Abstract: Compounds of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 is each --R.sup.5, --CH.dbd.CH--R.sup.5 or --C.tbd.C--R.sup.5, wherein R.sup.5 is optionally substituted aryl or aromatic heterocyclic; R.sup.3 is hydrogen, alkyl, cyano or --R.sup.5 ; X is oxygen or sulfur; A is 1,4-piperazin-1,4-diyl or a 1,4-homopiperazin-1,4-diyl; B' is alkylene, carbonyl, thiocarbonyl, sulfinyl or sulfonyl; and R.sup.4 is optionally substituted phenyl and pharmaceutically acceptable salts thereof have valuable PAF antagonist activity, and may be prepared by reacting a compound containing the piperazine or homopiperazine part of the molecular with a compound containing the other part of the molecule.

Abstract: Piperidine derivatives of formula ##STR1## wherein A is a radical of formula ##STR2## wherein one or two hydrogen atoms in said radicals (a-1) to (a-3) may be replaced by a C.sub.1-6 alkyl radical;R.sup.1 is hydrogen or halo; R.sup.2 is hydrogen, amino, mono or di(C.sub.1-6 alkyl)amino or C.sub.1-6 alkylcarbonylamino; R.sup.3 is hydrogen or C.sub.1-6 alkyl; L is C.sub.3-6 cycloalkyl, C.sub.5-6 cycloalkanone, C.sub.3-6 alkenyl optionally substituted with aryl, or L is a radical of formula ##STR3## the N-oxide forms, addition salts and stereochemically isomeric forms thereof, said compounds having gastrointestinal motility stimulating properties. Pharmaceutical compositions containing these compounds as active ingredient, and a method of preparing said compounds and pharmaceutical compositions.

Abstract: The invention is selected, novel, and known analogs of isoquinolinones of the formula ##STR1## and pharmaceutically acceptable salts thereof; novel pharmaceutical compositions; and a method for enhancing the lethal effects for tumor cells to treatment having DNA damaging activity such as ionizing radiation or with chemotherapeutic agents.

Abstract: The present invention relates to unsaturated carboxylic acid amide derivatives of the formula ##STR1## wherein ring A stands for an optionally substituted aromatic ring; R.sup.1 stands for a hydrogen atom or an optionally substituted hydrocarbon residue or forms an optionally substituted carbocyclic ring with the adjacent group --CH.dbd.C-- together with two carbon atoms constituting the ring A; R.sup.2 stands for a hydrogen atom, an optionally substituted hydrocarbon residue or an optionally substituted acyl group; R.sup.3 stands for an optionally substituted hydrocarbon residue; and n denotes an integer ranging from 2 to 6, and salts thereof, as well as the production thereof.The compounds of the present invention act on the central nervous system of mammals and has a strong anti-cholinesterase activity, which can be used for the prophylaxis and therapy of, for example, senile dementia, Alzheimer's diseases, Huntington's chorea, et., and are useful as medicines.

Abstract: Compounds of the formula ##STR1## in which R.sup.1, R.sup.2, X.sup.1, X.sup.2, Y.sup.1 and Y.sup.2 have the following meaningsR.sup.1 and R.sup.2 designate optionally substituted aryl, or an optionally substituted heterocyclic radical which contain 1 or 2 five-, six- or seven-membered rings at least one of which contains 1, 2 or 3 hetero atoms from the series comprising O, N and S which has a C.dbd.C in conjugation with the C.dbd.C bond in the five-membered ring of III,X.sup.1, X.sup.2, Y.sup.1 and Y.sup.2 designate O, S, NR.sup.5, or X.sup.1 and Y.sup.1 or X.sup.2 and Y.sup.2 in each case form parts of a fused-on heterocyclic five-membered or six-membered ring,processes for their preparation and their use as dyestuffs and pigments.

Abstract: Anti-virally active pyridazinamines, compositions containing the same and methods of treating viral diseases in warm-blooded animals.

Abstract: [(Bicyclic heterocyclyl)methyl and -hetero] substituted hexahydro-1H-azepines and pyrrolidines and their pharmaceutically acceptable acid addition salts having anti-histaminic properties, compositions containing the same, and methods of treating allergic diseases in warm-blooded animals.

