| 10th week of 2012 patent applcation highlights part 41 |
| Patent application number | Title | Published |
|---|
| 20120058940 | AZINONE-SUBSTITUTED AZAPOLYCYCLE MCH-1 ANTAGONISTS, METHODS OF MAKING, AND USE THEREOF - Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention. | 2012-03-08 |
| 20120058941 | GLUCOPYRANOSIDE COMPOUND - A compound of the formula: | 2012-03-08 |
| 20120058942 | METHODS FOR CONTROLLING BLOOD-GLUCOSE LEVELS IN INSULIN-REQUIRING SUBJECTS - The present invention relates to methods of controlling blood glucose levels in subjects receiving an insulin therapy. The methods include administering to the subject receiving an insulin therapy a dipeptidyl peptidase inhibitor and a GLP-1 related peptide. The present invention relates also to the use of such a combination for treating insulin-requiring diabetes mellitus and conditions related thereto. | 2012-03-08 |
| 20120058943 | Bioactive Hydrogel - The invention relates to a bioactive hydrogel as a hybrid material of heparin and star-branched polyethylene glycol with functionalized end groups, wherein the heparin is bound directly by reaction of the carboxyl groups activated with 1-ethyl-3-(3-dimethylaminopropyl) carbodiimides/N-hydroxysulfosuccinimide (EDC/s-NHS) with the terminal amino groups of the polyethylene glycol covalently by amide bonds. | 2012-03-08 |
| 20120058944 | BONE MORPHOGENETIC PROTEIN 2 (BMP2) VARIANTS WITH REDUCED BMP ANTAGONIST SENSITIVITY - The present invention is directed to an isolated peptide comprising or consisting of an amino acid sequence with an amino acid identity of at least 90% compared to mature human BMP2 with SEQ ID No. 1, characterized in that said amino acid sequence comprises at least two amino acid substitutions characterized in that a first amino acid substitution occurs at a position corresponding to N59, S88, E94, V99, K101 and/or N102 of SEQ ID No. 1 and to uses thereof. | 2012-03-08 |
| 20120058945 | NEUROPROTECTIVE IRON CHELATORS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM - Novel iron chelators exhibiting neuroprotective and good transport properties are useful in iron chelation therapy for treatment of a disease, disorder or condition associated with iron overload and oxidative stress, e.g., a neurodegenerative or cerebrovascular disease or disorder, a neoplastic disease, hemochromatosis, thalassemia, a cardiovascular disease, diabetes, an inflammatory disorder, anthracycline cardiotoxicity, a viral infection, a protozoal infection, a yeast infection, retarding aging, and prevention and/or treatment of skin aging and skin protection against sunlight and/or UV light. The iron chelator function is provided by a 8-hydroxyquinoline, a hydroxypyridinone or a hydroxamate moiety. The neuroprotective function is imparted to the compound, e.g., by a neuroprotective peptide. A combined antiapoptotic and neuroprotective function is provided by a propargyl group. | 2012-03-08 |
| 20120058946 | COMPOUND AND METHOD FOR TREATING MYOTONIC DYSTROPHY - An antisense compound for use in treating myotonic dystrophy DM1 or DM2, a method of enhancing antisense targeting to heart and quadricep muscles, and a method for treating DM1 or DM2 in a mammalian subject are disclosed. The oligonucleotide has 8-30 bases, with at least 8 contiguous bases being complementary to the polyCUG or polyCCUG repeats in the 3′UTR region of dystrophia myotonica protein kinase (DMPK) mRNA in DM1 or DM2, respectively. Conjugated to the oligonucleotide is a cell-penetrating peptide having the sequence (RXRR(B/X)R) | 2012-03-08 |
| 20120058947 | PROPHYLACTIC AGENT FOR HEART FAILURE - The present invention provides an agent having a suppressive action against the thickening of the heart wall, a prophylactic agent for heart failure containing the above described agent, and functional foods expected to have a prophylactic effect for heart failure. The agent for suppressing heart wall thickening comprises Xaa Pro Pro as an active ingredient. | 2012-03-08 |
| 20120058948 | Collagen peptides as immune modulators - The invention relates to collagen peptides, as well as related methods. The invention also relates to methods and products for modulating cytokine production and/or inflammation. | 2012-03-08 |
| 20120058949 | Methods of Treating Neurological Disorders - The present invention provides methods of treating epilepsy and other neurological disorders. The methods generally involve administering to an individual in need thereof an effective amount of an agent that blocks a transforming growth factor-beta pathway. | 2012-03-08 |
| 20120058950 | DETECTION OF NEUROPEPTIDES ASSOCIATED WITH PELVIC PAIN DISORDERS AND USES THEREOF - Diagnostic assessment and therapeutic treatment of pelvic pain disorders, including bladder disorders, bowel disorders, and/or reproductive tissue or organ disorders that are characterized by increased expression of the neuropeptides CGRP and/or PACAP. Additionally, applicants have developed a transgenic non-human model for pelvic pain disorders, where the transgenic animal expresses in bladder sensory neurons a recombinant neuropeptide implicated in the pelvic pain disorder. | 2012-03-08 |
| 20120058952 | HMG-COA REDUCTASE DERIVED PEPTIDE AND COSMETIC OR PHARMACEUTICAL COMPOSITION CONTAINING SAME - The present invention relates to a peptide of general formula (I):
| 2012-03-08 |
