Abstract: The invention relates to certain 3-isoxazolyl-2-imidazolidinone derivatives, namely 3-[5- or 3-substituted-3- or 5-isoxazolyl]-1-substituted-4-substituted amino-2-imidazolidinones and the uses thereof for preemergence or postemergence control of noxious plants, i.e., weeds.

Abstract: 1-Aryl-5-alkoximinoalkylamino-pyrazoles of the formula ##STR1## in which R represents cyano or nitro, or represents an optionally substituted heterocyclic radical,R.sup.1 represents hydrogen or alkyl,R.sup.2 represents hydrogen or alkyl, or represents optionally substituted aryl,R.sup.3 represents hydrogen, alkyl or alkenyl, or represents in each case optionally substituted aralkyl or aryl andAr represents optionally substituted phenyl or pyridyl,are active as herbicides and plant growth regulants. Compounds of the formula ##STR2## in which R" has the same definition as R other than cyano, are also active and useful as intermediates as well.

Abstract: A new process for preparing a pyrone-3-carboxamide compound of the formula (IV): ##STR1## wherein R.sub.1 is aryl or heterocyclic group optionally substituted, R.sub.2 is alkyl, aralkyl or like group, comprising reacting a compound of the formula (I) or (I'): ##STR2## wherein R.sub.3 is dialkylamino group and n is 0 to 6, and R.sub.1 and R.sub.2 are as above,with a compound of the formula (II): ##STR3## wherein R.sub.4 and R.sub.5 are hydrogen atom, alkyl or like group, or reacting a compound of the formula (III): ##STR4## wherein R.sub.6 is alkyl, aryl or like group, and R.sub.1 and R.sub.2 are as above,with a compound of the formula (II) or diketene in the presence of a tertiary organic base.

Abstract: Certain new 2-oxindole-3-carboxamide compounds having an acyl substituent at the 1-position are inhibitors of the cyclooxygenase (CO) and lipoxygenase (LO) enzymes, and are useful as analgesic and anti-inflammatory agents in mammalian subjects. In particular, the compounds of the invention are useful for acute administration for ameliorating or eliminating pain in human subjects recovering from surgery or trauma, and also for chronic administration for alleviating the symptoms of chronic diseases, such as rheumatoid arthritis and osteoarthritis, in human subjects.

Abstract: 1,3-Dicarboxamidooxindoles as antiinflammatory agents prepared by reaction of the 1-carbamoyloxindole with an isocyanate or by aminolysis of the corresponding alkyl 1-carbamoyloxindole-3-carboxylate.

Abstract: The invention relates to certain 3-isoxazolyl-2-imidazolidinone derivatives, namely 3-[5- or 3-substituted-3- or -5-isoxazolyl]-1-substituted-4- or 5-substituted amino-2-imidazolidinones and the use thereof for preemergence or postemergence control of noxious plants, i.e., weeds.

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: Tricyclic oxindole carboxamides, prepared by (a) reaction of an isocyanate with the basic ring system or (b) ammonolysis of a corresponding alkyl ester, are non-steroidal antiinflammatory agents useful in the treatment of rheumatoid arthritis.

Abstract: This invention relates to certain 3-isoxazolyl-2-imidazolidinone derivatives, namely 3-[5- or 3-substituted -3- or -5-isoxazolyl]-1-,4- or 5-substituted-2-imidazolidinones and the use thereof for preemergence or post-emergence control of noxious plants, i.e., weeds.

