Abstract: Aqueous solutions of antibacterially active sulfonamides and sulfonamide potentiators, which are suitable for parenteral administration and which contain no organic solvent, are prepared by reacting a sulfonamide RH with an aldehyde R.sup.1 CHO to give a compound of the formula R.sup.1 CH(R).sub.2 and dissolving said compound in water together with the sulfonamide potentiator.

Abstract: The pyrimidine derivatives of formula I ##STR1## wherein R.sup.1 is naphthyl, substituted naphthyl or substituted phenyl; R.sup.2 is hydrogen or lower alkoxy; and A is an optionally present ethylene or 1,3-propylene, and wherein the diaminopyridine group has the exo-configuration when A is present,are described. These compounds are useful as antibacterial agents, antimalarial agents and antitumor agents, and can be used in combination with sulfonamides in the control of bacterial infections.

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: Compounds of the formula (II) ##STR1## or a salt, N-oxide or acyl derivative thereof, wherein Y is a group ##STR2## which is linked to the pyrimidinylmethyl moiety at the 1 or 7-position and is optionally substituted at the 2, 3, 4 or 6-position or at the 7-position when the linkage to the pyrimidinylmethyl moiety is at the 1-position wherein X is an oxygen or sulphur atom, a group CH.sub.2, a group S(O).sub.n where n=1 or 2, a group NR.sup.1 wherein R.sup.1 is hydrogen C.sub.1-4 alkyl or a group COR.sup.2 where R.sup.2 is hydrogen, C.sub.1-4 alkoxy or amino and the dotted line represents a single or double bond, have antimicrobial activity. Processes for making these compounds, pharmaceutical compositions containing them and the medical use of the compounds are also disclosed.

Abstract: Novel 2,4-diaminopyrimidines having substituted heterobicyclomethyl moieties in the 5-position have superior antibacterial properties.

Abstract: Antibacterial activity is exhibited by .beta.-lactams having a ##STR1## substituent in the 1-position and an acylamino substituent in the 3-position wherein Z is oxygen or sulfur, and R is alkyl, alkenyl, alkynyl, substituted alkyl, phenyl, substituted phenyl, a 5,6 or 7-membered heterocycle (R.sub.c), phenylalkyl, (substituted phenyl)alkyl, R.sub.c -alkyl or --NR.sub.a R.sub.b wherein R.sub.a and R.sub.b are the same or different and each is hydrogen, alkyl, substituted alkyl, phenyl, substituted phenyl, phenylalkyl, or (substituted phenyl)alkyl or one of R.sub.a and R.sub.b is hydrogen, alkyl, phenyl, substituted phenyl, phenylalkyl or (substituted phenyl)alkyl and the other is amino, alkanoylamino, arylcarbonylamino, alkoxycarbonylamino, alkylsulfonylamino, alkylamino, dialkylamino, phenylamino, (substituted phenyl)amino, hydroxy, cyano, alkoxy, phenyloxy, (substituted phenyl)oxy, phenylalkoxy, (substituted phenyl)alkoxy, R.sub.c, R.sub.c -alkyl, R.sub.

Abstract: Compounds of the formula (II) ##STR1## or a salt, N-oxide or acyl derivative thereof, wherein Y is a group ##STR2## which is optionaly substituted and which optionally contain a nitrogen atom at one of positions A, B, C, D or E, in which the dotted line represents aromatic rings unless one of the rings contains a nitrogen atom in which case this ring is either aromatic or partially saturated, have antimicrobial properties. Processes for making these compounds, pharmaceutical compositions containing them and the medical use of the compounds are also disclosed.

Abstract: A compound having the formula ##STR1## can be prepared by heating an anion having the formula ##STR2## with a cation having the formula ##STR3## or a cation having the formula ##STR4##

Abstract: Antibacterial activity is exhibited by 2-azetidinones having a 3-acylamino substituent and a 1-substituent of the formula ##STR1## (or a salt or ester thereof).

Abstract: 2,4-Diamino-5-(4-amino- and 4-loweralkylamino-3,5-disubstitutedbenzyl)pyrimidines are prepared by a novel method using 2,6-disubstituted anilines and pyrimidines. Several novel intermediates are involved.

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: The invention relates to 2-amino-8-cyclopropyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxyli c acid compounds, processes for their preparation and their use as antibacterial agents, and also as feed additives.

