Abstract: Compounds of the formula ##STR1## wherein m is the integer 1, 2 or 3; R is independently selected from the group C.sub.1 to C.sub.6 alkyl, C.sub.1 to C.sub.6 alkoxy, halo, trifluoromethyl and hydroxy when m is the integer 1, 2 or 3 and methylenedioxy when m is the integer 2; Z is hydroxymethylene, esterified hydroxymethylene, alkoxymethylene, alkylthiomethylene, carbonyl, or ketal-, thioketal- or hemithioketal- protected carbonyl, and the pharmaceutically acceptable acid addition salts thereof, are useful as anticonvulsants, anti-secretory agents and spermatocides.

Abstract: 1-Substituted imidazole derivatives exhibit spermatostatic and spermatocidal activity and are useful for contraceptive purposes both in male and female mammals.

Abstract: A unique crystalline form of flunisolide is prepared by crystallizing flunisolide from a solution of an alkanol of three or four carbon atoms, e.g. n-butanol, containing 0.2 to 5%, preferably 1.0 to 4.0% by volume water.

Abstract: Certain pregn-4-ene-3,20-diones or pregn-1,4-diene-3,20-diones 4-substituted with a fluoro or chloro are useful as topical anti-inflammatory steroids. These compounds are substituted at 9.alpha. with hydrogen, fluoro, chloro or bromo; at 6.alpha. with hydrogen, fluoro or chloro; at the 11 position with a keto, a .beta.-hydroxy or a .beta.-chloro (the latter only when there is a 9.alpha.-chloro); at 16.alpha., 17.alpha.-positions with isopropylidenedioxy or at 16.alpha.- (or 16.beta.) with methyl when 17.alpha. is hydroxy (or an ester); and at the 21-position with mono-fluoro, chloro, bromo, hydroxy or alkanoyloxy of 2-6 carbons or difluoro, dichloro, dihydroxy or dimethoxy.

Abstract: The compounds of the present invention are represented by the formula ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and are optionally substituted furyl or thienyl the substituents independently selected from the group halo, C.sub.1 to C.sub.6 alkyl and C.sub.1 to C.sub.6 alkoxy or optionally substituted phenyl the substituents independently selected from the group halo, C.sub.1 to C.sub.4 alkyl, C.sub.1 to C.sub.4 alkoxy and trifluoromethyl; X is oxygen or sulfur; m is the integer 0; and n is the integer 2 or 3; and the antimicrobial acid addition salts thereof, with the proviso that when either R.sup.1 or R.sup.2 is said optionally substituted phenyl the other R.sup.1 or R.sup.2 is said optionally substituted furyl or thienyl.The compounds are useful for combatting fungi, bacteria and protozoa. They also have spermatocidal and spermatostatic activity.

Abstract: Certain 16.beta.-methyl-3-oxoandrost-4-ene and 16.beta.-methyl-3-oxoandrosta-1,4-diene 17.beta.-thiocarboxylic acid esters are useful as anti-inflammatory steroids. These compounds are optionally substituted at the 6.alpha.-position with fluoro or chloro; optionally substituted at the 9.alpha. position with fluoro, chloro or bromo; substituted at the 11 position with a keto, a .beta.-hydroxy or a .beta.-chloro (the latter only when there is a 9.alpha.-chloro); and substituted with 17.alpha.-hydroxy (or an ester thereof).

Abstract: Certain 3-oxoandrost-4-ene and 3-oxoandrosta-1,4-diene 17.beta.-thiocarboxylic acid esters substituted at the 4-position with a fluoro or chloro, optionally substituted at the 6- position with fluoro or chloro and at 16.beta. with methyl are useful as anti-inflammatory steroids. These compounds are optionally substituted at the 9.alpha. position with fluoro, chloro or bromo; substituted at the 11 with a keto, a beta-hydroxy or a beta-chloro (the latter only when there is a 9.alpha.-chloro); when there is a 17.alpha.-hydroxy (or an ester).

Abstract: The biological activity of super agonist analogues of LH-RH is extended for long periods of time by incorporation of such analogues in a vehicle comprising an oil of vegetable origin and a gelling agent, preferably an aluminum mono-fatty acid ester. Pharmaceutical compositions thus formed are suitable for depot injection.

Abstract: The 2,3-diesters of 6-substituted-2,3-dihydroxy-1,4-naphthoquinones exhibit useful anti-psoriatic activity in mammals.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are the same or different and are hydrogen, C.sub.1 to C.sub.6 alkyl, C.sub.6 to C.sub.12 carbocyclic aryl or aralkyl of 1 to 6 carbon atoms in the alkyl moiety and 6 to 12 carbon atoms in the carbocyclic aryl moiety;R.sup.4 and R.sup.5 are the same or different and are hydrogen or C.sub.1 to C.sub.6 alkyl; andR.sup.6 and R.sup.7 are the same or different and are hydrogen, C.sub.1 to C.sub.6 alkyl or C.sub.1 to C.sub.6 alkoxy. Methods for preparing these compounds are also disclosed. The compounds are useful as antihypertensives and as diuretics. They also function as antihistamines and as bronchodilating agents and are therefore effective in inhibiting the effects of allergic reactions. They are also of use in the treatment of migraine and in the treatment of vasospastic disorders.

