Abstract: Novel pyrazinyl sulfonamides of the formulaQ--SO.sub.2 --NH.sub.2wherein Q is a substituted pyrazine group are intermediates for the production of sulfonylureas and suflonylthioureas which are useful in controlling weeds or selectively influencing plant growth.

Abstract: The invention relates to novel N-(2-nitrophenyl)-4-aminopyrimidine derivatives of the general formula I ##STR1## wherein R.sub.1 is NO.sub.2 or CF.sub.3,R.sub.2 is NO.sub.2 or CF.sub.3,R.sub.3 is hydrogen or halogen,R.sub.4 is hydrogen or the --C(O)R.sub.7 group, wherein R.sub.7 is C.sub.1 -C.sub.4 alkyl which is unsubstituted or substituted by halogen, C.sub.1 -C.sub.3 alkoxy or C.sub.1 -C.sub.3 alkylthio,R.sub.5 and R.sub.6 are each independently halogen, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkyl which is substituted by halogen or C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.6 alkoxy which is substituted by halogen or C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.6 alkylthio or C.sub.1 -C.sub.6 alkylthio which is substituted by halogen or C.sub.1 -C.sub.3 alkoxy, or are C.sub.3 -C.sub.6 cycloalkoxy, C.sub.3 -C.sub.6 cycloalkylthio, C.sub.3 -C.sub.6 alkenyloxy, C.sub.3 -C.sub.6 alkenylthio, C.sub.3 -C.sub.6 alkynyloxy, C.sub.1 -C.sub.6 alkylsulfoxyl, C.sub.1 -C.sub.6 -alkylsulfonyl, C.sub.1 -C.sub.

Abstract: 5-fluorocytosine is prepared by reacting 2,5-difluoro-4-chloro-pyrimidine with a proton acid in the presence of water to yield 2-hydroxy-4-chloro-5-fluoropyrimidine and reacting the 2-hydroxy-4-chloro-5-fluoropyrimidine with ammonia to yield 5-fluoro-cytosine.

Abstract: The present invention provided pyrrolobenzimidazoles or tautomer thereof, of the general formula: ##STR1## wherein R.sub.1 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl or C.sub.3 -C.sub.7 cycloalkyl;R.sub.2 is hydrogen, cyano, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, or a carbonyl group substituted by hydroxyl, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkyoxy, amino, C.sub.1 -C.sub.6 alkylamino, C.sub.2 -C.sub.12 dialkylamino or hydrazino, orR.sub.2 and R.sub.1 together with the carbon to which they are attached form a C.sub.3 -C.sub.8 spirocycloalkyl ring, or R.sub.1 and R.sub.2 together form C.sub.3 -C.sub.7 alkylidene or C.sub.3 -C.sub.7 cycloalkylkidene,X is a valency bond, C.sub.1 -C.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: Compounds of the formula ##STR1## wherein 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: Pharmaceutical compositions of specific substituted pyrimidines and methods of treatment of certain cardiovascular disorders are disclosed. Also disclosed are novel substituted acrylated pyrimidines which are useful as calcium channel blockers.

Abstract: Substituted aminoalkylphenoxy derivatives represented by the general formula of: ##STR1## wherein the substituting group Z is either one of the following groups of: ##STR2## were prepared. These derivatives exert antagonism against Histamine H.sub.2 -receptors and hence are efficacious for the treatments of digestive ulcers.

Abstract: Novel 4-heterocyclylvinyl-4'-styryl-biphenyls of the formula ##STR1## are described, i which A is an isoxazolyl, oxadiazolyl, pyrimidinyl or triazinyl radical which is unsubstituted or substituted by a non-chromophoric substituent, R.sub.1 is hydrogen or a non-chromophoric substituent and R.sub.2 is hydrogen, halogen, or alkyl; processes for the preparation of these compounds are also described.The novel 4-heterocyclylvinyl-4'-styryl-biphenyls can be used as fluorescent brighteners for high-molecular organic materials, in particular materials of polyamide and polyester, especially for polyester textiles.

Abstract: The invention relates to guanidine 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 and R.sup.2, same or different, are hydrogen or 1-10C alkyl, 3-8C cycloalkyl or 4-15C 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 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.

