Abstract: Quinazoline derivatives having an oxy substituent in 5 and 6 positions are described. The novel quinazoline derivatives are useful as cardiotonic agents.

Abstract: Quinazolinone derivatives having an oxy substituent in the 5- and 6-positions are disclosed. The quinazolinone derivatives are useful as cardiovascular agents.

Abstract: The synthesis of substituted 2(1H)-quinazolinone-1-alkanoic acids and their esters is described. The novel quinazolinones are renal vasodilators and as such reduce vascular resistance to renal blood flow. The quinazolinones are useful as cardiovascular agents.

Abstract: A process for the preparation of 6,7-dihydroxy-4-alkyl-2(1H) quinazolinone-1-propionic acids is described. The propionic acid compounds are renal vasodilators and thereby increase renal blood flow. They are useful as cardiovascular agents.

Abstract: There are described novel dyes of the formulae ##STR1## in which R.sub.1 and R.sub.2 independently of one another are each hydrogen, unsubstituted or substituted alkyl, cycloalkyl, aralkyl or aryl, and R.sub.1 and R.sub.2 together with the nitrogen atom, and optionally with the inclusion of further hetero atoms, can also form a 5- to 7-membered heterocycle, or one of the radicals R.sub.1 or R.sub.2 can be linked with the carbon atom, in the o-position with respect to the amino group, of the ring A to form a fused-on, saturated, unsubstituted or substituted 5- or 6-membered ring,X is .dbd.NR.sub.3, .dbd.NCOR.sub.4, ##STR2## .dbd.NH or .dbd.O, wherein R.sub.3 is alkyl or unsubstituted or substituted phenyl,R.sub.4 is unsubstituted or substituted alkyl, aralkyl, aryl, vinyl, alkoxy, phenoxy or amino, andR.sub.5 is cyano, carbalkoxy, or unsubstituted or substituted carbonamide, andR.sub.

Abstract: The synthesis of substituted quinazolinones is described. The novel quinazolinones are renal vasodilators and thereby increase renal blood flow, and are useful as cardiovascular agents.

Abstract: 2-Permissibly-substituted-6-dialkylaminotetrahydroquinazolines, receptor agonists.

Abstract: 4-Alkyl-5,6-, 6,7-methylenedioxy-2-1[H]-quinazolinones are prepared from 2,3-methylenedioxyacetophenones. The 4-alkyl-5,6-, 6,7-methylenedioxy-2-1[H]-quinazolinones are active as cardiotonic agents.

Abstract: The present invention relates to novel quinazolinone derivatives and pharmaceutically acceptable salts thereof. More particularly, it relates to novel quinazolinone derivatives and pharmaceutically acceptable salts thereof which have antiallergic activities, to processes for the preparation thereof, to pharmaceutical composition comprising the same, and to a method of using the same therapeutically in the treatment of allergic symptoms in human being and animals.

Abstract: This invention relates to the compound 3-[2-(2-Benzimidazolyl) Benzoyloxyethyl]-4(3H)-Quinazolinone of Formula I, and a process for the preparation thereof. The compound exhibits strong analgesic activity and almost zero toxicity in laboratory mice. ##STR1## The compound of Formula I is prepared by acylation of the compound 3-(2-hydroxyethyl)-4(3H)-quinazolinone with a reactive derivative of 2-(2-benzimidazolyl)benzoic acid, preferably its imidazolide, formed by treatment of the acid of Formula III with 1,1'-carbonyldiimidazole. The compounds of Formula II and Formula III are reacted in situ, at room temperature, and in the presence of an inert organic solvent. The product compound is isolated and purified by common techniques.

Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, lower cycloalkyl, lower alkoxy, hydroxy, halo, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, di-(C.sub.1 -C.sub.7) alkyl-N(CH.sub.2).sub.n O-- or 2-hydroxyethoxy; n is 2 to 7; R.sub.2 is hydrogen, lower alkyl or lower alkoxy; R.sub.3 is hydrogen or methyl; R.sub.4 is hydrogen or lower alkyl; R.sub.5 is hydrogen or lower alkyl provided however if R.sub.2 is other than hydrogen R.sub.5 is hydrogen; m is 1 to 7; Y is ##STR2## --O-- or --S--; w is zero or one; and A is an unsubstituted or substituted aromatic 5- or 6-membered heterocyclic radical;or pharmaceutically acceptable addition salts thereof are described. The compounds of formula I are useful for treating allergic conditions and vascular disorders.