| 20120058953 | COMPOSITIONS AND METHODS FOR ENHANCING APOPTOSIS - The present invention is directed to compositions of matter useful for the enhancement of apoptosis in mammals and to methods of using those compositions of matter for the same. | 2012-03-08 |
| 20120058954 | Diaza Heterocyclic Compounds for Phototherapy - The invention relates generally to optical agents, including phototherapeutic agents, for biomedical applications, including phototherapy. The invention includes optical agents, and related therapeutic methods, comprising alicyclic diaza compounds, including 1,2 diaza heterocyclic compounds, having a photolabile N—N bond directly or indirectly linked to at least one carbocyclic aromatic and/or heterocyclic aromatic group. In some embodiments, for example, the invention provides alicyclic diaza compounds for phototherapeutic methods having a photolabile N—N bond that undergoes photoactivated cleavage to produce reactive species, such as radicals, ions, etc., that achieve a desired therapeutic effect, such as selective and/or localized tissue damage and/or cell death. | 2012-03-08 |
| 20120058955 | USE OF DECORINE FOR INCREASING MUSCLE MASS - The invention concerns decorin for increasing muscle mass, particularly in the treatment of muscular dystrophies. | 2012-03-08 |
| 20120058956 | PEPTIDES DERIVED FROM FICOLIN AS SURFACTANTS - Provided are peptides having a sequence that is a subsequence of a ficolin protein and methods of use thereof. The peptide may be a subsequence of human ficolin in which case it is essentially non-toxic. Further provided is a pharmaceutical composition including such peptides. The pharmaceutical composition can include an active ingredient for delivery through a body surface such as skin. | 2012-03-08 |
| 20120058957 | COMPOSITIONS AND METHODS FOR COUNTERACTING EFFECTS OF REACTIVE OXYGEN SPECIES AND FREE RADICALS - Peptide compounds and methods for upregulating expression of a gene encoding an antioxidative enzyme, such as superoxide dismutase or catalase, to counteract harmful oxidative effects of reactive oxygen species and other free radicals are described. The peptide compounds may be used to treat or prevent diseases and conditions characterized by undesirable elevation of reactive oxygen species and other free radicals, to upregulate AP-1 gene expression, and to treat pain. The peptide compounds may be used as components of pharmaceuticals and dietary supplements. | 2012-03-08 |
| 20120058958 | Small Peptides And Methods For Blocking IgE Mediated Activation Of An Immune Cell - Methods for treating cutaneous inflammation, are described. Also described is a method for inhibiting the mucous release into airways of a patient, a method for blocking IgE activation of an immune cell, a method for stabilizing the cell membrane of an immune cell, thereby preventing their further involvement in the increased inflammatory response to an IgE antigen challenge, and a method for inhibiting the migration of T-cells. Such methods involve administering to said patient a therapeutically effective amount of a peptide having the formula f-Met-Leu-X, wherein X is selected from the group consisting of Tyr, Tyr-Phe, Phe-Phe and Phe-Tyr. | 2012-03-08 |
| 20120058959 | TOPICAL ANTIVIRAL FORMULATIONS - The disclosure provides novel topical antiviral pharmaceutical compositions comprising one or more antiviral compounds and 2-deoxy-D-glucose in the form of lip-balms, creams and ointments. A specific embodiment discloses a lip-balm composition comprising acyclovir and 2-deoxy-D-glucose. | 2012-03-08 |
| 20120058960 | FEEDBACK PRODRUG - Compounds and methods for use in selectively inhibiting a lytic enzyme based on feedback inhibition are described. The conjugated compound serves as a substrate for a lytic enzyme. Cleavage of the conjugated compound by the lytic enzyme releases an inhibitor of the enzyme. | 2012-03-08 |
| 20120058961 | Pharmaceutical Composition for Treating Cancers - The preset invention relates to a new approach for treating cancer by using a synergistic combination of a histone deacetylase inhibitor and a furost-5-ene-3,22,26-triol glycoside. A pharmaceutical composition for treating a cancer comprising the synergistic combination and the treatment of a cancer with the synergistic combination are provided. | 2012-03-08 |
| 20120058962 | BUCCAL AND/OR SUBLINGUAL THERAPEUTIC FORMULATION - A buccal and/or sublingual formulation comprising one or more active compounds; and a buccal matrix which releases the active compounds at a predetermined rate for transport across the buccal and/or sublingual membranes, wherein the rate of release of the active compounds is either (A) the same or substantially the same rate at which the active compounds are transported across the buccal and/or sublingual membranes; or (B) a rate which releases the active compounds over an extended period as required by the therapeutic affect or treatment window for those active compounds. | 2012-03-08 |
| 20120058963 | Macrolides with Anti-Inflammatory Activity - The present invention relates to novel semi-synthetic macrolides having anti-inflammatory activity. More particularly, the invention relates to 14- and 15-membered macrolides substituted at the 4″ position, to their pharmaceutically acceptable derivatives, to processes and intermediates for their preparation, to pharmaceutical compositions containing them and to their activity and use in the treatment of inflammatory diseases and conditions in humans and animals, especially those diseases associated with excessive secretion of TNF-α, IL-1, IL-8, IL-2 or IL-5; and/or inhibitor of excessive lymphocyte proliferation; and/or excessive granulocyte degranulation. | 2012-03-08 |