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 or Ar 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: A series of novel alkanesulphonamidophenyl-N-alkyl-N-(heterocyclic-alkyl)alkylamine derivatives have been prepared, including their pharmaceutically acceptable salts. These compounds are useful in therapy as anti-arrhythmic agents and therefore, are of value in the treatment of various cardiac arrhythmias. Said sulfonamide compounds are of the formula: ##STR1## wherein R and R.sup.1 are each C.sub.1 -C.sub.4 alkyl; X is --CH.sub.2 --, --CO-- or --CH(OH)--; n is two, three or four; and "Het" is a nitrogen-containing heterocyclic group wherein said heterocyclic group is preferably 2H-3,4-dihydroisoquinol-1-on-2-yl or 2H-isoquinol-1-on-2-yl, each optionally substituted with halogen or C.sub.1 -C.sub.4 alkyl.

Abstract: Piperidinyl, pyrrolidinyl, azepinyl and piperazinyl pyridazines of formula ##STR1## wherein one or two carbon atoms of the ##STR2## moiety may be substituted with C.sub.1-4 alkyl, C.sub.1-4 alkyloxy or two carbon atoms of the CH.sub.2 groups of said moiety may be bridged with a C.sub.2-4 alkanediyl radical;X represents CH or N; R.sup.1 represents hydrogen, C.sub.1-4 alkyl, halo, hydroxy, trifluoromethyl, cyano, C.sub.1-4 alkyloxy, C.sub.1-4 alkylthio, C.sub.1-4 alkylsulfinyl, C.sub.1-4 alkylsulfonyl, C.sub.1-4 alkyloxycarbonyl, C.sub.1-4 alkylcarbonyl or aryl; R.sup.2 and R.sup.3 each independently represent hydrogen or C.sub.1-4 alkyl; Alk represents C.sub.1-4 alkanediyl;R.sup.4 and R.sup.5 each independently represent hydrogen, C.sub.1-4 alkyl or halo; andHet represents ##STR3## the addition salts and stereochemically isomeric forms thereof, said compounds having antipicornaviral activity.

Abstract: 4-Phenylphthalazine derivatives having platelet aggregation inhibitory activity of the formula: ##STR1## wherein R.sup.1 is an alkyl or hydroxyalkyl group of 1-5 carbon atoms; R.sup.2 is a hydrogen atom or an alkyl group of 1-5 carbon atoms; or R.sup.1 and R.sup.2, when taken together, may represent an alkylene group of 2-6 carbon atoms, said group optionally containing one or more oxygen atoms; R.sup.3 and R.sup.4 are independently a hydrogen or halogen atom, an alkyl or alkoxy group of 1-4 carbon atoms, or when two of R.sup.3 are adjacently positioned, (R.sup.3)l may represent a --O--(CH.sub.2).sub.p --O-- group and/or when two of R.sup.4 are adjacently positioned, (R.sup.4).sub.m may represent a --O--(CH.sub.2).sub.p --O-- group; R.sup.5 is a hydrogen or halogen atom, an alkyl or alkoxy group of 1-4 carbon atoms, a trifluoromethyl group or a hydroxy group, or when two of R.sup.5 are adjacently positioned, (R.sup.5).sub.n may represent a --O--(CH.sub.2).sub.

Abstract: There is provided a pest control composition containing a compound represented by the formula, ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and independently mean a hydrogen atom, a hydrocarbon group which may be substituted or a heterocyclic group which may be substituted and X means an electron attracting group or a salt thereof.The compounds are of minimal toxicity to man, domestic animals and fish and selectively display remarkable control effect on pests.

Abstract: The invention relates to the compounds of general formula I: ##STR1## in which: m represents an integer from 2 to 4,n and p, which may be identical or different, each represent an integer from 1 to 3,q represents 0 or 1, andR represents:either a group of formula (A): ##STR2## or a radical of formula (B): ##STR3## or a 2,4-dioxo-1,2,3,4-tetrahydroquinazolinyl radical, on condition, however, that, in this case, n and p do not simultaneously represent the number 2,or a benzhydryloxy group,or a 1-oxophthalazinyl radical,or a 5-oxothiazolo[3,2-A]pyrimidinyl radical,or a group of formula C: ##STR4## their possible stereoisomers and their addition salts with a pharmaceutically acceptable inorganic or organic acid.The compounds of formula I are medicinal products with useful 5-HT.sub.2 - and .alpha..sub.1 -antagonistic activities.

