12th week of 2013 patent applcation highlights part 49 |
Patent application number | Title | Published |
20130072434 | INACTIVATION RESISTANT FACTOR VIII - The present invention provides novel purified and isolated nucleic acid sequences encoding procoagulant-active FVIII proteins. The nucleic acid sequences may encode amino acid sequences corresponding to known human FVIII sequences, wherein residue Phe309 is mutated. The nucleic acid sequences also may encode amino acid sequences corresponding to known human FVIII sequences, wherein the APC cleavage sites, Arg336 and Ile562, are mutated. The nucleic acid sequences of the present invention further encode amino acid sequences corresponding to known human FVIII sequences, wherein the B-domain is deleted, the von Willebrand factor binding site is deleted, a thrombin cleavage site is mutated, an amino acid sequence spacer is inserted between the A2- and A3-domains. Provided herein are methods of producing the FVIII proteins of the invention, nucleotide sequences encoding such proteins, pharmaceutical compositions containing the nucleotide sequences or proteins, as well as methods of treating patients suffering from hemophilia. | 2013-03-21 |
20130072435 | TRIBONECTINS - The invention features a tribonectin and a method of tribosupplementation carried out by administering tribonectins directly to an injured or arthritic joint. | 2013-03-21 |
20130072436 | PROCESS FOR MANUFACTURING COLLAGEN AND TRACE ELEMENTS FROM SEA WATER - The process for manufacturing collagen and trace elements from sea water consists of various steps which are raw material preparation, resting of raw material, preliminary filtration to remove heavy metals, deodorize and purity remaining impurities, spraying of water, separation of heavy metals, collagen and trace elements from water and separation of collagen and trace elements. The process according to this invention, apart from sea water, can be applied to other type of salt water by adjusting the salinity and density of the water to an optimal value. The process according to this invention yields clean and purified collagen which is easily absorbed by human body and contains numerous types of trace elements. | 2013-03-21 |
20130072437 | NEUREGULIN ISOFORMS,NEUREGULIN POLYPEPTIDES AND USES THEREOF - The present invention relates to new therapeutic and diagnostic uses of soluble neuregulin-1 isoforms and polypeptides, particularly neurological disorders. | 2013-03-21 |
20130072439 | PEPTIDOMIMETIC MACROCYCLES - Disclosed are peptidomimetic macrocycles comprising a helix, such as an alpha helix, and methods of using such macrocycles for the treatment of disease such as cancer. In other aspects, the peptidomimetic macrocycle comprises an a,a-disubstituted amino acid, or may comprise a crosslinker linking the a-positions of at least two amino acids or at least one of said two amino acids may be an a,a-disubstituted amino acid. Further included is the targeting of components of the Wnt signaling pathway such as the Tcf4-/3-catenin complex. | 2013-03-21 |
20130072440 | CO-CRYSTALS AND PHARMACEUTICAL FORMULATIONS COMPRISING THE SAME - The pharmaceutical composition including a co-crystal. The co-crystal includes a) a co-former; and b) an active pharmaceutical ingredient (API) with solubility in water is less than one part by weight of the API in ten parts by weight of water. Furthermore, the formulation includes a polymer, and a weight ratio of the co-crystal to the polymer is about 0.5:99.5 to about 99.5:0.5. The kinetic solubility of the co-crystal after being in contact with an environment of use is at a therapeutically acceptable level for a prolonged period of time. | 2013-03-21 |
20130072441 | Protease Inhibitors and Preventives or Remedies for Disease | 2013-03-21 |
20130072442 | Viral Complement Control Proteins for Eye Disorders - The present invention provides compositions and methods for treating and/or preventing age related macular degeneration and other conditions involving macular degeneration or choroidal neovascularization, ocular inflammation, or any combination of these. Certain of the compositions comprise a poxvirus complement control protein or a complement binding fragment or variant thereof. Other compositions comprise a poxvirus complement control protein linked to a moiety that binds to a component present on or at the surface of cell or noncellular molecular entity, e.g., a component present in the eye of a subject at risk of or suffering from age related macular degeneration or a related condition or choroidal neovascularization, ocular inflammation, or any combination of these. Certain of the methods comprise administering a poxvirus complement control protein or complement binding fragment or variant thereof to a subject. | 2013-03-21 |
20130072443 | STABILIZED MUTANT OPSIN PROTEINS - Methods and compositions for stabilizing opsin protein in a vertebrate visual system are provided by administration of opsin-binding synthetic retinoids. | 2013-03-21 |
