33rd week of 2010 patent applcation highlights part 25 |
Patent application number | Title | Published |
20100210519 | PEPTIDE SLOW-RELEASE FORMULATIONS - A composition for the delayed delivery of a peptide active agent comprising; i) a salt of said peptide active agent comprising at least one positively charged peptide ion and at least one negatively charged counter-ion ii) a sustained-release delivery vehicle. Wherein said at least one negatively charged counter-ion is a halide ion, preferably a chloride or bromide ion. | 2010-08-19 |
20100210520 | REGULATION OF FUNCTION OF ANGIOPOIETIN - Pharmaceutical compositions that comprise a pharmaceutically acceptable carrier and either a therapeutically effective amount of an ECM-binding fragment of Ang-1 protein that comprises SEQ ID NO:1 and/or SEQ ID NO:2 or a homologous peptide thereof and pharmaceutical compositions that comprise a pharmaceutically acceptable carrier and a vector comprising a nucleic acid molecule that comprises the nucleotide sequence that encodes an ECM-binding fragment of Ang-1 protein that comprises SEQ ID NO:1 and/or SEQ ID NO:2 or a homologous peptide thereof are disclosed. Methods of using such compositions to treat individuals suspected of having coronary artery disease, vascular disease or a condition involving ischemia and to promote angiogenesis, endothelial survival and maintaining vascular integrity are disclosed. Methods to identify compounds that modulates binding of Ang-1 to ECM are disclosed. Pharmaceutical compositions which comprise a therapeutically effective amount of Ang-2 protein and/or a vector comprising a nucleic acid molecule that comprises the nucleotide coding sequence of Ang-2 and methods of using such compositions to treat individuals suspected of having cancer are disclosed. | 2010-08-19 |
20100210521 | Compositions and methods for modulating ampa receptor-mediated excitotoxicity - The present invention provides AMPAR excitotoxicity mediating polypeptides comprising the GluR2 NT1-3-2 (Y142-K172) amino acid sequence (SEQ ID NO:1) or the GAPDH(2-2-1-1) (I221-E250) amino acid sequence (SEQ ID NO:2). Also disclosed are nucleotide sequences encoding the polypeptides, methods of inhibiting GAPDH association with the GluR2 subunit or p53. Methods of inhibiting AMPA receptor mediated excitotoxicity using the polypeptides and nucleic acids are also disclosed. | 2010-08-19 |
20100210522 | METHOD FOR DETERMINING PRESENCE OF CANCER IN A SAMPLE BY ASSAYING FOR EXPRESSION OF DPPA-2 NUCLEOTIDE SEQUENCES - The invention relates to the discovery of known molecule “ESCA/DPPA-2” and a so-called “cancer-testis antigen.” ESCA/DPPA-2 is also a possible cancer stem cell marker. One can determine presence of cancer by assaying for the molecule, and also prevent or treat cancer via administration of the molecule. | 2010-08-19 |
20100210525 | COMBINED PREPARATION OF A THIAZIDE DIURETIC AND A LOOP DIURETIC - The specific molecular basis of the interaction between talin and integrin β | 2010-08-19 |
20100210526 | ORAL ADMINISTRATION OF A CALCITONIN - The invention is directed to a method of administering pharmaceutical compositions comprising peptide drugs such as a calcitonin in combination with one or more oral delivery agents, together with an amount of a liquid, and method of treatment of disorders responsive to the action of peptide drugs such as a calcitonin employing such method of administration so as to enhance the oral bioavailability of a calcitonin. The methods of the invention increase the oral absorption and systemic bioavailability of peptide drugs, such as a calcitonin. | 2010-08-19 |
20100210527 | PRO- AND ANTI-ANGIOGENIC TREATMENTS - The invention provides a method of selectively pro-oranti-angiogenic treatment of a mammalian subject, comprising site-specific control of alternative splicing during processing of VEGF pre-mRNA transcribed from the C terminal exon 8 of the VEGF gene using controlling agents for the splicing, wherein one or more controlling agent which favours proximal splice site (PSS) splicing in said processing is used in the pro-angiogenic treatment and one or more controlling agent which favours distal splice site (DSS) splicing in said processing is used in the anti-angiogenic treatment. | 2010-08-19 |
20100210528 | Compositions, methods and uses for inhibition and/or treatment of influenza infection - Embodiments of the present invention illustrate methods and compositions for treating medical disorders. In certain embodiments, compositions and methods relate to reducing or inhibiting a the onset or development of a viral disorder. | 2010-08-19 |
20100210533 | USE OF UROCORTIN AND CORTICOTROPIN-RELEASING FACTOR AS THERAPEUTIC AGENTS - The present invention is directed to the use of the peptide compound Asp-Asn-Pro-Ser-Leu-Ser-Ile-Asp-Leu-Thr-Phe-His-Leu-Leu-Arg-Thr-Leu-Leu-Glu-Leu-Ala-Arg-Thr-Gln-Ser-Gln-Arg-Glu-Arg-Ala-Glu-Gln-Asn-Arg-Ile- Ile-Phe-Asp-Ser-Val-NH | 2010-08-19 |
