Abstract: Compounds of the formula ##STR1## R.sub.1 is hydrogen or alkyl of 1 to 4 carbon atoms; R.sub.2 is hydrogen, methyl, hydroxyl, alkoxy of 1 to 4 carbon atoms, di(alkyl of 1 to 2 carbon atoms)amino-(alkoxy of 1 to 4 carbon atoms) or NHCOCOOR.sub.1 ;R.sub.3 is hydrogen or NHCOCOOR.sub.1 ;A is ##STR2## R.sub.4 is hydrogen, methyl, alkoxy of 1 to 4 carbon atoms, hydroxyl, amino, alkanoyloxy of 1 to 2 carbon atoms, di(alkyl of 1 to 2 carbon atoms)-amino-(alkoxy of 1 to 4 carbon atoms) or acetamido; andR.sub.5 is hydrogen, amino, alkoxy of 1 to 4 carbon atoms, halogen or NHCOCOOR.sub.1 ;and, when R.sub.1 is hydrogen, nontoxic, pharmaceutically acceptable salts thereof. The compounds as well as their salts are useful for the treatment of immunological, inflammatory and allergic disorders such as asthma, rhinitis, conjunctivitis, hay fever, urticaria, food allergies and the like.

Abstract: Compounds useful for inhibiting gastric acid secretion and for the treatment of peptic ulcers caused or exacerbated by gastric acidity having the following formula (I): ##STR1## in which R.sup.1 and R.sup.2, are H, C.sub.1-10 alkyl, C.sub.3-8 cycloalkyl or cycloalkylalkyl in which the alkyl part is C.sub.1-6 and the cycloalkyl part is C.sub.3-8, each of the alkyl, cycloalkyl and cycloalkylalkyls being optionally substituted by one or more halogens selected from F, Cl and Br, provided that at least one of R.sup.1 and R.sup.2 is a halogen substituted alkyl, cycloalkyl or cycloalkylalkyl and provided that there is no halogen substituent on the carbon directly attached to the nitrogen; and X, m, Y, n and R.sup.3 are as described in the specification; and the pharmaceutically-acceptable acid-addition salts thereof.

Abstract: N-Pyrazinyl-haloacetamide having insecticidal, herbicidal, or fungicidal activity. The compound has the general formula: ##STR1## wherein R is hydrogen, hydrocarbyl, halogen, epoxy, hydroxy, alkoxy, mercapto, alkylthio, nitro, cyano or amino; R' is hydrogen or hydrocarbyl; X is halogen; m is an integer from 1 to 4; and n is 0, 1 or 2. The compound may also be a tautomer or acid addition salt of this formula.

Abstract: Nitrogen-containing heterocyclic compounds of the formula IR.sup.I --(A--Z).sub.n --A--R.sup.2 Iwherein R.sup.1 and R.sup.2 in each case independently of one another are alkyl group with 1-15 C atoms, wherein one or two non-adjacent CH.sub.2 groups can also be replaced by 0 atoms and/or --CO-- group and/or --O--CO-- groups and/or --CO--O-- groups, and one of the radicals R.sup.1 and R.sup.2 can also be H, CN, F, Cl or Br, the groups A in each case independently of one another are a 1,4-phenylene group, wherein one or two CH groups can also be replaced by N atoms, a 1,4-cyclohexylene group, wherein one or two CH.sub.2 groups which are not adjacent can be replaced by 0 atoms, a 1,3-dithiane-2,5-diyl group, a 1,4-bicyclo(2,2,2)-octylene group, a decahydronapthalene-2,6-diyl group or a 1,2,3,4-tetrahydronaphthalene-2,6-diyl group, the group Z in each case independently of one another are --CO--O--, --O--CO--, --CH.sub.2 CH.sub.2 --, --OCH.sub.2 --, --CH.sub.

Abstract: 2,6-Disubstituted derivatives of 3-nitropyrazine are disclosed to have activity in increasing the sensitivity of tumor cells to radiation. Also disclosed are methods of preparing such compounds and pharmaceutical compositions including such compounds.

Abstract: Novel 2-aminopyrazines and processes for the preparation of 2-aminopyrazines and pyrazines by reaction of an .alpha.-iminodiacetonitrile (a) with a hydrogen halide or (b) with an alcohol or a thioalcohol and a hydrogen halide or (c) with an alcohol or a thioalcohol in the presence of an alkali metal compound and/of an alkaline earth metal compound. The 2-aminopyrazines and pyrazines obtainable by the process of the invention are useful starting materials for the preparation of dyes, fungicides, bactericides, textile assistants, scents, folic acid derivatives, flavorings, and active ingredients in crop protection and drugs.

