Abstract: Compounds of the general formula ##STR1## or pharmaceutically acceptable salts thereof, wherein Z is a saturated or unsaturated 3 to 6 carbon chain,m is 2 or 3,R.sub.1 is a hydrogen atom, or a straight or branched C.sub.1-4 alkyl group,R.sub.2, R.sub.3 and R.sub.13 are situated in the ortho, meta, or para position of the phenyl ring and are the same or different and selected from the following groups: H, OH, OR.sub.14, halogen, CO.sub.2 R.sub.9, CN, CF.sub.3, NO.sub.2, NH.sub.2, COCH.sub.3,OSO.sub.2 CF.sub.3,OSO.sub.2 CH.sub.3,CONR.sub.10 R.sub.11, OCOR.sub.12, whereinR.sub.9, R.sub.12 and R.sub.14 is a straight or branched C.sub.1-4 alkyl group,R.sub.10 and R.sub.11 are the same or different and represents hydrogen or a straight or branched C.sub.1-6 alkyl group,R is 1) ##STR2## processes for their preparation, pharmaceutical preparations containing them and the use of the compounds in the treatment psychiatric disorders.

Abstract: The invention concerns heterocyclic compounds of the general formula (I) in which A, B, R, R.sup.2, R.sup.3, W, Y, Z.sup.1, Z.sup.2 and r are as defined in the description, methods of preparing them and their use as inhibitors of thrombocyte aggregation, the metastization of carcinoma cells and the binding of osteoclasts on bone surfaces.

Abstract: Novel succinimides and maleimides are inhibitors of tumor necrosis factor .alpha. and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. A typical embodiment is methyl 3-(3',4',5',6'-tetrahydrophthalimido)-3-(3",4"-dimethoxyphenyl)propionate.

Abstract: Methods of treatment for inflammatory and autoimmune dermatoses which comprises topical and/or systemic administration of a therapeutically-effective amount of thalidomide alone or in combination with other dermatological agents.

Abstract: Coenzyme A-independent transacylase is required for the release of free arachidonic acid, and the production of arachidonic acid metabolites and platelet activation factor. Blocking of this enzyme inhibits the production of these inflammatory mediators and will be of therapeutic utility in a broad range of allergic and inflammatory diseases and disorders. Compounds are described herein which inhibit the action of CoA-IT and are therefore useful in the treatment of disease states caused thereby.

Abstract: In accordance with the present invention, a method is provided for treating reperfusion injury, ischemia and runaway inflammatory conditions with thalidomide alone or in combination with other drugs selected from the group consisting of nitrates, beta-adrenoceptor blocking agents, anti-platelet/thrombolytic drugs, drugs acting as the arachindonic acid cascade and calcium antagonists. Pharmaceutical compositions comprising thalidomide alone or in combination with other drugs are also provided.

Abstract: Glucosidase I inhibitors as therapeutic agents for combatting nondefective retroviral pathogens, including the aetiological agents of AIDS and feline leukemia. Administration of a processing glucosidase I inhibitor, preferably castanospermine, interrupts the replication of the retrovirus in infected cells, alleviates pathogenic effects associated with the presentation of vital env glycoproteins on infected cells, and may furthermore prevent infection of target cells by interrupting expression of endogenous receptors recognized by the virion.

Abstract: Disclosed are compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty. Independently, R.sub.1 and R.sub.2 are hydrogen, a straight or branched chain alkyl, alkenyl or alkynyl of up to twenty carbon atoms in length or --(CH.sub.2).sub.w R.sub.5. If R.sub.1 or R.sub.2 is --(CH.sub.2).sub.w R.sub.5, w may be an integer from one to twenty and R.sub.5 may be an hydroxyl, halo, C.sub.1-8 alkoxyl group or a substituted or unsubstituted carbocycle or heterocycle. Alternatively, R.sub.1 and R.sub.2 may jointly form a substituted or unsubstituted, saturated or unsaturated heterocycle having from four to eight carbon atoms, N being a hetero atom of the resulting heterocycle. R.sub.3 may be either hydrogen or C.sub.1-3. In the compounds, a total sum of carbon atoms comprising R.sub.1 or R.sub.2, (CH.sub.2).sub.n and (CH.sub.2).sub.m does not exceed forty. R.sub.