Abstract: Novel derivatives of 2,3-dihydro-5H-thiazolo[2,3-b]quinazoline, such as (3-oxo-5H-thiazolo[2,3-b]quinazolin-2(3H)-ylidene)acetic acid ethyl ester, N-Benzyl-[3-oxo-5H-thiazolo[2,3-b]quinazolin-2(3H)-ylidene]acetamide, N-tertbutyl-N-benzyl-(3-oxo-5H-thiazolo[2,3-b]quinazolin-2(3H)-ylidene)ace tamide, and 2,3-dihydro-3-oxo-5H-thiazolo[2,3-b]quinazoline-2-acetic acid methyl ester; useful as immunomodulators.

Abstract: Certain novel heterocyclic compounds, aromatic thioesters, their preparation, and their use in inhibiting serine proteases with chymotrypsin-like and elastase-like specificity and in the treatment of diseases such as emphysema which involve tissue proteolysis.

Abstract: Heterocyclic compounds which are inhibitors of histamine activity, in particular, inhibitors of H-2 histamine receptors. A specific compound of this invention is 2-[2-(4-methyl-5-imidazolylmethylthio)ethylamino]-4-pyrimidone.

Abstract: This invention relates to cytosine derivatives which have histamine H.sub.2 -antagonist activity. A specific compound of this invention is 4-[3-(3-(piperidinomethyl)phenoxy)propylamino]-pyrimidin-2-thione.

Abstract: A process for preparing 4-alkyl-2(1H)quinazolinone-1-alkanoic acid derivatives is described. The 4-alkyl-2(1H)quinazolinones are useful as cardiovascular agents.

Abstract: The synthesis of substituted 2(1H)-quinazolinone-1-alkanoic acids and their esters is described. The novel quinazolinones are renal vasodilators and as such reduce vascular resistance to renal blood flow. The quinazolinones are useful as cardiovascular agents.

Abstract: A process for preparing 4-alkyl-2-(1H) quinazolinone-1-alkanoic acid derivatives is described. The 4-alkyl-2-(1H) quinazolinones are useful as cardiovascular agents.

Abstract: There are described novel dyes of the formulae ##STR1## in which R.sub.1 and R.sub.2 independently of one another are each hydrogen, unsubstituted or substituted alkyl, cycloalkyl, aralkyl or aryl, and R.sub.1 and R.sub.2 together with the nitrogen atom, and optionally with the inclusion of further hetero atoms, can also form a 5- to 7-membered heterocycle, or one of the radicals R.sub.1 or R.sub.2 can be linked with the carbon atom, in the o-position with respect to the amino group, of the ring A to form a fused-on, saturated, unsubstituted or substituted 5- or 6-membered ring,X is .dbd.NR.sub.3, .dbd.NCOR.sub.4, ##STR2## .dbd.NH or .dbd.O, wherein R.sub.3 is alkyl or unsubstituted or substituted phenyl,R.sub.4 is unsubstituted or substituted alkyl, aralkyl, aryl, vinyl, alkoxy, phenoxy or amino, andR.sub.5 is cyano, carbalkoxy, or unsubstituted or substituted carbonamide, andR.sub.

Abstract: This invention is directed to new quinazoline derivatives of the following formula having use in the treatment of symptoms associated with allergic manifestations. ##STR1## wherein R.sub.a.sup.1 and R.sub.b.sup.1 are C.sub.2 -C.sub.7 alkoxycarbonyl or R.sub.a.sup.1 and R.sub.b.sup.1 is linked together to form a group of the formula: ##STR2## R.sup.2 and R.sup.3 are hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, nitro, amino, C.sub.1 -C.sub.6 alkoxy, phenoxy, C.sub.1 -C.sub.6 alkylthio, C.sub.1 -C.sub.6 alkylpiperazinyl, C.sub.1 -C.sub.18 alkanoylamino, di(C.sub.1 -C.sub.6)alkanoylamino, C.sub.3 -C.sub.9 alkoxalylamino, C.sub.4 -C.sub.8 cycloalkylcarbonylamino, C.sub.3 -C.sub.7 cycloalkyl(C.sub.1 -C.sub.6)alkanoylamino, benzamido, phenyl(C.sub.1 -C.sub.6)alkanoylamino, C.sub.1 -C.sub.6 alkylsulfonylamino or di(C.sub.1 -C.sub.6)alkylamino which may be substituted with hydroxy,A.sup.1 is a group of the formula: ##STR3## in which R.sup.4 is hydrogen C.sub.1 -C.sub.6 alkyl, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.

