Abstract: Isoindole compounds of the formula (I) ##STR1## wherein R.sub.1 represents hydrogen; C.sub.1 -C.sub.6 alkyl; benzyl optionally substituted with halogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, methylenedioxy; C.sub.2 -C.sub.8 aliphatic acyl; benzoyl optionally substituted with halogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.6 alkanoyl, C.sub.2 -C.sub.6 alkanoyloxy, C.sub.1 -C.sub.4 alkyl, trifluoromethyl, methylenedioxy;R.sub.2 -R.sub.3 are selected independently from hydrogen; halogen; C.sub.1 -C.sub.4 alkyl; trifluoromethyl; hydroxy; nitro; amino; mono or di C.sub.1 -C.sub.4 alkylamino; cyano; C.sub.1 -C.sub.6 alkoxy; C.sub.2 -C.sub.6 alkoxycarbonyl;Y is ethylene, or a straight or branched alkylene chain containing from 3 to 6 carbon atoms, and the salts thereof of pharmaceutically acceptable acids. The compounds possess antianginal activity and are used in the preparation of medicaments for antianginal therapy.

Abstract: Polyimides can be obtained by reacting a dianhydride component comprising 3,4,3',4'-bisphenyltetracarboxylic dianhydride, oxydiphthalic dianhydride and in addition further aromatic dianhydrides, and a diamine component comprising diamines of the formula ##STR1## and in addition further aromatic diamines.

Abstract: 1,4-dihydropyridine derivatives and optically active 1,4-dihydropyridine derivatives with the following formula, having vasodilating activity based on calcium antagonism, and PAF antaognism, and methods of producing the same are disclosed: ##STR1## wherein (*) indicates a chiral center in the case of the optically active 1,4-dihydropyridine derivatives.

Abstract: The invention concerns a bicyclic heterocyclic derivative of the formula I ##STR1## wherein Q is an optionally substituted 9-membered bicyclic heterocyclic moiety containing 1 or 2 N's and optionally a further N, O or S heteroatom;A.sup.1 is a direct link to X.sup.1 or (1-3C)alkylene;X.sup.1 is oxy, thio, sulphinyl, sulphonyl or imino;Ar is optionally substituted phenylene or pyridylene;R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- which, together with the carbon atom to which A.sup.2 and A.sup.3 are attached, defines a ring having 5 to 7 ring atoms, wherein each of A.sup.2 and A.sup.3 is (1-3C)alkylene and X.sup.2 is oxy, thio, sulphinyl or sulphonyl;or a pharmaceutically-acceptable salt thereof.The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.

Abstract: A class of imidazo[1,2-a]pyridinylalkyl phosphonic acid compounds is described for treatment to reduce neurotoxic injury associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of a compound of this class alone or in a composition in an amount effective as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites. Compounds of most interest are those of the formula: ##STR1## and the carboxylic and phosphonic alkyl esters and salts thereof; wherein the substituents are defined herein.

Abstract: A method for preparing an aromatic ether bisimide is provided. The mixture obtained from reacting a substituted phthalimide with a metal salt of a hydroxy aromatic compound in a non-polar solvent is extracted with about 4% to about 6% by weight aqueous alkali hydroxide solution to remove the reaction's by-products and thus provide substantially pure aromatic ether bisimide. The method is particularly suitable for extracting aromatic ether bisimide by-products from a continuous process preparing aromatic ether bisimide.

Abstract: 3-Piperidino-1-chromanol derivatives and analogs having the formula ##STR1## wherein A and B are taken together and are --CH.sub.2 CH.sub.2 -- or A and B are taken separately and are each H;X is CH.sub.2 or O;X.sup.1 is H or OH;Z is H, F, Cl, Br or OH;Z.sup.1 is H, F, Cl, Br or (C.sub.1 -C.sub.3)alkyl;n is 0 or 1; andm is 0 or an integer from 1 to 6;pharmaceutical compositions thereof; methods of treating CNS disorders therewith; and intermediates useful in the preparation of said compounds.

Abstract: There is described novel (N-phthalimidoalkyl) piperidine compounds which exhibit selective sigma-receptor antagonism and therefore are useful in the treatment of physiological or drug induced psychosis and dyskinesia in a mammal. Also described are pharmaceutical compositions containing sigma selective compounds and methods of using these compositions for treating physiological or drug induced psychosis or dyskinesia in a mammal. Further provided are methods for preparing the compounds of this invention.

Abstract: The invention concerns 4-hydroxy-5-methoxyindole and 5-ethoxy-4-hydroxy-2-methylindole which are useful as dyes for dyeing keratin materials.

Abstract: The present invention provides processes for the synthesis of kainic acid. More specifically, the present invention is directed to a process for preparing a compound of the formula ##STR1## wherein R.sub.1 is hydrogen, acyl, alkoxycarbonyl, or arylalkoxycarbonyl;R.sub.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, aryl, or arylalkyl; andR.sub.3 is hydrogen, C.sub.1 -C.sub.6 alkyl, aryl, or arylalkyl.The present invention also provides processes for the preparation of intermediates that are useful for the synthesis of kainic acid. More specifically, the present invention provides processes for preparing a compound of the formula ##STR2## wherein R.sub.4 is hydrogen, acyl , alkoxycarbonyl, or arylalkoxycarbonyl; andR.sub.5 is hydrogen, C.sub.1 -C.sub.6 alkyl, or arylalkyl.

