Abstract: New pharmacologically active amidino and guanidino derivatives which are 5-HT.sub.3 receptor antagonists useful as antiemetic, gastric prokinetic and antimigrainic agents of the following general formula (I) ##STR1## , wherein the substituents are defined hereinbelow, which compounds are 5-HT.sub.3 receptor antagonists useful as antiemetic gastric prokinetic and antimigraine agents, inter alia.

Abstract: The present invention describes a group of polyhydroxylated indolizidines and quinolizidines and their esters. These compounds are prepared starting from 2,6-dideoxy-2,6-dideoxy-2,6-imino-1,3,4,5-tetrakis-O- (phenylmethyl)-D-glycero-L-gulo-heptitol or a corresponding N-substituted compound. The compounds are useful in the treatment of diabetes and as .alpha.-glucosidase I inhibitors.

Abstract: The object of the invention is a process for the preparation of derivatives of 3-sulfonyl indolizine of general formula: ##STR1## in which: R is selected from hydrogen, alkyl, cycloalkyl, substituted or unsubstituted phenyl,R.sub.1 is a protecting group for hydroxyl,R.sub.2 and R.sub.3, identical or different, is each selected from hydrogen, methyl or ethyl or halogen.These compounds are intermediates which can be used for the preparation of 3-aminoalkoxyphenylsulfonyl-indolizines, which are useful in the treatment of certain diseases of the cardiovascular system.

Abstract: A new compound, dioscoretine, as well as the process for making the same is described. According to a preferred embodiment, dioscoretine is derived from the tuber of Dioscorea dumetorum. Dioscoretine is a hypoglycemic agent and thus is useful for therapeutic treatment of conditions such as diabetes mellitus.

Abstract: Castanospermine mono- and di-esters and glycosides active as inhibitors of carbohydrate digestive enzymes and useful in treating diabetes are described herein. The compounds are prepared by the reaction of castanospermine with an appropriate acid halide or anhydride or with an appropriate glycosyl halide or glycosyl acetimidate under conditions which would favor the isolation of the mono- and di-esterified and glycosylated products. Various blocking groups, which can be selectively removed under mild conditions, can also be used to favor the formation of certain isomers.

Abstract: A compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 each is hydrogen, hydroxy, oxo, halogen, azido, amino, C.sub.1 -C.sub.3 alkylamino, or aminomethyl, in which said amino, C.sub.1 -C.sub.3 alkylamino and aminomethyl each is optionally substituted by one or two members selected from the group consisting of C.sub.1 -C.sub.3 alkyl and amino-protecting group; n is an integer of 1 to 3; p and q each is an integer of 0 to 3 with proviso that p+q=1 to 4 or acid-addition salts thereof, being useful materials for preparing side chains of antibacterial quinolonecarboxylic acids, cephalosporines, or other antibiotics.

Abstract: Disclosed are the compounds of formula I ##STR1## wherein R and R.sub.1 -R.sub.3 independently represent hydrogen or lower alkyl, and m represents the integer 2 or 3; their methods of preparation; pharmaceutical compositions thereof, and their use for treating cognitive disorders in mammals.

Abstract: Compounds of formula ##STR1## (wherein R, R.sub.1, R.sub.2 and Y have the meanings indicated in the description), a process for the preparation thereof and pharmaceutical compositions containing them as active ingredient are described.Compounds of formula I exhibit anto-serotonin activity.

Abstract: A 3-aryl-pyrrolidine-2,4-dione (e) derivative of the formula (I) ##STR1## in which X represents alkyl, halogen and alkoxy,Y represents hydrogen, alkyl, halogen, alkoxy and halogenoalkyl,Z represents alkyl, halogen and alkoxy,m represents a number from 1-4,n represents a number from 0-3, R represents hydrogen, ##STR2## or A where A represents a metal cation equivalent or represents an ammonium ion,R.sup.1 represents optionally halogen-substituted alkyl, alkenyl, alkoxyalkyl, alkylthioalkyl, polyalkoxyalkyl and optionally substituted cycloalkyl which can be interrupted by hetero atoms, or represents optionally substituted phenyl, optionally substituted phenylalkyl, substituted hetaryl, substituted phenoxyalkyl and substituted hetaryloxyalkyl andR.sup.2 represents optionally halogen-substituted alkyl, cycloalkyl, alkenyl, alkoxyalkyl, polyalkoxyalkyl and optionally substituted phenyl,as well as the pure enantiomeric forms of compounds of the formula (I).

