Entries |
Document | Title | Date |
20080200532 | Fluvastatin sodium crystal forms XIV, LXXIII, LXXIX, LXXX and LXXXVII, processes for preparing them, compositions containing them and methods of using them - Provided are polymorphic forms of fluvastatin sodium and processes for their preparation. | 08-21-2008 |
20080207731 | 3-(3-INDOLYL) PROPIONIC ACID CALCIUM SALT AND METHOD OF MAKING 3-(3-INDOLYL) PROPIONIC ACID FREE ACID THEREFROM - Substantially pure 3-(3-indolyl)propionic acid free acid is synthesized by converting the free acid to 3-(3-indolyl)propionic acid calcium salt (3-IPA calcium), precipitating and washing, and then reconverting the 3-IPA calcium to the free acid. 3-IPA calcium is suitable for use in pharmaceutical compositions in tablet and sustained-release dosage forms. 3-IPA calcium can be used to inhibit the cytotoxic effects of amyloid beta protein on cells, to treat fibrillogenic diseases in a mammal, and to treat diseases or conditions in which free radicals or oxidative stress plays a role. | 08-28-2008 |
20080214646 | Novel Nsaids Possessing a Nitric Oxide Donor Diazen-1-Ium-1,2-Diolate Moiety - This invention provides a prodrug that help arthritis patients without increasing cardiovascular and gastrointestinal risk. A novel group of hybrid nitric oxide-releasing non-steroidal anti-inflammatory drugs (NO-NSAIDs), moiety attached via a one -carbon methylene spacer to the carboxylic acid group of the traditional NSAIDs aspirin, ibuprofen and indomethacin were synthesized. The ester prodrugs showed equipotent anti-inflammatory activities in vivo to that of the parent aspirin, ibuprofen and indomethacin. The simultaneous release of parent drug and nitric oxide from the NO- prodrugs constitutes a potentially beneficial property for the prophylactic prevention of thrombus formation and adverse cardiovascular events such as stroke and myocardial infarction. Data acquired in an in vivo ulcer index (UI) assay showed that this group of ester prodrugs in which no lesions were observed when compared to the parent drugs at equivalent doses. Accordingly, these hybrid NO-NSAID prodrugs possessing a diazen-1-ium-1,2-diolate moiety, represents a new approach for the rational design of anti-inflammatory drugs with reduced gastric ulcerogenicity. | 09-04-2008 |
20080214647 | SUBSTITUTED INDOLE ACID DERIVATIVES AS INHIBITORS OF PLASMINOGEN ACTIVATOR INHIBITOR-1 (PAI-1) - This invention provides compounds of the formula: | 09-04-2008 |
20080221197 | INDOLE ANTAGONISTS OF P2Y1 RECEPTOR USEFUL IN THE TREATMENT OF THROMBOTIC CONDITIONS - The present invention provides indole compounds of Formula (I) or (II): | 09-11-2008 |
20080221198 | Novel Crystalline Forms of Antidiabetic Compounds - Novel crystalline forms of two indole compounds connected to phenoxyalkylcarboxylic acid groups are selective PPAR gamma partial agonists that are useful in the treatment of type 2 diabetes, hyperglycemia, obesity, dyslipidemia, and the metabolic syndrome. The novel crystal forms include a crystalline free acid dihydrate and crystalline free acid anhydrate of one compound and several crystalline forms of the free acid and the sodium salt of the second compound. The invention also relates to pharmaceutical compositions comprising these novel crystal forms, processes to prepare the crystal forms and their pharmaceutical compositions, and uses of the crystal forms in the treatment of type 2 diabetes and other PPAR gamma modulated diseases. | 09-11-2008 |
20080221199 | METHOD FOR IMPROVING MEMORY IN MAMMALS - A method for improving memory in healthy subjects is disclosed. This method makes use of melatonin receptor antagonists such as luzindole and/or K-185 to reverse the inhibitory effect of melatonin. This invention is particularly relevant among subjects that do not show signs of central nervous system disorders and wish to improve their cognitive performance, especially in tasks. | 09-11-2008 |
20080227846 | METHODS OF TREATING JUVENILE TYPE 1 DIABETES MELLITUS - The present disclosure describes methods for treating or preventing Type 1 diabetes mellitus in juveniles, particularly in juveniles newly diagnosed with Type 1 diabetes. This prevention or treatment of Type 1 diabetes is achieved by administering one or more therapeutic agents to a juvenile in need, wherein the therapeutic agent is, for example, a competitive inhibitor of mevalonate synthesis, a competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, or an inducer of AMP protein kinase (AMPK) activity. In certain embodiments, juveniles with Type 1 diabetes are treated with an HMG-CoA reductase inhibitor such as a statin, thereby decreasing the destruction of islet cells, or maintaining endogenous insulin production, in the juvenile. | 09-18-2008 |
20080249155 | 5-Hydroxyindole-3-Carboxylate Derivatives and Uses Thereof - The present invention relates to 5-hydroxy-indole-3-carboxylate derivatives of formula I, or racemic mixture or optical isomers or pharmaceutically acceptable salts and/or hydrates thereof, | 10-09-2008 |
20080262072 | Compositions And Kits Comprising A Melatonin Component And A Flavanol Component - Disclosed herein are compositions and kits, wherein each composition comprises a melatonin component, a flavanol component, or both, and wherein each kit comprises a melatonin component and a flavanol component. The compositions and kits are useful for restorative sleep function and enhanced energy. Further disclosed herein are methods of using the compositions and kits. | 10-23-2008 |
20080269312 | Inhibitors of Ccr9 Activity - N-(benzenesulphonyl)-2,3-dihydro-1H-indols, wherein the indol is substituted by cyano, carboxy or alkylcarbonyloxy and their use as therapeutical agents. | 10-30-2008 |
