| 17th week of 2013 patent applcation highlights part 49 |
| Patent application number | Title | Published |
| 20130102559 | METHODS OF USING (+)-1,4-DIHYDRO-7-[(3S,4S)-3-METHOXY-4-(METHYLAMINO)-1-PYRROLIDINYL]-4-OX- O-1-(2-THIAZOLYL)-1,8-NAPHTHYRIDINE-3-CARBOXYLIC ACID FOR TREATMENT OF ANTECEDENT HEMATOLOGIC DISORDERS - Methods of treating, preventing or managing antecedent hematologic disorders, such as myelodysplastic syndrome, including chronic myelomonocytic leukemia are disclosed. The methods encompass the administration of SNS-595. Also provided are methods of treatment using this compound with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy. In certain embodiments, the method of treatment comprise administering SNS-595 in combination with cytarabine. Pharmaceutical compositions and single unit dosage forms suitable for use in the methods are also disclosed. | 2013-04-25 |
| 20130102560 | NUTRITIONAL COMPOSITION COMPRISING IMMUNOGLOBULINS AND OLIGOSACCHARIDES - The present invention provides a method and composition for the treatment and/or prevention of infection, said method comprising orally administering a composition to a mammal, said composition comprising a galactose containing indigestible oligosaccharide and immunoglobulin from the milk or colostrum of hyperimmunized cows. | 2013-04-25 |
| 20130102561 | Stabalized Glycosaminoglycan Preparations and Related Methods - Compositions comprising a glycosaminoglycan (e.g., a hyaluronan, hyaluronic acid, hyaluronate, sodium hyaluronate, dermatan sulfate, karatan sulfate, chondroitin 6-sulfate, heparin, etc.) in combination with at least one component selected from; i) polyglycols (e.g., polyethylene glycol), ii) long chain hydroxy polyanionic polysaccharides (e.g., dextran, sodium alginate, alginic acid, propylene glycol alginate, carboxymethyl cellulose and carboxyethyl cellulose, hydroxyl ethyl starch, hydroxyl propyl methyl cellulose, hydroxy propyl ethyl cellulose, hydroxy propyl cellulose, methyl cellulose, polylysine, polyhistidine, polyhydroxy proline, poly ornithine, polyvinyl pyrolidone, polyvinyl alcohol, chitosan, etc.) and iii) long chain Nitrogen containing polymers (e.g., Polylysine, Polyvinylpyrrolidone, and polyvinyl alcohol). The invention also includes methods for using such compositions (e.g., as substance delivery materials, tissue fillers or bulking agents, as moistening or hydrating agents, etc.) | 2013-04-25 |
| 20130102562 | INHIBITION OF CATHEPSIN K ACTIVITY AND THE TREATMENT AND PREVENTION OF DISEASE - The present invention provides a candidate compound that is suitable for use in methods of treating animals (preferably mammals) and in the preparation of a medicament, wherein the candidate compound down regulates Cathepsin K activity. | 2013-04-25 |
| 20130102563 | DERMAL FILLER WITH LIDOCAINE - Disclosed herein are cohesive soft tissue fillers, for example, dermal and subdermal fillers, based on hyaluronic acids and pharmaceutically acceptable salts thereof. In one aspect, hyaluronic acid-based compositions described herein include a therapeutically effective amount of at least one anesthetic agent, for example, lidocaine. The present hyaluronic acid-based compositions including lidocaine have an enhanced stability and cohesivity, relative to conventional compositions including lidocaine, for example when subjected to sterilization techniques or when stored for long periods of time. Methods and processes of preparing such hyaluronic acid-based compositions are also provided. | 2013-04-25 |
| 20130102564 | TOPICAL PHARMACEUTICAL COMPOSITION COMPRISING HEPARIN - The present invention relates to a topical pharmaceutical composition comprising heparin and to the use thereof for preventing a functional complication of A-V fistulas and A-V grafts in chronic haemodialysis patients. | 2013-04-25 |
| 20130102565 | SEMULOPARIN FOR THE PREVENTION OF A MORTALITY AND/OR MORBIDITY EVENT IN A PATIENT UNDERGOING MAJOR ORTHOPEDIC SURGERY - The invention relates to the use of semuloparin or a pharmaceutically acceptable salt thereof for the prevention of a mortality and/or morbidity event, more specifically venous thromboembolism and death, in a patient undergoing major orthopedic surgery, such as hip replacement, knee replacement or hip fracture surgery. | 2013-04-25 |
| 20130102566 | SEMULOPARIN FOR USE AS AN ANTITHROMBOTIC TREATMENT IN HIP REPLACEMENT SURGERY WITH IMPROVED SAFETY IN TERMS OF CLINICALLY RELEVANT BLEEDINGS AND MAJOR BLEEDINGS - The invention relates to the use of semuloparin or a pharmaceutically acceptable salt thereof as an antithrombotic treatment in patients undergoing hip replacement surgery, wherein said use involves an improved safety in terms of clinically relevant bleedings and of major bleedings compared to a standard antithrombotic treatment. | 2013-04-25 |
| 20130102567 | 3-Desoxy-2-Methylene-Vitamin D Analogs and Their Uses - This invention discloses 3-desoxy-2-methylene-vitamin D analogs, and specifically (20S)-3-desoxy-1α,25-dihydroxy-2-methylene-vitamin D | 2013-04-25 |
