43rd week of 2013 patent applcation highlights part 53 |
Patent application number | Title | Published |
20130281410 | METHODS FOR THE TREATMENT OF PSYCHIATRIC DISORDERS - The invention provides methods for the treatment of major depressive disorder in male subjects and methods for the treatment of psychiatric disorders at high altitudes by administering one or more creatine-containing compounds. | 2013-10-24 |
20130281411 | COMPOSITIONS FOR TREATING INFLAMMATORY DERMATOLOGICAL DISEASES AND CONDITIONS AND METHODS OF USE THEREOF - Compositions are disclosed that contain an effective inflammatory-dermatological disease-treating or condition-treating active agent and a pharmaceutically-acceptable carrier or vehicle. Methods of using the compositions to treat a subject's skin are also disclosed. | 2013-10-24 |
20130281412 | PHARMACEUTICAL COMPOSITION OF SALICYLANILIDE-DERIVED SMALL MOLECULES AND PREPARATION AND APPLICATION THEREOF - The present invention provides a pharmaceutical composition of salicylanilide-derived small molecules include:
| 2013-10-24 |
20130281413 | Salicylate Conjugates Useful For Treating Metabolic Disorders - The present invention is directed to methods for treating metabolic disorders with compounds that are conjugates. The conjugates of the present invention are comprised of salicylic acid, triflusal, diflusinal, salsalate, IMD-0354, ibuprofen, diclofenac, licofelone, or HTB, and one or more antioxidants. | 2013-10-24 |
20130281414 | THIAZOLIDINEDIONE ANALOGUES - The present invention relates to thiazolidinedione analogues that are useful for treating liver afflictions such as nonalcoholic fatty liver disease (NAFLD) or nonalcoholic steatohepatitis (NASH). | 2013-10-24 |
20130281415 | NEW CYCLOHEXYLAMINE DERIVATIVES HAVING 2 ADRENERGIC AGONIST AND M3 MUSCARINIC ANTAGONIST ACTIVITIES - The present disclosure relates to novel compounds having β2 adrenergic agonist and M3 muscarinic antagonist dual activity, to pharmaceutical compositions containing them, to the process for their preparation and to their use in respiratory therapies. | 2013-10-24 |
20130281416 | PHARMACEUTICAL COMPOSITION - A pharmaceutical composition comprising: (A) an androgen; (B) a cyclic enhancer of the type used in the compositions and methods claimed by U.S. Pat. No. 5,023,252 to Hsieh; and (C) a thickening agent; including, for example, a composition in which the cyclic enhancer is a macrocyclic ester or a macrocyclic ketone; the use of the composition to treat a condition, for example, male hypogonadism, in a patient by applying the composition to the membrane of the patient; and a method for making the composition. | 2013-10-24 |
20130281417 | Implants and methods for treating inflammation-mediated conditions of the eye - Methods for treating inflammation-mediated conditions of the eye are described, comprising: implanting into the vitreous of the eye of an individual a bioerodible implant comprising a steroidal anti-inflammatory agent and a bioerodible polymer, wherein the implant delivers the agent to the vitreous in an amount sufficient to reach a concentration equivalent to at least about 0.05 μg/ml dexamethasone within about 48 hours and maintains a concentration equivalent to at least about 0.03 μg/ml dexamethasone for at least about three weeks. | 2013-10-24 |
20130281418 | Use of hydroxypregnenolone derivatives for enhancing health and physical performance - A method for the use of derivatives of hydroxypregnenolone (3-beta,17-alpha-dihydroxypregn-5-en-3-one) to enhance health and physical performance in humans and more particularly to the use of hydroxypregnenolone derivatives for restoring renal hormonal balance, decreasing body weight, reducing adipose tissue, increasing endurance, promoting skeletal muscle growth, boosting androgen levels, inhibiting aromatase, and increasing cognitive function. | 2013-10-24 |
20130281419 | Therapeutic Uses for an Aminosterol Compound - A pharmaceutical composition includes, as an active ingredient, a compound according to formula 1436 as shown in FIG. | 2013-10-24 |
20130281420 | Ophthalmic Formulations of Squalamine - The invention relates to ophthalmic formulations of squalamine or its pharmaceutically acceptable salts for the treatment of conditions of the eye such as, for example, wet age-related macular degeneration (wet AMD), choroidal neovascularization, retinopathy, dry age-related macular degeneration (dry AMD), polypoidal choroidal vasculopathy, neovascularization following ocular surgery, macular edema, retinal venous occlusion, subchoroidal neovascularization, retinal epithelial detachment, pterygum or foveal geographic atrophy of the retinal pigment epithelium. | 2013-10-24 |