Abstract: Novel alkyl .beta.-oxo-benzenepropanoates of the formula ##STR1## wherein X is in the 5-,6-,7- or 8-position and is selected from the group consisting of hydrogen, halogen, alkyl of 1 to 5 carbon atoms, alkoxy of 1 to 4 carbon atoms, CF.sub.3 --, CF.sub.3 S-- and CF.sub.3 O--, R.sub.1 ' is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, R.sub.2 ' is selected from the group consisting of hydrogen, thiazolyl, 4,5-dihydrothiazolyl, pyridinyl, oxazolyl, isoxazolyl, imidazolyl, pyrimidyl, tetrazolyl, thienyl, benzothiazolyl and phenyl optionally substituted with at least one member of the group consisting of halogen, alkoxy of 1 to 4 carbon atoms, hydroxy, phenyl, CF.sub.3 --, NO.sub.2 -- alkyl of 1 to 4 carbon atoms and alkyl of 1 to 4 carbon atoms substituted with amino, alkylamino or dialkylamino with alkyls of 1 to 3 carbon atoms or R.sub.1 ' and R.sub.

Abstract: Ketone containing 1-substituted oxindole-3-carboxamides as antiinflammatory agents prepared by reaction of the 1-substituted oxindole with an isocyanate or by aminolysis of the corresponding alkyl oxindole-3-carboxylate.

Abstract: The invention provides 5-membered heteroaromatic compounds of formula IArN(Y)COCH.sub.2 Cl Iwherein Ar is a 5-membered heteroaromatic group comprising 1 or 2 heteroatoms selected from O, S and N and linked by a ring C-atom to the N-atom of the N(Y)COCH.sub.2 Cl group to which it is bound, whereby where Ar is pyrazolyl, said N(Y)COCH.sub.2 Cl group is in the 4-position,and Y is as specified in the description,the use of these compounds as herbicides, compositions for facilitating such use and the preparation of the chloroacetamides.

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: Imidazolidinone imines are provided as well as a process for preparing same including corresponding imidazolidinone amines which compounds are useful as herbicides.

Abstract: Novel dihydroisoxazole compounds are disclosed having activity against parasitic worms and showing little or no toxicity to the host animal. These compounds are 3-chloro-4-dialkylaminophthaloylamino-4,5-dihydroisoxazoles and 3-dialkylamino-4-dialkylaminophthaloylamino-4,5-dihydroisoxazoles. A process for making these compounds and a method of administering them to infested animals is also disclosed.

Abstract: Novel antibacterially-active esters of antibiotic nodusmicin. Activity is demonstrated against Staphylococcus aureus, Streptococcus pyogenes, and Sarcina lutea. Thus, these esters can be used in various known environments, using well-known procedures, to eradicate or control susceptible microbes.

Abstract: 4-Hydroxy-N-[5-[(substituted hetero)methyl]-3-isoxazolyl]-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxides as agents for treating pain in mammals resulting from inflammation.

Abstract: New (2-propynylamino)isoxazole and (3-iodo-2-propynylamino)isoxazole derivatives having anti-microbial activity which are used as active ingredients in anti-microbial compositions for medical use, for agricultural use and also for veterinary use.

Abstract: This invention concerns certain 3-(3- or 5-substituted-5- or -3-yl)-1-substituted-1-(2,2-substituted)ureas having herbicidal activity, and their use to control weeds.

Abstract: 7-[2-(3-Amino-5-isoxazolyl)-2-alkyloxyiminoacetamido]-ceph-3-em-4-carboxyli c acid derivatives are antibacterial agents effective against gram-positive and gram-negative bacterium.

Abstract: A process for the preparation of a urea derivative having the formula: ##STR1## in which A represents a straight- or branched-chain alkyl group having 1-20 carbon atoms, an aryl group, or a heterocyclic group, and each of R.sup.1 and R.sup.2 represents hydrogen, a straight- or branched-chain alkyl group having 1-20 carbon atoms, an alicyclic group, or an aryl groups, which comprises:reacting sodium salt of an N-halogenamide with a quaternary ammonium salt to obtain its addition salt and then,reacting said addition salt with an amine derivative in the absence or presence of an organic solvent.

Abstract: 1-Heterocyclic-2-pyrrolidinone analogs, and intermediates thereof, as aquatic and terrestrial herbicides and aquatic algicides. The compounds and intermediates can also be used together with one or more herbicides to provide useful terrestrial herbicidal combinations.