Abstract: The present invention relates to new derivatives of formula: ##STR1## in which: R.sub.3 denotes a halogen, preferably chlorine, or a nitro group,R.sub.4 represents hydrogen or a lower alkyl group having from 1 to 4 atoms of carbon,R.sub.5 represents an atom of halogen, preferably chlorine or fluorine.It also relates to a process for preparing products of formula (II) and to the drugs containing at least one product of formula (II).

Abstract: Novel quinazoline derivatives, comprising in the heterocyclic part of their quinazoline nucleus at least one carbonyl or thiocarbonyl group and a particularly substituted piperidinyl-alkyl side chain, said compounds being potent serotonin-antagonists.

Abstract: The synthesis of substituted quinazolinones is described. The novel quinazolinones are renal vasodilators and thereby increase renal blood flow, and are useful as cardiovascular agents.

Abstract: Quinazoline derivatives of the formulae: ##STR1## wherein A.sup.1 is ##STR2## A.sup.2 is ##STR3## R.sup.1 is hydrogen, carboxy or esterified carboxy, R.sub.a.sup.1 and R.sub.b.sup.1 are esterified carboxy,R.sup.2 and R.sup.3 are hydrogen, alkyl, halogen, nitro, amino, alkoxy, aryloxy, alkylthio, alkylpiperazinyl, acylamino or dialkylamino which may be substituted with hydroxy,R.sup.4 is hydrogen, alkyl, hydroxy, alkoxy, alkenyloxy, dialkylamino or 2,2-dialkoxycarbonylvinylaminoR.sub.a.sup.4 is hydrogen, alkyl, hydroxy, alkoxy, alkenyloxy or dialkylamino,R.sup.5 is alkyl or alkenyl, andR.sup.6 is carboxy or esterified carboxy.

Abstract: The invention provides amidoxime derivatives of the general formula ##STR1## wherein R.sub.1 is an alkyl group of 1 to 8 carbon atoms, phenyl, a heterocyclic ring structure of 5 to 8 atoms containing one or more nitrogen or oxygen atoms or combinations thereof or a bicyclic condensed ring system optionally containing at least one heterocyclic ring which groups may each be optionally substituted. R.sub.2 is a mono or bicyclic heterocyclic radical containing at least two nitrogen atoms which radical is also optionally substituted. R.sub.3 and R.sub.4 are independently H, or an alkyl of 1 to 4 carbon atoms or one, but not both, is ##STR2## and the other, H, wherein R.sub.5 or R.sub.6 are alkyls of 2 to 5 carbon atoms optionally substituted by R.sub.1, or a phenyl optionally substituted by R.sub.1 or R.sub.5 or R.sub.6 is combined with R.sub.1 to jointly form cyclic imidoximes or imidedioximes.

Abstract: A process for the production of 4-phenyl-2(1H)-quinazolinones and -4a,5,6,8a-tetrahydro-2(1H)-quinazolinones which comprises introducing the desired phenyl radical into a corresponding quinazolin-2,4(1H,3H)-dione by way of a Grignard reaction and hydrolysis of the resulting product.

Abstract: 2(1H)-Quinazolinone and quinazolinethione derivatives having excellent pharmacological activities are produced in high yield with high purity by heating the corresponding 3,4-dihydro-2(1H)-quinazolinone or quinazolinethione derivatives together with sulfur in an inert solvent.

Abstract: Quinazoline derivatives of the formulae: ##STR1## wherein A.sup.1 is ##STR2## A.sup.2 is ##STR3## R.sup.1 is hydrogen, carboxy or esterified carboxy, R.sub.a.sup.1 and R.sub.b.sup.1 are esterified carboxy,R.sup.2 and R.sup.3 are hydrogen, alkyl, halogen, nitro, amino, alkoxy, aryloxy, alkylthio, alkylpiperazinyl, acylamino or dialkylamino which may be substituted with hydroxy,R.sup.4 is hydrogen, alkyl, hydroxy, alkoxy, alkenyloxy, dialkylamino or 2,2-dialkoxycarbonylvinylaminoR.sub.a.sup.4 is hydrogen, alkyl, hydroxy, alkoxy, alkenyloxy or dialkylamino,R.sup.5 is alkyl or alkenyl, andR.sup.6 is carboxy or esterified carboxy.

