Abstract: This invention provides thiadiazinone derivatives represented by the following formula (I) ##STR1## wherein R.sup.1 represents a hydrogen atom or C.sub.1 -C.sub.5 alkyl, R.sup.2 represents a 5- or 6-membered heterocyclic ring having (a) 1-3 nitrogen atoms, (b) a oxygen atom, (c) one sulfur atom, (d) 1-3 nitrogen atoms and one oxygen atom, or (e) 1-3 nitrogen atoms and one sulfur atom each of which rings may optionally be substituted by at least one substituent selected from the group consisting of C.sub.1 -C.sub.5 alkyl, cyano, hydroxy, C.sub.1 -C.sub.5 alkoxy, amino, C.sub.1 -C.sub.5 alkylamino, C.sub.2 -C.sub.6 dialkylamino, C.sub.2 -C.sub.5 acylamino, carboxyl, C.sub.2 -C.sub.5 alkoxycarbonyl and carbamoyl; or a pharmaceutically acceptable salt thereof. The compounds according to the present invention have an excellent cardiotonic activity, and are useful as active ingredients of a cardiotonic drug.

Abstract: Disclosed are antihypertensive pharmaceutical compositions and compounds which include the thiocarbamoylacetonitrile having the formula: ##STR1## wherein: R.sup.1 is selected from the group consisting of hydrogen, a C.sub.1 to C.sub.6 alkyl, a C.sub.3 to C.sub.6 cycloalkyl or --(CH.sub.2).sub.n --A (where A is selected from the group consisting of a C.sub.6 to C.sub.12 aryl, a 5- or 6-membered heterocyclic group or a fused heterocyclic group constituted by 9 or 10 atoms, each of which may be substituted by at least one substitute group selected from a C.sub.1 to C.sub.6 alkyl and a halogen and n is 0 or an integer of 1 to 6),R.sup.2 represents a C.sub.1 to C.sub.10 alkyl, and Ar represents an aryl, a 5- or 6-membered heterocyclic group or a fused heterocyclic group, each of which may be substituted by at least one substituent group selected from the group consisting of a C.sub.1 to C.sub.6 alkyl, a C.sub.1 to C.sub.6 alkoxy, a C.sub.2 to C.sub.7 alkylcarbonyl, a C.sub.7 to C.sub.

Abstract: A novel 1-phenylalkyl-3-phenylurea derivative represented by the following formula (I): ##STR1## wherein R.sup.1 and R.sup.5 represent independently hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.5 alkoxyl or halo; R.sup.2 represents hydrogen or C.sub.1 -C.sub.15 alkyl; R.sup.3 represents C.sub.1 -C.sub.15 alkyl or R.sup.3 represents together with R.sup.2 C.sub.2 -C.sub.9 alkylene; R.sup.4 and R.sup.5 represent independently C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxyl or halo; X represents oxygen or sulfur; Y represents --O--(CH.sub.2).sub.l --O-- wherein l is an integer of 1 to 3 or --(CH.sub.2).sub.p -- wherein p is an integer of 3 to 5; m is 0 or an integer of 1 to 5; and n is 0 or an integer of 1 to 3, is provided. The 1-phenylalkyl-3-phenylurea derivative (I) have the action of reducing cholesterol in blood by ACAT inhibition, and therefore, useful for treating hyperlipemia and atherosclerosis.

Abstract: Novel 1-phenylakyl-3-phenylurea derivatives represented by the following formula (I): ##STR1## wherein R.sup.1 is an alkyl group of 1 to 8 carbon atoms, an alkoxy group of 1 to 5 carbon atoms or a halogen atom, R.sup.2 is an alkyl group of 1 to 15 carbon atoms, each of R.sup.3 and R.sup.4 is independently an alkyl group of 1 to 5 carbon atoms, m is an integer of 1 to 3, and n is 0 or 1, are provided.The compounds are potent in reducing the cholesterol level in serum, and useful for treating hyperlipemia and atherosclerosis.