| 20130102568 | ALKOXYIMINO DERIVATIVE AND PEST CONTROL AGENT - [PROBLEMS] The present invention provides a novel alkoxyimino derivative or a salt thereof, as well as to a pest control agent containing the derivative or salt thereof as an active ingredient, which shows an excellent pest control effect on a wide range of pests in the agricultural and horticultural field and is also capable of controlling resistant pests. | 2013-04-25 |
| 20130102569 | Methods and Compositions for Preventing or Treating Age-Related Diseases - The invention provides methods for treating or preventing an age-related disease, condition, or disorder comprising administering a therapeutically effective amount of an inhibitor of TOR to a patient in need thereof. The invention also provides pharmaceutical compositions and topical formulations for treating or preventing an age-related disease, condition, or disorder comprising an inhibitor of TOR and a pharmaceutically acceptable carrier. In particular, the invention provides methods, pharmaceutical compositions, and topical formulations comprising rapamycin or an analog of rapamycin. | 2013-04-25 |
| 20130102570 | PROPHYLACTIC AGENT OR THERAPEUTIC AGENT FOR DIABETES OR OBESITY - A medicament having an excellent CaSR agonist action which enables the prevention or treatment of diabetes or obesity is provided by a composition comprising the compound represented by general formula (I) as defined, or a salt thereof. | 2013-04-25 |
| 20130102571 | SELECTIVE SIGMA-1 RECEPTOR LIGANDS - The invention provides compounds of the formulas described herein and compositions thereof. The invention further provides methods of using the compounds and compositions. The compounds of the invention can provide high affinity binding to sigma-1 receptors in a mammal. The compounds can exhibit selectivity for the sigma-1 receptor over the sigma-2 receptor. The compounds and compositions of the invention can also be used to treat conditions that involve the sigma-1 receptor, such as addiction, cardiovascular conditions, and cancer, for example, cancer of the breast, lung, prostate, ovarian, colorectal, or the CNS. | 2013-04-25 |
| 20130102572 | METHODS OF TREATING SKIN CONDITIONS EXHIBITING TELANGIECTASIA - The present application relates to methods of preventing or treating skin disorders exhibiting telangiectasia, for example, rosacea exhibiting an erythematotelangiectatic subtype. Exemplary methods comprise administering to a patient a formulation comprising a therapeutically effective amount of an mTOR inhibitor, such as rapamycin, wherein the mTOR inhibitor is the only active agent in the formulation. Suitably, the formulations are topical formulations administered to the face. | 2013-04-25 |
| 20130102573 | 2-METHYLENE-VITAMIN D ANALOGS AND THEIR USES - This invention discloses 2-methylene-vitamin D analogs, and specifically (20S)-25-hydroxy-2-methylene-vitamin D | 2013-04-25 |
| 20130102574 | 2-METHYLENE-VITAMIN D ANALOGS AND THEIR USES - This invention discloses 2-methylene-vitamin D analogs, and specifically (20S)-1α,25-dihydroxy-2-methylene-vitamin D | 2013-04-25 |
| 20130102575 | PHARMACEUTICAL COMPOSITIONS COMPRISING DGLA, 15-OHEPA, AND/OR 15-HETRE AND METHODS OF USE THEREOF - The present disclosure provides compositions comprising fatty acids, or derivatives thereof (e.g., C1-C4 esters) including, for example, DGLA, 15-OHEPA and/or 15-HETrE, used singly or in combination with anti-bacterial agents for the treatment of disease and/or disorders such as acne or atopic dermatitis. | 2013-04-25 |
| 20130102576 | DERIVATIVES OF 1-PHENYL-2-PYRIDINYL ALKYL ALCOHOLS AS PHOSPHODIESTERASE INHIBITORS - Compounds, pyridine N-oxides, and pharmaceutically acceptable salts of formula (I) are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme and for preventing and/or treating diseases of the respiratory tract characterized by airway obstruction, such as asthma or COPD. | 2013-04-25 |
| 20130102577 | SHIP INHIBITORS AND USES THEREOF - The present invention relates to SHIP inhibitor compounds and methods for using these compounds. In particular, the present invention discloses the following methods: (i) a method of treating graft versus host disease in a subject; (ii) a method of inhibiting a SHIP1 protein in a cell; (iii) a method of selectively inhibiting a SHIP1 protein in a cell; (iv) a method for treating or preventing graft-versus-host disease (GVHD) in a recipient of an organ or tissue transplant; (v) a method of modulating SHIP activity in a cell expressing SHIP1 or SHIP2; (vi) a method of ex vivo or in vitro treatment of transplants; (vii) a method of inhibiting tumor growth and metastasis in a subject; (viii) a method of treating a hematologic malignancy in a subject; (ix) a method of inducing apoptosis of multiple myeloma cells; (x) a method of treating multiple myeloma in a subject; (xi) a method of inhibiting the proliferation of a human breast cancer cell; and (xii) a method of treating breast cancer in a subject. | 2013-04-25 |
