Abstract: Compounds of the formula I ##STR1## where X is hydrogen, halogen, alkyl, alkoxy, trifluoromethyl, cyano or nitro,Y is an amino, methylamino or dimethylamino group,Z is a group CHCH.sub.3, CHOCH.sub.3 or NOCH.sub.3,R is hydrogen or alkyl,A is hydrogen, alkyl, haloalkyl or cycloalkyl,B is unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocyclyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl or the group ##STR2## where W is hydrogen, alkyl, alkoxy, alkylthio, alkylamino or dialkylamino, unsubstituted or substituted aryl or heteroaryl, unsubstituted or substituted aryloxy, arylthio, arylamino or aryl-N-(C.sub.1 -C.sub.6 -alkyl)amino, heteroaryloxy, heteroarylthio, heteroarylamino or heteroaryl-N-(alkyl)amino orA and B, together with the C atom whose substituents they are, are an isocyclic or heterocyclic ring which can also be quinonoid,and fungicides containing these compounds.

Abstract: The present invention refers to the use of 5-methyltetrahydrofolic acid, of 5-formyltetrahydrofolic acid and of their pharmaceutically acceptable salts for the preparation of controlled release pharmaceutical compositions suitable for the use in the therapy of depressive disturbances, in particular major depression, dysthymia or depressive neurosis and not otherwise specified depressive disturbances, independently from folate plasmatic levels, and to the pharmaceutical composition thus prepared.

Abstract: The present invention relates to a compound of the formula ##STR1## and the pharmaceutically acceptable salts thereof wherein W is a bicyclic heterocyclic ring system. The compounds are .alpha.-1 adrenergic antagonists and are useful in the treatment of BPH; also disclosed are .alpha.-1 antagonist compositions and a method for antagonizing .alpha.-1 receptors and treating BPH.

Abstract: Compounds having the formula I: ##STR1## are antagonists of the actions of leukotrienes. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.

Abstract: The present invention is directed to compounds of formula (I), ##STR1## wherein R.sup.1 is OH, NH.sub.2 ; R.sup.2 is a heteroaromatic or aromatic substituent; R.sup.3 is H, OH, F, OCH.sub.3 ; R.sup.4 is H, F, OH or an ether or ester residue thereof, OCH.sub.3, CN, C.dbd.CH, N.sub.3 ; R.sup.5 is OH or an ether or ester residue thereof including mono, di- and triphosphate esters (.alpha.), wherein n is 0 or 1 and M is hydrogen or a pharmaceutically acceptable counterion such as sodium, potassium, ammonium or alkylammonium; and pharmaceutically acceptable salts thereof; and pharmaceutical compositions comprising said compounds can be used for therapeutic treatment of virus infections. The present invention is also directed to compounds of formula (I'), ##STR2## wherein R.sup.1 and R.sup.2 are as defined above, as intermediates.

Abstract: The invention relates to N-sulfonyl derivatives of formulae (I) and (I)' ##STR1## to their preparation, and to pharmaceutical compositions in which they are present. The compounds of formulae (I) and (I)' have an affinity for the vasopressin and ocytocin receptors.

Abstract: Cephalosporins derivatives having a 3-position substituent of the formula I are described: ##STR1## wherein R.sup.1 is hydrogen, alkenyl or optionally substituted alkyl, Het is a 5- or 6-membered heterocyclic ring bonded via a carbon atom to the amide linkage, wherein Het is selected from a group of the formulae II-III: ##STR2## wherein A is CH or a nitrogen atom; B is oxygen, sulphur or a group NR.sup.4 ; one or two of D, E, F and G are nitrogen atoms and the remainder are CH groups: or Het is a pyrazinone, pyridinone, pyridazinone or pyrimidinone ring, or is a thione equivalent of such a ring, said rings having a substituent R.sup.4 on one nitrogen atom, or is pyranone, or pyranthione; the ring Het being fused by any two adjacent carbon atoms to the benzene ring; and Het being attached to the --CH.sub.2 NR.sup.1 CO-- group via a carbon atomR.sup.2 is hydroxy or an in vivo hydrolysable ester thereof;R.sup.3 is ortho to R.sup.2 and is hydroxy or an in vivo hydrolysable ester thereof; and R.sup.

