33rd week of 2013 patent applcation highlights part 54 |
Patent application number | Title | Published |
20130210774 | POTENT AND SELECTIVE INHIBITORS OF HEPATITIS C VIRUS - The present invention is directed to compounds, compositions and methods for treating or preventing hepatitis C virus (HCV) infection in human subjects or other animal hosts. The compounds are as also pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof as pharmaceutical compositions and methods for treatment or prevention of HCV infection. | 2013-08-15 |
20130210775 | AGENT FOR INHIBITING ODOR OF PYRAZINE DERIVATIVES - Provided is an agent for reducing odors of pyrazine derivatives based on an olfactory receptor antagonism. The agent for reducing odors of pyrazine derivatives includes at least one antagonist of olfactory receptor OR5K1 as an active ingredient. | 2013-08-15 |
20130210776 | COMPOSITION FOR THE TREATMENT OF SUPERFICIAL LESIONS - The invention relates to a composition for the treatment of superficial lesions, in particular skin lesions, mucous membrane lesions and/or nail lesions, an applicator comprising such a composition and the use of such a composition. The composition comprises an effective amount of trichloroacetic acid, at least one thickener, and at a physiologically acceptable solvent. And is effective against a plethora of superficial lesions selected from the group consisting of viral warts, verrucae, water warts (molluscum contagiosum), corns and calluses, and skin hyperpigmentation: age spots, solar lentigo, senial lentigo, acne, keratosis pilaris, actinic keratosis, mouth ulcers (canker sores), cold sores, ingrown toenails, onychomycosis, eyelid xanthelasma. | 2013-08-15 |
20130210777 | Amelioration of the Appearance of Bruises - The present invention is directed to compositions and processes for their use that ameliorate the appearance of bruises, making them less cosmetically unappealing. The composition functions by acting both as a humectant and occlusive agent attracting water, returning the skin surface to a smooth state and holding water in place. The re-establishment of a homeostatic state in the skin results in a rapid dissipation of the negative cosmetic effects of the bruise on the skin. | 2013-08-15 |
20130210778 | FORMULATION FOR THE PREVENTION OF CARDIOVASCULAR DISEASE - This invention relates to a method for the prevention of cardiovascular disease, a formulation for the prevention of cardiovascular disease, the use of specified active principals for the manufacture of such a formulation for use in the method and to a method of preparing said formulation. The formulation of the present invention is a combination of active principals for use in the prevention of cardiovascular disease, notably ischaemic heart disease (including heart attacks) and stroke among the general adult population. | 2013-08-15 |
20130210779 | METHOD OF IDENTIFYING TRIPLE NEGATIVE BREAST CANCER - The present invention provides means for identifying or classifying breast tumors based on the levels of nuclear cathepsin-L (CTSL) and nuclear p53 binding protein (53BP1), and methods of treating thereof. | 2013-08-15 |
20130210780 | Nutritional Composition for the Stimulation of Muscle Protein Synthesis - The invention relates to the use of an anabolic amino acid derivative stimulus acting in combination with vitamin D for the manufacture of a medicament or nutritional composition for the prevention and/or treatment of a loss of any one of muscle mass, muscle strength, muscle function, and physical function, or any combination thereof, in a mammal. | 2013-08-15 |
20130210781 | 23-YNE-VITAMIN D3 DERIVATIVE - To provide a novel vitamin D | 2013-08-15 |
20130210782 | TREATING HYPERGLYCEMIA WITH 25-HYDROXYVITAMIN D3 - We disclose treating hyperglycemia in a human with 25-hydroxyyitamin D3 (calcifediol). Blood glucose is reduced to a level which is closer to normal than baseline. Vitamin D3 (cholecalciferol) may optionally be used together with 25-hydroxy vitamin D3. Forms and dosages of a pharmaceutical composition, as well as processes for manufacturing medicaments, are also disclosed. | 2013-08-15 |
20130210783 | NEUROACTIVE STEROID COMPOSITIONS AND METHODS OF USE THEREFOR - Provided are methods for ameliorating a symptom of a neuropsychiatric disorder. Also provided are methods for ameliorating at least one symptom resulting from tobacco cessation; and for ameliorating a symptom of Alzheimer's disease or other cognitive disorder; of schizophrenia, schizoaffective disorder, or other psychotic disorder; of a depressive disorder; of bipolar disorder; of post-traumatic stress disorder or other anxiety disorder; of a pain disorder; or of traumatic brain injury. Also provided are methods for ameliorating a sleep disorder; for improving cognitive functioning; for predicting a predisposition to suicide, suicidal ideation, and/or suicidal behavior; and for ameliorating a neurodegenerative disorder. In some embodiments, the methods include administering to a subject in need thereof an effective amount of a neuroactive steroid composition, pharmaceutically acceptable salts thereof, derivatives thereof, or combinations thereof. | 2013-08-15 |
