Abstract: The present invention relates to a process for the production of N-substituted acrylic acid amides by conversion of 2-carboalkoxy-t-oxabicyclo(2,2,1)hept-5-enes with primary or secondary amines to 2-carboxamide-7-oxabicyclo(2,2,1)hept-5-enes and the thermal decomposition of the latter, preferably in the presence of Lewis acids and in a vacuum, to furane and N-substituted acrylic acid amides. The process according to the invention results in high purity N-substituted acrylic acid amides that are, in the main, free of bifunctional monomers which would disrupt the subsequent polymerization of the N-substituted acrylic acid amides by undesired cross-linking.

Abstract: There are disclosed compounds of the formula ##STR1## wherein X is ##STR2## W is ##STR3## Y is ##STR4## n is 0-8; R.sup.1 is hydrogen, loweralkyl, loweralkoxy, lower alkanoyl, halo, trifluoromethyl, cyano or nitro;R.sup.2 is hydrogen or loweralkyl;and the pharmaceutically acceptable salts thereof, and their use in the treatment of leukotriene-mediated naso-bronchial obstructive airpassageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like, and in antithrombotic therapy.

Abstract: 5-(4-Chloro-3-sulfamoylbenzoyl)-2,3-dihydro-2-benzofurancarboxylic acids of the formula I ##STR1## in which R.sup.1 and R.sup.2 are identical or different and represent hydrogen, halogen or methyl, both as racemic mixtures and in the form of their optical isomers, and their physiologically tolerated salts are described, as is their preparation. They are outstanding diuretics and saluretics with an additional uricosuric component.

Abstract: Benzofuran derivatives represented by the general formula: ##STR1## in which: R represents an ethyl, n-propyl, isopropyl or n-butyl radical;R.sub.1 represents a branched-chain alkyl radical having from 4 to 7 carbon atoms of which at least one does not bear a hydrogen atom;R.sub.2 represents hydrogen, chlorine or bromine;n is 1 or 2and pharmaceutically acceptable acid addition salts thereof.These derivatives have been found to possess calcium translocation inhibiting properties and antiadrenergic properties and can thus be used in the treatment of certain pathological syndromes of the cardiovascular system.

Abstract: Amidine compounds of the formula ##STR1## and pharmaceutically acceptable acid addition salts thereof are novel compounds and are useful as powerful anti-trypsin, anti-plasmin, anti-kallikrein and anti-thrombin agents. They are also useful as a powerful anti-complement agent.

Abstract: 1,2-Benzoxathiine derivatives of the formula I ##STR1## wherein Hal is chlorine, bromine or iodine,R is hydrogen, halogen, nitro, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, cyano or a --X--R.sup.1, --CO--X--R.sup.2, --CO--NR.sup.3 R.sup.4, --SO--R.sup.5 or --SO.sub.2 --R.sup.6 group, whereR.sup.1 is C.sub.3 -C.sub.5 alkynyl, or is C.sub.1 -C.sub.4 alkyl, unsubstituted or substituted by halogen or C.sub.1 -C.sub.4 alkoxy, or is C.sub.3 -C.sub.5 alkenyl, unsubstituted or substituted by halogen or C.sub.1 -C.sub.4 alkoxy,R.sup.2 and R.sup.5 are each independently of the other C.sub.1 -C.sub.4 alkyl,-C.sub.1 -C.sub.4 haloalkyl, C.sub.2 -C.sub.4 alkoxyalkyl, C.sub.3 -C.sub.5 alkenyl, C.sub.3 -C.sub.5 alkynyl, phenyl or benzyl,R.sup.3 and R.sup.4 are each independently of the other hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.2 -C.sub.4 alkoxyalkyl, C.sub.3 -C.sub.5 alkenyl, C.sub.3 -C.sub.5 alkynyl, phenyl or benzyl, R.sup.6 is C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.

Abstract: Naphthenic and heterocyclic retinoic acid analogues such as (E)-6-[2-(2,6,6-trimethyl-1-cyclohexen-1-yl)ethenyl]-2-naphthaldehyde, methyl 6-[2-(2,6,6-trimethyl-1-cyclohexen-1-yl)ethenyl]-2-naphthoate, 6-[2-(2,6,6-trimethyl-1-cyclohexen-1-yl)ethenyl]-2-naphthoic acid, (E)-1-(5-carbethoxy-2-furanyl)-2-methyl-4-(2,6,6-trimethyl-1-cyclohexen-1- yl)-1,3-butadiene, (E)-1-(5-carboxy-2-furanyl)-2-methyl-4-(2,6,6-trimethyl-1-cyclohexen-1-yl) -1,3-butadiene, (E)-1-(5-carbethoxythien-2-yl)-2-methyl-4-(2,6,6-trimethyl-1-cyclohexen-1- yl)-1,3-butadiene, and (E)-1-(5-carboxythien-2-yl)-2-methyl-4-(2,6,6-trimethyl-1-cyclohexen-1-yl) -1,3-butadiene. These retinoids are useful as chemopreventive agents for inhibiting tumor promotion in epithelial cells and for treating nonmalignant skin disorders.