Abstract: An acrylic acid compound useful for fungicides is provided. The compound has the following formula (I) ##STR1## wherein X represents a phenyl group which may be substituted, or a methylene group, n represents 0 or 1, Y represents an oxygen atom or a sulfur atom, Z represents a phenyl group, an aralkyl group, an aromatic heterocyclyl group or an aromatic heterocyclylmethylene group and Z may be substituted.

Abstract: Fluorogenic chelators for Eu.sup.3+ and Tb.sup.3+ are provided, they form highly fluorescent complexes with Eu.sup.3+ and Tb.sup.3+. In all cases, the fluorescence observed was lanthanide-specific, long-lived and it was monitored by microsecond time-resolved fluorometry. The fluorogenic chelators could be quantified, in the presence of excess lanthanide, at levels <10.sup.-8 mol/L. Two new fluorogenic chelators can form ternary complexes with Eu.sup.3+ and Tb.sup.3+, in the presence of EDTA. The structures of the identified chelators is such that enzyme substrates can be used for enzyme-labelled time-resolved fluorometric immunoassays. The chelator 4-methylumbelliferyl phosphate which forms fluorescent, long-lived complexes with Eu.sup.3+, can be split by alkaline phosphatase to phosphate and 4-methylumbelli-ferone which does not form fluorescent complexes with Eu.sup.3+. Highly sensitive immunoassays for thyrotropin and thyroxine in human serum are demonstrated.

Abstract: Compounds of formula I, and pharmaceutically acceptable salts thereof, ##STR1## in which R1 is hydrogen (1-6C)alkyl or (1-4C)alkanoyl;A is --N.dbd.CQ--O--, N.dbd.CQ--NR.sup.8 --, --N.dbd.CQ--CH.dbd.N--or --N.dbd.CH--CQ.dbd.N--;Q is 2-furyl;R.sup.8 is hydrogen or C1-4C)alkyl;and R.sup.2 has any of the meanings given in the specification, processes for preparing the compounds and pharmaceutical compositions containing them. The compounds are useful as adenosine antagonists.

Abstract: Novel substituted fused pyrimidinones of formula (I) are useful as angiotensin II antagonists.

Abstract: Novel substituted fused pyrimidinones of formula (I), which are useful as angiotensin II antagonists, are disclosed.

Abstract: Substituted 1,2,4-triazolo[1,5-c]pyrimido[1,4]azines have been found to have potent bronchodilator activity. Pharmacological methods for inducing bronchodilation using such compounds, pharmaceutical compositions containing such compounds, and synthetic intermediates for preparing such compounds are also described.

Abstract: This invention relates to certain herbicidal thiadiazoloazines, agriculturally suitable compositions thereof and a method for their use as a general or selective preemergent or postemergent herbicide or as a plant growth regulant.

Abstract: There are disclosed certain 6-piperazinopurines and heteroaromatic derivatives thereof which have oral hypoglycemic acitivity and with such ability to lower blood sugar are useful in the treatment of type II diabetes and/or obesity with associated insulin resistance. Processes for the preparation of such compounds and compositions containing such compounds as the active ingredient thereof are also disclosed.

Abstract: Certain piperazinylpyrimidines have pronounced .beta.-adrenergic blocking properties and some of the compounds are particularly useful in the treatment of elevated intraocular pressure and glaucoma.

Abstract: A class of novel 5H-1,3,4-thiadiazolo[3,2-a]-pyrimidin-5-one derivatives are disclosed. These compounds exhibit remarkable fungicidal activities for pathogenic fungi of cucumber gray mold, cucumber downy mildew. Alternaria sooty spot of Chinese mustard, apple Alternaria leaf spot, pear black spot, rice blast, tomato late blight, etc.

