20th week of 2012 patent applcation highlights part 52 |
Patent application number | Title | Published |
20120122809 | ANTIBACTERIAL AMINOGLYCOSIDE ANALOGS - Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): | 2012-05-17 |
20120122810 | Fused Pentacyclic Polyethers - Disclosed are polycyclic polyether compounds of formula I and pharmaceutical compositions comprising such compounds. | 2012-05-17 |
20120122811 | BICYCLIC NUCLEOSIDES AND NUCLEOTIDES AS THERAPEUTIC AGENTS - The present disclosure relates to the use and methods of manufacture of bicyclic nucleosides and nucleotides for the treatment and prevention of infectious and proliferative diseases, including microbial infections and cancer. | 2012-05-17 |
20120122812 | ANTI-AGING AGENT - The invention relates to chemical and pharmaceutical industry, in particular, to the medicinal products and medications in the form of intra-articular and intradermal solutions and gels, and can be applied in Orthopedics, Traumatology, Arthrology, Reumatology and Vertebrology as an agent for protection of the cartilages and restoration of fluid balance in the synovial cavity and also in Dermatology, Medical Cosmetology and Plastic Surgery to delay skin ageing. | 2012-05-17 |
20120122813 | COMPOSITION CONTAINING OLIGOSACCHARIDES FOR THE TREATMENT/PREVENTION OF INFECTIONS - The present invention relates to oligosaccharide mixtures and their use in the treatment and/or prevention of infections, and in particular, for reducing the severity of childhood infection or in the treatment and/or prevention of childhood infection. | 2012-05-17 |
20120122814 | Composition for Prevention or Treatment of Hypertrophic Scars or Keloids - The present invention relates to a composition for preventing or treating hypertrophic scar or keloid, comprising as an active ingredient a compound represented by the following general formula I: | 2012-05-17 |
20120122815 | Composition for Treating Dry Eye and Related Methods of Manufacture and Methods of Use - The present invention is directed to a composition for treating dry eye comprising, in one embodiment, carboxymethylcellulose and a polyol. Such compositions have been found to alleviate the symptoms of dry eye and remain in the eye for a long period of time. | 2012-05-17 |
20120122816 | COMPOSITIONS AND METHODS FOR ORGAN PRESERVATION - The invention relates to reducing, preventing or reversing organ damage, reducing and/or preventing stem cell damage and/or death, enhancing organ preservation and/or survival, or enhancing stem cell preservation and/or survival comprising administering a compound of formula A, a compound of any one of formulae 1-49 or I-III, a lipoxin compound, an oxylipin compound, or a combination of aspirin and an omega-3 fatty acid. | 2012-05-17 |
20120122817 | HETEROCYCLIC UREA DERIVATIVES AND METHODS OF USE THEREOF - Compounds of formula (IA) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described. | 2012-05-17 |
20120122818 | LUNG-TARGETED DRUGS - Methods and compositions are provided for treating lung diseases, including but not limited to infections and small cell and non-small cell lung cancer, by conjugating a drug of interest to glycerol ethers or glycerol phosphate ethers. | 2012-05-17 |
20120122819 | GUANINE RIBOSWITCH BINDING COMPOUNDS AND THEIR USE AS ANTIBIOTICS - The present invention includes novel compounds and pharmaceutically acceptable formulations of said compounds which exhibit antibiotic activity against microorganisms bearing a guanine riboswitch that controls the expression of the guaA gene, including organisms which are resistant to certain antibiotic families, and which are useful as antibacterial agents for treatment or prophylaxis of bacterial infections in animals or in humans, in particular but not limited to infections of the mammary gland, or their use as antiseptics, agents for sterilization or disinfection. | 2012-05-17 |
20120122820 | PRODRUGS AND THE USE THEREOF - The present application relates to prodrug derivatives of 2-amino-6-({[2-(4-chlorophenyl)-1,3-thiazol-4-yl]methyl}thio)-4-[4-(2-hydroxyethoxy)phenyl]pyridine-3,5-dicarbonitrile, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially of cardiovascular disorders. | 2012-05-17 |
