Abstract: One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.

Abstract: Couplers for hair coloring compositions for oxidative dyeing of hair are compounds of the formula (1): 1

Abstract: This invention provides a compound of the formula (I): 1

Abstract: The present invention provides compositions and their use in the treatment of inflammatory diseases caused by T-cell proliferation such as sepsis, inflammatory bowel diseases, autoimmune encephalomyelitis, or lupus.

Abstract: The invention is directed to inhibition of p38-&agr; kinase using compounds of the formula 1

Abstract: Disclosed are novel piperazine derivatives, useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, and myocardial infarction.

Abstract: Disclosed herein is a method for reducing the rate of degradation of proteins in an animal, comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.

Abstract: Compounds having the formula 1

Abstract: This invention discloses amino acid derivatives which display inhibitory effects on the serine protease factor Xa. The invention also discloses pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable compositions comprising the compounds or their salts, methods for the preparation of the compounds, and methods of using them as therapeutic agents for treating or preventing disease states in mammals characterized by abnormal thrombosis.

Abstract: The present invention relates to a method for reacting amines of the general formula (I) 1

Abstract: Disclosed are guanidine and biguanidine derivatives which have anti-viral and anti-bacterial activity. Also disclosed are pharmaceutical compositions containing such compounds as an active ingredient, and anti-viral and anti-bacterial methods utilizing such compounds.

Abstract: Novel PDF inhibitors and novel methods for their use are provided.

Abstract: Nitrone derivatives are efficiently prepared by increasing reagent concentrations in reaction solutions. Aldehydes and amines may be condensed to prepare an imine intermediate. Elimination of the solution media generally renders the imine formation more efficient. The imine is then reacted with a peroxysulfate oxidizing agent in a solution having at least about 0.1M concentration of the imine. The oxaziridine is rearranged to produce the nitrone derivative in high yield and good purity.

Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.

Abstract: This invention relates to a method of treating disorders responsive to the blockade of sodium ion channels using novel aminoalkyl-substituted aryl compounds of Formula I: 1

Abstract: The present application describes modulators of MCP-1 of formula (I): 1

Abstract: The present invention relates to a compound represented by the following formula (I): 1

Abstract: The present invention discloses novel substituted aryl alkylamine compounds of Formula (I) or pharmaceutically acceptable salts thereof which have selective histamine-H3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such cyclic amines as well as methods of using them to treat obesity and other histamine H3 receptor-related diseases.

Abstract: This invention is directed to proteinase (protease) inhibitors, and more particularly to thiol sulfonamide inhibitors for matrix metalloproteinase 13(MMP-13), compositions of proteinase inhibitors, intermediates for the syntheses of proteinase inhibitors, processes for the preparation of proteinase inhibitors and processes for treating pathological conditions associated with pathological matrix metalloproteinase activity related to MMP-13.

Abstract: The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R1 is optionally substituted C1-6alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C1-6alkoxy, —NR2R3 or —NR4SO2R5; X is the linkage —(CH2)n— or —(CH2)q—O— (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by C1-4alkoxy; hydroxy; hydroxy(C1-3alkyl); C3-7cycloalkyl; carbocyclyl; heterocyclyl; or by C1-4alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6 or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two R8 groups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5- or 6-membered carbocyclic or heterocyclyic ring.

Abstract: An object of the present invention is to provide a modified cyclic aliphatic polyamine having a low viscosity and a small content of unreacted polyamine which can provide, when it is used as a curing agent for epoxy resin, an epoxy resin composition having an improved workability without adding solvent or diluent and an excellent property of epoxy resin cure product. The above modified cyclic aliphatic polyamine is obtained by addition reaction of a cyclic aliphatic polyamine such as isophoronediamine and norbornanediamine and an alkenyl compound such as styrene. The modified cyclic aliphatic polyamine thus obtained is added in epoxy resin to be used as a curing agent for epoxy resin.

