Abstract: Lipid derivatives represented by the formula: ##STR1## wherein R.sup.1 stands for an optionally substituted higher alkyl group, R.sup.2 stands for an optionally substituted lower alkyl group or an optionally substituted nitrogen-containing heterocyclic group, R.sup.3 stands for a tertiary amino group or a quaternary ammonium group, J stands for oxygen atom or S(O)t (where t deontes 0, 1 or 2), m and n respectively denotes 1 or 2, p denotes 0, 1 or 2, q and r respectively denote an integer of 2 to 5.and salts thereof have antitumor activities including differentiation-inducing activity and are useful as antitumor agents.

Abstract: Novel 1,6-diaza [4.4] spirodilactams having heterocyclic-containing substituents on each spiro ring nitrogen atom are produced by reaction of a heterocyclic-substituted primary amine compound and a spirodilactam precursor selected from 4-oxoheptanedioic acid compounds or 1,6-dioxaspiro[4.4]nonane-2,7-dione compounds. The substituted spirodilactam products have a plurality of heterocyclic rings and are useful in biological applications and as stabilizers.

Abstract: Novel monomeric compounds containing aliphatic and/or aromatic substituents on the 1,6-diazaspiro[4.4]nonane-2,7-dione ring system are produced by contacting an amine or an amine hydrohalide and a 1,6-dioxaspiro[4.4]nonane-2,7-dione or a 4-oxoheptanedioic acid. The resulting spirodilactam compounds are characterized by improved hydrolytic and thermal oxidative stability and some of the compounds are useful as intermediates to polymers containing the 1,6-diazaspiro[4.4]nonane-2,7-dione ring system.

Abstract: A 1,6-diaza[4.4]spirodilactam monomer or oligomer having an aliphatically-unsaturated imido-containing substituent on each terminal spiro ring nitrogen atom and cured products thereof.

Abstract: A compound represented by the formula: ##STR1## wherein R represents a hydrogen atom or a lower alkyl group;R.sup.1 represents a higher alkyl group which may be substituted;R.sup.2 represents a hydrogen atom or a lower alkyl group, a lower alkanoyl group or a nitrogen-containing 5- to 7-membered heterocyclic group each of which may be substituted; X represents a divalent group represented by the formula:--(OCH.sub.2 CH.sub.2).sub.p --wherein p represents an integer of 1 to 5, a divalent group represented by the formula:--O(CH.sub.2).sub.q --wherein q represents an integer of 3 to 8, or a divalent group represented by the formula:--(OCH.sub.2 CH.sub.2).sub.p --J--(CH.sub.2).sub.q --wherein J represents an oxygen atom or a group represented by the formula: --S(O).sub.

Abstract: Novel cyclic 1,6-diazaspiro [4.4] lactams are produced by reaction of at least one hydroxy-containing primary amino compound with a 4-ketocyclicdiacid compound or a cyclic-1,6-dioxaspiro[4.4] lactone.

Abstract: Certain spirocyclic heterocyclic compounds, and their pharmaceutically-acceptable salts, are inhibitors of the aldose reductase enzyme, and so are useful for the control of diabetic complications. Exemplary compounds include compounds of the formula ##STR1## wherein Y is ##STR2## X is --O-- or ##STR3## R.sub.1 and R.sub.2 are each independently H, alkyl C.sub.1 -C.sub.6,aryl or arylalkyl (C.sub.1 -C.sub.6);W.sub.1 and W.sub.2 are each independently hydrogen, halogen or nitro; andthe pharmaceutically acceptable base addition salts thereof.

Abstract: A novel class of cured products is derived from unsaturated polycylic ethers or esters comprising unsaturated ether or ester derivatives of a hydroxyaryl-substituted 1,6-diaza [4.4] spirodilactum having a hydroxyaryl substitute attached to each spiro ring nitrogen atom.