Abstract: Compounds capable of interacting with the strychnine-insensitive glycine modulatory site of the N-methyl-D-aspartate (NMDA) receptor are active in preventing or reducing dependence on dependence-inducing agents such as morphine, but lack the undesirable side-effects of agents hitherto employed for this purpose.

Abstract: The invention relates to new 1H-3-aryl-pyrrolidine-2,4-dione derivatives of the formula (I) ##STR1## in which A, B, X, Y and G have the meanings given in the description, to a plurality of processes for their preparation, and to their use as pesticides.

Abstract: There are provided substituted 3-aryl-pyrrolidine-2,4-dione derivatives of the formula (I) ##STR1## The new compounds (I) have highly pronounced insecticidal, acaricidal and herbicidal properties.

Abstract: The use of NMDA receptor antagonists or their physiologically compatible salts for preventing the development of tolerance during the long-term treatment with benzodiazepine-receptor-binding active ingredients as well as the combination of new pharmaceutical agents with benzodiazepine-receptor-binding active ingredients is described.

Abstract: Maleimide pesticides having enhanced efficacy represented by the formula (I), ##STR1## wherein X represents a halogen atom or a hydrogen atom, and R represents an alkyl group a cycloalkyl or haloalkyl group, a pesticidal composition containing the same as an active ingredient, and a process for producing the same.

Abstract: There are provided novel substituted 3-aryl-pyrrolidine-2,4-dione derivatives of the formula (I) ##STR1## in which X represents alkyl, halogen or alkoxy,Y represents hydrogen, alkyl, halogen, alkoxy or halogenoalkyl,Z represents alkyl, halogen or alkoxy,n represents a number from 0-3,A represents hydrogen, or represents alkyl, alkoxyalkyl or alkylthioalkyl, each of which is optionally substituted by halogen, cycloalkyl which is optionally interrupted by hetero atoms, or represents aryl, arylalkyl or hetaryl, each of which is optionally substituted by halogen-, alkyl-, halogenoalkyl-, alkoxy- or nitro,B represents hydrogen, alkyl or alkoxyalkyl,or in whichA and B together with the carbon atom to which they are bonded form an optionally substituted saturated or unsaturated cycle which can be interrupted by oxygen and/or sulphur.R represents the groups ##STR2## in which L, M as well as R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 have the meaning given inthe text of the application.

Abstract: Ionene polymers having biologically-active organic and/or inorganic anions are described. Methods to prepare the ionene polymers, compositions containing them and their methods of use are also described.

Abstract: A physiologically acceptable, radiolabelled compound of general formula ##STR1## where k is an integer from 2 to 5l is an integer from 1 to 5X and Y are independently selected from phenyl or naphthyl radical each of which can be substituted by one or more amino, mono- or di- substituted amino, halogen, hydroxy, mercapto, nitro, cyano, thiocyano, alkyl, alkoxy, halogenoalkyl, acyl, acylamino, acyloxy, carboxyl, alkoxycarbonyl, carbamoyl, pyridoylamino, N-carboxyalkyl-carbamoyl, sulpho, sulphamoyl, mono- or dialkylated or phenylated sulphamoyl which can also carry one or more substituents R', alkylsulphonyl, alkoxysulphonyl, --(CH.sub.2).sub.p NHCOR", --COR" or by an optionally hydroxy-containing phenylsulphonyl or phenoxysulphonyl; or X and Y are independently selected from pyridine or quinoline radical each of which can be substituted by amine, halogen, hydroxy, alkyl, or carbamoyl; where R' is as defined for X and Y; R" is alkyl-L where L is halogen or other leaving group; 2,5-diketo-pyrrolinyl, --Het--CH.

Abstract: The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises substituted or unsubstituted tetramic and tetronic acids capable of inhibiting the formation of advanced glycosylation endproducts of target proteins by reacting with a carbonyl moiety of an early glycosylation product of such target proteins formed by their initial glycosylation. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.

