Abstract: N-Cyanoaryl nitrogen heterocycles having sulfur-containing groups of the formula (1), in which Q1 represents oxygen or sulfur, R1 represents hydrogen or halogen, R2 represents halogen, cyano, nitro, amino or the grouping —N(A1)SO2A, in which A represents, in each case, optionally substituted alkyl, alkenyl, alkinyl, dialkylamino, cycloalkyl, cycloalkylalkyl, aryl or arylalkyl, and A1 represents hydrogen, formyl or, in each case optionally substituted, alkyl, alkenyl, alkinyl, alkylcarbonyl, alkoxycarbonyl or alkylsulphonyl, or together with A represents alkanediyl, R3 represents hydrogen, halogen, cyano or optionally substituted alkyl, R4 represents optionally substituted alkyl or together with R3 represents alkanediyl, and Z represents one of the groups in which Q2 represents oxygen or sulfur and R5 represents hydrogen or, in each case optionally substituted, alkyl, alkenyl, alkinyl or alkylcarbonyl, and salts of compounds of the formula (1) with the pro

Abstract: Imido and amido substituted alkanohydroxamic acids reduce the levels of TNF&agr; and inhibit phosphodiesterase in a mammal. A typical embodiment is 3-(3-cyclopentyloxy-4-methoxyphenyl)-N-hydroxy-3-phthalimidopropionamide.

Abstract: A process for the preparation of compounds having plant protecting, in particular fungicidal properties, of the formula I 1

Abstract: Compounds of formula wherein W is —OH or —NHOH; X is a heterocycle with the proviso that when X is a nitrogen containing heterocycle, the heterocycle is attached to the (CH2)m moiety by a ring nitrogen, —CONR2R3, —NR1COR2, —NR1SO2R2, —NR1CONR2R3, —NR1COOR4, heteroarylthio, alkylthio, arylalkylthio, heteroarylalkylthio, heterocycloalkylalkylthio, heterocycloalkylthio or arylthio; Y is carbon, nitrogen, oxygen or sulfur, provided that when Y is carbon, n is 2; Z is alkyl, aryl, alkoxy, aryloxy, aralkoxyaryl, aralkoxyheteroaryl, heteroaryl, heterocycloalkyl, heteroaryloxy, —CONR2R3, —NR1COR2, —NR1CONR2R3, —OCONR2R3, —NR1COOR4, or —SO2R2; R1 is hydrogen, alkyl, heterocycloalkylalkyl, aralkyl or heteroarylalkyl; R2 and R3 are independently R1, aryl or heteroaryl; or R2 and R3 taken together with the nitrogen atom to which they are attached form a 5- to 7-membered ring, which may optionally contain another heteroat

Abstract: A method for controlling wheat powdery mildew is provided which encompasses applying to the plant, seed, seedling or portion of the plant to be protected, or, to its growing media, an effective amount of a compound of Formula II where Q is O, n is 0, R3 is halogen, R4 is halogen or hydrogen, R5 is an alkyl group having from three to five carbon atoms and R6 is an alkyl group having from three to eight carbon atoms. Also provided are certain compositions for controlling wheat powdery mildew which contain a compound of Formula II together with a surfactant, an organic solvent and/or a solid or liquid diluent. Also provided are certain fungicidal compounds within Formula II for controlling wheat powdery mildew.

Abstract: Imido and amido substituted alkanohydroxamic acids reduce the levels of TNF&agr; and inhibit phosphodiesterase in a mammal. A typical embodiment is 3-(3-cyclopentyloxy-4-methoxyphenyl)-N-hydroxy-3-phthalimidopropionamide.

Abstract: The present invention is directed in part towards methods of modulating the function of serine/threonine protein kinases with quinazoline-based compounds. The methods incorporate cells that express a serine/threonine protein kinase, such as RAF. In addition, the invention describes methods of preventing and treating serine/threonine protein kinase-related abnormal conditions in organisms with a compound identified by the invention. Furthermore, the invention pertains to quinazoline compounds and pharmaceutical compositions comprising these compounds.

