23rd week of 2009 patent applcation highlights part 44 |
Patent application number | Title | Published |
20090143313 | Treatment or Prevention of Hemorrhagic Viral Infections with Immunomodulator Compounds - An immunomodulatory compound is administered to a patient having, or at risk of a hemorrhagic viral infection. | 2009-06-04 |
20090143314 | COMPOSITIONS AND METHODS FOR COMBINATION ANTIVIRAL THERAPY - The present invention relates to therapeutic combinations of [2-(6-amino-purin-9-yl)-1-methyl-ethoxymethyl]-phosphonic acid diisopropoxycarbonyloxymethyl ester (tenofovir disoproxil fumarate, Viread®) and (2R, 5S, cis)-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one (emtricitabine, Emtriva™, (-)-cis FTC) and their physiologically functional derivatives. The combinations may be useful in the treatment of HIV infections, including infections with HIV mutants bearing resistance to nucleoside and/or non-nucleoside inhibitors. The present invention is also concerned with pharmaceutical compositions and formulations of said combinations of tenofovir disoproxil fumarate and emtricitabine, and their physiologically functional derivatives, as well as therapeutic methods of use of those compositions and formulations. | 2009-06-04 |
20090143315 | Salix extract, its use and formulations containing it - The present invention relates to an extract of | 2009-06-04 |
20090143316 | COCRYSTAL OF C-GLYCOSIDE DERIVATIVE AND L-PROLINE - A cocrystal of (1S)-1,5-anhydro-1-[3-(1-benzothien-2-ylmethyl)-4-fluorophenyl]-D-glucitol and L-proline. It is a cocrystal of known compound A, which has a constant quality, is superior in storage stability, has no moisture absorptivity, and is suitable as a crystal of a drug substance used for preparing pharmaceuticals. | 2009-06-04 |
20090143317 | Quercetin Glycoside Composition and Method of Preparing the Same - The present invention provides an α-glycosyl isoquercitrin-containing novel composition which has a high in vivo absorbability, and hence exhibits a significant in vivo antioxidative activity. The present invention further provides preparation methods for such a composition. The composition contains a mixture of quercetin glycosides represented by the following formula: | 2009-06-04 |
20090143318 | DEGRANULATION INHIBITOR - An object of the invention is to find in nature a compound having a degranulation inhibitory action comparable to that of steroidal or non-steroidal degranulation inhibitors, but without any side effect such as hormone action or gastrointestinal disturbances which are observed in these inhibitors, and there is provided a degranulation inhibitor comprising as an active ingredient an ellagic acid derivative of the formula (I): | 2009-06-04 |
20090143319 | Transcription factor decoy - Double-stranded oligonucleotides useful as decoy oligonucleotides having a high binding ability to a transcription factor and having a reduced cytotoxicity are disclosed. Each of the double-stranded oligonucleotides is formed by hybridization of a sense strand oligonucleotide of the following Formula A: | 2009-06-04 |
20090143320 | Kinase suppressor of Ras inactivation for therapy of Ras mediated tumorigenesis - The present invention relates to methods and compositions for the specific inhibition of kinase suppressor of Ras (KSR). In particular, the invention provides genetic approaches and nucleic acids for the specific inhibition of KSR, particularly of KSR expression. The invention relates to antisense oligonucleotides and the expression of nucleic acid which is substantially complementary to KSR RNA. Oligonucleotide and nucleic acid compositions are provided. The invention provides methods to inhibit KSR, including inhibition of KSR expression. Methods for blocking gf Ras mediated tumorigenesis, metastasis, and for cancer therapy are provided. Methods for conferring radiosensitivity to cells are also provided. | 2009-06-04 |
20090143321 | NUCLEIC ACID AGENTS FOR DOWNREGULATING H19 AND METHODS OF USING SAME - The present invention provides isolated oligonucleotides capable of down-regulating a level of H19 mRNA in cancer cells. Articles of manufacture comprising agents capable of downregulating H19 mRNA in combination with an additional anti-cancer treatment are disclosed as well as methods of treating cancer by administering same. | 2009-06-04 |
20090143322 | CELL TRANSFECTING FORMULATIONS OF SMALL INTERFERING RNA RELATED COMPOSITIONS AND METHODS OF MAKING AND USE - Compositions incorporating small interfering ribonucleic acid (siRNA) and certain lipid-conjugated polyamide compound-based delivery vehicles that are particularly useful in the delivery siRNA and other polynucleotides to cells. Also, methods of making and using the compositions. | 2009-06-04 |