20080287520 | Use of Melatonin in Preventing Postoperative Complications - The invention relates to the use of melatonin, either alone or in combination with at least one compound selected from the group consisting of L-arginine, a physiologically acceptable salt thereof, one or more other physiologically acceptable compounds associated with the synthesis of nitric oxide and mixtures thereof, for the manufacture of a medicament for the therapeutic treatment, prophylactic treatment and/or prevention of postoperative infectious and/or non-infections complications induced by surgical interventions wherein the infectious complications may be pneumonia, wound infection (wound dehiscence), intra-abdominal abscess, and urinary tract infections (UTI) or wherein the non-infectious complication may be anastomotic leak, a pharmaceutical formulation comprising melatonin and at least one compound selected from the group consisting of L-arginine, a physiologically acceptable salt thereof, one or more other physiologically acceptable compounds associated with the synthesis of nitric oxide and mixtures thereof and a method for the therapeutic and/or prophylactic treatment of postoperative infectious and/or non-infectious complications induced by surgical interventions. | 11-20-2008 |
20080293801 | Solid Amorphous Dispersions of An Mtp Inhibitor For Treatment of Obesity - A composition comprises a solid amorphous dispersion comprising (S)—N-{2-[benzyl(methyl)amino]-2-oxo-1-phenylethyl}-methyl-5-[4′-(trifluoromethyl)[1,1′-biphenyl]-2-carboxamido]-1H-indole-2-carboxamide and a polymer. | 11-27-2008 |
20080293802 | Chemical Compounds - The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula (I). | 11-27-2008 |
20080293803 | MELATONIN DAILY DOSAGE UNITS - The present invention relates to a disposable container for a medicament or cosmetic agent for topical application, containing a single dose of melatonin or of a melatonin derivative which corresponds to a locally effective dose but which does not cause any systemic effect. | 11-27-2008 |
20080306135 | Process for the Preparation of Crystalline Perindopril - The present invention relates to a new process for the preparation of crystalline perindopril. The present invention also relates to new alkyl ammonium salts of perindopril and the processes for the preparation thereof. | 12-11-2008 |
20080312308 | SUBSTITUTED ACETIC ACID DERIVATIVES - The present invention relates generally to substituted acetic acid derivatives and methods of using them. | 12-18-2008 |
20080319045 | Combination of Histone Deacetylase Inhibitors and Radiation - This invention relates to organic compounds of formula (I): | 12-25-2008 |
20080319046 | SUBSTITUTED SULFONAMIDE-INDOLES - The present invention relates generally to substituted sulfonamide indoles such as substituted sulfonamide indoles, and methods of using them. | 12-25-2008 |
20090023797 | Indol-Alanine Derivatives as Selective S1P4-Agonists - The present invention relates to agonists of the S1P4 receptor, which are selective for the S1P4 receptor over one or more of the S1P1, S1P2, S1P3 or S1P5 receptors of at least 10 fold, in particular new indol-alanine derivatives of structure 1, process for their production, their uses, in particular in transplantation, and pharmaceutical compositions containing them | 01-22-2009 |
20090023798 | THIOHYDROXAMATES AS INHIBITORS OF HISTONE DEACETYLASE - Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase. Also described herein are methods of using such HDAC inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC activity. | 01-22-2009 |
20090054511 | Tryptophan derivative and application thereof - 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. | 02-26-2009 |
20090062369 | USE OF SECRETORY PHOSPHOLIPASE A2 (SPLA2) INHIBITORS TO DECREASE SPLA2 LEVELS - Administration of sPLA | 03-05-2009 |
20090062370 | Method for increasing the speed of recovery and/or the speed of wound healing of injured animals - This invention is in the field of animal food, in particular food for wounded animals. Surprisingly, it has now been found that the speed of recovery of wounded animals may be increased by feeding the animal with a certain amount of natural occurring immune enhancing ingredients such as beta-glucans and/or phytohormones like auxin or gibberellic acid. Also, combinations of these substances, in particular the combination of beta-glucans and phytohormones, were shown to have a synergistic effect in that they improved the recovery speed of the animal more than the individual components on their own. | 03-05-2009 |
20090099248 | INHIBITORS OF D-AMINO ACID OXIDASE - The present invention provides novel inhibitors of the enzyme D-amino acid oxidase. The compounds of the invention are useful for treating or preventing diseases and/or condition, wherein modulation of D-serine levels, and/or its oxidative products, is effective in ameliorating symptoms. The invention further provides methods of enhancing learning, memory and/or cognition. For example, the invention provides methods for treating or preventing loss of memory and/or cognition associated with neurodegenerative diseases, such as Alzheimer's disease. The invention further provides methods for preventing loss of neuronal function characteristic of neurodegenerative diseases. In addition, methods are provided for the treatment or prevention of neuropsychiatric diseases (e.g., schizophrenia) and for the treatment or prevention of pain and ataxia. | 04-16-2009 |
20090118351 | Angiotensin I-Converting Enzyme (ACE) Inhibitors - 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. | 05-07-2009 |
20090124682 | Indan-Amide Derivatives with Glycogen Phosphorylase Inhibitory Activity - A compound of the formula (1) or a pharmaceutically-acceptable salt: (A chemical formula should be inserted here—please see paper copy enclosed herewith) (1) possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity. Processes for the manufacture of compounds and pharmaceutical compositions containing them are described. | 05-14-2009 |
20090163571 | PHARMACEUTICAL FOR USE IN THE TREATMENT OF URETEROLITHIASIS - The present invention provides pharmaceutical compositions useful for relieving pain caused by ureteral calculi, facilitating exclusion of ureteral calculi or the like. That is, the present invention provides a pharmaceutical composition for the treatment of ureteral lithiasis, which comprises as an active ingredient an indoline derivative represented by the following general formula (I) or a salt thereof. In the formula, R represents saturated or unsaturated aliphatic acyl which may have a substituent; hydroxyalkyl; aliphatic acyloxyalkyl; lower alkyl which has as a substituent lower alkoxy, carboxy, lower alkoxycarbonyl, aryl-substituted lower alkoxycarbonyl, carbamoyl, mono or di(lower alkyl)-substituted carbamoyl or cyano; optionally substituted aromatic acyl; furoyl or pyridylcarbonyl; R | 06-25-2009 |
