Abstract: A process for preparing polycyclic aromatic compounds by cross-coupling aromatic boronic acids with aromatic halogen compounds or perfluoroalkylsulfonates in the presence of metallic palladium, if desired applied to a support material, as catalyst, wherein the coupling is carried out in the presence of a ligand and a base. The process of the invention allows the yield of polycyclic aromatic compounds to be significantly increased in comparison with processes not using a ligand and thus allows a yield optimum for the Pd(0)-catalyzed cross-coupling of aromatic boronic acids with aromatic halogen compounds to be achieved.

Abstract: Compounds of the formula I ##STR1## processes for their preparation, pharmaceutical preparations, use of and method of treatment of disorders in CNS by using compounds of formula I.

Abstract: 3,4,N-triaryl-4,5-dihydro-1H-pyrazole-1-carboxamide compounds having an aryl moiety in the 4-position that is an optionally substituted pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or quinolinyl moiety and aryl moieties in the 3-position and the N-position that are optionally substituted phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or quinolinyl moieties, such as N-(4-chlorophenyl)-4,5-dihydro-3-(4-fluorophenyl)-4-(5-trifluoromethyl-2-p yridinyl)-1H-pyrazole-1-carboxamide, were prepared and found to possess insecticidal utility. 1,2-Diarylethanone compounds were converted to 1,2-diaryl-2-propen-1-one compounds by treatment with bis(dimethylamino)methane, the 1,2-diaryl-2-propen-1-one compounds were converted to 3,4-diaryl-4,5-dihydro-1H-pyrazole compounds by treatment with hydrazine, and the 3,4-diaryl-4,5-dihydro-1H-pyrazole compounds were converted to the insecticidal subject compounds by treatment with an aryl isocyanate.

Abstract: Optical active compounds which are chemically stable, are not colored, have a good optical stability, and which give a liquid crystal composition having a large spontaneous polarization when the compound is incorporated, are provided. The optical active compound have an asymmetric carbon atom fixed by a .delta.-valerolactone ring and the permanent dipole moment derived from the carboxylic group is fixed by the .delta.-valerolactone ring and two alkyl groups which can be regarded as a part of a measogen.

Abstract: Compounds of the Formulae I or II ##STR1## wherein Z and R.sub.1, are as described herein which compounds are muscarinic agonists useful in treating central cholinergic disfunction and pharmaceutical compositions containing the compounds.

Abstract: The present invention provides novel substituted pyrazines or pyrazine derivatives ("NPD") which are functional and have useful application as a monomer for a variety of high performance polymers such as polyester, polyarylate, polycarbonate, polyetherketones, epoxides, polyimides, polyamides, and polyamides-imides. These NPD have the general formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are defined herein.

Abstract: Process for the preparation of compounds of the formula (I) ##STR1## in which R.sup.1, R.sup.2, R.sup.3, X and n have the meaning given in the description, by reacting acetates with carbon monoxide in the presence of a basic auxiliary, followed by alkylation. The products are intermediates for fungicidal acrylates.

Abstract: The present invention relates to new 1-heteroarylazetidines and new 1-heteroarylpyrrolidines endowed with 5-HT.sub.3 agonist activity of formula (IV): ##STR1## The substituents A, R', R.sub.1 and P, and the variables n and m, are as herein described.

Abstract: A compound of the formula ##STR1## V, W, Y, and Z are each independently C--H, oxygen, nitrogen, or sulfur; T is C--H or nitrogen;n is 0 or 1;R.sup.4 is hydrogen or one, two or three substituents independently selected from C.sub.1 -C.sub.4 -alkyl, halo-substituted C.sub.1 -C.sub.4 -alkyl, hydroxy-substituted C.sub.1 -C.sub.4 -alkyl, halogen, hydroxy, C.sub.1 -C.sub.4 -alkoxy, mercapto, amino, mono-(C.sub.1 -C.sub.4 -alkyl)amino, di-(C.sub.1 -C.sub.4 -alkyl)amino, formamido, mono-(C.sub.1 -C.sub.4 -alkyl)amido, di-(C.sub.1 -C.sub.4 -alkyl)amido, cyano, nitro, C.sub.1 -C.sub.4 -alkoxycarbonyl, carboxyl, aminomethyl, mono-(C.sub.1 -C.sub.4 -alkyl)aminomethyl, di-(C.sub.1 -C.sub.4 -alkyl)aminomethyl, wherein free hydroxy and amino groups may be protected.