20130281421 | 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. | 2013-10-24 |
20130281422 | Treatment of Pain Associated with Dislocation of Basal Endometrium - The present invention relates generally to gynecological diseases and in particular to a method for reducing pain associated with dislocation of basal endometrium. | 2013-10-24 |
20130281423 | METHODS AND COMPOSITIONS FOR AMELIORATING PANCREATIC CANCER - Embodiments of the present invention include methods and compositions for ameliorating cancer. Some embodiments include methods and compositions for ameliorating pancreatic cancer targeting the CXCR4 receptor and the CXCL12 ligand. | 2013-10-24 |
20130281424 | ANTI-BACTERIAL SIDEROPHORE-AMINOPENICILLIN CONJUGATES - An artificial tris-catecolate siderophore with a tripodal backbone and its conjugates with ampicillin and amoxicillin were synthesized. Both conjugates exhibited significantly enhanced in vitro antibacterial activities against Gram-negative species compared to the parent drugs, especially against | 2013-10-24 |
20130281425 | USE OF LIQUID MEDIUM EXCHANGE BY CROSS FLOW FILTRATION IN THE PREPARATION OF DRUG SUSPENSIONS - Disclosed is a method of making particles of a drug wherein use is made of diafiltration. The diafiltration can be with anti-solvent, in which case a precipitate is obtained of particles as such. The diafiltration can also be with a pharmaceutically acceptable suspension medium. In that case several process steps of isolating, drying, transporting of particles can be avoided, because the suspension resulting from the synthesis of the particles is directly turned into a final drug product formulation. | 2013-10-24 |
20130281426 | PYRIDAZINONES, THE PREPARATION METHOD AND THE USE THEREOF - The present invention relates to a class of pyridazinones of formula I, which comprises 6-[3-(trifluoromethyl)phenyl]pyridazin-3(2H)-one as a mother nucleus, the preparation method thereof and the use thereof in manufacturing medicaments against tumors, especially liver cancer. | 2013-10-24 |
20130281427 | CRYSTALLINE FORM OF ERTAPENEM SODIUM AND PREPARATION METHOD THEREFOR - Provided is a crystalline form E of ertapenem sodium. Further provided is a method for preparing a crystalline form E of ertapenem sodium, characterized by using an aqueous ertapenem sodium solution at a low concentration as a raw material. The crystalline form E can be easily filtered and dried, the properties in the drying process are stable, and the purity of the crystal is high and can be up to 98.5% or higher. | 2013-10-24 |
20130281428 | Pyridone Derivatives - Novel compounds or salts thereof, or crystals thereof, which inhibit Axl and are useful for treating diseases caused by Axl hyperfunction, diseases associated with Axl hyperfunction and/or diseases accompanied by Axl hyperfunction are provided. Pyridone derivatives represented by the formula (1) having various substituents or salts thereof, or crystals thereof (where R | 2013-10-24 |
20130281429 | 2,4-DIAMINO-PYRIMIDINES AS AURORA INHIBITORS - The present invention encompasses compounds of general formula (1) | 2013-10-24 |
20130281430 | Amino-Indolyl-Substituted Imidazolyl-Pyrimidines and Their Use as Medicaments - The invention relates to new amino-indole-substituted imidazolyl-pyrimidines of formula 1 | 2013-10-24 |
20130281431 | DNA-PK INHIBITORS - The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. | 2013-10-24 |
20130281432 | PYRIDINONES/PYRAZINONES, METHOD OF MAKING, AND METHOD OF USE THEREOF - Pyridone and pyrazinone compounds of Formula I including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. | 2013-10-24 |
20130281433 | THERAPEUTIC COMPOUNDS - Compounds disclosed herein including compounds of formula I′: | 2013-10-24 |
20130281434 | THERAPEUTIC COMPOUNDS - Compounds of formula I′: | 2013-10-24 |
20130281435 | THERAPEUTIC AGENT FOR IRRITABLE BOWEL SYNDROME | 2013-10-24 |
20130281436 | DEUTERATED 1-PIPERAZINO-3-PHENYL INDANES FOR TREATMENT OF SCHIZOPHRENIA - The present invention relates to deuterated 1-piperazino-3-phenyl-indanes and salts thereof with activity at dopamine receptors D | 2013-10-24 |
20130281437 | METHOD FOR CANCER THERAPY - The present invention provides a method for treating a patient having cancer comprising administering to the patient a therapeutically effective amount of compound (1), or a pharmaceutically acceptable salt thereof, having the formula: | 2013-10-24 |