Abstract: Oxophthalazinyl acetic acids having benzothiazole side chains are prepared by reacting an oxophthalazinyl thioacetamide acetate with hydrogen sulfide and a nitrophenyl compound having a reactive group such that the benzothiazole side chain may be formed by ring closure involving the thiocaetamide group. The oxophthalazinyl thioacetamide may be prepared by reacting the corresponding cyanomethyloxophthalazinyl acetate with hydrogen sulfide in the presence of tertiary amines. Analogous indazole and oxopyridopyridazinone acetic acids may be prepared similarly, as well as oxophthalazinyl, indazole and oxopyridopyridazinone acetic acids having thiazolopyridinyl side chains.

Abstract: Insecticidally active substituted heteroaryl phenyl ethers of the formula ##STR1## in which Het represents an optionally substituted heteroaromatic radical,X represents O, S, --CH.sub.2 --, --O--CH.sub.2 --, --S--CH.sub.2 --, --CH.sub.2 --O--, ##STR2## Y represents O, --O--CH.sub.2 -- or S, Z represents an optionally substituted aromatic or heteroaromatic radical;m represents integers from 1-4n represents 0, 1, 2, 3, 4O represents 0, 1, 2, 3, 4, provided than n and o do not simultaneously represent 0p represents integers from 1-4,R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 independently of one another represent hydrogen, C.sub.1 -C.sub.6 -alkyl which is optionally substituted; two radicals adjacent to one another can also, together with the C atoms to which they are bonded, form a saturated carbocyclic 5- or 6-ring,R.sup.1 represents identical or different radicals hydrogen, halogen, CN, C.sub.1-4 -alkyl, 1-5-halogeno-C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy, C.sub.1-4 -alkylthio, 1-5-halogeno-C.sub.

Abstract: Substituted hydroxylamines of the formula ##STR1## in which R.sup.1 stands for an aromatic or heterocyclic radical,are especially useful in the treatment of hyperlipoproteinaemia, lipoproteinaemia and atherosclerosis.

Abstract: The invention relates to compounds of formula I: ##STR1## in which m=2-4,n and p, which may be identical or different, are an integer equal to 1, 2 or 3, with the proviso that the sum of n and p is not less than 3 and not more than 5,q=0 or 1,R is a 1,2,3,4-tetrahydro-3-quinazolinyl radical, optionally substituted, a 1,3,4,6,11,11a-hexahydro-1,3-dioxo-2H-pyrazino[1,2,-b]isoquinol-2-yl radical, a 1,2-dihydro-1-oxo-2-phthalazinyl radical, optionally substituted, a 2,6-dioxo-1-piperazinyl radical of formula W: ##STR2## (R.sub.3 is a 2-pyridyl radical or an optionally substituted phenyl radical),a radical of formula Z: ##STR3## (R.sub.4 is a carbamoyl radical, a cyano radical, a hydroxycarbonyl radical or an alkoxycarbonyl radical having 1 to 6 carbon atms),or a radical of formula Y: ##STR4## (R.sub.

Abstract: Compounds suitable for use as extreme pressure (EP)/anti-wear (AW) agents in lubricating oil compositions, which compounds have the formula:R.sup.1 --S--X--S--S--R (I)wherein R.sup.1 is either R--S-- or hydrogen,R is independently either hydrocarbyl or substituted hydrocarbyl, andX comprises a heterocyclic ring having six atoms of which two are nitrogen atoms.

Abstract: A series of novel 5-substituted imidazolidinedione derivatives and their base salts with pharmacologically acceptable cations are disclosed. These particular compounds are useful in therapy as aldose reductase inhibitors for the control of certain chronic diabetic complications. 5-Naphthalimido-imidazolidine-2,4-dione and 5-[3-(4'-bromo-2'-fluorobenzyl)-3,4-dihydro-4-oxophthalazin-1-yl]-imidazol idine-2,4-dione represent typical and preferred member compounds. Methods for preparing all these compounds from known starting materials are provided.

Abstract: Substituted 2-acylpyridine-.alpha.-(N)-hetarylhydrazones are described, which are suitable as active substances for the treatment of antimicrobial and in particular antimycobacterial diseases, as well as active substances for the treatment of malaria or malignant tumours. The compounds have a marked synergistic activity combined with inhibitors of folate synthase, dihydrofolic acid reductase, DNA-synthesis and RNA-synthesis.

