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    Cardenolido-3-{8 4{40 -amino-2{40 , 3{40 , 4{40 -tridesoxy-glycosides{9 {0 and process for their manufacture
    1.
    发明授权
    Cardenolido-3-{8 4{40 -amino-2{40 , 3{40 , 4{40 -tridesoxy-glycosides{9 {0 and process for their manufacture 失效
    卡丁德多-3- {8 4 {40-氨基-2 {40,3 {40,4 {40-二酰氧基 - 糖苷{9 {0及其制备方法

    公开(公告)号：US3914213A

    公开(公告)日：1975-10-21

    申请号：US41174773

    申请日：1973-11-01

    Applicant: HOECHST AG

    Inventor： STACHE ULRICH ,  FRITSCH WERNER ,  HAEDE WERNER ,  LINDNER ERNST

    IPC: C07J41/00 ,  A61K31/585 ,  C07J17/00 ,  C07J19/00

    Abstract: Cardenolido-3-(4''-amino-2'', 3'', 4''-tridesoxy-glycosides) of the general formula

    WHEREIN R1 stands for a steroid radical of the 3hydroxycardenolide series, R2 stands for hydrogen, lower alkyl, alkenyl, cycloalkyl, phenyl, benzyl, phenylethyl, lower aliphatic acyl, or one of the acid radicals of benzoic acid, cinnamic acid or cyclohexane-carboxylic acid, and R3 stands for methyl, the CH2OR2-group or hydrogen, and a process for their preparation are described. The compounds have valuable pharmaceutical properties.

    Abstract translation: 通式为：WHEREIN R1代表3-羟基僵硬醚系列的类固醇基的卡固伦多-3- [4'-氨基-2'，3'，4'-三酰氧基 - 糖苷]，R2代表氢，低级烷基，烯基 ，环烷基，苯基，苄基，苯基乙基，低级脂族酰基或苯甲酸，肉桂酸或环己烷羧酸的酸基之一，R 3代表甲基，CH 2 OR 2 - 基或氢，及其制备方法 被描述。 这些化合物具有有价值的药物性质。

    Digoxigenin-12-formiate and process for its manufacture
    5.
    发明授权
    Digoxigenin-12-formiate and process for its manufacture 失效
    地高辛-12-形成并加工制造

    公开(公告)号：US3895008A

    公开(公告)日：1975-07-15

    申请号：US41642773

    申请日：1973-11-16

    Applicant: HOECHST AG

    Inventor： STACHE ULRICH ,  FRITSCH WERNER ,  HAEDE WERNER

    IPC: C07J19/00 ,  A61K20060101 ,  C07D20060101 ,  C07C173/02

    CPC classification number: C07J19/00

    Abstract: Digoxigenin-12-formiate prepared by a selective acylation of digoxigenin with a mixed anhydride of formic acid and acetic acid in the presence of a tertiary organic base. The product is suitable for the treatment of the disturbed circulatory system.

    Abstract translation: 通过在三级有机碱存在下，将地高辛与甲酸和乙酸的混合酸酐选择性酰化制备的地高辛-12-甲酸酯。 该产品适用于干扰循环系统的治疗。

    19-alkylene-14- ' -hydroxy-cardenolide derivatives and process for preparing them
    6.
    发明授权
    19-alkylene-14- ' -hydroxy-cardenolide derivatives and process for preparing them 失效
    19-烷基-14-羟基羧酸衍生物及其制备方法

    公开(公告)号：US3859272A

    公开(公告)日：1975-01-07

    申请号：US26961272

    申请日：1972-07-07

    Applicant: HOECHST AG

    Inventor： STACHE ULRICH ,  FRITSCH WERNER ,  HAEDE WERNER ,  RADSCHEIT KURT ,  LINDMER ERNAT

    IPC: C07C173/00

    Abstract: Cardiotonically active 19-alkylene-14 Beta -hydroxycardenolides of the formula

