Abstract: 1-Azinyl-tetraozolinones of the following formulae (I) and (II): ##STR1## wherein R.sup.1 and R.sup.2 are independently represent alkyl, haloalkyl, cycloalkyl, alkenyl, haloalkenyl, alkynyl or optionally substituted phenyl, orR.sup.1 and R.sup.2, together with the nitrogen atom to which they are bonded, may form a 5- or 6-membered heterocyclic ring which may optionally contain a further heteroatom, and said heterocyclic ring may optionally be benzo-condensed and/or be substituted by one or more of C.sub.1-4 alkyl(s), andR.sup.3 is a 6-membered heterocyclic aromatic group consisting of carbon atoms and 2 or 3 nitrogen atoms, which may optionally be substituted by halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, di(C.sub.1-4 alkyl)amino or phenyl.The compounds of the formula (I) exhibit an excellent herbicidal activity and the compounds of the formula (II) are useful as starting materials in the production of the compounds of the formula (I).

Abstract: This invention relates to compounds of Formula I ##STR1## which are useful in association with a pharmaceutical carrier as antiatherosclerotic agents. In addition, various compounds of Formula I are useful inhibitors of cell proliferation.

Abstract: Herbicidal substituted hydroxybenzyl-heteroaryl compounds and derivatives thereof of the formula ##STR1## wherein Ar is a substituted or unsubstituted 5- or 6-membered heteroaryl group having 2 or 3 ring nitrogen atoms or a substituted or unsubstituted 5-membered heteroaryl group having two ring heteroatoms, one of the ring heteroatoms being nitrogen and the other being sulfur or oxygen. Herbicidal compositions containing such substituted hydroxybenzyl-heteroaryl compounds and derivatives thereof and methods of controlling undesirable vegetation employing these compounds and derivatives are also disclosed. The compounds in which XR is hydroxyl are also useful as intermediates for producing the disclosed substituted hydroxybenzyl-heteroaryl derivatives.

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: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Intermediates of structural formula ##STR1## can be made by reacting glycidol or an activated derivative thereof with an amide. The process and intermediates are useful for synthesizing HIV protease inhibitor compounds.

Abstract: Novel pyrazine derivatives represented by the formula (1) and salts thereof which possess inhibitory effect against superoxide radicals (O.sub.2.sup.-) released from the macrophage cells of guinea pig by stimulation, and also possess anti-albuminuria activity in Masugi nephritis. ##STR1## The pyrazine derivatives (1) and salts thereof are useful agents for preventing and treating of various diseases caused by the superoxide radicals, for example, diseases of autoimmune such as rheumatoid arthritis, arteriosclerosis, ischemic heart disease, transient cerebral ischematic attack, hepatic insufficiency, renal insufficiency and the like, as well as they are useful agents for preventing and treating the nephritis in various clinical fields.

Abstract: A compound having the formula ##STR1## wherein A is CR.sub.7 ; and R.sup.1 through R.sup.7 are substituents such as hydrogen, halogen, branched and straight chain hydrocarbons, cyclic hydrocarbons, aromatics, and sulfur and nitrogen containing functional groups. Further, R.sup.5 and R.sup.6 may be taken together with the atom to which they are attached to form a group ##STR2## in which R.sup.9 and R.sup.10 are further functional groups. The compounds are useful in herbicidal compositions, particularly in combination with carriers and surfactants. A process for making this compound is also presented.

Abstract: Novel 9-amino-7-(substituted amino)-6-demethyl-6-deoxytetracyclines having activity against a wide spectrum of organisms including organisms which are resistant to tetracyclines are disclosed. Also disclosed are intermediates and methods for making the novel compounds of the present invention.

Abstract: A 2-Acylaminothiazole of formula: ##STR1## in which R.sub.1 is H, an alkyl or a substituted alkyl; R.sub.IV is a cycloalkyl, an aromatic group such as phenyl or a heterocyclic group which are unsubstituted or substituted; R.sub.V is a substituted alkyl, a substituted carboxy such as an ester or an amide; or R.sub.IV and R.sub.V together represent a phenoxyalkylene group which may be substituted on the phenyl; and Z is a heterocyclic e.g. indolyl group; or a salt of compound (I).