20120122821 | STEROID-CONTAINING SUSTAINED RELEASE INTRAOCULAR IMPLANTS AND RELATED METHODS - Biocompatible intraocular implants include a steroid and an auxiliary agent, where the auxiliary agent is present in an amount sufficient to lessen the severity of at least one side effect compared to the use of an otherwise identical implant lacking said auxiliary agent. The steroid and the auxiliary agent may be present on the same intraocular implant or on different implants. The steroid and auxiliary agent may be associated with a biodegradable polymer matrix, such as a matrix of a two biodegradable polymers. Or, the steroid may be associated with a polymeric coating having one or more openings effective to permit the steroid to be released into an external environment. The implants containing the steroid and an auxiliary agent may be placed in an eye to treat one or more ocular conditions while reducing the side effects otherwise accompanying steroid use. | 2012-05-17 |
20120122822 | COMPOSITIONS FOR REDUCING BETA-AMYLOID-INDUCED NEUROTOXICITY COMPRISING BETA-SECRETASE INHIBITOR - Disclosed are a composition for reducing beta amyloid-induced neurotoxicity by inhibiting β-secretase activity, comprising a dibenzofuran derivative, and a method for preparing the same. Further disclosed is that the combination of the dibenzofuran derivative with a γ-secretase inhibitor or an anti-inflammatory agent shows higher activity with respect to reducing beta amyloid-induced neurotoxicity. | 2012-05-17 |
20120122823 | AQUEOUS DRUG DELIVERY SYSTEM - Novel water stable pharmaceutical compositions, their liquid form oral pharmaceutical compositions and kits thereof, rehydration beverages containing these water stable pharmaceutical compositions methods of manufacture and methods of use thereof are disclosed. The novel aqueous delivery systems are useful, inter alia, as alternative pharmaceutical dosing agents to tablets, capsules and other forms of delivering medication to a mammalian host in need thereof. | 2012-05-17 |
20120122824 | Reduction of Side Effects From Aromatase Inhibitors Used for Treating Breast Cancer - The present invention is directed generally to pharmaceutical compositions, methods, and kits for improving side effects associated with aromatase inhibitor treatment in a subject diagnosed with breast cancer. More specifically, the present invention provides compositions, methods, and kits comprising an aromatase inhibitor and an androgenic agent. | 2012-05-17 |
20120122825 | USE OF PICOPLATIN TO TREAT PROSTATE CANCER - The invention provides a method of treatment of metastatic hormone-refractory prostate cancer involving substantially as concurrent administration of picoplatin and docetaxel. Prednisone may also be administered. Dosages and dosing regimens are provided. | 2012-05-17 |
20120122826 | NOVEL QUINUCLIDINE DERIVATIVES AND MEDICINAL COMPOSITIONS CONTAINING THE SAME - The invention provides 3-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane bromide in combination with a steroid, and methods of using it for treatment of respiratory disorders. | 2012-05-17 |
20120122827 | Novel derivatives of cholest-4-en-3-one oxime, pharmaceutical compositions containing them and preparation method - The object of the invention is the use as a drug of a compound fitting formula I | 2012-05-17 |
20120122828 | Method for on-demand contraception - The invention relates to a method for on-demand contraception, which method comprises administering a progestogen agent or progesterone receptor modulator, such as 17a-acetoxy-11b-[4-N,N-dimethylamino-phenyl)-19-norpregna-4,9-diene-3,20-dione (ulipristal acetate) in a woman, within 72 hours before an intercourse or within 120 hours after the intercourse. | 2012-05-17 |
20120122829 | PHARMACEUTICAL COMPOSITION FOR TRANSDERMAL OR TRANSMUCOUS ADMINISTRATION - The present invention relates to a novel pharmaceutical composition for transdermal or transmucous administration of at least one active substance, and comprising especially a fatty acid as a percutaneous absorption promoter, at least one alcoholic vehicle and also a stabilizer capable of stabilizing the fatty acid in the said pharmaceutical composition. | 2012-05-17 |
20120122830 | PREGNENOLONE SULFATE FOR THE TREATMENT OF NEUROLOGIC DISORDERS - The disclosure relates, in part, to methods of using pregnenolone sulfate (PREGS) to protect against the neurotoxicity of the β-amyloid peptide Aβ | 2012-05-17 |
20120122831 | METHOD AND DEVICE FOR RAPID DETECTION OF BACTERIAL ANTIBIOTIC RESISTANCE/SUSCEPTIBILITY - Described herein is a method and a device for expediting delivery of an agent to a damaged bacterial cell. In one embodiment, the methods and devices are useful for screening candidate antibiotics. In another embodiment, the methods and devices described herein are used to determine susceptibility of bacteria to an antibiotic. The methods also provide a method for determining an appropriate antibiotic to treat an individual having a bacterial infection. | 2012-05-17 |