20130281438 | 2,4-DIAMINO-6,7-DIHYDRO-5H-PYRROLO[2,3]PYRIMIDINE DERIVATIVES AS FAK/Pyk2 INHIBITORS - The invention relates to a novel class of 2,4-diamino-6,7-dihydro-5H-pyrrolo[2,3]pyrimidine derivatives as a FAK and/or Pyk2 inhibitor, to a process for their preparation, and to a composition thereof, as well as to use of the compounds for the inhibiting FAK and/or Pyk2 and method for the treatment of a FAK and/or Pyk2 mediated disorder or disease. | 2013-10-24 |
20130281439 | TOSYLATE SALT OF CYCLOPROPANECARBOXYLIC ACID 4-(6-CHLORO-3-METHYL-4, 10-DIHYDRO-3H-2,3,4,9-TETRABENZO[F]AZULENE-9-CARBONYL)-2-FLUOROBENZYLAMID- E - The invention provides cyclopropanecarboxylic acid 4-(6-chloro-3-methyl-4,10-dihydro-3H-2,3,4,9-tetraazabenzo[f]azulene-9-carbonyl)-2-fluoro-benzylamide para-toluenesulphonate, pharmaceutical compositions containing it, and its use in therapy. | 2013-10-24 |
20130281440 | DDX3 AS A BIOMARKER FOR CANCER AND METHODS RELATED THERETO - The invention encompasses methods for treating or preventing diseases and disorders associated abnormal cell growth, for example, treating or preventing cancer or tumor growth, by administering to a subject in need thereof a composition comprising a therapeutically or prophylactically effective amount of a compound that downregulates DDX3, for example a fused diimidazodiazepine ring compound or a pharmaceutically acceptable salt thereof. The invention also encompasses the use of DDX3 as a biomarker for diagnostic and treatment purposes, for example, to identify a hyperproliferative disorder susceptible to treatment by down regulation of DDX3. | 2013-10-24 |
20130281441 | DIAZEPINEDIONE DERIVATIVE - A diazepinedione derivative represented by the formula (I) or a pharmacologically acceptable salt thereof is used as a P2X | 2013-10-24 |
20130281442 | Compounds for Treatment of Bovine Mastitis - Described herein are methods of treating mastitis in female mammals, e.g., cows, wherein the methods may include administering to mammals in need thereof compounds disclosed herein. | 2013-10-24 |
20130281443 | INHIBITORS OF FOCAL ADHESION KINASE - The invention provides inhibitors of focal adhesion kinase, an enzyme involved in the attachment of the cytoskeleton of a cell to an extracellular matrix, which has been implicated in processes such as cell migration, cell proliferation, and cell survival. The inhibitors are derivatives of a 5-substituted 2,4-diaminopyridine wherein the substituents are as defined herein. The invention also provides a method of using the inhibitors in treatment of cancer, and methods of preparation of the inhibitors by use of coupling reactions. | 2013-10-24 |
20130281444 | PREPARATION AND PHARMACEUTICALS OF BIPHENYL BENZAMIDE-DERIVED DERIVATIVES - The present invention provides a biphenyl benzamide-derived derivatives, which structure is selected from formula I or formula II: | 2013-10-24 |
20130281445 | COMPOUNDS USEFUL AS INHIBITORS OF CHOLINE KINASE - The present invention relates to compounds useful as inhibitors of choline kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. | 2013-10-24 |
20130281446 | XINAFOATE SALT OF N4-(2,2-DIFLUORO-4H-BENZO[1,4]OXAZIN-3-ONE)-6-YL]-5-FLUORO-N2-[3-(METHYLA- MINOCARBONYLMETHYLENEOXY)PHENYL]2,4-PYRIMIDINEDIAMINE - The present invention relates to the xinafoate salt of N4-[(2,2-difluoro- | 2013-10-24 |
20130281447 | JNK INHIBITORS FOR THE TREATMENT OF ENDOMETRIOSIS - This invention relates to a method of treating and/or preventing endometriosis comprising administering a JNK inhibitor. The JNK inhibitor can also be administered combined with a hormonal suppressor. The invention further relates to the treatment of endometriosis. | 2013-10-24 |
20130281448 | SMALL MOLECULE COMPOUNDS FOR TARGETING INFLAMMATORY CONDITIONS - Provided herein are small molecule compounds for the treatment of inflammatory conditions, and pharmaceutical compositions and methods relating thereto. For example, provided herein are compositions comprising small molecule compounds for the treatment of conditions such as multiple sclerosis, type 2 diabetes, psoriasis, rheumatoid arthritis, Hashimoto's thyroiditis, and Crohn's disease. In some embodiments, the pharmaceutical composition and methods described herein pertain to small molecule compounds previously known for the treatment of another condition, such as non-small-cell lung cancer (NSCLC). | 2013-10-24 |
20130281449 | Oxazine Derivatives and their Use in the Treatment of Neurological Disorders - The invention relates to novel heterocyclic compounds of the formula (I), in which all of the variables are as defined in the specification, in free form or in pharmaceutically acceptable salt form, to their preparation, to their medical use and to medicaments comprising them. | 2013-10-24 |