Abstract: Novel succinimide derivatives of formula I!: ##STR1## wherein Ring A is tri-lower alkoxyphenyl, R.sup.1 and R.sup.2 combine each other to form a group of the formula:>N--R.sup.3or one of R.sup.1 and R.sup.2 is lower alkoxy, and the other is group of the formula: --NHR.sup.3, in which R.sup.3 is hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkoxy, substituted or unsubstituted amino, hydroxy or pyridylcarbonyl, or salts thereof, these compounds have excellent antithrombotic activity and are useful as antithrombotic drug, or synthetic intermediate for preparing other antithrombotic drug.

Abstract: The invention provides a concentrate for dilution with water in the preparation of an agriculatural composition for application to crops, soil or animals and comprising an agricultural chemical whose agricultural activity varies with the pH of the water; and the invention provides a method of preparing such agricultural composition by mixing the concentrate with water and effecting such pH modification to the composition as is necessary to obtain a pH in the composition at which the agricultural activity of the chemical is acceptable. The concentrate comprises an active ingredient and a pH indicator for colouring the water, and the proportions of pH indicator and active ingredient are selected so that when the concentrate is diluted with water to provide an effective concentration of active ingredient in the water, the pH indicator indicates visually whether or not the pH of the water is suitable for acceptable agricultural activiy of the chemical.

Abstract: Haloalkylthio, -sulfinyl and -sulfonyl arylpyrrole compounds which are effective for the control of insects and acarids are described. A method for the insecticidal and acaricidal use of said compounds and methods for the preparation of said compounds are presented.

Abstract: The present invention includes N-substituted maleimides (1(H)-Pyrrole-2,5-dione (Maleimide) analogs and succinimides which act as potent nonsteroidal anti-inflammatory drugs and are capable of dual inactivation or selective inactivation of the cyclooxygenase and the peroxidase activities of prostaglandin endoperoxide synthase (PGHS).

Abstract: A method of controlling the attachment of organisms to an underwater surface is disclosed. The method comprises contacting the organisms with a compound of Formula I ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are each independently hydrogen, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, halogen, or hydroxyl. Antifouling coatings and cementitious compositions containing a compound of Formula I are also disclosed.

Abstract: Therapeutic compounds have the formula:(X)j-(non-cyclic core moiety),j being an integer from one to three, the core moiety is non-cyclic and X is a racemic mixture, R or S enantiomer, solvate, hydrate, or salt of: ##STR1## *C is a chiral carbon atom, n is an integer from one to four (preferably from one to three), one or more carbon atoms of (CH.sub.2).sub.n may be substituted by a keto or hydroxy group, and m is an integer from one to fourteen. Independently, R.sub.1 and R.sub.2 may be a hydrogen, a straight or branched chain alkane or alkene of up to twelve carbon atoms in length, or --(CH.sub.2).sub.w R.sub.5, w being an integer from two to fourteen and R.sub.5 being a mono-, di- or tri-substituted or unsubstituted aryl group, substituents on R.sub.5 being hydroxy, chloro, fluoro, bromo, or C.sub.1-6 alkoxy. Or jointly, R.sub.1 and R.sub.2 form a substituted or unsubstituted, saturated or unsaturated heterocyclic group having from four to eight carbon atoms, N being a hetero atom. R.sub.

Abstract: A composition comprising (a) a metal salt or complex with an organic compound of the general formula ##STR1## and (b) an oxy-phosphorus compound where W may be --SH or an optionally substituted hydrocarbyl group, Q is --OH, hydrogen or optionally substituted hydrocarbyl and Z is hydrogen or optionally substituted hydrocarbyl and Q and Z or Z and W may complete a ring. The compounds are typically metal complexes of thiohydroxamic acids or dithiocarbamates. The metal is typically zinc. The compositions exhibit improved aqueous solubility compared with the metal complexes alone, and can be used as industrial biocides, especially fungicides and particularly in paint films and latices.

