Adenosine derivatives
    1.
    发明授权

    公开(公告)号:US3901876A

    公开(公告)日:1975-08-26

    申请号:US28897372

    申请日:1972-09-14

    申请人: SCHERING AG

    CPC分类号: C07H19/16

    摘要: Adenosine derivatives of the formula

    WHEREIN A is saturated or unsaturated, straight-chain, branched or cyclic alkylene optionally substituted by one of hydroxy, acyloxy, carboxy or acyl; X is a valence bond, oxygen, sulfur, or an alkylated or acylated imino group; and B is 3-indolyl or 4imidazolyl optionally substituted by one or more of halogen, alkyl, haloalkyl, alkoxy, aryloxy, acyloxy, hydroxy, mercapto, alkylmercapto, nitro, carboxy, carboxyalkyl, or methylsulfonylamino, and processes for their preparation and use. These adenosine derivatives exert pharmacological effects on the central nervous system, the circulation, and the heart.

    N(6)-disubstituted adenosine compounds
    2.
    发明授权
    N(6)-disubstituted adenosine compounds 失效
    N(6) - 衍生腺苷化合物

    公开(公告)号:US3840521A

    公开(公告)日:1974-10-08

    申请号:US28711572

    申请日:1972-09-07

    IPC分类号: C07H19/16 C07D51/54

    CPC分类号: C07H19/16

    摘要: 1. N(6)-DISUBSTITUTED ADENOSINE COMPOUND OF THE FORMULA

    6-(R1-N(-R2)-),9-(3,4,5-TRI(HO-)-TETRAHYROFUR-2-YL-)-

    9H-PURINE

    WHEREIN R1 IS ALKYL OF FROM 1 TO 6 CARBON ATOMS; AND R2 IS STRAIGHT-CHAINED OR BRANCHED ALKYL OF FROM 4 TO 10 CARBON ATOMS; CYCLOALKYL OR METHYLCYCLOALKYL WHEREIN THE CYCLOALKYL MOIETY CONTAINS FROM 3 TO 10 CARBON ATOMS, CYCLOALKYL-ALKYL WITH FROM 3 TO 10 CARBON ATOMS IN THE CYCLOALKYL GROUP AND FROM 1 TO 4 CARBON ATOMS IN THE ALKYL SIDE-CHAIN OR BICYCLOALKYL OF FROM 5 TO 7 CARBON ATOMS IN EACH RING; AND THE PHARMACOLOGICALLY COMPATIBLE SALTS THEREOF.

    N1-oxides of adenosine-5'-carboxylates
    3.
    发明授权
    N1-oxides of adenosine-5'-carboxylates 失效
    腺苷-5'-羧酸的N1-氧化物

    公开(公告)号:US3830793A

    公开(公告)日:1974-08-20

    申请号:US29474172

    申请日:1972-10-03

    申请人: ABBOTT LAB

    发明人: PRASAD R

    CPC分类号: C07H19/16

    摘要: N1-OXIDES OF ADENOSINE-5''-ALKYL CARBOXYLATES REPRESENTED BY THE STRUCTURAL FORMULA

    1-(O=),6-(H2N-),9-(2-(R1O-CO-),3-(R2O-),4-(R3O-)-TETRAHY

    DROFUR-5-YL)-9H-PURINE

    WHEREIN R1 IS LOWERALKYL, LOWERHYDROXYALKYL OR LOWERHALOALKYL, AND R2 AND R3 EACH ARE HYDROGEN OR ACYL OR WHEN TAKEN TOGETHER FORM AN ISOPROPYLIDENE OR A BENZYLIDENE MOIETY, AND THE PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF. THE COMPOUNDS ARE USEFUL AS ANTI-ANGINAL AGENTS.

    Purine-ribofuranoside-3',5'-cyclophosphates and process for their preparation
    5.
    发明授权
    Purine-ribofuranoside-3',5'-cyclophosphates and process for their preparation 失效
    嘌呤 - 呋喃糖苷-3',5'-环磷酸酯及其制备方法

    公开(公告)号:US3712885A

    公开(公告)日:1973-01-23

    申请号:US3712885D

    申请日:1969-09-08

    IPC分类号: C07H19/20 C07D51/54

    CPC分类号: C07H19/20

    摘要: NOVEL PURINE-RIBOFURANOAIDE-3'',5''-CYCLOPHOSPHATE COMPOUNDS OF THE FORMULA:

