Abstract: The invention relates to benzimidazoles of general formula ##STR1## Exemplary compounds are: (a) 4'-[[2-Ethyl-4-methyl-6-[(2-dimethylamino-3,4-dioxo-1-cyclobuten-1-yl)amin o]-1H-benzimidazol-1-yl]-methyl]-2-(1H-tetrazol-5-yl)-biphenyl,(b) 4'-[[2-n-Propyl-4-methyl-6-(2-cyano-3,3-dimethyl-guanidino)-1H-benzimidazo l-1-yl]-methyl]-2-(1H-tetrazol-5-yl)-biphenyl,(c) 4'-[[2-n-Propyl-4-methyl-6-(2,2-dicyano-1-dimethylamino-etheneamino)-1H-be nzimidazol -1-yl]-methyl]-2-(1H-tetrazol-5-yl)-biphenyl,(d) 4'-[[2-n-Propyl-4-methyl-6-(1-morpholino-2-nitro-etheneamino)-1H-benzimida zol -1 -yl]-methyl]-2-(1H-tetrazol-5-yl)-biphenyl, and(e) 4'-[[2-n-Propyl-4-methyl-6-(1,1-dimethylamino-2-nitro-etheneamino)-1H-benz imidazol -1-yl]-methyl]-2-(1H-tetrazol-5-yl)-biphenyl.The new compounds are angiotensin-antagonists.

Abstract: The present invention is new 3-(indol-3-yl)-propenoic acid derivatives and pharmaceutical compositions thereof. These new 3-indolyl-3-yl-prpopenoic acid derivatives are useful as NMDA antagonist.

Abstract: Substituted phenols of the formula I ##STR1## processes for their preparation and compositions containing substituted phenols of the formulae I and II ##STR2## for the treatment of disorders caused by cell proliferation, such as psoriasis, tumor disorders and immunological disorders, are described.

Abstract: Compounds having the structure ##STR1## or a pharmaceutically acceptable salt thereof have activity as inhibitors of cylooxygenase and 5-lipoxygenase, reduce the biosynthesis of leukotrienes B.sub.4, C.sub.4, D.sub.4, and E.sub.4 and cylooxygenase products such as prostaglandins and thromboxane and are useful in the treatment of inflammatory and allergic disease states. The compounds have the structure indicated above wherein A is selected from (a) optinally substituted carbocyclic aryl, (b) optinally substituted furyl, (c) optinally substituted benzo[b]furyl, (d) optinally substituted thienyl, (e) optinally substituted pyridyloxy, (f) optinally substituted pyridylalkyl, (g) optinally substituted benzo[b]thienyl, (h) optinally substituted pyridyl, (i) optinally substituted quinolyl, and (j) optinally substituted indolyl; X is selected from (a) optionally substituted alkyl, (b) optinally substituted alkenyl, and (c) optinally substituted alkynyl; R.sup.1 and R.sup.

Abstract: Disclosed are derivatives of the indolocarbazole alkaloid K-252a of the Formulae I-VI, useful for enhancing neurotrophin-induced activity of neurotrophin responsive cells. A particularly preferred neurotrophin is NT-3, and a particularly preferred neurotrophin responsive cell is one which comprises a trk receptor. The enhanced neurotrophin-induced activity occasioned by the disclosed K-252a derivatives may be determined by the following assays: ChAT activity; DRG neuronal survival; or cell division (mitogenesis).

Abstract: 3,5-Substituted aminobenzoylguanidines, process for their preparation, their use as a medicament or diagnostic and medicament containing themThere are described benzoylguanidines of the formula I ##STR1## where one of the substituents R(1), R(2), R(3) or R(4) is: an amino group ##STR2## where R(5), R(6)=inter alia, H or alkyl, or alternatively R(5) and R(6), together with the nitrogen atom, are a 5-7-membered ring, and the other substituents R(1), R(2), R(3) and R(4) in each case are: H, Hal, CN, CF.sub.3, NO.sub.2, CF.sub.3 --O--, C.sub.m F.sub.2m+1 --CH.sub.2 --O--, R(11)--C.sub.q H.sub.2q --X.sub.p --, X=O or NR(12), R(11)=H, (cyclo)alkyl, phenyl, and where R(1) and R(4) are not simultaneously hydrogen.The compounds I have very good antiarrhythmic and cardio-protective properties, but no undesired salidiuretic properties.

Abstract: A process for preparing dye compositions which comprises hydrolyzing an O-protected 5,6-dihydroxyindole with an alkaline material under anaerobic condition and the products made by such process.

Abstract: Macrocyclic polyetherimide oligomer compositions are prepared by the reaction of an alkali metal salt of a dihydroxyaromatic compound, preferably of bisphenol A, with a substituted bis-phthalimide, typically a chloro-, fluoro- or nitro-substituted o- or m-phenylene bis-phthalimide. The reaction takes place in a substantially non-polar solvent such as o-dichlorobenzene and at temperatures in the range of about 180.degree.-225.degree. C. in the presence of a phase transfer catalyst which is stable at such temperatures, such as a guanidinium salt. The concentration of phase transfer catalyst is such as to maintain the alkali metal salt at high dilution in the solvent, and the substituted bis-phthalimide is preferably also maintained at high dilution by portionwise addition.