Abstract: This invention relates to N-aryl-3-aryl-4,5-dihydro-1H-pyrazole-1-carboxamide compounds which are useful as pesticides, compositions containing those compounds, methods of controlling pests and processes for preparing these compounds.

Abstract: Microbicidally active novel 1-heteroaryl-4-aryl-pyrazolin-5-ones of the formula ##STR1## in which R represents hydrogen or alkyl,R.sup.1 represents halogen, hydroxyl, optionally substituted alkyl, optionally substituted alkoxy, optionally substituted phenoxy, a radical --S(O).sub.p -- alkyl which is optionally substituted in the alkyl part, nitro, optionally substituted amino or a fused-on carbocyclic or heterocyclic radical,p represents an integer 0, 1 or 2,R.sup.2 represents halogen or optionally substituted alkyl, or represents alkoxy, alkylmercapto, nitro, cyano, carboxamide or a fused-on carbocyclic radical,m represents an integer from 0 to 5,n represents an integer from 0 to 4, it being possible for the substituents to be identical or different when m and/or n represent a number greater than 1, andX, Y and Z are identical or different and represent a nitrogen atom or the radical .dbd.CH or ##STR2## wherein R.sup.

Abstract: The invention relates to certain sulfonylurea compounds having an ester group ortho to the sulfonylurea linkage which have been found to be excellent preemergent and postemergent herbicides or plant growth regulators.

Abstract: Dihydropyridine Anti-ischaemic agents of the formula ##STR1## and their salts where R is aryl, R.sup.1 and R.sup.2 are each C.sub.1 -C.sub.4 alkyl or 2-methoxyethyl, Y is --(CH.sub.2).sub.n -- where n is 2, 3 or 4 and is optionally substituted by 1 or 2 methyl groups and R.sup.3 is pyrimidyl or di- or tetrahydropyrimidyl.

Abstract: Ethane derivatives of the formula IR.sup.1 --A.sup.1 --CH.sub.2 CH.sub.2 --A.sup.2 --(A.sup.3).sub.n --R.sup.2 IwhereinR.sup.1 is H, an alkyl group with 1-12 C atoms, in which one or two non adjacent CH.sub.2 groups can also be replaced by O atoms and/or CO groups and/or --O--CO-- groups and/or --CO--O groups, F, Cl, Br or R.sup.3 --A.sup.4 --Z.sup.1 --,R.sup.2 is --CN or --Z.sup.2 --A.sup.4 --CN,A.sup.1 is --A--, --A--A.sup.5 -- or --A.sup.5 --A--,A.sup.2 is an 1,4-phenylene group which is unsubstituted or substituted by one or two F and/or Cl atoms and/or CH.sub.3 groups and/or CN groups and in which one or two CH groups can also be replaced by N atoms,A is a 1,4-cyclohexylene group, in which one or two non adjacent CH.sub.2 groups can also be replaced by O atoms, or is a 1,3-dithiane-2,5-diyl group or 1,4-bicyclo(2,2,2)-octylene group,A.sup.3, A.sub.4 are each a 1,4-cyclohexylene group, in which one or two non adjacent CH.sub.

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: Compounds of the formula formula IA or IB ##STR1## wherein A represents an optionally substituted saturated divalent grouping which together with the two carbon atoms to which it is attached represents a fused 5-, 6- or 7-membered carbocyclic or heterocyclic ring selected from optionally substituted fused cyclopenteno, cyclohexeno, cyclohepteno, dihydrothieno, dihydrothiopyrano, tetrahydrothiepino, dihydrofuro, dihydropyrano, tetrahydrooxepino, dihydropyrrolo, tetrahydropyrido and tetrahydroazepino; R.sub.1 represents lower alkyl, phenyl, or phenyl mono- or disubstituted by lower alkyl, lower alkoxy, halogen or trifluoromethyl; or R.sub.1 represents an aromatic heterocyclic radical selected from e.g. optionally substituted pyridyl, quinolyl, isoquinolyl, pyrimidyl and thiazolyl; R.sub.2, R.sub.3, R.sub.3 ' are hydrogen or lower alkyl; and pharmaceutically acceptable salts; are useful as benzodiazepine receptor modulators for the treatment of nervous system disorders.

