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64 条记录 (耗时 0.016 秒)

    Terpenoidic derivatives useful as antitumor agents
    23.
    发明授权
    Terpenoidic derivatives useful as antitumor agents 失效
    用作抗肿瘤剂的萜类衍生物

    公开(公告)号：US5869514A

    公开(公告)日：1999-02-09

    申请号：US765436

    申请日：1997-01-15

    申请人： Carlo Battistini ,  Marina Ciomei ,  Francesco Pietra ,  Michele D'Ambrosio ,  Antonio Guerriero

    发明人： Carlo Battistini ,  Marina Ciomei ,  Francesco Pietra ,  Michele D'Ambrosio ,  Antonio Guerriero

    IPC分类号： C07D493/08 ,  A61K31/335 ,  A61K31/415 ,  A61K31/4178 ,  A61P35/00 ,  C07D233/64

    CPC分类号： A61K31/4178

    摘要： A method of treating tumors in a human or animal by administering thereto a pharmaceutically effective amount of a Sarcodictyin compound selected from Sarcodictyin A, B, C, D, E, and F. Sarcodictyin A has the formula (-)-(4R,4aR,7R,10S,11S,12aR,1Z,5E,8Z)-7,10-Epoxy3,4,4a,7,10,11,12,12a-octahydro-7-hydroxy-6-(methoxy-carbonyl)-1,10- dimethyl-4-(1-methylethyl)benzo cyclodecen-11-yl(E)-3-(1-Methyl-1H-imidazol-4-yl) acrylate (Sarcodictyin A).

    摘要翻译： PCT No.PCT / EP96 / 01688 Sec。 371日期1997年1月15日 102（e）日期1997年1月15日PCT 1996年4月23日PCT PCT。 出版物WO96 / 36335 日本1996年11月21日一种通过向其施用药学有效量的选自Sarcodictyin A，B，C，D，E和F的Sarcodictyin化合物来治疗人或动物肿瘤的方法。Sarcodictyin A具有式（ - ） - （4R，4aR，7R，10S，11S，12aR，1Z，5E，8Z）-7,10-环氧基3,4,4a，7,10,11,12,12a-八氢-7-羟基-6-（ 甲氧基羰基）-1,10-二甲基-4-（1-甲基乙基）苯并环十一碳烯-11-基（E）-3-（1-甲基-1H-咪唑-4-基）丙烯酸酯（Sarcodictyin A）。

    Substituted camptothecin derivatives and process for their preparation
    24.
    发明授权
    Substituted camptothecin derivatives and process for their preparation 失效

    公开(公告)号：US5856333A

    公开(公告)日：1999-01-05

    申请号：US776192

    申请日：1997-01-27

    申请人： Walter Cabri ,  Ilaria Candiani ,  Angelo Bedeschi ,  Franco Zarini ,  Sergio Penco

    发明人： Walter Cabri ,  Ilaria Candiani ,  Angelo Bedeschi ,  Franco Zarini ,  Sergio Penco

    IPC分类号： A61K31/435 ,  A61P35/00 ,  C07D491/22

    CPC分类号： C07D491/22

    摘要： The present invention relates to substituted camptothecin derivatives of formula (I) wherein the symbol - - - - represents a single or double bond; R.sub.1, R.sub.2 and R.sub.3 are as defined under (a) or (b) below: (a) R.sub.1 and R.sub.2 are, each independently, hydrogen; C.sub.1 -C.sub.4 alkyl; C.sub.3 -C.sub.7 cycloalkyl; phenyl C.sub.1 -C.sub.6 alkyl; an optionally substituted phenyl ring; --NR.sub.5 R.sub.6 wherein one of R.sub.5 and R.sub.6 is hydrogen, C.sub.1 -C.sub.6 alkyl or benzyl and the other is hydrogen, C.sub.1 -C.sub.6 alkanoyl, an optionally substituted C.sub.1 -C.sub.6 alkoxycarbonyl, an optionally substituted benzoyl, phenyl C.sub.1 -C.sub.6 alkanoyl, an optionally substituted C.sub.1 -C.sub.6 alkoxycarbonyl, an optionally substituted phenoxycarbonyl or phenyl C.sub.1 -C.sub.6 alkoxycarbonyl, or R.sub.5 and R.sub.6, combined together with the nitrogen atom to which they are linked, form a 4-7 membered saturated, optionally substituted, heteromonocyclic ring residue; COOR.sub.8 wherein R.sub.8 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl or phenyl C.sub.1 -C.sub.6 alkyl; or COR.sub.9 wherein Rg is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, phenyl C.sub.1 -C.sub.6 alkyl, an optionally substituted phenyl ring or NR.sub.10 R.sub.11 wherein R.sub.10 and R.sub.11 are, each independently, hydrogen or C.sub.1 -C.sub.6 alkyl; and R.sub.3 is hydrogen, C.sub.1 -C.sub.6 alkyl or an optionally substituted phenyl ring; or (b) R.sub.1 and R.sub.3, combined together, form a 5-8 membered, optionally substituted, carbomonocyclic ring, and R.sub.2 is hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.3 -C.sub.7 cycloalkyl; R.sub.4 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl or phenyl C.sub.1 -C.sub.6 alkyl; X is hydrogen,C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.3 -C.sub.7 cycloalkoxy, C.sub.1 -C.sub.6 alkanoyloxy, benzoyloxy, amino, hydroxy, nitro, halogen or it is a methylenedioxy group linked to the positions 10 and 11 of the molecule, and the pharmaceutically acceptable salts thereof. The compounds according to the invention are useful in therapy as antitumor agents. ##STR1##