Abstract: Heterocyclic acetylenes of the formula (I): ##STR1## wherein Y is alkyl, alkoxy, alkoxyalkyl, chloro, fluoro, bromo or carboxamidoalkyl and R.sup.1 is hydrogen, alkyl, alkoxy, alkylthio, alkoxycarbonyl, chloro, fluoro or dialkylamino, m is 0-2, R.sup.2 is branched alkyl and Het is an aromatic heterocycle. The acetylenes are useful in treating hypertension and/or angina.

Abstract: The invention relates to carbonyl derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion. According to the invention where is provided a guanidine derivative of the formula I: ##STR1## in which R.sup.1 and R.sup.2, same or different, are hydrogen or 1-10C alkyl, 3-8C cycloalkyl or 4-14C cycloalkylalkyl, each alkyl, cycloalkyl or cycloalkylalkyl optionally carrying one or more F, Cl or Br atoms, provided that one of R.sup.1 and R.sup.2 is halogen substituted, or R.sup.2 is hydrogen and R.sup.1 is R.sup.5 -E-W in which W is 2-6C alkylene optionally substituted by 1 or 2 1-4C alkyls, E is O, S, SO, SO.sub.2 or NR.sup.6 in which R.sup.6 is H or 1-6C alkyl, R.sup.5 is H or 1-6C alkyl optionally substituted by 1 or 2 1-4C alkyls, or R.sup.5 and R.sup.6 are joined to form a pyrrolidine, piperidine, morpholine, piperazine or N-methylpiperazine ring, or R.sup.2 is H and R.sup.

Abstract: 2,6-Disubstituted derivatives of 3-nitropyrazine are disclosed to have activity in increasing the sensitivity of tumor cells to radiation. Also disclosed are methods of preparing such compounds and pharmaceutical compositions including such compounds.

Abstract: Compounds useful for inhibiting gastric acid secretion and for the treatment of peptic ulcers caused or exacerbated by gastric acidity having the following formula (I): ##STR1## in which R.sup.1 and R.sup.2, are H, C.sub.1-10 alkyl, C.sub.3-8 cycloalkyl or cycloalkylalkyl in which the alkyl part is C.sub.1-6 and the cycloalkyl part is C.sub.3-8, each of the alkyl, cycloalkyl and cycloalkylalkyls being optionally substituted by one or more halogens selected from F, Cl and Br, provided that at least one of R.sup.1 and R.sup.2 is a halogen substituted alkyl, cycloalkyl or cycloalkylalkyl and provided that there is no halogen substituent on the carbon directly attached to the nitrogen; and X, m, Y, n and R.sup.3 are as described in the specification; and the pharmaceutically-acceptable acid-addition salts thereof.

Abstract: Hyperuretic agents of the formula: ##STR1## wherein Y is O or NH;R is OH; NHCONR.sup.4 R.sup.5 ; or N.dbd.C(NR.sup.4 R.sup.5).sub.2 ;R.sup.1 and R.sup.2 are hydrogen, amino, or mono- or disubstituted amino, provided that R.sup.1 and R.sup.2 may not both be amino or substituted amino; andR.sup.3 is hydrogen or halo; enhance renal excretion of urea, thereby lowering plasma urea concentration, and are therefore useful for treating hypertension, eclampsia, uremia, and similar disorders.

Abstract: 4-Cyano-2-azetidinone derivatives represented by the formula ##STR1## wherein R.sup.1 is an amino group which may be acylated or protected, X is a hydrogen atom or a methoxy group and W is a hydrogen atom or a sulfo group, and methods of producing the same, for example, as represented by ##STR2## wherein R.sup.2 is an acylated or protected amino group, Y is a halogen atom or a group having the formula --OCOR.sup.3, --SCOR.sup.3 or --S(O).sub.n --R.sup.3 (R.sup.3 being a hydrocarbyl group and n an integer 1 or 2), R.sup.4 is an amino group which may be acylated or protected and X is as defined above. Compounds [I] are useful as advantageous intermediates for the synthesis of optically active 4-substituted-2-azetidinone derivatives, and, when W=SO.sub.3 H, [I] are also useful as antimicrobial agents and as beta-lactamase inhibitors.

Abstract: Disclosed are compounds of the general formula: ##STR1## wherein R.sub.1 is amino, an acylated amino or a protected amino group, X is hydrogen or methoxy, and R' is hydrogen, R or R.sup.4 wherein R is an organic residue attached to the azetidine ring through a carbon atom therein and R.sub.4 is azido, a halogen, an amino group which may optionally be acylated or a group of the formula --OR.sub.5, ##STR2## or --S--S--R.sub.5 wherein R.sub.5 is an organic residue and n is 0, 1 or 2, and pharmaceutically acceptable salts and esters thereof.The compounds have antimicrobial and/or .beta.-lactamase-inhibitory activity and are of value as drugs for human beings and domesticated animals.

