Abstract: The invention is directed to certain 2,4-diaminoquinazoline compounds, their pharmaceutically acceptable salts, the pharmaceutical compositions comprising those compounds and their therapeutic methods of use. The compounds possess anti-ischemic activity.

Abstract: Quinazolines of the formula ##STR1## wherein R.sup.1 is typically methyl, hydrogen or amino; R.sup.2 is typically methyl or propargyl; Ar is typically phenylene or 2'-fluorophenylene; R.sup.3 is the residue of a dipeptide substituted, typically by methyl, at position (a), (b) or (c), shown in the following partial formula: ##STR2## R.sup.4, R.sup.5, R.sup.6 and R.sup.8 are typically hydrogen, R.sup.7 is typically hydrogen or methyl; or a pharmaceutically acceptable salt, ester or amide thereof are of value in the treatment of cancer.

Abstract: A process for the preparation of quinazoline-2,4-diones of the formula (I) ##STR1## in which R.sup.1 is aryl and R.sub.2, R.sup.3, R.sup.4, and R.sup.5 independently of one another are halogen, alkyl, alkoxy or hydrogen, by reacting anthranilic acid esters of the formula (II) ##STR2## in an aprotic reaction medium with aryl isocyanates R.sup.1 --N.dbd.C.dbd.O to give N-arylcarbamoyl-anthranilic acid esters of the formula (III) ##STR3## and cyclizing these in the presence of a base selected from the group of alkali metal or alkaline earth metal alkoxides, amides, hydrides or tetraalkylammonium hydroxides.

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: There is disclosed an olefin-substituted compound having the formula:R--(core moiety),wherein R is a straignt chain hydrocarbon having at least one double bond and a carbon chain length of from about 6 to about 18 carbon atoms, wherein multiple double bonds are separated from each other by at least three carbon atoms, wherein the closest double bond to the core moiety is at least five carbon atoms from the core moiety, and wherein the hydrocarbon chain may be substituted by a hydroxyl, halo, keto or dimethylanimo group and/or interrupted by an oxygen atom and salts thereof and pharmaceutical compositions thereof.

Abstract: The cyclic amide derivative is defined by the formula (I) or a salt thereof:R.sup.1 --(CH.sub.2).sub.n --Zin which R.sup.1 is a group derived from a cyclic amide compound, substituted or unsubstituted, n is zero or an integer of 1 to 10 and Z is ##STR1## R.sup.2 being an aryl, a substituted aryl, a cycloalkyl or a heterocyclic group, m being an integer of 1 to 6, R.sup.3 being hydrogen or a lower alkyl, R.sup.4 being an aryl or a substituted aryl, a cycloalkyl or a heterocyclic group, p being an integer of 1 to 6, provided that the cyclic amide compound is quinazoline-on or quinazoline-dion, R.sup.2 and R.sup.4 are neither aryl nor substituted aryl. The cyclic amide compound is pharmacologically effective to prevent and treat diseases due to insufficiency of the central choline functions.

Abstract: Abstract of the Disclosure: Compounds of the formula I ##STR1## where R.sup.1, R.sup.2, n , R.sup.3, A, X, Y and Z have the meanings stated in the description, and the preparation thereof are described. The novel compounds are suitable for controlling diseases , i.e., as neuroleptics, antidepressants, sedatives, hypnotics, CNS protectives or muscle relaxants.

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: Novel A-II receptor antagonists have the formula ##STR1## and its isomer ##STR2## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are as defined herein.

Abstract: Quinazolines of the formula: ##STR1## wherein R.sup.1 -R.sup.8 are defined as in the specification, or a pharmaceutically acceptable salt, ester or amide thereof areof therapeutic value, particularly in the treatment of cancer.

