摘要:
Compounds of the formula ##STR1## wherein R is methyl or ethyl,R.sub.1 is methyl, ethyl or ##STR2## and R.sub.2 is methyl, ethyl, ##STR3## where Alk is alkyl of 1 to 4 carbon atoms,Q is ethyl, propyl, isopropyl or 2-hydroxy-propyl,A is 3-phenoxy-2-hydroxy-propyl, where the phenyl ring is substituted in the o-position by hydroxy, methoxy, n-hexyloxy or benzyloxy,B is alkyl of 1 to 4 carbon atoms, phenyl, p-methyl-phenyl, 3-phenyl-3-hydroxy-isopropyl or A, as defined above, andn is an integer from 2 to 6, inclusive,Provided, however, that one of R.sub.1 and R.sub.2 must be methyl or ethyl and the other has one of the other respective meanings indicated; and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as the salts are useful as peripheral vasodilators.
Where R1 and R2 are alkyl of one to four carbon atoms or one of them is hydrogen, R3 is hydrogen or alkyl of one to two and n is 1 or 2 or a salt thereof. The compounds have outstanding broncholytic activity.
摘要:
THE PRESENT PYRIDINECARBONYL DERIVATIVES OF 7-(W-(NALKYL-N-OPTIONALLY HYDROXYALKYL SUBSTITUTED AMINO)-HYDROXYALKYL)THEOPHYLLINE POSSESS DIURETIC, BRONCHIOLAR DILATING, MYOCARDINAL STIMULATING, SMOOOTH MUSCLE RELAXING, LIPOTROPIC AND VASODILATING ACTIVITY AND ARE USEFUL AS CARDIOTONIC AGENTS. THE COMPOUNDS ARE PREPARED BY REACTION OF THE CORRESPONDING 7 - (W - (N-ALKYLAMINO)-HYDROXYALKYL) THEOPHYLLINE OR 7-(W-(N-ALKYL-(-HYDROXYALKYLAMINO)-HYDROXYALKYL)THEOPHYLLINE WITH A PYRIDINECARBOXYLIC ACID OR A REACTIVE DERIVATIVE THEREOF SUCH AS THE PYRIDINECARBONYL HALIDES. ALTERNATIVELY THE COMPOUNDS CAN BE PREPARED BY REACTION OF THEOPHYLLINE WITH THE APPROPRIATE PYRIDINECARBONYL DERIVATIVE OF AN W-(N-ALKYL-N-OPTIONALLY HYDROXYALKYL SUBSTITUTED AMINO)-HYDROXYALKYL HALIDE OR BY REACTION OF AN APPROPRIATE 7-(W-HALO-HYDROXYALKYL)THEOPHYLLINE DERIVATIVE WITH THE APPROPRIATE SECONDARY AMINE.
摘要:
(4-(3-(POLYAZAHETEROCYCLIC) ALKANOYL)PHENOXYL)ALKANOIC ACIDS, A CLASS OF COMPOUNDS POSSESSING DIURETIC AND SALURETIC PROPERTIES FOR USE IN TREATING CONDITIONS ASSOCIATED WITH ELECTROLYTE AND FLUID RETENTION AND PREPARED BY THE ADDITION OF A POLYAZAHETEROCYCLE TO A (4-(2-ALKYLIDENACYL)PHENOXY) ALKANOIC ACID IN THE PRESENCE OF A BASE FOLLOWD BY ACIDIFICATION TO PRECIPITATE THE PRODUCT.
