Abstract: The invention provides a novel class of substituted isoindolinone derivatives, useful for the treatment of inflammation and reperfusion injuries. Pharmaceutical compositions, and methods of making and using the compounds, or pharmaceutically acceptable salts, hydrates, stereoisomers or mixtures thereof are also described. The novel isoindolinone derivatives have the formula: or a pharmaceutically acceptable base or acid addition salt, hydrate, stereoisomer, or mixtures thereof, wherein R14 is described herein.

Abstract: The invention relates to compounds based on merocyanines with the general formulas I and/or II, 1

Abstract: Compounds and compositions are provided which are useful for the treatment of viral infections, particularly human Cytomegalovirus infection. The compounds include novel pyrimidine-based derivatives.

Abstract: Multicyclic aromatic compounds useful as complexing agents having the general formula: Methods of complexing and quantitating a component in a sample such as urea or guanidine are also disclosed.

Abstract: Compounds of the formula: (where R1, R2 and R3 are defined in the specification) are inhibitors of AICARFT. These compounds, as well as their pharmaceutically acceptable salts, solvents, prodrugs, and pharmaceutically active metabolites, are useful in pharmaceutical compositions for treating diseases such as cancer.

Abstract: The present invention relates to methods for preparing macrocyclic products having 9 or more ring atoms by ring-closing diyne metathesis of suitable diyne substrates. The diyne substrates can be converted into cycloalkynes or into cycloalkadiynes by cyclodimerization, depending on the particular reaction conditions. Any alkyne metathesis catalyst can be used as the catalyst, regardless of whether said catalysts are heterogeneously or homogeneously present in the reaction medium. The preferred catalysts or pre-catalysts are transition metal alkylidyne complexes, transition metal compounds which form alkylidyne complexes under the reaction conditions, and transition metal compounds with metal-metal triple bonds. The method can be carried out with numerous functional groups, solvents, and additives.

Abstract: N-Heterocyclic derivatives selected from the group consisting of the following formulae: where Z1, Z2, Z3, R1, R2, R3, R4, R5 and R6 are described herein, are useful as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein.

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 concerns antiviral compounds, their compositions, and use in the treatment of viral infections. More particularly, the invention provides benzimidazolone derivatives for the treatment of respiratory syncytial virus infection.

Abstract: The novel compounds of formula I: 1

Abstract: The invention relates to novel substituted cyanophenyluracils of the general formula (I) in which R1, R2, R3, R4, R5 and Q are each as defined in the description, to processes for their preparation, to novel intermediates and to their use as herbicides and insecticides.

Abstract: Therapeutic oligonucleotide analogs which have improved nuclease resistance and improved cellular uptake are provided. Replacement of phosphorodiester inter-sugar linkages found in wild type oligomers with four atom linking groups forms unique di- and poly-nucleosides and nucleotides useful in regulating RNA expression and in therapeutics. Methods of synthesis and use are also disclosed.

Abstract: The present invention relates to ester, ether and N-alkylcarbamoyl derivatives of compound (Ia) and pharmaceutically acceptable salts thereof. These compounds exhibit excellent antibacterial activity and are useful for the treatment or prevention of bacterial infections. (wherein R1 is a hydrogen atom or a methyl group; R2a is a hydrogen atom, a protecting group for a hydroxy group, or a methyl group; R3 is a hydrogen atom or a protecting group for a hydroxy group; R4a is a hydrogen atom, a hydroxy group or a protected hydroxy group; R5 is a hydrogen atom or a protecting group for a hydroxy group; and X is a methylene group or a sulfur atom). The invention also includes compounds which are related to the aforeidentified compounds.

Abstract: The present invention pertains to the field of medicine and more precisely relates to a novel immuno-modulator of the following formula which exhibits anti-microbial and anti-mycobacterial activities. This modulator is produced by reacting equimolecular amount of 6-methyluracyl-5-sulphochloride and isoniazide in acetonitrile at a high temperature. The preparation is practically not toxic (LD50 in severe conditions exceeding 7000 mg/kg) and can be used according to a given clinical tests for expressing the immuno-modulating and anti-mycobacterial activity. This preparation can be used for correcting various immuno-deficiencies including in HIV-infected patients as well as for treating mycobacterioses such as leprosy, tuberculosis, etc. This preparation can be administrated internally or parenterally.

Abstract: A compound of the general formula (I): 1

Abstract: The invention relates to substituted polycyclic aryl and heteroaryl uracil compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.