Abstract: 3(R)-[2-(6-trifluoromethylpyrazin)yl]-1-azabicyclo[2.2.2]octane and its salts, and pharmaceutical formulations thereof are useful in medicine. In particular, they are useful for the treatment of neurological and mental illnesses whose clinical manifestations are due to cholinergic deficiency, and for lowering intraocular pressure. The compound may be prepared by dehydroxylating or decarboxylating the corresponding 3-hydroxy- or carboxy-quinuclidine analogue.

Abstract: Sulfonamide thrombin inhibitors are provided which have the structure ##STR1## including all stereoisomers thereof, wherein n is 1, 2 or 3; m is 0, 1 or 2; R.sup.1 and R.sup.2 are independently H, lower alkyl, cycloalkyl, aryl, heteroaryl or heteroaryl-alkyl, or R.sup.1 and R.sup.2 can be taken together with the N atom to which they are attached to form a 4- to 8-membered ring; R.sup.3 is monocyclic heteroaryl; and R.sup.4 is alkyl, cycloalkyl, aryl, heteroaryl, quinolinyl or tetrahydroquinolinyl, and pharmaceutically acceptable salts thereof.

Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is selected from ##STR2## Y is a bond or lower alkylene; R.sub.2 and R.sub.3 are independently hydrogen, lower-alkyl or halogen;R.sub.4 is ##STR3## R.sub.5 is hydrogen, lower-alkyl or halogen; R.sub.6 is hydrogen, lower-alkyl or halogen;R.sub.7 is hydrogen or lower-alkyl;R.sub.8 is hydrogen, lower-alkyl, or trifluoromethyl;R.sub.9 is lower-alkyl;R.sub.10 is lower-alkyl, trifluoromethyl or difluoromethyl;or pharmaceutically acceptable acid addition salts thereof are useful as antiviral agents.

Abstract: Use of optically active carboxylic esters of oxygen-containing heterocycles as doping substances in liquid crystal mixtures and liquid crystal mixtures containing them.Optically active 1,3-dioxolane-4-carboxylic esters and oxirane-2-carboxylic esters of the general formula (I)R(--A.sup.1).sub.j (--M.sup.1).sub.k (--A.sup.2).sub.l (--M.sup.2).sub.m (--A.sup.3).sub.n --X--Acin whichR.sup.1 is, for example, (C.sub.1 -C.sub.16)-alkyl or (C.sub.1 -C.sub.16)-alkoxy,A.sup.1, A.sup.2, A.sup.3 are, for example, phenyl or pyrimidine-2, 5-diyl,M.sup.1, M.sup.2 are, for example, CO--O, CH.sub.2 --CH.sub.2,j, l are 0, 1, 2,k, m are 0, 1,n is 0, 1, 2,X is O, S andAc is ##STR1## in which R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 for example, H or methyl, are particularly suitable doping substances for liquid crystalline mixtures, since they induce a high spontaneous polarization and effect a substantial decrease in the melting point.

Abstract: The invention relates to a process for making compounds of formula: ##STR1##

Abstract: Fungicidal compounds of the formula (I): ##STR1## and stereoisomers thereof, wherein Y is a specified small group or single atom and R.sup.1 and R.sup.2 are selected from a wide range of specified substituents.

Abstract: This invention encompasses compounds of the formula: ##STR1## and pharmaceutically acceptable non-toxic salts thereof wherein: ##STR2## represents: ##STR3## where n is 0, 1, or 2; R.sub.1 and R.sub.2 are hydrogen or straight or branched chain alkyl groups;Y represents various organic and inorganic substituents;W represents an aromatic group substituted with various organic and inorganic substituents;A is CH or N;B is a substituted or unsubstituted carbon or N; andE is hydrogen or straight or branched alkyl groupsThese 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 type drugs, and enhancement of alertness.

