WHEREIN R1 REPRESENTS METHOXY, HYDROXY, OR AN ACYLOXY GROUP, WITH THE PROVISO THAT TWO R1 GROUPS MAY TOGETHER FORM A ALKYLENEDIOXY GROUP, M IS AM INTEGER OF 1 TO 3, EACH R2 REPRESENTS AN ALKYL GROUP HAVING AT MOST 4 CARBON ATOMS, AND R4 STANDS FOR HYDROGEN, AN ALIPHATIC OR CYCLOALIPHATIC GROUP HAVING AT MOST 6 CARBON ATOMS, AN ARALKYL GROUP HAVING UP TO 10 CARBON ATOMS, AN ALKYLAMINOCARBONYLALKYL OR MONO-OR DI-ALKYLAMINOALKYL GROUP WHEREIN THE ALKYL HAS AT MOST 3 CARBON ATOMS, ALKYLCARBONYL OF UP TO 5 CARBON ATOMS, CYCLOPROPYLCARBONYL, BENZOYL, PHENYLACETYL, TOSSYL OR TETRAHYDROFURFURYL GROUP, ARE NON-NARCOTIC ANALGESIC COMPOUNDS.
IN WHICH R1 AND R2 ARE HYDROGEN, HALOGEN OR NITRO, WHICH INVOLVES REACTING AN ANTHRANYL COMPOUND OF THE FORMULA
3-(R2-PHENYL),R1-2,1-BENZISOXAZOLE
WHEREIN R1 AND R2 HAVE THE SIGNIFICANCES ABOVE WITH (2) AN ACID SALT OF GLYCINE ESTER, SAID REACTION BEING CARRIED IN THE PRESENCE OF AN ORGANIC BASE UNDER HEATING. THE FINALLY PRODUCED BENZODIAZEPINE COMPOUNDS HAVE EXCELLENT PHARMACOLOGICAL PROPERTIES AND MAY SPECIFICALLY BE USED AS SEDATIVE AGENTS.
Abstract:
SALTS OF N-PHENYL-N-(2-PYRIDYLMETHYL)-2-(N-PIPERIDINO)-ETHYLAMINE WITH A SATURATED FATTY ACID HAVING 14 TO 22 CARBON ATOMS OR WITH HYDROXYPHENYL-BENZOYLBENZOIC ACID ARE ANTITUSSIVE AGENTS.
Abstract:
The process for preparing benzodiazepin-2-one derivatives of the formula
WHEREIN R1 is hydrogen or lower alkyl, and rings A and B are either unsubstituted or substituted by one or more groups of nitro, trifluoromethyl, halogen, alkyl and alkoxy groups, which comprises subjecting a 2-amino- Alpha phenylbenzylideneaminoacetal derivative to ring-closure, hydrolyzing the resultant product to obtain the 2hydroxybenzodiazepine derivative, and subjecting such derivative to oxidation to yield the benzodiazepin-2-one derivative. Also provided are novel 1-alkyl-2-hydroxybenzodiazepine derivatives of the formula
WHEREIN R''1 is lower alkyl and rings A and B may be either unsubstituted or substituted as defined above, such derivatives being useful as intermediates in the above process and also as tranquilizing agents.
Abstract:
WITH A COMPOUND OF THE FORMULA Compounds of the formula
WHEREIN R1 has the same meaning as above and the respective benzene rings A and B may have one or more substituents as defined above to a ring closure reaction. Compounds of the formula II are produced by reacting a compound of the formula
WHEREIN R1 is hydrogen or alkyl and the respective benzene rings A and B may have one or more substituents which are the same or different and selected from the group consisting of halogen, nitro, trifluoromethyl, alkyl and alkoxy are prepared by subjecting a compound of the formula
WHEREIN R1 has the same meaning as defined above and R2 is hydrogen, alkyl, hydroxyalkyl or aralkyl with aminoacetonitrile. Compounds of the formula III are produced by reacting a compound of the formula
Abstract translation:式WHERE R1的化合物是氢或烷基,相应的苯环A和B可以具有一个或多个相同或不同的取代基,选自卤素,硝基,三氟甲基,烷基和烷氧基,通过使 式WHEREIN R 1具有与上述相同含义的化合物,并且相应的苯环A和B可具有一个或多个如上定义的取代基进行闭环反应。 通式II的化合物通过使式WHEREIN R 1具有与上述相同的含义并且R 2是氢,烷基,羟基烷基或芳烷基与氨基乙腈反应来制备。 式III的化合物通过使下式的化合物与其中R2是氢,烷基,羟基烷基或芳烷基的式R2NH2的化合物反应来制备。
Abstract:
BENZODIAZEPHINE DERIVATIVES OF THE FORMULA
1-R1,2-(R2-NH-C(=Y)-N=),5-PHENYL(B)-1,2-DIHYDRO-
3H-1,4-BENZODIAZEPINE OR =BOND IN 1-2 POSITION
WHEREIN R1 IS HYDROGEN OR ALKYL, R2 IS A HYDROCARBON GROUP, Y IS OXYGEN OR SULFUR ATOM AND THE RESPECTIVE BENZENE RINGS A AND B MAY HAVE ONE OR MORE SUBSTITUENTS FROM THE GROUP OF NITRO, TRIFLUOROMETHYL, HALOGEN, ALKYL AND ALKOXY, AND THEIR 4 N-OXIDES, AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, ARE USEFUL TRANQUILIZING, MUSCLE RELAXANT AND ANTICONVULSANT AGENTS.
Abstract:
THE MORPHOLINE AND PIPERAZINE SALTS OF TRANS-DIHYDROXYBIS-HYDROXYCARBONYLETHYLENE (DIHYDROXY) FUMARIC ACID) ARE USEFUL AS ANTIPYRETIC, ANALGESIC AND ANTI-INFLAMMATORY AGENTS OF LOW TOXICITY. UNLIKE ACETYL SALICYLIC ACID, THEY CAUSE NO GASTROENTERIC DISORDERS; UNLIKE DIHYDROXY FUMARIC ACID THEY ARE STABLE TO ELEVATED TEMPERATURE AND HUMIDITY.