Abstract: The invention relates to novel compounds derived from pentaerythrite compounds of formula (XII) and (XVI), which can be used as pharmaceutically active substances, specially in the treatment of cardiac and circulatory diseases.

Abstract: Picornaviral 3C protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of picornaviral 3C proteases. These compounds, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses. Several novel methods and intermediates can be used to prepare the novel picornaviral 3C protease inhibitors of the present invention.

Abstract: A granular detergent composition containing a secondary (2,3) alkyl sulfate surfactant and a bleach/bleach activator system which has improved cleaning performance is provided. The detergent composition comprises: (a) from about 1% to about 40% of a secondary (2,3) alkyl sulfate surfactant; (b) from about 0.005% to about 5% of an enzyme; (c) from about 0.5% to about 20% of a peroxygen bleaching agent; and (d) from about 0.5% to about 20% of a bleach activator. The peroxygen bleaching compound and the bleach activator are in a molar ratio from about 1:1 to about 9:1. The detergent composition is stable, exhibits superior cleaning and contains a more biodegradable surfactant.

Abstract: The present invention provides a novel compound represented by the general formula I; wherein R is H or COR3; R1 is H, R2, phenyl, or COR3, wherein R2 is C1-C5 lower alkyl and R3 is R2 or phenyl; Z is CH2 or O; Y is OH, OCOR3 or ═O; x is 0 or 1; and X is C1-C5 n-alkyl, C3-C7 cycloalkyl, phenyl, furanyl, thienyl or substituted derivatives thereof, wherein the substituents maybe selected from the group consisting of C1-C5 alkyl, halogen, CF3, CN, NO2, NR42, CO2R4 and OR4 wherein R4 is hydrogen or C1-C5 alkyl and dotted lines represent the presence or absence of a double bond and wavy lines represent a cis or trans bond. These novel compounds are especially useful for treating elevated intraocular pressure (ocular hypertension) and glaucoma.

Abstract: Disclosed are novel metal pterin and pterin analog complexes and compositions useful as antineoplastic and antiviral agents.

Abstract: Epothilones with a modified side chain and process for the preparation thereof are disclosed.

Abstract: The present invention relates to carboxylic acid derivatives of the formula I the substituents having the meanings explained in the description, preparation and use as endothelin receptor antagonists.

Abstract: Novel compounds and pharmaceutical compositions useful as EGFR tyrosine kinase inhibitors. Methods of the invention include administration of the EGFR TK inhibitors to treat diseases characterized by enhanced expression of EGF, including cancers, particularly breast cancer. Additionally, a homology model representing the structure of EGFR kinase domain is provided, which model is useful for the rationally design and screening of compounds predicted to bind favorably to EGFR and to inhibit EGFR TK.

Abstract: This invention provides a substituted isoxazolylthiophene compound represented by the formula wherein R1 and R2 individually represent an alkyl group of 1-5 carbon atoms, R3 represents a cyano group or a group CONR5R6 (in which R5 and R6 individually represent a hydrogen atom or an alkyl group of 1-10 carbon atoms), R4 represents an alkyl group of 1-5 carbon atoms or a phenyl group, and n is an integer of 0-2, or a salt thereof. The compounds of the invention are useful for the treatment or prevention of various bone diseases or nerve diseases, because they specifically enhance the action of the cell differentiation induction factors found in a living body.

Abstract: The present invention comprises small molecular weight, non-peptidic inhibitors of formula I and II of Protein Tyrosine Phosphatase 1 (PTP1) which are useful for the treatment and/or prevention of Non-Insulin Dependent Diabetes Mellitus (NIDDM).

Abstract: This invention provides new thiazolindinedione derivatives and new arylacetic acid derivatives. These compounds are useful for the treatment of cardiovascular diseases, certain endocrine diseases, certain inflammatory diseases, certain neoplastic (malignant) and non-malignant proliferative diseases, certain neuro-psychiatric disorders, certain viral diseases, and diseases associated with these viral infections as discussed herein.

Abstract: This invention provides compounds and their pharmaceutically-acceptable salts, pharmaceutical formulations of said compounds, and methods for treating hyperglycemia associated with non-insulin dependent diabetes and for treating hyperlipidemia.

Abstract: Biologically active sultams are disclosed which have potent anti-HIV activity. A combinational method of synthesis, which uses a solid support and variants thereof, are described. Biological compositions and method of treating mammals for viral infections with compositions comprising the sultams of the invention, especially HIV are described.

Abstract: The present invention relates to novel 2-aminocarbonyl-5(2H)-isoxazolones as selective ligands of a high-affinity binding site of diisopropyl fluorophosphate (DFP) on brain membranes for the prophylaxis and treatment of disorders of the central nervous system, in particular cognitive disorders, depression, schizophrenia and anxiety.

Abstract: 1,3-diazolino and 1,3-diazolidino heterocycle derivatives useful as nitric oxide synthase inhibitors.

Abstract: Methods of synthesizing 9-Halo-13,14-dihydroprostaglandins useful in the treatment of glaucoma and ocular hypertension are disclosed. Also disclosed are ophthalmic, pharmaceutical compositions comprising such prostaglandins.

Abstract: The present invention relates to novel tyrosine alkoxyguanidine compounds that are inhibitors of alpha V (&agr;v) integrins, for example &agr;v&bgr;3 and &agr;v&bgr;5 integrins, their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. The compounds may be used in the treatment of pathological conditions mediated by &agr;v&bgr;3 and &agr;v&bgr;5 integrins, including conditions such as tumor growth, metastasis, restenosis, osteoporosis, inflammation, macular degeneration, diabetic retinopathy, and rheumatoid arthritis. The compounds have the general formula: where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, m and n are defined herein.

Abstract: The subject of the invention is the compounds of formula: in which R1, R2, R3, R4, R5 and R6 are as defined in Claim 1. The compounds have a high affinity for CRF receptors.

Abstract: A process for the purification of a compound of general formula I: wherein: R1 is hydrogen or C1-C6 alkyl, C2-C6 alkenyl or C2-C6 alkynyl (any of which may optionally be substituted with one or more substituents selected from halogen and OH) or COOR4, COR6, CONR4R5 or CONHSO2R4; R4 and R5 are each independently hydrogen or C1-C4 alkyl optionally substituted with one or more halogen atoms; R6 is a halogen atom or a group R4; R2 is hydrogen or halo; R3 is C1-C4 alkyl, C2-C4 alkenyl or C2-C4 alkynyl, any of which may optionally be substituted with one or more halogen atoms, or halo; or, where appropriate, a salt thereof; from a mixture containing the compound of general formula I together with one or more isomers or di-nitrated analogues thereof; the process comprising dissolving the mixture in a suitable crystallisation solvent and recrystallising the product from the resulting crystallisation solution; characterised in that the crystallisation solution contains not more than 25% loadin

Abstract: A superoxide radical inhibitor containing, as an effective ingredient, an azole derivative represented by the general formula (1), [wherein R1 represents a phenyl group which may have 1-3 lower alkoxy groups as substituent(s) on the phenyl ring, a phenyl group having a lower alkylenedioxy group, or the like; R2 represents a hydrogen atom, a phenyl group, a halogen atom, a lower alkoxycarbonyl group, a lower alkyl group, an amino-lower alkyl group which may have a lower alkyl group as a substituent, a dihydrocarbostyril group, or the like; R3 represents a group of the formula, (R4B represents a hydroxyl group, a carboxy group, a lower alkenyl group or a lower alkyl group, m represents 0, 1 or 2); X represents a sulfur atom or an oxygen atom] or a salt thereof.