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: Alkanolamine derivatives of the formula ##STR1## wherein Ar is phenyl or napthyl which is unsubstituted or which bears one or two defined substituents, or Ar is certain defined heterocyclic or bicyclic aromatic systems;wherein R.sup.1 is halogen, cyano, trifluoromethyl or trifluoromethylthio;wherein either R.sup.2 and R.sup.3 each is hydrogen or alkyl, or R.sup.2 is hydrogen and R.sup.3 is cycloalkyl or cycloalkyl-alkyl, or R.sup.2 and R.sup.3 are joined to form, together with the adjacent nitrogen atom, a heterocyclic group;wherein either R.sup.4 is hydrogen and R.sup.5 is hydrogen or alkyl, or R.sup.4 is hydrogen and R.sup.5 and R.sup.6 are joined together to form alkylene, or R.sup.4, R.sup.5 and R.sup.6 are joined together to form alk-1-yl-.omega.-ylidene;wherein either R.sup.6 and R.sup.7 each is hydrogen or alkyl, or R.sup.6 is joined to R.sup.4 or to R.sup.4 and R.sup.5 as defined above and R.sup.7 is hydrogen or alkyl, or R.sup.6 and R.sup.7 are joined together to form alkylene, or one of R.sup.

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

Abstract: Antimicrobial compounds of the formula: ##STR1## wherein: Hal is bromine or chlorine;R is chloro, but only when R.sup.1 is other than hydrogen; 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; andR.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;are useful in various agricultural and industrial areas.

Abstract: Hydrolysis of nitrile to amide by use of a quaternary ammonium hydroxide at 60.degree. to 95.degree. C.

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; andR.sup.1 is C.sub.6-12 alkyl;are useful in various agricultural and industrial applications.

Abstract: Compounds are prepared which correspond to the formulae ##STR1## wherein R represents a nitrogen containing heterocyclic radical corresponding to one of the formulae ##STR2## each X independently represents chloro, fluoro, bromo, nitro, alkyl of 1 to 4 carbon atoms, amino, mono- or dialkylamino wherein each alkyl group independently contains from 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, alkylthio of 1 to 4 carbon atoms, alkylsulfinyl of 1 to 4 carbon atoms, alkylsulfonyl of 1 to 4 carbon atoms, cyano, trifluoromethyl, trichloromethyl, phenoxy or substituted phenoxy of the formula ##STR3## wherein each Z independently represents chloro, fluoro, bromo, nitro, cyano, alkoxy of 1 to 4 carbon atoms or alkylthio of 1 to 4 carbon atoms, with the proviso that when either n is 2 or 3, all X groups are sterically compatible with each other and all Z groups are sterically compatible with each other; Y represents oxygen or sulfur; each n can independently represent an integer of from 0 to 3, inclusive; R.sup.

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 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: 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: 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: 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: The invention relates to N-amino-3,4,5-trihydroxypiperidines, methods for their production, compositions containing said compounds. Also included are methods for the use of said compounds and compositions.

Abstract: The case involves novel heterocyclic substituted pyrazinoylguanidines and a process for preparing same. The heterocyclic pyrazinoylguanidines are eukalemic agents possessing diuretic and natriuretic properties.

Abstract: The case involves novel N-pyrazinecarbonyl-N'-alkoxycarbonyl and N',N"-bis(alkoxycarbonyl)guanidines and processes for preparing same. The compounds are excellent eukalemic agents possessing diuretic and natriuretic properties.

Abstract: N-amidino-3,5-diamino-6-substituted-2-pyrazinecarboxamides and a process for their synthesis.

Abstract: The case involves novel pyrazine-2-carbonyloxyguanidines and processes for preparing same. The pyrazine-2-carbonyloxyguanidines are eukalemic or antikaliuretic agents possessing diuretic and natriuretic properties.

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: The case involves novel N-pyrazinecarbonyl-N'-substituted-sulfamoylguanidine and processes for preparing same. The N-pyrazinecarbonyl-N'-substituted-sulfamoylguanidines are excellent eukalemic agents possessing diuretic and natriuretic properties.

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.