Abstract: Fused polycyclic 2-aminopyrimidines of formula (1): ##STR1## wherein Ar is an optionally substituted aromatic or heteroaromatic group;X is a carbon or nitrogen atom;Y is a carbon or nitrogen atom;Z is a linker group;A together with X and Y forms an optionally substituted monocyclic or bicyclic aromatic or heteroaromatic group;and the salts, solvates, hydrates and N-oxides thereof are described. The compounds are potent and selective inhibitors of the protein tyrosine kinases p56.sup.lck and p59.sup.fyn and are of use in the prophylaxis and treatment of immune diseases, hyperproliferative disorders and other diseases in which inappropriate p56.sup.lck and/or p59.sup.fyn activity is believed to have a role.

Abstract: The present invention encompasses structures of the Formula: ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: X is oxygen, H.sub.2, or sulfur;Y is oxygen or sulfur;W is alkyl, arylalkyl, or heteroarylalkyl, each of which is optionally substituted; orW is aryl or heteroaryl; ##STR2## wherein: Z.sub.1, Z.sub.2, Z.sub.3, and Z.sub.4 independently represent nitrogen or C--R.sub.a, whereeach R.sub.a independently is hydrogen, an inorganic substitutent or an optionally substituted aromatic group;n is 1, 2 or 3; andR.sub.b is hydrogen, alkyl, or an optionally substituted aromatic group,which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine drugs, and enhancement of memory.

Abstract: The present invention relates to heteroatom-containing cyclopentanopyridyl-oxazolidinones, processes for their preparation and their use as medicaments, in particular as antibacterial medicaments.

Abstract: A sulfonamide derivative or a sulfonic ester derivative represented by the following general formula (I): ##STR1## {G represents an aromatic 5- or 6-membered ring; L represents O or --N(R.sup.1)-- (R.sup.1 represents hydrogen or lower alkyl); and M represents ##STR2## rings A and B represent each an unsaturated 5- or 6-membered ring; Y represents O, S(O).sub.n, C(R.sup.3)(R.sup.4), C(O), N(R.sup.5), CH(R.sup.6)CH(R.sup.7), C(R.sup.8).dbd.C(R.sup.9), N(R.sup.10)C(O), N.dbd.C(R.sup.11), OCH(R.sup.12), S(O).sub.n CH(R.sup.13) or N(R.sup.14)CH(R.sup.15).

Abstract: Disclosed are biologically active, non-indole-containing compounds referred to as fused isoindolones, which are represented by the following general formula: ##STR1## The fused indolones can be obtained by complete chemical synthesis. Methods for making and using the fused isoindolones are disclosed.

Abstract: Disclosed are compounds of compounds of the formula: ##STR1## or the pharmaceutically acceptable nontoxic salts thereof wherein: X is oxygen, H.sub.2 or sulfurY is hydrogen, or optionally substituted alkyl, alkenyl, (substituted)arylalkyl, aryl or heteroaryl, or a carbonyl group substituted with alkyl, cycloalkyl, aryl, or amino groups;W is alkyl, arylalkyl or heteroarylalkyl, where each aryl group is optionally substituted with up to two groups; orW is aryl, thienyl, pyridyl or heteroaryl, each of which is optionally substituted; andZ.sub.1, Z.sub.2, Z.sub.3, and Z.sub.4 independently represent nitrogen or C-R.sub.1 whereR.sub.1 is hydrogen, halogen, hydroxy, amino, or phenyl or pyridyl optionally mono- or independently disubstituted with halogen, hydroxy, lower alkyl, or lower alkoxy,which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists or inverse agonists for GABAa brain receptors.

Abstract: Compounds of the formula (I): ##STR1## are prepared by reaction of the phenylacetic acid derivatives substituted by the appropriate heterocycles, optionally in an activated form, with phenylglycinols. The compounds are suitable as active compounds in medicaments, in particular in medicaments having antiatherosclerotic activity.

Abstract: Compounds of Formula I, and their N-oxides and agriculturally-suitable salts, are disclosed which are useful for controlling undesired vegetation ##STR1## wherein: X and Y are independently N or CH;Z is O, S(O).sub.n, NR.sup.7, C(.dbd.O), C(.dbd.S), C(.dbd.N--OR.sup.8), CH(OR.sup.9), or CR.sup.10 (R.sup.11);n is 0, 1 or 2; andR.sup.1 -R.sup.11 are as defined in the disclosure.Also disclosed are compositions containing the compounds of Formula I and a method for controlling undesired vegetation which involves contacting the vegetation or its environment with an effective amount of a compound of Formula I.

