group and R7 is -SO 3 - or -OSO 3 - ; or b) X = -SCH 2 - and r = 1; wherein Q is e.g. 1,2,3,4-tetrazol-5-yl and R7 is -SO 3 H or -OSO 3 H; or c) X = -CH 2 NH 2 -, r = 1 and Q is e.g. phenyl or a 5-6-membered heterocycle and R7 is -SO 3 H or -OSO 3 H; or d) X = -NH 2 - and r = 1, wherein Q is e.g. phenyl and R7 is - SO 3 H or -OSO 3 H; are beta-lactamase inhibitors. They may be used in combination with monobactams against gram-negative bacteria.

3. 发明授权

EP2721034B1 N-HETEROTRICYCLIC ANTIBIOTICS 有权
标题翻译： N-异三环抗生素
公开(公告)号：EP2721034B1
公开(公告)日：2016-07-20
申请号：EP12728438.8
申请日：2012-06-11
申请人： Basilea Pharmaceutica AG
发明人： GAUCHER, Bérangère , DANEL, Franck Hubert , XIE, Tong , XU, Lin
IPC分类号： C07D491/14 , C07D491/147 , C07D491/052 , C07D495/04 , C07D498/04 , A61K31/4375 , A61K31/436 , A61K31/4365 , A61P31/04
CPC分类号： C07D498/04 , C07D491/052 , C07D491/14 , C07D491/147 , C07D495/04

4. 发明授权

EP2513115B1 TRICYCLIC ANTIBIOTICS 有权
标题翻译：三环抗生素
公开(公告)号：EP2513115B1
公开(公告)日：2013-10-09
申请号：EP10793255.0
申请日：2010-12-17
申请人： Basilea Pharmaceutica AG
发明人： GAUCHER, Bérangère , DANEL, Franck, Hubert , TANG, XiaoHu , XIE, Tong , XU, Lin
IPC分类号： C07D491/04 , C07D495/04 , A61K31/4741 , A61K31/4743 , A61P31/04
CPC分类号： C07D513/04 , C07D491/04 , C07D491/052 , C07D491/147 , C07D495/04 , C07D498/04 , C07D498/14

5. 发明公开

EP2513115A1 TRICYCLIC ANTIBIOTICS 有权
标题翻译： Tricyclische Antibiotika
公开(公告)号：EP2513115A1
公开(公告)日：2012-10-24
申请号：EP10793255.0
申请日：2010-12-17
申请人： Basilea Pharmaceutica AG
发明人： GAUCHER, Bérangère , DANEL, Franck, Hubert , TANG, XiaoHu , XIE, Tong , XU, Lin
IPC分类号： C07D491/04 , C07D495/04 , A61K31/4741 , A61K31/4743 , A61P31/04
CPC分类号： C07D513/04 , C07D491/04 , C07D491/052 , C07D491/147 , C07D495/04 , C07D498/04 , C07D498/14
摘要： Compound of formula (I): wherein A1 represents -O-, -S- or -N-R3; A2 represents -CH
2 -, -O-, -N-R4, -C(=O)- or -CH(O-R4)-; A3 represents C
3 -C
8 cycloalkylene; saturated and unsaturated 4 to 8-membered heterocyclodiyl with 1, 2 or 3 heteroatoms selected from nitrogen, oxygen and sulphur, which group A3 is unsubstituted or substituted; A4 represents C
1 -C
4 alkylene, C
2 -C
4 alkenylene, >C=O or a group selected from - C
2 H
4 NH-, -C
2 H
4 O-, and -C
2 H
4 S- being linked to the adjacent NR5-group via the carbon atom; and G represents aryl or heteroaryl, which is unsubstituted or substituted and R1 and R2 independently of one another, represent hydrogen or a substituent selected from hydroxy, halogen, mercapto, cyano, nitro, C
1 -C
6 alkyl, C
1 -C
6 alkoxy, C
1 -C
6 alkylthio, C
1 -C
6 alkylcarbonyloxy, C
1 -C
6 alkylsulfonyloxy, C
1 -C
6 heteroalkylcarbonyloxy, C5-C
6 heterocyclylcarbonyloxy, C
1 -C
6 heteroalkoxy, wherein heteroalkyl, heteroalkoxy groups or heterocyclyl comprise 1, 2 or 3 heteroatoms selected from nitrogen, oxygen and sulphur, in which substituents the alkyl moieties are unsubstituted or further substituted; R3, R4 and R5 independently of one another, represent hydrogen or C
1 -C
6 alkyl; X1 and X2 independently of one another, represent a nitrogen atom or CR2, with the proviso that at least one of Xl and X2 represents a nitrogen atom; m is 1; and the (CH2)m moiety is optionally substituted by C
1 -C
4 alkyl; halogen, carboxy, hydroxy, C
1 -C
4 alkoxy, C
1 -C
4 -alkylcarbonyloxy, amino, mono- or di-(C
1 -C
4 alkyl)amino or acylamino n is 0, 1 or 2 or pharmaceutically acceptable salt thereof are valuable for use as a medicament for the treatment of bacterial infections.

