Abstract: The novel compounds of formula I ##STR1## (A and R.sup.1 through R.sup.4 are defined in the specification) show selective fungicidal activity. The new compounds are obtainable by a new synthetic method and processed with carriers and adjuvants to fungicidal compositions.

Abstract: This invention relates to novel heterocycles including 3-?1-?3-(imidazolin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(benzylo xycarbonylamino)propionic acid, which are useful as antagonists of the .alpha..sub.v .beta..sub.3 integrin and related cell surface adhesive protein receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.

Abstract: 6-Aryl pyrazolo?3,4-d!pyrimidin-4-one derivatives, pharmaceutical compositions containing them and methods for effecting c-GMP-phosphodiesterase inhibition and for treating heart failure and/or hypertension.

Abstract: Disubstituted heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein G is ##STR2## wherein n is 0, 1 or 2 or 3; m is 0, 1, 2 or 3; Y is NH or S; p is 0, 1 or 2, Q is a single bond or ##STR3## and Z, A, R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.6 are as defined herein.

Abstract: Disclosed are xanthine derivatives represented by the following Formula (I): ##STR1## in which R.sup.1, R.sup.2, and R.sup.3 independently represent hydrogen or lower alkyl;Q.sup.1, Q.sup.2, and Q.sup.3 independently represent hydrogen, lower alkyl, lower alkoxy, or halogen;and X represents --COR.sup.4 (in which R.sup.4 represents hydrogen, hydroxy, lower alkyl, or lower alkoxy) or --SO.sub.2 R.sub.5 {in which R.sup.5 represents hydroxy, lower alkoxy, trifluoromethyl, ##STR2## in which R.sup.6 and R.sup.7 independently represent hydrogen, hydroxy-substituted or unsubstituted lower alkyl, aryl, or ##STR3## (in which m represents an integer of 1 to 3; and R.sup.8 and R.sup.9 independently represent hydrogen or lower alkyl), or ##STR4## (in which Y represents a single bond, oxygen, or N--R.sup.10 in which R.sup.10 represents hydrogen or lower alkyl; and n1 and n2 independently represent an integer of 1 to 3)}, and pharmaceutically acceptable salts thereof.

Abstract: Novel quinazoline inhibitors of endothelin converting enzyme are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin and in controlling hypertension, myocardial infarction and ischemia, metabolic, endocrinological, and neurological disorders, congestive heart failure, endotoxic and hemorrhagic shock, septic shock, subarachnoid hemorrhage, arrhythmias, asthma, acute and chronic renal failure, cyclosporin-A induced nephrotoxicity, angina, gastric mucosal damage, ischemic bowel disease, cancer, pulmonary hypertension, preeclampsia, atherosclerotic disorders including Raynaud's disease and restenosis, cerebral ischemia and vasospasm, and diabetes.

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: Quinazoline compounds represented by general formula (1) or (2) possess an activity of significantly inhibiting the production or secretion of a tumor necrosis factor and are useful as drugs for the treatment of diseases wherein a tumor necrosis factor is considered to be involved in causing those diseases: ##STR1## wherein R.sup.1 through R.sup.

Abstract: Disclosed are compounds of the formula ##STR1## wherein Ar represents an aryl or heteroaryl group; andR.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 represent organic or inorganic substituents,which compounds are highly selective partial agonists or antagonists at human CRF1 receptors and, thus, are useful in the diagnosis and treatment of treating stress related disorders such as post trumatic stress disorder (PTSD) as well as depression, headache and anxiety.

Abstract: Pyridine-N-oxide-substituted salicylaldehyde and salicylic acid derivatives of the general formula I ##STR1## where R is a formyl group, a CO.sub.2 H group or a radical which can be hydrolyzed to CO.sub.2 H and the other substituents have the following meanings:R.sup.2 is halogen, alkyl, haloalkyl, alkoxy, haloalkoxy or alkylthio;X is nitrogen or CR.sup.13, R.sup.13 being hydrogen or halogen or together with R.sup.3 forming a 3- to 4-membered alkylene or alkenylene chain in which at least one methylene group is replaced by oxygen;R.sup.3 is halogen, alkyl, haloalkyl, alkoxy, haloalkoxy or alkylthio, or R.sup.3 is linked with R.sup.13 as indicated above to give a 5- or 6-membered ring;Y is oxygen or sulfur;R.sup.14 -R.sup.