20130072444 | ORGANIC COMPOUND FOR THE REGULATION OF VECTORIAL ION CHANNELS - A cyclic organic compound which comprises 16 amino acids or 17 amino acids and has no carboxyl group C-terminally and/or no amino group N-terminally. Optionally, one of the amino acids is a normatural amino acid. The ring closure is formed between a side chain of one amino acid and the C-terminus of another amino acid, or the ring closure is effected with the aid of a normatural amino acid. A process for producing and using the compound for regulating vectorial ion channels, for treating diseases associated with the lung function and for treating oedemas is provided. | 2013-03-21 |
20130072445 | DEVELOPMENT OF C-REACTIVE PROTEIN MUTANT WITH IMPROVED THERAPEUTIC BENEFIT IN IMMUNE THROMBOCYTOPENIA AND LUPUS NEPHRITIS - The present invention relates to the use of a mutant CRP molecule in which tyrosine 175 is replaced by leucine (Y175L CRP) or the leucine 176 is replaced by glutamic acid (L176E CRP) for the treatment of various disease states and conditions associated with SLE, including lupus of the skin (discoid), systemic lupus of the joints, lungs and kidneys, hematological conditions including hemolytic anemia and low lymphocyte counts, lymphadenopathy and CNS effects, including memory loss, seizures and psychosis, among numerous others as otherwise disclosed herein. In another aspect of the invention, the reduction in the likelihood that a patient who is at risk for an outbreak of a disease state or condition associated with SLE will have an outbreak is an additional aspect of the present invention. The present invention relates to the use of mutant Y175L CRP or L176E CRP in the treatment of a number of disease states or conditions that occur secondary to systemic lupus SLE. The present invention also relates to the treatment of immune thrombocytopenic purpura. Pharmaceutical compositions are also disclosed based these mutant CRP molecules. | 2013-03-21 |
20130072446 | ANTI-INFLAMMATORY PHARMACEUTICAL PRODUCTS - Polypeptides having homology to regions of the N-terminal 50 residues of human Annexin 1 are provided for medical use as anti-inflammatory agents. Some of the polypeptides have homology to the N-terminal 48 residues of human Annexin 1, especially to residues 2-48 and 11-48 thereof. In some embodiments, properties of these compounds are improved by at least one modification at residues corresponding to residues 11, 22, 25 and/or 36 of human Annexin 1, and/or by C-terminal amidation of the polypeptide. Analogs of amino acids 2-26 of human Annexin 1, especially acetylated at the N-terminus and/or amidated at the C-terminus and having modifications at 11 and/or 22 are also disclosed for medical use as anti-inflammatory agents. | 2013-03-21 |
20130072447 | ENHANCED ORAL TRANSCOMPARTMENTAL DELIVERY OF THERAPEUTIC OR DIAGANOSTIC AGENTS - The invention is directed to pharmaceutical compositions and methods for delivery of a therapeutic or diagnostic agent from one bodily compartment to one or more other bodily compartment by administering one of the following conjugates: a polymer having multiple functional groups at least one of which is covalently bound to a therapeutic or diagnostic agent, and at least one cell uptake promoter covalently bound to the therapeutic or diagnostic agent; or a polymer and at least one cell uptake promoter bound thereto; the polymer further comprising multiple functional groups at least one of which is covalently bound a therapeutic or diagnostic agent. | 2013-03-21 |
20130072448 | Drug Combination Comprising A Glycolysis Inhibitor And A Tyrosine Kinase Inhibitor - A drug combination comprising at least one inhibitor of tyrosine kinase and at least one inhibitor of glycolysis. The drug combination may be used in the treatment of proliferative disorders, such as liver or colon cancer. The inhibitor of tyrosine kinase may be an inhibitor of at least one of the tyrosine kinases Fer and FerT. | 2013-03-21 |
20130072449 | LYSOPHOSPHATIDIC ACID RECEPTOR ANTAGONISTS - Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided. | 2013-03-21 |
20130072450 | ANTIOXIDATIVE AND HEPATOPROTECTIVE COMPOSITIONS CONTAINING DIARYLHEPTANOIDS FROM ALNUS JAPONICA - The present invention relates to antioxidative and hepatoprotective compositions, and more particularly to antioxidative and hepatoprotective compositions comprising diarylheptanoid compounds from | 2013-03-21 |
20130072451 | Low Viscosity Personal Care Composition - A low viscosity personal care composition comprising from about 10 % to about 99% of water, from about 0.01% to about 20% of a suspended particulate material, from about 0.01% to about 5% of an acrylic polymer, wherein the composition has a viscosity of from about 80 to about 1000 mPa·s, and a pH of from about 4 to about 9, wherein the acrylic polymer provide a selection yield value of at least 0.11 Pa. An array of two or more low viscosity personal care compositions, wherein one of the personal care compositions comprises said particulate material at a level different from those in the other personal care compositions. | 2013-03-21 |
20130072452 | PHARMACEUTICAL COMPOSITION AND METHOD FOR INHIBITING INFLAMMATION - A pharmaceutical composition for inhibiting inflammation is provided. The pharmaceutical composition comprises (a) hyaluronic acid, (b) a vitamin and (c) a pharmaceutically acceptable carrier. | 2013-03-21 |
20130072453 | HEAT STABLE HYALURONIC ACID COMPOSITIONS FOR DERMATOLOGICAL USE - The disclosure provides hyaluronic acid (HA) gel formulations and methods for treating the appearance of the skin. The formulations hyaluronic acid and at least one additional ingredient. Methods for treating lines, wrinkles, fibroblast depletions, and scars with the disclosed composition are provided as well. | 2013-03-21 |
