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    Cyclopropyl analogs as estrogenic and anti-fertility agents
    7.
    发明授权
    Cyclopropyl analogs as estrogenic and anti-fertility agents 失效
    环丙基类似物作为雌激素和抗生育剂

    公开(公告)号：US4442119A

    公开(公告)日：1984-04-10

    申请号：US402112

    申请日：1982-07-26

    申请人： Robert A. Magarian ,  Joseph T. Pento

    发明人： Robert A. Magarian ,  Joseph T. Pento

    IPC分类号： C07C13/28 ,  C07C23/18 ,  C07C39/15 ,  C07C43/21 ,  C07C43/225 ,  A01N43/36 ,  A01N29/04 ,  A61K31/40

    CPC分类号： C07C43/225 ,  C07C13/28 ,  C07C23/18 ,  C07C39/15 ,  C07C43/21 ,  Y10S514/843

    摘要： Estrogenic cyclopropyl analogs, when administered to a female subject, function as anti-fertility agents to prevent pregnancy in the subject. Further, the estrogenic cyclopropyl analogs may be used as estrogenic agents to produce an estrogenic response in a female subject. The estrogenic cyclopropyl analogs useful as estrogenic agents have the general structure: ##STR1## wherein: X is a halogen or hydrogen atom:R.sub.1 is a hydrogen atom, an alkyl group containing from 1 to about 3 carbon atoms, a monocyclic group, a hydroxy substituted monocyclic group, or an alkoxy substituted monocyclic group in which the alkyl substitutent contains from 1 to about 3 carbon atoms;R.sub.2 is a hydrogen atom, an acetate group, a hydroxyl group, an alkoxy group in which the alkyl substituent contains from 1 to about 3 carbon atoms, a beta-dialkylaminoethoxy group in which the alkyl substituent contains from 1 to about 3 carbon atoms, a beta-monoaminoheterocycloethoxy group, or pharmaceutically acceptable salts thereof;R.sub.3 is a hydrogen atom, or an alkyl group containing from 1 to about 3 carbon atoms;R.sub.4 is a hydrogen atom, an acetate group, a hydroxyl group, or an alkoxy group in which the alkyl substituent contains from 1 to about 3 carbon atoms.

    摘要翻译： 当向女性受试者施用时，雌激素环丙基类似物用作抗生育剂以预防受试者的怀孕。 此外，雌激素环丙烯类似物可以用作雌激素剂，以在女性受试者中产生雌激素反应。 可用作雌激素剂的雌激素环丙基类似物具有以下通用结构：其中：X为卤素或氢原子：R1为氢原子，含有1至约3个碳原子的烷基，单环基团，羟基 取代的单环基团或烷基取代基含有1至约3个碳原子的烷氧基取代的单环基团; R2是氢原子，乙酸酯基，羟基，烷基取代基含有1至约3个碳原子的烷氧基，其中烷基取代基含有1至约3个碳原子的β-二烷基氨基乙氧基， β-单氨基杂环基乙氧基，或其药学上可接受的盐; R3是氢原子或含有1至约3个碳原子的烷基; R4是烷基取代基含有1〜约3个碳原子的氢原子，乙酸酯基，羟基或烷氧基。

    Gem-dichlorocyclopropanes as antitumor agents
    8.
    发明授权
    Gem-dichlorocyclopropanes as antitumor agents 失效
    宝石二氯环丙烷作为抗肿瘤剂

