Abstract: Substituted dihydrophthalazine compositions are provided which are active as non-NMDA ionotropic excitatory amino acid (EAA) receptor antagonists. The compositions are useful for treating disorders associated with excessive activation of the non-NMDA subtype of the ionotropic EAA receptor. The compounds further are useful as testing agents to identify and characterize other compounds for the treatment of these disorders. The compounds are useful therapeutically as sedatives or for the treatment of neurosychopharmacological disorders such as stroke, ischemia and epilepsy. The compositions may be provided in combination with a suitable carrier for oral or parenteral administration. The compounds may be administered orally or parenterally for the treatment of a variety of disorders associated with non-NMDA EEA receptor function.

Abstract: Novel compounds of the formula ?1! are disclosed, wherein X is hydrogen, fluorine or chlorine; Y is fluorine, chlorine or bromine; R.sup.1 is hydrogen or C.sub.1 -C.sub.3 alkyl; and R.sup.2 and Q are various groups. Also disclosed are herbicidal compositions containing these compounds as active ingredients and methods for controlling unfavorable weeds by application of these compounds.

Abstract: Hetaryloxy-.beta.-carbolines of formula I ##STR1## in which R.sup.A means a triazine or benzocondensed hetaryl radical with 1-2 nitrogen atoms optionally substituted with halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, trifluoromethyl or SO.sub.2 --R.sup.1 or a 5- or 6-membered hetaryl radical with 1-2 nitrogen atoms substituted with halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, trifluoromethyl or SO.sub.2 --R.sup.1are useful pharmaceutical agents.

Abstract: The present invention relates to imidazoquinazoline derivatives represented by formula (I): ##STR1## wherein R.sup.1 represents hydrogen, substituted or unsubstituted lower alkyl, cycloalkyl, lower alkenyl, substituted or unsubstituted aralkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroarylalkyl, or substituted or unsubstituted heteroaryl, R.sup.2 and R.sup.3 represent independently hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted aralkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroarylalkyl, or substituted or unsubstituted heteroaryl, or R.sup.2 and R.sup.3 are combined to represent a heterocyclic group containing a nitrogen atom, R.sup.4 represents hydrogen or substituted or unsubstituted lower alkyl, X represents O or S, Y represents a single bond or O, n represents 0, 1, 2, or 3, and pharmaceutically acceptable salts thereof.

Abstract: Novel substituted phthalazinones of the formula (I) ##STR1## are useful as neurotensin antagonists.

Abstract: The present invention relates to an adenosine uptake inhibitor and an agent for the myocardium protection or the prevention or treatment of inflammatory edema, comprising a 1,2,3,4-tetrahydro-2,4-dioxoquinazoline derivative represented by formula (I): ##STR1## wherein R.sup.1 represents hydrogen, substituted or unsubstituted lower alkyl, alkenyl, or substituted or unsubstituted aralkyl; R.sup.2, R.sup.3, R.sup.4, and R.sup.5 independently represent hydrogen, halogen, amino, mono- or di(lower alkyl)amino, lower alkanoylamino, nitro, cyano, substituted or unsubstituted lower alkyl, hydroxy, lower alkoxy, lower alkylthio, carboxy, lower alkoxycarbonyl, lower alkanoyl, aralkyloxy, or lower alkanoyloxy; R.sup.6, R.sup.7, R.sup.8, and R.sup.9 independently represent hydrogen, hydroxy, substituted or unsubstituted lower alkoxy, or aralkyloxy, or any adjoining two of them are combined to form methylenedioxy; R.sup.10 represents hydrogen or lower alkyl; and Y and Z independently represent N or C--R.sup.11 (wherein R.

Abstract: The present invention discloses novel substituted aryl- and heteroarylphenyloxazolidinones which are useful as anti-bacterial agents. More specifically, the substituted aryl- and heteroarylphenyloxazolidinones of the invention are characterized by oxazolidinones having aryl or heteroaryl group at the p-position of the 3-phenyl ring and additional substitutions at the m-position(s) of the 3-phenyl ring. A compound representative of this new class of oxazolidinones is (.+-.)-5-(acetamidomethyl)-3-[4-(3-pyridyl)-3,5-difluorophenyl]-2-oxazolid inone.