20100210534 | USE OF A PEPTIDE AS A THERAPEUTIC AGENT - The present invention is directed to the use of the peptide compound Ala-Ala-Val-Ala-Leu-Leu-Pro-Ala-Val-Leu-Leu-Ala-Leu-Leu-Ala-Pro-Val-Gln-Arg-Lys-Arg-Gln-Lys-Leu-Met-Pro-OH as a therapeutic agent for the prophylaxis and/or treatment of cancer, autoimmune diseases, fibrotic diseases, inflammatory diseases, neurodegenerative diseases, infectious diseases, lung diseases, heart and vascular diseases and metabolic diseases. Moreover the present invention relates to pharmaceutical compositions preferably in form of a lyophilisate or liquide buffer solution or artificial mother milk formulation or mother milk substitute containing the peptide Ala-Ala-Val-Ala-Leu-Leu-Pro-Ala-Val-Leu-Leu-Ala-Leu-Leu-Ala-Pro-Val-Gln-Arg-Lys-Arg-Gln-Lys-Leu-Met-Pro-OH optionally together with at least one pharmaceutically acceptable carrier, cryoprotectant, lyoprotectant, excipient and/or diluent. | 2010-08-19 |
20100210539 | USE OF PEPTIDE LL-37 AS A THERAPEUTIC AGENT - The present invention is directed to the use of the peptide compound Leu-Leu-Gly-Asp-Phe-Phe-Arg-Lys-Ser-Lys-Glu-Lys-Ile-Gly-Lys-Glu-Phe-Lys-Arg-Ile-Val-Gln-Arg-Ile-Lys-Asp-Phe-Leu-Arg-Asn-Leu-Val-Pro-Arg-Thr-Glu-Ser-NH | 2010-08-19 |
20100210540 | USE OF THE PEPTIDE COMBINATION THYMOSIN BETA 4 AND DELTA SLEEP INDUCING PEPTIDE AS A THERAPEUTIC AGENT - The present invention is directed to the use of the combination of the peptide compounds Ac-Ser-Lys-Pro-Asp-Met-Ala-Glu-Ile-Glu-Lys-Phe-Asp-Lys-Ser-Lys-Leu-Lys-Lys-Thr-Glu-Thr-Gln-Glu-Lys-Asn-Pro-Leu-Pro-Ser-Lys-Glu-Thr-Ile-Glu-Gln-Glu-Lys-Gln-Ala-Gly-Glu-Ser-OH and Trp-Ala-Gly-Gly-Asp-Ala-Ser-Gly-Glu-OH as a therapeutic combination for prophylaxis and/or treatment of cancer, a heart and vascular disease, an infectious disease, a fibrotic disease, an inflammatory disease, a neurodegenerative disease, or an autoimmune disease. | 2010-08-19 |
20100210543 | Aldehyde-Tagged Protein-Based Drug Carriers and Methods of Use - The disclosure provides aldehyde-tagged protein carriers that can be covalently and site-specifically bound to drug to provide a drug-containing scaffold. The invention also encompasses methods of production of such drug-containing scaffolds and intermediates, as well as methods of use. | 2010-08-19 |
20100210544 | PEPTIDES AND PHARMACEUCAL COMPOSITIONS FOR TREATING CONNECTIVE TISSUE - Provided is a pharmaceutical composition for sequestering cells in connective tissue. The composition includes a biocompatible scaffolding to which one or more peptides or proteins are linked. The peptides or proteins have an amino acid sequence that is a subsequence of human ficolin and are capable of binding the cells to be sequestered. The pharmaceutical composition can be used in the treatment of connective tissue, and can be used as a dermal filler. | 2010-08-19 |
20100210547 | METHOD FOR THE PRODUCTION OF CONJUGATES OF INSULIN-LIKE GROWTH FACTOR-1 AND POLY(ETHYLENE GLYCOL) - The present invention relates to a fusion protein comprising IGF-I or an IGF-I variant N-terminally linked to the C-terminus of a propeptide. The invention relates also to a method involving the use of the aforementioned fusion protein in the production of a lysine-PEGylated IGF-I or IGF-I variant. The method comprises the steps of cultivating a prokaryotic host cell comprising an expression vector containing a nucleic acid encoding the fusion protein and causing the cell to express the fusion protein, recovering and PEGylating said fusion protein, cleaving said PEGylated fusion protein with IgA protease, and recovering lysine-PEGylated IGF-I or IGF-I variant. The invention relates also to a lysine-PEGylated IGF-I or IGF-I variant produced using the above method. In addition, the invention relates to a method for treating a neurodegenerative disorders like Alzheimer's Disease using the lysine-PEGylated IGF-I or IGF-I variant and a composition comprising the lysine-PEGylated IGF-I or IGF-I variant. | 2010-08-19 |
20100210548 | Novel Bacillus Thuringiensis Crystal Polypeptides, Polynucleotides, and Compositions Thereof - The present invention provides insecticidal polypeptides related to | 2010-08-19 |
20100210553 | USE OF THE PEPTIDE ASN-ASP-ASP-CYS-GLU- LEU-CYS-VAL-ASN-VAL-ALA-CYS-THR-GLY-CYS-LEU ALONE OR IN COMBINATION WITH THE PEPTIDE THR-THR-SER-GLN-VAL- ARG-PRO-ARG AS A THERAPEUTIC AGENT - The present invention is directed to the use of the peptide compound Asn-Asp-Asp-Cys-Glu-Leu-Cys-Val-Asn-Val-Ala-Cys-Thr-Gly-Cys-Leu-OH or its combination with the peptide Thr-Thr-Ser-Gln-Val-Arg-Pro-Arg-OH as a therapeutic agent for the prophylaxis and/or treatment of cancer, autoimmune diseases, fibrotic diseases, inflammatory diseases, neurodegenerative diseases, infectious diseases, lung diseases, heart and vascular diseases and metabolic diseases. Moreover the present invention relates to pharmaceutical compositions preferably in form of a lyophilisate or liquid buffer solution or artificial mother milk formulation or mother milk substitute containing the peptide Asn-Asp-Asp-Cys-Glu-Leu-Cys-Val-Asn-Val-Ala-Cys-Thr-Gly-Cys-Leu-OH optionally together with at least one pharmaceutically acceptable carrier, cryoprotectant, lyoprotectant, excipient and/or diluent. | 2010-08-19 |
