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321 条记录 (耗时 0.013 秒)

    Digoxin complexes
    91.
    发明授权
    Digoxin complexes 失效
    DIGOXIN复合物

    公开(公告)号：US3839317A

    公开(公告)日：1974-10-01

    申请号：US37505273

    申请日：1973-06-29

    申请人： INTERX RESEARCH CORP

    发明人： HIGUCHI T

    IPC分类号： A61K9/20 ,  A61K31/045 ,  A61K31/585 ,  C07C19/00 ,  C07C39/08 ,  C07J9/00 ,  C07J17/00 ,  C07J19/00 ,  C07C173/02

    摘要： Digoxin forms novel complexes with dihydroxybenzenes such as hydroquinone, resorcinol and pyrocatechol. These complexes exhibit rapid dissolution and high solubility in aqueous media. These complexes are useful in the treatment of cardiac insufficiency.

    摘要翻译： 地高辛与二羟基苯如氢醌，间苯二酚和邻苯二酚形成新型配合物。 这些配合物在水性介质中表现出快速溶解和高溶解度。 这些复合物可用于治疗心功能不全。

    Pharmaceutical composition essentially containing,and method of treatment with,delta4,20,22-bufatrienolide rhamnoside ethers
    92.
    发明授权
    Pharmaceutical composition essentially containing,and method of treatment with,delta4,20,22-bufatrienolide rhamnoside ethers 失效
    含有药物组合物及其与DELTA4,20,22-十六烷基胆碱盐酸盐治疗剂的方法

    公开(公告)号：US3836646A

    公开(公告)日：1974-09-17

    申请号：US31124972

    申请日：1972-12-01

    申请人： KNOLL AG

    发明人： KUBINYI H

    IPC分类号： C07J19/00 ,  A61K27/14

    CPC分类号： C07J19/005

    摘要： CARDIOACTIVE $4,20,22-BUFATRDIENOLIDE RHAMNOSIDE ETHERS OF THE FORMULA

    3-((2-(H3C-),3-(HO-),4-(R''2O-),5-(R''2O-)-TETRAHYDROPYRAN-

    6-YL)-O-),10-R,14-(HO-),17-(TETRAHYDROPYRAN-2-ON-5-YL)-

    ESTR-4-ENE

    WHEREIN R IS METHYL OR FORMYL; R1 AND R2 TAKEN ALONE ARE HYDROGEN, LOWER ALKYL, OR ACETYL; R1 AND R2 TAKEN TOGETHER ARE

    -C(-CH3)2-

    R3 IS HYDROGEN, LOWER ALKYL, OR ACETYL; AND WHEREIN AT LEAST ONE OF R1, R2, OR R3 IS ALKYL, AND THE METHOD OF PREPARING THEM BY REACTION OF THE CORRESPONDING 2'',3'',4''-HYDROXY COMPOUNDS OR 2'',3''-ISOPROPYLIDENE-4''-HYDROXY COMPOUNDS WITH AN ALKYL HALIDE, OPTIONALLY FOLLOWED BY HYDROLYSIS OF THE ISOPROPYLIDENE GROUP AND/OR ACETYLATION OF UNETHERIFIED HYDROXY GROUPS.

    Steroid compounds effective against cardiac conditions and method of their preparation
    94.
    发明授权
    Steroid compounds effective against cardiac conditions and method of their preparation 失效
    有效的针对心脏病症的甾体化合物及其制备方法

    公开(公告)号：US3706727A

    公开(公告)日：1972-12-19

    申请号：US3706727D

    申请日：1969-06-10

    申请人： LAEVOSAN GMBH & CO KG

    发明人： BERAN WILHELMINE

    IPC分类号： C07J71/00 ,  A61K31/585 ,  B01J31/00 ,  B01J31/04 ,  C07J19/00 ,  C07C173/00

    CPC分类号： C07J19/00

    摘要： THE PRESENT INVENTION PROVIDES NOVEL STEROID COMPOUNDS HAVING THE FORMULA

    3-(R1-O-),4-R5,5-R6,6-R2,8-R4,10-R3,14-(HO-),17-(2-(O=)-

    2H-PYRAN-5-YL)ESTRANE

    WHEREIN R1 IS HYDROGEN OR A SUGAR RADICAL; R2 IS HYDROGEN, A HYDROXYL GROUP OR AS ESTER OR AN ETHER THEREOF WITH A LOWER ALKYL CARBOXYLIC ACID OR A LOWER ALKY ALCOHOL; R3 IS A LOWER ALKYL RADICAL WHICHMAY BE SUBSTITUTED WITH ANOXYGEN ATOM, A HYDROXYL GROUP, A LOER ALKOXY GROUP, OR WITH THE ACYL RADICAL OF A LOWER ALKYL CARBOXYLIC ACID; R4 IS HYDROGEN, THE HYDROXYL GROUP OR AN ESTER THEREOF WITH A LOWER ALKYL CARBOXYLIC ACID, OR IS THE ETHOXY GROUP; AND R5 AND R6 ARE EACH A HYDROXYL GROUP OR TOGETHER FORM AN EPOXY GROUP.