Abstract: The present invention relates to novel tetramethylpiperidine compounds of the formula (I) ##STR1## in which R.sub.1 is e.g. hydrogen or methyl, R.sub.2 and R.sub.3 are e.g. --(CH.sub.2).sub.2 --, R.sub.4 is e.g. --CO--, --COCO-- or --COCH.sub.2 CO--, n is e.g. 1 and R.sub.5 is e.g. hydrogen or allyl.These compounds are suitable for use as light stabilizers, heat stabilizers and oxidation stabilizers for organic materials.

Abstract: Water-insoluble naphthalic acid imide dyestuffs of the following formula: ##STR1## wherein D is ##STR2## wherein R.sup.1 is C.sub.1 -C.sub.8 alkyl which may be substituted, R.sup.2 is hydrogen, halogen, lower alkyl, lower alkoxy or cyano, X is oxygen or sulfur, and m is 0 or 1; A is phenylene, alkylene, aralkylene or --C.sub.2 H.sub.4 OC.sub.2 H.sub.4 --; B is oxygen, sulfur or ##STR3## wherein R.sup.3 is hydrogen or lower alkyl; Y is a 6-membered nitrogen-containing heterocyclic ring having at least one active halogen atom; and n is 0 or 1.

Abstract: Substituted quinazolinones and pyridopyrimidines of structural formula I ##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: Compounds of formula I ##STR1## wherein A, X.sub.1, X.sub.2, X.sub.3, X.sub.4, Y, Z and R.sub.1 to R.sub.6 have the meanings given in the description, have valuable pharmaceutical properties and are effective especially against tumours. They are prepared in a manner known per se.

Abstract: Pyrimidine-4,6-dicarboxylic acid diamides, processes for the use thereof, and pharmaceuticals based on these compoundsThe invention relates to pyrimidine-4,6-dicarboxylic acid diamides of the formula I ##STR1## in which R.sup.1 and R.sup.2 have the meanings given. The compounds according to the invention inhibit proline hydroxylase and lysine hydroxylase and can be employed as fibrosuppressants and immunosuppressants.

Abstract: Substituted cyclohexanols and cyclohexylamines and derivatives thereof are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as dopaminergic, antipsychotic, and antihypertensive agents as well as for treating hyperprolactinaemia-related conditions and central nervous system disorders.

Abstract: Novel aminomethyloxooxazolidinyl arylbenzene derivatives, wherein the aryl includes the phenyl, substituted phenyl, pyridyl, and substituted pyridyl groups, such as (l)-N-{3-[4- (4'-pyridyl)phenyl]-2-oxooxazolidin-5-ylmethyl}acetamide, possess useful antibacterial activity.

Abstract: The invention relates to new piperazinylalkyl-3(2H)-pyridazinones of the formula ##STR1## in which the radicals R.sub.1 represents hydrogen, phenyl, benzyl, or (C.sub.1 -C.sub.6)-alkyl which is unsubstituted or substituted one or more times by hydroxyl, piperidine, morpholine or by a group NR.sub.4 R.sub.5 in which R.sub.4 and R.sub.5 can be identical or different and which represent hydrogen, methyl or ethyl,R.sub.2 and R.sub.3 represent hydrogen, halogen, (C.sub.1 -C.sub.6)-alkoxy or (C.sub.1 -C.sub.6)-alkyl, where at least one of the radicals R.sub.2 or R.sub.3 denotes hydrogen,R.sub.6 represents hydrogen, (C.sub.1 -C.sub.4)-alkyl, phenyl, benzyl or phenylethyl,B represents (C.sub.1 -C.sub.7)-alkylene which is unsubstituted or substituted one or more times by hydroxyl, (C.sub.1 -C.sub.4)-alkyl or by the group NR.sub.4 R.sub.5 and which can optionally be closed to form an alicyclic 4- to 7-membered ring,R.sub.8 and R.sub.9, which can be identical or different, represent hydrogen or (C.sub.1 -C.sub.