Abstract: There is provided a 1-(3-heterocyclylphenyl)-s-triazine-2, 4,6-oxo or thiotrione compound having the structural formula I ##STR1## Further provided are a composition and a method comprising that compound for the control of undesirable plant species.

Abstract: The present invention encompasses structures of the Formula: ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: X is oxygen, H.sub.2, or sulfur;Y is oxygen or sulfur;W is alkyl, arylalkyl, or heteroarylalkyl, each of which is optionally substituted; orW is aryl or heteroaryl; ##STR2## wherein: Z.sub.1, Z.sub.2, Z.sub.3, and Z.sub.4 independently represent nitrogen or C--R.sub.a, whereeach R.sub.a independently is hydrogen, an inorganic substitutent or an optionally substituted aromatic group;n is 1, 2 or 3; andR.sub.b is hydrogen, alkyl, or an optionally substituted aromatic group,which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine drugs, and enhancement of memory.

Abstract: The invention relates to new imidazoazines of the general formula (I) ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, A, D, E and G have the meanings given in the description, to processes for their preparation, and to their use as herbicides.

Abstract: The present invention is directed to irreversible inhibitors of serine and cysteine proteases which most preferably contain a 1-oxytriazole or 1-oxyimidazole functionality. Methods for the use of the protease inhibitors are also described.

Abstract: This invention relates to new nucleotide analogues and solves the technical problem of their use as biologically active compounds. The subject of this invention are N-(2-phosphonylmethoxyethyl) and N-(3-hydroxy-2-phosphonylmethoxypropyl) derivatives of pyrimidine and purine bases, easily accessible from heterocyclic bases and their N-(2-hydroxyethyl) or N-(2,3-dihydroxypropyl) derivatives. Some of the compounds, according to this invention, exhibit a marked antiviral activity or can be converted into such active compounds by chemical transformations.

Abstract: This invention relates to carbocyclic and heterocyclic fused-ring quinolinecarboxylic acid compounds, to pharmaceutical compositions comprising such compounds, and to methods of using such compounds for the treatment and/or prevention of organ transplantation rejection, graft versus host disease, autoimmune diseases, chronic inflammatory diseases, including but not limited to psoriasis and rheumatoid arthritis, and cancer in a mammal.

Abstract: Compounds of Formula I, and their N-oxides and agriculturally-suitable salts, are disclosed which are useful for controlling undesired vegetation ##STR1## wherein: ##STR2## T is O or S; W is a single bond, O, S or NR.sup.6 ;X is N or CH;Y is N or CH;Z is N or CR.sup.7 provided that when Z is CR.sup.7, then Y is N;R.sup.6 is H, CH.sub.3 or OCH.sub.3 ;m is 1 or 2; andR.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.7 are as defined in the disclosure.Also disclosed are compositions containing the compounds of Formula I and a method for controlling undesired vegetation which involves contacting the vegetation or its environment with an effective amount of a compound of Formula I.

Abstract: There are provided novel (2-imidazolin-2-yl) fused heteropyridine compounds, and intermediate compounds for the preparation thereof, and a method for controlling a wide variety of annual and perennial plant species therewith.

Abstract: There are provided novel (2-imidazolin-2-yl) fused heteropyridine compounds, and intermediate compounds for the preparation thereof, and a method for controlling a wide variety of annual and perennial plant species therewith.

Abstract: The present invention is directed to irreversible inhibitors of serine and cysteine proteases which most preferably contain a 1-oxytriazole or 1-oxyimidazole functionality. Methods for the use of the protease inhibitors are also described.

Abstract: This invention relates to substituted fused heterocyclic compounds of Formula I which have utility as herbicides: ##STR1##

Abstract: This invention relates to heterocyclic derivatives useful for inhibiting the production of Interleukin-1 (IL-1) and tumor necrosis factor (TNF) and the like, which can be represented by the following formula: ##STR1## to a process for their production, to a pharmaceutical composition containing the same and to uses thereof.