Abstract: Antimicrobial compounds of the formula: ##STR1## wherein: Hal is bromine or chlorine; andR is 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; are useful in various agricultural and industrial areas.

Abstract: Antimicrobial compounds of the formula: ##STR1## wherein: Hal is bromine or chlorine;R 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; 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.1-3 alkyl substituted amino; heteroaryl; formyl C.sub.2-4 alkenyl; or C.sub.2-4 alkenyl; andR.sup.2 is straight or branched C.sub.

Abstract: The instant invention is directed to a pyrazine compound represented by the formula ##STR1## wherein Z is --NH--, --NHSO.sub.2 --, --NHCO-- or --S--,Ar is a phenyl ring substituted by 1 or 2 substituents selected from the group consisting of halo, lower alkyl, lower alkoxy or nitro, andn is 0 or 1.

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 (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: 8-Halo-6-nitro-1,2,4-triazolo[4,3-a]pyrazine and its corresponding 3-alkyl derivatives are prepared by converting amino-5,6-dichloropyrazinecarboxylic acid to 5-chloro-6-hydrazino-3-nitropyrazinamine and treating said hydrazino compound with a lower alkyl ortho ester of a loweraliphatic carboxylic acid to produce an 8-chloro-6-nitro-1,2,4-triazolo[4,3-a]pyrazine-5-amine or the corresponding 3-loweralkyl derivatives thereof.

Abstract: The present invention relates to aminoalkenoate ester derivatives of 2-amino-5-chloro-3-nitropyrazine useful as sensitizers of hypoxic tumor cells to therapeutic radiation. It also relates to the process of preparing such compounds by reaction of 2-amino-5,6-dichloro-3-nitro-pyrazine with an amino or alkylamino substituted .alpha.,.beta.-unsaturated alkenoate ester. In addition the application relates to pharmaceutical compositions containing such compounds and to methods of treatment comprising administering such compounds to patients undergoing radiation treatment to enhance the effectiveness of such treatment by sensitizing hypoxic tumor cells to therapeutic radiation.

Abstract: Disclosed and exemplified are insecticidal and acaricidal optionally substituted furylbenzyl, thienylbenzyl, pyrazinylbenzyl, or pyridinzylbenzyl esters of the pyrethroid acids, novel pyrethroid alcohols and other intermediates, and compositions, a method of use and a process for preparation of the esters.

Abstract: Di(alkylamino) derivatives of chloronitropyrazines are prepared from dichloronitropyrazinamine by diazotization of the amine followed by halogen exchange to produce an intermediate dichloro-halo nitropyrazine followed by reaction with one or two moles of an alkyl amine to effect replacement of one or two of the pyrazine halogens.

Abstract: N-Acyl derivatives of 6-(alkylamino)-5-chloro-3-nitro-pyrazinamines are disclosed to have activity in increasing the sensitivity of tumor cells to radiation. Also disclosed are methods of preparing such compounds and pharmaceutical compositions including such compounds.

Abstract: Novel alkanolamine derivatives of the formula: ##STR1## wherein Ar is phenyl or naphthyl which is unsubstituted or which bears one or two substituents selected from halogen, trifluoromethyl, hydroxy, amino, nitro, carbamoyl, carbamoylmethyl and cyano, and alkyl, alkenyl, alkoxy, alkenyloxy, alkylthio, alkanoyl and alkanoylamino each of up to 6 carbon atoms, or Ar is 4-indolyl, 4-benzo[b]thienyl, 5-benzo[1,4]dioxanyl, 4- or 5-indanyl, 5- or 6- 1,2,3,4-tetrahydronaphthyl), 2,3-dihydroxy-1,2,3,4-tetrahydronaphth-5-yl or 4- morpholino-1,2,5-thiadiazol-3-yl;wherein R is halogen;wherein A.sup.1 is alkylene of 2 to 6 carbon atoms; andwherein A.sup.2 is alkylene of 1 to 7 carbon atoms which in unsubstituted or bears a phenyl, hydroxy or carbamoyl substituent, or A.sup.2 is cycloalkylene of 3 to 6 carbon atoms;or acid-addition salts thereof.The compounds possess either .beta.-adrenergic blocking activity or diuretic activity or both such activities and may be used in the treatment of heart disease or hypertension.