Abstract: The present invention relates to novel compounds which possess a broad range of useful biological activities. These compounds can maintain, increase, or restore sensitivity of cells to therapeutic or prophylactic agents. They can also suppress, modify, or significantly reduce an immune response, including an autoimmune response in a mammal. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well-suited for treatment of multi-drug resistant cells, for prevention of the development of multi-drug resistance, for use in multi-drug resistant cancer therapy, and for prevention or treatment of graft rejection and various autoimmune diseases.

Abstract: Substituted pyridines and pyrimidines, processes for their preparation and their use as pesticides and fungicides.The invention relates to compounds of the formula ##STR1## in which A is N or CH, R is H, halogen, alkyl or cycloalkyl, R.sup.2 and R.sup.3 are H, halogen or an aliphatic radical or together form a ring, X is O, NH Or S(O).sub.q where q=0, 1 or 2, R.sup.4.sub.q is 0-4 radicals selected from the series consisting of halogen, optionally substituted alkyl or alkoxy, cycloalkyl and optionally substituted phenyl, n=0-2, m=1-3 and Y is optionally substituted methylene or imino.The invention furthermore relates to a process for their preparation and for their use as pesticides, in particular as insecticides, acaricides and fungicides. The compounds are furthermore suitable for controlling nematodes, helminths and molluscs, and for controlling endoparasites and ectoparasites in the field of veterinary medicine.

Abstract: This invention relates to certain triazolopyrimidine derivatives of formula I ##STR1## wherein R.sub.1 represents an optionally substituted alkyl, alkenyl, alkynyl, alkadienyl, cycloalkyl, bicycloalkyl or heterocyclyl group; R.sub.2 represents a hydrogen atom or an alkyl group; or R.sub.1 and R.sub.2 together with the interjacent nitrogen atom represent an optionally substituted heterocyclic ring; R.sub.3 represents an optionally substituted aryl group; and R.sub.4 represents a hydrogen or halogen atom or a group --NR.sub.5 R.sub.6 where R.sub.5 represents a hydrogen atom or an amino, alkyl, cycloalkyl or bicycloalkyl group and R.sub.6 represents a hydrogen atom or an alkyl group; processes for their preparation; compositions containing such compounds and their use as fungicides.

Abstract: Heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein n, R, R.sup.1, R.sup.2, R.sup.3, G, G.sub.x, R.sup.6', Ra, Xa, R.sup.6, Rb, R.sub.3, p, Q, A and R.sup.4 are as defined herein.

Abstract: Thrombin inhibitors are provided which have the formula ##STR1## wherein Z is a thrombin inhibitor substructure containing distal and proximal binding site residues; andR.sup.1 is cyano, hydroxyl, alkoxy, amino, aminoalkyl or nitro.

Abstract: Novel A-II receptor antagonists have the formula ##STR1## and its isomer ##STR2## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are as defined herein.

Abstract: The compounds of the formula: ##STR1## wherein R.sup.1, Y, A, Z, CyB, R.sup.3, R.sup.4, n and m are described in the specification and claims.and acid addition salts thereof, salts thereof, and hydrates thereof; have inhibitory effect on cGMP-PDE, and additionally on TXA.sub.2 synthetase.

Abstract: The compounds of the formula: ##STR1## wherein R.sup.1, Y, A, R.sup.4, n, Z, CyB, R.sup.3, and m are defined in the specification.

Abstract: A condensed pyrimidine derivative of the formula (I): ##STR1## wherein the ring A stands for an optionally substituted 5-membered ring; B stands for an optionally substituted divalent 5- or 6-membered homo- or hetero-cyclic group; X stands for, among others, amino group; Y stands for, among others, hydrogen atom, halogen atom or amino group; Z stands for a divalent aliphatic group having five or less atoms forming straight chain, optionally having nitrogen, whose chain portion may optionally have a hetero-atom; W stands for, among others, --NH--CO-- or --CO--NH--; R.sup.1 stands for an optionally substituted cyclic or chain-like group; COOR.sup.2 stands for an optionally esterified carboxyl group; and p denotes an integer of 1 to 4, provided that when --W--R.sup.1 denotes a moiety represented by the formula: ##STR2## wherein COOR.sup.16 and COOR.sup.

Abstract: Heteroaromatically condensed hydroxypyridonecarboxamides of the structure I ##STR1## where the substituents and the ring Q have the following meanings: R.sup.1 hydrogen, hydroxyl, substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy;R.sup.2 hydrogen, substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl, alkenyloxy, dialkylamino; orR.sup.1, R.sup.2 together denote an alkylene chain with 2-6 members and which may be interrupted by oxygen, sulfur or N-methyl;X oxygen or sulfur;Q a 5- or 6-membered heteroaromatic ring containing from 1 to 3 nitrogen atoms and/or one oxygen or sulfur atom as heteroatoms, and which may be substituted one to three times,and environmentally compatible salts thereof.