Abstract: The invention relates to new morpholines and morpholine-N-oxides of formula ##STR1## wherein the substituents are defined hereunder, which compounds have valuable pharmacological properties, namely an effect on the metabolism, preferably the effect of lowering blood sugar and reducing body fat, and the effect of lowering the atherogenic .beta.-lipoproteins VLDL and LDL, and a performance enhancing effect in animals.

Abstract: A novel pyridine compound of the formula ##STR1## wherein each symbol is as defined in the specification, or a salt thereof which exhibit inhibitory activity or prolylendopeptidase and a pharmaceutical use thereof are disclosed.

Abstract: A compound of the formula ##STR1## wherein Q is --CO-- or --CH.sub.2 --, R is hydroxyl, lower alkoxy, halogen, --NH-lower alkylene-OH, --NH-lower alkylene-arylthio, --NH-lower alkylene-halogen, ##STR2## is dilower alkylamino, cycloalkylamino, morpholino, ##STR3## in which R.sub.9 is hydrogen, lower alkyl or aryl, R.sub.10 is hydrogen, lower alkyl, hydroxy-lower alkyl, hydroxy-lower alkoxy-lower alkyl or di(aryl)-lower alkyl, m is an integer from 4 to 6, n is 2 or 3, R.sub.1 is alkyl or aryl-lower alkyl, R.sub.2 and R.sub.3 are each lower alkyl, or together form tetramethylene, and R.sub.4 is hydrogen, lower alkyl or aryl, in which aryl is phenyl which is optionally substituted with a group selected from the group consisting of 1-3 halogen, nitro, lower alkyl and lower alkoxy, or a pharmaceutically acceptable salt thereof, inhibits blood platelet aggregation, has vasodilating activity and inhibits lipoperoxide generation.

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

Abstract: Novel substituted isonicotinic acid amides of the general formula ##STR1## in which X in ortho/ortho'-position are equal and represent fluorine, chlorine, bromine or iodine;Q.sub.1 is unsubstituted pyridimin-4-yl, or pyrimidin-4-yl substituted by R.sub.1, R.sub.2 and R.sub.3 ;Q.sub.2 is unsubstituted pyrimidin-2-yl, or pyrimidin-2-yl substituted by R.sub.1, R.sub.2 and R.sub.3 ;Q.sub.3 is unsubstituted pyrimidin-5-yl, or pyrimidin-5-yl substituted by R.sub.1, R.sub.2 and R.sub.3 ;Q.sub.4 is pyridin-2-yl, pyridin-3-yl or pyridin-4-yl each of which is unsubstituted or substituted by R.sub.1, R.sub.2 and R.sub.3 ;Q.sub.5 is pyridazin-3-yl or pyridazin-4-yl each of which is unsubstituted or substituted by R.sub.1, R.sub.2 and R.sub.3 ;Q.sub.6 is unsubstituted pyrazin-2-yl, or pyrazin-2-yl substituted by R.sub.1, R.sub.2 and R.sub.3 ;R.sub.1, R.sub.2, R.sub.3 are hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 haloalkyl having from 1 to 3 halogen atoms, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.

Abstract: Fungicidal substituted 3-amino-2-pyrazolin-5-ones of the formula ##STR1## in which R.sup.1 represents unsubstituted or substituted alkyl, unsubstituted or substituted alkenyl or alkinyl, or unsubstituted or substituted cycloalkyl or cycloalkenyl,R.sup.2 represents hydrogen, unsubstituted or substituted alkyl, unsubstituted or substituted alkenyl or alkinyl, unsubstituted or substituted cycloalky or cycloalkenyl, unsubstituted or substituted aryl or unsubstituted or substituted heterocyclyl, or represents one of the radicals --CX--YR.sup.3, --CXNR.sup.4 R.sup.5, ##STR2## --SO.sub.2 NR.sup.4 R.sup.5 or --SO.sub.2 R.sup.7, R.sup.3 represents unsubstituted or substituted alkyl or unsubstituted or substituted alkenyl or alkinyl,R.sup.4 and R.sup.