Abstract: The invention relates to novel combined compositions for combatting plant, animal and sanitarian as well as forestry, horticultural and warehouse pests. These compositions contain a pyrethroid-type insecticide as an insecticidally active ingredient and at least one fungicide inhibiting the ergosterol biosynthesis as activity-strengthening agent as well as optionally piperonylbutoxide and other additives.The advantages of the compositions according to the invention consist therein that the activity-strengthening substances used are fungicidal agents widely used and have an advantageous toxicology. The activity-strengthening agent exerts a synergistic effect together with the pyrethroid-type insecticide.The combinations according to the invention bear an outstanding importance in the protection of stored crops.

Abstract: A class of 4-hydroxy-2(1H)-pyrrolone derivatives, substituted at the 3-position by an optionally substituted aryl substituent, are selective non-competitive antagonists of NMDA receptors and/or are antagonists of AMPA receptors, and are therefore of utility in the treatment of conditions, such as neurodegenerative disorders, convulsions or schizophrenia, which require the administration of an NMDA and/or AMPA receptor antagonist.

Abstract: The use of the compound 2R,5R-dihydroxymethyl-3R,4R-dihydroxypyrrolidine (DMDP) ##STR1## or an acid addition salt thereof in controlling diseases caused by parasitic nematodes in plants or mammals.

Abstract: Heterocylic chelating agents and salts thereof of formula I: ##STR1## wherein X represents a bond, O or S, or a group CHR.sup.1 or NR.sup.3 ; R.sup.1 represents H, a group OR.sup.3 or NR.sup.3 R.sup.3, or an alkyl or alkoxyalkyl group optionally substituted by a hydroxyl group or by a group NR.sup.3 R.sup.3 or CON.sup.3 R.sup.3 ;each R.sup.2 represents H, or an alkyl or alkoxy group optionally substituted by a hydroxyl or alkoxy group;each R.sup.3 represents H, an optionally hydroxylated alkyl group or a group CH.sub.2 Y;Y represents a group COZ, CON(OH)R.sup.4, POZ.sub.2 or SO.sub.2 Z;Z represents a group OR.sup.4, NR.sup.4 R.sup.4 or ##STR2## where each R.sup.11 is H, a hydroxyl group or an optionally hydroxylated alkyl group, s is 0, 1 or 2, and W is CHR.sup.11, NR.sup.11 or an oxygen atom; andeach R.sup.4 represents H, or an optionally mono- or poly-hydroxylated alkyl, alkoxyalkyl or polyalkoxyalkyl group;with the provisos that where s is 0 then W is CHR.sup.11 and that where X represents a bond or CHR.

Abstract: Maleimide derivatives of oxotremorine and their alkylthiol addition products having the general formulae: ##STR1## wherein R.sub.1 and R.sub.2 are independently alkyl, hydroxyalkyl, acyloxy, trialkylsilyloxy or R.sub.1 and R.sub.2 taken together are substituted or unsubstituted pyrrolidine or piperidine, and pharmaceutical compositions for the treatment of central cholinergic disfunction.

Abstract: There are provided N-oxy- and thioalkylcarbonyloxyalkylpyrrole compounds of formula I and their use for the control of insects, acarina and mollusks. Further provided are compositions and methods comprising those compounds for the protection of plants from attack by insects, acarina and mollusks.

Abstract: There are provided N-aminoalkylcarbonyloxyalkylpyrrole compounds of formula I ##STR1## and their use for the control of insects, acarina and mollusks. Further provided are compositions and methods comprising those compounds for the protection of plants from attack by insects, acarina and mollusks.

Abstract: N-succinimidyl and N-phthalimidyl esters of phenylalkanoic acid derivatives which are useful as inhibitors of HLE or HNE.