Abstract: Compounds having an Rho kinase inhibitory activity. These compounds include the compound of general formula (I): Het-X-Z, pharmaceutically acceptable salts thereof and solvates of the same, wherein Het represents a monocyclic or dicyclic heterocycle group containing at least one nitrogen atom (for example, pyridyl, phthalimido); X represents (i) an —NH—C(═O)—NH-Q1- group, (ii) an —NH—C(═O)-Q2- group, etc. (wherein Q1 and Q2 represent each a bond, alkylene or alkenylene); and Z represents hydrogen, halogeno, a monocyclic, dicyclic ortricyclic carbon cycle or heterocycle, etc. (for example, optionally substituted phenyl).

Abstract: The invention provides an N,N-substituted cyclic amine compound represented by the following formula (VIII): wherein A represents an aryl group etc.; E represents a group represented by the formula —CO— or a group represented by the formula —CHOH—; G represents an oxygen atom etc.; J represents an aryl group which may be substituted; R1 represents a lower alkyl group etc.; Alk represents a linear or branched lower alkylene group; n, v, w, x and y are independent of each other and each represents 0 or 1; and p represents 2 or 3, or a pharmacologically acceptable salt thereof. The compound of the present invention or a salt thereof is effective to treat a disease against which calcium antagonism is effective.

Abstract: The present invention relates to biguanide derivatives of formula (I), wherein R1, R2, R3 and R4 have the meanings as given in claim (1). Compounds are useful in the treatment of pathologies associated with hyperglycaemia, such as diabetes.

Abstract: The present invention relates to a class of compounds represented by formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of Formula (I), and methods of selectively antagonizing the &agr;&ngr;&bgr;3 and/or the &agr;&ngr;&bgr;5 integrin without significantly antagonizing the IIb/IIIa integrin.

Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.

Abstract: The present application describes novel &bgr;-amino acid derivatives of formula I: 1

Abstract: Described are novel 1-phenylalkylpiperazines having affinity for serotonergic receptors. These compounds and their enantiomers, diastereoisomers, N-piperazine 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 activity. Also described are the preparation of the compounds and the pharmaceutical compositions containing them.

Abstract: Novel quaternary amine containing compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating conditions in mammals characterized by undesired thrombosis.

Abstract: Disclosed herein are novel morpholinoketone derivatives of formula (I): 1

Abstract: The present invention provides compounds of Formula (I): 1

Abstract: The present invention relates to alanine 2,6-dialkoxyphenyl ester derivatives having the general formula I, Formula (I) wherein R1 is (C1-3)alkyloxy, (C1-3)alkyloxy(C1-3)alkyl, (C1-3)alkylthio, (C1-3)alkylthio(C1-3)alkyl, (C1-3)alkylsulfinyl, (C1-3)alkylsulfinyl(C1-3)alkyl, (C1-3)alkylsulfonyl, (C1-3)alkylsulfonyl(C1-3)alkyl, (C1-3)alkyloxycarbonyl, (CH2)n—CO—NR8R9? or (CH2)n—NR8R9?; n is 0, 1 or 2; R2 is hydrogen or (C1-3?)alkyl; R3 is (C1-3)alkyl or (C1-3)alkyloxy(C1-3?)alkyl; R4 is (C1-3)alkyloxy(C1-3)alkyl; or R3 and R4 form together with the nitrogen atom to which they are bound a 5-, 6-, or 7-membered ring, optionally containing a further heteroatom selected from O and S, and which ring may optionally contain a double bond and be optionally substituted with (C1-3)alkyl or (C1-3)alkyloxy; R5 and R6 are independently (C1-3)alkyl; R7 is hydrogen, (C1-3)alkyl, (C1-3)alkyloxy or (C2-3)alkenyl; R8 and R9 are independently (C1-3)alkyl; or R8 and R9 form together with

Abstract: A compound of the formula 1

Abstract: The invention relates to new products of formula (I): 1

Abstract: The present invention relates to compounds that are useful exhibit activity as serotonin, norepinephrine and dopamine reuptake inhibitors, and their pharmaceutically acceptable salts, and their use in the treatment of central nervous system and other disorders.