Abstract: Cyanatoaryl-substituted 1,6-diaza[4.4]spirodilactam having a cyanatoaryl-containing substituent on each spiro ring nitrogen atom self-cure upon application of heat to produce cured, crosslinked thermoset resins of high glass transition temperature.

Abstract: A method for preparation of 1,3-oxathiolanes is described. The method comprises reacting, in a solvent, a fluoride ion source, a carbonyl compound, and a halomethyl trimethylsilylmethyl sulfide, wherein the halomethyl trimethylsilyl methyl sulfide is selected from a group consisting of chloromethyl trimethylsilylmethyl sulfide, bromomethyl trimethylsilylmethyl sulfide, or iodomethyl trimethylsilylmethyl sulfide.

Abstract: A novel class of bis(spirolactonelactam) compounds is produced by reaction of a primary diamine in the presence of a stoichiometric excess of a spirodilactam precursor selected from ketodiacid compounds and 1,6-dioxo [4.4] spirodilactones.

Abstract: Novel 1,6-diaza[4.4]spirodilactams having a hydroxyaryl substituent on each spiro ring nitrogen atom and at least one alkenyl group located on an aromatic ring carbon atom which is ortho to the hydroxy of the hydroxyaryl substituents are produced by Claisen Rearrangement of an alkenyl ether of the hydroxyaryl-substituted spirodilactam having one fewer ortho-alkenyl substituent.

Abstract: Arylcyclobutenealkyl ether of hydroxyaryl-substituted 1,6-diaza [4.4] spirodilactams having a hydroxyaryl substituent on each spiro ring nitrogen atom are self-curing upon application of heat to produce cured products of relatively high glass transition temperature having good physical properties.

Abstract: Novel monomeric compounds containing the 2,7-diazaspiro[4.4]-nonane-1,6-dioine ring system are produced by contacting an amine hydrohalide and a 2,7-dioxaspiro[4.4]nonane-1,6-dione. The resulting spirodilactam compounds are characterized by improved hydrolytic and thermal oxidative stability.

Abstract: This invention relates to novel spirosuccinimide derivatives, to the processes for their preparation, to methods for using the compounds, and to pharmaceutical preparations thereof. The compounds have pharmaceutical properties which render them beneficial for the treatment of diabetes mellitus and associated conditions.

Abstract: Novel unsaturated derivatives of 1,6-diaza [4,4] spirodilactams having a monovalent unsaturated substituent on each spiro ring nitrogen atom are produced by reaction of an unsaturated amine and a spirodilactam precursor selected from a 4-oxoheptanedioic acid compound or a 1,6-dioxo [4,4] spirodilactone.

Abstract: The present invention provides a compound of formula I or a salt or prodrug thereof: ##STR1## wherein the dotted line represents an optional chemical bond in one of the two possible positions;A represents a group of formula II: ##STR2## in which R.sup.1 represents hydrogen, hydroxy, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.1-6 alkoxy, benzyloxy, hydroxy (C.sub.1-6)alkyl, halogen, amino, cyano, nitro, --CONR.sup.6 R.sup.7 or --SO.sub.2 NR.sup.6 R.sup.7, in which R.sup.6 and R.sup.7 independently represent hydrogen, halogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.2-6 alkynyl;R.sup.2 represents hydrogen, halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or C.sub.1-6 alkylcarbonyl;V represents nitrogen, --CH or --C--; andW represents oxygen, sulphur or --NR.sup.8, in which R.sup.8 represents hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.

Abstract: Primary diamines, employed in stoichiometric excess, react with a spirodilactam precursor selected from 4-oxoheptandioic acid compounds or 1,6-dioxaspiro[4.4]nonane-2,7-diones, to produce 1,6-diaza[4.4]spirodilactams having an amino-containing substituent on each spiro ring nitrogen atom. The spirodilactams are useful in the production of thermoplastic polyamides by reaction with diacids and as curing agents for epoxy resins in the production of thermoset resins.

