Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.

Abstract: The invention relates to a novel process for preparing known asymmetrical 4,6-bis(aryloxy)pyrimidine derivatives.

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: The present invention relates to novel butyne diol derivatives of the general formula I and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more compounds of the general formula I and especially their use as endothelin receptor antagonists.

Abstract: A compound, suitable as an alpha-2B-adrenoceptor antagoist, having a structure of formula (I) 1

Abstract: The invention relates to novel substituted phenyluraciles of the general formula (I) in which m, n, Q and R1-7 are each as defined in the description, and to processes for their preparation and to their use as herbicides.

Abstract: A method for inhibiting sexual transmission of HIV comprising topically applying to the skin or epithelial tissue of a human a composition comprising a non-nucleoside reverse transcriptase inhibitor (“NNRTI”) that is able to inhibit viral replication for periods exceeding 12, 24, or even 36 days, at concentrations below even 10 &mgr;M. In one embodiment the NNRTI is a dihydro-alkyloxy-benzyl-oxopyrimidine (DABO).

Abstract: The invention provides fungicidal compounds of formula (I) or stereoisomers thereof: 1

Abstract: The present invention relates to an uracil compound of the formula [I]: [wherein, Q—R3 represents a R3-substituted group of a 5-membered or 6-membered heterocyclic ring having one or two nitrogen selected from the group consisting of moieties represented in the specification (wherein, this heterocyclic ring may be substituted with at least one kind of substituent, Y represents oxygen, sulfur, imino or C1 to C3 alkylimino, R1 represents C1 to C3 alkyl or C1 to C3 haloalkyl, R2 represents C1 to C3 alkyl, R3 represents carboxy C1 to C6 alkyl, C1 to C6 alkoxycarbonyl C1 to C6 alkyl, OR7, SR8, N(R9)R10 or the like, X1 represents halogen, cyano, thiocarbamoyl or nitro, X2 represents hydrogen or halogen. {wherein, each of R7, R8 and R10 independently represents carboxy C1 to C6 alkyl, C1 to C6 alkoxycarbonyl C1 to C6 alkyl, C1 to C6 haloalkoxycarbonyl C1 to C6 alkyl, or the like, and R9 represents hydrogen or C1 to C6 alkyl.}.].

Abstract: The present invention relates to compounds of the formula 1 1

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: 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 relates to novel hypolipidemic, antihyperglycemic compounds, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. More particularly, the present invention relates to novel &bgr;-aryl-&agr;-oxysubstituted alkylcarboxylic acids of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them.

Abstract: The invention relates to compounds of the general formula 1

Abstract: Novel derivatives of 5-thia- and 5-selenopyrimidinone are found to inhibit the enzyme glycinamide ribonucleotide formyl transferase (GARFT) and amino imidazole carboxamide ribonucleotide formyl transferase (AICARFT). Novel intermediates of these compounds are also disclosed. A novel method of preparing such compounds is also disclosed, as well as methods and compositions for employing the compounds as antiproliferative agents.

Abstract: The present invention relates to pharmaceutically acceptable salts of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them.

Abstract: The invention relates to a process for preparing ar(alk)yluracils of the general formula (I) in which A represents a single bond or represents alkanedlyl, Ar represents optionally substituted aryl, R1 represents optionally substituted alkyl and R2 represents hydrogen, halogen or alkyl, and to novel intermediates for this purpose and to processes for their preparation.

Abstract: Compounds having one or more structures represented by general formula (I) as partial structure thereof, which are typified by pyrimidone and pyridone compounds, have two or more reaction sites in alkylation reactions. Accordingly, there is no process for producing O-alkylated products of these compounds at a high selectivity or such processes, if any, are applicable exclusively to those having limited structures. A process for selectivity O-alkylating such a compound as described above by converting it into the copper salt by using a monovalent copper compound such as copper suboxide and then reacting it with an alkylating agent having a leaving group in the presence of a phosphorus compound such as a phosphite. Pyrimidyloxy derivatives or pyridyloxy derivatives obtained by this reaction is useful as intermediates of pesticides or drugs.