Abstract: Quinazoline compounds which demonstrate antiproliferative activity, such as antitumor activity, processes of preparing these compounds, pharmaceutical compositions containing these compounds, and the use of these compounds. These compounds inhibit the growth and proliferation of the cells of higher organisms and microorganisms, such as bacteria, yeasts and fungi. Preferred quinazoline compounds are capable of inhibiting the enzyme thymidylate synthase. Effects derived from the inhibition of the enzyme thymidylate synthase include those discussed above.

Abstract: Substituted quinazolines of the formula (1): ##STR1## wherein: R.sup.1 to R.sup.4 are independently H, halo, (C.sub.1 -C.sub.4) alkyl, branched (C.sub.3 -C.sub.4) alkyl, halo (C.sub.1 -C.sub.4) alkyl, (C.sub.1 -C.sub.4) alkoxy, NO.sub.2, or NH.sub.2,provided thatat least two of R.sup.1 to R.sup.4 are H;Y is H, Cl, X--W--Ar, or O--Alk;X is O, NR.sup.7, or CR.sup.8 R.sup.9 ;Z is H, Cl, OCH.sub.3, CH.sub.3, or --NR.sup.7 --W--Ar, provided that Z can be --NR.sup.7 --W--Ar only if Y is H, Cl, or NR.sup.7 --W--Ar and Z must be --NR.sup.7 --W--Ar if Y is H or Cl, which are plant fungicides, miticides, and insecticides.

Abstract: Phenoxyphenylacetic acids and derivatives of general structural formula I ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebal and cardiac ischemia, myocardial infarction, inflammatory diseases, Raynaud's disease, and endotoxic shock, and asthma.

Abstract: The invention relates to quinazoline derivatives, or pharmaceutically-acceptable salts thereof, which possess anti-tumour activity; to processes for their manufacture; and to pharmaceutical compositions containing them.The invention provides a quinazoline of the formula: ##STR1## wherein R.sup.1 is hydrogen or amino, or alkyl or alkoxy each of up to 6 carbon atoms; or R.sup.1 is substituted alkyl or alkoxy each of up to 3 carbon atoms;R.sup.2 is hydrogen, alkyl, alkenyl, alkynyl, hydroxyalkyl, halogenoalkyl or cyanoalkyl each of up to 6 carbon atoms;Ar is phenylene or heterocyclene;L is a group of the formula --CO.NH--, --NH.CO--, --CO.NR.sup.3 --, --NR.sup.3.CO--, --CH.dbd.CH--, --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 S--, --SCH.sub.2 --, --CO.CH.sub.2 --, --CH.sub.2.CO-- or --CO.O--, wherein R.sup.3 is alkyl of up to 6 carbon atoms; andY is aryl or heteroaryl or a hydrogenated derivative thereof; orY is a group of the formula --A--Y.sup.

Abstract: Fibrinogen receptor antagonists of the ##STR1## are disclosed for use in inhibiting the binding of fibrinogen to blood platelets and for inhibiting the aggregation of blood platelets wherein G is: ##STR2## for example, ##STR3##

Abstract: The invention relates to certain substituted fused compounds of Formula I ##STR1## which are useful as herbicides, and their agriculturally suitable compositions, as well as methods for their use as general or selective preemergent or postemergent herbicides or as plant growth regulants.

Abstract: The present invention relates to a composition comprising an antimicrobial effective amount of a biocide selected from the group consisting of aromatic 2-N-hydroxy-thiourea and N-hydroxy-quinazolinone, and derivatives and combinations thereof, and at least one component selected from the group consisting of soaps, shampoos, skin-care medicaments, cosmetics, plastics and paints. Also disclosed is a novel process for making the biocide.

Abstract: The present invention provides a novel series of 3-substituted methyl-2,3-dihydroimidazo[1,2-c]quinazoline compounds. These compounds are found useful as an active ingredient for the treatment of hypertension and dysuria.

