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14th week of 2013 patent applcation highlights part 40
Patent application numberTitlePublished
20130085098FIBROBLAST GROWTH FACTOR 21 VARIANTS - This present invention relates to pharmacologically potent and/or stable variants of human fibroblast growth factor 21 (FGF21), pharmaceutical compositions comprising FGF21 variants, and methods for treating type 2 diabetes, obesity, dyslipidemia, or metabolic syndrome, or any combination thereof, using such variants.2013-04-04
20130085099THERAPEUTIC AGENTS COMPRISING ELASTIN-LIKE PEPTIDES - The present invention provides therapeutic agents and compositions comprising elastin-like peptides (ELPs) and therapeutic proteins. In some embodiments, the therapeutic protein is a GLP-1 receptor agonist, insulin, or Factor VII/VIIa, including functional analogs. The present invention further provides encoding polynucleotides, as well as methods of making and using the therapeutic agents. The therapeutic agents have improvements in relation to their use as therapeutics, including, inter alia, one or more of half-life, clearance and/or persistence in the body, solubility, and bioavailability.2013-04-04
20130085100New Uses of Oxytocin-Like Molecules and Related Methods - The present invention is directed to a derivative selected from oxytocin, an oxytocin derivative, and an oxytocin agonist useful for the treatment of a disorder selected from obesity and insulin resistance and related methods and pharmaceutical formulations. In particular, the invention relates to a derivative selected from oxytocin, an oxytocin derivative, and an oxytocin agonist useful in the treatment of metabolic syndrome.2013-04-04
20130085101LONG-ACTING INSULIN ANALOGUE PREPARATIONS IN SOLUBLE AND CRYSTALLINE FORMS - A pharmaceutical formulation comprises an insulin analogue or a physiologically acceptable salt thereof, wherein the insulin analogue or a physiologically acceptable salt thereof contains an insulin A-chain sequence that contains paired Histidine substitutions at A4 and A8, and optionally a substitution at A21. The formulation further contains a pharmaceutically acceptable buffer containing at least about 4 zinc ions per 6 insulin analogue molecules. The formulation forms a long-acting zinc-dependent subcutaneous depot upon subcutaneous injection. In a zinc-free formulation, the insulin analogue monomer exhibits decreased affinity for the Insulin-like Growth Factor receptor and at least 20% of the affinity for the insulin receptor of the same species, in comparison to an otherwise identical insulin or insulin analogue that does not contain the His2013-04-04
20130085102PREVENTION OF HYPOGLYCEMIA IN DIABETES MELLITUS TYPE 2 PATIENTS - A method for the prevention of hypoglycaemia in diabetes mellitus type 2 comprising administering 2013-04-04
20130085103NOVEL SYNERGISTIC PHARMACEUTICAL COMPOSITION FOR TOPICAL APPLICATIONS - A synergistic pharmaceutical composition for the preparation of topical formulations for use in prophylaxis and treatment of wounds, burn wounds, skin grafts, pressure ulcers, diabetic foot ulcers and other skin diseases is provided. The composition may include one or more synergistically active ingredients and one or more inactive ingredients. The synergistically active ingredients may include Recombinant Human Epidermal Growth Factor (rh-EGF) (REGEN-D™ of Bharat Biotech International Limited) and/or Platelet Derived Growth Factor (rh-PDGF-BB), silver sulfadiazine (SSD) and chlorhexidine gluconate (CHG). One or more inactive ingredients may comprise carriers, preservatives, emulsifiers, skin emollients and soothers and one or more other constituents.2013-04-04
20130085104THERAPEUTIC AGENTS COMPRISING ELASTIN-LIKE PEPTIDES - The present invention provides therapeutic agents and compositions comprising elastin-like peptides (ELPs) and therapeutic proteins. In some embodiments, the therapeutic protein is a GLP-1 receptor agonist, insulin, or Factor VII/VIIa, including functional analogs. The present invention further provides encoding polynucleotides, as well as methods of making and using the therapeutic agents. The therapeutic agents have improvements in relation to their use as therapeutics, including, inter alia, one or more of half-life, clearance and/or persistance in the body, solubility, and bioavailability.2013-04-04
20130085105Transdermal Administration Of Peptides - The present invention relates to a method of increasing the bioavailability of a peptide. The method includes altering the lipophilicity of a peptide by the creation of fatty acid peptide salts of the peptide. The fatty acid peptide salts exhibit increased transdermal and transmucosal permeability.2013-04-04
20130085106METHODS AND FORMULATIONS FOR OXYTOCIN TREATMENT OF SUBSTANCE USE, PSYCHIATRIC AND OTHER DISORDERS - The invention provides a method of treating a psychiatric or medical disorder in a mammalian subject, the method comprising administering to the subject an effective amount of an oxytocin receptor agonist (e.g., oxytocin). Optionally, the oxytocin receptor agonist is delivered by intranasal administration. Further provided is a method of increasing social cognition, increasing social functioning, increasing empathy, increasing trust of others, reducing paranoia and/or reducing hostility in a subject with a psychotic disorder, a mood disorder characterized by psychotic features, a personality disorder or a pervasive developmental disorder, the method comprising administering to the subject an effective amount of an oxytocin receptor agonist. The invention also contemplates a method of preventing opioid dependence, opioid tolerance and/or opioid withdrawal symptoms in a subject receiving opioid treatment for pain relief, the method comprising administering to the subject an effective amount of an oxytocin receptor agonist. The invention also provides pharmaceutical compositions comprising an effective amount of an oxytocin receptor agonist and a pharmaceutically acceptable carrier.2013-04-04