Abstract: Novel purine derivatives, particularly novel guanines and hypoxanthines, are described as agents for treating autoimmune diseases. Also novel methods of manufacture for the derivatives, pharmaceutical compositions thereof, and methods of use therefor are the invention.

Abstract: Novel 1-alkyl substituted benzimidazole derivatives 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: The invention relates to sulfonylurea compounds with a substituted or unsubstituted bicyclic nine-membered ring having one to five heteroatoms which are preemergent and/or postemergent herbicides or plant growth regulants.

Abstract: Novel tricyclic triazolopyrimidine compounds represented by formula (I) shown in the specification and physiologically acceptable salts thereof are disclosed. These compounds have an excellent anti-allergic activity and are useful for treatment and prophylaxis of allergic diseases.

Abstract: A compound of the general formula ##STR1## wherein R.sub.1 is a phenyl group which may be substituted, R.sub.2 and R.sub.3 respectively are a lower alkyl or lower alkoxy group, Z is CH or N and n is 0 or 1, or a salt thereof which is useful as a herbicide.

Abstract: 7,8-Dihydro-4-(1-piperazinyl)-6H-thiopyranopyrimidines have .beta.-adrenergic blocking properties and are thus useful in the treatment of cardiovascular ailments known to be amenable to .beta.-blocker therapy. Certain of the compounds are useful in the treatment of elevated intraocular pressure by topical ocular administration.

Abstract: Novel compounds of the formula: ##STR1## wherein R.sub.1 is a pyrazolyl group which may be substituted; R.sub.2 and R.sub.3 respectively are a lower alkyl group or a lower alkoxy group; and Z is CH or N, which are useful as herbicides.

Abstract: A class of novel 5H-1,3,4-thiadizaolo[3,2-a]pyrimidin-5-one derivatives are disclosed. These compounds exhibit remarkable fungicidal activities for pathogenic fungi of cucumber gray mold, cucumber downy mildew, Alternaria sooty spot of Chinese mustard, apple Alternaria leaf spot, pear black spot, rice blast, tomato late blight, etc.

Abstract: This invention relates to novel heterocyclic carbonyl sulfonamides which are particularly useful as agricultural chemicals.

Abstract: Novel substituted N-[(4-piperidinyl)alkyl] bicyclic condensed oxazol- and thiazolamines useful as anti-depressives, in the treatment of Parkinson's disease and in the treatment of diseases related with disturbed enterokinesia.

Abstract: A process for the preparation of a dimeric aromatic acyl cyanide of the formula ##STR1## in which Ar is optionally substituted phenyl, naphthyl or hetaryl,comprising reaction an acyl halide of the formulaAr--CO--Halin whichHal is fluorine, chlorine or bromine, with an alkali metal cyanide in a two-phase system comprising water and a water-immiscible or only sparingly water-miscible aliphatic ketone, and in the presence of a phase-transfer catalyst. The products are known intermediates for pesticides.

Abstract: Novel substituted N-[(4-piperidinyl)alkyl] bicyclic condensed oxazol- and thiazolamines useful as anti-depressives, in the treatment of Parkinson's disease and in the treatment of diseases related with disturbed enterokinesia.

Abstract: Sulfonamides such as N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-1,3-dihydro-6-methyl-3-oxof uro[3,4-c]pyridine-4-sulfonamide are useful as herbicides and plant growth regulants.

