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.
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.
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.
ARE DISCLOSED WHEREIN R1 IS HYDROGEN OR LOWER ALKYL AND R2 IS A HYDROCARBON RESIDUE OR A HETEROCYCLIC, EACH OF WHICH MAY BE OPTIONALLY SUBSTITUTED, OR R1 AND R2 TAKEN TOGETHER WITH THE ADJOINING CARBON ATOM CONSTITUTE INDANIDENE OR N-METHYLBENZOTHIAZOLIDENE. THESE COMPOUNDS ARE USEFUL AS HYPOTENSIVE AGENTS.
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.
摘要:
CLEAR, NON-PARTICULATE, FREE-FLOWING, STERILE, AQUEOUS SOLUTIONS OF POLYINOSINIC:POLYCYTIDILIC ACID COMPLEXES SUITABLE FOR MEDICINIAL APPLICATION ARE PREPARED BY AN IMPROVED PROCESS.
摘要:
2-MERCAPTOINOSINE IS OBTAINED IN A HIGH YIELD BY REACTING UNDER MILD REACTION CONDITIONS 5-AMINO-1-B-D-RIBOFURANOSYL-4-IMIDAZOLECARBOXAMIDE WITH AN ISOTHIOCYANATE HAVING THE FORMULA:
摘要:
NOVEL 2-AMINO-ADENOSINE DRIVATIVES CHARACTERIZED BY CARDIAC AND CIRCULATORY ACTIVITY AND BY THEIR HIGH CORONARY SPECIFICITY HAVING THE FOLLOWING STRUCTURAL FORMULA:
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.
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.
摘要:
THIS INVENTION RELATES TO 5''-CYCLIC ESTERS OF 3''-DEOXY-3''DIHYDROXYPHOSPHINYLMETHYL - B-D-RIBOFURANOSYL NUCLEOSIDES AND 2''-CYCLIC ESTERS OF 3''-DEOXY-3''-DIHYDROXYPHOSPHINYLMETHYL-B-D-RIBOFURANOSYL NUCLEOSIDES WHICH ARE VALUABLE PHARMACOLOGICAL AGENTS. FOR EXAMPLE, THEY ARE USEFUL IN REGULATING AND CONTROLLING METABOLISM AND FOR PRODUCING METABOLIC DEFICIENCIES '' IN BIOLOGICAL SYSTEMS. THIS INVENTION ALSO RELATES TO 3-PHODPHINYLMETHYLFURANOSE AND 3'' - DEOXY-3'' -DIHYDROXYPHOSPHINYLMETHYL-B-D-RIBOFURANOSYL NUCLEOSIDE INTERMEDIATES FOR PREPARING THESE CYCLIC ESTERS.