51st week of 2011 patent applcation highlights part 50 |
Patent application number | Title | Published |
20110312900 | BChE ALBUMIN FUSIONS FOR THE TREATMENT OF COCAINE ABUSE - A method of attenuating a biological effect of cocaine exposure in a primate. Such method includes administering to the primate an amount of a BChE-albumin fusion protein comprising the amino acid substitutions A227S, S315G, A356W, and Y360G, wherein the amount of the fusion protein is effective to cause attenuation of the biological effect of cocaine exposure in the primate. | 2011-12-22 |
20110312901 | METHODS OF INHIBITING CELL DEATH OR INFLAMMATION IN A MAMMAL BY ADMINISTERING A BCL PROTEIN - In one aspect the present invention provides methods for inhibiting cell death or inflammation in a mammal, wherein the methods each include the step of administering to a mammal a Bcl protein in an amount sufficient to inhibit cell death or inflammation in the mammal. The invention also provides methods for identifying a Bcl protein that inhibits cell death or inflammation when administered to a mammal. | 2011-12-22 |
20110312902 | CYTOPROTECTIVE THEREAPEUTIC AGENTS FOR THE PREVENTION OF REPERFUSION INJURY FOLLOWING ISCHEMIC STROKE - The present invention relates generally to the use of γ-glutamyl antioxidants, particularly γ-glutamyl-cysteine, as cytoprotective agents to prevent reperfusion injury (i.e., hemorrhagic transformation) of the blood-brain barrier during reperfusion following an ischemic stroke. The γ-glutamyl antioxidants can be used alone or used in combination with an agent which inhibits the reverse movement of Na/Ca exchange in the blood-brain barrier such as 2-[2-[4-(4-nitrobenzyloxy)phenyl]ethyl]isothiourea methanesulphonate (KB-R7943). | 2011-12-22 |
20110312903 | FLUORINATION OF ORGANIC COMPOUNDS - Methods for fluorinating organic compounds are described herein. | 2011-12-22 |
20110312904 | COMPOUNDS, COMPOSITIONS AND METHODS FOR REDUCING TOXICITY AND TREATING OR PREVENTING DISEASES - The present invention provides compounds of Formula (I), compositions comprising an effective amount of a compound of Formula (I), optionally with chemotherapeutic drugs such as a tubulin-binding drug, and methods of their use for reducing the toxicity of cytotoxic agents, treating or preventing cancer or a neuropathic disorder, inducing a chemoprotective phase II enzyme, DNA, or protein synthesis, enhancing the immune system, treating inflammation, improving and enhancing general health or well-being, and methods for making compounds of Formula (I). | 2011-12-22 |
20110312905 | STIMULUS-TRIGGERED PRODRUGS - Set forth herein, inter alia, are compositions and methods for treating diseases with prodrugs. Provided herein are prodrug compositions for inhibiting the function of proteins, compositions and methods for treating diseases associated with oxidative compounds, oxidatively-sensitive prodrugs of inhibitors of metalloproteases. and methods of inhibiting metalloproteases using oxidatively-sensitive prodrugs. | 2011-12-22 |
20110312906 | TREATMENT OR REDUCTION OF MENOPAUSAL SYMPTOMS - There is described a method for the treatment or prevention of menopausal symptoms or osteoporosis wherein there is administered to a subject in need of such treatment a therapeutically effective amount of the isotlavone formononetin, or a method for the treatment or prevention of menopausal symptoms wherein there is administered to a subject in need of such treatment a therapeutically effective amount of the isoflavone daidzein, the isotlavone being optionally administered with one or more pharmaceutically acceptable adjuvants, carriers and/or excipients. Therapeutic uses and compositions/foods are also described, comprising daidzein or formononetin optionally in association with one or more pharmaceutically acceptable adjuvants, carriers, food components and/or excipients. | 2011-12-22 |
20110312907 | POLYMORPHISMS PREDICTIVE OF ANTHRACYCLINE- INDUCED CARDIOTOXICITY - Provided are methods, nucleic acids, and arrays for assessing the susceptibility of a subject to the development of cardiotoxicity in response to receiving one or more anthracycline compounds, the method including determining the presence or absence of one or more polymorphisms, wherein the presence or absence of one or more such polymorphisms is indicative of susceptibility to the development of cardiotoxicity. | 2011-12-22 |
20110312908 | SMALL MOLECULE MYRISTATE INHIBITORS OF BCR-ABL AND METHODS OF USE - The present invention provides novel heteroaryl compounds that are linked to an aryl group via an amine linker. Such compounds are useful for the treatment of cancers. | 2011-12-22 |
