Abstract: This invention relates aryl substituted pyridines, pyrimidines, pyrazines and triazines of Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein A1, A2, A3, R1-R4, X and Y are set in the specification. The invention is also directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.

Abstract: Dihydropyrimidine derivatives of the following formula or analogs thereof have selective N-type calcium channel antagonistic activity, and they are used as therapeutic agents for various diseases participating in the N-type calcium channels.

Abstract: The present invention provides novel compounds, and pharmaceutical compositions thereof, and methods of using same in the treatment of affective disorders, anxiety, depression, post-traumatic stress disorders, eating disorders, supranuclear palsey, irritable bowl syndrome, immune supression, Alzheimer's disease, gastrointestinal diseases, anorexia nervosa, drug and alcohol withdrawal symptoms, drug addiction, inflammatory disorders, or fertility problems. The novel compounds provided by this invention are those of formula: wherein R1, R3, R5, Q, Z, Y, V, X and X′ are as defined herein.

Abstract: Fungicidal pyrimidine derivatives and the use as a fungicide of the compounds of formula (1): wherein R1 is H, C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl C3-C6cycloalkyl, C1-C6alkoxy, C3-C6cycloalkoxy, C1-C6alylthio, C1-C6alkylsulfinyl, C1-C6alkylsulfonyl, phenyl, pyridinyl or azolyl groups, (being optionally substituted by one or more substituents); or N(R4)C(O)R5, R2 is polyfluoroalkyl, R3 is fluorine, chlorine, bromine or iodine; ethenyl or ethynyl (being optionally substituted by one or more of halogen), R4 and R5 are, independently, H, C1-C6alkyl, C2-C6alkenyl or C2-C6alkynyl groups, (being optionally substituted by one or more of halogen or cyano); or R4 and R5 can join together to form a 5 or 6-membered ring, Q is a heteroaromatic ring selected from the following ring system; imidazol-1-yl, pyrazol-1-yl, 1,2,3-triazol-1-yl, 1,2,3-triazol-2-yl, 1,2,4-triazol-1-yl, 1,2,4-triazol-1-yl, benzimidazol-1-yl or tetrazol-5-yl groups, (being optionally substituted by one or more of substituents).

Abstract: Pyrimidine derivatives having excellent herbicidal activities for crop plants and selectivity between crop plants and weeds, are presented. Pyrimidine derivatives represented by the following formula (I): wherein R1 is a hydrogen atom, an alkyl group, a haloalkyl group or the like; R2 is an alkyl group, a phenyl group which may be substituted, or the like; R3 is a hydrogen atom, an alkyl group, an alkynyl group or the like; R7 is a hydrogen atom, a halogen atom, an alkyl group or the like; R8 is a hydrogen atom, an alkyl group or the like, W is a —C(═Q) Z— group or a —SO2— group; Q is O or S; Z is O, S, a —C(R4)R5—, a —NR6 group or the like; each of R4 and R5 is a hydrogen atom, an alkyl group, an alkoxy group or the like; R6 is a hydrogen atom or an alkyl group; and Ar is a phenyl group which may be substituted, a pyridyl group which may be substituted, or the like, and herbicides containing such pyrimidine derivatives as active ingredients.

Abstract: The invention relates to pyridines and uses thereof, including to inhibit lysophosphatidic acid acyltransferase &bgr; (LPAAT-&bgr;) activity and/or proliferation of cells such as tumor cells.

Abstract: The present invention provides an AP-1 activation inhibitor, a NF-kappaB activation inhibitor, an inflammatory cytokine production inhibitor, a production inhibitor for matrix metalloprotease or an inflammatory cell adhesion factor expression inhibitor, which contains a heterocyclic compound or a pharmaceutically acceptable salt thereof as an active ingredient.

Abstract: Isoxazolone compounds having the generic structure: are used to treat disease associated with unwanted cytokine activity, including rheumatoid arthritis, osteoarthritis, diabetes, HIV/AIDS, inflammatory bowel disease, Crohn's disease, ulcerative colitis, congestive heart, hypertension, chronic obstructive pulmonary disease, septic shock syndrome, tuberculosis, adult respiratory distress, asthma, atherosclerosis, muscle degeneration, periodontal disease, cachexia, Reiter's syndrome, gout, acute synovitis, anorexia and bulimia nervosa fever, malaise, myalgia and headaches.

Abstract: Nitrogen-containing heterocyclic carboxamide derivatives represented by the following general formula: wherein ring A is a substituted or unsubstituted pyrazine, pyrimidine, pyridazine or triazine ring; R1 is O or OH; R2 is a hydrogen atom, an acyl group or a substituted or unsubstituted carbamoylalkyl or carboxyalkyl group; and the broken line represents a single bond or a double bond; or salts thereof are useful for preventing and treating virus infections and especially influenza virus infections.