Abstract: Herbicidal isoxazolyl imidazolidinones are prepared by reaction of an isoxazolyl-allylurea with ozone and reduction.

Abstract: The invention relates to a guanidine derivative of the formula: ##STR1## in which W is a 2-6C alkylene chain optionally substituted by 1 or 2 1-4C alkyls; E is O, S, SO, SO.sub.2 or NR.sup.3 in which R.sup.3 is H or 1-6C alkyl; R.sup.1 is H or a straight chain 1-6C alkyl optionally substituted by 1 or 2 1-4C alkyls; or R.sup.1 and R.sup.3 are joined to form a morpholine, pyrrolidine, piperidine or piperazine ring; X, P, Y, Q and R.sup.2 are as defined in the specification, and the pharmaceutically-acceptable acid-addition salts thereof. Manufacturing process, pharmaceutical compositions and intermediates are also described. The compounds of the formula I are histamine H-2 antagonists.

Abstract: Amidines are one of the strongest organic bases and find application where this property is needed, such as in phase transfer catalysis in the form of their substituted derivatives. Their use, however, has been hampered by their expensive nature due to only mediocre yields in their preparation. The present invention provides a process for the preparation of substituted amidines in essentially quantitative yields.

Abstract: N-Substituted 2-methylnaphthylamides of the general formula ##STR1## where R.sup.1 is ##STR2## R.sup.3 being hydrogen or alkoxy, or R.sup.1 is ##STR3## R.sup.4 and R.sup.5 being unsubstituted or substituted alkyl, or R.sup.4 and R.sup.5 together forming a heterocyclic ring which contains two oxygen atoms and is unsubstituted or substituted by alkyl or aryl,R.sup.2 is alkyl which is unsubstituted or substituted by halogen, alkoxy, imidazolyl, pyrazolyl or oxo (.dbd.O), or is alkenyl, alkynyl, cycloalkenyl or alkoxy, or substituted or unsubstituted phenyl, or substituted or unsubstituted hetaryl andX is hydrogen, methyl or halogen, fungicides containing these compounds, and processes for the preparation of the compounds.

Abstract: Oxothia compounds, especially 2-oxo-2,3-dihydro-benzo[b]-thiophene compounds of the formula ##STR1## in which Ph represents an optionally substituted 1,2-phenylene radical, X represents oxygen or sulphur, R.sub.1 represents an organic radical bonded via a carbon atom and R.sub.2 denotes hydrogen or an optionally substituted hydrocarbon radical of aliphatic character, and their salts are useful as peripheral analgetics and/or as antiphlogistic uricosuric and/or thrombolytic agents.

Abstract: 7-[2-(3-Amino-5-isoxazolyl)-2-alkyloxy-iminoacetamido]-ceph-3-em-4-carboxyl ic acid derivatives are antibacterial agents effective against gram-positive and gram-negative bacterium.

Abstract: The herbicide 1-(5-t-butylisoxazol-3-yl)-3,3-dimethylurea is prepared in high yield and high purity by a multiple-step process without the isolation of intermediate products.

Abstract: Broad spectrum cephalosporin antibiotics represented by the formula, ##STR1## pharmaceutical compositions of the antibiotics, and a method for treating infections are provided. In the formula, R is 2-aminooxazol-4-yl, 5-amino-1,2,4-oxadiazol-3-yl or 5-aminoisoxazol-3-yl; R' is eg. C.sub.1 -C.sub.4 alkyl; R.sub.1 is H, NH.sub.2, chloro, C.sub.1 -C.sub.4 NH--, (C.sub.1 -C.sub.4).sub.2 N--, etc. The antibiotics are best prepared by reacting a pyrazine with a 3-iodomethyl cephalosporin.