20130281450 | ISOINDOLONE DERIVATIVES - The present invention provides for compounds of formula (I) | 2013-10-24 |
20130281451 | INDOLIN-2-ONE DERIVATIVES AS PROTEIN KINASE INHIBITORS - A novel class of indoline-2-one derivatives are disclosed. These compounds are protein kinase inhibitors which are useful for treating hyperproliferative diseases such as cancer. | 2013-10-24 |
20130281452 | SUBSTITUTED 4-AMINOBENZAMIDES AS KCNQ2/3 MODULATORS - Substituted 4-aminobenzamides, pharmaceutical compositions containing these compounds and also methods of using these compounds in the treatment and/or prophylaxis of pain and further diseases and/or disorders. | 2013-10-24 |
20130281453 | ANTI-CANCER SERINE HYDROLASE INHIBITORY CARBAMATES - Serine hydrolases are implicated in malconditions such as cancer, central nervous system disorders, cardiovascular disorders, obesity, and metabolic disorders. Many serine hydrolases expressed in proteomic libraries are of unknown function in vivo. Compounds identified through library versus library screening can be used for treatment of malconditions associated with the specific serine hydrolase KIAA1363 (also known as AADACL1). A library of inhibitors of KIAA1363 was prepared and candidate compounds were identified as a potent inhibitors having submicromolar IC | 2013-10-24 |
20130281454 | PROSTAGLANDIN AND VASOCONSTRICTOR PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE - Compositions containing a prostaglandin agent and a vasoconstrictor agent for ophthalmic applications are provided as well as methods of treating ophthalmic diseases using the same. In certain embodiments, the compositions and methods are useful for treating glaucoma without causing conjunctival hyperemia. | 2013-10-24 |
20130281455 | Phenylpyri(mi)dinylazoles - Phenylpyri(mi)dinylazoles of the formula [I-a] and [I-b], | 2013-10-24 |
20130281456 | SYNTHESIS OF DEUTERATED MORPHOLINE DERIVATIVES - The present invention is directed to a process for preparing a 2,26,6-d | 2013-10-24 |
20130281457 | PHARMACEUTICAL COMPOSITIONS COMPRISING 5-CHLORO-N-(-METHYL)-2-THIOPHENCARBOXAMID - The invention relates to pharmaceutical compositions comprising 5-Chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-mor-pholinyl)-phenyl]-1,3-oxazolidin-5-yl}-methyl)-2-thiophencarbox-amid and processes of preparing such compositions. In a second aspect, the present invention relates to a preferred pellet-layering process for preparing such compositions. | 2013-10-24 |
20130281458 | ARTHROPOD PEST CONTROL COMPOSITION AND METHOD FOR CONTROLLING ARTHROPOD PESTS - Disclosed is an arthropod pest control composition having an excellent controlling effect on arthropod pests, which comprises an amide compound represented by formula (1): | 2013-10-24 |
20130281459 | Heteroaromatic Aryl Triazole Derivatives as PDE10A Enzyme Inhibitors - This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. | 2013-10-24 |
20130281460 | 6-THIO-SUBSTITUTED IMIDAZOPYRAZINES FOR USE AS MPS-1 AND TKK INHIBITORS IN THE TREATMENT OF HYPERPROLIFERATIVE DISORDERS - The present invention relates to substituted imidazopyrazine compounds of general formula (I): (I) in which R | 2013-10-24 |
20130281461 | Spirocyclic Heterocycles Medicaments Containing Said Compounds, Use Thereof And Method For Their Production - The present invention relates to spirocyclic heterocycles of general formula (I) | 2013-10-24 |
20130281462 | ARYL DIAMIDINES AND PRODRUGS THEREOF FOR TREATING MYOTONIC DYSTROPHY - Disclosed herein are compounds (for example, diamidine derivatives and prodrugs) and methods of use thereof, for example in treating muscular dystrophy (DM) or disease caused by a toxic RNA in a subject. In some embodiments, the methods include administering an effective amount of one of more of the disclosed compounds to a subject to treat or inhibit DM or a disease caused by or associated with toxic RNA, such as DM1, DM2, spinocerebellar ataxia type 8 (SCA8), fragile X tremor ataxia syndrome (FXTAS), or Huntington disease-like 2 (HLD2). In some examples, the methods include selecting a subject for treatment, for example selecting a subject with DM1, DM2, SCA8, FXTAS, or HLD2. | 2013-10-24 |
20130281463 | DIAZA-SPIRO[5.5]UNDECANES USEFUL AS OREXIN RECEPTOR ANTAGONISTS - The invention relates to compound of the formula (I), in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it. | 2013-10-24 |
20130281464 | BIGUANIDE DERIVATIVE COMPOUND - Provided is a novel compound which simultaneously inhibits both NMDA receptors and ASIC1a, which are associated with neurodegenerative disease and so on, and thus is useful for the prevention and treatment of various nervous system diseases. A biguanide derivative represented by the following general formula (1), a salt thereof, or a hydrate of the derivative or the salt: | 2013-10-24 |
