Abstract: The invention relates to indol-1-yl-acetic acid derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and methods of treatment comprising administration of said compounds.

Abstract: The present invention relates to hydrazone compounds of Formula I: and pharmaceutically acceptable salts and stereoisomers thereof, wherein R1, R2, R3, R4, L1, and L2 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I as inhibitors of TRPM5 protein.

Abstract: A mechanism of macrophage-induced T cell suppression is the selective elimination of tryptophan and/or increase in one or more tryptophan metabolites within the local macrophage microenvironment. Studies demonstrate that expression of IDO can serve as a marker of suppression of T cell activation, and may play a significant role in allogeneic pregnancy and therefore other types of transplantation, and that inhibitors of IDO can be used to activate T cells and therefore enhance T cell activation when the T cells are suppressed by pregnancy, malignancy or a virus such as HIV. Inhibiting tryptophan degradation (and thereby increasing tryptophan concentration while decreasing tryptophan metabolite concentration), or supplementing tryptophan concentration, can therefore be used in addition to, or in place of, inhibitors of IDO.

Abstract: The present invention relates to compounds, as well as to compositions, methods and kits comprising such compounds, for use in the treatment or prophylaxis of fibromyalgia, chronic fatigue syndrome, myofascial pain syndrome, Gulf War syndrome and related conditions, wherein the compound is a fatty acid oxidation inhibitor and/or a carbohydrate oxidation activator.

Abstract: The object of the present invention is to provide a pharmaceutical composition for preventing or treating viral infectious diseases. The compounds of the present invention have extremely potent anti-HCV activity and HCV growth inhibitory effects, and since they also only demonstrate mild cytotoxicity in vivo, a pharmaceutical composition containing the compound of the present invention is extremely useful as an anti-HCV preventive/therapeutic agent.

Abstract: The present invention relates to indole compounds of the formula (I): wherein R1, R2, R3, R4, A, E and X are as defined herein, and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepatitis C infections.

Abstract: A controlled release biocidal salt of a first component comprises a cation of a N?—(C1-C22)alkanoyl di-basic amino acid alkyl(C1-C22)ester cationic biocidal molecule and a second component comprising an anion of a monomeric anionic molecule having insignificant biocidal activity. The salt is characterized such that when the salt is exposed to an aqueous medium, the salt partially dissolves thereby releasing biocidal ions in an amount sufficient to exceed the MIC or MBC of a target bacteria being controlled, and further characterized as leaving a residual reservoir of undissolved salt capable of releasing more biocidal ions as the salt is consumed or otherwise removed from the environment encompassing the target bacteria. The preferred cationic biocidal molecule comprises N?-lauroyl-L-arginine ethyl ester (“LAE”).

Abstract: Novel trans-1,2-diphenylethylene derivatives are synthesized which can be used to form nanoparticles-monomer-nanomolecule-receptor nanosensors. These trans-1,2-diphenyl-ethylene derivatives are soluble in both water and organic solvents, highly fluorescent and can be synthesized in high yields. The trans-1,2-diphenylethylene derivatives are bonded to a nanoparticle, a nanomolecule bonded to the derivative and a receptor bonded to the nanomolecule to form a nanosensor that can be used to detect chemical and biological agents.

Abstract: The present invention herein provides, for instance, a stable isotope-labeled phenylalanine wherein a carbon atom of the phenyl group linked to an amino acid residue is 13C, 2 to 4 carbon atoms of the remaining 5 carbon atoms constituting the phenyl group are 12C atoms to which deuterium atoms are bonded, and the remaining carbon atoms are 13C atoms to which hydrogen atoms are linked, and a stable isotope-labeled tyrosine wherein a carbon atom of the phenyl group linked to an amino acid residue is 13C, the carbon atom bonded to the hydroxyl group (OH group) of the phenyl group is 12C or 13C, 2 to 4 carbon atoms of the remaining 4 carbon atoms constituting the phenyl group are 12C atoms to which deuterium atoms are bonded, and the remaining carbon atoms are 13C atoms to which hydrogen atoms are linked.