Abstract: This invention relates to a new class of thienamycins (I) and their pharmaceutically acceptable salts and esters which are useful as antibiotics: ##STR1## wherein the stylized radical (hereafter referred to as R'): ##STR2## attached to the amino nitrogen group of thienamycin represents a mono- or polycyclic N-containing heterocyclic group; R is, inter alia, hydrogen, substituted and unsubstituted: alkyl, aryl, alkenyl, heterocyclylalkenyl, aralkenyl, heterocyclylalkyl, aralkyl, --NR.sub.2, COOR, CONR.sub.2, --OR, or CN.

Abstract: Bisamidines carrying one unsaturated nitrogen heterocyclo-containing substituent, representative of which i; 1-[N'-(2-(5-methyl-4-imidazolyl)methylthio)ethyl)guanidino]-8-[N'-methylgu anidino]octane, are histamine H.sub.2 -antagonists.

Abstract: The invention relates to guanidine derivatives, particularly to substituted guanidines of the formula ##STR1## having hypoglycaemic activity, for the oral treatment of hyperglycaemia in mammals, especially for the oral treatment of Diabetes mellitus.

Abstract: The present invention is directed to 1-(benzoyl)-3-(isoxazolyl or benzisoxazolyl)urea or thiourea compounds useful as insecticides.

Abstract: The present invention is directed to isoxazolyl and benzisoxazolyl benzamide compounds useful as insecticides.

Abstract: Chemical process for preparing AT-125 and its analogs and intermediates used in the process.

Abstract: Herbicidal compounds represented by the formula: ##STR1## wherein R is t-butyl; R.sup.1 is hydrogen or methyl; R.sup.2 is alkyl (C.sub.2 to C.sub.6), alkenyl (C.sub.3 to C.sub.4) or cyclopropyl; and X is hydrogen or halogen; and herbicidal compositions containing them.

Abstract: 3-Amino-5-(t-butyl)isoxazole, in optimum yield, is prepared in a stepwise manner by reacting a lower alkyl pivalate and acetonitrile in the presence of a base to yield pivalyl acetonitrile, which in turn is allowed to react with hydroxylamine under controlled conditions of pH to yield the desired compound. The compound is a useful intermediate for the preparation of isoxazole derivatives having utility as herbicides.

Abstract: 3-Amino-5-t-butylisoxazole is prepared by reacting pivaloylacetonitrile with hydroxylamine in aqueous medium under basic conditions and treating the reaction products with an acid. The process is economical and industrial.

Abstract: Chemical process for preparing AT-125 and its analogs and intermediates used in the process.

Abstract: The invention relates to a compound selected from the group consisting of compounds of the formula: ##STR1## in which R.sub.1, R.sub.2 and R.sub.3 are independently selected from hydrogen, halogen, trifluoromethyl, nitro, C.sub.1-4 alkoxy and C.sub.1-4 alkyl,R.sub.4 represents a heterocyclic radical selected from the radicals having the formulae ##STR2## in which R.sub.5 and R.sub.6 are independently selected from hydrogen, C.sub.1-4 alkyl, phenyl and halophenyl,R.sub.7 is selected from hydrogen and C.sub.1-4 alkyl, and a pharmaceutically acceptable acid addition salt thereof. These compounds are useful for the treatment of gastric ulcers.

Abstract: Novel amidoxime derivatives having the following structural formula (IV) or (IV'): ##STR1## wherein R.sub.1 represents methyl or ethyl group and R.sub.2 represents hydrogen or methyl group, useful as a raw material for 3-amino-5-methyl isoxazole, are prepared from .beta.-amino crotonitrile. Said isoxazole, useful as an intermediate for various medicines, may be prepared without producing any by-products of isomer.