20110312909 | THERAPEUTIC COMBINATION COMPRISING A CDKS INHIBITOR AND AN ANTINEOPLASTIC AGENT - The present invention provides a therapeutic combination comprising (a) a compound of formula (I) as set forth in the specification and (b) one or more antineoplastic agents selected from the group consisting of alkylating or alkylating-like agents, antimetabolite agents and topoisomerase I inhibitors, wherein the active ingredients are present in each case in free form or in the form of a pharmaceutically acceptable salt or any hydrate thereof. | 2011-12-22 |
20110312910 | PHARMACEUTICAL COMPOSITION BASED ON A HEPATOPROTECTOR AND A PREBIOTIC, AND PRODUCTION AND APPLICATION THEREOF - The invention relates to medicine, hepatology and pharmacology and can be used for producing and using a pharmaceutical composition based on a hepatoprotector and a prebiotic for treating and preventing liver diseases which are caused by lipid-cholesterol exchange and selected from the following group: cholelitiasis mainly with cholesterol stones, alcoholic and non-alcoholic steatohepatitis, biliary cirrhosis, cholesterol imbibition gallbladder and drug-induced and toxic liver damage. The pharmaceutical composition is administered by mouth and contains a hepatoprotector and a prebiotic taken, as an active agent, in therapeutically effective doses. The invention contributes to the liver's functional recovery in a short time and prevents disease recidivation owing to the recovery of cholesterol exchange and intestinal biocenosis as a result of the synergistic interaction of a hepatoprotector and a prebiotic, thereby also preventing hepatoprotector side effects. | 2011-12-22 |
20110312911 | GLUCAGON RECEPTOR ANTAGONIST COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF USE - Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included. | 2011-12-22 |
20110312912 | TREATMENT OF ARTHRITIS AND OTHER MUSCULOSKELETAL DISORDERS WITH CROSSLINKED HYALURONIC ACID - A method of treating a subject having a musculoskeletal disorder includes administering to a subject's articular site in need thereof an effective amount of a hyaluronic acid (HA) composition. In one embodiment, the HA composition includes an HA derivative, wherein carboxyl functionalities of the hyaluronic acid derivative are each independently derivatized to include an N-acylurea or O-acyl isourea, or both N-acylurea and O-acyl isourea. In another embodiment, the HA composition includes a crosslinked HA gel that is prepared by reacting an uncrosslinked HA with a biscarbodiimide in the presence of pH buffer in a range of between about 4 and about 8. The composite can optionally include at least one second bioactive agent other than the HA derivative, such as a steroid. | 2011-12-22 |
20110312913 | METHOD AND PHARMACEUTICAL TO TREAT SPINAL DISCS - Methods for reducing chronic pain caused by a disrupted spinal disc are described. In one method, a solution is injected into the disc. The solution includes chondroitin sulphate, glucosamine HCl, and dextrose. The solution may optionally include dimethyl sulfoxide and/or an anesthetic such as bupivicaine. | 2011-12-22 |
20110312914 | CARBON MONOXIDE REMOVAL AGENT - The present invention provides a carbon monoxide removal agent that can be easily administered to a patient by injection or orally. The carbon monoxide removal agent of the present invention contains, as an active ingredient, an inclusion complex in which a cyclodextrin dimer represented by chemical formula (1) below includes a water-soluble metalloporphyrin. (In the formula, m represents either of number 1 or 2 and n represents any of number 1, 2, or 3.) | 2011-12-22 |
20110312915 | Novel cosmetic compositions - The present invention is concerned with novel cosmetic or pharmaceutical compositions. More particularly, the invention is concerned with novel cosmetic or pharmaceutical compositions for treating or preventing any symptoms caused by negative developments of the physiological homeostasis of healthy skin, as well as for the promotion of hair growth and protection from hair loss. | 2011-12-22 |
20110312916 | NOVEL PRODRUGS OF STEROIDAL CYP17 INHIBITORS/ANTIANDROGENS - Prodrugs of C-17-heterocyclic-steroidal drugs providing improved oral bioavailability and pharmacokinetics are described. The drugs are inhibitors of human CYP 17 enzyme, as well as potent antagonists of both wild type and mutant androgen receptors (AR), and are useful for the treatment of urogenital and/or androgen-related cancers, diseases and/or conditions, such as human prostate cancer, breast cancer, and prostate hyperplasia. The disclosure describes methods of synthesizing and using the prodrugs in cancer therapy. | 2011-12-22 |