| 20130102578 | New Steroids Having Increased Water Solubility and Resistance Against Metabolism and Methods For Their Production - Steroid compounds having increased resistance against metabolism and increased water solubility are disclosed, together with methods for their production. These substances are suitable for the manufacture of pharmaceuticals for the treatment of steroid related or steroid induced CNS disorders and for use in methods of prevention, alleviation or treatment of such disorders. | 2013-04-25 |
| 20130102579 | Steroids Having Increased Water Solubility and Resistance Against Metabolism and Methods For Their Production - Steroid compounds having increased resistance against metabolism and increased water solubility are disclosed, together with methods for their production. These substances are suitable for the manufacture of pharmaceuticals for the treatment of steroid related or steroid induced CNS disorders and for use in methods of prevention, alleviation or treatment of such disorders. | 2013-04-25 |
| 20130102580 | COMPOSITIONS AND METHODS RELATED TO DEOXYCHOLIC ACID AND ITS POLYMORPHS - Provided herein are polymorphic forms of deoxycholic acid (DCA), improved methods of synthesizing DCA and intermediates thereto, and compositions and fat removal methods employing the DCA as provided herein. | 2013-04-25 |
| 20130102581 | COMPOSITION AND METHOD FOR TREATMENT OF DIABETES - The present invention relates to a method of treating an incretin related disease such as diabetes, obesity and the like by delivery of butyric acid, bile acid, long chain fatty acid, or glutamine to the colon by bypassing the upper digestive tract. | 2013-04-25 |
| 20130102582 | COMPOSITIONS AND METHODS FOR TREATING AND PREVENTING CORONARY HEART DISEASE - The invention pertains to a method of determining a statin dosage for an individual in need of treatment with a statin, comprising determining a SLCO1B1 genotype from a nucleic acid sample of the individual, said genotype comprising the presence or absence of the SLCO1B1-056 polymorphism, and determining an ApoE genotype or phenotype identifying an ApoE polymorphism selected from the group consisting of ApoE2, ApoE3, ApoE4, and any combination thereof, wherein the combination of a SLCO1B1 genotype identifying the presence of the SLCO1B1-056 C polymorphism and the ApoE genotype or phenotype identifying one of the ApoE3/4 or ApoE4/4 genotypes indicates the statin dosage. | 2013-04-25 |
| 20130102583 | CEPHEM COMPOUND HAVING CATECHOL GROUP - A compound of the formula: | 2013-04-25 |
| 20130102584 | PIPERIDIN-4-YL-AZETIDINE DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds, and enantiomers, diastereomers, and pharmaceutically acceptable salts thereof, are represented by Formula (I) as follows: | 2013-04-25 |
| 20130102585 | AZETIDINYL DIAMIDES 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: | 2013-04-25 |
| 20130102586 | SUBSTITUTED 5-(PYRAZIN-2-YL)-1H-PYRAZOLO [3, 4-B] PYRIDINE AND PYRAZOLO [3, 4-B] PYRIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS - Substituted 5-(pyrazin-2-yl)-1H-pyrazolo[3,4-b]pyridine, 5-(pyrazin-2-yl)-1H-pyrrolo[2,3-b]pyridine and pyrazolo[3,4-b]pyridine derivatives according to formula I, II and VII, and methods for making same, which are inhibitors of constitutively activated Tyrosine Kinase-Like (TKL), CMGC protein kinases family members and can be useful in the treatment of Parkinson's disease, Alzheimer's disease, Down's Syndrome, Huntington's disease, other neurodegenerative and central nervous system disorders, cancer, metabolic disorders and inflammatory diseases. Also disclosed are pharmaceutical compositions including the compounds and methods of inhibiting wild type and/or mutated protein kinase activities of these families and the treatment of disorders associated therewith using compounds and pharmaceutical compositions including the compounds. | 2013-04-25 |
| 20130102587 | New Enzyme Inhibitor Compounds - Disclosed are compounds which inhibit SSAO enzyme activity. Also disclosed are pharmaceutical compositions comprising these compounds and the use of these compounds in the treatment or prevention of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases, immune disorders and the inhibition of tumour growth. | 2013-04-25 |
| 20130102588 | TOLVAPTAN SOLID DISPERSION AND ITS PREPARATION METHOD - A tolvaptan solid dispersion and its preparation method are disclosed. The solid dispersion comprises tolvaptan and cross-linked polyvinylprrolidone at a weight ratio of 1:0.05-20, preferably 1:0.1-10, and more preferably 2:1. The solid dispersion can further comprise one or more water-soluble polymers, such as polyvinylprrolidone, hydroxypropyl cellulose, hydroxyethyl cellulose or methylcellulose, wherein the weight ratio of tolvaptan:the crosslinked polyvinylprrolidone:the water-soluble polymers is preferably 2:1:0.1. The solid dispersion exhibits good thermodynamic stability and solubility. The pharmaceutical composition thereof has improved release rate and bioavailability. | 2013-04-25 |