Abstract: The invention concerns compounds of formula I ##STR1## or a salt thereof, wherein R.sup.1 and R.sup.2 each independently represent hydrogen, lower alkyl, lower alkoxy, carboxyloweralkyl, carboxy, hydroxyloweralkyl, halogen, haloloweralkyl, lower alkoxycarbonyl, optionally substituted aryl or optionally substituted aralkyl, n represents an integer from 3 to 6; R.sup.3 represents hydrogen or single or multiple substitution on one or more of the aliphatic carbons by one or more substituents selected from lower alkyl, optionally substituted aryl and optionally substituted aralkyl; A represents a group of formula (i) or (ii) below:--CR.sup.4 R.sup.5 --(CR.sup.6 R.sup.7).sub.m -- (i)--CX--(CR.sup.6 R.sup.7).sub.m -- (ii)in which R.sup.4, R.sup.6 and R.sup.7 each independently represent hydrogen or lower alkyl (providing that when R.sup.5 is NH.sub.2, R.sup.4 is hydrogen); m is O or 1; R.sup.5 represents hydrogen, NH.sub.2, OH or loweralkoxy, and X is .dbd.O, .dbd.NH or .dbd.

Abstract: An aminoalkoxyphenyl compound of formula ##STR1## as well as a pharmaceutically acceptable salt of this compound.

Abstract: The present invention provides a compound of formula I or a salt or prodrug thereof: ##STR1## wherein the dotted circle represents one or two double bonds in any position in the 5-membered ring;X, Y and Z independently represent oxygen, sulphur, nitrogen or carbon, provided that at least one of X, Y and Z represents oxygen, sulphur or nitrogen;A represents a group of formula II: ##STR2## in which R.sup.1 represents hydrogen, hydroxy, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.1-6 alkoxy, hydroxy(C.sub.1-6)alkyl, halogen, amino, cyano, --CONR.sup.6 R.sup.7 or --SO.sub.2 NR.sup.6 R.sup.7, in which R.sup.6 and R.sup.7 independently represent hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.2-6 alkynyl;R.sup.2 represents hydrogen, halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or C.sub.1-6 alkylcarbonyl;V represents nitrogen, ##STR3## and W represents oxygen, sulphur or ##STR4## in which R.sup.8 represents hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.

Abstract: A compound of the formula (I) ##STR1## where A is an alkylene or alkenylene group, R.sub.1 is an aryl group which may be substituted, R.sub.2 is a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a halogenated lower alkyl group, a cycloalkyl group, a lower alkoxyalkyl group, a lower alkylthioalkyl group, a phenyl group which may be substituted or an aralkyl group which may be substituted, R.sub.3 is a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group or a halogenated lower alkyl group, or R.sub.2 and R.sub.3 may be combined to form a group of --(CH.sub.2).sub.n --(n is 3 or 4), or salt thereof, which is useful as a herbicide.

Abstract: This invention provides bicyclic carboxylic esters and amides, their pharmaceutical formulations, and a method for their use in treating migraine, emesis, gastrointestinal disorders, schizophrenia, or anxiety in mammals.

Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein the various substituents are defined hereinbelow, having 5-HT.sub.3 receptor antagonist activity, processes for their preparation and their use as pharmaceuticals.

Abstract: 3-(2,3,4,5,6-pentafluorophenoxy)-8-azabicyclo[3.2.1]octanes and methods for treating depression, convulsions, pain, and hypertension utilizing compounds or compositions thereof are disclosed.

Abstract: N-(3-hydroxy-4-piperidinyl)substituted benzamides, their N-oxide forms and pharmaceutically acceptable acid-addition salts having gastrointestinal motility stimulating properties, compositions containing the same, and methods of treating warm blooded animals suffering from a decreased peristalsis of the gastrointestinal system.

Abstract: Compounds of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are, for example, H, alkyl, cycloalkyl, aryl or alkaryl are suitable as an ammonium salt-forming component for acid pharmaceutical active ingredients, and in particular for the preparation of azabicyclo[3.1.1.]heptane-substituted alkanediphosphonic acids for the treatment of diseases which can be attributed to disturbances in calcium metabolism.

Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt thereof:Y-CO-L-Z (I)whereinL is NH or O; Y is a group of formula (a), (b) or (c): ##STR1## wherein R.sub.1 and R.sub.2, R.sub.5 and R.sub.6, R.sub.9 and R.sub.10, are independently selected from hydrogen or halogen;X is N or CR.sub.3whereinR.sub.3 is hydrogen or C.sub.1-6 alkoxy;R.sub.4 is hydrogen, halogen, CH.sub.3, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkylsulphinyl, C.sub.1-7 acyl, cyano, C.sub.1-6 alkoxycarbonyl, C.sub.1-7 acylamino, hydroxy, nitro or amino, aminocarbonyl, or aminosulphonyl, optionally N-substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, and C.sub.3-8 cycloalkyl C.sub.1-4 alkyl or disubstituted by C.sub.4 or C.sub.5 polymethylene; phenyl or phenyl C.sub.1-4 alkyl group optionally substituted in the phenyl ring by one or two of halogen, C.sub.1-6 alkoxy or C.sub.1-6 alkyl groups;one of R.sub.7 and R.sub.8 is C.sub.

Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## in which A represents a bond or --CH.sub.2 -- and B represents hydrogen, or A and B together with the carbon atom to which they are both attached represents a group ##STR2## R represents R.sub.1 OOC-- in which R.sub.1 is C.sub.1-4 alkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkynyl; R.sub.2 O-- in which R.sub.2 is C.sub.1-3 alkyl, C.sub.1-2 alkylcarbonyl or aminocarbonyl optionally substituted by one or two methyl groups; or R.sub.3 CH.sub.2 - in which R.sub.3 is C.sub.1-2 alkoxy; and p represents an integer of 2 to 4, and wherein compounds of formula (I) where B is hydrogen have the stereochemical configuration in which the group R and the methylene bridge are both on the same side of the plane of the molecule which contains both bridge head atoms and the ring carbon atom bonded to the group R.

Abstract: The compounds of the invention comprise the condensation product, as well as derivatives thereof, of two equivalents of a trimethyl cyclohexane-anhydride acid chloride derivative with one equivalent of an aromatic diamine. The scope of the invention includes the method of using the compounds of the invention as chelating agents for metals, metal ions or ions of metal complexes. In a preferred embodiment of the invention the binding moieties of the cyclohexane derivatives are rigidly held opposite each other, by restricting their rotation about the N-C aryl bonds, in order to more effectively bind the metals or the ions.

Abstract: 3-(2,3,4,5,6-pentafluorophenoxy)-8-azabicyclo[3.2.1]octanes and methods for treating depression, convulsions, pain, and hypertension utilizing compounds or compositions thereof are disclosed.

Abstract: Compounds of the formula ##STR1## where R.sup.1 is lower alkyl, R.sup.2 is chlorophenyl, Y is alkylene, X is heterocyclic and Z is a fused ring are useful as antiinflammatory and antiallergy agents.

Abstract: An anthraquinone compound represented by formula: ##STR1## wherein R and X are as defined in the specification, and a polarizing film containing the same. The anthraquinone compound exhibits satisfactory compatibility with organic polymers and high dichroism, and the polarizing films have excellent performance characteristics.

Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## wherein L is NH or O;X is N or CR.sub.3 wherein R.sub.3 is hydrogen or C.sub.1-6 alkoxy;Y is N or CR.sub.4 wherein R.sub.4 is hydrogen, halogen, CF.sub.3, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkylsulphinyl, C.sub.1-7 acyl, cyano, C.sub.1-6 alkoxycarbonyl, C.sub.1-7 acylamino, hydroxy, nitro or amino, aminocarbonyl, or aminosulphonyl, optionally N-substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, and C.sub.3-8 cycloalkyl C.sub.1-4 alkyl or disubstituted by C.sub.4 or C.sub.5 polymethylene; phenyl or phenyl C.sub.1-4 alkyl group optionally substituted in the phenyl ring by one or two of halogen, C.sub.1-6 alkoxy or C.sub.1-6 alkyl groups;R.sub.1 and R.sub.2 are independently selected from hydrogen, or halogen;Z is a group of formula (a), (b) or (c): ##STR2## wherein n is 2 or 3; p is 1 or 2; q is 1 to 3; r is 1 to 3; andR.sub.5 or R.sub.

Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## wherein: Het is monocyclic heteroaryl having two adjacent carbon atoms, a and b, depicted in formula (I); p1 R.sub.1 and R.sub.2 are independently selected from hydrogen, halogen, CF.sub.3, C.sub.1-6 alkyl and C.sub.1-6 Alkoxy;R.sub.3 is hydroxy, C.sub.1-6 alkoxy, C.sub.3-7 alkenyl-methoxy, phenoxy or phenyl C.sub.1-4 alkoxy in which either phenyl moiety may be substituted by one or two C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halo; CO.sub.2 R.sub.6 wherein R.sub.6 is hydrogen or C.sub.1-6 alkyl, CONR.sub.7 R.sub.8 or SO.sub.2 NR.sub.7 R.sub.8 wherein R.sub.7 and R.sub.8 are independently hydrogen or C.sub.1-6 alkyl or together are C.sub.4-6 polymethylene, NO.sub.2, (CH.sub.2).sub.m OR.sub.9 wherein m is 1 or 2 and R.sub.9 is C.sub.1-6 alkyl or S(O).sub.n R.sub.10 wherein n is 0, 1 or 2 and R.sub.10 is C.sub.

Abstract: The dicarboxylic, heterocyclic and substituted benzoic acid alkylene bridged piperidyl amides and esters are serotonin M antagonists.

Abstract: The dicarboxylic, heterocyclic and substituted benzoic acid alkylene bridged piperidyl amides and esters are serotonin M antagonists.

Abstract: Nitrofuran derivatives of formula (I) ##STR1## in which n is 0 or 1 and R is a selected heterocyclic radical have useful antibacterial, antiparasitic and antifungal activity.

Abstract: The dicarboxylic, heterocyclic and substituted benzoic acid alkylene bridged piperidyl amides and esters are serotonin M antagonists.

Abstract: Polycyclic 1,3-dione imides N-alkylated with variously N-substituted alkyl- or cycloalkyl amines afford histamine H.sub.1 -receptor antagonists of the formula ##STR1## wherein R is polycyclic alkyl moiety;R.sup.1 is hydrogen or alkyl;R.sup.4 is an aromatic amine or a cycloalkyl amine containing N-substitution;R.sup.7 and R.sup.8 are hydrogen, alkyl or form a spiro cycloalkyl group.

Abstract: The invention relates to new anti-arrythmic azabicyclo[3.3.1]nonanes of the general formula (I) ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are C.sub.1-4 alkyl groups which are the same or different, or one of them is a benzyl group and the others are C.sub.1-4 alkyl groups, andR.sup.4 is a hydroxy group, or an etherified hydroxy group of the formula --OR.sup.5, or an esterified hydroxy group of the formula --OOCR.sup.6, in which the esterifying groupR.sup.5 is a phenyl or benzyl group which optionally each can have a trihalomethyl substituent or one or more halogen or C.sub.1-4 substituents, or is a diphenyl or benzhydryl group, and the esterifying groupR.sup.6 is a C.sub.1-8 alkyl or a C.sub.3-6 cycloalkyl group, or a phenyl or benzyl group which optionally each can have a halo-substituent or one or more C.sub.1-4 alkyl, C.sub.1-4 alkoxy, nitro or phenyl substituents, or is an optionally halogenated or hydrogenated naphthyl group, or a cinnamyl group optionally substituted by a halogen atom or C.sub.

Abstract: A process for producing pyridine-2,3-dicarboxylic acid derivatives of the formula ##STR1## is described. The process is based on the cleavage of HNR.sub.10 R.sub.11 from 1-amino-1,2,3,4-tetrahydropyridine-2,3-dicarboxylic acid derivatives of the formula II ##STR2## to give 1,4-dihydropyridine-2,3-dicarboxylic acid derivatives of the formula III ##STR3## and subsequent oxidation of these compounds to obtain pyridine-2,3-dicarboxylic acid derivatives of the formula I. According to one variant of the process, the 1,4-dihydropyridine-2,3-dicarboxylic acid derivatives of the formula III are obtained directly, without isolation of the intermediately formed 1-amino-1,2,3,4-tetrahydropyridine-2,3-dicarboxylic acid derivatives of the formula II, by reaction of .alpha.,.beta.-unsaturated hydrazones of the formula IV ##STR4## with ethene-1,2-dicarboxylic acid derivatives of the formula V ##STR5## and subsequently oxidized to pyridine-2,3-dicarboxylic acid derivatives of the formula I. In the above formulae, R.sub.1, R.