Abstract: A propane derivative represented by the following formula ##STR1## wherein R represents a lower alkyl group; one of A and B represents a group of the formula ##STR2## and the other represents a group of the formula ##STR3## in which R.sup.1 and R.sup.2 are identical or different and each represents a hydrogen atom, a lower alkyl group, an aryl group or an aralkyl group, R.sup.3 represents a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted aryl group or a substituted or unsubstituted heterocyclic group, and X represents a sulfonyl group or a carbonyl group,and an acid addition salt thereof. The compounds provided by this invention have useful biological activities such as the spasmolytic activity on the vascular smooth muscles and anti-platelet aggregatory activity and are useful as drugs for treating cardiovascular diseases such as angina pectoris, cerebral circulation disorder and thrombosis.

Abstract: Novel compounds having the formula: ##STR1## wherein ##STR2## represents a nitrogen-containing aromatic 6-membered ring; R.sup.1 represents a higher alkyl group which may be substituted; R.sup.2 represents a tertiary amino group or a quaternary ammonium group; and m represents 2 or 3; and salts thereof have superior antitumor activities including differentiation-inducing activity, and are useful as antitumor agents.

Abstract: Compounds of formula (I): ##STR1## (wherein n is 0, 1 or 2 and R.sup.1, R.sup.2, R.sup.4, R.sup.5, R.sup.6, X, Y and Z are a variety of groups and atoms) have the ability to inhibit the synthesis of thromboxane A.sub.2 and hence are useful in the treatment or prophylaxis of thrombotic conditions.

Abstract: The present invention provides indole derivatives of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl, alkenyl, cycloalkyl, cycloalkenyl, carboxyl, cyano, alkylcarbonyl, alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl or aryl radical, R.sub.2 is a hydrogen atom or an alkyl, trihalogenomethyl, hydroxyl, cycloalkyl, cyano, carboxyl, alkoxycarbonyl, alkylcarbonyl, aminocarbonyl, alkylaminocarbonyl or dialkylaminocarbonyl radical; R.sub.2 is a heterocyclic five-membered ring containing 1 to 4 heteroatoms or a heterocyclic six-membered ring containing 1 to 5 heteroatoms, the heteroatoms of the five- and six-membered rings being the same or different and being nitrogen, oxygen or sulphur and one or more of the nitrogen atoms optionally carrying an oxygen atom, the said five- and six-membered rings optionally being substituted by one or more alkyl, alkoxy, alkylthio, oxo, hydroxyl, nitro, amino, halogen or cyano groups; or R.sub.

Abstract: 2-Arylmethyliminopyrazines of the formula I ##STR1## in which R.sub.1 is SR.sub.2 ; OR.sub.2 ; O--CHR.sub.10 R.sub.2 ; N(R.sub.3)(CHR.sub.10 R.sub.4); N(R.sub.11)(CHR.sub.10 R.sub.4) or NR.sub.3 R.sub.4 ; R.sub.2 is C.sub.1 -C.sub.10 - alkyl which is unsubstituted or substituted by hydroxyl, mercapto, C.sub.1 -C.sub.4 -alkoxycarbonyl, mercaptoalkoxy, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylcarbonyl, mono- or di-C.sub.1 -C.sub.4 -alkylamino, C.sub.1 -C.sub.4 -haloalkoxy, tri-(C.sub.1 -C.sub.4 -alkoxy)-silyl, cyano, nitro or phenyl; C.sub.1 -C.sub.4 -haloalkyl; C.sub.3 -C.sub.8 -alkenyl; (3-methyl-oxetan-3-yl)methyl; C.sub.3 -C.sub.8 -alkynyl; or a radical from the group comprising phenyl, benzyl, C.sub.3 -C.sub.7 -cycloalkyl, furanyl or furfuryl which is unsubstituted or mono-, di- or trisubstituted by identical or different substituents from the group comprising halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkylcarbonyl, nitro, C.sub.1 -C.sub.4 -alkoxy and C.sub.1 -C.sub.4 -haloalkyl; R.sub.

