Abstract: 2-(Substituted imino)thiazolidines and thiazolines are inhibitors of indoleamine-N-methyl transferase in vivo. They are prepared by alkylation or acylation of the free imino group.

Abstract: 2-Hydroxy-3-butynoic acid is disclosed which inhibits glycolic acid oxidase and thus is useful in the treatment and prevention of calcium oxalate urolithiasis (calcium oxylate kidney and bladder stone disease).

Abstract: [1-Oxo-2-aryl or thienyl-2-substituted-5-indanyloxy (or thio)]alkaoic acid, derivatives thereof, their salts, esters and amides are disclosed. The products display a dual pharmaceutical utility in that they exhibit diuretic, saluretic and uricosuric activity. Also disclosed are processes for the preparation of such [1-oxo-2-aryl or thienyl-2-substituted-5-indanyloxy (or thio)]alkanoic acids, pharmaceutical compositions comprising therapeutically effective amounts of such compounds and methods of treatment comprising administering such compounds and compositions.

Abstract: Novel interphenylene derivatives of 11,12-secoprostaglandins are prepared by the stepwise alkylation of the ethyl ester or the t-butyl ester of acetoacetic acid. One such method involves treatment of the t-butyl ester of acetoacetic acid with a strong base to form the anion followed by treatment with ethyl p-(3-bromopropyl)benzoate to produce ethyl 4-(4-tert-butoxycarbonyl-5-oxo-hexyl)benzoate, subsequently reacting the anion of the thus-formed benzoate with 1-chloro-4-acetoxynonane to produce ethyl 4-(4-acetyl-4-tert-butoxycarbonyl-8-acetoxytridecyl)benzoate followed by decarboxylation and alkaline hydrolysis to produce the desired product 4-(4-acetyl-8-hydroxytridecyl)benzoic acid which is useful as a pharmaceutical in the treatment of patients with renal failure and in the prevention of transplant rejection.

Abstract: The invention relates to novel 2,2-dioxo-1,2,3-benzoxathiazines substituted in the benzene nucleus, as well as the 3,4-dihydro analogs thereof, useful as anti-inflammatory, antipyretic, analgesic agents.

Abstract: 2,3-Dihydro-6,7-disubstituted-5-(acyl)benzofuran-2-carboxylic acids, the pharmaceutically acceptable salt, ester and amide derivatives thereof and combinations of these compounds with antikaluretic agents are disclosed having diuretic-saluretic, uricosuric and antihypertensive activity.

Abstract: The case involves novel 3-amino-N-[(phosphonoamino)iminomethyl]-6-halopyrazinecarboxamides, derivatives thereof and processes for preparing same. 3-Amino-N-(phosphonoaminoiminomethyl)-6-halopyrazinecarboxamides of the instant case are eukalemic agents possessing diuretic and natriuretic properties.

Abstract: Nuclear substituted 2-hydroxyphenylmethanesulfamic acids and their pharmaceutically acceptable salts wherein the phenyl nucleus is substituted with 2 to 4 nuclear substituents and which are useful saluretic-diuretics and anti-inflammatories are disclosed. The products may be prepared by reacting nuclear substituted salicylaldehydes with ammonium sulfamate to generate intermediate imines which are reduced to afford the compounds of this invention.

Abstract: Substituted 1,2-benzisoxazoles of the formula ##STR1## where: R.sup.1 and R.sup.3 =H or lower alkoxy;R.sup.2 =halo or .alpha.-branched lower alkyl;R.sup.4 =halo, halo lower alkyl, or lower alkylthio; provided, where R.sup.1 and R.sup.3 =H,R.sup.2 and R.sup.4 are other than simultaneously Cl or Br, which are active as antiinflammatory, antipyretic and analgesic agents, are derived from cyclodehydrating the corresponding salicylaldoximes with an isocyanate under extremely mild conditions.

Abstract: This invention relates to 9-thia- , 9-oxothia, and 9-dioxothia-11,12-seco-prostaglandins and processes for their manufacture. These compounds have prostaglandin-like biological activity and are particularly useful for the treatment of skin diseases such as psoriasis, for the prevention of thrombus formation, in stimulating the production of growth hormone in intact animals, and as regulators of the immune response.