Abstract: The present invention provides a process for preparing a 2-substituted-1,4-dihydropyridine by providing a regiospecific bromine containing intermediate which is then reacted with a nucleophile to provide a wide range of substituents at the 2-position of 1,4-dihydropyridines. Also the present invention is novel 3-substituted-1,4-dihydropyridines having cardiovascular activity.

Abstract: The compounds of the invention comprise the condensation product, as well as derivatives thereof, of two equivalents of a trimethyl cyclohexane-anhydride acid chloride derivative with one equivalent of an aromatic diamine. The scope of the invention includes the method of using the compounds of the invention as chelating agents for metals, metal ions or ions of metal complexes. In a preferred embodiment of the invention the binding moieties of the cyclohexane derivatives are rigidly held opposite each other, by restricting their rotation about the N-C aryl bonds, in order to more effectively bind the metals or the ions.

Abstract: 1-phenyl-3-azabicyclo[3.1.1]-heptane-2,4-diones of the formula ##STR1## in which R.sub.1 represents hydrogen or a saturated or unsaturated, aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, aromatic or aromatic-aliphatic hydrocarbon radical having up to and including 18, preferably up to and including 12, carbon atoms, R.sub.2 represents hydrogen, lower alkyl, sulpho or acyl, R.sub.3 represents hydrogen or lower alkyl and R.sub.4 represents hydrogen, lower alkyl, phenyl or phenyl substituted by --N(R.sub.2)(R.sub.3), and salts of these compounds, have valuable pharmacological properties, are effective as aromatase inhibitors and can therefore be used for the treatment of hormone-dependent diseases, especially mammary carcinoma.

Abstract: A method of making dendrobatid alkaloids with the formula ##STR1## in which A is either CH.sub.3 or H, and n is an integer from 1-9, and R is CH.sub.2 OH, CHO, ##STR2## and R.sub.1 and R.sub.2 are alkyl groups; and the use of such alkaloids to treat cardiovascular illness.

Abstract: Octahydro-5-oxoindolizine-6-propanoic acids and octahydro-6-oxopyrido[1,2-a]pyridine-7-propanoic acids, the decarboxy and related ester and perhydro derivatives thereof inhibit angiotensin I converting enzyme and are hypotensive agents. Hydrogenation of A58365 factors A and B, obtained by culturing Streptomyces chromofuscus, provides the ACE inhibitors. Also provided are O-acyl and O-sulfonyl derivatives of A and B factors which are useful in preparing deoxy factors A and B via hydrogenolysis.

Abstract: 7.beta.-Acylamino-3-trifluoromethylsulfonyloxy-1-carba-3-cephem-4-carboxyli c acid antibiotic compounds, esters and salts thereof, and the corresponding 7-amino and protected 7-amino 1-carbacephalosporins are provided. The 3-trifluoromethylsulfonyloxy-substituted 1-carbacephalosporins also are useful in a process for preparing 3-halo-1-carbacephalosporins which comprises reacting a 3-triflate ester with a lithium halide in an aprotic polar solvent.

Abstract: Carbacephem compounds represented by the formula: ##STR1## [wherein R.sub.1 is a lower alkylsulfonyloxy, unsubstituted or substituted arylsulfonyloxy, azido, cyano, carbamoyloxy, unsubstituted or substituted heterocyclic thio ("heterocyclic" means a 5- or 6-membered heterocyclic group having 1 to 4 O, S or N atoms), unsubstituted or substituted lower alkylthio, or unsubstituted or substituted arylthio group; R.sub.2 and R.sub.3 are groups frequently used in the cephalosporin chemistry] have strong antibacterial activity against Gram-positive and Gram-negative bacteria, and are useful for curing various infections.

