Abstract: Novel compounds which are selective dopamine agonists are useful for treating disorders characterized by abnormal dopamine levels, such as Parkinson's Disease, as well as cardiovascular disorders.

Abstract: A pharmaceutical composition comprising a pharmaceutically acceptable carrier or diluent and an effective amount of an azaspirane derivative, a method of treating an animal in need of immunomodulation which comprises administering to such animal an effective amount of an azaspirane derivative, and certain azaspirane derivatives.

Abstract: Novel HMG-CoA reductase inhibitors are useful as antihypercholesterolemic agents and are represented by structural formulae (I) or (II): ##STR1## wherein position 5 of the polyhydronaphthyl ring is singly or doubly bonded to oxygen or incorporated into a C.sub.3-7 carbocyclic ring.

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: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: X, Y and R.sub.1 -R.sub.6 are as defined have blood pressure lowering activity and K+ channel activator activity and are useful in the treatment of hypertension.

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: A method is provided for inhibiting onset of or treating anxiety by administering an ACE inhibitor, such as captopril, fosinopril, zofenopril or SQ 29,852, alone or in combination with a calcium channel blocker such as diltiazem or nifedipine, over a prolonged period of treatment.

Abstract: Mannich bases of spirosuccinimides are provided having anticonvulsant, sedative and antileukemic activity.

Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## wherein L is NH or O;R.sub.1 is hydrogen, fluoro or chloro;R.sub.2 and R.sub.5 are independently hydrogen or C.sub.1-6 alkyl or together are a bond; orR.sub.2 and R.sub.3 and/or R.sub.4 and R.sub.5, together are C.sub.2-7 polymethylene or --(CH.sub.2).sub.m --O--(CH.sub.2).sub.x -- where m and x. are 1 to 5 such that m+x is 2 to 6;R.sub.4 is C.sub.1-7 acyl, C.sub.1-6 alkoxycarbonyl, hydroxycarbonyl, aminocarbonyl optionally substituted by one or two C.sub.1-6 alkyl groups, CF.sub.3, C.sub.1-6 alkyl substituted by C.sub.1-6 alkoxy, C.sub.1-6 alkylthio or by C.sub.1-6 alkoxycarbonyl, or R.sub.4 is phenyl or phenyl-C.sub.1-4 alkyl optionally substituted in the phenyl ring by one or two of halogen, C.sub.1-6 alkyl or C.sub.1-6 alkoxy;Z is a group of formula (a), (b) or (c).

Abstract: Mitomycin derivatives having potent anti-tumor activity having the formula: ##STR1## wherein one of R.sub.1 and R.sub.2 represents carbamoyloxymethyl and the other represents hydrogen or R.sub.1 and R.sub.2 are bonded together to form methylene;X is hydrogen or halogen;Y is hydrogen or methyl;Z is hydrogen, methyl or acyl; andn is an integer of 2 or 3.

Abstract: The present invention provides compounds of the general formula ##STR1## wherein the variables are as defined herein. The present invention also provides processes for the preparation thereof, pharmaceutical compositions containing them and intermediates for the preparation thereof.

Abstract: Novel 13-spiro-2'-[tetrahydrofuran]-milbemycins of the formula I ##STR1## in which X represents one of the groups --CH(OR.sub.1)--, --C(.dbd.O)-- or --C(.dbd.N--OH)--;R.sub.1 represents hydrogen or a OH-protecting group;R.sub.2 represents methyl, ethyl, isopropyl or sec.-butyl or the group --C(CH.sub.3).dbd.CH--A in which A represents methyl, ethyl or isopropyl; andR.sub.3 represents hydrogen; C.sub.1 -C.sub.10 -alkyl; C.sub.1 -C.sub.10 -alkyl substituted by at least one substituent selected from the group consisting of halogen, C.sub.1 -C.sub.6 -alkoxy, C.sub.2 -C.sub.6 -alkoxyalkoxy C.sub.3 -C.sub.9 -alkoxyalkoxyalkoxy, C.sub.1 -C.sub.6 -alkylthio, C.sub.3 -C.sub.7 -cycloalkyl, C.sub.1 -C.sub.3 -alkyl-substituted C.sub.3 -C.sub.7 -cycloalkyl, hydroxy, benzyloxy, C.sub.1 -C.sub.6 -acyl and C.sub.1 -C.sub.6 -acyloxy, it being possible for each of the above-mentioned radicals representing or containing an alkoxy group to be terminally substituted at a terminal alkoxy group by hydroxy, halogen, C.sub.1 -C.sub.