Abstract: [S]-(+)-2-acetyl-7-(2,3-epoxypropoxy)benzofuran (SEBF) is prepared by subjecting 2-acetyl-7-hydroxybenzofuran and [R]-glycidol to dehydration condensation in an inert organic solvent in the presence of triphenylphosphine and a dialkyl azodicarboxylate. The [S]-(+)-2-acetyl-7-(2,3-epoxypropoxy)benzofuran can be easily converted into [S]-2-acetyl-7-(2-hydroxy-3-isopropylaminopropoxy)benzofuran ([S]-befunolol) or salts thereof which are useful as a .beta.-adrenergic blocking agent, by reacting it with isopropylamine.

Abstract: The present invention relates, as new industrial products, to (.+-.)-, (+)- and (-)-2,4-diacetyl-5-(3-alkyl-amino-2-hydroxy-propyloxy)-benzofurans of general formula: ##STR1## where R is CH(CH.sub.3).sub.2 or C(CH.sub.3).sub.3, and to their acid addition salts. These products are useful in therapeutics, particularly as cardioselective beta-blocking agents.

Abstract: Naphthenic and heterocyclic retinoic acid analogues such as (E)-6-[2-(2,6,6-trimethyl-1-cyclohexen-1-yl)ethenyl]-2-naphthaldehyde, methyl 6-[2-(2,6,6-trimethyl-1-cyclohexen-1-yl)ethenyl]-2-naphthoate, 6-[2-(2,6,6-trimethyl-1-cyclohexen-1-yl)ethenyl]-2-naphthoic acid, (E)-1-(5-carbethoxy-2-furanyl)-2-methyl-4-(2,6,6-trimethyl-1-cyclohexen-1- yl)-1,3-butadiene, (E)-1-(5-carboxy-2-furanyl)-2-methyl-4-(2,6,6-trimethyl-1-cyclohexen-1-yl) -1,3-butadiene, (E)-1-(5-carbethoxythien-2-yl)-2-methyl-4-(2,6,6-trimethyl-1-cyclohexen-1- yl)-1,3-butadiene, and (E)-1-(5-carboxythien-2-yl)-2-methyl-4-(2,6,6-trimethyl-1-cyclohexen-1-yl) -1,3-butadiene. These retinoids are useful as chemopreventive agents for inhibiting tumor promotion in epithelial cells and for treating nonmalignant skin disorders.

Abstract: Described are compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 independently of one another denote hydrogen or loweralkyl; A is CO, CH.sub.2, O, S, SO or CHOH; X is hydrogen, halo, loweralkyl, or --CH.sub.2 NR.sub.1 R.sub.2 wherein R.sub.1 and R.sub.2 are as defined above; W is COOR wherein R is hydrogen or alkyl of 1-10 carbon atoms, CH.sub.2 OH, CONR.sub.1 R.sub.2 or CH.sub.2 NR.sub.1 R.sub.2 wherein R.sub.1 and R.sub.2 are as defined above; Z.sub.1 and Z.sub.2 independently of one another denote hydrogen, halo or loweralkyl; and pharmaceutically acceptable salts thereof.The compounds are effective as diuretic agents.

Abstract: There are described compounds of formula I, ##STR1## in which Ra, Rb, Rc, Rd, Re, Rf and Rg, which may be the same or different, each represent hydrogen, amino, hydroxy, alkoxy, alkenyloxy, halogen, acyl, alkenyl, alkyl, or alkoxy substituted by phenyl,Rh is hydrogen, alkyl or --COOH.X is a hydrocarbon chain containing from 2 to 10 carbon atoms and optionally substituted by a hydroxy group,A has no significance or represents Y, OY, or SY and Y represents a C 1 to 4 hydrocarbon chain which is optionally substituted by alkyl C 1 to 4,E and G, which may be the same or different, each represent --O--, --S-- or --CH.sub.2 --, provided that at least one of E and G is --O-- or --S--,L, together with the carbon atoms to which it is attached, forms a benzene, furan, thiophene, pyrrole, or pyran-2-one ring,and pharmaceutically acceptable derivatives thereof.

Abstract: Imidazoline derivatives of the formula ##STR1## wherein R.sup.1 is hydrogen or alkyl C.sub.1-6 ;R.sup.2 is hydrogen, methyl, chloro, bromo or fluoro;R.sup.3 is hydrogen, methyl, hydroxy, methoxy, fluoro, chloro or bromo; and their non-toxic salts.Processes for their preparation and pharmaceutical compositions thereof. The compounds exhibit presynaptic .alpha..sub.2 -adrenoreceptor antagonist activity.

Abstract: 2,3-Dihydro-substituted-5-(acyl)benzofuran-2-carboxylic acids, the pharmaceutically acceptable salt, ester and amide derivatives thereof and combinations of these compounds with antikaluretic agents are disclosed having diuretic-saluretic, uricosuric and antihypertensive activity.