Abstract: A new piperidine derivative represented by the formula: ##STR1## wherein X is oxygen, sulfur, carbonyl, hydroxymethylene or methylene; R is straight-chain alkylene having 1-4 carbon atoms with or without lower alkyl substituent(s); m and n are 0 or 1, and are different from each other (i.e., both m and n are not 0 or 1); and (D).sub.m', R.sup.1 and (R.sup.2)n' are usually used as substituents, has a hypotensive activity.

Abstract: Novel quinazoline derivatives, comprising in the heterocyclic part of their quinazoline nucleus at least one carbonyl or thiocarbonyl group and a particularly substituted piperidinyl-alkyl side chain, said compounds being potent serotonin-antagonists.

Abstract: A compound of the formula ##STR1## in which R.sub.1 denotes optionally substituted lower alkyl which is optionally branched at the linking carbon atom, R.sub.2 represents hydrogen or lower alkanoyl and R.sub.3 is a group of the formula --R.sub.3.sup.a --(R.sub.3.sup.b).sub.n -- (Ia), in which R.sub.3.sup.a represents the radical of the formula --N(R.sub.4)-- or --O-- and R.sub.4 represents hydrogen or lower alkyl, R.sub.3.sup.b denotes the radical of the formula --CH.sub.2 -- or, if R.sub.3.sup.a represents --N(R.sub.4)--, denotes the radical of the formula --C(.dbd.O)-- and n represents nought or 1, and a group of the formula Ia, in which n represents 1, can be linked to the carbonyl group of the carbamoyl grouping either via the group R.sub.3.sup.a or the group R.sub.3.sup.b, or acid addition salts thereof, which can be used pharmaceutically can be used as beta-receptor blocking agents for the treatment of disorders in the cardiac rhythm and coronary heart diseases.

Abstract: Heterocyclic sulfenamides, such as N-[2-chloro-5-(trifluoromethyl)phenyl]-N-[2,4-dinitro-6-trifluoromethyl)ph enyl]-3-nitro-2-pyridinesulfenamide, are useful as miticides, insecticides, fungicides and ovicides.

Abstract: Improved process for the preparation of 6-substituted-4-phenylquinazolinone 3-oxides. Such compounds are useful as intermediates in the preparation of 3-fluorobenzodiazepines, which are useful as tranquilizers, muscle relaxants and sedatives.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1,R.sup.2,R.sup.3 and R.sup.4 are as hereinafter described, tautomers and salts thereof, are disclosed. The foregoing compounds inhibit the aggregation of blood platelets which renders them useful as therapeutic agents in the prophylaxis of thromboses. Furthermore, they are useful for the treatment and prophylaxis of cardiac insufficiency and cardiac failure, due to their inotropic activity without substantial tachycardia.

Abstract: The invention provides a process for the production of 4-phenyl-2(1H)-quinazolinones by cyclising a corresponding 2-aminobenzophenone with urea or an alkylcarbamate in the presence of an aromatic acid. The products are known anti-inflammatory agents.

Abstract: An azo dye of the general formula ##STR1## where A is cyano or carbamoyl,R is hydrogen, alkyl or phenyl,R.sup.1 is hydrogen, bromine, chlorine or nitro,R.sup.2 is hydrogen, chlorine, bromine, nitro, methyl, trifluoromethyl, sulfamoyl, N-monoalkyl- or N,N-dialkylsulfamoyl (where alkyl is of 1 to 4 carbon atoms), or a sulfonic acid phenyl ester, methylphenyl ester, chlorophenyl ester or methoxyphenyl ester group,R.sup.3 is hydrogen or alkyl of 1 to 8 carbon atoms which may be interrupted by oxygen and may be substituted by hydroxyl, pyrrolidonyl, phthalimidyl, alkoxy of 1 to 8 carbon atoms, allyloxy, benzyloxy, phenylethoxy, phenoxy, methylphenoxy, chlorophenoxy, methoxyphenoxy, or optionally substituted arylsulfonyl, or is benzyl, phenylethyl or cyclohexyl, or is phenyl which is unsubstituted or substituted by chlorine, bromine, nitro, methyl, ethyl, methoxy, ethoxy, phenoxy or dialkylamino (where alkyl is of 1 to 4 carbon atoms), or is naphthyl, pyridyl, thienyl or furyl,the substituents B.sup.