| 20130102589 | Novel Compound for the Treatment of Hepatitis C - The present invention provides (1aR,12bS)-8-cyclohexyl-11-fluoro-N-((1-methylcyclopropyl)sulfonyl)-1a-((3-methyl-3,8-diazabicyclo[3.2.1]oct-8-yl)carbonyl)-1,1a,2,12b-tetrahydrocyclopropa[d]indolo[2,1-a][2]benzazepine-5-carboxamide (formula I), including pharmaceutically acceptable salts, as well as compositions and methods of using the compound. The compound has activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV. | 2013-04-25 |
| 20130102590 | PYRIDOPYRIMIDINONE INHIBITORS OF KINASES - The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, | 2013-04-25 |
| 20130102591 | COMPOSITIONS AND METHODS FOR PREVENTION AND TREATMENT OF PULMONARY HYPERTENSION - The invention provides compositions and methods for prevention, treatment, or management of pulmonary hypertension using piperidine, pyrrolidine, or azepane derivatives comprising one to four nitric oxide (NO) donor groups and a reactive oxygen species (ROS) degradation catalyst. The invention further provides a water dispersible powder comprising nanoparticles comprising said derivatives, as well as pharmaceutical compositions thereof and methods of use. | 2013-04-25 |
| 20130102592 | OXAZOLE TYROSINE KINASE INHIBITORS - The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar | 2013-04-25 |
| 20130102593 | PYRROLIDINE COMPOUNDS WHICH INHIBIT BETA-SECRETASE ACTIVITY AND METHODS OF USE THEREOF - Described herein are novel beta-secretase inhibitors and methods for their use, including methods of treating Alzheimer's disease. | 2013-04-25 |
| 20130102594 | Pharmaceutical Formulation of Valsartan - The present invention relates to a pharmaceutical composition in a form of suspension for oral administration comprising valsartan or its pharmaceutically acceptable salts and at least one or two or more of the components selected from glycerol or syrup or the mixture thereof, a preservative, a buffer system and a suspending/stabilizing agent. The present invention further relates to the therapeutic uses of the pharmaceutical composition. | 2013-04-25 |
| 20130102595 | TREATMENT OF CANCERS HAVING K-RAS MUTATIONS - The present invention provides a method of treating a cancer associated with a K-ras mutation in a subject in need thereof. The method comprises the steps of: (1) identifying a subject with a cancer associated with a K-ras mutation; and (2) administering to the subject (i) an inhibitor of PI3 kinase and (ii) an HDAC inhibitor, wherein the PI3 kinase inhibitor and the HDAC inhibitor are administered in amounts which together are therapeutically effective. | 2013-04-25 |
| 20130102596 | METHOD AND DEVICE FOR ADMINISTERING XINAFOATE SALT OF N4-(2,2-DIFLUORO-4H-BENZO [1,4]OXAZIN-3-ONE)-6-YL]-5-FLUORO-N2-[3- (METHYLAMINOCARBONYLMETHYLENEOXY) PHENYL]2,4-PYRIMIDINEDIAMINE - Disclosed embodiments concern a device for administering a xinafoate salt of N4-[(2,2-difluoro-4H-benzo[1,4]oxazin-3-one)-6-yl]-5-fluoro-N2-[3-(methylaminocarbonylmethyleneoxy)phenyl]-2,4-pyrimidinediamine, or compositions thereof, and a method for making and using the device. Particular disclosed embodiments concern formulating the xinafoate salt for administration via the device. | 2013-04-25 |
| 20130102597 | COMPOUNDS AND METHODS FOR TREATING INFLAMMATORY AND FIBROTIC DISORDERS - Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system. | 2013-04-25 |
| 20130102598 | INDENOQUINOLONE COMPOUND, PREPARATION METHOD AND USE THEREOF - An indenoquinolone compounds of Formula (A) is disclosed, wherein the definition of each group is described in the description. These compounds may specifically inhibit topoisomerase I, and they have good activities against many kinds of human tumor cells, such as lung cancer, colon cancer, breast cancer, liver cancer and the like. They can be used in the manufacture of antitumor drugs. The method for preparing the compound of formula (A), and pharmaceutical compositions containing such compounds and the use in the manufacture of antitumor drugs are also disclosed. | 2013-04-25 |
| 20130102599 | PYRAZOLO [4,3-C] CINNOLIN-3-ONE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS - The present invention is directed to pyrazolo[4,3-c]cinnolin-3-one compounds of formula (I) | 2013-04-25 |
| 20130102600 | Heteroaryl hydroxamic acid derivatives and their use in the treatment, amelioration or prevention of a viral disease - The present invention relates to a compound having the general formula I, optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, | 2013-04-25 |
| 20130102601 | Pyrimidin-4-one derivatives and their use in the treatment, amelioration or prevention of a viral disease - The present invention relates to a compound having the general formula II, optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, | 2013-04-25 |
| 20130102602 | 2-Aryl-4-Quinazolinones And Their Pharmaceutical Compositions - Provided is a compound of the formula I or a pharmaceutically acceptable salt, solvate or stereoisomer thereof: | 2013-04-25 |
