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    • 10. 发明公开
    • AMINOBENZOPHENONES AS INHIBITORS OF IL-1BETA AND TNF-ALPHA
    • 作为IL-1BETA和TNF-α的抑制剂的氨基苯并EN酮
    • EP1210320A1
    • 2002-06-05
    • EP00943699.9
    • 2000-07-11
    • LEO PHARMACEUTICAL PRODUCTS LTD. A/S(LOVENS KEMISKE FABRIK PRODUKTIONSAKTIESELSKAB)
    • OTTOSEN, Erik, Rytter
    • C07C235/04C07C237/04C07C229/18A61K31/165A61K31/222
    • C07C225/22C07C229/18C07C233/43C07C235/10C07C235/72C07C235/74C07C237/20
    • The present invention relates to a compound of general formula (I) wherein R1, R2, and R3 represents one or more, same or different substituents selected from the group consisting of halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, -CONH2, phenyl, or nitro; further R2 can be hydrogen, and R3 can be carboxy and carbamoyl; R4 represents hydrogen, (C1-C3)alkyl, or allyl; X represents oxygen or sulphur; Q represents -(CO)-, -(CS)-, or a bond; Y represents (C5-C15)alkyl; (C2-C15)olefinic group; (C3-C10)monocyclic hydrocarbon group; or phenyl; any of which may be optionally substituted by one or more, same or different substituents selected from the group consisting of the formula R5 defined below; (C1-C4)alkyl substituted by one or more substituents selected for the group R5; or a group of the formula -(Z-O)n-Z, wherein Z is a (C1-C3)alkyl, n is an integer > 1; and no continuous linear sequence of atoms in the group Y exceeds 15; R5 represents halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, azido, nitro, -COOH, -CONH2, -CONHR', or COONR'R' wherein R' represents (C1-C3)alkyl; or a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof. The compounds are valuable in the human and veterinary therapy.
    • 本发明涉及通式(I)的化合物,其中R 1,R 2和R 3表示一个或多个相同或不同的选自卤素,羟基,巯基,三氟甲基,氨基,(C 1 -C 3) (C 1 -C 3)烷氧基,(C 1 -C 3)烷硫基,(C 1 -C 6)烷基氨基,(C 1 -C 3)烷氧基羰基,氰基,-CONH 2,苯基或硝基; 另外的R 2可以是氢,并且R 3可以是羧基和氨基甲酰基; R4代表氢,(C1-C3)烷基或烯丙基; X代表氧或硫; Q表示 - (CO) - , - (CS) - 或键; Y代表(C5-C15)烷基; (C2-C15)烯基; (C3-C10)单环烃基; 或苯基; 它们中的任何一个可以任选地被一个或多个,选自由以下定义的式R5组成的组中的相同或不同的取代基取代; (C 1 -C 4)烷基被一个或多个选自基团R 5的取代基取代; 或式 - (Z-O)n-Z的基团,其中Z是(C1-C3)烷基,n是> 1的整数; 并且Y组中没有连续的线性原子序列超过15; (C1-C3)烷氧基,(C1-C3)烷硫基,(C1-C6)烷基氨基,(C1-C3)烷氧基羰基,氰基,叠氮基,硝基,-COOH, - CONH 2,-CONHR'或COONR'R',其中R'表示(C 1 -C 3)烷基; 或其药学上可接受的盐,或其水合物或溶剂合物。 这些化合物在人类和兽医疗法中是有价值的。