20110312917 | CLEANING COMPOSITION FOR TREATING TISSUE FOR TRANSPLANTATION DERIVED FROM HUMAN/ANIMAL - The present invention relates to a cleaning composition for removing cellular components from tissue for transplantation derived from humans and animals. More particularly, the present invention relates to a cleaning composition for treating tissue for transplantation comprising a polyoxyethyleneglycol C | 2011-12-22 |
20110312918 | METHOD FOR IDENTIFYING AGENTS FOR INHIBITING CELL MOTILITY AND INVASIVENESS - The present invention provides a novel mechanistic pathway and methods related to this pathway for the identification of compounds for the treatment of diseases involving cell proliferation, invasion and/or metastasis such as cancer. In particular, the instant invention relates to the phosphatase activity of Eya and the Eya-Six complex as a target for identifying novel therapeutic agents for the treatment of proliferative, invasive and/or metastatic disorders, and compositions identified using the methods disclosed herein. | 2011-12-22 |
20110312919 | INHIBITORS OF TYROSINE KINASE RECEPTOR DIMERIZATION - The teachings relate to methods of identifying inhibitors of dimerization of tyrosine receptor kinases such as EGFR. The methods comprise providing, on a digital computer, a molecular model comprising a complex of extracellular dimerization domains of an RTK, docking a chemical databases to the molecular model, scoring the compounds comprised by the database, and identifying one or more high-scoring compounds. The methods further comprise testing a compound for RTK inhibitory activity in vitro, and testing a compound for specificity as an RTK inhibitor. Also disclosed are compounds selected by the described methods, and methods of treatment using the compounds. Two compounds (NSC11241 and NSC56452) are disclosed that inhibit EGF receptor kinase activation in a dose-dependent manner. | 2011-12-22 |
20110312920 | CAVITY INDUCED ALLOSTERIC MODIFICATION OF INTERMOLECULAR INTERACTIONS AND METHODS OF IDENTIFYING COMPOUNDS THAT EFFECT THE SAME - Method of identifying compounds that modulate intermolecular interactions between a target protein and a modifier are disclosed. Pharmaceutical composition comprising compounds that inhibit intermolecular interactions between a target protein and a modifier are disclosed. Methods of treating individual suffering from inflammatory conditions, undesirable immune responses, immunological conditions and bacterial infections are disclosed. | 2011-12-22 |
20110312921 | N-Myristoyl Transferase Inhibitors - The present invention relates to N-heterocyclic sulphonamide compounds, in particular pyrazole sulphonamide compounds, and their use as N-myristoyl transferase inhibitors. | 2011-12-22 |
20110312922 | EDTA Resistant S100A12 Complexes (ERAC) - The present invention relates to the discovery of a new protein complex in human biological materials that can be used for diagnostic and other purposes. The invention further relates to products, methods and uses related to said protein complex. | 2011-12-22 |
20110312923 | FORMULAS COMPRISING HIGHLY SOLUBLE ELEMENTS AND VITAMIN FOR THE PREVENTION AND AMELIORATION OF OSTEOPOROSIS - The present invention provides formulas of elemental compositions encompassing acetate salts of calcium, magnesium and zinc along with vitamin D | 2011-12-22 |
20110312924 | NOVEL STEROIDAL CYP17 INHIBITORS/ANTIANDROGENS - Steroidal C-17 nitrogen-containing heterocycles of Formula I: | 2011-12-22 |
20110312925 | METHODS OF TREATING OR PREVENTING ESTROGEN-RELATED DISEASES - Methods for treating or reducing the likelihood of acquiring estrogen-related (e.g. estrogen-exacerbated) diseases including endometriosis include administering to a patient a selective estrogen receptor modulator (SERM), in combination with inhibiting ovarian secretions, e.g., by administering an LHRH agonist or antagonist. In some embodiments, a precursor of sex steroids, said precursor being selected from the group consisting of dehydroepiandrosterone (DHEA), dehydroepiandrosterone sulfate (DHEA-S), androst-5-ene-3β,17β-diol (5-diol), and androstenedione or a compound transformed into one of these, is also administered | 2011-12-22 |
20110312926 | 2-(N-Substituted Piperazinyl) Steroid Derivatives - Novel chemical agents are described herein. More specifically, 2-(N-substituted piperazinyl) pregnane and 2-(N-substituted piperazinyl) androstane derivatives exhibiting cytotoxicity on a variety of cancer cell lines are disclosed herein. | 2011-12-22 |