20130072454 | ANTI-DIABETIC COMPOSTIONS AND METHODS - The present invention is concerned with synergistic compositions effective in the treatment of diabetes. In particular, the present invention is concerned with synergistic compositions comprising inulin, or a suitable source thereof, and Sulphonylureas used in the treatment of type-2 Diabetes Mellitus (T2DM) and hyperglyacemia. | 2013-03-21 |
20130072455 | Methods and Compositions for Treating Ectoparasite Infestation - Compositions and methods for killing ectoparasites on a subject. Compositions containing a fatty acid ester, e.g., isopropyl myristate, effective for killing ectoparasites is described. Also described are compositions containing a fatty acid ester and a siloxane (e.g., decacyclomethicone). The compositions can also contain a mectin and/or a mycin, and S-methoprene. The compositions are useful against a variety of ectoparasites that afflict humans, animals, and plants, e.g., head lice, fleas, body lice, crab lice, scabies, ticks, and plant parasites. | 2013-03-21 |
20130072456 | BICYCLIC TETRAHYDROPYRROLE COMPOUNDS - The present invention relates to substituted bicyclic tetrahydropyrrole compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well their use in the manufacture of a medicament for the treatment of humans and animals. | 2013-03-21 |
20130072457 | PYRAZOLYL QUINAZOLINE KINASE INHIBITORS - The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer. | 2013-03-21 |
20130072458 | Methods of Treating Viral Associated Diseases - The present invention provides methods of treating diseases associated with at least one virus. The methods include administering a compound described in the invention in a therapeutically effective amount. According to some aspects of the present invention, the methods may further comprise at least one immunosuppressant agent to treat diseases associated with at least one virus of a subject in need of immunosuppressant agents. | 2013-03-21 |
20130072459 | PHARMACEUTICAL COMPOSITION FOR THE PREVENTION OR THE TREATMENT OF NON-ALCOHOLIC FATTY LIVER DISEASE AND THE METHOD FOR PREVENTION OR TREATMENT OF NON-ALCOHOLIC FATTY LIVER DISEASE USING THE SAME - The present invention provides a pharmaceutical composition for the prevention and treatment of a non-alcoholic fatty liver disease (NAFLD), containing an active ingredient selected from the group consisting of Compound 1 represented by formula 1, sitagliptin, vildagliptin, linagliptin or a pharmaceutically acceptable salt thereof. Further, the present invention provides a method for the prevention or treatment of a non-alcoholic fatty liver disease, including administering an effective amount of an active ingredient selected from the group consisting of Compound 1 represented by formula 1, sitagliptin, vildagliptin, linagliptin or a pharmaceutically acceptable salt thereof to a mammal including a human in need thereof. Further, the present invention provides use of Compound 1 represented by formula 1, sitagliptin, vildagliptin, linagliptin or a pharmaceutically acceptable salt thereof, for manufacturing a pharmaceutical composition for the prevention or treatment of a non-alcoholic fatty liver disease. | 2013-03-21 |
20130072460 | Methods Of Treating Retroviral Infections And Related Dosage Regimes - The present invention relates to compounds and methods for treating retroviral infections and/or Hepatitis B viral infections. Some compounds of the invention are described by Formula (I) or a stereoisomer, a diastereomer, an enantiomer or racemate thereof. | 2013-03-21 |
20130072461 | TRIAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY - The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound. | 2013-03-21 |
20130072462 | Mitochondrial Compositions and Uses Thereof | 2013-03-21 |
20130072463 | PHARMACEUTICAL COMPOSITIONS USEFUL FOR PREVENTING AND TREATING CANCER - Disclosed is a method of treating a cancer on a mammal, comprising administering to the mammal in need thereof a therapeutically effective amount of a compound | 2013-03-21 |
20130072464 | PROGESTERONE RECEPTOR ANTAGONISTS - The invention relates to 17-hydroxy-17-pentafluoroethyl-estra-4,9(10)-dien-11-aryl derivatives of formula I with progesterone-antagonizing action and methods of production thereof, use thereof for the treatment and/or prevention of diseases and use thereof for producing medicinal products for the treatment and/or prevention of diseases, in particular uterine fibroids (myomata, uterine leiomyomata), endometriosis, heavy menstrual bleeding, meningiomata, hormone-dependent breast cancers and menopause-associated complaints or for fertility control and emergency contraception. | 2013-03-21 |
20130072465 | NOVEL BETULINIC ACID DERIVATIVES WITH ANTIVIRAL ACTIVITY - Compounds of Formula I: | 2013-03-21 |
20130072466 | COMPOSITION CONTAINING PLACENTA EXTRACTS - Provided is a composition containing placenta extracts as active ingredients. Placenta extracts are natural substances extracted from placentas of livestock and show effects that can replace steroids and reduce adverse effects of steroids, so that placenta extracts have a wide range of applications including contraceptives, anti-osteoporosis drugs, anti-anemic drugs, therapeutic agents for wasting diseases of muscular atrophy, agents for treating sexual dysfunction, therapeutic agents for wounds, and adipocyte differentiation stimulating agents for improving meat quality of livestock, etc. | 2013-03-21 |