20090186934 | Beta Crystalline form of the Arginine Salt of Perindopril, a Process for its Preparation and Pharmaceutical Compositions Containing it. - β-crystalline form of the compound of formula (I): | 07-23-2009 |
20090186935 | TASTE TITRATION THERAPIES - The teachings provided herein generally relate to formulations, systems, and methods that have the ability to remit deficiencies and imbalances in a subject's serotonin and dopamine levels. The teachings relate to the preparation and uses of a formulation comprising a serotonergic agent or dopaminergic agent in a form capable of oral transmucosal delivery to a subject. The formulation includes a flavoring agent and a carrier base. The flavoring agent functions as a taste indicator of the endpoint of a taste titration of the serotonergic or dopaminergic agent for a subject receiving an oral administration of the formulation in the form of a taste titration, and the endpoint is indicated to the subject by a change in the intensity of the flavor of the flavoring agent. | 07-23-2009 |
20090197936 | SALTS OF N-HYDROXY-3-[4-[[[2-(2-METHYL-1H-INDOL-3-YL)ETHYL]AMINO]METHYL]PH- ENYL]-2E-2-PROPENAMIDE - Salts of N-hydroxy-3-[4-[[[2-(2-methyl-1H-indol-3-yl)ethyl]amino]methyl]phenyl]-2E-2-propenamide are prepared and characterized. | 08-06-2009 |
20090209611 | Fluvastatin sodium crystal forms, processes for preparing them, compositions containing them and methods of using them - Provided are crystalline forms of fluvastatin sodium and processes for their preparation. | 08-20-2009 |
20090264496 | Compounds, Compositions and Methods for Making the Same - The present invention provides compounds and/or compositions that modulate PP2A methylation and/or activity and methods for preparing the same, which are useful for modulating the demethylation of PP2A, modulating the methylation of PP2A and/or modulating the activity of PP2A. | 10-22-2009 |
20090281160 | Angiotensin I-converting enzyme (ace) inhibitors - This invention relates to a process for the synthesis of ketomethylene derivatives of the tripeptide Phe-Gly-Pro (“keto-ACE”, compound 5 | 11-12-2009 |
20090306171 | INDOLE COMPOUNDS HAVING C4-AMIDE SUBSTITUENTS AND USE THEREOF AS PHOSPHOLIPASE-A2 INHIBITORS - Indole and indole-related compounds according to the formula (I) or (II) optionally having additional heteroatoms, compositions and methods are disclosed. The compounds of the invention are useful as phospholipase inhibitors. The compounds and compositions of the invention are useful for treatment of phospholipase-related conditions, such as insulin-related, weight-related and/or cholesterol-related conditions in an animal subject. Formula (I), formula (II). R | 12-10-2009 |
20090312391 | UNIFYING MECHANISM AND METHODS TO PREVENT CANCER AND NEURODEGENERATIVE DISEASES - The present invention relates to methods for preventing the development of cancer or neurodegenerative diseases by administering N-Acetylcysteine (NAC), melatonin, or a combination thereof. The present invention also relates to methods for diagnosing cancer and/or neurdegenerative disease by detecting or determining the amount of dopamine metabolites, 4-CE, 2-CE, methylation of CE or CE-Q conjugates. | 12-17-2009 |
20090318528 | HYDRATE CRYSTALS - New (2R,4R) monatin monosodium salt hydrate crystals characterized by having specific characteristic X-ray diffraction peaks provide general-purpose, stable, and safe monatin sodium salt crystals incorporating no organic solvent. These crystal may be prepared by a method that requires no organic solvent in the crystallization, separation, and drying steps. These crystal are useful as sweeteners and for the preparation of orally consumed products, such as foods, beverages, pharmaceutical products, topical pharmaceutical products, and feeds containing general-purpose, stable, and safe monatin sodium salt crystals. | 12-24-2009 |
20090326037 | Medicinal Agent For Treating Viral Infections - The invention relates to medicine, in particular to searching and developing novel medicinal agents for treating and preventing viral infections, mainly influenza viruses. The aim of said invention is to develop more efficient and low toxic medicinal agents by combining arbidol and the analogs thereof with a preparation exhibiting another mechanism of action. Said combinations enhances the efficiency of the preparation small doses and makes it possible to reduce the probability of side effects and appearance of virus resistant strain by reducing the dose. The result is attained by the combined use of arbidol and the analogies thereof with at least one type of preparation selected from the following group of antiviral preparations: ribavirin, zanamivirin, oseltavirin, peramirin, amantadin or remantadin. | 12-31-2009 |
20100004309 | Dietary Compositions and Methods for Protection Against Chemotherapy, Radiotherapy, Oxidative Stress, and Aging - The present invention relates to dietary compositions comprising reduced level of methionine, tryptophan, all amino acids, or protein, dietary compositions comprising glycerol as a substitute for monosaccharides, disaccharides, and polysaccharides, and hypocaloric or calorie free diets with reduced level of energy, carbohydrates, or protein. Also disclosed are methods of using these compositions and diets, as well as fasting, to protect subjects against chemotherapy, radiotherapy, oxidative stress, or aging. | 01-07-2010 |
20100029742 | CRYSTALLINE FORMS OF THE MONO-SODIUM SALT OF D-ISOGLUTAMYL-D-TRYPTOPHAN - The present invention relates to crystalline forms of the mono-sodium salt of D-isoglutamyl-D-tryptophan, pharmaceutical compositions comprising them, their use in the treatment of various diseases and conditions, and processes for their preparation. In particular, the present invention relates the crystal modification 1 (polymorphic form F), the crystal modification 2 (polymorphic form I), and the crystal modification 3 (polymorphic form X) of the mono-sodium salt of D-isoglutamyl-D-tryptophan. | 02-04-2010 |
20100076052 | PERINDOPRIL FORMULATIONS - Pharmaceutical formulations comprising perindopril or its salts, isomers, enantiomers, polymorphs, metabolites, solvates, hydrates, and mixtures thereof, and at least one surface stabilizer. Also disclosed are methods of stabilizing perindopril in the formulations, and polyoxyethylene-polyoxypropylene block copolymers as surface stabilizers. | 03-25-2010 |