| 20120058964 | PHARMACEUTICAL FORMULATION - Disclosed are novel formulations for the treatment of otic infections in an animal comprising a triazole anti-fungal compound, a quinolone antibiotic and a corticosteroid such as mometasone furoate monohydrate. | 2012-03-08 |
| 20120058965 | METHODS AND SYSTEMS FOR MODULATING HORMONES AND RELATED METHODS, AGENTS AND COMPOSITIONS - Provided herein are bitter taste receptor ligands, related agents, combinations, compositions, methods and systems for modulating release of a metabolic hormone in vitro or in vivo from cells of the GI tract of an individual. | 2012-03-08 |
| 20120058966 | Sphingosine Kinase Inhibitor Prodrugs - The invention relates to prodrugs of hydroxyl-substituted adamantane compounds, pharmaceutical compositions thereof, and methods for inhibiting sphingosine kinase and for treating or preventing hyperproliferative disease, inflammatory disease, or angiogenic disease. | 2012-03-08 |
| 20120058967 | VASCULAR PROTECTING AGENT HAVING SALT-ABSORPTION INHIBITORY ACTIVITY - This invention provides a vascular protecting agent having salt-absorption inhibitory activity with the use of alginate oligosaccharide salt absorbed by the body via degradation to an oligosaccharide, so that a patient can easily and safely ingest such agent on a routine basis. A vascular protecting agent having salt-absorption inhibitory activity comprises, as an active ingredient, alginate oligosaccharide obtained by treating sodium alginate with a | 2012-03-08 |
| 20120058968 | COMPOSITION CONTAINING FERMANTABLE POLYSACCHARIDES - The present invention relates to a composition to a nutritional composition comprising 0.1 to 15 gram fermentable partially hydrolysed gum having a degree of polymerisation between 10 and 300 per 100 gram dry weight of the composition and 0.1 to 15 gram fermentable, indigestible polysaccharide other than a hydrolysed gum having a DP between 10 and 300 per 100 gram dry weight of the composition. | 2012-03-08 |
| 20120058969 | Cystitis treatment with high dose chondroitin sulfate - Interstitial cystitis and related GAG-deficient conditions of the bladder and urinary tract are treated by instillation of high dose chondroitin sulfate, such as 400 mg/20 mL. The higher dose of chondroitin is effective for the rapid reduction of symptoms, particularly in patients with severe and otherwise recalcitrant cystitis. | 2012-03-08 |
| 20120058970 | METHOD AND SYSTEM FOR REVERSAL OF INTERACTIONS BETWEEN HYDROPHOBICALLY MODIFIED BIOPOLYMERS AND VESICLES OR CELL MEMBRANES - A method for reversing gelation of hydrophobically modified biopolymer attached to vesicle or cell membranes. The gelation of hydrophobically modified biopolymer attached to vesicles or cell membranes is reversed by application of a supramolecule, such as cyclodextrin, to the gelled composition. The supramolecule disrupts the interactions between the hydrophobically modified biopolymer and the vesicle or cell membrane, without affecting the structure of the membrane or the hydrophobically modified polymer to which the hydrophobic substituents are attached. A kit for treating wounds that includes a hydrophobically modified biopolymer and a supramolecule. The hydrophobically modified biopolymer is used to stop bleeding and the supramolecule is used to remove the hydrophobically modified biopolymer. | 2012-03-08 |
| 20120058971 | CYCLODEXTRIN-BASED POLYMERS FOR THERAPEUTIC DELIVERY - Methods and compositions relating to CDP-taxane conjugates are described herein. | 2012-03-08 |
| 20120058972 | NOVEL USE - The present invention relates to the use of a galactooligosaccharide in the prevention or treatment of an inflammatory disorder, in particular an intestinal inflammatory disorder. | 2012-03-08 |
| 20120058973 | COMPOSITIONS COMPRISING A SILICONE WATER-IN-OIL EMULSIFIER AND A LOW NITROGEN CONTAINING AMINO-FUNCTIONAL SILICONE GUM - Provided are compositions comprising a silicone water-in-oil emulsifier, a low nitrogen containing amino-functional silicone gum, a hydrophobic agent, a non-silicone primary emulsifier, and water. | 2012-03-08 |
| 20120058974 | Composition comprising pesticide and benzotriazole UV absorbers - The present invention relates to an agrochemical composition comprising pesticide and UV absorber. The invention furthermore relates to UV-absorbers and to the use thereof in agrochemical compositions. It moreover relates to a method of controlling phytopathogenic fungi and/or undesirable plant growth and/or undesirable insect or mite infestation and/or of regulating plant growth. | 2012-03-08 |
| 20120058975 | Phosphonate Compounds - The present invention relates to phosphonate compounds, compositions containing them, processes for obtaining them, and their use for treating a variety of medical disorders, e.g., osteoporosis and other disorders of bone metabolism, cancer, viral infections, and the like. | 2012-03-08 |