20130072467 | NITROGEN-CONTAINING HETEROCYCLIC COMPOUND - The present invention provides a novel compound having a superior activity as an ERR-α modulator and useful as an agent for the prophylaxis or treatment of ERR-α associated diseases. | 2013-03-21 |
20130072468 | SUBSTITUTED PIPERAZINES AS CB1 ANTAGONISTS - Compounds of Formula (I): | 2013-03-21 |
20130072469 | HETEROARYL COMPOUNDS AND USES THEREOF - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. | 2013-03-21 |
20130072470 | NOVEL TRICYCLIC COMPOUNDS - The invention provides compounds of Formula (I) | 2013-03-21 |
20130072471 | Inhibitors of Ion Channels - Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-gated sodium channels. More particularly, the invention provides substituted aryl sulfonamides, compositions comprising these compounds, as well as methods of using these compounds or compositions in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrence of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a voltage-gated sodium channel. | 2013-03-21 |
20130072472 | NORIBOGAINE SALT ANSOLVATES - Stable noribogaine salt ansolvates are useful for preparing pharmaceutical compositions and for alleviating nociceptive pain in a patient. Such ansolvates can be prepared by slurrying solvated forms, preferably MeOH solvated noribogaine hydrochloride in EtOH/water. | 2013-03-21 |
20130072473 | COMPOUNDS FOR TREATING PROTEIN FOLDING DISORDERS - The present invention is directed to compounds of Formulae (I), (IIa-IIh), (IIIa-IIIe), (IVa-IVc), (Va-V1), (VIa-VII), (VII), (VIII) and (IX), pharmaceutical compositions thereof and methods of use thereof in the treatment of conditions associated with a dysfunction in proteostasis. | 2013-03-21 |
20130072474 | TREATMENT OF DEMENTIA OF ALZHEIMER'S TYPE WITH MASITINIB - The present invention relates to the use of masitinib or a pharmaceutically acceptable salt thereof, for the preparation of a medicament for the treatment of dementia of Alzheimer's type, at appropriate dosage regimen. | 2013-03-21 |
20130072475 | COMPOSITIONS AND METHODS FOR THE TREATMENT OF ASTHMA AND ASSOCIATED DISORDERS - This disclosure provides methods for treating asthma or an associated disorder in a patient in need thereof, by administering to the patient an effective amount of an autophagy inducing agent, thereby treating the asthma or the associated disorder. Disorders that can be treated include, allergic asthma, chronic obstructive pulmonary disease, lung inflammation, respiratory tolerance and a lung infection or disorder. | 2013-03-21 |
20130072476 | NOVEL PARENTERAL CARBAMAZEPINE FORMULATION - The present invention is directed to a carbamazepine-cyclodextrin inclusion complex useful for the parenteral administration of carbamazepine. The carbamazepine-cyclodextrin inclusion complex is prepared by the admixture of a modified cyclodextrin and carbamazepine in a physiologically acceptable fluid. Modified cyclodextrins include 2-hydroxypropyl-beta-cyclodextrin and sulfoalkyl cyclodextrins. More particularly, the sulfoalkyl cyclodextrins are those described and disclosed in U.S. Pat. Nos. 5,134,127 and 5,376,645. A physiologically acceptable fluid includes sterile isotonic water, Ringer's lactate, D5W (5% dextrose in water), physiological saline, and similar fluids suitable for parenteral administration. | 2013-03-21 |
20130072477 | TREATMENT OF PARKINSON'S DISEASE AND ENHANCEMENT OF DOPAMINE SIGNAL USING PDE 10 INHIBITOR - The present invention relates to a therapeutic or prophylactic method for treating Parkinson's disease by administering an effective amount of a compound having a phosphodiesterase 10 inhibitory activity; and also relates to a pharmaceutical composition for treatment or prophylaxis of Parkinson's disease comprising as an active ingredient a compound having a phosphodiesterase 10 inhibitory activity. Moreover, the present invention relates to a method for enhancing dopamine signal in the brain, which comprises administering an effective amount of a compound having a phosphodiesterase 10 inhibitory activity; and also relates to pharmaceutical composition for enhancing dopamine signal in brain comprising as an active ingredient a compound having a phosphodiesterase 10 inhibitory activity. | 2013-03-21 |
20130072478 | N-(3-(2-AMINO-6,6-DIFLUORO-4,4A,5,6,7,7A-HEXAHYDRO-CYCLOPENTA[E][1,3]OXAZI- N-4-YL)-PHENYL-AMIDES AS BACE1 INHIBITORS - The present invention provides N-(3-(2-amino-6,6-difluoro-4,4a,5,6,7,7a-hexahydro-cyclopenta[e][1,3]oxazin-4-yl)-phenyl)-amides of formula I | 2013-03-21 |
20130072480 | Cyclothiocarbamate Derivatives as Progesterone Receptor Modulators - Methods of using compounds which are progesterone receptor agonists for contraception and the treatment of progesterone-related maladies alone or in combination with an estrogen receptor agonist or progesterone receptor antagonist are provided. These compounds have the structure: | 2013-03-21 |