Abstract: Novel 1-azaspiro[4.4] lactams are produced by reaction of at least one hydroxy-containing primary amino compound with a 4-ketodiacid compound or a 1,6-dioxaspiro[4.4]lactone. Molar excesses of amion compound result in production of spirodilactams, while limited molar quantities of amino compound results in production of a spirolactam-lactone which reacts further with hydroxy-containing primary amino compound or with hydroxy-free primary amino compound to produce a spirodilactam. Certain of the spirolactams are useful as precursors for glycidyloxy derivatives which react with epoxy curing agents to form insoluble thermoset resins while others are useful as curing agents and yet others are converted to glycidyloxy derivatives useful as reactive diluents in epoxy resin applications.

Abstract: A compound of formula (I), or a pharmaceutically acceptable salt thereof, ##STR1## in which, R.sub.1 is hydrogen, lower alkyl or CH.sub.2 OR.sub.6 ;R.sub.2 is hydrogen or lower alkyl;R.sub.3 is hydrogen or lower alkyl;each of W and Z, which are different, represents --CR.sub.4 R.sub.5 -- or --(CR.sub.x R.sub.y).sub.n --, in which,R.sub.4 is hydrogen, C.sub.1-3 alkyl, C.sub.1-3 alkylthio or C.sub.1-3 alkoxy;R.sub.5 is C.sub.1-3 alkyl, C.sub.1-3 alkylthio or C.sub.1-3 alkoxy; or together R.sub.4 and R.sub.5 form a 3 to 6 membered carbocyclic ring, or a heterocyclic ring containing one or two ring oxygen, nitrogen or sulphur atoms;or R.sub.4 and R.sub.5 together form an oxo or methylene group;each of R.sub.x and R.sub.y is hydrogen or C.sub.1-3 alkyl; n is zero or 1;R.sub.6 is hydrogen, lower alkyl, lower alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, heteroarylcarbonyl, optionally substituted aminocarbonyl, lower alkoxycarbonyl and aryloxycarbonyl;R.sub.

Abstract: This invention relates to novel spirosuccinimide derivatives, to the processes for their preparation, to methods for using the compounds, and to pharmaceutical preparations thereof. The compounds have pharmaceutical properties which render them beneficial for the treatment of diabetes mellitus and associated conditions.

Abstract: Novel epoxyalkoxy-containing [4.4] spirodilactams having ring nitrogen atoms in the 1- and the 6- ring positions and having a substituent on each ring nitrogen atom, at least one of which substituents contains an epoxyalkyl moiety. Such epoxy compounds are produced by reaction of a 1-halo-2,3-epoxyalkane and the corresponding hydroxy-containing spirodilactam followed by treatment with strong base.

Abstract: Heterocyclic substituted indolinones of the formula: ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl or hydroxyalkyl radical, R.sub.2 is a carboxyl group or an alkoxy-carbonyl, hydroxyalkyl or alkylcarbonyloxyalkyl radical or R.sub.1 and R.sub.2, together with the carbon atom to which they are attached, form a lactone having 4, 5 or 6 ring atoms, A-B is --CH.sub.2 --CH(R.sub.3)--, --CH.dbd.CR.sub.3 --, --CH.sub.2 --NH--, --NH--CH.sub.2 --, --CH.sub.2 --O--, --O--CH.sub.2 --, --CH.sub.2 --S-- or --S--CH.sub.2 -- radical, R.sub.3 being a hydrogen atom or an alkyl or hydroxyalkyl radical, or A is a valency bond and B is a methylene radical ##STR2## or an imino group ##STR3## R.sub.4, R.sub.5, and R.sub.