Abstract: 1-Substituted alkyl-1,2-dihydro-2-pyrazinone derivatives of the formula ##STR1## wherein A is lower alkyl; R.sub.1 is selected from the group consisting of alkyl, phenyl-lower alkyl, and substituted phenyl-lower alkyl; R.sub.2 and R.sub.3 are each lower alkyl, or together form tetramethylene and R is selected from the group consisting of hydroxyl, hologen, lower alkanoyloxy R.sub.4 -carbamoyloxy, arylthio, 1-methyltetrazole-5-yl-thio, 1-imidazole, morpholino, ##STR2## in which R.sub.4 is lower alkyl or aryl, R.sub.5 is lhydrogen, lower alkyl or aryl, R.sub.6 is hydrogen, lower alkyl, hydroxy-lower alkyl, aryl, aryl-lower alkanoyl, arylcarbonyl, arylsulfonyl or thienyl-lower alkanoyl, Ar is phenyl or phenyl substituted with C.sub.1-3 alkyl, halogen, nitro, or lower alkoxy, A, R.sub.1, R.sub.2 and R.sub.3 are as defined above, m is an integer from 4-6, and n is 2 or 3; and pharmaceutically acceptable salts thereof.

Abstract: Disclosed are novel bis-dioxopiperazine derivatives, process for their preparation, antitumor agents comprising them and compositions containing them.The bis-dioxopiperazine derivatives are represented by the following general formula (I): ##STR1## wherein R.sub.1 represents a hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms; R.sub.2 represents a hydrogen atom or a group of ##STR2## R.sub.3 and R.sub.4, which are respectively independent and are the same or different, represent respectively a lower alkyl group having 1 to 4 carbon atoms, a cycloalkyl group having 3 to 7 carbon atoms or a heterocyclic radical selected from the group consisting of substituted or unsubstituted piperidino, substituted or unsubstituted piperazino, substituted or unsubstituted morpholino and substituted or unsubstituted thiomorpholino, or R.sub.3 and R.sub.

Abstract: This invention concerns tetrahydropyridoindoles of the formula: ##STR1## wherein Q represents ##STR2## in which R.sub.3 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, or --COO(C.sub.1-2) alkyl, and n is an integer from 1 to 7; R.sub.1 is hydrogen, halogen, hydroxy, or C.sub.1-3 alkyl; and R.sub.2 is hydrogen, C.sub.1-4 alkyl or --(CH.sub.2).sub.m --A where A is --N(CH.sub.3).sub.2,--N(C.sub.2 H.sub.5).sub.2, ##STR3## in which Ar is 2-pyrimidinyl, 2-pyrazinyl, phenyl, or phenyl substituted by a methyl, ethyl, methoxy, ethoxy, or trifluoromethyl group; and m is an integer from 1-4, or physiologically acceptable salts thereof, providing however that when n is 1, Q may not be quinolinyl. These compounds exhibit antihypertensive properties. Four of the disclosed compounds also exhibit antipsychotic properties.Also disclosed are compounds of Formula XX in which Q of Formula I is replaced by Q.sub.1, wherein Q.sub.1 is 2- or 3-pyridinyl, and R.sub.2 of Formula I is restricted to hydrogen.

Abstract: This invention relates to a novel 4-oxo-1,4-dihydronicotinic acid derivative ##STR1## or a salt thereof, wherein R.sup.1 is hydrogen or carboxyl-protecting group;R.sup.2 is substituted phenyl and naphthyl, or a substituted or unsubstituted heterocyclic group; andR.sup.3 is haloalkyl, aminoalkyl, or substituted or unsubstituted alkenyl, phenylalkenyl, naphthylalkenyl, phenylalkyl, naphthylalkyl, phenylalkynyl, naphthylalkynyl, heterocyclic alkyl, heterocyclic alkenyl, phenyl, naphthyl, cycloalkyl, cycloalkenyl, carboxylic acyl, iminoalkyl, heterocyclic or bridged hydrocarbon, which has a broad antibacterial spectrum and a low toxicity, and are useful for treatment of diseases of human beings and animals, to a process for producing the same and to an antibacterial agent containing the same.