20130085107Treatments for Gastrointestinal Disorders - The present invention provides peptides that are useful for the treatment of gastrointestinal disorders. The present invention also provides compositions and methods of treating gastrointestinal disorders and pharmaceutical compositions for accomplishing the same. In some embodiments, these pharmaceutical compositions include oral dosage forms.2013-04-04
20130085108PEPTIDES FOR PROMOTING ANGIOGENESIS AND AN USE THEREOF - The present invention relates to a peptide promoting angiogenesis and novel use thereof. More particularly, the invention relates to peptides promoting angiogenesis, and the use of the peptide for promoting angiogenesis and preventing or treating angiogenesis-related disease. The peptide of the present invention have an excellent effect on promoting angiogenesis. Accordingly, it is useful for preventing or treating angiogenesis-related disease and for preparing regeneration of skin flap, wound and burn healing, implantation of artificial-skin and preparation of blood vessels for transplantation.2013-04-04
20130085109METHODS OF CARDIOVASCULAR PATIENT TREATMENT USING SUBSTANCES SUFFICIENT TO REDUCE ACTIN DEPOLYMERIZATION - Methods of cardiovascular patient treatment using substances sufficient to reduce actin depolymerization. In an exemplary embodiment of a method of treating a patient of the present disclosure, the method comprises the step of administering a therapeutically effective dose of a substance that reduces actin depolymerization within a vasculature of a patient to treat a cardiovascular condition of the patient. In at least one embodiment, the substance the substance is selected from the group consisting of jasplakinolide, Jasplaskinolide V, and Amphidinolide H.2013-04-04
20130085110RECOMBINANT FACTOR VIII HAVING INCREASED STABILITY - The present invention relates to a recombinant factor VIII that includes one or more mutations that result in enhanced stability of both factor VIII and factor VIIIa. Methods of making and using the recombinant factor VIII, and pharmaceutical compositions containing the same are also disclosed. The present invention further relates to an isolated nucleic acid molecule that encodes the recombinant factor VIII, as well as DNA expression systems and host cells containing the isolated nucleic acid molecule.2013-04-04
20130085111PRODUCTION OF HUMAN C1 INHIBITOR IN HUMAN CELLS - Vector constructs comprising the coding sequence for human C1 inhibitor are described. Expression of glycosylated recombinant human C1 inhibitor is achieved human cells in high yields.2013-04-04
20130085112TREATMENT OF ATONAL HOMOLOG 1 (ATOH1) RELATED DISEASES BY INHIBITION OF NATURAL ANTISENSE TRANSCRIPT TO ATOH1 - The present invention relates to antisense oligonucleotides that modulate the expression of and/or function of Atonal homolog 1 (ATOH1), in particular, by targeting natural antisense polynucleotides of Atonal homolog 1 (ATOH1). The invention also relates to the identification of these antisense oligonucleotides and their use in treating diseases and disorders associated with the expression of ATOH1.2013-04-04
20130085113TEAR LIPOCALIN IN MUTEINS BINDING IL-4 R ALPHA - The present invention relates to novel muteins derived from human tear lipocalin, which bind to IL 4 receptor alpha. The sequences of the muteins comprise particular combinations of amino acids. In particular a mutated amino acid residue is present at any one or more of the sequence positions 27, 28, 30, 31, 33, 53, 57, 61, 64, 66, 80, 83, 104-106 and 108 of the linear polypeptide sequence of the mature human tear lipocalin. A mutated amino acid residue is also present at any 2 or more of the sequence positions 26, 32, 34, 55, 56, 58 and 63 of the linear polypeptide sequence of the mature human tear lipocalin. The invention also provides a corresponding nucleic acid molecule encoding such a mutein and a method for producing such a mutein and its encoding nucleic acid molecule.2013-04-04
20130085114METHOD FOR TREATING VARICOCELE OR MALE INFERTILITY USING ANTHOCYANIN EXTRACTED FROM BLACK SOYBEAN - The present invention relates to the therapeutic or ameliorating effects of anthocyanin extracted from black soybean on varicocele or male infertility. In particular, the present invention relates to a method for treating or ameliorating varicocele or male infertility using anthocyanin extracted from black soybean.2013-04-04
20130085115COMBINATION THERAPY FOR LYMPHOMA - Methods of treating, preventing or managing lymphomas are disclosed. The methods encompass the administration of an HDAC inhibitor romidepsin and a DNA demethylating agent 5-azacitidine, also known as VIDAZA®. Pharmaceutical compositions and single unit dosage forms suitable for use in the methods provided herein are also disclosed2013-04-04
20130085116COMPOSITIONS INCLUDING TRICIRIBINE AND EPIDERMAL GROWTH FACTOR RECEPTOR INHIBITOR COMPOUNDS OR SALTS THEREOF AND METHODS OF USE THEREOF - This application relates to combination therapies including triciribine compounds and epidermal growth factor receptor inhibitor compounds, particularly erlotinib-like compounds and compositions with reduced toxicity for the treatment and prevention of tumors, cancer, and other disorders associated with abnormal cell proliferation.2013-04-04
20130085117Compositions Comprising Plant Material and Sugar For The Control of Pests and Methods of Making - Compositions and methods for controlling pests are described. The compositions comprise (a) a material obtainable from a plant comprising an effective amount of a glucosinolate breakdown product and (b) a sugar. The novel compositions exhibit improved properties over known formulations, for example with respect to their potency, ease of manufacture and ease of application.2013-04-04