20100210554 | THERAPEUTIC USES OF GASTRIN- 1 AND G- PEN-GRGDSPCA - The present invention is directed to the use of the peptide compound Pyr-Gly-Pro-Trp-Leu-Glu-Glu-Glu-Glu-Glu-Ala-Tyr-Gly-Trp-Met-Asp-Phe-NH2 as a therapeutic agent for the prophylaxis and/or treatment of cancer, autoimmune diseases, fibrotic diseases, inflammatory diseases, neurodegenerative diseases, infectious diseases, lung diseases, heart and vascular diseases and metabolic diseases. Moreover the present invention relates to pharmaceutical compositions preferably in form of a lyophilisate or liquid buffer solution or artificial mother milk formulation or mother milk substitute containing the peptide Pyr-Gly-Pro-Trp-Leu-Glu-Glu-Glu-Glu-Leu-Glu-Glu-Glu-Glu-Glu-Ala-Tyr-Gly-Trp-Met-Asp-Phe-NH2 optionally together with at least one pharmaceutically acceptable carrier, cryoprotectant, lyoprotectant, excipient and/or diluent. | 2010-08-19 |
20100210555 | USE OF A LAMININ PEPTIDE AS A THERAPEUTIC AGENT - The present invention is directed to the use of the peptide compound Cys-Ser-Arg-Ala-Arg-Lys-Gln-Ala-Ala-Ser-Ile-Lys-Val-Ala-Val-Ser-Ala-Asp-Arg-OH as a therapeutic agent for the prophylaxis and/or treatment of cancer, autoimmune diseases, fibrotic diseases, inflammatory diseases, neurodegenerative diseases, infectious diseases, lung diseases, heart and vascular diseases and metabolic diseases. Moreover the present invention relates to pharmaceutical compositions preferably in form of a lyophilisate or liquid buffer solution or artificial mother milk formulation or mother milk substitute containing the peptide Cys-Ser-Arg-Ala-Arg-Lys-Gln-Ala-Ala-Ser-Ile-Lys-Val-Ala-Val-Ser-Ala-Asp-Arg-OH optionally together with at least one pharmaceutically acceptable carrier, cryoprotectant, lyoprotectant, excipient and/or diluent. | 2010-08-19 |
20100210556 | USE OF A PEPTIDE AS A THERAPEUTIC AGENT - The present invention is directed to the use of the peptide compound Ala-Ile-Phe-Ile-Phe-Ile-Arg-Trp-Leu-Leu-Lys-Leu-Gly-His-His-Gly-Arg-Ala-Pro-Pro-OH as a therapeutic agent for the prophylaxis and/or treatment of cancer, autoimmune diseases, fibrotic diseases, inflammatory diseases, neurodegenerative diseases, infectious diseases, lung diseases, heart and vascular diseases and metabolic diseases. Moreover the present invention relates to pharmaceutical compositions preferably in form of a lyophilisate or liquid buffer solution or artificial mother milk formulation or mother milk substitute containing the peptide Ala-Ile-Phe-Ile-Phe-Ile-Arg-Trp-Leu-Leu-Lys-Leu-Gly-His-His-Gly-Arg-Ala-Pro-Pro-OH optionally together with at least one pharmaceutically acceptable carrier, cryoprotectant, lyoprotectant, excipient and/or diluent. | 2010-08-19 |
20100210561 | USE OF PEPTIDE AS A THERAPEUTIC AGENT - The present invention is directed to the use of the peptide compound Tyr-D-Cys(tBu)-Gly-Phe-Leu-Thr(tBu)-OH as a therapeutic agent for the prophylaxis and/or treatment of cancer, autoimmune diseases, fibrotic diseases, inflammatory diseases, neurodegenerative diseases, infectious diseases, lung diseases, heart and vascular diseases and metabolic diseases. Moreover the present invention relates to pharmaceutical compositions preferably in form of a lyophilisate or liquide buffer solution or artificial mother milk formulation or mother milk substitute containing the peptide Tyr-D-Cys(tBu)-Gly-Phe-Leu-Thr(tBu)-OH optionally together with at least one pharmaceutically acceptable carrier, cryoprotectant, lyoprotectant, excipient and/or diluent. | 2010-08-19 |
20100210562 | USE OF IL-1 RECEPTOR PEPTIDE, ALONE OR IN COMBINATION WITH D-ALA-GLN-OCTADECYL ESTER, AS A THERAPEUTIC AGENT - The present invention is directed to the use of the peptide compound Lys-lle-Cys-lle-Arg-lle-Gln-lle-Ser-OH as a therapeutic agent for the prophylaxis and/or treatment of cancer, autoimmune diseases, fibrotic diseases, inflammatory diseases, neurodegenerative diseases, infectious diseases, lung diseases, heart and vascular diseases and metabolic diseases. Moreover the present invention relates to pharmaceutical compositions preferably in form of a lyophilisate or liquide buffer solution or artificial mother milk formulation or mother milk substitute containing the peptide Lys-lle-Cys-lle-Arg-lle-Gln-lle-Ser-OH optionally together with at least one pharmaceutically acceptable carrier, cryoprotectant, lyoprotectant, excipient and/or diluent. | 2010-08-19 |
20100210565 | METHODS AND APPARATUS FOR THE ENHANCED DELIVERY OF PHYSIOLOGIC AGENTS TO TISSUE SURFACES - Apparatus and methods deliver physiologically active agents in the presence of adjuvant gases. The adjuvant gases can enhance the effectiveness of the drug, lower the dosage of drug or concentration of drug necessary to achieve a therapeutic result, or both. Exemplary adjuvant gases include carbon dioxide, nitric oxide, nitrous oxide, and dilute acid gases. | 2010-08-19 |
20100210566 | AZAPEPTIDES AS CD36 BINDING COMPOUNDS - An azapeptide derivative of growth hormone releasing peptide (GHRP) of Formula I: A-(Xaa) | 2010-08-19 |
20100210567 | USE OF A TUFTSIN AS A THERAPEUTIC AGENT - The present invention is directed to the use of the peptide compound Thr-Lys-Pro-Arg-OH as a therapeutic agent for the prophylaxis and/or treatment of cancer, autoimmune diseases, fibrotic diseases, inflammatory diseases, neurodegenerative diseases, infectious diseases, lung diseases, heart and vascular diseases and metabolic diseases. Moreover the present invention relates to pharmaceutical compositions preferably in form of a lyophilisate or liquid buffer solution or artificial mother milk formulation or mother milk substitute containing the peptide Thr-Lys-Pro-Arg-OH optionally together with at least one pharmaceutically acceptable carrier, cryoprotectant, lyoprotectant, excipient and/or diluent. | 2010-08-19 |
