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

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: 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.14 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 and R.sup.4 is selected from the group having the formula ##STR2## where R is C.sub.1 to C.sub.8 alkyl, C.sub.1 to C.sub.8 alkoxy, halo, cyano, AlkNHC(O)-- or AlkC(O)NH-- and R' is Alk NHC(O) or Alk C(O)NH where Alk is C.sub.1 to C.sub.6 alkyl or the group 2-(endobicyclo[3.1.0]hexyl)ethyl. Methods for preparing the compounds are disclosed. The compounds are useful for the treatment of hypertension and cardiac disorders.

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: 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: A method for preparing 4,5-dihydro-2-alkoxycarbonylamino-5-carbocyclic aryl imidazoles and substituted aryl derivatives thereof is disclosed. The compounds are prepared by treating a 1-(carbocyclic aryl)-2-(2',3'-bis-carboalkoxyguanidino) ethane of the formula ##STR1## where R is C.sub.1 to C.sub.6 linear or branched alkyl, R' is phenyl optionally substituted with the radial methylenedioxy or at least one hydroxy, halo, trifluoromethyl, C.sub.1 to C.sub.6 linear or branched alkoxy, or 1-naphthyl or 2-naphthyl and X is halo, mesyloxy or tosyloxy with a protic solvent solution or dispersion of an alkali metal or alkaline earth metal hydroxide, carbonate or alkoxide. 1-(Optionally substituted carbocyclic aryl)-2-(carboalkoxyguanidino) ethanes are also disclosed herein, such prepared by treating the above bis-carboalkoxyguanadino ethane with an aprotic solvent solution or dispersion of an alkali metal or alkaline earth metal hydroxide, carbonate or alkoxide.

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.

Abstract: Compounds of the formula ##STR1## where R.sup.1 and R.sup.2 are the same or different and are C.sub.1 to C.sub.6 alkyl; C.sub.5 or C.sub.6 cycloalkyl; C.sub.5 or C.sub.6 cycloalkenyl; phenyl optionally substituted with a substitutent selected from the group C.sub.1 to C.sub.6 alkyl, C.sub.1 to 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; Y is the radical selected from (CH.sub.2).sub.n, (C.sub.4 H.sub.8 S), (C.sub.4 H.sub.8 O) and ##STR2## where R is hydrogen or C.sub.1 to C.sub.6 alkyl and n is the integer 4 or 5; and X is selected from the group methanesulfonate, benzenesulfonate, p-toluenesulfonate, 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: Vicinal steroidal epoxides are prepared by reacting the corresponding vicinal steroidal bromohydrin with a heterocyclic base such as 1,5-diazabicyclo[4.3.0]non-5-ene or 1,5-diazabicyclo[5.4.0]-undec-5-ene.

Abstract: Certain 3-ketoandrost-4-ene and 3-ketoandrosta-1,4-diene 17 beta-carboxylic acids and esters substituted at the 6 alpha and 6 beta positions with fluorine substituents 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); substituted at 16 alpha (or 16 beta) with methyl or hydrogen when there is a 17 alpha-hydroxy (or an ester).

Abstract: This invention is a process for preparing 3-keto-androst-4-ene 17.alpha.-carboxylic acids, androsta-1,4-diene 17.alpha.-carboxylic acids and their 17.alpha.-esters by reacting a corresponding 21-hydroxypregn-4-ene-3,20-dione, 21-hydroxypregna-1,4-diene-3, 20-dione, or their 21-esters with an alkali metal carbonate base in a lower alkanol in the presence of oxygen. The 17.alpha.-esters are formed by reacting the 17.alpha.-carboxylic acid with a suitable alkylating agent.

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, chloro or bromo and optionally substituted at the six position with fluoro or chloro 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); substituted at 16 alpha,-17 alpha-positions with isopropylidenedioxy; and substituted at 16 alpha (or 16 beta) with methyl or hydrogen when there is a 17 alpha-hydroxy (or an ester).