20090143323 | COMPOSITIONS AND METHODS FOR INHIBITING EXPRESSION OF A GENE FROM THE EBOLA - The invention relates to a double-stranded ribonucleic acid (dsRNA) for inhibiting the expression of a gene from the Ebola virus. | 2009-06-04 |
20090143324 | RNA INTERFERENCE MEDIATED INHIBITION OF INTERLEUKIN AND INTERLEUKIN RECEPTOR GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA) - This invention relates to compounds, compositions, and methods useful for modulating interleukin and/or interleukin receptor gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of other genes involved in pathways of interleukin and/or interleukin receptor gene expression and/or activity by RNA interference (RNAi) using small nucleic acid molecules. In particular, the instant invention features small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules and methods used to modulate the expression of interleukin and/or interleukin receptor genes such as IL-1, IL-2, IL-3, IL-4, IL-5, IL-6, IL-7, IL-8, IL-9, IL-10, IL-1, IL-12, IL-13, IL-14, IL-15, IL-16, IL-17, IL-18, IL-19, IL-20, IL-21, IL-22, IL-23, IL-24, IL-25, IL-26, and IL-27 genes and IL-1R, IL-2R, IL-3R, IL-4R, IL-5R, IL-6R, IL-7R, IL-8R, IL-9R, IL-10R, IL- | 2009-06-04 |
20090143325 | RNA INTERFERENCE MEDIATED INHIBITION OF INTERLEUKIN AND INTERLEUKIN RECEPTOR GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA) - This invention relates to compounds, compositions, and methods useful for modulating interleukin and/or interleukin receptor gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of other genes involved in pathways of interleukin and/or interleukin receptor gene expression and/or activity by RNA interference (RNAi) using small nucleic acid molecules. In particular, the instant invention features small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules and methods used to modulate the expression of interleukin and/or interleukin receptor genes, IL-1, IL-2, IL-3, IL-4, IL-5, IL-6, IL-7, IL-8, IL-9, IL-10, IL-11, IL-12, IL-13, IL-14, IL-15, IL-16, IL-17, IL-18, IL-19, IL-20, IL-21, IL-22, IL-23, IL-24, IL-25, IL-26, and IL-27 genes and IL-1R, IL-2R, IL-3R, IL-4R, IL-5R, IL-6R, IL-7R, IL-8R, IL-9R, IL-10R, IL-11R, IL-12R, IL-13R, IL-14R, IL-15R, IL-16R, IL-17R, IL-18R, IL-19R, IL-20R, IL-21R, IL-22R, IL-23R, IL-24R, IL-25R, IL-26R, and IL-27R. | 2009-06-04 |
20090143326 | MICROMIRs - The present invention relates to very short heavily modified oligonucleotides which target and inhibit microRNAs in vivo, and their use in medicaments and pharmaceutical compositions. | 2009-06-04 |
20090143327 | General composition framework for ligand-controlled regulatory systems - The invention provides an improved design for the construction of extensible nucleic acid-based, ligand-controlled regulatory systems, and the nucleic acid regulatory systems resulting therefrom. The invention contemplates improving the design of the switches (ligand-controlled regulatory systems) through the design of an information transmission domain (ITD). The improved ITD eliminates free-floating ends of the switching and the competing strands, and localizes competitive hybridization events to a contiguous strand of competing and switching strands in a strand-displacement mechanism-based switch, thereby improving the kinetics of strand-displacement. The improved regulatory systems have many uses in various biological systems, including gene expression control or ligand-concentration sensing. | 2009-06-04 |
20090143328 | Method of Treating Cancer by Administration of Topical Active Corticosteroids - The present invention provides for methods of treating cancer comprising administering a topical active corticosteroid in conjunction with a form of non-myeloablative conditioning, wherein the above regimen results in a reduction or elimination of cancer cells in an individual. | 2009-06-04 |
20090143329 | GIP SECRETION INHIBITOR - The present invention provides a postprandial GIP secretion inhibitor comprising potassium alginate as an active ingredient. The postprandial GIP secretion inhibitor of the present invention is useful as a medicine or a food product. The present invention also provides use of potassium alginate for the manufacture of a postprandial GIP secretion inhibitor. The present invention also provides a method for inhibiting postprandial GIP secretion, which comprises administering potassium alginate to a subject in need thereof or causing a subject in need thereof to consume potassium alginate. | 2009-06-04 |
20090143330 | Crystalline Polymorphic Forms Of Monosodium N-[-8-(2-Hydroxybenzoyl)Amino]Caprylate - The present invention relates to crystalline polymorphic forms of monosodium N-[8-(2-hydroxybenzoyl)amino] caprylate (“SNAC”), including two hydrates, a methanol solvate, and an ethanol solvate, of SNAC. More specifically, the present invention provide six polymorphic forms of SNAC (hereafter referred to as Forms I-VI). The present invention also provides an amorphous form of SNAC. | 2009-06-04 |