Abstract: The present invention relates to an adenosine uptake inhibitor and an agent for the myocardium protection or the prevention or treatment of inflammatory edema, comprising a 1,2,3,4-tetrahydro-2,4-dioxoquinazoline derivative represented by formula (I): ##STR1## wherein R.sup.1 represents hydrogen, substituted or unsubstituted lower alkyl, alkenyl, or substituted or unsubstituted aralkyl; R.sup.2, R.sup.3, R.sup.4, and R.sup.5 independently represent hydrogen, halogen, amino, mono- or di(lower alkyl)amino, lower alkanoylamino, nitro, cyano, substituted or unsubstituted lower alkyl, hydroxy, lower alkoxy, lower alkylthio, carboxy, lower alkoxycarbonyl, lower alkanoyl, aralkyloxy, or lower alkanoyloxy; R.sup.6, R.sup.7, R.sup.8, and R.sup.9 independently represent hydrogen, hydroxy, substituted or unsubstituted lower alkoxy, or aralkyloxy, or any adjoining two of them are combined to form methylenedioxy; R.sup.10 represents hydrogen or lower alkyl; and Y and Z independently represent N or C--R.sup.11 (wherein R.

Abstract: Compounds having the formula (I): ##STR1## and stereoisomers thereof, wherein A is hydrogen, halo, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 haloalkyl, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylcarbonyl, C.sub.1-4 alkoxycarbonyl, phenoxy, nitro or cyano; R.sup.1 and R.sup.2, which may be the same or different, are hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocyclylalkyl, optionally substituted cycloalkylalkyl, optionally substituted aralkyl, optionally substituted heteroarylalkyl, optionally substituted aryloxyalkyl, optionally substituted heteroaryloxyalkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted alkoxy, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted aryloxy, optionally substituted heteroaryloxy, nitro, halo, cyano, --NR.sup.3 R.sup.4, --CO.sub.2 R.sup.3, --CONR.sup.3 R.sup.4, --COR.sup.3, --S(O).sub.n R.sup.3 wherein n is 0, 1 or 2, (CH.sub.2).sub.m PO(OR.

Abstract: The present invention relates to an adenosine uptake inhibitor and an agent for the myocardium protection or the prevention or treatment of inflammatory edema, comprising a 1,2,3,4-tetrahydro-2,4-dioxoquinazoline derivative represented by formula (I): ##STR1## wherein R.sup.1 represents hydrogen, substituted or unsubstituted lower alkyl, alkenyl, or substituted or unsubstituted aralkyl; R.sup.2, R.sup.3, R.sup.4, and R.sup.5 independently represent hydrogen, halogen, amino, mono- or di(lower alkyl)amino, lower alkanoylamino, nitro, cyano, substituted or unsubstituted lower alkyl, hydroxy, lower alkoxy, lower alkylthio, carboxy, lower alkoxycarbonyl, lower alkanoyl, aralkyloxy, or lower alkanoyloxy; R.sup.6, R.sup.7, R.sup.8, and R.sup.9 independently represent hydrogen, hydroxy, substituted or unsubstituted lower alkoxy, or aralkyloxy, or any adjoining two of them are combined to form methylenedioxy; R.sup.10 represents hydrogen or lower alkyl; and Y and Z independently represent N or C--R.sup.11 (wherein R.

Abstract: The present invention relates to an adenosine uptake inhibitor and an agent for the myocardium protection or the prevention or treatment of inflammatory edema, comprising a 1,2,3,4-tetrahydro-2,4-dioxoquinazoline derivative represented by formula (I): ##STR1## wherein R.sup.1 represents hydrogen, substituted or unsubstituted lower alkyl, alkenyl, or substituted or unsubstituted aralkyl; R.sup.2, R.sup.3, R.sup.4, and R.sup.5 independently represent hydrogen, halogen, amino, mono- or di(lower alkyl)amino, lower alkanoylamino, nitro, cyano, substituted or unsubstituted lower alkyl, hydroxy, lower alkoxy, lower alkylthio, carboxy, lower alkoxycarbonyl, lower alkanoyl, aralkyloxy, or lower alkanoyloxy; R.sup.6, R.sup.7, R.sup.8, and R.sup.9 independently represent hydrogen, hydroxy, substituted or unsubstituted lower alkoxy, or aralkyloxy, or any adjoining two of them are combined to form methylenedioxy; R.sup.10 represents hydrogen or lower alkyl; and Y and Z independently represent N or C-R.sup.11 (wherein R.