20130281465 | PYRAZOLE DERIVATIVE - A compound represented by formula (IA) or a pharmaceutically acceptable salt thereof, which is useful for the treatment or prevention of diseases such sleep disorder, depression, anxiety disorder, panic disorder, schizophrenia, drug dependence, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, pain, gastrointestinal diseases, epilepsy, inflammation, immune-related diseases, endocrine-related diseases, and hypertension, and of which the action relies on an orexin (OX) receptor antagonistic activity. | 2013-10-24 |
20130281466 | ARTHROPOD PEST CONTROL COMPOSITION AND METHOD FOR CONTROLLING ARTHROPOD PESTS - Disclosed is an arthropod pest control composition having an excellent controlling effect on arthropod pests, which comprises a compound represented by formula (I): | 2013-10-24 |
20130281467 | NOVEL MICROBICIDES - Compounds of formula (I), wherein G represents together with the two carbon atoms of the pyrimidine ring to which it is attached, a 5- to 7-membered aliphatic carbocyclic or heterocyclic ring system which contain 0 to 2 heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur; and wherein said 5- to 7-membered aliphatic carbocyclic or heterocyclic ring system can be mono-, di- or trisubstituted by substituents selected from the group consisting of halogen, keto, C | 2013-10-24 |
20130281468 | BICYCLIC ARYL AND BICYCLIC HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS - Bicyclic aryl substituted triazoles or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed. | 2013-10-24 |
20130281469 | THIOACETATE COMPOUNDS, COMPOSITIONS AND METHODS OF USE - Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid. | 2013-10-24 |
20130281470 | Use of (R)-Penciclovir Triphosphate for the Manufacture of a Medicament for the Treatment of Viral Diseases - A method of treatment of: i) HIV-1 infections in mammals, including humans; or ii) HBV infections in mammals, including humans; which method comprises the administration to the human in need of such treatment, an effective amount of the (R)-enantiomer of the triphosphate of a compound of formula (A) or a pharmaceutically acceptable salt thereof; and compounds for use in the method. | 2013-10-24 |
20130281471 | Acyclovir Formulations - The present invention relates to an acyclovir formulation having improved bioavailability resulting in better efficacy and/or requiring less frequent administration. | 2013-10-24 |
20130281472 | COMPOSITION AND METHOD FOR TREATING OR PREVENTING SKELETAL MUSCLE FIBROSIS - A compound in combination with a pharmaceutically acceptable carrier, the compound having a formula: wherein: R | 2013-10-24 |
20130281473 | SUBSTITUTED ISOQUINOLINONES AND QUINAZOLINONES - The invention relates to substituted nitrogen containing bicyclic heterocycles of the formula (I) | 2013-10-24 |
20130281474 | FUSED TRICYCLIC INHIBITORS OF MAMMALIAN TARGET OF RAPAMYCIN - This invention relates to novel fused tricyclic compounds that are inhibitors of mammalian Target of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP, and are useful in the treatment of cellular proliferative diseases, for example cancer and other proliferative disorders. | 2013-10-24 |
20130281475 | INHIBITORS OF C-FMS KINASE - The invention is directed to compounds of Formula I: | 2013-10-24 |
20130281476 | Modulators of Muscarinic Receptors - The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases. | 2013-10-24 |
20130281477 | HYDROCHLORIDE SALTS OF 8-[1-(3,5-BIS-(TRIFLUOROMETHYL)PHENYL)-ETHOXYMETHYL]-8-PHENYL-1,7-DIAZASP- IRO[4,5]DECAN-2-ONE AND PREPARATION PROCESS THEREFOR - Disclosed are hydrochloride and tosylate crystalline salt forms of (5S,8S)-8-[{(1R)-1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one, represented by Formula I and methods of preparing the same. | 2013-10-24 |
20130281478 | COMBINATION OF SYROSINGOPINE AND MITOCHONDRIAL INHIBITORS FOR THE TREATMENT OF CANCER AND IMMUNOSUPPRESSION - The invention relates to a combination of syrosingopine and a mitochondrial inhibitor, e.g. metformin or oligomycin, and the use of the combination of syrosingopine and a mitochondrial inhibitor for the treatment of cancer and for achieving immunosuppression. The invention also relates to a fluorescence-based method for predicting syrosingopine sensitivity of a cancer cell. | 2013-10-24 |
