专利号:WO-2004087679-A1 优先权日:2003-04-01 标 题 :2, 4, 6-trisubstituted pyrimidine derivatives useful for the treatment of neoplastic and autoimmune diseases 发明人:OBRECHT DANIEL; ERMERT PHILIPP; LUTHER ANATOL; EBERLE MARTIN; BACHMANN FELIX 权利人:APONETICS AG; OBRECHT DANIEL; ERMERT PHILIPP; LUTHER ANATOL; EBERLE MARTIN; BACHMANN FELIX 摘要:The invention relates to substituted pyrimidines of formula (I) wherein V represents a bond or CR6R7, W represents a bond, NR8 or oxygen, X represents sulfur, or nitrogen substituted by hydrogen or R5, Y represents -CH2-, -CH2CH2-, -CO- or -CS-, R1 represents unsubstituted or substituted aryl or heteroaryl, and the substituents R2, R3, R4, R5, R6, R7 and R8 have the meanings given in the specification. These compounds are selectively inducing apoptosis in cancer cells and can be used for the treatment of neoplastic and autoimmune diseases. The invention relates also to methods of synthesis of such compounds, to their use as medicaments, to pharmaceutical compositions containing same, and to methods of treatment of neoplastic and autoimmune diseases using such compounds of formula (I) or of pharmaceutical compositions containing same.
专利号:US-3823164-A 优先权日:1971-08-26 标 题 :5,6,7,8-tetrahydro-2,5(and 4,5)-dioxo-1-benzopyrans 发明人:SELLSTEDT J; BELL S; MC CAULLY R 权利人:AMERICAN HOME PROD 摘要:COMPOUNDS OF THE FORMULA: 2,3-(-X-O-),R,R2-CYCLOHEX-2-EN-1-ONE IN WHICH X IS THE MOIETY -CO-C(-R3)=C(-CO-Z)- Z IS A MEMBER SELECTED FOR THE GROUP CONSISTING OF -OR4, -N(-R5)-R6 -CL,-BR, AND -OM; R, R2, R3, AND R5 ARE INDEPENDENTLY SELECTED FROM THE GROUP CONSISTING OF -H, LOWER ALKYL, PHENYL AND BENZYL, R6 IS SELECTED FROM THE GEOUP CONSISTING OF -H, LOWER ALKYL, PHEMYL, BENZYL, LOWER DIALKYLAMINOALKYL AND CYCLOALKYL OF 3 TO 10 CARBON ATOMS, AND WHEN TAKEN WITH R5 AND THE NITROGEN ATOM TO WHICH THEY ARE BONDED FORMS THE MORPHOLINO, PIPERIDINO AND PIPERAZINO GROUPS, AND M IS SELECTED FROM ALKALI METAL CATION AND -NH4, ARE IMMUNO-INFLAMMATORY AGENTS POSSESSING ANTIALLERGIC AND ANTIINFLAMMATORY ACTIVITY. THE COMPOUNDS OF THSI INVENTION ARE ALSO INTERMEDIATES FOR THE SYNTHESIS OF KNOWN CHROMONE AND COUMARIN DERIVATIVES.