Abstract: Compounds of formula (I): wherein: V represents a single bond or a linear or branched (C1-C6)alkylene chain, M represents a single bond or a linear or branched (C1-C6)alkylene chain, A and E each represents nitrogen or CH, but at least one of the two groups A or E represents nitrogen, W represents a group of formula (i): X represents carbonyl, G1 represents a linear C3 alkylene chain optionally containing a double bond and/or being optionally substituted by a hydroxyl group, their isomers, their hydrates, their solvates, and additional salts thereof with a pharmaceutically acceptable acid, and medicinal products containing the same which are useful in the treatment of diseases or pathological conditions in which endothelial dysfunction is known.

Abstract: The invention relates to a process for the preparation of alkylimidazolidone (meth)acrylates, generally expressed as compound (I): 1

Abstract: A triazolone compound of the formula [I]: wherein; R1 represents optionally substituted phenyl or the like, T represents m-phenylene optionally substituted by methyl or the like; and a fungicidal composition containing it as an active ingredient.

Abstract: This invention discloses and claims diary heterocycles of formula (I) 1

Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: 1

Abstract: Novel pyridylpyrimidines of the formula 1

Abstract: This invention relates to certain novel 2′-halomethylidene, 2′-ethenylidene and 2′-ethynyl cytidine, uridine and guanosine derivatives, and compositions thereof, which are useful in the treatment of patients afflicted with neoplastic or viral disease states.

Abstract: The present invention relates to novel heterocyclic fluoroalkenyl thioethers of the formula (I) in which m represents integers from 3 to 10, n represents 0, 1 or 2 and Het represents the following, in each case optionally substituted, groupings: to processes for their preparation and to their use as pesticides.

Abstract: The present invention relates to carboxylic acid derivatives of the formula where the radicals have the meanings stated in the description, to the preparation of these compounds and to their use as drugs.

Abstract: This invention describes novel pyrazole compounds of formula IIIa: wherein R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx, Ry, R2, and R2′ are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.

Abstract: The present invention relates generally to a novel class of pyrimidinones of Formula (I): that are useful as serine protease inhibitors, and more particularly as Hepatitis C virus NS3 protease inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of using the same.

Abstract: Fungicidal compounds of the formula (I): and stereoisomers thereof, wherein R1 is optionally substituted aryl or optionally substituted heteroaryl; Y is oxygen, sulphur or NR4; R2, R3 and R4, which may be the same or different, are hydrogen, C1-4 alkyl or C2-4 alkenyl; X is halogen, C1-4 alkyl, C2-4 alkenyl, C1-4 alkoxy, nitro or cyano, and n is 0 or an integer of 1 to 4; provided that when Y is oxygen, n is 0 and R1 is unsubstituted phenyl at least one of R2 and R3 is other than hydrogen or methyl.

Abstract: This invention describes novel pyrazole compounds of formula I′: wherein Q′ is —O—, —C(R6′)2—, 1,2-cyclopropanediyl, 1,2-cyclobutanediyl, or 1,3-cyclopropanediyl, and R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T—R3 or L—Z—R3, or Rx and Ry are taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-7 membered ring having 0-3 heteroatoms; and R2 and R2′ are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.

Abstract: aP2 inhibiting compounds are provided having the formula wherein A, B, X, and Y are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, employing such aP2 inhibitor or a combination of such aP2 inhibitor and another antidiabetic agent such as metformin, glyburide, troglitazone and/or insulin.

Abstract: The invention relates to novel fluoromethoximino compounds, to a process for their preparation and to their use as pesticides, and also to novel intermediates and to a plurality of processes for their preparation.

Abstract: The present invention relates to novel heterocyclic fluoroalkenyl thioethers of the formula (I) 1

Abstract: The invention relates to carboxylic acid derivatives of the formula where the radicals have the meanings defined in the description, to the preparation of these compounds and to their use as drugs.

Abstract: Compounds of formula (I) and pharmaceutically-acceptable and -cleavable esters thereof and acid addition salts thereof, wherein the symbols are as defined are MAP kinase inhibitors, useful pharmaceutically for treating TNF&agr; and IL-1 mediated diseases such as rheumatoid arthritis and diseases of bone metabolism, e.g. osteoporosis.

Abstract: Nucleoside analogues or base analogues having structure (I), where X=O or NH or S, Y=N or CHR6 or CR6, W=N or NR6 or CHR6 or CR6 or S, n=1 or 2; each R6 is independently H or O or alkyl or alkenyl or alkoxy or aryl or a reporter moiety; where necessary (i.e. when Y and/or W is N or CR6 where R6 is not O) a double bond is present between Y and W or W and W, and Q is H or a sugar or a sugar analogue or a nucleic acid backbone or backbone analogue.

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

Abstract: This invention concerns the use of compounds of formula 1

Abstract: Compounds of formula I wherein the symbols have meaning as defined herein, are p38 MAP kinase inhibitors, and are useful pharmaceutically for treating TNF&agr; and IL-1 mediated diseases, such as rheumatoid arthritis, and diseases of bone metabolism, e.g. osteoporosis.