Abstract: Metal-containing steroid mimic complexes are provided. Compositions containing a metal ion incorporated into a steroid skeleton structure and ligands useful in the preparation of such compositions are also provided. The metal ion is preferably a radionuclide, such as technetium, rhenium or gallium. Methods for using the metal complexes for diagnostic and therapeutic purposes are further provided.

Abstract: Substituted pyridines and pyrimidines, processes for their preparation and their use as pesticides and fungicides.The invention relates to compounds of the formula ##STR1## in which A is N or CH, R is H, halogen, alkyl or cycloalkyl, R.sup.2 and R.sup.3 are H, halogen or an aliphatic radical or together form a ring, X is O, NH Or S(O).sub.q where q=0, 1 or 2, R.sup.4.sub.q is 0-4 radicals selected from the series consisting of halogen, optionally substituted alkyl or alkoxy, cycloalkyl and optionally substituted phenyl, n=0-2, m=1-3 and Y is optionally substituted methylene or imino.The invention furthermore relates to a process for their preparation and for their use as pesticides, in particular as insecticides, acaricides and fungicides. The compounds are furthermore suitable for controlling nematodes, helminths and molluscs, and for controlling endoparasites and ectoparasites in the field of veterinary medicine.

Abstract: Hydrazone compound useful as an excellent organic nonlinear optical material and a highly sensitive coloring chelation agent, represented by the following formula (1): ##STR1## wherein Ar is a substituted or an non-substituted 2-imidazolyl group, a 4-imidazolyl group, 3-pyrazolyl group, 3-pyridazinyl, 2-pyrimidinyl, 4-pyrimidinyl, 2-quinolyl, 1-isoquinolyl, 3-isoquinolyl, 1-phthalazinyl, 2-quinazolinyl, 2-benzimidazolyl, 2-benzothiazolyl, or 2-thiazolyl group,R.sup.1 is a nitro group, cyano group or trifluoromethyl group,R.sup.2 is a nitro group, cyano group, trifluoromethyl group or a halogen atom, or a substituted or an non-substituted alkyl group,R.sup.3 is a hydrogen atom, andn is an integer from 0 to 3.

Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which R.sub.1, R.sub.2, R.sub.2', R.sub.2", R.sub.2'", R.sub.3 and n are as defined in the description, an optical isomer, and an addition salt thereof with a pharmaceutically-acceptable acid or base,and medicinal product containing the same useful for treating a mammal afflicted with a disorder associated to 5-HT.sub.1A or 5-HT.sub.2C receptors.

Abstract: There are provided nitrogen-containing bicyclic compounds, pharmaceutical compositions containing these compounds and methods of using these compounds to treat physiological or drug-induced psychosis or diskinesia in a mammal.

Abstract: Metal oxidizing agents (such as silver oxide or silver nitrate) are added to a solution of organic chemicals which comprise an unwanted level of organic reducing agents (either aqueous or organic solutions in which the metal oxidizing agent does not dissolve) and the metal oxidizing agent oxidizes at least some portion of said organic reducing agents. Because the metal oxidizing agent is insoluble in the solution, it is readily removed (e.g., by filtration or sedimentary techniques) to leave a solution with reduced amounts of reducing agents therein. This process is particularly useful for purifying phthalazine, behenic acid, and other toners, the component forming the counterion with silver ion in forming the light-insensitive silver source material and any other additives and raw materials which can be dissolved in a solvent medium in which the metal oxidizing agent is not highly soluble.

Abstract: The invention concerns the use of phthaloylhydrazide derivatives and their salts as anti-hypoxic and defensive agents, with special focus on the use of 5-aminophthaloylhydrazide and its salts, when administered in high doses.