Abstract: The compounds of formula (I) 1

Abstract: The invention relates to novel substituted phenyluracils of the general formula (I) in which R1, R2, R3, R4, R5 and R6 are each as defined in the description, to processes for their preparation, to novel intermediates and to their use as herbicides.

Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women.

Abstract: The invention relates to novel acridine derivatives of formula 1, to their preparation and to their use as medicaments, in particular for treating tumors.

Abstract: The invention relates to novel substituted thienyl(amino)sulphonyl(thio)ureas of the formula (I) in which A represents nitrogen or a CH grouping, E represents a single bond or an NH grouping, Q represents oxygen or sulphur, R1 and R2 independently of one another represent hydrogen, halogen or in each case optionally substituted alkyl, alkoxy, alkylthio, alkylamino, dialkylamino, cycloalkyl, cycloalkyloxy, aryloxy or heterocyclyloxy, R3 represents hydrogen or optionally substituted alkyl, R4 and R5 independently of one another each represent cyano, halogen or represent in each case optionally substituted alkyl, alkoxy, alkenyl, alkenyloxy, alkinyl or alkinyloxy, and R6 represents hydrogen, cyano, halogen or represents in each case optionally substituted alkyl, alkoxy, alkenyl, alkenyloxy, alkinyl or alkinyloxy, and to salts of compounds of the formula (I), to processes for preparing the novel compounds and to their use as herbicides.

Abstract: The invention relates to novel substituted aryluracils of the formula (I): to processes for their preparation and to their use as crop protection agents.

Abstract: The present invention relates to novel antidiabetic compounds, their tautomeric forms, their derivatives, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them.

Abstract: The invention relates to novel substituted p-trifluoromethylphenyluracils of the general formula (I) in which R1, R2, R3, R4 and R5 are each as defined in the description, to a process for their preparation and to their use as herbicides.

Abstract: The invention relates to novel pyridine derivatives of formula 1, to their preparation and to their use as medicaments, in particular for treating tumors.

Abstract: There is provided a uracil substituted 1-phenylbenzotriazole compound having the structural formula I.

Abstract: Novel and efficient syntheses create novel piperazinone intermediates which facilitate the production and use of PNAs. Such syntheses and the products enhance the feasibility of a system which permits the rapid identification of PNA oligomers useful as therapeutics, diagnostics and/or gene characterization tools. A first component of the system is a universal PNA library that most preferably incorporates one or more universal nucleotide bases into carefully selected positions within each oligomer species thereby providing the library with the screening ability of a much larger library. The second component of the system is a high throughput screening system that includes a number of assays designed to provide information on the binding activities of the different PNAs to a target nucleotide sequence (generally, a DNA or RNA sequence).

Abstract: The invention relates to novel substituted phenyluracils of the general formula (I) in which the radicals n, Q, R1 to R6 are each as defined in the description, and to processes for this preparation and to their use as herbicides.

Abstract: Pyrimidine-5-carboxamide derivatives represented by a general formula (I) or salts thereof [wherein each symbol has the following meaning; X: O, S, NR1, CO, NR1CO, CONR1, C═N—OR1 or a bond, Y: a lower alkylene group which may be substituted by OR1 or —NHR1, or a bond, Z: O, NR2 or a bond, A: H, or a lower alkyl which may have a substituent, a —CO-lower alkyl which may have a substituent, an aryl which may have a substituent, a heteroaryl which may have a substituent, a cycloalkyl which may have a substituent or a nitrogen-containing saturated heterocyclic group which may have a substituent, B: an aryl which may have a substituent or a heteroaryl group which may have a substituent, R1, R2: H, a lower alkyl or a —CO-lower alkyl group].

Abstract: The invention relates to novel quinoline derivatives of the formula 1, to their preparation and to their use as medicaments, in particular for treating tumors.

Abstract: The invention provides a compound, useful as an optical probe or sensor of the activity of at least one cytochrome P450 enzyme, and methods of using the compound to screen candidate drugs, and candidate drugs identified by these methods.

Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.

Abstract: A group of novel pyrimidone compounds are inhibitors of the enzyme LDL PLA2 and therefore of use in treating atherosclerosis.

Abstract: The invention relates to novel aminouracils of the general formula (I) in which, Q, R1, R2, R3, R4, R5, R6 and R7 are each as defined in the description, to their use as herbicides and to novel intermediates.

