Abstract: A method of treating neurotoxic injury, where the injury is the result of the release of oxygen-derived free radicals, is disclosed. The method utilizes carboxyfullerenes as free radicals scavengers to reduce the damage caused by the free radicals.

Abstract: The invention relates to compounds of the general formula ##STR1## wherein R.sup.1 is C.sub.6-12 -cycloalkyl, optionally substituted by lower alkyl or C(O)O lower alkyl, indan-1-yl or indan-2-yl, optionally substituted by lower alkyl; acenaphthen-1-yl; bicyclo[3.3.1]non-9-yl, octahydro-inden-2-yl; 2,3-dihydro-1H-phenalen-1-yl; 2,3,3a,4,5,6-hexahydro-1H-phenalen-1-yl, decahydro-azulen-2-yl; bicyclo[6.2.0]dec-9-yl; decahydro-naphthalen-1-yl, decahydro-naphthalen-2-yl; tetrahydro-naphthalen-1-yl, tetrahydro-naphthalen-2-yl or 2-oxo-1,2-diphenyl-ethyl;R.sup.2 is .dbd.O or hydrogen,R.sup.3 is hydrogen, isoindolyl-1,3-dione, lower alkoxy, lower alkyl, amino, benzyloxy, --CH.sub.2 OR.sup.5 or --CH.sub.2 N(R.sup.5).sub.2 ;R.sup.4 is hydrogen or --CH.sub.2 OR.sup.5 ;R.sup.5 is hydrogen or lower alkyl; ##STR2## is cyclohexyl or phenyl, optionally substituted by lower alkyl, halogen or alkoxy; to racemic mixtures and their corresponding enantiomers and or pharmaceutically acceptable acid addition salts thereof.

Abstract: The present invention concerns a process for the preparation of a 2,5 disubstituted pyridine of the formula (I) ##STR1## which comprises the steps of a) reacting a compound of the formula (II)R.sup.1 --CH.dbd.CH--R.sup.2 (II)with an acrylic compound of the formula (III) ##STR2## to form a compound of the formula (IV) ##STR3## and b) reacting the compound of formula (IV) under water free conditions with a hydrogen halide in which formula R.sup.1 signifies lower alkyl, R.sup.2 signifies di-(lower alkyl)amino or a 5- or 6-membered --N-heterocyclyl group having the free valence bond at the nitrogen atom, and X signifies halogen.

Abstract: The present invention relates to compounds of the general formula whereinR.sup.1 is C.sub.5-12 -cycloalkyl, optionally substituted by lower alkyl; decahydro-naphthalen-1-yl; decahydro-naphthalen-2-yl; indan-1-yl or indan-2-yl, optionally substituted by lower alkyl; decahydro-azulen-2-yl; bicyclo[6.2.0]dec-9-yl; acenaphthen-1-yl; bicyclo[3.3.1]non-9-yl; 2,3-dihydro-1H-phenalen-1-yl; 2,3,3a,4,5,6-hexahydro-1H-phenalen-1-yl; octahydro-inden-2-yl; 1,2,3,4-tetrahydro-naphthalen-1-yl; 1,2,3,4-tetrahydro-naphthalen-2-yl; naphthalen-lower alkyl-1-yl; naphthalen-lower alkyl-2-yl; acenaphthen-1-yl; and 5-isopropyl-2-methyl-bicyclo[3.1.0]hex-3-yl;R.sup.2, R.sup.3 are hydrogen; hydroxy; lower alkyl; .dbd.O; or phenyl, optionally substituted by lower allyl, halogen or alkoxy;R.sup.4 is hydrogen; lower alkyl; --(CH.sub.2).sub.n CH(OH)CF.sub.3 ; --(CH.sub.2).sub.n C.sub.3-6 -cycloalkyl; phenyl; benzyl; tetrahydrofuran-3-yl; --(CH.sub.2).sub.n OCH.sub.2 C.sub.6 H.sub.5 ; --(CH.sub.2).sub.