Abstract: Cardiovascular activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sub.1 is alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3 or halo substituted alkyl;R.sub.2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, --(CH.sub.2).sub.n --Y.sub.1, or halo substituted alkyl;R.sub.3 is hydrogen, alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3, or halo substituted alkyl;R.sub.4 is aryl or heterocyclo;R.sub.5 is hydrogen, alkyl, aryl, arylalkyl, cyano, nitro, ##STR2## Y.sub.1 is cycloalkyl, aryl, heterocyclo, hydroxyl, alkoxy, aryl-(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl-(CH.sub.2).sub.m --S--, amino, substituted amino, carbamoyl, ##STR3## Y.sub.2 is cycloalkyl, aryl, heterocyclo, carbamoyl, ##STR4## amino, or substituted amino; m is 0 or an integer of 1 to 6;n is an integer of 1 to 6; andp is an integer of 2 to 6.

Abstract: Cardiovascular activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein X is oxygen or sulfur;R.sub.1 is alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.1, or halo substituted alkyl;R.sub.2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, --(CH.sub.2).sub.n --Y.sub.1, or halo substituted alkyl;R.sub.3 is hydrogen, alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3, or halo substituted alkyl;R.sub.4 is aryl or heterocyclo;Y.sub.1 is cycloalkyl, aryl, heterocyclo, hydroxyl, alkoxy, aryl--(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl--(CH.sub.2).sub.m --S--, amino, substituted amino, carbamoyl, ##STR2## Y.sub.2 is cycloalkyl, aryl, heterocyclo, carbamoyl, ##STR3## Y.sub.3 is hydroxyl, alkoxy, aryl--(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl--(CH.sub.2).sub.

Abstract: A guanidine derivative of the formula I: ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, ring X and D are a variety of radicals defined in the specification and A is a 3-8C alkylene chain which is substituted by a hydroxy radical and into which is optionally inserted, as part of the backbone of the chain, one or two groups selected from oxygen and sulphur atoms and NH and 1-6C N-alkyl radicals; and the pharmaceutically-acceptable acid additions salts thereof. Pharmaceutical compositions and methods of manufacture are also described. The compound of the formula I is a histamine H-2 antagonist and is therefore useful in ulcer therapy.

Abstract: This invention relates to substituted 4-pyrimidinones which are useful as intermediates in preparing H.sub.2 -antagonists.

Abstract: Compounds of the formula I ##STR1## in which n represents 1, 2 or 3, Ar represents a carbocyclic or heterocyclic aryl radical, Ac represents the acyl radical of an acid, Z represents a radical --OR.sub.7 or --NR.sub.8 R.sub.9, R.sub.1 represents hydrogen, unsubstituted or substituted lower alkyl, a carbocyclic or heterocyclic aryl radical or free, etherified or esterified hydroxy, R.sub.2 and R.sub.3, independently of one another, each represents hydrogen, unsubstituted or substituted lower alkyl, formyl or functionally modified formyl, carboxy or functionally modified carboxy, a carbocyclic or heterocyclic aryl radical or unsubstituted or mono- or di-substituted amino, R.sub.4 represents hydrogen or lower alkyl, R.sub.5 and R.sub.6, independently of one another, each represents hydrogen, unsubstituted or substituted lower alkyl or a carbocyclic or heterocyclic aryl radical, R.sub.7, R.sub.8 and R.sub.

Abstract: The compound of the formula ##STR1## wherein X is a cyclic group which may optionally be substituted; Y is a carboxyl group which may optionally be esterified or amidated; Z is --CH.dbd.CH--CH.dbd.CH--, --S--(CH.sub.2).sub.l --S--(l is an integer of 1 to 3), --N.dbd.CH--CH.dbd.N-- or --(CH.sub.2).sub.m --(m is an integer of 3 to 5); ring A may optionally be substituted with halogen, nitro, amino, alkanoylamino, alkoxycarbonyl, carboxyl or carbamoyl; and n is an integer of 1 to 3, and salts thereof. The compounds display a strong antianxiety effect to mammalian animals and are useful for the prevention or treatment of a disease such as psychosomatic disease and anxiety neurosis.

