Abstract: The present invention relates to pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein X, Y, Ar1, Z, R1, R2 and R3 are as defined in the specification, and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.

Abstract: A process for the preparation of a compound of the formula: wherein the variables are herein below defined.

Abstract: Provided herein are compounds of the formula (I): wherein R1-R8 are as described herein, R4 being aryl or heteroaryl Such compounds are particularly useful in the treatment of a disorder which is created by or is dependent upon decreased availability of serotonin, norepinephrine or dopamine.

Abstract: Processes for the preparation of 1,3-oxathiolane nucleosides are provided that include efficient methods for the preparation of the 1,3-oxathiolane ring and subsequent condensation of the 1,3-oxathiolane with a pyrimidine or purine base. Using the processes described herein, the compounds can be provided as isolated enantiomers.

Abstract: The present invention provides compounds of formula I, which are effective in absorbing ultraviolet radiation and can be used as sunscreen agents: wherein R1 and R2 are each independently C2-C18 alkyl, C5-C7 cycloalkyl, or C2-C18 alkyl in which at least one methylene group is replaced by oxygen; R3 is hydrogen, C1-C18 alkyl, C2-C18 alkyl in which at least one methylene group is replaced by oxygen, C1-C18 alkyl carbonyl, C3-C18 alkenyl, C3-C18 alkynyl, or a group YS; R4 is hydrogen, C1-C8 alkyl or a group OR3; Y is a linker group; and S is a silane-, an oligosiloxane- or a polysiloxane-moiety.

Abstract: There is disclosed a process for producing a 2-substituted thiopyrimidine-4-carboxylate represented by the formula (3): wherein R2 represents a substituted or unsubstituted hydrocarbon group and R3 represents a hydrocarbon group, which comprises reacting-an &agr;-keto ester compound represented by the formula (1): R1OCH═CHCOCO2R2  (1) wherein R1 represents a substituted or unsubstituted hydrocarbon group, and R has the same meaning as defined above, with an isothiourea compound represented by the formula (2): wherein R3 has the same meaning as defined above.

Abstract: A process for isolating one or more enantiomer components from a mixture of enantiomers through co-crystallization is disclosed.

Abstract: A process for preparing triazolopyrimidine derivatives of the formula (I): wherein R1 represents a hydrogen or an alkyl radical of one to ten carbon atoms, or a cycloalkyl radical of three to six carbon atoms, or an alkenyl radical of up to four carbon atoms; R2 represents a hydrogen, a halogen atom, a hydroxyalkyl or alkyl radical of one to ten carbon atoms; R3 represents a hydrogen, a hydroxyalkyl or alkyl radical of one to four carbon atoms; by rapidly preparing diamino-1,2,4-triazole which is reacted with an aldehyde to form an imide which is reacted with an &agr;,&bgr;-unsaturated acid derivative, the reaction product of which is hydrolyzed in the presence of an acid to produce the triazolopyrimidine derivatives of formula (I). The compounds of the formula (I) are capable of preventing bronchospasm.

Abstract: A compound selected from those of formula (I): wherein: R1 and R2, which may be identical or different, represent a group of formula U-V wherein U represents single bond, or alkylene which is optionally substituted and/or unsaturated, and V is as defined in the description, G represents oxygen, or NR3 wherein R3 is as defined in the description, X represents hydrogen, hydroxy, alkoxy, mercapto or alkylthio, Y represents hydrogen, or X+Y represents carbonyl, X1 represents hydrogen, hydroxy, alkoxy, mercapto or alkylthio, Y1 represents hydrogen, or X1+Y1 represents carbonyl, R4, R5, and R6 are as defined in the description, its isomers, and pharmaceutically-acceptable acid or base addition salts thereof, and medicinal products containing the same are useful in the treatment of cancer.

