Abstract: Disclosed are monoacyl and diacyl derivatives of rapamycin, processes for their preparation, methods of using the derivatives and pharmaceutical compositions of the derivatives. The derivatives are useful, inter alia, as antifungal antibiotics.

Abstract: A 1,2,3,4-tetrahydroisoquinoline having smooth muscle relaxant activity of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each hydrogen or lower alkyl and X is --O-- or --S--, and pharmaceutically acceptable salts thereof.

Abstract: 1-Difluoromethyl-6,7-methylenedioxy-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid and certain of its alkylaminoalkyl esters, useful in treating bacterial infections in mammals.

Abstract: Isoquinolines of the formula ##STR1## of which representative compounds are such as 3-N-methylpiperazino-1-phenyl-isoquinoline-4-aldehyde, 3-N-methylpiperazino-1-(2-fluorophenyl)-isoquinoline-4-aldehyde, or 3-N-[3-(4-fluoro-benzoyl)-propyl]-piperazino-1-phenyl-isoquinoline-4-aldeh yde and medicaments containing the isoquinolines which are useful as antidepressants.

Abstract: Isoquinolines of the formula ##STR1## in which R.sub.1 is piperidino, piperazino or piperazino N-substituted thereof by alkyl of 1 to 4 carbon atoms, alkylene of 1 to 4 carbon atoms wherein said alkylene is substituted in turn by fluorobenzoyl, or CHO; R.sub.2 is phenyl or phenyl substituted by alkyl of 1 to 4 carbon atoms, halogen, amino or nitro; and R.sub.3 is hydrogen or halogen, a process for their preparation and medicaments containing the isoquinolines, especially the use of said medicaments as antidepressants.

Abstract: Disclosed are compounds which are 4-hydroxy-2-quinolinone-3-carboxylic acids and salts thereof, e.g., 1-allyl-6,7-dimethoxy-4-hydroxy-2-quinolinone-3-carboxylic acid, useful as anti-allergic agents, and prepared by hydrolysis of the corresponding carboxylic acid esters.

Abstract: Disclosed are compounds which are 4-hydroxy-2-quinolinone-3-carboxylic acid esters, e.g., 1-methyl-4-hydroxy-2-quinolinone-3-carboxylic acid ethyl ester, useful as anti-allergic agents and intermediates for 1-alkyl-4-alkoxy-quinolin-2(1H)-ones, and prepared by reacting an isatoic anhydride with an alkali metal salt of a malonic ester.

Abstract: Isoquinoline derivatives of the formula ##STR1## wherein the substituent is such as chlorine or bromine; R.sub.1 is phenyl etc.; R.sub.2 is hydrogen, halogen etc.; R.sub.3 is e.g. aminoalkyl and their use as medicaments, in particular as antidepressants.

Abstract: Isoquinoline-4-aldehydes of the formula ##STR1## in which X denotes bromine or chlorine, R.sub.1 is phenyl optionally mono- or disubstituted by halogen, hydroxy, nitro, amino, or amino substituted by one or two aliphatic, cycloaliphatic or aromatic hydrocarbon radicals having from 2 to 18 carbon atoms, the nitrogen atom possibly being included in a heterocyclic ring, acyl amino, alkyl or alkoxy each having from 1 to 6 carbon atoms, benzoyloxy, or trifluoromethyl, or is pyridyl or thienyl;R.sub.2 is hydrogen, halogen, hydroxy, alkyl or alkoxy having from 1 to 6 carbon atoms, nitro, amino, benzyloxy, methylene dioxy or ethylene dioxy andm is 1 or 2;which are effective in the treatment of spasms and as tranquilizers.

Abstract: Imidazolylethoxymethyl derivatives of dioxoloquinolines having the general formula ##STR1## and their acid addition salts are useful as antifungal and antibacterial agents.

Abstract: The reaction of isatoic anhydrides with malononitrile in a reaction-inert solvent in the presence of a base to produce 2-amino-3-cyano-4-hydroxy-quinolines and 2-amino-.alpha.,.alpha.-dicyanoacetophenones which are then hydrolyzed and decarboxylated under acid or base conditions to produce 2-amino-4-hydroxy-quinolines, useful as intermediates for preparation of 1-oxo-1H-6-alkoxy-pyrimido[1,2-a]quinoline-2-carboxylic acids and esters of value as antiallergy agents.

Abstract: Imidazolylethoxymethyl derivatives of dioxoloquinolines having the general formula ##STR1## and their acid addition salts are useful as antifungal and antibacterial agents.

Abstract: 1-Difluoromethyl-6,7-methylenedioxy-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid and certain of its alkylaminoalkyl esters, useful in treating bacterial infections in mammals.

Abstract: Anti-allergic 4-hydroxy-3-nitro-quinoline-2(1H)-ones are prepared by reacting an isatoic anhydride with the carbanion resulting from the treatment of nitro acetic acid alkyl esters with a proton abstracting agent.

