Abstract:
WHERE R1 is hydrogen or lower alkyl; R2 is lower alkoxy(lower)alkyl, di(lower)alkylamino (lower)alkyl, halobenzyl or morpholino(lower)alkyl; and R1 and R2 taken together with the nitrogen of the sulfonamide group are piperidino, piperazino, phenylpiperazino and morpholino. The compounds have activity as central nervous system depressants.
The disclosure is directed to 9-oxoxanthene-N,N''bis(substituted)-2,7-disulfonamides which have the formula
Abstract:
This invention is directed to novel central nervous system depressants of Formula I:
wherein R1 is selected from the group consisting of (lower)alkyl and ar(lower)alkyl; R2 is selected from the group consisting of di(lower)alkylamino(lower)alkyl and diaryl(lower)alkylamino(lower)alkyl; R1 and R2 may be concatenated to form a radical selected from the group consisting of
WHEREIN R4 is selected from the group consisting of (lower)alkyl, aryl, hydroxy(lower)alkyl, ar(lower)alkyl and (lower)alkoxy(lower)alkyl; R5 is selected from the group consisting of (lower)-alkylamino and piperidino; n is an integer from 3 to 5; m is an integer from 1 - 2; r is an integer from 2 to 3; s is an integer from 0 to 6; t is an integer from 0 - 6; with the proviso that the sum of s and t is 3 to 6; R3 is selected from the group consisting of hydrogen, (lower)alkyl, ar(lower)alkyl and (lower)alkoxy(lower)alkyl; X is selected from the group consisting of halogen, cyano, trifluoromethyl, nitro and (lower)alkylthio; Y is selected from the group consisting of hydrogen, halogen, trifluoromethyl, nitro and (lower)alkylthio; and the pharmaceutically acceptable salts thereof, in addition to the method of their preparation and administration and administrable compositions containing the active compounds.
Abstract:
A NOVEL SERIES OF COMPOUNDS ARE DESCRIBED WHICH ARE BIOLOGICALLY ACTIVE AS INHIBITORS OF MYCOBACTERIUM TUBERCULOSIS. THE COMPOUNDS ARE CHARACTERIZED AS (5(7)-ACETAMIDO-3-(SUBSTITUTEDPHENYL)-2,3-DIHYDRO-3-HYDORXY - 7(5) - OXO - 7(5)H - THIAZOLO(3,2-A)PYRIMIDINE2-ALKANOIC ACID, ALKYL ESTERS.
R1 IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, HALOGEN, (LOWER) ALKYL, TRIFLUOROMETHYL, NITRO AND AMINO; R2 IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND (LOWER) ALKYL; R3 IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, HALOGEN, (LOWER)ALKYL, TRIFLUOROMETHYL, NITRO, AMINO, PHENYL, HALOPHENYL AND (LOWER)PHENYL; N IS AN INTEGER OF FROM 1 TO 3;
AND THE PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF.
Abstract:
2-AMINO PHENYLBENZLIDENEAMINOACETIC ACID N-OXIDES ARE REACTED WITH ETHYL CHLOROFORMATE TO PRODUCE THE CORRESPONDING (2 - BENZOYLPHENYLCARBAMOY)METHYL)HYDROXYCARBAMIC ACID, ETHYL ESTER, ETHYL CARBONATE. THE PRODUCTS ARE INTERMEDIATES IN THE PREPARATION OF 1,4BENZODIAZEPINE COMPOUNDS WHICH HAVE CENTRAL NERVOUS SYSTEM ACTIVITY.
Abstract:
THE INVENTION IS DIRECTED TO N-ARYL-A-OXOCYCLOPOLYMETHYLENE AMINES AND N-ARYL-A-IMINOCYCLOPOLYMETHYLENE AMINES WHICH ARE CENTRAL NERVOUS SYSTEM DEPRESSANTS.
Abstract:
4-PHENYLQUINAZOLINES ARE PREPARED BY REACTING A 2-AMINODIPHENYLMETHYLENEIMINOACETIC ACID N-OXIDE WITH A REACTANT SELECTED FROM THE GROUP OF LOWER ALKANOYL ANHYDRIDES AND HALO-(LOWER)ALKANOYL ANHYDRIDES TO FORM THE CORRESPONDING 2''-(A-(HYDROXYMETHYLIMINO)BENZYL)-(LOWER)ALKANOYL ANILIDE, ALKANOATE WHICH IS THEN CYCLIZED TO FORM THE 4-PHENYLQUINAZOLINES. THE PRODUCTS HAVE KNOWN PHARMACEUTICAL PROPERTIES WHICH RENDER THEM USEFUL AS MUSCLE RELAXANTS AND VASODILATORS.