Abstract: .beta.-Carboxy sulfonates of the formula ##STR1## wherein R.sub.1 is aryl, R.sub.3 and R.sub.4 are hydrogen or alkyl, Y is -O-, -S-, or -NR.sub.2 -, and R.sub.5 is alkyl or aryl are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT) and are thus useful for treating hypercholesterolemia and atherosclerosis.

Abstract: Novel 3,4-dihydro-4-oxo-3(prop-2-enyl)-1-phtalazineacetic acids and derivatives of formula (I) ##STR1## in which R.sub.1 R.sub.2 and R.sub.3 are the same or different and stand for H, a halogen or a linear or branched aliphatic, saturated or unsaturated radical, substituted or not by at least one halogen or R.sub.4 residue such as defined below, except when R.sub.4 is H; R.sub.4 and R.sub.5 are the same or different and stand for H, a linear or branched aliphatic radical, saturated or unsaturated, an aryl or heteroaryl radical, said radicals being substituted or not by at least one grouping such as fluorine, chlorine, bromine, methyl or trifluoromethyl, where R.sub.4 and R.sub.5 do not simultaneously denote H; R.sub.6 stands for hydroxy or alkoxy radical; R.sub.

Abstract: 6-amino carboxylic acid derivatives having antiasthmatic and antiallergic properties which can be used for the preparation of medicaments. The compounds have the formula: ##STR1## wherein R.sub.1 and R.sub.2 represent hydrogen, a straight-chain or branched alkyl radical with 1-6 carbon atoms, benzyl or phenylethyl, R.sub.3 represents hydrogen, a straight-chain or branched alkyl radical with 1-6 carbon atoms or benzyl, X represents hydrogen, halogen, C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.6 -alkoxy, Y.sub.1 and Y.sub.2 represent hydrogen, halogen, C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.6 -alkoxy, where m, n and o can assume the values from 0-4.

Abstract: The present invention involves photoprotective compositions which are useful for topical application to prevent damage to skin caused by acute or chronic exposure to ultraviolet light comprising chelating agents having the structure: ##STR1## wherein each --R.sup.1 is independently selected from the group consisting of alkyl, aryl, heteroaryl and heterocycle, or the --R.sup.1 's are covalently bonded together to form a cyclic alkyl or heterocyclic ring; --R.sup.2 and --R.sup.3 are --OR.sup.4, in which case there is no bond or a polar bond between --R.sup.2 and the nitrogen covalently bonded to --R.sup.3, each --R.sup.4 being independently selected from the group consisting of hydrogen, alkyl and aryl, except that both --R.sup.4 's are not methyl when both --R.sup.1 's are furyl; or --R.sup.2 is --O-- and is covalently bonded to the nitrogen which is covalently bonded to --R.sup.3, and --R.sup.3 is --O-- (there being a + charge on the nitrogen to which it is bonded) or nil;wherein the .alpha.

Abstract: A 3,6-disubstituted pyridazine derivative having excellent platelet agglutination inhibitory effects. It is useful for a preventive medicine or a therapeutic medicine for a cerebrovascular disorder such as cerebral thrombosis and cerebral embolism, an ischemic heart disease such as myocardial infarction, and a circulation disorder such as peripheral circulation disorder. A pharmaceutical composition containing a compound of the present invention as an effective ingredient and a process for preparing the same are also disclosed.

Abstract: Amide tetrazoles of the formula ##STR1## wherein aryl includes phenyl and naphthyl, unsubstituted or substituted, X is .dbd.O, .dbd.N--R.sub.5, or --NR.sub.3 R.sub.4, where R.sub.2, R.sub.4, and R.sub.5 include alkyl and alkoxy and R.sub.3 includes alkyl, are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT) and are thus useful for treating hypercholesterolemia or atherosclerosis.

Abstract: A method for reducing an .alpha.,.beta.-unsaturated ketone of the present invention includes the step of treating the .alpha.,.beta.-unsaturated ketone with a silyl compound in the presence of a Lewis acid and alcohol to selectively reduce the carbonyl group of the .alpha.,.beta.-unsaturated ketone. According to this method, a deoxy-compound can be obtained from the .alpha.,.beta.-unsaturated ketone by selectively reducing the carbonyl group without reducing an .alpha.,.beta.-unsaturated bond.