Abstract: The invention concerns an aryl derivative of the formula I, ##STR1## wherein Ar.sup.1 is optionally substituted phenyl, naphthyl or a heterocyclic moiety, and X.sup.1 is oxy, thio, sulphinyl, sulphonyl, difluoromethylene, imino, (1-4C)alkylimino or optionally substituted (1-4C)alkylene, or X.sup.1 is a group of the formula--X.sup.4 --CR.sub.2 -- or --CR.sub.2 --X.sup.4 --whereinX.sup.4 is oxy, thio, sulphinyl, sulphonyl or carbonyl and each R is hydrogen, methyl or ethyl;each of Ar.sup.2 and Ar.sup.3 is optionally substituted phenylene;X.sup.2 is oxy, thio, sulphinyl or sulphonyl;R.sup.1 is (1-4C)alkyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.1 --X.sup.3 --A.sup.2 -- which together with the carbon atom to which A.sup.1 and A.sup.2 are attached define a ring having 5 to 7 ring atoms, wherein each of A.sup.1 and A.sup.2 is (1-3C)alkylene and X.sup.

Abstract: The present invention relates to 4(3H)-pteridinones represented by the formula: ##STR1## in which X is an oxygen atom or a sulphur atom, Y is a hydrogen atom, a lower alkyl radical, especially a methyl radical, at the 6-position or a hydroxyl group at the 7-position, R.sub.1 is a hydrogen atom, a lower alkyl radical, a substituted or unsubstituted phenyl radical, a benzyl radical, a methoxymethyl group, an acetyl group, a 2-acetoxyethyl group or a 2,2,2-trifluoroethyl group and R.sub.2 is a hydrogen atom or a lower alkyl radical, especially a methyl radical.Application of these compounds as anti-allergic drugs.

Abstract: The invention relates to compounds of formula: ##STR1## in which Y represents--either a group Cy--N in whichCy represents a phenyl, optionally substituted; a C.sub.3 -C.sub.7 cycloalkyl group; a pyrimidinyl group or a pyridyl group;or a group ##STR2## in which Ar represents a phenyl, optionally substituted, a pyridyl group; a thienyl group;x is zero or one;X represents a hydroxyl, a C.sub.1 -C.sub.4 alkoxy; a hydroxyalkyl; a C.sub.1 -C.sub.4 acyloxy; a phenacyloxy; a carboxyl; a C.sub.1 -C.sub.4 carbalkoxy; a cyano; an aminoalkylene; a group --N--(X.sub.1).sub.2 in which the groups X.sub.1 independently represent hydrogen, a C.sub.1 -C.sub.4 alkyl; a group ##STR3## in which Alk represents a C.sub.1 -C.sub.6 alkyl; a group ##STR4## in which the Alk.sub.1 is a C.sub.1 -C.sub.3 alkylene and Alk'.sub.1 is a C.sub.1 -C.sub.3 alkyl; a C.sub.1 -C.sub.4 acyl; a group --S--X.sub.2 in which X.sub.2 represents hydrogen or a C.sub.1 -C.sub.

Abstract: Insecticidally active nitro compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, cyano or alkyl,R.sup.2 is hydrogen or an organic radical,R.sup.3 is ##STR2## R.sup.4 is an organic radical, R.sup.5 and R.sup.6 are hydrogen or organic radicals,Y is CH or N, andZ is an optionally substituted 5- or 6-membered heterocyclic group,with certain conditions and exceptions.