Abstract: Chloromethyl group substituted heterocyclic compounds of the formulae ##STR1## wherein X is O or S;Y together with the two carbons to which Y is attached forms phenyl, pyridyl or pyrimidyl, each of which may be substituted by R;R is one of iodo or trifluoromethylthio or one or two of fluoro, chloro, bromo, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, (C.sub.1 -C.sub.4)alkylthio, (C.sub.1 -C.sub.4)alkylsulfinyl, (C.sub.1 -C.sub.4)alkylsulfonyl or trifluoromethyl; andR.sup.1 is hydrogen or R, are prepared by reacting a bifunctional compound of the formulae ##STR2## with a 2-chloro-1,1,1-tri(C.sub.1 -C.sub.6)alkoxyethane. Most of the compounds of formulae I and II are novel. These compounds are intermediates of use in the preparation of compounds having pharmaceutical activity. The 2-chloro-1,1,1-tri(C.sub.1 -C.sub.6)alkoxyethanes are prepared from the corresponding tri(C.sub.1 -C.sub.6)alkoxyethanes by chlorination with N-chlorosuccinimide or with chlorine in pyridine and a chlorohydrocarbon cosolvent.

Abstract: Novel substituted N-[(4-piperidinyl)alkyl] bicyclic condensed oxazol- and thiazolamines useful as anti-depressives, in the treatment of Parkinson's disease and in the treatment of diseases related with disturbed enterokinesia.

Abstract: The present invention relates to new compounds of the formula ##STR1## where X is ##STR2## alkylene, or --S-- where R.sub.1 is hydrogen, alkyl, or aryl; W is hydrogen, hydroxy, amino, alkyloxy, aryloxy, O-alkyl, or O-aralkyl; (Y).sub.A is --CH.sub.2 NR.sub.2 R.sub.3 where R.sub.2 and R.sub.3 may be hydrogen, substituted alkyls, aryls, or together with N form a 5 to 7 membered heterocyclic group; and Ar is a substituted or unsubstituted aryl. These compounds are useful in the treatment of various cardiac arrhythmias.

Abstract: 2,4-Disubstituted 6-[3,6-dihydro-1(2H)-pyridyl]pyrimidine-3-oxides of the formula ##STR1## wherein R.sup.1 is lower alkyl or lower alkoxy-lower alkyl, R.sup.2 is hydrogen or --COOR.sup.3 wherein R.sup.3 is lower alkyl or lower alkoxy-lower alkyl,which are important for the preparation of therapeutically valuable 1,2,5,6-tetrahydropyridyl-substituted 2-oxo-2H-[1,2,4]oxadiazolopyrimidinecarbamates, are described. The foregoing oxides of formula I can be prepared by reacting the corresponding arylsulfonyloxy- or alkylsulfonyl-substituted derivatives with 1,2,5,6-tetrahydropyridine.

Abstract: Novel 5H-thiazolo- and 5H-1,3,4-thiadiazolo[3,2-a]pyrimidin-5-one and 3,4-dihydro-2H,6H-pyrimido[2,1-b] [1,3]-thiazin-6-one derivatives, which compounds are useful psychotropic agents.

Abstract: Compounds of the formula (I) ##STR1## wherein R.sub.1 is(a) hydrogen or halogen;(b) a C.sub.1 -C.sub.6 alkyl group, unsubstituted or substituted by C.sub.1 -C.sub.4 alkoxy or by halogen;(c) a phenyl ring unsubstituted or substituted by a group chosen from halogen, C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.4 alkoxy;(d) a C.sub.1 -C.sub.6 alkylthio group;R.sub.2 is hydrogen or halogen;R.sub.3 is 2-pyridyl, 3-pyridyl or 4-pyridyl, wherein each pyridyl group is unsubstituted or substituted by C.sub.1 -C.sub.4 alkyl; and the pharmaceutically acceptable salts thereof. The compounds possess anti-ulcerogenic and gastric anti-secretory activity.