20130210784 | COMBINATIONS AND METHODS FOR TREATING NON AGE-RELATED HEARING IMPAIRMENT IN A SUBJECT - The present invention generally relates to treating non age-related hearing impairments. More specifically, the present invention provides combinations and methods for treatment and prevention of non age-related hearing impairment in a subject. | 2013-08-15 |
20130210785 | PROGESTERONE ANALOGS AND USES RELATED THERETO - This disclosure relates to progesterone derivatives and uses related thereto. In certain embodiments, the disclosure relates to compounds disclosed herein and uses for managing inflammation resulting from traumatic brain injury or stroke. | 2013-08-15 |
20130210786 | TREATMENT OF L-DOPA, DOPAMINE AGONIST AND/OR DOPAMINE ENHANCER INDUCED DISORDERS - One or more agent selected from A/B-cis furostane, furostene, spirostane and spirostene steroidal sapogenins and ester, ether, ketone or glycosylated forms thereof, including E and/or F ring opened derivatives thereof, is used to treat or prevent L-DOPA, dopamine agonist and/or dopamine enhancer induced disorders, such as L-DOPA induced dyskinesia (LID), which is a side effect of L-DOPA, dopamine agonist and/or dopamine enhancer therapies, e.g., for Parkinson's disease. The agent according to the invention may be administered in association with the therapeutic agent for the treatment of the Parkinson's disease or another dopamine-responsive disorder. | 2013-08-15 |
20130210787 | C-3 CYCLOALKENYL TRITERPENOIDS WITH HIV MATURATION INHIBITORY ACTIVITY - Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-3 cycloalkenyl triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II, III and IV: | 2013-08-15 |
20130210788 | METHOD FOR POST COITAL CONTRACEPTION IN OVERWEIGHT OR OBESE FEMALE SUBJECTS USING ULIPRISTAL ACETATE - The invention provides a method for providing post coital contraception in a female subject, comprising providing the subject with a therapeutically effective amount of ulipristal acetate, wherein the female subject is overweight or obese. | 2013-08-15 |
20130210789 | TESTOSTERONE GEL AND METHOD OF USE - The present invention relates to an improved transdermal hydroalcoholic testosterone gen formulation that provides, among other things, a desirable pharmacokinetic hormone profile, and methods of use. | 2013-08-15 |
20130210790 | TESTOSTERONE GEL AND METHOD OF USE - The present invention relates to an improved transdermal hydroalcoholic testosterone gel formulation that provides, among other things, a desirable pharmacokinetic hormone profile, and methods of use. | 2013-08-15 |
20130210791 | TESTOSTERONE GEL AND METHOD OF USE - The present invention relates to an improved transdermal hydroalcoholic testosterone gen formulation that provides, among other things, a desirable pharmacokinetic hormone profile, and methods of use. | 2013-08-15 |
20130210792 | METHOD OF TREATING DISORDER RELATED TO HIGH CHOLESTEROL CONCENTRATION - A method of treating a disorder related to a high cholesterol concentration, comprising administering to a subject in need thereof a compound of formula (I): | 2013-08-15 |
20130210793 | PHOTOLABILE CAGED TRANSITION METAL COMPLEXES AND METHODS OF USING THE SAME - The present invention provides compounds of Formula I: | 2013-08-15 |
20130210794 | NANOSTRUCTURED EZETIMIBE COMPOSITIONS, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM - The present invention is directed to nanostructured Ezetimibe compositions, process for the preparation thereof and pharmaceutical compositions containing them. The nanoparticles of Ezetimibe according to the invention have an average particle size of less than about 400 nm. The stable nanostructured particles of the invention are presented by increased solubility, dissolution rate, permeability and bioequivalent or enhanced biological performance compared to the marketed drug. Ezetimibe is an anti-hyperlipidemic medication that is used to lower cholesterol levels. It acts by decreasing cholesterol absorption in the intestine. | 2013-08-15 |
20130210795 | SUBSTITUTED DICYANOPYRIDINES AND USE THEREOF - The present application relates to novel substituted dicyanopyridines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prophylaxis of cardiovascular disorders. | 2013-08-15 |
20130210796 | TETRAZOLE COMPOUNDS AS CALCIUM CHANNEL BLOCKERS - The present invention relates to novel tetrazole compounds; to processes for their preparation; to pharmaceutical compositions containing the compounds; and to the use of the compounds in therapy to treat diseases for which blocking the Ca | 2013-08-15 |
20130210797 | ADENOSINE A1 AGONISTS FOR THE TREATMENT OF GLAUCOMA AND OCULAR HYPERTENSION - The present invention relates to the use of selective adenosine A1 agonists, in particular the dicyanopyridines of formula (I), for the treatment and/or prophylaxis of glaucoma and ocular hypertension as well as the their use for the production of a medicament for the treatment and/or prophylaxis of glaucoma and ocular hypertension. | 2013-08-15 |