    公开(公告)号：US5663207A

    公开(公告)日：1997-09-02

    申请号：US376961

    申请日：1995-01-20

    申请人： Robert A. Magarian ,  Joseph T. Pento ,  May T. Griffin

    发明人： Robert A. Magarian ,  Joseph T. Pento ,  May T. Griffin

    IPC分类号： A61K31/03 ,  C07C217/18 ,  C07C309/66 ,  C07D295/092 ,  A61K31/045

    CPC分类号： C07D295/088 ,  A61K31/03 ,  C07C217/18 ,  C07C309/66 ,  C07C2101/02

    摘要： Gem-Dichlorocyclopropanes (Analog II derivatives) which demonstrate antiproliferative activity toward MCF-7 cells, in vitro and are generally not reversed by estradiol or having intrinsic estrogenicity (except the hydroxyphenyl derivative Compound 30). In general the cyclopropane compounds have the formula: ##STR1## or any pharmaceutically acceptable salt thereof. X is selected from a group consisting of hydrogen and halogen atoms. The group R.sub.1 may he a hydrogen atom, an alkyl group, an acyl group, or an arylalkyl group. The group R.sub.2 may be a hydrogen atom, an unsubstituted aryl group or a substituted aryl group. The group R.sub.3 may be a hydrogen atom, an alkyl group, a cycloalkyl group, a substituted aryl group or an unsubstituted aryl group. The group R.sub.4 may be a hydrogen atom, an unsubstituted aryl group or a substituted aryl group. The R.sub.4 is absent when R.sub.3 is a cycloalkyl group having a first position carbon and a terminal position carbon bonded to the same carbon of the cyclopropane. Further, no more than any two of R.sub.2, R.sub.3 and R.sub.4 has an aryl group.

    摘要翻译： 在体外表现出对MCF-7细胞的抗增殖活性的Gem-二氯环丙烷（模拟II衍生物），通常不被雌二醇逆转或具有固有的雌激素（除了羟基苯基衍生物化合物30）。 一般来说，环丙烷化合物具有下式：其中R 1代表氢或其任何药学上可接受的盐。 X选自氢和卤素原子。 R1基可以是氢原子，烷基，酰基或芳基烷基。 基团R2可以是氢原子，未取代的芳基或取代的芳基。 基团R3可以是氢原子，烷基，环烷基，取代的芳基或未取代的芳基。 基团R4可以是氢原子，未取代的芳基或取代的芳基。 当R3是具有与环丙烷的相同碳键合的第一位置碳和末端位置碳的环烷基时，R4不存在。 此外，R 2，R 3和R 4中不超过2个具有芳基。

    Gem-dichlorocyclopropanes as antitumor agents
    9.
    发明授权
    Gem-dichlorocyclopropanes as antitumor agents 失效
    宝石二氯环丙烷作为抗肿瘤剂

    公开(公告)号：US5397802A

    公开(公告)日：1995-03-14

    申请号：US20922

    申请日：1993-02-22

    申请人： Robert A. Magarian ,  Joseph T. Pento ,  May T. Griffin

    发明人： Robert A. Magarian ,  Joseph T. Pento ,  May T. Griffin

    IPC分类号： A61K31/03 ,  C07C217/18 ,  C07C309/66 ,  C07D295/092 ,  A01N37/02

    CPC分类号： C07D295/088 ,  A61K31/03 ,  C07C217/18 ,  C07C309/66 ,  C07C2101/02

    摘要： Gem-Dichlorocyclopropanes (Analog II derivatives) which demonstrate antiproliferative activity toward MCF-7 cells, in vitro and are generally not reversed by estradiol or having intrinsic estrogenicity (except the hydroxyphenyl derivative Compound 30). In general the cyclopropane compounds have the formula: ##STR1## or any pharmaceutically acceptable salt thereof. X is selected from a group consisting of hydrogen and halogen atoms. The group R.sub.1 may be a hydrogen atom, an alkyl group, an acyl group, or an arylalkyl group. The group R.sub.2 may be a hydrogen atom, an unsubstituted aryl group or a substituted aryl group. The group R.sub.3 may be a hydrogen atom, an alkyl group, a cycloalkyl group, a substituted aryl group or an unsubstituted aryl group. The group R.sub.4 may be a hydrogen atom, an unsubstituted aryl group or a substituted aryl group. The R.sub.4 is absent when R.sub.3 is a cycloalkyl group having a first position carbon and a terminal position carbon bonded to the same carbon of the cyclopropane. Further, no more than any two of R.sub.2, R.sub.3 and R.sub.4 has an aryl group.

    摘要翻译： 在体外表现出对MCF-7细胞的抗增殖活性的Gem-二氯环丙烷（模拟II衍生物），通常不被雌二醇逆转或具有固有的雌激素（除了羟基苯基衍生物化合物30）。 一般来说，环丙烷化合物具有下式：其中R 1代表氢或其任何药学上可接受的盐。 X选自氢和卤素原子。 基团R1可以是氢原子，烷基，酰基或芳基烷基。 基团R2可以是氢原子，未取代的芳基或取代的芳基。 基团R3可以是氢原子，烷基，环烷基，取代的芳基或未取代的芳基。 基团R4可以是氢原子，未取代的芳基或取代的芳基。 当R3是具有与环丙烷的相同碳键合的第一位置碳和末端位置碳的环烷基时，R4不存在。 此外，R 2，R 3和R 4中不超过2个具有芳基。