Abstract: The present invention relates to new carboxamido-derivatives of 5H-1,3,4-thiadiazolo[3,2-a]pyrimidines, to a process for their preparation and to pharmaceutical (i.e. anti-inflammatory and analgesic) compositions containing them.The invention provides compounds having the following general formula (I) ##STR1## wherein R.sub.1 represents:(a) a hydrogen or halogen atom or a C.sub.1 -C.sub.6 alkyl group unsubstituted or substituted by C.sub.1 -C.sub.6 alkoxy;(b) a ##STR2## group, wherein n is zero, 1, 2 or 3 and each of R.sub.4 and R.sub.5 is, independently, hydrogen or C.sub.1 -C.sub.6 alkyl, or R.sub.4 and R.sub.5, taken together with the nitrogen atom to which they are linked, form an unsubstituted N-pyrrolidinyl ring or a piperidino, morpholino, N-piperazinyl or ##STR3## ring, wherein m is zero, 1 or 2, the piperidino and morpholino rings are unsubstituted or substituted by one or two C.sub.1 -C.sub.6 alkyl groups and the N-piperazinyl ring is unsubstituted or substituted by a substituent chosen from C.sub.

Abstract: The present invention provides pharmaceutical compositions containing N-substituted aziridine-2-carboxylic acid derivatives of the general formula: ##STR1## wherein X is a carboxyl, a cyano, an alkoxycarbonyl or an optionally substituted carbamoyl radical, R is a hydrogen atom, an aliphatic hydrocarbon radical which is saturated or can contain one or more unsaturations and can be substituted one or more times by halogen, alkoxy, hydroxyl, dialkylamino, dialkylaminoxy, cycloalkylamino, acylamino, acyl, nitro, alkylthio, alkylsulphinyl, alkylsulphonyl, cyano, carboxyl, alkoxycarbonyl or carbamoyl or by cycloalkyl or cycloalkenyl radicals optionally carrying alkyl, alkoxy or alkoxycarbonyl radicals, optionally interrupted by hetero atoms and optionally bridged, or by an aryl, hetaryl, aryloxy, arylthio, acyloxy, alkoxycarbonylamino or isothioureido radical, or R is a cycloalkyl or cycloalkenyl radical optionally substituted by alkyl, alkoxy or oxo groups, optionally interrupted by hetero atoms and optionally bri

Abstract: Isoxazolo[3,4-d]pyrimidines of the formula ##STR1## wherein R.sup.1 and R.sup.2, respectively, are lower alkyl; R.sup.3 is lower alkyl or acyl; and R.sup.4 is hydrogen, lower alkyl, or acyl have antiflammatory, analgesic and antipyretic activities in mammals and low acute and subacute toxicities, as well. The compounds are particularly useful as an antiinflammatory, analgesic and antipyretic drug.

Abstract: The compound related to this invention is 7-diethylamino-5-methyl-thiazolo[5,4-d]pyrimidine.The compound related to this invention possesses vasodilating action, hypotensive action, inhibitory action on platelet aggregation, and lowering action on cholesterol levels in blood, and is useful as a therapeutic agent for cardiovascular diseases.

Abstract: Fused [1,2,4]oxadiazolylidenebenzenesulfonamides such as 2-chloro-N-(5,7-dimethyl-2H-[1,2,4]oxadiazolo-[2,3-a]pyrimidin-2-ylidene)b enzenesulfonamide and 2-chloro-N-(7-methoxy-5-methyl-2H-[1,2,4]oxadiazolo-[2,3-a][1,3,5]triazin- 2-ylidene)benzenesulfonamide are general and selective pre- or post-emergence herbicides and can be useful in regulating plant growth.

Abstract: A 2-cyanaziridine derivative of the formula ##STR1## wherein R' is a straight-chained or branched, saturated or mono- or polyunsaturated aliphatic hydrocarbon radical with up to 8 carbon atoms, which is substituted by an aromatic nitrogen-containing heterocyclic radical with 5 or 6 ring-members and 1, 2 or 3 nitrogen atoms optionally substituted by halogen, alkoxy with up to 8 carbon atoms, alkyl with up to 8 carbon atoms, hydroxyl, carbalkoxy with up to 9 carbon atoms, carbamoyl, dialkylamino the alkyl moieties of which having up to 8 carbon atoms, cycloalkylamino, the cycloalkyl moiety having 3-10 carbon atoms, acetylamino, nitro, cyano, acetyl, alkylthio with up to 8 carbon atoms, alkylsulphinyl with up to 8 carbon atoms, alkylsulphonyl with up to 8 carbon atoms, sulphamoyl, phenyl, trifluoromethyl, phenoxy, acetoxy or methylenedioxy;or a pharmacologically acceptable salt thereof, exhibits immune stimulating activity.