20130085118METHOD AND MIXTURE FOR TREATING AND PREVENTING INFLAMMATORY BOWEL DISEASE - A method and a mixture for treating and preventing the inflammatory bowel disease (IBD) by applying a predetermined therapeutically effective amount of a mixture of hyaluronic acid to individuals is disclosed. The mixture includes at least two different average molecular weight hyaluronic acids (Mw) with different rheology to gain a hyaluronic acid with the proper adhesion property, functions of tissue scaffold and insulation and treatment time, in order to treat and to prevent IBD (inflammatory bowel disease) includes ulcerative colitis, Crohn's disease or wound healing in stomach and intestine, thus to achieve the prompt treatment and to prolong the effect.2013-04-04
20130085119AGENT FOR THE TREATMENT OF SKIN CONDITIONS - Disclosed are methods of treatment and compositions containing at least one non-volatile silicone oil in combination with at least one spreading agent for use in the treatment of skin conditions in mammals typified by scales, plaques and scabs and associated with punctiform bleeding during the removal of scales, plaque or scabs. Preferred conditions are selected from the group consisting of seborrheic dermatitis, psoriasis, and cradle cap wherein the incidence of punctiform bleeding and formation of bloody tear points on the skin during removal of the scales is diminished or prevented.2013-04-04
20130085120Phosphate Ester Compound of Hydroxy Acid Substituted Phenol Ester, Preparation Method and Medical Use Thereof - Phosphate ester compound of hydroxy acid substituted phenyl ester, preparation method and medical use thereof are provided. The title compound is shown in formula (I), in which Y=C2013-04-04
20130085121PHARMACEUTICAL COMPOSITIONS COMPRISING PHOSPHATE BINDER, CALCIUM RECEPTOR-ACTIVE COMPOUND AND/OR ACTIVE VITAMIN D - The present invention is an oral solid pharmaceutical compositions for the treatment of kidney diseases and mineral bone disorder including a phosphate binder, a calcium receptor-active compound and at least one pharmaceutically acceptable excipient, the invention further including a method for preparing the pharmaceutical compositions including the steps of granulating cinacalcet and/or sevelamer and/or vitamin D by one of a wet and a dry granulation process, each with at least one pharmaceutically acceptable excipient to form cinacalcet granules and/or sevelamer granules and/or vitamin D granules, mixing at least two of the cinacalcet granules, sevelamer granules and vitamin D granules to form a granules mixture and compressing the granules mixture to tablets or encapsulating the granules mixture into capsules or pulverizing the granules mixture into a dispersion powder.2013-04-04
20130085122BACLOFEN AND ACAMPROSATE BASED THERAPY OF NEUROLOGICAL DISORDERS - The present invention relates to combinations and methods for the treatment of neurological disorders related to glutamate excitotoxicity and Amyloid β toxicity. More specifically, the present invention relates to novel combinatorial therapies of Multiple Sclerosis, Alzheimer's disease, Alzheimer's disease related disorder, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, neuropathic pain, alcoholic neuropathy, alcoholism or alcohol withdrawal, or spinal cord injury, based on Baclofen and Acamprosate combination.2013-04-04
20130085123ORGANIC COMPOUNDS - Optionally substituted 4,5,7,8-tetrahydro-(optionally 4-oxo, 4-thioxo or 4-imino)-(1H or 2H)-imidazo[1,2-a]pyrazolo[4,3-e]pyrimidine or 4,5,7,8,9-pentahydro-(optionally 4-oxo, 4-thioxo or 4-imino)-(1H or 2H)-pyrimido[1,2-a]pyrazolo[4,3-e]pyrimidine compounds, processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.2013-04-04
20130085124USE OF LEVOCETIRIZINE AND MONTELUKAST IN THE TREATMENT OF INFLUENZA, COMMON COLD AND INFLAMMATION - The embodiments described herein include methods and formulations for treating influenza, common cold and associated acute inflammation. The methods and formulations include, but are not limited to, methods and formulations for delivering effective concentrations of levocetirizine and montelukast to a patient in need. The methods and formulations can comprise conventional and/or modified-release elements, providing for drug delivery to the patient.2013-04-04
20130085125METHODS FOR THE SYNTHESIS AND PURIFICATION OF DEOXYCHOLIC ACID - Synthesis and purification of deoxycholic acid and its salts are provided.2013-04-04
20130085126PYRAZOLE COMPOUNDS - Compounds of formula (I):2013-04-04
20130085127HETEROCYCLIC COMPOUND AND H1 RECEPTOR ANTAGONIST - A heterocyclic compound useful as an antiallergic agent is provided.2013-04-04
201300851286-(4-Hydroxy-phenyl)-3-alkyl-1H-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors - The present invention relates to pyrazolo[3,4-b]pyridine compounds of the formula I,2013-04-04
20130085129MONOACYLGLYCEROL LIPASE INHIBITORS FOR THE TREATMENT OF METABOLIC DISEASES AND RELATED DISORDERS - Disclosed are compounds, compositions and methods for treating metabolic diseases, including obesity and diabetes, and for reducing weight gain. Such compounds are represented by formula (I) as follows:2013-04-04
20130085130MONOACYLGLYCEROL LIPASE INHIBITORS FOR THE TREATMENT OF METABOLIC DISEASES AND RELATED DISORDERS - Disclosed are compounds, compositions and methods for treating metabolic diseases, including obesity and diabetes. Such compounds are represented by formula (I) as follows:2013-04-04
20130085131HETEROCYCLIC COMPOUNDS AND THEIR USES - Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with pi 110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.2013-04-04
20130085132PYRAZOLE COMPOUND AND PHARMACEUTICAL USE THEREOF - The present invention provides a pyrazole compound of the following general Formula [Ib] having SGLT1 inhibitory activity, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the same, and its pharmaceutical use:2013-04-04