Abstract: Isoindolin-1-one compounds represented by the following formula (I); ##STR1## {wherein n represents an integer of 1 to 6; m represents 0 or 1; R.sub.1, R.sub.2 and R.sub.3 are each independently hydrogen or lower alkyl, and when m is 1, R.sub.1 and one of R.sub.2 and R.sub.3 may form a five-membered or six-membered ring over N atom; X represents hydrogen or hydroxy; Ar represents naphthyl, pyridyl or substituted phenyl represented by the formula (II); Ar and X may form a lactone ring; ##STR2## [wherein Y represents carboxyl, lower alkoxycarbonyl, carbamoyl, N,N-lower alkyl-substituted carbamoyl or amino represented by the formula (III): ##STR3## (wherein R.sub.6 and R.sub.7 are each independently hydrogen, lower alkyl or lower alkanoyl); R.sub.4 and R.sub.5 are each independently hydrogen, lower alkyl, cyano or halogen]} or a pharmaceutically acceptable acid addition salt or metal salt thereof have an excellent antiarrhythmic activity.

Abstract: A novel class of unsaturated polycyclic ethers and esters comprises unsaturated ether and ester derivatives of a hydroxyaryl-substituted [4.4] spirodilactams having nitrogen atoms in the 1- and 6-positions of the spiro ring system and having the hydroxyaryl groups attached to each spiro ring nitrogen. Such unsaturated ethers and esters react with conventional curing agents to produce cured, insoluble products having high glass transition temperatures.

Abstract: There are disclosed compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 taken together represent ##STR2## with the proviso that in ##STR3## when X is lower alkylene or O, m is other than 1; and when R.sup.1 and R.sup.2 taken together represent ##STR4## R.sup.3 is other than unsubstituted or substituted 2-pyridinyl or 2-pyrimidinyl;R.sup.3 is unsubstituted or substituted 2-pyridinyl, 2-pyrimidinyl, 2-pyrazinyl or 3-pyridazinyl, where the substituents are selected from the group lower alkyl, lower alkoxy, halo, cyano and nitro;Z is --(CH.sub.2).sub.n -- or vinylene;X is lower alkylene, vinylene or O;m is 1-4;n is 1-3;o is 1-5;p is 0-1;and the pharmaceutically acceptable salts thereof and their use as antipsychotic/anxiolytic agents having a low liability for extrapyramidal side effects.

Abstract: Pyrimidoindoles of formula (I) ##STR1## and their pharmaceutically acceptable acid addition salts, wherein R represents lower alkyl a mono- or bicyclic aryl radical or a group of mormula R.sup.3 O--B--[where R.sup.3 O is (lower)alkoxy,aryl(lower)alkoxy or hydroxy and B is a lower alkylene chain optionally containing one double or triple bond], R.sup.1 and R.sup.2 which may be the same or different each represent hydrogen, hydroxyl, lower alkyl, lower alkoxy, halo(lower)alkyl, halogen, amino or mono- or di(lower) alkylamino and A, together with the carbon atom to which it is attached, represents 5, 6 or 7 membered saturated carbocyclic or heterocyclic ring, are useful as hypoglyceamics.

Abstract: Disclosed are nadimido-substituted cyclophosphazene derivatives and thermosets thereof. The thermosets are useful as high temperature, flame resistant matrices for composites and as metal adhesives.

Abstract: The invention concerns a novel process for the racemization of unwanted enantiomeric forms of 1'-substituted spiro[imidazolidine-4,3'-indoline]-2,2',5-triones and 1'-substituted spiro[pyrrolidine-3,3'-indoline]-2,2',5-triones which comprises heating an unwanted enantiomeric form (or a mixture containing an excess of one enantiomer over the other) alone or, more conveniently, in the presence of a solvent or diluent at a temperature in the range 80.degree. to 280.degree. C.

Abstract: Novel 1-amino-naphthyridine- and quinoline-carboxylic acids as antibacterial agents are described as well as methods for their manufacture, formulation, and use in treating bacterial infections.

Abstract: Compounds of the formula ##STR1## wherein X is various imino or amino acids or esters are disclosed. These compounds possess angiotensin converting enzyme inhibition activity and depending upon the definition of X also possess enkephalinase inhibition activity.