20130210798 | SOLUBLE GUANYLATE CYCLASE ACTIVATORS - This inventions relates to compounds having the structure Formula I and pharmaceutically acceptable salts thereof which are soluble guanylate cyclase activators. The compounds are useful for treatment or prevention of cardiovascular diseases, endothelial dysfunction, diastolic dysfunction, atherosclerosis, hypertension, pulmonary hypertension, angina pectoris, thromboses, restenosis, myocardial infarction, strokes, cardiac insufficiency, pulmonary hypertonia, erectile dysfunction, asthma bronchiale, chronic kidney insufficiency, diabetes, or cirrhosis of the liver. | 2013-08-15 |
20130210799 | NOVEL AZETIDINE DERIVATIVES - The invention relates to a compound of formula (I) | 2013-08-15 |
20130210800 | PYRIDINE-2-DERIVATIVES AS SMOOTHENED RECEPTOR MODULATORS - The present application relates to compounds of Formula (I), and Formula (II), or pharmaceutically acceptable salt thereof, wherein A, X, Y, Z, e, f, R | 2013-08-15 |
20130210801 | 2-QUINOLINYL-ACETIC ACID DERIVATIVES AS HIV ANTIVIRAL COMPOUNDS - The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula (I), processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula (I). | 2013-08-15 |
20130210802 | IMIDAZOPYRIDINES SYK INHIBITORS - Certain imidazopyridines (I) and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample. | 2013-08-15 |
20130210803 | FUSED TETRACYCLIC PYRIDO [4,3-B] INDOLE AND PYRIDO [3,4-B] INDOLE DERIVATIVES AND METHODS OF USE - This disclosure is directed to fused tetracyclic pyrido[4,3-b]indoles and pyrido[3,4-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder. | 2013-08-15 |
20130210804 | TRICYCLIC MGLUR5 RECEPTOR MODULATORS - The present invention is directed to tricyclic compounds which are positive allosteric modulators of metabotropic glutamate receptors, particularly the mGluR5 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved. | 2013-08-15 |
20130210805 | QUINAZOLINONE-TYPE COMPOUNDS AS CRTH2 ANTAGONISTS - This application provides for compounds of the formula Formula I or a pharmaceutically acceptable salt thereof, wherein the individual variables are defined herein, as well as processes to prepare these compounds, pharmaceutical compositions comprising the same and their use in treating disease state associated with the CRTH | 2013-08-15 |
20130210806 | TRICYCLIC INDOLE DERIVATIVES USEFUL ENDOTHELIAL LIPASE INHIBITORS - The present invention is directed to tricyclic indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by endothelial lipase, for example, cardiovascular disorders. | 2013-08-15 |
20130210807 | Tricyclic Compounds as Allosteric Modulators of Metabotropic Glutamate Receptors. - The present invention describes and claims compounds of the Structural Formula I, Structural Formula II, or Structural Formula III: wherein R | 2013-08-15 |
20130210808 | CHOLINERGIC ENHANCERS WITH IMPROVED BLOOD-BRAIN BARRIER PERMEABILITY FOR THE TREATMENT OF DISEASES ACCOMPANIED BY COGNITIVE IMPAIRMENT - The present invention refers to compounds that, in addition to enhancing the sensitivity to acetylcholine and choline, and their exogenous agonists, of neuronal cholinergic receptors and/or acting as cholinesterase inhibitors and/or neuroprotective agents, have enhanced blood-brain barrier permeability in comparison to their parent compounds. The compounds are derived (either formally by their chemical structure or directly by chemical synthesis) from natural compounds belonging to the class of amaryllidaceae alkaloids e.g., galantamine, narwedine and lycoramine, or from metabolites of said compounds. The compounds of the present invention can either interact as such with their target molecules, or they can act as “pro-drugs”, in the sense that after reaching their target regions in the body they are converted by hydrolysis or enzymatic attack to the original parent compound and react as such with their target molecules, or both. The compounds of this invention may be used as medicaments. | 2013-08-15 |
20130210809 | NOVEL 2-AMINO-4-PYRAZOLYL-THIAZOLE DERIVATIVES AND THEIR USE AS ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS - The present invention relates to novel compounds of Formula (1), wherein M, A and B are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors-subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved. | 2013-08-15 |
20130210810 | Protein Kinase C Inhibitors and Uses Thereof - This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes. | 2013-08-15 |