20090143331 | POLYSACCHARIDE GEL FORMULATION HAVING INCREASED LONGEVITY - Described herein are polysaccharide gel formulations including at least one inhibitor of polysaccharide degradation and methods of making the same. The methods described herein involve the steps of providing at least one polysaccharide and incorporating at least one inhibitor of degradation into the polysaccharide. In some embodiments, the incorporating step comprises 1) mixing the at least one inhibitor with the at least one polysaccharide at a highly hydrated state thereby encapsulating the at least one inhibitor in a polysaccharide network, and 2) dehydrating the polysaccharide network thereby controlling release kinetics or final swell ratio. In another embodiment, the incorporating step comprises 1) encapsulating at least one inhibitor into a biocompatible or biodegradable vessel and 2) combining the polysaccharide and the vessel into a gel formulation. The polysaccharide gel formulations described herein can be used for a variety of cosmetic applications. | 2009-06-04 |
20090143332 | Cyclodextrin Cyanohydrins - The present invention relates to a compound having a cyclodextrin skeleton wherein a hydrogen atom at the C-6 position in at least one of the sugar moieties has been substituted with a cyano group thereby forming a cyanohydrin-type group. The compounds are found to be excellent catalysts, e.g. for the hydrolysis of aryl glycosides. Accordingly, the compounds of the invention are useful as medicaments, in particular for the treatment of poisoning and drug abuse. The compounds, optionally immobilized to a solid phase material, are useful to reduce the content of harmful substances, e.g. metabolites of fungi, insects, etc., from compositions such as foodstuff. | 2009-06-04 |
20090143333 | SILICONE GEL-BASED COMPOSITIONS FOR WOUND HEALING AND SCAR REDUCTION - This invention is a composition comprising a cyclic siloxane, a silicone occlusive fluid, a silicone occlusive gel, and a silicone resin powder. The composition is useful for wound healing. | 2009-06-04 |
20090143334 | Method of Protecting Wood Through Enhanced Penetration of Wood Preservatives and a Related Solution - A method of protecting wood through enhanced penetration of wood preservatives includes providing a solution including (a) at least one amine oxide. (b) at least one organic wood preservative and (c) a buffering agent. The solution preferably has a pH of about 7 to 10. The solution is applied to the surface of the wood after which, with or without intervening storage, the materials are activated to effect enhanced penetration of the organic wood preservative into the wood. One may effect application at a solution temperature of about 30 to 75° C. and preferably about 50 to 60° C. to effect activation at a higher temperature and high relative humidity. In a preferred practice, the wood may be heated before and/or after application of the solution. The solution is also disclosed as a product. | 2009-06-04 |
20090143335 | MODIFIED ABSORPTION FORMULATION OF GABOXADOL - The present invention relates to a pharmaceutical composition comprising gaboxadol or a pharmaceutically acceptable salt thereof and one or more inhibitors of PAT1 and/or one or more inhibitors of OAT. The present invention further relates to a pharmaceutical composition comprising from about 0.5 mg to about 50 mg gaboxadol or a pharmaceutically acceptable salt thereof, wherein the composition provides an in vivo plasma profile comprising a mean Tmax which is longer than about 20 minutes. | 2009-06-04 |
20090143336 | Novel phosphonic acid compounds as inhibitors of serine proteases - The present invention is directed to phosphonic acid compounds useful as serine protease inhibitors, compositions thereof and methods for treating inflammatory and serine protease mediated disorders. | 2009-06-04 |
20090143337 | C2-C5-Alkyl-Imidazole-Bisphosphonates | 2009-06-04 |
20090143338 | Metal coordinated compositions - A metal coordination complex of a biologically active moiety and a metal is disclosed. The complex confers to the biologically active moiety an improved performance which can include potency, stability, absorbability, targeted delivery, and combinations thereof. | 2009-06-04 |
20090143339 | METHODS USING PHOSPHATIDYLSERINE, LYSOPHOSPHATIDYLSERINE, AND/OR SALTS THEREOF TO INCREASE TESTOSTERONE LEVELS - Methods using phosphatidylserine, lysophosphatidylserine, and/or salts thereof to increase testosterone levels in subjects in need thereof are disclosed herein. The methods can be useful for subjects having age related decline in testosterone, exercise induced decline in testosterone, and/or hypogonadism. | 2009-06-04 |