20130072481 | mTOR SELECTIVE KINASE INHIBITORS - The 4-urea-phenyl substituted 6-morpholin-4-yl-pyrazolo[3,4-d]pyrimidine derivatives are potent and selective inhibitors of mTOR kinase and are useful in treating disorders related to abnormal mTOR activities such as cancer, immune disorders, cardiovascular disease, ocular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. | 2013-03-21 |
20130072482 | ANTI-INFLAMMATORY COMPOUND HAVING INHIBITORY ACTIVITY AGAINST MULTIPLE TYROSINE KINASES AND PHARMACEUTICAL COMPOSITION CONTAINING SAME - The present invention is for the anti-inflammatory compounds that have an inhibitory activity against protein tyrosine kinases and their pharmaceutical composition(s) containing the compound as the active ingredient. Since the compounds of the present invention can inhibit multiple protein kinases associated with inflammatory diseases and immune disorders, they are useful for their prevention or treatment. | 2013-03-21 |
20130072483 | SUBSTITUTED HYDROXYETHYL AMINE COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE - The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I | 2013-03-21 |
20130072484 | TYROSINE KINASE INHIBITORS AS ANTI-KINETOPLASTID AND ANTI-APICOMPLEXAN AGENTS - The present invention provides methods of killing, inhibiting the growth, and/or inhibiting the reproduction of kinetoplastid or apicomplexan protozoan with tyrosine kinase inhibitors. | 2013-03-21 |
20130072485 | SOLUBLE MTOR COMPLEXES AND MODULATORS THEREOF - The present invention relates to small molecule modulators of mTORC1 and mTORC2, syntheses thereof, and intermediates thereto. Such small molecule modulators are useful in the treatment of proliferative diseases (e.g., benign neoplasms, cancers, inflammatory diseases, autoimmune diseases, diabetic retinopathy) and metabolic diseases. Novel small molecules are provided that inhibit one or more of mTORC1, mTORC2, and PI3K-related proteins. Novel methods of providing soluble mTORC1 and mTORC2 complexes are discussed, as well as methods of using the soluble complexes in a high-throughput manner to screen for inhibitory compounds. | 2013-03-21 |
20130072486 | PYRIMIDINE CYCLOHEXYL GLUCOCORTICOID RECEPTOR MODULATORS - The present invention provides a class of pyrimidinedione cyclohexyl compounds and methods of using these compounds as glucocorticoid receptor modulators. | 2013-03-21 |
20130072487 | PROLYL HYDROXYLASE INHIBITORS - The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I) | 2013-03-21 |
20130072488 | ARALKYL DIAMINE DERIVATIVES AND USES THEREOF AS ANTIDEPRESSANTS - Aralkyl diamine derivative of the following formula, pharmaceutically acceptable salts or uses thereof as antidepressants. The derivatives have triplex inhibiting activities of the reuptake of 5-HT, dopamine and noradrenalin, which can be administered to the patients in need of such treatment in the form of compositions orally or injectedly et al. | 2013-03-21 |
20130072489 | TRIAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY - The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to the use of a substituted triazole compound of the invention, or a composition comprising such a compound in the preparation of a medicament for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof. | 2013-03-21 |
20130072490 | POLYCYCLIC COMPOUNDS AS LYSOPHOSPHATIDIC ACID RECEPTOR ANTAGONISTS - Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases. | 2013-03-21 |
20130072491 | PROPHYLACTIC OR THERAPEUTIC AGENT FOR DIABETES OR OBESITY - An object is to provide a CaSR agonist agent that has excellent CaSR agonist effects, and particularly, a pharmaceutical product that can prevent or remedy diabetes or obesity by the effect of CaSR activation. The aforementioned object is achieved by a composition that contains a compound represented by the following General Formula (I) or a salt thereof (refer to the Description for the definitions of the symbols used in the formula). | 2013-03-21 |
20130072492 | SOLUBLE GUANYLATE CYCLASE ACTIVATORS - A compound of Formula (I): or a pharmaceutically acceptable salt thereof, are capable of modulating the body's production of cyclic guanosine monophosphate (“cGMP”) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of Formula I, or a pharmaceutically acceptable salt thereof, for their use in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of Formula (I) or a pharmaceutically acceptable salt thereof. | 2013-03-21 |
20130072493 | N-[4-(1H-PYRAZOLO[3,4-b]PYRAZIN-6-YL)-PHENYL]-SULFONAMIDES AND THEIR USE AS PHARMACEUTICALS - The present invention relates to N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides of the formula I, | 2013-03-21 |
20130072494 | INHIBITORS OF JUN N-TERMINAL KINASE - The present disclosure provides inhibitors of c-Jun N-terminal kinases (JNK) having a structure according to the following formula: | 2013-03-21 |
20130072495 | FUSED BICYCLIC KINASE INHIBITORS - Compounds of Formula I, as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as but not limited to tumors driven at least in part by at least one of RON, MET, IR, IGF-1R, or ALK. This Abstract is not limiting of the invention. | 2013-03-21 |