Abstract: The present invention relates to new tetralones having the formula I: ##STR1## wherein: R.sup.1 and R.sup.2 represent hydrogen, halogen, cyano, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trifluoromethyl, pentafluoroethyl, ethynyl, trimethylsilylethynyl, C.sub.1-4 alkylcarbonylamino being the amino optionally substituted by a C.sub.1-4 alkyl group; R.sup.3 is hydrogen or C.sub.1-4 alkyl, and R.sup.4 is C.sub.1-4 alkyl, or R.sup.3 and R.sup.4 together form a C.sub.2-5 polymethylene chain; either R.sup.5 represents hydroxyl, acetoxy or formyloxy and R.sup.6 and R.sup.7 are both hydrogen, or R.sup.5 together with R.sup.6 form a carbonyl group and R.sup.7 is hydrogen, or R.sup.5 and R.sup.7 together form a bond and R.sup.6 is hydrogen; R.sup.8 is, among others, 1,2-dihydro-2-oxo-1-pyridyl, 2,3-dihydro-1-oxo-1H-isoindol-2-yl, 2-oxo-1-pyrrolidinyl, 2-oxo-1-pyperidinyl. The invention also relates to a procedure for their preparation and to pharmaceutical compositions containing them.

Abstract: There are described a phenoxybenzene derivative having the formula (I): ##STR1## wherein R.sup.1 is hydrogen atom; an alkyl group having 1 to 3 carbon atoms; --OR.sup.6 or a halogen atom,R.sup.2 is hydrogen atom, nitro group or amino group,R.sup.3 is hydrogen atom, an alkyl group having 1 to 8 carbon atoms, a cycloalkyl group having 3 to 5 carbon atoms, allyl group, vinyl group or --(CH.sub.2)n.sup.1 R.sup.7R.sup.4 is hydrogen atom, an alkyl group having 1 to 3 carbon atoms or --(CH.sub.2)n.sup.3 R.sup.25R.sup.5 hydrogen atom; an alkyl group having 1 to 3 carbon atoms; or phenyl group,X is ##STR2## wherein Y is oxygen atom or sulfur atom; or --CHR.sup.27 -- and line means a single bond or a double bond provided that n is 2 in case that the line means a single bond and n is 1 in case that the line means a double bond, ora pharmacologically acceptable salt thereof,a cognition enhancer comprising the same as an effective ingredient andan antidepressant comprising the same as an effective ingredient.

Abstract: Glucosidase I inhibitors as therapeutic agents for combatting nondefective retroviral pathogens, including the aetiological agents of AIDS and feline leukemia. Administration of a processing glucosidase I inhibitor, preferably castanospermine, interrupts the replication of the retrovirus in infected cells, alleviates pathogenic effects associated with the presentation of viral env glycoproteins on infected cells, and may furthermore prevent infection of target cells by interrupting expression of endogenous receptors recognized by the virion.

Abstract: Novel N-oxygenated arylpyrrole compounds which are effective for the control of insects, acarids and nematodes are described. A method for the insecticidal, acaricidal and nematicidal use of said compounds and a method for the preparation of said compounds are presented.

Abstract: There are provided N-substituted carbonyloxyalkylpyrrole compounds of formula I ##STR1## and their use for the control of insects, acarina and mollusks. Further provided are compositions and methods comprising those compounds for the protection of plants from attack by insects, acarina and mollusks.

Abstract: 2-Phenylalkanoate esters which are useful as inhibitors of human leukocyte elastase.

Abstract: A compound of formula (I): ##STR1## in which R, R.sub.1 and R.sub.2 are as defined in the description. Medicinal product, which is useful in treating disorders related to a dysfunction of GABA.sub.B receptors.

Abstract: 1-arylsulphonyl-2-pyrrolidone derivatives for treating spasmodic disorders in gastro-enterology, in gynaecology, in obstetrics, in urology; intermediates in the preparation of such products; methods for preparing such products and pharmaceutical preparations containing such products.

Abstract: 1,2,3,4-tetrahydronaphthlamines of formula (1) ##STR1## wherein R is H or OCH.sub.3 ; ##STR2## is either at 1 or 2 position R.sub.1 is H;R.sub.2 is selected from:L-prolyl, optionally N-substituted with acetyl or carbobenzoxy,L-pyroglutamyl,(pyrrolidin-2-one-1-yl)acetyl,3-carboxy-2-hydroxypropyl:or R.sub.1 and R.sub.2 taken together with the nitrogen atom form the ring ##STR3## wherein n=1,2,3 and R.sub.3 -H, OH are nootropic substances potent enhancers of learning processes and memory.Orally or parenterally administrable pharmaceutical compositions in unit dosage form comprise between about 100 and about 500 mg of a compound of formula (1).

