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    • 7. 发明授权
    • Barbituric acid derivatives, processes for their production and pharmaceutical agents containing these compounds
    • 巴比妥酸衍生物,其制备方法和含有这些化合物的药剂
    • US06472396B1
    • 2002-10-29
    • US09594700
    • 2000-06-16
    • Elmar BosiesAngelika EssweinFrank GramsHans-Willi KrellErnesto Menta
    • Elmar BosiesAngelika EssweinFrank GramsHans-Willi KrellErnesto Menta
    • C07D23962
    • C07D401/04C07D239/62
    • Compounds of formula I, useful as matrix metalloprotease inhibitors, wherein X, Y and Z are each oxygen; R1 is selected from the group consisting of (a) n-octyl, (b) n-decyl, (c) biphenyl and (d) (4-phenoxy)phenyl, wherein the terminal monocycle for moieties (c)-(d) is unsubstituted or substituted by a substituent selected from the group consisting of —NH2, —NO2, —SO2NH2, —SO2CH3, acetyl, hydroxy, methoxy, ethoxy, cyano and halogen; R2 and R3 are each hydrogen; and R4 and R5, together with the nitrogen atom to which they are bound, form a piperazinyl or piperidyl ring, wherein the piperazinyl ring is substituted in the 4-position with a substituent selected from the group consisting of (a) a 6-membered aromatic monocycle having 0, 1 or 2 nitrogen atoms and the remainder of the atoms in the monocycle being carbon and (b) hydroxy-C1-C6 alkyl, wherein the monocycle is unsubstituted or substituted by a substituent selected from the group consisting of halogen, —NH2, —NO2, —SO2NH2, —SO2CH3, acetyl and cyano.
    • 可用作基质金属蛋白酶抑制剂的式I化合物,其中X,Y和Z各自为氧; R 1选自(a)正辛基,(b)正癸基,(c)联苯和(d) (4-苯氧基)苯基,其中部分(c) - (d)的末端单环是未取代的或被选自-NH 2,-NO 2,-SO 2 NH 2,-SO 2 CH 3,乙酰基,羟基,甲氧基 ,乙氧基,氰基和卤素; R 2和R 3各自为氢; 和R 4和R 5与它们所连接的氮原子一起形成哌嗪基或哌啶基环,其中哌嗪环在4位被取代基取代,所述取代基选自(a)6元芳族 具有0,1或2个氮原子的单环,并且单环中的其余原子为碳和(b)羟基-C 1 -C 6烷基,其中所述单环是未取代的或被选自以下的取代基取代:卤素, NH 2,-NO 2,-SO 2 NH 2,-SO 2 CH 3,乙酰基和氰基。