20130210811 | PICOLINAMIDE AND PYRIMIDINE-4-CARBOXAMIDE COMPOUNDS, PROCESS FOR PREPARING AND PHAMACEUTICAL COMPOSITION COMPRISING THE SAME - Provided are picolinamide and pyrimidine-4-carboxamide compounds, a method for preparing the same, a pharmaceutical composition containing the same, and a medical use using the compound as an agent for preventing, regulating, and treating diseases related to regulation of glucocorticoids by using selective inhibitory activity of the compound for an 11β-HSD1 enzyme. The picolinamide and pyrimidine-4-carboxamide compounds of the present invention are selective inhibitors of human-derived 11β-HSD1 enzymes, and are useful in an agent for preventing, regulating, and treating diseases related to glucocorticoid regulation in which human-derived 11β-HSD1 enzymes are involved, for example, metabolic syndromes such as, type 1 and type 2 diabetes, diabetes later complications, latent autoimmune diabetes adult (LADA), insulin tolerance syndromes, obesity, impaired glucose tolerance (IGT), impaired fasting glucose (IFG), damaged glucose tolerance, dyslipidemia, atherosclerosis, hypertension, etc. | 2013-08-15 |
20130210812 | Aqueous Pharmaceutical Composition With Enhanced Stability - The present invention is an aqueous pharmaceutical composition that includes an ionized therapeutic agent, an ionic component and guar gum. The guar gum is present in the composition a concentration sufficient to limit interactions between the ionized therapeutic agent and the ionic component thereby imparting stability to the composition. The composition is preferably at or near physiologic pH. The aqueous pharmaceutical composition has been found particularly useful as an aqueous ophthalmic, otic or nasal composition. The pharmaceutical composition, due to its characteristics, is particularly suitable as an ophthalmic composition. | 2013-08-15 |
20130210813 | Male Contraceptive Compositions and Methods of Use - The invention relates to compositions and methods for effecting male contraception. | 2013-08-15 |
20130210814 | Cycloalkyl Substituted Pyrimidinediamine Compounds And Their Uses - The present disclosure provides 2,4-pyrimidinediamine compounds having antiproliferative activity, compositions comprising the compounds and methods of using the compounds to inhibit cellular proliferation and to treat proliferate diseases such as tumorigenic cancers. | 2013-08-15 |
20130210815 | SUBSTITUTED IMIDAZOPYRAZINES - The present invention relates to substituted imidazopyrazine compounds of general formula (I) in which A, R | 2013-08-15 |
20130210816 | FUSED-IMIDAZOYL COMPOUNDS USEFUL AS ANTIMICROBIAL AGENTS - The invention relates to fused-imidazoyl compounds of Formula (I): wherein ring A, R | 2013-08-15 |
20130210817 | METHODS OF CONTROLLING NEONICOTINOID RESISTANT APHIDS - The invention relates to a method of controlling aphids that are resistant to neonicotinoid insecticides, using the compound pyrifluquinazon in free form or in agrochemically acceptable salt form as well as the use of compositions comprising said compound to control neonicontinoid resistant insects. In particular the methods relate to controlling neonicotinoid resistant insects in the Aphididae family, that are resistant to one or more neonicotinoid insecticides. Methods of the invention find particular use in controlling neonicotinoid resistant insects in crops of useful plants. Furthermore, the invention extends to methods of controlling plant viruses spread by neonicotinoid resistant insects. | 2013-08-15 |
20130210818 | Novel Heterocyclic Compounds and Uses Thereof - New substituted heterocyclic compounds, compositions containing them, and methods of using them for the inhibition of Raf kinase activity are provided. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer. | 2013-08-15 |
20130210819 | QUINAZOLINE DERIVATIVES - Compounds of the formula I in which R, X, L | 2013-08-15 |
20130210820 | Pharmaceutical Compounds - The invention provides a compound of the formula (1): | 2013-08-15 |
20130210821 | Methods for Treating Obesity - The disclosure provides for methods of treating obesity and related disorders. Pharmaceutical compositions and methods of using, e.g. in the treatment of obesity are provided. | 2013-08-15 |
20130210822 | Compositions for Modulating a Kinase Cascade and Methods of Use Thereof - The invention relates to compositions comprising 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts. The invention provides an efficient process for the synthesis of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts and methods for modulating one or more components of a kinase cascade using the compositions of the invention. The present invention also provides a novel polymorph of the mesylate salt of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide (Form A), characterized by a unique X-ray diffraction pattern and Differential Scanning calorimetry profile, as well as a unique crystalline structure. | 2013-08-15 |
20130210823 | METHODS FOR CONTROLLING MITES - The present invention relates to the use of pymetrozine, and salts and compositions thereof, as a miticide, to methods and compositions comprising pymetrozine for the control of bee mites and for the reduction of bee mite infestations, such as the control and reduction of infestations of parasitic bee mites, such as | 2013-08-15 |
