Abstract: The invention relates to compounds of general formula I as well as the production and use thereof as a medication.

Abstract: The invention relates to a group of novel indole compounds of Formula (I): wherein: R1, R2, R4, R6, R6a, R7, R8, R9, R10, and A are as defined in the specification, which are useful as gonadotrophin releasing hormone antagonists. The invention also relates to pharmaceutical formulations of said compounds, methods of treatment using said compounds and to processes for the preparation of said compounds.

Abstract: This invention is directed to inhibitors of copper-containing amine oxidases (E.C.1.4.3.6) including semicarbazide-sensitive amine oxidase (SSAO; also known as vascular adhesion protein-1, VAP-I), and their therapeutic use in inflammatory diseases, diabetes and its associated complications, atherosclerosis, neurodegenerative diseases, obesity, hypertension and cancer.

Abstract: The present invention relates to carboxylic acid derivatives that are inhibitors of histone deacetylase (HDAC). The compounds of the present invention are useful for treating cellular proliferative diseases, including cancer. Further, the compounds of the present invention are useful for treating neurodegenerative diseases, schizophrenia and stroke among other diseases.

Abstract: The invention relates to a process for the manufacture of a compound of formula or a salt, especially a pharmaceutically acceptable salt with a base, thereof or a lactone thereof wherein the element represents —CH2—CH2— or —CH?CH— and R represents a cyclic residue.

Abstract: By simultaneously carrying out an isomerization reaction at position 2 of monatin in different configurations at positions 2 and 4 in the presence of an aldehyde under a condition of pH 4 to 11 in a mixture solvent of water and an organic solvent, and the crystallization of monatin in the same configurations at positions 2 and 4 or a salt thereof, monatin useful as a sweetener, particularly optically active monatin can efficiently be produced.

Abstract: The present invention relates to processes of producing glutamic acid compounds, for example, monatin, which are useful as, for example, production intermediates for sweetener or pharmaceutical products.

Abstract: The invention provides compounds, pharmaceutical compositions, and methods for the treatment of thromboembolic disorders, such as, for example, arterial cardiovascular thromboembolic disorders, venous cardiovascular thromboembolic disorders, or thromboembolic disorders in the chambers of the heart.

Abstract: The invention provides compounds of formula (I) wherein m, n, A, R, R?, R?, R0, X and Y are as defined in the description, and their preparation. The compounds of formula (I) are useful as pharmaceuticals in the treatment of e.g.

Abstract: The present invention relates to hydroxamate compounds which are inhibitors of histone deacetylase. More particularly, the present invention relates to acylurea/sulfonylurea containing compounds and methods for their preparation. These compounds may be useful as medicaments for the treatment of proliferative disorders as well as other diseases involving, relating to or associated with enzymes having histone deacetylase activities.

Abstract: Disclosed are substituted indolealkanoic acids useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds and methods of treatment employing the compounds, as well as methods for their synthesis.

Abstract: The invention relates to compounds of formula I which are useful for elevating the plasma level of growth hormone in a mammal as well as for the treatment of growth hormone secretion deficiency, growth retardation in child and metabolic disorders associated with growth hormone secretion deficiency.

Abstract: The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.

Abstract: Substituted cyclohexylcarboxylic acid amide compounds, processes for their production, pharmaceutical compositions containing these compounds and the use of substituted cyclohexylcarboxylic acid compounds for producing pharmaceutical compositions for treating conditions or disease states associated with the opioid receptor system and/or with noradrenalin and/or serotonin re-uptake.

Abstract: Tuberculosis in an animal is treated by administration of a therapeutically effective amount of an immunomodulator of formula A. In formula (A), n is 1 or 2, R is hydrogen, acyl, alkyl or a peptide fragment, and X is an aromatic or heterocyclic amino acid or a derivative.

Abstract: The present invention provides compounds of Formula (I): or a stereoisomer or pharmaceutically acceptable salt or hydrate form thereof, wherein the variables A, B, L1, L2, X1, X2, X3, X4 and W are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

Abstract: The present invention relates to novel indole derivatives, to their preparation and to their use, as inhibitors of the enzyme poly(ADP-ribose)polymerase or PARP (EC 2.4.2.30), for producing drugs.