Abstract: This invention relates to a process for the preparation of a stabilized aqueous alkali metal-2-hydroxy-4,6-dichloro-s-triazine (AHDT) solution, which entails starting at 5 to 40° C. with a solution containing either the corresponding alkali hydrogencarbonate, acetone, or a mixture thereof, and then, while cooling, adding cyanuric chloride and an alkali lye simultaneously in such a manner that the reaction temperature does not exceed 25° C. and the pH does not drop below 5.5, and during a subsequent stirring time of 2 to 30 hours adding either a very small quantity of alkali lauryl sulfate if the original starting solution contained hydrogencarbonate, or adding alkali hydrogencarbonate if exclusively acetone was used in the first reaction step, and then finally adding an alkali borate and/or a dialkali hydrogenphosphate and/or potassium hexacyanoferrate (II) as buffer. The pH, which should be ≧7.0 during the entire process, may, if necessary, be adjusted with an acid to a value between 8.0 and 9.5.

Abstract: This invention provides compounds of Formula (I): wherein R1 and R2 may be single substituents or fused to form spirocyclic or hetero-spirocyclic rings; R3 is H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, substituted C1 to C6 alkenyl, alkynyl, or substituted alkynyl, CORC; RC is H, C1 to C3 alkyl, substituted C1 to C3 alkyl, aryl, substituted aryl, C1 to C3 alkoxy, substituted C1 to C3 alkoxy, C1 to C3 aminoalkyl, or substituted C1 to C3 aminoalkyl; R4 is H, halogen, CN, NO2, C1 to C6 alkyl, substituted C1 to C6 alkyl, alkynyl, or substituted alkynyl, C1 to C6 alkoxy, substituted C1 to C6 alkoxy, amino, C1 to C6 aminoalkyl, or substituted C1 to C6 aminoalkyl; and R5 is selected from a trisubstituted benzene ring of a five or six membered ring with 1, 2, or 3 heteroatoms from the group including O, S, SO, SO2 or NR6 and containing one or two independent substituents from the group including H, halogen, CN, NO2, amino, and C1 to C3 alky, C1 to C3 alkoxy, C1 to C3 a

Abstract: The present invention relates to a process for preparing 4-chloro-6-hydroxypyrimidine from 4-chloro-6-methoxypyrimidine.

Abstract: The invention relates to novel substituted phenyluracils of the general formula (I) in which A represents alkanediyl or alkenediyl, each of which has 2 to 5 carbon atoms and each of which is optionally substituted by cyano, halogen or by in each case optionally halogen- or C1-C4-alkoxy-substituted C1-C4-alkyl, C1-C4-alk-oxy-carbonyl or C2-C4-alkenyl or interrupted by O (oxygen), or represents cyclohexane-1,2-diyl or 1,2-phenylene, Q1 represents O (oxygen) or S (sulphur), Q2 represents O (oxygen) or S (sulphur), R1 represents hydrogen, amino or optionally cyano-, halogen- or C1-C4-alkoxy-substituted alkyl having 1 to 4 carbon atoms, R2 represents optionally halogen-substituted alkyl having 1 to 4 carbon atoms, R3 represents hydrogen, halogen or optionally halogen-substituted alkyl having 1 to 4 carbon atoms, R4 represents hydrogen, cyano, carbamoyl, thiocarbamoyl or halogen, R5 represents cyano, carbamoyl, thiocarbamoyl or in each case optionally halogen-substituted alkyl or alkoxy ha

Abstract: wherein R is alkyl, alkenyl, or alkynyl; R1 and R2 are each independently hydrogen alkyl, or aryl; and Ar is phenyl, indanyl, benzhydryl, or phenyl, substituted with one or more groups selected from the group consisting of halogen, alkyl, perfluoroalkyl, lower alkoxy, perfluoroalkylalkoxy, dialkylamino, and aroyloxy.