20100099732 | MEDICAMENTS USEFUL AS POTASSIUM CHANNEL MODULATORS - This invention relates to pharmaceutical compositions comprising phenylcarbamoyl-methyl-indole derivatives that are found to be potent modulators of potassium channels and, as such, are valuable candidates for the treatment of diseases or disorders as diverse as those which are responsive to the modulation of potassium channels. | 04-22-2010 |
20100120887 | SUSTAINED RELEASE FORMULATION OF MELATONIN - The present invention relates to low-dose formulations of melatonin, and methods of use thereof, which provide a sustained release of melatonin so as to rapidly increase plasma levels of melatonin, maintain a relatively high level (which mimics the endogenous level of a young subject) for approximately 5-6 hours, and then decrease so as to achieve low levels by early morning (rapid washout), thereby avoiding a “hangover effect”. The sustained release formulations of the invention may be used to treat a variety of sleep-related disorders, including, but not limited to, delayed onset and maintenance forms of insomnia. | 05-13-2010 |
20100137400 | PHARMACEUTICAL FORMULATION CONTAINING AN HMG-COA REDUCTASE INHIBITOR AND METHOD FOR THE PREPARATION THEREOF - The present invention relates to improved pharmaceutical formulation for oral administration comprising a therapeutically effective quantity of an HMG-CoA reductase inhibitor, and more particularly Fluvastatin, Atorvastatin or salts thereof in combination with a linear sulphated polysaccharide such as Carrageenan and a method for the preparation thereof. | 06-03-2010 |
20100137401 | 2-METHYLPROP ANAMIDES AND THEIR USE AS PHARMACEUTICALS - The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess. | 06-03-2010 |
20100184819 | METHOD FOR REDUCING INTRACRANIAL PRESSURE - The present invention relates generally to methods for reducing intracranial pressure in a subject. More particularly, the methods of the present invention include administering to the subject an effective amount of a substance P receptor antagonist. | 07-22-2010 |
20100197758 | ISCHEMIA/REPERFUSION PROTECTION COMPOSITIONS AND METHODS OF USING - The invention provides for ischemia/reperfusion protection compositions having one or more ketone bodies and melatonin. The invention also provides for methods of using such compositions to reduce or prevent ischemia/reperfusion injury due to blood loss, stroke or cardiopulmonary arrest or surgery. | 08-05-2010 |
20100204295 | TREATMENT OF ALLERGIC DISEASE WITH IMMUNOMODULATOR COMPOUNDS - A method of treatment for treating, preventing, inhibiting or reducing allergic disease or its effects in a subject, comprises administering to the subject an effective amount of an immunomodulator compound, which composes an aromatic or heterocyclic amino acid residue or a derivative thereof. Preferably, the immunomodulatory compound is a dipeptide which comprises a D- or L-tryptophan residue. | 08-12-2010 |
20100240727 | Model for Glutamate Racemase Inhibitors and Glutamate Racemase Antibacterial Agents - The increase in antibacterial resistance has created the demand for new antibiotics. The present invention relates to a more potent antibiotic that targets the enzyme glutamate racemase from known glutamate racemase inhibitors. Glutamate racemase catalyses the interconversion of L-glutamate to D-glutamate, making D-glutamate available, which is required for bacterial peptidoglycan biosynthesis. Knockout mutations have shown glutamate racemase to be necessary for bacterial cell survival and, before the present invention, no antibiotic on the market targeted this enzyme. The present invention relates to new, ligand based glutamate racemase inhibitors, developed using software to extract a pharmacophore model from a group of known glutamate racemase inhibitors. Forty-seven (47) known inhibitors were collected from the literature and several pharmacophore models were extracted therefrom. The functional groups common to all the known inhibitors were included in a pharmacophore model that described the requirements for glutamate racemase inhibition with 82% accuracy. Of these models, one was found to describe the requirements for glutamate racemase inhibition with 82% accuracy. The model was used to search databases of commercially available chemical compounds and 2-(2-(1H-indol-3-yl)ethylamino)-4-oxo-4-p-tolylbutanoic acid and 2-(2-(1H-indol-3-yl)ethylamino)-4-(4-fluorophenyl)-4-oxobutanoic acid were identified as showing antibacterial activity. These compounds were assayed against | 09-23-2010 |
20100249204 | CALCIUM SALTS OF INDOLE DERIVED STATINS - The present invention provides calcium salts of indole derived statins of the formula | 09-30-2010 |
20100261774 | Methods for the modulation of Leishmania major infection in mammals - Embodiments of the invention include methods for treating an infection of a mammal by an organism, such as | 10-14-2010 |
20100280092 | N-ACYLHYDRAZONE DERIVATIVES USEFUL AS MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS - This invention relates to N-acylhydrazone derivatives, which are found to be useful as modulators of the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. | 11-04-2010 |
20100305183 | METHOD AND COMPOSITION FOR REDUCING REPERFUSION INJURY - The present invention relates to a method of preventing and/or reducing reperfusion injury to a tissue, organ, or organ system in a subject. The method includes administering to the subject an effective amount of a substance P receptor antagonist. | 12-02-2010 |
20100305184 | INHIBITORS OF THE ATB(0,+) TRANSPORTER AND USES THEREOF - The present invention includes inhibitors of the amino acid transporter ATB | 12-02-2010 |
20100311805 | COMBINATION OF HISTONE DEACETYLASE INHIBITORS AND RADIATION - This invention relates to organic compounds of formula (I): | 12-09-2010 |
20100317710 | 3-(3-INDOLYL) PROPIONIC ACID CALCIUM SALT AND METHOD OF MAKING 3-(3-INDOLYL) PROPIONIC ACID FREE ACID THEREFROM - Substantially pure 3-(3-indolyl)propionic acid free acid is synthesized by converting the free acid to 3-(3-indolyl)propionic acid calcium salt (3-IPA calcium), precipitating and washing, and then reconverting the 3-IPA calcium to the free acid. 3-IPA calcium is suitable for use in pharmaceutical compositions in tablet and sustained-release dosage forms. 3-IPA calcium can be used to inhibit the cytotoxic effects of amyloid beta protein on cells, to treat fibrillogenic diseases in a mammal, and to treat diseases or conditions in which free radicals or oxidative stress plays a role. | 12-16-2010 |