    Process for the preparation of bufalin and related compounds
    95.
    发明授权
    Process for the preparation of bufalin and related compounds 失效
    制备BUFALIN及相关化合物的方法

    公开(公告)号：US3687944A

    公开(公告)日：1972-08-29

    申请号：US3687944D

    申请日：1970-05-08

    申请人： GEORGE R PETTIT ,  LEONARD E HOUGHTON ,  JOHN C KNIGHT ,  FRED BRUSCHWEILER

    发明人： PETTIT GEORGE R ,  HOUGHTON LEONARD E ,  KNIGHT JOHN C ,  BRUSCHWEILER FRED

    IPC分类号： C07J19/00 ,  C07C173/04

    CPC分类号： C07J19/00

    摘要： There is provided a novel method of preparing the cardiac active agents bufalin and its immediate precursor resibufogenin from the well known cardenolide, digitoxigenin. The method comprises conducting a ring expansion of the five-membered lactone at C-17 to the corresponding six-membered lactone. In this process the five-membered lactone is cleaved to provide a 20-acetal-21-nor-5 Beta norchol-14-enate ester. The 20-acetal is protected by the formation of an alkylenethioacetal or similar thio derivative, and the carboxylic residue at C-22 homoligized using a modified Arndt-Eistert sequence. Removal of the protecting thio groups yields the corresponding 20-formyl-21-nor-5 Beta -chol-14-enic acid which is then subjected to ring closure and dehydrogenation to yield the known 14-dehydrobufalin which may be converted by known methods to resibufogenin and bufalin.

    摘要翻译： 提供了一种制备心脏活性剂蟾蜍灵及其直接前体抗纤维蛋白原的新方法，该方法来自众所周知的心灵素，地辛毒素。 该方法包括将C-17上的五元内酯环扩展至相应的六元内酯。 在该方法中，将五元内酯裂解以提供20-乙缩醛-21-降-5β-胆碱-14-酸酯。 通过形成亚烷基硫醛或类似的硫代衍生物来保护20-缩醛，并且使用改性的Arndt-Eistert序列使C-22的羧酸残基同源化。 除去保护的硫代基产生相应的20-甲酰基-21-去甲-β-胆醇-14-酸，然后将其进行闭环和脱氢，得到已知的14-脱氢支架蛋白，其可通过已知方法转化为 抗生素和蟾蜍灵。

    14beta-hydroxy-15alpha-acyloxy-cardenolides
    97.
    发明授权
    14beta-hydroxy-15alpha-acyloxy-cardenolides 失效
    14BETA-HYDROXY-15ALPHA-ACYLOXY-CARDENOLIDES

    公开(公告)号：US3655643A

    公开(公告)日：1972-04-11

    申请号：US3655643D

    申请日：1970-07-27

    申请人： SCHERING AG

    发明人： LEHMANN HANS-GUNTER ,  WIECHERT RUDOLF

    IPC分类号： A61K31/585 ,  C07J19/00 ,  H02G13/00 ,  C07C173/00

    CPC分类号： A61K31/585 ,  C07J19/00 ,  H02G13/00

    摘要： 14B-HYDROXY-UKX-ACYLOXY-CARDENOLIDES OF THE FORMULA

    14-HO,15-(R-O-),17-(5-(O=)-2,5-DIHYDROFUR-3-YL)-

    ANDROST-4-ENE WHERE THE C IN 3 POSITION IS REPLACED BY X

    WHEREIN-OR IS AN ESTERIFIED HYDROXY GROUP AND X IS >C=O OR >CH-OR'' IN WHICH-OR'' IS A FREE OR ESTERIFIED HYDROXY GROUP, TETRAHYDROPYRANYLOXY GROUP OR SIMILAR READILY CLEAVABLE GLYCOSIDE GROUP ARE CARDIOACTIVE COMPOUNDS WHICH INCREASE HERT STRENGTH WITHOUT REDUCING HEART FREQUENCY.

    Steroidal lactones
    99.
    发明授权
    Steroidal lactones 失效
    Steroidal Lactones

    公开(公告)号：US3591583A

    公开(公告)日：1971-07-06

    申请号：US3591583D

    申请日：1969-02-24

    申请人： AMERICAN HOME PROD

    发明人： LEFEBVRE YVON

    IPC分类号： C07J19/00 ,  C07C173/00

    CPC分类号： C07J19/00

    摘要： THERE ARE DISCLOSED HERIN STEROIDAL LACTONES OF 4-HYDROXY-2-BUTENOIC ACID IN WHICH THE LACTONE RING IS ATTACHED IN POSITION 3 TO 17 A-POSITION OF THE STEROID, WITH THE STEROIDS BEING SELECTED FROM 3,17 B-DIHYDROXYESTRA-1,35(10)-TRIENES, 3, 17B-DIHYDROXYESTRA-1,3,5(10),6,8-PENTAENES AND 3,17B-DIHYDROXY-7A,8-EPOXYESTRA-1,3,5(10)-TRIENES. THE 3-HYDROXY GROUP ON THE STEROID NUCLEUS MAY ALSO CARRY AN ACYL SUBSTITUENT CONTAINING FROM 2 TO 4 CARBONS ATOMS, AN ALKYL SUBSTUTUENTS CONTAINING FROM 1 TO 4 CARBON ATOMS OR A CYCLOALKYL SUBSTITUENT CONTAINING FROM 5 TO 6 CARBON ATOMS. THE PROCESS FOR PREPARING THE STEROIDAL LACTONES OF THIS INVENTION COMPRISES TREATING THE CORRESPONDING 17 A-FURYL-SUBSTITUTED STEROIDS WITH AN ORGANIC PERACID IN THE PRESENCE OF A NUCLEOPHILIC REAGENT, THUS OBTAINING AS INTERMEDIATES THE CORRESPONDING STEROIDAL 4,4-DIHYDROXY-2-BUTENOIC ACID LACTONES, IN WHICH THE 4-HYDROXY GROUP MAY BE ACYLATED, IF DESIRED. TREATMENT OF SAID INTERMEDIATES WITH SODIUM BOROHYDRIDES YIELDS THE STEROIDAL LACTONES OF THIS INVENTION. SAID LAST-NAMED COMPOUNDS ARE HIGHLY ACTIVE ESTROGENS AND METHODS FOR THEIR USE ARE ALSO DISCLOSED.