Abstract: Aromatic sulfonamides with a saturated heterocycle fused thereto are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.

Abstract: Fungicidally effective aminomethyl heterocyclic compounds of the formula ##STR1## in which X represents oxygen or sulphur,R represents hydrogen or alkyl, or represents in each case optionally substituted cyclohexyl or phenyl andR.sup.1 and R.sup.2 independently of one another each represent hydrogen, alkyl, alkenyl, alkinyl, alkoxyalkyl, dialkoxyalkyl, hydroalkyl, hydroxyalkoxyalkyl, alkoxycarbonylalkyl, dioxolanylalkyl, dioxanylalkyl or oxolanylalkyl, or represent in each case optionally substituted cycloalkylalkyl, cycloalkyl, aralkyl, aralkenyl or aryl, orR.sup.1 and R.sup.2, together with the nitrogen atom to which they are bonded, represent an optionally substituted saturated heterocyclic radical, which can optionally contain further hetero atoms,or acid addition salts thereof.

Abstract: A method for reducing intraocular pressure by topically applying 7-{N-[1(S)-Carboxy-3-phenylpropyl]-(S)-alanyl}-1,4-dithia-7-azaspiro[4.4]n onane-8(S)-carboxylic acid is disclosed.

Abstract: The present invention provides oxindole derivatives of the formula: ##STR1## wherein the various substituents are defined hereinbelow. The above compounds display nitrate-like as well as .beta.-blocking actions.

Abstract: Hapalindolinone compounds are produced by the controlled aerobic fermentation of a cyanobacterium of the genus Fischerella, ATCC No. 53558.

Abstract: Fungicidally active aminomethyltetrahydrofurans of the formula ##STR1## in which A represents a divalent alkylene or alkenylene chain which is in each case optionally substituted andR.sup.1 and R.sup.2 independently of one another each represent hydrogen, alkyl, alkenyl, alkinyl, alkoxyalkyl, dialkoxyalkyl, hydroxyalkyl, hydroxyalkoxyalkyl, dioxolanylalkyl, oxolanylalkyl, or dioxanylalkyl, or represent in each case optionally substituted cycloalkylalkyl, cycloalkyl, aralkyl, aralkenyl or aryl, orR.sup.1 and R.sup.2, together with the nitrogen atom to which they are bonded, represent an optionally substituted saturated heterocyclic radical, which can optionally contain further heteroatoms,or an acid addition salts thereof. Some intermediates therefor wherein NR.sup.1 R.sup.2 is replaced by halogen or sulphonyloxy are also new.

Abstract: The present invention is concerned with the use of azoniaspironortropanol esters of the general formula: ##STR1## wherein R signifies one of the following radicals: (a) an alkylene radical of the general formula: ##STR2## in which R.sub.3 is a hydrogen atom or an alkyl, benzyl, aryl or alkoxy radical and n is a whole number of from 1 to 4,(b) an alkenyl radical of the general formula: ##STR3## in which R.sub.4 and R.sub.5, which can be the same or different, are hydrogen atoms or alkyl or alkenyl radicals and n is a whole number of from 1 to 4,(c) an azaalkylene radical of the general formula: ##STR4## in which R.sub.6 is a hydrogen atom or an alkyl, alkoxycarbonyl or acyl radical and n is a whole number of from 2 to 4,(d) an oxaalkylene radical of the general formula:--(CH.sub.2).sub.n --O--(CH.sub.2).sub.