Abstract: A physical form of (R)-3-methoxy-4-[1-methyl-5-(2-methyl-4,4,4-trifluorobutylcarbamoyl)indol -3-ylmethyl]-N-(2-methylphenylsulphonyl)benzamide substantially free of other physical forms, which form is crystalline and has an X-ray powder diffraction pattern with specific peaks at 2.theta.=14.0, 19.4, 22.0, 22.4 and 24.7.degree. , processes for preparing the form and pharmaceutical compositions containing it. The compound is a leukotriene antagonist useful in the treatment of diseases such as asthma.

Abstract: The present invention relates to a series of novel imidazolinium quaternary polymers. The compounds of the present invent ion are prepared by the reaction of chloracetic acid with a pendant hydroxyl group which is present on a polyoxyalkylene polymer, followed by the reaction of the halo-ester with a tertiary amine to give a quaternary compound. In a preferred embodiment the polyoxyalkylene glycol has been prepared by the reaction of both ethylene oxide and propylene oxide. In a more preferred embodiment, the ethylene oxide is at the terminal portion of the molecule and the propylene oxide is in the center.

Abstract: Novel indanes in all possible stereoisomer forms of the formula ##STR1## wherein the substrates are as defined in the application and their non-toxic, pharmaceutically acceptable acid addition salts and their hydrates are disclosed as having central analgesic properties as well as antiarrhythmic and diuretic activities.

Abstract: The process for the preparation of chiral 3-(1-amino-1,1-bisalkylmethyl)-1-substituted-pyrrolidines used as key intermediates for the preparation of naphthyridine and quinolone antibacterial agents which comprises reacting readily available chiral 1-substituted-3-pyrrolidinols to their corresponding chiral sulfonate esters; converting the sulfonate esters to chiral 1-substituted-3-cyanopyrrolidines having an inverse configuration, and then dialkylating the chiral cyanopyrrolidines with alkyl lithium in the presence of a Lewis acid without racemization at the asymmetric carbon atom is described.

Abstract: Plant growth regulators comprising, as an active ingredient, a substituted dicarboxylic acid derivative having the formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same as defined in the present specification, the substituted dicarboxylic acid derivatives, and processes for preparing the same, are disclosed. The plant growth regulators provided according to the present invention have a regulating activity on plant growth; more specifically, an action thereof of lowering the content of endogenous ethylene in a plant is utilized.

Abstract: Lysine and arginine salts of thionaphthene-2-carboxylic acid (TNCA) are disclosed. These compounds are useful as treatments for osteoporosis and exhibit an increased water solubility.

Abstract: A method of protecting 3-isothiazolones of the formula: ##STR1## wherein Y is (C.sub.1 -C.sub.18)alkyl or (C.sub.3 -C.sub.12)cycloalkyl each optionally substituted with one or more of hydroxy, halo, cyano, alkylamino, dialkylamine, arylamino, carboxy, carbalkoxy, alkoxy, aryloxy, alkylthio, arylthio, haloalkoxy, cycloaklylamino, carbamoxy, or isothiazolonyl; an unsubstituted or halo-substituted (C.sub.2 -C.sub.8)alkenyl or alkynyl; a (C.sub.7 -C.sub.10)aralkyl optionally substituted with one or more of halogen, (C.sub.1 -C.sub.4)alkyl or (C.sub.1 -C.sub.4)alkoxy; and an aryl optionally substituted with one or more of halogen, nitro, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkyl-acylamino, carb(C.sub.1 -C.sub.4)alkoxy or sulfamyl; and R and R.sup.1 is each independently H, halogen (C.sub.1 -C.sub.4)alkyl, (C.sub.4 -C.sub.

Abstract: A novel prolinal derivative of the general formula: ##STR1## [wherein A represents alkylene or alkenylene group of from 1 to 8 carbon atom(s) or a saturated hydrocarbon ring of from 3 to 7 carbon atoms, R represents hydrogen atom, phenyl group, benzyl group, alkyl group of from 1 to 8 carbon atom(s) or cycloalkyl group of from 3 to 7 carbon atoms,B represents alkylene group of from 1 to 8 atom(s) unsubstituted or substituted by phenyl group or benzyl group, or a single bond,D represents carbocyclic or heterocyclic ring unsubstituted or substituted by from one to three of halogen atom, alkyl or alkoxy group of from 1 to 4 carbon atom(s), nitro group or trifluoromethyl group.]possess inhibitory activity on prolyl endopeptidase, and therefore are useful for treating and/or preventing agent as a amnesia.

Abstract: A process of preparing 1,3,3-trinitroazetidine including forming a 5-hydroxymethyl-5-nitro-1-alkyltetrahydro-1,3-oxazine, e.g., reacting a 1,3,5-trialkyl hexahydrotriazine and tris(hydroxymethyl)nitromethane, ring opening said 5-hydroxymethyl-5-nitro-1-alkyltetrahydro-1,3-oxazine to form a 3-alkylamino-2-hydroxymethyl-2-nitro-1-propanol salt, ring closing said 3-alkylamino-2-hydroxymethyl-2-nitro-1-propanol salt to form a 3-hydroxymethyl-3-nitro-1-alkylazetidine salt, nitrating said 3-hydroxymethyl-3-nitro-1-alkylazetidine salt to form a 1-alkyl-3,3-dinitroazetidine, and converting said 1-alkyl-3,3-dinitroazetidine into 1,3,3-trinitroazetidine is disclosed.

Abstract: A method is provided for preparing a chiral benzaldehyde of the structure ##STR1## by acylating an anhydride of the structure ##STR2## with a chiral oxazolidine of the structure ##STR3## where Q is MgHal or Li, and X, Y and Z are as described herein, to form a keto acid which is reduced and cyclized. The resulting benzaldehyde may be used in making the final anti-thrombotic - anti-vasospastic compounds. Novel intermediates are also provided.