Abstract: Pyrimidones of formula (I) are inhibitors of the enzyme LpPLA2 and thereof use in treating inter alia atherosclerosis, in which: R1 is COOH or a salt thereof, COOR10, CONR11R12, CN or CH2OH; R2 is a mono- or bicyclic aromatic ring system or a mono- or bicyclic heteroaromatic ring system; R3 is C1-20alkyl, C3-6cycloalkyl, C3-6cycloalkylC1-5alkyl, C1-10alkoxyC1-10alkyl, or an aromatic or heteroaromatic ring system; W is SO2 or a bond; X is O or S; and Y is a group of the formula A1—A2—A3 in which A1 and A3 each represent a bond or a straight chain or branched alkylene group, said alkylene group(s) containing a total of 1 to 10 carbon atoms and A2 represents a bond or O, S, SO, SO2, CO, C═CH2, CONH, NHCO, CR15R16, CH═CH or C═C, providing that when A2 is O, S, SO, SO2 or CONH, A3 contains at least two carbon atoms linking the A2 group and the CH2 group in formula (I).

Abstract: Novel macrocyclic compounds are constructed to include large cyclic structures that are interrupted by at least one ring system. Each interrupting ring system includes two bridgehead atoms. Bridgehead atoms are bonded to one or more bridges that interconnect one or more ring systems thereby forming a large cyclic structure. Located in each bridge are two or more nitrogenous moieties that are derivatized with chemical functional groups. The ring systems can include further nitrogenous moieties, either as ring atoms or on pendant groups attached to the ring. These can also be derivatized with chemical functional groups. The totality of the chemical functional groups imparts certain conformational and other properties to the macrocyclic compounds. In accordance with certain embodiments of the invention, libraries of such macrocyclic compounds are prepared utilizing permutations and combinations of the chemical functional groups and the nitrogenous moieties to build complexity into the library.

Abstract: The invention relates to a process for the preparation of substituted pyrimidines of formula I, wherein R1, R2, R3, R4 and X are as defined in claim 1, which comprises reacting an amidine of formula II, or a salt thereof, with a 3,3-disubstituted vinylcarbonyl compound of formula III wherein L represent a halogen atom or a group of formula —X—R2, (a) in an inert solvent, in the presence of a base and a compound of formula IV H—X—R2  (IV) in the event that L represent a halogen atom, or (b) in an inert solvent and in the presence of a base, in the event that L represents a group of formula —X—R2.

Abstract: In the proposed condensation product based on amino-s-triazines with at least two amino groups, formaldehyde and sulphite, the molar ratio of amino-s-triazine, formaldehyde and sulphite is 1:2.5-6.0:1.51-2.0 and the formiate content is less than 0.3 wt %. The condensation product is obtained by a) heating amino-s-triazine, formaldehyde and a sulphite in the molar ratio 1:2.5-6.0:1.51-2.0 in an aqueous solution at a temperature of 60-90° C. and a pH level of between 9.0 and 13.0 until the sulphite can no longer be detected; b) continuing the condensation at a pH level of between 3.0 and 6.5 and a temperature of 60-80° C. until the condensation product has a viscosity of 5-50 mm/s at 80° C.; and c) adjusting the pH level of the condensation product to 7.5-12.0 or carrying out thermal secondary treatment at a pH level of >10.0 and a temperature of 60-100° C. The product can be used as an additive for inorganic binders such as cement.

Abstract: Provided are chromophores of the formula Q—(—L—Z)x, wherein x is 3 or 4, wherein Q is selected from the group consisting of wherein L is selected from the group consisting of wherein R is an alkyl group having 1 to 20 carbon atoms, and wherein Z is selected from the group consisting of

Abstract: 6-Phenyl-Pyrazolopyrimidines of formula I wherein R1 is alkyl, alkenyl, alkynyl, alkadienyl or haloalkyl, cycloalkyl, bicycloalkyl, phenyl, naphthyl, or 5- or 6-membered heterocyclyl, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom, or 5- or 6-membered heteroaryl, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom,  where these radicals may be unsubstituted or substituted as defined in the specification, Y is oxygen, sulfur, NR2 or a single bond; wherein R2is defined in the specification; and R1 and R 2 together with the interjacent nitrogen atom may represent a 5- or 6-membered heterocyclic ring, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom, which may be substituted by one or more Rc radicals; m is 0 or an integer from 1 to 4; L each independently is halogen, nitro, alkyl, alkoxy, and X is halogen; processes and intermediates fo