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    Steroid esters of N-(2-halogenoethyl)-N-nitroso-carbamoyl-amino acids and peptides thereof, as well as methods for preparing them
    2.
    发明授权
    Steroid esters of N-(2-halogenoethyl)-N-nitroso-carbamoyl-amino acids and peptides thereof, as well as methods for preparing them 失效
    N-（2-卤代乙基）-N-亚硝基氨基甲酰基 - 氨基酸的类固醇酯及其肽，以及它们的制备方法

    公开(公告)号：US4609496A

    公开(公告)日：1986-09-02

    申请号：US557138

    申请日：1983-11-17

    申请人： Gerhard Eisenbrand ,  Joachim Schreiber

    发明人： Gerhard Eisenbrand ,  Joachim Schreiber

    IPC分类号： A61K31/565 ,  A61K31/17 ,  A61K31/22 ,  A61K31/57 ,  A61K38/00 ,  A61P35/00 ,  C07C275/16 ,  C07J1/00 ,  C07J41/00 ,  C07K5/06

    CPC分类号： C07J41/0072 ,  C07J41/0038 ,  C07J41/005

    摘要： Steroid-N-(2-halogen ethyl)-N-nitroso-carbamoyl-amino acid or peptide esters of the general formula: ##STR1## where R.sub.1 and R.sub.2, which may be identical or different, mean the radical of an amino acid beyond the C atom in the beta position (if present), R.sub.3 means the radical of a steroid or a stilbene derivative pharmacologically similar in action, n is a number from 0-5 and Hal stands for chlorine or fluorine, as well as the method for preparing them by the conversion of an appropriate carbamoyl-amino acid or carbamoyl-peptide in a manner known per se with steroid alcohols or the conversion of steroid-amino acid or steroid-peptide esters with corresponding N-nitroso-carbamoylation or corresponding N-nitroso-carbamoyl-amino acids or peptides in a manner known per se.

    摘要翻译： PCT No.PCT / EP83 / 00090 Sec。 371日期1983年11月17日 102（e）日期1983年11月17日PCT提交1983年3月23日PCT公布。 第WO83 / 03414号公报 日期：1983年10月13日。具有以下通式的类似N-（2-卤代乙基）-N-亚硝基氨基甲酰基 - 氨基酸或肽酯：其中R 1和R 2可以是 相同或不同，是指β位置（如果存在）之外的C原子以外的氨基酸的基团，R3表示在作用中药理学上相似的类固醇或二苯乙烯衍生物的基团，n为0-5的数，Hal为 代表氯或氟，以及通过适当的氨基甲酰基 - 氨基酸或氨基甲酰基 - 肽以类固醇或已知的类固醇 - 氨基酸或类固醇 - 肽酯转化来制备它们的方法 以相应的N-亚硝基 - 氨基甲酰基化或相应的N-亚硝基 - 氨基甲酰基 - 氨基酸或肽以本身已知的方式进行。

    Analogs of 1-(2-chloroethyl)-1-nitroso-3-(cycloheyl)-urea substituted by heterocyclic rings or alkyl radicals
    3.
    发明授权
    Analogs of 1-(2-chloroethyl)-1-nitroso-3-(cycloheyl)-urea substituted by heterocyclic rings or alkyl radicals 失效
    由杂环或烷基取代的1-（2-氯乙基）-1-亚硝基-3-（环己基） - 脲的类似物

    公开(公告)号：US4377687A

    公开(公告)日：1983-03-22

    申请号：US256558

    申请日：1981-04-22

    申请人： Gerhard Eisenbrand

    发明人： Gerhard Eisenbrand

    IPC分类号： A61K31/175 ,  A61K31/395 ,  A61P35/00 ,  C07C67/00 ,  C07C239/00 ,  C07C291/02 ,  C07D265/30 ,  C07D295/28 ,  C07C133/02