20100210568 | THYROTROPIN RELEASING HORMONE FOR THERAPEUTIC APPLICATIONS - The present invention is directed to the use of the peptide compound Pyr-His-Pro-NH | 2010-08-19 |
20100210571 | TOPICAL FORMULATIONS FOR TREATMENT OF SKIN DISORDERS - Topical compositions and methods of using same for treating skin disorders or conditions comprising a storage-stable mixture of a benzoyl peroxide dispersion, clindamycin or pharmaceutically acceptable salts or esters thereof, and a pharmaceutically acceptable carrier. | 2010-08-19 |
20100210572 | HYDROLYSATE OF CROCIN - The present invention relates to a composition derived from the hydrolysate of plant containing crocin or the derivatives thereof. The composition includes a significant amount of crocetin monoester. The present invention also provides a method to hydrolyze crocin existing in a plant extract, and further relates to the use. | 2010-08-19 |
20100210573 | COMPOUND AND COMPOSITIONS FOR TREATMENT OF DISEASE - The present invention relates to flavonoids and to flavonoid-containing compositions for use in the treatment of parasites. | 2010-08-19 |
20100210574 | AVERMECTIN B1 AND AVERMECTIN B1 MONOSACCHARIDE DERIVATIVES HAVING AN ALKOXYMETHYL SUBSTITUENT IN THE 4"-OR 4'-POSITION - What is described are a compound of the formula | 2010-08-19 |
20100210577 | CYCLIC CARBOXYLIC ACID RHODANINE DERIVATIVES FOR THE TREATMENT AND PREVENTION OF TUBERCULOSIS - Disclosed are methods for the prevention or treatment of tuberculosis in a subject infected with | 2010-08-19 |
20100210578 | Prevention/Treatment of Ichthyosis Vulgaris, Atopy and Other Disorders - The present invention relates to the prevention/treatment of ichthyosis vulgaris (IV), atopy and potentially other disorders associated with loss-of-function mutations in the filaggrin gene sequence. The prevention/therapy is based on the use of agents which enable the host's translational machinery to read through a nonsense mutation found in a mutant allele of the filaggrin gene. | 2010-08-19 |
20100210583 | NOVEL ANTIFOLATE COMBINATION THERAPIES - A method of administering an antifolate to a mammal in need thereof, comprising administering an effective amount of said antifolate in combination with a methylmalonic acid lowering agent. | 2010-08-19 |
20100210584 | LIQUID OR PASTE COMPOSITIONS INTENDED TO PROVIDE ELEMENTS ESSENTIAL FOR THE SYNTHESIS AND FORMATION OF PROTEOGLYCANS, IN PARTICULAR, FOR THE TREATMENT OF CARTILAGE DEGRADATION - The invention relates to the field of pharmaceuticals, dietary supplements and food and, more specifically, to the field of dietary supplements intended for the treatment of degradation of cartilage of any origin. The invention relates to liquid or paste compositions based on glucosamin and chondroitin sulphate, intended to provide elements essential for the synthesis and formation of proteoglycans, in which the chondroitin sulphate/glucosamin combination is stabilised with the addition of carboxylic acids such that the pH of the medium is between 2 and 5 and the chemical degradation rate of the active substances is less than 10% when stored at 25° C. and 60% relative humidity for 10 months for doses of between 300 and 2400 mg chondroitin sulphate and between 500 and 3000 mg glucosamin. The invention is suitable for the treatment of cartilage degradation and, more specifically, arthrosis. | 2010-08-19 |
20100210587 | Swellable Crosslinked Hyaluronan Powder And Method For Producing The Same - The present invention is provides a crosslinked hyaluronan powder excellent in swellability in water and a method for simply producing the same. A method for producing the swellable crosslinked hyaluronan powder is characterized by comprising mixing a crosslinking agent with a hyaluronan powder in a state dispersed in a liquid medium containing a monovalent alcohol having 1 to 4 carbon atoms and a solubility of the hyaluronan powder of less than 0.1 g/L to cause a crosslinking reaction. Also, the swellable crosslinked hyaluronan powder produced by the method has a swelling ratio in water of 500% or more. | 2010-08-19 |
20100210588 | Hyaluronic Acid Linked with a Polymer of an Alpha Hydroxy Acid - The invention concerns a product comprising hyaluronic acid or a salt thereof, wherein the hyaluronic acid has been partially or fully linked or crosslinked with a polymer of an alpha hydroxy acid. The invention also concerns manufacture of the product, uses of the product of the invention in the field of biodegradable plastic materials for the preparation of sanitary and surgical articles, in the pharmaceutical and cosmetic fields; including the various articles made with the same in such fields. | 2010-08-19 |