20120122832 | METHOD OF MAKING CEFQUINOME PARTICLES - Disclosed is a process for the production of particles of a cefquinome acid addition salt, preferably cefquinome sulfate particles, by precipitation of cefquinome acid addition salt, preferably the sulfate, from a cefquinome betaine solution, wherein acid, preferably sulfuric acid, is added to the betaine solution. According to the invention the acid, preferably sulfuric acid, is added quickly in a single shot, in a molar excess of 40% to less than 100%. As a result, particles are formed that comprise agglomerates of microscale primary crystalline particles. This enables providing particles of cefquinome acid addition salt, preferably cefquinome sulfate, in particle sizes commensurate with micronized material, but with improved stability. | 2012-05-17 |
20120122833 | DEUTERIUM-ENRICHED MEROPENEM - The present application describes deuterium-enriched meropenem, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 2012-05-17 |
20120122834 | SMALL MOLECULE CD4 MIMETICS AND USES THEREOF - The invention provides for compounds of formula I: wherein Z is absent or (CR | 2012-05-17 |
20120122835 | Poly (ADP-Ribose) Polymerase (PARP) Inhibitors - Disclosed are compounds of the following formula: | 2012-05-17 |
20120122836 | POLYMORPHIC FORM OF 1-(4--2-ETHYL-BENZYL)-AZETIDINE-3-CARBOXYLIC - This invention relates to a novel crystalline form (Form A) of 1-(4-{1-[(E)-4-cyclohexyl-3-trifluoromethyl-benzyloxyimino]-ethyl}-2-ethyl-benzyl)-azetidine-3-carboxylic acid (Compound I), to pharmaceutical compositions comprising this crystalline form, to processes for forming it and to its use in medical treatment. | 2012-05-17 |
20120122837 | INHIBITORS OF FATTY ACID BINDING PROTEIN - The present invention relates to novel heterocyclic compounds as Fatty Acid Binding Protein (“FABP”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. | 2012-05-17 |
20120122838 | HETEROCYCLIC COMPOUNDS AND USES THEREOF - Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein. | 2012-05-17 |
20120122839 | NOVEL PYRROLIDIN-2-ONES - The present invention provides compounds of formula (I) or (Ia) which are ligands binding to the HDM2 protein, inducing apoptosis and inhibiting proliferation, and having therapeutic utility in cancer therapy and prevention. | 2012-05-17 |
20120122840 | COMPOUNDS AND THERAPEUTIC USES THEREOF - The invention relates to compounds, pharmaceutical compositions, and uses thereof, including therapeutic uses thereof, such as methods useful for treating cancer. | 2012-05-17 |
20120122841 | Biological Markers Predictive Of Anti-Cancer Response To Insulin-like Growth Factor-1 Receptor Kinase Inhibitors - The present invention provides diagnostic and prognostic methods for predicting the effectiveness of treatment of a cancer patient with an IGF-1R kinase inhibitor. Methods are provided for predicting the sensitivity of tumor cell growth to inhibition by an IGF-1R kinase inhibitor, comprising assessing whether the tumor cell has undergone an epithelial to mesenchymal transition (EMT), by determining the expression level of epithelial and/or mesenchymal biomarkers, wherein tumor cells that have undergone an EMT are substantially less sensitive to inhibition by IGF-1R kinase inhibitors. Improved methods for treating cancer patients with IGF-1R kinase inhibitors that incorporate the above methodology are also provided. | 2012-05-17 |
20120122842 | NAMPT AND ROCK INHIBITORS - Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed. Disclosed are compounds which inhibit the activity of ROCK, compositions containing the compounds and methods of treating diseases during which ROCK is expressed. | 2012-05-17 |
20120122843 | Compounds and Their Use for Treatment of Amyloid Beta-Related Diseases - The present invention relates to novel compounds of formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising said compounds, processes for making said compounds, and their use as medicaments for treatment and/or prevention of Aβ-related diseases. | 2012-05-17 |
20120122844 | METHOD OF TREATING CONTRAST-INDUCED NEPHROPATHY - The present invention provides the use of a neutral endopeptidase inhibitor, in the manufacture of a medicament for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The invention also relates to the use of a compound of Formula I: | 2012-05-17 |
