Abstract: The present invention relates to novel hydantoin derivatives, processes for producing said hydantoin derivatives, pharmaceutical compositions containing at least one of said hydantoin derivatives as aldose reductase inhibitors and novel intermediate compounds in the synthesis of said hydantoin derivatives.The present invention is based on the selection of a hydantoin which is bonded by a sulfonyl group to various substituents at the 1-position of the hydantoin skeleton.The compounds of the present invention have a strong inhibitory activity against aldose reductase. These compounds are extremely useful for the treatment and/or prevention of various forms of diabetic complications based on the accumulation of polyol metabolites.

Abstract: 9.alpha.-Hydroxy-19,11.beta.-bridged steroids of general formula I ##STR1## are described. The more detailed meaning of A, B, R.sup.1, R.sup.2, G, Z, R.sup.4 --Y and R.sup.4' --Y' follows from the description. The steroids of general formula I have antigestagen and/or antiglucocorticoidal action and can be used for the production of pharmaceutical agents.

Abstract: Anti-inflammatory 4-substituted 2-furanones are made from intermediates having the formulas: ##STR1## in which R.sub.1, R.sub.2 and R.sub.3 independently are n-alkyl of 1 to 6 carbons, or branched chain alkyl of 1 to 6 carbons; X is H, OH, NH.sub.2, I or Br; R.sub.4 is H, alkyl of 1-20 carbons, phenyl[C.sub.1 -C.sub.20 alkyl], naphthyl[C.sub.1 -C.sub.20 alkyl], CH.sub.2 OH, CH.sub.2 NH.sub.2, CH.sub.2 CH.sub.2 OH, CH.sub.2 --CHO, CH.sub.2 --COOH or CH.sub.2 --COOR.sub.5, and R.sub.5 is alkyl of 1 to 6 carbons, with the proviso that when X is hydrogen then R.sub.4 is selected from the group consisting of CH.sub.2 OH, CH.sub.2 NH.sub.2, CH.sub.2 CH.sub.2 OH, CH.sub.2 --CHO, or CH.sub.2 --COOR.sub.5 ; ##STR2## in which R.sub.1, R.sub.2 R.sub.3 independently are n-alkyl of 1 to 6 carbons, or branched chain alkyl of 1 to 6 carbons, and R.sub.5 is alkyl of 1 to 6 carbons; ##STR3## in which R.sub.1, R.sub.2 and R.sub.3 independently are n-alkyl of 1 to 6 carbons, or branched chain alkyl of 1 to 6 carbons, and R.sub.

Abstract: The present invention provides an agent for treating ischemic brain damage comprising 3-sulfamoylmethyl-1,2-benzisoxazole or its alkali metal salt as an active ingredient. This agent can be used for the prevention and/or treatment of cerebral ischemia-induced intracranial diseases or various symptoms associated therewith in mammals including human beings.

Abstract: Compounds of the formula ##STR1## wherein A taken together with the two carbon atoms denoted as .alpha. and .beta. is a group of the formula ##STR2## and the dotted line is the double bond present in formulas (i) and (iii); and wherein n is zero, 1, 2 or 3, one of R.sup.1 and R.sup.2 is carboxy or alkoxycarbonyl and the other is hydrogen, R.sup.3 is hydrogen, alkyl, alkoxy, aryloxy, azido, cyano or alkylthio, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 each, independently, is hydrogen or alkyl or, when R.sup.1 is carboxy or alkoxycarbonyl and n stands for 1, R.sup.4 and R.sup.6 taken together can be a carbon-carbon bond or, when R.sup.2 is carboxy or alkoxycarbonyl, R.sup.5 and R.sup.7 taken together can be a carbon-carbon bond, R.sup.8 is halogen, alkyl, haloalkyl or alkoxy and R.sup.9 is hydrogen, halogen, alkyl or alkoxy, and pharmaceutically acceptable salts of the compounds of formula I in which one of R.sup.1 and R.sup.

Abstract: The object of the invention are anticonvulsant heterocyclic compounds of general formula: ##STR1## in which R.sub.1 and R.sub.2 is each selected from C.sub.1 -C.sub.4 alkyl, phenyl, benzyl, trifluoromethyl or halogen, R.sub.3 is selected from hydrogen, hydroxy, C.sub.1 -C.sub.4 alkyl or alkoxy, R.sub.4, in position 3 or 5, is selected from hydrogen, trifluoromethyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkyl, or C.sub.1 -C.sub.4 hydroxyalkyl,R.sub.5 is selected from hydrogen or C.sub.4 -C.sub.4 alkyl or R.sub.4 and R.sub.5 together form a tetramethylene group, Z at position 3 or 5 on the heterocycle is selected from:--N(R.sub.6)--CO--, --CO--N(R.sub.6)--, --N(R.sub.6)--CO--N(R.sub.6)----CH(R.sub.6)--NH--CO--, or --NH-CO--CH(R.sub.6),in which R.sub.6 is selected from hydrogen or C.sub.1 -C.sub.4 alkyl.