Abstract: Spiro-succinimides are disclosed which are useful as aldose reductase inhibitors and as therapeutic agents for the treatment of complications arising from diabetes. Pharmaceutical compositions containing the spiro- compounds and a method of treating diabetic complications are also disclosed.

Abstract: Novel substituted tetrahydro-, hexahydro- and octahydro-[3,4'-bi-2H-pyrrole]-2,2'-diones of the formula ##STR1## in which each of R.sub.1 and R.sub.

Abstract: A combination of drugs including a kappa opioid receptor agonist and a dopamine receptor blocker or dopamine receptor agonist provides a synergistic effect in inducing hypothermia and/or poikilothermia in humans and animals. Hypothermia as much as 10.degree. C. at an ambient temperature of 20.degree. C. is possible, with complete recovery and few, if any, side effects.

Abstract: Substituted phenoxy-, 1-, and 2-naphthalenyloxy-, indenyl-, indolyl-, benzofuranyl-, and benzo[b]thiofuranylcarboxamides of 7,8-(substituted-diamino)-1-oxaspiro[4.5]decanes are useful as analgesic agents.A method of making the compounds, pharmaceutical compositions employing the compounds, and a method of alleviating pain in warm-blooded animals are also disclosed.

Abstract: Spiro compounds, comprising a five-membered carbocyclic ring interrupted by two heteroatoms in ring positions 1 and 3 chosen from oxygen and sulfur atoms and in which the carbon atom in ring position 4 is common to a 4 to 8-membered carbocyclic ring interrupted by a nitrogen atom, are useful as pharmaceuticals.

Abstract: Novel optically active isomers or racemic mixtures of thiophene acetic acid derivatives of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms, Y is selected from the group consisting of --OR.sub.2 and ##STR2## R.sub.2 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms and ##STR3## n is an integer from 2 to 5, X' and X" are individually selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms or taken together with the nitrogen atom form an optionally unsaturated heterocycle of 5 to 6 ring members, R.sub.3 and R.sub.4 are individually selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms and their non-toxic, pharmaceutically acceptable salts with acids and bases having a good analgesic and anti-inflammatory activity and inhibition of 5-lipoxygenase and cyclooxygenase, a process and intermediates for their preparation.

Abstract: Method of promoting healing of ocular wounds comprising the topical application of an aldose reductase inhibitor; compositions comprising such inhibitors are also disclosed.

Abstract: Compounds of formula (I): ##STR1## wherein: either one of R.sub.1 and R.sub.2 is hydrogen and the other is selected from C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkoxycarbonyl, C.sub.1-6 alkylcarbonyloxy, C.sub.1-6 alkylhydroxymethyl, nitro, cyano, chloro, trifluoromethyl, C.sub.1-6 alkylsulphinyl, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkoxysulphinyl,C.sub.1-6 alkoxysulphonyl, C.sub.1-6 alkylcarbonylamino, C.sub.1-6 alkoxycarbonylamino, C.sub.1-6 alkyl-thiocarbonyl, C.sub.1-6 alkoxy-thiocarbonyl, C.sub.1-6 alkyl-thiocarbonyloxy, C.sub.1-6 alkyl-thiolmethyl, formyl or aminosulphinyl, aminosulphonyl or aminocarbonyl, the amino moiety being optionally substituted by one or two C.sub.1-6 alkyl groups, or C.sub.1-6 alkylsulphinylamino, C.sub.1-6 alkylsulphonylamino C.sub.1-6 alkoxysulphinylamino or C.sub.1-6 alkoxysulphonylamino or ethylenyl terminally substituted by C.sub.1-6 alkylcarbonyl, nitro or cyano, or --C(C.sub.1-6 alkyl)NOH or --C(C.sub.1-6 alkyl)NNH.sub.2, or one of R.sub.1 and R.sub.2 is nitro, cyano or C.

Abstract: Substituted benzopyrans of the formula ##STR1## in which --A-- is a single or double bond,X is a direct bond, optionally substituted methylene, oxygen or optionally substituted --NH--, and the various other radicals can have various meanings,or pharmaceutically acceptable addition salts thereof, which possess anti-hypertensive activity.