Abstract: A compound represented by the following formula (I) or a salt thereof is provided: wherein X represents a halogen atom; R1 represents a hydrogen atom, substituted or unsubstituted C1-6 alkyl group, substituted or unsubstituted C2-6 alkenyl group, substituted or unsubstituted C2-6 alkynyl group, substituted or unsubstituted aromatic group, substituted or unsubstituted aralkyl group, substituted or unsubstituted acyl group, substituted or unsubstituted arylsulfonyl group, substituted or unsubstituted C1-6 alkylsulfonyl group, substituted or unsubstituted C2-7 alkoxycarbonyl group, or hydroxyl group; R2 represents a substituted or unsubstituted C1-21 alkyl group; R3, R5, and R6 are the same or different and represent a hydrogen atom or halogen atom; R4 represents a hydrogen atom or substituted or unsubstituted C1-6 alkyl group; and R7 represents a hydrogen atom or substituted or unsubstituted C1-21 hydrocarbon group.

Abstract: This invention provides compounds of Formula I, having the structure: that are useful in treating diseases or disorders mediated by TNF-?. The invention further provides methods for use of the compounds for treating such a disease or disorder or for alleviating symptoms thereof.

Abstract: The present invention is directed to 2-phenyl-indole compounds, their preparation, pharmaceutical compositions containing these compounds, and their pharmaceutical use in treating a patient suffering from a PGD2-mediated disorder including, but not limited to, allergic disease (such as allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, bronchitis, eczema, urticaria diseases accompanied by itch (such as atopic dermatitis and urticaria), diseases (such as cataract, retinal detachment, inflammation, infection and sleeping disorders) which are generated secondarily as a result of behavior accompanied by itch (such as scratching and beating), inflammation, chronic obstructive pulmonary diseases, ischemic reperfusion injury, cerebrovascular accident, chronic rheumatoid arthritis, pleurisy, ulcerative colitis and the like.

Abstract: This invention relates to a process for synthesising an amino acid derivative of a tripeptidomimetic, such as lisinopril. The invention also relates to a derivative of lisinopril, incorporating a amino acid moeity such as tryptophan at the P2? position.

Abstract: It is intended to provide a tryptophan derivative that activates osteoblasts and to provide a therapeutic drug for osteoporosis and an osteoblast activator using this tryptophan derivative.

Abstract: The present invention relates to substituted acetamides of the general formula I, process for their preparation, and the use thereof for the manufacture of pharmaceutical compositions for the treatment of disorders and indications connected with the EP2 receptor.

Abstract: The present invention relates, in general, to isoprenylcysteine carboxylmethyltransferase (Icmt) and, in particular, to inhibitors of Icmt and to methods of disease treatment using same.

Abstract: The invention concerns 4-aminomethyl-1-aryl-cyclohexylamine compounds, methods for producing same, pharmaceutical formulations containing said compounds and the use of 4-aminomethyyl-1-aryl-cyclohexylamine compounds for producing medicines and in related methods of treatment.

Abstract: Processes for extracting amino acids from mixtures of amino acids, and compositions and mixtures formed therefrom. Applications include isolating natural L-?-3-indolylalanine (L-?-3) and providing natural or other amino acid mixtures enriched with the extracted L-?-3. The source of amino acids may include a natural source, such as enzymatic or other natural protein hydrolysates containing mixtures of free amino acids. The process includes contacting the mixture of amino acids with a resin or hydrophobic substance that is attractive to aromatic amino acids but not attractive to aliphatic amino acids to separate the aromatic amino acids from the rest of the mixture. This contacting may include agitating the mixture and hydrophobic substance to increase contact therebetween. The L-?-3 may then be separated from the monocylic amino acids by contacting the hydrophobic substance with an acid, and L-?-3 may be removed from the hydrophobic substance by contact with a base.

Abstract: Compounds of the formula I, in which R1, R2, R3, R4, R5, and R6 have the meanings given in the description, and their physiologically acceptable salts. The compounds are suitable for use, for example, as hypolipidemics.

Abstract: The present invention provides a process for efficiently producing an optically active ?-amino acid and an optically active ?-amino acid amide. After contacting with cells or processed cells thereof having an ability to asymmetrically hydrolyse, a water solvent is substituted with at least one solvent selected from the group consisting of linear, branched, or cyclic alcohol having 3 or more carbon atoms and the optically active ?-amino acid is preferentially precipitated from the alcohol solution. The addition of basic compounds, particularly potassium compounds to the alcohol solution containing the optically active ?-amino acid amide, which is obtained after the separation of the optically active ?-amino acid, enables the purification of the amide without the inclusion of amino acid into amino acid amide. Thus, the amide is subjected to the step of racemization and then recycled.