20130072496 | FORMULATIONS CONTAINING PYRIDAZINE COMPOUNDS - The invention relates to chemical compounds, compositions and methods of making and using the same. In particular, the invention provides selected pyridazine compounds of the formula I wherein R1, R4, R5, R6, R7, R8, R9, R12, R13 ET R14 are independently hydrogen, hydroxyl, alkyl, alkenyl, alkynyl, alkylene, alkenylene, alkoxy, alkenyloxy, cycloalkyl, cycloalkenyl, cycloalkynyl, cycloalkoxy, aryl, aryloxy, arylalkoxy, aroyl, heteroaryl, heterocyclic, acyl, acyloxy, amino, imino, azido, thiol, thioallyl, thioalkoxy, thioaryl, nitro, cyano, halo, sulfate, sulfonyl, sulfinyl, sulfonyl, sultanate, sulfoxide, silyl, silyloxy, silylalkyl, silylthio, =0, ═S, phosphonate, ureido, carboxyl, carbonyl, carbamoyl, or carboxamide; and X is optionally substituted pyrimidinyl or pyridazinyl, an isomer, a pharmaceutically acceptable salt, or derivative thereof. The invention additional relates to compositions comprising the compounds, and methods of using the compounds and compositions for modulation of cellular pathways, for treatment or prevention of inflammatory diseases, for research, drug screening, and therapeutic applications. | 2013-03-21 |
20130072497 | N- SUBSTITUTED PIPERAZINES - Novel N-alkyl substituted piperazines have been discovered, which are useful as insecticides or fungicides. Such compounds are of Formula (I) | 2013-03-21 |
20130072498 | TRANSDERMAL DELIVERY OF BENEFICIAL SUBSTANCES EFFECTED BY A HOSTILE BIOPHYSICAL ENVIRONMENT - The present invention generally relates to the transdermal delivery of substances and, in some embodiments, to the transdermal delivery of beneficial substances by a hostile biophysical environment. In one aspect, various methods for the transdermal delivery of beneficial substances are disclosed. By creating a hostile biophysical environment, beneficial substances may be delivered, according to certain embodiments, through the stratum corneum of the skin into the body. Beneficial substances include, but are not limited to, pharmaceutical agents, drugs, vitamins, co-factors, peptides, dietary supplements, and others. The beneficial effects disclosed include, for instance, relief of pain and inflammation, prevention and healing of ulcers of the skin, relief of headache, improved sexual function and enjoyment, growth of hair on the scalp, improving muscle size and/or function, removing body fat and/or cellulite, treating cancer, treating viral infections and others. | 2013-03-21 |
20130072499 | PIPERAZINE DERIVATIVES FOR BLOCKING Cav2.2 CALCIUM CHANNELS - The present invention relates to novel piperazine compounds; to pharmaceutical compositions containing the compounds; and to the use of the compounds in therapy to treat diseases for which blocking the Ca | 2013-03-21 |
20130072500 | PYRIMIDYL CYCLOPENTANES AS AKT PROTEIN KINASE INHIBITORS - The present invention provides compounds of Formula I including tautomers, resolved enantiomers, resolved diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. | 2013-03-21 |
20130072501 | 2,5-SUBSTITUTED OXAZOLOPYRIMIDINE DERIVATIVES - The invention relates to oxazolopyrimidine compounds of formula I, where A, R | 2013-03-21 |
20130072502 | HETEROCYCLIC CARBOXYLIC ACID DERIVATIVES HAVING A 2,5-SUBSTITUTED OXAZOLOPYRIMIDINE RING - Heterocyclic carboxylic acid derivatives comprising a 2,5-substituted oxazolopyrimidine ring as Edg-1 receptor agonists | 2013-03-21 |
20130072503 | TRISUBSTITUTED TRIAZOLOPYRIMIDINES FOR USE IN PLATELET AGGREGATION INHIBITION - The invention provides new triazolo[4,5-d]pyrimidine compounds, their use as medicaments, compositions containing them and processes for their preparation. | 2013-03-21 |
20130072504 | CRYSTALLINE FORMS OF A PURINE DERIVATIVE - The present invention relates to new crystalline forms of a purine derivative which exhibits excellent anti-tumour activity. The invention also relates to a pharmaceutical composition containing said crystalline forms as an active ingredient, and use thereof in the prevention or treatment of disease. The invention further relates to a process for preparing the crystalline forms. | 2013-03-21 |
20130072505 | 6,9-Disubstituted Purine Derivatives and Their Use for Treating Skin - The present invention provides methods and compositions for countering the adverse effects of aging on mammalian cells in vitro and in vivo, especially human skin cells and human skin, and treatment of hyperproliferative and related skin diseases in mammals by administering compositions containing 6,9-disubstituted purine derivatives. | 2013-03-21 |
20130072506 | 6,8-DISUBSTITUTED PURINE COMPOSITIONS - 6,8-Disubstituted purines which can be used in drug and cosmetic compositions and/or applications are provided. These 6,8-disubstituted purines have a wide range of biological activities, including for example anti-inflammatory, anti-senescent, as well as well as other activities which are especially useful in pharmaceutical and cosmetic applications. The 6,8-disubstituted purine compounds and compositions containing such 6,8-disubstituted purines provide growth-regulatory, differentiating, antisenescent and antiaging properties with improved selectivities and efficiencies and lower toxicities than analogues known heretofore. | 2013-03-21 |
20130072507 | COMBINATION - The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering N-{3-Chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methanesulphonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine, or a pharmaceutically acceptable hydrate and/or salt thereof, and N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide, or a pharmaceutically acceptable salt thereof, to a human in need thereof. | 2013-03-21 |