Abstract: For inhibiting 3-hydroxy-3-methyl-glutaryl coenzyme A (HMG-CoA) reductase, the novel substituted pyrroles of the formula ##STR1## in which R.sup.1 is optionally alkyl or cycloalkyl,R.sup.2 and R.sup.3 each is optionally substituted aryl or heteroaryl,R.sup.4 is H or an organic radical,X is --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--,A is ##STR2## R.sup.7 is H or alkyl, and R.sup.8 is H or an ester or cation radical.Novel intermediates therefor are also provided.

Abstract: Novel pyridazinamine derivatives having antiviral activity, compositions containing these compounds as active ingredient, and a method of destructing viruses or preventing the growth thereof in warm-blooded animals suffering from diseases caused by these viruses. Processes for preparing said compounds and compositions.

Abstract: A series of novel alkanesulphonamidophenyl-N-alkyl-N-(heterocyclic-alkyl) alkylamine derivatives have been prepared, including their pharmaceutically acceptable salts. These compounds are useful in therapy as anti-arrhythmic agents and therefore, are of value in the treatment of various cardiac arrythmias. Said sulfonamide base compounds are of the formula: ##STR1## wherein R and R.sup.1 are each C.sub.1 -C.sub.4 alkyl; X is --CH.sub.2 --, --CO--or --CO(OH)--; n is two, three or four; and "Het--" is a nitrogen-containing heterocyclic group wherein said heterocyclic group is phenyl or benzyl-substituted 2H-pyridazin-3-on-2-yl, or it is 2H-phthalazin-1-on-2-yl, 4-halo-2H-phthalizin-1-on-2-yl or 4-(C.sub.1 -C.sub.4 alkyl)-2H-phthalazin-1-on-2-yl, 2H-isoindolin-1-on-2-yl, 3H-quinazolin-4-on-3-yl, 2H-3,4-dihydroisoquinol-1-on-2-yl, 2H-isoquinol-on-2-yl, 1H-3,4-dihydroquinol-2-on-1-yl, benzoxazol-2-on-3-yl, quinol-2-on-1-yl, quinol-2-yl or indol-2-yl, each optionally mono substituted with halogen or C.sub.1 -C.sub.

Abstract: Inhibiting HMG-CoA reductase, as in treating hyperlipopproteinaemia, lipoproteinaemia and arteriosclerosis, with the new N-substituted N-amino-pyrroles of the formula ##STR1## in which R.sup.1 is an organic radical,R.sup.2 is an aryl or heteroaryl radical,R.sup.3 is a hydrogen or an organic radical,R.sup.4 and R.sup.5 each independently is hydrogen or an organic radical or, together, they complete a heterocylic ring,X is --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--,A is ##STR2## R.sup.10 is hydrogen or alkyl, and R.sup.11 is hydrogen, an organic radical or a cation.

Abstract: A saturated heterocyclic carboxamide derivative of the following general formula (I) and salts thereof which have platelet activating factor (PAF) antagonizing activity.

Abstract: Compounds having the formula ##STR1## wherein R is 2-[1-oxo-(2H)-phthalazinyl], R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, X, Y, m and n have the meanings shown in the description. The compounds of formula I are pharmaceutically active as anti-vasospastic, anti-aggregating, and anti-proliferative agents.

Abstract: There are provided novel pyridazinone derivatives having the general formula (I): ##STR1## wherein A represents 5- or 6-membered heterocyclic ring having 1-3 nitrogen atoms, which may be substituted by at least one member selected from the group consisting of C.sub.1-5 alkyl, cyano, hydroxyl, C.sub.1-5 alkoxyl, amino, C.sub.1-5 alkylamino, C.sub.2-6 dialkylamino, C.sub.2-5 acylamino, carboxyl, C.sub.2-5 alkoxycarbonyl and carbamoyl, and R.sup.1 and R.sup.2 independently represent hydrogen atom or C.sub.1-5 alkyl or R.sup.1 and R.sup.2 may form together C.sub.1-5 alkylene, and salts thereof.