20130085133ANTI-VIRAL TREATMENT AND ASSAY TO SCREENFOR ANTI-VIRAL AGENT - The present disclosure relates to novel compounds of formulas (1) through (19) and to a method for treating humans infected with a virus including various respiratory viruses such as members of the Paramyxoviridae family (respiratory syncytial virus (RSV), human metapneumovirus (HMPV), human parainfluenza virus (HPIV), measles virus, and mumps virus) with a compound of formulas (1) through (19). The present disclosure also relates to a cytopathic effect (CPE)-based assay that will assess virus-induced CPE for screening of compounds for treating viral diseases or inhibiting a virus.2013-04-04
20130085134QUINOXALINE COMPOUND - Quinoxaline compounds of formula (I) have a PDE9-inhibiting action and are useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, and bladder/urethral diseases, and the like.2013-04-04
201300851355H-CYCLOPENTA[D]PYRIMIDINES AS AKT PROTEIN KINASE INHIBITORS - Compounds of Formula I are useful for inhibiting AKT protein kinases. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.2013-04-04
20130085136NOVEL ANTIFUNGAL 5,6-DIHYDRO-4-[(DIFLUOROETHYL)PHENYL]-4H-PYRROLO[1,2-a][1,4]BENZODIAZEPIN- E AND 4-(DIFLUOROETHYL)PHENYL-6H-PYRROLO[1,2-a][1,4]BENZODIAZEPINE DERIVATIVES - The present invention concerns novel compounds of Formula (I):2013-04-04
20130085137Topical antimicrobial compositions and methods of using same - The invention includes a method of treating a mammal comprising topically applying an aqueous composition to a target site on the mammal, wherein the aqueous composition comprises: active ingredients comprising i) a cosmetic dye selected from a violet, blue or green dye, or combinations thereof, and ii) an enhancing ingredient, wherein the relative weight percentage of the cosmetic dye to the enhancing ingredient is about 1:2 to about 40:1, wherein the cosmetic dye interacts with keratinous material thereby i) substantially staining the target site and ii) inhibiting the active ingredients from significantly leaching from the target site.2013-04-04
20130085138Selective NR2B Antagonists - The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, antagonists of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system.2013-04-04
20130085139Oligomers - Certain disclosed oligomers induce exon skipping during processing of myostatin pre-mRNA. The oligomers may be in a vector or encoded by the vector. The vector is used for inducing exon skipping during processing of myostatin pre-mRNA. A therapeutically effective amount of the oligomer may be administered to a subject patient such that exon skipping during processing of myostatin pre-mRNA is induced. The administration to a subject may be used in order to increase or maintain muscle mass, or slowing degeneration of muscle mass in the subject. The administration to a subject may ameliorate muscle wasting conditions, such as muscular dystrophy. Examples of such muscular dystrophies which may be so treated include Becker's muscular dystrophy, congenital muscular dystrophy, Duchenne muscular dystrophy, distal muscular dystrophy, Emery-Dreifuss muscular dystrophy, facioscapulohumeral muscular dystrophy (FSHD), limb-girdle muscular dystrophy, myotonic muscular dystrophy, and oculopharyngeal muscular dystrophy2013-04-04
20130085140INDENOISOQUINOLINONE DERIVATIVES, MANUFACTURING METHOD AND MEDICAL USE THEREOF - Indenoisoquinolinone derivatives (I), the manufacturing method and the medical use thereof, which belong to pharmaceutical chemistry and organic chemistry field, are disclosed. These compounds can be used for treating several medical symptoms related to postmenopausal syndrome, uterine fibers deterioration and aortic smooth muscle cells proliferation, especially ER-(+) depend breast cancer. Meanwhile, these compounds can also be used for treating glioma and lung cancer, and have inhibiting effect on tumor metastasis effect on tumor metastasis.2013-04-04
20130085141SUBSTITUTED OCTAHYDROPYRROLO[1,2-a]PYRAZINE SULFONAMIDES AS CALCIUM CHANNEL BLOCKERS - The present application relates to: (a) compounds of Formula (I):2013-04-04
20130085142SUBSTITUTED OCTAHYDROPYRROLO[1,2-a]PYRAZINES AS CALCIUM CHANNEL BLOCKERS - The present application relates to: (a) compounds of Formula (I):2013-04-04
20130085143AMINOACID DERIVATIVES, THEIR PROCESS OF PREPARATION AND THEIR THERAPEUTICAL USES AS INHIBITORS OF ONCOGENIC SIGNALS BY THE MET FAMILY - Novel amino acids derivatives, in particular some amino acid amides derivatives, their process of preparation and their use for inhibiting Met-triggered disorders, in particular cancer.2013-04-04
20130085144DERIVATIVES OF AZAINDAZOLE OR DIAZAINDAZOLE TYPE AS MEDICAMENT - The present invention relates to a compound of following formula (I):2013-04-04
20130085145IMATINIB MESILATE PHARMACEUTICAL TABLET - The present invention provides a pharmaceutical tablet, comprising Imatinib in an amount of 50-75% w/w of the total tablet weight and comprising at least one pharmaceutically acceptable excipient without a binding agent and the process for preparation of the same.2013-04-04
20130085146LIPID-DRUG FORMULATIONS AND METHODS FOR TARGETED DELIVERY OF LIPID-DRUG COMPLEXES TO LYMPHOID TISSUES - The present application is directed to lipid-drug complexes and related methods for producing stable lipid-drug complexes at or near the neutral pH range and administering pharmaceutical lipid-drug complexes to patients. In certain examples, the lipid-drug complex has a lipid-to-drug molar ratio of approximately 3:1. In certain examples, the lipid-drug complex may have lipid-to-drug molar ratios of less than 3:1 to 10:1 or higher. The present application is also directed to methods of administering a drug to a patient though subcutaneous injection of the lipid-drug complexes into particular tissues to effect higher localized concentrations of the at least one drug. Lipid-anti-HIV-drug complexes can be subcutaneously injected into the lymphoid tissue of a HIV-infected mammalian subject via the lymphatic vessels to deliver high concentrations of stable lipid-anti-HIV-drug complexes, rather than delivery of the anti-HIV drug intravenously via the blood stream which will eventually reach the lymphatic system at lower concentrations.2013-04-04
