Abstract: The present invention relates to a novel retinoid derivative compound represented by the formula I: 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: A process for preparing amide alkoxylates. More specifically, the invention provides a butoxylation process for producing poly(oxyalkylene) amides and poly(oxyalkylene) esters via an exchange reaction of (trans-amidation/trans-esterification) and involving removal of the poly(oxyalkylene) esters in the product mixtures so that a better performance products can be obtained. The invention further relates to the use of these compounds as fuel additives to decrease intake valve deposits, positively affecting the engine's octane requirement, control the increase of combustion chamber deposits and improve fuel quality. The invention further discloses a composition used as engine fuel, characterized in that it contains said poly(oxyalkylene)amide as the fuel additive.

Abstract: The invention relates to a highly active, highly specific urokinase inhibitor which is suitable for therapeutic applications and can be synthesized in an extremely simple manner. Surprisingly, it was found that amidino benzylamine derivatives, especially 4-amidino-benzylamine, with two bonded amino acids represent a new group of highly active and very selective uPA inhibitors. The urokinase inhibitors can be used in medical applications, e.g. in the treatment of malign tumors such as in cases of metastatic spread.

Abstract: The present invention relates to compounds of formula (I): 1

Abstract: The present invention is to provide manufacturing intermediates which can be led to useful &agr;-ketoamide compounds having protease-inhibiting activity extremely economically and stereoselectively, and to provide epoxycarboxamide compounds, azide compounds and amino alcohol compounds represented by the following formulae: 1

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.

Abstract: The present invention relates to small molecules according to the formula [I]: 1

Abstract: A compound selected from the group consisting of a compound of formula I 1

Abstract: A class of compounds is described which can be used for the treatment of viral infections.

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

Abstract: Compounds having the formula (I), 1

Abstract: Compounds of Formula I are antagonists of VLA-4 and/or &agr;4&bgr;7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.

Abstract: The present invention related to an oligocycloalkanoid compound comprising formula (I) wherein m, n, and o are independently an integer from 0 to 2; A1 through A10 are independently a direct link, alkylene, alkylene-O—, carbonyl, oxygen, or sulfur; X and Y are independently hydrogen, hydroxy, alkyl, or in combination an electrophilic group; and R1 through R10 are independently hydrogen, hydroxy, alkyl, alkenyl, alkynyl, substituted or unsubstituted aryl, N-, S-, or O-heterocycles, fused or multi-ring aryl with or without hetero ring members, arylalkyl, arylalkenyl, arylalkynyl, alkylphenyl, alkenylphenyl, alkynylphenyl, alkoxy, alkenyloxy, alkynyloxy, substituted or unsubstituted aryloxy, substituted or unsubstituted arylalkoxy, alkylacyl, alkenylacyl, alkynylacyl, arylacyl, aroyl, alkylaroyl, aminoaroyl, aminoalkylacyl, aminoalkyl, aminoalkenyl, aminoalkynyl, amino, alkylamino, alkenylamino, alkynylamino, arylamino, dialkylamino, dialkenylamino, dialkynylamino, arylalkylamino, arylalk

Abstract: A compound represented by the following general formula (I): 1

Abstract: A novel tandem acyl-Claisen rearrangement reaction is provided. An allylic reactant such as an allylic amine or an allylic thioether, having at least two functional groups that enable the reactant to undergo at least two successive Claisen rearrangement reactions, is reacted with an acid chloride in the presence of a Lewis acid catalyst composition composed of a Lewis acid and a second catalyst component selected from the group consisting of tertiary amines and non-nitrogenous bases. The stereochemistry of the reaction product is readily controlled by the positioning and size of substituents on the allylic reactant. The reaction may be carried out on a solid support, i.e., on the surface of a substrate suitable for conducting solid phase chemical reactions.

Abstract: Compounds of formula (I), in which M, A1, A2, K1 and K2 have the meanings as indicated in the description are novel active tryptase inhibitors.