20130281480 | Oral Drug Delivery System - Dosage forms and drug delivery devices suitable for administration of pharmaceutical compounds and compositions, including the oral drug administration of compounds. | 2013-10-24 |
20130281482 | NICOTINIC ACETYLCHOLINE RECEPTOR AGONISTS - The invention provides novel nicotinic acetylcholine receptor agonists, for example, phantasmidine and derivatives thereof, for example a compound of formula (I). Also disclosed are methods of treating disorders responsive to nicotinic acetylcholine receptor agonists such as Alzheimer's disease, schizophrenia, Myasthenia Gravis, Tourette's syndrome, Parkinson's disease, epilepsy, pain, and cognitive dysfunction by treatment with the nicotinic acetylcholine for agonists. | 2013-10-24 |
20130281484 | HDAC Inhibitors and Therapeutic Methods of Using Same - Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a neurological disease, traumatic brain injury, stroke, malaria, an autoimmune disease, autism, and inflammation, also are disclosed. | 2013-10-24 |
20130281485 | BRIDGED BICYCLIC RHO KINASE INHIBITOR COMPOUNDS, COMPOSITIONS AND USE - The present invention is directed to synthetic bridged bicyclic compounds that are inhibitors of rho-associated protein kinase. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with cytoskeletal reorganization. The method comprises administering to a subject a therapeutically effective amount of a Rho kinase inhibitory compound of Formula I, wherein said amount is effective to influence the actomyosin interactions, for example, by leading to cellular relaxation and alterations in cell-substratum adhesions. In one embodiment, the method treats increased intraocular pressure, such as primary open-angle glaucoma. In another embodiment, the method treats diseases or conditions of the lung associated with excessive cell proliferation, remodeling, inflammation, vasoconstriction, bronchoconstriction, airway hyperreactivity and edema. | 2013-10-24 |
20130281486 | 2,3-DIHYDROBENZO(1,4) DIOXIN-2-YLMETHYL DERIVATIVES AS ALPHA2C ANTAGONISTS FOR USE IN THE TREATMENT OF PERIPHERIC AND CENTRAL NERVOUS SYSTEM DISEASES - Compounds of formula I | 2013-10-24 |
20130281487 | Solid Forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3-carboxamide - The present invention relates to crystalline solvate forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1) and methods for their preparation. The present invention further relates to pharmaceutical compositions comprising the crystalline solvate forms, as well as methods of treatment therewith. | 2013-10-24 |
20130281488 | MALEATE SALTS OF (E)-N--4-(DIMETHYLAMINO)-2-BUTENAMIDE AND CRYSTALLINE FORMS THEREOF - The present invention relates to maleate salt forms of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, methods of preparing crystalline maleate salt forms, the associated compounds, and pharmaceutical compositions containing the same. The maleate salts are useful in treating cancers, particularly those affected by kinases of the epidermal growth factor receptor family. | 2013-10-24 |
20130281489 | QUATERNARY AMMONIUM COMPOUNDS USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS - The invention provides compounds of the formula: | 2013-10-24 |
20130281490 | Disubstituted Beta-lactones as Inhibitors of N-Acylethanolamine Acid Amidase (NAAA) - The present invention provides compounds and pharmaceutical compositions for inhibiting N-acylethanolamine acid amidase (NAAA). Inhibition of NAAA is contemplated as a method to sustain the levels of palmitoylethanolamide (PEA) and oleylethanolamide (OEA), two substrates of NAAA, in conditions characterized by reduced concentrations of PEA and OEA. The invention also provides methods for treating inflammatory diseases and pain, and other disorders in which decreased levels of PEA and OEA are associated with the disorder. | 2013-10-24 |
20130281492 | NOVEL OXAZOLIDINONE DERIVATIVES - The present invention relates to novel derivatives of oxazolidinone, a method thereof and pharmaceutical compositions comprising the derivatives for use in an antibiotic. The oxazolidinone derivatives of the present invention show inhibitory activity against a broad spectrum of bacteria and lower toxicity. The prodrugs, prepared by reacting the compound having hydroxyl group with amino acid or phosphate, have an excellent efficiency on solubility thereof against water. Further, the derivatives of the present invention may exert potent antibacterial activity versus various human and animal pathogens, including Gram-positive bacteria such as | 2013-10-24 |