Abstract: 3-Aryluracil derivatives of the formula I ##STR1## in which --W-- is the group ##STR2## where the ring nitrogen atom is bonded via the C atom; R.sub.1 is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.3 alkenyl or C.sub.4 alkenyl or C.sub.3 alkynyl or C.sub.4 alkynyl;R.sub.2 is halogen or cyano;R.sub.3 is hydrogen or halogen;R.sub.4 is hydrogen, halogen or C.sub.1 -C.sub.4 alkyl;R.sub.5 is C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 haloalkyl; or R.sub.4 and R.sub.5 together are --(CH.sub.2).sub.n --;n is the number 3 or 4;R.sub.13 is C.sub.1 -C.sub.4 alkyl, C.sub.3 alkenyl or C.sub.4 alkynyl or C.sub.3 alkynyl or C.sub.4 alkynyl; andQ is one of the groups a) to e): ##STR3## where R.sub.6 to R.sub.12 are substituents, m is 3, 4 or 5, X is oxygen or sulfur and t is 2, 3 or 4, and if R.sub.1 is hydrogen, the agrochemically acceptable salts of compounds of the formula I. the compounds of formula I have herbicidal properties and are suitable as the active ingredient in a herbicide.

Abstract: Biphenyl derivatives of cyclobutene-1,2-dione of formula 1 are angiotensin II antagonists and are useful for the treatment of hypertension and congestive heart failure ##STR1## wherein: Y is O, NR.sup.7, NCOR.sup.7 ; or R.sup.5 and Y taken together represent a linking chain of N.dbd.CR.sup.8 N; or R.sup.5 and Y taken together represent a linking chain of (CR.sup.9 R.sup.10).sub.n CON where n=1,2,3,4, or 5;X is N, CR.sup.7 ;Z is N, CR.sup.7 ;R.sup.1 is H, alkyl, benzyl, alkoxyalkyl, phenyl;R.sup.2 is H, alkyl, benzyl, alkoxyalkyl, phenyl, alkoxy, alkyl-OH, perfluoroalkyl, F, Cl, Br, I, NR.sup.7 R.sup.8 ;R.sup.3 is H, alkyl, benzyl, alkoxyalkyl, phenyl, alkoxy, alkyl-OH, perfluoroalkyl, F, Cl, Br, I, NR.sup.7 R.sup.8 ;R.sup.4 is H, NR.sup.7 R.sup.8, OR.sup.1, CN, F, Cl, I, Br, perfluoroalkyl, alkyl, phenyl, alkoxy, alkyl-OH, alkoxyalkyl, --(CH.sub.2).sub.n CO.sub.2 R.sup.1, --(CH.sub.2).sub.n CONR.sup.7 R.sup.8 where n=1, 2, 3, 4, or 5;R.sup.5, R.sup.

Abstract: Substituted quinazolinones and pyridopyrimidines of structural formula 1 ##STR1## are angiotensin II antagonists useful in the treatment of disorders related to the renin-angiotensin system (RAS) such as hypertension, congestive heart failure, ocular hypertension and certain CNS disorders.

Abstract: A compound or its tautomer of Formula I, ##STR1## wherein R.sup.1 is hydrogen, a 6-methyl, 6-fluoro, 6-chloro, 6-bromo, or 6,7-dimethoxy residue,R.sup.2 is hydrogen, or a methyl residue,and n is 1 or 2,and tautomers and their pharmaceutically acceptable alkali, or ammonium salts.

Abstract: A novel piperidine derivative is defined by the formula (I), including a salt thereof, ##STR1## wherein R.sup.1 denotes a univalent group derived from substituted or unsubstituted quinazolinedione,X denotes a group of the formula ##STR2## n is an integer of 1 through 7, the ring A denotes a group of the formula ##STR3## a group of the formula ##STR4## or a group of the formula ##STR5## and R.sup.2 denotes a hydrogen atom, a lower alkyl group, a substituted benzoyl group, a pyridyl group, a 2-hydroxyethyl group, a pyridylmethyl group, or a group of the formula ##STR6## wherein Z represents a halogen atom). The novel compounds of this invention are used for treating dementias and sequelae of cerebrovascular diseases.