Abstract: Compositions containing and methods of employing as the essential ingredients substituted xanthone carboxylic acid compounds which are useful in the prevention of complications of diabetes. Methods for preparing these compounds and the compositions and intermediates therein are also disclosed.

Abstract: 1-Substituted imidazole derivatives exhibit spermatostatic and spermatocidal activity and are useful for contraceptive purposes both in male and female mammals.

Abstract: Nonapeptide and decapeptide analogs of LH-RH of the formula(pyro)Glu-His-V-Ser-W-X-Y-Arg-Pro-Z (I)and the pharmaceutically acceptable salts thereof wherein:V is tryptophyl, phenylalanyl or 3-(1-naphthyl)-L-alanyl;W is tyrosyl, phenylalanyl or 3-(1-pentafluorophenyl)-L-alanyl;X is a D-amino acid residue ##STR1## wherein R is (a) a carbocyclic aryl-containing radical selected from the group consisting of naphthyl, anthryl, fluorenyl, phenanthryl, biphenylyl, benzhydryl and phenyl substituted with three or more straight chain lower alkyl groups; or(b) a saturated carbocyclic radical selected from the group consisting of cyclohexyl substituted with three or more straight chain lower alkyl groups, perhydronaphthyl, perhydrobiphenylyl, perhydro-2,2-diphenylmethyl and adamantyl;Y is leucyl, isoleucyl, nor-leucyl or N-methyl-leucyl;Z is glycinamide or --NH--R.sup.1, whereinR.sup.1 is lower alkyl, cycloalkyl, fluoro lower alkyl or ##STR2## wherein R.sup.2 is hydrogen or lower alkyl,are disclosed.

Abstract: The tricyclic intermediate ##STR1## is prepared in a three step sequence from the bicyclic intermediate ##STR2## The key step of this process involves the addition of a Grignard reagent to a mixed anhydride. Tricyclic compound of formula (I) may be readily converted by known methods to valuable steroids.

Abstract: Novel 5-alkylsulfinylbenzoyl- and 5-alkylsulfonylbenzoyl,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acid compounds represented by the formula ##STR1## and the pharmaceutically acceptable, non-toxic esters and salts thereof, wherein n is 1 or 2, R is hydrogen or a lower alkyl group containing from 1-4 carbon atoms and R.sup.1 is a lower alkyl group having from 1-4 carbon atoms at the ortho, meta or para postions of the benzoyl group and process for the production of such compounds. These compounds are useful as anti-inflammatory, analgesic and antipyretic agents and as smooth muscle relaxants.

Abstract: Compositions containing and methods of employing as the essential ingredients substituted xanthone carboxylic acid compounds which are useful in the prevention of complications of diabetes. Methods for preparing these compounds and the compositions and intermediates therein are also disclosed.

Abstract: Psoriasis in mammals is relieved by topically administering substituted naphthaquinones of the formula: ##STR1## where R.sup.1 and R.sup.2 are the same or different and are hydrogen, hydroxy, alkoxy or acylamino and R.sup.3 is hydrogen, halo, cyano or alkoxy with the proviso that R.sup.1 and R.sup.2 are not both hydrogen.

Abstract: Compounds of the formula ##STR1## where R.sup.1 and R.sup.2 are the same or different and are phenyl optionally substituted with a substituent selected from the group C.sub.1 and C.sub.6 alkyl, C.sub.1 and C.sub.6 alkoxy and halo; or C.sub.4 or C.sub.5 heterocyclic aryl, the heteroatom selected from the group oxygen, nitrogen and sulfur; R.sup.3 and R.sup.4 are the same or different and are C.sub.1 to C.sub.6 alkyl; m is the integer 2 through 5; and X is selected from the group methanesulfonate, benzenesulfonate, p-toluene-sulfonate, nitrate, chloride, bromide and iodide. Methods for preparing these compounds are also disclosed. The compounds of the present invention are useful as anticholinergic agents.

Abstract: Compositions containing and methods employing, as the essential ingredient, novel substituted xanthone-2-carboxylic acid compounds which are useful in the treatment of allergic conditions. Methods for preparing these compounds and compositions and intermediates therein are also disclosed.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is phenethyl and R.sup.2 is phenyl, each of said phenethyl or phenyl independently being unsubstituted or substituted in the phenyl ring by from 1 to 3 substituents selected from the group consisting of halo, lower alkyl and lower alkoxy with the proviso that at least one of R.sup.1 and R.sup.2 be substituted by lower alkoxy; X is oxygen or sulfur; and the antimicrobial acid addition salts thereof are useful as antifungal, antibacterial and antiprotozoal agents.