Abstract: Glycol aldehyde and lactic acid derivatives and their sulfur analogs of the formula I ##STR1## where R.sup.1 to R.sup.3 have the meanings given in the specification, X is oxygen, sulfur or a single bond, and Y is a C.sub.2 -C.sub.4 -alkylene or C.sub.2 -C.sub.4 -alkenylene chain where in each case a methylene group may be substituted by an oxo group (.dbd.O), environmentally compatible salts of the compounds I, methods of preparing the compounds I, and their use as herbicides.

Abstract: This invention provides novel pyrimidines or their pharmaceutically acceptable salts thereof and process for preparation thereof. The novel compounds are useful for neurological diseases of the peripheral and central nervous systems of animals.

Abstract: The present invention relates to novel substituted pyrimidobenzimidazole derivatives of the formula ##STR1## wherein the substituents are as described in the specification, and pharmaceutically acceptable salts thereof.The products have an inhibitory action on the DNA-gyrase activity in bacteria. They can accordingly be used for the prevention or control of bacterial infections.

Abstract: Oxazolyl derivatives of formula (I) ##STR1## wherein --A.sup.1 .dbd.A.sup.2 --A.sup.3 .dbd.A.sup.4 -- represents a bivalent radical having the formula--CH.dbd.CH--CH.dbd.CH-- (a-1),--N.dbd.CH--CH.dbd.CH-- (a-2),--CH.dbd.N--CH.dbd.CH-- (a-3),--CH.dbd.CH--N.dbd.CH-- (a-4),--CH.dbd.CH--CH.dbd.N-- (a-5),--N.dbd.CH--N.dbd.CH-- (a-6)or--CH.dbd.N--CH.dbd.N-- (a-7);R represents hydrogen or C.sub.1-4 alkyl; R.sup.1 represents hydrogen, C.sub.1-6 alkyl or hydroxyC.sub.1-6 alkyl; m represents 1 or 2; D represents C.sub.1-4 alkanediyl; B represents NR.sup.2, CH.sub.2, O, S, SO or SO.sub.2 wherein R.sup.2 is hydrogen or C.sub.1-4 alkyl; n represents 0, 1 or 2; L represents hydrogen; C.sub.1-12 alkyl; C.sub.3-6 cycloalkyl; C.sub.3-6 alkenyl optionally substituted with aryl; C.sub.1-6 alkylcarbonyl; C.sub.1-6 alkyloxycarbonyl; arylcarbonyl; arylC.sub.1-6 alkyloxycarbonyl; or a radical of formula --Alk--R.sup.3 (b-1); --Alk--Y--R.sup.4 (b-2); --Alk--Z.sup.1 --C(.dbd.X)--Z.sup.2 --R.sup.5 (b-3); or --CH.sub.2 --CHOH--CH.sub.

Abstract: Aminopyrimidine derivatives, their preparation, and agents containing them, and their use as fungicides comprising ##STR1## in which R.sup.1 is alkyl, alkoxyalkyl, alkylthioalkyl, cycloalkyl, alkenyl, alkynyl, cycloalkylalkyl, substituted aminoalkyl, phenyl, phenylalkyl, phenoxyalkyl, phenylmercaptoalkyl or phenoxyphenoxyalkyl, R.sup.2, R.sup.3 and R.sup.4 are H, alkyl, or phenyl, R.sup.5 is H, alkyl, cycloalkyl, cycloalkylalkyl, haloalkyl, alkoxy, alkylthio, alkoxyalkyl, R.sup.7 R.sup.8 N-,alkylthioalkyl, R.sup.7 R.sup.8 N-alkyl, halogen, alkenyl, alkynyl, phenyl, phenoxy, phenylalkyl, phenoxyalkyl, phenylmercaptoalkyl, phenylmercapto, phenylalkoxy or phenylalkylthio, R5 is H, alkyl, alkyloxy, alkenyloxy, alkynyloxy, alkylthio, halogen, or phenyl or R.sup.5 and R.sup.6 together form a chain, and R.sup.7 and R.sup.8 are H, alkyl, alkoxyalkyl, hydroxyalkyl, alkylthioalkyl, alkenyl, substituted formyl, phenyl or phenylalkyl, or R.sup.7 or R.sup.