摘要:
1.3 - DIMETHYL - 1.2.3,4-TETRAHYDROPYRIDO(2.1-F) PURINE2.4-DIONE IS PREPARED BY EXTRUDING SULFUR MONOXIDE FROM 1.3 - DIMETHYL - 1.2.3.4 - TETRAHYDROPYRIDO (1.2-B)-6-HPYRIMIDO(4,5-E)(1,2,4)THIADIAZINE-2.4.5-TRIONE. WHICH IS PREPARED BY TREATING 1,3-DIMETHYL-6-(2-PYRIDYLAMINO)URACIL WITH THIONY CHLORIDE. THE EXTRUSION PROVIDES A GENERAL ROUTE TO VARIOUS IMIDAZOLES, ESPECIALLY HETEROCYCLOIMIDAZOLES, THROUGH INTERMEDIATE 2H-1.2.4-THIADIAZINE-1OXIDES WHICH CAN BE PREPARED FROM N-VINYLAMIDINES. AN ALTERNATIVE ROUTE IS HEATING 1,3-DIMETHYL-5-HALO-6-(2PYRIDYLAMINO)URACIL. NOVEL 1,3-DIMETHYL-1,2,3,4-TETRAHYDROHETEROCYCLO(X,Y-F)PURINE-2,4-DIONES ARE USEFUL FOR A VARIETY OF BIOLOGICAL AND CHEMOTHERAPEUTIC PURPOSES.
摘要:
DIALKYL-XANTHINE DERIVATIVES INCLUDING THE PHARMACEUTICALLY ACCEPTABLE SALTS AND QUATERNARY AMMONIUM SALTS CHARACTERIZED BY THEIR CORONARY DILATING AND CENTRAL INHIBITING ACTIVITY AND HAVE THE FORMULA:
A-CH2-CH(-O-R1)-CH2-N WHEREIN A DESIGNATES A 1,3-DIMETHYL-XANTHINE OR A 3,7,DIMETHYL-XANTHINE RADICAL, R1 AND R2 EACH DESIGNATE HYDROGEN, AN ALIPHATIC, CYCLOALIPHATIC, HETEROCYCLIC OR AROMATIC ACYL RADICAL, X DESIGNATES ALKYLENE HAVING 2 TO 3 CARBON ATOMS AND Y DESIGNATES ALKYLENE HAVING 2 TO 4 CARBON ATOMS,
WHEREIN EACH TH IS 7-THEOPHYLINE OR 1-THEOBROMINE AND R2 IS SELECTRED FROM ALKYL AND HYDROXYALKYL GROUPS, WHEREIN EACH OF SAID ALKYL AND HYDROXYALKYL GROUPS IS A STRAIGHT OR BRANCHED CHAIN ALKYL CONTAINING 1-4 CARBON ATOMS.
WHEREIN X is oxycarbonyl, carboxyl or carbonyl and R is a lower alkyl group containing from 1 to 5 carbon atoms which have excellent coronary vasodilating effects are produced by reacting a compound having the formula
WHEREIN A is hydroxyl, or a carboxyl containing group or a halogenide, acid anhydride or ester thereof, with a compound having the formula
WHEREIN B is hydrogen, hydroxyl, or a carboxyl containing group or a halogenide, acid anhydride or ester thereof, and R is defined as before.
2-((CYCLOPENTYL)-N(-Y)-)-2-IMIDAZOLINE, OR 2-((CYCLO-
HEPTYL)-N(-Z)-)-2-IMIDAZOLINE
WHEREIN 1 IS 2,6-DICHLORO-PHENYL, 2-CHLORO-L-METHY6-PHENYL, 2CHLORO-4-METHYL-PHENYL, 2-METHYL-4-CHLORO-PHENYL,2CHLORO-PHENYL, 2,4-DICHLORO-PHENYL, 2-METHYL-PHENYL. 2,6-DIETHYL-PHENYL, 4-BROMO-PHENYL, 2,6- DICHLORO-4BROMO-PHENYL, 4-CYANO-PHENYL, 4-FLUORO-PHENYL OR 2-TRI FLUOROMETHYL-PHENYL, 2-METHOXY-4-CHLORO-PHENYL OR 2CHLORO-3-METHYL-PHENYL, AND Z IS
(2-CL,6-R7-PHENYL)-
WHERE R7 IS CHLORINE OR METHYL, AND THEIR NON-TOXIC, PHARMACOLOGICALLY ACCEPTABLE ACID ADDITION SALTS, THE COMPOUNDS AS WELL AS THEIR SALTS ARE USEFUL AS ANALGESICS.