20100210589 | METHOD FOR IMPROVING HEPATIC FUNCTION - An object of the present invention is to provide a means for improving hepatic function of mammals including humans to normal condition. The present invention achieves the above object by providing a hepatic function-improving agent comprising α-glucosyl-hesperidin as an effective ingredient. | 2010-08-19 |
20100210590 | COMPOSITIONS AND TREATMENTS FOR SEIZURE-RELATED DISORDERS - The present invention relates to therapeutic and/or prophylactic uses of pyridazine compounds and to pharmaceutical compositions containing one or more of these compounds as an active component for treating a disorder characterized by conduction disturbances, electroconvulsions and/or seizures, in particular epilepsy, more particularly pediatric epilepsy. In an aspect of the invention, the pyridnsine compound has the Formula (Ia) or (Ib) wherein R | 2010-08-19 |
20100210593 | Pyridine- and Pyrimidinecarboxamides as CXCR2 Modulators - There is disclosed pyridine- and pyrimidinecarboxamide compounds useful as pharmaceutical agents, synthesis processes, and pharmaceutical compositions which include pyridine- and pyrimidinecarboxamides compounds. More specifically, there is disclosed a genus of CXCR2 inhibitor compounds that are useful for treating a variety of inflammatory and neoplastic disorders. | 2010-08-19 |
20100210594 | SUBSTITUTED ARYLSULFONYLAMINOMETHYLPHOSPHONIC ACID DERIVATIVES, THEIR PREPARATION AND THEIR USE IN THE TREATMENT OF TYPE I AND II DIABETES MELLITUS - The present invention relates to substituted arylsulphonylaminomethyl-phosphonic acid derivatives of general formula | 2010-08-19 |
20100210601 | FLEA CONTROL METHOD - This invention relates to a method of controlling or preventing maturation of fleas on an animal or its environment comprising applying to a warm blooded animal or its environment a composition comprising an developmentally disruptive amount of a compound of Formula 1 or an N-oxide, or a salt thereof. | 2010-08-19 |
20100210602 | PhoU (PerF), A PERSISTENCE SWITCH INVOLVED IN PERSISTER FORMATION AND TOLERANCE TO MULTIPLE ANTIBIOTICS AND STRESSES AS A DRUG TARGET FOR PERSISTER BACTERIA - The PhoU protein is a widely expressed protein in bacteria, but not in eukaryotes. The PhoU protein is required for persister formation in bacteria. The invention includes compositions to reduce persister formation and their use as therapeutic agents. The invention further includes methods for identification of compounds to reduce persister formation. The invention further includes kits for the identification of agents that modulate the activity and expression of PhoU. | 2010-08-19 |
20100210603 | NOVEL SULFONAMIDE INHIBITORS OF ASPARTYL PROTEASE - The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity. | 2010-08-19 |
20100210604 | ZWITTERION SOLUTION FOR LOW-VOLUME THERAPEUTIC DELIVERY - A formulation is provided that includes a volume of an aqueous multivalent physiological ion solution compatible with cerebrospinal fluid containing at least one divalent cation of magnesium or calcium, and at least one anion of carbonate or phosphate, and having a pH between 6.5 and 8.0. A zwitterionic therapeutic agent other than baclofen is dissolved the solution to achieve higher concentration or ease of solution and/or storage relative to therapeutic saline solutions of the same agent. A process of delivering a zwitterionic therapeutic agent into a subject is provided that includes dissolving a therapeutic amount of the zwitterionic therapeutic agent in a volume of artificial cerebrospinal fluid to form a stable formulation. The solution is then administered to the subject using an intrathecal pump. | 2010-08-19 |
20100210607 | HYDROGEN SULFIDE DERIVATIVES OF NON-STEROIDAL ANTI-INFLAMMATORY DRUGS - The present invention relates to derivatives of non-steroidal anti-inflammatory drugs (NSAIDs) having improved anti-inflammatory properties useful in the treatment of inflammation, pain and fever. More particularly, NSAIDs are derivatized with a hydrogen sulfide (H | 2010-08-19 |
20100210608 | THERAPEUTIC TREATMENT - The invention describes the use of betaine for treating and preventing arterites. The invention also describes an orally administered composition for treating arterites and, in particular, intermittent claudication, said composition containing, as an active ingredient, an active therapeutic quantity of betaine glycine by single dose. The invention particularly describes a medicament provided for treating a patient suffering from an intermittent claudication caused by peripheral circulatory disorders such as arteriosclerosis obliterans or by thromboangiitis obliterans. | 2010-08-19 |
20100210611 | COMBINATION THERAPY - The present invention provides inhalation compositions comprising montelukast acid and a second active agent selected from a PDE4 inhibitor and an inhaled corticosteroid. Also provided is a method for the treatment of respiratory disorders such as asthma using such compositions. | 2010-08-19 |