Abstract: Insecticidal 1,2,3,4-Tetrahydro-5-nitropyrimidine derivatives, and salts thereof, of the formula ##STR1##

Abstract: This invention relates to pyrimidopyrimidine derivatives which have bronchodilator and anti-allergic activities. A compound of the invention is 7-cyclopropylamino-4-oxo-2-(2-propoxyphenyl)-3,4-dihydropyrimido[4,5-d] pyrimidine.

Abstract: [(Bicyclic heterocyclyl)methyl and -hetero] substituted hexahydro-1H-azepines and pyrrolidines and their pharmaceutically acceptable acid addition salts having anti-histaminic properties, compositions containing the same, and methods of treating allergic diseases in warm-blooded animals.

Abstract: A compound of the formula ##STR1## (symbols defined in the specification), its 3,4-dihydropyrimidine tautomer form and pharmaceutically acceptable salts thereof have calcium entry blocking activity. A process of preparation, pharmaceutical composition and method of using the compound to reduce blood pressure are also provided.

Abstract: 3,4-Dihydrothieno[2,3-d]pyrimidine compounds having immunoregulating and carcinostatic actions of the general formula ##STR1## wherein A represents a C.sub.1-4 alkylene; R.sup.1 represents hydrogen, an alkyl, an aryl which may be substituted or --N(R.sup.7)(R.sup.8); R.sup.2, R.sup.3 and R.sup.4 represent hydrogen, a halogen, hydroxy, an alkyl which may be substituted by a halogen, an alkoxy, nitro, cyano or --N(R.sup.9)(R.sup.10); R.sup.5 represents hydrogen, a halogen, nitro, amino, cyano, an alkyl or an alkoxycarbonyl; R.sup.6 represents hydrogen, a halogen, nitro, amino, cyano, an alkyl, an alkoxycarbonyl, a halogenosulfonyl or --SO.sub.2 N(R.sup.12)(R.sup.13); or R.sup.5 and R.sup.6 may, taken together, form a C.sub.3-6 alkylene chain, and their pharmaceutical use.

Abstract: Novel dibenz[b,e]oxepin derivatives are employed in the treatment and control of allergic conditions such as allergic asthma and also employed in the treatment of inflammation.

Abstract: Novel compounds of the formula ##STR1## wherein X is sulfur or oxygen, R.sub.2 is aryl or heterocyclo and R.sub.1 is as defined herein, are disclosed. Compounds of formula I possess calcium channel activating activity.

Abstract: The invention relates to compounds of formula I: ##STR1## in which m=2-4,n and p, which may be identical or different, are an integer equal to 1, 2 or 3, with the proviso that the sum of n and p is 5,q=0 or 1,R is a 1,2,3,4-tetrahydro-3-quinazolinyl radical, optionally substituted, a 1,3,4,6,11,11a-hexahydro-1,3-dioxo-2H-pyrazino[1,2-b]isoquinol-2-yl radical, a 1,2-dihydro-1-oxo-2-phthalazinyl radical, optionally substituted, a 2,6-dioxo-1-piperazinyl radical of formula W: ##STR2## (R.sub.3 is a 2-pyridyl radical or an optionally substituted phenyl radical),a radical of formula Z: ##STR3## (R.sub.4 is a carbamoyl radical, a cyano radical, a hydroxycarbonyl radical or an alkoxycarbonyl radical having 1 to 6 carbon atoms),or a radical of formula Y: ##STR4## (R.sub.5 is a 2-pyrimidinyl radical, a 1-isoquinolyl radical, a 2-quinolyl radical, a 2-pyridyl radical, a benzyl radical, optionally substituted, a 2-thiazolyl radical, optionally substituted, or a 2-benzothiazolyl radical) andeither R.sub.1 and R.sub.

Abstract: This invention relates to fused pyrimidine derivatives which have bronchodilator and anti-allergic activities. A compound of the invention is 2-(2-propoxyphenyl)pyrido[2,3-d]pyrimid-4(3H)-one.

Abstract: 2-Amino-pyrimidininone derivatives possessing antihistaminic and serotonin-antagonistic properties. Compositions containing these compounds as the active ingredient and a method of treating subjects from allergic diseases.

Abstract: [(Bicyclic heterocyclyl)methyl and -hetero] substituted hexahydro-1H-azepines and pyrrolidines and their pharmaceutically acceptable acid addition salts having anti-histaminic properties, compositions containing the same, and methods of treating allergic diseases in warm-blooded animals.

Abstract: Cyclic amine derivatives of the formula: ##STR1## or the pharmacologically acceptable salts thereof, wherein the symbols are as defined in the specification, as effective in relieving, curing or preventing mental symptoms due to cerebral vascular disorders.