Abstract: The present invention provides hydroxamate compounds which are deacetylase inhibitors. The compounds are suitable for pharmaceutical compositions having anti-proliferative properties.

Abstract: The present invention relates to processes of producing glutamic acid compounds, for example, monatin, which are useful as, for example, production intermediates for sweetener or pharmaceutical products.

Abstract: The present invention relates to compounds, process for their synthesis, compositions and methods for the treatment and prevention of hepatitis C virus (HCV) infection. In particular, the present invention provides novel compounds, pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment or prevention of HCV infection. The present invention also provides processes and intermediates for the synthesis of these compounds.

Abstract: N-heterocyclic moiety containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: Novel compounds are disclosed which inhibit the activity of phospholipase enzymes in a mammal, particularly cytosolic phospholipase A2. Pharmaceutical compositions comprising such compounds and methods of treatment using such compositions are also disclosed.

Abstract: Compounds having a metalloproteinase inhibitory activity, represented by the formula (I), its optically active isomers, their pharmaceutically acceptable salts, or hydrates thereof.

Abstract: A composition for treating or preventing glomerulopathy which contains a compound of the formula (I): wherein, for example, R1 and R2 are each independently hydrogen atom, optionally substituted lower alkyl, optionally substituted aralkyl, etc.; R3 is 1,4-phenylene and 2,5-thiophendiyl; R4 is the substituents represented by the formula, etc.: wherein R5 is hydrogen atom, optionally substituted amino, etc.; and Y is NHOH or OH, its optically active substance, their pharmaceutically acceptable salt, or hydrate thereof.

Abstract: The invention relates to 1-(R1)-2-(R2)-3-(Y-X—NH-A- or Z-A-)-4,5,6,7-R)0.4-indoles, and their acid addition salts where the compounds are basic, wherein A is C1-4 alkylene, X is >CH2, >C?O or >C?S, and the other symbols have various defined values, and to pharmaceutical, skin-protective and cosmetic compositions which comprise them.

Abstract: The present invention relates to a synthetic process for the preparation of a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor.

Abstract: Described herein are compounds of formula (I) useful as antagonists of tachykinins in general, and in particular of neurokinin A; and the pharmaceutical formulations comprising the compounds of formula (I) 1

Abstract: This invention relates to compounds which have generally 5-HT6 receptor affinity and which are represented by Formula I: 1

Abstract: Novel compounds of formula wherein the substituents are defined as in the specification and are useful for inhibiting neuronal NO synthase or inducible NO synthase as well as inhibiting lipidic peroxidation.

Abstract: The invention relates to compounds of formula I 1

Abstract: The present invention pertains to specific peptides obtainable from cocoa beans and giving rise to a particular and distinct savor when subjected to a Maillard reaction with reducing sugars. In particular, the present invention pertains to the use of one or more of these specific peptides for the preparation of a chocolate flavor, specifically a cocoa and a caramel flavor, a floral or specifically, a bonbon flavor, a bready flavor, a roasted flavor or a meat flavor.

Abstract: A method for assessing levels of soluble A-beta as an indicator of Alzheimer's disease, and other amyloid-related diseases, in vitro, ex vivo, in vivo, and in situ which employs an imaging agent binds specifically to soluble A-beta and is labeled for detection.

Abstract: The invention provides a novel amino acid, neo-tryptophan, as well as polypeptides containing this novel amino acid such as neurotensin analogs. In addition, the invention provides neo-tryptophan derivatives, serotonin-like neo-tryptophan derivatives, and polypeptides containing such derivatives. The invention also provides methods for making neo-tryptophan, neo-tryptophan derivatives, serotonin-like neo-tryptophan derivatives, and compositions containing these compounds. Further, the invention provides methods for inducing a neurotensin response in a mammal as well as methods for treating a mammal having a serotonin recognition molecule.