Abstract: 3,4-Dihydro-2(1H)-quinazolinones and quniazolinethiones such as 1-cyclopropylmethyl-4-phenyl-6-methoxy-3,4-dihydro-2(1H)-quinazolinone and its thione derivative, are prepared in high yield with high purity by heating the corresponding arylurea or thiourea such as N-cyclopropylmethyl-N-(p-methoxyphenyl) urea or its thiourea derivative, with the corresponding aldehyde such as benzaldehyde in the presence of hydrobromic acid in an inert solvent.

Abstract: 1-Polyhaloalkyl-2(1H)-quinazoline derivatives of the formula, ##STR1## wherein R is polyhaloalkyl having C.sub.2 -C.sub.4 alkyl; and R.sub.1, R.sub.2 and R.sub.3 are individually hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, nitro, trifluoromethyl or halogen, have excellent anti-inflammatory and analgesic activities with very low toxicity. These quinazolinone derivatives can be prepared, for example, by reacting a trihalogenoacetamidobenzophenone derivative with ammonia.

Abstract: Tricyclic quinazolines of the formula, ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and A are as defined in the specification, such as 4,5-dihydro-5-arylimidazo[1,2-a]quinazolines, 4,5-dihydro-5-aryl-s-triazolo[4,3-a]quinazolines and 4,5-dihydro-5-aryltetrazolo[1,5-a]quinazolines having anti-inflammatory and analgesic activity are, for example, prepared by reducing the corresponding 4,5-unsaturated compounds, and then, if necessary, by alkylating the thus produced compounds.

Abstract: Imidazo- and pyrimido[2,1-b]quinazolines of the formula, ##STR1## wherein R.sub.1 and R.sub.2 are independently hydrogen, halogen, trifluoromethyl, nitro, C.sub.1-4 alkyl or C.sub.1-4 alkoxy, or R.sub.1 and R.sub.2 may together represent methylenedioxy; R.sub.3 is hydrogen, C.sub.1-4 alkyl, phenyl or substituted phenyl of the formula, ##STR2## (wherein R is halogen, C.sub.1-4 alkyl or C.sub.1-4 alkoxy); R.sub.4 is hydrogen, C.sub.1-4 alkyl or aralkyl; and A is C.sub.2-3 alkylene wich may be optionally substituted by one or two C.sub.1-2 alkyl radicals, and pharmaceutically acceptable acid addition salts thereof, are prepared by reacting a compound of the formula, ##STR3## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and A are as defined above; and X is oxygen or sulfur, with a halogenating agent at a temperature of about 30.degree. C. to about 180.degree. C. In the above imidaxo- and pyrimido[2,1-b]quinazolines, those having C.sub.1-4 alkyl, or ##STR4## as R.sub.

Abstract: Quinazoline-2(1H)-ones are prepared by dehydrogenating a 5,6,7,8-tetrahydro-2(1H)-quinazolinone with sulfur in the presence of a metal oxide, hydroxide or halide.

Abstract: 1-Methyl-6-substituted-4-phenyl-quinazolin-2-one-3-oxides and their use as intermediates in the preparation of 3-fluorobenzodiazepines which are useful as tranquilizers, muscle relaxants and sedatives.

Abstract: Viral infections caused by viruses which belong to, e.g. Pox, Herpes, Adeno, Myxo, Paramyxo groups are controlled by administering an effective amount of quinazoline derivatives of the formula ##STR1## wherein R.sub.1 is cyclo, C.sub.3 -C.sub.8 alkyl, cyclo C.sub.3 -C.sub.8 alkyl C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy C.sub.1 -C.sub.4 alkyl, C.sub.2-C.sub.5 alkenyloxy C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkylthio C.sub.1 -C.sub.4 alkyl, polyhalo C.sub.1- C.sub.4 alkyl, a group of the formula ##STR2## (wherein m is an integer of 1 to 3; and R.sub.4 and R.sub.5 are individually C.sub.1 -C.sub.4 alkyl, and may form together with the adjacent nitrogen atom an unsubstituted or C.sub.1 -C.sub.4 alkyl substituted 3 to 6 membered saturated heterocyclic ring, which may contain another nitrogen or oxygen atom) or a group of the formula --C.sub.n H.sub.2n --R.sub.6 (wherein n is 0 or an integer of 1 to 3; and R.sub.