Abstract: Histamine H.sub.2 -receptor antagonists of the formula ##STR1## wherein A, m, Z, n and R.sup.

Abstract: There are provided ergoline derivatives of the formula: ##STR1## wherein R.sub.1 represents a hydrogen atom or a methyl group, R.sub.2 represents a hydrogen or halogen atom or a methyl group, R.sub.3 represents a hydrogen atom or a methoxy group, R.sub.4 represents a hydrocarbon group having from 1 to 4 carbon atoms; each of X and W independently represents a hydrogen atom, a methyl group, a chlorine atom or a methoxy group, and n is 0, 1 or 2. A method for their preparation is also provided. The compounds have strong antiprolactin 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: Dihydropyridine derivatives of the formula: ##STR1## and their pharmaceutically acceptable acid addition salts; wherein R is a substituted aryl group;R.sup.1 and R.sup.2 are each independently C.sub.1 -C.sub.3 alkyl;Y is --(CH.sub.2).sub.n -- where n is 2, or --CH.sub.2 CH(CH.sub.3)--; and Het is a 6-membered aromatic heterocyclic group attached to the adjacent oxygen atom by a carbon atom.The compounds have utility as anti-ischaemic and anti-hypertensive agents.

Abstract: A fluorinated isophthalonitrile compound having the general formula ##STR1## wherein Y is --O, --S, or --N(R'), R and R' are independently hydrogen, an alkyl group, an alkyl group, an alkynyl group, a haloalkyl group, an alkoxyl group, alkoxyalkyl group, a phenyl group which may be substituted, a tetrahydrofurfuryl group, or a cycloalkyl group, provided that, in the case of Y=--N(R'), R and R' or Y may be a tetrahydrofurfuryl group, or a cycloalkyl group, a heterocyclic compound residue.This fluorinated isophthalonitrile compound is suitable for use as an agricultural fungicide.

Abstract: Substituted triazolo[4,3-c]pyrimidines which are bronchodilators. The pharmacological use of these compounds, pharmaceutical compositions containing these compounds, and synthetic intermediates for the preparation of these compounds are also described.

Abstract: New pyrimidine derivatives of the formula: ##STR1## wherein Z is a group selected from ##STR2## in which R.sup.1 and R.sup.2 are each hydrogen, alkenyl, ar(lower)alkyl or lower alkyl optionally substituted with epoxy, hydroxy, amino and/or lower alkylamino and R.sup.5 is lower alkyl,R.sup.3 is hydrogen, aryl optionally substituted with lower alkyl, lower alkoxy and/or halogen, or pyridyl optionally substituted with lower alkyl,R.sup.4 is hydrogen, lower alkyl or phenyl optionally substituted with lower alkoxy, andY is .dbd.O, .dbd.S or .dbd.N--R.sup.6, in which R.sup.6 is lower alkyl; cyclo(lower)alkyl; ar(lower)alkyl optionally substituted with lower alkoxy; N-containing unsaturated heterocyclic group optionally substituted with lower alkyl; or aryl optionally substituted with hydroxy, lower alkyl, halogen or lower alkoxy, in which lower alkoxy substituent may be substituted with epoxy, hydroxy, amino and/or lower alkylamino,provided that Y is .dbd.N--R.sup.6 when R.sup.3 and R.sup.

Abstract: Antibacterial activity is exhibited by novel compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof.

Abstract: The present invention provides aryloxypropanolamines of the general formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be the same or different, are hydrogen or halogen atoms or lower alkyl, cyano, carboxamide, hydroxyl, lower acyloxy, lower alkoxy, lower alkenyloxy or aryl lower alkoxy radicals, R.sub.5 and R.sub.6, which may be the same or different, are hydrogen atoms or lower alkyl radicals, X is a straight or branched alkylene chain containing 2 to 6 carbon atoms, A is a mono-, bi- or tricyclic heteroaromatic or hydroheteroaromatic radical or, when at least one of the symbols R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is other than a hydrogen atom, may also be a phenyl radical, with the proviso that when A is a uracil-6-yl radical, the 5-position of the uracil moiety does not contain a hydrogen atom, R.sub.7, R.sub.8, R.sub.9, R.sub.10 and R.sub.

