Abstract:
Novel 4-(alkylaminoalkyl)-(4H)-thieno-(3,2-b)(f)-benzazepines of the formula WHEREIN R1 and R2 are selected from the group consisting of hydrogen, halogen, -CF3, lower alkoxy optionally substituted, lower alkylthio, lower alkyl, optionally substituted sulfonamido, diloweralkylamino and acylamino wherein the acyl is derived from an organic carboxylic acid of one to 18 carbon atoms, R is selected from the group consisting of hydrogen and lower alkyl, A is alkylene of two to five carbon atoms, optionally substituted by lower alkyl, B is selected from the group consisting of hydrogen, lower alkyl and arloweralkyl, C is selected from the group consisting of lower alkyl and arloweralkyl and B and C taken together are alkylene of two to six carbon atoms optionally interrupted with one or two heteroatoms, Y is selected from the group consisting of hydrogen, hydroxy, lower alkoxy and lower alkanoyloxy, X is hydrogen and taken together with Y forms a carbon-carbon double bond, Z'' is selected from the group consisting of hydrogen and lower alkyl and Z is selected from the group consisting of hydrogen, lower alkyl and lower alkoxy and taken with Y forms a member of the group consisting of 0, lower alkylenedioxy, loweralkylenedithio and thioloweralkyleneoxy and their non-toxic, pharmaceutically acceptable acid addition salts having antidepressant activity with a large therapeutic index and their preparation and novel intermediates.
Abstract:
P and Q being selected from the group consisting of alkyl aralkyl and aryl and the non-toxic, pharmaceutically acceptable addition salts when R and R'' are hydrogen, which possess notable anti-inflammatory activity and intense analgesic activity.
WHEREIN THE CF3 radical is in the seven or eight-position, R and R'' are hydrogen and taken together form a ketonide of the formula
Novel 4-(ortho-(2'',3''-dihydroxypropyloxycarbonyl)-phenyl)-aminoquinolines of the formula
(2-HAL,4-(R-OOC-Z-)PHENYL)-CH WHEREIN X IS SELECTED FROM THE GROUP CONSISTING OF OXYGEN, SULFUR, SO AND SO2, R IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, ANION OF A NON-TOXIC; THERAPEUTICALLY ACCEPTABLE ORGANIC OR MINERAL BASE AND RESIDUE OF AN ALCOHOL, AN Z IS SELCETED FROM THE GROUP CONSISTING OF -CHR1- AND >C=R2 WHEREIN R1 IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND STRAINGT OR BRANCHED ALKYL OF 1 TO 4 CARBON ATOMS, AND R2 IS A STRAIGHT OR BRANCHED ALKYLIDENE OF 1 TO 4 CARBON ATOMS AND HAL IS SELECTED FROM THE GROUP CONSISTING OF FLUORINE, BROMINE AND CHLORINE, WHICH COMPOUNDS WHICH CONTAIN AT LEAST ONE ASYMMETRIC CARBON ATOM CAN BE IN RACEMIC OR OPTICALLY ACTIVE GORM, AND THEIR PREPARATION WHICH COMPOUNDS HAVE ANALGESIC AND ANTIINFLAMMATORY ACTIVITY.
Abstract:
3-AMINO-4,4-DIHALO-5-PYRAZOLONES OF THE FORMULA
1-Y,3-(R-N(-R1)-),4,4-DI(X-),5-(O=)-2-PYRAZOLINE
WHEREIN X AND X'' ARE SELECTED FROM THE GROUP CONSISTING OF CHLORINE AND BROMINE, Y IS SELECTED FROM THE GROUP CONSISTING OF ALKYL, CYCLOALKYL AND ARYL WHICH MAY BE SUBSTITUTED AND R AND R1 ARE SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, ALKYL, ARYL, CYCLOALKYL AND ARALKYL WHICH POSSESS FUNGICIDAL ACTIVITY.
Abstract:
NOVEL SPRIO BENZOCYCLANE ACETIC ACID COMPOUND OF THE FORMULA WHEREIN R IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND LINEAR AND BRANCHED ALKYL OF 1 TO 4 CARBON ATOMS R1 IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, CHLORINE, TRIFLUOROMETHYL AND LOWER ALKOXY, Y IS SELECTED FROM THE GROUP CONSISTING OF METHYLENE, OXYGEN AND SULFUR, N IS 2,3, OR 4 AND R2 IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, SUBSTITUTED OR UNSUBSTITUTED ALKYL OF 1 TO 6 CARBON ATOMS AND CATION OF NONTOXIC, PHARMACEUTICALLY ACCEPTABLE MINERAL AND ORGANIC BASES. PROCESSES FOR THEIR PREPARATION AND NOVEL INTERMEDIATES. THE COMPOUNDS OF FORMULA 1 HAVE ANALGESIC AND ANTI-INFLAMMATORY PROPERTIES.
