Abstract: The cyclic amide derivative is defined by the formula (I) or a salt thereof: R1--(CH2)n-z in which R1 is a group derived from a cyclic amide compound, substituted or unsubstituted, n is zero or an integer of 1 to 10 and Z is ##STR1## R2 being an aryl, a substituted aryl, a cycloalkyl or a heterocyclic group, m being an integer of 1 to 6, R3 being hydrogen or a lower alkyl, R4 being an aryl or a substituted aryl, a cycloalkyl or a heterocyclic group, p being an integer of 1 to 6, provided that the cyclic amide compound is quinazoline-on or quinazoline-dion, R2 and R4 are neither aryl nor substituted aryl. The cyclic amide compound is pharmacologically effective to prevent and treat diseases due to insufficiency of the central choline functions.

Abstract: The invention concerns a bicyclic heterocyclic compound of the formula I ##STR1## wherein Q is an optionally substituted 10-membered bicyclic heterocyclic moiety containing 1 or 2 N's and a further O or S heteroatom;A.sup.1 is a direct link to X.sup.1 or (1-3C)alkylene;X.sup.1 is oxy, thio, sulphinyl, sulphonyl or imino;Ar is optionally substituted phenylene or pyridylene;R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- which, together with the carbon atom to which A.sup.2 and A.sup.3 are attached, defines a ring having 5 to 7 ring atoms, wherein each of A.sup.2 and A.sup.3 is (1-3C)alkylene and X.sup.2 is oxy, thio, sulphinyl or sulphonyl; or a pharmaceutically-acceptable salt thereof.The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.

Abstract: The invention relates to substituted 2-pyrimidinyl-1-piperazine derivatives defined herein by formula (I), processes for their manufacture, compositions containing said substituted 2-pyrimidinyl-1-piperazine derivatives as active materials and the use of said compounds and compositions as agents effecting the central nervous system. Also included in the invention are intermediates of formula (VIII) for making the active formula (I) compounds.

Abstract: Cycloalkanecarboxylic acid derivatives of formula I ##STR1## wherein W is ##STR2## and A is CO--R.sub.3 or CN; R.sub.1 is hydrogen or fluorine; R.sub.2 is halogen or cyano; R.sub.3 is chlorine, X--R.sub.5, amino, C.sub.1 -C.sub.4 alkylamino, d-C.sub.1 -C.sub.4 alkylamino, C.sub.2 -C.sub.4 haloalkylamino, di-C.sub.2 -C.sub.4 haloalkylamino, C.sub.1 -C.sub.4 hydroxyalkylamino, di-C.sub.1 -C.sub.4 hydroxyalkylamino, C.sub.3 -C.sub.4 alkenylamino, diallylamino, --N-pyrrolidino, --N-piperidino, --N-morpholino, --N-thiomorpholino, --N-piperidazino, the group --O--N.dbd.C--(R.sub.9)R.sub.10 or the group --N--R.sub.6 (OR.sub.6); each of R.sub.4 and R.sub.14, independently of the other, is hydrogen, fluorine, chlorine, bromine, C.sub.1 -C.sub.4 alkyl or trifluoromethyl; R.sub.5 is hydrogen, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.4 alkoxy-C.sub.1 -C.sub.4 alkyl, halo-C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.10 alkylthio-C.sub.1 -C.sub.4 alkyl, di-C.sub.1 -C.sub.4 alkylamino-C.sub.1 -C.sub.4 alkyl, cyano-C.sub.1 -C.sub.

Abstract: Combating unwanted vegetation with N-phenyl-substituted oxazinediones of the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 can each be hydrogen or an organic radical or R.sup.2 and R.sup.3 and/or R.sup.6 and R.sup.7 can form a ring, andQ is oxygen or sulphur.Those compounds are new wherein at least three of the radicals R.sup.1 to R.sup.5 are other than hydrogen or the two radicals R.sup.2 and R.sup.3 together represent --O--CH.sub.2 --O--CH.sub.2 -- or the group --X--(CO).sub.n --A--Y--.

Abstract: There are described compounds of the formula ##STR1## where X is hydrogen, loweralkyl, loweralkoxy or halogen;R when present is hydrogen, loweralkyl or aryloweralkyl;R.sub.1 is hydrogen, loweralkyl or arylloweralkyl; andR.sub.2 when present is hydrogen or loweralkyl;which compounds are useful for alleviating various memory dysfunctions characterized by a decreased cholinergic function such Alzheimer's disease.

Abstract: Quinolonecarboxylic acid intermediates useful in the preparation of antibacterial 6-fluoro-7-substituted-quinolonecarboxylic aids are prepared from 2-(iodo, bromo or chloro)-3-fluoro-4-(fluoro or chloro)-phenyl carboxylic acid or ester.