6. 发明公开

EP2389376A1 NOVEL BICYCLIC ANTIBIOTICS 审中-公开
标题翻译： NEW双环抗生素
公开(公告)号：EP2389376A1
公开(公告)日：2011-11-30
申请号：EP10700583.7
申请日：2010-01-21
申请人： Basilea Pharmaceutica AG
发明人： GAUCHER, Bérangère , DANEL, Franck Hubert , ROUSSEL, Patrick
IPC分类号： C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14 , A61K31/4375 , A61K31/47 , A61P33/00
CPC分类号： C07D513/04 , C07D215/20 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D495/04 , C07D498/04 , C07D519/00
摘要： The antibacterial compound of formula I wherein X1, X3; X4 and X6, each independently of the others, represents a nitrogen atom or CR2, with the proviso that at least one of X1, X3; X4 and X6 represents a nitrogen atom; X2 represents C—H, C—(C1-C6alkyl), C—(C1-C6alkoxy), C-halogen, C—COOH; X5 represents C—H or C—(C1-C6alkyl), C-halogen; A1, A2, A3, R1 and R4 represent various substituents, G represents aryl or heteroaryl, which is unsubstituted or substituted which compounds show good activity against pathogenic bacteria.

7. 发明授权

EP1965798B1 USEFUL MONOBACTAM ANTIBIOTICS 有权
标题翻译：有用的单环内酰胺抗生素
公开(公告)号：EP1965798B1
公开(公告)日：2011-10-19
申请号：EP06817737.7
申请日：2006-12-07
申请人： Basilea Pharmaceutica AG
发明人： DESARBRE, Eric , GAUCHER, Bérangère , PAGE, Malcolm, G.,P. , ROUSSEL, Patrick
IPC分类号： A61K31/4436 , A61K31/427 , A61K31/407 , A61K31/43 , A61K31/545 , A61K31/69 , A61K31/662 , C07D417/14 , C07D487/04
CPC分类号： C07D417/14 , A61K31/407 , A61K31/41 , A61K31/427 , A61K31/43 , A61K31/433 , A61K31/4375 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4725 , A61K31/496 , A61K31/506 , A61K31/545 , A61K31/662 , A61K31/69 , A61K45/06 , C07D401/14 , C07D403/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D487/04 , Y02A50/473
摘要： Compounds of the formula II: in which R8 is of the formula Q-(X) r -CO- wherein either a) X = - CH 2 -, r = 1, Q is a pyridinium group and R7 is -SO 3 - or -OSO 3 - ; or b) X = -SCH 2 - and r = 1; wherein Q is e.g. 1,2,3,4-tetrazol-5-yl and R7 is -SO 3 H or -OSO 3 H; or c) X = -CH 2 NH 2 -, r = 1 and Q is e.g. phenyl or a 5-6-membered heterocycle and R7 is -SO 3 H or -OSO 3 H; or d) X = -NH 2 - and r = 1, wherein Q is e.g. phenyl and R7 is - SO 3 H or -OSO 3 H; are beta-lactamase inhibitors. They may be used in combination with monobactams against gram-negative bacteria.

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