Abstract: Pyrazole sulfonylureas are expected to show pre- and post-emergence herbicidal activity. Specifically preferred in this class of compounds is N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-4,6-dihydro-2-methyl-4-oxo- 2H-furo[3,4-c]pyrazole-3-sulfonamide.

Abstract: Substituted 2-amino-4(1H)pyridones are provided which are renal vasodilators and bronchodilators.

Abstract: Octahydro-5-oxoindolizine-6-propanoic acids and octahydro-6-oxopyrido[1,2-A]pyridine-7-propanoic acids, the decarboxy and related ester and perhydro derivatives thereof inhibit angiotensin I converting enzyme and are hypotensive agents. Hydrogenation of A58365 factors A and B, obtained by culturing Streptomyces chromofuscus, provides the ACE inhibitors. Also provided are O-acyl and O-sulfonyl derivatives of A and B factors which are useful in preparing deoxy factors A and B via hydrogenolysis.

Abstract: Oxoindolizine and oxoindolizinium dyes are novel compounds useful in imaging, such as laser recording and reading. These dyes are formed by (1) the reaction of a cyclopropenone and a pyridine compound, (2) by reaction of (a) color-forming couplers with (b) reaction products from the reaction of cyclopropenones with pyridine compounds, or (3) by condensation reactions of indolizinols, indolizinones, and indolizinium ions.

Abstract: This invention relates to hexahydroindolizinones, which are useful as inhibitors of cardiac arrhythmias and of platelet aggregation and are therefore useful in the treatment of irregular heartbeat and in the prevention of thrombus formation.

Abstract: Compounds of formula (I): ##STR1## wherein X is methoxy or ethoxy, Y is amino or C.sub.1-6 alkanoylamino, Z is hydrogen, chloro or bromo and R.sub.1 is methyl, chloro or fluoro, have anti-psychotic activity, and are useful in the treatment of CNS disorders. Intermediates for the above compounds are also disclosed.

Abstract: .beta.-Lactam antibiotics having an .alpha.-formamido substituent on the carbon atom adjacent to the carbonyl group of the .beta.-lactam ring and in particular bicyclic compounds having the partial structure: ##STR1## Intermediates and processes for the preparation of the compounds are further disclosed.

Abstract: A compound of formula (1) or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof: ##STR1## wherein R.sup.1 is phenyl, substituted phenyl or a 5- or 6-membered heterocyclic ring containing up to three heteroatoms selected from oxygen, sulphur or nitrogen, optionally substituted with hydroxy, amino, halogen or C.sub.1-6 alkoxy;X represents; ##STR2## wherein R.sup.Y is methyl or acetyl; R.sup.2 and R.sup.3 may be the same or different and each is hydrogen, an aryl group, a heterocyclyl group or a C.sub.1-6 alkyl group optionally substituted by an aryl group or a heterocyclyl group; and R.sup.4 is hydrogen, a C.sub.1-6 alkylcarbonyl group, an aryl group, a heterocyclyl group, a C.sub.1-6 alkyl group optionally substituted by an aryl group or a heterocyclyl group;R.sup.5 represents, hydrogen, methoxy or --NHCHO; and Y is: ##STR3## wherein Y.sup.1 is oxygen, sulphur or --CH.sub.2 -- and Z represents hydrogen, halogen or an organic group such as C.sub.1-4 alkoxy, --CH.sub.2 Q or --CH.dbd.

Abstract: X is in the 8 position and is O(CH.sub.2).sub.n, N(CH.sub.2).sub.n ;Y is O(CH.sub.2).sub.n, N(CH.sub.2).sub.n ;R.sub.2 is monosubstituted or independently disubstituted H, carboxyl, or alkylcarboxy;Z is 0; andn is 0 to 10 inclusive,useful in the treatment of ischemic heart disease and hypertriglyceridemia.

Abstract: A novel process for the preparation of 2-(5,5-disubstituted-4-oxoor thiono)-2-imidazolin-2-yl)nicotinic acids, quinoline-3-carboxylic acids and benzoic acids by the base-catalyzed cyclization of appropriately substituted 2-carbamoyl nicotinic acids, 3-quinolinecarboxylic, or benzoic acids. The products are useful as herbicides.