Abstract: Pyridobenzodioxin compounds, which are useful as pharmacological agents, especially as agents for the treatment of senility and reversal of amnesia, and methods for their preparation are disclosed. Pharmaceutical compositions containing said compounds and methods for using said compositions in treating senility and reversal of amnesia are also taught.

Abstract: The reaction of isatoic anhydrides with malononitrile in a reaction-inert solvent in the presence of a base to produce 2-amino-3-cyano-4-hydroxyquinolines and 2-amino-.alpha.,.alpha.-dicyanoacetophenones which are then hydrolyzed and decarboxylated under acid or base conditions to produce 2-amino-4-hydroxyquinolines, useful as intermediates for preparation of 1-oxo-1H-6-alkoxypyrimido[1,2-a]quinoline-2-carboxylic acids and esters of value as antiallergy agents.

Abstract: Hydroxypyridine carbamates of the formula ##STR1## wherein R.sub.1 to R.sub.5 as defined below are valuable insecticides and particularly aphicides andCompounds of the formula ##STR2## wherein one of R'.sub.1 and/or R'.sub.3 are substituted carbamoyl and the other is preferably hydrogen or methyl, R'.sub.2 is a variety of substituents among which is hydrogen and acetyl, and R'.sub.3 and R'.sub.4 preferably form together a saturated or unsaturated C.sub.4 -chain which may be substituted, are valuable aphicides.

Abstract: A compound having one of the structural formulae: ##STR1## AND HYDROGENATED, CHLORINATED AND BROMINATED DERIVATIVES THEREOF; ##STR2## WHEREIN R is H or lower alkyl; ##STR3## WHEREIN X is Cl or Br and n is an integer from 0 to 6; ##STR4## WHEREIN X is Cl or Br and m is an integer from 0 to 8; ##STR5## AND HYDROGENATED, CHLORINATED AND BROMINATED DERIVATIVES THEREOF; AND, ##STR6## USEFUL AS INSECTICIDES.

Abstract: Racemic and optically active compounds of the formulaQ--C.sub.n H.sub.2n --NH--Rwherein Q is ##STR1## where R.sub.1 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, trifluoromethyl or amino,R.sub.2 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms or trifluoromethyl,R.sub.1 and R.sub.2, together with each other, are methylenedioxy or ethylenedioxy, andA is --O--, --CH.sub.2 --CH.sub.2 --, --O--CH.sub.2 -- where the oxygen is bonded to the benzene ring, or --NR.sub.3 -- where R.sub.3 is hydrogen or alkyl of 1 to 4 carbon atoms,N is an integer from 2 to 6, inclusive, andR is hydrogen, benzyl or ##STR2## where R.sub.4 is hydrogen, methyl or ethyl,R.sub.5, r.sub.6 and R.sub.7, which may be identical to or different from each other, are each hydrogen, halogen, hydroxymethyl, trifluoromethyl, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, nitro, cyano, --CONHR.sub.3, --CONHOH, --COOR.sub.3, R.sub.

Abstract: 1-Difluoromethyl-6,7-methylenedioxy-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid and certain of its alkylaminoalkyl esters, useful in treating bacterial infections in mammals.

Abstract: Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.6, which may be identical to or different from each other, are each hydrogen or lower alkyl;R.sub.3 is lower alkoxy;R.sub.4 is lower alkoxy or, together with R.sub.3, methylenedioxy or ethylenedioxy;R.sub.5 is hydrogen, lower alkyl or benzyl;R.sub.7 is hydrogen or lower alkoxy;R.sub.8 is hydrogen, lower alkoxy or, together with R.sub.7, methylenedioxy or ethylenedioxy;M is 1 or 2; andN is 2 or 3;And non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antihypertensives and heart rate reducers.

Abstract: Triglycerides carrying an anti-bacterial drug moiety in the 2-position and a hydrocarbon acyl moiety in the 1- and 3-positions exhibit excellent anti-bacterial properties without causing the side effects often associated with oral antibiotics when used by themselves.

Abstract: Anti-allergic 4-hydroxy-3-sulfonyl-quinolin-2(1H)-ones are prepared by reacting an isatoic anhydride with the carbanion resulting from the treatment of sulfonyl acetic acid alkyl esters with a proton abstracting agent.

Abstract: 4-Acetoxy-1,2,3,4-tetrahydro-2,2-dimethyl-6,7-methylenedioxyisoquinolinium iodide is useful as a gastric acid antisecretory agent.

Abstract: Anti-allergic 4-hydroxy-3-sulfinyl-quinolin-2(1H)-ones are prepared by reacting an isatoic anhydride with the carbanion resulting from the treatment of sulfinyl acetic acid alkyl esters with a proton abstracting agent.