Abstract: This invention relates to certain 1-heterocycloalkylquinazolin-2,3-dione derivatives, certain pharmaceutically acceptable salts thereof, the process of making those compounds, and the method of using the compounds. The compounds and compositions display effects on the peripheral or central nervous system.

Abstract: The present invention relates to a composition comprising an antimicrobial effective amount of a biocide selected from the group consisting of aromatic 2-N-hydroxy-thiourea and N-hydroxy-quinazolinone, and derivatives and combinations thereof, and at least one component selected from the group consisting of soaps, shampoos, skin-care medicaments, cosmetics, plastics and paints. Also disclosed is a novel process for making the biocide.

Abstract: A compound of the formula: ##STR1## in which R.sup.1 and R.sup.2 are each hydrogen, halogen, nitro, amino, protected amino, hydroxyamino, lower alkyl, hydroxy, protected hydroxy, sulfamoyl, carboxy, protected carboxy, mercapto, optionally substituted heterocyclic-carbonyl, optionally substituted heterocyclic-(lower)alkyl, lower alkylthio, hydroxy(lower)alkyl or protected hydroxy(lower)alkyl,R.sup.3 is aryl which may have suitable substituent(s), andA is lower alkylene,or pharmaceutically acceptable salts thereof.

Abstract: The invention relates to quinazoline derivatives, or pharmaceutically-acceptable salts thereof, which possess anti-tumour activity; to processes for their manufacture; and to pharmaceutical compositions containing them.The invention provides a quinazoline of the formula: ##STR1## wherein R.sup.1 includes hydrogen, amino and alkyl or alkoxy each of up to 4 carbon atoms;R.sup.2 includes hydrogen, alkyl, hydroxyalkyl and halogenoalkyl each of up to 4 carbon atoms;R.sup.3 is hydrogen or alkyl or up to 3 carbon atoms;Ar is phenylene or heterocyclene;L is a group of the formula --CO.NH--, --NH.CO--, --CO.NR.sup.4 --, --NR.sup.4.CO--, --CH.dbd.CH-- or --CO.O--, wherein R.sup.4 is alkyl of up to 4 carbon atoms; and Y is a branched alkyl group bearing substituents Y.sup.2 and Y.sup.3 the definition of each independently including hydroxy, cyano, aryl and heteroaryl, and the definition of Y.sup.

Abstract: There are provided substituted quinazoline compounds of formula I ##STR1## and their use for the prevention, control or amelioration of diseases caused by phytopathogenic fungi. Further provided are compositions and methods comprising those compounds for the protection of plants from fungal infestations and diseases.

Abstract: The invention relates to quinazoline derivatives, or pharmaceutically-acceptable salts thereof, which possess anti-tumour activity; to processes for their manufacture; and to pharmaceutical compositions containing them.The invention provides a quinazoline of the formula: ##STR1## wherein R.sup.1 is hydrogen or amino, or alkyl or alkoxy each of up to 6 carbon atoms; or R.sup.1 is substituted alkyl or alkoxy each of up to 3 carbon atoms;R.sup.2 is hydrogen, alkyl, alkenyl, alkynyl, hydroxyalkyl, halogenoalkyl or cyanoalkyl each of up to 6 carbon atoms;Ar is phenylene or heterocyclene;L is a group of the formula --CO.NH--, --NH.CO--, --CO.NR.sup.3 --, --NR.sup.3.CO--, --CH.dbd.CH--, --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 S--, --SCH.sub.2 --, --CO.CH.sub.2 --, --CH.sub.2 CO-- or --CO.O--, wherein R.sup.3 is alkyl of up to 6 carbon atoms; andY is aryl or heteroaryl or a hydrogenated derivative thereof; orY is a group of the formula --A--Y.sup.