    CPC分类号： C07D295/32

    摘要： This invention relates to compounds having the formula: ##STR1## wherein R.sub.1 and R.sub.2 are selected from the group consisting of hydrogen, acyl, trifluoroacetyl, straight chained and branched alkyl groups with up to 6 carbon atoms, such alkyl groups with up to 3 substituents selected from the group consisting of OH, OSO.sub.2 CH.sub.3, COOH, COOR, CONH.sub.2 and Hal, where R is an alkyl group with up to 6 carbon atoms, and R.sub.1 and R.sub.2 together form a heterocyclic ring containing 4 to 6 carbon atoms and optionally further heteroatoms and such rings with up to 3 substituents selected from the group consisting of lower alkyl, OH, COOH, COOR, CONH.sub.2, where R has the above meaning, the chloroethyl nitrosoureido group and Hal, and Hal is selected from the group consisting of chlorine and fluorine, which heterocyclic ring is not the para-methyl piperazine group, said nitroso ureas having a tumor inhibiting effect.This invention also related to a method of inhibiting transplanted tumors which comprises treating a tumor-afflicted subject with one of the foregoing 1,3 - disubstituted nitroso ureas. It also involves a method of preparing such new compounds by reacting N-(2-halogenethyl)-N-nitrosocarbamoylazide with hydrazine or a monocyclic N-amino heterocyclic or their derivatives.

    摘要翻译： 本发明涉及具有下式的化合物：其中R 1和R 2选自氢，酰基，三氟乙酰基，具有至多6个碳原子的直链和支链烷基，这种烷基具有至多3个取代基 选自OH，OSO 2 CH 3，COOH，COOR，CONH 2和Hal，其中R是具有至多6个碳原子的烷基，并且R 1和R 2一起形成含有4至6个碳原子的杂环和任选的另外的杂原子 和具有至多3个选自低级烷基，OH，COOH，COOR，CONH 2的取代基的环，其中R具有上述含义，氯乙基亚硝基脲基，Hal和Hal选自氯和 氟，该杂环不是对甲基哌嗪基，所述亚硝基脲具有肿瘤抑制作用。 本发明还涉及抑制移植肿瘤的方法，其包括用前述1,3-二取代亚硝基脲之一治疗患有肿瘤的受试者。 它还涉及通过N-（2-卤代乙基）-N-亚硝基氨基甲酰基叠氮化物与肼或单环N-氨基杂环或其衍生物反应制备这种新化合物的方法。

    Hydroxylated indirubin derivatives
    5.
    发明申请
    Hydroxylated indirubin derivatives 审中-公开
    羟基靛玉红衍生物

    公开(公告)号：US20050080020A1

    公开(公告)日：2005-04-14

    申请号：US10922376

    申请日：2004-08-19

    申请人： Gerhard Eisenbrand ,  Frankie Hippe

    发明人： Gerhard Eisenbrand ,  Frankie Hippe

    IPC分类号： A61K31/404 ,  A61P35/00 ,  C07D209/36 ,  C07H15/26 ,  A61K31/7052 ,  C07D43/04

    CPC分类号： C07D209/36

    摘要： The present invention relates to hydroxylated indirubin derivatives having the formula (I) wherein the group R represents a straight-chain or branched-chain alkyl group or a straight chain or branched-chain alkoxy group each having 1 to 18 carbon atoms, the group R′ represents H, a straight-chain or branched-chain alkyl group having 1 to 4 carbon atoms or a glucuronide group, and X is H or OH; which can be used for the manufacture of a medicament for the treatment of solid cancers and leukemia and metastases thereof.

    摘要翻译： 本发明涉及具有式（I）的羟基化靛玉红衍生物，其中基团R表示直链或支链烷基或各自具有1至18个碳原子的直链或支链烷氧基，基团R '表示H，具有1至4个碳原子的直链或支链烷基或葡糖苷酸基，X是H或OH; 其可用于制备用于治疗固体癌症和白血病及其转移的药物。

    Steroid esters of N-(2-halogenethyl)-N-nitroso-carbamoylamino and acids and peptides therefore, as well as method for preparing them
    6.
    发明授权
    Steroid esters of N-(2-halogenethyl)-N-nitroso-carbamoylamino and acids and peptides therefore, as well as method for preparing them 失效
    因此，N-（2-卤代乙基）-N-亚硝基氨基甲酰基氨基酸和酸和肽的类固醇以及它们的制备方法