Abstract: The present invention relates to compounds of the formula ##STR1## wherein A together with the two carbon atoms to which it is attached forms the group ##STR2## and the broken line represents the double bond in group (a); R.sub.1 represents a lower alkyl group; R.sub.2 represents the residue of an aromatic heterocyclic ring containing from 1 to 4 hetero atoms, which may be substituted by one or two lower alkyl groups, or a phenyl group which may be substituted by halogen, hydroxy, lower alkyl, trifluoromethyl or lower alkoxy and R.sub.3 and R.sub.4 each represent a hydrogen atom or a lower alkyl group.Also provided are methods for their preparation. The thienothiazine derivatives provided by this invention have anti-flammatory, analgesic and anti-rheumatic activity.

Abstract: 3-Isoxazolylurea derivatives of the formula: ##STR1## (wherein R represents hydrogen, C.sub.1 -C.sub.6 alkyl, or C.sub.6 -C.sub.8 aryl; R.sup.1 represents hydrogen or C.sub.1 -C.sub.6 alkyl; R.sup.2 represents C.sub.1 -C.sub.6 alkyl, C.sub.6 -C.sub.8 aralkyl, or C.sub.6 -C.sub.8 aryl; or ##STR2## represents pyrrolidino, piperidino, morpholino, or 4-alkylpiperazino; X represents hydrogen or halogen; or R and X may optionally form C.sub.3 -C.sub.5 alkylene), are prepared by reacting a carboxamide of the formula: ##STR3## (wherein R and X each is as defined above) with an amine of the formula:R.sup.1 --NH--R.sup.2(wherein R.sup.1 and R.sup.2 each is as defined above) in the presence of an alkaline hypohalite and an alkaline hydroxide in an inert solvent medium.

Abstract: 3-Aminoisoxazoles of the formula: ##STR1## (wherein R is C.sub.1 -C.sub.6 alkyl, phenyl or halo-phenyl) are prepared by reacting a .beta.-ketonitrile of the formula:R--CO--CH.sub.2 CN(wherein R is as defined above) with a compound of the formula:HY(wherein Y is C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 alkylthio) in the presence of an acid in a solvent to give an iminium salt of the formula: ##STR2## (wherein X is the residue of said acid; R and Y are each as defined above) and further reacting the iminium salt with hydroxylamine in an inert solvent.

Abstract: The compounds are N-(heterocyclomethylthioalkyl) derivatives of alkylguanidines, C-alkyl and C-aryl amidines and S-alkylisothioureas. The compounds may also have N'-lower alkyl or N'(heterocyclomethylthioalkyl) substituents. Three compounds of the invention are S-methyl-N-[2-(5-methyl-4-imidazolylmethylthio)ethyl]isothiourea, N,N'-bis-[2-(5-methyl-4-imidazolylmethylthio)ethyl]acetamidine, N,N'-bis-[2-(5-methyl-4-imidazolylmethylthio)ethyl]N"-methylguanidine. The compounds of this invention are histamine H.sub.2 -antagonists.

Abstract: Lower alkyl 2-chloro-2-hydroxyiminoacetates are produced by (A) reacting chloral with a lower alkanol and a hydroxylamine salt in the presence of a Lewis acid or a metal oxide which is convertible into said Lewis acid during the course of the reaction to give a lower alkyl 2-hydroxyiminoacetate and then chlorinating the resulting product or (B) reacting chloral oxime with a lower alkanol in the presence of a base to give a lower alkyl 2-hydroxyiminoacetate and finally chlorinating the thus formed product.

Abstract: Urea derivatives of the formula ##STR1## (wherein Ar represents a residue of 5- or 6-membered heteroaromatic ring; R represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group; R.sup.1 represents a C.sub.1 -C.sub.6 alkyl group; and R.sup.2 represents a C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, or C.sub.1 -C.sub.6 alkoxy group) are produced by reacting an amine of the formulaAr--NH--R(wherein Ar and R have the significance given above) with a carbamoyl halogenide of the formula ##STR2## (wherein X represents a halogen atom, and R.sup.1 and R.sup.2 have the significance given above) in the presence of a Lewis acid in an inert solvent.