20090143340 | Pyrocatechin Derivatives - Pyrocatechin derivatives of formula I | 2009-06-04 |
20090143341 | MICROBICIDAL COMPOSITION - The invention relates to a microbicidal composition which comprises a mixture of at least two components, the first component being 2-methyl-3-isothiazolone (MIT) and the second component being at least one active compound selected from the following groups of active compounds: a) compound having activated methylol groups b) quats or polyquats c) carbamates d) organic acids e) aromatic alcohols. | 2009-06-04 |
20090143342 | 26,27-homologated-20-EPI-2-alkylidene-19-nor-vitamin D compounds - This invention provides a novel class of vitamin D related compounds, namely, the 2-alkylidene-19-nor-vitamin D derivatives, as well as a general method for their chemical synthesis. The compounds have the formula: | 2009-06-04 |
20090143343 | COMPOSITIONS FOR THE TREATMENT OF INFLAMMATION OF THE GASTROINTESTINAL TRACT - Provided herein are methods for treating the symptoms of and inflammation associated with gastroesophageal reflux disease (GERD) and other conditions. Also provided herein are pharmaceutical compositions useful for the methods of the present invention. | 2009-06-04 |
20090143344 | METHODS FOR TREATING OR PREVENTING SYMPTOMS OF HORMONAL VARIATIONS - The present invention relates to methods for treating or preventing symptoms of hormonal variation. The method comprises the steps of administering an effective amount of a receptor antagonist to a subject having one or more symptoms of hormonal variations, wherein the receptor antagonist binds to at least one receptor selected from the group consisting of a serotonin type 2A (5-HT | 2009-06-04 |
20090143345 | THIOAMIDE DERIVATIVES AS PROGESTERONE RECEPTOR MODULATORS - Thioamide compounds, and specifically, thioamide pyrrole compounds, and preparation thereof are provided. These thioamide compounds can be used as progesterone receptor modulators, in contraception, and in the treatment of progesterone-related maladies. | 2009-06-04 |
20090143346 | Method for synthesizing furanosteroids - The present invention is a method for synthesizing furanosteroids. The method involves intramolecular Diels-Alder/retro-Diels-Alder reaction and tautomerization of a functionalized alkyne oxazole to produce a furo[2,3-b]phenol derivative which is elaborated by intermolecular and intramolecular condensations to generate ring-A of the furanosteroid. Furanosteroids and pharmaceutical compositions containing the same are also provided. | 2009-06-04 |
20090143347 | Use of 3-methoxy-pregnenolone for the preparation of a drug for treating depressive disorders and long-term neurological diseases - The invention relates to the therapeutic use of pregnenolone derivatives for treating depressive disorders and long-term neurological diseases. | 2009-06-04 |
20090143348 | POLYSACCHARIDE GEL COMPOSITIONS AND METHODS FOR SUSTAINED DELIVERY OF DRUGS - Methods of producing a biocompatible polysaccharide gel composition having sustained release properties are disclosed. Also disclosed is a biocompatible polysaccharide gel composition having sustained release properties, a method of treating a disease or condition using the present biocompatible polysaccharide gel composition, and a method of controlling rate of release of at least one target solute from the biocompatible polysaccharide gel composition. Pharmaceutical compositions which include the present biocompatible polysaccharide gel composition also are disclosed. | 2009-06-04 |
20090143349 | STEROID TETROL SOLID STATE FORMS - The invention relates to solid state forms of androst-5-ene-3β,7β,16α,17β-triol, formulations containing or prepared from such solid state forms and use of such materials for modulating acute and chronic non-productive inflammation. The formulations can be used to prevent, treat or slow the progression of conditions related to autoimmunity such as arthritis, multiple sclerosis, ulcerative colitis or Type 1 diabetes. The formulations can also be used to prevent, treat or slow the progression of conditions related to metabolic disorders such as Type 2 diabetes. | 2009-06-04 |
20090143350 | Anxiolytic Marcgraviaceae Compositions Containing Betulinic Acid, Betulinic Acid Derivatives, and Methods - Pharmaceutical compositions for preventing or treating anxiety, comprising betulinic acid or derivatives thereof are provided. Methods for preventing or treating anxiety with betulinic acid or derivatives thereof are also provided. The invention further provides betulinic-acid containing preparations of plants of the family Marcgraviaceae having anxiolytic activity and methods for making such extracts and using them to prevent or treat anxiety in a subject. | 2009-06-04 |