Abstract: A process for preparing, on an industrial scale, 4-halo-5-(hydroxymethyl) imidazole compounds that are useful as intermediates for medicines. A 4-chloro-5-(hydroxymethyl) imidazole compound, a 4-bromo-5-(hydroxymethyl) imidazole compound or a like compound is synthesized by reacting a 4,5-bis(hydroxymethyl) imidazole compound with a halogenating agent such as an N-chlorosuccinimide, an N-bromosuccinimide, a chlorinated isocyanuric acid compound or the like compound.

Abstract: The invention concerns ether derivatives of the formula IQ.sup.1 -X-Ar-Q.sup.2 Iwherein Q.sup.1 is an optionally substituted 9-, 10- or 11-membered bicyclic heterocyclic moiety containing one or two nitrogen heteroatoms and optionally containing a further heteroatom selected from nitrogen, oxygen and sulphur; X is oxy, thio, sulphinyl or sulphonyl; Ar is optionally substituted phenylene, pyridinediyl, pyrimidinediyl, thiophenediyl, furandiyl, thiazolediyl, oxazolediyl, thiadiazolediyl or oxadiazolediyl; and Q.sup.2 is selected from the groups of the formulae II and III: ##STR1## wherein R.sup.1 is hydrogen, (2-5C)alkanoyl or optionally substituted benzoyl; R.sup.2 is (1-4C)alkyl; and R.sup.3 is hydrogen or (1-4C)alkyl; or R.sup.2 and R.sup.3 are linked to form a methylene, vinylene, ethylene or trimethylene group; or a pharmaceutically-acceptable salt thereof; processes for their preparation; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.

Abstract: An indole derivative represented by formula (1), ##STR1## wherein A is a group ##STR2## wherein R.sup.10 is hydrogen or lower alkyl, dotted lines may optionally be present, and R.sup.1 -R.sup.9 represents various substitutional groups. The compound (1) exhibits a positive inotropic action on cardiac muscle, an anti-arrhythmic action, and a vasodilation action without increasing the heart rate. A heart affection therapeutic agent comprising this compound as an effective component is extremely effective for treating heart failures and arrhythmia.

Abstract: This invention relates to compounds of the formula: ##STR1## wherein R is an electron withdrawing group; R.sub.1 is H or COZ;X.sub.1 and X.sub.2 are independently H, lower alkyl,aryl, aryl lower-alkyl or polystyrene orR and X.sub.1 taken together with the carbon atoms to which they are attached form a ring containing from 4 to 15 ring carbon atoms and may contain up to 2 heteroatoms, wherein the heteroatoms are O, S, or N; andZ is an amino acid residue, a peptide residue or a leaving group. The compounds of the present invention are adaptable as blocking or protecting groups for an amine composition useful in peptide synthesis. The present invention is also directed to a method of protecting an amino group of an organic molecule during a reaction which modifies a portion of the molecule other than the protected amino group.

Abstract: Compounds of formulaA--X--Y--NH--Bwherein A is derived from optionally substituted benzothiophene, indole, 4-aza-and 7-aza-benzothiophene or-indole, A bearing in position 5 hydrogen, halogen, optionally substituted alkyl, hydroxy, nitro, amino, alkylamino, acylamino, alkoxycarbonyl, sulfamoyl, cyano, trimethylsilyl, carboxy, carbamoyl, phosphate, oxycarbamoyl, heterocyclic radical or ether or ester group, X-Y is --CR.sub.8 .dbd.N-- or CH(R.sub.8)--NH-- wherein R.sub.8 is -H or alkyl and attached at position 3 of A, and B is a heterocyclic radical or a residue ##STR1## wherein R.sub.10 is H, optionally substituted alkyl, cycloalkyl, aryl, adamantyl, acyl or carbamoyl and X.sub.2 is alkylthio or NR.sub.3 R.sub.10 wherein R.sub.3 is H or alkyl or R.sub.3 and R.sub.10 together with the nitrogen atom to which they are attached form a heterocyclic radical, in free form or in salt form, have pharmacological activity, e.g. for treating gastrointestinal disorders.

Abstract: A class of substituted imidazole, triazole and tetrazole derivatives of formula (I), wherein the broken circle represents two non-adjacent double bonds in any position in the five-membered ring; two, three or four of V,W,X,Y and Z represent nitrogen and the remainder represent carbon provided that, when two of V,W,X,Y and Z represent nitrogen and the remainder represent carbon, then the said nitrogen atoms are in non-adjacent positions within the five-membered ring; E represents a bond or a straight or branched alkylene chain containing from 1 to 4 carbon atoms; F represents a group of formula (lI); U represents nitrogen or C--R.sup.2 ; B represents oxygen, sulphur or N--R.sup.3 ; are selective agonists of 5--HT.sub.1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated.