Abstract: Compounds of formula (I): ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are independently hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, alkylcycloalkyl, halogen, haloalkyl, alkoxy, alkenoxy, alkoxyalkyl, haloalkoxy, alkylthio, cyano, nitro, amino, NR.sup.5 R.sup.6, hydroxy, acylamino, --CO.sub.2 R.sup.4, --O(CH.sub.2).sub.m CO.sub.2 R.sup.4, phenyl, phenoxy, benzyl or benzyloxy, the phenyl group or phenyl moiety of the benzyl group being optionally substituted in the ring; or R.sup.2 and R.sup.3 when taken together form a 5- or 6-membered ring; m is 1 or 2; R.sup.4 and R.sup.6 are hydrogen or C.sub.1-4 alkyl; R.sup.5 is C.sub.1-4 alkyl; n is 0, 1 or 2; are useful as nematicides.

Abstract: Compounds of formula (I): ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are independently hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, alkylcycloalkyl, halogen, haloalkyl, alkoxy, alkenoxy, alkoxyalkyl, haloalkoxy, alkylthio, cyano, nitro, amino, NR.sup.5 R.sup.6, hydroxy, acylamino, --CO.sub.2 R.sup.4, --O(CH.sub.2).sub.m CO.sub.2 R.sup.4, phenyl, phenoxy, benzyl or benzyloxy, the phenyl group or phenyl moiety of the benzyl group being optionally substituted in the ring; or R.sup.2 and R.sup.3 when taken together form a 5 - or 6-membered ring; m is 1 or 2; R.sup.4 and R.sup.6 are hydrogen or C.sub.1-4 alkyl; R.sup.5 is C.sub.1-4 alkyl; n is 0, 1 or 2; provided that when n is 0, R.sup.1, R.sup.2 and R.sup.3 are not all hydrogen, or when n is 0 and R.sup.2 is hydrogen, R.sup.1 and R.sup.3 are not both methyl, or when n is 0 and R.sup.2 and R.sup.3 are both hydrogen, R.sup.1 is not methyl; are useful as nematicides.

Abstract: The invention concerns a thioxo heterocycle of the formula I ##STR1## wherein Q is a 10-membered bicyclic heterocyclic moiety containing 1 or 2 N's which bears 1 or 2 thioxo substituents and which is optionally further substituted;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 compound of formula I: ##STR1## wherein R is hydrogen; oran alkyl, alkenyl or alkynyl group of up to 6 carbon atoms; nis O; 1 or 2; Z represents --CH.dbd.CH-- or --S--; each X independently represents halogeno, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, nitro or trifluoromethyl; and Y represents a group of formula: ##STR2## or a pharmaceutically acceptable salt or ester thereof.

Abstract: The present invention relates to quinazoline-3-alkanoic acid derivatives having both an inhibitory effect on platelet aggregation and a hindering effect on aldose reductase together, represented by a general formula [I] ##STR1## [wherein R is hydrogen or a protecting group for carboxyl group, R.sup.1 is a lower alkyl group, alkenyl group, alkinyl group, lower alkoxy group, lower alkylthio group, halogen, phenyl group (this phenyl group may be substituted by one to three of lower alkyls, lower alkoxys, halogens, trifluoromethyls, carboxyethylenes or ethoxycarbonylethylenes, naphthyl group, heterocycle (this heterocycle may be substituted by one to three of lower alkyls), cycloalkyl group or benzoyl group (this benzoyl group may be substituted by lower alkyl or halogen), R.sup.2 and R.sup.3 are identically or differently hydrogens, halogens, lower alkyl groups, lower alkoxy groups, aralkyl groups which may be substituted, nitro groups, imidazolyl groups, imidazolylmethyl groups or ##STR2## (R.sup.4 and R.sup.

Abstract: Substituted quinazolinones and pyridopyrimidines of structural formula 1 ##STR1## are angiotensin II antagonists useful in the treatment of disorders related to the reninangiotensin system (RAS) such as hypertension, congestive heart failure, ocular hypertension and certain CNS disorders.