| 20120058976 | Phosphonate Ester Derivatives and Methods of Synthesis Thereof - The disclosure describes methods of synthesis of phosphonate ester derivatives. Preferred methods according to the disclosure allow for large-scale preparation of phosphonate ester compounds having high purity. In some embodiments, preferred methods according to the disclosure also allow for the preparation of phosphonate ester derivatives without the use of chromatographic purification methods and in better yield than previously used methods for preparing such compounds. Also disclosed are morphic forms of phosphonate ester derivatives. | 2012-03-08 |
| 20120058977 | PHARMACEUTICAL COMPOSITIONS AND METHODS FOR TREATING TUBERCULOSIS - A pharmaceutical composition for the treatment of a disease caused by a bacterium that belongs to the group of nocardioform actinomycetes, said composition comprising an effective amount of a compound selected from compound I, (+)-compound II, (−)-compound II, compound III, or mixtures thereof. | 2012-03-08 |
| 20120058978 | METHOD FOR THE TREATMENT OF CENTRAL NERVOUS SYSTEM CANCERS AND COMPOSITIONS RELATED THERETO - Use of compounds disclosed herein, typically progesterone or analog or derivative thereof, in the treatment of central nervous system cancers, specifically neuroblastoma and glioblastoma is provided. The treatment offers a reduced toxicity as compared to the currently available chemotherapeutic agents. The progesterone may be administered alone or in combination with, or in conjunction with other therapeutic agents. | 2012-03-08 |
| 20120058979 | METHODS AND REAGENTS FOR THE TREATMENT OF IMMUNOINFLAMMATORY DISORDERS - The invention features a method for treating a patient diagnosed with, or at risk of developing, an immunoinflammatory disorder by administering to the patient a tetra-substituted pyrimidopyrimidine, either alone or in combination with one or more additional agents. The invention also features a composition containing a tetra-substituted pyrimidopyrimidine in combination with one or more additional agents. | 2012-03-08 |
| 20120058980 | AEROSOL FORMULATION FOR THE INHALATION OF BETA AGONISTS - The present invention relates to a propellant-free aerosol formulation which contains one or more compounds of general formula 1, | 2012-03-08 |
| 20120058981 | ANDROGEN PHARMACEUTICAL COMPOSITION AND METHOD FOR TREATING DEPRESSION - The present invention relates to methods, kits, combinations, and compositions for treating, preventing or reducing the risk of developing a depressive disorder, or the symptoms associated with, or related to a depressive disorder in a subject in need thereof. The present invention also relates to a method of administering a steroid in the testosterone synthetic pathway, for example testosterone, to a subject in need thereof. In addition, the methods, kits, combinations and compositions may be used in conjunction with other pharmaceutical agents including agents effective at treating, preventing, or reducing the risk of developing a depressive disorder in a subject. | 2012-03-08 |
| 20120058982 | Analogs of Benzoquinone-Containing Ansamycins and Methods of Use Thereof - The present invention provides analogs of benzoquinone-containing ansamycins and uses thereof for treating and modulating disorders associated with hyperproliferation, such as cancer. The present invention provides analogs of benzoquinone-containing ansamycins where the benzoquinone is reduced to a hydroquinone and trapped by reaction with a suitable acid, preferably ones that increase the solubility and air stability of the resulting 17-ammonium hydroquinone ansamycin analog. | 2012-03-08 |
| 20120058983 | Adenosine A1 agonists for the treatment of glaucoma and ocular hypertension - The present invention relates to the use of selective adenosine A | 2012-03-08 |
| 20120058984 | PYRIMIDINE DERIVATIVES USED AS ITK INHIBITORS - The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): | 2012-03-08 |
| 20120058985 | CYCLOPROPYL DICARBOXAMIDES AND ANALOGS EXHIBITING ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES - The disclosed compounds are useful in the treatment of mammalian cancers and especially human cancers. Compounds, pharmaceutical compositions, and methods of Formula I are disclosed: | 2012-03-08 |
| 20120058986 | DI-AZETIDINYL DIAMIDE AS MONOACYLGLYCEROL LIPASE INHIBITORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: | 2012-03-08 |
| 20120058987 | THERAPEUTIC USES OF QUINAZOLINEDIONE DERIVATIVES - The subject matter of the present invention is the use of compounds of formula (I) in the form of a base, a hydrate or a solvate, or of mixtures thereof, as a medicament or for preparing a medicament intended for the treatment and/or prevention of disorders associated with the central nervous system (abbreviated to CNS) and/or associated with the peripheral nervous system (abbreviated to PNS). | 2012-03-08 |
| 20120058988 | CARBAZOLE AND CARBOLINE KINASE INHIBITORS - The present invention provides compounds of Formula (I) | 2012-03-08 |
| 20120058989 | ANTIBACTERIAL FLUOROQUINOLONE ANALOGS - Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): | 2012-03-08 |
| 20120058990 | Trans-4-[[(5S)-5-[[[3,5-bis(trifluoromethyl)phenyl]methyl] (2-methyl-2H-tetrazol-5-yl)amino]-2,3,4,5-tetrahydro-7,9-dimethyl-1H-1-be- nzazepin-1-yl]methyl]-cyclohexanecarboxylic acid - Abstract Compounds of a formula entitled, trans-4-[[(5S)-5-[[[3,5-bis(trifluoromethyl)phenyl]methyl](2-methyl-2H-tetrazol-5-yl)amino]-2,3,4,5-tetrahydro-7,9-dimethyl-1H-1-benzazepin-1-yl]methyl]-cyclohexanecarboxylic acid, as a free acid or a pharmaceutically acceptable salt thereof, hydrate, and hydrate in crystalline form; pharmaceutical formulations; and methods of use are disclosed. | 2012-03-08 |