20130210824 | Substituted fused imidazoles and pyrazoles and use thereof - The present application relates to novel substituted fused imidazoles and pyrazoles, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases and to the use thereof producing medicaments for the treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of cardiovascular disorders. | 2013-08-15 |
20130210825 | SUBSTITUTED IMIDAZO[1,2-B]PYRIDAZINES - The invention relates to imidazo[1,2-b]pyridazines of general formula (I) a process for their manufacuture and their use for the treatment of benign and malignant neoplasia. | 2013-08-15 |
20130210826 | METHODS FOR TREATING PAIN - The present invention features methods and compositions for preventing, reducing, or treating a traumatic, metabolic, or toxic peripheral nerve lesion or pain including neuropathic pain, inflammatory, and nociceptive pain by administering to a mammal a compound that reduces expression or activity of BH4. This reduction may be achieved by reducing activity of a BH4 synthetic enzyme, including GTP cyclohydrolase, sepiapterin reductase, or dihydropteridine reductase; antagonizing the cofactor function of BH4 or BH4-dependent enzymes; or blocking BH4 binding to membrane bound receptors. The invention provides methods for diagnosing pain or a peripheral nerve lesion in a mammal by measuring levels of BH4 or its metabolites in biological sample or the levels or activity of any one of the BH4 synthetic enzyme in tissue samples of a mammal. Disclosed are screening methods that use BH4 or BH4 synthetic enzymes, BH4-dependent enzymes, and BH4-binding receptors to identify therapeutics for the treatment, prevention, or reduction of pain. | 2013-08-15 |
20130210827 | NOVEL BENZENESULFONAMIDES AS CALCIUM CHANNEL BLOCKERS - The present application relates to calcium channel inhibitors comprising compounds of formula (I), formula (II), formula (III), or formula (IV), | 2013-08-15 |
20130210828 | STRUCTURE, SYNTHESIS, AND APPLICATIONS FOR POLY (PHENYLENE) ETHYNYLENES (PPEs) - The present disclosure provides novel poly(phenylene ethynylene) (PPE) compounds, methods for synthesizing these compounds, and materials and substances incorporating these compounds. The various PPEs show antibacterial, antiviral and antifungal activity. | 2013-08-15 |
20130210829 | APPLICATION OF 5-HT6 RECEPTOR ANTAGONISTS FOR THE ALLEVIATION OF COGNITIVE DEFICITS OF DOWN SYNDROME - Methods for treating Down syndrome and improving cognitive function of a patient with an intellectual disability are disclosed. 5-hydroxytryptamine sub-receptor six (5-HT | 2013-08-15 |
20130210830 | THERAPEUTIC COMPOSITIONS - The invention relates to a product containing the compound of formula (I) below (I) or a pharmaceutically acceptable salt of this compound, in combination with at least one compound having PDE5-inhibitory properties, or a pharmaceutically acceptable salt thereof, for therapeutic use, simultaneously, separately or over a period of time, in the treatment of a disease wherein vasoconstriction is involved. | 2013-08-15 |
20130210831 | PYRROLOPYRIMIDINE COMPOUNDS AND USES THEREOF - The present disclosure provides pyrrolopyrimidine compounds and methods of use therefor. For example, the disclosure provides certain pyrrolopyrimidine compounds capable of inhibiting JAK kinases. The disclosure further provides the pharmaceutical compositions containing these pyrrolopyrimidine compounds, and use of these pyrrolopyrimidine compounds in the treatment of disorders or diseases, such as inflammatory diseases and cancer. | 2013-08-15 |
20130210832 | 1H-IMIDAZO[4,5-C]QUINOLINES - The present invention encompasses compounds of general formula (1), wherein the groups R | 2013-08-15 |
20130210833 | PROCESS FOR THE PREPARATION OF CHIRAL TRIAZOLONES - A process for the preparation of a chiral compound, in particular posaconazole, wherein the process comprises mixing and reacting the compounds of formula (I) Y | 2013-08-15 |
20130210834 | INDIRUBIN DERIVATIVES AND USES THEREOF IN TREATING CHRONIC MYELOGENOUS LEUKEMIA - Indirubin is the major active anti-tumor component of a traditional Chinese herbal medicine used for treatment of chronic myelogenous leukemia (CML). One aspect of the invention relates to a method of treating CML using at least one indirubin derivative compound or a pharmaceutical composition thereof. Indirubin derivatives (IRDs) potently inhibited Signal Transducer and Activator of Transcription 5 (Stat5) protein in CML cells. Compound IRD 810 inhibits Bcr-Abl/Stat5 or Src/Stat5 signaling in human KCL-22 CML and imatinib-resistant human KCL-22 CML cells expressing the T315I mutant Bcr-Abl. Previous studies indicate that SFKs cooperate with Bcr-Abl to activate downstream Stat5 signaling. Activation of Stat5 was strongly blocked by IRD 810 in CML cells. IRDs disclosed herein have been identified as potent inhibitors of Bcr-Abl/Stat5 or SFK/Stat5 signaling pathway. IRDs disclosed herein are new therapeutics for wild type or T315I mutant Bcr-Abl-positive CML patients, and may also treat other solid tumors, including prostate cancer and lymphoma. | 2013-08-15 |