Abstract: Certain 3-oxoandrost-4-ene and 3-oxoandrosta-1,4-diene 17 beta-thiocarboxylic acid esters are useful as antiinflammatory 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 on a beta-chloro (the latter only when there is a 9 alpha-chloro); substituted at 16 alpha, 17 alpha-positions with isopropylidenedioxy; and substituted at 16 alpha (or 16 beta) with methyl or hydrogen when there is a 17 alpha-hydroxy (or an ester).

Abstract: Certain 3-oxoandrost-4-ene and 3-oxoandrosta-1,4-diene 17 beta-thiocarboxylic acid esters substituted at the 6 alpha, 6 beta-positions with fluorine substituents 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); substituted at 16 alpha, 17 alpha-positions with isopropylidenedioxy; and substituted at 16 alpha (or 16 beta) with methyl or hydrogen when there is a 17 alpha-hydroxy (or an ester).

Abstract: 22-Optionally substituted steroids of the corticoid series are prepared from the corresponding 21-methylene steroids through the 20,21-dione steroid intermediates. These compounds have utility as anti-inflammatory agents.

Abstract: Novel 16-phenoxy and 16-(o, m or p)-substituted phenoxy derivatives of (dl)-9-keto-11.alpha.,15.alpha.-dihydroxy-17,18,19,20-tetranorprosta-4,5,1 3-trans-trienoic acid, the pharmaceutically acceptable, non-toxic lower alkyl esters and salts thereof and processes for the production of such compounds. These compounds possess prostaglandin-like activities and thus are useful in the treatment of mammals where prostaglandins are indicated. They are particularly useful as inhibitors of gastric acid secretion; and as agents for the control of asthmatic attack, because of their bronchodilating activity.

Abstract: 1-Alkylamino-3-(4-[(endobicyclo[3.1.0]hex-6-yl)alkylure ido]-1-phenoxy)-2-propanol and substituted derivatives thereof; 1-alkylamino-3-(4-[(endobicyclo[3.1.0]hex-6-yl)-alkylcarbonylamino]-1-phen oxy)-2-propanol and substituted derivatives thereof; and 1-alkylamino-3-(4-[(endobicyclo-[3.1.0]hex-6-yl)alkoxycarbonylamino]-1-phe noxy)-2-propanol and substituted derivatives thereof as well as methods for preparing such compounds are disclosed. 5-(4-[(Endobicyclo[3.1.0]hex-6-yl)alkylureido]-1-phenoxy) methyl-3-alkyl-2-optionally substituted oxazolidine and derivatives thereof; 5-(4-[(endobicyclo[3.1.0]hex-6-yl alkylcarbonylamino]-1-phenoxy)methyl-3-alkyl-2-optionally substituted oxazolidine and derivatives thereof; and 5-(4-[(endobicyclo[3.1.0]hex-6-yl)alkoxycarbonylamino]-1-phenoxy)methyl-3- alkyl-2-optionally substituted oxazolidine and derivatives thereof and methods for preparing these compounds are also 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: 1-Alkylamino-3-(3- or 4-[2-(endobicyclo[3.1.0]-hex-6-yl)ethylaminocarbonyl]-1-phenoxy)-2-propano l and substituted derivatives thereof and methods for preparing such compounds are disclosed. 5-(3- Or 4-[2-(endobicyclo[3.1.0]hex-6-yl)ethylaminocarbonyl]-phenoxy)methyl 3-alkyl-2-optionally substituted oxazolidine and derivatives thereof, and methods for preparing such compounds are also disclosed. These compounds exhibit cardiovascular acitivity and are useful in the treatment of abnormal heart condition as well as hypertension in mammals. The former compounds are prepared by treatment of the corresponding 1,2-epoxy-3-(3- or 4-[2-(endobicyclo[3.1.0]hex-6-yl)-ethylaminocarbonyl]phenoxy)propane with the desired alkylamine or by base or acid hydrolysis of the corresponding 5-(3- or 4-[2-(endobicyclo[3.1.0]hex-6-yl)-ethylaminocarbonyl)-3-alkyl oxazolidine. The latter compounds are prepared from the corresponding 1-alkylamino-3-(3- or 4-[2-(endobicyclo[3.1.