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    Cardio-active glycosides of 3beta,14-dihydroxy - 4,5beta - oxido - 14beta - bufa - 20,22-dienolides and process for their preparation
    1.
    发明授权
    Cardio-active glycosides of 3beta,14-dihydroxy - 4,5beta - oxido - 14beta - bufa - 20,22-dienolides and process for their preparation 失效
    3BETA，14-二羟基-4,5BETA-OXIDO-14BETA-BUFA-20,22-二醇的制备活性糖苷及其制备方法

    公开(公告)号：US3741956A

    公开(公告)日：1973-06-26

    申请号：US3741956D

    申请日：1971-04-29

    Applicant: HOECHST AG

    Inventor： RADSCHEIT K ,  STACHE U ,  LINDNER E ,  FRITSCH W ,  HAEDE W

    IPC: A61K31/58 ,  A61K31/585 ,  C07J19/00 ,  C07J71/00 ,  C07C173/00

    CPC classification number: A61K31/58 ,  A61K31/585 ,  C07J19/00 ,  C07J71/00

    Abstract: IN WHICH R1 IS CH3-, CHO-, CH2OH, CH2O-ALKYL, CH2O ACYL AND R2 IS MONO-, DI- OR TRISACCHARIDYL, OPTIONALLY ESTERIFIED, ETHERIFIED OR CONDENSED WITH CARBONYL COMPOUNDS, E.G. 3B,14 - DIHYDROXY-4,5B-OXIDO-14B-BUFA20,22-DIENOLIDE, 3B-(A-L-RHAMNOSIDE) AND 3B,14-DIHYDROXY - 4,5B-OXIDO-14B-BUFA-20,22-DIENOLIDE, 3B-(B-D-GLUCOSIDE). METHOD FOR MAKING THESE COMPOUNDS (1) BY ACYLATING THE CORRESPONDING GLYCOSIDES, REACTING THE ACYLATES WITH HOHAL-FORMING AGENTS TO THE CORRESPONDING 4,5-HALOHYDRINS WHICH ARE THEN CONVERTED INTO 4,5B-EPOXIDES BY SPLITTING OFF HYDROGEN HALIDE, OF (2) BY REACTING THE CORRESPONDING AGLYCONES OF THE ABOVE FORMULA (R2"H) WITH ACYLATED 1-HALOPYRANOSES IN INERT SOLVENTS IN THE PRESENCE OF SILVER SALTS, AND FINALLY HYDROLYZING THE ACYLATED COMPOUNDS TO YIELD THE FREE GLYCOSIDES. THESE COMPOUNDS HAVE STRONG POSITIVE INOTROPIC ACTION AND A PRONOUNCED CARDIOACTIVE EFFICACY.

    ESTRANE

    17-(2-(O=)PYRAN-5-YL),14-HO,10-R1,4,5-(-O-),3-(R2-O-)-

    3-HYDROXY-4,5B-OXIDO - BUFADIENOLIDES OF THE GENERAL FORMULA

    3-amino-4,5-dehydro-cardenolides and process for their manufacture
    2.
    发明授权
    3-amino-4,5-dehydro-cardenolides and process for their manufacture 失效
    3-氨基-4,5-脱氢半胱氨酸及其制备方法

    公开(公告)号：US3801570A

    公开(公告)日：1974-04-02

    申请号：US3801570D

    申请日：1971-10-27

    Applicant: HOECHST AG

    Inventor： HAEDE W ,  RADSCHEIT K ,  STACHE U ,  FRITSCH W ,  LINDNER E

    IPC: A61K20060101 ,  A61K31/585 ,  C07C20060101 ,  C07D20060101 ,  C07J17/00 ,  C07J41/00 ,  C07C173/02

    CPC classification number: C07J19/00

    Abstract: 3-AMINO - 4,5 - DEHYDRO-CARDENOLIDES OF THE GENERAL FORMULA

    1-R7,3-(R1-NH-),11-R8,12-R5,14-R2,15-R3,16-R4,17-(5-(O=)-

    2,5-DIHYDROFUR-3-YL),19-R6-ANDROST-4-ENE

    IN WHICH R1 REPRESENTS HYDROGEN OR A LOWER ALIPHATIC ACYL RADICAL, R2 AND R3 EACH REPRESENT HYDROGEN OR HYDROXY, OR R2 AND R3 TOGETHER REPRESENT A FURTHER C-C BOND OR AN A- OR B-OXIDO GROUP, R4, R5, R6 AND R7 EACH REPRESENT HYDROGEN OR A HYDROXY GROUP WHICH MAY BE ESTERIFIEDTHE OH GROUP FOR R6 MAY ALSO BE ETHERIFIED-R8 REPRESENTS HYDROGEN OR HYDROXY, AND THE SALTS THEREOF WITH INORGANIC OR ORGANIC ACIDS, IF R1 REPRESENTS HYDROGEN. THE COMPOUNDS HAVE VALUABLE PHARMALOGICAL PROPERTIES, ESPECIALLY A POSITIVE OR NEGATIVE INOTROPIC ACTION AND A SUBSTANTIALLY INPROVED LIPID SOLUBILITY. METHODS FOR MAKING AND USING THE COMPOUNDS.

