Abstract: A process for the preparation of Phosphodiesterase IV inhibitors is described. The process consists of eight chemical steps involving five isolations to prepare the title compound from readily available isovanillin in 35% overall yield (Scheme 1). The process is highlighted by: a) a highly diastereoselective Michael addition of phenyllithium using (1R, 2S) cis-aminoindanol as a chiral auxiliary, b) highly crystalline intermediates providing for efficient purifications, c) crystallization of the final compound as its CSA salt for excellent enantiomeric purity.

Abstract: The present invention provides a method for producing a alcohol including an optically active alcohol by hydrogenating a carbonyl compound in the presence of a homogeneous catalyst, a base and a nitrogen-containing organic compound. Thus, the reaction employs an inexpensive catalyst and proceeds in high yield and high efficiency.

Abstract: A process for the preparation of a compound of structural formula I ##STR1## wherein R.sup.1 is alkyl, alkenyl, phenyl or substituted phenyl, which comprises the addition of R.sup.1 to an intermediate 2: ##STR2## by treatment of 2 with (R.sup.1).sub.3 M followed by reductive removal of the sulfinyl group.

Abstract: A cyclobutenedione derivative. It comprises substituted or non-substituted aromatic group A; conjugated chain B which may contain an aromatic bonding group; and hydrogen bonding or ion bonding cyclobutenedionyl group C having an aromatic group which is bonded to the conjugated chain B, wherein A and B and C are bonded in the form of A--B--C. Crystal of the derivative is used as a non-linear optical device.

Abstract: 3-(Het)arylcarboxylic acid derivatives of the formula I ##STR1## where R is formyl, CO.sub.2 H or a radical hydrolyzable to COOH and the other substituents have the following meanings:R.sup.2 and R.sup.3 are each halogen, alkyl, haloalkyl, alkoxy, haloalkoxy or alkylthio;X is nitrogen or CR.sup.14, where R.sup.14 is hydrogen or, together with R.sup.3, forms an alkylene or alkenylene chain, in each of which a methylene group is replaced by oxygen;R.sup.4 is phenyl or naphthyl, each of which is unsubstituted or substituted or an unsubstituted or substituted five-membered or six-membered heteroaromatic structure containing one to three nitrogen atoms or one sulfur or oxygen atom;R.sup.5 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, haloalkyl, alkoxyalkyl, alkylthioalkyl or phenyl;R.sup.6 is C.sub.1 -C.sub.8 -alkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl or C.sub.3 -C.sub.

Abstract: This invention relates to a process of making a compound of formula I ##STR1## where R.sub.1 contains an .alpha.,.beta.-unsaturated carbonyl group & R.sub.n is hydrogen or nonhydrogen radicals which do not have a functional group which interferes with the coupling reaction, which process comprises coupling a thiolphenol or phenylalkylmercaptan with a chloromethylpyridine in the presence of DBU under an inert atmosphere. These compounds are leukotriene antagonists and as such can be used in treating various diseases associated with leukotrienes.

Abstract: Provided is a process for preparing chloroalkyl pyridinium hydrochloride compounds and various regioisomers and analogs thereof having substantially high purity levels and yields and a free-flowing, non-dusting form.

Abstract: This invention relates to certain 1,3,3-(trisubstituted)cyclohex-1-ene monomers and related compounds which are useful in treating allergic and inflammatory diseases and for inhibiting the production of Tumor Necrosis Factor (TNF).

Abstract: This invention relates to a compound of formula 1 ##STR1## or an N-oxide, or a pharmaceutically acceptable salt, where A is CH.sub.2 and Z is S(O).sub.q where q is 0, 1 or 2, CH.sub.2, CHOH, CO, NR.sub.x, or O, orA is C.dbd.O and Z is NR.sub.x ;m is 0-5;R.sub.x is hydrogen or lower alkyl;R is C.sub.1 to C.sub.20 -aliphatic, unsubstituted or substituted five-membered heteroaryl-C.sub.1 to C.sub.10 -aliphatic-O--, unsubstituted or substituted phenyl-C.sub.1 to C.sub.10 -aliphatic where substituted p from the group consisting of lower alkoxy, lower alkyl, trihalomethyl, and halo, or R is C.sub.1 to C.sub.20 -aliphatic-O--, or R is unsubstituted or substituted phenyl-C.sub.1 to C.sub.10 -aliphatic-O-- where substituted phenyl has one or more radicals selected from the group consisting of lower alkoxy, lower alkyl, trihalomethyl, and halo;R.sub.1 is R.sub.4, --(C.sub.1 to C.sub.5 aliphatic)R.sub.4, --(C.sub.1 to C.sub.5 aliphatic)CHO, --(C.sub.1 to C.sub.5 aliphatic)CH.sub.2 OR.sub.5;R.sub.2 and R.sub.

