Abstract: The present invention pertains to derivatives of 5,5-disubstituted pyrimidine-2,4,6,-trianones having the formula: wherein R1, R2, R3, and R4 are described herein. These compounds have antitumor and antimetastatic activity.

Abstract: The invention relates to inhibitors of matrix metalloproteases, more specifically a 3-aryl-succinamido-hydroxamic acid of formula (I) and its salt, ester and derivative thereof, along with methods of producing a compound of formula (I) and pharmaceutical compositions thereof.

Abstract: Compounds of formula I in which R1 represents a substituted or unsubstituted phenoxy, phenylthio, phenylsulfinyl, phenylsulfonyl, phenylamino or phenylmethyl residue, and R2 represents an optionally substituted aryl or heteroaryl residue, with metallo-proteinase inhibitor activity.

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: There is described the use of a compound represented by general formulae (I), (II) or (III), for the inhibition of matrix metalloproteinases (MMP), wherein X1 is oxygen or sulfur, R1 is OH, SH, CH2OH, CH2SH or NHOH, R2 is a residue of 2 to 10 hydrocarbon backbone atoms, which binds to the amino acid 161 of HNC, said residue being saturated or unsaturated, linear or branched, and contains preferably homocyclic or heterocyclic structures, X2 is oxygen or sulfur and binds as hydrogen acceptor on amino acid 160 of HNC, Y is a residue which binds to the S1′ pocket of HNC and consists of at least 4 backbone atoms Z1-Z2-Z3-Z4-R3, and R3 is n-propyl, isopropyl, isobutyl or a residue with at least 4 backbone atoms, which is not larger than a tricyclic ring system. These compounds bind to MMPs in a manner different from the mode of binding of the inhibitors of the state of the art.

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: Compounds of formula I wherein R1, R2, R3 and R4 have the meanings indicated in the specification. The compounds are useful as inhibitors of metalloproteases of the M2, M3 family and the astacin subfamily of M12 and M13.

Abstract: The invention provides novel azulene derivatives of general formula I ##STR1## wherein R.sub.1 to R.sub.6 have the significance given in the description, as well as their tautomers, enantiomers, diastereomers, racemates and physiologically compatible salts or esters and substances which are hydrolyzed or metabolized in vivo to compounds of formula I.The invention is also concerned with a process and intermediates for the manufacture of the above compounds, pharmaceutical compositions which contain such compounds as well as the use of these compounds in the treatment of inflammatory conditions.

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.