Abstract: The invention concerns a novel process for the racemisation of unwanted enantiomeric forms of 1'-substituted spiro[imidazolidine-4,3'-indoline]-2,2',5-triones and 1'-substituted spiro[pyrrolidine-3,3'-indoline]-2,2',5-triones which comprises heating an unwanted enantiomeric form (or a mixture containing an excess of one enantiomer over the other) alone or, more conveniently, in the presence of a solvent or diluent at a temperature in the range 80.degree. to 280.degree. C.

Abstract: The invention provides a pharmaceutical composition comprising an aldose reductase inhibitory 1'substituted-spiro[pyrrolidine-3,3'-indoline]-2,2',5-trione of the formula: ##STR1## wherein Ra is (2-7C)alkyl or (3-7C)alkenyl, naphthylmethyl or cinnamyl optionally bearing one or two halogeno nuclear substituents, or Ra is benzyl optionally bearing one or two substituents and benzene ring A optionally bears one or two substituents, trifluoromethyl and nitro; or a salt thereof with a base affording a pharmaceutically acceptable cation; or a non-toxic, biodegradable precursor thereof; together with a pharmaceutically acceptable diluent or carrier. The invention also provides novel compounds of formula I and processes for their manufacture.The compositions are of application in the treatment or prophylaxis of the side effects of diabetes or galactosemia.

Abstract: The invention provides various medical compositions for use in treating or preventing certain of the side effects of diabetes or galactosemia. The active ingredients are selected from a series of novel aldose reductase inhibitory spiro-linked pyrrolidine-2,5-diones of the general formula: ##STR1## or a pharmaceutically acceptable salt, or a non-toxic, biodegradable precursor thereof. Processes for the production of these compounds are also provided. A particular compound suitable for use as an active ingredient is spiro[pyrrolidine-3,9'-xanthene]-2,5-dione.

Abstract: The invention provides a pharmaceutical composition comprising an aldose reductase inhibitory 1'-substituted-spiro[pyrrolidine-3,3'-indoline]-2,2',5-trione of the formula: ##STR1## wherein Ra is (2-7C)alkyl or (3-7C)alkenyl, naphthylmethyl or cinnamyl optionally bearing one or two halogeno nuclear substituents, or Ra is benzyl optionally bearing one or two substituents and benzene ring A optionally bears one or two substituents, trifluoromethyl and nitro; or a salt thereof with a base affording a pharmaceutically acceptable cation; or a non-toxic, biodegradable precursor thereof; together with a pharmaceutically acceptable diluent or carrier. The invention also provides novel compounds of formula I and processes for their manufacture.The compositions are of application in the treatment or prophylaxis of the side effects of diabetes or galactosemia.

Abstract: A series of spiro-imide compounds and their base salts with pharmacologically acceptable cations are disclosed. These particular compounds are useful in therapy as agents for the control of certain chronic diabetic complications. Preferred member compounds include 2,3-dihydro-spiro-[1H-indene-1,3'-pyrrolidone]-2', 5'-dione, 2,3-dihydro-spiro-[1H-indene-2,3'-pyrrolidine]-2',5'-dione, 3,4-dihydro-spiro-[2H-naphthalene-1,3'-pyrrolidine]-2',5'-dione, 3,4-dihydro-spiro-[2H-naphthalene-1,3'-piperidine]-2', 6'-dione, 6-chloro-2,3-dihydro-spiro-[4H-1-benzopyran-4,3'-pyrrolidine]-2',5'-dione and 6,7-dihydro-spiro-[5H-benzo(b)thiophene-4,3'-pyrrolidine]-2',5'-dione. Methods for preparing these compounds from known starting materials are provided.

Abstract: Novel substituted 1,3-dihydrospiro[benzo(c)thiophene]s and methods of preparing the same are described. These compounds are useful as antidepressants and tranquilizers and intermediates therefor.