20090143351 | SUBSTITUTED AZETIDINONES - Compounds are provided which have the structure | 2009-06-04 |
20090143352 | PYRROLO-PYRIDINE KINASE MODULATIORS - The present invention provides novel pyrrolo-pyridine kinase modulators and methods of using the novel pyrrolo-pyridine kinase modulators to treat diseases mediated by kinase activity. | 2009-06-04 |
20090143353 | ANTIFUNGAL BICYCLIC HETERO RING COMPOUNDS - A 1,6-β-glucan synthetase inhibitor is provided, having potent growth inhibition and having excellent safety. | 2009-06-04 |
20090143354 | P2X7 Receptor Antagonists and Their Use - The invention provides compounds of formula (IA), processes for their preparation, pharmaceutical compositions containing them, and their use in therapy. | 2009-06-04 |
20090143355 | Substituted aryl-amine derivatives and methods of use - Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds of Formula I and II | 2009-06-04 |
20090143356 | Polycylclic Carbamoylpyridone Derivative Having HIV Integrase Inhibitory Acitvity - Is to provide a novel compound having an anti-viral activity, particularly a HIV integrase inhibitory activity, and a pharmaceutical composition, particularly an anti-HIV agent. | 2009-06-04 |
20090143357 | HETEROARYL UREA DERIVATIVES USEFUL FOR INHIBITING CHK1 - Substituted urea compounds useful in the treatment of diseases and conditions related to DNA damage or lesions in DNA replication are disclosed. Methods of making the compounds, and their use as therapeutic agents, for example, in treating cancer and other diseases characterized by defects in DNA replication, chromosome segregation, or cell division, also are disclosed. | 2009-06-04 |
20090143358 | INHIBITORS OF ION CHANNELS - Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-gated sodium channels. More particularly, the invention provides substituted aryl sulfonamides, compositions comprising these compounds, as well as methods of using these compounds or compositions in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrence of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a voltage-gated sodium channel. | 2009-06-04 |
20090143359 | Percutaneously Absorptive Ophthalmic Preparation Comprising Epinastine - The present invention provides a percutaneously absorptive preparation for preventing or treating allergic eye disease, which comprises epinastine or a salt thereof as an active ingredient. In addition, the present invention provides a method for preventing or treating allergic eye disease, which comprises applying a percutaneously absorptive preparation comprising epinastine or a salt thereof to the skin surface including the skin surface of an eyelid, thereby causing transfer of a therapeutically effective amount of epinastine or a salt thereof from the preparation to an anterior ocular segment through the skin of the eyelid rather than a systemic blood flow. The present preparation can exert a pharmacological effect over a prolonged period by a single application, as compared to conventional preparations such as eye drops. | 2009-06-04 |
20090143360 | Oxcarbazepine Formulation - The present invention relates to novel uncoated, color-stable tablet formulations comprising oxcarbazepine, a disintegrant and iron oxide pigments. The oxcarbazepine of the present invention has a particle size of about 14 to about 30 microns with a maximum residue on a 40 micron sieve from about 10% to about 35%. The present invention further provides for a process of preparing the tablet formulations, and a method of treating mammals in need of oxcarbazepine with the novel formulation. | 2009-06-04 |
20090143361 | Pyrido[3,2-E]Pyrazines, Process For Preparing The Same, And Their Use As Inhibitors Of Phosphodiesterase 10 - The invention relates to pyrido[3,2-e]pyrazines, to processes for preparing them, to pharmaceutical compositions which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 10, as active compounds for treating central nervous system disorders, obesity, and metabolic disorders. | 2009-06-04 |
20090143362 | CARBAMAZEPINE FORMULATIONS - The present invention relates to a process for preparing a pharmaceutical composition comprising carbamazepine that has a constant release profile. | 2009-06-04 |
20090143363 | Deuterated lorcaserin - This invention relates to novel compounds that are 3-benzazepine derivatives and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel 3-benzazepine derivatives that are derivatives of lorcaserin. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering a 5-HT | 2009-06-04 |
20090143364 | CHIRAL CIS-IMIDAZOLINES - and the pharmaceutically acceptable salts and esters thereof, wherein X | 2009-06-04 |