    Distamycin derivatives, process for preparing them, and their use as antitumor and antiviral agents
    28.
    发明授权
    Distamycin derivatives, process for preparing them, and their use as antitumor and antiviral agents 失效
    雷帕霉素衍生物，其制备方法及其作为抗肿瘤剂和抗病毒剂的用途

    公开(公告)号：US6165980A

    公开(公告)日：2000-12-26

    申请号：US101758

    申请日：1998-07-17

    申请人： Paolo Cozzi ,  Italo Beria ,  Marina Caldarelli ,  Maria Cristina Geroni ,  Enrico Pesenti

    发明人： Paolo Cozzi ,  Italo Beria ,  Marina Caldarelli ,  Maria Cristina Geroni ,  Enrico Pesenti

    IPC分类号： A61K31/00 ,  A61K31/40 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4178 ,  A61K31/505 ,  A61K31/506 ,  A61P31/00 ,  A61P31/12 ,  A61P35/00 ,  C07D207/34 ,  C07D403/14 ,  H04R3/00 ,  H04R7/06 ,  A61K38/00

    CPC分类号： C07D403/14 ,  C07D207/34

    摘要： A distamycin derivative of formula (I): ##STR1## wherein: n is 2, 3 or 4;R.sub.0 is C.sub.1 -C.sub.4 alkyl or --CH.sub.2 CH.sub.2 --X.sub.2, wherein X.sub.2 is a halogen atom;R.sub.1 and R.sub.2 are selected, each independently, from: hydrogen, C.sub.1 -C.sub.4 alkyl optionally substituted by one or more fluorine atoms, C.sub.1 -C.sub.4 alkoxy, and halogen;X.sub.1 is a halogen atom;B is selected from: ##STR2## wherein R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, and R.sub.9 are, each independently, hydrogen or C.sub.1 -C.sub.4 alkyl, and m is 0, 1 or 2; with the proviso that, when R.sub.0 is --CH.sub.2 CH.sub.2 --X.sub.2, B is different from --(CH.sub.2).sub.m --NR.sub.6 R.sub.7 and at least one of R.sub.3, R.sub.4, and R.sub.5 is C.sub.1 -C.sub.4 alkyl;or a pharmaceutically acceptable salt thereof.

    摘要翻译： PCT No.PCT / EP97 / 00369 Sec。 371日期：1998年7月17日 102（e）日期1998年7月17日PCT 1997年1月22日PCT PCT。 公开号WO97 / 28123 日期：1997年8月7日一种式（I）的分心霉素衍生物：其中：n为2,3或4; R 0是C 1 -C 4烷基或-CH 2 CH 2 -X 2，其中X 2是卤素原子; R 1和R 2各自独立地选自氢，任选被一个或多个氟原子取代的C 1 -C 4烷基，C 1 -C 4烷氧基和卤素; X1是卤原子; B选自：其中R 3，R 4，R 5，R 6，R 7，R 8和R 9各自独立地为氢或C 1 -C 4烷基，m为0,1或2; 条件是当R 0是-CH 2 CH 2 -X 2时，B不同于 - （CH 2）m -NR 6 R 7，且R 3，R 4和R 5中的至少一个是C 1 -C 4烷基; 或其药学上可接受的盐。

    Phenylsubstituted 4-azasteroid fluoroderivatives
    30.
    发明授权
    Phenylsubstituted 4-azasteroid fluoroderivatives 失效
    苯基取代的4-azasteroid氟代衍生物

    公开(公告)号：US6114345A

    公开(公告)日：2000-09-05

    申请号：US300454

    申请日：1999-04-28

    申请人： Achille Panzeri ,  Marcella Nesi ,  Enrico Di Salle

    发明人： Achille Panzeri ,  Marcella Nesi ,  Enrico Di Salle

    IPC分类号： A61K31/58 ,  A61P43/00 ,  C07J73/00

    CPC分类号： C07J73/005

    摘要： Compounds of formula (I), wherein: the symbol ---- represents a single or a double bond; R is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group; R.sub.f and R'.sub.f, each independently, are C.sub.1 -C.sub.4 alkyl groups substituted by one or more fluorine atoms; and R.sub.1 and R.sub.2, each independently, are selected from: a hydrogen atom; a phenyl group; a C.sub.1 -C.sub.4 alkyl group unsubstituted or substituted by one or more fluorine atoms; a halogen atom; a cyano (CN) group; a group OR.sub.4, wherein R.sub.4 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group; a group SR.sub.5, wherein R.sub.5 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group; and a group COR.sub.6, wherein R.sub.6 is a group OR.sub.4 in which R.sub.4 is as defined above or a C.sub.1 -C.sub.4 alkyl group unsubstituted or substituted by one or more fluorine atoms. They are useful as testosterone 5a-reductase inhibitors.

    摘要翻译： 式（I）的化合物，其中：符号+ E，uns ---- + EE表示单键或双键; R是氢原子或C 1 -C 4烷基; Rf和R'f各自独立地是被一个或多个氟原子取代的C 1 -C 4烷基; 并且R 1和R 2各自独立地选自：氢原子; 苯基; 未被取代或被一个或多个氟原子取代的C 1 -C 4烷基; 卤素原子; 氰基（CN）基团; OR 4，其中R 4是氢原子或C 1 -C 4烷基; 基团SR5，其中R5是氢原子或C1-C4烷基; 和基团COR6，其中R6是其中R4如上定义的基团OR4或未被取代或被一个或多个氟原子取代的C 1 -C 4烷基。 它们可用作睾酮5a还原酶抑制剂。