20100210612 | DETECTION OF ESR1 AMPLIFICATION IN ENDOMETRIUM CANCER AND OVARY CANCER - The present invention relates to an in-vitro method of identifying a tumor resulting from a proliferative disease of the endometrium or ovary as responsive to anti-estrogen treatment. Further, the invention relates to an in-vitro method of identifying a candidate patient with a proliferative disease of the endometrium or ovary as suitable for anti-estrogen treatment. In a further aspect, the invention provides an in-vitro method of identifying an individual with a non-cancerous proliferative disease of the endometrium or ovary who is at risk of developing endometrial or ovarian cancer. The invention also provides kits for performing the above methods. | 2010-08-19 |
20100210614 | COMPOSITIONS AND METHODS FOR ENHANCING CORTICOSTEROID DELIVERY - The present invention comprises a composition, method of enhancing potency and method of delivering corticosteroids in a vehicle comprising at least two penetration enhancers, and solvents and emulsifiers. The propylene glycol and penetration enhancers are present in ratio to the total of the propylene glycol, penetration enhancers, and solvents and emulsifiers of at least about 0.70. | 2010-08-19 |
20100210621 | CRYSTALLINE POLYMORPHIC FORM 631 - A new polymorphic form of 3-{[5-(azetidin-1-ylcarbonyl)pyrazin-2-yl]oxy}-5-{[(1S)-1-methyl-2-(methyloxy)ethyl]oxy}-N-(5-methylpyrazin-2-yl)benzamide, processes for making it and its use as an activator of glucokinase are described. | 2010-08-19 |
20100210622 | HETEROCYCLIC COMPOUNDS AND METHODS OF USE - In one aspect, the present invention provides for a compound of Formula I | 2010-08-19 |
20100210623 | THERAPEUTIC COMPOUNDS - The present invention relates to pyrazine substituted pyrrolopyridines which are inhibitors of JAK kinases (JAK1, JAK2, JAK3 and/or TYK2) and/or PDK1 and are thus useful for the treatment of myeloproliferative disorders or cancer. | 2010-08-19 |
20100210624 | ARYLOXY- AND HETEROARYLOXY-SUBSTITUTED TETRAHYDROBENZAZEPINES AND USE THEREOF TO BLOCK REUPTAKE OF NOREPINEPHRINE, DOPAMINE, AND SEROTONIN - The aryloxy- and heteroaryloxy-substituted tetrahydrobenzazepine derivative compounds of the present invention are represented by formulae (I) (A-E) having the following structure where the carbon atom designated * is in the R or S configuration and the substituents X and R | 2010-08-19 |
20100210629 | 1,6-DIHYDRO-1,3,5,6-TETRAAZA-AS-INDACENE BASED TRICYCLIC COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS COMPRISING SAME - The present invention provides for tricyclic compounds having the formula (I), | 2010-08-19 |
20100210630 | Diamine Derivatives as Inhibitors of Leukotriene A4 Hydrolase - This invention is directed to compounds of formula (I): | 2010-08-19 |
20100210633 | CARBOXAMIDE COMPOUNDS AND THEIR USE - Chemokine receptor antagonists, in particular, compounds of Formula (I) that act as antagonists of the chemokine CCR2 receptor, including pharmaceutical compositions and uses thereof to treat or prevent diseases associated with monocyte accumulation, lymphocyte accumulation or leukocyte accumulation are described herein. | 2010-08-19 |
20100210634 | Certain Chemical Entities, Compositions and Methods - Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure. | 2010-08-19 |
20100210635 | RENIN INHIBITORS - Compounds, pharmaceutical compositions, kits and methods are provided for use with Renin that comprise a compound selected from the group consisting of: wherein the variables are as defined herein. | 2010-08-19 |
20100210636 | BENZOXAZINONE DERIVATIVE | 2010-08-19 |
20100210637 | HETEROARYLOXY NITROGENOUS SATURATED HETEROCYCLIC DERIVATIVE - Provided are compounds of a formula (I) and their pharmaceutically-acceptable salts: | 2010-08-19 |
20100210638 | 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. | 2010-08-19 |
20100210641 | Organic Compounds - Compounds of formula I: in free or salt or solvate form, where R | 2010-08-19 |
20100210642 | ACETYLENYL-PYRAZOLO-PYRIMIDINE DERIVATIVES - The present invention relates to compounds of formula (I): | 2010-08-19 |
20100210647 | INDOLE COMPOUNDS AS AN INHIBITOR OF CELLULAR NECROSIS - The present invention relates to new indole compounds, pharmaceutically acceptable salts or isomers thereof which are useful for the prevention or treatment of cellular necrosis and necrosis-associated diseases. The present invention also relates to a method and a composition for the prevention or treatment of cellular necrosis and necrosis-associated diseases, comprising said indole compounds as an active ingredient. | 2010-08-19 |
20100210648 | PYRAZOLYLAMINOPYRIMIDINE DERIVATIVES USEFUL AS TYROSINE KINASE INHIBITORS - This invention relates to novel compounds having the formula (I): | 2010-08-19 |
20100210655 | NOVEL sEH INHIBITORS AND THEIR USE - The invention is directed to novel sEH inhibitors and their use in the treatment of diseases mediated by the sEH enzyme. Specifically, the invention is directed to compounds according to Formula I: | 2010-08-19 |
20100210656 | NOVEL sEH INHIBITORS AND THEIR USE - The invention is directed to novel sEH inhibitors and their use in the treatment of diseases mediated by the sEH enzyme. Specifically, the invention is directed to compounds according to Formula I: | 2010-08-19 |
20100210657 | Bicyclic Benzamides of 3-or 4-Substituted 4-(Aminomethyl)-Piperidine Derivatives - The present invention of compounds of formula (I) | 2010-08-19 |