Abstract: Intermediates for the preparation of benzothiazole derivatives useful for the prevention and treatment of diseases for which an inhibitory action against the production of leukotriene and thromboxane is efficacious, and industrially advantageous processes for the preparation of the intermediates.

Abstract: The invention relates to new pyridine derivatives of general formula I which have useful properties, e.g., as leukotriene-B.sub.4 -antagonists. Pharmaceutical compositions containing these compounds can be used to treat various diseases.

Abstract: Compounds of the formula ##STR1## the symbols have the meaning described in the specification have retinoid-like biological activity.

Abstract: A pharmaceutical composition which comprises a pharmaceutically effective amount of a compound of the formula ##STR1## wherein R.sup.1 represents a hydrogen atom,R.sup.2 represents --(CH.sub.2).sub.m -Awherein m is an integer of 0 to 3, andA represents pyridyl which is unsubstituted or is substituted by C.sub.1 -C.sub.3 alkyl said alkyl being unsubstituted or substituted by phenyl, and R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 each independently represent a hydrogen atom, a halogen atom, C.sub.1 -C.sub.5 alkyl which is unsubstituted or is substituted with a halogen atom or --OR.sup.13 wherein R.sup.13 represents a hydrogen atom or C.sub.1 -C.sub.5 alkyl which is unsubstituted or is substituted with a halogen atom or phenyl, or when their adjacent substituents are taken together, they represent C.sub.1 -C.sub.3 oxyalkylene having one or two oxygen atoms;or a pharmaceutically acceptable salt thereof, anda pharmaceutically acceptable carrier therefor.

Abstract: Leukotriene-B.sub.4 analogs of formula I ##STR1## in which R.sup.1 means radical COOR.sup.2 with R.sup.2 meaning a hydrogen atom or a (C.sub.1 -C.sub.4)-alkyl group or R.sup.1 means radical CH.sub.2 OH,B means an alkylene group with 1-3 C atoms in the chain, a radical ##STR2## or a radical ##STR3## with R.sup.3 meaning a hydrogen atom, a carboxy or methoxycarbonyl group, A means groups ##STR4## --NH--CO--, --CO--NH--, --OCH.sub.2 --, --CH.dbd.CH--, --C.tbd.C--, --COCH.sub.2 -- or --CHOH--CH.sub.2 --,X means N or CH,D means groups or ##STR5## and . . . . . means a single or double bond, as well as optionally their salts with physiologically harmless bases, process for their production and their pharmaceutical use.

Abstract: Compounds of the formula ##STR1## wherein the symbols have the meaning defined in the specification.

Abstract: Compounds having the general formula: ##STR1## wherein each of R.sup.1 and R.sup.2 independently represents hydrogen or alkyl of 1 to 4 carbon atoms;A represents --O-- or --CR.sup.4 R.sup.5, where R.sup.4 and R.sup.5 are defined as for R.sup.1 or R.sup.2 ;R.sup.3 represents an adamantyl group; andPy represents a 3- or 4-pyridyl group, as free bases or their pharmaceutically acceptable salts are useful in treating androgen-dependent, especially prostatic, cancer.

Abstract: Compounds having the formula ##STR1## wherein Q is ##STR2## R.sup.1 is C.sub.1 -C.sub.8 alkyl; R.sup.2 is C.sub.6 -C.sub.18 aryl, unsubstituted or substituted with one or more C.sub.1 -C.sub.6 alkyl, halo, C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 haloalkyl; or C.sub.4 -C.sub.17 heterocyclic aryl comprising one or more oxygen or nitrogen atoms;X is nitrogen or --CH--; andn is 2, 3 or 4,or a stereoisomer thereof, with the proviso that when Q is ##STR3## and X is N, then R.sup.2 is not phenyl or substituted phenyl. These compounds are useful as fungicides.

Abstract: Novel 1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols, intermediates and processes for the preparation thereof, and methods of reducing inflammation and cell proliferation, and relieving memory dysfunction, and inhibiting bacterial and fungal growth fire disclosed.

Abstract: The small nonpeptides of the instant invention are tachykinin antagonists. The compounds are highly selective and functional NK.sub.3 antagonists expected to be useful in the treatment of pain, depression, anxiety, panic, schizophrenia, neuralgia, addiction disorders, inflammatory diseases, gastrointestinal disorders, vascular disorders, and neuropathological disorders.