Abstract: This invention relates to certain novel 2′-halomethylidene, 2′-ethenylidene and 2′-ethynyl cytidine, uridine and guanosine derivatives, and compositions thereof, which are useful in the treatment of patients afflicted with neoplastic or viral disease states.

Abstract: The present invention relates to compound which are capable of preventing the extracellular release of inflammatory cytokines, said compounds, including all enantiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, have the formula: 1

Abstract: The invention relates to a process for the preparation of alkylimidazolidone (meth)acrylates, generally expressed as compound (I): 1

Abstract: The present invention relates to compound which are capable of preventing the extracellular release of inflammatory cytokines, said compounds, including all enantiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, have the formula: wherein R comprises ethers or amines; R1 is: a) substituted or unsubstituted aryl; or b) substituted or unsubstituted heteroaryl; two R2 units on the same carbon atom are taken together to form a spirocyclic ring having from 4 to 7 atoms, the balance of the R2 units are independently selected from the group consisting of: a) hydrogen; b) —O(CH2)jR8; c) —(CH2)jNR9aR9b; d) —(CH2)jCO2R10; e) —(CH2)jOCO2R10 f) —CH2)jCON(R10)2; and g) two R2 units can be taken together to form a carbonyl unit; R8, R9a, R9b, and R10 are each independently hydrogen, C1-C4 alkyl, and mixtures thereof; R9a and R9b can be taken together to form a carbocyclic or heterocyclic ring comprising from 3 to 7 atoms; two R10 uni

Abstract: N-Heterocyclic derivatives of the formula (I): 1

Abstract: Novel 1,4,5-subsituted imidazole compounds and compositions for use in therapy as cytokine inhibitors.

Abstract: The invention relates to a process for preparing essentially formic acid-free N-alkyl-N′-methylalkyleneureas of the formula with R1=H or CH3, R2=CnH2n+1 with n=1-4 and x=0 or 1, from the corresponding alkyleneureas by reaction with monomeric or polymerized formaldehyde in the presence of formic acid. This entails feeding the mixture, obtained in the reaction, of N-alkyl-N′-methylalkyleneurea and formic acid to the upper region of a distillation column, distilling without further additions and removing essentially formic acid-free N-alkyl-N′-methylalkyleneurea in the lower region of the column.

Abstract: 3-Arylphenyl sulfide derivatives represented by general formula (I): 1

Abstract: Compound represented by the structural formula 1

Abstract: Novel uracil substituted phenyl sulfamoyl carboxamides I and salts thereof, where A=oxygen or sulfur; X1=H, halogen, C1-C4-alkyl; X2=H, CN, CS—NH2, halogen, C1-C4-alkyl, C1-C4-haloalkyl; X3=H, CN, C1-C6-alkyl, C1-C6-alkoxyalkyl, C3-C7-cycloalkyl, C3-C6-alkenyl, C3-C6-alkynyl, optionally substituted benzyl; R1, R2=H, halogen, optionally substituted hydroxy, C1-C10-alkyl, C2-C10-alkenyl, C3-C10-alkynyl, C3-C7-cycloalkyl, phenyl, benzyl or C5-C7-cycloalkenyl, or R1+R2 together with the atom to which they are attached form 3- to 7-membered heterocyclic ring; Q is selected from Q1 to Q40 as defined in the description. Use: As herbicides; for the desiccation/defoliation of plants.

Abstract: The present invention relates to novel dihydropyrones with tethered heterocycles having improved pharmacologic properties which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of the dihydropyrones and intermediates useful in the preparation of the final compounds.

Abstract: This invention encompasses the novel compounds of Formula I, which are useful in the treatment of caspase-3 mediated diseases. The invention also encompasses certain pharmaceutical compositions comprising compounds of Formula I as well as methods for treatment of caspase-3 mediated diseases.

Abstract: This invention describes novel pyrazole compounds of formula IIIa: 1

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 invention relates to carboxylic acid derivatives of formula (I), wherein the substituents have the meaning as commented in the description. It also relates to the production and use of same as endothelin receptor antagonists.

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 invention relates to heterocyclic derivatives, or pharmaceutically-acceptable salts thereof, which possess antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals. The, invention also relates to processes for the preparation of the heterocyclic derivatives, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect, formula (I).

Abstract: A compound selected from those of formula (I): wherein: R1 and R2 each independently represent hydrogen or, alkyl, T1 and T2 each independently represent alkylene, G represents a heterocyclic group selected of formula (&agr;):  wherein: W1 to W5 and X1 to X4 are so defined in the description. Medicinal products containing the same are useful as serotonin-reuptake inhibitors.

Abstract: The present invention relates to novel 1,4,5-substituted imidazole compounds and compositions for use in therapy as CSBP/p38 inhibitors.