| 20130102603 | 2,4-DIARYL - SUBSTITUTED [1,8] NAPHTHYRIDINES AS KINASE INHIBITORS FOR USE AGAINST CANCER - The present invention relates to novel [1,8]naphthyridine derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumors. | 2013-04-25 |
| 20130102604 | NOVEL CYCLOPROPANE INDOLINONE DERIVATIVES - The present invention relates to a compound of formula (I) | 2013-04-25 |
| 20130102605 | INHIBITORS OF AKT ACTIVITY - The instant invention provides for substituted thiazoles that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer. | 2013-04-25 |
| 20130102606 | Compositions and Methods for Stimulating Collagen Synthesis in the Skin - Cosmetic compositions comprising substituted carbamoyl heterocyclic analogs and methods of using such compositions to impart anti-aging benefits to the skin are disclosed. The substituted carbamoyl heterocyclic analogs are believed to have modulatory activity against one or more biochemical pathways implicated in skin aging. | 2013-04-25 |
| 20130102607 | UREIDO-PYRAZOLE DERIVATIVES FOR USE IN THE TREATMENT OF RHINOVIRUS INFECTIONS - Medicinal use The disclosure relates to compounds of formula (I) for use in the treatment or prophylaxis of respiratory syncitial virus (RSV) infection in particular viral exacerbation of a respiratory disorder such as bronchitis, asthma, COPD and/or cystic fibrosis, methods of treating or preventing RSV infection employing said compounds or pharmaceutical composition comprising the same. | 2013-04-25 |
| 20130102608 | BIPYRIDYL DERIVATIVES - The present invention relates to novel bipyridyl derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumors. | 2013-04-25 |
| 20130102609 | BIARYL OXYACETIC ACID COMPOUNDS - The present invention provides biaryl oxyacetic acid compounds which may be useful for treating inflammatory disorders, including disorders affecting the respiratory system and skin. The compounds provided include those of the general formula I: | 2013-04-25 |
| 20130102610 | PHENOXY ACETIC ACIDS AS PPAR DELTA ACTIVATORS - Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are activators of PPARδ and should be useful for treating conditions mediated by the same. | 2013-04-25 |
| 20130102611 | IP RECEPTOR AGONIST HETEROCYCLIC COMPOUNDS - The present invention provides heterocyclic derivatives which activate the IP receptor. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients. Pharmaceutical compositions comprising such derivatives are also encompassed. Examples of compounds of the invention include the compounds according to Formula Ia, or a pharmaceutically acceptable salt thereof, and the compounds of the examples. | 2013-04-25 |
| 20130102612 | TOPICAL DERMAL BRIMONIDINE COMPOSITIONS - The present invention provides topical dermal compositions comprising an effective amount of brimonidine or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier selected from the group consisting of drops, creams, gels and ointments, wherein the composition is suitable for application to skin. | 2013-04-25 |
| 20130102613 | TREATMENT OF CANCER WITH TOR KINASE INHIBITORS - Provided herein are methods for treating or preventing a solid tumor, non-Hodgkin lymphoma or multiple myeloma in a patient, comprising administering an effective amount of a TOR kinase inhibitor to a patient having a solid tumor, non-Hodgkin lymphoma or multiple myeloma. | 2013-04-25 |
| 20130102614 | CHIRALLY PURE ISOMERS OF ITRACONAZOLE FOR USE AS ANGIOGENESIS INHIBITORS - Described herein are methods of inhibiting angiogenesis, and treating and preventing disorders associated with angiogenesis by administering anti-angiogenesis compounds to a subject. | 2013-04-25 |
| 20130102615 | THIOAMIDE, AMIDOXIME AND AMIDRAZONE DERIVATIVES AS HIV ATTACHMENT INHIBITORS - A compound of Formula I, including pharmaceutically acceptable salts thereof: | 2013-04-25 |
| 20130102616 | POLYMORPHIC FORMS OF 1-[4-(5-CYANOINDOL-3-YL)BUTYL]-4-(2-CARBAMOYLBENZOFURAN-5-YL)PIPERAZINE HYDROCHLORIDE - The invention relates to new crystalline modifications of the hydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine, crystalline modification of the dihydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine and amorphous 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride which are suitable in particular for the preparation of solid medicaments for the treatment or prevention of depressive disorders, anxiety disorders, bipolar disorders, mania, dementia, substance-related disorders, sexual dysfunctions, eating disorders, obesity, fibromyalgia, sleeping disorders, psychiatric disorders, cerebral infarct, tension, for the therapy of side-effects in the treatment of hypogonadism, secondary amenorrhea, premenstrual syndrome and undesired puerperal lactation. | 2013-04-25 |
| 20130102617 | METHOD OF TREATING DIABETES, METABOLIC SYNDROME AND OBESITY USING PHENYLACETAMIDE DERIVATIVE - Phenylacetamide compounds of the formula | 2013-04-25 |