Abstract: A compound of the formula:A--CH.sub.2 CH.sub.2 --O--B[wherein A stands for an aromatic ring residue, a group shown by R.sup.1 --CO-- (wherein R.sup.1 stands for an aliphatic hydrocarbon residue, aromatic hydrocarbon residue, a heterocyclic residue, an aromatic alipahtic hydrocarbon residue or an alicyclic hydrocarbon residue) or R.sup.2 --CH.dbd.CH-- (wherein R.sup.2 stands for an aliphatic hydrocarbon residue an aromatic hydrocarbon residue a heterocyclic residue an aromatic aliphatic hydrocarbon residue or an alicyclic hydrocarbon residue), and B stands for an aromatic ring residue], can be obtained in high yield, at high purity level by short reaction time, by reacting a compound of the formula:A--CH.sub.2 CH.sub.2 --X(wherein A is of the same meaning as defined above, and X stands for a leaving group) with a compound represented by the general formula:MO--B(wherein M stands for an alkali metal atom or an alkaline earth metal atom and B is of the same meaning as defined above) in a non-aqueous solvent.

Abstract: Provided is a process for preparing chloroalkyl pyridinium hydrochloride compounds and various regioisomers and analogs thereof having substantially high purity levels and yields and a free-flowing, non-dusting form.

Abstract: Compounds of the formula ##STR1## where A-B-D, R.sup.1, R.sup.2 and R.sup.3 have the meanings stated in the description, and their preparation are described. The compounds are suitable for controlling diseases.

Abstract: A novel 6-chloro-3-vinyl-pyridine of formula ##STR1## where X represents -H, -SO.sub.2 Ph, -CO.sub.2 Et, -COCH.sub.3 and -CHO; which is used for the synthesis of Epibatidine of formula ##STR2## by reacting said 6-chloro-3-vinyl pyridine with N-1-alkyl-2,5-di(trialkyl silyl) pyrrolidine of formula ##STR3## to obtain N-alkyl Epibatidine which is hydrogenated to obtain the Epibatidine.

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: This invention relates to 1-aryl-3-pyridinyl-2-propene-1-ones, the use of these compounds as calcium uptake inhibitors in leukocytes and thrombocytes, and pharmaceutical compositions containing these compounds as active ingredients, and the process of their preparation.

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: Ionic monomeric diallylammonium compounds having a targeted combination of diallylammonium cations with selected anions have particularly high and constant charge control properties and very good heat stabilities and dispersibilities.The compounds according to the invention are outstandingly suitable for use as colorless charge control agents in toners and developers for electrophotographic recording processes and for use as charge-improving agents in powders and paints for surface coating, in particular in triboelectrically or electrokinetically sprayed powder paints.

Abstract: Bis(perfluorosulphonyl)methanes, process for preparing same and uses thereof. The compounds of the invention are based on the formula (1/nM)+[(R.sub.F SO.sub.2).sub.2 CY].sup.- in which Y denotes an electron-attracting group chosen from --C.dbd.N and RZ groupings in which Z denotes a carbonyl grouping, sulphonyl grouping or a phosphonyl grouping and R denotes an organic monovalent grouping, M denotes a metal having valency n or an organic group capable of existing in the cationic form, R.sub.F denotes a perfluoroalkyl or perfluoroaryl grouping. Said compounds are especially useful in the production of electrochemical devices.

Abstract: The present invention relates to a leukotriene-B.sub.4 analog according to formula I ##STR1## in which R.sup.1 is a COOR.sup.2 group, wherein R.sup.2 is a C.sub.2-4 -alkyl group;B is a C.sub.1-3 -alkylene group, a radical ##STR2## wherein R.sup.3 is a hydrogen atom or a carboxy or methoxycarbonyl group; ##STR3## . . . is a single or double bond; or optionally, their salts with physiologically compatible bases. The present invention also relates to the production of the latter leukotriene-B.sub.4 analogs and their use as pharmacological agents.

Abstract: Polishes for metal surfaces, based on dispersions of waxes, fluorinated polymers and perfluoropolyoxyalkylene oils acquire high gloss characteristics combined with improved water-repellency and resistance to soiling of 0.1-5% by weight of at least a cationic emulsifier comprised in the general formula(I) R-L-Q.sup.+ X.sup.-where:R=a chain of perfluoropolyoxyalkylene units;L=a divalent organic group;Q=a polar group;X=a halogen, or a group of formulaCH.sub.3 -Phenylene-SO.sub.3.sup.-R"SO.sub.3.sup.-R"=F-(CF.sub.2).sub.m -;t=1 or 2;m=1-4.The polished containing the emulsifiers of formula (I) as well as the compounds comprised in said formula are claimed as new products.

