Abstract: The present invention relates to oxygenated esters of 4-substituted-phenylamino benzhydroxamic acid derivatives, pharmaceutical compositions, and methods of use thereof.

Abstract: The present invention relates to a method of manufacturing aspartyl dipeptide ester compounds, which can be used as sweeteners.

Abstract: The present invention provides solid and liquid sweetening compositions with a high intensity sweetness containing aspartyl dipeptide ester compounds, processing of making the aspartyl dipeptide ester compounds, as well as food and beverages containing the compositions.

Abstract: The present invention provides compounds having formula (I): 1

Abstract: The invention refers to new alkylating di- and tripeptides based on a melphalan unit, and one or two additional amino acids or amino acid derivatives, which can be used in the treatment of carcinogenic diseases. Further, the invention refers to a a pharmaceutical composition comprising the alkylating peptides of the invention.

Abstract: Described are 6-substituted indanoyl amino acid conjugates as defined in claim 1 of the present invention as potent plant elicitors and efficient mimics of the phytotoxin coronatine. Also, processes for producing the improved elicitors are provided, which allow a rapid and convenient access to large quantifies of the highly active compounds. Furthermore, there are compositions and plant protecting agents described, comprising as active ingredient a compound of the present invention. The plant protecting agents are useful for inducing resistance to pathogens in plants. The compositions may also be used to selectively induce senescence in fruit of plants.

Abstract: Novel compounds of the formula I in which W, X, Y, T, R1 and R2 are as defined in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disorders.

Abstract: The present invention relates to N-alkylated GABA (Gamma-aminobutyric acid) compounds, to processes for their preparation, to their use in therapy and to pharmaceutical compositions containing them. More particularly these compounds are useful for treatment of disorders of the central and/or peripheral nervous system. Of particular interest is their potent anticonvulsant activity.

Abstract: A compound having general formula 1

Abstract: Compounds of Formula I Each R is independently linear or branched C1 to C8 alkyl, or linear or branched C1 to C8 alkoxy or one R is H and the other R is linear or branched C1 to C8 alkyl, or linear or branched C1 to C8 alkoxy; R1 is selected from the group consisting of COCH3, CO2R3, CONH2, CONH(R4)2, CN, COX(CH2)n-N—(R2)(R4)(R3), and the quaternized salt form of the formula COX(CH2)n-N—(R2)(R4)(R3)+Y−; X is O or NH; n is an integer of 1 to 5; Y is an anion; and R2, R3 and R4 are independently linear or branched C1 to C20. Hair care formulations and other compounds containing compounds of Formula I, and methods for protecting hair and substrates such as polymers, textiles, fabrics, leathers and paints using the compounds herein.

Abstract: 3-(3-Methyl-4-hydroxyphenyl)-3-methylbutyl aldehyde may be produced from 3-(3-methyl-4-hydroxyphenyl)-3-methylbutyric acid by converting the carboxyl group into a formyl group. N-[N-[3-(3-methyl-4-hydroxyphenyl)-3-methylbutyl]-L-&agr;-aspartyl]-L-phenylalanine 1-methyl ester, which is useful as a sweetener having a high potency of sweetness, can be easily and efficiently prepared on an industrial production from such an aldehyde derivative, via a reductive alkylation reaction with aspartame. Therefore, 3-(3-Methyl-4-hydroxyphenyl)-3-methylbutyl aldehyde is extremely excellent as an intermediate for the production of N-[N-[3-(3-methyl-4-hydroxyphenyl)-3-methylbutyl]-L-&agr;-aspartyl]-L-phenylalanine 1-methyl ester.

Abstract: The present invention relates to novel retinol derivatives, the methods of preparation and the uses thereof. According to the present invention, retinol derivatives comprise carboester linkage between di-, tri-, polypeptide having functional group of COOH and retinol. Retinol derivatives in the present invention comprise carboester linkage between amino acid having functional group of di-COOH and retinol. Retinol derivatives comprise carboester linkage between retinol and the compounds having the function group of COOH and multiple double bonds on carbon chain. Retinol derivatives in the present invention comprise carboester linkage between retinol and the compounds having the functional group of di-COOH and one double bond. Retinol derivatives in the present invention comprise ether linkage between the compounds with OH functional group and retinol.

Abstract: The synthesis of 1-(acyloxy)-alkyl carbamates of GABA analogs from 1-haloalkyl carbamates of GABA analogs are described. Also described are new 1-haloalkyl carbamates of GABA analogs.