20130281493 | Method for Treating Cancer Harboring a p53 Mutation - A method for determining if a subject with cancer or precancerous lesions or a benign tumor, will respond to treatment with an inhibitor selected from the group comprising an inhibitor of one or more enzymes in the mevalonate pathway, an inhibitor of geranylgeranyl transferase, an inhibitor of farnesyl transferase or an inhibitor of squalene synthase, by (i) obtaining a sample of the cancer cells, precancerous cells or benign tumor cells from the subject, (ii) assaying the cells in the sample for the presence of a mutated p53 gene or a mutant form of p53 protein or a biologically active fragment thereof, and (iii) if the cells have the mutated p53 gene or mutant form of the p53 protein, then determining that the subject will respond to treatment with the inhibitor or combinations thereof. Some embodiments are directed to treatment with the inhibitors. | 2013-10-24 |
20130281494 | POLYMORPHS OF N-(6-(4-CHLOROPHENOXY)HEXYL)-N'-CYANO-N"-(4-PYRIDYL)GUANIDINE, AND PREPARATION THEREOF AND USE THEREOF - Disclosed are a polymorphs I-VI of N-(6-(4-chlorophenoxy)hexyl)-N′-cyano-N″-(4-pyridyl)guanidine or of a solvate thereof, a preparation method thereof, and a use thereof as a biological active ingredient. The polymorphs are useful in treatment of cancers, and diseases or disorders caused by abnormal cell proliferation. | 2013-10-24 |
20130281495 | SYDNONIMINES-SPECIFIC DOPAMINE REUPTAKE INHIBITORS AND THEIR USE IN TREATING DOPAMINE RELATED DISORDERS - Derivatives of Sydnonimine and its analogues, which bind selectively to dopamine transporter (DAT) proteins are useful for treating and delaying the progression of disorders and illnesses that are alleviated by inhibiting dopamine reuptake. | 2013-10-24 |
20130281496 | Synergistic Fungicidal Active Substance Combinations - The novel active compound combinations of a carboxamide of the general formula (I) (group 1) | 2013-10-24 |
20130281497 | MACROCYCLIC COMPOUNDS AND METHODS OF TREATMENT - The instant invention describes macrocyclic compounds having therapeutic activity, and methods of treating disorders such as methods of modulating bone processes, and methods of treating bone-related disease, disorders, and symptoms thereof. | 2013-10-24 |
20130281498 | AMINOTHIAZOLE MODULATORS OF BETA-3-ADRENORECEPTOR - The present invention relates to new aminothiazole modulators of beta-3-adrenoreceptor activity, pharmaceutical compositions thereof, and methods of use thereof. | 2013-10-24 |
20130281499 | COMPOUNDS - The present invention relates to substituted triazole compounds of the formula (I): | 2013-10-24 |
20130281500 | Synergistic Fungicidal Active Substance Combinations - The novel active compound combinations of a carboxamide of the general formula (I) (group 1) | 2013-10-24 |
20130281501 | TOPICAL LOCALIZED ISOXAZOLINE FORMULATION - This invention provides topical localized formulations comprising an isoxazoline compound and a pharmaceutically or veterinary acceptable liquid carrier vehicle comprising N,N-diethyl-3-methylbenzamide as a solvent and an improved method for controlling, and preventing parasite infestation in animals. | 2013-10-24 |
20130281502 | POST-TREATMENT BREAST CANCER PROGNOSIS - The disclosure includes the identification and use of gene expression profiles, or patterns, with clinical relevance to extended treatment and cancer-free survival in a patient. In particular, the disclosure includes the identities of genes that are expressed in correlation with benefit in a switch in endocrine therapy used to treat a patient. The levels of gene expression are disclosed as a molecular index for predicting clinical outcome, and so prognosis, for the patient. The disclosure further includes methods for predicting cancer recurrence, and/or predicting occurrence of metastatic cancer, after initial treatment with an anti-estrogen agent. The disclosure further includes methods for determining or selecting the treatment of a subject based upon the likelihood of life expectancy, cancer recurrence, and/or cancer metastasis. | 2013-10-24 |
20130281503 | MODULATION OF RESPONSE REGULATORS BY IMIDAZOLE DERIVATIVES - The present disclosure provides methods and compositions useful for screening agents for activity in modulating response regulator signaling activity, which is, in turn, useful for determining whether these agents modulate biofilm formation or lowers the minimum inhibitory concentration (MIC) of an antibiotic, useful in determining or selecting optimum agents and/or agent dosages in modulating a biofilm of interest or lowering the minimum inhibitory concentration (MIC) of an antibiotic, and useful as a research tool for studying response regulators. | 2013-10-24 |