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 mechanism of the inhibition of advanced glycosylation by aminoguanidine and other hydrazine type compounds was investigated using a solution of one or two molecules of aminoguanidine or other hydrazine type compound incubated with an Amadori product (1-propylamine-1-deoxy-D-fructose) under physiological conditions. This inhibition was found to proceed through the reactive intermediate 1-propylamino-1, 4-dideoxyosone to form the corresponding triazine and the dehydrazone of 1,4-dideoxyglucosone, respectively.The triazine and dehydrazone products are useful as macrophage stimulants to activate a macrophage to effect removal of advanced glycosylation endproducts (AGEs). Additionally, they can be used in a variety of investigative methods in an effort to measure the extent of nonenzymatic glycosylation of a protein sample wherein aminoguanidine or other hydrazine-type compound is or was present during the glycosylation process.

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: Substituted Imidazo-fused 6-membered heterocycles of structural formula: ##STR1## wherein A, B, C, and D are independently carbon atoms or nitrogen atoms are angiotensin II antagonists useful in the treatment of hypertension and congestive heart failure.

Abstract: Substituted quinazolinones and pyridopyrimidines of structural formula I ##STR1## are angiotensin II antagonists useful in the treatment of disorders related to the renin-angiotensin system (RAS) such as hypertension, congestive heart failure, ocular hypertension and certain CNS disorders.

Abstract: Compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein, R is H, halogen, (C.sub.1 -C.sub.6) alkyl, N(C.sub.1 -C.sub.6 alkyl/aryl).sub.2, OH, O--(C.sub.1 -C.sub.6) alkyl/aryl, CH.sub.2 OH, COOH, COO-alkyl/aryl, SO.sub.2 NH.sub.2, or SO.sub.2 NH (C.sub.1 -C.sub.6 alkyl/aryl);R.sub.1 is C.sub.1 -C.sub.6 alkyl, cycloalkyl, C.sub.2 -C.sub.6 alkenyl, heteroaryl, substituted heteroaryl, heterocycloalkyl, --CH.sub.2 -aryl, --CH.sub.2 -substituted aryl, --CH.sub.2 -heteroaryl, or --CH.sub.2 -substituted heteroaryl;R.sub.2 is H, C.sub.1 -C.sub.6 alkyl or aryl; ##STR2## is an aromatic ring or a heteroaromatic ring; and X is O or N-(alkyl/aryl/alkyl-aryl/alkoxylalkoxyaryl)are described. These compounds are useful as agents for treating viruses.

Abstract: Substituted Imidazo-fused 6-membered heterocycles of structural formula: ##STR1## wherein A, B, C, and D are independently carbon atoms or nitrogren atoms are angiotensin II antagonists useful in the treatment of hypertension and congestive heart failure.

Abstract: Herbicidal agents containing a pyrimido[5,4-e]-as-triazine-5,7-(6H,8H)-dione Ia ##STR1## (R.sup.1, R.sup.2 .dbd.H, C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.6 -cycloalkyl, C.sub.2 -C.sub.8 -alkenyl, phenyl or benzyl, R.sup.3 .dbd.H, halogen, nitro, C.sub.1 -C.sub.8 -alkyl which may carry up to three further substituents, C.sub.2 -C.sub.6 -alkenyl, phenyl-C.sub.2 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -cycloalkyl which may carry up to 3 C.sub.1 -C.sub.4 -alkyl substituents, a 5- or 6-membered heterocyclic structure where up to 2 of the ring members are O, S or NR.sup.4 ; --CO--R.sup.4 or --CO--O--R.sup.4 ; phenyl or hetaryl, which may carry up to 3 further substituents; or ZR.sup.6 ; R.sup.4 .dbd.H, C.sub.1 -C.sub.6 -alkyl; Z.dbd.O, S or --N(R.sup.7)--; R.sup.6 .dbd.H, C.sub.1 -C.sub.6 -alkyl, phenyl or benzyl, which may carry up to 3 further substituents; R.sup.7 .dbd.H, C.sub.1 -C.sub.6 -alkyl or R.sup.6 and R.sup.

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: Oxetanocin derivatives represented by formula: ##STR1## wherein X represents H or ##STR2## or a pharmacologically acceptable salt thereof exhibit an anti-viral activity. Anti-viral compositions comprising the oxetanocin derivatives or their pharmacologically acceptable salts as the effective ingredient are also provided.

