Abstract: Pharmaceutical compositions for combatting cancer comprising a compound of formula (I) ##STR1## (wherein R.sup.1 represents a hydrogen atom or a C.sub.1-4 alkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkynyl group;R.sup.2 represents a hydrogen atom or a hydroxyl, C.sub.1-4 alkoxy or C.sub.2-4 alkanoyloxy group;R.sup.3 represents a hydrogen atom, or (when R.sup.2 is other than a hydrogen atom) optionally a hydroxyl, C.sub.1-4 alkoxy or C.sub.2-4 alkanoyloxy group, or R.sup.2 and R.sup.3 together represent a methylenedioxy group;R.sup.4 represents a hydrogen or halogen atom or a C.sub.1-3 alkyl group or a phenyl group optionally substituted by a halogen atom or a hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or C.sub.1-4 alkanoyloxy group; and the ring A represents a group of formula ##STR2## where R.sup.5 and R.sup.6 each represent a hydrogen atom or a hydroxyl, C.sub.1-4 alkoxy or C.sub.1-4 alkanoyloxy group,R.sup.7 and R.sup.8 each represents a hydrogen atom or a methyl group, and one of X, X.sup.1, X.sup.2 and X.sup.

Abstract: There are disclosed compounds having the formula ##STR1## wherein n is 1, 2 or 3; X is hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, NHCOR.sub.2 where R.sub.2 is loweralkyl, or NR.sub.3 R.sub.4 where R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl; R is hydrogen or loweralkyl; R.sub.1 is hydrogen, loweralkyl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, furylloweralkyl, thienylloweralkyl, oxygen-bridged arylloweralkyl, oxygen-bridged diarylloweralkyl, oxygen-bridged furylloweralkyl or oxygen-bridged thienylloweralkyl; Y is C.dbd.O or CR.sub.5 OH where R.sub.5 is hydrogen or loweralkyl; Z is CH.sub.2 or C.dbd.CR.sub.6 R.sub.7 where R.sub.6 and R.sub.7 are independently hydrogen or loweralkyl; or Y and Z taken together is CR.sub.5 .dbd.CH where CR.sub.

Abstract: Tertiary hydroxyalkylxanthines having the general formula (I), characterized by the fact that at least one of the residues R.sup.1 and R.sup.3 represents a tertiary hydroxyalkyl group of formula (Ia) in which R.sup.4 represents an alkyl group having up to 3 carbon atoms and n a whole number from 2 to 5; the other residue which may remain R.sup.1 or R.sup.3 is a hydrogen atom or an aliphatic hydrocarbon residue R.sup.5 having up to 6 carbon atoms, in which the carbon chain may be separated by a maximum of two oxygen atoms or be substituted by an oxo group or two hydroxy groups at the most, and R.sup.2 represents an alkyl group with 1 to 4 carbon atoms. Also described is a process for manufacturing these compounds, which are suitable for the manufacture of medicines, in particular for use in the prevention and/or treatment of peripheral and/or cerebral irrigation disorders.

Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is optionally substituted phenyl, pyridyl, thienyl, furyl, pyrrolyl, thiazolyl, or ribofuranosyl; X is oxygen, NR, or sulfur; R is hydrogen, lower alkyl, lower alkenyl, or lower alkynyl; and ring A is (a) an optionally substituted 5-8 membered monocycloalken-1,2-diyl; (b) an optionally substituted carbobicyclic ring of the formula ##STR2## wherein n and m are each independently one or two; or (c) an optionally substituted 5-6 membered heterocycle having one or two heteroatoms, the atoms of which are selected from carbon, oxygen, nitrogen, and sulfur. Also disclosed are tautomers of the above and pharmaceutically acceptable salts; compositions thereof; and methods of using the compounds, tautomer, or salts.

Abstract: The invention relates to vinca (indole-dihydroindole) alkaloid derivatives, in which a fatty chain containing at least 7 aliphatic carbon atoms is present at least at the C.sup.3 /C.sup.4 -position.The derivatives according to the present invention are useful as drugs.

Abstract: Alkaloids present in Catharanthus roseus tissue are selectively concentrated by aqueous extraction of ground tissue followed by extraction with organic solvent e.g. ethyl acetate. The resultant concentrate is rich in catharanthine, vindoline and 3',4'-anhydrovinblastine (AVLB). Yield of AVLB is enhanced by addition to the aqueous extraction medium of acid, salt, or hydrogen peroxide and can be further enhanced through the addition of sodium borohydride.