Abstract: The invention relates to new tetrahydropyridine derivatives, processes for preparing them and their use as pharmaceutical compositions with cholinomimetic properties.

Abstract: This invention relates to 1-phenyl-3-aryl-2-propyne-1-ones, the use of these compounds as calcium uptake inhibitors in leukocytes and thrombocytes, and pharmaceutical compositions containing these compounds as active ingredients, and the process of their preparation.

Abstract: New substituted pyridines are prepared by reducing suitably substituted pyridine derivatives. The new substituted pyridines are suitable as active compounds in pharmaceuticals, in particular for the treatment of hyperlipoproteinaemia.

Abstract: Chiral, nonracemic compounds of the general formula: ##STR1## wherein m and n are either both zero, both equal one or n is equal to one and m is equal to zero, X and Y and Z are halogens, R' is an alkyl, alkoxyl, alkenyl, thioalkyl, thioether, ether, or alkylsilyl group containing three to fifteen carbon atoms, and R is an alkyl group having one to fifteen carbon atoms and where Ar is:--A.sub.a --(E).sub.e --B.sub.b --(F).sub.f --D.sub.d --where A, B and D independently of one another are aromatic rings which are selected from the group consisting of a phenyl, a pyridine ring, a pyrimidine ring, a pyridizine ring, a pyrazine ring and a thiadiazole ring, wherein a, b and d are integers from 0-3 such that a+b+d=2-3, where E and F independently of one another are linking groups selected from the group consisting of a --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --O--, --CH.sub.2 --S--, --O--CH.sub.2 --, --S--CH.sub.

Abstract: Indane-1, 3-dione derivatives of the following general formula [I]: ##STR1## and herbicidal compositions containing them as an active ingredient are provided. The derivatives are highly valuable in exhibiting excellent herbicidal activity while causing markedly low damage on crops.

Abstract: This invention relates to compounds having selective LTB.sub.4 antagonist properties, compositions comprising said compounds and methods for the treatment of disorders involving LTB.sub.4 agonist-mediated activity utilizing said compositions wherein the compounds are described by the general formula ##STR1## and pharmaceutically acceptable salts thereof.

Abstract: Optically active compounds of the formula ##STR1## wherein m stands for the number 1 and R.sup.2 is an unsubstituted or halogen-substituted alkyl or alkenyl group in which optionally one methylene group is replaced by oxygen and/or optionally one methylene group is replaced by an ester group --COO-- or --OOC--; or m stands for the number 0 or 1 and R.sup.2 denotes a group of the formula ##STR2## R.sup.1 and R.sup.3 each independently represent an alkyl or alkenyl group in which optionally one methylene group is replaced by oxygen; Z.sup.1, Z.sup.2 and Z.sup.3 each independently are a single covalent bond, --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 CH.sub.2 --, --COO-- or --OOC--; n stands for the number 0 or 1; rings A.sup.1 and A.sup.2 each independently are unsubstituted or halogen, cyano and/or methyl-substituted 1,4-phenylene in which optionally 1 CH group or 2 CH groups is/are replaced by nitrogen; and C.sup.* denotes a chiral carbon atom; with the proviso that simultaneously R.sup.

Abstract: The present invention relates to new tetralones having formula I: ##STR1## wherein R.sup.1 to R.sup.7 are as defined in claim 1. The invention also relates to processes for their preparation, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments. These compounds are antihypertensive and bronchodilator agents.

Abstract: The present invention discloses pesticidally active compounds of formula (II) ##STR1## or a salt thereof, wherein Q is an monocyclic aromatic ring, or fused bicyclic ring system of which at least one ring is aromatic containing 9 or 10 atoms of which one may be nitrogen and the rest carbon each ring system being optionally substituted, or Q is a dihalovinyl group or a group R.sup.6 --C.tbd.C-- where R.sup.6 is C.sub.1-4 alkyl, tri C.sub.1-4 alkylsilyl, halogen or hydrogen; R.sup.2, R.sup.3 , R.sup.4 and R.sup.5 are the same or different with at least one being hydrogen and the others being independently selected from hydrogen, halo, C.sub.1-4 alkyl or C.sub.1-4 haloalkyl; and R.sup.1 is selected from hydrogen and C.sub.1-8 hydrocarbyl optionally substituted by dioxalanyl, halo, cyano, trifluoromethyl, trifluoromethylthio or C.sub.1-6 alkoxy and X.sup.1 is hydrogen, fluoro or chloro.

Abstract: N-fluoropyridinium salts of the following formula are prepared by reacting a pyridine compound with a Br nsted acid and fluorine, wherein the reaction solvent contains a greater than equimolar amount of the pyridine compound relative to an amount of the Br nsted acid. ##STR1## The method can produce N-fluoropyridinium salts with a high yield.