20100210661 | STAT3/5 ACTIVATION INHIBITOR - An object of the present invention is to provide a STAT3/5 activation inhibitor. The present invention provides a STAT3/5 activation inhibitor containing an aromatic compound represented by the general formula or a salt thereof as an active ingredient: | 2010-08-19 |
20100210662 | INDOL-2-ONE DERIVATIVES DISUBSTITUTED IN THE 3-POSITION, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The present invention relates to 3-disubstituted indol-2-one derivatives, to their preparation and to their therapeutic application. | 2010-08-19 |
20100210663 | Hybrid 2-Aminotetralin and Aryl-Substituted Piperazine Compounds and their Use in Altering CNS Activity - Hybrid compounds containing an aminotetralin moiety or a heterocyclic and/or open chain analog thereof linked through an alkylene group to an aryl ring system-substituted piperidiene moiety exhibit high levels of CNS activity, in some cases exhibiting especially high relative binding efficiencies between D3 and D2 dopaminergic receptor subtypes. | 2010-08-19 |
20100210664 | BENZENESULFONAMIDE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECEPTOR - The invention relates to compounds of the formula R | 2010-08-19 |
20100210667 | IMIDAZO [1, 2-C] PYRIMIDIN-2-YLMETHYLPIPERIDINES AS OREXIN RECEPTOR ANTAGONISTS - Disclosed are imidazo[1,2-c]pyrimidin-2-ylmethyl substituted piperidine derivatives having the formula: | 2010-08-19 |
20100210673 | PYRIMIDYLAMINOBENZAMIDE DERIVATIVES FOR SYSTEMIC MASTOCYTOSIS - The present invention relates to the use of pyrimidylaminobenzamide derivatives for the preparation of a drug for the treatment of systemic mastocytosis. | 2010-08-19 |
20100210674 | Spiroindolinone Derivatives - There are provided compounds of the formula | 2010-08-19 |
20100210675 | SOLVENT-FREE CRYSTALLINE FORM OF NALTREXONE - Solvent-free crystalline polymorphic form of naltrexone, characterized in that it has the XRD data listed in Table 1, and a method for the preparation of this polymorphic form; and a method for converting this polymorphic form of naltrexone into a known polymorphic form of naltrexone. | 2010-08-19 |
20100210676 | Chemically Modified Small Molecules - Methods of modifying the rate of systemic absorption of a drug administered to a subject by a pulmonary route, the method comprising covalently conjugating a hydrophilic polymer to a drug, wherein the drug has a half-life of elimination from the lung of less than about 180 minutes, to form a drug-polymer conjugate, wherein the drug-polymer conjugate has a net hydrophilic character and a weight average molecular weight of from about 50 to about 20,000 Daltons, and wherein the half-life of elimination from the lung of the drug-polymer conjugate is at least about 1.5-fold greater than the half-life of elimination from the lung of the drug, wherein the half-life of elimination from the lung is measured by bronchoalveolar lavage followed by assaying residual lung material. | 2010-08-19 |
20100210679 | PREVENTIVE AND THERAPEUTIC MEDICAMENT FOR GASTROESOPHAGEAL REFLUX DISEASE - The compound of the following formula: | 2010-08-19 |
20100210680 | TRICYCLIC HETEROCYCLIC DERIVATIVES - The present invention relates to a tricyclic heterocyclic derivative of Formula (I) wherein the variables are as defined in the specification. The present invention further relates to pharmaceutical compositions comprising these compounds and to their use in therapy, in particular for the treatment of serotonin-mediated disorders such as obesity, schizophrenia and cognitive dysfunction. | 2010-08-19 |
20100210685 | Novel Substituted Indoles | 2010-08-19 |
20100210686 | THERAPEUTIC AGENTS USEFUL FOR TREATING PAIN - Piperidine Compounds; compositions comprising a Piperidine Compound; and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Piperidine Compound are disclosed. In one embodiment, the Piperidine Compound has the formula: | 2010-08-19 |
20100210687 | Compounds which have activity at M1 receptor and their uses in medicine - Compounds of formula (I) or a salt thereof are provided: | 2010-08-19 |
20100210688 | Novel Benzothiazolone Derivatives - The present invention provides compounds of formula (I) wherein e, R | 2010-08-19 |
20100210689 | THERAPEUTIC SUBSTITUTED CHLOROCYCLOPENTANOLS - Disclosed herein is a compound having a formula | 2010-08-19 |
20100210690 | N-(PYRAZOLE-3-YL)-BENZAMIDE DERIVATIVES AS GLUCOKINASE ACTIVATORS - Novel heterocyclic compounds of the formula I | 2010-08-19 |
20100210699 | IMIDAZOLIDINE DERIVATIVES, USES THEREFOR, PREPARATION THEREOF AND COMPOSITIONS COMPRISING SUCH - Compounds of formula (I): | 2010-08-19 |
20100210700 | METHODS OF TREATMENT USING INTRAVENOUS FORMULATIONS COMPRISING TEMOZOLOMIDE - This invention relates to methods and drug products for treating proliferative disorders using intravenous formulations comprising temozolomide over a specific infusion time. These methods and drug products are particularly well-suited for patients who cannot swallow oral formulations. These methods and drug products also afford an added convenience to patients who are already receiving other therapeutic treatments. | 2010-08-19 |