Abstract: This invention relates to 5-(phenyl)-2(1H)-pyrazinones substituted in the 4-position of the phenyl ring by an amino or acylamino group. These compounds have inotropic activity. One specific compound is 5-(4-acetamidophenyl)-2(1H)-pyrazinone.

Abstract: This invention relates to certain amino-5,6-diarylpyrazines useful as activators of GABA and benzodiazepine binding.

Abstract: A process for the preparation of a pyrazine derivative of the formula ##STR1## wherein R.sub.1 represents hydroxy, C.sub.1 -C.sub.6 alkoxy, or a group of the formula NR.sub.2 R.sub.3 in which R.sub.2 and R.sub.3 are independently a hydrogen atom or C.sub.1 -C.sub.6 alkyl or, together with the nitrogen atom to which they are linked, form a saturated ring having five or six atoms which may contain one or more additional heteroatoms; which process comprises reacting a compound of the formula: ##STR2## wherein R represents a hydrogen atom, C.sub.1 -C.sub.6 alkyl, or C.sub.1 -C.sub.6 alkoxy, Y represents a hydrogen atom or a sodium, lithium, or potassium ion, and A is a nitrile group or a substituent of the formula COR.sub.1 where R.sub.1 is as defined above either with pyruvic aldehyde oxime of the formula: ##STR3## or with a pyruvic aldehyde oxime acetal derivative of the formula: ##STR4## wherein R.sub.4 and R.sub.5 are independently a hydrogen atom or C.sub.1 -C.sub.

Abstract: The invention relates to amide derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion. According to the invention there is provided a guanidine derivative of the formula I: ##STR1## in which R.sup.1 is a hydrogen or 1-10C alkyl, 3-8C cycloalkyl, 4-14C cycloalkylalkyl, 3-6C alkenyl, 3-6C alkynyl, 1-6C alkanoyl, 6-10C aryl, 7-11C aralkyl or 7-11C aroyl, the aryl, aralkyl and aroyl radical being optionally substituted; ring X is a heterocyclic ring as defined in the specification; A is phenylene or 5-7C cycloalkylene, or a 1-8C alkylene into which is optionally inserted one or two groups; D is O or S; and R.sup.2 and R.sup.3 are hydrogen or a variety of radicals described in the specification: and the pharmaceutically-acceptable acid-addition salts thereof. Manufacturing processes and pharmaceutical compositions are also described.

Abstract: Novel imidazoquinoxalines of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydroxy, alkoxy of 1 to 5 carbon atoms and cyclohexylcarbonyloxymethoxy, R.sub.2 is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms, alkoxycarbonylvinyl of 4 to 7 carbon atoms, --COR, --CONH(CH.sub.2).sub.n --X and --A--(CH.sub.2).sub.m --Y, R is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, alkenyl of 2 to 4 carbon atoms, alkoxy of 1 to 5 carbon atoms, alkoxycarbonyl of 2 to 5 carbon atoms, amino, --CF.sub.3, --CHCl.sub.2 --, phenyl, aralkyl of 7 to 10 carbon atoms, aralkoxy of 7 to 10 carbon atoms, n is 0 and X is phenyl or n is an integer from 1 to 5 and X is selected from the group consisting of ##STR2## R.sub.3 and R.sub.

Abstract: Novel 2,3-dicyanopyrazine derivatives of the formula ##STR1## wherein A represents a hydrogen atom, a lower alkyl group, an unsubstituted or substituted phenyl group, a benzyl group, or a group of the formula --ZR.sub.1 in which Z represents an oxygen or sulfur atom and R.sub.1 represents an unsubstituted or substituted lower alkyl group, a lower alkenyl group, a lower alkynyl group, an unsubstituted or substituted phenyl group, or an unsubstituted or substituted benzyl group; and B represents a halogen atom, an alkyl group containing at least 3 carbon atoms, a phenyl group having a substituent at the ortho- and/or meta-position of the benzene ring, a group of the formula ZR.sub.1 in which Z and R.sub.1 are as defined, or a group of the formula ##STR2## in which R.sub.2 and R.sub.