20110312927 | Progesterone Containing Oral Dosage Forms and Related Methods - The present invention provides for progesterone containing pharmaceutical oral dosage forms and related methods. The oral dosage forms can each include an amount of progesterone as well as a pharmaceutically acceptable carrier. The oral dosage forms can be formulated to have at least one of the following characteristics: the oral dosage form produces an pregnane metabolite mean blood plasma level of less than about 1000 nmol/L; the oral dosage form produces an pregnane metabolites mean blood plasma level, after administration of single dose of progesterone composition, such that the ratio of pregnane metabolite level to parent progesterone level of less than 10:1; has a dissolution rate in vitro, when measure using a USP Type-1 dissolution apparatus in 900 mL of deionized water with 2.0% (w/v) of sodium lauryl sulfate at 100 rpm, such that the oral dosage form releases at least 10 wt % of the progesterone within the first 30 minutes and/or releases less than 45 wt % in the first 4 hours; and the oral dosage form produces a ratio of mean plasma progesterone AUC to the amount of progesterone administered of more than 1.5×10 | 2011-12-22 |
20110312928 | Progesterone Containing Oral Dosage Forms and Related Methods - The present invention provides for progesterone containing pharmaceutical oral dosage forms and related methods. The oral dosage forms can each include an amount of progesterone as well as a pharmaceutically acceptable carrier. The oral dosage forms can be formulated to have at least one of the following characteristics: the oral dosage form produces an pregnane metabolite mean blood plasma level of less than about 1000 nmol/L; the oral dosage form produces an pregnane metabolites mean blood plasma level, after administration of single dose of progesterone composition, such that the ratio of pregnane metabolite level to parent progesterone level of less than 10:1; has a dissolution rate in vitro, when measure using a USP Type-1 dissolution apparatus in 900 mL of deionized water with 2.0% (w/v) of sodium lauryl sulfate at 100 rpm, such that the oral dosage form releases at least 10 wt % of the progesterone within the first 30 minutes and/or releases less than 45 wt % in the first 4 hours; and the oral dosage form produces a ratio of mean plasma progesterone AUC to the amount of progesterone administered of more than 1.5×10−6 hr/mL:1. | 2011-12-22 |
20110312929 | TREATMENT OF VAGINAL ATROPHY IN WOMEN WITH CARDIOVASCULAR PATHOLOGY RISK - The present invention relates to the use of estriol in the preparation of a pharmaceutical formulation for vaginal administration with the capacity to self-limit the absorption of estriol, for the prevention and/or the treatment of urogenital atrophy in women said women having a high probability of suffering from a cardiovascular pathology or suffering or having suffered from a cardiovascular pathology. | 2011-12-22 |
20110312930 | Aryl compounds with aminoalkyl substituents and their use - The present application relates to novel aryl compounds with aminoalkyl substituents, to processes for their preparation, to their use for treatment and/or prevention of diseases and to their use for the preparation of medicaments for treatment and/or prevention of diseases, in particular for treatment and/or prevention of hyperproliferative and angiogenic diseases and those diseases which arise from metabolic adaptation to hypoxic states. Such treatments can be carried out as monotherapy or also in combination with other medicaments or further therapeutic measures. | 2011-12-22 |
20110312931 | GLYCINE TRANSPORTER-1 INHIBITORS, METHODS OF MAKING THEM, AND USES THEREOF - The compounds of the present invention are represented by the following formula (I): | 2011-12-22 |
20110312932 | Therapeutic Uses of Compounds Which Selectively Modulate The CB2 Receptor - Compounds of formula (I) | 2011-12-22 |
20110312933 | OXYINDOLE DERIVATIVES WITH MOTILIN RECEPTOR AGONISTIC ACTIVITY - The present invention relates to novel oxyindole derivatives of formula (I) or a pharmaceutically acceptable salt thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the motilin receptor (GPR38). | 2011-12-22 |
20110312934 | 2-ALKYL-6-CYCLOAMINO-3-(PYRIDIN-4-YL)IMIDAZO[1,2-B]-PYRIDAZINE DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTIC APPLICATION THEREOF - The invention relates to 2-alkyl-6-cycloamino-3-(pyridin-4-yl)imidazo[1,2-b]pyridazine derivatives of the general formula (I) where: R | 2011-12-22 |
20110312935 | 1H-Benz Imidazole-5-Carboxamides As Anti-Inflammatory Agents - There are provided compounds of formula (I), wherein R | 2011-12-22 |
20110312936 | CYCLOHEXYL-AZETIDINYL ANTAGONISTS OF CCR2 - The present invention comprises compounds of Formula I. | 2011-12-22 |
20110312937 | 2,5,6,7-TETRAHYDRO-[1,4]OXAZEPIN-3-YLAMINE OR 2,3,6,7-TETRAHYDRO-[1,4]OXAZEPIN-5-YLAMINE COMPOUNDS - This invention relates to compounds of the formula | 2011-12-22 |