20120122845 | METHOD FOR THE PRODUCTION OF BIOADHESIVE COMPACT MATRICES - A method for the preparation of a bioadhesive compact matrix, which comprises the preparation of a uniform mixture of powders comprising one alkylcellulose or one hydroxy alkylcellulose and a non-water-soluble, water-swellable cross-linked polycarboxylic polymer; the preparation of compressed units starting from such powder mixture by direct compression and finally the heating of the compressed units thus obtained to a temperature in the range of 80-250° C. for a time of 1-60 minutes; the powder mixture can also comprise at least one active substance and the compressed units thus obtained are characterized by a prolonged release, and have a release kinetics of the active substance substantially of zero order in an aqueous solution at pH 4-8. | 2012-05-17 |
20120122846 | FURO[3,2-d]PYRIMIDINE COMPOUNDS - The present invention is directed to novel compounds of Formula (I) | 2012-05-17 |
20120122847 | AURORA KINASE MODULATORS AND METHOD OF USE - The present invention relates to chemical compounds having a general formula I | 2012-05-17 |
20120122848 | (+)-3-HYDROXYMORPHINAN DERIVATIVES AS NEUROPROTECTANTS - A novel (+)-3-hydroxymorphinan derivatives and a pharmaceutical composition comprising the same as an active ingredient, which are useful for preventing or treating a neurodegenerative disease, are provided. | 2012-05-17 |
20120122849 | PKM2 MODULATORS FOR USE IN THE TREATMENT OF CANCER - Compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are pharmaceutical compositions comprising the compounds, and methods of using the compounds in the treatment of cancer. | 2012-05-17 |
20120122850 | BIPHENYL COMPOUNDS USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS - The invention provides compounds of formula I: | 2012-05-17 |
20120122851 | PHARMACEUTICAL PREPARATION AND DELIVERY SYSTEM - The present invention relates to unique delivery systems and the use of an imidazobenzodiazepine derivative, such as flumazenil either alone or in combination with other receptor antagonists in the treatment of disease or medical disorders. | 2012-05-17 |
20120122852 | TRICYCLIC N-HETEROARYL-CARBOXAMIDE DERIVATIVES CONTAINING A BENZIMIDAZOLE UNIT, METHOD FOR PREPARING SAME AND THEIR THERAPEUTIC USE - The invention concerns tricyclic N-heteroaryl-carboxamide derivatives containing a benzimidazole unit of general formula (I): | 2012-05-17 |
20120122853 | ANNELATED N-HETEROCYCLIC SULFONAMIDES WITH OXADIAZOLONE HEADGROUP, PROCESSES FOR THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS - Annelated N-heterocyclic sulfonamides with oxadiazolone headgroup, processes for their preparation and their use as pharmaceuticals The invention relates to annelated N-heterocyclic sulfonamides with oxadiazolone headgroup and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARalpha agonist activity. What is described are compounds of the formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system. | 2012-05-17 |
20120122854 | Carbocyclic Fused Cyclic Amines - The invention is concerned with novel carbocyclyl fused cyclic amines of formula (I) | 2012-05-17 |
20120122855 | BENZOXAZINES, BENZOTHIAZINES, AND RELATED COMPOUNDS HAVING NOS INHIBITORY ACTIVITY - The present invention features benzoxazines, benzothiazines, and related compounds that inhibit nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing various medical conditions. | 2012-05-17 |
20120122856 | Liquid Termiticide Compositions of Pyrethroids and Neonicitinoids - The present invention relates to liquid termiticide compositions comprising a pyrethroid and a neonicotinoid selected from the group consisting of imidacloprid, nithiazine, thiamethoxam, dinotefuran, nitenpyram, thiacloprid and clothianadin, these compositions result in an increase in termite mortality at low application rates and a continuous chemical bather of a termiticide in soil surrounding and beneath a structure in a locus where termites are suspected or known to exist. | 2012-05-17 |
20120122857 | HETEROBICYCLIC CARBOXAMIDES AS INHIBITORS FOR KINASES - The invention relates to novel compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula (I) and to the use of a compound of formula (I) for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in particular tumour diseases. | 2012-05-17 |
20120122858 | LACTAM COMPOUNDS AND THEIR USE AS PHARMACEUTICALS - The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess. | 2012-05-17 |
20120122859 | METHODS OF USING DIAMINOPYRIMIDINE AS P2X3 AND P2X2/3 RECEPTOR MODULATORS FOR TREATMENT OF RESPIRATORY AND GASTROINTESTINAL DISEASES - Methods for treating respiratory and gastrointestinal diseases mediated by a P2X | 2012-05-17 |