Abstract: The invention concerns novel, pharmaceutically useful, amide derivatives of certain benzoheterocyclylalkanoic acids (and related tetrazoles and acylsulphonamides) of the formula I and salts thereof, wherein the radicals R.sup.1, R.sup.2, L, X, Y, Z, A.sup.1, Q, A.sup.2 and M have the meanings set out in the specification. The invention also includes pharmaceutical compositions incorporating a formula I compound or a salt thereof, a process for the manufacture of the said compound, together with intermediates for use in the latter process.

Abstract: There are disclosed compounds having the formula ##STR1## wherein R.sub.1 is hydrogen or loweralkyl; R.sub.2 is loweralkyl, arylloweralkyl, diarylloweralkyl or --CH.sub.2 CHOHCH.sub.2 OR.sub.5, R.sub.5 being aryl, or alternatively --NR.sub.1 R.sub.2 taken together is ##STR2## R.sub.6 being aryl, arylloweralkyl, diarylloweralkyl, ##STR3## and R.sub.3 and R.sub.4 are each independently methoxy or hydroxy, which compounds are useful as analgesic and hypotensive agents.

Abstract: There are disclosed compounds having the formula ##STR1## wherein R.sub.1 is hydrogen or loweralkyl; R.sub.2 is loweralkyl, arylloweralkyl, diarylloweralkyl or --CH.sub.2 CHOHCH.sub.2 OR.sub.5, R.sub.5 being aryl, or alternatively --NR.sub.1 R.sub.2 taken together is ##STR2## R.sub.6 being aryl, arylloweralkyl, diarylloweralkyl, ##STR3## and R.sub.3 and R.sub.4 are each independently methoxy or hydroxy, which compounds are useful as analgesic and hypotensive agents.

Abstract: The present invention is novel nitroimidazoles useful as radiosensitizing or chemosensitizing agents in the treatment of hypoxic tumor cells. Also, the present invention is a novel process for preparing both known and novel nitroimidazoles having novel intermediates. The process advantageously reduces the number of process steps, provides increased yield with both greater safety and greater control of stereo-isomerism in the products.

Abstract: 3-Aryl-2,1-benzisoxazole compounds having the formula: ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen or methyl;R.sup.3 and R.sup.4 are hydroxyl, loweralkoxy, amino or --OM wherein M is a pharmaceutically acceptable cation;X is hydrogen, halogen, loweralkyl or nitro;Y is selected from hydrogen, halogen, loweralkyl, loweralkoxy, nitro or trifluoromethyl;n and p are zero or one with the proviso that either n or p must be oneare disclosed, having anti-inflammatory activity and novel intermediates in the preparation thereof.

Abstract: The invention concerns novel, pharmaceutically useful, amide derivatives of certain benzoheterocyclylalkanoic acids (and related tetrazoles and acylsulphonamides) of the formula I and salts thereof, wherein the radicals R.sup.1, R.sup.2, L, X, Y, Z, A.sup.1, Q, A.sup.2 and M have the meanings set out in the specification. The invention also includes pharmaceutical compositions incorporating a formula I compound or a salt thereof, a process for the manufacture of the said compound, together with intermediates for use in the latter process.

Abstract: Disclosed are 1,2-benzisoxazole and 1,2-benzisothiazole derivatives represented by formula I ##STR1## wherein X represents oxygen or sulfur; Z rep;esents carbon (CH) so as to complete the imidazol-1-yl ring radical or Z represents nitrogen (N) so as to complete the 1,2,4-triazol-1-yl ring radical; R.sub.1 represents hydrogen, lower alkenyl, lower alkynyl, aryl-lower alkyl or lower alkyl; R.sub.2 represents hydrogen, lower alkenyl, lower alkynyl, aryl-lower alkyl or lower alkyl; or R.sub.1 and R.sub.2 combined represent lower alkylene; or R.sub.1 combined with R.sub.5 located on the Z-carbon atom of the imidazolyl radical represents C.sub.2 -C.sub.4 -alkylene; R.sub.3 and R.sub.4 independently represent hydrogen, lower alkyl, cycloalkyl, halogen, trifluoromethyl, cyano, nitro, amino, hydroxy, lower alkanoyloxy, carbocyclic aroyloxy, lower alkoxy, or carbocyclic aryl; or R.sub.3 and R.sub.4, together when located on adjacent carbon atoms, represent lower alkylenedioxy; or R.sub.3 and R.sub.