20130210835 | PHARMACEUTICAL COMPOSITIONS - A composition of an antitussive, a decongestant, or an antihistamine to treat respiratory and oral pharyngeal congestion and related symptoms in a patient. | 2013-08-15 |
20130210836 | MICROBICIDES - The present invention relates to a compound of formula (I): wherein the substituents have the definitions as defined in claim | 2013-08-15 |
20130210837 | Compounds and Their Use as BACE Inhibitors - The present invention relates to compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Down's syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration. | 2013-08-15 |
20130210838 | PYRAZOLO[1,5-A]PYRIMIDINES AS MARK INHIBITORS - The invention encompasses pyrazolo[1,5-a]pyrimidine derivatives which selectively inhibit microtubule affinity regulating kinase (MARK) and are therefore useful for the treatment or prevention of Alzheimer's disease. Pharmaceutical compositions and methods of use are also included. | 2013-08-15 |
20130210839 | FUSED AMINODIHYDROPYRIMIDINE DERIVATIVE - The present invention provides, for example, the following compound: | 2013-08-15 |
20130210840 | Anti-Cellulite Composition and Method of Treating Cellulite - A cellulite-reducing topical composition comprising a lecithin organogel, an ethylene oxide-propylene oxide-ethylene oxide triblock copolymer, caffeine, a retinoid, and optionally at least one vitamin, vitamin derivative or vitamin precursor. | 2013-08-15 |
20130210841 | MUCOADHESIVE BUCCAL TABLETS FOR THE TREATMENT OF OROFACIAL HERPES - The present invention relates to the treatment and/or prevention of muco-cutaneous herpes simplex virus diseases using prolonged release mucoadhesive buccal tablets comprising an acyclic guanosine antiviral agent. These tablets are particularly-suitable for the treatment and/or prevention of orofacial herpes. | 2013-08-15 |
20130210842 | PURE ERLOTINIB - The present invention relates to processes for the preparation of erlotinib and salts and polymorphs thereof, preferably of high purity. The present invention also relates to erlotinib and salts and polymorphs thereof preparable by said processes, to medical uses of said erlotinib, salts and polymorphs, and to pharmaceutical compositions comprising the same. | 2013-08-15 |
20130210843 | PREDICTIVE MARKER FOR EGFR INHIBITOR TREATMENT - The present invention provides a biomarker which is predictive for the clinical benefit of EGFR inhibitor treatment in cancer patients. | 2013-08-15 |
20130210844 | BICYCLIC COMPOUNDS AS mPGES-1 INHIBITORS - The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases. | 2013-08-15 |
20130210845 | Tricyclic Proteasome Activity Enhancing Compounds - Proteinopathies result from the proteasome not acting efficiently enough to eliminate harmful proteins and prevent the formation of the pathogenic aggregates. As described herein, inhibition of proteasome-associated deubiquitinase Usp14 results in increased proteasome efficiency. The present invention therefore provides novel compositions and methods for inhibition of Usp14, enhancement of proteasome activity and treatment of proteinopathies. | 2013-08-15 |
20130210846 | USE OF NOVEL PAN-CDK INHIBITORS FOR TREATING TUMORS - The invention relates to the use of selected sulfoximine-substituted anilinopyrimidine derivatives of the formula (I) for treating tumors. | 2013-08-15 |
20130210847 | PROCESS FOR THE PREPARATION OF NILOTINIB - The present invention relates a process for the preparation of a compound of formula (I): | 2013-08-15 |
20130210848 | NEW SALT OF A PYRIMIDIN DERIVATIVE - The present invention relates to a salt of a pyrimidin derivative of the acid (3R,5S,6E)-7-[4-(4-fluorophenyl)-2-(N-methylmethanesulfonamide)-6-(propan-2-yl)pyrimidin-5-yl]-3,5-dihydroxyhept-6-enoic, to a method for preparing same and to the use thereof in formulating pharmaceutical formulations. | 2013-08-15 |
20130210849 | Methods for treating disorders associated with mGLU receptors including addiction and depression - Methods are provided for treating disorders associated with mGlu receptors by simultaneously inhibiting at least two mGluRs belonging to at least two different groups. In one embodiment, there are provided methods for treating a disorder associated with mGlu receptors 2, 3, and 5, including administering to a subject in need thereof an effective amount of at least one antagonist which modulates mGluR2, mGluR3, and mGluR5. The disorders treated by the method include, for example, nicotine addiction, cocaine addiction, and depression. | 2013-08-15 |
20130210850 | Furo[3,4-c]quinoline derivatives, medicaments containing such compounds, their use and process for their preparation - The present invention relates to compounds defined by formula I | 2013-08-15 |