20130085147Hepatitis C Virus Inhibitors - The present disclosure is generally directed to antiviral compounds, and more specifically directed to compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such compounds, and methods for inhibiting the function of the NS5A protein.2013-04-04
20130085148Pyridine Derivatives - The present application provides novel pyridine compounds and pharmaceutically acceptable salts or prodrugs thereof. Also provided are methods for preparing these compounds. These compounds are useful in inhibiting CYP17 activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with CPY17 activity. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer, such as prostate cancer.2013-04-04
20130085149OSMOLYTE-CONTAINING PREPARATION FOR THE TREATMENT OF DRY MUCOUS MEMBRANES - The present invention relates to osmolyte-containing preparations for the local treatment of dry mucous membranes. It describes the use of osmolytes for the production of a medicament, medical product or cosmetic product for the prevention, therapy and/or care of dry mucous membranes. The present invention relates to topical compositions based on osmolytes to which sodium chloride and/or moisturizers can optionally be added. The group of osmolytes proposed by the invention embraces various low-molecular substances, in particular ectoine, homoectoine, hydroxyectoine, di-myo-inositol phosphate (DIP), cyclic 2,3-diphosphoglycerate (cDPG), 1,1-di-glycerol phosphate (DGP), β-mannosylglycerate (Firoin), β-mannosylglyceramide (Firoin-A), di-mannosyl di-inositol phosphate (DMIP), glucosylglycerol and/or a derivative, e.g. an acid, salt or ester, of these compounds.2013-04-04
20130085150ANALOGUES FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS - Compounds represented by formula I2013-04-04
20130085151HETEROCYCLIC COMPOUNDS AND THEIR USES - Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.2013-04-04
20130085152Method For Assay On The Effect Of Vascularization Inhibitor - The present invention provides a method of predicting the antitumor effect of an angiogenesis inhibitor. It is possible to predict the antitumor effect of an angiogenesis inhibitor by evaluating the EOF dependency of a tumor cell for proliferation and/or survival and using the EGF dependency as an indicator. Since the antitumor effect of an angiogenesis inhibitor correlates with the EGF dependency of a tumor cell for proliferation and/or survival, the angiogenesis inhibitors is capable of producing excellent antitumor effect when combined with a substance having EGF inhibitory activity.2013-04-04
20130085153COMBINATION OF AN IAP INHIBITOR AND A TAXANE FOR THE TREATMENT OF A PROLIFERATIVE DISEASE - The invention provides a pharmaceutical combination comprising: 2013-04-04
20130085154CRYSTALLINE FORMS OF PRASUGREL SALTS - Salts of prasugrel were prepared including, for example, crystalline forms of prasugrel hydrobromide. These salts are useful, for example, in medicaments that inhibit the aggregation of platelets.2013-04-04
20130085155THIAZOLOPYRIDINE SIRTUIN MODULATING COMPOUNDS - Provided herein are novel sirtuin-modulating compounds of Structural Formula (Ia) 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, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.2013-04-04
20130085156NOVEL 2-PYRIDINECARBOXAMIDE DERIVATIVES - The present invention relates to a compound which has a glucokinase-activating effect and is useful as a therapeutic agent for diabetes mellitus, being represented by a formula (I):2013-04-04
20130085157ARYLSUBSTITUTED THIAZOLOTRIAZOLES AND THIAZOLOIMIDAZOLES - This disclosure relates to compounds, compositions and methods for the treatment of various disorders. In particular, the disclosure relates to thiazolotriazole and thiazoloimidazole compounds which agonize the activity of the protein TGR5.2013-04-04
20130085158SOLID FORMS OF 3-(6-(1-(2,2-DIFLUOROBENZO[D][1,3]DIOXOL-5-YL) CYCLOPROPANECARBOXAMIDO)-3-METHYLPYRIDIN-2-YL)BENZOIC ACID - The present invention relates to a substantially a solid form of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid (Compound 1, Solvate Form A and Compound 1, HCl Salt Form A), processes for making such forms, pharmaceutical compositions thereof, and methods of treatment therewith.2013-04-04
20130085159COMPOUNDS DERIVED FROM ARTESUNATE, PREPARATION PROCESS, PHARMACEUTICAL COMPOSITION AND USE OF THE RESPECTIVE MEDICINE - The present invention refers to new compounds represented by the general formula (I) where X is represented by the general formula (II) and Y is represented by the general formula (III). The relation X to Y may vary from 1:1 to 1:7. The radicals R2013-04-04
20130085160NOVEL BENZAMIDE DERIVATIVES - The present invention provides a novel benzamide derivative or a pharmaceutically acceptable salt thereof, a method for preparing the same, and a 5-HT2013-04-04
20130085161PIPERIDINYL SUBSTITUTED 1,3-DIHYDRO-BENZOIMIDAZOL-2-YLIDENEAMINE DERIVATIVES - The invention relates to new derivatives of formula (I),2013-04-04
20130085162AMIDO COMPOUNDS AS RORyT MODULATORS AND USES THEREOF - Amido compounds are disclosed that have a formula represented by the following:2013-04-04
20130085163Pyripyropene Derivative Having ACAT2 Inhibiting Activity and Stable to Metabolizing Enzymes - A compound effective in prevention and treatment of arteriosclerosis with a mechanism different from that of statin drugs has the following formula or a pharmaceutically acceptable salt, solvate, or hydrate thereof:2013-04-04