Abstract: The present invention relates to the use of pyrrolidine and piperidine derivatives of the general formula ##STR1## wherein R.sup.1 and R.sup.2 are, independently from each other, hydrogen, lower alkoxy, hydroxy, halogen, --CONH.sub.2 or --C(O)O-lower alkyl; or taken together are --O--CH.sub.2 O;R.sup.3 and R.sup.4 are, independently from each other, hydrogen, lower alkoxy, benzyloxy, halogen, hydroxy, --CONH.sub.2 or --SCH.sub.3 ; or taken together are --O--CH.sub.2 --O--;Y is --CH(OH)--, --(CH.sub.2).sub.n --, --C(O)-- or --CH(lower alkoxy)--; andm, n and p are 1 or 2;and to their pharmaceutically acceptable addition salts for the treatment of diseases caused by over activation of NMDA receptor subtypes.

Abstract: The invention provides processes for producing Alpha-Interferon (IFN-.alpha.) free from possible mouse and/or virus contamination. The present invention further provides homogeneous IFN-.alpha. free from mouse and/or virus contamination and its use in antitumor and/or antiviral treatment.

Abstract: The present invention relates to novel compounds of the general formula ##STR1## wherein R.sup.1 is hydrogen;R.sup.2 is hydrogen, trifluoromethyl or lower alkyl;R.sup.3 is hydrogen or amino; orR.sup.1 and R.sup.2 or R.sup.3 and R.sup.2 taken together are --CH.dbd.CH--CH.dbd.CH--;Z is pyrimidin-4-yl, pyridin-4-yl, pyridin-2-yl or phenyl;R.sup.4, R.sup.5 are each independently hydrogen, lower alkyl, trifluoromethyl, halogen, lower alkoxy, nitrilo, amino, lower alkyl-amino, di-lower alkyl-amino, piperazinyl, morpholinyl, pyrrolidinyl, vinyl, C.sub.3 -C.sub.6 cycloalkyl, C.sub.3 -C.sub.6 cycloalkenyl, t-buthylethinyl, hydroxyalkylethinyl, phenylethinyl, naphthyl, thiophenyl, or phenyl, which may be substituted by halogen, lower alkoxy, lower alkyl, trifluoromethyl or nitro, or a group --NH(CH.sub.2).sub.n NR.sup.6 R.sup.7, --N(CH.sub.3)(CH.sub.2).sub.n NR.sup.6 R.sup.7, --NH(CH.sub.2).sub.n -morpholin-4-yl or --NH(CH.sub.2).sub.n OH;n is 2-4R.sup.6 and R.sup.

Abstract: The invention is concerned with compounds of the general formula ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, phenyl or benzyl,R.sup.2 is lower alkyl, lower alkoxy, --O(CH.sub.2).sub.n N(R.sup.13)(R.sup.14), --(CH.sub.2).sub.n N(R.sup.13)(R.sup.14) or --N(R.sup.15)(CH.sub.2).sub.n N(R.sup.13)(R.sup.14),R.sup.3 -R.sup.12 are hydrogen, halogen, trifluoromethyl, lower alkyl, cycloalkyl, lower alkoxy, hydroxy, nitro, cyano, --N(R.sup.13).sub.2, phenyl, phenyloxy, benzyl or benzyloxy, orR.sup.6 and R.sup.7 together are a benzene ring,R.sup.13 -R.sup.15 are hydrogen, lower alkyl or cycloalkyl andn is 1-5,as well as their pharmaceutically acceptable salts.

Abstract: A process for the manufacture of an optionally protected 4,8,8-trimethyl-1-oxaspiro?2.5!oct-4-en-6-ol (I) starting from protected 4-hydroxy-2,6,6-trimethyl-2-cyclohexen-1-one (II) comprises reacting the protected compound (II) with dihalomethyllithium and, if desired, cleaving off the protecting group from the thus-obtained protected 4,8,8-trimethyl-1-oxaspiro?2.5!oct-4-en-6-ol. The dihalomethyllithium can be produced in situ by reacting a dihalomethane with a lower alkyllithium in the presence of the compound of formula II. Preferably, protected (S)-4-hydroxy-2,6,6-trimethyl-2-cyclohexen-1-one is converted into protected (3S,6S)-4,8,8-trimethyl-1-oxaspiro?2.5!oct-4-en-6-ol in this manner. Both the starting material (II) and the end product (I) of the process in accordance with the invention are known, valuable intermediates for the manufacture of carotenoids.