Abstract: Process for the preparation of substituted and unsubstituted 2-(cyanomethyl)benzimidazoleA process for the preparation of substituted or unsubstituted 2-(cyanomethyl)benzimidazole, of the formula (I) ##STR1## which comprises reacting an o-phenylenediamine of the formula (II) ##STR2## in which R.sup.1 is C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -alkoxy, preferably methyl or methoxy, and n is an integer from 0 to 2, preferably 0 or 1, in particular 0, with a cyanoacetic ester of the formula (III)NC--CH.sub.2 --COOR.sup.2 (III)in which R.sup.2 is unsubstituted or substituted, linear, branched or cyclic C.sub.2 -C.sub.12 -alkyl and 1 to 3 CH.sub.2 groups of the alkyl radical can in each case be replaced by oxygen, at a temperature of 150.degree.-175.degree. C. in a halogen-free inert solvent whose boiling point is 150.degree. C. or more, or in a mixture of two or more of such solvents, without adding an aromatic sulfonic acid as catalyst.

Abstract: This invention relates to derivatives of perhydroisoindol of formula: ##STR1## in which the radicals R are hydrogen atoms or together form a bond, the symbols R.sub.2 are phenyl radicals which can be substituted by a halogen atom or a methyl radical in position 2 or 3, R.sub.3 is a halogen atom or a hydroxy radical, R.sub.4 is H or halogen if R.sub.3 is halogen, in their isomer forms, or mixture thereof, and possibly also their salts when they exist, and preparation thereof. The derivatives of the invention are particularly interesting as P substance antagonist.

Abstract: A process for the catalytical preparation of condensation products of formaldehyde, in which formaldehyde or a formaldehyde-forming compound is caused to undergo reaction using a catalyst which has been produced, in the presence of an auxiliary base, from a triazolium salt of formula I ##STR1## in which R.sup.1 and R.sup.3 are the same or different and stand for aliphatic groups having from 1 to 30 carbon atoms, optionally substituted aryl groups, optionally substituted aralkyl groups, and/or optionally substituted heteroaryl groups,R.sup.2 represents hydrogen, the hydroxymethylene group --CH.sub.2 OH or the hydroxy-hydroxymethylene-methylidyne group --CH(OH)(CH.sub.2 OH), andR.sup.4 denotes hydrogen, a halogen atom, a nitro or cyano group, an aliphatic group having from 1 to 30 carbon atoms, an optionally substituted aryl group, an optionally substituted aralkyl group, an optionally substituted heteroaryl group, an alkoxy group --OR.sup.5, a thioether group --SR.sup.6, an amino group --NR.sup.7 R.sup.

Abstract: Disclosed is a process for producing an ultra-white N,N'-ethylene-bis(tetrabromophthalimide) product useful as a flame retardant. Also disclosed is a flame retardant composition predominantly comprised of N,N'-ethylene-bis(tetrabromophthalimide) and having unprecedented color and high purity.

Abstract: Unsaturated cyclohexenone oxime ethers I ##STR1## (Q.dbd.H, alkylcarbonyl, benzoyl, alkali metal or alkaline earth metal ion, substituted or unsubstituted ammonium ion, phosphonium ion, sulfonium ion, sulfoxonium ion, an equivalent of a transition metal cation;W=--C.tbd.C-- or --CH.dbd.CH--;R.sup.1 =substituted or unsubstituted cycloalkyl, cycloalkenyl or 6-membered heterocyclic group which has 1-2 oxygen and/or sulfur atoms and can be saturated or partially unsaturated; substituted or unsubstituted 5-membered saturated heterocycle with 1-2 oxygen and/or sulfur atoms; substituted or unsubstituted 5-membered heteroaromatic group with 1-2 nitrogen atoms and/or 1 oxygen or sulfur atom; substituted or unsubstituted phenyl, pyridyl or R.sup.9 -X-substituted alkyl with X=O, S, --SO--, --SO.sub.2 -- and R.sup.9 =alkyl, phenyl, 5/6-membered hetaryl with 1-3 hetero atoms;R.sup.2 =alkyl;R.sup.3 =H, alkyl;R.sup.4 =H, halogen, alkyl;R.sup.5 =H, alkyl;or R.sup.3 +R.sup.4, R.sup.3 +R.sup.5 or R.sup.4 +R.sup.

Abstract: The invention provides a pharmaceutical composition comprising a particular physical form of N- 4- 5-(cyclopentyloxy-carbonyl)amino-1-methylindol-3-yl-methyl!-3-methox ybenzoyl!-2-methylbenzenesulphonamide and polyvinylpyrrolidone. It also provides methods for preparing this physical form, and another physical form of N- 4- 5-(cyclopentyloxycarbonyl)amino-1-methylindol-3-yl-methyl!-3-methoxy benzoyl!-2-methylbenzenesulphonamide useful in the preparation of the first mentioned physical form. The compositions are useful in the treatment of diseases in which leukotrienes are implicated, for example asthma.