| 20120058991 | Formulations and Methods of Administration of Cephalotaxines, Including Homoharringtonine - The present invention is directed to compositions and methods for the treatment of patients with cephalotaxines, for example, homoharringtonine. The invention is also directed to improvements in the purity, manufacturing process, formulation and administration of homoharringtonine for the treatment of cancer and other aberrant cellular diseases. The invention also provides methods and compositions for antiparasitic, antifungal, antiviral and antibacterial treatments. | 2012-03-08 |
| 20120058992 | THERAPEUTIC APPROACHES FOR TREATING ALZHEIMER DISEASE AND RELATED DISORDERS THROUGH A MODULATION OF ANGIOGENESIS - The present invention relates to compositions and methods for the treatment of Alzheimer's disease and related disorders. More particularly, the invention relates to combined therapies that modulate angiogenesis for treating said disease. | 2012-03-08 |
| 20120058993 | Stable Suspension Formulation - A physicochemically stable aqueous composition including clozapine suspension. | 2012-03-08 |
| 20120058994 | NOVEL COMPOUNDS - The invention relates to the novel salts AB of the base A with a physiologically acceptable acid B which is selected from the group consisting of hydrochloric acid, hydrobromic acid, sulfuric acid, fumaric acid and silcylic acid and the polymorphic compounds, the corresponding solvates and hydrates thereof. | 2012-03-08 |
| 20120058995 | METHODS OF CHEMICAL SYNTHESIS OF DIAMINOPHENOTHIAZINIUM COMPOUNDS INVOLVING THE USE OF PERSULFATE OXIDANTS - This invention pertains generally to the field of chemical synthesis and purification, and more specifically to methods of synthesizing and purifying certain 3,7-diamino-phenothiazin-5-ium compounds (referred to herein as “diaminophenothiazinium compounds”) including Methylthioninium Chloride (MTC) (also known as Methylene Blue). In one embodiment, the e//i method comprises the steps of in order: a thiosulfonic acid formation (TSAF) as illustrated below, wherein the reaction is carried out in the presence of a thio sulfate and an oxidizing agent that is or comprises persulfate an oxidative coupling (OC); and a ring closure (RC). The resulting compounds and compositions comprising them (e.g., tablets, capsules) are useful in methods of medical treatment and diagnosis, etc., for example, tauopathies, or Alzheimer's disease (AD). | 2012-03-08 |
| 20120058996 | CARBAZOLE CARBOXAMIDE COMPOUNDS USEFUL AS KINASE INHIBITORS - Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, | 2012-03-08 |
| 20120058997 | IMIDAZO[1,2-B]PYRIDAZINE AND PYRAZOLO[1,5-A]PYRIMIDINE DERIVATIVES AND THEIR USE AS PROTEIN KINASE INHIBITORS - The present invention provides protein kinase inhibitors comprising imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine compounds of the following structure (I) and (II): | 2012-03-08 |
| 20120058998 | Compounds, Compositions and Methods for the Treatment of Inflammatory Diseases - A method of inhibiting the inflammatory process, the method comprising administering to a mammal suffering from inflammation a therapeutically effective amount of a pharmaceutical composition comprising a compound | 2012-03-08 |
| 20120058999 | Substituted Tetrahydropyrrolopyrazine Compounds - Tetrahydropyrrolopyrazine compounds, methods for their preparation, pharmaceutical compositions containing such compounds, and a method of using such compounds for the treatment of pain and other conditions mediated at least partially by Bradykinin 1 receptors (B1R). | 2012-03-08 |
| 20120059000 | CHEMICAL COMPOUNDS, COMPOSITIONS AND METHODS FOR KINASE MODULATION - Chemical compounds that modulate kinase activity, including PI3 kinase activity, and chemical compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein. | 2012-03-08 |
| 20120059001 | NOVEL KINASE MODULATORS - The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them. | 2012-03-08 |
| 20120059002 | NOVEL ANTI-INFLAMMATORY AGENTS - Disclosed are methods of regulating interleukin-6 (IL-6) and/or vascular cell adhesion molecule-1 (VCAM-1) and methods of treating and/or preventing cardiovascular and inflammatory diseases and related disease states, such as, for example, atherosclerosis, asthma, arthritis, cancer, multiple sclerosis, psoriasis, and inflammatory bowel diseases, and autoimmune disease(s) by administering a naturally occurring or synthetic quinazolone derivative. The invention provides novel synthetic quinazolone compounds, as well as pharmaceutical compositions comprising those compounds. | 2012-03-08 |
| 20120059003 | INHIBITORS OF INV(16) LEUKEMIA - This invention describes the development of targeted small molecule inhibitors of the inv(16) fusion, the causative agent in ˜12% of acute myeloid leukemia (AML). The inv(16) fusion results in expression of the CBFβ-SMMHC fusion protein in the blood cells of afflicted patients. The present invention provides compounds which inhibit the function of both CBFβ and the CBFβ-SMMHC fusion. These compounds block the growth of an inv(16) leukemia cell line as well as increase its apoptosis, while showing minimal effects against non inv(16) cell lines. As a mechanism to develop inhibitors with selectivity for the CBFβ-SMMHC fusion protein, the present invention further provides dimeric derivatives of these compounds which show both increased potency as well selectivity for CBFβ-SMMHC. These compounds show potent inhibition of an inv(16) leukemia cell line with minimal effects on non inv(16) cell lines. Analysis of the pharmacokinetics of the developed compounds has made it possible to improve the lifetime of the compound in the plasma of mice to a level commensurate with long-term treatment. | 2012-03-08 |