20120122860 | SOLID FORMS OF SULFONAMIDES AND AMINO ACIDS - Solid forms of phenyl sulfonamide compounds of formula (I) active on protein kinases, including Raf protein kinases, are described, as well as methods of using such solid forms to treat diseases and conditions associated with activity of protein kinases, e.g. Raf protein kinases, including pain, polycystic kidney disease, melanoma and colorectal cancer. | 2012-05-17 |
20120122861 | BICYCLIC AMIDE DERIVATIVES FOR ENHANCING GLUTAMATERGIC SYNAPTIC RESPONSES - This invention relates to compounds, pharmaceutical compositions and methods for use in the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for basic and higher order behaviors. These brain networks, which are involved in cognitive abilities related to memory impairment, such as is observed in a variety of dementias, in imbalances in neuronal activity between different brain regions, as is suggested in disorders such as Parkinson's disease, schizophrenia, sleep apneas, attention deficit hyperactivity disorder and affective or mood disorders, and in disorders wherein a deficiency in neurotrophic factors is implicated, as well as conditions such as stroke-induced central sleep apnea, obstructive sleep apnea, congenital hypoventilation syndrome, among others. In a particular aspect, the invention relates to bicyclic amide compounds useful for treatment of such conditions, and methods of using these compounds for such treatment. | 2012-05-17 |
20120122862 | ARGININE DERIVATIVES WITH NP-I ANTAGONISTIC ACTIVITY - The present invention is a compound of formula (I) or formula (II) which are suitable as NP-1 antagonists. | 2012-05-17 |
20120122863 | Quinazolinedione Chymase Inhibitors - Disclosed are small molecule inhibitors which are useful in treating various diseases and conditions involving Chymase. | 2012-05-17 |
20120122864 | INHIBITORS OF HCV NS5A - Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C. | 2012-05-17 |
20120122865 | ISOINDOLINE COMPOUNDS AND METHODS OF THEIR USE - Provided herein are isoindoline compounds, pharmaceutical compositions comprising one or more of such compounds, and methods of their use for treating, preventing, or managing various diseases. | 2012-05-17 |
20120122866 | TOPICAL PHARMACEUTICAL COMPOSITION INCLUDING REL-N-[6-[(2R,6S)-2,6-DIMETHYL-4-MORPHOLINYL]-3-PYRIDINYL]-2-METHYL-4'-(T- RIFLUOROMETHOXY)-[1,1'-BIPHENYL]-3-CARBOXAMIDE - The present invention relates to pharmaceutical compositions of 2-Methyl-4′-trifluoromethoxy-biphenyl-3-carboxylic acid [6-(cis-2,6-dimethyl-morpholin-4-yl)-pyridin-3-yl]-amide, to the use of such compositions in therapeutic applications and to methods for manufacturing such compositions. | 2012-05-17 |
20120122867 | NOVEL PYRIMIDINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF CANCER AND FURTHER DISEASES - The invention concerns compounds of Formula (I): wherein L | 2012-05-17 |
20120122868 | APAF-1 INHIBITOR COMPOUNDS - Derivatives of 2,5-piperazinedione of formula (I) are apoptotic peptidase activating factor 1 (Apaf-1) inhibitors, therefore they are useful as active pharmaceutical ingredients for the prophylaxis and/or treatment of a pathological and/or physiological condition associated with an increase of apoptosis. | 2012-05-17 |
20120122869 | TRIZAOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY - The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound. | 2012-05-17 |
20120122870 | Treatment Of Ischemia-Reperfusion Injury - Ischemia-reperfusion injury remains a primary cause of morbidity and mortality in individuals who experience disruption of normal blood flow to one or more major organs. For example, there are no clinically proven strategies that prevent acute renal failure following cardiac surgery. The present invention provides a variety of methods for the treatment or prevention of ischemia-reperfusion injury. In one aspect of the invention, a method for treating or preventing ischemia-reperfusion injury includes administering to a subject an effective amount of a sphingosine kinase inhibitor. Sphingosine kinase inhibitors are very effective in the protection against IR-induced acute renal failure and liver failure. Moreover, the effects occur very early after administration, requiring only a very short time of treatment. Toxicology studies with sphingosine kinase inhibitors demonstrate that they have low toxicity, even in long-term treatment. | 2012-05-17 |
20120122871 | Oligomer-Containing Substituted Aromatic Triazine Compounds - The invention relates to (among other things) oligomer-containing substituted aromatic triazine compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits one or more advantages over corresponding compounds lacking the oligomer. | 2012-05-17 |