    WHEREIN R1 taken alone is -CH, -CO2R5, -CON(R6)2, -CH(OR6)2, C6H5, -CH CH2, or -SCH3, or, taken together with an -OH group in the R3-position, forms a lactone ring; R2 is -H, -CH3, -F, -Cl, Br, or -I; R3 is 5 Alpha -H, 5 Beta -H, or 5 Beta -OH; R4 is -OH, substituted or unsubstituted 3-pyranyl ether, or a 5-or 6membered substituted or unsubstituted cyclic glycoside; R5 is -H, -CH3, -C2H5, -C3H7, -C4H9, -C5H11, or -CH2-C6H5; and R6 is -CH3 or -C2H5, or, when -CH(OR6)2 is a cyclic acetal, the R6''s together are -CH2CH2- or -CH2C(CH3)2CH2-. A process for preparing these compounds from the corresponding 19-oxo-14 Beta hydroxy cardenolides.

    Process for the manufacture of 14beta-hydroxy-3-oxo-5alpha-card-20(22)-enolides
    7.
    发明授权
    Process for the manufacture of 14beta-hydroxy-3-oxo-5alpha-card-20(22)-enolides 失效
    制备14BETA-羟基-3-氧代-5ALPHA-CARD-20（22） - 酚的方法

    公开(公告)号：US3639394A

    公开(公告)日：1972-02-01

    申请号：US3639394D

    申请日：1969-06-25

    Applicant: HOECHST AG

    Inventor： STACHE ULRICH ,  FRITSCH WERNER ,  HAEDE WERNER ,  RADSCHEIT KURT

    IPC: C07J19/00 ,  C07C173/00

    CPC classification number: C07J19/00

    Abstract: A 14B-HYDROXY-3-OXO-5A-CARD-20(22)-ENOLIDE IS PREPARED BY KETALIZING A 3-OXO-5A-CARDA-14,20(22)-DIENOLIDE, COVERING THE 3-KETAL SO OBTAINED WITH AN N-HALOGENOAMIDE UNDER WHEAKLY ACID CONDITIONS INTO A 3-KETAL OF A 3-OXO-14B-HYDROXY-15A-BROMO-5A-CARD-20(22)ENOLIDE, CATALYTICALLY HYDROGENATING THIS KETAL TO FORM THE CORRESPONDING 3-OXO-14B-HYDROXY-5A-CARD-20 (22)-ENOLIDE, THE PH VALUE BEING BETWEEN 4.5 AND 7, AND SPLITING OFF THE 3-KETAL GROUP UNDER WEAKLY ACID CONDI TIONS. THE PRODUCTS OF INVENTION HAVE VALUABLE PHARMACOLOGICAL PROPERTIES.

    Cardioactive anhydrotalomethylosides and process for preparing them
    10.
    发明授权
    Cardioactive anhydrotalomethylosides and process for preparing them 失效
    心脏活性脱水甲基氯化物及其制备方法

    公开(公告)号：US3910882A

    公开(公告)日：1975-10-07

    申请号：US38266273

    申请日：1973-07-26

    Applicant: HOECHST AG

    Inventor： HAEDE WERNER ,  FRITSCH WERNER ,  STACHE ULRICH ,  LINDNER ERNST

    IPC: C07J19/00 ,  A61K20060101 ,  A61K31/585 ,  A61K31/704 ,  A61P7/10 ,  A61P9/04 ,  C07C20060101 ,  C07D20060101

    CPC classification number: C07J19/00

    Abstract: The invention relates to 3'', 4''-anhydro- Beta , Ltalomethylosides of the general formula I

    wherein R1 is methyl or formyl and R2 stands for Beta -H or Beta -OH, if there is no double bond in 4,5-position, and R3 is a butenolide or cumalin ring, a process for preparing them and their use in the treatment of cardiac and circulatory disturbances. The compounds are especially suitable for treating cardiac insufficiency, tachycardia and conduction defects.

    Abstract translation: 本发明涉及通式Ⅰ的3'，4'-脱氢-β，L-天门冬氨酸盐，其中R1是甲基或甲酰基，R2代表β-H或β--OH，如果4,5中没有双键 - 位，R3是丁烯内酯或坎加林环，其制备方法及其在治疗心脏和循环障碍中的应用。 该化合物特别适用于治疗心功能不全，心动过速和传导缺陷。

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