Abstract: 3-Piperidinyl-indazole derivatives and their pharmaceutically acceptable acid addition salts being useful antagonists of neurotransmitters; pharmaceutical compositions containing the same and a method of treating warm-blooded animals suffering from diseases associated with the release of said neutrotransmitters.

Abstract: The invention relates to substituted 2-pyrimidinyl-1-piperazine derivatives defined herein by formula (I), processes for their manufacture, compositions containing said substituted 2-pyrimidinyl-1-piperazine derivatives as active materials and the use of said compounds and compositions as agents effecting the central nervous system. Also included in the invention are intermediates of formula (VIII) for making the active formula (I) compounds.

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 present invention is novel selected hydroxamic acid derivatives of fenamic acids having 5-lipoxygenase and cyclooxygenase inhibiting properties, pharmaceutical compositions for treating conditions advantageously affected by the inhibition and methods for treating these conditions in mammals, including humans suffering therefor.

Abstract: A novel piperidine derivative is defined by the formula (I), including a slt thereof, ##STR1## wherein R.sup.1 denotes a univalent group derived from one selected among substituted or unsubstituted benzene, pyridine, pyrazine, indole, anthraquinone, quinoline, substituted or unsubstituted phthalimide, homophthalimide, pyridinecarboxylic acid imide, pyridine N-oxide, pyrazinedicarboxylic acid imide, naphthalenedicarboxylic acid imide, substituted or unsubstituted quinazolinedione, 1,8-naphthalimide, bicyclo [2.2.2] oct-5-ene-2,3-dicarboxylic acid imide and pyromerylimide,X denotes a group of the formula --(CH.sub.2).sub.n --, a group of the formula --O(CH.sub.2).sub.n --, a group of the formula --S(CH.sub.2).sub.n --, a group of the formula --NH(CH.sub.2).sub.n --, a group of the formula --SO.sub.2 NH(CH.sub.2).sub.n --, a group of the formula ##STR2## a group of the formula ##STR3## a group of the formula ##STR4## a group of the formula --CH.sub.2 NH(CH.sub.2).sub.

Abstract: Compounds of the formula (I) ##STR1## wherein R represents H or C.sub.1-6 alkyl;R.sub.1 and R.sub.2 represent H, halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkythio, C.sub.1-6 alkoxycarbonyl, carboxyl, hydroxy, nitro, cyano, optionally C.sub.1-4 alkyl mono- or disubstituted carbamoyl, optionally C.sub.1-4 alkyl mono- or disubstituted amino, C.sub.1-6 acylamino, C.sub.1-4 alkoxy carbonylamino, C.sub.1-6 alkylsulphynyl, C.sub.1-6 alkylsulphonyl or C.sub.1-6 acyl;R.sub.3 represents H, C.sub.1-6 alkyl, aryl or aralkyl, or it may be absent;A represents CO or C.dbd.S;E represents nitrogen;D represents CO or CR.sub.4 R.sub.5 when the E--D bond is single, or D is C--R when the D--E bond is double, in which R.sub.4 represents H, C.sub.1-6 alkyl, aryl, aralkyl, hydroxy or C.sub.1-4 alkoxy and R.sub.5 represents H;X represents oxygen or N--R, or it is absent;Y represents a basic group selected from: ##STR2## in which n is 2 or 3; p is 0 or 1 at the same time or not; q is 0,2 or 3; R.sub.6 and R.sub.

