发明名称 1,6-diazabicyclo [3,2,1] octan-7-one derivatives and their use in the treatment of bacterial infections
摘要 Compounds of Formula (I), their preparation and use in preventing or treating bacterial infection is disclosed.;
申请公布号 US8822450(B2) 申请公布日期 2014.09.02
申请号 US201214111592 申请日期 2012.08.24
申请人 Wockhardt Ltd. 发明人 Patel Mahesh Vithalbhai;Deshpande Prasad Keshav;Bhawsar Satish;Bhagwat Sachin;Jafri Mohammed Alam;Mishra Amit;Pavase Laxmikant;Gupta Sunil;Kale Rajesh;Joshi Sanjeev
分类号 C07D471/08;A61K31/542;A61K31/529;A61K31/429;A61K45/06;A61K31/407;A61K31/496;A61K31/167;A61K31/427 主分类号 C07D471/08
代理机构 Bio Intellectual Property Services LLC (Bio IPS) 代理人 Bio Intellectual Property Services LLC (Bio IPS) ;Zaghmout O. (Sam)
主权项 1. A compound of Formula (I)or a stereoisomer or a pharmaceutically acceptable salt thereof;wherein: R1 is: (a) hydrogen,(b) (CO)n—R3, or(c) COOR4. n is 0, 1 or 2; R2 is: (a) SO3M,(b) SO2NH2,(c) PO3M,(d) CH2COOM,(e) CF2COOM,(f) CHFCOOM, or(g) CF3; M is hydrogen or a cation; R3 is: (a) hydrogen,(b) C1-C6 alkyl optionally substituted with one or more substituents independently selected from halogen, OR5, CN, COOR5, CONR6R7, NR6R7, NR5COR8, NR5CONR6R7, heterocyclyl, heteroaryl, cycloalkyl or aryl,(c) CN,(d) NR6R7,(e) CONR6R7,(f) NHCONR6R7,(g) aryl optionally substituted with one or more substituents independently selected from C1-C6 alkyl, OR5, NR6R7, halogen, CN, CONR6R7, SO2-alkyl, SO2-aryl, OSO2-alkyl, OSO2-aryl, or NHCONR6R7,(h) heterocyclyl optionally substituted with one or more substituents independently selected from C1-C6 alkyl, OR5, NR6R7, halogen, CN, CONR6R7, SO2-alkyl, SO2-aryl, OSO2-alkyl, OSO2-aryl, or NHCONR6R7,(i) heteroaryl optionally substituted with one or more substituents independently selected from C1-C6 alkyl, OR5, NR6R7, halogen, CN, CONR6R7, SO2-alkyl, SO2-aryl, OSO2-alkyl, OSO2-aryl, or NHCONR6R7,(j) cycloalkyl optionally substituted with one or more substituents independently selected from C1-C6 alkyl, OR5, NR6R7, halogen, CN, CONR6R7, SO2-alkyl, SO2-aryl, OSO2-alkyl, OSO2-aryl, or NHCONR6R7,(k) cycloalkyl substituted with C1-C6 alkyl wherein C1-C6 alkyl is further substituted with one or more substituents independently selected from OR5, NR6R7, halogen, CN, or CONR6R7, or(i) OR8; R4 is: (a) hydrogen,(b) C1-C6 alkyl optionally substituted with one or more substituents independently selected from halogen, OR5, CN, COOR5, CONR6R7, NR6R7, NR5COR8, heterocyclyl, heteroaryl, cycloalkyl or aryl,(c) aryl optionally substituted with one or more substituents independently selected from C1-C6 alkyl, OR5, NR6R7, halogen, CN, CONR6R7, SO2-alkyl, SO2-aryl, OSO2-alkyl, OSO2-aryl, or NHCONR6R7,(d) heterocyclyl optionally substituted with one or more substituents independently selected from C1-C6 alkyl, OR5, NR6R7, halogen, CN, CONR6R7, SO2-alkyl, SO2-aryl, OSO2-alkyl, OSO2-aryl, or NHCONR6R7,(e) heteroaryl optionally substituted with one or more substituents independently selected from C1-C6 alkyl, OR5, NR6R7, halogen, CN, CONR6R7, SO2-alkyl, SO2-aryl, OSO2-alkyl, OSO2-aryl, or NHCONR6R7, or(f) cycloalkyl optionally substituted with one or more substituents independently selected from C1-C6 alkyl, OR5, NR6R7, halogen, CN, CONR6R7, SO2-alkyl, SO2-aryl, OSO2-alkyl, OSO2-aryl, or NHCONR6R7; R5 and R8 are each independently: (a) hydrogen, or(b) C1-C6 alkyl optionally substituted with one or more substituents independently selected from halogen, CN, CONR6R7, NR6R7, heterocyclyl, heteroaryl, cycloalkyl or aryl; R6 and R7 are each independently: (a) hydrogen,(b) C1-C6 alkyl optionally substituted with one or more substituents independently selected from halogen, OR5, CN, COOR5, CONR5R8, NR5R8, NR5COR8, heterocyclyl, heteroaryl, cycloalkyl or aryl,(c) aryl optionally substituted with one or more substituents independently selected from C1-C6 alkyl, OR5, NR5R8, halogen, CN, CONR5R8, SO2-alkyl, SO2-aryl, OSO2-alkyl, OSO2-aryl, or NHCONR5R8,(d) heterocyclyl optionally substituted with one or more substituents independently selected from C1-C6 alkyl, OR5, NR5R8, halogen, CN, CONR5R8, SO2-alkyl, SO2-aryl, OSO2-alkyl, OSO2-aryl, or NHCONR5R8,(e) heteroaryl optionally substituted with one or more substituents independently selected from C1-C6 alkyl, OR5, NR5R8, halogen, CN, CONR5R8, SO2-alkyl, SO2-aryl, OSO2-alkyl, OSO2-aryl, or NHCONR5R8,(f) cycloalkyl optionally substituted with one or more substituents independently selected from C1-C6 alkyl, OR5, NR5R8, halogen, CN, CONR5R8, SO2-alkyl, SO2-aryl, OSO2-alkyl, OSO2-aryl, or NHCONR5R8, or(g) R6 and R7 are joined together to form a four to seven member ring.
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