Abstract: Disclosed are methods of inhibiting neovascularization in a subject by administering to the subject a pharmaceutical preparation of R?-Glu-Trp-R?.

Abstract: This invention relates to derivatives of hemiasterlin or Geodiamolide G having anti-mitotic activities and useful in treating cancer. These derivatives are represented by general formula I, wherein Y, n, R1, R2, R3, R6, R7, R70, R71, R72, R74, and R75 are as defined in the specification.

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: 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: Phytopharmaceutical food products which contain plant extracts and aminoacids and which can be used in order to reduce tobacco smoke addiction.

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: A composition for an infant formula which comprises a low threonine content; a method of producing the composition; use of the composition in the manufacture of a medicament or nutritional product for addressing the nutritional needs and providing healthy growth of an infant; and a method of addressing the nutritional needs and providing healthy growth of an infant which comprises administering an effective amount of the composition. A preferred embodiment of the composition comprises all of: i) acid whey protein or sweet whey protein from which caseino-glyco-macropeptide has been removed; and ii) free arginine; and iii) free histidine; and iv) free tyrosine or free tryptophan or tryptophan rich milk protein or a mixture thereof.

Abstract: Compounds of the formula (I) are disclosed which are FabI inhibitors and are useful in the treatment of bacterial infections.

Abstract: The invention relates to compounds of formula (I): wherein 0≦n≦3, 0≦m≦6, R3 and R4 together form phenyl, B represents heteroaryl, R1 and R2 represent hydrogen or groups as defined in the description. and medicinal products containing the same which are useful in treating or preventing arterial hypertension and cardiovascular diseases.

Abstract: A method for treating circadian rhythm disorders is described. The method involves the administration of melatonin, melatonin agonists or compounds that stimulate endogenous melatonin production so that the durations of the effective plasma concentrations of melatonin, melatonin agonists or compounds that stimulate endogenous melatonin production overlap with onset or offset of pre-treatment endogenous melatonin production, to provide a circadian-rhythm phase advance or phase delay, respectively. The methods of the invention also provide for concentration and/or duration of the effective plasma concentrations of melatonin, melatonin agonists or compounds that stimulate endogenous melatonin production to be greater in the time interval between about 8 hours before the dim light endogenous melatonin onset (DLMO) to about 4 hours after DLMO than in the time interval from about 4 hours after DLMO to about 8 hours before DLMO to achieve a circadian-rhythm phase advance.

Abstract: The present invention relates to a method of inhibiting matrix metalloproteinases using compounds that are dibenzofuran sulfonamide derivatives having the Formula I More particularly, the present invention relates to a method of treating diseases in which matrix metalloproteinases are involved such as multiple sclerosis, atherosclerotic plaque rupture, restenosis, aortic aneurism, heart failure, periodontal disease, corneal ulceration, burns, decubital ulcers, chronic ulcers or wounds, cancer metastasis, tumor angiogenesis, arthritis, or other autoimmune or inflammatory diseases dependent upon tissue invasion by leukocytes.

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: This invention relates to methods and compositions of tripeptides and dipeptides having anti-inflammatory activities that can be used for the treatment of allergic and inflammatory reactions. A peptide of the formula: X-R.sub. 1 -R.sub.2 -R.sub.3 -Y  (I) or X-R.sub. 1 -R.sub.2 -Y  (II) wherein X is selected from the group consisting of H and acetyl; R.sub. 1 is selected from the group consisting of D or L-phenylalanine; tyrosine; tryptophan; phenylglycine; Nor-methylphenylalanine; cyclohexylalanine; and norleucine; R.sub.2 is selected from the group consisting of D or L-glutamate; and aspartate; and in the case of peptide (II), R.sub.3 is selected from the group consisting of glycine; D or L-alanine; beta-alanine; valine; leucine; isoleucine; sarcosine; and gamma-aminobutyric acid or another aliphatic amino acid; and Y is selected from the group consisting of OH and NH.sub.2, but excluding the dipeptides H-L-Phe-L-Glu-OH, H-L-Trp-L-Glu-OH, H-D-Phe-D-Glu-OH and H-D-Trp-D-Glu-OH.

