Abstract: Disclosed are carbostyril derivatives and their salts of the formulas ##STR1## The compounds have anti-peptic ulcer effects, and are useful as a treating agent for curing peptic ulcers in the digestive system, such as ulcers in the stomach and in the duodenum. The compounds particularly have prophylaxis and curing effects for treating chronic ulcers, for example experimental acetic acid-induced ulcers and cautery ulcers, with both low toxicity and few side-effects. Also disclosed are processes for preparing the compounds and for preparing pharmaceutical compositions containing them.

Abstract: The invention relates to 5H-[1]benzopyrano-[2,3-d]pyrimidine derivatives of the general formula I ##STR1## which may be prepared by means of a new chemical process and have a protective effect similar to that of cimetidine, but do not exhibit the undesired side effects of antisecretory agents. The invention is based on a new mucoprotective mode of action which prevents lesions of the mucous membrane epithelium to arise.

Abstract: Phosphorus derivatives of 2-perfluoroalkyl-4-pyrimidinols which possess insecticidal properties are disclosed.

Abstract: This invention concerns novel water-soluble salts and compositions of the antitumor agent 4'-(9-acridinylamino) methanesulfon-m-anisidide (m-AMSA). More particularly, there are provided (1) the mono- and dipyroglutamate salts of m-AMSA and (2) compositions of m-AMSA with pyroglutamic acid. The novel salts and compositions provided enable m-AMSA to be administered as an aqueous solution without the necessity of using dimethylacetamide as a pharmaceutical vehicle.

Abstract: The compounds are of the class of 9-anilinoacridines, useful as antitumor agents and are analogs of m-AMSA. These compounds have the formula ##STR1## in which R.sup.1 is Br, Cl or CH.sub.3, and R.sup.2 is CH.sub.2 NHCH.sub.3, CH.sub.2 N(CHO)CH.sub.3 or CH.sub.2 NHCHO. Intermediate 3-substituted-9(10H)acridone-5-carboxylic acids are prepared by converting diphenylaminedicarboxylic acids via acyl chloride to dipiperidides, purifying the dipiperidides, treating said dipiperidides with phosphorous oxychloride in an inert organic solvent at a temperature in the range of about 70.degree. C. to 110.degree. C. to yield 9-acridine, subjecting said 9-acridine to mild acid hydroylsis to yield 9-acridone and thereafter hydroylzing said 9-acridones to the acid product.

Abstract: Substituted 9H-8-oxo-pyrimido[2,1-f]purine-2,4-diones their tautomers and salts are anti-inflammatory agents.Methods for their preparation and use are described.

Abstract: A new synthesis of 5-deazariboflavine is afforded by condensing N-D-ribityl-3,4-xylidine with a novel chemical intermediate, 6-chloro-5-formyluracil.

Abstract: Compounds of the formula ##STR1## wherein X is an amino acid or ester are useful hypotensive agents due to their angiotensin converting enzyme inhibition activity.

Abstract: Riboflavin of the formula I ##STR1## is prepared by condensing a 4,5-dimethyl-N-(D)-ribityl-2-phenylazoaniline of the formula II ##STR2## where R is H or --Cl, --NO.sub.2 or --CH.sub.3 in the o- or p-position, with barbituric acid of the formula III ##STR3## in the presence of an acid as the condensing agent, by an improved process in which the acidic condensing agent used is an aliphatic or cycloaliphatic/aliphatic tertiary carboxylic acid of the general formula IV ##STR4## where R.sup.1, R.sup.2 and R.sup.3 are each a lower alkyl group, R.sup.1, R.sup.2 and R.sup.3 together containing 3 to 20, preferably 3 to 10, carbon atoms, or R.sup.1 is a lower alkyl group, in particular methyl, and R.sup.2 and R.sup.3 together form a tetramethylene or pentamethylene group.The process can be particularly advantageously carried out using trimethylacetic acid or a commercial mixture of saturated tertiary carboxylic acids, e.g. Versatic .sup.R 10-acid.

Abstract: An improved process for the purification of crude riboflavin which has been prepared by condensation of an N-(D)-ribityl-2-arylazo-4,5-dimethylaniline and barbituric acid or another N-(D)-ribityl-4,5-dimethyl-aniline derivative with a barbituric acid derivative, by dissolving the crude riboflavin in sulfuric acid or phosphoric acid which has been diluted with water and oxidizing the impurities by treating the solution with hydrogen peroxide, or by dissolving the riboflavin in dilute nitric acid at elevated temperature and then isolating the pure riboflavin by precipitation with water, wherein the mineral acid solution of the riboflavin and the oxidizing agent or the solution of the riboflavin in 20 to 70% strength by weight nitric acid is heated extremely rapidly to a temperature at which the solution clearly changes color from greenish to yellow-orange, the solution is kept at this temperature for from 1 to 50, seconds and the oxidation reaction is then interrupted by addition of water.

Abstract: Novel carbostyril derivatives and their salts having antihistaminic effect and central nervous system controlling effect and are useful as antihistaminic agents and central nervous system controlling agents, represented by the general formula (1), ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkyl group, a phenyl-lower alkyl group, a lower alkenyl group, a lower alkynyl group; A is a group of the formula ##STR2## or a group of the formula ##STR3## (wherein R.sup.2 is a hydrogen atom or a lower alkyl group); B is a lower alkylene group; l is 1 when A is a group of the formula ##STR4## or l is 0 or 1 when A is a group of the formula ##STR5## Z is a group of the formula ##STR6## (wherein R.sup.