Abstract: Antihypertensive compounds of formula (I): ##STR1## wherein the various substituents are defined hereinbelow.

Abstract: Compounds of formula (I): ##STR1## wherein: R.sub.1 -R.sub.6 are as defined in the specification;X is oxygen or sulphur; and the R.sub.6 NCXR.sub.5 and OCOH moieties are trans and, when one or the other of R.sub.1 and R.sub.2 is an amino group, pharmaceutically acceptable salts thereof, a process and intermediates for preparing them, pharmaceutical compositions containing them, and their use in the treatment of mammals.

Abstract: 3,3-Dialkyl- or 3,3-alkylene-indolines which are unsubstituted at the 1- and 2-positions and which are substituted at the 4- or 6-position by an optionally etherified hydroxy group or substituted at the 5- or 7-position by an etherified hydroxy group, as well as their physiologically-hydrolyzable and -acceptable esters. The said indolines and esters as well as their pharmaceutically acceptable acid addition salts possess analgesic activity.

Abstract: A compound of formula (I): ##STR1## wherein: either one of R.sub.1 and R.sub.2 is hydrogen and the other is selected from the class of C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkoxycarbonyl, C.sub.1-6 alkylcarbonyloxy, C.sub.1-6 alkylhydroxymethyl, nitro, cyano, chloro, trifluoromethyl, C.sub.1-6 alkylsulphinyl, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkoxysulphinyl, C.sub.1-6 alkoxysulphonyl, C.sub.1-6 alkylcarbonylamino, C.sub.1-6 alkoxycarbonylamino, C.sub.1-6 alkyl-thiocarbonyl, C.sub.1-6 alkoxy-thiocarbonyl, C.sub.1-6 alkyl-thiocarbonyloxy, 1-mercapto-C.sub.2-7 alkyl, formyl or aminosulphinyl, aminosulphonyl or aminocarbonyl, the amino moiety being optionally substituted by one or two C.sub.1-6 alkyl groups, or C.sub.1-6 alkysulphinylamino, C.sub.1-6 alkylsulphonylamino C.sub.1-6 alkoxysulphinylamino or C.sub.1-6 alkoxysulphonylamino or ethylenyl terminally substituted by C.sub.1-6 alkylcarbonyl, nitro or cyano, or --C(C.sub.1-6 alkyl)NOH or --C(C.sub.1-6 alkyl)NNH.sub.2, or one of R.sub.1 and R.sub.

Abstract: Method of treating glaucoma comprising the topical or systemic application of an aldose reductase inhibitor; compositions comprising such inhibitors are also disclosed.

Abstract: Method of promoting healing of ocular wounds comprising the topical application of an aldose reductase inhibitor; compositions comprising such inhibitors are also disclosed.

Abstract: N-[2-(2,5-dihydro-1H-pyrrol-1-yl)cycloaliphatic)]benzeneacetamide and -benzamide compounds, e.g., (1.alpha.,2.beta.)-(.+-.)-3,4-dichloro-N-[2-(2,5-dihydro-1H-pyrrol-1-yl)cy clohexyl]-N-methylbenzeneacetamide, and salts thereof, have useful analgesic activity, low abuse or physical dependence liability properties. Processes for their preparation are disclosed. Pharmaceutical compositions containing such compounds and methods for their use are also disclosed.

Abstract: Analgesic 2-oxa-spirocyclic compounds of the formula ##STR1## where the wavy line bonds, p, n, m, A, q, X, Y, R, R.sub.1, R.sub.2 and E are as defined in the specification, e.g., trans-4-bromo-N-methyl-N-[7-(1-pyrrolidinyl)-2-oxaspiro[4.5]dec-8-yl]benza mide, and trans-3,4-dichloro-N-methyl-N-[7-(1-pyrrolidinyl)-2-oxaspiro[4.5]dec-8-yl] benzeneacetamide, and acid addition salts thereof. Pharmaceutical compositions and methods of using these compounds as analgesics are disclosed. Processes for preparing the class of compounds are also disclosed.