Abstract: Substituted hydroxylamines of the formula ##STR1## in which R.sup.1 stands for an aromatic or heterocyclic radical, are especially useful in the treatment of hyperlipoproteinaemia, lipoproteinaemia and atherosclerosis.

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: The invention relates to novel substituted N-phenylthioureas, N-phenylisothioureas and N-phenylcarbodiimides of formula ##STR1## wherein R.sub.1 to R.sub.5 and Z are as defined in the specification.The invention further relates to the preparation of said compounds and to compositions containing them for use in pest control, especially for controlling insects and representatives of the order Acarina that are pests of plants and animals, in particular plant-destructive sucking and eating pests.

Abstract: Therapeutically useful pyrrolo[2,1-a]phthalazine derivatives of the formula: ##STR1## wherein R.sup.1 and R.sup.2 represent cycloalkyl, optionally substituted alkyl, alkenyl, alkynyl, aryl or heteroaryl, X represents ethylene or vinylene, R.sup.3 represents a group of the formula:--Y--CH.sub.2 --CH(OH)--CH.sub.2 --COOR.sup.5wherein Y represents carbonyl or hydroxymethylene and R.sup.5 represents hydrogen or optionally substituted alkyl, or R.sup.3 represents a lactone ring and the symbols R.sup.4 represent hydrogen, halogen, optionally substituted alkyl, alkenyl, alkynyl, aryl or heteroaryl, or R.sup.6 O-- wherein R.sup.6 represents alkyl, aryl or arylalkyl and salts thereof, processes for their preparation and compositions containing them are described.

Abstract: Oxophthalazinyl acetic acids having benzothiazole side chains are prepared by reacting an oxophthalazinyl thioacetamide acetate with hydrogen sulfide and a nitrophenyl compound having a reactive group such that the benzothiazole side chain may be formed by ring closure involving the thioacetamide group. The oxophthalazinyl thioacetamide may be prepared by reacting the corresponding cyanomethyloxophthalazinyl acetate with hydrogen sulfide in the presence of tertiary amines. Analogous indazole and oxopyridopyridazinone acetic acids may be prepared similarly, as well as oxophthalazinyl, indazole and oxopyridopyridazinone acetic acids having thiazolopyridinyl side chains.

Abstract: A piperazine derivative represented by the following formula or a salt thereof: ##STR1## which is useful for curing cerebro-vascular disease and post-cerebro-vascular disease.

Abstract: Novel 1-alkyl substituted benzimidazole derivatives and their pharmaceutically acceptable acid addition salts having anti-histaminic properties, compositions containing the same, and methods of treating allergic diseases in warm-blooded animals.

Abstract: This invention relates to a process for the production of phthalazineacetic acid ester derivatives of the formula ##STR1## wherein R is (C.sub.1 -C.sub.4)alkyl which comprises reacting (Z)-3-oxo-1(3H)-isobenzofuranylideneacetic acid with hydrazine in the presence of a solvent; reacting the resulting mixture of the novel compound 1-hydrazino-1,2,3,4-tetrahydro-4-oxo-phthalazineacetic acid and 3,4-dihydro-4-oxo-phthalazineacetic acid with acid in the presence of a solvent; and reacting the resulting 3,4-dihydro-4-oxo-phthalazineacetic acid with acid in the presence of an alcohol.This invention also relates to the novel compound 1-hydrazino-1,2,3,4-tetrahydro-4-oxo-phthalazineacetic acid of the formula ##STR2## which is an intermediate formed in the process of this invention and which is useful for the production of phthalazineacetic acid ester derivatives of formula IV. The compounds of formula IV are useful for the preparation of certain heterocyclic oxophthalazinyl acetic acids and esters thereof.

Abstract: For inhibiting 3-hydroxy-3-methylglutaryl coenzyme A and cholesterol biosynthesis, the novel disubstituted pyrroles of the formula ##STR1## in which R.sup.1 is aryl or heteroaryl,R.sup.2 is cycloalkyl or optionally substituted alkyl,R.sup.3 is hydrogen or cycloalkyl, or optionally substituted alkyl, aryl or heteroaryl,X is --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--,A is ##STR2## R.sup.6 is hydrogen or alkyl, and R.sup.7 is hydrogen, a cation or alkyl, aryl or aralkyl.