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: Compounds of formula (I), pharmaceutically acceptable salts, quaternary derivatives and N-oxides thereof, and pharmaceutically acceptable solvates of any of the foregoing: ##STR1## wherein p is 1 to 3;B is C.sub.1-7 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl-C.sub.1-2 alkyl, or a group (CH.sub.2).sub.t R.sub.11 where t is 1 or 2 and R.sub.11 is thienyl or furyl optionally substituted or is phenyl optionally substituted; and(i) A is a group of formula (II): ##STR2## in which either (a) one of X and Y is CO and the other is NH; or X is CO and Y is NR.sub.6 ; and or(b) one of X and Y is CO and the other is NH; or(ii) A is a group of formula (III): ##STR3## in which one of X and Y is CO and the other is NH, having useful pharmacological properties, pharmaceutical compositions containing them, a process and intermediates for their preparation, and the use of the compounds.

Abstract: 2,4-Diamino-5-benzylpyrimidines of the formula ##STR1## wherein R.sup.1, R.sup.2, A, Z and n are as hereinafter set forth, are described. The 2,4-diamino-5-benzylpyrimidines of the invention have useful antibacterial activity. More particularly, they inhibit bacterial dihydrofolate reductase and potentiate the antibacterial activity of sulfonamides.

Abstract: A process for preparing Tetroxoprim starting from 3,5-dimethoxy-4-methoxyethoxy-benzaldehyde and 2,4-diamino-6-hydroxy-pyrimidine, by successive hydrogenation, halogenation and hydrogenolysis of the 2,4-diamino-6-oxo-5-(3,5-dimethoxy-4-methoxyethoxy-benzylidene)-pyrimidine obtained in the initial reaction.

Abstract: Novel 2,4-diamino-5-(substituted naphthylmethyl)pyrimidines have been found to have superior antibacterial activity.

Abstract: N-(Heterocycliccarbamoyl)arylsulfonamides, such as N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-2-hydroxybenzenesulfonamide , methanesulfonate are useful for plant growth retardation, brush control and weed control in crops.

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.

Abstract: The present invention relates to novel soluble N.sub.2 substituted derivatives of 2,4-diamino 5-benzyl pyrimidines. These derivatives correspond to the general formula III below: ##STR1## The novel soluble N.sub.2 substituted derivatives are powerful antibacterial agents.

Abstract: The novel compounds of the formula I are useful selective herbicides for postemergence application in crops of cereals, maize and rice.In formula I, ##STR1## A is an unsubstituted or substituted amino group, Q is a C.sub.2 -C.sub.6 alkylene bridge, Y is an oxygen or sulfur atom or an unsubstituted or substituted nitrogen atom, and Z is an unsubstituted or substituted phenyl, naphthyl or heterocyclic radical, which phenyl radical, containing the bridge member Y, can additionally carry one to four further substituents.

Abstract: This invention relates to compounds having the formula ##STR1## wherein R represents hydrogen, alkyl containing one to four carbon atoms, or alkoxyalkyl, alkenyl or alkynyl containing two to four carbon atoms, R.sub.1 represents hydrogen or 1-oxoalkyl containing one to two carbon atoms and wherein X and Y are carbon or nitrogen with the proviso that one of X and Y must be nitrogen and the other carbon and which are useful diuretic agents.

Abstract: 4-Amino- and 2,4-diaminopyrimidines with a quaternized ring nitrogen and an oxygen bearing substituent such as hydroxyalkyl, alkoxyalkyl, or alkanoyl on one of the exo- or endocyclic nitrogens and a C.sub.6-18 alkyl on another, are highly active antimicrobial agents with a relatively low acute mammalian toxicity.

Abstract: 5-Benzyl-4-amino-pyrimidine-2-amidines which may or may not be substituted in the phenyl ring, and their physiologically acceptable addition salts with acids, processes for their preparation, drugs containing these compounds, and their use in infectious diseases.

Abstract: Compounds of the general formula (I) ##STR1## wherein R.sup.1 and R.sup.2 are selected from a lower alkyl group, a phenyl group (optionally substituted by one or more hydroxy or lower alkoxy groups), a pyridyl group or a group --CO.sub.2 R where R is a lower alkyl group, (provided that when R.sup.1 is a group --CO.sub.2 R, R.sup.2 is a lower alkyl group) are disclosed.The compounds of formula (I) are useful as intermediates to compounds of other ring systems which are of pharmacological interest.Certain of the compounds of formula (I) are also useful as antimicrobial agents.

Abstract: Unsubstituted or substituted 5-phenyl- and 5-benzyl-4-amino-pyrimidine-2-imidoacid esters, their preparation, drugs containing these compounds, and their use in infectious diseases.

Abstract: What is disclosed are 4-amino-2-ureido (or -thioureido)-pyrimidine-5-carboxylic acid anilides of the formula ##STR1## further defined in the specification, and physiologically acceptable acid addition salts thereof, methods for treating adiposity and disturbances of the lipometabolism with these compounds or salts, and pharmaceutical compositions containing these compounds or salts and useful for inducing anorexia or affecting the lipometabolism.