20130281504 | Reduction of Microglia-Mediated Neurotoxicity by KCa3.1 Inhibition - Methods for deterring microglia-mediated neurotoxicity in a human or non-human animal subjects comprising the step of inhibiting or blocking the intermediate-conductance calcium-activated potassium channel KCa3.1 in microglia, such as in subjects how suffer from neurodegenerative diseases (e.g., Alzeheimer's Disease) or ischemic/anoxic/hypoxic conditions. The inhibition or blocking of the KCa1.3 channels may be accomplished by administering a KCa3.1 inhibiting substance, such as 1-[(2-chlorophenyl)diphenylmethyl]-1H-pyrazole (TRAM-34). | 2013-10-24 |
20130281505 | PYRAZOL-4-YL CARBOXAMIDE DERIVATIVES AS MICROBIOCIDES - Compounds of formula (I) wherein R | 2013-10-24 |
20130281506 | COMBINATION OF A NON-STEROIDAL ANTI-INFLAMMATORY DRUG WITH AN ANTI-HISTAMINIC DRUG INTENDED FOR OPHTHALMIC USE - The present invention is directed to a stable formulation of a combination of ketorolac (non-steroidal anti-inflammatory drug) with olopatadine (anti-histaminic drug) intended for ophthalmic use. This pharmaceutical composition is used for treatment of ophthalmic diseases and conditions, particularly seasonal ocular surface allergy. | 2013-10-24 |
20130281507 | METHOD FOR DEPIGMENTING KERATIN MATERIALS USING RESORCINOL DERIVATIVES - The invention relates to compounds of formula (I): The invention likewise relates to a cosmetic method for depigmenting, lightening and/or whitening keratin materials, more particularly the skin, that utilizes these compounds | 2013-10-24 |
20130281508 | MicroRNA target site for cell- or tissue-specific inhibition of expression of a transgene - The present invention is directed to an isolated miR-206 target site, comprising or consisting of a nucleic acid sequence with a sequence identity of at least 80% compared to wild type miR-206 target site with SEQ ID No. 1, characterized in that the nucleic acid sequence comprises at least one nucleotide substitution at a position from nucleotide 2 to 8 and/or at least one nucleotide substitution at a position from nucleotide 12 to 16 of SEQ D No. 1, wherein the nucleotide positions of SEQ ID No. 1 are numbered from the 3′- to the 5′-end; as well as to an expression cassette, vector and pharmaceutical composition comprising at least one isolated miR-206 target site of the invention. | 2013-10-24 |
20130281509 | ANTISENSE MODULATION OF FIBROBLAST GROWTH FACTOR RECEPTOR 4 EXPRESSION - Provided herein are methods, compounds, and compositions for reducing expression of fibroblast growth factor receptor 4 (FGFR4) mRNA and protein in an animal. Such methods, compounds, and compositions are useful to treat, prevent, delay, or ameliorate a metabolic disease, or a symptom thereof. | 2013-10-24 |
20130281510 | siRNA Therapy for Transthyretin (TTR) Related Ocular Amyloidosis - The invention relates to a method of treating ocular amyloidosis by reducing TTR expression in a subject by administering a double-stranded ribonucleic acid (dsRNA) that targets a TTR gene to the retinal pigment epithelium of the subject. | 2013-10-24 |
20130281511 | COMPOSITIONS AND METHODS FOR INHIBITING EXPRESSION OF THE ALAS1 GENE - The invention relates to double-stranded ribonucleic acid (dsRNA) compositions targeting the ALAS1 gene, and methods of using such dsRNA compositions to alter (e.g., inhibit) expression of ALAS1. | 2013-10-24 |
20130281512 | AGENTS FOR TREATING DISORDERS INVOLVING MODULATION OF RYANODINE RECEPTORS - The present invention relates to 1,4-benzothiazepine derivatives and their use to treat conditions, disorders and diseases associated with ryanodine receptors (RyRs) that regulate calcium channel functioning in cells. The invention also discloses pharmaceutical compositions comprising the compounds and uses thereof to treat diseases and conditions associated with RyRs, in particular cardiac, musculoskeletal and central nervous system (CNS) disorders. | 2013-10-24 |
20130281513 | siRNA FOR INHIBITION OF Hif1alpha EXPRESSION AND ANTICANCER COMPOSITION CONTAINING THE SAME - Disclosed are small interfering RNA (siRNA) that complementarily binds to a base sequence of Hif1α mRNA transcript, thereby inhibiting expression of Hif1α without inducing immune responses, and a use of the siRNA for prevention and/or treatment of cancer. Since Hif1α is commonly overexpressed in almost all cancer cells, the siRNA that complementarily binds to Hif1α-encoding mRNA may inhibit expression of Hif1α through RNA-mediated interference (RNAi), thereby inhibiting proliferation and metastasis of cancer cells, and thus, the siRNA may be useful as an anticancer agent. | 2013-10-24 |