Abstract: Substituted-1-arylpyrrole compounds of general formula (I) below, are useful as pesticides, in particular for the control of insects, arachnids, and nematodes. Processes to make the compounds and intermediates used for their preparation are described. Additionally, compositions containing the compounds and methods of use therefore are provided. Preferred compounds are the compounds of general formula (I) ##STR1## wherein typically preferred substituents are: X is halogen or a group R.sup.5 S(O).sub.n, in which n is 0, 1, or 2 and R.sup.5 is CH.sub.3, CF.sub.3, CCl.sub.3, CF.sub.2 Cl, CFCl.sub.2, CF.sub.2 Br, CHF.sub.2, CHCl.sub.2 or CHClF;R.sup.1 is H, F, Cl, Br, OCH.sub.3, SCH.sub.3, or CH.sub.3 optionally substituted;R.sup.2 is CN;R.sup.3 is H, F, Cl, Br, OCH.sub.3, or CH.sub.3 optionally substituted;Y is CF.sub.3, CF.sub.3 O, H, F, Cl or Br;X.sup.1 and X.sup.4 are individually H, F, Cl, Br, CH.sub.3, OCH.sub.3 or SCH.sub.3 ; andX.sup.2 and X.sup.3 are each H.

Abstract: A method of treating anxiety with the aid of R(+)-3-amino-1-hydroxypyrrolidin-2-one of the formula ##STR1## is disclosed.

Abstract: The dermal use of non-irritating retinoids such as the esters and amides of 13-cis and 13-trans-retinoic acid for effecting the reduction and reversal of photoaging and skin cancer is disclosed.

Abstract: This invention relates to a method for administering systemically active agents including therapeutic agents through the skin or mucosal membranes of humans and animals and into the blood stream in a transdermal device or formulation comprising topically administering with said systemic agent an effective amount of a membrane penetration enhancer being a carboxylic acid derivative or a salt thereof represented in one embodiment by the general formula ##STR1## wherein W represents oxygen, sulfur, or two hydrogen radicals; wherein Z represents oxygen, sulfur, or --CH.sub.2 --;wherein R represents alkyl optionally substituted with one to three double or triple bonds, --SR'", --OR'", --NHR'", --CH.sub.3, or COOR.sub.1, and wherein R.sub.1 represents hydrogen or lower alkyl;wherein R'" represents alkyl, alkylthioalkyl, alkoxyalkyl, substituted aminoalkyl, optionally substituted with a phenyl, benzoyl or heterocyclic group;wherein R' represents hydrogen, alkyl, alkoxy, acyloxy, alkylthio, hydroxy, --(CH.sub.2).sub.

Abstract: Optically active or racemic compounds are provided having the formula ##STR1## where R.sub.2, R.sub.3, R.sub.4 and R.sub.6 are defined in the specification; R.sub.1 is selected from the group consisting of ##STR2## wherein Y is selected from the group consisting of hydroxy, nitro, cyano, azido, amino, acylamino, carboxyamido, trifluoromethyl, sulfate, sulfonamido, halogen, hydrocarbyl and hetero atom-substituted hydrocarbyl radicals, wherein said heteroatoms are selected from the group consisting of halogen, nitrogen, oxygen, sulfur and phosphorus and said hydrocarbyl radicals comprise from 1 to 12, preferably 1 to 6, carbon atoms, and a is an integer of from zero to 3, for instance zero to 2; and pharmaceutically acceptable salts thereof; as dopaminergics.

Abstract: Substituted furan and pyrrole compounds which are useful in inhibiting lipoxygenase enzymes, particularly 5-lipoxygenase.

Abstract: The dermal use of non-irritating retinoids such as the esters and amides of 13-cis and 13-trans-retinoic acid for effecting the reduction and reversal of photoaging and skin cancer is disclosed.

Abstract: The invention relates to diketontrile derivatives which have been discovered useful against arthropods, plant nematodes, helminth protozoan pests or as intermediates for such useful compounds which have a general formula: ##STR1##