| 20130102618 | 3-AMINO-5,6-DIHYDRO-1H-PYRAZIN-2-ONE DERIVATIVES USEFUL FOR THE TREATMENT OF ALZHEIMER'S DISEASE AND OTHER FORMS OF DEMENTIA - The present invention relates to novel 3-amino-5,6-dihydro-1H-pyrazin-2-one derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretase is involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease or dementia associated with beta-amyloid. | 2013-04-25 |
| 20130102619 | 2-PYRIDYLOXY-4-NITRILE OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to 2-pyridyloxy-4-nitrile compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyl-oxy-4-nitrile compounds described herein in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved. | 2013-04-25 |
| 20130102620 | PYRAZOLOPYRIMIDINE DERIVATIVE - The invention provides a pyrazolopyrimidine derivative of formula (I), wherein, for example, R | 2013-04-25 |
| 20130102621 | NOVEL CONDENSED PYRIDINE OR CONDENSED PYRIMIDINE DERIVATIVE, AND MEDICINAL AGENT COMPRISING SAME - The present invention relates to provision of a novel compound that has an activity of promoting insulin secretion from pancreatic β cells and thus is useful as a prophylaxis and/or therapeutic agent for diseases caused by hyperglycemia such as diabetes mellitus, and | 2013-04-25 |
| 20130102622 | Novel Quinazoline-2,4-Dione Derivative, and Medical Compositions for the Prophylaxis and Treatment of Cranial Nerve Disease Containing the Same - The present invention relates to a novel quinazoline-2,4-dione derivative of formula (I), a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising a compound of formula (I) as an active ingredient for preventing or treating neurological brain disease. | 2013-04-25 |
| 20130102623 | Tricyclic Compounds Having Cytostatic and/or Cytotoxic Activity and Methods of Use Thereof - The present invention provides tricyclic compounds having cytostatic and cytotoxic activity in a single molecule having receptor tyrosine kinase(s), dihydrofolate reductase, thymidylate synthase and/or dihydroorotate dehydrogenase inhibitory activity, which are useful as anti-angiogenic and anti-tumor agents. Also provided are methods of utilizing these inhibitors to treat tumor cells and other proliferative diseases and disorders. | 2013-04-25 |
| 20130102624 | EARLY DETECTION OF THIAMINE DEFICIENCY - A method is provided for determining the thiamine status of a human or animal based on the relative levels of thiamine and its metabolites. Certain embodiments of the present invention also provide methods for determining the effectiveness of a thiamine deficiency treatment. | 2013-04-25 |
| 20130102625 | Artemisinin with Berberine Compositions and Methods of Making - An all-natural herbal composition and methods of preparing the same are provided. The novel Artemisinin Combination Therapy (ACT) consists of artemisinin and its derivatives and berberine, the two active substances mixed with various selected excipient compounds to form a single pill, tablet or capsule for treatment and prevention of malaria, dengue fever, yellow fever, dysentery, Lyme disease, babesiosis, progressive multifocal leukoencephalopathy, | 2013-04-25 |
| 20130102626 | TARGETED NITROXIDE AGENTS - Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation. | 2013-04-25 |
| 20130102627 | Acridines As Inhibitors Of Haspin And DYRK Kinases - The present disclosure is directed to compounds of Formula I: which are inhibitors of Haspin kinase and DYRK kinases. The compounds of the present disclosure, and compositions thereof, are useful in the treatment of disease related to Haspin kinase and DYRK kinase expression and/or activity. | 2013-04-25 |
| 20130102628 | CRYSTAL OF FUSED PYRIDINE COMPOUND SALT - [Problem] A salt or crystal of a compound which is highly stable in a solid state and useful as a bulk material for the preparation of a pharmaceutical product is provided. | 2013-04-25 |
| 20130102629 | ANALOGUES FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS - Compounds represented by formula (I) | 2013-04-25 |
| 20130102630 | Derivatives of the Aminated Hydroxyquinoline Class For Treating Cancers - The invention relates to compounds of the aminated hydroxyquinoline type capable of preventing the migration of metastases or tumoral cells. Such compounds are useful for treating cancers. | 2013-04-25 |
| 20130102631 | NOVEL MICROBIOCIDAL DIOXIME ETHER DERIVATIVES - The present invention provides compounds of formula (I) wherein R | 2013-04-25 |
| 20130102632 | SUBSTITUTED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS - The present invention relates to sodium channel inhibitors of Formula (I): | 2013-04-25 |
| 20130102633 | TRANSGLUTAMINASE INHIBITORS AND METHODS OF USE THEREOF - Transglutaminase inhibitors and methods of use thereof are provided. | 2013-04-25 |
| 20130102634 | Stabilized and Preserved Ketotifen Ophthalmic Compositions - Ophthalmic compositions comprising ketotifen, a source of hydrogen peroxide providing an amount of hydrogen peroxide of from about 0.001 to about 0.1% (w/v), one or more ocular-compatible hydrogen peroxide stabilizers, HPMC and CMC, and methods for the treatment and prevention of allergic conjunctivitis using these ophthalmic compositions are provided herein. | 2013-04-25 |