Abstract: Metal oxidizing agents (such as silver oxide or silver nitrate) are added to a solution of organic chemicals which comprise an unwanted level of organic reducing agents (either aqueous or organic solutions in which the metal oxidizing agent does not dissolve) and the metal oxidizing agent oxidizes at least some portion of said organic reducing agents. Because the metal oxidizing agent is insoluble in the solution, it is readily removed (e.g., by filtration or sedimentary techniques) to leave a solution with reduced amounts of reducing agents therein. This process is particularly useful for purifying phthalazine, behenic acid, and other toners, the component forming the counterion with silver ion in forming the light-insensitive silver source material and any other additives and raw materials which can be dissolved in a solvent medium in which the metal oxidizing agent is not highly soluble.

Abstract: There are provided novel nitrogen-containing bicyclic compounds which are useful in the treatment of physiological or drug induced psychosis or dyskinesia in a mammal. These novel compounds are selective sigma receptor antagonists and have a low potential for movement disorder side effects associated with typical antipsychotic agents.

Abstract: Triarylborane derivatives corresponding to the formula (1) ##STR1## in which R either represents a group --CR.sub.1 R.sub.2 R.sub.3 where R.sub.1, R.sub.2 and R.sub.3 are each, independently of one another, a (C.sub.1 -C.sub.2)alkyl or aryl group, or represents a group --CH.sub.2 OR.sub.4 where R.sub.4 is a (C.sub.1 -C.sub.2)alkyl or benzyl group, or represents a group --Si(R.sub.5).sub.3 where R.sub.5 is a (C.sub.1 -C.sub.2)alkyl or aryl group, R being in the 1 or 2 position of the tetrazole ring, their preparation and their use as synthesis intermediates.

Abstract: Cephalosporins derivatives having a 3-position substituent of the formula I are described: ##STR1## wherein R.sup.1 is hydrogen, alkenyl or optionally substituted alkyl, Het is a 5- or 6-membered heterocyclic ring bonded via a carbon atom to the amide linkage, wherein Het is selected from a group of the formulae II-III: ##STR2## wherein A is CH or a nitrogen atom; B is oxygen, sulphur or a group NR.sup.4 ; one or two of D, E, F and G are nitrogen atoms and the remainder are CH groups: or Het is a pyrazinone, pyridinone, pyridazinone or pyrimidinone ring, or is a thione equivalent of such a ring, said rings having a substituent R.sup.4 on one nitrogen atom, or is pyranone, or pyranthione; the ring Het being fused by any two adjacent carbon atoms to the benzene ring; and Het being attached to the --CH.sub.2 NR.sup.1 CO-- group via a carbon atomR.sup.2 is hydroxy or an in vivo hydrolysable ester thereof;R.sup.3 is ortho to R.sup.2 and is hydroxy or an in vivo hydrolysable ester thereof; and R.sup.

Abstract: Abstract of the Disclosure: Styrene derivatives I ##STR1## where R.sup.1 is H or halogen, R.sup.2 is halogen, R.sup.3 is H, halogen or C.sub.1 -C.sub.4 -alkyl, R.sup.4 is CN or C.sub.1 -C.sub.6 -alkylcarbonyl and A is a heterocyclic radical A.sub.1 to A.sub.5 : ##STR2## where R.sup.5 and R.sup.6 are H, CH.sub.3 or C.sub.2 H.sub.5, n is 0 or 1 and X is oxygen or sulfur, with the proviso that R.sup.4 is alkylcarbonyl when R.sup.1 is H and at the same time A is A.sub.2 where n is 0, and agriculturally useful salts thereof, processes for the preparation of the styrene derivatives I and herbicides containing them.