20120122872 | Treatment or Prevention of Fungal Infections with PDK1 Inhibitors - Provided are methods of treating or preventing a fungal infection in a subject. The methods comprise identifying a subject with or at risk of developing a fungal infection and administering to the subject a therapeutically effective amount of an inhibitor or a fungal phosphoinositide-dependent kinase 1 (PDK-1) or a homolog thereof. Inhibition of the fungal PDK-1 or homolog thereof results in the treatment or prevention of a fungal infection in the subject. Also provided are compositions comprising an inhibitor of a fungal phosphoinositide-dependent kinase 1 (PDK-1) or a homolog thereof, and a pharmaceutically acceptable carrier. | 2012-05-17 |
20120122873 | AMINO DERIVATIVES OF DIHYDRO-1,3,5-TRIAZINE USED IN THE TREATMENT OF ISCHEMIA AND/OR REPERFUSION RELATED DISEASES - The invention relates to amino derivatives of dihydro-1,3,5-triazine, used for the treatment and/or prevention of diseases induced by ischemia and/or reperfusion, notably cardiac and renal complications. | 2012-05-17 |
20120122874 | COMBINATION OF A SEDATIVE AND A NEUROTRANSMITTER MODULATOR, AND METHODS FOR TREATING DEPRESSION - One aspect of the present invention relates to pharmaceutical compositions containing two or more active agents that when taken together can be used to treat, e.g., insomnia and/or depression. The first component of the pharmaceutical composition is a GABA receptor modulating compound. The second component of the pharmaceutical composition is a serotonin reuptake inhibitor, a norepinephrine reuptake inhibitor, a 5-HT | 2012-05-17 |
20120122875 | Salts of Methyl (R)-7-[3-Amino-4-(2,4,5-Trifluoro-Phenyl)-Butyryl]-3-Trifluoromethyl-5,6,- 7,8-Tetrahydro-Imidazo[1,5-A]Pyrazine-1-Carboxylate - The pharmaceutically acceptable salts of methyl (R)-7-[3-amino-4-(2,4,5-trifluoro-phenyl)-butyryl]-3-trifluoromethyl-5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine- | 2012-05-17 |
20120122876 | PYRIDOPYRAZINONES DERIVATIVES INSULIN SECRETION STIMULATORS, METHODS FOR OBTAINING THEM AND USE THEREOF FOR THE TREATMENT OF DIABETES - The present invention relates to pyridopyrazinone derivatives of formula (I), wherein X, Y, Z1 W, A and R1 are as defined in claim | 2012-05-17 |
20120122877 | Compositions for Treating Bacterial Infections - The present invention is antibiotic compositions having the ability to disrupt a MazEF complex in | 2012-05-17 |
20120122878 | COMBINATION PRODUCTS - The invention concerns the combinations of an mGluR modulator, e.g. an mGluR5 modulator and at least one of L-dopa, a dopamine modulator, e.g. a dopamine agonist, a dopa decarboxylase inhibitor or a catechol-O-methyl transferase inhibitor. | 2012-05-17 |
20120122879 | COMPOUNDS USEFUL AS PROTEIN KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of protein 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. | 2012-05-17 |
20120122880 | THIOXANTHENE DERIVATIVES FOR THE TREATMENT OF INFECTIOUS DISEASES - The claimed subject matter is directed to certain thioxanthene derivatives and phenothiazine derivatives suitable for use as anti-infective agents, in particular, for the treatment of infectious diseases. The claimed subject matter furthermore relates to compositions including said anti-infective agents. | 2012-05-17 |
20120122881 | FORMULATION OF QUINAZOLINE BASED EGFR INHIBITORS CONTAINING A ZINC BINDING MOIETY - The present invention relates to a composition comprising an inclusion complex of a cyclodextrin and quinazoline containing zinc-binding moiety based derivatives. The cyclodextrin is preferable a β-cyclodextrin or a derivative thereof. The quinazolines have enhanced and unexpected properties as inhibitors of epidermal growth factor receptor tyrosine kinase (EGFR-TK) and their use in the treatment of EGFR-TK related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors. | 2012-05-17 |
20120122882 | Substituted Pyrrolo-Pyrimidine Derivatives, Process for Their Preparation and Their Use as Kinase Inhibitors - Substituted pyrrolo-pyrimidine derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a dysregulated protein kinase activity, like cancer. | 2012-05-17 |
20120122883 | NEW SALTS - The present invention relates to new crystalline salt forms of flibanserine which have valuable pharmacological properties, to a process for their manufacture, to pharmaceutical formulations containing them and to their use as medicament. | 2012-05-17 |