Abstract: 6-Substituted-2-halofluoromethyl-1,2-dihydro-2-hydroxy-1-methyl-4-phenylqui nazolines and their use as intermediates in the preparation of 3-fluorobenzodiazepines, which are useful as tranquilizers, muscle relaxants and sedatives.

Abstract: A compound of the formula ##STR1## in which R.sub.1 denotes optionally substituted lower akyl which is optionally branched at the linking carbon atom, R.sub.2 represents hydrogen or lower alkanoyl and R.sub.3 is a group of the formula --R.sub.3.sup.a -(R.sub.3.sup.b).sub.n -- (Ia), in which R.sub.3.sup.1 represents the radical of the formula --N(R.sub.4)-- or --O-- and R.sub.4 represents hydrogen or lower alkyl, R.sub.3.sup.b denotes the radical of the formula --CH.sub.2 -- or, if R.sub.3.sup.a represents --N(R.sub.4)--, denotes the radical of the formula --C(.dbd.O)-- and n represents nought or 1, and a group of the formula Ia, in which n represents 1, can be linked to the carbonyl group of the carbamoyl grouping either via the group R.sub.3.sup.a or the group R.sub.3.sup.b, or acid addition salts thereof, which can be used pharmaceutically can be used as beta-receptor blocking agents for the treatment of disorders in the cardiac rhythm and coronary heart diseases.

Abstract: A one-stage process for the production of a 2-equivalent acylacetamide yellow coupler, in which one hydrogen atom of the .alpha.-methylene group of the acyl acetamide coupler molecule is substituted by a group which is attached through an oxygen or nitrogen atom and which can be split off during chromogenic development with an oxidized color developer containing a primary aromatic amino group, which process is carried out by reactingA 4-equivalent acylacetamide yellow coupler withA compound containing an aromatic hydroxyl group or an --NH-- group in a heterocyclic ringIn the presence of a halogen, or an agent which releases halogen, andA basic condensation agentIn a substantially aprotic solvent.

Abstract: A one-step process for the preparation of 2,4-dihaloquinazolines is disclosed beginning with methoxycarbonyl- or phenoxycarbonyl-derivatives of substituted phenylureas which are cyclized and concomitantly halogenated with a cyclizing-halogenating reagent such as N,N-dimethylaniline in phosphorus oxychloride. The 2,4-dihaloquinazolines of the instant process are particularly valuable as intermediates in the preparation of 4-amino-2-(4-substituted-piperazin-1-yl) quinazolines useful in the treatment of cardiovascular disorders such as hypertension.

Abstract: 3,4-Dihydro-2(1H)-quinazolinone derivatives of the formula, ##STR1## wherein R.sub.1 and R.sub.2 signify individually a hydrogen atom, a lower alkyl group, a lower alkoxy group, a nitro group, a trifluoromethyl group, a lower alkylthio group, a lower alkylsulfonyl group or a halogen atom; R.sub.3 signifies a phenyl group, a halophenyl group, a lower alkylphenyl group, a lower alkoxyphenyl group, a trifluoromethylphenyl group, a lower cycloalkyl group, a lower cycloalkenyl group, a pyridyl group, a pyrrolyl group, a furyl group, a thienyl group or a naphthyl group; R.sub.

Abstract: 1,4-Substituted-2(1H)-quinazolinone derivatives are prepared by contactng a 2-aminophenyl ketone derivative with an alkaline agent such as alkali metal, alkali metal hydride, alkali metal amide, etc., reacting the thus obtained metal salt of 2-aminophenyl ketone derivative with a reactive ester of alcohols, reacting the thus obtained 2-(N-mono-substituted amino)-phenyl ketone derivative with a lower alkyl haloformate or a benzyl haloformate, and reacting the thus obtained carbamate derivative with ammonia. The 1,4-substituted-2(1H)-quinazolinone derivatives have excellent pharmacological properties, particularly as anti-inflammatory and analgesic effects.

Abstract: Optionally substituted 1,2,3,5-tetrahydroimidazol[2,1-b]-quinazolin-2-ones and 6-[H]-1,2,3,4-tetrahydropyrimidol[2,1-b]quinazolin-2-ones or the pharmaceutically acceptable salts thereof are compounds useful as blood platelet anti-aggregative and/or antihypertensive and/or bronchodilator agents in mammals, including humans.