- 专利标题: Derivatives of pyrimido[6, 1-A]isoquinolin-4-one
-
申请号: US12150232申请日: 2008-04-24
-
公开(公告)号: US20080206163A1公开(公告)日: 2008-08-28
- 发明人: Alexander William Oxford , David Jack
- 申请人: Alexander William Oxford , David Jack
- 申请人地址: GB London
- 专利权人: Verona Pharma PLC
- 当前专利权人: Verona Pharma PLC
- 当前专利权人地址: GB London
- 优先权: GB9907454.4 19990331; GB9909802.2 19990428
- 主分类号: A61K9/12
- IPC分类号: A61K9/12 ; C07D471/04 ; A61K31/519
摘要:
Compounds of general formula (I) wherein each of R1 and R2 independently represents a C1-6 alkyl or C2-7 acyl group; R5 represents a hydrogen atom or a C1-3 alkyl, C2-3 alkenyl or C2-3 alkynyl group; R6 represents a hydrogen atom or a C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, amino, C1-6 alkylamino, di(C1-6) alkylamino or C2-7 acylamino group; each of R7 and R8 independently represents a hydrogen or halogen atom or a hydroxy, trifluoromethyl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C2-7 acyl, C1-6 alkythio, C1-6 alkoxy, C3-6 cycloalkyl; and R9 represents a hydrogen or halogen atom or a hydroxy, trifluoromethyl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C2-7 acyl, C1-6 alkythio, C1-6 alkoxy or C3-6 cycloalkyl group; X represents OCH2 or a group CR3R4, wherein each of R3 and R4 independently represents a hydrogen atom or a C1-3 alkyl group; each of R10 and R11 independently represents a hydrogen atom, a C1-3 alkyl, C3-6 cycloalkyl or phenyl group; y represents an oxygen atom or a group CHNO2, NCN, NH or NNO2, n is an integer from 2 to 4; or a salt thereof; are useful for treatment of respiratory disorders such as asthma. Compounds of the invention have a longer duration of action than the known compound trequinsin (9,10-dimethoxy-3-methyl-2-mesitylimino-2,3,6,7-tetrahydro-4H-pyrimido[6,1-a]isoquinolin-4-one) and do not have trequinsin's very bitter taste.
公开/授权文献
- US08242127B2 Derivatives of pyrimido[6,1-A]isoquinolin-4-one 公开/授权日:2012-08-14
信息查询