Abstract: Novel chiral phosphorus compounds of the general formula ##STR1## wherein R signifies substituted or unsubstituted phenyl, R.sup.1 and R.sup.2, which can be the same or different, signify hydrogen, lower alkyl, lower alkoxy, di-lower alkylamino or protected hydroxymethyl or R.sup.1 and R.sup.2 together signify the group ##STR2## in which m represents a number 3 to 5, R.sup.4 represents lower alkyl, substituted or unsubstituted phenyl or benzyl and R.sup.5 represents lower alkyl or both R.sup.5 's together represent lower alkylene, R.sup.3 signifies methyl, lower alkoxy, di-lower alkylamino or fluorine and n signifies the number 0, 1, 2 or 3, are described.The compounds of formula I are useful in the form of complexes with a metal of Group VIII as catalysts for asymmetric hydrogenations and enantioselective hydrogen displacements in prochiral allylic systems.

Abstract: Tricyclic imidazole derivatives of the formula ##STR1## wherein R.sup.1 is 2-pyridyl optionally substituted by lower alkyl or lower alkoxy, n is the integer 0 or 1, R.sup.2 is hydrogen or lower alkyl, R.sup.3 and R.sup.4, independently, are hydrogen or lower alkyl, A is a group of the formula ##STR2## m is the integer 2 or 3, R.sup.5, R.sup.6, R.sup.7 and R.sup.8, independently, are hydrogen or lower alkyl, and R.sup.9 is hydrogen and R.sup.10 is hydrogen or lower alkyl or R.sup.9 and R.sup.10 taken together are oxo, provided that at least one of R.sup.3 and R.sup.4 is lower alkyl when A is a group of the formula--CH.dbd.CH--CH.dbd.CH-- or --(CH.sub.2).sub.4 --,and their pharmaceutically acceptable acid addition salts. The compounds of formula I inhibit gastric acid secretion and prevent the formation of gastric ulcers.

Abstract: The invention relates to a new series of penicillin esters and salts thereof, to methods of their preparation and to intermediates in the production of the esters of the general formula ##STR1## in which R.sub.1 and R.sub.2 represent an alkyl radical having from 1 to 6 carbon atoms, a cycloalkyl or cycloalkylalkyl radical the cycloalkyl part having from 3 to 10 carbon atoms, or R.sub.1 and R.sub.2 together with the nitrogen atom represent a heterocyclic ring with from 4 to 8 carbon atoms; R.sub.3 represents radicals known from natural, biosynthetic, and semisynthetic penicillins; and pharmaceutically acceptable salts thereof.The new compounds are efficiently absorbed from the gastrointestinal tract and after the absorption they are rapidly transformed into the corresponding free penicillins and amidinopenicillanic acids, whereby a broad-spectrum infection can be combated.

Abstract: Compounds of the formula ##STR1## wherein X.sup.2 is a single covalent bond or --COO--; X.sup.1 is a single covalent bond, --COO--, --CH.sub.2 CH.sub.2 -- or when X.sup.2 is --COO--, X.sup.1 also can be p--C.sub.6 H.sub.4 --, p--C.sub.6 H.sub.4 --CH.sub.2 CH.sub.2 --, --CH.sub.2 CH.sub.2 --p--C.sub.6 H.sub.4, p--C.sub.6 H.sub.4 --COO-- or --COO--p--C.sub.6 H.sub.4 ; ring A is a benzene ring or trans-1,4-cyclohexylene; ring B is a benzene ring or when X.sup.2 is --COO-- and X.sup.1 is a single covalent bond, --COO-- or --CH.sub.2 CH.sub.2 --, ring B also can be trans-1,4-cyclohexylene; Z.sup.1, Z.sup.2 and Z.sup.3 individually are hydrogen or when positioned on a benzene ring which is not linked directly with a further ring via a single covalent bond, Z.sup.1, Z.sup.2 and Z.sup.3 also can be halogen, cyano or methyl; Y.sup.2 is cyano, nitro, 2,2-dicyanovinyl or when Y.sup.1 is hydrogen Y.sup.2 also can be 2,2-dicyano-1-methylvinyl; Y.sup.1 is halogen, cyano, C.sub.1 -C.sub.3 -alkyl or, when X.sup.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 -R.sup.4 is hydrogen or chlorine, R.sup.5 is --COOMe or --SO.sub.3 Me, Me is an alkali metal cation and X is oxygen, sulfur or selenium, photosensitizers for the conversion of tachysterol into previtamin D are described. The tachysterol content in mixtures of previtamin D and tachysterol can be greatly reduced by visible light irradiation in the presence of such photosensitizers.