20130072508 | SOLID PHARMACEUTICAL DOSAGE FORM - A solid pharmaceutical dosage form providing improved oral bioavailability is disclosed for inhibitors of HIV protease. In particular, the dosage form comprises a solid dispersion of at least one HIV protease inhibitor and at least one pharmaceutically acceptable water-soluble polymer and at least one pharmaceutically acceptable surfactant, said pharmaceutically acceptable water-soluble polymer having a Tg of at least about 50° C. Preferably, the pharmaceutically acceptable surfactant has an HLB value of from about 4 to about 10. | 2013-03-21 |
20130072509 | PTEROSTILBENE AND STATIN COMBINATION FOR TREATMENT OF METABOLIC DISEASE, CARDIOVASCULAR DISEASE, AND INFLAMMATION - A pharmaceutical composition is provided comprising a therapeutically effective amount of pterostilbene, a therapeutically effective amount of a statin compound, and a pharmaceutically acceptable carrier. The embodiments of the pharmaceutical compositions can have lipid lowering properties, or alternatively can have properties that can treat oxidative stress, by decreasing inflammation or inflammatory processes contributing to neurodegenerative diseases. A method of lowering lipid levels in an individual is also provided, comprising administering to the individual in need of such treatment a pharmaceutical composition including a therapeutically effective amount of pterostilbene, a therapeutically effective amount of a statin compound, and a pharmaceutically acceptable carrier, wherein lipid levels are decreased. | 2013-03-21 |
20130072510 | Benzoimidazol-2-yl pyrimidines and pyrazines as modulators of the histamine H4 receptor - Benzoimidazol-2-yl pyrimidines and pyrazines, pharmaceutical compositions and methods for H | 2013-03-21 |
20130072511 | ANDROGEN RECEPTOR MODULATOR FOR THE TREATMENT OF PROSTATE CANCER AND ANDROGEN RECEPTOR-ASSOCIATED DISEASES - Described herein, inter alia, are compounds useful for the prevention or treatment of hyperproliferative diseases or disorders. | 2013-03-21 |
20130072512 | RIFAXIMIN READY-TO-USE SUSPENSION - A stable, taste-masked, ready-to-use suspension comprising rifaximin dispersed in a suspension base and one or more pharmaceutically acceptable additive(s). Also provided is a process for preparing a stable, taste-masked, ready-to-use suspension of rifaximin comprising the steps of mixing rifaximin with the suspension base and further sizing the particles of rifaximin by milling the suspension to obtain a homogenously dispersed rifaximin suspension. | 2013-03-21 |
20130072513 | COMBINATIONS OF BERBERINE, ARTEMISININ, Loperamide AND THEIR DERIVATIVES TO TREAT MALARIA, DIARRHEA, TRAVELERS' DIARRHEA, DYSENTERY, DENGUE FEVER, PARASITES, CHOLERA AND VIRUSES - This invention relates to compositions and methods of combining berberine, artemisinin and loperamide or their derivatives in a therapeutic product for mammals suffering from malaria, diarrhea, travelers' diarrhea, dysentery, dengue fever, parasites, cholera and viruses by administration of a therapeutically effective amount of the composition. | 2013-03-21 |
20130072515 | CRYSTALLINE FORMS OF AN 8-AZABICYCLO[3.2.1]OCTANE COMPOUND - The invention provides a crystalline sulfate salt of 3-endo-(8-{2-[cyclohexylmethyl-((S)-2,3-dihydroxy-propionypamino]ethyl}-8-aza-bicyclo[3.2.1]oct-3-yl) benzamide or a solvate thereof. The invention also provides pharmaceutical compositions comprising such crystalline salt forms, methods of using such crystalline salt forms to treat diseases associated with mu opioid receptor activity, and processes useful for preparing such crystalline salt forms. | 2013-03-21 |
20130072516 | METHOD OF ALCOHOL CESSATION AND TREATMENT - A method of alcohol cessation and treatment for a patient generally comprises the steps of administering a multi-vitamin to the patient, administering a medication group to the patient, and monitoring the patient. In various embodiments, the medication group may be administered to the patient via a first and second injection solution. The first injection solution generally comprises a therapeutically effective amount of an anti-addictive agent, such as naltrexone palmitate. The second injection solution generally comprises a therapeutically effective amount of an inhibitor of alcohol dehydrogenase, such as disulfiram. The method, which may also be referred to as procedure, may include various pre- and/or post-procedural steps as described herein. | 2013-03-21 |
20130072517 | PHARMACEUTICAL COMPOSITIONS COMPRISING DEXTROMETHORPHAN AND QUINIDINE FOR THE TREATMENT OF NEUROLOGICAL DISORDERS - Pharmaceutical compositions and methods for treating neurological disorders by administering same are provided. The compositions comprise dextromethorphan in combination with quinidine. | 2013-03-21 |
20130072518 | BICYCLIC COMPOUNDS AS alpha4 beta2 NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS - The present invention relates to novel bicyclic compounds of the formula (I), and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. These compounds are useful in the treatment and prevention of various disorders that are related to α | 2013-03-21 |