Abstract: Hydrogen bis(oxalato)borate of the formula ##STR1## is used as a protonic acid catalyst in condensation reactions, such as Friedel-Crafts condensations, vinyl ether condensations of acetals with vinyl or propenyl ethers and acylations of phenols. The products of such condensations are, for example, dihydro-vitamin K.sub.1 monobenzoate, d,l-.alpha.-tocopherol, various intermediates in the synthesis of carotenoids as well as d,l-.alpha.-tocopherol acetate. As a result of the use in accordance with the invention of hydrogen bis(oxalato)borate various disadvantages associated with the use of other protonic acid catalysts, e.g. problems with corrosion, toxicity and environmental contamination, are avoided. The novel catalyst has advantages with respect to selectivity, yields, amounts required as well as working up after completion of the respective condensation.

Abstract: The invention relates to a compound of the formula ##STR1## wherein R is hydroxy and R.sup.1 is H.sub.2 or .dbd.CH.sub.2 or R is hydrogen or fluoro and R.sup.1 is .dbd.CH.sub.2 and (b) an inert carrier.Compounds of formula I are useful as agents for the treatment of hyperproliferative skin diseases, such as psoriasis, neoplastic diseases, such as leukemia, and sebaceous gland diseases, such as acne and sebhorreic dermatitis.

Abstract: Antisense oligomers of the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.4 are independently hydrogen, lower alkyl or acyl;R.sub.3 is hydrogen or lower alkyl;B is a nucleobase or a protected nucleobase, such that said oligomer has a sequence of bases complementary to a selected RNA;n is 5 to 30;X is NR.sub.3 R.sub.4 ;Y is OR.sub.3, or NHR.sub.3 ;as well as, pharmaceutically acceptable salts thereof.

Abstract: An aldehyde dehydrogenase having the physico-chemical properties: molecular weight: 91,000.+-.5,000; substrate specificity:active on aldehyde compounds; inhibition: by Cu.sup.2+, Zn.sup.2+, Ni.sup.2 + and ethylenediamine tetraacetic acid; optimum pH: 6.0-8.5; optimum temperature: 20.degree.-40.degree. C.; and stimulator: Ca.sup.2+ and pyrroloquinoline quinone, is derived from a microorganism belonging to the genus Gluconobacter. Said aldehyde dehydrogenase can be produced by cultivating a microorganism of the genus Gluconobacter which is capable of producing an aldehyde dehydrogenase having the above properties, in an aqueous nutrient medium under aerobic conditions, disrupting the cells of the microorganism and isolating and purifying the aldehyde dehydrogenase from the cell-free extract of the disrupted cells of the microorganism.

Abstract: A process for the preparation of vitamin K.sub.1 by the oxidation of an alkali metal salt of dihydrovitamin K.sub.1 with hydrogen peroxide in the presence of an iron (III) salt at a pH of 13.7 to 14.3. The dihydrovitamin K.sub.1 alkali metal salt is produced by the saponification of a dihydrovitamin K.sub.1 diester with sodium hydroxide or potassium hydroxide. Conveniently, the oxidation process follows the saponification of dihydrovitamin K.sub.1 without isolation of the product of the saponification reaction.

Abstract: The invention provides hydroxamic acid derivatives of the general formula ##STR1## wherein R.sup.1 represents cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; R.sup.2 represents a saturated 5- to 8-membered monocyclic or bridged N-heterocyclic ring, which N-heterocyclic ring is attached via the N atom and when it is monocyclic, optionally contains NR.sup.4, O, S, SO or SO.sub.2 as a ring member and/or is optionally substituted on one or more C atoms by hydroxy, lower alkyl, lower alkoxy, oxo, ketalized oxo, amino, mono(lower alkyl)amino, di(lower alkyl)amino,carboxy, lower alkoxycarbonyl, hydroxy-methyl, lower alkoxymethyl, carbamoyl, mono(lower alkyl)-carbamoyl, di(lower alkyl)carbamoyl or hydroxyimino; R.sup.3 represents a 5- or 6-membered N-heterocyclic ring which (a) is attached via the N atom, (b) optionally contains N, O and/or S, SO or SO.sub.