发明名称 Aminobenzophenones as inhibitors of IL-1beta and TNF-alpha
摘要 A compound of formula I, where: - R1 represents one or more, same or different substituents selected from halogen, hydroxy, mercpato, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3alkoxycarbonyl, cyano, carbamoyl, nitro and phenyl; - R2 represents one substituent in the ortho position being selected from halogen, hydroxy, mercapto, trufluoromethyl, amino, (C1-C3)alkyl, (C2-C3)alkoxycarbonyl, cyano, carbamoyl, nitro and phenyl; - R3 represents one or more, same or different substituents selected from the group consisting of hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C6)alkylmino, (c1-C3)alkoxycarbonyl, cyano, carbamoyl, phenyl and carboxy; - R4 represents hydrogen, (C1-C3)alkyl or allyl; - Q represents a bond, or C(R6)(R7)(-O-C=O)-, in which R6 and R7 independently represents hydrogen, trifluoromethyl, or (C1-C4)alkyl; - Y represents either (C5-C15)alkyl, (C2-C15)alkyl, (C2-C15)olefinic group, (C3-C10)monocyclic hydrocarbon, or phenyl, any of which may be optionally substituted with one or more, same or different substitutents represented by the formula R5; or (C1-C4)alkyl substituted with at least one or more substituents with the formula R5; - R5 represents halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-6)alkylamino, (C1-3)alkoxycarbonyl, cyano, azido, nitro, -COOH, -CONH2, CONHR', or CONR'R', where R' represents (C1-3)alkyl; and - X represents oxygen or sulphur. A compound formula I as described may be used in treatingastham, allergy, arthritis, gout, atherosclerosis, chronic inflammatory bowel disease, proliferative and inflammatory skin disorders, uvetis, septic shock, AIDS or osteoporosis. A compound of formula I may be used in combination with other drugs such as: Glucocorticosteroids, vitamin D analogues, anti-histamines, PAF antagonists, certain NSAIDs, gold slats, retinoids, cholesterol lowering agents, zinc salts, salazopyrin, methyl xanthines.
申请公布号 NZ516825(A) 申请公布日期 2004.05.28
申请号 NZ20000516825 申请日期 2000.07.11
申请人 LEO PHARMACEUTICAL PRODUCTS LTD 发明人 OTTOSEN, ERIK RYTTER;DANNACHER, HEINZ WILHELM
分类号 A61K45/08;A61K31/00;A61K31/136;A61K31/27;A61K45/06;A61P1/00;A61P7/00;A61P9/10;A61P11/06;A61P17/00;A61P17/02;A61P17/06;A61P19/02;A61P19/06;A61P19/10;A61P27/02;A61P29/00;A61P31/18;A61P37/02;A61P37/08;A61P43/00;C07C225/22;C07C271/28;C07C271/38;C07C271/58;(IPC1-7):C07C271/06 主分类号 A61K45/08
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