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: Compounds of the formula formula IA or IB ##STR1## wherein A represents an optionally substituted saturated divalent grouping which together with the two carbon atoms to which it is attached represents a fused 5-, 6- or 7-membered carbocyclic or heterocyclic ring selected from optionally substituted fused cyclopenteno, cyclohexeno, cyclohepteno, dihydrothieno, dihydrothiopyrano, tetrahydrothiepino, dihydrofuro, dihydropyrano, tetrahydrooxepino, dihydropyrrolo, tetrahydropyrido and tetrahydroazepino; R.sub.1 represents lower alkyl, phenyl, or phenyl mono- or disubstituted by lower alkyl, lower alkoxy, halogen or trifluoromethyl; or R.sub.1 represents an aromatic heterocyclic radical selected from e.g. optionally substituted pyridyl, quinolyl, isoquinolyl, pyrimidyl and thiazolyl; R.sub.2, R.sub.3, R.sub.3 ' are hydrogen or lower alkyl; and pharmaceutically acceptable salts; are useful as benzodiazepine receptor modulators for the treatment of nervous system disorders.

Abstract: This invention relates to ureas and isoureas which are useful as herbicides and plant growth regulants. In particular, compounds of the instant invention have demonstrated great selectivity.

Abstract: A novel compound, useful as an intermediate in the production of compounds of high antimicrobial activity, of the formula: ##STR1## wherein R.sub.a.sup.1 is hydrogen, amino or a protected amino group,R.sub.b.sup.1 and R.sub.c.sup.1 are each hydrogen, halogen, lower alkoxy or arylthio,R.sup.14 is carboxy or a protected carboxy group,X is lower alkylene or a group of the formula: ##STR2## in which R.sup.6 is hydrogen or an organic residue which may have suitable substituent(s), andZ is N or CH,or a salt thereof.

Abstract: Certain 2-substituted-2-penem-3-carboxylic acid compounds and pharmaceutically-acceptable salts thereof can be prepared from the appropriate xanthate or trithiocarbonate by desulfurization and addition of an electrophilic sulfur compound followed by halogenation and ring closure. The corresponding desulfurized and halogenated olefinic intermediates are disclosed.

Abstract: Cardiotonic 5-heteroaryl-substituted-2-pyridone compounds, pharamaceutical compositions, and a method for the treatment of congestive heart failure.

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: 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 .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: Pyrimidone derivatives of the formula ##STR1## wherein n is the integer 1 or 0; A.sup.1 and A.sup.2 are independently methylene or mono-lower alkyl or di-lower alkyl methylene; X is methylene, mono-lower alkyl or di-lower alkyl methylene, nitrogen or lower alkyl nitrogen; R is hydrogen or lower alkyl; and Y and Z taken together are the group .dbd.NR.sup.5, or R and Z taken together form a N--C--bond and Y is a group --N(H)R.sup.5 ; R.sup.1, R.sup.2 and R.sup.3 are hydrogen, lower alkyl or lower alkoxy, or R.sup.1 and R.sup.2 or R.sup.2 and R.sup.3 taken together are methylenedioxy or ethylenedioxy; R.sup.4 is hydrogen or lower-alkyl; R.sup.5 is phenyl or phenyl substituted by one or more of R.sup.6, R.sup.7 and R.sup.8 which, independently, are chlorine, fluorine, bromine, lower-alkyl or lower-alkoxy; and provided that at least one of the methylene groups A.sup.1 and A.sup.2 is mono-lower alkyl or di-lower alkyl methylene, when R.sup.

