发明名称 Anthracyclinone derivatives and their use in treating amyloidosis
摘要 Use in the manufacture of a medicament for use in the treatment of amyloidosis of an anthracyclinone of formula A wherein, R1 represents hydrogen or hydroxy, or a group of formula OR6 in which R6 is C1-C6 alkyl, C5-C6 cycloalkyl or CH2Ph with the phenyl (Ph) ring optionally substituted by 1, 2 or 3 substituents selected from F, Cl, Br, C1-C6 alkyl, C1-C6 alkoxy and CF3, or a group of formula OSO2R7 in which R7 is C1-C6 alkyl or Ph optionally substituted by 1, 2 or 3 substituents selected from halogen and C1-C6 alkyl, R2 represents hydrogen, hydroxy, or OR6, COOH or COOR6 wherein R6 is as above defined, R3 represents hydrogen, hydroxy, or OR6 as above defined, R4 represents hydrogen, methyl or a group of formula XCH2R8 in which X is CO, CH2, CHOH or a group of formula i or ii, in which m is 2 or 3, R8 is hydrogen or hydroxy or a group of formula NR9R10 in which, R9 and R10 are each independently selected from, (a) hydrogen, (b) a C1-C6 alkyl or C2-C6 alkenyl group optionally substituted with hydroxy, CN, COR11, COOR11, CONR11R12, O(CH2)nNR11R12 (n is 2 to 4) or NR11R12 in which R11 and R12 are each independently selected from hydrogen, a C1-C12 alkyl or C2-C12 alkenyl group or phenyl optionally substituted by one or more substituents selected from C1-C6 alkyl, C1-C6 alkoxy, F, Br, Cl, CF3, OH, NH2 or CN, (c) C3-C6 cycloalkyl optionally substituted with COR11, COOR11 or OH wherein R11 is as above defined, (d) phenyl (C1-C4 alkyl or C2-C4 alkenyl) optionally substituted on the phenyl ring by one or more substituents selected from C1-C6 alkyl, C1-C6 alkoxy, F, Br, Cl, CF3, OH, NH2 or CN, or (e) COR11, COOR11, CONR11R12, COCH2NR11R12, CONR11COOR12 or SO2R12 in which R11 and R12 are as above defined, or R9 and R10 together with the nitrogen atom to which they are attached form, (f) a morpholino ring optionally substituted with C1-C4 alkyl or C1-C4 alkoxy, (g) a piperazino ring optionally substituted by C1-C6 alkyl, C2-C6 alkenyl or phenyl optionally substituted by one or more substituents selected from C1-C6 alkyl, C1-C6 alkoxy, F, Br, Cl, CF3, OH, NH2 or CN, or (h) a pyrrolidino, piperidino or tetrahydropyridino ring optionally substituted by OH, NH2, COOH, COOR11 or CONR11R12 wherein R11 and R12 are as above defined, C1-C6 alkyl, C2-C6 alkenyl or phenyl optionally substituted by one of more substituents selected from C1-C6 alkyl, C1-C6 alkoxy, F, Br, Cl, CF3, OH, NH2 or CN, a group of formula OR6 or SR6 in which R6 is as above defined, a group of formula OPh wherein the phenyl (Ph) ring is optionally substituted by nitro, amino or NR9R10 as above defined, a group of formula B, wherein R13 represents hydrogen, COR11 wherein R11 is as above defined, or a peptidyl residue and R14 is halogen or a group of formula OSO2R7 wherein R7 is as above defined, or a group of formula C or D, wherein E is a group or formula COOR11 or CONR9R10 in which R9, R10 and R11 are as above defined, and R5 represents hydrogen, hydroxy a group of formula OR6 or NR9R10 wherein R6, R9 and R10 are as above defined, or a group of formula F, wherein R6, R9 and R10 are as above defined and p is from 1 to 6, or a pharmaceutically acceptable salt thereof.
申请公布号 NZ291157(A) 申请公布日期 2001.03.30
申请号 NZ19950291157 申请日期 1995.07.24
申请人 PHARMACIA & UPJOHN S 发明人 SUARATO, ANTONINO;LANSEN, JACQUELINE;CARUSO, MICHELLE;BALLINARI, DARIO;BANDIERA, TIZIANO
分类号 C07D309/10;A61K31/12;A61K31/122;A61K31/135;A61K31/165;A61K31/35;A61K31/351;A61K31/445;A61K31/495;A61K31/535;A61K31/5375;A61K31/65;A61P3/00;A61P25/00;A61P25/28;C07C46/00;C07C50/36;C07C50/38;C07C66/00;C07C225/32;C07C225/34;C07C225/36;C07C233/31;C07C233/36;C07C309/65;C07C309/73;C07D295/108;C07D295/112;C07D317/26;(IPC1-7):A61K31/535;C07D295/10 主分类号 C07D309/10
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