Abstract: Oxyalkyne compounds corresponding to the formula I ##STR1## in which the substituent Y in the meta- or para-position is R.sup.1 represents CH.sub.3 or NH.sub.2, R.sup.2 represents H or CH.sub.3, R.sup.3 represents H, C.sub.1-3 -alkyl or COCH.sub.3, and Ar represents an aromatic residue selected from the group ##STR2## with the proviso that the substituents R.sup.4, R.sup.5 and R.sup.6 are the same or different and each substituent represents H, F, Cl, Br, C.sub.1-6 -alkyl, CF.sub.3 or C.sub.1-6 -alkoxy, and R.sup.7 represents H, F, Cl, Br, C.sub.1-3 -alkyl or CF.sub.3,in the form of their racemates or mixtures of diastereoisomers or in optically active form, which are suitable active ingredients in pharmaceutical compositions.

Abstract: The invention concerns the use of a compound of formula (I) ##STR1## wherein R and R.sub.1, each independently, represent a hydrogen atom or a methyl group, and its pharmaceutically acceptable acid addition salts, as free radical scavengers. The pharmaceutical compositions containing these compounds may be employed in the treatment and/or prevention of pathological processes involving cell damage due to the formation of free radicals.The invention also concerns the compounds of formula (I) wherein at least one of R and R.sub.1 is methyl, which are new compounds, as well as the process for the preparation thereof and the pharmaceutical compositions containing them.

Abstract: The invention concerns novel, pharmaceutically useful 1,3-dioxane alkenoic acid derivatives of the formula I containing a pyridyl moiety at position 4 of the dioxane ring and in which the groups at positions 2, 4 and 5 have cis-relative stereochemistry, X is hydrogen, alkoxy or hydroxy, Y is vinylene, n is 1 or 2, A.sup.1 is alkylene, R.sup.1 is a variety of substituents defined hereinafter, and R.sup.2 is hydroxy, a physiologically acceptable alcohol residue or alkanesulphonamido, and the pharmaceutically acceptable salts thereof. The invention also includes processes for the manufacture and use of the acid derivatives as well as pharmaceutical compositions for therapeutic use in one or more of a variety of diseases such as ischaemic heart disease, cerebrovascular disease, asthmatic disease and/or inflammatory disease.

Abstract: Thioformamide derivatives of the formula (I) ##STR1## wherein R represents an alkyl group; A represents either:(1) a phenyl group which is optionally substituted; or(2) heteroaromatic group (e.g. pyrid-3-yl, quinolin-3-yl);Y represents:an ethylene or methylene group or a direct bond; and B represents either:a) a phenyl, pyridyl, furyl or thienyl group, each of which may be optionally substituted, orb) a straight- or branched-chain alkyl, alkenyl, or cycloalkyl group, each of which may be optionally substituted.These compounds may be formulated into pharmaceutical preparations and have utility in the treatment of disorders associated with smooth muscle contraction.

Abstract: Optically active compounds of the formula ##STR1## wherein m stands for the number 1 and R.sup.2 is an unsubstituted or halogen-substituted alkyl or alkenyl group in which optionally one methylene group is replaced by oxygen and/or optionally one methylene group is replaced by an ester group --COO-- or --OOC--; or m stands for the number 0 or 1 and R.sup.2 denotes a group of the formula ##STR2## R.sup.1 and R.sup.3 each independently represent an alkyl or alkenyl group in which optionally one methylene group is replaced by oxygen; Z.sup.1, Z.sup.2 and Z.sup.3 each independently are a single covalent bond, --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 CH.sub.2 --, --COO-- or --OOC--; n stands for the number 0 or 1; rings A.sup.1 an A.sup.2 each independently are unsubstituted or halogen, cyano and/or methyl-substituted 1,4-phenylene in which optionally 1 CH group or 2 CH groups is/are replaced by nitrogen; and C* denotes a chiral carbon atom; with the proviso that simultaneously R.sup.

Abstract: The present invention relates to novel 1,2,3,6-tetrahydropyridine derivatives of the general formula (I) ##STR1## wherein R stands for hydrogen or an alkyl group,X stands for an unsubstituted phenyl or benzyl group or for a phenyl or benzyl group substituted with a halogen atom,Y stands for hydrogen or halogen or a trifluoro-methyl groupas well as enantiomers acid addition salts thereof.The invention further extends to pharmaceutical compositions containing said compounds as active ingredient mainly for improving cerebral blood circulation and antihypoxic activity.