Abstract: A compound of the general formula: ##STR1## wherein Q is a condensed heterocyclic group having an N atom in the bridgehead which may be substituted, W is O or S, R.sub.1 and R.sub.2 each are an alkyl group, an alkoxy group or halogen and Z is CH or N, and a salt thereof, which is useful as a herbicide.

Abstract: Herbicidal triazoloazines of the formula ##STR1## in which A stands for nitrogen or for a radical C--R.sup.3,R.sup.1, R.sup.2 and R.sup.3 independently of one another each stand for hydrogen, hydroxyl, halogen, for optionally substituted alkyl, for alkoxy, alkylthio or for optionally substituted aryl, or eitherR.sup.1 and R.sup.3 together or R.sup.3 and R.sup.2 together stand for a fused, optionally substituted carbocyclic or heterocyclic ring,X stands for oxygen, sulphur, a sulphinyl group, or a sulphonyl group andAr stands for in each case optionally substituted aryl or heteroaryl.

Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein X is N or CH;R.sub.1 and R.sub.2 are the same or different and are hydrogen, halogen, CF.sub.3, C.sub.1-6 alkyl, C.sub.1-7 acyl, C.sub.1-7 acylamino, or amino, aminocarbonyl or aminosulphonyl, optionally substituted by one or two C.sub.1-6 alkyl or C.sub.3-8 cycloalkyl groups, or by C.sub.4-5 polymethylene or by phenyl, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkylsuphinyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, hydroxy or nitro; or R.sub.1 and R.sub.2 taken together are methylenedioxy or ethylenedioxy;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.3 or R.sub.4 is C.sub.1-4 alkyl;having 5-HT.sub.3 receptor antagonist activity, a process for their preparation and their use as pharmaceuticals.

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: Compounds of the formula ##STR1## wherein A represents a grouping of the formula ##STR2## in which R.sup.1 and R.sup.2 each individually represent hydrogen, halogen, trifluoromethyl, nitro, amino, cyano, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, C.sub.3 -C.sub.6 -alkenyloxy, C.sub.1 -C.sub.6 -alkylthio, C.sub.1 14 C.sub.6 -alkanoylamino, aryloxy, aryl-(C.sub.1 -C.sub.6 -alkyl), aryl-(C.sub.1 -C.sub.6 -alkoxy), aryl-(C.sub.1 -C.sub.6 -alkoxy)carbonylamino or a group of the formula --O--CH.sub.2 --R.sup.3 or R.sup.1 and R.sup.2 on adjacent carbon atoms together represent a group of the formula --CH.dbd.CH--CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --O-- and R.sup.3 represents hydroxy-(C.sub.1 -C.sub.4 -alkyl) or vicinal dihydroxy-(C.sub.2 -C.sub.5 -alkyl), and pharmaceutically acceptable acid addition salts of those compounds of formula I in which R.sup.1 and/or R.sup.

Abstract: Novel substituted 3-phenyl-7H-thiazolo[3,2-b][1,2,4]-triazin-7-ones of the formula I are disclosed ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 have the meaning recited in the specification. The compounds are suitable for prevention and treatment of inflammatory disorders.

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

Abstract: Heterocyclic compounds of formulae (I) and (II): ##STR1## where R.sup.1 and R.sup.2 are alkyl, R.sup.3 is H or alkyl, m is 2-5 and Het is a hetercycle such as thiazole, benzothiazole, substituted benzothiazole, pyrazine, triazine, thiadiazole, substituted thiadiazole, pyrimidine or substituted pyrimidine. The compounds are calcium channel blockers useful in the treatment of cardiovascular conditions such as hypertension or angina.

Abstract: The invention concerns the novel racemic and laevorotatory optically active forms of the thromboxane A.sub.2 antagonist 5(Z)-7-([ 2,4,5-cis]-4-o-hydroxyphenyl-2-trifluoromethyl-1,3-dioxan-5-yl)heptenoic acid of formula I, their salts, pharmaceutical compositions, and processes for their manufacture and intermediates therefor. The pharmaceutical agents and their compositions are of value in certain pulmonary and/or vascular disorders.

Abstract: Novel fluorine-containing N-sulfenylated indazoles are prepared by reacting the corresponding indazoles with sulfenyl halides in the presence of a solvent and/or diluent and in the presence of an acid-binder. The novel fluorine-containing N-sulfenylated indazoles are useful in the protection of industrial materials against attack by microorganisms such as bacteria, fungi, yeast, algae, and slime as plant protection agents, and in combating insects and arachrids.