| 20120059004 | Compounds And Compositions For Treating Cancer - The invention relates to compounds and composition for the treatment and prevention of cancer. The invention also covers all diseases that may be treated by selective modulation of levels of reactive oxygen species in diseased cells versus normal cells. Methods for the preparation and administration of such compositions are also disclosed. | 2012-03-08 |
| 20120059005 | COMBINATION OF (A) A PHOSPHOINOSITIDE 3-KINASE INHIBITOR AND (B) AN ANTIDIABETIC COMPOUND FOR USE IN THE TREATMENT OF PROLIFERATIVE DISEASES - The invention relates to a pharmaceutical combination which comprises (a) a phosphoinositide 3-kinase inhibitor compound and (b) an insulin sensitivity enhancer compound for the treatment of a proliferative disease, especially a solid tumor disease; a pharmaceutical composition comprising such a combination; the use of such a combination for the preparation of a medicament for the treatment of a proliferative disease; a commercial package or product comprising such a combination as a combined preparation for simultaneous, separate or sequential use; and to a method of treatment of a warm-blooded animal, especially a human. | 2012-03-08 |
| 20120059006 | SIGMA RECEPTOR INHIBITORS - The invention relates to compounds of formula I | 2012-03-08 |
| 20120059007 | Pharmacologically-active vanilloid carbamates - This application relates to pharmacologically-active vanilloid compounds which are useful for the treatment of various anti-inflammatory states characterized by inhibition of FAAH, such as, Alzheimer's dementia, Parkinson's disease, depression, pain, rheumatoid arthritis, pathophysiology of mood disorders, multiple sclerosis, and inflammation, or antagonism of TRPV1, such as, for example, Huntington's disease, hypertension, arthritis, allergic airway inflammation, Crohn's disease, ulcerative colitis, and neuropathic pain. | 2012-03-08 |
| 20120059008 | DIALKYLAMINO ALKYL ESTERS OF PIVAGABINE AS MEDICAMENTS FOR THE TREATMENT OF CENTRAL NERVOUS SYSTEM DISORDERS - The present embodiments are related to the compound of Formula 1 or Formula 2 below and pharmaceutical formulations thereof as well as treatments for a wide variety of Central Nervous System disorders with the pharmaceutical formulations. Some embodiments include the use of a variety of the instant compounds which surprisingly and advantageously exhibit improved pharmacokinetic and therapeutic profiles in comparison to pivagabine. | 2012-03-08 |
| 20120059009 | ANTI-TUMOR AGENT CONTAINING TEGAFUR-GIMERACIL-OTERACIL POTASSIUM COMBINATION DRUG AND OXALIPLATIN - To provide a novel combination therapy which exhibits remarkable anti-tumor effect. | 2012-03-08 |
| 20120059010 | ALPHA-HELIX MIMETICS AND METHODS RELATING TO THE TREATMENT OF FIBROSIS - The invention provides α-helix mimetic structures and a chemical library relating thereto. The compounds, pharmaceutical compositions comprising the compounds, and methods of the invention using the compounds, relate to the treatment of diseases including fibrosis, such as pulmonary fibrosis. | 2012-03-08 |
| 20120059011 | PHARMACEUTICAL COMPOSITIONS OF COMBINATIONS OF DIPEPTIDYL PEPTIDASE-4 INHIBITORS WITH PIOGLITAZONE - This invention relates to pharmaceutical compositions comprising fixed-dose combinations of a dipeptidyl peptidase-4 inhibitor and pioglitazone, methods of preparing such pharmaceutical compositions, and methods of treating Type 2 diabetes with such pharmaceutical compositions. | 2012-03-08 |
| 20120059012 | 3-(4-AMINOPHENYL)-2-FURANCARBOXYLIC ACID DERIVATIVE AND PHARMACEUTICALLY ACCEPTABLE SALT THEREOF - Disclosed is a compound represented by Formula (I) or a pharmaceutically acceptable salt thereof: | 2012-03-08 |
| 20120059013 | METHOD OF TREATING EARLY MORNING AKINESIA IN SUBJECTS HAVING PARKINSON'S DISEASE - The present invention provides a method for treating early morning akinesia, comprising continuous administration to a patient in need of such treatment a therapeutically effective amount of a dopamine agonist or a pharmaceutically acceptable salt, enantiomer, solvate, hydrate, polymorph or prodrug thereof. | 2012-03-08 |
| 20120059014 | Compounds for the Treatment of Metabolic Disorders - The present invention is directed to therapeutic compounds of the following formula (I) | 2012-03-08 |
| 20120059015 | NOVEL SPIROHETEROCYCLIC COMPOUNDS AS MGLU5 ANTAGONISTS - The invention is directed to methods of using antagonists selective for the metabotropic mGlu5 receptor to treat conditions of neuromuscular dysfunction of the lower urinary tract in a mammal. Provided are methods of treating a mammal suffering from a condition of neuromuscular dysfunction of the lower urinary tract by administering a selective mGlu5 antagonist. The selective mGlu5 antagonist may be administered alone or in combination with one or more additional therapeutic agents for treating such a condition. Also provided are methods of identifying selective mGlu5 antagonists that are useful for treating neuromuscular dysfunction of the lower urinary tract in a mammal. Methods for treating migraine and gastroesophageal reflux disease (GERD) using selective mGlu5 antagonists are also disclosed. | 2012-03-08 |