20130210851 | Crystalline forms of a hexahydrofuro[3,4-c]quinoline derivative - The present invention relates to crystalline forms of (3R,9S)-4-isopropyl-7,7-dimethyl-3-(4-(trifluoromethyl)phenyl)-2′,3′,5′,6,6′,7,8,9-octahydro-3H-spiro[furo[3,4-c]quinoline-1,4′-pyran]-9-ol and its hydrochloride or hydrobromide salts, to a process for the manufacture thereof, and to the use thereof in pharmaceutical compositions. | 2013-08-15 |
20130210852 | METHODS FOR TREATING INFECTION - The present invention provides new methods and kits for treating and preventing bacterial infection. | 2013-08-15 |
20130210853 | Injectable Flowable Composition Comprising Buprenorphine - The present invention is directed to a buprenorphine sustained release delivery system capable of delivering buprenorphine, a metabolite, or a prodrug thereof for a duration of about 14 days to about 3 months. The buprenorphine sustained release delivery system includes a flowable composition and a solid implant for the sustained release of buprenorphine, a metabolite, or a prodrug thereof. The implant is produced from the flowable composition. The buprenorphine sustained release delivery system provides in situ 1-month and 3-month release profiles characterized by an exceptionally high bioavailability and minimal risk of permanent tissue damage and typically no risk of muscle necrosis. | 2013-08-15 |
20130210854 | Compositions Comprising Enzyme-Cleavable Prodrugs of Active Agents and Inhibitors Thereof - The present disclosure provides pharmaceutical compositions, and their methods of use, where the pharmaceutical compositions comprise a prodrug that provides enzymatically-controlled release of a drug and an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of the drug from the prodrug so as to attenuate enzymatic cleavage of the prodrug. The disclosure provides pharmaceutical compositions which comprise an enzyme inhibitor and a prodrug that contains an enzyme-cleavable moiety that, when cleaved, facilitates release of the drug. | 2013-08-15 |
20130210855 | 2 X 2 X 2 WEEK DOSING REGIMEN FOR TREATING ACTINIC KERATOSIS WITH PHARMACEUTICAL COMPOSITIONS FORMULATED WITH 3.75 % IMIQUIMOD - Pharmaceutical formulations and methods for the topical or transdermal delivery of 1-isobutyl-1H-imidazo[4,5-c]-quinolin-4-amine or 1-(2-methylpropyl)-1H-imidazo[4,5-c]quinolin-4-amine, i.e., imiquimod, to treat actinic keratosis with short durations of therapy, than currently prescribed for the commercially available Aldara® 5% imiquimod cream, as now approved by the U.S. Food & Drug Administration (“FDA”), are disclosed and described. More specifically, lower dosage strength imiquimod formulations to deliver an efficacious dose of imiquimod for treating actinic keratosis with an acceptable safety profile and dosing regimens that are short and more convenient for patient use than the dosing regimen currently approved by the U.S. Food & Drug Administration (“FDA”) for Aldara® 5% imiquimod cream to treat actinic keratosis are also disclosed and described. | 2013-08-15 |
20130210856 | COMPOSITIONS AND METHODS FOR TREATING SLEEP DISORDERS - The present invention provides liquid dosage forms for treating narcolepsy. The liquid dosage form includes zolpidem or a pharmaceutically acceptable salt thereof, a carbonate salt, a metal oxide, and a borate salt. The present invention also provides methods for treating somnambulism. The methods include administering an emulsion that includes zolpidem, a bicarbonate salt, a citrate salt, and a phosphate salt. | 2013-08-15 |
20130210857 | Inhibitors of Human Immunodeficiency Virus Replication - The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection. | 2013-08-15 |
20130210858 | SULFAMOYL BENZOIC ACID HETEROBICYCLIC DERIVATIVES AS TRPM8 ANTAGONISTS - The present invention relates to sulfamoyl benzoic acid heterobicyclic derivatives of the formula (I) or a pharmaceutically acceptable salt thereof or a prodrug thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the TRPM8 receptor. | 2013-08-15 |
20130210859 | NOVEL CORTISTATIN A ANALOG AND USE THEREOF - A compound represented by the general formula (M): | 2013-08-15 |
20130210860 | PROPHYLACTIC AND/OR THERAPEUTIC AGENT AGAINST LYMPHEDEMA - Provided is a new prophylactic and/or therapeutic agent for lymphedema, for which until now there has been no effective means of treatment, and the prophylactic and/or therapeutic agent for lymphedema comprises, as an active ingredient, a compound represented by the following formula (1), a lactone derivative thereof, or a salt of the compound or lactone derivative: | 2013-08-15 |
20130210861 | METHODS AND COMPOSITIONS FOR MANAGING CARDIOVASCULAR DISEASE ASSOCIATED WITH CHRONIC KIDNEY DISEASE - Methods of treating cardiovascular disease in patients predisposed to or afflicted with kidney disease, particularly chronic kidney disease, are described. In such methods, therapeutically effective amounts of chloroquine-based compounds, for example, hydroxychloroquine, are administered to prevent or otherwise ameliorate arthrosclerosis and other cardiovascular diseases. | 2013-08-15 |