    2-B,7-(2,3-(-CH2-O-P(=O)(-OH)-O-),4-Y-FURAN-5-YL),6-Z-

    PURINE

    WHEREIN B IS A HYDROGEN ATOM OR A HYDROXYXYL OR AMINO GROUP; Z IS A HALOGEN ATOM, AN ETHER GROUP OR A MONOOR DISUBSTITUTED AMINO GROUP WHEN X IS A HYDROGEN ATOM AND OTHERWISE Z IS A HYDROGEN ATOM, A HYDROXYL GROUP OR AN UNSUBSTITUTED AMINO GROUP, Y IS A HYDROXYL GROUP OR, WHEN X IS OTHER THAN A HYDROGEN ATOM, Y IS A HYDROGEN ATOM AND X IS A HYDROGEN OR HALOGEN ATOM, A HYDROXYL GROUP, AN ETHER GROUP, A SULPHYDRYL GROUP, A THIOETHER GROUP OR AN UNSUBSTITUTED OR SUBSTITUTED AMINO GROUP; AND THE SALTS THEREOF, ARE PROVIDED; THESE COMPOUNDS CAN BE PREPARED BY REACTING THE CORRESPONDING CYCLOPHOSPHATE WHEREIN Y AND Z IN THE ABOVE FORMULA ARE HYDROXY, AND X IS HYDROGEN, WITH (A) PHOSPHORUS OXYHALIDE AFTER ACYLATION OR (B) MOLECULAR HALOGEN IN ALKALINE MEDIUM, TO FORM THE CORRESPONDING (A)6-HALO OR (B) 8-HALO COMPOUND, AND THE 6- OR 8-HALO COMPOUND THEREBY OBTAINED IS CONVERTED, IF NECESSARY, INTO THE CORRESPONDING DESIRED COMPOUND BY, E.G., REACTING THE HALO COMPOUND WITH AN ALCOHOL OR ALCOHOLATE TO GIVE THE CORRESPONDING ETHER; OR WITH AMMONIA OR AN AMINE TO GIVE THE CORRESPONDING AMINO COMPOUND; OR WITH HYDRAZINE TO GIVE THE CORRESPONDING HYDRAZIDE; OR WITH THIOUREA OR AN ALKYL SULFIDE TO GIVE THE CORRESPONDING SULPHHYDRYL COMPOUND, WHICH CAN IN TURN BE CONVERTED TO THE THIOETHER COMPOUNDS.

    2-amino-adenosine derivatives
    8.
    发明授权
    2-amino-adenosine derivatives 失效
    2-氨基腺苷衍生物

    公开(公告)号:US3590029A

    公开(公告)日:1971-06-29

    申请号:US3590029D

    申请日:1968-08-22

    IPC分类号: C07H19/16 C07D51/54

    CPC分类号: C07H19/16

    摘要: NOVEL 2-AMINO-ADENOSINE DRIVATIVES CHARACTERIZED BY CARDIAC AND CIRCULATORY ACTIVITY AND BY THEIR HIGH CORONARY SPECIFICITY HAVING THE FOLLOWING STRUCTURAL FORMULA:

    2-NH2,6-(R1-N(-R2)-),9-(3,4,5-TRI(HO-)-2-TETRAHYDRO-

    PYRANYL)-9H-PURINE

    WHEREIN R1 IS HYDROGEN, A SUBSTITUTED OR UNSUBSTITUDED, SATURATED OR UNSATURATED, STRAIGHT OR BRANCHED CHAIN ALIPHATIC HYDROCARBON RADICAL, WHEREIN SAID SUBSTITUENT IS AT LEAST ONE OF AMINO, ALKYLAMINO, DIALKYLAMINO, ACYLAMINO, ALKOXY, ACYLOXY, HYDROXY, MERCAPTO, ALKYLMERCAPTO, CARBOXY, CARBOXY ALKYL OR CARBOXAMIDO AND R2 IS A SATURATED OR UNSATURATED CYCLOALKYL RADICAL WHICH CAN CARRY ENDOALKYLENE RADICALS OR ANNELLATED, SATURATED OR UNSATURATED CYCLIC ALIPHATIC HYDROCARBON RADICALS, WHEREIN SAID SUBA-X-3, WHEREIN A IS A SUBSTITUTED OR UNSUBSTITUTED, SATURATED OR UNSATURATED, STRAIGHT OR BRANCHED CHAIN, OR CYCLIC ALIPHATIC HYDROCARBON RADICAL, WHEREIN SAID SUBSTITUENT IS AT LEAST ONE OF HYDROXY, ACYLOXY, CARBOXY AND ARYL RADICALS, X IS A VALENCY BOND, AN OXYGEN OR SULFUR ATOM, ALKYLATED IMINO OR ACYLATED IMINO, AND B IS A SUBSTITUTED OR UNSUBSTITUTED ALKYL, ALKENYL, ARYL, FURYL, PYRIDYL, INDOLYL OR IMIDAZOLYL RADICAL, WHEREIN SAID SUBSTITUENT IS AT LEAST ONE OF HALOGEN, ALKYL, HALOALKYL, ALKOXY, ARYLOXY, ACYLOXY, HYDROXY, MERCAPTO, ALKYLMERCAPTO, NITRO, CARBOXY, CARBOXYLALKYL AND METHYLSULFONYLAMINO RADICALS.

    Preparation of nucleoside-5'-phosphoramidates
    9.
    发明授权
    Preparation of nucleoside-5'-phosphoramidates 失效
    核苷-5'-磷酰胺的制备

    公开(公告)号:US3575958A

    公开(公告)日:1971-04-20

    申请号:US3575958D

    申请日:1968-04-16

    申请人: AJINOMOTO KK

    IPC分类号: C07H1/02 C07D51/32 C07D51/54

    CPC分类号: C07H1/02 Y02P20/55

    摘要: NUCLEOSIDES OR 2'',3''-O-PROTECTED NUCLEOSIDES ARE READILY CONVERTED TO THE CORRESPONDING DICHLOROPHOSPHATES BY REACTION WITH PHOSPHORUS OXYCHLORIDE. THE DICHLOROPHOSPHATES, WHEN PARTLY HYDROLYZED TO THE MONOCHLOROPHOSPHATES, CAN BE REACTED WITH AMMONIA OR AMINES AT HIGH YIELDS TO THE AMMONIUM OR AMINE SALTS OF THE 5''-PHOSPHORAMIDATES IN A SOLVENT MEDIUM ESSENTIALLY CONSISTING OF TRIALKYL PHOSPHATES OR TRI-HALOALKYL PHOSPHATES.