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: The present invention relates to an uracil compound of the formula [I]: wherein W represents oxygen, sulfur, imino or C1 to C3 alkylimino; Y represents oxygen, sulfur, imino or C1 to C3 alkylimino; R1 represents C1 to C3 alkyl or C1 to C3 haloalkyl; R2 represents C1 to C3 alkyl; R4 represents hydrogen or methyl; R5 represents C1 to C6 alkyl, C1 to C6 haloalkyl, or the like; X1 represents halogen, cyano or nitro; X2represents hydrogen or halogen; and each of X3 and X4 independently represents hydrogen, halogen, C1 to C6 alkyl, or the like. The present compound has an excellent herbicidal activity.

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 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: There are provided compositions and methods comprising compounds of formula I: wherein R1, A, B, X, Y and Z have the meaning given in claim 1, for the control of insect and acarid pests.

Abstract: The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.

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

Abstract: Pyrimidone compounds of formula (I): 1

Abstract: The invention relates to compounds of the formula 1

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: Aminoguanidine and alkoxyguanidine compounds are described, including componds of the Formula VII: 1

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: The present invention provides an uracil compound of the formula: wherein A1 represents amino or C1-C3 alkyl, A2 represents C1-C3 haloalkyl, X represents hydrogen or halogen, Y represents halogen, R1 represents —OR21, —ON(R22)R23, —ON═C(R24)R25, —SR26, —N(R27)R28, —N(29)OR30, —N(R31)SO2R32 or —N(R33)N(R34)R35, and R2, R3, R4 and R5 independently represent hydrogen or C1-C3 alkyl and a herbicidal composition comprising the above uracil compound as an active ingredient. The uracil compound has excellent herbicidal activity.

Abstract: The present invention relates to an optically active uracil compounds of the formula (I): wherein, R1 is C1-C8 alkyl or C3-C8 alkenyl, and * represents an asymmetric carbon atom whose configuration is R. The compounds have excellent herbicidal activity.

Abstract: Novel phenethyl-5-bromopyridylthiourea (PBT) and dihydroalkoxybenzyloxopyrimidine (DABO) derivatives exhibiting spermicidal activity as well as anti-viral activity. These novel compounds can be incorporated within contraceptive compositions to provide for spermicidal or sperm-immobilizing activity.

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: This invention relates to single enantiomers of novel cis-substituted 1,3-oxathiolanes, of the formula (I): wherein; R1 is hydrogen, and R2 is cytosine or 5-fluorocytosine; and pharmaceutically acceptable salts and esters thereof. This invention also relates to pharmaceutical compositions containing them and to the use of these compounds as antiviral agents, particularly in combination therapy.

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: Nucleoside analogues containing a 1,3-dioxolane structure are suitable antiviral agents, particulary for the treatment of the HIV infections in mammals, especially humans. Examples of the nucleoside analogues include: cis-2-acetoxymethyl-4-(thymin-1′-yl)-1,3,-dioxolane, cis-2-hydroxymethyl-4-(thymin-1′-yl)-1,3-dioxolane, cis-2-benzoyloxymethyl-4-(cytosin-1′-yl)-1,3-dioxolane, and cis-2-hydroxymethyl-4-(cytosin-1′-yl)-1,3-dioxolane. These compounds can be in the form of their racemates or their separate enantiomers.

Abstract: The present invention relates to novel anticancer agents, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, and their pharmaceutically acceptable solvates. The present invention more particularly relates to novel derivatives of andrographolide, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, and their pharmaceutically acceptable solvates. The novel derivatives of andrographolide have the general formula (I).