Abstract: This invention is directed to aromatic sulfone hydroxamates (also known as “aromatic sulfone hydroxamic acids”) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. This invention also is directed to a prevention or treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP and/or aggrecanase activity.

Abstract: The present invention relates to biphenyl and biphenyl-analogous compounds, their preparation and use as pharmaceutical compositions, as integrin antagonists and in particular for the production of pharmaceutical compositions for the treatment and prophylaxis of cancer, arteriosclerosis, restenosis, osteolytic disorders such as osteoporosis and ophthalmic diseases. The compounds according to the invention have the formula (1) wherein R1, R2, U, V, A, B, W, R3, C and R4 have the meaning as defined in the claims.

Abstract: Antipathogenic benzamide compounds having the formula 1

Abstract: The present invention relates to an anthranilic acid derivative expressed by the following formula (1) or the following formula (2), or its pharmacologically permissible salt or solvate.

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, —NR2 R3 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: The present invention provides a novel process for the crystallization of &agr;-L-aspartyl-L-phenylalanine methyl ester crystals wherein initial nucleation and initial crystal growth is conducted in a controlled manner in a metastable supersaturated solution, followed by further crystal growth via a cooling crystallization step. The process disclosed herein can be performed in an industrial scale.

Abstract: N-Biphenyl(substituted methyl)aminocycloalkanecarboxamide derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.

Abstract: A novel process affords &ohgr;-ketocarboxylic acid derivatives of the formula (I) 1

Abstract: The present invention provides compositions containing one or more aspartyl dipeptide derivatives represented by formulas (1) and/or (2) mixed with another high intensity sweetner, such Aspartame, sugar, sugar alcohol, and oligosaccharide; food, beverages, and/or medicinal products containing these compositions, methods of using the compositions to impart sweetness in food, beverages, and/or medicinal products to impart sweetness or suppress a bitter taste; and methods of making the compositions and products.

Abstract: The present invention includes a number of novel intermediates such as the (S)-secondary alcohol of formula (VIIIA)

Abstract: Pro-drug compounds of the formula (I) or (II) and compositions containing them are provided that when administered to humans or other mammals provide an increased duration of active compound in the plasma compared to compounds of corresponding structure in which labile groups are not present. In the above formulae n, P, Q, R1, R2; and R3; are as defined in the specification. The compounds may be used to treat a range of neurological conditions. e.g. epilepsy or pain.

Abstract: This invention relates to certain sulfonamide derivatives that are inhibitors of procollagen C-proteinase, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.

Abstract: Peptide conjugates in which cytocidal and cytostatic agents, such as polyamine analogs or naphthoquinones, are conjugated to a polypeptide recognized and cleaved by enzymes such as prostate-specific antigen (PSA) and cathepsin B are provided, as well as compositions comprising these conjugates. Methods of using these conjugates in the treatment of prostate diseases are also provided.

Abstract: Aspartyl dipeptide ester derivatives, such as a N-[N-[3-(3,4-dihydroxyphenyl)-3-methylbutyl]-L-&agr;-aspartyl]-L-phenylalanine 1-methyl ester, or salts thereof, having a high degree of sweetness compared to conventional sweeteners. These derivatives are excellent in sweetening potency and may be used as sweetener components in products such as foods and drinks. They may also be used as low calorie sweeteners and in methods of sweetening products. Foods and drinks comprising these derivatives as well as methods for their production.

Abstract: Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are of the following general formula, where X1, X2, Y, and Z are defined variables: Such compounds and their pharmaceutically acceptable salts, multimers, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.

Abstract: Disclosed is a noble &bgr;-hydroxyamide of general formula wherein R1 is alkyl, alkoxyalkyl or hydroxyalkoxyalkyl derived from at least one hydroxyfunctional compound, R2 is alkyl, aryl, alkylaryl or arylalkyl derived from at least one carboxyfunctional compound or at least one anhydride, halide or ester of at least one carboxyfunctional compound, R3 is N-alkyl or N-cycloalkyl derived from at least one alkanolamine and wherein m and n are independent integers and at least 1. In a further aspect the present refers to a process for synthesis of said &bgr;-hydroxyamide. The process comprises the Steps of (i) subjecting a di, tri or polyalcohol to alcoholysis with at least one di, tri or polyalkyl ester of a di, tri or polyfunctional carboxylic acid and (ii) subjecting obtained reaction product to aminolysis with at least one alkanolamine.