20130210862 | SUSTAINED RELEASE INTRAOCULAR IMPLANTS CONTAINING TYROSINE KINASE INHIBITORS AND RELATED METHODS - Biocompatible intraocular implants include a tyrosine kinase inhibitor and a biodegradable polymer that is effective to facilitate release of the tyrosine kinase inhibitor into an eye for an extended period of time. The therapeutic agents of the implants may be associated with a biodegradable polymer matrix, such as a matrix that is substantially free of a polyvinyl alcohol. The implants may be placed in an eye to treat or reduce the occurrence of one or more ocular conditions. | 2013-08-15 |
20130210863 | SYNERGISTIC INSECTICIDAL MIXTURES - The present invention relates to synergistic insecticidal mixtures comprising a) a Pyrethroid insecticide (preferably bifenthrin), b) a Neonicotinoid insecticide (preferably imidacloprid) and c) a Benzoylphenyl urea insecticide (preferably novaluron) and to the related compositions and methods of controlling insects. | 2013-08-15 |
20130210864 | N-BENZYL HETEROCYCLIC CARBOXAMIDES - The present invention relates to N-benzyl heterocyclic carboxamides derivatives or their thiocarboxamides derivatives, their process of preparation, their use as fungicide, particularly in the form of compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions. | 2013-08-15 |
20130210865 | SORAFENIB DIMETHYL SULPHOXIDE SOLVATE - The present invention provides dimethyl sulphoxide solvate of 4-(4-{3-[4-chloro-3-(trifluoromethyl)phenyl]ureido}phenoxy)-N | 2013-08-15 |
20130210866 | METHODS FOR TREATING AN IMPAIRMENT IN GAIT AND/OR BALANCE IN PATIENTS WITH MULTIPLE SCLEROSIS USING AN AMINOPYRIDINE - Disclosed herein is use of one or more aminopyridines in methods and compositions for treatment of impairments in gait or balance in patients with multiple sclerosis. | 2013-08-15 |
20130210868 | STABLE TOPICAL COMPOSITIONS FOR 1,2,4-THIADIAZOLE DERIVATIVES - The present application provides a stable topical composition comprising a compound of 1,2,4-thiadiazole derivatives and the related thiourea derivatives. The stable topical composition may be present in various forms, including aqueous gel, cream, and emulsion. The stable topical composition may be stored at refrigerated or ambient condition for a reasonable shelf-life. The present application also provides a method of treating dermatologic disorders mediated by a melanocortin receptor using the stable topical composition. The stable composition may be delivered using a single chamber or dual chamber device. A method of preparing and delivering the stable composition is also provided. | 2013-08-15 |
20130210869 | METHOD OF INCREASING THE EXTENT OF ABSORPTION OF TIZANIDINE - An article and method for increasing the extent of tizanidine absorption in a patient receiving tizanidine therapy. Tizanidine may be administered in the form of an immediate release tablet composition at or around the time food is consumed. The composition may be packaged in a container for distribution. | 2013-08-15 |
20130210870 | DESFERRITHIOCIN POLYETHER ANALOGUES - A relatively non-toxic desazadesferrithiocin analog having the formula: | 2013-08-15 |
20130210871 | Clothianidin, Metofluthrin, and Piperonyl Butoxide Mixture for Bed Bug Control - The invention relates to a mixture comprising clothianidin, metofluthrin, and piperonyl butoxide which provides superior insect knockdown and mortality rates, and is especially effective against bed bugs. This mixture of actives may be formulated with adjuvants, such as solvents, anti-caking agents, stabilizers, defoamers, slip agents, humectants, dispersants, wetting agents, thickening agents, emulsifiers, and/or preservatives which increase the activity of the mixture. Mixtures of the present invention have long lasting residual control. | 2013-08-15 |
20130210872 | COMBINATION THERAPY USING RILUZOLE TO ENHANCE TUMOR SENSITIVITY TO IONIZING RADIATION - Disclosed is a method of treating a tumor in a patient, comprising (a) administering riluzole in an amount effective to sensitize the tumor cells to ionizing radiation, and (b) irradiating the tumor cells with ionizing radiation in a dose effective to reduce tumor cell growth. The method can further comprise administering an effective amount of one or more additional therapeutic agents. | 2013-08-15 |
20130210873 | WOOD PRESERVATIVE FORMULATIONS COMPRISING ISOTHIAZOLONES WHICH PROVIDE PROTECTION AGAINST SURFACE STAINING - The present invention provides a wood preservative formulation comprising an isothiazolone, an organic fungicidal timber decay preservative and an unsaturated carboxylic or sulphonic acid, salt or precursor thereof. The formulations of the invention are surprisingly effective at protecting wood and other cellulosic substrates, in particular at providing prolonged protection against in-service surface staining. The invention also provides methods for treating wood and other cellulosic substrates with said formulations. | 2013-08-15 |
20130210874 | DUAL-ACTING ANTIHYPERTENSIVE AGENTS - In one aspect, the invention relates to compounds having the formula: | 2013-08-15 |