Abstract: The present invention relates to a compound selected from those of formula (I): wherein: R1 represents alkyl, R2 represents hydroxy, alkoxy, or amino, n represents an integer from 1 to 12 inclusive, R3 represents: hydrogen, optionally substituted alkyl, cycloalkyl, pyrimidinyl or optionally substituted phenyl, its isomers, and addition salts thereof with a pharmaceutically acceptable acid or base, medicinal products containing the same are useful in the prevention or treatment of acute and chronic cell ischaemia.

Abstract: The invention relates to non-peptidic compounds that possess bioactive properties, such as the ability to protect neuronal cells from otherwise lethal treatments or the ability to promote the growth or regeneration of neuronal cells. In part, the invention provides compounds that interact with or bind to a cyclophilin and compounds that have activity towards neuronal cells. Methods for using the compounds, such as administering them to cells or animals or using them to treat neurodegenerative conditions, are specifically included.

Abstract: This invention relates to novel succinoylamino heterocycles having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A&bgr;-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to &bgr;-amyloid production such as Alzheimer's disease and Down's Syndrome.

Abstract: The present invention relates to the compounds of the formula (I) and salts thereof (all the symbols are the same meanings as described in the specification).

Abstract: This invention generally relates to new polyol ester derivatives of polyamines for use as dispersant additives compatible in synthetic ester-based turbo oils. The dispersant additives of the present invention consist of a hydrocarbon acid, a polyol, an amine carrier such as diacid or cyclic anhydride and a polyamine. The hydrocarbon acid makes up the non-polar hydrocarbon portion of the dispersant and the polyamine functions as the polar headgroup. The diacid or cyclic anhydride provides a means for attaching the polar polyamine to the dispersant structure through an amide linkage. Different dispersant structures are obtained by varying the hydrocarbon acid, the polyol and the nature of the polyamine.

Abstract: The invention relates to new &agr;-arylethylpiperazine derivatives, which are useful as neurokinin receptor antagonists (NK1antagonists). It also relates to processes for the preparation of said &agr;-arylethylpiperazine derivatives, to their use for the prevention and/or treatment of a condition associated with pathogical levels of substance P in a patient and to pharmaceutical compositions containing them.

Abstract: Compounds of the formula: 1

Abstract: The present invention relates to novel aromatic amines of general formula (I) and to the use of these amines for the treatment of obesity, anorexia, inflammation, mental disorders an other diseases associated with the melanocortin receptors or related systems, e.g. the melanocyte stimulating hormones.

Abstract: The invention relates to novel aminothiol ester compounds having the general formula (I): 1

Abstract: Novel compounds of the general formula: 1

Abstract: The invention relates to bifunctional tryptase inhibitors of formula (I) wherein H1 and H2 comprise a Q group and L is a linker of formula and the conformation of the H1, H2 and L groups is such that the groups are separated by a distance of from 20 to 45 Å. Pharmaceutical compositions and crystal forms of the compounds are described in addition to methods for producing and identifying such compounds, as well as the use of such compounds in methods of treating allergic and inflammatory diseases.

Abstract: The present invention relates to a compound selected from those of formula (I): 1

Abstract: This invention is directed to acyl piperazine derivatives which are useful as anti-inflammatory agents. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat inflammatory disorders in humans.

Abstract: Provided are processes for synthesizing structurally diverse pyruvate-derived compounds using a parallel approach on a solid phase support. Examples of such a solid phase support include resins which have also been used in solid phase peptide synthesis.

Abstract: The invention concerns novel compounds of the N-acylamino-amide family, compositions, in particular cosmetic or pharmaceutical, containing them, and their use for treating body or face skin ageing, whether chronobiologic or light-induced, and in particular skin ageing caused by decrease of skin elasticity and/or by collagen degradation in the structure of tissues.