| 20130102635 | Methods for Treating Disorders Associated with Hyperlipidemia in a Mammal - The invention is directed to methods for treating hyperlipidemia in a mammal. The methods involve combination therapies using a microsomal triglyceride transfer protein (MTP) inhibitor (for example, BMS-201038 and implitapide) and a HMG-CoA reductase inhibitor (for example simvastatin or atorvastatin). Co-administration of the MTP inhibitor with the HMG-CoA reductase inhibitor produces a therapeutic benefit, for example, a reduction in the concentration of cholesterol and/or triglycerides in the blood stream, but with fewer or reduced side effects than when higher dosages of the MTP inhibitor are used during monotherapy to provide the same or similar therapeutic benefit. | 2013-04-25 |
| 20130102636 | 5-Lipoxygenase-Activating Protein (FLAP) Inhibitors - A method for treating a human comprises administering a therapeutically effective amount of 3-[3-tert-butylsulfanyl-1-[4-(6-methoxy-pyridin-3-yl)-benzyl]-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid or a pharmaceutically acceptable salt or a pharmaceutically acceptable N-oxide thereof, to the human in need. | 2013-04-25 |
| 20130102637 | PEST CONTROL AGENT - Provided is a novel pest control agent using at least one imino derivative represented by the following chemical formula (I): | 2013-04-25 |
| 20130102638 | METHODS AND COMPOSITIONS FOR CONTROLLING ALGAE - Described are preferred methods and compositions for controlling algae which involve the use of bleaching pyridinecarboxamide compounds. | 2013-04-25 |
| 20130102639 | INHIBITORS OF PROTEIN PRENYLTRANSFERASES - The present invention is directed to novel compounds. These compounds can be useful in inhibiting the activity of protein prenyltransferases including GGTase I and/or RabGGTase. The compounds can also be used as anti-cancer therapeutics including as part of methods for treating cancer, in assays, and in kits. | 2013-04-25 |
| 20130102640 | METHOD FOR THE PREPARATION OF CIS-1,2-DIOLS IN THE KILOGRAM SCALE - The present invention relates to the scale up of the preparation of cis-1,2-diols of formula I | 2013-04-25 |
| 20130102641 | PRODRUGS OF GABA ANALOGS, COMPOSITIONS AND USES THEREOF - The present invention provides prodrugs of GABA analogs, pharmaceutical compositions of prodrugs of GABA analogs and methods for making prodrugs of GABA analogs. The present invention also provides methods for using prodrugs of GABA analogs and methods for using pharmaceutical compositions of prodrugs of GABA analogs for treating or preventing common diseases and/or disorders. | 2013-04-25 |
| 20130102642 | SYNERGISTIC PESTICIDAL MIXTURES - Synergistic pesticidal mixtures are provided. | 2013-04-25 |
| 20130102643 | CYTOCHROME P450 INHIBITORS AND USES THEREOF - The present invention provides compounds having the general structural formula (I) and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving fibrosis and proliferation, and where anti-fibrotic or anti-proliferative activity is beneficial. | 2013-04-25 |
| 20130102644 | Prophylactic or Ameliorating Agent for Genetic Diseases - An object of the present invention is to provide a prophylactic or ameliorating agent for a genetic disease that is caused by a mutation in an exon of a gene and is capable of forming a functional truncated protein by skipping of the exon comprising the mutation. The prophylactic or ameliorating agent used in the present invention is a prophylactic or ameliorating agent for a genetic disease that is caused by a mutation in an exon of a gene and is capable of forming a functional truncated protein by skipping of the exon comprising the mutation, wherein the prophylactic or ameliorating agent contains a compound having a molecular weight of 1500 or lower. | 2013-04-25 |
| 20130102645 | Methods and compositions for controlling vascularization in ophthalmological and dermatological diseases - A method for controlling vascularization in a patient's eye or skin includes administering to the patient's eye or skin a pharmaceutical composition having | 2013-04-25 |
| 20130102646 | MICROBICIDAL COMPOSITION - The invention relates to a microbicidal composition which comprises a mixture of at least two components, the first component being 2-methyl-3-isothiazolone (MIT) and the second component being at least one active compound selected from the following groups of active compounds:
| 2013-04-25 |
| 20130102647 | PLANT DISEASE CONTROL COMPOSITION AND ITS USE - A plant disease control composition comprising a carboxamide compound represented by following formula (I), wherein R | 2013-04-25 |
| 20130102648 | PESTICIDAL COMPOSITION AND ITS USE - A composition comprising a carboxamide compound represented by following formula (I), wherein R | 2013-04-25 |