20090143365 | DERIVATIVES OF ALKYLPIPERAZINE- AND ALKYLHOMOPIPERAZINE-CARBOXYLATES, PREPARATION METHOD THEREOF AND USE OF SAME AS FATTY ACID AMIDO HYDROLASE ENZYME INHIBITORS - The present invention comprises alkylpiperazine- and alkylhomopiperazine carboxylates and their derivatives, methods for their preparation and the therapeutic use thereof as fatty acid amido hydrolase (FAAH) enzyme inhibitors. These derivatives exert various pharmacological activities by interacting, inter alia, with cannabinoid and vanilloid receptors. By inhibiting the metabolic activity of the FAAH enzyme, compounds often responsible for the onset of disease and other pathological conditions are not generated and the incidence of the disease is greatly reduced. | 2009-06-04 |
20090143366 | CHEMICAL COMPOUNDS - The present invention relates to dihydrobenzodiazepine derivatives, compositions and medicaments containing the same, as well as processes for the preparation and use of such compounds, compositions and medicaments. Such dihydrobenzodiazepine derivatives are useful in the treatment of diseases associated with inappropriate ROCK kinase. | 2009-06-04 |
20090143367 | ARYL AND HETEROARYL FUSED IMIDAZO[1,5-a]PYRAZINES AS INHIBITORS OF PHOSPHODIESTERASE 10 - The invention relates to imidazo[1,5-a]pyrazine derivatives, to processes for preparing them, to pharmaceutical preparations which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 10 (PDE10), as active compounds for treating central nervous system diseases of mammals, including humans. | 2009-06-04 |
20090143368 | Use of Cinnamoyl Compound - A composition for inhibiting the extracellular matrix gene transcription comprising a cinnamoyl compound represented by the formula (I): | 2009-06-04 |
20090143369 | METHODS OF USING SUBSTITUTED MORPHOLINE AND THIOMORPHOLINE DERIVATIVES - The present invention relates to morpholine and thiomorpholine derivatives of the general formula I or pharmaceutically acceptable salts thereof and their use. | 2009-06-04 |
20090143370 | Non-nucleoside Reverse Transcriptase Inhibitors - Compounds of formula (I): | 2009-06-04 |
20090143371 | ISOXAZOLE-PYRIDINE DERIVATIVES - The present invention is concerned with isoxazole-pyridine derivatives of formula I | 2009-06-04 |
20090143372 | CHEMICAL COMPOUNDS - The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula I: | 2009-06-04 |
20090143373 | QUINOLONE CARBOXYLIC ACID-SUBSTITUTED RIFAMYCIN DERIVATIVES - The compounds include substituted rifamycin derivatives in which a quinolone carboxylic acid pharmacophore is covalently bonded to a benzoxazinorifamycin or a spiropiperidinorifamycin. The rifamycin derivatives are useful as antimicrobial agents and are effective against a number of human and veterinary Gram positive and Gram negative pathogens. The advantage of the inventive compounds is that both the rifamycin and quinolone antibacterial pharmacophores are co-delivered with matched pharmacokinetics to the targeted pathogens of interests. Delivery of multiple antibacterial pharmacophores simultaneously to the targeted pathogens has the maximum chance of achieving synergy and minimizing the development of resistance to the antibiotics given. | 2009-06-04 |
20090143374 | Use of Compounds and Compositions for the Treatment of Amyloid Diseases - Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially Aβ amyloidosis, such as observed in Alzheimer's disease, use in the reduction of Aβ peptide in vivo, use in modulating APP processing, and use in modulating the activity of APP secretase. | 2009-06-04 |
20090143375 | Tricyclic Lactam Derivatives, Their Manufacture and Use as Pharmaceutical Agents - Objects of the present invention are the compounds of formula I | 2009-06-04 |
20090143376 | Fused Heterocyclic Compounds and Their Use as Sirtuin Modulators - Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, chemotherapeutic induced neuropathy, neuropathy associated with an ischemic event, polyglutamine diseases, ocular diseases and/or disorders, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent. | 2009-06-04 |
20090143377 | METHODS AND COMPOSITIONS FOR TREATING DISORDERS - Compounds and compositions for treating disorders related to TRPA1 are described herein. | 2009-06-04 |
20090143378 | THIENOPYRIMIDINE AND THIENOPYRIDINE KINASE MODULATORS - The invention is directed to thienopyrimidines and thienopyridines compounds of Formula I and Formula II: | 2009-06-04 |
20090143379 | Storage stable perfusion solution for dihydropteridinones - Disclosed are storage stable aqueous infusible or injectable solutions containing an active substance of general formula (I) | 2009-06-04 |
20090143380 | 2H- OR 3H-BENZO[E]INDAZOL-1-YL CARBAMATE DERIVATIVES, THE PREPARATION AND THERAPEUTIC USE THEREOF - Compounds corresponding to the formula (I) | 2009-06-04 |
20090143381 | MODULATORS OF ATP-BINDING CASSETTE-TRANSPORTERS - Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention. | 2009-06-04 |
