Abstract: Hydrates of N-[1-butyl-4-[3-[3-(hydroxy)propoxy]-phenyl]-1,2-dihydro-2-oxo-1,8-naphthyridin-3-yl]-N′-(2,6-diisopropyl-4-aminophenyl)urea hydrochloride of the formula: 1

Abstract: Substituted quinazolin-4-ylamine analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

Abstract: Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are also disclosed.

Abstract: Indole derivatives represented by formula (I): (wherein all symbols are described in the description), a process for the preparation of the same and a DP receptor antagonist comprising it as an active ingredient. Since the compounds of formula (I) binds to and are antagonistic to a DP receptor, they are useful in for the prevention and/or treatment of diseases, for example, allergic diseases (allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma, food allergy, etc., systemic mastocytosis; disorders due to systemic mastocyte activation, anaphylactic shock, bronchoconstriction, urticaria, eczema, etc.), diseases accompanied with itching (atopic dermatitis, urticaria, etc.), secondary diseases caused by behaviors (scratching behaviors, beating, etc.) (cataract, retinal detachment, inflammation, infection, sleep disorder, etc.

Abstract: Medicines for the prevention and treatment of neurodegenerative diseases such as Alzheimer's disease and schizophrenia of mammals (including human beings) through the retardation or inhibition of neurodegeneration due to hypofunction of glutamic acid receptor and which contain as an active ingredient 5-substituted-3-oxadiazolyl-1,6-naphthyridin-2(1H)-one derivatives of the formula (I): wherein Het is oxadiazolyl; R1 is hydrogen, lower alkyl, cyclo-lower alkyl, lower alkenyl, lower alkoxy, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, etc.; and R2 is hydrogen, lower alkyl, cyclo-lower alkyl, substituted or unsubstituted aryl, etc., or physiologically acceptable acid addition salts thereof.

Abstract: 2-Oxo-1,2-dihydro-1,8-naphthyridine derivatives characterized by bearing a specific substituent, —X—R6, at the 3-position and a cyclic substituent, R5, at the 4-position; or salts thereof. The derivatives and the salts are useful as drugs, particularly preventive or therapeutic agents for respiratory diseases related to PDE IV.

Abstract: Mono-flourinated and di-fluorinated benzothiepine apical sodium co-dependent bile acid transport (ASBT) inhibitors are disclosed together with methods of making the same, methods of using the same to treat hyperlipidemic conditions as well as pharmaceutical compositions containing the same compounds.

Abstract: The present invention relates to a compound of Formula (I), which are useful for inhibiting resistant neoplasms where the resistance is conferred in part or in total by MRP1.

Abstract: The present invention relates to a class of compounds represented by the Formula I 1

Abstract: Therapeutically active thiazole derivatives of formula (I) wherein R1, R2, X and X′ are as defined in the specification, processes for the preparation thereof, the use thereof in therapy, particularly in the treatment or prophylaxis of disorders characterized by overexpression of transforming growth factor &bgr;(TAG-&bgr;), and pharmaceutical compositions for use in such therapy.

Abstract: The invention relates to novel compounds which bind to integrin receptors, their use as ligands of integrin receptors, in particular as ligands of the &agr;v&bgr;3 integrin receptor, their use, and pharmaceutical preparations comprising these compounds.

Abstract: Therapeutically active pyrazole derivatives of formula (I) wherein R1-R3 are as defined in the specification, processes for the preparation thereof, the use thereof in therapy, particularly in the treatment or prophylaxis of disorders characterised by overexpression of transforming growth factor (TGF-), and pharmaceutical compositions for use in such therapy.

Abstract: Pleuromutilin compounds of the formula: 1

Abstract: Aminopiperidine derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man.

Abstract: The present invention relates to novel compounds and the treatment of mammalian diseases in which inappropriate, excessive or undesirable angiogenesis has occurred and/or where excessive Tie2 receptor activity has occurred.

Abstract: Disclosed are compounds of the formula 1

Abstract: This invention provides compounds defined by Formula I 1

Abstract: The present invention relates to a method of producing an optically active pyridineethanol derivative. More particularly, it relates to a method of producing an optically active polycyclic pyridineethanol derivative by causing an enzyme or enzyme source to act on polycyclic acetylpyridine derivatives.

Abstract: This invention provides compounds defined by Formula I 1

Abstract: This invention provides compounds defined by Formula I 1

Abstract: This invention provides compounds defined by Formula I 1

Abstract: The present invention provides compounds of the Formula I: 1

Abstract: The present invention relates to novel chain-fluorinated alkanoic acid derivatives thereof, their synthesis, and their use as &agr;v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3 and/or &agr;v&bgr;5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, inflammatory arthritis, viral disease, cancer, and metastatic tumor growth.

Abstract: This invention provides compounds defined by Formula I 1

Abstract: Certain compounds which contain a piperidine moiety flanked by aryl groups are inhibitors of p38-&agr; kinase and thus useful in the treatment of a variety of conditions characterized by inappropriate p38-&agr; kinase activity.