Abstract: Novel substituted and unsubstituted 13-(alkoxy)methoxy derivatives of the avermectin aglycones are useful as anthelmintic and antiparasitic agents. The compounds are also useful as pesticides and insecticides against agricultural pests. Included herein are novel intermediates useful in the process for preparing said avermectin aglycone derivatives. Compositions of said derivatives and methods of administering said compositions are also disclosed.

Abstract: (Benzothiadiazine, benzamido and benzenesulfonyl)phenyl-substituted carboxyalkyl dipeptide compounds are disclosed. Compounds of this invention are useful as antihypertensive agents.

Abstract: There are disclosed novel avermectin and milbemycin compounds wherein the 13-position is oxidized to a keto function. The 13-keto derivatives are prepared from the 13-hydroxy compounds by oxidizing the 13-position with a suitable oxidizing agent. The avermectin and milbemycin 13-keto derivatives are active in their own right and also serve as intermediates in the preparation of 13-imino and 13-amino derivatives. The 13-keto, imino and amino compounds have utility as anti-parasitic agents and compositions for that use are also disclosed. The compounds are also highly potent insecticides against agricultural pests.

Abstract: Compounds of formula (I): ##STR1## wherein: either one of R.sub.1 and R.sub.2 is hydrogen and the other is selected from the class of C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkoxycarbonyl, C.sub.1-6 alkylcarbonyloxy, C.sub.1-6 alkylhydroxymethyl, nitro, cyano, chloro, trifluoromethyl, C.sub.1-6 alkylsulphinyl, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkoxysulphinyl, C.sub.1-6 alkoxysulphonyl, C.sub.1-6 alkylcarbonylamino, C.sub.1-6 alkoxycarbonylamino, C.sub.1-6 alkyl-thiocarbonyl, C.sub.1-6 alkoxy-thiocarbonyl, C.sub.1-6 alkyl-thiocarbonyloxy, 1-mercapto C.sub.2-7 alkyl, formyl or aminosulphinyl, aminosulphonyl or aminocarbonyl, the amino moiety being optionally substituted by one or two C.sub.1-6 alkyl groups, or C.sub.1-6 alkylsulphinylamino, C.sub.1-6 alkylsulphonylamino C.sub.1-6 alkoxysulphinylamino or C.sub.1-6 alkoxysulphonylamino, or ethylenyl terminally substituted by C.sub.1-6 alkylcarbonyl, nitro or cyano, or --C(C.sub.1-6 alkyl)NOH or --C(C.sub.1-6 alkyl)NNH.sub.2, or one of R.sub.1 and R.sub.

Abstract: The invention relates to compounds of the formula I ##STR1## in which n denotes 1, 2, 3 or 4, R is alkyl, alkenyl cycloalkyl, aryl, optionally mono-, di- oder trisubstituted by alkyl, alkoxy, hydroxy, halogen, nitro, amino, alkylamino, dialkylamino or methylenedioxy, or indol-3-yl, R.sup.1 denotes an optionally protected radical of a naturally occurring amino acid HOOC--CH(NH.sub.2)--R.sup.1, R.sup.2 denotes hydrogen, alkyl or optionally nitro-substituted aralkyl, R.sup.3 denotes hydrogen, alkyl or cycloalkyl or optionally nitro-substituted aralkyl and X denotes 2 hydrogen atoms or 1 oxygen atom, their physiologically tolerated salts with acids and, if R.sup.2 and/or R.sup.3 denote hydrogen, with bases, a process for their preparation, agents containing these derivatives and their use as medicaments.

Abstract: Compounds of the formula (I): ##STR1## wherein: one of R.sub.1 and R.sub.2 is hydrogen and the other is C.sub.1-6 alkyl-thiocarbonyl, C.sub.1-6 alkoxy thiocarbonyl, C.sub.1-6 alkyl-thiocarbonyloxy, 1-mercapto C.sub.2-7 alkyl or formyl;one of R.sub.3 and R.sub.4 is hydrogen or C.sub.1-4 alkyl and the other is C.sub.1-4 alkyl, or R.sub.3 and R.sub.4 together with the carbon atom to which they are attached are C.sub.3-6 spiroalkyl;R.sub.5 is hydrogen, C.sub.1-3 alkyl or C.sub.1-8 acyl; andn is 1 or 2; the lactam group being trans to the OR.sub.5 group, having anti-hypertensive activity.