Abstract: A process for preparing a 3-dihalobenzyl-2,4-quinazolinedione derivative represented by the formula (V): (wherein X1, X2, X3 are independently a halogen atom, and A is an alkylene group), which comprises: reacting a dihalobenzyl derivative represented by the formula (III): (wherein X2 and X3 are each as defined above, and L is an acid residue) with a 2,4-quinazolinedione derivative having a carboxyalkyl group represented by the formula (I): (wherein X1 and A are each as defined above) to selectively substitute a hydrogen atom of an imino group at the 3-position of the derivative (1). The above process enables the efficient preparation of the compounds of the above formula (V) useful as inhibitors against aldose reductases, makes it possible to secure the safety and hygiene of workers, and can facilitate waste disposal to reduce the expenses, thus being industrially extremely advantageous.

Abstract: The present invention is directed to certain N-amino- and N-hydroxy-quinazolinone compounds and synthetic methods for synthesis thereof, which compounds may find use in combinatorial libraries. More specifically, the invention is directed to the synthesis of 3-hydroxy- and 3-amino-4(1H)-quinazolinones via the reaction of an appropriate 2-aminobenzamide compound with a carboxylic acid or acyl halide at ambient temperature performed on a solid support or in solution.

Abstract: The present invention relates generally to an asymmetric synthesis of 4,4-disubstituted-3,4-dihydro-2(1H)-quinazolinones, and intermediates thereof. The target compounds are useful for the treatment of human immunodeficiency virus (HIV) as an inhibitor of reverse transcriptase.

Abstract: Heterocyclically substituted benzamides of the formula I are described, where R1, R2, R3, R4, R5, X, m and n have the meanings given in the description. The novel compounds are useful for controlling diseases.

Abstract: The invention provides compounds comprising glycoprotein IIb/IIIa receptor-binding benzodiazepine derivatives covalently linked to metal ion chelators. The compounds of the invention may be labeled with a radionuclide such as 99mTc and used to image thrombi.

Abstract: This invention provides advantageous processes for preparing quinazolinones of Formula I ##STR1## wherein: R.sup.1 is C.sub.1 -C.sub.10 alkyl; C.sub.3 -C.sub.10 alkenyl; C.sub.3 -C.sub.10 cycloalkyl; C.sub.3 -C.sub.10 halocycloalkyl; C.sub.4 -C.sub.10 cycloalkylalkyl; C.sub.4 -C.sub.10 halocycloalkylalkyl; or C.sub.3 -C.sub.10 alkynyl;R.sup.2 is C.sub.1 -C.sub.10 alkyl; C.sub.3 -C.sub.10 alkenyl; C.sub.3 -C.sub.10 cycloalkyl; C.sub.3 -C.sub.10 halocycloalkyl; C.sub.4 -C.sub.10 cycloalkylalkyl; C.sub.4 -C.sub.10 halocycloalkylalkyl; C.sub.4 -C.sub.10 cycloalkyl; C.sub.4 -C.sub.10 halocycloalkyl; or C.sub.3 -C.sub.10 alkynyl; andR.sup.3 and R.sup.4 are each independently hydrogen or halogen; from compounds containing the moiety IIg ##STR2## This invention further provides certain compounds of Formula II, IIIa, or IVa ##STR3## where R.sup.7 is C.sub.2 -C.sub.6 alkyl.

Abstract: The present invention is concerned with a process for the preparation of antiviral 1,3-oxathiolane nucleosides comprising an intramolecular glycosylation reaction to produce exclusively the .beta.-diastereomer, and intermediates useful in the process.

Abstract: Novel 4-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using 4-substituted piperidine analogs as selectively active antagonists of N-methyl-D-aspartate (NMDA) receptor subtypes for treating conditions such as stroke, cerebral ischemia, central nervous system trauma, hypoglycemia, anxiety, convulsions, aminoglycoside antibiotics-induced hearing loss, migraine headaches, glaucoma, CMV retinitis, chronic pain, opioid tolerance or withdrawals, or neurodegenerative disorders, such as lathyrism, Alzheimer's Disease, Parkinsonism and Huntington's Disease are described. Also described are novel methods for preparing 4-substituted piperidine analogs and novel intermediates of the 4-substituted piperidine analogs.

Abstract: Compounds of Formula I, and their N-oxides and agriculturally suitable salts, are disclosed which are useful as fungicides ##STR1## wherein W is O, S(O).sub.n or NR.sup.5 ;n is 0, 1 or 2;Q is O or S;G is a fused phenyl, naphthalene, thiophene, furan, pyrrole, pyridine, thiazole, oxazole, imidazole, pyrazine, pyridazine or pyrimidine ring; andR.sup.1 -R.sup.5 are as defined in the disclosure.Also disclosed are compositions containing the compounds of Formula I and a method for controlling plant diseases caused by fungal plant pathogens which involves applying an effective amount of a compound of Formula I.