20100324109 | Composition for Topical Use - The use, as a dermatological or cosmetic medicament, of compounds capable of transiently interacting with the AhR receptor (aryl hydrocarbon receptor) as agents for modulating skin functions such as sebaceous function, skin healing, skin atrophy termed “dermatoporosis”, estrogen deprivation and defense against infection, without inducing other toxic effects of the TCDD type. | 12-23-2010 |
20110034531 | USE OF HDAC INHIBITORS FOR THE TREATMENT OF MELANOMA - The invention relates to the use of an HDAC inhibitor, more specifically or a pharmaceutically acceptable salt thereof for the manufacture of pharmaceutical compositions for the treatment of melanoma; the use of an HDAC inhibitor or a pharmaceutically acceptable salt thereof in the treatment of melanoma; a method of treating warm-blooded animals including mammals, especially humans, suffering from melanoma by administering to a said animal in need of such treatment a dose effective against said disease of an HDAC inhibitor or a pharmaceutically acceptable salt thereof. | 02-10-2011 |
20110060026 | Indoles Active on CRTH2 Receptor - Indole derivatives having therapeutic utility are of formula (I): X is —SO | 03-10-2011 |
20110118327 | IN VIVO ASSESSMENT OF TOXICITY AND PHARMACOKINETICS OF METHYLGLYOXAL - A pharmaceutical composition and treatment method to reduce the proliferation of cancerous or tumor cells, in which the combined active agents are methylglyoxal, ascorbic acid, creatine and melatonin. | 05-19-2011 |
20110178150 | Use of Indole Derivatives as NURR-1 Activators for Treating Parkinson's Disease - The present invention relates to a compound derived from indole, especially a therapeutically useful compound, characterized in that it is selected from compounds of formula (I) | 07-21-2011 |
20110196013 | Animal feed composition - The present invention relates to an animal feed composition that comprises free indole acetic acid (free IAA) or a derivative thereof. The invention also relates to a method for enhancing animal growth by feeding the animal with a composition according to the invention. The invention also relates to the use of free IAA or a derivative thereof in a method of therapy of animals in need of a growth-promoting treatment, such as immunocompromised animals, animals with a growth deficit or slow growing animals. The invention also relates to the use of free IAA or a derivative thereof for the preparation of a therapeutical composition for increasing the growth rate and/or the feed conversion rate and/or the immunity of animals in need of such a treatment, in particular immunocompromised or slow growing animals. A composition according to the invention may preferably be in the form of a food or feed supplement. | 08-11-2011 |
20110218227 | HYDRATE CRYSTALS - New (2R,4R) monatin monosodium salt hydrate crystals characterized by having specific characteristic X-ray diffraction peaks provide general-purpose, stable, and safe monatin sodium salt crystals incorporating no organic solvent. These crystal may be prepared by a method that requires no organic solvent in the crystallization, separation, and drying steps. These crystal are useful as sweeteners and for the preparation of orally consumed products, such as foods, beverages, pharmaceutical products, topical pharmaceutical products, and feeds containing general-purpose, stable, and safe monatin sodium salt crystals. | 09-08-2011 |
20110245316 | PREVENTION OR DELAY OF ONSET OF ORAL MUCOSITIS - The present invention provides a method for preventing or delaying the onset of oral mucositis, including the onset of ulcerative or severe OM, in a patient receiving cancer therapy. The method comprises administering to the patient an effective regimen of γ-D-glutamyl-L-tryptophan (SCV-07) over the course of therapy. The regimen, which includes scheduled doses of SCV-07 with respect to radiation exposure and/or chemotherapy, is effective for preventing or delaying the onset of OM. In accordance with the invention, the patient is more able to complete the planned course of cancer therapy (including chemotherapy and/or radiation therapy), by maintaining a sufficient nutritional state, and by avoiding the significant pain and discomfort associated with OM. | 10-06-2011 |
20110257239 | SUSTAINED RELEASE PHARMACEUTICAL COMPOSITION AND METHOD OF RELEASING PHARMACEUTICALLY ACTIVE AGENT - The present invention is directed to solid, sustained-release, oral dosage form pharmaceutical compositions which contain therapeutic amounts of a pharmaceutically active agent, hydroxypropyl methyl cellulose and a non-ionic, hydrophilic polymer selected froth the group consisting of hydroxyethyl cellulose having a number average molecular weight ranging from 90,000 to 1,300,000, hydroxypropyl cellulose having a number average molecular weight of 370,000 to 1,500,000, and poly(ethylene oxide) having a number average molecular weight ranging from 100,000 to 500,000. | 10-20-2011 |
20110288145 | Novel Formulation For L-Tryptophane Comprising Carbidopa/Benserazide - The present invention relates to the use of L-tryptophan and a peripheral degradation inhibitor of L-tryptophan for the manufacture of a medicament for prevention or therapy of pain, depressions, sleeping disorders and other serotonin dependent diseases of the CNS, wherein L-tryptophan is present in a retarded and the peripheral degradation inhibitor is present in a non-retarded formulation. | 11-24-2011 |
20110313014 | PRODUCTS COMPRISING N-PHENYLPROPENOYL AMINO ACID AMIDES AND USES THEREOF - The present invention relates to use of a composition comprising N-phenylpropenoyl amino acid amides for the preparation of a product to treat or prevent neurodegenerative disorders, cognitive decline, mild cognitive impairment, dementia, mood disorders, depression, sleep disorders, diseases involving protein aggregation in a human or animal, Alzheimer's disease, macular degeneration or diabetes. The invention further relates to products comprising N-phenylpropenoyl amino acid amides, including food and beverage products, food supplements, and pet food products, and methods for affecting cognitive performance of humans and animals. | 12-22-2011 |