Abstract: There is disclosed an aminobenzenesulfonic acid derivative of the formula: ##STR1## wherein R.sub.1 represents hydrogen atom, a C.sub.1 -C.sub.6 alkyl group, a C.sub.3 -C.sub.7 cycloalkyl group, a C.sub.1 -C.sub.4 halogenated alkyl group, a halogen atom or a C.sub.6 -C.sub.12 aryl group, R.sub.2 represents hydrogen atom, a C.sub.1 -C.sub.6 alkyl group or a C.sub.7 -C.sub.12 aralkyl group which may have at least one substituent selected from cyano group, nitro group, C.sub.1 -C.sub.6 alkoxy groups, halogen atoms, C.sub.1 -C.sub.6 alkyl groups and amino groups, and n represents an integer of 1 to 4, of a pharmaceutically acceptable salt thereof.

Abstract: There are provided novel pyridazinone derivatives having the general formula (I): ##STR1## wherein A represents 5- or 6-membered heterocyclic ring having 1-3 nitrogen atoms, which may be substituted by at least one member selected from the group consisting of C.sub.1-5 alkyl, cyano, hydroxyl, C.sub.1-5 alkoxyl, amino, C.sub.1-5 alkylamino, C.sub.2-6 dialkylamino, C.sub.2-5 acylamino, carboxyl, C.sub.2-5 alkoxycarbonyl and carbamoyl, and R.sup.1 and R.sup.2 independently represent hydrogen atom or C.sub.1-5 alkyl or R.sup.1 and R.sup.2 may form together C.sub.1-5 alkylene, and salts thereof.

Abstract: Pyridazinone derivatives represented by the following general formula (I): ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 represent a hydrogen atom, hydroxy group or alkoxy group of not more than 5 carbon atoms, or two of R.sub.1, R.sub.2 and R.sub.3 may be combined together to form a group of --O--CH.sub.2 --O-- or --O--CH.sub.2 --CH.sub.2 --O--, R.sub.4 represents an alkyl group, n represents an integer of 0 to 4 and the dotted line represents a single or double bond, or salts thereof.

Abstract: There are provided novel pyridazinone derivatives having the general formula (I): ##STR1## wherein A represents 5- or 6-membered heterocyclic ring having 1-3 nitrogen atoms, which may be substituted by at least one member selected from the group consisting of C.sub.1-5 alkyl, cyano, hydroxyl, C.sub.1-5 alkoxy, amino, C.sub.1-5 alkylamino, C.sub.2-6 dialkylamino, C.sub.2-5 acylamino, carboxyl, C.sub.2-5 alkoxycarbonyl and carbamoyl, and R.sup.1 and R.sup.2 independently represent hydrogen atom or C.sub.1-5 alkyl or R.sup.1 and R.sup.2 may form together C.sub.1-5 alkylene, and salts thereof.

Abstract: A 7.alpha.-acylthio-4-en-3-oxosteroid such as 7.alpha.-acetylthio-17-hydroxy-3-oxo-17.alpha.-pregn-4-ene-21-carboxylic acid .gamma.-lactone (spironolactone) which is an antialdosteronic diuretic effective in therapy is prepared by contacting a steroidal material which contains a 7.beta.-acylthio-4-en-3-oxosteroid with a thiocarboxylic acid.

Abstract: An alkali metal salt of a 3-(17.beta.-hydroxyandrosten-3-one 3-acetal-17.alpha.-yl)propiolic acid which is useful as an intermediate in the preparation of 3-(3-oxo-7.alpha.-acetylthio-17.beta.-hydroxyandrost-4-en-17.alpha.-yl)-pr opiolactone (spironolactone) as antialdosteronic diuretics and hypotensive agents is prepared by reacting a 17.beta.-hydroxypregnen-20-yn-3-one 3-acetal (I) with an alkali metal dimsyl (II) to give an alkali metal salt of the 17.beta.-hydroxypregnen-20-yn-3-one 3-acetal (III), and reacting the compound (III) with carbon dioxide followed by hydrolysis.

Abstract: A steroidal 7.alpha.-acylthio-4-en-3-one is produced by adding a thiocarboxylic acid to a steroidal 4,6-dien-3-one in the presence of a strong acid in a neutral organic solvent.