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    Polymer-bound camptothecin derivatives
    4.
    发明授权
    Polymer-bound camptothecin derivatives 失效
    聚合物键合的喜树碱衍生物

    公开(公告)号：US5773522A

    公开(公告)日：1998-06-30

    申请号：US448330

    申请日：1995-06-08

    申请人： Francesco Angelucci ,  Antonino Suarato

    发明人： Francesco Angelucci ,  Antonino Suarato

    IPC分类号： A61K47/48 ,  C08F220/36 ,  C08F220/56 ,  C08F220/60 ,  C08F20/56 ,  A01N43/42 ,  C08F120/56

    CPC分类号： A61K47/48176 ,  A61K47/4823 ,  A61K47/48338

    摘要： A polymeric conjugate consists essentially of: (i) from 60 to 99 mol % of N-(2-hydroxypropyl) methacryloylamide units represented by formula 1: ##STR1## (ii) from 1 to 40 mol % of 20-0-(N-methacryloylglycyl-aminoacyl) camptothecin units represented by formula 2 ##STR2## wherein �A! is a spacer group having respective terminal amino and carbonyl groups which are separated by at least three atoms and O-CPT represents a residue of a camptothecin, the C-20 hydroxy group of the camptothecin being linked to the terminal carbonyl group of the spacer group �A!; and (iii) from 0 to 10 mol % of N-methacryloylglycine or N-(2-hydroxy-propyl)methacryloylglycinamide units represented by formula 3: ##STR3## wherein Z represents hydroxy or a residue of formula --NH--CH.sub.2 --CH(OH)--CH.sub.3.

    摘要翻译： PCT No.PCT / EP94 / 03154 Sec。 371日期：1995年6月8日 102（e）日期1995年6月8日PCT 1994年9月21日PCT公布。 公开号WO95 / 10304 日期1995年04月20日一种聚合共轭物基本上由以下组成：（i）60至99mol％由式1表示的N-（2-羟丙基）甲基丙烯酰胺单元：乙酰丙酰基甘氨酰 - 氨酰基）喜树碱单元由式2 其中[A]是具有分别具有至少三个原子的末端氨基和羰基的间隔基，O-CPT表示喜树碱的残基，喜树碱的C 20羟基与末端羰基连接 的间隔基[A]; 和（iii）0至10摩尔％的由式3表示的N-甲基丙烯酰基甘氨酸或N-（2-羟基 - 丙基）甲基丙烯酰基甘氨酰胺单元：其中Z表示羟基或式-NH-CH2-CH （OH）-CH 3。

    Thiohydrazoazetidinones
    6.
    发明授权
    Thiohydrazoazetidinones 失效
    THIOHYDRAZOAZETIDINONES

    公开(公告)号：US4143037A

    公开(公告)日：1979-03-06

    申请号：US797608

    申请日：1977-05-16

    申请人： Maurizio Foglio ,  Giovanni Franceschi ,  Paolo Masi ,  Antonino Suarato

    发明人： Maurizio Foglio ,  Giovanni Franceschi ,  Paolo Masi ,  Antonino Suarato

    IPC分类号： C07D205/095 ,  C07D205/08

    CPC分类号： C07D205/095

    摘要： A process is disclosed for preparing compounds of structure: ##STR1## where R.sup.1 is hydroxyl, alkoxy with 1 to 4 carbon atoms, trichloroethoxy, benzyloxy, p-methoxybenzyloxy, p-nitrobenzyloxy, benzhydryloxy, triphenylmethoxy, phenacyloxy, or p-halophenacyloxy;Z is hydrogen, hydroxyl, --O-alkyl, --O--CO-alkyl, --Br, --I, --N.sub.3, --O--CO--CH.sub.3, O--CO--NH.sub.2, or an S-mononuclear heterocyclic ring,Starting from ##STR2## where R is hydrogen, alkyl having from 1 to 4 carbon atoms, cyano-methyl, thienyl-methyl, furyl-methyl, naphthyl-methyl, phenyl-methyl, phenoxy-methyl, phenyl-isopropyl, phenoxy-isopropyl, pyridyl-4-thiomethyl, or tetrazolyl-1-methyl;R.sup.2 and R.sup.3 are lower alkyl, a mononuclear aryl ring, CN, a mononuclear heterocyclic ring or the radicals --COR.sup.4, --COOR.sup.4, ##STR3## --CONHR.sup.4, or R.sub.2 and R.sub.3 together represent ##STR4## where T represents ##STR5## and R.sup.4 is a lower alkyl, a mononuclear aryl or heterocyclic ring, WHEREIN THE COMPOUND (II') is reacted with a phosphorous halide in the presence of a tertiary amine, the corresponding imino chloride is reacted with a lower aliphatic alcohol, the iminoether so formed is hydrolyzed in an acid medium, and the resultant 3-amino-2-.beta.-thiohydrazoazetidinone: ##STR6## in which R.sup.1, R.sup.2, R.sup.3 and Z have the meanings given heretofore,Is reacted between -100.degree. and +120.degree. C. with inorganic basic or weakly acid oxides or inorganic and organic bases, to give (V).

    Amino anthracyclinone derivatives and their use in the treatment of amyloidosis
    7.
    发明授权
    Amino anthracyclinone derivatives and their use in the treatment of amyloidosis 失效
    氨基蒽环类衍生物及其在治疗淀粉样变性中的应用

    公开(公告)号：US06268362B1

    公开(公告)日：2001-07-31

    申请号：US09622921

    申请日：2000-09-07

    申请人： Tiziano Bandiera ,  Daniele Fancelli ,  Mario Varasi ,  Michele Caruso ,  Jacqueline Lansen ,  Antonino Suarato

    发明人： Tiziano Bandiera ,  Daniele Fancelli ,  Mario Varasi ,  Michele Caruso ,  Jacqueline Lansen ,  Antonino Suarato

    IPC分类号： A61K315377

    CPC分类号： C07D405/06 ,  C07D211/70

    摘要： A compound of formula (1), wherein R1 represents hydrogen, hydroxy, a group of formula OR7, wherein R7 is C1-C6 alkyl, C2-C6 alkenyl; R2 represents hydrogen, hydroxy, diethylamino, piperidino, tetrahydropyridino or morpholino, and either R3, taken alone, represtnts hydrogen or hydroxy, and R4 and R5, taken alone, independently represent hydrogen, hydroxy or, taken together with the carbon atom, represent a carbonyl group; or R3 and R4, taken together, represent a group of formula (A), wherein R8 and R9 represent a C1-C6 alkyl and R5 represents hydrogen; R6 represents hydrogen or a phenyl group, optionally substituted by methyl, methoxy or halogen and the pharnaceutically acceptable salt thereof, is useful in the treatment of amyloidosis. Processes for the preparation and pharmaceutical compositions are also described.

    摘要翻译： 式（1）的化合物，其中R 1表示氢，羟基，式OR 7的基团，其中R 7是C 1 -C 6烷基，C 2 -C 6烯基; R2代表氢，羟基，二乙基氨基，哌啶子基，四氢吡啶基或吗啉代，独立的R 3独立地代表氢或羟基，独立地，R 4和R 5独立地表示氢，羟基或与碳原子一起代表 羰基; 或R 3和R 4一起表示式（A）的基团，其中R 8和R 9表示C 1 -C 6烷基，R 5表示氢; R6代表氢或任选被甲基，甲氧基或卤素取代的苯基及其药物上可接受的盐，可用于治疗淀粉样变性。 还描述了制备方法和药物组合物。