20120010263 | ACETYLENE DERIVATIVES HAVING MGLUR 5 ANTAGONISTIC ACTIVITY - The invention provides compounds of formula I | 01-12-2012 |
20120016000 | METHOD TO ASSAY PHOSPHOLIPID AND TRIGLYCERIDE TRANSFER ACTIVITY OF MICROSOMAL TRIGLYCERIDE TRANSFER PROTEIN - The present invention is directed to a method for identifying an antagonist compound of microsomal triglyceride transfer protein (MTP), wherein the antagonist at least partially inhibits triglyceride transfer activity while not significantly inhibiting phospholipids transfer activity of MTP. In particular, the present invention is directed to assays for phospholipid (PL) and triglyceride (TG) transfer activity having considerably improved sensitivity. In addition, antagonist compounds that modulate the lipid transfer activity of MTP are provided. Kits for measuring the lipid transfer activity of MTP are also provided by the present invention. | 01-19-2012 |
20120095071 | 3-(3-INDOLYL) PROPIONIC ACID CALCIUM SALT AND METHOD OF MAKING 3-(3-INDOLYL) PROPIONIC ACID FREE ACID THEREFROM - Substantially pure 3-(3-indolyl)propionic acid free acid is synthesized by converting the free acid to 3-(3-indolyl)propionic acid calcium salt (3-IPA calcium), precipitating and washing, and then reconverting the 3-IPA calcium to the free acid. 3-IPA calcium is suitable for use in pharmaceutical compositions in tablet and sustained-release dosage forms. 3-IPA calcium can be used to inhibit the cytotoxic effects of amyloid beta protein on cells, to treat fibrillogenic diseases in a mammal, and to treat diseases or conditions in which free radicals or oxidative stress plays a role. | 04-19-2012 |
20120142750 | INDOLEAMINE 2,3-DIOXYGENASE PATHWAYS IN THE GENERATION OF REGULATORY T CELLS - The present invention provides methods for the control of the generation of regulatory T cells (Tregs) and uses thereof. | 06-07-2012 |
20120149752 | KIT FOR BALANCING NEUROTRANSMITTER LEVELS - The teachings provided herein generally relate to formulations, systems, and methods that have the ability to remit deficiencies and imbalances in a subject's serotonin and dopamine levels. The teachings relate to the preparation and uses of a formulation comprising a serotonergic agent or dopaminergic agent in a form capable of oral transmucosal delivery to a subject. The formulation includes a flavoring agent and a carrier base. The flavoring agent functions as a taste indicator of the endpoint of a taste titration of the serotonergic or dopaminergic agent for a subject receiving an oral administration of the formulation in the form of a taste titration, and the endpoint is indicated to the subject by a change in the intensity of the flavor of the flavoring agent. | 06-14-2012 |
20120245213 | HUMAN TYPE I TASTE RECEPTOR SUBUNIT 3 MODULATORS AND METHODS OF USING SAME - Methods and compositions are provided for modulating the activity of human type I taste receptor subunit 3 (hT1R3). Such materials and methods are useful for the screening and preparation of compositions and methods for the treatment of carbohydrate and lipid metabolic diseases and disorders. | 09-27-2012 |
20120283308 | ANIMAL FEED COMPOSITION - Disclosed is an animal feed composition that comprises free indole acetic acid (free IAA) or a derivative thereof. Also disclosed is a method for enhancing animal growth by feeding the animal with a composition according to the invention. Further disclosed is the use of free IAA or a derivative thereof in a method of therapy of animals in need of a growth-promoting treatment, such as immunocompromised animals, animals with a growth deficit or slow-growing animals. Disclosed is the use of free IAA or a derivative thereof for the preparation of a therapeutical composition for increasing the growth rate and/or the feed conversion rate and/or the immunity of animals in need of such a treatment, in particular, immunocompromised or slow-growing animals. A composition may be in the form of a food or feed supplement. | 11-08-2012 |
20120289574 | HYDRATE CRYSTALS - New (2R,4R) monatin monosodium salt hydrate crystals characterized by having specific characteristic X-ray diffraction peaks provide general-purpose, stable, and safe monatin sodium salt crystals incorporating no organic solvent. These crystal may be prepared by a method that requires no organic solvent in the crystallization, separation, and drying steps. These crystal are useful as sweeteners and for the preparation of orally consumed products, such as foods, beverages, pharmaceutical products, topical pharmaceutical products, and feeds containing general-purpose, stable, and safe monatin sodium salt crystals. | 11-15-2012 |
20130158093 | GPR 17 Agonists and Screening Assay - The present invention is related to a method of determining a test compound's ability to modify the biological activity of a GPR17. Said method comprises, among others, the step of contacting the test compound with a GPR17, or a functional GPR17 fragment in the presence of a suitable amount of a GPR17 agonist of formula I. | 06-20-2013 |
20130172397 | USE OF INHIBITORS OF PORPHOBILINOGEN DEAMINASE IN THE TREATMENT OF CONGENITAL ERYTHROPOIETIC PORPHYRIA - The invention relates to the use of a compound of general formula (I), wherein R | 07-04-2013 |
20130197053 | PHARMACEUTICAL COMPOSITION CONTAINING A TRYPTOPHAN DERIVATIVE - Pharmaceutical compositions containing a compound of formula (I) wherein the radicals denote e.g.: R | 08-01-2013 |
20130237579 | STABLE PHARMACEUTICAL COMPOSITIONS COMPRISING ONE OR MORE HMG-COA REDUCTAS INHIBITIORS - The present invention relates to stable pharmaceutical compositions comprising one or more HMG-CoA reductase inhibitors, processes for preparing the stable compositions and uses for the compositions. The stable pharmaceutical compositions of the invention may be used, in particular, for the treatment of hyperlipoproteinemia and atherosclerosis. | 09-12-2013 |
20130237580 | PEPTIDOMIMETIC COMPOUNDS AS IMMUNOMODULATORS - The present invention relates to novel peptidomimetic compounds as therapeutic agents capable of inhibiting the programmed cell death 1 (PD1) signalling pathway. The invention also relates to derivatives of the therapeutic agents. The invention also encompasses the use of the said therapeutic agents and derivatives for treatment of disorders via immunopotentiation comprising inhibition of immunosuppressive signal induced due to PD-1, PD-L1, or PD-L2 and therapies using them. | 09-12-2013 |