Abstract: Pharmacologically active compounds of the General Formula ##STR1## where X is oxygen or sulphur and the radical R represents a quinuclidyl radical, an C.sub.1 -C.sub.6 -alkyl radical, a phenyl radical, a pyridyl radical, a phenyl or pyridyl radical substituted by the radicals R.sub.1, R.sub.2, and/or R.sub.3, a C.sub.1 -C.sub.6 -alkyl radical substituted by pyridyl or alkylpyridyl or a C.sub.1 -C.sub.6 -alkyl radical substituted by phenyl, where each phenyl radical may also be substituted by the radicals R.sub.1, R.sub.2 and/or R.sub.3 and the radicals R.sub.1, R.sub.2 and R.sub.3 are the same or different and represent hydrogen, halogen, trihalogenmethyl, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, carboxy, Carb-C.sub.1 -C.sub.6 -alkoxy, amino, C.sub.1 -C.sub.6 -alkylamino, C.sub.1 -C.sub.6 -dialkylamino, C.sub.1 -C.sub.6 -trialkylamino, C.sub.2 -C.sub.6 -alkanoylamino, or C.sub.2 -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: Compounds useful as luminescent labelling reagents or reagents for determining hydrogen peroxide of the following formula: ##STR1## Wherein R is selected from the group consisting of hydrogen, amino, carboxyl, thiol, n-propyl, isopropyl, n-butyl, sec-butyl, benzyl, carboxyethyl, tert-butyl, and--(CH.sub.2).sub.n1 CH.sub.3 wherein n.sub. is 0 or an integer of 1-15;--(CH.sub.2).sub.n2 COOH wherein n.sub.2 is 0 or an integer of 1-5;--CH.sub.2 SH; --CH.sub.2 X.sub.1 wherein X is Br, Cl or F;--(CH.sub.2).sub.n3 NH.sub.2 wherein n.sub.3 is an integer of 1-5; ##STR2## wherein n.sub.4 is 0 or 1 and n.sub.5 is 0 or ##STR3## wherein n.sub.6 is 0 or 1 and X.sub.2 is H, Br, Cl, F or I; and --(CH.sub.2).sub.n7 R.sub.1 wherein n.sub.7 is 0 or an integer of 1-5 and R.sub.1 is selected from COCl, CON.sub.3, CONHNH.sub.

Abstract: The invention relates to novel ureas and urethanes of Formula I: ##STR1## which stimulate cytokine production and may be used to accelerate recovery from neutropenia accompanying radio- or chemotherapy, bone marrow transplantation, or infections. Compounds in the invention or pharmaceutical compositions employing these compounds may be useful in the treatment of cancer, AIDS, aplastic anemia, myelodysplastic syndrome, and infectious diseases, and in the enhancement of immune response.

Abstract: Benzamide derivatives of the following formula (I) ##STR1## [wherein R.sup.1 : ##STR2## B, D: hydrogen atom, etc. E: pyridyl group, etc.n: integer from 0 to 2R.sup.2 : R.sup.3 R.sup.4 N-- etc.(R.sup.3,R.sup.4 : optionally substituted C.sub.6 -C.sub.14 aryl group, etc.)A; ##STR3## --CH.sub.2 --, --N.dbd.N--, --CH.dbd.N--, --N.dbd.CH--, --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --].Optical antipodes thereof or pharmaceutically acceptable salts thereof, show excellent PAF antagonism and are effective for therapy and prophylaxis of diseases caused by PAF (bronchial asthma, nephritis, shocks, cardiac infarction, cerebral hemorrhage, ulcer, DIC, autoimmune diseases, thrombosis, etc.).

Abstract: A method of preparation of substituted halogenodiazines which are useful as intermediates in the synthesis of novel unfused heterobicyclic compounds, and the products thereof.The reaction consists of the addition of an organolithium reagent with subsequent dehydrogenation of the addition product. The reaction takes place in one reaction vessel, without isolation of the substituted halogenodihydrodiazine intermediate. The reactions proceed at moderate temperature and in a short amount of time, which decreases the probability of side reactions and increases yield. Furthermore, the workup step is conducted under two-phase conditions to prevent hydrolysis of the substituted halogenodiazine to a substituted hydroxydiazine. The method is easy, efficient and results in a high yield of product.