Abstract: A process to prepare compounds of formula I ##STR1## in which n=0, 1 or 2 comprising the cyclisation of compounds of formula II ##STR2## in which n=0, 1 or 2. The cyclisation may be effected in the presence of an organic or inorganic base or thermally at a temperature in the range 40.degree.-160.degree. C.Compounds of formula II and certain analogues thereof are disclosed as cardiovascular agents.

Abstract: The invention relates compounds of the formula ##STR1## wherein R.sup.1 -R.sup.5 and X have the significance given in the description, and their pharmaceutically acceptable salts. The compounds of formula I inhibit the enzyme collagenase and can be used in the form of medicaments for the control or prevention of degenerative joint diseases such as rheumatoid arthritis and osteoarthritis.

Abstract: The invention relates to substituted 2-pyrimidinyl-1- piperazine derivatives defined herein by formula (I), processes for their manufacture, compositions containing said substituted 2-pyrimidinyl-1-piperazine derivatives as active materials and the use of said compounds and compositions as agents effecting the central nervous system. Also included in the invention are intermediates of formula (VIII) for making the active formula (I) compounds.

Abstract: The invention relates to substituted 2-pyrimidinyl-1-piperazine derivatives defined herein by formula (I), processes for their manufacture, compositions containing said substituted 2-pyrimidinyl-1-piperazine derivatives as active materials and the use of said compounds and compositions as agents effecting the central nervous system. Also included in the invention are intermediates of formula (VIII) for making the active formula (I) compounds.

Abstract: Haloisatoic anhydrides are prepared by halogenating appropriately unsubstituted isatoic anhydrides with elemental chlorine or bromine in the presence of chlorosulfonic acid at from -10.degree. C. to +100.degree. C. using not less than 0.5 mole of halogen per mole of isatoic anhydride.

Abstract: The invention relates to substituted 2-pyrimidinyl-1-piperazine derivatives defined herein by formula (I), processes for their manufacture, compositions containing said substituted 2-pyrimidinyl-1-piperazine derivatives as active materials and the use of said compounds and compositions as agents effecting the central nervous system. Also included in the invention are intermediates of formula (VIII) for making the active formula (I) compounds.

Abstract: The adducts of isocyanates wtih benzoxazolones or benzoxazinediones are novel compounds which may be employed as blocked isocyanates and are particularly useful as latent, epoxide curing agents. At typical epoxide curing temperatures, the isocyanate is oxirane or hydroxyl reactive and the benzoxazole or benzoxazinedione acts like a di- or trifunctional phenol, respectively.

Abstract: Compounds which, in one of the possible tautomeric forms and as free acidic compounds, are of the general formula I ##STR1## where R is unsubstituted or substituted alkyl, alkoxy, cycloalkoxy or aryloxy and the ring A may be further substituted, are prepared by a process in which a compound of the formula II ##STR2## where X is hydrogen or an alkoxycarbonyl group and R has the above meanings with the exception of unsubstituted or substituted alkyl, is converted in an alcoholate-containing solution, and the product is then acidified.The compounds prepared according to the invention are useful intermediates for the preparation of dyes.

Abstract: The invention relates to pharmaceutical compositions containing active ingredients of Formula (I) and methods for the use of said compositions to treat cardiac insufficiencies. Also included in the invention are methods of the manufacture of said active ingredients of Formula (I). The invention includes, additionally, compounds of Formula (I).

Abstract: 2-Nitro-4-(4-pyridinyl)benzoic acids, such as 2-nitro-4-(4-pyridinyl)benzoic acid, are prepared by oxidizing the appropriate 4-(4-alkyl-3-nitrophenyl)pyridine with, e.g., potassium permanganate or nitric acid. The products are particularly useful in the preparation of antibacterial 1-alkyl-1,4-dihydro-4-oxo-7-pyridinyl-3-quinolinecarboxylic acids.

Abstract: 4-(3-Aminophenyl)pyridines, useful in the preparation of 1-alkyl-1,4-dihydro-4-oxo-7-pyridinyl-3-quinolinecarboxylic acids, are prepared by heating a 2-amino-4-(4-pyridinyl)benzoic acid at decarboxylation temperatures.

Abstract: 4-(4-Pyridinyl)isatoic anhydrides are prepared by reacting a 2-amino-4-(4-pyridinyl)benzoic acid, i.e., an acid, ester, or salt, with phosgene, preferably gaseous phosgene. The products are particularly useful in the preparation of antibacterial 1-alkyl-1,4-dihydro-4-oxo-7-pyridinyl-3-quinolinecarboxylic acids.