Abstract: A p-aminophenol derivative having anti-inflammatory activity, represented by the formula ##STR1## wherein each of R.sup.1 and R.sup.2 is independently a hydrogen atom or a C.sub.1-6 acyl group; Ar is a pyrazine, pyrazine N-oxide, thiazole, benzene, pyridine, pyridazine, pyrimidine or triazine ring; R.sup.3 is a hydrogen atom, a C.sub.1-6 alkyl group, a C.sub.1-6 alkoxy-carbonyl-C.sub.1-6 alkyl group, a C.sub.1-6 alkoxy group, a halogen atom or a carboxy-C.sub.1-6 alkyl group; A is a C.sub.1-6 alkylene group; and B is a C.sub.1-6 alkyl group, or a salt thereof.

Abstract: The present invention relates to a compound of the formula: ##STR1## wherein A is halogen, N(O)mR.sup.1 R.sup.2, N.sup..sym. R.sup.1 R.sup.2 R.sup.3 .multidot.X.sup..crclbar., S(O)nR.sup.1 or S.sup..sym. (O)mR.sup.1 R.sup.2 .multidot.X.sup..crclbar. where R.sup.1, R.sup.2 and R.sup.3 are each optionally substituted hydrocarbon or heterocyclic group, X.sup..crclbar. is a counter anion; m is an integer of 0 or 1; n is an integer of 0 to 2; R.sup.1 and R.sup.2 may form a nitrogen-containing or a sulfur-containing heterocyclic ring, which may further form a condensed ring, with the adjacent nitrogen atom or sulfur atom, and these nitrogen-containing or sulfur-containing heterocyclic rings may have substituents, Z is O or NR.sup.4 where R.sup.

Abstract: An optically active liquid crystal compound which is represented by the formula: ##STR1## wherein R.sub.1 and R.sub.2 each represents an alkyl or aralkyl group of 4-18 carbon atoms, R.sub.3 represents a haloalkyl group, X represents O, COO, OCO, CO or a single bond, Y represents COO, OCO, CH.sub.2 O or OCH.sub.2, Z represents COO or O, (A) represents a cyclic group shown by ##STR2## (B) represents a cyclic group shown by ##STR3## and l shows that the cyclic groups are substituted by at least one halogen atom.

Abstract: Optically active nitrogen-containing heterocycles of the formula I according to claim 1 are suitable as components for ferroelectric liquid crystalline materials.

Abstract: The invention concerns a thiazole of the formula I, ##STR1## wherein Q.sup.1 is an optionally substituted 6-membered monocyclic or 10-membered bicyclic heterocyclic moiety containing one or two nitrogen atoms;X is oxy, thio, sulphinyl, sulphonyl or imino;Ar is phenylene which may optionally bear one or two substituents, orAr is an optionally substituted 6-membered heterocyclene moiety continuing up to three nitrogen atoms;R.sup.1 is hydrogen, (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl or substituted (1-4C)alkyl;R.sup.2 is hydrogen, (1-6C)alkyl, (3-6C)alkenyl, (3-6C)alkynyl or substituted (1-4C)alkyl or R.sup.2 is optionally substituted benzoyl; andQ.sup.2 is optionally substituted thiazolyl; or a pharmaceutically-acceptable salt thereof.The invention also concerns processes for the manufacture of a thiazole of the formula I and pharmaceutical compositions containing said thiazole.

Abstract: Naphthylacetylenes of the formula IR.sup.1 --(A.sup.1 --Z.sup.1).sub.m --A.sup.2 --C.tbd.C--A.sup.3 --(Z.sup.2 --A.sup.4).sub.n --R.sup.2 Iin which R.sup.1, A.sup.1, Z.sup.1, m, A.sup.2, A.sup.3, Z.sup.2, A.sup.4, n and R.sup.2 have the meanings described herein, are suitable as components of liquid crystal phases.