20140057959 | NOVEL COMPOUNDS DERIVED FROM TAURINE, PROCESS OF THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THESE - The present invention relates to compounds derived from taurine with non-steroidal anti inflammatory activity. | 02-27-2014 |
20140113949 | METHODS FOR REDUCING NEURODEGENERATION - The invention provides methods for reducing neurodegeneration in animals by administering a neurodegeneration reducing amount of melatonin to the animal. Generally, the melatonin is administered in amounts of either 0.1 ng/kg/day to about 10 mg/kg/day or from about 0.2 ng/day to about 3 g/day. In preferred methods, the melatonin is administered as part of a food composition. | 04-24-2014 |
20140128445 | POLYMERIC BENZYL CARBONATE-DERIVATIVES - The present invention relates to polymeric derivatives, which can be conjugated to an amino-containing drug to improve its in vivo properties. The polymeric derivative can subsequently be released to yield the drug in its native form. Methods of preparing and using these polymeric derivatives and drug conjugates are described. | 05-08-2014 |
20140187600 | USE OF METABOTROPIC GLUTAMATE RECEPTORS - The invention concerns the use an mGluR modulator, e.g. an mGluR5 modulator, for the treatment, prevention or delay of progression of cognitive dysfunction. | 07-03-2014 |
20140206741 | N-SUBSTITUTED ISOPROPYLDIMETHYL AZULENE SULFONAMIDE DERIVATIVES, AND PREPARATION METHOD AND USE THEREOF - The present invention provides an N-substituted isopropyldimethyl azulene sulfonamide derivative as represented by formula (I), and preparation method and uses thereof, wherein R1 is an alkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, amino, or a substituted alkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, and amino. The N-substituted isopropyldimethyl azulene sulfonamide derivative can be used in treating gastric ulcer. | 07-24-2014 |
20140213627 | NAPHTHOQUINONE DERIVATIVES USEFUL FOR PREVENTION OF AMYLOID DEPOSITS AND TREATMENT OF DISEASES INVOLVING AMYLOIDOGENESIS - The present invention provides pharmaceutical compositions comprising substituted 1,4 naphthoquinones that are effective in preventing oligomerization of beta amyloid and subsequent pathologies associated with amyloid fibrils. These compositions are useful for the treatment of disease involving amyloidogenesis including neurodegenerative diseases such as Alzheimer's Disease or senile dementia. Particularly effective compositions comprise 1,4 naphthoquinones substituted with an amino acid residue selected from a heterocyclic or aromatic amino acid. | 07-31-2014 |
20140221452 | COMPOSITIONS COMPRISING EICOSAPENTAENOIC ACID AND 5-HTP AND METHODS OF USE THEREOF - The present invention relates to, inter alia, pharmaceutical compositions comprising a polyunsaturated fatty acid and to methods of using the same to treat or prevent cardiovascular-related diseases. | 08-07-2014 |
20140303227 | TRANSMUCOSAL HORMONE DELIVERY SYSTEM - The present invention provides a pharmaceutical composition for sublingual or buccal administration of actives with low to poor aqueous solubility, e.g. the hormone melatonin, which contains a solution of the active in a pharmaceutically acceptable solvent adsorbed or absorbed onto particles of a pharmaceutically acceptable carrier and methods of preparing and using the pharmaceutical composition. | 10-09-2014 |
20140303228 | Biomarkers for Amyotrophic Lateral Sclerosis and Methods Using the Same - The disclosure provides biomarkers of amyotrophic lateral sclerosis (ALS). The disclosure also provides various methods of using the biomarkers, including methods for diagnosis of ALS, methods of determining predisposition to ALS, methods of monitoring progression/regression of ALS, methods of assessing efficacy of compositions for treating ALS, methods of screening compositions for activity in modulating biomarkers of ALS, methods of treating ALS, as well as other methods based on biomarkers of ALS. | 10-09-2014 |
20140343116 | CYTOCHROME P450 2C9 INHIBITORS - This invention is to provide multiple specific inhibitors of cytochrome P450 isozyme CYP2C9. These inhibitors can be derived from any combinations with the following compounds including: Tamarixetin, Formononetin, isoliquritigenin, Phloretin, luteolin, Quercitrin, quercetin, myricetin, Wongonin, Puerarin, Genistein, Nordihydroguaiaretic acid, Narigenin, Capillarisin, Chrysin, Fisefin, eriodictyol, 6-Gingerol, Isorhamneti, isoquercitrin, Morin, (+)-Taxifolin, isovitexin, 3-Phenylpropyl Acetate, Oleanolic acid, ursolic acid, β-Myrcene, cinnamic acid, Luteolin-7-Glucoside, Liquiritin, (+)Limonene, Homoorientin, Swertiamarin, Embelin, Daidzein, Poncirin, (−)-Epicatechin, ergosterol. These natural products can be used to enhance the bioavailability of therapeutic agents (drugs). | 11-20-2014 |
20140371288 | PLANT DISEASE CONTROL COMPOSITION - To provide a plant disease control composition having excellent control effect against plant diseases. | 12-18-2014 |
20140378522 | UNIFYING MECHANISM AND METHODS TO PREVENT CANCER AND NEURODEGENERATIVE DISEASES - The present invention relates to methods for preventing the development of cancer or neurodegenerative diseases by administering N-Acetylcysteine (NAC), melatonin, or a combination thereof. The present invention also relates to methods for diagnosing cancer and/or neurdegenerative disease by detecting or determining the amount of dopamine metabolites, 4-CE, 2-CE, methylation of CE or CE-Q conjugates. | 12-25-2014 |
20150031740 | COSMETIC COMPOSITION FOR STIMULATING THE CELLULAR ANTI-AGING FUNCTIONS OF THE SKIN - The use of a compound of general formula (I), where: R | 01-29-2015 |
20150031741 | COMPOSITIONS AND METHODS FOR IMPROVING LACTATION - The present disclosure relates to the use of pharmaceutical agents to manipulate serotonin in animal mammary glands. Use of the serotonin agents results in increased PTHrP levels, resulting in the release of calcium from the bone, which improves lactation. | 01-29-2015 |