Abstract: This disclosure describes compositions of matter containing certain substituted imidazo[1,5-d]-1,2,4-triazin-1(2H)-ones and the method of treating hypertension therewith.

Abstract: Benzenesulfonamide compounds such as N-[(4,6-dimethoxy-1,3,5-triazin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl-4 -oxo-1-phenyl-indeno[1,2-C]pyrazole-5-sulfonamide and N-[(4-methoxy-6-methyl-pyrimidin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl- 4-oxo-1-phenyl-indeno[1,2-C]pyrazole-5-sulfonamide, agricultural compositions containing them, and their herbicidal utility are disclosed.

Abstract: The invention relates to novel 2-phenyl-imidazoles of the formula ##STR1## and the tautomers and acid addition salts thereof, particularly the pharmacologically acceptable acid addition salts, which exhibit valuable pharmacological properties, particularly an effect on the contractility of the heart muscle. The compounds of Formula I may be prepared by methods conventionally used for similar compounds.

Abstract: Compounds of the formula ##STR1## wherein A, B, C and D are --N.dbd., HN.dbd., R.sub.3 N.dbd., O.dbd.C.dbd., HC.tbd., HO--C.tbd. or R.sub.3 SO.sub.2 --O--C.tbd.; andR.sub.1 and R.sub.2 are substituents of various types.The compounds are useful as hypotensives and cardiotonics.

Abstract: Compounds of the formula ##STR1## wherein A, B, C and D are each independently --N.dbd. or --CH.dbd., provided, however, that at least two of them must be --N.dbd., and when A and C are both --N.dbd., at least one or both of B and D must be --N.dbd.; andR.sub.1, R.sub.2 and R.sub.3 are substituents of diverse types;tautomers thereof; and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds are useful as cardiotonics.

Abstract: This invention provides for certain phenyl-substituted imidazo compounds, their pharmaceutical formulations, and their use as positive inotropic agents and vasodilators.

Abstract: Fused tetracyclic compounds containing two thiophene rings, one pyridine ring and a triazine ring and which are useful as antiallergic agents are described herein. The compounds are prepared by the reaction of an appropriate substituted aminocarboxamine with sodium nitrite in an acid such as acetic acid.

Abstract: A pollen suppressant of the formula ##STR1## wherein R.sup.1 and R.sup.4 independently represent C.sub.1 -C.sub.4 alkyl, phenyl, naphthyl, or phenyl or naphthyl substituted with one to three substituents selected from the group consisting of halogen, trihalomethyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkyl, and cyano; R.sup.2 is ##STR2## where R.sup.5 is a C.sub.1 -C.sub.12 alkyl group, optionally substituted with one or more halogen atoms, or an aryl group selected from the group consisting of 6-membered rings containing 0-3 nitrogens and fused bicyclic 10-membered rings containing 6 atoms in each ring and 0-3 nitrogens per ring with the remaining atoms in the ring or rings of said aryl group being carbon atoms, said aryl group being optionally substituted with a C.sub.1 -C.sub.4 alkyl group or an electron-withdrawing group, R.sup.3 is hydrogen, a halogen a C.sub.1 -C.sub.4 alkyl group, a carboxy group or an agronomically acceptable alkali metal salt thereof, or a group of the formula --COOR.sup.

Abstract: This invention relates to benzo- and thieno-triazine-1,2,3 ones-4 represented by the formula ##STR1## in which m is 2, 3 or 4, X is the vinylene group --CH.dbd.CH-- or a sulfur atom; R.sub.1 and R.sub.2 can be alike or different and are hydrogen, halogen, a lower alkyl radical, lower alkoxy radical or trifluoromethyl radical; when X is --CH--CH-- n is 0, 1 or 2 and R is hydrogen, halogen, a lower alkyl radical, lower alkoxy radical or nitro group; when X is a sulfur atom, R is hydrogen or constitutes a --CH.sub.2 --.sub.4 chain between the two open positions of the thiophenic ring. The compounds are useful as antidepressant drugs.

Abstract: This invention provides for certain phenyl-substituted imidazo compounds, their pharmaceutical formulations, and their use as positive inotropic agents and vasodilators.