Abstract: The present invention relates to novel alkanoic acid derivatives thereof, their synthesis, and their use as &agr;v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3 and/or &agr;v&bgr;5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth.

Abstract: This invention provides compounds of Formula (I), having the structure where T, Z, X, A, R1, R2a, R2b, R2c, R3, R4, and n are defined herein, or a pharmaceutically acceptable salt thereof which are useful as antineoplastic agents and in the treatment of osteoporosis and polycystic kidney disease.

Abstract: The invention relates generally to naphthyridine derivatives of the formula 1

Abstract: The invention relates generally to naphthyridine derivatives of the formula wherein one of U, X, Y and Z is nitrogen and the others are C—R, where R is hydrogen or a substituent. More specifically, the invention relates to 1,6-naphthyridine derivatives and pharmaceutical compositions containing such derivatives. Methods of the invention comprise administration of a naphthyridine derivative of the invention for the treatment of diabetes and related disorders.

Abstract: The present invention provides a compound of a formula (I): 1

Abstract: The present invention relates to a blue light-emitting compound for organic polymer EL devices and organic EL devices having superior color purity and light-emitting efficiency by providing a blue light-emitting compound for organic EL devices represented by Chemical Formula 1 and an organic EL device using the blue light-emitting compound: 1

Abstract: Compounds of the formula I 1

Abstract: Disclosed are compounds of formula (I): 1

Abstract: A cyclic compound of the formula (I) or a pharmacologically acceptable salt thereof, 1

Abstract: Compounds of formula (I): 1

Abstract: Enamine derivatives of formula (1) are described: 1

Abstract: Compounds of the formula (I), or a pharmaceutically acceptable salt, or an in-vivo-hydrolysable ester thereof, 1

Abstract: Piperidine derivatives of formula (I) or a pharmaceutically acceptable derivative thereof and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man.

Abstract: The present invention provides a compound represented by the formula (I) 1

Abstract: The present invention relates to methods for making racemic 2-(7-chloro-1,8-naphthyridin-2-yl)-3-(5-methyl-2-oxohexyl)-1-isoindolinone and (+)-2-(7-chloro-1,8-naphthyridine-2-yl)-3-(5-methyl-2-oxo-hexyl)-1-isoindolinone.

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

Abstract: This invention concerns amide derivatives of Formula (I) wherein X is CH or N; Y is CH or N; m is 0-3; R1 is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino, carboxy and carbamoyl; n is 0-3; R2 is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino, carboxy and (1-6C)alkoxycarbonyl; R3 is hydrogen, halogeno, (1-6C)alkyl or (1-6C)alkoxy; q is 0-4; and Q is a group such as aryl, aryloxy, aryl-(1-6C)alkoxy, arylamino, N-(1-6C)alkyl-arylamino and aryl-(1-6C)alkylamino; or pharmaceutically-acceptable salts or in-vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.

Abstract: Described are novel N-acylated heterocycle derivatives having affinity for serotonergic receptors. These compounds and their enantiomers, diastercoisomers, N-oxides, polymorphs, solvates and pharmaceutically acceptable salts are useful in the treatment of patients with neuromuscular dysfunction of the lower urinary tract and diseases related to 5-HT1A receptor.

Abstract: Pyridoarylphenyl oxazolidinone compounds of the formula: 1

Abstract: The present invention provides compounds of the Formula I and II: 1

Abstract: Medicines for the prevention and treatment of neurodegenerative diseases such as Alzheimer's disease and schizophrenia of mammals (including human beings) through the retardation or inhibition of neurodegeneration due to hypofunction of glutamic acid receptor and which contain as an active ingredient 5-substituted-3-oxadiazolyl-1,6-naphthyridin-2(1H)-one derivatives of the formula (I): 1

Abstract: Squaric acid Derivatives of formula (1) are described: 1

Abstract: Novel compounds of formula (I) to (VI), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis.

Abstract: Enamine derivatives of formula (1) are described: wherein R1 is a group Ar1 L2Ar2Alk- in which Ar1 is an aromatic or heteroaromatic group, L2 is a covalent bond or a linker atom or group, Ar2 is an arylene or heteroarylene group and Alk is a chain —CH2—CH(R)—, —CH═C(R)— or in which R is a carboxylic acid or a derivative or biostere thereof; R2 is a hydrogen atom or a C1-6alkyl group; Cy is a cycloaliphatic or heterocycloaliphatic ring in which X is a N atom or a C(Rw) group; Rx is a oxo, thioxo, or imino group; Rw and Rz is each a hydrogen atom or optional substituent; provided that Cy is not a cyclobutenedione group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders, or disorders involving the inappropriate growth or migration of cells.

Abstract: Compounds of the invention are useful in inhibiting thrombin and treating blood coagulation and cardiovascular disorders and have the following structure: wherein R3 is hydrogen or halogen, and u is N or CH.