Abstract: Oxime ether derivatives of the formula (I): ##STR1## wherein Het is a monocyclic heteroaromatic group containing two hetero atoms at least one of which is nitrogen, or a bicyclic heteroaromatic group containing one or two hetero atoms at least one of which is nitrogen, Ar is a phenyl or a 5- or 6-membered monocyclic heteroaromatic group, and R is an alkyl, alkenyl, alkynyl, cyanoalkyl, carbamidoalkyl or aminoalkyl group, or N-oxides thereof, have anti-ulcer activity in the gastro-intestinal tract of mammals.

Abstract: 2-(4-Aminopiperidino)pyrazines are useful as analgesic and antidepressant agents. They are prepared by reductive amination of the corresponding 2-(4-oxopiperidino)pyrazines.

Abstract: Novel 1-(mono-o-substituted benzoyl)-3-(substituted pyrazinyl) ureas, active as insecticides, and methods for their use as insecticides.

Abstract: The invention relates to novel piperidino-propanols, especially 1-(3-heterocyclyloxy-2-hydroxy-propanol)-4-(N-diazcyclyl)-piperidines of the formula ##STR1## in which R.sub.1 is a substituted or unsubstituted heteroaryl radical, R.sub.2 is hydrogen or a substituted or unsubstituted aliphatic, cycloaliphatic, cycloaliphatic-aliphatic or araliphatic hydrocarbon radical or an acyl radical and alk is lower alkylene which separates the two nitrogen atoms from one another by 2 or 3 carbon atoms, or is a substituted or unsubstituted 1,2-phenylene radical, and salts thereof, as well as processes for their preparation, and also to pharmaceutical preparations containing these compounds and the use thereof, preferably in the form of pharmaceutical preparations as antihypertensive agents, antitachycardiac agents and .alpha.-sympathicolytic agents.

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: The compounds are sulphoxides of heterocyclicthioalkylthioureas, ureas and guanidines which are useful to produce inhibition of histamine H-2 receptors.

Abstract: A series of 2-chloro-3-phenoxypyrazines and 2-chloro-6-phenoxypyrazines exhibiting antiviral activity are disclosed. Methods of using the disclosed compounds as antiviral agents are also described as well as pharmaceutically-acceptable compositions.

Abstract: Novel 1-(substituted benzoyl)-3-(substituted pyrazinyl)ureas, active as insecticides, and methods for their use as insecticides.

Abstract: Organic chemical compounds based upon the urea molecule are disclosed which have potent gastric secretion inhibitory properties. The urea is substituted with a 6 membered heterocyclic substituent containing 2 or 3 heteroatoms, and also with a substituted amino alkyl group. Further substitution is also possible. The compounds have profound effects on the inhibition of gastric secretions in the gastro-intestinal tract, and compositions for such uses are also disclosed.

Abstract: A treatment to alleviate the symptoms of psoriasis consisting of topical application of a cream, ointment or lotion containing, as the principal active ingredient, one or more 6-substituted nicotinamides and or 2-substituted pyrazinamides is disclosed. The therapeutic composition may include a single member of the above active ingredients present in a total amount of from 0.01 to 5 percent by weight of the total composition, or a plurality thereof present in a preferred concentration range of from 0.02 to 2 percent by weight of the total composition. Topical application of the therapeutic composition in a cream, ointment, or a water or alcohol solution has been found to achieve from substantial to complete remissions of psoriasis in humans.

Abstract: Benzoylureas are prepared from a benzamide, an alkyllithium, a phenyl chloroformate, and an amine. Two reaction sequences are described. The benzoylureas obtained by the process are useful as insecticides.

Abstract: Novel substituted pyrazine derivatives are disclosed having the general formula (I): ##STR1## where R.sub.1 and R.sub.2 may be methyl, methoxy, halogen (particularly chlorine, bromine or fluorine), or hydrogen, with the proviso that R.sub.1 and R.sub.2 cannot both be hydrogen, and X may be S or NH.These novel substituted pyrazine derivatives show a remarkable activity as inhibitors of platelet aggregation at very low dosages.

Abstract: Compounds are prepared which correspond to the formula ##STR1## wherein n represents an integer of 0 to 3; p represents an integer of 0 to 2 and the sum of n + p is an integer of 0 to 3; and r is 0 or 1. These compounds have been found to be active as pesticides and find particular usage as fungicides, bactericides, nematocides and herbicides.

Abstract: The present invention is concerned with the preparation of chemical intermediates, namely, beta-amino-acrylic acid ester derivatives of nitrogen heterocycles, i.e. pyridine, quinoline, quinoxaline, pyrazine, pyrimidine and the like. Said intermediates are cyclized to form pyrido-pyrimidine type final products possessing analgesic activity.