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    • 3. 发明申请
    • COMPOUNDS
    • 化合物
    • WO2004002992A1
    • 2004-01-08
    • PCT/EP2003/006756
    • 2003-06-25
    • GLAXO GROUP LIMITEDAXTEN, Jeffrey, MichaelDAINES, Robert, A.DAVIES, David, ThomasGALLAGHER, Timothy, FrancisJONES, Graham, ElginMILLER, William, HenryPEARSON, Neil, DavidPENDRAK, Israil
    • AXTEN, Jeffrey, MichaelDAINES, Robert, A.DAVIES, David, ThomasGALLAGHER, Timothy, FrancisJONES, Graham, ElginMILLER, William, HenryPEARSON, Neil, DavidPENDRAK, Israil
    • C07D491/06
    • C07D493/04C07D417/12C07D513/04
    • Cyclohexane and cyclohexene derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly man. A compound of formula (I) or a pharmaceutically acceptable derivative thereof: (I) R A is an optionally substituted bicyclic carbocyclic or heterocyclic ring system of structure: containing 0-3 heteroatmoms in each ring in which: at least one of the rings (x) and (y) is aromatic; one of Z 4 and Z 5 is C or N and the other is C; Z 3 is N, NR 13 , O, S(O) x , CO, CR 1 or CR 1 R 1a ; Z1 and Z2 are indendently a 2 or 3 atom linker group each atom of which is independently selected from N, NR 13 , O, S(O) x , CO, CR 1 , and CR 1 R 1a ; such that each ring is independently substituted with 0-3 groups R 1 and/or R 1a . R 4 is a group -CH 2 -R 5 1 in which R 5 1 is selected from: (C 4-8 ) alkyl; hydroxy (C 4-8 ) alkyl; (C 1-4 )alkoxy (C 4-8 )alkyl; (C 1-4 ) alkanoyloxy (C 4-8 ) alkyl; (C 3-8 )cycloalkyl (C 4-8 )alkyl;hydroxy-, (C 1-6 ) alkoxy- or (C 1-6 ) alkanoyloxy-(C 3-8 )cycloalkyl (C 4-8 )alkyl; cyano(C 4-8 )alkyl; (C 4-8 )alkenyl; (C 4-8 )alkynyl; tetrahydrofuryl; mono- or di-(C 1-6) alkylamino (C 4-8 )alkyl; acylamino (C 4-8 )alkyl; C( 1-6 )alkyl- or acyl-aminocarbonyl (C 4-8 ) alkyl; mono- or di- (C 1-6 )alkylamino(hydroxy) (C 4-8 )alkyl; or R 4 is a group-U-R 5 2 where R 5 2 is an optionally substituted bicyclic carbocyclic or heterocyclic ring system (A): containing up to four heteroatoms in each ring in which at least one of rings (a) and (b) is aromatic; X 1 is C or N when part of an aromatic ring or CR 14 when part of a non-aromatic ring.
    • 环己烷和环己烯衍生物及其药学上可接受的衍生物可用于治疗哺乳动物,特别是人的细菌感染的方法。 式(I)化合物或其药学上可接受的衍生物:(I)R AA是任选取代的双环碳环或杂环体系,其结构为:在每个环中含有0-3个异质体,其中:至少一个 环(x)和(y)是芳族的; Z 4和Z 5之一是C或N,另一个是C; Z 3为N,NR 13,O,S(O)x,CO,CR 1或CR 1 R 1a; Z1和Z2独立地是2或3个原子连接基团,其各自的原子独立地选自N,NR 13,O,S(O)x,CO,CR 1和CR 1 R 1a >; 使得每个环独立地被0-3个基团R 1和/或R 1a取代。 R 4是基团-CH 2 -R 5 1,其中R 5选自:(C 4-8)烷基; 羟基(C 4-8)烷基; (C 1-4)烷氧基(C 4-8)烷基; (C 1-4)烷酰氧基(C 4-8)烷基; (C 3-8)烷基;羟基 - ,(C 1-6)烷氧基 - 或(C 1-6)烷酰氧基 - (C 3-8)环烷基(C 4-8)烷基; 氰基(C 4-8)烷基; (C4-8)链烯基; (C4-8)炔基; 四氢呋喃; 单 - 或二 - (C 1-6)烷基氨基(C 4-8)烷基; 酰基氨基(C 4-8)烷基; C(1-6)烷基 - 或酰基 - 氨基羰基(C 4-8)烷基; 单 - 或二 - (C 1-6)烷基氨基(羟基)(C 4-8)烷基; 或R 4是基团UR 5,其中R 5是任选取代的双环碳环或杂环系统(A):在每个环中含有至多四个杂原子,其中至少一个环( a)和(b)是芳香族的; 当芳族环的一部分或非芳族环的一部分时,X 1为C或N。