    公开(公告)号：US4615835A

    公开(公告)日：1986-10-07

    申请号：US731861

    申请日：1985-05-08

    申请人： Gerhard Eisenbrand ,  Joachim Schreiber

    发明人： Gerhard Eisenbrand ,  Joachim Schreiber

    IPC分类号： C07J41/00 ,  C07J1/00

    CPC分类号： C07J41/0072

    摘要： Steroid-N-(2-halogen ethyl)-N-nitroso-carbamoylamino acid or peptide esters of the general formula: ##STR1## where R.sub.1 and R.sub.2, which may be identical or different, mean the radical of an amino acid beyond the C atom in the beta position (if present), R.sub.3 means the radical of a steroid or a stilbene derivative pharmacologically similar in action, n is a number from 0-5 and Hal stands for chlorine or fluorine, as well as the method for preparing them by the conversion of an appropriate carbamoyl-amino acid or carbamoyl-peptide in a manner known per se with steroid alcohols or the conversion of steroid-amino acid or steroid-peptide esters with corresponding N-nitroso-carbamoylation or corresponding N-nitroso-carbamoyl-amino acids or peptides in a manner known per se.

    摘要翻译： 类固醇-N-（2-卤代乙基）-N-亚硝基氨基甲酰基氨基酸或具有以下通式的肽酯：其中R 1和R 2可以相同或不同，意指“ 在β位（如果存在）之外的C原子以外的氨基酸，R3表示在作用中药理学上类似的类固醇或二苯乙烯衍生物的基团，n是0-5的数，Hal代表氯或氟，以及 通过本领域已知的类固醇或转化类固醇 - 氨基酸或类固醇 - 肽酯与相应的N-亚硝基 - 氨基甲酰化或相应的方法转化合适的氨基甲酰基 - 氨基酸或氨基甲酰基 - 肽来制备它们的方法 N-亚硝基氨基甲酰基 - 氨基酸或肽。

    Process for the preparation of unsymmetrically 1,3-disubstituted nitroso ureas
    8.
    发明授权
    Process for the preparation of unsymmetrically 1,3-disubstituted nitroso ureas 失效
    制备不对称1,3-二取代亚硝基脲的方法

    公开(公告)号：US4150146A

    公开(公告)日：1979-04-17

    申请号：US800452

    申请日：1977-05-25

    申请人： Gerhard Eisenbrand

    发明人： Gerhard Eisenbrand

    IPC分类号： A61K31/165 ,  A61K31/17 ,  A61K31/195 ,  A61K31/22 ,  A61K31/255 ,  A61P35/00 ,  C07C67/00 ,  C07C239/00 ,  C07C247/20 ,  C07C269/06 ,  C07C271/60 ,  C07C275/04 ,  C07C275/66 ,  C07C275/68 ,  C07C281/06 ,  C07C301/00 ,  C07C303/28 ,  C07C305/00 ,  C07C309/66

    CPC分类号： A61K31/17

    摘要： The invention relates to the preparation of unsymmetrically 1,3-disubstituted nitroso ureas from the corresponding N-substituted alkyl-N-nitrosocarbamoyl azide which is reacted with an amine, a diamine, an aminoalcohol, an aminoacid or an aminoacid derivative. The N-nitrosocarbamoyl azide is obtained by reacting the corresponding alkylcarbamoyl azide with nitrogen tetroxide in the cold. The alkylcarbamoyl azide is obtained by reacting the corresponding isocyanate with an alkali metal azide.The invention further relates to novel nitroso ureas obtained thereby, to novel N-substituted alkyl-N-nitrosocarbamoyl azides, and to novel therapeutic compositions containing, as the active ingredient, the novel nitroso ureas.

    摘要翻译： 本发明涉及从与胺，二胺，氨基醇，氨基酸或氨基酸衍生物反应的相应的N-取代的烷基-N-亚硝基氨基甲酰基叠氮化物制备不对称的1,3-二取代的亚硝基脲。 N-亚硝基氨基甲酰基叠氮化物是通过使冷却下的相应的烷基氨基甲酰基叠氮化物与四氧化氮反应得到的。 烷基氨基甲酰基叠氮化物通过使相应的异氰酸酯与碱金属叠氮化物反应而获得。