发明名称 AMINOBENZOPHENONES AS INHIBITORS OF IL-1.BETA. AND TNF-.ALPHA.
摘要 The present invention relates to compounds of formula (I) wherein R1, R2 and R3 independently represent 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-C3)alkoxycarbonyl, cyano, carbamoyl , or phenyl; R1 and R2 further represented by nitro and R3 by carboxy; R4 represents hydrogen, (C1-C3)alkyl, or allyl; Q represents a bond, or - C(R6)(R7)(-O-C=O)-, in which formula R6 and R7 independently represent hydrogen, trifluoromethyl, or (C1-C4)alkyl; Y represents either (C5-C15)alky l, (C2-C15)olefinic group, (C3-C10)monocyclic hydrocarbon, or phenyl, any of which may be optionally substituted with one or more, same or different substituents represented by the formula R5; or (C1-C4)alkyl substituted with at least one or more substituents with the formula R5; or Y represents a gro up of formula -CH2-(Z-O)n-Z where Z is a (C1-C3)alkyl, where n is a integer &gt ; 1 and no continuous linear sequence of atoms in the group Y > 15; R5 repres ents 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' stands for (C1-C3)alkyl; X represents oxygen or sulphur, or a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof. The compounds are valuable in the human and veterinary therapy.
申请公布号 CA2379286(A1) 申请公布日期 2001.01.25
申请号 CA20002379286 申请日期 2000.07.11
申请人 LEO PHARMACEUTICAL PRODUCTS LTD. A/S (LOVENS KEMISKE FABRIK PRODUKTIONSA KTI 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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