Abstract: Derivatives of 5,5-disubstituted pyrimidine-2,4,6-trianones are disclosed. These compounds have antitumor and antimetastatic activity.

Abstract: Compounds of formula I, useful as matrix metalloprotease inhibitors, wherein X, Y and Z are each oxygen; R1 is selected from the group consisting of (a) n-octyl, (b) n-decyl, (c) biphenyl and (d) (4-phenoxy)phenyl, wherein the terminal monocycle for moieties (c)-(d) is unsubstituted or substituted by a substituent selected from the group consisting of —NH2, —NO2, —SO2NH2, —SO2CH3, acetyl, hydroxy, methoxy, ethoxy, cyano and halogen; R2 and R3 are each hydrogen; and R4 and R5, together with the nitrogen atom to which they are bound, form a piperazinyl or piperidyl ring, wherein the piperazinyl ring is substituted in the 4-position with a substituent selected from the group consisting of (a) a 6-membered aromatic monocycle having 0, 1 or 2 nitrogen atoms and the remainder of the atoms in the monocycle being carbon and (b) hydroxy-C1-C6 alkyl, wherein the monocycle is unsubstituted or substituted by a substituent selected from the group consisting of halogen, —

Abstract: 5-Arylidene-4-oxo-2-thioxo-3-thiazolidinecarboxylic acids of formula I 1

Abstract: 1 The present invention ocncerns new amidinopyrroline derivatives of formula (I) with the meanings of the symbols as given in the description as well as a process for their production and their use in pharmaceutical preparations.

Abstract: The invention is directed to barbituric acid derivatives having inhibitory activity for matrix maetalloproteases comprised of formula (I): pharmaceutical compositions thereof, processes for preparing the derivatives, and methods for treating diseases associated with elevated or uncontrolled levels of matrix metalloprotease activity, e.g., cancer, specifically tumor progression and tumor metastasis, inflammation, or as a method of contraception.

Abstract: New compounds of formula I wherein: R and R1 are independently selected from hydrogen, (C1-C6)alkyl, styryl and (C3-C6)cycloalkyl or, taken together with the carbon to which they are linked, form a (C3-C6)cycloalkyl group; A is selected from the following groups: —CH2C≡CCH2—, or —(CH2)q—NH—(CH2)q—, wherein q is an integer from 2 to 3 B is selected from T is selected from —CH2—C≡CH, —C≡CH, —(CH2)p—R3, —CH═CH—R3, —CH2—NHCO—R3, —(CH2)p—O—R3, —CH(NH2)—CH2R3, in which p is 0 or an integer from 1 to 4, R3 is a carbocyclic or heterocyclic ring as medicaments having antitumor and/or antimetastatic activities.

Abstract: Compounds of formula I, useful as matrix metalloprotease inhibitors, ##STR1## wherein X, Y and Z are each oxygen;R.sub.1 is selected from the group consisting of (a) n-octyl, (b) n-decyl, (c) biphenyl and (d) (4-phenoxy)phenyl, wherein the terminal monocycle for moieties (c)-(d) is unsubstituted or substituted by a substituent selected from the group consisting of --NH.sub.2, --NO.sub.2, --SO.sub.2 NH.sub.2, --SO.sub.2 CH.sub.3, acetyl, hydroxy, methoxy, ethoxy, cyano and halogen;R.sub.2 and R.sub.3 are each hydrogen; andR.sub.4 and R.sub.5, together with the nitrogen atom to which they are bound, form a piperazinyl or piperidyl ring, wherein the piperazinyl ring is substituted in the 4-position with a substituent selected from the group consisting of (a) a 6-membered aromatic monocycle having 0, 1 or 2 nitrogen atoms and the remainder of the atoms in the monocycle being carbon and (b) hydroxy-C.sub.1 -C.sub.

Abstract: The present invention concerns the use of beta-carboline derivatives of formula I bearing at least a free or esterified carboxylic group on the piperidine ring, for the preparation of pharmaceutical compositions having antimetastatic properties.

Abstract: Compound of formula (I) are disclosed ##STR1## as well as optically active isomers or pharmacologically acceptable salts thereof. The compounds are useful active ingredients in pharmaceutical compositions, and methods of treating osteoporosis, inflammation or diseases which are due to thromboembolic events. Compounds of formula (II) are also disclosed ##STR2## which are useful as starting compounds for preparing compounds of formula (I).

Abstract: The invention concerns a microbial esterase which enantioselectively cleaves (S)-1-phenylethyl acetate and is obtainable from Arthrobacter spec. (DSM 7034), Pseudomonas fluorescens (DSM 7033) or Bacillus subtilis (DSM 7035) as well as a process for enantioselectively cleaving a 1-arylalkyl ester of a carboxylic acid and a process for the production of an enantiomerically-pure 1-arylalkanol using this esterase.

Abstract: Enzyme specific for bilirubin which has a phenol oxidase activity of less than 0.5% and an activity for biliverdin of less than 10%, a broad pH optimum as well as a good thermostability. The enzyme is obtainable from plants such as alfalfa and is suitable for the determination as well as for the degradation of bilirubin in particular in biological liquids.

Abstract: The invention concerns a microbial esterase which enantioselectively cleaves (S)-1-phenylethyl acetate and is obtainable from Arthrobacter spec. (DSM 7034), Pseudomonas fluorescens (DSM 7033) or Bacillus subtilis (DSM 7035) as well as a process for enantioselectively cleaving a 1-arylalkyl ester of a carboxylic acid and a process for the production of an enantiomerically-pure 1-arylalkanol using this esterase.