Abstract: A compound of the formula ##STR1## wherein A.sup.1 and A.sup.2 are independently N or CH;B is a covalent bond or C.dbd. O;R.sup.1 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sup.2 is hydrogen, fluorine, chlorine, bromine, trifluoromethyl, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, or C.sub.1 -C.sub.4 alkylthio;R.sup.3 is ##STR2## wherein R.sup.4 is phenyl optionally substituted;X is oxygen or sulphur;Y is hydrogen; or Y forms an indole group with the carbon on the ortho position of the phenyl in R.sup.4 ; or a pharmaceutically acceptable base salt thereof when R is hydrogen;with the proviso that when B is a covalent bond, A.sup.1 and A.sup.2 are each CH, and use for the inhibition of aldose reductase activity.

Abstract: Novel carbostyril derivatives of the formula: ##STR1## wherein X is 0 or S; Y is H or alkyl; R.sup.A is a group of the ##STR2## {wherein n is 1 or 2, A is alkylene, R.sup.1 is benzoyl having optionally 1-3 substituents, R.sup.2A is ##STR3## is (i) alkoxy, (ii) substituted or unsubstituted 5- or 6-membered heterocylic group, (iii) alkenylthio, (iv) pyrrolidinyl-alkyl--S--, (v) pyrrolidinyl-alkyl--SO--, (vi) pyrrolidinyl-alkyl--SO.sub.2 --, (vii) --O--B--NR.sup.4 R.sup.5 [B is alkylene having optionally OH, R.sup.4 is H, R.sup.5 is tricyclo[3.3.1.1]decanyl, tricyclo[3.3.1.1]decanylalkyl, etc., or R.sup.4 and R.sup.5 may together form a group of ##STR4## (R.sup.6 is substituted or unsubstituted amino)] or (viii) substituted alkoxy; m is 1 to 3]}, which have excellent vasopressin antagonistic activities and are useful as vasodilator, hypotensive agent, water diuretics, platelet agglutination inhibitor, and a vasopressin antagonistic composition containing the compound as the active ingredient.

Abstract: A class of novel heterocyclic aromatic carbamate compounds is described. A method of derivatizing amine-functional compounds with the novel carbamates is also disclosed. The derivatives can be detected using a fluorescence detector. The present composition and method allow femtomole quantities of amine compounds to be detected and measured.

Abstract: The present invention provides tertiary and secondary amine compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof which are antagonists for alpha-2 adrenoreceptors and which inhibit serotonin (5-hydroxytryptamine, 5-HT) uptake.

Abstract: Pyrimidine derivatives of the Formula Ia or Ib ##STR1## where the substituents have the following meanings: R.sup.1 is hydrogen or alkyl;A is a substituted or unsubstituted bi- or tricyclic carbo- or heterocyclic radical which may contain one or several double bonds;R.sup.5 is H or alkyl;X is halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio or haloalkylthio; and addition salts thereof with organic or inorganic acids and the use of said pyrimidine derivative to control undesirable plant growth.

Abstract: Osmium-catalyzed methods of addition to an olefin are discussed. In the method of asymmetric dihydroxylation of the present invention, an olefin, a chiral ligand, an organic solvent, an aqueous solution, a base, a ferricyanide salt and an osmium-containing compound are combined. The chiral ligand is an alkaloid or alkaloid derivative linked to an organic substituent of at least 300 daltons molecular weight through a planar aromatic spacer group. The organic substituent can be another alkaloid or alkaloid derivative. With the described chiral ligands, asymmetric dihydroxylation of olefins with high yields and enantiomeric excesses are achieved.

Abstract: Certain novel compounds having the structural formula ##STR1## where R.sub.2, R.sub.3 and R.sub.4 are each selected from the group consisting of H and OA; A is H or is selected from the group consisting of hydrocarbyl radicals, e.g. lower alkyl radicals, i.e. methyl, ethyl, propyl, etc., or ##STR2## wherein R.sub.5 is selected from the group consisting of hydrocarbyl radicals, e.g. alkyl and aromatic residues; n is 2 or 3; and R.sub.1 is selected from the group consisting of organic radicals having fused aromatic rings, that is, radicals comprising at least two rings that share a pair of carbon atoms or share a carbon and nitrogen atom are useful for inducing a dopaminergic response and reducing the intraocular pressure in a mammal.