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

Abstract: The present invention provides a method of reducing intraocular pressure by administering pharmaceutical compositions comprising indole derivatives. The pharmaceutical compositions useful in this invention comprise indole derivatives and melatonin analogs of Formulae I-IV. A preferred embodiment is a method of lowering intraocular pressure using 5-(methoxycarbonylamino)-N-acetyltryptamine (5-MCA-NAT), also known as GR 135531, which has a prolonged duration of action and greater efficacy in lowering intraocular pressure compared to melatonin. The present invention further provides a method of treating disorders associated with ocular hypertension, and a method of treating various forms of glaucoma; the method comprises administering an effective dose of a pharmacuetical composition comprising an indole derivative with or without agents commonly used to treat such disorders.

Abstract: A method for treating circadian rhythm phase disorders is described. The invention provides methods to specifically advance or delay the phase of certain circadian rhythms in humans. The disclosed methods relate to the administration of melatonin at times determined with relation to the time of dim light endogenous melatonin onset. Embodiments capable of alleviating the effects of jet lag, winter depression and shift-work sleep disturbance are provided.

Abstract: Diaminodicarboxylic acid:peptide gemini surfactant compounds are disclosed. Uses of the diaminodicarboxylic acid: peptide-based gemini surfactant compounds and methods for their production are also disclosed.

Abstract: Conjugates in which polyamine analogs are conjugated to an amino acid are provided, as well as compositions comprising these conjugates. Methods of using these conjugates as anticancer treatments are also provided.

Abstract: An amide of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: A —(CH2)p—R1, where R1 can be pyrrolidine, morpholine, piperidine, —NR5R6 and  and R5, R6 and R7 can, independently of one another, be hydrogen, C1-C4-alkyl, CH2Ph, Ph, CH2CH2Ph, it also being possible for the phenyl rings to be substituted by R6, and p can be 1 and 2, and B can be phenyl, pyridyl, pyrimidyl and pyridazyl, it also being possible for the rings to be substituted by up to 2 R8 radicals, and D can be a bond, —(CH2)m, —CH═CH—, —C≡C—, and Y is phenyl, pyridine, pyrimidine and pyrazine and n is a number 0, 1 or 2, and m,q are, independently of one another, a number 0, 1, 2, 3 or 4.

Abstract: The present invention is directed to novel dipeptide thereof, represented by the general Formula I: 1

Abstract: The purpose of the invention concerns a family of pseudodipeptides which are coupling products between tryptamine, an indole-primary amine, and a selection of alpha-amino acids, the said pseudodipeptides having the following general formula (I) 1

Abstract: This invention relates to peptide-containing &agr;-ketoamide inhibitors of cysteine and serine proteases, methods for making these compounds, and methods for using the same.

Abstract: This invention relates to compounds of the Formula (I): 1

Abstract: Compounds of the formula (I) 1

Abstract: The present invention relates to a compound of formula I 1

Abstract: The present invention relates to a novel fatty acid derivative of the following formula: 1

Abstract: The present invention relates to a class of compounds represented by the Formula I or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the &agr;v&bgr;3 and/or &agr;v&bgr;5 integrin. The ring A-B, is selected from the group consisting of the formula II all optionally substituted and bonded to X and Z1 at any position.

Abstract: A diverse set of tubulin binding agents have been discovered which are structurally characterized, in a general sense, by a semi-rigid molecular framework capable of maintaining aryl-aryl, pseudo pi stacking distances appropriate for molecular recognition of tubulin. In phenolic or amino form, these ligands may be further functionalized to prepare phosphate esters, phosphate salts, phosphoramidates, and other prodrugs capable of demonstrating selective targeting and destruction of tumor cell vasculature.

Abstract: The invention relates to a novel method for producing 3,3-diarylpropylamines of formula (I), wherein A represents a substituted or unsubstituted aryl radical, X represents H, OH or OR3 and Y, R1, R2 and R3 have the meanings given in the description, by hydroformylation/hydrocarbonylation and subsequent reductive amination using a transition metal catalyst.

Abstract: The invention includes selected novel optically active &agr;-amino ketones which either are themselves useful or are intermediates for the preparation of known ketomethylene pseudopeptides useful as antibiotics, antibiotic enhancers, or enzyme inhibitors. Further, the present invention provides a method for dehydrogenation/asymmetrical hydrogenation to obtain essentially pure antipodes of ketomethylene pseudopeptides having two chiral centers.