Abstract: Antimicrobial compounds of the formula: ##STR1## wherein: Hal is bromine or chlorine; andR is halo; mono- or di-substituted mono- or diloweralkylamino wherein the loweralkyl substituents are hydroxy or loweralkanoyloxy; 4-morpholino; thiocyano; mercapto; straight or branched chain C.sub.1-8 alkylthio; mono- or di-substituted loweralkylthio wherein the substituents are hydroxy, amino, loweralkanoylamino, or loweralkoxycarbonyl; arylthio; loweralkylsulfoxy; or loweralkylsulfonyl;R.sup.1 is hydrogen; or loweralkyl;R.sup.2 is (CH.sub.2).sub.n COOR.sup.3, where R.sup.3 is hydrogen, loweralkyl, or benzyl; and n is 1 to 3; andR.sup.1 and R.sup.2 are taken together with an oxygen or nitrogen atom to form morpholino, piperazinyl, or piperazinyl which is N-loweralkyl substituted; are useful in various agricultural and industrial areas.

Abstract: Antimicrobial compounds of the formula: ##STR1## wherein: Hal is bromine or chlorine; andR is halo; mono- or di-substituted mono- or diloweralkylamino wherein the loweralkyl substituents are hydroxy or loweralkanoyloxy; 4-morpholino; thiocyano; mercapto; straight or branched chain C.sub.1-8 alkylthio; mono- or di-substituted loweralkylthio wherein the substituents are hydroxy, amino, loweralkanoylamino, or loweralkoxycarbonyl; arylthio; loweralkylsulfoxy; or loweralkylsulfonyl;R.sup.1 is hydrogen; or loweralkyl;R.sup.2 is (CH.sub.2).sub.n COOR.sup.a, where R.sup.a is hydrogen, loweralkyl, or benzyl; and n is 1 to 3;R.sup.1 andR.sup.2 are taken together with an oxygen or nitrogen atom or form morpholino, piperazinyl, or piperazinyl which is N-loweralkyl substituted;R.sup.3 is hydrogen; straight or branched C.sub.1-8 alkyl; aryl; aryl substituted with up to two members selected from the group consisting of C.sub.1-3 alkyl, C.sub.1-3 alkoxy, halo, and mono- or di-C.sub.

Abstract: Antimicrobial compounds of the formula: ##STR1## wherein: Hal is bromine or chlorine; andR is halo; mono- or di-substituted mono- or diloweralkylamino wherein the loweralkyl substituents are hydroxy or loweralkanoyloxy; 4-morpholino; thiocyano; mercapto; straight or branched chain C.sub.1-8 alkylthio; mono- or di-substituted loweralkylthio wherein the substituents are hydroxy, amino, loweralkanoylamino, or loweralkoxycarbonyl; arylthio; loweralkylsulfoxy; or loweralkylsulfonyl;R.sup.1 is hydrogen; or loweralkyl;R.sup.2 is hydroxyloweralkyl; (CH.sub.2).sub.n COOR.sup.a, where R.sup.a is hydrogen, loweralkyl, or benzyl; and n is 1 to 3;R.sup.1 and R.sup.2 are taken together with an oxygen or nitrogen atom to form morpholino, piperazinyl, or piperazinyl which is N-loweralkyl substituted; andR.sup.3 is hydrogen; straight or branched C.sub.1-8 alkyl, provided that when R.sup.3 is hydrogen or C.sub.

Abstract: 2-Substituted amino derivatives of 6-amino-3-chloro-5-nitropyrazin-2-yl are prepared by converting 3-amino-5,6-dichloropyrazinecarboxylic acid to 5,6-dichloro-3-nitropyrazinamine and treating said compound with an amine to produce the corresponding 2-substituted amino compound.

Abstract: Novel 3-methoxy-2-oxoazetidine derivatives, which are shown by the following formula ##STR1## wherein R.sub.1 is amino, acylated amino or protected amino, are of value as intermediates for the synthesis of useful compounds represented by the formula ##STR2## wherein R.sub.1 has the same meaning as defined above, as drugs in the treatment of bacterial infections.