Abstract: The present invention relates to novel antidiabetic compounds, their tautomeric forms, their derivatives, their analogues, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. This invention particularly relates to novel azolidinediones of the general formula (I), their analogues, their derivatives, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutical compositions containing them.

Abstract: N-substitued 3-azabicyclo[3.2.0]heptane derivatives of formula (I) ##STR1## in which R.sup.1, R.sup.2, A, X, Y and Z have the meanings given in the description, their method of preparation and their use as pharmacological agents.

Abstract: Quinazoline-2,4-diones are obtained in high yields and purities by reacting anthranilic acids with isocyanates and then, without isolation of the urea formed as intermediate, treating the reaction mixture with acid.

Abstract: Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented. The compounds of the invention have the generalized formulas: ##STR1## wherein r is 0-2, T is selected from ##STR2## and R.sup.40 is a mono- or bi-heterocyclic structure. These compounds are useful for inhibiting matrix metalloproteases and, therefore, combating conditions to which MMP's contribute, such as osteoarthritis, rheumatoid arthritis, septic arthritis, periodontal disease, comeal ulceration, proteinuria, aneurysmal aortic disease, dystrophobic epidermolysis, bullosa, conditions leading to inflammatory responses, osteopenias mediated by MMP activity, tempero mandibularjoint disease, demyelating diseases of the nervous system, tumor metastasis or degenerative cartilage loss following traumatic joint injury, and coronary thrombosis from athrosclerotic plaque rupture.

Abstract: A compound of the formula: ##STR1## wherein --X.sup.3 .dbd.X.sup.2 --X.sup.1 .dbd.N-- is a group of the formula: ##STR2## R.sup.1 is hydrogen or halogen, R.sup.2 is halogen,R.sup.3 is hydrogen, nitro, amino optionally having at least one substituent or a heterocyclic group optionally having at least one substituent,R.sup.4 and R.sup.5 are each hydrogen, or halogen,R.sup.6 and R.sup.8 are each hydrogen, halogen, lower alkyl, hydroxy, lower alkylthio, amino optionally substituted with lower alkyl, or lower alkoxy optionally substituted with a substituent selected from the group consisting of hydroxy, lower alkoxy, amino, lower alkylamino and aryl optionally substituted with lower alkoxy,R.sup.7 is hydrogen or lower alkyl,A is lower alkylene, andQ is O or N--R.sup.9 is hydrogen or acyl,provided that R.sup.3 is not hydrogen when X.sup.1 is C--R.sup.6, in which R.sup.6 is hydrogen, andpharmaceutically acceptable salts thereof.

Abstract: Compounds of the formula I ##STR1## where B, R.sup.1, R.sup.2, n, R.sup.3, A, X, Y and Z have the meanings stated in the description, and their preparation are described. The novel ompounds are suitable for controlling diseases.

Abstract: Quinazoline compounds which demonstrate antiproliferative activity, such as antitumor activity, processes of preparing these compounds, pharmaceutical compositions containing these compounds, and the use of these compounds. These compounds inhibit the growth and proliferation of the cells of higher organisms and microorganisms, such as bacteria, yeasts and fungi. Preferred quinazoline compounds are capable of inhibiting the enzyme thymidylate synthase. Effects derived from the inhibition of the enzyme thymidylate synthase include those discussed above.

Abstract: Compounds of the formula ##STR1## in all possible racemic, enantiomeric and diastereoisomeric forms and their non-toxic, pharmaceutically acceptable salts with acids and bases having antagonistic properties for angiotensin II receptors and a process and novel intermediates for their properties.

Abstract: A chymase inhibitor containing as its effective ingredient a quinazoline derivative, or a pharmaceutically acceptable salt thereof, having the formula (1): ##STR1## and a pharmaceutical preparation for the prevention of cardiac and circulatory system diseases derived from abnormal exacerbation of Ang II production containing the same as its effective ingredient.