Abstract: Pyrido[2,1-b]quinazoline derivatives of the formulas ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are as hereinafter set forth, are described. The compounds of formulas I and II are useful as agents for the treatment of allergic conditions as well as for the treatment of vascular disorders involving thrombosis.

Abstract: The purification of solutions of recombinant interferons is achieved by chromatography on metal chelate resins of the formula ##STR1## in which Me represents copper or nickel.

Abstract: Naphthalenyloxy carboxylic acids of the formula ##STR1## wherein X, R, m and n are as hereinafter set forth, are described. The compounds of formula I are antagonists of slow reacting substance of anaphylaxis (SRS-A), which renders them useful as agents for the treatment of allergic conditions.

Abstract: There is presented 3H-2-benzazepines and 4,5-dihydro-3H-2-benzazepines of the formula ##STR1## wherein X is hydrogen, chloro or bromo, Y is hydrogen, fluoro or chloro with the proviso that X and Y cannot both be hydrogen and R.sub.1 is selected from the group consisting of hydrogen, bromo, chloro, iodo, a radical of the formula ##STR2## and a radical of the formula ##STR3## wherein R.sub.2 is hydrogen, phthalimido, lower alkyl, hydroxy, amino, monoalkylamino and dialkylamino and R.sub.3 is hydroxy, phthalimido or amino with the proviso that where R.sub.1 is other than hydrogen then the bonding at the 4,5-position is unsaturated,and the pharmaceutically acceptable salts thereof.

Abstract: The invention relates to 4-pyridone-3-carboxylic acid derivatives, a process for the preparation thereof and pharmaceutical compositions containing same. The 4-pyridone-3-carboxylic acid derivatives are useful as antibacterial agents and/or as agents having a stimulating activity on the central nervous system.

Abstract: There is presented a compound of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, lower alkyl, chloro, bromo, alkoxy, hydroxy, lower alkyl substituted thio and NR.sub.4 R.sub.5 wherein R.sub.4 and R.sub.5 are hydrogen, lower alkyl and di-substituted lower alkylamino lower alkyl; R.sub.2 is selected from the group consisting of hydrogen, lower alkyl and amino; R.sub.3 is selected from the group consisting of hydrogen, acyloxy and hydroxy; X is halogen and Y is hydrogen or halogen and the N-oxides thereof when R.sub.3 is hydrogenand the pharmaceutically acceptable salts thereof.The pyrimido[4,5-d][2]benzazepines are useful as anxiolytic and sedative agents.Also presented are processes and intermediates in the production of the above pyrimido[4,5-d][2]benzazepines.

Abstract: 2,4-Disubstituted 6-[3,6-dihydro-1(2H)-pyridyl]pyrimidine-3-oxides of the formula ##STR1## wherein R.sup.1 is lower alkyl or lower alkoxy-lower alkyl, R.sup.2 is hydrogen or --COOR.sup.3 wherein R.sup.3 is lower alkyl or lower alkoxy-lower alkyl,which are important for the preparation of therapeutically valuable 1,2,5,6-tetrahydropyridyl-substituted 2-oxo-2H-[1,2,4]oxadiazolopyrimidinecarbamates, are described. The foregoing oxides of formula I can be prepared by reacting the corresponding arylsulfonyloxy- or alkylsulfonyl-substituted derivatives with 1,2,5,6-tetrahydropyridine.

Abstract: There is presented compounds of the formula ##STR1## wherein A is selected from the group consisting of ##STR2## R.sub.1 is selected from the group consisting of hydrogen, chlorine, bromine, lower alkyl, the group NR.sub.4 R.sub.5, the group --CH.sub.2 --CO--R.sub.7, the group --NH(CH.sub.2).sub.m NR.sub.8 R.sub.9, hydroxy, lower alkoxy, mercapto and lower alkyl mercapto; R.sub.2 is selected from the group consisting of hydrogen, amino and di-lower alkyl amino; R.sub.3 is selected from the group consisting of hydrogen, lower acyloxy and hydroxy; X is selected from the group consisting of hydrogen, halogen, trifluoromethyl, ethyl, .alpha.-hydroxy ethyl and acetyl; Y is hydrogen or halogen; R.sub.4 and R.sub.5 are hydrogen or lower alkyl or together with their co-bonded nitrogen atom form a five to seven membered heterocyclic group; R.sub.7 is selected from the group consisting of hydroxy lower alkoxy and NR.sub.8 R.sub.9 ; R.sub.8 and R.sub.