Abstract: Oxadiazolo[2,3-c]pyrimidine derivatives of the formula ##STR1## wherein R is alkyl, alkenyl, alkynyl or alkoxyalkyl, as well as their salts, are described. The compounds of formula I have valuable, long-lasting vasodilating and/or blood pressure-lowering properties and are useful for the treatment of vascular-conditioned hypertensions or as vasodilators in peripheral blood supply disorders. The compounds are prepared, inter alia, by carbamoylating the corresponding derivative containing a free amino group and optional salt formation.

Abstract: Oxadiazolo[2,3-c]pyrimidine derivatives of the formula ##STR1## wherein R is alkyl, alkenyl, alkynyl or alkoxyalkyl, as well as their salts, are described. The compounds of formula I have valuable, long-lasting vasodilating and/or blood pressure-lowering properties and are useful for the treatment of vascular-conditioned hypertensions or as vasodilators in peripheral blood supply disorders. The compounds are prepared, inter alia, by carbamoylating the corresponding derivative containing a free amino group and optional salt formation.

Abstract: The present invention provides novel 8-heteroaryltetrahydrobenzopyrans and analogs thereof. These novel compounds are useful as inhibitors of endoperoxide cyclooxygenase which prevents the conversion of unsaturated fatty acids to endoperoxides. Because of this pharmacological activity, these compounds represent potent platelet aggregation inhibitors.

Abstract: Derivatives of 7H-1,3,4-thiadiazolo-[3,2-a]-pyrimidin-7-one-5-carboxylic acid having basic substituents in the 2-position, the alkyl esters and/or pharmaceutically useable salts of these compounds are new substances having immunstimulating properties, being especially valuable for antiinfectious therapy in mammals including man. The new products are prepared by reacting 2-amino-5-(basically substituted)-1,3,4-thiadiazoles with dialkylacetylenedicarboxylates and splitting the ester grouping in the obtained compound if desired and/or forming pharmaceutically acceptable salts.

Abstract: 2-Alkylsulfonyl-7,8-dihydro-5-hydroxy-7-oxo-pyrido[2,3-d]pyrimidine-6-carbo xylic acid derivatives are intermediates useful in the production of 7,8-dihydro-2-amino or alkoxy-7-oxo-pyrido[2,3-d]pyrimidine-6-carboxylic acid derivatives which are gastric anti-secretory agents for treatment of peptic ulcer disease and generally anti-allergic agents useful in the treatment of atopic immediate hypersensitivity reactions.

Abstract: 7-Chloro-7,8-dihydro-7-oxo-pyrido[2,3]-d]pyrimidine-6-carboxylic acid derivatives are intermediates useful for the production of 7,8-dihydro-2,5,8-trisubstituted-7-oxo-pyrido[2,3-d]-pyrimidine-6-carboxyl ic acid derivatives which in turn are gastric anti-secretory agents for treatment of peptic ulcer disease and generally anti-allergic agents useful in the treatment of atopic immediate hypersensitivity reactions.

Abstract: .alpha.-Acylacetamide 2-equivalent yellow couplers may be prepared by reacting .alpha.-halo-.alpha.-acyl-acetamides with phenols or NH-acidic organic compounds in the presence of a non-alkylatable bicyclic nitrogen-containing base, such as 1,5-diazabicyclo[4,3,0]non-5-ene or 1,8-diazabicyclo[5,4,0]-undec-7-ene.

Abstract: A process for preparing oxadiazolopyrimidines of the formula ##STR1## wherein R is alkyl or alkoxyalkyl, by reacting a compound of the formula ##STR2## wherein R is as set forth above, with phosgene, is described.