Abstract: Pyrazinone derivatives useful as insecticides have the formula (I): ##STR1## wherein A is N or C-R.sup.1 ; R.sup.1 and R.sup.2 are independently selected from hydrogen, halogen, haloalkyl, cyano or nitro; R.sup.3 and R.sup.4 are independently selected from hydrogen, halogen, alkyl or cycloalkyl; R.sup.5 is cyano, halo, nitro, alkoxy, haloalkyl, haloalkoxy or --S(O).sub.n R.sup.10 ; R.sup.6 is halo, cyano, nitro, haloalkyl, haloalkoxy, alkoxycarbonyl or --S(O).sub.n R.sup.10 ; R.sup.7 is hydrogen, halogen, cyano, nitro, alkyl, alkoxy, alkylthio, haloalkylthio, alkoxycarbonyl, NR.sup.11 R.sup.12 or haloalkyl; R.sup.8 is H, halo, NR.sup.11 R.sup.12, alkyl, cycloalkyl or S(O).sub.n R.sup.10 ; and R.sup.9 is oxygen or sulphur; where n is 0, 1 or 2; and R.sup.10 is alkyl, haloalkyl or cycloalkyl and R.sup.11 and R.sup.12 are independently selected from hydrogen, alkyl, cycloalkyl, benzyl or substituted benzyl.

Abstract: The compound (R)-3-[2-(6-chloropyrazin)yl]-1-azabicyclo[2.2.2]octane and its salts behave as M.sub.1, M.sub.3 muscarinic agonists and are useful in the treatment of neurological and mental disorders, preferably in a pharmaceutical formulation comprising the active compound in association with a pharmaceutically acceptable carrier. The compound can be prepared by via methods analogous to those known in the art and a chiral acid resolution.

Abstract: Insecticidally active substituted heteroaryl phenyl ethers of the formula ##STR1## in which Het represents an optionally substituted heteroaromatic radical,X represents O, S, --CH.sub.2 --, --O--CH.sub.2 --, --S--CH.sub.2 --, --CH.sub.2 --O--, ##STR2## Y represents O, --O--CH.sub.2 -- or S, Z represents an optionally substituted aromatic or heteroaromatic radical;m represents integers from 1-4n represents 0, 1, 2, 3, 4O represents 0, 1, 2, 3, 4, provided than n and o do not simultaneously represent 0p represents integers from 1-4,R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 independently of one another represent hydrogen, C.sub.1 -C.sub.6 -alkyl which is optionally substituted; two radicals adjacent to one another can also, together with the C atoms to which they are bonded, form a saturated carbocyclic 5- or 6-ring,R.sup.1 represents identical or different radicals hydrogen, halogen, CN, C.sub.1-4 -alkyl, 1-5-halogeno-C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy, C.sub.1-4 -alkylthio, 1-5-halogeno-C.sub.

Abstract: This invention concerns a process for killing internal parasites, especially nematodes, trematodes and cestodes affecting warm blooded animals such as sheep, cattle, swine, goats, dogs, cats, horses and humans as well as poultry by administering an effective amount of a compound of the Formula I. ##STR1## The compounds are readily prepared by conventional chemical reactions.

Abstract: Novel aminomethyloxooxazolidinyl arylbenzene derivatives, wherein the aryl includes the phenyl, substituted phenyl, pyridyl, and substituted pyridyl groups, such as (l)-N-{3-[4- (4'-pyridyl)phenyl]-2-oxooxazolidin-5-ylmethyl}acetamide, possess useful antibacterial activity.

Abstract: Compounds of the Formula I: ##STR1## and pharmaceutically acceptable salts thereof are leukotriene antagonists. These compounds inhibit SRS-A and leukotriene synthesis and are antagonists of SRS-A and are thus useful in the treatment of asthma, allergic disorders, inflammation, skin diseases and certain cardiovascular disorders.

Abstract: Compounds of the general formula (I) ##STR1## and physiologically acceptable salts and solvates thereof, which have .beta..sub.2 -adrenoreceptor stimulant activity. They may be used in the treatment of diseases associated with reversible airways obstruction, such as asthma and chronic bronchitis.In preferred embodiments, Q represents a chlorine atom or a trifluoromethyl group, X represents a C.sub.3-4 alkylene chain, Y a C.sub.1-5 alkylene chain, R, R.sup.1 and R.sup.2 are each preferably a hydrogen atom or a methyl group and Het represents a pyrimidinyl pyrazinyl, triazinyl, thiazolyl, quinolinyl, benzimidazolyl, benzothiazolyl, benzoxazolyl or pyridyl group.