Abstract: There are provided new alkane and alkoxyalkane derivatives of the general formula I ##STR1## in which R.sub.1, R.sub.2, R.sub.3, R.sub.4 and A have the meanings given in the description, processes for their preparation and insecticidal and acaricidal compositions containing these compounds.

Abstract: Novel furobenzisoxazole derivatives of the formula (I): ##STR1## (wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 which may be the same or different represent a hydrogen atom, a halogen atom, or a lower alkyl group having 1-4 carbon atoms; R.sub.5 is a hydroxymethyl group, a carboxyl group or a lower alkoxy carbonyl group having 1-3 carbon atoms; and X is a sulfur atom or a --CH.dbd.CH-- group), as well as intoxic salts thereof when R.sub.5 is a carboxyl group, and process for preparing the same are disclosed.The derivatives of formula (I) and nontoxic salts thereof have hypotensive, uricosuric and diuretic activities and hence ae useful as therapeutics for treating hyperuricemia, edema and hypertension.

Abstract: Microbicidal substituted pyrazolin-5-ones of the formula ##STR1## in which R.sup.1 and R.sup.2 independently of one another each represent hydrogen, alkyl, alkenyl, alkinyl, cyanoalkyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkoxycarbonyl, hydroxycarbonylalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, alkylaminocarbonylalkyl or dialkylaminocarbonylalkyl, or represent in each case optionally substituted oxiranylalkyl, aralkyl, heterocyclyl or aryl andHet represents an optionally substituted heterocyclic radical.Intermediates therefor of the formula ##STR2## in which R is alkyl, are also disclosed.

Abstract: Dioxolobenzisoxazole derivatives of the formula ##STR1## wherein R.sub.1 is a phenyl group which may be substituted with a halogen atom, a lower alkyl group having 1-3 carbon atoms or a lower haloalkyl group, or a thienyl group; R.sub.2 is a hydrogen atom or a lower alkyl group having 1-4 carbon atoms; and X and Y which may be the same or different represent a hydrogen atom or a halogen atom, as well as non-toxic salts thereof wherein R.sub.2 is a hydrogen atom, a process for preparing the same and a pharmaceutical composition containing the same are disclosed.The derivatives have diuretic and uricosuric activities and, therefore, are useful as a drug for treating hyperuricemia or hypertension.

Abstract: Novel 1,2-benzisoxazoloxyacetic acids and related compounds, methods for preparing same and methods of treatment by administering compositions containing such a compound are described. These compounds are useful as diuretic, uricosuric and antihypertensive agents.

Abstract: There are described compounds of the formula ##STR1## where X is O or NR, R being hydrogen or loweralkyl; R.sub.1 is hydrogen; and R.sub.2 is loweralkyl, arylloweralkyl, aryloxyloweralkyl or loweralkyl substituted with ##STR2## or alternatively --NR.sub.1 R.sub.2 taken together is ##STR3## R.sub.3 being arylloweralkyl or a pharmaceutically acceptable acid addition salt thereof, which are useful as ocular or systemic antihypertensive agents.

Abstract: Novel (1,2-benzisoxazol)sulfinylalkanoic and -sulfonylalkanoic acids and derivative compounds, methods for preparing them and methods of treatment administering compositions containing the compounds which are useful as antihypertensives.

Abstract: Novel 6-fluoro-3-[3-(1-heterocyclo)propyl]-1,2-benzisoxazoles, processes for the preparation thereof, and methods of treating psychoses, alleviating pain and reducing blood pressure employing the compounds and compositions thereof are disclosed. 3-{3-[N-(1-Piperidino)]aminopropyl}-6-fluoro-1,2-benzisoxazole, processes for the preparation thereof, and methods of treating pyschoses and alleviating pain employing the compound and compositions thereof are also disclosed.

Abstract: New (2-propynylamino)isoxazole and (3-iodo-2-propynylamino)isoxazole derivatives having anti-microbial activity which are used as active ingredients in anti-microbial compositions for medical use, for agricultural use and also for veterinary use.

Abstract: Disclosed are compounds of the formula: ##STR1## wherein X is hydrogen, loweralkyl, loweralkoxy or halo, Y is hydroxymethyl, carboxyl, carboxamido or carboloweralkoxy, and R is cyclohexyl, benzyl, norbornyl, loweralkyl, or a pharmaceutically acceptable salt thereof.The compounds are effective as diuretic agents.

Abstract: A treating agent whose effective ingredient is an anthranyl derivative of the formula: ##STR1## (wherein R.sub.1 and R.sub.2 may be the same or different and represent a hydrogen atom, a hydroxyl group, a lower alkoxy group, preferably C.sub.1 -C.sub.3 alkoxy group, a lower alkyl group, preferably C.sub.1 -C.sub.3 alkyl group, a nitro group or a halogen atom) is disclosed.