Abstract: The present invention provides compounds comprising propynyl uracils having the formula wherein R1 is hydrogen, chlorine, bromine, iodine, fluorine, —CN, substituted or unsubstituted linear or branched C1-C4 alkyl, —NO2, methoxy, ethoxy, n-propoxy, or iso-propoxy; R2 is iodine or bromine; and R3 is propynyl, 3-iodopropynyl, 3-bromopropynyl, substituted or unsubstituted 2-furanyl, substituted or unsubstituted 3-furanyl, substituted or unsubstituted 2-pyrrolidinyl, substituted or unsubstituted 3-pyrrolidinyl, D-ribose, or deoxyribose. Another embodiment of the invention encompasses propynyl uracils having the formula wherein R4 is hydrogen, chlorine, bromine, iodine, fluorine, —CN, substituted or unsubstituted linear or branched C1-C4 alkyl, —NO2, methoxy, ethoxy, n-propoxy, or iso-propoxy; R5 is hydrogen or propynyl; and R6 is iodine or bromine. Also, methods of preparing these propynyl uracils are provided.

Abstract: The uracil compounds represented by the formula [V]: wherein R1 represents C1-C5 perfluoroalkyl group and Q represents an aromatic group, can be produced by making the amide compounds represented by the formula [II]: wherein R1 and Q have the same meanings defined above, or its hydrate react with a cyanate salt in the presence of a protonic acid.

Abstract: Diaryl ether compounds useful in the control of weeds are described. An exemplary compound is represented by the general formula (I): In this formula Q is represented by Q9: X and Y represent a hydrogen atom, halogen atom, cyano group, nitro group or (C1-6)haloalkyl group. A1 and A2 are independently oxygen or sulfur atoms. R9 and R10 represent a hydrogen atom, a (C1-6)alkyl group, an acyl group, or a (C1-6)alkylsulfonyl group; or R9 and R10 may form a ring consisting of polymethylene, (CH2)m groups, where m is an integer of 2, 3, 4 or 5, together with the nitrogen atom of NR9R10, which may or may not have a (C1-6)alkyl substituent. Methods of making the compounds are also described.

Abstract: The invention relates to a diastereoselective process for the preparation of compounds of formula (1), wherein W is S, S═O, SO2 or O; X is S, S═O, SO2 or O; R1 is hydrogen or acyl, and R2 is a purine or pyrimidine base or an analogue or derivative thereof.

Abstract: The novel compounds of formula I: (A, B, R1, R2, R3, X and m are defined in the specification) show selective herbicidal activity. The new compounds can be prepared according to known methods and can be used as herbicides in agriculture and related fields.

Abstract: A compound having the formula (I) or a pharmaceutically acceptable salt thereof where the variables are defined in the specification are useful in the treatment of sickle-cell anemia.

Abstract: This invention is directed to poly-hydroxylated monocyclic N-heterocyclic derivatives selected from the following formulae: 1

Abstract: This invention is directed to polyhydroxylated monocyclic N-heterocyclic derivatives selected from the following formulae: 1

Abstract: The present invention provides an AP-1 activation inhibitor, NF-kappa B activation inhibitor, inflammatory cytokine production inhibitor, matrix metalloprotease production inhibitor, inflammatory cell adhesion molecule expression inhibitor, anti-inflammatory agent, antirheumatic agent, immunosuppressant, cancer metastasis inhibitor, remedy for arteriosclerosis and antiviral agent which contain the benzene derivative of the following general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient.

Abstract: Novel compounds are provided that are effective to inhibit the activity of DHUDase or UrdPase. Such compounds have the general formula where X is S or Se; Y is H, I, F, Cl, Br, methoxy, benzyl, selenenylphenyl, or thiophenyl, and R1 is H or an acyclo tail having the general formula where R2 is H, CH2 OH or CH2 NH2; R3 is OH, NH2, or OCOCH2CH2CO2H; and R4 is O, S, or CH2. The compounds can be used in pharmaceutical compositions, along with various chemotherapeutic agents to increase the efficacy of the treatment. These compounds can also be used in methods of treating patients by coadministering or sequentially administering the enzyme inhibiting compounds with a chemotherapeutic agent effective to treat cancers, or viral, fungal, bacterial, or parasitic infections. The compounds have further utility in enhancing imaging. Further, they can be administered alone to prevent and/or treat disorders of pyrimidine catabolism and other physiological disorders.

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.