| 20130102649 | SUBSTITUTED BIARYL ALKYL AMIDES - Disclosed herein are substituted biaryl alkyl amide compounds, methods of synthesizing substituted biaryl alkyl amide compounds and methods of treating diseases and/or conditions with substituted biaryl alkyl amide compounds. | 2013-04-25 |
| 20130102650 | ANTIMICROBIAL COMPOUNDS OF 1,4-NAPHTOQUINONE STRUCTURE - The present invention relates to a compound having formula (I) wherein: R | 2013-04-25 |
| 20130102651 | GENERAL COMPOSITION FRAMEWORK FOR LIGAND-CONTROLLED RNA REGULATORY SYSTEMS - The invention provides an improved design for the construction of extensible nucleic acid-based, ligand-controlled regulatory systems, and the nucleic acid regulatory systems resulting therefrom. The invention contemplates improving the design of the switches (ligand-controlled regulatory systems) through the design of an information transmission domain (ITD). The improved ITD eliminates free-floating ends of the switching and the competing strands, and localizes competitive hybridization events to a contiguous strand of competing and switching strands in a strand-displacement mechanism-based switch, thereby improving the kinetics of strand-displacement. The improved regulatory systems have many uses in various biological systems, including gene expression control or ligand-concentration sensing. | 2013-04-25 |
| 20130102652 | METHODS AND COMPOSITIONS RELATED TO MODIFIED ADENOSINES FOR CONTROLLING OFF-TARGET EFFECTS IN RNA INTERFERENCE - Disclosed are compositions and methods related to modified nucleobases. Also disclosed are compositions and methods related to modified interfering RNAs. Also disclosed are compositions and methods related to modified adenonsine for controlling off-target effects in RNA interference. | 2013-04-25 |
| 20130102653 | GNA11 AND GNAQ EXON 4 MUTATIONS IN MELANOMA - The present invention provides methods of detecting activating mutations in exon 4 of a GNAQ or a GNA11 gene in a melanocytic neoplasm for diagnostic and prognostic purposes. The invention further provides methods of treating such melanocytic neoplasm by modulating the activity of the mutated GNAQ or GNA11. | 2013-04-25 |
| 20130102654 | RNA APTAMERS AGAINST BAFF-R AS CELL-TYPE SPECIFIC DELIVERY AGENTS AND METHODS FOR THEIR USE - In one embodiment, a B cell specific aptamer-siRNA chimera is provided. The B cell specific aptamer-siRNa chimera may include an RNA aptamer that binds BAFF-R and an siRNA molecule conjugated to the RNA aptamer via a nucleotide linker. In another embodiment, a B cell specific RNA aptamer is provided. The RNA aptamer may be a molecule that binds to BAFF-R that has the sequence SEQ ID NO:37, SEQ ID NO:38 or SEQ ID NO:39. In some embodiments, the RNA aptamer is conjugated, via a nucleotide linker, to an siRNA molecule that suppresses expression of one or more target oncogenes in one or more B cells. In one aspect, the one or more target oncogenes are selected from Bcl6, Bcl2, STAT3, Cyclin D1, Cyclin E2 and c-myc. In another embodiment, methods for treating a B cell malignancy in a cancer patient are provided. Such methods may include administering a therapeutically effective amount of a therapeutic composition, the therapeutic composition comprising a B cell specific RNA aptamer that binds BAFF-R. | 2013-04-25 |
| 20130102655 | ALKYNYL-DERIVATIZED CAP ANALOGS, PREPARATION AND USES THEREOF - Alkynyl-derivatized cap analogs, alkynyl-modified capped RNA, 1,4-disubstituted triazole-derivatized capped RNA, methods of preparation, methods of isolation, and uses thereof are provided. The “click” modification facilitates detection and isolation of capped RNAs and the 1,4-disubstituted triazole derivatives formed by the “click” reaction are useful for producing RNA transcripts and encoded protein. | 2013-04-25 |
| 20130102656 | USE OF A GRANULIN OR A GRANULIN-LIKE COMPOUND FOR THE THERAPY OR PROPHYLAXIS OF CHRONIC PAIN - The invention relates to the use of a granulin or a granulin-like compound for producing a pharmaceutical composition for the therapy or prophylaxis of chronic pain, in particular for neuropathic pain. | 2013-04-25 |
| 20130102657 | ANTI-ANGIOGENIC COMPOSITIONS AND METHODS OF USE - The present invention provides compositions comprising an anti-angiogenic factor, and a polymeric carrier. Representative examples of anti-angiogenic factors include Anti-Invasive Factor, Retinoic acids and derivatives thereof, and paclitaxel. Also provided are methods for embolizing blood vessels, and eliminating biliary, urethral, esophageal, and tracheal/bronchial obstructions. | 2013-04-25 |
| 20130102658 | DOXEPIN ISOMERS AND ISOMERIC MIXTURES AND METHODS OF USING THE SAME TO TREAT SLEEP DISORDERS - The invention relates to use of the cis-(Z) isomer or isomeric mixtures containing specified ratios of the cis-(Z) and trans-(E) isomers of doxepin, metabolites of doxepin, pharmaceutically-acceptable salts of doxepin and prodrugs of the same; compositions containing the same, for the treatment of sleep disorders | 2013-04-25 |