Abstract: A xanthine oxidase enzyme system to provide long lived entities capable of being recognized by a chemiluminescent reagent is disclosed. In the examples provided, a specific binding pair ligand or analyte is coupled with xanthine oxidase, either directly or via a streptavidin bridge. Thereafter the presence of an analyte can be determined by a chemiluminescent emission upon addition of a signal reagent comprising hypoxanthine, iron EDTA complex and luminol dissolved in barbital buffer. The resulting chemiluminescent signal is stable and detectable for many hours after initiation. The chemiluminescent xanthine oxidase system is particularly useful for immunoassays and DNA probe analysis.

Abstract: 2-Pyridylmethylthio derivatives of formula (I) are provided. ##STR1## wherein A represents 4-methyl-2-quinazolinyl, 4-(2-pyridylmethylthio)-1-phthalazinyl or 4-oxo-3-phenyl-3,4-dihydropyrido[2,3-d]pyrimidine-2-yl, or a pharmaceutically acceptable acid addition salt thereof. They are useful as antiulcer agents.

Abstract: Substituted N-phenylthioureas, N-phenylisothioureas and N-phenylcarbodiimides of formula ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.12 alkyl, C.sub.3 -C.sub.8 cycloalkyl, polycyclic alkyl containing a total of 7 to 10 carbon atoms, C.sub.1 -C.sub.12 alkyl which is substituted by 1 to 12 halogen atoms, C.sub.1 -C.sub.4 alkyl which is substituted by one or two C.sub.3 -C.sub.6 cycloalkyl radicals, alkoxyalkyl containing a total of 3 to 10 carbon atoms, C.sub.1 -C.sub.5 alkyl which is substituted by a phenyl radical, C.sub.1 -C.sub.5 alkyl which is substituted by a phenyl radical which is in turn substituted by one or two members selected from the group consisting of halogen, methyl, methoxy and ethoxy; or is C.sub.3 -C.sub.10 -alkenyl or C.sub.3 -C.sub.10 alkynyl, R.sub.2 is hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.3 is C.sub.1 -C.sub.4 alkyl, R.sub.4 is hydrogen or C.sub.1 -C.sub.4 alkyl, and R.sub.

Abstract: Novel chromophor derivatives of cyclic anhydrides are provided which have the ability to react with a variety of organic substrates forming adducts which are useful in analytical techniques for the detection and measurement of biological compounds.

Abstract: A method for increasing cardiotonic contractility in humans or other animals using a class of benzodiazinone-pyridazinone and hydroxy-pyrazolyl compounds and pharmaceutical compositions including the same.

Abstract: This invention relates to a process for the production of phthalazineacetic acid ester derivatives of the formula ##STR1## wherein R is (C.sub.1 -C.sub.4) alkyl which comprises reacting (Z)-3-oxo-1(3H)-isobenzofuranylideneacetic acid with hydrazine in the presence of a solvent; reacting the resulting mixture of the novel compound 1-hydrazino-1,2,3,4-tetrahydro-4-oxo-phthalazineacetic acid and 3,4-dihydro-4-oxo-phthalazineacetic acid with acid in the presence of a solvent; and reacting the resulting 3,4-dihydro-4-oxo-phthalazineacetic acid with acid in the presence of an alcohol.This invention also relates to the novel compound 1-hydrazino-1,2,3,4-tetrahydro-4-oxo-phthalazineacetic acid of the formula ##STR2## which is an intermediate formed in the process of this invention and which is useful for the production of phthalazineacetic acid ester derivatives of formula IV. The compounds of formula IV are useful for the preparation of certain heterocyclic oxophthalazinyl acetic acids and esters thereof.

Abstract: A benzopylpiperazine ester of the following formula: ##STR1## wherein A represents a single bond or an alkylene group, vinylene group, --O--alkylene group or methine group, R.sub.1 represents a bicyclic carbon ring residue which may be substituted with a lower alkyl group, lower alkoxy group, oxo group or nitro group or a halogen atom, or may be partially saturated; a fluorene residue which may contain an oxo group; a fluorenylidene group; an anthracene residue; a phenanthrene residue which may be substituted with a lower alkyl group, or may be partially saturated; a benzofuran residue or thianaphthene residue which may be substituted with a lower alkyl group or lower alkoxy group; a benzopyran residue or benzoazine residue which may be substituted with an oxo group or phenyl group and partially saturated; a phthalimide residue; a benzodiazine residue; an isozazole residue which may be substituted with a lower alkyl group or phenyl group; or an alkylene dioxybenzene residue or xanthene residue; and R.sub.