Abstract: There is presented compounds of the formula ##STR1## wherein A is selected from the group consisting of ##STR2## R.sub.1 is selected from the group consisting of hydrogen, chlorine, bromine, lower alkyl, the group NR.sub.4 R.sub.5, the group --CH.sub.2 --CO--R.sub.7, the group --NH(CH.sub.2).sub.m NR.sub.8 R.sub.9, hydroxy, lower alkoxy, mercapto and lower alkyl mercapto; R.sub.2 is selected from the group consisting of hydrogen, amino and di-lower alkyl amino; R.sub.3 is selected from the group consisting of hydrogen, lower acyloxy and hydroxy; X is selected from the group consisting of hydrogen, halogen, trifluoromethyl, ethyl, .alpha.-hydroxy ethyl and acetyl; Y is hydrogen or halogen; R.sub.4 and R.sub.5 are hydrogen or lower alkyl or together with their co-bonded nitrogen atom form a five to seven membered heterocyclic group; R.sub.7 is selected from the group consisting of hydroxy lower alkoxy and NR.sub.8 R.sub.9 ; R.sub.8 and R.sub.

Abstract: Oxime ester compounds of the formula ##STR1## wherein A is one of the groups ##STR2## wherein B is --CH.dbd. or nitrogen and R.sub.1 is one of the groups ##STR3## wherein R.sub.2 -R.sub.7, m and n are as hereinafter set forth, processes for their preparation, herbicidal compositions containing these compounds as the active ingredient and methods of use of the herbicidal compositions are disclosed.

Abstract: 4-Hydroxy-2-methyl-3-(2-pyridylcarbamoyl)-6-trifluoromethyl-2H-thieno[2,3-e ]-1,2-thiazine 1,1-dioxide of the formula ##STR1## and its pharmaceutically acceptable salts which possess valuable pharmacodynamic properties are described. More particularly, the compound and its salts display antiinflammatory, analgesic and antirheumatic activities and they are readily accessible by reacting a corresponding alkyl ester with 2-aminopyridine and, if desired, subsequent salt formation.

Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 is a 2,6,6-trimethyl-1-cyclohexen-1-yl or 2,3,6-trimethylphenyl group, either of which may be unsubstituted or substituted by a hydroxy group or a protected hydroxy group, R.sup.2 is aryl, and X.sup.- is an anionare manufactured by hydrogenating a compound of the formula: ##STR2## wherein R.sup.1, R.sup.2 and X.crclbar. are as above, in an organic solvent or aqueous-organic solvent in the presence of a nickel-, palladium-, platinum-, cobalt-, rhodium-, iridium-, or ruthenium-containing catalyst.The process is suitable as an intermediate step in carotenoid and retinoid syntheses.

Abstract: Substituted isoquinolines of the formula ##STR1## wherein R is lower alkoxy, n is the integer zero or 1, and A is ##STR2## wherein R.sub.1 is phenyl, halophenyl, lower-alkylphenyl or lower-alkoxyphenyl, and pharmaceutically acceptable acid addition salts thereof, are described. The compounds of formula I are useful in the treatment of cerebral and cardiac ischemias.

Abstract: Acridanone derivatives of the formula ##STR1## wherein the dotted line is an optional bond, R.sup.1 is hydrogen, halogen or nitro, R.sup.2 is hydrogen or lower alkyl, one of the substituents R.sup.3 and R.sup.4 is hydrogen or lower alkyl and the other together with R is an additional bond and R.sup.5 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl or lower alkyl substituted by halogen or lower alkoxy,and pharmaceutically acceptable acid addition salts thereof, processes for their preparation and pharmaceutical compositions based thereon, are described. The compounds of formula I are useful as schistosomicidal agents.

Abstract: A process for the preparation of mefloquin and its physiologically compatible acid addition salts by reacting 6-phthalimido-1-hexene with a 4-halo-2,8-bis-(trifluoromethyl)-quinoline in the presence of a base, epoxidizing the resulting N-[6-<2,8-bis-(trifluoromethyl)-4-quinolyl>-5-hexenyl]-phthalimide to give N-[4-{3-<2,8-bis-(trifluoromethyl)-4-quinolyl>-2-oxiranyl}-butyl]-phthalim ide, treating the latter with hydrazine hydrate and, where applicable, converting the product into an acid addition salt as well as intermediates obtained in this process.