Abstract: 5,14-Dihydrobenz[5,6]isoindolo[2,1-b]isoquinoline-8,13-dione ##STR1## exhibits anticancer activity. The compound can be prepared by reaction of 2-formyl-3-carboxyl-1,2,3,4-tetrahydroisoquinoline with 1,4-naphthoquinone and is particularly suitably administered parenterally in microcrystalline suspension form.

Abstract: Non-aqueous solutions of 3-isothiazolones are stabilized against chemical decomposition by using organic hydroxylic solvents. These compositions exhibit bactericidal, fungicidal and algaecidal properties.

Abstract: Novel platinum complexes represented by the formula: ##STR1## wherein A is alkylene having carbon atoms of from 1 to 3; R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are the same or different and are hydrogen or alkyl having carbon atoms of from 1 to 4; X and Y are independently a halogen atom, or combined together to form ##STR2## and l, m and n are independently 0 or 1, and a process for preparing the same are disclosed.These platinum complexes have high antitumor activity and low toxicity, and are easily soluble in water. Therefore, they are very useful as an antitumor agent.

Abstract: Delta-opioid receptor antagonists are disclosed of the formula: ##STR1## wherein R.sup.1 is (C.sub.1 -C.sub.5)alkyl, C.sub.3 -C.sub.6 (cycloalkyl)alkyl, C.sub.5 -C.sub.7 (cycloalkenyl)alkyl, aryl, aralkyl, trans-(C.sub.4 -C.sub.5)alkenyl, allyl or furan-2-ylalkyl, R.sup.2 is H, OH or O.sub.2 CR, wherein R is (C.sub.1 -C.sub.5)alkyl; R.sup.3 is H, (C.sub.1 -C.sub.5)alkyl or RCO; X is O, S or NY, wherein Y is H or (C.sub.1 -C.sub.5)alkyl; M is N or CH; and R.sup.4 and R.sup.5 are individually H, F, Cl, Br, NO.sub.2, NH.sub.2, (C.sub.1 -C.sub.5)alkyl or (C.sub.1 -C.sub.5)alkoxy or R.sup.4 and R.sup.5 together are benzo; and the pharmaceutically acceptable salts thereof.

Abstract: Process for the preparation of a 6,13-dihydroquinacridone of the general formula (I) ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 designate hydrogen or substituents customary for quinacridone, characterized in that an optionally substituted dialkyl 2,5-di-(phenylamino)-3,6-dihydroterephthalate is heated to temperatures of 240.degree.-320.degree. C. in an essentially oxygen-free atmosphere in the presence of a dimethyl-diphenyl ether isomer mixture of the formula ##STR2## as the solvent and/or diluent, and a process for the preparation of optionally substituted quinacridone, characterized in that the resulting 6,13-dihydroquinacridone is oxidized in the customary manner.

Abstract: Bicyclic lactams of the general formula I ##STR1## in which R.sup.1 and R.sup.2, which can be identical or different, denote a hydrogen atom or an alkyl group with 1 to 3 carbon atoms, R.sup.3 denotes an unsubstituted phenyl group or a phenyl group which is substituted by a halogen atom, one or two alkoxy groups, a methylenedioxo group or one or several hydroxyl groups, or denotes a pyridyl group, an indolyl group, a 1,2-benzisoxazolyl group which is optionally substituted by a halogen atom or the benzimidazol-2-one or 1,4-benzodioxane radical, R.sup.

Abstract: The invention relates to a new process for preparing novel racemic and optically active 9- or 11-nitroapovincaminic acid derivatives of the general formula (I) ##STR1## wherein R stands for a --CO--X group, wherein X means a halogen atom; orfor a --CO--OR.sup.1 group, wherein R.sup.1 means an optionally mono- or polysubstituted C.sub.1-10 aliphatic group, a C.sub.3-8 alicyclic group or an aromatic C.sub.6-14 hydrocarbyl group; orfor a --CO--NR.sup.2 R.sup.3 group, wherein R.sup.2 and R.sup.3 are the same or different and stand for a hydrogen atom or a C.sub.1-8 alkyl group optionally forming a saturated heterocycle together with the adjacent nitrogen atom and optionally with one or more further nitrogen atoms or other heteroatoms, and R.sup.3 may also represent an amino group when R.sup.2 stands for a hydrogen atom; orfor a cyano group,as well as their salts and pharmaceutical preparations containing these compounds.