Abstract: N-alkyl-4-(4-pyridinyl)isatoic anhydrides are prepared by alkylating a 4-(4-pyridinyl)isatoic anhydride, suitably in the presence of sodium hydride and N,N-dimethylformamide. The products are particularly useful in the preparation of antibacterial 1-alkyl-1,4-dihydro-4-oxo-7-pyridinyl-3-quinolinecarboxylic acids.

Abstract: Quinolinone derivatives of the formula (I) ##STR1## in which X represents oxy or a direct bond, R.sub.1 represents an aliphatic, cycloaliphatic, aromatic, araliphatic, heterocyclic or heterocyclic-aliphatic radical or hydrogen, Ph represents an optionally additionally substituted 1,2-phenylene radical containing the group R.sub.1 --X--C(O)--, and one of the radicals R.sub.2 and R.sub.3 represents an optionally esterified or amidated carboxy group R.sub.4 and the other represents hydrogen or an aliphatic radical or, in the case of a radical R.sub.3, hydroxy, and in which either R.sub.A and R.sub.B together represent oxo, R.sub.C and R.sub.D together represent an additional bond, or, when R.sub.2 represents a radical R.sub.4, R.sub.C is hydrogen and R.sub.3 and R.sub.D together represent oxo, and R.sub.E represents a radical R.sub.5 which represents hydrogen or an aliphatic, cycloaliphatic, araliphatic heterocyclic-aliphatic radical, or R.sub.A represents an optionally etherified hydroxy group and R.sub.

Abstract: Ammonium salts of fluorophthalamic acids characterized by the formula ##STR1## wherein n is 1 or 2, are prepared by the steps of (A) reacting a chlorophthalic anhydride of the formula ##STR2## where n is as defined previously, with potassium fluoride or cesium fluoride to form a fluorophthalic anhydride of the formula ##STR3## where n is as previously defined, and (B) reacting the fluorophthalic anhydride with ammonium to form an ammonium salt of a fluorophthalamic acid.

Abstract: Fluorophthalamic acids characterized by the formula ##STR1## wherein n is 1 or 2, are prepared by the steps of(A) reacting a chlorophthalic anhydride of the formula ##STR2## where n is as defined previously, with potassium fluoride or cesium fluoride to form a fluorophthalic anhydride of the formula ##STR3## where n is as previously defined, and (B) reacting the fluorophthalic anhydride with ammonia to form an ammonium salt of a fluorophthalamic acid, and(C) acidifying the ammonium salt to form a fluorophthalamic acid.

Abstract: Preparation of a compound of the following formula (I): ##STR1## wherein R.sup.1 is alkyl of 1 to 12 carbons, from the compound of the following formula (II): ##STR2## by the steps of coupling (II) with 3,4-dichlorobenzotrifluoride; reacting the --NH.sub.2 and COOH groups with a COX.sub.2 compound, X being a leaving group, to produce a heterocycle; opening the heterocycle with an alkanesulphonamide; and oxidizing the resultant --NH.sub.2 group to an --NO.sub.2 to yield a compound of formula (I). Novel intermediates are also described. Compounds of formula (I) are useful as selective pre- and post-emergent herbicides.

Abstract: A process for the continuous preparation of isatoic anhydrides by two-stage reaction of an alkali metal phthalamate and/or alkali metal phthalimidate with an alkali metal hypohalite, the first stage being carried out substantially adiabatically and both stages being carried out at high flow rates, wherein phthalimide and/or phthalamic acid is first dissolved in a certain amount of an alkali metal hydroxide solution, the resulting solution is mixed with a hypohalite and reacted at a particular temperature, acid is then added and the reaction is completed at a particular temperature. The compounds obtainable by the process of the invention are valuable starting materials for the preparation of dyes, crop protection agents and scents.

Abstract: A mixture of an alkyl 3-chloroanthranilate and an alkyl 6-chloroanthranilate, with a particular molar ratio of the components, is prepared by (a) reacting 3-chlorophthalic anhydride with ammonia, an alkali metal hydroxide and an alkali metal hypochlorite or (b) converting 3-chlorophthalic anhydride to 3-chlorophthalimide followed by reaction of the latter with an alkali metal hydroxide and an alkali metal hypochlorite, and, finally, esterifying the mixture of 5-chloroisatoic anhydride and 8-chloroisatoic anhydride, obtained by method (a) or method (b), with an alkanol.The compounds obtainable by the process of the invention are valuable starting materials for the preparation of dyes, crop protection agents and scents.