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

Abstract: Compounds of the formulae

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: Amide, sulfonamide and urea compounds having an inhibitory effect on Src kinase including enantiomers, stereoisomers and tautomers thereof, as well as pharmaceutically acceptable salts or solvates of said compound, said compound having the general structure shown in Formulae I and II: 1

Abstract: Processes for isolating substantially pure natural L-&bgr;-3-indolylalanine (L-&bgr;-3) from a mixture of amino acids, such as a protein hydrolysate. A protein hydrolysate, for example of casein or soy protein, is passed over a polymeric resin attractive to aromatic amino acids but not attractive to aliphatic amino acids. The aromatic amino acids are retained on the resin while the aliphatic amino acids pass over the resin and are collected. The resin is then washed to displace any residual aliphatic acids which may be physically associated with but not bound to the resin. Thereafter, the resin is eluted with a dilute acid to displace L-phenylalanine and L-tyrosine and provide a solution thereof while allowing L-&bgr;-3 to be retained on the resin. The resin is then further eluted with a dilute base to displace L-&bgr;-3 from the resin and provide a solution of L-&bgr;-3. Substantially pure natural L-&bgr;-3 is recoverable from this solution.

Abstract: Compounds of 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: The invention concerns cholecystokinin (CCK) antagonists useful in the treatment of cognitive disorders. Especially useful are CCKB antagonists such as CI-988.

Abstract: Processes for isolating substantially pure natural L-&bgr;-3-indolylalanine (L-&bgr;-3) from a mixture of amino acids, such as a protein hydrolysate. A protein hydrolysate, for example of casein or soy protein, is passed over a polymeric resin attractive to aromatic amino acids but not attractive to aliphatic amino acids. The aromatic amino acids are retained on the resin while the aliphatic amino acids pass over the resin and are collected. The resin is then washed to displace any residual aliphatic acids which may be physically associated with but not bound to the resin. Thereafter, the resin is eluted with a dilute acid to displace L-phenylalanine and L-tyrosine and provide a solution thereof while allowing L-&bgr;-3 to be retained on the resin. The resin is then further eluted with a dilute base to displace L-&bgr;-3 from the resin and provide a solution of L-&bgr;-3. Substantially pure natural L-&bgr;-3 is recoverable from this solution.

Abstract: Compounds of formula (I) are antibacterials: 1

Abstract: The present invention provides illudin analogs of the general formula (I): 1

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

Abstract: This invention provides analogs of L-Glu-L-Trp and methods of using them for immunomodulation and treatment of pathological neovascular conditions. The analogs include the substitution of a carbon atom for a nitrogen atom in the indole ring of tryptophan.

Abstract: Non-nucleoside reverse transcriptase inhibitors of formula (P-1) wherein: Ar1 is an unsaturated, optionally substituted, mono or bicyclic ring structure comprising 0 to 3 hetero atoms selected from S, O and N; Ar2 is an aromatic, optionally substituted, monocyclic ring structure comprising at least one nitrogen hetero atom and zero to two further hetero atoms selected from S, O and N; R4 and R5 are independently H or C3-C8 cycloalkyl, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C5 alkoxy, C1-C4 alkanoyloxy, C1-C4 alkylthio, amino, carboxy, carbamoyl, cyano, halo, hydroxy, aminomethyl, hydroxymethyl, carboxymethyl, or halo substituted C1-C6 alkyl mercapto, nitro; or R4 and RS join to form a 3-6 membered, optionally substituted ring structure; R6 is 0 or S; Rx is the residue of a natural or unnatural amino acid; and L* is a linker moiety which is ether-, carbonate- or ester-bound to the adjacent oxygen and ester linked to Rx; and pharmaceutically acceptable salts thereof are anti-HIV agents with favourable ph

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 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: The invention relates to compounds of formula: wherein R1 is selected from the group consisting of fatty acid acyl groups of 12 to 30 carbon atoms and fatty alcohol groups of 12 to 30 carbon atoms, and wherein R2 is selected from the group consisting of H, fatty acid acyl of 12 to 30 carbon atoms and fatty alcohol groups of 12 to 30 carbon atoms, the same as or different from R1, and the residue of a nutrient, drug, or other bioactive compound, and to the use of these compounds to deliver drugs and other bioactive compounds.