20150038544 | ANIMAL FEED COMPOSITION - Disclosed is an animal feed composition that comprises free indole acetic acid (free IAA) or a derivative thereof. Also disclosed is a method for enhancing animal growth by feeding the animal with a composition according to the invention. Further disclosed is the use of free IAA or a derivative thereof in a method of therapy of animals in need of a growth-promoting treatment, such as immunocompromised animals, animals with a growth deficit or slow-growing animals. Disclosed is the use of free IAA or a derivative thereof for the preparation of a therapeutical composition for increasing the growth rate and/or the feed conversion rate and/or the immunity of animals in need of such a treatment, in particular, immunocompromised or slow-growing animals. A composition may be in the form of a food or feed supplement. | 02-05-2015 |
20150105439 | TREATMENT OF DRUG-RESISTANT CANCER WITH 2-ARYL-2-(3-INDOLYL) ACETOHYDROXAMATES - A pharmaceutical composition, a method of producing same, and a method of providing cancer therapy therein comprising a pharmaceutically acceptable excipient or carrier and a compound Formula 3 as follows: | 04-16-2015 |
20150111942 | IPA AS A THERAPEUTIC AGENT, AS A PROTECTIVE AGENT, AND AS A BIOMARKER OF DISEASE RISK - Indole-3-propionic acid as a marker and for treatment for Huntington Disease. | 04-23-2015 |
20150328142 | Sublingual Administration of Statins - The invention provides a pharmaceutical composition for the transmucosal delivery of a statin, said composition comprising a statin and a carrier in which said statin is soluble or forms a suspension or emulsion. The invention also provides a pharmaceutical composition comprising a statin for use in inhibiting cholesterol synthesis in vivo, where in said use said composition is delivered by the transmucosal route. | 11-19-2015 |
20150359252 | Nutrition Composition - The present invention provides a food intake regulating agent which improves anorexia and overeating and is safe for ingestion for a long term. The present invention relates to a food intake regulating agent containing 3 kinds of amino acids: threonine, methionine and tryptophan, as active ingredients. | 12-17-2015 |
20150368195 | INDOLINE COMPOUNDS FOR TREATMENT AND/OR PREVENTION OF INFLAMMATION DISEASES - The invention is based on the discovery that 1-arylsulfonyl-5-(N-hydroxyacrylamide)indolines and 1-arylsulfonyl-5-(N-hydroxyacrylamide)indoles has great potential as a novel agent to be used in the treatment of inflammation-associated diseases, particularly, inflammatory arthritis and fibrosis. | 12-24-2015 |
20160022636 | PHYSIOLOGICAL LIGANDS FOR GPR139 - Provided herein are compounds capable of activating GPR139. Also provided are methods of increasing and decreasing the activity of GPR139. Methods of using the identified compounds to modulate GPR139 activity or conditions that may be affected by GPR139 activity are also disclosed. | 01-28-2016 |
20160067186 | Controlled-Release Melatonin Compositions and Related Methods - A method of treating a human subject in need of melatonin therapy includes administering to a human subject a compressed tablet comprising melatonin, citric acid, and a cellulosic polymer. The melatonin, citric acid, and cellulosic polymer combine after ingestion to form an acidic hydrogel that dissolves the melatonin and is effective to provide a first release dose of melatonin for assisting in inducement of sleep and a subsequent sustained release dose of melatonin for assisting in sustaining sleep while in the human subject's gastrointestinal tract. | 03-10-2016 |
20160074331 | COMPOSITE STRUCTURAL MATERIAL AND PHARMACEUTICAL COMPOSITION THEREOF - A composite structural material and pharmaceutical composition comprising same, the use of the composite structural material in preparing a sustained release formulation, and a pharmaceutical composition formulation method; the composite structural material comprises a hydrophobic structural material and a hydrophilic structural material; the proportion of the hydrophobic structural material to the hydrophilic structural material ranges from 1:0.01 to 1:5, preferably 1:0.05 to 1:4, more preferably 1:0.1 to 1:3, and most preferably 1:0.4 to 1:2, such as 1:0.4 to 1:1.3. The pharmaceutical composition comprises the composite structural material and one or more active pharmaceutical ingredients, and preferably the proportion of the composite structural material to the active pharmaceutical ingredients ranges from 1:0.01 to 1:8, more preferably 1:0.02 to 1:5, and most preferably 1:0.03 to 1:1, such as 1:0.3 to 1:0.7. | 03-17-2016 |
20160106712 | FATTY ACID COX INHIBITOR DERIVATIVES AND THEIR USES - The invention relates to fatty acid COX inhibitor derivatives; compositions comprising an effective amount of a fatty acid COX inhibitor derivative; and methods for treating or preventing a metabolic, autoimmune inflammatory, or neurodegenerative disorder comprising the administration of an effective amount of a fatty acid COX inhibitor derivative. | 04-21-2016 |
20160143881 | METHOD FOR PREVENTING AND/OR TREATING CHRONIC TRAUMATIC ENCEPHALOPATHY-I - The present invention relates to a method of preventing and/or treating chronic traumatic encephalopathy. | 05-26-2016 |
20160199348 | Compounds | 07-14-2016 |
20190142853 | Inhibition of Galectin 3 Binding to the Airway Epithelial Surface to Treat or Prevent Septic Shock Resulting From Influenza and Subsequent Pneumococcal Pneumonia Infection | 05-16-2019 |
20220133667 | Method of Making a Magnesium Salt of an Alpha Keto Acid of Leucine, Isoleucine, and Valine - A method of making a magnesium salt of an alpha keto acid of the amino acid comprising valine, leucine, and/or isoleucine: 1) combining ingredients comprising: a calcium salt of an amino acid valine, leucine, or isoleucine; water; hydrochloric acid; and methyl tert-butyl ether; 2) stirring for about thirty minutes; 3) allowing the composition to settle into two layers, and collecting the top organic layer, and adding water and magnesium carbonate to the top organic layer; 4) heating the composition for one hour to 60-65° Celsius; 5) removing the solvent, cooling, and adding methyl-tert-butyl ether; 6) stirring the composition for one hour at 25-30° Celsius; 7) filtering, washing, drying under vacuum, and storing the composition as a powder; and 8) wherein the powder is a safe consumable low nitrogen product orally administered within a food, a beverage, or a tablet to treat kidney disease. | 05-05-2022 |