20130072519 | 2-PHENYL BENZOYLAMIDES - Compounds of Formula I that inhibit microsomal triglyceride transfer protein (MTP) and/or apolipoprotein B (Apo B) secretion and their uses in the treatment of diseases linked thereto in animals are described herein. | 2013-03-21 |
20130072520 | ANTIBACTERIAL AGENTS - Compounds of formula (I) have antibacterial activity: | 2013-03-21 |
20130072521 | THIENOPYRIDINE ESTER DERIVATIVE CONTAINING CYANO GROUP, PREPARATION METHOD, USE AND COMPOSITION THEREOF - A compound with the structure of the formula (I) or a pharmaceutically acceptable salt, a preparation method and use thereof are disclosed in the present invention, wherein R is cyano group. The compound provided by the present invention has an antiplatelet aggregation activity and can be used in preparing a medicament for preventing or treating cardiac and cerebral vascular diseases such as coronary artery syndromes, myocardial infarction and myocardial ischemia which are caused by platelet aggregation. | 2013-03-21 |
20130072522 | Process for Making Modulators of Cystic Fibrosis Transmembrane Conductance Regulator - The invention provides a process for the preparation of a compound of Formula 1, | 2013-03-21 |
20130072523 | ANALOGUES FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS - Compounds represented by Formula I: (I) or pharmaceutically acceptable salts thereof, wherein A, B, B′, X, Y, R1, R | 2013-03-21 |
20130072524 | Compositions And Methods Of Synthesis Of Pyridinolypiperidine 5-HT1F Agonists - The present invention provides a novel polymorph of the hemisuccinate salt of 2,4,6-trifluoro-N-[6-(1-methyl-piperidine-4-carbonyl)-pyridin-2-yl]-benzamide (Form A) characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure. This polymorph is useful in pharmaceutical compositions, for example, for the treatment and prevention of migraine. The invention also provides a process for the synthesis of pyridinoylpiperidine compounds of Formula I in high yield and high purity. In particular, the provides a process for the preparation of 2,4,6-trifluoro-N-[6-(1-methyl-piperidine-4-carbonyl)-pyridin-2-yl]-benzamide, its hemisuccinate salt and polymorph (Form A). | 2013-03-21 |
20130072525 | NITRATE AND DIAZENIUMDIOLATE DERIVATIVES OF PIOGLITAZONE - Nitrate ester and diazeniumdiolate derivatives of pioglitazone are described. They have valuable properties in the treatment of vascular and metabolic diseases, for example type 2 diabetes. | 2013-03-21 |
20130072526 | HYDROXYPYRIDONE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS THEREOF, AND THEIR THERAPEUTIC USE FOR TREATING PROLIFERATIVE DISEASES - Provided herein are hydroxypyridone derivatives, for example, a compound of Formula I, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a proliferative disease. | 2013-03-21 |
20130072527 | METHODS OF USING SUSTAINED RELEASE AMINOPYRIDINE COMPOSITIONS - Disclosed herein are methods and compositions related to use of aminopyridines, such as fampridine, to improve impairments of patients with a demyelinating condition, such as MS. | 2013-03-21 |
20130072528 | Methods for Treating HCV - The present invention features interferon-free therapies for the treatment of HCV. The therapies comprise administering Compound I (or a pharmaceutically acceptable salt thereof) and another anti-HCV agent. Preferably, the therapies are both interferon- and ribavirin-free. | 2013-03-21 |
20130072529 | PHARMACEUTICAL COMPOSITION COMPRISING ALEGLITAZAR - The invention relates to a pharmaceutical composition comprising aleglitazar and to the process of manufacture and uses thereof. | 2013-03-21 |
20130072530 | NOVEL EP4 AGONIST - Provided is a compound represented by the formula (1): | 2013-03-21 |
20130072531 | SOLID DISPERSION COMPRISING AN ANTI-HIV AGENT - The present invention relates to solid dispersions comprising a compound of formula | 2013-03-21 |
20130072532 | TOPICAL TRANSDERMAL DEXMEDETOMIDINE COMPOSITIONS AND METHODS OF USE THEREOF - Analgesic topical formulations of dexmedetomidine and methods of use thereof in the treatment and management of pain and other conditions. | 2013-03-21 |
20130072533 | COMPOUNDS WITH BOTH ANALGESIC AND ANTI-HYPERALGESIC EFFICACY - The present invention relates to molecules of formula (I), deriving from lipoic acid and camosine, their preparation and use as analgesics. | 2013-03-21 |
20130072534 | COMPOSITIONS COMPRISING VENLAFAXINE AND CELECOXIB IN THE TREATMENT OF PAIN - The present invention relates to pharmaceutical compositions comprising venlafaxine and celecoxib and their uses as medicaments, more particularly for the treatment of pain, including chronic pain; or of depression in patients which suffer from pain or in patients with a chronic musculo-skeletal inflammatory illness, with the inflammatory illness preferably being selected from osteoarthritis or rheumatoid arthritis. | 2013-03-21 |
20130072535 | PYRAZOLECARBOXAMIDE DERIVATIVES AND THEIR USE AS MICROBIOCIDES - Compounds of Formula (I) wherein R | 2013-03-21 |
20130072536 | PYRAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY - Compounds of formula (I), pharmaceutical compositions comprising compounds of formula (I) and methods of inhibiting Hsp90 in a cell, treating or preventing a proliferation disorder in a mammal and treating cancer in a mammal comprising administering a compound of formula (I) to a patient or a cell. | 2013-03-21 |