20100210701 | Novel Forms of Bendamustine Free Base - Novel polymorphic forms of bendamustine free base are described, including amorphous bendamustine free base, six anhydrous crystalline forms, four hydrate forms, and five solvate forms, with methods of their preparation and use also being described. | 2010-08-19 |
20100210702 | ANTI-FUNGAL FORMULATION - Provided herein are compositions and formulations comprising an antifungal agent. Pharmaceutical compositions comprising luliconazole in an amount effective for the treatment of onychomycosis are provided. Also provided are methods for treating dermatomycoses and onychomycosis using the compositions and formulations. | 2010-08-19 |
20100210703 | ANTI-FUNGAL FORMULATION - Provided herein are compositions and formulations comprising an antifungal agent. Pharmaceutical compositions comprising luliconazole in an amount effective for the treatment of onychomycosis are provided. Also provided are methods for treating dermatomycoses and onychomycosis using the compositions and formulations. | 2010-08-19 |
20100210704 | 3-ALKOXY-1-PHENYLPYRAZOLE DERIVATIVES AND PESTICIDES - To provide pesticides such as insecticides, miticides and nematicides, which are excellent in the safety, pesticidal effects, residual effectiveness, etc., which further have infiltration, and which can be applied by soil treatment. | 2010-08-19 |
20100210705 | Pyrrole and Isoindole Carboxamide Derivatives as P2X7 Modulators - The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: | 2010-08-19 |
20100210706 | PYRROLIDINONE ANILINES AS PROGESTERONE RECEPTOR MODULATORS - The present invention relates to a compound represented by the following formula: | 2010-08-19 |
20100210707 | Small Activating RNA Molecules and Methods of Use - The present invention provides compositions, pharmaceutical preparations, kits and methods for increasing expression of a gene product in a cell by contacting the cell with a small activating RNA (saRNA) molecule comprising a ribonucleic strand that is complementary to a non-coding nucleic acid sequence of the gene. | 2010-08-19 |
20100210708 | COMPOUND PROFILING METHOD - The present invention provides a method for deriving an upstream or downstream component of a component necessary for phenotypic alteration of a living organism, the method comprising the steps of: specifying a pathway of interest related to the phenotypic alteration and a reference pathway different from the pathway of interest, and specifying a stimulant of interest and a reference stimulant which respectively stimulate the pathway of interest and the reference pathway; giving the stimulant of interest to the living organism to identify a collection of components of interest necessary for the phenotypic alteration; giving the reference stimulant to the living organism to identify a collection of reference components necessary for the phenotypic alteration; calculating an intersection between the collections of the components of interest and the reference components; and calculating a differential collection by subtracting the intersection from the collection of components of interest. | 2010-08-19 |
20100210715 | BIODEGRADABLE CATIONIC POLYMERS - Polymers comprising a polyethylenimine, a biodegradable group, and a relatively hydrophobic group are useful for the delivery of bioactive agents to cells. | 2010-08-19 |
20100210716 | Process for Preparing an Alpha-Lipoic Acid/Cyclodextrin Complex and Product Prepared - The invention relates to a process for the preparation of a cyclodextrin/alpha-lipoic acid complex, wherein in a first step, an alpha-lipoic acid and a cyclodextrin are dissolved in an aqueous alkaline solution having a pH above pH 7, and in a second step an acid is added to lower the pH of the solution to a pH below pH 7. | 2010-08-19 |
20100210717 | PHARMACEUTICAL COMPOSITIONS COMPRISING MYCOPHENOLIC ACID OR MYCOPHENOLATE SALT - The invention provides a solid dosage form, e.g. a tablet, comprising mycophenolic acid or mycophenolate salt and a process for its production. | 2010-08-19 |
20100210718 | SYNERGISTIC ANTI-OXIDANT TREATMENT FOR LIPOTOXICITY AND OTHER METABOLICALLY RELATED PHENOMENA - A method for ameliorating, reducing, and/or preventing lipotoxicity-induced metabolic dysfunction in at least one cell is disclosed, said method comprising a step of contacting said at least one cell with a therapeutically effective amount of a synergistic anti-lipotoxicity cocktail, said cocktail comprising N-acetylcysteine, ascorbic acid, and resveratrol. Also disclosed is a method for treating at least one lipotoxicity-related metabolic disorder chosen from the group comprising (a) metabolic syndrome; (b) non-alcoholic steatohepatitis; (c) obesity; and (d) coronary heart disease, said method comprising the step of administering to a patient a therapeutically effective amount of an anti-lipotoxicity cocktail, said cocktail comprising N-acetylcysteine, ascorbic acid, and resveratrol. Finally, a composition for treating the effects of lipotoxicity, containing a synergistic combination of N-acetylcysteine, ascorbic acid, and resveratrol is disclosed. | 2010-08-19 |
20100210725 | COPOLYMER-GRAFTED POLYOLEFIN SUBSTRATE HAVING ANTIMICROBIAL PROPERTIES AND METHOD FOR GRAFTING - A method for grafting a copolymer onto a polyolefin substrate includes the following steps:
| 2010-08-19 |