Abstract: A 5,6-dihydrouracil compound given by the formula [I]: wherein, R1 represents C1-C2 haloalkyl group and Q represents Q1 of the formula below, etc.: wherein, R3 is hydrogen atom or halogen atom, R15 is C3-C6 alkynyl group, etc., Z is oxygen atom, sulfur atom or NH group, and T is direct bond or methylene group, has an excellent herbicidal efficacy.

Abstract: There are described cycloalkyl derivatives of the formula (I) R1—Y—A—B—D—E—F—G  (I) in which R1, Y, A, B, D, E, F and G have the meaning indicated herein, their preparation and their use as medicaments. The compounds according to the invention can be used as vitronectin receptor antagonists and as inhibitors of bone resorption.

Abstract: Novel hydroximic acid derivatives I and salts thereof, where X=O, S; Y=O, S; R1=H, C1-C4-alkyl, NH2, C1-C4-alkylamino or di(C1-C4-alkyl)amino; R2=C1-C3-haloalkyl; R3=H, halogen, C1-C4-alkyl; R4=H, halogen; R5=CN, halogen; R6=C1-C6-alkyl, C2-C6-alkenyl, C3-C6-alkynyl or phenyl-C1-C6-alkyl, where the phenyl ring of this group may be unsubstituted or may carry 1-3 substituents; R7=a C1-C6-alkyl, C2-C6-alkenyl, C3-C6-alkynyl or phenyl-C1-C6-alkyl, where these 4 groups may be unsubstituted or may carry 1 to 2 substituents; Use: As herbicides; for the desiccation/defoliation of plants.

Abstract: Compounds of Formula I are disclosed, having activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4, and accordingly useful for treating diseases whose symptoms and or damage are related to the binding of VCAM-1 to cells expressing VLA-4.

Abstract: The invention relates to novel 3-heterocycl-1-yluracils of formula I: wherein R1 and R2 together with the interjacent nitrogen atom form an optionally substituted, optionally benzo-condensed 5-membered heterocyclic ring and R3 through R5 have the meaning given in claim 1. The invention also relates to a method of the production of these substances and to herbicidal compositions containing such compounds as active ingredients.

Abstract: A compound of the formula 1

Abstract: This invention is directed to aryl and heterocyclyl substituted pyrimidine derivatives selected from the following formulae: wherein Z1, Z2, R1, R2, R3, R4, R5 and R6 are defined herein. These compounds are useful as anti-coagulants.

Abstract: The present invention relates to a method for controlling weeds in corn field which comprises applying a herbicidal composition comprising 2-[2-chloro-4-fluoro-5-{3-methyl-2,6-dioxo-4-(trifluoromethyl)-1,2,3,6-tetrahydropyrimidin-1-yl}phenoxy]propionic acid ester as an active ingredient to corn fields after seeding corn. According to the present method, kinds of weeds in corn fields can be controlled widely and no problematic phytotoxicity to corn is caused.

Abstract: Compounds of formula 1 wherein R1 is hydrogen, fluorine, chlorine, bromine or methyl; R2 is C1-C4alkyl, C1-C4halogenalkyl, halogen, hydroxy, C1-C4alkoxy, C1-C4halogenalkoxy, nitro, amino or cyano; R3, R15 to R39 and X6 to X19 are as defined in claim 1, and the agrochemically acceptable salts and stereoisomers of these compounds of formula I are suitable for use as herbicides.

Abstract: The invention relates to substituted phenyluracils of the general formula (I) in which the radicals R1 to R5, Q and n are each as defined in the description, and to processes for their preparation and to their use as herbicides.

Abstract: This invention provides compounds of Formula I having the structure 1

Abstract: An improved process and intermediate compounds for the preparation of 2-(N,N-disubstituted)amino-4-(perfluoroalkyl)-1,3-oxazin-6-one compounds having the structural formula I and an improved process for the preparation of 6-(perfluoroalkyl)uracil compounds having the structural formula V

Abstract: The present invention relates to novel 3-(substituted)-2-indolinones compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related disorders such as cancer.

Abstract: The present invention relates to a process for preparing 5′-acetylstavudine, an intermediate which is useful in the preparation of 2′,3′-didehydro-3′-deoxythymidine, an active principle with antiviral action which is commonly known as stavudine (D4T).

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: The disclosure concerns pyrimidine derivatives represented by the following general formulas [I] and [I′] and having antiviral activity, particularly antiretroviral activity such as anti-HIV activity: and pharmaceutical compositions having antiviral activity and comprising the above-described derivative(s) as an active ingredient.