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: The present invention relates to a method for the synthesis of 1,3-disubstituted quinazolinedione derivatives which comprises:(a) reacting a haloformate functionalized polystyrene resin with a substituted anthranilic acid derivative under conditions effective to form a urethane-linkage;(b) reacting the product of step (a) with a primary amine under conditions effective to form an anthranilamide derivative;(c) heating the anthranilamide to effect intramolecular cyclization thereby liberating the 1,3-disubstituted quinazolinedione derivative from the resin into solution; and(d) isolating the 1,3-disubstituted quinazolinedione by filtration and solvent removal.

Abstract: A process for producing an dioxoquinazoline of following formula (II): ##STR1## wherein R.sub.1 and R.sub.2 independently represent a hydrogen atom, a halogen atom, a nitro group, a lower alkyl group, an aralkyl group, an alkoxy group, an alkoxylcarbonyl group or a group represented by YNR.sub.3 R.sub.4, wherein Y represents a direct bond, a lower alkylene group or a carbonyl group, and R.sub.3 and R.sub.4 independently represent a lower alkyl group or N, R.sub.3 and R.sub.4 may bond together to form a five- or six-membered heterocycle which comprises reacting an anthranylamide of formula (I): ##STR2## wherein X, R.sub.1 and R.sub.2 are as defined above.

Abstract: Disclosed is a process for preparing compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty. Independently, R.sub.1 and R.sub.2 are hydrogen, a straight or branched chain alkyl, alkenyl or alkynyl of up to twenty carbon atoms in length or --(CH.sub.2).sub.w R.sub.5. If R.sub.1 or R.sub.2 is --(CH.sub.2).sub.w R.sub.5, w may be an integer from one to twenty and R.sub.5 may be an hydroxyl, halo, C.sub.1-8 alkoxyl group or a substituted or unsubstituted carbocycle or heterocycle. Alternatively, R.sub.1 and R.sub.2 may jointly form a substituted or unsubstituted, saturated or unsaturated heterocycle having from four to eight carbon atoms, N being a hetero atom of the resulting heterocyle. R.sub.3 may be either hydrogen or C.sub.1-3. In the compounds, a total sum of carbon atoms comprising R.sub.1 or R.sub.2, (CH.sub.2).sub.n and (CH.sub.2).sub.m does not exceed forty. R.sub.

Abstract: A novel compound of the formula:A--Z--Ar.sup.1 1'CO--Ar.sup.2wherein A is a condensed pyrimidinone or condensed pyridazinone ring; Ar.sup.1 and Ar.sup.2 are independently a ring; Z is a divalent group, or a salt thereof which have an excellent antitumor activity.

Abstract: This invention pertains to compounds of Formulae I, II and III, as defined in the disclosure and claims, including all geometric and stereoisomers, N-oxides, agriculturally suitable salts thereof, agricultural compositions containing them and their use as fungicides.

Abstract: The invention relates to a process for the preparation of substituted 3-arylquinazoline-2,4-diones of the formula (I) ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined in claim 1 and Ar is ##STR2## where R.sup.5 to R.sup.9 are as defined in claim 1, by reacting a compound of the formula (II) ##STR3## with a compound Z in the presence of a catalyst, a ligand and a solvent, where Z isa) an anthranilic acid derivative of the formula (III) ##STR4## or b) an alcohol R.sup.10 --OH and where, in case b), the resulting carbamate is then reacted with an anthranilic acid derivative of the formula III.

Abstract: Phthalazinedione compounds and pharmaceutical compositions are described. The compositions are useful in treating human or animal patients to alleviate or cure disease or disease symptoms caused by nuclear ADP-ribosyl and similar transferases.

Abstract: Chroman derivatives of the formula ?I! ##STR1## wherein R.sup.1 is a cyano, a nitro, a trihalomethyl, a trihalomethoxy or a halogen atom; R.sup.2 is a lower alkoxyalkyl, an aryloxyalkyl or a dialkoxyalkyl; R.sup.3 is a lower alkoxyalkyl or an aryloxyalkyl; R.sup.4 is a hydroxy, a formyloxy or a lower alkanoyloxy; X is N--H, an N--optionally substituted lower alkyl, an oxygen atom, a sulfur atom or a single bond; and Y is an optionally substituted aromatic ring residue or an optionally substituted heterocyclic residue, pharmaceutically acceptable salts thereof and pharmaceutical use thereof. The compound of the present invention and pharmaceutically acceptable salts thereof have selective and excellent coronary vasodilating action and extremely weak hypotensive action.