Abstract: Pyrazine derivatives useful as plant growth regulating agents have the general formula: ##STR1## and stereoisomers thereof, wherein R.sup.1 is C.sub.1 -C.sub.4 alkyl optionally substituted with halogen, or cyclopropyl optionally substituted with C.sub.1 -C.sub.4 alkyl; R.sup.2 is C.sub.1 -C.sub.8 alkyl, C.sub.2 -C.sub.8 alkenyl, or C.sub.2 -C.sub.8 alkynyl each optionally substituted with halogen; C.sub.3 -C.sub.6 cycloalkyl, C.sub.3 -C.sub.6 cycloalkenyl, C.sub.3 -C.sub.6 cycloalkylalkyl, C.sub.3 -C.sub.6 cycloalkenylalkyl, phenylalkenyl or phenylalkynyl each optionally substituted on the ring group; R.sup.3 is hydrogen or C.sub.1 -C.sub.4 alkyl; R.sup.4 is hydrogen, C.sub.1 -C.sub.4 alkyl, halogen, alkylamino, cyano, or alkoxy; n is 0 or 1; and salts, ethers, acylates and metal complexes thereof.

Abstract: Compounds of formula I ##STR1## wherein X.sup..crclbar. is Cl.sup..crclbar. or Br.sup..crclbar.,M is Cu.sup.2.sbsb..sym. or Ni.sup.2.sbsb..sym.,Z is a halogen atom, --NH.sub.2, C.sub.1 -C.sub.4 alkyl or C.sub.2 -C.sub.4 alkoxy,R.sup.1 is H, methyl methoxy, halogen or --NH.sub.2, andA is a group ##STR2## wherein R.sup.2 and R.sup.3 each independently have the same meaning as R.sup.1.The compounds are simultaneously cryochromic or thermochromic and are suitable as warning indicators for cooled or heated structural elements.

Abstract: Novel compositions are prepared from (1) amino substituted pyrazine compounds such as pyrazinamine and (2) at least one of (a) a carboxylic acid, (b) carboxylic acid anhydride, (c) carboxylic acid ester or (d) combination thereof, such as tall oil fatty acid, and (3) optionally in the presence of sodium hydride. These novel compositions are useful as oil and gas well corrosion inhibitors.

Abstract: Compounds of the formula ##STR1## where Het is a heterocyclic group, n is an integer of 0 to 2 and R.sup.1 is hydrogen or lower alkyl are protease inhibitors useful as anti-plasmin and anti-thrombin agents.

Abstract: There are disclosed compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, lower alkyl, aryl or halo, or R.sup.1 and R.sup.2 taken together represent ##STR2## where the dotted lines represent optional double bonds; R.sup.3, R.sup.4 and R.sup.5 are each, independently, hydrogen, lower alkyl, aryl or halo;R.sup.6 is 2-pyridinyl, 2-pyrazinyl, 2-quinolyl, 2-quinoxalinyl or any of the foregoing R.sup.6 moieties substituted by lower alkyl, lower alkoxy, trifluoromethyl, cyano, nitro or halo; or ##STR3## wherein R.sup.7 is phenyl, 2-pyridinyl, 2-pyrimidinyl, 3-pyridazinyl or 2-pyrazinyl or any of the foregoing R.sup.7 moieties substituted by lower alkyl, lower alkoxy, halo, cyano, trifluoromethyl or nitro;Z is ##STR4## X is lower alkylene, vinylene, O or NH; m is 1-5;n is 0-4;p is 1-4;q is 1-2;and the pharmaceutically acceptable salts thereof, and their use as antipsychotic/anxiolytic agents having a low liability for extrapyramidal side effects.