20130085164Imidazole Derivatives - The present application provides novel imidazole compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in inhibiting CYP17 activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with CPY17 activity. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer, such as prostate cancer.2013-04-04
20130085165Buccal Drug Delivery - A lozenge is provided that has stable pH and stable levels of active ingredient over time. It comprises a combination of (i) at least one gum and (ii) at least one non-crystallising sugar or non-crystallising sugar alcohol in a matrix designed for controlled buccal delivery of a drug. The lozenge also contains water and optional components selected from flavourings, taste masking agents, colourings, buffer components, pH adjusting agents, excipients, stabilizers and sweeteners. Methods of preparing the lozenge are also provided.2013-04-04
20130085166FORMULATIONS AND USES OF RETINOIC ACID RECEPTOR SELECTIVE AGONISTS - The invention provides retinoic acid receptor (RAR) selective agonists and formulations thereof for the treatment of disease or for inducing a medically beneficial effect.2013-04-04
20130085167METHODS FOR TREATING A STROKE-RELATED SENSORIMOTOR IMPAIRMENT USING AMINOPYRIDINES - Disclosed herein are methods and compositions related to therapeutic use of aminopyridines in patients with a stroke-related impairment, in particular, in patients with a stroke-related sensorimotor impairment.2013-04-04
20130085168GAMMA-GLUTAMYL TRANSPEPTIDASE INHIBITORS AND METHODS OF USE - Compositions and methods for inhibiting human gamma-glutamyl transpeptidase (GGT) in vivo or in vitro and for inhibiting and killing neoplastic cancer cells, for example for the treatment, inhibition or prevention of tumors or malignant growths or other neoplasias in mammals, or sensitizing tumor to other therapies including radiation therapy. The GGT inhibitor compounds comprise a class of benzylthiadiazol benzenesulfoniamides. The compounds may also be used to treat a reversible airways obstruction in a mammal or a disease associated with reverse airways obstruction such as asthma, chronic obstructive pulmonary disease (COPD), allergic reaction, respiratory tract infection or upper respiratory tract disease. Other diseases or conditions which may be treated include, for example, degenerative diseases, renal diseases, liver diseases, cardiovascular disease and inner ear conditions or diseases.2013-04-04
20130085169METHODS AND COMPOSITIONS COMPRISING AMPK ACTIVATOR (METFORMIN/TROGLITAZONE) FOR THE TREATMENT OF MYOTONIC DYSTROPHY TYPE 1 (DM1) - The present invention relates to methods and compositions for the treatment of Myotonic Dystrophy type 1 (DM1) with an AMPK activator .2013-04-04
20130085170COMPOSITIONS COMPRISING AMINO ACIDS, WITH PRO-ANGIOGENIC ACTIVITY - Composition comprising leucine, isoleucine, valine threonine and lysine for treating angiogenic disorders in elderly subjects.2013-04-04
20130085171COMPOUNDED TRANSDERMAL PAIN MANAGEMENT - The present embodiments relate to topically delivered medication (compounded) for treatment of pain, inflammation, muscle fatigue, spasms, and/or other ailments. A transdermal cream may provide the effective topical administration of multiple medications simultaneously. The transdermal cream may include a salt load of approximately 30% or greater. The transdermal cream may include a unique base composition such that the transdermal cream may be able to remain stable and avoid degradation for six months or more and capable of effective delivery of active ingredient concentrations exceeding approximately 40% or more of the total formulation weight. The active ingredients may include a nerve depressant, NSAID, muscle relaxant, opiate agonist, local anesthetic, NMDA receptor antagonist, and a tricyclic antidepressant. In one embodiment, the transdermal cream may comprise ketamine HCL, gabapentin, clonidine HCL and baclofen. The transdermal cream may deliver an enhanced topical delivery flux of ketamine via a single transdermal application.2013-04-04
20130085172CRYSTALLINE FORMS OF A 3-[2-METHANESULFONYL-1-(4-TRIFLUOROMETHYL-PHENOXY)ETHYL]PYRROLIDINE COMPOUND - The invention provides crystalline hydrochloride salts of (S)-3-[(S)-2-methanesulfonyl-1-(4-trifluoromethylphenoxy)ethyl]pyrrolidine. This invention also provides pharmaceutical compositions comprising the crystalline salts, processes and intermediates for preparing the crystalline salts, and methods of using the crystalline salts to treat diseases.2013-04-04
20130085173SUPERCOILED MINICIRCLE DNA FOR GENE THERAPY APPLICATIONS - The present invention relates to nucleic acid molecule compositions comprising minivectors encoding a nucleic acid sequence and methods of gene therapy and prophylaxis against infection using minivectors encoding a nucleic acid sequence.2013-04-04
20130085174ACNE TREATMENT - The invention relates to the use of lipooxigenase inhibitors for treating acne, particularly inflammatory acne. The inventive lipooxigenase inhibitor can be used alone or in combination with other lipooxigenase inhibitors or anti-acne active agents in a pharmaceutically suitable composition, particularly through oral and/or local-topic application.2013-04-04
20130085175PROCESS FOR THE PREPARATION OF SULFAMIDE DERIVATIVES - The present invention is directed to an improved process for the preparation of sulfamide derivatives.2013-04-04
20130085176PROCESS FOR THE PREPARATION OF SULFAMIDE DERIVATIVES - The present invention is directed to a process for the preparation of sulfamide derivatives.2013-04-04