20090143382 | FLUOROALKOXY-SUBSTITUTED 1,3-DIHYDRO-ISOINDOLYL COMPOUNDS AND THEIR PHARMACEUTICAL USES - The invention encompasses novel compounds, pharmaceutically acceptable salts, hydrates, solvates, clathrates, enantiomers, diastereomers, racemates, or mixtures of stereoisomers thereof, pharmaceutical compositions of these compounds, and methods of using these compounds and compositions in mammals for treatment or prevention of diseases associated with PDE4. | 2009-06-04 |
20090143383 | ARYLOXYETHYLAMINE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECEPTOR - The present invention relates to aryloxyethylamine compounds of the formula I | 2009-06-04 |
20090143384 | 2,4,6-Trisubstituted Pyrimidines as Phosphotidylinositol (Pi) 3-Kinase Inhibitors and Their Use in the Treatment of Cancer - The invention concerns pyrimidine derivatives of Formula (I) wherein each of Q | 2009-06-04 |
20090143385 | ISOXAZOLO-PYRIDAZINE DERIVATIVES - The invention relates to isoxazolo-pyridazine compounds, in particular those of formula I as described above and to a pharmaceutically acceptable salts thereof, having affinity and selectivity for the GABA A α5 receptor binding site, their manufacture, pharmaceutical compositions containing them and their use as cognitive enhancers or for the treatment of cognitive disorders like Alzheimer's disease. | 2009-06-04 |
20090143386 | Human adam-10 inhibitors - The present invention provides compounds useful for inhibiting the ADAM-10 protein. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more ADAM-10 inhibitors according to the invention in combination with a pharmaceutically acceptable carrier. Such compositions are useful for the treatment of cancer, arthritis, and diseases related to angiogenesis. Correspondingly, the invention also comprises methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role. The invention also provides methods for making bis-aryl ether sulfonyl chlorides and ADAM-10 modulators therefrom. | 2009-06-04 |
20090143387 | SUSTAINED-RELEASE TABLET COMPOSITION - A sustained-release pharmaceutical composition in a form of an orally deliverable tablet containing reboxetine, or a pharmaceutically acceptable salt thereof, dispersed in a matrix containing a hydrophilic polymer and a starch, wherein the starch has a tensile strength of at least 0.15 kN cm | 2009-06-04 |
20090143388 | TREATMENT OF BRAIN DISORDERS - Striatal neurodegenerative disorders, e.g. Parkinson's disease, are treated by administration of an effective dose of an antioxidant compound of formula I, formula II or a pharmaceutically acceptable salt thereof, in a regimen that decreases the adverse effects of the disorder. Such adverse effects can motor deficits, which include catalepsy or akinesia. Also provided are kits and systems for practicing the subject methods, as well as methods of use of agents identified in the screening method of the invention. | 2009-06-04 |
20090143389 | HETEROCYCLIC INHIBITORS OF MEK AND METHODS OF USE THEREOF - Disclosed are compounds of the Formulas III and IV | 2009-06-04 |
20090143390 | Parenteral Formulations of Dopamine Agonists - This invention relates to stable pharmaceutical compositions for parenteral administration comprising dopamine agonists and peripheral acting agents_useful for treatment of metabolic disorders or key elements thereof. The parenteral dosage forms exhibit long stable shelf life and distinct pharmacokinetics. | 2009-06-04 |
20090143391 | Aryl and heteroaryl fused imidazo [1,5-a] pyrazines as inhibitors of phosphodiesterase 10 - The invention relates to imidazo[1,5-a]pyrazine derivatives, to processes for preparing them, to pharmaceutical preparations which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 10 (PDE10), as active compounds for treating central nervous system diseases of mammals, including humans. | 2009-06-04 |
20090143392 | Methods of Treating Obesity and Metabolic Disorders - The invention relates to methods of treating or preventing obesity, type 2 diabetes, metabolic syndrome, or glucose intolerance using pyrido[3,2-e]pyrazines which are inhibitors of PDE10. The invention further relates to methods of reducing body fat or body weight. | 2009-06-04 |
20090143393 | METHOD OF STIMULATING HAIR GROWTH - The present invention is directed to the discovery that (3S,4R)-3,4-dihydro-4-(2,3-dihydro-2-methyl-3-oxopyridazin-6-yl)oxy-3-hydroxy-6-(3-hydroxyphenyl)sulphonyl-2,2,3-trimethyl-2H-benzo[b]pyran may be used to promote hair growth and alleviate alopecia. | 2009-06-04 |
20090143394 | COMPOUNDS FOR ACTIVATING TGF-BETA SIGNALING - Compositions and methods for treatment and prevention of disorders and conditions characterized by reduced TGF-β signaling are described. | 2009-06-04 |