Abstract: 5-Benzyl-2,4-diaminopyrimidines, in which the 2-amino group is substituted, and which may or may not be substituted in the phenyl ring, and their physiologically acceptable addition salts with acids, processes for their manufacture, drugs containing these compounds, and the use of the said compounds in infectious diseases.

Abstract: A group of aryl-Z-alkoxy-5-benzylpyrimidines wherein Z is oxy, thio, imino, carbonyl, carbamoyl, sulfonyl, sulfinyl or sulfamoyl has been prepared from 2,4-diamino-5-benzylpyrimidine via alkylation with either an aryl-Z-alkyl halide or a substituted glycidyl ether. These compounds are potent dihydrofolate reductase (DHFR) inhibitors which are useful as antibacterial, anti-protozoal and antitumor agents.

Abstract: A process for preparing a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are lower alkoxy or taken together are methylenedioxy; R.sub.3 is lower alkyl or hydrogen, which comprises the step of reacting an aromatic compound of the formula ##STR2## wherein R.sub.1, R.sub.2 and R.sub.3 are as previously described, with a diamino-pyrimidine of the formula ##STR3## wherein R.sub.4 is lower alkoxy, benzyloxy, hydroxy or halogen, in the presence of an inorganic or organic acid selected from the group consisting of ortho-phosphoric acid, poly-phosphoric acid, hydrohalic acids and tri-haloacetic acids, at a temperature in the range of from about 50.degree. C. to about 110.degree. C., is described.

Abstract: Compounds of the general formula (I) ##STR1## wherein R.sup.1 and R.sup.2 are selected from a lower alkyl group, a phenyl group (optionally substituted by one or more hydroxy or lower alkoxy groups), a pyridyl group or a group --CO.sub.2 R where R is a lower alkyl group, (provided that when R.sup.1 is a group --CO.sub.2 R, R.sup.2 is a lower alkyl group) are disclosed.The compounds of formula (I) are useful as intermediates to compounds of other ring systems which are of pharmacological interest.Certain of the compounds of formula (I) are also useful as antimicrobial agents.

Abstract: The novel derivatives correspond to the general formula II: ##STR1## in which: R.sub.1 R.sub.2 R.sub.3 and R.sub.4 represent identical or different groups which can each be a hydrogen or halogen atom or an alkyl group, alkoxy, or benzyloxy group and R is the residue of an R--CHO aldehyde selected from among linear or branched saturated aliphatic aldehydes including 1 to 4 carbon atoms or again represents the Z--CH.dbd.CH radical in which Z represents a hydrogen atom, a linear or branched saturated alkyl group, an aromatic nucleus or an aromatic heterocyclic nucleus or again R represents the radical HO CH.sub.2 (CH OH)n--in which n has the value of 3 or 4. The novel compounds have high solubility in water and antibacterial activity and potentiating power.

Abstract: Benzyl cyanoacetals of formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are the same or different and each is a halogen or a hydrogen atom, an alkoxy group, an alkyl group, or a dialkylamino group; R.sup.4 is an alkoxycarbonyl group, or an aldehyde group; and R.sup.5 is an alkyl group; the alkyl or alkoxy groups each having from 1 to 4 carbon atoms, and their use as intermediates in the preparation of antibacterial 2,4-diamino-5-benzylpyrimidines. They are prepared from a reaction between an orthoester and an .alpha.-substituted-.beta.-benzylpropionitrile and then the resulting cyanoacetal is converted to the benzylpyrimidine by reaction with guanidine.

Abstract: Benzylpyrimidines of the formula ##STR1## wherein R.sup.1 and R.sup.2, independently, are C.sub.1-6 -alkyl, R.sup.3 isC.sub.1-3 -alkyl and R.sup.4 is methylene or C.sub.2-4 -alkylideneand physiologically compatible acid addition salts thereof, are described. The compounds of formula I are useful as antibacterial agents and as potentiators of sulfonamides.

Abstract: Benzylpyrimidines of the formula ##STR1## wherein R.sup.1 and R.sup.2, independently, are C.sub.1-3 -alkyl, and R.sup.3 and R.sup.4, independently, are hydrogen or methyl,and physiologically acceptable acid addition salts thereof, are described. The compounds of formula I are useful as antibacterial agents and as potentiators of sulfonamides.

Abstract: 2-Acylamino-4-amino-5-benzylpyrimidines substituted in the phenyl ring of the benzyl radical, their production and their use as sulfonamide potentiators, as well as agents containing the same, are disclosed. The compounds 4-amino-2-formamido-5-(3,4,5-trimethoxybenzyl)-pyrimidine and 4-amino-2-acetamido-5-(3,4,5-trimethoxybenzyl)-pyrimidine are examples of the subject pyrimidines.