| 20120059016 | PIPERIDINE AND PIPERAZINE DERIVATIVES AS AUTOTAXIN INHIBITORS - The present invention relates to piperidine and pyrazine derivatives according to formulae (Ia), (Ib) and (II) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers. | 2012-03-08 |
| 20120059017 | CGRP Receptor Antagonist - The disclosure generally relates to the compound of formula I, (R)-N-(3-(7-methyl-1H-indazol-5-yl)-1-(4-(1-methylpiperidin-4-yl)piperazin-1-yl)-1-oxopropan-2-yl)-4-(2-oxo-1,2-dihydroquinolin-3-yl)piperidine-1-carboxamide, including pharmaceutically acceptable salts, which is a CGRP-receptor antagonist. The disclosure also relates to pharmaceutical compositions and methods for using the compound in the treatment of CGRP related disorders including migraine headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases such as asthma, chronic obstructive pulmonary disease (COPD), and cancer. | 2012-03-08 |
| 20120059018 | NOVEL CHLORIN E6-FOLIC ACID CONJUGATE, PREPARATION METHOD THEREOF, AND A PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF CANCER COMPRISING THE SAME - The present invention relates to a novel chlorin e6-folic acid conjugate, a preparation method thereof, and a pharmaceutical composition for the treatment of cancer comprising the same, and more particularly, to a novel compound prepared by linking chlorin e6 to folic acid, which effectively produces singlet oxygen in various media and has much better tumor selectivity than the known porphyrin-based photosensitizers, thereby being used effectively in photodynamic therapy for malignant tumors, a preparation method thereof, and a pharmaceutical composition for photodynamic treatment of solid tumors comprising the compound. | 2012-03-08 |
| 20120059019 | Compounds for the Treatment of Hepatitis C - The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV. | 2012-03-08 |
| 20120059020 | PROPHYLACTIC OR THERAPEUTIC AGENT FOR PULMONARY FIBROSIS - Disclosed is a compound which has an inhibitory activity on plasminogen activator inhibitor-1 (PAI-1) and has a propanedioic acid structure represented by formula (1) [wherein R | 2012-03-08 |
| 20120059021 | COMPOSITIONS AND METHODS FOR TREATING CANCER AND METHODS FOR PREDICTING A RESPONSE TO SUCH TREATMENTS - The present disclosure relates to the regulation and function of the Wnt/β-catenin signaling pathway and the ERK signaling pathway. The disclosure provides methods of treatment for melanoma by administering both an inhibitor of ERK signaling and an activator of Wnt/β-catenin signaling. These methods may be used alone or in combination with other strategies targeting melanoma cell survival. The disclosure also provides diagnostic methods for predicting a patient's clinical response to inhibitors of ERK signaling. | 2012-03-08 |
| 20120059022 | Crystalline Form of Bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]- pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoicacid] Calcium Salt - Two polymorphic forms of bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid] calcium salt, processes for making them and their use as HMG Co-A reductase inhibitors are described. | 2012-03-08 |
| 20120059023 | USE OF POLYMORPHIC FORMS OF RIFAXIMIN FOR MEDICAL PREPARATIONS - The present invention relates to Rifaximin polymorphic forms α, β and γ, to their use in medicinal preparations for the oral or topical route and to therapeutic methods using them. | 2012-03-08 |
| 20120059025 | DRY POWDER COMPOUND FORMULATIONS AND USES THEREOF - The present invention provides lyophilized formulations comprising methylnaltrexone, and processes for preparation of provided formulations. Additionally provided are compositions and products containing the methylnaltrexone formulation, as well as methods for producing formulations, compositions and products. Provided formulations as well as compositions and products containing methylnaltrexone formulations are useful for preventing, treating delaying, diminishing or reducing the severity and/or incidence of side effects resulting from administration of analgesic opioids. | 2012-03-08 |
| 20120059026 | ANTIMICROBIAL AGENTS - The invention provides a compound of formula (I): or a salt or prodrug thereof, wherein Y, W, Z, Z | 2012-03-08 |
| 20120059027 | TACROLIMUS INJECTION PREPARATION - A tacrolimus injection preparation comprising tacrolimus, polyoxyethylene castor oil (35), and non-aqueous solvent is disclosed. Preferably the weight ratio of polyoxyethylene castor oil (35) to tacrolimus in the injection preparation is 0-20:1. The injection preparation significantly decreased the clinical risk. | 2012-03-08 |
| 20120059028 | THIENO [2, 3-B] PYRIDINE DERIVATIVES AS VIRAL REPLICATION INHIBITORS - The present invention relates to a series of compounds having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to methods for the preparation of such compounds, as well as to novel intermediates useful in one or more steps of such syntheses. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutic amount of such compounds, optionally combined with one or more other drugs having anti-viral activity. | 2012-03-08 |