Abstract: Liquid Crystal compounds represented by the following formula are disclosed. ##STR1## wherein R and R' are independently selected from alkyl groups containing 1.about.20 carbon atoms; X is --O--, --O--CO--O-- or direct bond; A.sub.1 and A.sub.2 are independently cyclic groups (such as phenylene and biphenylene), said cyclic groups may be substituted with 1.about.4 fluorine, chlorine or bromine atoms, or 1 or 2 substituent groups selected from the group consisting of cyano, nitro and trifluoromethyl groups; Y is --CO--O--, --O--CO--, --C.tbd.C--, --CH.sub.2 O--, --OCH.sub.2 --, --CH.dbd.N--, --N.dbd.CH--, --N.dbd.N--, --CH.sub.2 S--, --SCH.sub.2 -- or direct bond; and * represents asymmetric atom providing optical activity.

Abstract: This invention pertains to novel substituted N-heterocyclic-N-(4-piperidinyl)amides useful as analgesics and antagonists of opiods, wherein the compounds have the general formula: ##STR1## including optically active isomeric forms, and the pharmaceutically acceptable acid addition salts thereof, wherein:R is a substituted or unsubstituted unsaturated heterocyclic ring system having 5 to 6 cyclic member atoms containing at least one nitrogen atom, and is preferably selected from the group consisting of pyridinyl, pyrimidinyl, and pyrazinyl;R.sub.1 is selected from the group consisting of unsubstituted or substituted heterocyclic ring systems having 5 cyclic member atoms, lower cyclic alkyl ring systems, lower-alkyl and lower-alkoxy lower-alkyl, and is preferably selected from the group consisting of furanyl lower-alkyl, thienyl lower-alkyl, pyrrolyl lower-alkyl, lower-alkyl, lower-cycloalkyl, and lower-alkoxy lower-alkyl of 2 to 6 carbons;R.sub.

Abstract: This invention relates to imidazolidinone compounds of the formula ##STR1## wherein Q is methylene group or a single bond:R is a heterocyclic group selected from the group consisting of pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl and 1,3-thiazolyl which may be unsubstituted or with a substituent selected from the group consisting of lower alkyl, lower alkoxy and halogen atom, wherein R is bonded to Q or, when Q is a single bond, to the imidazolidinone ring, through the carbon atom of R;the ring A is an unsubstituted phenyl or a substituted phenyl having 1 or 2 substituent(s) selected from the group consisting of lower alkyl, lower alkoxy, halogen, lower alkylthio, trihalogeno-lower alkyl and nitro;Y is vinylene group or ethynylene;m is a integer from 1 to 6 andn is 0, 1 or 2,or a pharmacetically acceptable salt thereof.These compounds aer useful as cerebral activators, anti-depressants and nootropic drugs.

Abstract: Cognitive deficiencies and/or neurological function deficits and/or mood and/or mental disturbances are treated by the administration of 3,3-disubstituted indolines. The indolines have the formula: ##STR1## wherein: p is 0 or 1;Z is O or S;R is C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.8 cycloalkyl, 2-pyridyl, 3-pyridyl, 4-pyridyl or ##STR2## V, W, X, and Y independently are H, halo, C.sub.1 -C.sub.3 alkyl, OR.sup.1, NO.sub.2, CF.sub.3, CN or NR.sup.1 R.sup.2 ;R.sup.1 and R.sup.2 independently are H or C.sub.1 -C.sub.3 alkyl; ##STR3## independently are 6-membered heterocyclic aromatic rings containing at least one nitrogen atom as a part of the ring optionally substituted with one substituent selected from the group C.sub.1 -C.sub.3 alkyl, halo, OR.sup.1 or NR.sup.1 R.sup.2 ; oran N-oxide or pharmaceutically suitable acid addition salt thereof.

Abstract: Compounds of the formula ##STR1## where HET is a heterocyclic group, n is an integer of 0 to 2 and R.sup.1 is hydrogen or lower alkyl are protease inhibitors use as anti-plasmin and anti-thrombin agents.