Abstract: This invention features permeability enhancer molecules, and methods, to increase membrane permeability of various molecules, such as nucleic acids, polynucleotides, oligonucleotides, enzymatic nucleic acid molecules, antisense nucleic acid molecules, 2-5A antisense chimeras, triplex forming oligonucleotides, decoy RNAs, dsRNAs, siRNAs, aptamers, or antisense nucleic acids containing nucleic acid cleaving chemical groups, peptides, polypeptides, proteins, carbohydrates, steroids, metals and small molecules, thereby facilitating cellular uptake of such molecules.

Abstract: Disclosed are biological reagents which comprise compounds that inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in determining the cellular mechanism involved in the generation of &bgr;-amyloid peptide.

Abstract: 4,4-Diarylbutadienes of the formula I, where the diene system has the Z,Z; Z,E; E,Z or E,E configuration or a mixture thereof, and where the variables independently of one another have the following meanings: R1 and R2 are hydrogen, C1-C20-alkyl, C2-C10-alkenyl, C3-C10-cycloalkyl, C3-C10-cycloalkenyl, C1-C12-alkoxy, C1-C20-alkoxycarbonyl, C1-C12-alkylamino, C1-C12-dialkylamino, aryl, hetaryl, unsubstituted or substituted, substituents which confer solubility in water and are selected from the group consisting of carboxylate, sulfonate, or ammonium residues; R3 is COOR5, CONR5R6; R4 is COOR6, CONR5R6; R5 and R6 are hydrogen, C1-C20-alkyl, C2-C10-alkenyl, C3-C10-cycloalkyl, C7-C10-bicycloalkyl, C3-C10-cycloalkenyl, C7-C10-bicycloalkenyl, aryl, hetaryl, unsubstituted or substituted; n is 1 to 3; and R3 and R4 are not COOCH3 when R1 and R2 are hydrogen, are used as photostable UV filters in cosmetic and pharmaceutical preparations to protect the human skin or human hair from the sun's rays,

Abstract: A paving composition is disclosed comprising a bituminous material, such as asphalt, and a reaction product of at least one polycarboxylic acid reacted with at least one polyamine. The composition preferably is substantially free of water. The reaction product can be a diamide compound. The paving composition can further include mineral aggregate. The paving composition can be used in applications such as road construction or repair.

Abstract: Para-alkyl, aryl, cycloheteroalkyl or heteroaryl [carbonyl or sulfonyl] amino substituted phenyl amides active as glucokinase activators to increase insulin secretion which makes them useful for treating type II diabetes.

Abstract: Disclosed are novel multibinding compounds (agents) which bind macromolecular structures including cellular, extracellular, and microbial components derived from vectors, viruses, fungi, yeasts, bacteria, and the like. The compounds of this invention comprise a plurality of ligands each of which can bind to such macromolecular structures thereby modulating the biological processes/functions thereof. Each of the ligands is covalently attached to a linker (framework) to provide for the multibinding compound. The linker is selected such that the multibinding compound so constructed demonstrates increased modulation or disruption of the biological processes/functions of cell as compared to the aggregate of the individual units of the ligand.

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

Abstract: Compounds of peptide mimetic nature having the general formula I formula I 1

Abstract: Derivatives of N-deacetyl-thiocolchicine or of the isoster thereof of formula (I) 1

Abstract: The present invention relates to acylated indanyl amines according to the general formula (I) 1

Abstract: Novel perfluoroalkyl-substituted mono-, di- and poly-amide compounds which are reaction products of a mono-, di- or polyamine of 60 to 2000 molecular weight with a perfluoroalkyl substituted unsaturated acid or its corresponding lower alkyl ester and optionally a non-fluorinated amino-reactive compound such as an acid, ester, anhydride, epichlorohydrin, isocyanate or urea, are useful as internally or externally applied paper sizes to impart oil and grease resistance to paper, and as oil proofing coatings on textiles, wood, masonry and the like, or as high-performance surface active agents.

Abstract: A method of N-alkoxyalkylating ureides according to the invention comprises reacting a ureide of structure I 1

Abstract: Compounds of the formula: are provided, and are useful as cysteine protease inhibitors, particularly in the treatment of diseases such as osteoporosis or autoimmune disorders in which cathepsins K or S contribute to the pathology or symptomatolgy of the disease.

