发明名称 N-ARYL AND N-HETEROARYL-1,2-DIAMINOCYCLOBUTENE-3,4-DIONES WITH SMOOTH MUSCLE RELAXING ACTIVITIES
摘要 The compounds of formula (I), wherein R1 is hydrogen, C1-10 straight or branched chain alkyl, C3-10 cyclic or bicyclic alkyl, alkanoyl of 2 to 7 carbon atoms, alkylsulfonyl of 1 to 7 carbon atoms, aroyl of 7 to 12 carbon atoms, arylalkenoyl of 9 to 20 carbon atoms, arylsulfonyl of 6 to 12 carbon atoms, arylalkanoyl of 8 to 12 carbon atoms or arylalkylsulfonyl of 7 to 12 carbon atoms; R2 is hydrogen, C1-10 straight or branched chain alkyl or C3-10 cyclic or bicyclic alkyl; A is a group of formula (II), wherein R7 and R8, independent from each other, are selected from the following: cyano, nitro, amino, C1-6 alkyl, C1-6 perfluoroalkyl, C1-6 alkoxy, C1-6 perfluoroalkoxy, amino, C1-12 mono- or dialkylamino, sulfonamide, C1-6 alkylsulfonamido, C6-12 arylsulfonamido, C2-6 alkylcarboxamido, C7-12 arylcarboxamido, C1-6 alkylsulfonyl, C1-6 perfluoroalkylsulfonyl, C6-12 arylsulfonyl, chloro, bromo, fluoro, iodo, 1-imidazolyl, carboxyl, carboalkoxy of 2 to 7 carbon atoms, hydroxyl or hydrogen; or A is Het where Het is selected from (a), (b), (c), (d), (e), (f), (g), (h), (i), (j), (k), (l), (m), (n), (o), (p), wherein R9 is hydrogen, C1-6 alkyl, C1-6 perfluoroalkyl, C1-6 alkoxy, C1-6 perfluoroalkoxy, amino, C1-12 mono- or dialkylamino, C1-6 alkylsulfonamido, C2-6 alkylcarboxamido, nitro, cyano, carboxyl, chloro, bromo, fluoro, iodo; n is an integer from 0 to 6; R3 and R4 are, independent from each other, hydrogen, C1-10 straight or branched chain alkyl, or C3-10 cyclic or bicyclic alkyl; C1-10 perfluoro alkyl, C1-10 hydroxyalkyl, C2-10 alkoxyalkyl, fluoro; or, when taken together, form a spirocyclic ring containing a total of 3-7 carbon atoms; R5 and R6, independent from each other, are selected from the following: cyano, nitro, amino, C1-6 alkyl, C1-6 perfluoroalkyl, C1-6 alkoxy, C1-6 perfluoroalkoxy, amino, C1-12 mono- or dialkylamino, sulfonamide, C1-6 alkylsulfonamido, C6-12 arylsulfonamido, C2-6 alkylcarboxamido, C7-12 arylcarboxamido, C1-6 alkylsulfonyl, C1-6 perfluoroalkylsulfonyl, C6-12 arylsulfonyl, chloro, bromo, fluoro, iodo, 1-imidazolyl, carboxyl, C2-7 carboalkoxy, hydroxyl, or hydrogen; or a pharmaceutically acceptable salt thereof.
申请公布号 WO9614300(A1) 申请公布日期 1996.05.17
申请号 WO1995US14597 申请日期 1995.10.25
申请人 AMERICAN HOME PRODUCTS CORPORATION 发明人 BUTERA, JOHN, ANTHONY;ANTANE, SCHUYLER, ADAM;HIRTH, BRADFORD, HAMMOND
分类号 C07D239/42;A61K31/135;A61K31/275;A61K31/415;A61K31/4184;A61K31/44;A61K31/4406;A61K31/4409;A61K31/47;A61K31/472;A61P13/02;A61P15/00;A61P43/00;C07C225/20;C07C255/58;C07C255/60;C07D213/38;C07D213/75;C07D215/38;C07D217/02;C07D231/56;C07D235/04 主分类号 C07D239/42
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