    Heterocyclic ethers of piperazine n alkanols
    3.
    发明授权
    Heterocyclic ethers of piperazine n alkanols 失效
    哌嗪N醇的杂环化合物

    公开(公告)号：US3787411A

    公开(公告)日：1974-01-22

    申请号：US3787411D

    申请日：1970-09-08

    Applicant: HOECHST AG

    Inventor： MOHLER W ,  GOEBEL A ,  RUSCHIG H ,  SCHMITT K ,  LINDNER E

    IPC: C07D237/14 ,  C07D213/64 ,  C07D215/22 ,  C07D237/30 ,  C07D239/34 ,  C07D239/72 ,  C07D241/18 ,  C07D277/20 ,  C07D277/34 ,  C07D277/68 ,  C07D295/04 ,  C07D295/067 ,  C07D295/185 ,  C07D51/70

    CPC classification number: C07D213/64 ,  C07D241/18 ,  C07D295/067 ,  C07D295/185 ,  Y10S514/921

    Abstract: A HECTEROCYCLIC ETHER OF THE FORMULA

    1-(R1-O-A-),4-(R2-)-PIPERAZINE

    IN WHICH R1 IS 3-, 4- OR 6-ALKOXY-PYRIDYL-(2); 2-, 4- 5OR 6-ALKOXY-PYRIDYL-(3); 2- OR 3-ALKOXY-PYRIDYL-(4) WHICH HAVE 1-4 CARBON AOMS IN THE ALKOXY RADICAL: 3-, 4-, 5OR 6-METHYL-PYRIDYL-(2); 6 - ETHYL - PYRIDYL - (4)-; 2,6-DIMETHYL-PYRIDYL-(4); R2 IS PHENYL, O-TOLYL, M-TOLYL, P-TOLYL, O-AANISYL, M-ANISYL, P-ANISYL, O-CHLOROPHENYL, M-CHLOROPHENYL, P-CHLOROPHENYL, PYRIDYL (2), PYRIDYL (3), PYRIDYL (4); 2-CHLORO-4-METHYL-PHENYL, 2-CHLORO - 4 - METHOXYPHENYL AND 2-METHOXY-4 - METHYL - PHENYL, 6 - METHOXYPYRIDYL (2), 2-METHYL-PYRIDYL (4), 4,6-DIMETHYL-PYRIDYL (2) OR THEIR POSITION ISOMERS, AND A IS ALKYLENE HAVING FROM 2 TO 6 CARBON ATOMS WHEREIN THE SAME IS ETHYLENE, TRIMETHYLENE, 2-METHYL-ETHYLENE, 3-METHYL-ETHYLENE, TETRAMETHYLENE, 3-METHYL-TRIMETHYLENE, 2 - ETHYL - ETHYLENE, 1ETHYL-ETHYLENE, PENTAMETHYLENE, 4 - METHYL - TETRAMETHYLENE, 3-ETHYL-TRIMETHYLENE, 1-PROPYL - ETHYLENE, 1 - ISOPROPYL-ETHYLENE, 1,2-DIMETHYL - ETHYLENE, 1 HEXAMETHYLENE, 5METHYL-PETAMETHYLENE, 4 - ETHYL - TETRAMETHYLENE, 3 - PROPYL-TRIMETHYLENE, 2-BUTYL-ETHYLENE, 1 - BUTYL - ETHYLENE OR 1-METHYL-3-ETHYL-TRIMETHYLENE; AND PHYSIOLOGICALLY TOLERABLE ACID ADDITION SALTS THEREOF; THESE COMPOUNDS HAVE AN A-SYMPATHOLYTIC ACTION AND ARE USEFUL IN THE TREATMENT OF SHOCKS, MIGRAINE, HYPERTONIA AND BLOOD CIRCULATION DISORDERS OF THE EXTREMITIES.

    Pharmacologically effective substance isolated from cabucala madagascariensis
    5.
    发明授权
    Pharmacologically effective substance isolated from cabucala madagascariensis 失效
    药用化学物质分离自马齿苋（CABUCALA MADAGASCARIENSIS）的药理学有效物质

    公开(公告)号：US3773931A

    公开(公告)日：1973-11-20

    申请号：US3773931D

    申请日：1972-02-22

    Applicant: HOECHST AG

    Inventor： GROEBEL A ,  LINDNER E

    IPC: A61K20060101 ,  A61K36/00 ,  A61K36/24 ,  C07C20060101 ,  C07G5/00 ,  C07G99/00 ,  A61K27/00

    CPC classification number: A61K36/24

    Abstract: A PHARAMACOLOGICALLY ACTIVE SUBSTANCE AND PHYSIOLOGICALLY TOLERABLE SALTS THEREOF HAVING HYPOTENSIVE PROPERTIES. SAID AGENT, WHICH IS ISOLATED FROM CABUCALA MADAGASCARIENSIS, MELTS AT 87*C., CORRESPONDS TO THE MOLECULAR FORMULA C38H56O12N3CL, HAS A MOLECULAR WEIGHT BETWEEN 780 AND 800 AS DETERMINED BY MASS SPECTROSCOPY, SHOWS NO ABSORPTION IN ITS ULTRAVIOLET SPECTRUM BETWEEN 210 AND 40 MU, AND HAS A SPECIFIC ROTATION (A)20D IN WATER OF -20*. METHOD OF ISOLATING SAID SUBSTANCE FROM CABUCALA MADAGASCARIENSIS.

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