Abstract: This invention provides novel compounds that are effective as inhibitors of caspase and cellular apoptosis. The invention also provides methods for using the compounds to treat caspase-mediated diseases in mammals. The compounds have the general formula I: wherein X is F or Cl; R1 is COOH, COO(alkyl), or an isostere thereof; and R2 is an aryl group.

Abstract: Novel 3-aryl propionic acid derivatives and analogs, process and intermediate for their manufacture, pharmaceutical preparations containing them and the use of the compounds in clinical conditions associated with insulin resistance.

Abstract: Novel compounds of the formula I, in which R, R1 and R2 are as defined in patent claim 1, are inhibitors of coagulation factor Xa and VIIa and can be employed for the treatment of thromboses, myocardial infarction, arteriosclerosis, inflammation, apoplexis, angina pectoris, restenosis after angioplasty, claudicatio intermittens, tumours, tumour diseases and/or tumour metastases.

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

Abstract: A process for easily and efficiently separating aspartame (APM) from N-[N-(3,3-dimethylbutyl)-L-(&agr;-aspartyl]-L-phenylalanine methyl ester (APM derivative), and thus separating and purifying the APM and the above-mentioned APM derivative, more specifically the N-(3,3-dimethylbutyl)-APM each at a high purity, which comprises subjecting an aqueous solution containing the APM and the APM derivative, to column chromatography using a nonpolar highly porous polymer based resin.

Abstract: The present invention relates to a hydroxamic acid derivative of the formula (I) wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, a pharmaceutical composition containing the derivative or a salt thereof, and to pharmaceutical use thereof. The hydroxamic acid derivative and a pharmacologically acceptable salt thereof of the present invention have an inhibitory activity of TNF &agr; production, and are useful for, for example, the prophylaxis and treatment of the diseases such as autoimmune diseases and inflammatory diseases (e.g., sepsis, MOF, rheumatoid arthritis, Crohn's disease, cachexia, myasthenia gravis, systemic lupus erythematosus, asthma, I type diabetes, psoriasis and the like), and the like.

Abstract: A method for producing L-amino acid, such as L-phenylalanine and L-tryptophan, is provided using bacterium belonging to the genus Escherichia wherein the L-amino acid productivity of said bacterium is enhanced by enhancing an activity of protein encoded by the yddG gene.

Abstract: The present invention refers to synthetic protease inhibitors having an axis of symmetry C2 or pseudo-C2 characterised by possessing, in the central portion: (1) preferably, a dihydroxyethylene function, which is isosteric with a peptidic bond; (2) a peptidemimetic bridge between the two nitrogens of the main chain and (3) radicals capable of mimetising amino acids. These new protease inhibitors are a base for the preparation of anti-viral formulations capable of inhibiting HIV virus proliferation.

Abstract: Provided are processes for the synthesis of aniline derivatives, specifically certain aniline derivatives which have activity as thyroid receptor ligands.

Abstract: The invention provides compounds compositions and methods useful for inducing or maintaining general anesthesia or sedation in mammals.

Abstract: Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to &agr; 4 integrin. They are used as therapeutic agents for various diseases concerning &agr; 4 integrin.

Abstract: Modulators of PPAR&ggr; activity are provided which are useful in pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes and obesity.

Abstract: Compounds of formula I are useful for treating conditions associated with hyperglycemia, especially Type II diabetes. These compounds are useful in stimulating the kinase activity of the insulin receptor, activating the insulin receptor, and stimulating the uptake of glucose. Pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.

Abstract: A family of substituted chiral allosteric effectors of hemoglobin is useful for delivering more oxygen to hypoxic and ischemic tissues by reducing the oxygen affinity of hemoglobin in whole blood.

Abstract: Novel amidinophenol derivatives of formula (IB) and processes for the preparation thereof; compositions containing a compound of formula (IB) as active ingredient useful as antagonists of leukotine B4 and inhibitors of phospholipase A2 and/or trypsin; methods for preventing or treating diseases induced by phospholipase A2 and/or trypsin comprising administering to a patient a compound of formula (IB); and methods for treating diseases induced by leukotine B4 comprising administering to a patient a compound of formula (IB) or a known amidinophenol derivative of formula (IA)

Abstract: An agent comprising the benzoic acid of formula (I) 1

Abstract: A compound of formula I 1

Abstract: The invention relates to a process for preparing N-formylamino carboxylic esters by reacting amino carboxylic acids with formic esters.

Abstract: An assay is disclosed for determining whether a test compound modulates the activity of an enzyme having a metallated active site. The assay method employs a comparison of the binding ability of the metallated and unmetallated forms of the enzyme to the test compound.