20120122884 | COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE - The present invention relates to pyrazine and pyridine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. | 2012-05-17 |
20120122885 | PYRUVATE KINASE M2 MODULATORS, THERAPEUTIC COMPOSITIONS AND RELATED METHODS OF USE - Compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer. | 2012-05-17 |
20120122886 | THIADIAZOLE-SUBSTITUTED ARYLAMIDES AS P2X3 AND P2X2/3 ANTAGONISTS - Compounds of the formula I: | 2012-05-17 |
20120122887 | SOLID STATE FORMS OF A POTENT HCV INHIBITOR - This invention relates to novel sodium salt forms of the following Compound (1), and methods for the preparation thereof, pharmaceutical compositions thereof, and their use in the treatment of Hepatitis C Viral (HCV) infection: | 2012-05-17 |
20120122888 | Potassium Channel Modulators - Disclosed herein are KCNQ potassium channels modulators of formula (I) | 2012-05-17 |
20120122889 | SMALL MOLECULE INHIBITORS OF NECROPTOSIS - The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-α) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I)-(VIII) and by Compounds (I)-(I), (13)-(26), (27)-(33), (48)-(57), and (58)-(70). These necrostatins are shown to inhibit TNF-α induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring necrostatins. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role. | 2012-05-17 |
20120122890 | Potassium Channel Modulators - Disclosed herein are KCNQ potassium channels modulators of formula (I) | 2012-05-17 |
20120122891 | GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS AND METHODS RELATING THERETO - GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: | 2012-05-17 |
20120122892 | CHEMICAL COMPOUNDS - This invention relates to novel compounds having the formula (I): | 2012-05-17 |
20120122893 | METHODS OF TREATING CANCER - Described are methods and compositions for treating epithelial tumors with a folate-vinca conjugate in combination with at least one other chemotherapeutic agent in which the tumors include ovarian, endometrial or non-small cell lung cancer tumors, including platinum-resistant ovarian tumors and platinum-sensitive ovarian tumors. | 2012-05-17 |
20120122894 | INHIBITORS OF BRUTON'S TYROSINE KINASE - Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. | 2012-05-17 |
20120122895 | 5,6-BICYCLIC HETEROARYL-CONTAINING UREA COMPOUNDS AS KINASE INHIBITORS - The present invention provides 5,6-bicyclic heteroaryl-containing urea compounds of Formula I or II and use of the same for treating conditions mediated by protein kinase such as VEGFR2, c-Met, PDGFRβ c-Kit, CSF1R, or EphA2. | 2012-05-17 |
20120122896 | 2,1,3-BENZOXADIAZOL DERIVATIVES FOR THE INHIBITION OF INFLUENZA A AND B VIRUS AND RESPIRATORY SYNCYTIAL VIRUS REPLICATION - A 2,1,3-benzoxadiazole compound as a medicament according to the invention is one of the following compounds: 4-[(4-methoxybenzyl)thio]-7-nitro-2,1,3-benzoxadiazole, 2-[(7-nitro-2,1,3-benzoxadiazol-4-yl)thio]ethyl 4-methoxybenzene-1-sulfonate, 4-[(4-methylphenyl)thio]-7-nitro-2,1,3-benzoxadiazole, 4-[(2,4-dichlorophenyl)thio]-7-nitro-2,1,3-benzoxadiazole, 2-[(7-nitro-2,1,3-benzoxadiazol-4-yl)thio]ethan-1-ol, 4-[(4-methylbenzyl)thio]-7-nitro-2,1,3-benzoxadiazole, 4-[(4-fluorophenyl)thio]-7-nitro-2,1,3-benzoxadiazole, 4-[(3-chlorophenyl)-thio]-7-nitro-2,1,3-benzoxadiazole, 2-[(7-nitro-2,1,3-benzoxadiazol-4-yl)thio]ethyl-4-methoxy-benzoate, 5-[4-(tert-butyl)-1,3-thiazol-2-yl]-2,1,3-benzoxadiazole, N-benzyl-4-nitro-2,1,3-benzoxadiazol-5-amine, 4-nitro-7-(phenylmethylsulfanyl)-2,1,3-benzoxadiazole, 4-nitro-7-(phenylmethylsulfonyl)-2,1,3-benzoxadiazole, 2-(hydroxymethyl)-5-[6-[(4-nitro-2,1,3-benzoxadiazol-7-yl)sulfanyl]purin-9-yl]oxolane-3,4-diole, or 2-[2-amino-6-[(4-nitro-2,1,3-benzoxadiazol-7-yl)sulfanyl]purin-9-yl]-5-(hydroxymethyl)oxolane-3,4-diol; or a physiologically tolerable salt, solvate, or physiologically functional derivative thereof. Said compounds are particularly advantageous for treating and/or preventing influenza type A and/or influenza type B infections in humans, mammals and/or birds, and for treating and/or preventing respiratory syncytial virus infections in humans, mammals and/or birds. | 2012-05-17 |
20120122897 | METHODS OF TREATING PATIENTS SUFFERING FROM MOVEMENT DISORDERS - Methods of treating movement disorders by administering an effective amount of one or more adenosine A | 2012-05-17 |
