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    BENZOCYCLODECANE DERIVATIVES WITH ANTITUMOR ACTIVITY
    44.
    发明公开
    BENZOCYCLODECANE DERIVATIVES WITH ANTITUMOR ACTIVITY 审中-公开
    BENZOCYCLODECAN-DERIVATE MIT ANTITUMOR-EIGENS

    公开(公告)号：EP1458686A1

    公开(公告)日：2004-09-22

    申请号：EP02791850.7

    申请日：2002-12-18

    申请人： Pharmacia Italia S.p.A.

    发明人： DUCKI, Sylvie ,  MENICHINCHERI, Maria ,  MONGELLI, Nicola ,  VANOTTI, Ermes ,  ANGIOLINI, Mauro ,  CIOMEI, Marina

    IPC分类号： C07D233/54 ,  C07C69/013 ,  C07C69/616 ,  C07D277/30 ,  C07D263/32 ,  C07D213/55 ,  C07D405/12 ,  A61K31/44 ,  A61K31/42 ,  A61K31/425 ,  A61K31/415

    CPC分类号： C07D233/64 ,  C07C45/673 ,  C07C49/747 ,  C07C67/08 ,  C07C67/29 ,  C07C67/293 ,  C07C69/007 ,  C07C69/013 ,  C07C69/618 ,  C07C2602/12 ,  C07D213/56 ,  C07D263/32 ,  C07D277/30 ,  C07H15/203 ,  C07C69/16

    摘要： A compound which is a benzocyclodecane of the formula I wherein: ----- at positions 8-9 and 11-12 independently represents a single or double bond, -R1 is =O, or -OR7, R7 is H, C1-C7 alkanoyl, benzoyl, C1-C10 alkyl, C2-C10 alkenyl or COCH=CHR8, R8 is aryl or heterocyclyl;-R2 and -R3 are H, =O or -OR9, R9 is H, C1-C7 alkanoyl or benzoyl; when at position 11-12 there is a single bond, then -R4 represents=O, =CH2, =CHCOOR10, R10 is C1-C10 alkyl or aryl; =CH(OCH3), -OR9; -CH2OR11, R11 is H or a sugar residue, -COR12 , R12 is H, -OH or -OR10; or when at position 11-12 there is a double bond, then -R4 is -CH2OR11 or -COR12; - R5 and -R6 are H or, when at position 8-9 there is a single bond, taken together form a cyclopropane ring; R13 is H or 1-3 substituents selected from C1-C6 alkyl, C2-C6 alkenyl, phenyl, phenyl C1-C6 alkyl, halogen, hydroxy, C1-C6 alkoxy, aryloxy, cyano, nitro, amino, C1-C10 alkylamino, arylamino, C1-C7 alkanoylamino, aroylamino, hydroxycarbonyl, aminocarbonyl, C1-C6 alkylcarbonyl, C1-C6 alkylaminosulfonyl and arylaminosulfonyl group; with the provisos that if R1 and R4 =O, then one of R2, R3, R5, R6 and R13 is not H atom; or a pharmaceutically acceptable salt thereof. These benzocyclodecane derivatives are endowed with antitumor activity; a process and new intermediates for their preparation, the pharmaceutical compositions containing them, and their use in the prevention, control and treatment of cancer are also provided.

    摘要翻译： 作为式I的苯并环十一烷的化合物，其中： - 位置8-9和11-12独立地表示单键或双键，-R1 = O或-OR7，R7为H，C1- C7烷酰基，苯甲酰基，C1-C10烷基，C2-C10烯基或COCH = CHR8，R8是芳基或杂环基; -R2和-R3是H，= O或-OR9，R9是H，C1-C7烷酰基或苯甲酰基; 当在11-12位存在单键时，则-R4表示= O，= CH2，= CHCOOR10，R10为C1-C10烷基或芳基; = CH（OCH 3），-OR 9; -CH 2 OR 11，R 11为H或糖残基，-COR 12，R 12为H，-OH或-OR 10; 或当在11-12位存在双键时，则-R 4是-CH 2 OR 11或-COR 12; -R 5和-R 6是H或当位置8-9存在单键时，一起形成环丙烷环; R13是H或1-3个选自C1-C6烷基，C2-C6烯基，苯基，苯基C1-C6烷基，卤素，羟基，C1-C6烷氧基，芳氧基，氰基，硝基，氨基，C1-C10烷基氨基， 芳基氨基，C 1 -C 7烷酰基氨基，芳酰氨基，羟基羰基，氨基羰基，C 1 -C 6烷基羰基，C 1 -C 6烷基氨基磺酰基和芳基氨基磺酰基; 条件是如果R1和R4 = O，则R2，R3，R5，R6和R13之一不是H原子; 或其药学上可接受的盐。 这些苯并环十一烷衍生物具有抗肿瘤活性; 还提供了其制备方法和新的中间体，含有它们的药物组合物及其在预防，控制和治疗癌症中的用途。

    HETEROCYCLYL ANTHRACYCLINONE DERIVATIVES
    48.
    发明授权
    HETEROCYCLYL ANTHRACYCLINONE DERIVATIVES 有权
    杂环ANTHRACYCLINONDERIVATE

    公开(公告)号：EP1062212B1

    公开(公告)日：2004-05-12

    申请号：EP99915564.1

    申请日：1999-03-04

    申请人： Pharmacia Italia S.p.A.

    发明人： MANTEGANI, Sergio ,  TRAQUANDI, Gabriella ,  BANDIERA, Tiziano ,  LANSEN, Jacqueline ,  VARASI, Mario

    IPC分类号： C07D277/42 ,  C07D233/88 ,  A61K31/425 ,  A61K31/415

    CPC分类号： C07D417/04 ,  C07D233/88 ,  C07D277/40 ,  C07D277/42

    摘要： A compound of formula (1) wherein R1 is hydrogen, hydroxy, a group of formula OR5 wherein R5 is C1-C6 alkyl, C2-C6 alkenyl or C3-C8 cycloalkyl, halogen, amino which may be unsubstituted or mono or disubstituted by C1-C6 alkyl, C2-C6 alkenyl, aralkyl, acyl or trifluoroacetyl; R2 is hydrogen, hydroxy, a group NR6R7 wherein R6 and R7 independently represent hydrogen, an optionally substituted C1-C6 alkyl, C2-C6 alkenyl, C3-C8 cycloalkyl or, taken together with the nitrogen atom, represent an optionally substituted C3-C8 heterocyclic ring; R3 is hydrogen, hydroxy; R4 is a 2-substituted thiazolyl or imidazolyl system and the pharmaceutically acceptable salt thereof, is useful in the treatment of amyloidosis. Processes for the preparation and pharmaceutical compositions are also described.