20130085177COSMETIC COMPOSITION BASED ON ELLAGIC ACID OR A DERIVATIVE THEREOF AND ON A PARTICULAR MIXTURE OF SURFACTANTS - The invention relates to a cosmetic composition comprising, in a cosmetically acceptable medium: (i) from 0.2% to 10% by weight of one or more compounds selected from ellagic acid, ethers thereof, ellagic acid salts and ellagic acid ether salts, and mixtures thereof, and (ii) a system of surfactants selected from the following mixtures comprising: (iii) one or more anionic surfactants selected from ethoxylated alkyl sulphates, the corresponding acids, and mixtures thereof, and (iv) one or more anionic surfactants different from the abovementioned anionic surfactant(s) (iii), and (v) one or more anionic surfactants and (vi) one or more amphoteric or zwitterionic surfactants, in a weight ratio of the amount of anionic surfactant(s) to the amount of amphoteric or zwitterionic surfactant(s) of greater than 3. The invention also relates to a cosmetic treatment method using such a composition and to the use of said composition for washing keratin fibres.2013-04-04
20130085178COMPOSITION FOR TREATING BONE DISEASE COMPRISING A GLYCEOLLIN AS AN ACTIVE INGREDIENT - A method for preventing or treating a bone disease, includes administering to a patient having the bone disease a pharmaceutical composition comprising glyceollin as an active ingredient. The active ingredient, glyceollin promotes degradation of the Runx2 protein in osteoblasts and inhibits the mRNA expression of Rankl in osteoblasts to prevent the differentiation of osteoclasts. Furthermore, glyceollin is capable of ameliorating osteoporosis in animal models for osteoporosis. The composition promises drug or food for prevention or treatment of not only osteoporosis but also bone diseases caused by cancer metastatic to the bone.2013-04-04
20130085179METHODS OF THERAPEUTIC MONITORING OF NITROGEN SCAVENGING DRUGS - The present disclosure provides methods for evaluating daily ammonia exposure based on a single fasting ammonia blood level measurement, as well as methods that utilize this technique to adjust the dosage of a nitrogen scavenging drug, determine whether to administer a nitrogen scavenging drug, and treat nitrogen retention disorders.2013-04-04
20130085180ORAL BIOAVAILABLE PENTAMIDIN PRODRUGS FOR TREATMENT OF DISEASES - The present invention relates to prodrug derivatives of pentamidine, their use in the treatment and/or prophylaxis of diseases such as tumor diseases, as well as leishmaniasis, trypanosomiasis, pneumocystis carinii pneumonia (PcP), and malaria.2013-04-04
20130085181PHARMACEUTICAL FORMULATIONS - The present invention provides a modified release formulation comprising an active agent in a hydrophilic polymer matrix wherein the active agent is a salt of fenofibric acid wherein the release rate of the formulation in an in vitro dissolution is substantially independent of the ionic strength of the dissolution media.2013-04-04
20130085182SODIUM 2-MERCAPTOETHANE SULFONATE FOR USE IN THE TREATMENT OF LUMBAR PAIN - The present invention refers to 2-mercaptoethane sulfonate or pharmaceutically acceptable salts thereof and to pharmaceutical compositions comprising it for epidural use in the treatment of lumbar pain.2013-04-04
20130085183AROMATIC BUTAN-2-OL COMPOUNDS AND PREPARATION AND USES THEREOF - Aromatic butan-2-ol compounds, preparation methods for making the compounds, and uses of the compounds are provided. Specifically, the compound of Formula I, or an optical isomer, racemate, diastereomer, pharmaceutically acceptable salt, or solvate thereof, is provided, where each of the substituents is defined. In addition, a pharmaceutical composition containing the compound, and the use of the compound in manufacture of a medicament for the treatment and/or prophylaxis of a disease or disorder caused by 2013-04-04
20130085184Intrathecal or Epidural Administration of 3-[(1S,2S)-3-(Dimethylamino)-1-Ethyl-2-Methylpropyl]Phenol - The present invention relates to a method of providing pain management in a subject wherein the administration of the composition does not result in any non-central nervous system mediated systemic effect in the subject. In particular, the present invention relates to a method of administering 3-[(1S,2S)-3-(dimethylamino)-1-ethyl-2-methyl-propyl]-phenol in a space that is void of thrombocytes.2013-04-04
20130085185CONTROLLED HYDROLYSIS OF POLY-4-HYDROXYBUTYRATE AND COPOLYMERS - Methods for making P4HB polymers and copolymers thereof that are useful for preparing controlled release systems, medical devices and as intermediates in chemical synthesis, have been developed. These methods avoid the use of organic solvents, and basic conditions that can cause transesterification reactions with polymer terminal end groups or elimination reactions. A preferred embodiment is a method for producing polymers of P4HB with weight average molecular weight less than 250,000, and more preferably, less than 100,000, and a Pd of less than 3, which are useful in controlled release. A particularly preferred embodiment utilizes aqueous acetic acid to hydrolyze pellets of P4HB polymers and copolymers while in suspension.2013-04-04
20130085186COSMETIC PREPARATIONS BASED ON MOLECULARLY IMPRINTED POLYMERS - The present invention relates to cosmetic or dermatological formulations comprising at least one active compound, at least one polymer which is molecularly imprinted in the presence of this active compound and at least one fatty phase.2013-04-04
20130085187DEACETYLATION HYDROLASE OF HYALURONIC ACID, HYALURONIC ACID DEACETYLATED BY SAME AND DERIVATIVE THEREOF - The present disclosure relates to a deacetylation hydrolase of a hyaluronic acid a hyaluronic acid deacetylated by same and a derivative thereof. The deacetylated hyaluronic acid and the derivative thereof have the following characteristic: a delayed initial decomposition rate on a living body; minimized decrease of molecular weight and viscosity; accelerated gelation due to a lower gelation temperature than the gelation temperature for a non-deacetylated hyaluronic acid; and an hMSC survival rate that is hardly affected by increased concentration of the deacetylated hyaluronic acid and the derivative thereof in a culture medium. As a result, the deacetylated hyaluronic acid and the derivative thereof can be useful as a bioingredient such a delivery system for a cell, gene, drug, and the like, or a support for tissue engineering, etc.2013-04-04