20090143395 | Piperazine Derivatives - Compounds of general formula (I) | 2009-06-04 |
20090143396 | Sulfonyl-Substituted Aryl Compounds as Modulators of Peroxisome Proliferator Activated Receptors - Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed. | 2009-06-04 |
20090143397 | CATECHOL-BASED DERIVATIVES FOR TREATING OR PREVENTING DIABETICS - The present invention provides a catechol-based derivative and a pharmaceutical acceptable salt therefrom and a solvate therefrom. A pharmaceutical composition for preventing or treating diabetics and ischemics, comprising a catechol-based derivative of formula (I) and at least one selected from the group consisting of a pharmaceutical excipient, a diluent and a carrier. | 2009-06-04 |
20090143398 | PYRIMIDINYL-PIPERAZINES USEFUL AS D3/D2 RECEPTOR LIGANDS - The present invention relates to new dopamine D | 2009-06-04 |
20090143399 | Protein Kinase Inhibitors - Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the following structure: | 2009-06-04 |
20090143400 | PURINE DERIVATIVES HAVING IMMUNO-MODULATING PROPERTIES - The present invention provides compounds of formula | 2009-06-04 |
20090143401 | Pyridine and Pyrimidine Derivatives as Inhibitors of Histone Deacetylase - This invention comprises the novel compounds of formula (I) | 2009-06-04 |
20090143402 | ISOQUINOLINONE DERIVATIVES AS NK3 ANTAGONISTS - Isoquinolone derivatives of the general formula | 2009-06-04 |
20090143403 | Methods for Administering Aripiprazole - The present invention relates, in part, to the discovery that a pharmaceutical composition comprising aripiprazole and a carrier administered in a bolus injection resulted in an extended release profile similar to that obtained by the injection of a poly lactide-co-glycolide microsphere formulation containing the active agent. This surprising result suggests that pharmacologically beneficial extended release formulations without the complexities and expense associated with the manufacture microspheres. | 2009-06-04 |
20090143404 | Pharmaceutical composition - A preparation for oral administration comprising: a pregelatinized starch comprising N-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]-(2R,3R)-2,3-tetramethylene-butyl]-(1′R,2′S,3′R,4′S)-2,3-bicyclo[2,2,1]-heptanedicarboxyimide hydrochloride (lurasidone) represented by the formula (1) as an active ingredient; a water-soluble excipient; and a water-soluble polymeric binder, the preparation exhibiting an invariant level of elution behavior even when the content of its active ingredient is varied. | 2009-06-04 |
20090143405 | MELANIN CONCENTRATING HORMONE RECEPTOR ANTAGONIST - Novel compounds, or pharmaceutically-acceptable salts, tautomers or prodrugs thereof, of Formula I | 2009-06-04 |
20090143406 | New Phenylpiperazine - The invention relates to a novel group of phenylpiperazines having interesting pharmacological properties such as a high affinity for the dopamine D | 2009-06-04 |
20090143407 | ISOXAZOLO-PYRAZINE DERIVATIVES - The invention relates to isoxazolo-pyrazine derivatives and their pharmaceutically acceptable salts having affinity and selectivity for the GABA A α5 receptor binding site, their manufacture, and pharmaceutical compositions containing them. The compounds of present invention are inverse agonists of GABA A α5. The invention also relates to methods for enhancing cognition and for treating cognitive disorders like Alzheimer's disease. | 2009-06-04 |
20090143408 | COMPOSITIONS AND METHODS FOR INHIBITING CYTOCHROME P450 2D6 - Methods of inhibiting cytochrome P450 2D6 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450 2D6. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 2D6 enzymes. | 2009-06-04 |
20090143409 | 3-PYRIDINECARBOXAMIDE DERIVATIVES AS HDL-CHOLESTEROL RAISING AGENTS - The present invention relates to a method of raising HDL cholesterol comprising administering to a patient in need thereof a compound of the formula | 2009-06-04 |
20090143410 | Isoxazolines for Controlling Invertebrate Pests - Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, | 2009-06-04 |
20090143411 | Thiophens and Their Use as Anti-Tumor Agents - The present invention provides novel compounds and pharmaceutical compositions thereof, as well as methods for using the compounds and pharmaceutical compositions for treating tumors. Examples of specific tumor types that the compounds may be used to treat include, but are not limited to sarcomas, melanomas, neuroblastomas, carcinomas (including but not limited to lung, renal cell, ovarian, liver, bladder, and pancreatic carcinomas), and mesotheliomas. | 2009-06-04 |
20090143412 | FUROPYRIDINE AND FUROPYRIMIDINE DERIVATIVES FOR THE TREATMENT OF HYPER-PROLIFERATIVE DISORDERS - This invention relates to a compound of Formula I | 2009-06-04 |