Abstract: A series of novel heterobicyclic substituted 2-(1H)-quinolone compounds have been prepared, including the 3,4-dihydro derivatives thereof, wherein the heterobicyclic ring moiety is an optionally-substituted indolyl, phthalizinyl, benzimidazolyl, imidazopyridinyl, quinolinyl or isoquinolinyl group attached by an nitrogen or carbon atom of said group to the 6-position of the quinolone ring. The optional substituent is a C.sub.1 -C.sub.14 alkyl group located on either of the two heterobicyclic rings and/or an oxo group situated on the heterocyclic portion of said heterobicyclic ring system. These particular compounds are useful in therapy as cardiac stimulants and therefore, are of value in the treatment of various cardiac conditions. 6-{1(H)-Imidazo[4,5-b]pyridin-6-yl}-8-methyl-2-(1H)-quinolone represents a typical and preferred member compound. Methods for preparing these compounds from known starting materials are provided.

Abstract: Arylpiperazinyl-ethyl (or butyl)-heterocyclic compounds and their pharmaceutically acceptable acid addition salts are neuroleptic agents. They are useful in the treatment of psychotic disorders.

Abstract: The present invention concerns new 5-alkylbenzimidazoles of the formula: ##STR1## wherein R.sub.1 is a phenyl ring of the formula: ##STR2## or R.sub.1 is naphthyl, heterocycle or a bicyclic heterocycle and R.sub.1 -R.sub.7 are described in claim 1.These compounds are useful for prophylaxis or treatment of heart and circulatory disease especially to increase contractility of the heart, lower blood pressure and/or influence the thrombocyte function and improve the microcirculation.

Abstract: There is disclosed an improved process for the preparation of 3-[(4-bromo-2-fluorophenyl)-methyl]-3,4-dihydro-4-oxo-1-phthalazineacetic acid. The process is significantly improved over the prior art process in preparing the product in a one-step process where the prior art required three steps. The instant process directly alkylates a phthalazine ring nitrogen in the presence of the acetic acid moiety without the necessity of protecting the carboxylic acid group as was necessary in the prior art preferred process. The product is useful for treating the progressive deterioration resulting from diabetes.

Abstract: The invention relates to derivatives of 2,3-dihydro 3-imino-pyridazine responding to general formula: ##STR1## in which: A represents an atom of oxygen or of sulfur;R.sub.1 represents a lower alkyl group, or an aromatic group selected from:the phenyl group;the phenyl groups mono- or poly-substituted by a halogen group, a lower alkyl group, a lower alkoxy group, a nitro group, a hydroxy or methylenedioxy group;the naphthyl group;the furyl group;the thienyl group or the pyridyl group;R.sub.2 and R.sub.3 each designate independently hydrogen or a lower alkyl group; a phenyl group, or R.sub.2 and R.sub.3, taken together, constitute, with the 2 atoms of the pyridazinic cycle to which they are bonded, a benzene ring, and their pharmaceutically acceptable salts. Application: antidepressants or psychotonics.

Abstract: Novel compositions are prepared by reacting hydrocarbyl substituted nitrogen-containing aromatic heterocyclic compounds such as 2,5-dimethylpyridine or 2,4,6-collidine, an aldehyde such as formaldehyde, or a ketone such as acetone, or mixtures thereof and an amine having a combined total of at least seven carbon, nitrogen, oxygen or sulfur atoms and at least one reactive amine hydrogen atom such as 1-dodecanamine in the presence of a suitable catalyst such as hydrogen chloride. These novel compositions, as well as their free amine forms are useful as oil and gas well corrosion inhibitors.

Abstract: Oxophthalazinyl acetic acids having aldose reductase inhibitory properties of the formula ##STR1## wherein Z is hydrogen or methyl, U is S, CH.sub.2 or a covalent bond, and R.sup.1, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are as herein defined, are prepared by reacting an intermediate oxophthalazinyl acetic acid ester having a cyano or alkylamido group with an aniline derivative of the formula ##STR2## Processes for the preparation of the intermediate oxophthalazinyl acetic esters are disclosed.