Abstract: Simple arenes, aryl alcohols, aryl acids and aryl amides are reacted with an electrophilic thallium salt to provide arylthallium intermediates; and thereafter, the arylthallium compound is directly carbonylated by reacting with carbon monoxide in the presence of a noble metal carbonylation catalyst, such as palladium halide salts. The carbonylation reaction provides an excellent yield at room temperature and atmospheric pressure and is catalytic with respect to the noble metal salt.

Abstract: The N-m-trifluoromethylphenylanthranilates of O-alcoxycarbonylphenyl, having the formula ##STR1## wherein R is an alkyl group, preferably comprising 1 to 4 carbon atoms, besides being of low toxicity, are endowed with anti-inflammatory properties and are adapted for the treatment of inflammatory and thrombotic diseases. The method for the preparation of the above compounds comprises reacting the N-m-trifluoromethylphenylisatoic anhydride with an alkyl salicylate.

Abstract: This invention relates to compounds having the formula: ##STR1## in which R.sub.1 and R.sub.2 are independently hydrogen, a C.sub.1-4 alkyl group or an aliphatic or aromatic acyl group, provided R.sub.1 and R.sub.2 are not simultaneously hydrogen, or, together with the nitrogen atom to which they are attached, R.sub.1 and R.sub.2 form a 5- or 6-membered ring which may carry another heteroatom; R.sub.3 is a C.sub.1-4 alkyl group; and R.sub.4 and R.sub.5 represent independently a hydrogen or halogen atom, a C.sub.1-4 alkyl group or a C.sub.1-4 alkoxy group; and the acid addition salts of the above compounds. Said new compounds have an anxiolytic and diuretic action, together with a spasmolytic action of non-.alpha.-adrenalytic nature on the unstriated muscle fibers.

Abstract: Covers certain aromatic-amine amides which comprise the reaction product of a polyoxypropylene polyamine selected from the group consisting of diamines, triamines and mixtures thereof, and having an average molecular weight of 190 to about 3000 and an isatoic anhydride of the formula: ##STR1## where R is selected from the group consisting of hydrogen, alkyl, nitro, halo, hydroxy, amino, and cyano, and n is a number of 1-4. Also covers the use of said compounds as chain-extenders in polyurethane compositions. Such chain-extenders provide for the production of polyurethane elastomers having improved tensile strength, tear strength and elongation properties.

Abstract: 3,4-Dihydro-4-oxo-quinazoline derivatives substituted in the 2-position by a substituted phenyl group are disclosed. The derivatives possess anti-allergy properties and can be used for the treatment of allergic conditions.

Abstract: 2-Amino-3-pyridyl (or phenyl) nitromethylketones are prepared eg by reacting a 3,4-dihydro-1,3-dioxo-1H-pyrido [2,3-d][1,3]oxazine (a 3-azaisatoic anhydride) with the carbanion resulting from the reaction of nitromethane with a porton abstracting agent. The compounds are useful as anti-allergic agents.

Abstract: Substituted 3-(2-pyridinyl)-4(1H)-quinolinone N-oxides having the formula I: ##STR1## wherein R.sub.1 is hydrogen, halogen, lower alkyl, hydroxy or alkoxy; R.sub.2 is hydrogen or lower alkyl; R.sub.3 is hydrogen or --CH.sub.2 OH; the dotted line indicates the possible presence of a double bond at the 2,3-position of the quinoline ring; the pharmaceutically acceptable acid addition salts thereof; and a process for the preparation thereof, are described. The compounds of the invention are useful for the treatment of hyperacidity and for the prevention of allergic and asthmatic reactions.

Abstract: Anti-allergic 2-amino-quinolin-4-one-3-phosphonic acid esters are prepared by reacting an isatoic anhydride with the carbanion resulting from the treatment of an organo-methane phosphate with a proton abstracting agent.

Abstract: The invention relates to novel 1-(4-R.sub.1 O-phenyl)-2-(4-R.sub.2 -phenyl)-6-R.sub.3 -1,2,3,4-tetrahydroquinolines having antifertility and hypocholesterolemic activities, to their preparation, and to novel intermediates therefor.

Abstract: 1-Substituted-2-(2-pyridinyl)ethanone N-oxides having the formula I or II: ##STR1## wherein R.sub.1 is hydrogen or lower alkyl; R.sub.2 and R.sub.3 are each hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy, or benzyloxy; R.sub.4 is halogen, hydroxy, lower alkyl, lower alkoxy, benzyloxy, ortho-amino, ortho-lower alkylamino, ortho-alkanoylamino or ortho-benzoylamino; and R.sub.5 is hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy or benzyloxy; the pharmaceutically acceptable acid addition salts thereof, and a process for the preparation thereof, are described. The compounds of this invention are useful for the treatment of allergic conditions and for the treatment of hyperacidity.