Abstract: 6,7-Disubstituted-5-(acyl)benzofuran-2-carboxylic acids, the pharmaceutically acceptable salt, ester and amide derivatives thereof and combinations of these compounds with antikaluretic agents are disclosed having diuretic-saluretic, uricosuric and antihypertensive activity.

Abstract: Novel interphenylene derivatives of 11,12-secoprostaglandins are prepared by the stepwise alkylation of the ethyl ester or the t-butyl ester of acetoacetic acid. One such method involves treatment of the t-butyl ester of acetoacetic acid with a strong base to form the anion followed by treatment with ethyl p-(3-bromopropyl)benzoate to produce ethyl 4-(4-tert-butoxycarbonyl-5-oxo-hexyl)benzoate, subsequently reacting the anion of the thus-formed benzoate with 1-chloro-4-acetoxynonane to produce ethyl 4-(4-acetyl-4-tert-butoxycarbonyl-8-acetoxytridecyl)benzoate followed by decarboxylation and alkaline hydrolysis to produce the desired product 4-(4-acetyl-8-hydroxytridecyl)benzoic acid which is useful as pharmaceutical in the treatment of patients with renal failure and in the prevention of transplant rejection.

Abstract: The case involves novel pyrazine-2-carbonyloxyguanidines and processes for preparing same. The pyrazine-2-carbonyloxyguanidines are eukalemic or antikaliuretic agents possessing diuretic and natriuretic properties.

Abstract: The case involves novel N-pyrazinecarbonyl-N'-acylguanidines and processes for preparing same. The N-pyrazinecarbonyl-N'-acylguanidines are eukalemic agents possessing diuretic and natriuretic properties.

Abstract: Novel interphenylene derivatives of 11,12-secoprostaglandins are prepared by the stepwise alkylation of the ethyl ester or the t-butyl ester of acetoacetic acid. One such method involves treatment of the t-butyl ester of acetoacetic acid with a strong base to form the anion followed by treatment with ethyl p-(3-bromopropyl)benzoate to produce ethyl 4-(4-tert-butoxycarbonyl-5-oxo-hexyl)benzoate, subsequently reacting the anion of the thus-formed benzoate with 1-chloro-4-acetoxynonane to produce ethyl 4-(4-acetyl-4-tert-butoxycarbonyl-8-acetoxytridecyl)benzoate followed by decarboxylation and alkaline hydrolysis to produce the desired product 4-(4-acetyl-8-hydroxytridecyl)benzoic acid which is useful as a pharmaceutical in the treatment of patients with renal failure and in the prevention of transplant rejection.

Abstract: Organic chemical compounds based upon the naphthyridine molecule are disclosed which have potent gastric secretion inhibitory properties. The naphthyridinone is substituted with a substituted amino alkyl group at the 1-position, and variously substituted at the remaining positions. The compounds have profound effects on the inhibition of gastric secretions in the gastro-intestinal tract, and compositions for such uses are also disclosed.

Abstract: This invention relates to 9-thia-, 9-oxothia, and 9-dioxothia-11,12-seco-prostaglandins and processes for their manufacture. These compounds have prostaglandin-like biological activity and are particularly useful for the treatment of skin diseases such as psoriasis, for the prevention of thrombus formation, in stimulating the production of growth hormone in intact animals, and as regulators of the immune response.

Abstract: 2-R.sup.1 -Substituted-3-amino-R.sup.2 -substituted-1,2,5-thiadiazolium salts have broad spectrum antibacterial and antifungal activity. They are useful for cleansing inanimate surfaces as well as agents for agriculture.

Abstract: This invention relates to aryloxy-, alkoxy-, arylthio-, and alkylthio-11,12-seco-prostaglandins and to processes for their manufacture. These compounds have prostaglandin-like activity and are particularly useful in fertility control such as for estrus synchronization in animals and postcoital contraceptive agents in humans.

Abstract: 2,3-Dichloro-4-[(substituted sulfonyl)phenoxyl]-acetic acids and their salt, ester and amide derivatives thereof. The products are useful diuretic, saluretic and uricosuric agents. The acid products are prepared by treating a 2,3-dichloro-4-(2-substituted sulfonyl)phenol with a haloalkanoic acid or ester thereof and if the ester is employed hydrolyzing the ester.