WHEREIN R1 AND R2 ARE SELECTED FROM THE GROUP CONSISTING OF HYDROGE, HALOGEN, -CF3, LOWER ALOXY OPTIONALLY SUBSTITUTED, LOWER ALKYLTHIO, LOWER ALKYL, OPTIONALLY SUBSTITUTED SULFONAMIDE, DILOWERALKYLAMINO AND ACYLAMINO WHEREIN THE ACYL IS DERIVED FROM AN ORGANIC CARBOXYLIC ACID OF 1 TO 18 CARBON ATOMS, R IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND LOWER ALKYL, A IS ALKYLENE OF 2 TO 5 CARBON ATOMS, OPTIONALLY SUBSTITUTED BY LOWER ALKYL, B IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, LOWER ALKYL AND ARLOWERALKYL, C IS SELECTED FROM THE GROUP CONSISTING OF LOWER ALKYL AND ARLOWERALKYL AND B AND C TAKEN TOGETHER ARE ALKYLENE OR 2 TO 6 CARBON TOMS OPTIONALLY INTERRUPTED WITH 1 OR 2 HETEROATOMS, Y IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, HYDROXY, LOWER ALKOXY AND LOWER ALKANOYLOXY, X IS HYDROGEN AND TAKEN TOGETHER WITH Y FORMS A CARBON-CARBON DOUBLE BOND, Z'' IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND LOWER ALKYL AND Z IS SELECTED FROM THE GROUP CONSISTING OF HYDROGN, LOWER ALKYL AND LOWER ALKOXY AND TAKEN WITH Y FORMS A MEMBER OF THE GROUP CONSISTING OF =O, LOWER ALKYLENEDIOXY, LOWER ALKYLENEDITHIO AND THIOLOWERALKYLENEOXY AND THEIR NON-TOXIC, PHARMACEUTICALY ACCEPTABLE ACID ADDITION SALTS HAVING ANTIDEPRESSANT ACTIVITY WITH A LARGE THERAPEUTIC INDEX AND THEIR PREPARATION AND NOVEL INTERMEDIATES.
WHEREIN A AND A'' ARE INDIVIDUALLY SELECTED FROM THE GROUP CONSISTING OF LOWER ALKOXY AND LOWR ALKYLTHIO AND TAKEN TOGETHER ARE SELECTED FROM THE GROUP CONSISTING OF LOWER ALKYLENEDIOXY, LOWWE ALKYLENEDITHIO AND THIOLOWERALKYLENEOXY, R IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND LOWER ALKYL AND R1 AND R2 ARE INDIVIDUALLY SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, HALOGEN, -CF3, OPTIONALLY SUBSTITUTED LOWER ALKOXY, LOWER ALKYLTHIO, OPTIONALLY SUBSTITUTED SULFONAMIDO, DILOWERALKYL AMINO, AND ACYLAMINO WHERE THE ACYL IS DERIVED FROM AN ORGANIC CARBOXYLIC ACID OF 1 TO 18 CARBON ATOMS WHICH ARE INTERMEDIATES FOR 4-(ALKYLAMINOALKYL)-(4H)-THIENO(3,2-B) (F)-BENZAZEPINES HAVING ANTIDEPRESSANT ACTIVITY AND THE PROCESS FOR THE THEIR PREPARATION AND NOVEL INTERMEDIATES.
IN WHICH R1 AND R2 ARE IDENTICAL OR DIFFERENT AND REPRESENT AN ALKYL RADICAL CARRYING FROM 1 TO 6 CARBON ATOMS, AND THEIR ORGANIC OR MINERAL BASE SALTS, AND THEIR USE AS ANTI-CONVULSANT AGENTS. NOVEL MALONYUREAS OF THE FORMULA
Abstract:
Racemates and optically active isomers of benzoylphenylacetic acid esters of the formula
WHEREIN R is selected from the group consisting of hydrogen and alkyl of one to seven carbon atoms, R1 and R2 are hydrogen or taken together are
P and Q being alkyl of one to five carbon atoms and the two benzene rings may be optionally substituted with at least one member of the group consisting of chlorine, fluorine, bromine, trifluoromethyl and alkyl and alkoxy and alkylthio of one to seven carbon atoms, intermediates and process for their preparation and their use as analgesics and antiinflammatory agents.