Abstract: This disclosure described novel 5-(substituted-amino)-8-(substituted-phenyl)-3H,6H, -1,-4,5a,8a-tetraazaacenaphthylen-3-ones useful for the treatment of cognitive and related neural behavioral disorders in mammals.

Abstract: Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sub.4 is aryl are disclosed. These novel compounds are useful, for example, as cardiovascular agents.

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-- 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 psychoromatic disease and anxiety neurosis.

Abstract: New pyri(mi)dyl-oxy- or -thio-benzoic acid derivatives of the formula ##STR1## are taught which have herbicidal and plant growth regulating activity. In the formula Z can be Ch or N, X is oxygen or sulphur, A is oxygen, sulphur, a radical R.sup.5 --N.dbd.or a radical R.sup.6 O--N.dbd.and B is oxygen, sulphur, a radical ##STR2## with the proviso that at least one of the radicals R.sup.1, R.sup.2 or R.sup.3 represents alkyl or a part of a 3- to 6-membered fused carbocyclic ring.

Abstract: The present invention is directed to a group of compounds which are imidazo[2,1-b]quinazolin-5(3H)-ones, related tricyclic compounds, and pharmaceutically acceptable salts thereof. These compounds are useful as bronchodilators. These compounds are prepared by the reaction of an appropriate hydrazine with an appropriate 1-substituted-2-methyl-2-imidazoline or chemically equivalent compound.

Abstract: Cardiovascular activity is exhibited by compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein R.sub.1 is ##STR2## or ##STR3## and R.sub.2, R.sub.3 and R.sub.4 are as defined herein.

Abstract: 1,4-Dihydropyridine derivatives which combine both calcium agonist and alpha.sub.1 -antagonist activity are useful in treating congestive heart failure. These derivatives are compounds having the formula: ##STR1## wherein Ar, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are defined in the specification.

Abstract: The invention relates to condensed cyclic triazole derivatives of the general Formula I ##STR1## and pharmaceutically acceptable salts thereof. The compounds of the general Formula I possess useful sedative and tranquillant properties and exhibit particularly spasmolytic, motility inhibiting, and narcosis potentiating, yohimbine potentiating and local anaesthetic and also weak reserpine ptosis inhibiting effect.

Abstract: Novel N-(bicyclic heterocyclyl)-4-piperidinamines having antihistaminic and serotonin-antagonistic properties which are useful in the treatment of allergic diseases.

Abstract: Cardiovascular activity is exhibited by compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sub.1 is aryl or heterocyclo;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 hydrogen, alkyl, alkenyl, alkynyl, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3, halo substituted alkyl, or ##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## Y.sub.3 is hydroxyl, alkoxy, aryl--(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl--(CH.sub.2).sub.m --S--, ##STR5## amino, or substituted amino; Y.sub.4 is alkyl, cycloalkyl, aryl, heterocyclo, --(CH.

Abstract: There are described novel carboxylic acid derivatives of the formula ##STR1## and derivatives of the formula ##STR2## and the addition salts thereof, which exhibit an effect on the intermediary metabolism. Furthermore, the compounds of Formula Ia as well as the compounds of Formula I possess blood-sugar lowering properties.

Abstract: The novel 2-amino-alkenylsulfonylureas of the formula (I) ##STR1## in which R.sub.1 and R.sub.2 denote hydrogen, alkyl, cycloalkyl or (substituted) phenyl, or R.sub.1 and R.sub.2, together with the common nitrogen atom, form a 5-membered to 7-membered (hetero)aliphatic ring, R.sub.3 denotes hydrogen, cycloalkyl, alkyl, alk(en)(yn)yloxy, alkylsulfen(in)(on)yl, --SO.sub.2 (N)(mono- or di-alkyl), (substituted) phenyl, benzyl, substituted hydroxycarbonyl or (substituted) aminocarbonyl, R.sub.4 has the meaning of R.sub.3 and additionally denote formyl, alkanoyl, (substituted) benzoyl, cycloalkylcarbonyl or C.sub.6 H.sub.5 --CH.sub.2 --O--CO--, or R.sub.3 and R.sub.4, together with the olefinic carbon atoms connecting them, form a 5-membered to 8-membered aliphatic ring system, R.sub.5 denotes H, alkyl, alkenyl, alkynyl, alkoxy or alkoxycarbonyl and R.sub.

Abstract: The invention provides 4-pyridone-3-carboxylic acids and derivatives thereof together with a method for their preparation. Also included in the invention are compositions containing said 4-pyridone-3-carboxylic acids and derivatives and the use of said compounds and compositions as antibacterial and/or antifungal agents or for animal growth promotion or improved feed utilization.