Abstract: The present invention relates to a series of peptidyl heterocyclic ketones which are inflammatory cell serine protease inhibitors and their compositions and methods for the prevention and treatment of a variety of immunomediated inflammatory disorders. More particularly, these compounds are potent and selective inhibitors of tryptase and are therefore effective for the prevention and treatment of inflammatory diseases associated with the respiratory tract, such as asthma and allergic rhinitis.

Abstract: The present invention relates to compounds according to the general formula (I), 1

Abstract: The invention provides a composition containing particulate composite of a polymer and a therapeutic agent. The composition also contains a complexing agent. The polymer interacts with the complexing agent in a host-guest or a guest-host interaction to form an inclusion complex. A therapeutic composition of the invention may be used to deliver the therapeutic agent and to treat various disorders. Both the polymer of the particulate composite and the complexing agent may be used to introduce functionality into the therapeutic composition. The invention also relates to a method of preparing a composition. The method combines a therapeutic agent, a polymer having host or guest functionality, and a complexing agent having guest or host functionality to form the therapeutic composition. The complexing agent forms an inclusion complex with the polymer. The invention also relates to a method of delivering a therapeutic agent.

Abstract: The present invention relates to substituted phenylcyclohexanecarboxamides of the formula (I) 1

Abstract: The present invention provides methods for the asymmetric synthesis of (S,S,R)-(−)-actinonin and its analogs and the compounds thereby synthesized having a structural formula: 1

Abstract: Compositions for lithographic or flexographic inks are disclosed comprising at least one compound of Formula 1: 1

Abstract: This invention relates to a novel class of peptides having the Formula (I): 1

Abstract: PPAR alpha activators, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases, in mammals, including humans.

Abstract: Compounds of formula (I) 1

Abstract: The present invention relates to novel, non-peptidic small organic compounds having an affinity for cyclophilin (CyP)-type immunophilin proteins, and to pharmaceutical compositions comprising one or more of the said compounds. The invention further relates to the uses of these compounds and compositions for binding CyP-type proteins, inhibiting their peptidyl-prolyl isomerase activity, and for research, development, and therapeutic applications in a variety of medical disorders.

Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis.

Abstract: The present invention discloses biscyclopropanecarboxamide compounds and pharmaceutically acceptable salts thereof; and also NF-kappa B activation inhibitors, Inflammatory cytokine production inhibitors, matrix metalloprotease production inhibitors, inflammatory cell adhesion molecules incidence inhibitors, antiinflammatory agents, antirheumatic agents, immunosuppressive agents, cancerous metastasis inhibitors or antiviral agents each containing such a compound as the active ingredient.

Abstract: Terminally-branched polymeric prodrug platforms capable of high degrees of loading are disclosed. In preferred aspects of the invention, the prodrug platform releases multiple parent compounds after each branch holding the active agent undergoes a benzyl elimination reaction. Methods of preparing the prodrugs and using the same in the treatment of mammals are also disclosed.

Abstract: The present invention discloses novel peptide compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Abstract: The object of the present invention is an industrial process for the purification and removal of residual solvents from iohexol, based on the suspension of crystalline iohexol, eventually containing residual solvents above 100 ppm, in a fluid wherein it has a low solubility, followed by heating, filtration and drying. The process allows the formation of crystalline iohexol with no residual organic residual solvent above 100 ppm and with an increased purity level.

Abstract: Compounds with antithrombotic activity and factor Xa-inhibiting activity of the general formula: 1

Abstract: Compounds of formula (I) 1

Abstract: The present invention provides a series of compounds having structural formulas 1

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

Abstract: Amidomethyl esters, carbonylmercaptomethyl esters, keto-containing esters, amidomethyl thioesters, amidomethyl amides, and methylene dithioesters are disclosed. The novel compounds have two carbonyl groups connected by a linking moiety having an oxygen, sulfur or nitrogen attached to a methylene group, to which is further attached a sulfur, nitrogen or CH2 group. Methods of treating illnesses and conditions, such as cancer, hemological disorders, inherited metabolic disorders and others, using these compounds are also disclosed.