| 20120059029 | SELECTIVE INTEGRIN INHIBITORS - This invention provides methods for selectively antagonizing the α4β1 integrin heterodimer in a subject in need thereof, and preferably in a human subject. The methods of the invention utilize conjugates comprising two or more α4β1 small molecule antagonists covalently attached to a biocompatible polymer. These methods of selectively inhibiting α4β1 may be used modulate both normal and pathological biological processes mediated at least in part through α4β1 activity. | 2012-03-08 |
| 20120059030 | HETEROCYCLIC COMPOUND AND USE THEREOF - The present invention provides a heterocycle derivative having a superior amyloid β production inhibitory activity and/or a superior γ-secretase modulation activity, and use thereof. A compound represented by the formula (I): | 2012-03-08 |
| 20120059031 | COMBINATIONS COMPRISING ANTIMUSCARINIC AGENTS AND PDE4 INHIBITORS - A combination which comprises (a) a PDE4 inhibitor and (b) an antagonist of M3 muscarinic receptors which is (3R)-1-phenethyl-3-(9H-xanthene-9carbonyloxy)-1-azoniabicyclo[2.2.2]octane, in the form of a salt having an anion X, which is a pharmaceutically acceptable anion of a mono or polyvalent acid. | 2012-03-08 |
| 20120059032 | 1,2,3,4-TETRAHYDROISOQUINOLINE DERIVATIVES EFFECTIVE AS ANTIGLIOMA AGENTS, METHODS OF MAKING, AND THEIR USE - Disclosed are tetrahydroisoquinoline-derivative compounds effective for killing cancer cells, shrinking tumor size, and treating cancer. | 2012-03-08 |
| 20120059033 | Crystalline Salts of a Potent HCV Inhibitor - This invention relates to novel tris(hydroxymethyl)aminomethane, choline and N-methyl-D-glucamine salt forms of the following Compound (1) and methods for the preparation thereof, pharmaceutical compositions thereof, and their use in the treatment of Hepatitis C Viral (HCV) infection: | 2012-03-08 |
| 20120059034 | NOVEL CRYSTALLINE HYDRATE, AMORPHOUS AND POLYMORPHIC FORMS OF DIHYDRO-BENZOXAZOLE-6-YL-ACETAMIDE DERIVATIVE AND PROCESSES FOR THEIR PREPARATION - The invention relates to novel crystalline hydrate, amorphous and crystalline polymorphic forms of 2-[4-(4-Fluoro-benzyl)-piperidine-1-yl]-2-oxo-N-(2-oxo-2,3-dihydro-benzoxazole-6-yl)-acetamide (I) (radiprodil). Processes for the preparation of these forms, compositions containing these forms, and methods of use thereof are also described. | 2012-03-08 |
| 20120059035 | METHOD OF PREDICTING A PREDISPOSITION TO QT PROLONGATION - The present invention describes an association between genetic polymorphisms in the BAI3 gene and a predisposition to prolongation of the QT interval, and provides related methods for the prediction of such a predisposition, the administration of QT interval-prolonging compounds to individuals having such a predisposition, and determining whether a compound is capable of inducing QT prolongation. | 2012-03-08 |
| 20120059036 | METHOD FOR REDUCING THROMBOCYTOPENIA AND THROMBOCYTOPENIA-ASSOCIATED MORTALITY - Disclosed are methods for reducing the risk of thrombocytopenia-associated mortality and morbidity, and for reducing the risk of becoming thrombocytopenic, in patients whose treatment requires inhibition of platelet aggregation. The methods involve administration of a pharmaceutically acceptable salt of tirofiban. | 2012-03-08 |
| 20120059037 | SUBSTITUTED PYRIDINE DERIVATIVES AND THEIR MEDICAL USE - The present application discloses novel substituted pyridinyl-methylamine derivatives and their use as modulators of the voltage gated K | 2012-03-08 |
| 20120059038 | POLYKETIDE COMPOUND | 2012-03-08 |
| 20120059039 | ANTI-SHOCK AGENT COMPRISING DIAMINOTRIFLUOROMETHYLPYRIDINE DERIVATIVE - Septic shock is known to lead to, at the end stage, systematic inflammatory reaction syndrome and multiple organ failure (MOF) and cause the patients' death. In both diseases, the patient dies finally of MOF, and the infiltration by inflammatory cells plays a key role for MOF. Thus, development of therapeutic agents for septic shock by suppressing the infiltration by inflammatory cells has been desired. | 2012-03-08 |
| 20120059040 | NOVEL FORMS OF [R-(R*,R*)]-2-(4-FLUOROPHENYL)-beta,delta-DIHYDROXY-5-(1-METHYLETHYL)-3-P- HENYL-4-[(PHENYLAMINO)CARBONYL]-1H-PYRROLE-1-HEPTANOIC ACID MAGNESIUM - Novel forms of atorvastatin magnesium salt designated Form A, Form B, Form C, Form D, Form E, and Form F, pharmaceutical compositions containing such compounds, methods for their preparation and methods utilizing the compounds for treatment of hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia (BPH) and Alzheimer's disease are described. | 2012-03-08 |
| 20120059041 | Methods for Extending Lifespan in Subject - Disclosed is a method for extending lifespan in a subject. By screening for mutations that enhance resistance to multiple stresses, the invention identified multiple alleles of alpha-1, 2-mannosidase I (mas1) which, in addition to promoting stress resistance, also extended longevity. Meanwhile, longevity enhancement of a subject is also observed when either the expression of mas1 or its downstream gene Edm1 is reduced. Furthermore, this invention also found that the down-regulating mas1 and Edm1 may extend longevity by modulating DR (Dietary Restriction). Thus, via molecular biology techniques, the expression of the target genes such as mas1 and Edm1 can be regulated, and the lifespan extension for a subject also can be achieved. | 2012-03-08 |