Abstract: The invention relates to a process for the preparation of quinazoline-2,4-diones of the formula (I) ##STR1## in which R.sup.1 is (C.sub.1 -C.sub.12)alkyl, (C.sub.3 -C.sub.8)cycloalkyl or (C.sub.7 -C.sub.10)aralkyl, it being possible for the aryl group to be substituted by one or more halogen atoms, andR.sup.2, R.sup.3, R.sup.4 and R.sup.5, independently of one another, are halogen, alkyl, alkoxy or hydrogen, which comprises reacting anthranilic acid esters of the formula (II) ##STR2## in which R is (C.sub.1 -C.sub.10)alkyl and R.sup.2 to R.sup.5 are as defined above, with isocyanates R.sup.1 -.dbd.C.dbd.O in an aprotic reaction medium to give carbamoylanthranilic acid esters of the formula (III) ##STR3## in which R, R.sup.1 to R.sup.5 are as defined above, and cyclizing these products in the presence of alkali metal alcoholates, alkali metal amides, alkali metal hydrides, alkaline earth metal alcoholates, alkaline earth metal amides, alkaline earth metal hydrides or tetraalkylammonium hydroxides.

Abstract: Quinazoline compounds which demonstrate antiproliferative activity, such as antitumor activity, processes of preparing these compounds, pharmaceutical compositions containing these compounds, and the use of these compounds. These compounds inhibit the growth and proliferation of the cells of higher organisms and microorganisms, such as bacteria, yeasts and fungi. Preferred quinazoline compounds are capable of inhibiting the enzyme thymidylate synthase. Effects derived from the inhibition of the enzyme thymidylate synthase include those discussed above.

Abstract: Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof, wherein: R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 are the same or different and represent hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, hydroxy, amino, cyano, nitro, trifluoromethyl, trifluoromethoxy, C.sub.1 -C.sub.6 alkoxy, --O.sub.2 CR', --NHCOR', --COR', --SO.sub.m R', where R' is C.sub.1 -C.sub.6 alkyl and wherein m is 0, 1 or 2; orR.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 independently represent --CONR'R", or --NR'R" where R' and R" independently represent hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.10 is hydrogen or C.sub.1 -C.sub.

Abstract: The description relates to bicyclene derivatives of formula (I) in which A, B, D, E, G, K, L, R.sup.1, R.sup.2, Z.sup.1 and Z.sup.2 have the meanings given in the description, and their production. These compounds are suitable for treating diseases.

Abstract: The present invention is concerned with novel compounds having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof and the stereochemically isomeric forms thereof, whereinAlk represents C.sub.1-4 alkanediyl;D is a bicyclic heterocycle of formula ##STR2## wherein each R.sup.1 independently is C.sub.2-6 alkenyl; C.sub.2-6 alkynyl; C.sub.3-6 cycloalkyl optionally substituted with C.sub.1-4 alkyl; C.sub.1-19 alkyl optionally substituted with C.sub.3-6 cycloalkyl, halo, C.sub.1-6 alkyloxy or cyano; and each R.sup.2 independently is hydrogen or C.sub.1-4 alkyl. Novel compounds; compositions; processes for preparing novel compounds and intermediates are described.

Abstract: The invention provides novel compounds of formula (I) having nematicidal, insecticidal, acaricidal and fungicidal properties, compositions comprising them and processes and intermediates for their preparation: ##STR1## wherein R.sup.1 is --S(O).sub.n CH.sub.2 CH.sub.2 CH.dbd.CF.sub.2 ;n is selected from 0, 1 and 2;R.sup.2, R.sup.3, and R.sup.4 are independently selected from hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, alkylcycloalkyl, optionally substituted aryl, optionally substituted arylalkyl, optionally substituted aryloxy, optionally substituted arylalkoxy, alkoxy, alkenyloxy, alkynyloxy, hydroxyalkyl, alkoxyalkyl, alkylthio, alkenylthio, alkynylthio, haloalkyl, haloalkenyl, haloalkynyl, haloalkoxy, haloalkenyloxy, haloalkynyloxy, haloalkylthio, haloalkenylthio, haloalkynylthio, halogen, hydroxy, cyano, nitro, --NR.sup.5 R.sup.6, --NR.sup.7 COR.sup.8, --NR.sup.9 SO.sub.2 R.sup.10, --N(SO.sub.2 --R.sup.11)(SO.sub.2 --R.sup.12), --COR.sup.13, --CONR.sup.14 R.sup.15, --COOR.sup.16, --OCOR.sup.17, --OSO.