Abstract: Coumarin compounds of the general formula (1) ##STR1## in which A denotes an oxygen atom or a grouping >N--R in which R represents a hydrogen atom or an alkyl radical of 1 to 18 carbon atoms which may be substituted by fluorine, chlorine or bromine atoms or by alkoxy.sub.C.sbsb.1.sub.-C.sbsb.4, dialkyl.sub.C.sbsb.1.sub.-C.sbsb.4 -amino, --SO.sub.2 --N(alkyl.sub.C.sbsb.1.sub.-C.sbsb.4).sub.2 or cyano groups or a cycloaliphatic, aromatic or heterocyclic radical which may be substituted by fluorine, chlorine or bromine atoms or by alkyl.sub.C.sbsb.1.sub.-C.sbsb.4, alkoxy.sub.C.sbsb.1.sub.-C.sbsb.4, hydroxyl, cyano, sulfonamide or --SO.sub.2 --N--(alkyl.sub.C.sbsb.1.sub.-C.sbsb.4).sub.2 groups, X denotes an oxygen atom or a grouping .gtoreq.N--R' in which R' represents a hydrogen atom or an alkyl.sub.C.sbsb.1.sub.-C.sbsb.18 carbonyl, alkoxy.sub.C.sbsb.1.sub.-C.sbsb.4 carbonyl, alkyl.sub.C.sbsb.1.sub.-C.sbsb.4 carbamoyl or alkyl.sub.C.sbsb.1.sub.-C.sbsb.

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: Dihydropyridine anti-ischaemic agents of the formula: ##STR1## and their salts where R is aryl or heteroaryl, R.sup.1 and R.sup.2 are each C.sub.1 -C.sub.4 alkyl or 2-methoxyethyl, Y is --(CH.sub.2).sub.n -- where n is 2, 3, or 4 and is optionally substituted by 1 or 2 CH.sub.3 groups, and R.sup.3 is an optionally substituted 5- or 6-membered heterocyclic group attached to the adjacent N atom by a C atom, said group R.sup.3 being optionally fused to a further heterocyclic group or to a benzene ring.

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: Imidazo[1,2,-c]pyrimidines which are bronchodilators. Pharmacological methods of using these compounds, pharmaceutical compositions containing these compounds, and synthetic intermediates for preparing these compounds are also described.

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: Pyrimidine and s-triazine derivatives of formula (I) ##STR1## in which X=CH or N; Y=for example halogen, alkoxy; W=for example --S--CH.sub.2 --COOH, --O--CH.sub.2 --COO alkyl, --NH--CH.sub.2 --CONHCH.sub.2 CH.sub.2 OH; Z=for example 2,3-xylidino, and methods for the preparation thereof are described. The compounds show high antilipemic activity.

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: N-(heterocyclicaminocarbonyl)pyridinesulfonamides; are useful for the regulation of plant growth and as pre-emergence and post-emergence herbicides.

Abstract: N-(heterocyclicaminocarbonyl)arylsulfonamides in which the aryl radical is substituted in the 2-position by a carboxy radical, ester, thioester, or amide thereof; e.g. N-[(4,6-dimethylpyrimidin-2-yl)aminocarbonyl]-2-methoxycarbonylbenzenesulf onamide or N-[(4,6-dimethoxy-1,3,5-triazin-2-yl)aminocarbonyl]-2-methoxycarbonylbenze nesulfonamide; are useful for the regulation of plant growth and as pre-emergence and post-emergence herbicides.

Abstract: 1,2,4-Triazolo[4,3-c]pyrimidines substituted at the 5 or 7 position through a nitrogen atom which is part of a heterocyclic ring have been found to have potent bronchodilator activity and to be useful synthetic intermediates in the preparation of 1,2,4-triazolo[1,5-c]pyrimidines. Methods for inducing bronchodilation, pharmaceutical compositions, and synthetic processes and intermediates are also described.

Abstract: The invention relates to compounds of the formula ##STR1## said compounds being obtainable by cleavage of compounds of formula ##STR2## The compounds of the invention as well as compositions and medicaments containing a compound of the invention are useful as antimicrobial agents.

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: Pyrazolo[4,3-c]quinolin-3-ones of the formula ##STR1## e.g. wherein R.sub.1 is an aromatic heterocyclic radical selected from quinolyl, isoquinolyl, pyrimidyl and thiazolyl, or such said heterocyclic radical mono- or di-substituted by lower alkyl, lower alkoxy or halogen; R.sub.2 and R.sub.3, each independently, represents hydrogen or lower alkyl; R.sub.4 and R.sub.5, each independently, represents hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; and pharmaceutically acceptable salts thereof, are benzodiazepine receptor modulators.