Abstract: A compound selected from a 2,4-diamino-5-thiobenzylpyrimidine of the formula: ##STR1## in which R is selected from hydrogen, alkyl, lower alkoxy, and halogen and R' is alkyl; and pharmacologically acceptable acid addition salts thereof. These compounds have an anti-bacterial action and are sulphonamide potentiators.

Abstract: Benzaldehydes are reacted with cyanoacetaldehyde, for which reaction the cyanoacetaldehyde can be produced from isoxazole in a basic medium. The reaction gives .alpha.-cyanocinnamaldehydes, the hydrogenation of which gives the corresponding dihydrocinnamyl compounds, which can be converted to 2,4-diaminopyrimidines by reaction with guanidine, using various methods.

Abstract: A process for preparing a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are lower alkoxy or taken together are METHYLENEDIOXY; R.sub.3 is lower alkyl or hydrogen, which comprises the step of reacting an aromatic compound of the formula ##STR2## wherein R.sub.1, R.sub.2 and R.sub.3 are as previously described, with a diamino-pyrimidine of the formula ##STR3## wherein R.sub.4 is lower alkoxy, benzyloxy, hydroxy or halogen, in the presence of an inorganic or organic acid selected from the group consisting of ortho-phosphoric acid, poly-phosphoric acid, hydrohalic acids and tri-haloacetic acids, at a temperature in the range of from about 50.degree. C. to about 110.degree. C., is described.

Abstract: A benzylpyrimidines of the formula ##STR1## wherein r.sup.1 and R.sup.2 independently are C.sub.1-3 -alkyl or C.sub.1-3 -alkoxy, and R is hydrogen or lower alkyl, is treated with hydroxylamine or a salt thereof in polyphosphoric acid or alternatively, when R is hydrogen, is treated with sodium azide in polyphosphoric acid, to yield the corresponding 4-amino benzylpyrimidine.

Abstract: A process for the production of 2,4-diamino-5-(3',4',5'-trimethoxybenzyl)-pyrimidine by condensing trimethoxy benzaldehyde with a substituted propionitrile compound and reacting the condensation product obtained with guanidine, wherein a .beta.-akyl-(aryl-, benzyl-)-oxy-ethyleneoxy-propionitrile corresponding to the formulaR--O--CH.sub.2 --CH.sub.2 --O--CH.sub.2 --CH.sub.2 --CN (I)in which R represents an alkyl group, an optionally substituted phenyl group or a benzyl group, is condensed with trimethoxy benzaldehyde in the presence ofBasic reagents to form a compound corresponding to the general formula ##STR1## in which R is as defined above, and the condensation product (II) obtained is reacted with guanidine in known manner to form 2,4-diamino-5-(3',4',5'-trimethoxybenzyl)-pyrimidine.

Abstract: A method of preparation of 2,4-diamino-5-benzylpyrimidines involving the reaction of a 2,4-diamino-5-substituted methyl pyrimidine, for example 2,4-diamino-5-hydroxymethylpyrimidine, with an appropriately substituted phenol.

Abstract: A process of severely damaging or killing unwanted plants, which comprises applying to the plants, or to the growth medium thereof, a herbicidally effective amount of pyrimidine compound of the formula: ##STR1## or a herbicidal acid addition salt thereof, wherein R.sup.1 is an alkyl radical of 1 to 6 carbon atoms, cycloalkyl or alkenyl; R is a hydrogen atom or an alkyl or alkenyl radical of from 1 to 12 carbon atoms, which may be substituted by a phenyl radical; or R.sup.1 and R taken together form a trimethylene or tetramethylene radical; X is either (a) an --NR.sup.3 R.sup.4 radical wherein each of the groups R.sup.2 and R.sup.4 is a hydrogen atom or an alkyl or alkenyl radical of 1 to 3 carbon atoms or cycloalkyl, or --NR.sup.3 R.sup.4 constitutes a pyrrolidinyl, piperidinyl or morpholinyl ring; or (b) a group --OR.sup.5 wherein R.sup.5 is an alkyl or alkenyl radical of 1 to 10 carbon atoms or cycloalkyl; and R.sup.6 and R.sup.

Abstract: 2,4-Diaminopyrimidines bearing a substituted benzyl group in position-1 are prepared from the correspondingly substituted .alpha.-alkoxymethylcinnamonitrile by treatment of the latter with an alkali metal alkoxide in mono-methyl ether of ethylene glycol and subsequently reacting the resulting reaction mixture with guanidine.