Abstract: Novel methods for the synthesis of substituted ureas and guanidines including Terazosin, Prazosin, Doxazosin, Tiodazosin, Trimazosin, Quinasin and Bunazosin (exemplary of 2-amino substituted Quinazolines), Meobentine and Bethanidine and novel intermediates suitable for use in such methods of synthesis are taught.

Abstract: The subject invention relates to 5-Substituted trans-1-piperazinoindan derivatives having general formula (I), ##STR1## wherein X is halogen, trifluromethyl, alkyl, alkylthio, alkyloxy, hydroxy, alkylsulphonyl, alkyl- or dialkylamino, triflouromethylthio or cyano; R is hydrogen, or alkyl, alkenyl, cycloalkyl, cycloalkyl lower alkyl, optionally substituted with hydroxy, or R is a substituent, ##STR2## wherein n is an integer from 1 to 6; U is CH or N; Y is, CH.sub.2, O, S or N-R.sup.1, R.sup.1 being hydrogen or cycloalkyl, cycloalkylmethyl, alkyl or alkenyl optionally substituted with hydroxy or an optionally substituted phenyl group; W is O or S; Z is --(CH.sub.2).sub.4 --, ##STR3## where R.sup.2 and R.sup.3 are hydrogen or lower alkyl, --CH.dbd.CH--, --CH.dbd.CH--CH.sub.2 --, optionally substituted 1,2-phenylene, 1,2-C.sub.6 H.sub.4 CH.sub.2 -- (to form a quinazolidinone or -thione ring system) or 1,2-C.sub.6 H.sub.

Abstract: N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives, their N-oxide forms and pharmaceutically acceptable salts having gastrointestinal motility stimulating properties, compositions containing these compounds as active ingredient and methods of treating warm-blooded animals suffering from the decreased peristalsis of the gastrointestinal system.

Abstract: A process for the preparation of compounds of formula I ##STR1## wherein the general symbols are as defined in claim 1, which comprises reacting a compound of formula III ##STR2## wherein the general symbols are as defined in claim 1, with a compound of formula IV[H].sub.n --R.sub.1 (IV).

Abstract: The present invention relates to pyridazino[4,5-b]quinolines, and pharmaceutically useful salts thereof, which are excitatory amino acid antagonists and which are useful when such antagonism is desired such as in the treatment of neurological disorders. The invention further provides pharmaceutical compositions containing pyridazino[4,5-b]quinolines as active ingredient, and methods for the treatment of neurological disorders.

Abstract: The present invention relates to pyridazino[4,5-b]quinolines, and pharmaceutically useful salts thereof, which are excitatory amino acid antagonists and which are useful when such antagonism is desired such as in the treatment of neurological disorders. The invention further provides pharmaceutical compositions containing pyridazino[4,5-b]quinolines as active ingredient, and methods for the treatment of neurological disorders.

Abstract: Methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions and inducing anesthesia are disclosed by administering to an animal in need of such treatment a compound which has high binding to the glycine receptor.

Abstract: Antibacterial compounds having the formula ##STR1## and the pharmaceutically acceptable salts, esters and amides thereof, preferred examples of which include those compounds whereinA is .dbd.CR.sup.6 --;R.sup.1 is cycloalkyl of from three to eight carbon atoms or substituted phenyl;R.sup.2 is selected from the group consisting of ##STR2## R.sup.3 is halogen; R.sup.4 is hydrogen, loweralkyl, a pharmaceutically acceptable cation, or a prodrug ester group;R.sup.5 is hydrogen, loweralkyl, halo(loweralkyl), or --NR.sup.13 R.sup.14 ; andR.sup.6 is halogen, loweralkyl, halo(loweralkyl), hydroxy-substituted loweralkyl, loweralkoxy(loweralkyl), loweralkoxy, or amino(loweralkyl),as well as pharmaceutical compositions containing such compounds and the use of the same in the treatment of bacterial infections.

Abstract: This invention pertains to compounds of Formula I including all geometric and stereoisomers, N-oxides, agriculturally-suitable salts thereof, agricultural compositions containing them and their use as fungicides: ##STR1## wherein: Q is O or S; and n, R.sup.1, R.sup.2, X, and Y are described in the text.