Abstract: Substituted 5H-pyrimido[5,4-b]indoles of Formula I ##STR1## wherein R.sup.2 is halogen; the oxadiazolyl group ##STR2## wherein R" is lower alkyl with up to 3 carbon atoms; C.sub.1-5 -alkyl, cycloalkyl, aralkyl, or aryl; OR.sup.I, SO.sub.n R.sup.I with n being 0, 1, or 2, or ##STR3## wherein R.sup.I is hydrogen, C.sub.1-5 -alkyl, cycloalkyl, aralkyl, or aryl; ##STR4## wherein R.sup.II and R.sup.III are hydrogen, C.sub.1-5 -alkyl, C.sub.3-5 -alkenyl, cycloalkyl, aralkyl, aryl, or, with the connecting N-atom, a 5- or 6-membered heterocyclic ring; andR.sup.A is hydrogen; the oxadiazolyl group ##STR5## wherein R" is lower alkyl with up to 3 carbon atoms; halogen, nitro, OR.sup.I, SO.sub.n R.sup.I with n being 0, 1, or 2, ##STR6## wherein R.sup.I is hydrogen, C.sub.1-5 -alkyl, cycloalkyl, aralkyl, or aryl; ##STR7## wherein R.sup.II and R.sup.III are hydrogen, C.sub.1-5 -alkyl, cycloalkyl, C.sub.3-5 -alkenyl, aralkyl, aryl, or, with the connecting N-atom, a 5- or 6-membered heterocyclic ring; orPO(OR).sub.

Abstract: Novel substituted 2-(arylmethoxy)phenol compounds having the structural formula: ##STR1## where X is selected from the group consisting of: (a) napthyl, pyridyl, quinolyl and 2-benzimidazolyl; and(b) a substituted alkyl or alkoxy phenyl.

Abstract: This disclosure relates to a class of novel 6-substituted-5-phenyltetrazolo[1,5-a][1,2,4]triazole [1,5-c]pyrimidines and to pharmaceutical compositions containing such compounds. The compounds and compositions disclosed are useful as renal vasodilators, diuretics and/or anti-hypertensive agents for the treatment of hypertensive disorders in humans.

Abstract: This invention is directed to phosphinylmethylaminocarbonyl imino acid compounds of the formula ##STR1## wherein X represents various unsubstituted or substituted imino acids or esters.

Abstract: Phosphorus-containing N-phenylsulfonyl-N'-pyrimidinylureas and N-phenylsulfonyl-N'-triazinylureas of the formula ##STR1## and the salts of these compounds with amines, alkali or alkaline earth metal bases or quaternary ammonium bases have good pre-emergence and post-emergence selective herbicidal and growth-regulating properties.In this formula, X is a group ##STR2## Y is hydrogen, halogen, C.sub.1 -C.sub.5 -alkyl, trifluoromethyl, C.sub.2 -C.sub.5, alkenyl, C.sub.2 -C.sub.5 -alkynyl, nitro, --COOR.sup.6 or --Q--R.sup.6, Z is nitrogen or the methine group, E is oxygen or sulfur, R.sup.1 is hydrogen or C.sub.1 -C.sub.5 -alkyl and R.sup.2 and R.sup.3 independently of one another are C.sub.1 -C.sub.3 -alkyl, C.sub.1 -C.sub.3 -alkoxy, C.sub.1 -C.sub.3 -halogenoalkyl, C.sub.1 -C.sub.3 -halogenoalkoxy, cyclopropyl, amino, methylamino or dimethylamino, and A is oxygen, sulfur, C.sub.1 -C.sub.5 -alkylene, C.sub.2 -C.sub.5 -alkenylene, C.sub.1 -C.sub.5 -halogenoalkylene or --NR.sup.7 --(CH.sub.2).sub.m --; --CH.sub.

Abstract: Phosphorus derivatives of 2-fluoroalkyl-5-pyrimidinols are taught. These compounds possess insecticidal properties and especially both systemic and foliar activity for plants against insect pest.

Abstract: Stable, biologically available, orally active 1,5-naphthalenedisulfonate salt of vinzolidine.

Abstract: 10-bromosandwicine and 10-bromoisosandwicine and acid addition salts thereof are disclosed. There novel compounds possess valuable pharmacological properties e.g. heart rhythm regulatory properties. Furthermore they are valuable intermediates for the preparation of 10-brominated N.sub.b -quaternary sandwicine derivatives which exhibit heart rhythm regulatory and adrenolytic properties. 10-bromosandwicine is prepared by brominating sandwicine and can subsequently be isomerized into 10-bromoisosandwicine.

Abstract: New quaternary derivatives of 10-bromoajmaline and 10-bromoisoajmaline are disclosed which exhibit antiarrhythmic and adrenolytic properties and which have the formula I ##STR1## wherein R represents a carbon-attached organic group containing 1 to 10 carbon atoms and A.sup.- represents an acid anion as well as pharmaceutical formulations thereof and processes and intermediates for their preparation.