Abstract: Disclosed are compounds of the formula ##STR1## wherein: R.sup.1 is a lower alkyl group;R.sup.2 and R.sup.3 are each hydrogen or lower alkyl or R.sup.2 and R.sup.3 taken together may form --(CH.sub.2 (.sub.4)-- or --CH.dbd.CH--CH.dbd.CH--;.alpha. is a 5- or 6-membered heteroaromatic ring group containing 1 to 3 hetero-atoms selected from the group consisting of nitrogen, oxygen and sulfur, or a pyrazine-N-oxide ring, pyridazine-N-oxide ring or pyrimidine-N-oxide ring group, wherein each of these heteroaromatic ring groups may optionally have 1 to 3 substituents selected from the group consisting of a lower alkyl, halogen, phenyl, lower alkoxycarbonyl, amino, lower alkoxy and hydroxy-lower alkyl, with the proviso that said 5- or 6-membered heteroaromatic ring group is not thiazolyl, isothiazolyl, pyridyl or 1,3,5-triazinyl group; or salts thereof. These compounds and salts thereof have anti-inflammatory activity and lipoxygenase-inhibitory activity.

Abstract: Novel compositions are prepared from (1) amino substituted pyrazine compounds such as pyrazinamine and (2) at least one of (a) a carboxylic acid, (b) carboxylic acid anhydride, (c) carboxylic acid ester or (d) combination thereof, such as tall oil fatty acid, and (3) optionally in the presence of sodium hydride. These novel compositions are useful as oil and gas well corrosion inhibitors.

Abstract: Novel heterocyclic compounds of the formula ##STR1## wherein, R.sup.1 represents a hydrogen atom or an alkyl group, A represents an ethylene group which may be substituted by alkyl or a trimethylene group which may be substituted by alkyl, X represents an oxygen or sulfur atom or the group ##STR2## in which R.sup.2 represents a hydrogen atom of an optionally substituted alkyl, an alkenyl, an alkynyl or an acyl group, and R.sup.3 represents a hydrogen atom or an alkyl group, and Z represents an optionally sibstituted 5- or 6-membered heterocyclic group which contains at least two hetero atoms selected from oxygen, sulfur and nitrogen atoms, or an optionally substituted 3- or 4-pyridyl group.The above defined novel heterocyclic compounds of formula (I) exhibit powerful insecticidal properties.

Abstract: Optically active nitrogen-containing heterocycles of the formula I according to claim 1 are suitable as components for ferroelectric liquid crystalline materials.

Abstract: There are disclosed compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, lower alkyl, aryl or halo, or R.sup.1 and R.sup.2 taken together represent ##STR2## where the dotted lines represent optional double bonds; R.sup.3, R.sup.4 and R.sup.5 are each, independently, hydrogen, lower alkyl, aryl or halo;R.sup.6 is 2-pyridinyl, 2-pyrazinyl, 2-quinolyl, 2-quinoxalinyl or any of the foregoing R.sup.6 moieties substituted by lower alkyl, lower alkoxy, trifluoromethyl, cyano, nitro or halo; orR.sup.6 is ##STR3## wherein R.sup.7 is phenyl, 2-pyridinyl, 2-pyrimidinyl, 3-pyridazinyl or 2-pyrazinyl or any of the foregoing R.sup.7 moieties substituted by lower alkyl, lower alkoxy, halo, cyano, trifluoromethyl or nitro;Z is --(CH.sub.2).sub.

Abstract: A series of diazinylpiperidine compounds of Formula I ##STR1## wherein X is an ethylene chain or a 1,2-benzo ring; Y is carbonyl or methylene; R.sup.1 is hydrogen or lower alkyl; and Z is an R.sup.2, R.sup.3 -disubstituted diazinyl ring selected from pyridazine, pyrimidine, and pyrazine ring systems. Pharmacologic and neuroanatomical testing demonstrates that compounds of the series act to enhance cerebral function in mammals, particularly when there is a deficit in normal cerebral functioning. Specific pharmacologic test results indicate that compounds of Formula I possess cognition and memory enhancing activity.

Abstract: A pyrazolopyridine compound of the formula: ##STR1## or a salt thereof, wherein each symbol is as defined in the specification. Said compounds exhibit antiinflammatory, analgesic, antipyretic, antiallergic, antiarthritic, antirheumatic activities or inhibitory activities on platelet aggregation.