Abstract: Homopolymers and copolymers with high Tg's are produced from phthalazones which in turn are produced from phenolphthalein as a readily available starting material; the homopolymers may be represented by formula (IX): ##STR1## wherein R.sub.1 and R.sub.2, which may be the same or different, are selected from hydrogen, fluorine, phenyl and fluorophenyl, each m, which may be the same or different, is an integer of 0, 1, 2, 3 or 4, and n is an integer of 2 to 200. Novel phenyl substituted phenolphthaleins and novel hydroxybenzoylbenzoic acids, as well as novel phthalazones, all of which may be employed in the preparation of homopolymers and copolymers of the invention, are also provided.

Abstract: Compounds having the formula ##STR1## exhibiting antibacterial activity.

Abstract: Homopolymers and copolymers with high Tg's are produced from phthalazones which in turn are produced from phenolphthalein as a readily available starting material; the homopolymers may be represented by formula (IX): ##STR1## wherein R.sub.1 and R.sub.2, which may be the same or different, are selected from hydrogen, fluorine, phenyl and fluorophenyl, each m, which may be the same or different, is an integer of 0, 1, 2, 3 or 4, and n is an integer of 2 to 200. Novel phenyl substituted phenolphthaleins and novel hydroxybenzoylbenzoic acids, as well as novel phthalazones, all of which may be employed in the preparation of homopolymers and copolymers of the invention, are also provided.

Abstract: The invention concerns a heterocycle of the formula I ##STR1## wherein Q is an optionally substituted 6-membered monocyclic or 10-membered bicyclic heterocyclic moiety containing one or two nitrogen atoms;A is (1-6C)alkylene, (3-6C)alkenylene, (3-6C)alkynylene or cyclo(3-6C)alkylene;X is oxy, thio, sulphinyl, sulphonyl or imino;Ar is phenylene which may optionally bear one or two substituents orAr is an optionally substituted 6-membered heterocyclene moiety containing up to three nitrogen atoms;R.sup.1 is hydrogen, (1-6C)alkyl, (3-6C)alkenyl, (3-6C)alkynyl, cyano-(1-4C)alkyl or (2-4C)alkanoyl, or optionally substituted benzoyl;and R.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 4 to 7 ring atoms, wherein A.sup.2 and A.sup.3, which may be the same or different, each is (1-4C)alkylene and X.sup.

Abstract: N-fluoro perfluoroheterocyclic sulfonamides of the following Formula I ##STR1## wherein Het.sub.f represents an aromatic perfluoroheterocyclic radical of valency n and each R independently represents a substituted or unsubstituted C.sub.1 -C.sub.30 alkyl, C.sub.6 -C.sub.14 aryl substituted C.sub.1 -C.sub.10 alkyl, C.sub.6 -C.sub.14 aryl, or C.sub.1 -C.sub.10 alkyl substituted C.sub.6 -C.sub.14 aryl group, are novel electrophilic fluorinating agents. Preferably Het.sub.f is a perfluorinated nitrogen-containing aromatic group, especially pyridyl, pyrimidinyl, pyrazinyl or 1,3,5-triazinyl; n is 1; and R is perfluorinated, especially trifluoromethyl.

Abstract: Heterocyclically substituted cycloalkano[b]-indolesulphonamides can be prepared by reaction of appropriate N-unsubstituted indoles with acrylonitrile, followed by hydrolysis, esterification or amidation, or by reaction of heterocyclically substituted hydrazines with cycloalkanones or by subsequent introduction of the heterocyclic group into appropriate indole derivatives. The heterocyclically substituted cycloalkano[b]-indolesulphonamides can be employed for the treatment of thromboembolic disorders, ischaemias, arteriosclerosis, asthma, allergies and for the prophylaxis of myocardial infarcts.

Abstract: A process for producing benzylphthalazinone derivatives represented by the general formula (I); ##STR1## wherein X is a halogen atom and R.sup.1 is a lower alkyl group, and salts thereof, which comprises reacting a compound represented by the general formula (II); ##STR2## wherein X has the same meaning as mentioned above, or a salt thereof with a compound represented by the general formula (III); ##STR3## wherein R.sup.1 has the same meaning as mentioned above or salt thereof in the presence of a dehydration-condensation agent. The benzylphthalazinone derivatives thereof are suitable for use as an antihistaminic agent.