Abstract: Anti-hypertensive compounds of formula (I): ##STR1## wherein: one of R.sub.1 and R.sub.2 is nitro, cyano or C.sub.1-3 alkylcarbonyl, and the other is methoxy or amino optionally substituted by one or two C.sub.1-6 alkyl or by C.sub.2-7 alkanoyl;one of R.sub.3 and R.sub.4 is hydrogen or C.sub.1-4 alkyl and the other is C.sub.1-4 alkyl, or R.sub.3 and R.sub.4 together with the carbon atom to which they are attached are C.sub.3-6 spiroalkyl;R.sub.5 is hydrogen, C.sub.1-3 alkyl or C.sub.1-8 acyl; andn is 1 or 2; the lactam group being trans to the OR.sub.5 group; or, when the other of R.sub.1 and R.sub.2 is amino, a pharmaceutically acceptable salt thereof.

Abstract: Disclosed are substituted or unsubstituted planar tricyclic fluorene or nuclear analogs thereof, spiro-coupled to a five-membered ring containing a secondary amide, and the pharmaceutically acceptable salts thereof. These compounds are useful, inter alia, in the treatment of diabetes. Also disclosed are processes for the preparation of such compounds; pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions when indicated for, inter alia, long term, prophylactic treatment of the diabetes syndrome.

Abstract: Amide derivatives of the formula: ##STR1## wherein either R.sup.1 is aryl or heterocyclic and A.sup.1 is a direct link, or R.sup.1 is aryl or heterocyclic, or hydrogen or amino and A.sup.1 is alkylene; X is --CH.sub.2 -- or --CO-- or has the formula ##STR2## wherein R.sup.11 and R.sup.12, which may be the same or different, each is alkyl, or R.sup.11 and R.sup.12 are joined to form alkylene; A.sup.2 is alkylene; R.sup.2 is hydrogen, aryl or alkyl which is unsubstituted or which bears an aryl substituent; R.sup.3 is hydrogen or alkyl which is unsubstituted or which bears a halogeno, hydroxy, amino, guanidino, carboxy, carbamoyl, mercapto, alkoxy, alkylamino, dialkylamino, cyclic amino, alkylthio, alkanoylamino, alkoxycarbonyl, arylalkoxycarbonyl, aryl or heterocyclyl substituent; R.sup.4 is alkyl which is unsubstituted or which bears an aryl substituent, or R.sup.4 is phenyl or alkylphenyl; n is 0 or 1; and either R.sup.5, R.sup.6, R.sup.15 and R.sup.16 are all hydrogen, or R.sup.5 and R.sup.

Abstract: This invention relates to a method of using compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen, alkyl or alkenyl; R.sup.2 is hydrogen, alkyl, cycloalkyl or mononuclear aryl or R.sup.1 and R.sup.2, taken together with the carbon atom to which they are attached, form a cycloalkyl or cycloalkoxyalkyl; R.sup.3 is hydroxy, alkyl, alkoxycarbonyl, hydroxy lower alkyl or a radical of the formula: --C(.dbd.Y)NR.sup.4 R.sup.5 wherein R.sup.4 is hydrogen, alkyl, alkenyl, R.sup.5 is alkyl, alkenyl, alkoxyalkyl, carbalkoxy, mononuclear aryl, or R.sup.4 and R.sup.5 may be joined together with the nitrogen atom to which they are attached to form a 5 to 7 membered heterocyclic ring having from 1 to 3 hetero atoms; Y is O or S; X is alkyl, alkoxycarbonylalkyl or cyano; m is an integer of 0 to 2 and n and n' are integers each having a value of 1 to 2 and the dotted line indicates an optional double bond anywhere in the ring, compositions containing said compounds as insect repellents and to novel compounds.

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.