20120122898 | SOLID FORMS OF 3-(4-(AMINOMETHYL)-1-(5-METHYL-7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL)PIPERIDINE- -4-CARBOXAMIDO)PHENYL DIMETHYLCARBAMATE - Solid forms of 3-(4-(aminomethyl)-1-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamido)phenyl dimethylcarbamate and salts thereof are disclosed. Methods of its use to treat diseases and disorders of the eye are also disclosed. | 2012-05-17 |
20120122899 | PIPERIDINONE CARBOXAMIDE AZAINDANE CGRP RECEPTOR ANTAGONISTS - The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 CGRP is involved. | 2012-05-17 |
20120122900 | PIPERIDINONE CARBOXAMIDE AZAINDANE CGRP RECEPTOR ANTAGONISTS - The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 CGRP is involved. | 2012-05-17 |
20120122901 | PYRROLO[2,3-D]PYRIMIDINE COMPOUNDS - Described herein is pyrrolo{2,3-d}pyrimidine compounds, their use as Janus Kinase (JAK) inhibitors, pharmaceutical compositions containing this compounds, and methods for the preparation of these compounds. | 2012-05-17 |
20120122902 | PYRIMIDINE DERIVATIVE, PREPARATION METHOD AND USE THEREOF - A pyrimidine derivative and the preparation method and usethereof. The said pyrimidine derivative is a diaryl pyrimidine derivative or a diaryl benzo pyrimidine derivative which has the structure shown as the Formula I and IV. | 2012-05-17 |
20120122903 | 1-H-QUINAZOLINE-2, 4-DIONES FOR USE IN THE TREATMENT OF NEURONAL CEROID LIPOFUSCINOSIS - The invention concerns the use of competitive AMPA receptor antagonists for the treatment, prevention or delay of progression of neuronal ceroid lipofuscinosis. | 2012-05-17 |
20120122904 | SOLID FORMS OF (S)-2-AMINO-3-(4-(2-AMINO-6-((R)-1-(4-CHLORO-2-(3-METHYL-1H-PYRAZOL-1-YL)- PHENYL)-2,2,2-TRIFLUOROETHOXY)PYRIMIDIN-4-YL)PHENYL)PROPANOIC ACID - Solid forms of (S)-2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoic acid and salts thereof are disclosed. Pharmaceutical dosage forms and methods of their use are also disclosed. | 2012-05-17 |
20120122905 | NOVEL GPR 119 AGONISTS - The present invention relates to novel GPR 119 agonists of the general Formula (I), their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, stereoisomers, and polymorphs. The invention also relates to processes for the preparation of the compounds of the invention, pharmaceutical compositions containing the compounds and to methods for treating one or both of diabetes and obesity using the compounds of the invention. The present invention is directed to G-protein coupled receptor (GPCR) agonists that are useful for the treatment of obesity, diabetes and related metabolic disorders. | 2012-05-17 |
20120122906 | NOVEL SULFONAMIDE DERIVATIVE AND PHARMACEUTICAL PRODUCT CONTAINING SAME - Disclosed is a novel compound which has both angiotensin II receptor antagonist activity and PPARγ activating activity, and is useful as a prophylactic and/or therapeutic agent for hypertension, heart diseases, angina pectoris, cerebrovascular disorders, cerebral circulatory disorders, ischemic peripheral circulatory disorders, kidney diseases, arteriosclerosis, inflammatory diseases, type 2 diabetes, diabetic complication, insulin resistant syndrome, syndrome X, metabolic syndrome and hyperinsulinemia. Also disclosed is a pharmaceutical composition which contains the novel compound. Specifically disclosed are: a sulfonamide derivative represented by general formula (I), a salt thereof, or a solvate of the derivative or salt; and a pharmaceutical composition which contains the sulfonamide derivative, a salt thereof, or a solvate of the derivative or salt. (In the formula, R | 2012-05-17 |
20120122907 | Novel Pyrazole Derivatives and their use as Positive Allosteric Modulators of Metabotropic Glutamate Receptors - The present invention relates to novel compounds of Formula (I), wherein M, P, X | 2012-05-17 |
20120122908 | Novel C-4 Substituted Retinoids - C-4 substituted retinoic acid analogs, synthesis methods of C-4 substituted retinoic acid analogs and methods of using C-4 substituted retinoic acid analogs to treat various cancers and dermatological diseases and conditions. The C-4 substituted retinoic acid analogs include C-4 all-trans retinoic acid (ATRA) and 13-cis retinoic acid (13-CRA) analogs. The C-4 substituted retinoic acid analogs inhibit all-trans retinoic acid (ATRA) 4-hydroxylase activity, thereby inhibiting the catabolism of ATRA. The C-4 substituted retinoic acid analogs also have ATRA-mimetic activity. The preferred substitutions at C-4 are an azole group, a sulfur, oxygen, or nitrogen containing group, a pyridyl group, an ethinyl group, a cyclopropyl-amine group, an ester group, or a cyano group, or forms, together with the C-4 carbon atom, an oxime, an oxirane or aziridine group. | 2012-05-17 |