Abstract: Color formers of the formula ##STR1## in which X.sup.1 denotes hydroxyl, alkoxy, alkenyloxy, aralkoxy, cycloalkoxy, aryloxy or acyloxy,R.sup.1 denotes hydrogen, halogen, alkyl or alkoxy,R.sup.2 denotes hydrogen, alkoxy, aralkoxy, aryloxy or a radical of the formula ##STR2## Y.sup.1 and Y.sup.2, independently of one another, denote alkyl, cycloalkyl or aralkyl,R.sup.2 can form a heterocyclic ring with A in the o-position, in which a benzene ring can be additionally fused onto ring A in the o-/m-position with respect to R.sup.2,R.sup.3 denotes hydrogen, alkyl, alkenyl, aralkyl, cycloalkyl or aryl, or R.sup.3 is linked to ring B in the o-position with respect to the nitrogen,Z.sup.1 stands for the remaining members of a partially hydrogenated or completely hydrogenated ring, with the proviso that Z.sup.

Abstract: A quinazoline of the formula: ##STR1## wherein R.sup.1 is alkyl, cycloalkyl, alkenyl, alkynyl, alkoxy, alkylthio, aryl, aryloxy, arylalkyl, halogeno, hydroxy, mercapto, pyridylthio, pyrimidinylthio, or substituted alkyl or alkoxy;wherein R.sup.2 is hydrogen, alkyl, alkenyl, alkynyl, substituted alkyl or alkanoyl;wherein Ar is phenylene, naphthylene or heterocyclene which is unsubstituted or bears one or more substituents and wherein R.sup.3 is such that R.sup.3 --NH.sub.2 is an amino acid;or a pharmaceutically-acceptable salt or ester thereof. The compounds possess anti-tumor activity.

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: 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: 2,4-diaminoquinazoline compounds are inhibitors of the H.sup.+ K.sup.+ ATPase enzyme and useful for the treatment of diseases of the stomach based on excessive gastric acid secretion. A compound of the invention is 2-[2-methyl-4-fluorophenyl)amino]-4-(N-methylphenylamino)quinazoline.

Abstract: This invention pertains to novel substituted N-aryl-N-[4-(1-heterocyclicalkyl)piperidinyl]amides useful as analgesics, and methods of administering analgesia, which comprises the systemic administration to mammals of such compounds, and pharmaceutical compositions containing such compounds, wherein the novel compounds have the general formula: ##STR1## including optically active isomeric forms, and the pharmaceutically acceptable acid addition salts thereof, wherein R, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are defined in the disclosure.

Abstract: A novel piperidine derivative is defined by the formula (I), including a salt thereof, ##STR1## wherein R.sup.1 denotes a univalent group derived from one selected among substituted or unsubstituted benzene, pyridine, pyrazine, indole, anthraquinone, quinoline, substituted or unsubstituted phthalimide, homophthalimide, pyridinecarboxylic acid imide, pyridine N-oxide, pyrazinedicarboxylic acid imide, naphthalenedicarboxylic acid imide, substituted or unsubstituted quinazolinedione, 1,8-naphthalimide, bicyclo [2.2.2] oct-5-ene-2,3-dicarboxylic acid imide and pyromerylimide,X denotes a group of the formula --(CH.sub.2).sub.n --, a group of the formula --O(CH.sub.2).sub.n --, a group of the formula --S(CH.sub.2).sub.n --, a group of the formula --NH(CH.sub.2).sub.n --, a group of the formula --SO.sub.2 NH(CH.sub.2).sub.n --, a group of the formula ##STR2## a group of the formula ##STR3## a group of the formula ##STR4## a group of the formula --CH.sub.2 NH(CH.sub.2).sub.

Abstract: (1H-azol-1-ylmethyl)substituted quinazoline derivatives, compositions containing the same, and methods of treating mammals suffering from disorders which are characterized by an increased proliferation and/or abnormal differentiation of epithelial tissues.

Abstract: This invention pertains to novel substituted N/aryl-N-[4-(1-heterocyclicalkyl)piperidinyl]amides useful as analgesics, and methods of administering analgesia, which comprises the systemic administration to mammals of such compounds, and pharmaceutical compositions containing such compounds, wherein the novel compounds have the general formula: ##STR1## including optically active isomeric forms, and the pharmaceutically acceptable acid addition salts thereof, wherein R, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are defined in the disclosure.