Abstract: Indole derivatives characterized by having a 1,3,4,9-tetrahydropyrano[3,4-b]indole-1-acetic acid nucleus bearing a substituent in position 1,5, 6, 7 and 8. The derivatives are useful anti-inflammatory and analgesic agents and methods for their preparation and use are also disclosed.

Abstract: The invention relates to 9-(phosphonylmethoxyalkyl)adenines of the general formula I ##STR1## wherein R.sup.1 is a hydrogen atom, and alkyl group containing one to three carbon atoms, or a hydroxymethyl group, R.sup.2 is a methylene, ethylene, propylene, ethylidene, methoxyethylene, benzyloxyethylene, tetrahydropyran-2-yloxyethylene, (1-ethoxyethoxy)ethylene or 1,2-O-isopropylidene-1,2-dihydroxypropylene group the method of their preparation and utilization.Compounds of the general formula I exhibit biological effects (e.g. antiviral) or can be converted into compounds with such effects.

Abstract: Gut-selective agonist or antagonist opiates of the formula: ##STR1## wherein R is (C.sub.1 -C.sub.5) alkyl, C.sub.3 -C.sub.6 (cycloalkyl)alkyl, aryl, aralkyl or trans-(C.sub.2 -C.sub.5)alkenyl; Z is H or OH, R' is (C.dbd.O)-A(B)(C) wherein A is selected from the group consisting of (C.sub.1 -C.sub.5)alkyl, (C.sub.2 -C.sub.5)alkenyl and (C.sub.2 -C.sub.6)alkoxy (alkyl); B is selected from the group consisting of H, amino and a (C.sub.1 -C.sub.5)alkyl group optionally substituted with CO.sub.2 H, OH or phenyl and C is CO.sub.2 H, SO.sub.3 H, amino or guanidino; and R" is selected from the group consisting of NH-A(B) (C) or is guanidino; and the pharmaceutically-acceptable salts thereof.

Abstract: Novel purine derivatives are described as agents for treating autoimmune diseases as well as a method of manufacture and pharmaceutical compositions as well as novel intermediates in the manufacture thereof.

Abstract: Riboflavin of the formula I ##STR1## is prepared by an improved process by condensing a 4,5-dimethyl-N-(D)-ribityl-2-phenylazoaniline of the formula II ##STR2## where R is H, --CL, --NO.sub.2, --CH.sub.3 or --OCH.sub.3 in the o- or p-position, with barbituric acid of the formula III ##STR3## in the presence of an acid as a condensing agent, by a process in which the acidic condensing agent used is an aliphatic secondary carboxylic acid of the general formula IV ##STR4## where R.sup.1 is methyl or ethyl and R.sup.2 is alkyl of 3 or 4 carbon atoms.

Abstract: The present invention relates to novel, 1-substituted 3-aryl-7-chloro-3,4-dihydro-(2H)-acridone N-oxides, a process for their preparation, pharmaceutical compositions containing these compounds, and their use as chemotherapeutic agents, in particular as antimalarials and coccidiostatics.

Abstract: A 14-hydroxy group is introduced into a morphinan structure by singlet oxygen reaction with a novel dienol ester of an N-substituted-3-O-alkylnormorphinone. The resultant N-substituted-3-O-alkyl-141-hydroxynormorphinone is also a novel compound which may be catalytically hydrogenated to produce a novel N-substituted-3-O-alkylnoroxymorphone. The latter intermediate may be converted to a 3-O-alkylnoroxymorphone by hydrolytic removal of the N-substituent and to noroxymorphone by both hydrolysis and O-dealkylation.The dienol ester intermediate is prepared by N-demethylation of codeine or other 3-O-alkylmorphine by reaction with a cyanogen halide or haloformate ester, followed by oxidation of the resultant N-substituted-3-O-alkylnormorphine to an N-substituted-3-O-alkylnormorphinone and esterification of the latter with an acid anhydride or acid halide.