Abstract: Novel 19-oxygenated steroids of the 20-spiroxane series of the formula ##STR1## in which R.sup.3 is a lower alkyl radical carrying an oxygen-containing functional group and R.sup.4 is two hydrogen atoms or an oxo group, and which carry a double bond or a methylene group in the 6,7-position or carry a lower alkanoylthio group in the 7.alpha.-position, and the corresponding 17.beta.-hydroxy-21-carboxylic acids of the formula ##STR2## in which R.sup.3 is as defined above, and which carry a double bond or a methylene group in the 6,7-position, as well as salts thereof and 1,2-dehydro derivatives of all of these compounds are advantageous as potassium-saving diuretics in therapy since they antagonize the physiological effects of aldosterone but have only slight side effects on sexual functions of the body. The compounds are obtainable by conventional general preparation processes of steroid chemistry.
Type:
Grant
Filed:
October 3, 1977
Date of Patent:
April 17, 1979
Assignee:
Ciba-Geigy Corporation
Inventors:
Georg Anner, Hellmut Ueberwasser, Michel Biollaz, Peter Wieland
Abstract: 1-(Indolyl-3-alkyl)-3 or 4-(ureido or guanidino)-piperidines, e.g. those of the formula ##STR1## acyl derivatives and salts thereof are antihypertensive agents.
Abstract: 2-Piperidinoalkyl-1,4-benzodioxans, e.g. those of the formula ##STR1## R = H; alkyl; free, etherified or esterified OH or SH; CF.sub.3, NO.sub.2 or NH.sub.2x = y = 1-3R' = alkyl, iso- or heterocyclic aralkyl or arylR" = h, oh, alkoxy, alkenyloxy, alkynyloxy, or alkanoyloxyAnd acid addition salts thereof are neuroleptic agents.
Abstract: By incorporating solid drug substances into mixtures of higher alkanols and/or alkanoic acids melting above 25.degree. C, forming granules thereof and covering them with a prolamine, a pharmaceutical dosage form is obtained, which slowly and evenly releases the drug within the gastrointestinal tract of a mammal.
Abstract: New .alpha.-(cyclic tert. aminophenyl)-aliphatic acids, e.g. those of the formula ##STR1## AND FUNCTIONAL DERIVATIVES THEREOF, ARE ANTI-INFLAMMATORY AGENTS.
Abstract: 4-Amino-3-p-halophenylbutyric acids, acyl derivatives, esters and/or salts thereof reduce addiction liability, particularly that of narcotics, or the withdrawal symptoms observed after interruption of prolonged use of addicting agents, especially of narcotics.
Abstract: The present invention relates to anthelmintic preparations containing 4-(4-nitroanilino)-phenylisothiocyanate having a median of particle size of at most 10 .mu.m, particularly at most 5 .mu.m, and to the treatment of infections by parasitic helminthes, especially to the treatment of warm-blooded animals affected by shistosomiasis, hookworm infestation of filariasis, by administration of the preparations named above. Specific embodiments are suspensions of the active substance in triglycerides of medium saturated fatty acids, and mixtures of the active substance with a starch, particularly with maize starch.
Abstract: .alpha.-Phenoxyacetic acids, in which the .alpha.-position is substituted by an alkyl residue with 5 to 12 carbon atoms and the phenyl residue is substituted by a cycloaliphatic hydrocarbon residue which is unsaturated in the 1-position and is only singly unsaturated, and their esters and amides are useful as hypolipidaemic agents.
Abstract: New 1-(azacyclic aralkoxyphenyl)-2 or 3-(diphenylalkylamino)-alkanes, e.g. those of the formula ##STR1## Py=pyridyl unsubst. or subst. by 1-2 alkyl, alkoxy, F or Cl; Ph=phenyl unsubst. or subst. as Py or by CF.sub.3R.degree. =h or OH; m, n, p, =1 or 2Or therapeutically acceptable salts thereof, are hypotensive and cardioactive agents.
Abstract: 2-Pyrazolyl-benzophenones, e.g. those of the formula ##STR1## R = H or alkyl R.sup.o = H, alkyl, (HO, alkoxy, amino)-alkyl, aralkyl, or arylR', r" = h, alkyl, alkoxy, halo or CF.sub.3Am = open or cyclic aminoCorresponding ketals, or therapeutically useful acid addition salts thereof exhibit antianxiety and antidepressant effects.
Abstract: Phenylacetohydroxamic acids having the formula I ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4, independently of each other, represent hydrogen, chlorine, fluorine or bromine atoms or an alkyl or alkoxy group having at most 6 carbon atoms, and wherein R.sub.2 may additionally represent a trifluoromethyl group with the proviso that R.sub.1, R.sub.2 and R.sub.3 may not simultaneously represent hydrogen atoms and their pharmaceutically acceptable salts with bases, which compounds inhibit plateletaggregation and exhibit valuable pharmacological, in particular, antiphlogistic, analgesic and antipyretic activity.
Abstract: New 1-(azacyclic aralkoxyphenyl)-2- or 3-(diphenylalkylamino)-alkanes, e.g those of the formula: ##STR1## R = 5- or 6-membered, mono- or bicyclic, nitrogen-containing aromatic radicalM,n,p= 1-4; r = 1 or 2;R.sub.1 = h or OHor therapeutically acceptable salts thereof are hypotensive and cardioactive agents.
Abstract: 7-[3.alpha.-(3-hydroxy-3-hydrocarbylpropyl, or -1-propenyl, or 1-propynyl)-4-hydroxy-tetrahydro-2.beta.-furyl]-heptanoic or 4-heptenoic acids, esters or salts thereof are stable, prostaglandin-like acting agents.
Abstract: 7-[3.alpha.-(3-hydroxy-3-hydrocarbylpropyl, or -1-propenyl, or 1-propynyl)-4-hydroxy-tetrahydro-2.beta.-thienyl]-heptanoic or 5-heptenoic acids, sulfoxides, sulfones, esters or salts thereof are stable, prostaglandin-like acting and antiasthmatic agents.
Abstract: 7-[3.alpha.-(3-hydroxy-3-hydrocarbylpropyl, or -1-propenyl, or 1-propynyl)-4-hydroxy-tetrahydro-2.beta.-thienyl]-heptanoic or 5-heptenoic acids, sulfoxides, sulfones, esters or salts thereof are stable, prostaglandin-like acting and antiasthmatic agents.
Abstract: 1-(Indolyl-3-alkyl)-3 or 4-(ureido or guanidino)-piperidines, e.g. those of the formula ##STR1## R= H; alkyl; free, etherified or esterified OH or SH; CF.sub.3, NO.sub.2 or NH.sub.2m= 1-4; n= 2 or 3;X= O, S or NHacyl derivatives and salts thereof are antihypertensive agents.