20130085188PEPTIDE NETWORKS - Methods of modulating interfacial characteristics in a self-assembled, force-transmitting peptide network at a fluid-fluid interface are disclosed. The methods involve exposing a peptide capable of participating in a self-assembled, force-transmitting peptide network, either before or after it interacts with other peptides to form the peptide network to a stimulus that alters the chemical and/or physical properties of the peptide. Use of such methods in applications such as emulsions and foams are also disclosed.2013-04-04
20130085189Fischer-Tropsch Process Using Fibrous Composite Catalytic Structures Having at Least Three Solid Phases - A Fischer-Tropsch process for converting a syngas to hydrocarbon products in the presence of a permeable composite fibrous catalytic sheet comprised of at least three distinct solid phases. A first solid phase is a 3-dimensional porous network of a non-conductive porous ceramic material. A second solid phase is an electrically conductive phase comprised of randomly oriented electrically conductive fibers. A third phase is comprised of catalytic particles dispersed on said 3-dimensional porous network, said conductive fibers, or both. A fourth phase can be present, which fourth phase is comprised one or more conductive species or one or more non-conductive species embedded in said first solid phase.2013-04-04
20130085190AMINATED ION EXCHANGE RESINS AND PRODUCTION METHODS THEREOF - This invention relates to certain novel anion exchange resins and methods of making them. It relates more particularly to aminated cross-linked resin bead polymers containing an inert and/or chloromethylated core, and an aminated outer shell, and to methods for preparing the same. These resins exhibit improved anion exchange properties.2013-04-04
20130085191POROUS POLYMER SUPPORTED POLYOXOMETALATES - A composition for the destruction of chemical warfare agents and toxic industrial chemicals having a polyoxometalate (POM) attached to an amine, carboxylic acid, or ammonium substituted porous polymer. Also disclosed is a method for attaching a POM to an amine, carboxylic acid, or ammonium substituted porous polymer by (1) dissolving the POM in water or an organic solvent, adding the functionalized porous polymer, whereby the POM ionically attaches to the amine, carboxylic acid or ammonium group, or (2) heating the POM and functionalized polymer in the presence of a dehydrating agent whereby an imide bond is produced between the POM and the functionality on the porous polymer.2013-04-04
20130085192THERMALLY EXPANDABLE MICROCAPSULE AND PROCESS FOR PRODUCTION OF THERMALLY EXPANDABLE MICROCAPSULE - The present invention provides a thermally expandable microcapsule that is excellent in heat resistance and durability. The present invention is a thermally expandable microcapsule, which comprises a shell containing a copolymer, and a volatile liquid as a core agent included in the shell, the copolymer being obtainable by polymerization of a monomer mixture containing a monomer A and a monomer B, the monomer A being at least one selected from the group consisting of a nitrile group-containing methacrylic monomer and an amide group-containing methacrylic monomer, the monomer B being at least one selected from the group consisting of a carboxyl group-containing methacrylic monomer and an ester group-containing methacrylic monomer, a total amount of the monomer A and the monomer B accounting for 70% by weight or more of the monomer mixture, a weight ratio of the monomer A and the monomer B being 5:5 to 9:1, and the monomer mixture containing methacrylonitrile and methacrylic acid in a total amount of not more than 70% by weight of the monomer mixture.2013-04-04
20130085193TERTIARY AMINE COMPOSITION AND METHOD FOR MAKING THE COMPOSITION - A composition and method for producing a tertiary amine is disclosed. The tertiary amine is contacted with an inert gas. The inert gas is nitrogen or more preferably argon. The amine composition is useful in producing polyurethane foam with lower levels of chemical emissions particularly lower emissions of toxic chemicals.2013-04-04
20130085194CO-POLYMER BASED POLYIMIDE ARTICLES AND THEIR USES IN HIGH TEMPERATURE APPLICATIONS - Disclosed herein is a method for making polyimide articles that are suitable for high temperature applications. The articles disclosed herein are rigid, oxidatively stable, wear-resistant, and permeable to heated moisture and gases, and comprise co-polymer based polyimide, and at least one additive or filler, and are made using 20,000 to 50,000 psi of compression pressure.2013-04-04
20130085195CO-POLYMER BASED POLYIMIDE ARTICLES AND THEIR USES IN HIGH TEMPERATURE APPLICATIONS - Disclosed herein is a method for making polyimide articles that are suitable for high temperature applications. The articles disclosed herein are rigid, oxidatively stable, wear-resistant, and permeable to heated moisture and gases, and comprise co-polymer based polyimide, and at least one additive or filler, and are made using 20,000 to 50,000 psi of compression pressure.2013-04-04
20130085196DISPERSING AGENT FOR ADDITIVE FOR POLYOLEFIN-BASED RESIN, POLYOLEFIN-BASED RESIN COMPOSITION, AND MOLDED ARTICLE - Disclosed is a versatile dispersant for an additive for olefin resins. The dispersant (A) for an additive (B) for polyolefins contains an alkyl methacrylate polymer which comprises an alkyl methacrylate (a1) unit having an alkyl group with a carbon number of at least 2 as the main component, and which has a mass average molecular weight of 15,000-145,000.2013-04-04
20130085197DISPERSION COMPRISING A LIQUID PHASE AND A SOLID PHASE - Dispersions comprise a liquid phase and a solid phase.2013-04-04
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