20110312938 | Pyrrolopyridine Carboxylic Acid Derivatives - Disclosed are compounds and pharmaceutically acceptable salts of Formula (I) wherein R | 2011-12-22 |
20110312939 | NEW CHEMICAL COMPOUNDS - The present invention relates to new compounds of general formula (I), wherein the groups R | 2011-12-22 |
20110312940 | TETRA-AZA-HETEROCYCLES AS PHOSPHATIDYLINOSITOL-3-KINASES (P13-KINASES) INHIBITOR - The present invention encompasses compounds of general formula (1) wherein R | 2011-12-22 |
20110312941 | 1,4-DISUBSTITUTED PIPERIDINES AS VASOPRESSIN RECEPTOR VIA ANTAGONISTS - The present invention provides compounds of formula (1) compositions comprising such compounds; the use of such compounds in therapy (such as in the treatment of dysmenorrhoea); and methods of treating patients with such compounds; wherein A and G are as defined herein. | 2011-12-22 |
20110312942 | AURORA KINASE INHIBITORS FOR INHIBITING MITOTIC PROGRESSION - The present invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides potent inhibitors of Aurora A kinase, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treatment of cancer. | 2011-12-22 |
20110312943 | AURORA KINASE INHIBITORS FOR INHIBITING MITOTIC PROGRESSION - The present invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides potent inhibitors of Aurora A kinase, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treatment of cancer. | 2011-12-22 |
20110312944 | Heterocyclic Compounds Which Modulate The CB2 Receptor - Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain. | 2011-12-22 |
20110312945 | CRTH2 MODULATORS - Modulators of CRTH2, particularly antagonists of CRTH2, that are useful for treating various disorders, including asthma and respiratory disorders are disclosed. The compounds fall within a genus described by formula I | 2011-12-22 |
20110312946 | COMBINATION THERAPY FOR THE TREATMENT OF DIABETES - The present invention provides methods of treating, reducing, preventing, or inhibiting symptoms of diabetes and/or lowering plasma levels of HbA1c by co-administration of therapeutic or subtherapeutic doses of telenzepine and sertraline to a subject in need thereof. | 2011-12-22 |
20110312947 | Method of improving -adrenergic receptor function - The present invention relates to a method of increasing the sensitivity of a hyperinsulinemic patient to the anti-obesity and antidiabetic effects of a β adrenergic receptor (βAR) agonist. The method comprises administering to the patient the βAR agonist and an agent that reduces plasma insulin levels and thereby increases the sensitivity of the patient to the effects of the βAR agonist. | 2011-12-22 |
20110312948 | Crystalline Forms of the Tri-Mesylate Salt of Perphenazine-Gaba and Process of Producing the Same - Novel crystalline form of perphenazine 4-aminobutyrate trimesylate and a process of producing the same are disclosed. The novel crystalline form is characterized by a unique XRPD pattern and a DSC that exhibits an endothermic peak at a relatively high temperature (e.g., higher than 209° C.). Also disclosed are a process of preparing perphenazine 4-aminobutyrate trimesylate by in situ deprotection and salification, in a single-step synthesis, and a highly pure perphenazine 4-aminobutyrate trimesylate obtained thereby. Uses of any of the described perphenazine 4-aminobutyrate trimesylate are also disclosed. | 2011-12-22 |
20110312949 | PHARMACEUTICAL USE OF SUBSTITUTED AMIDES - The use of substituted amides for modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11βHSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable. | 2011-12-22 |
20110312950 | CYCLIC INHIBITORS OF 11beta-HYDROXYSTEROID DEHYDROGENASE 1 - This invention relates to novel compounds of the Formula Formulas (I), (Ia | 2011-12-22 |
20110312951 | C-Ring Modified Tricyclic Benzonaphthiridinone Protein Kinase Inhibitors and Use Thereof - Disclosed are C-ring modified tricyclic benzonaphthiridinone compounds and analogs thereof, pharmaceutical compositions comprising such compounds and processes for preparing the same. The compounds are useful in the treatment of diseases amenable to protein kinase signal transduction inhibition, regulation and/or modulation. | 2011-12-22 |
20110312952 | NOVEL SPIRO COMPOUNDS USEFUL AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE - Heteroaromatic compounds of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis. | 2011-12-22 |
20110312953 | ANTHRANILIC ACID DERIVATIVES - The present invention relates to novel anthranilic acid derivatives of the general formula (I) | 2011-12-22 |
20110312954 | MINERALOCORTICOID RECEPTOR ANTAGONIST AND METHODS OF USE - The present invention provides a compound of the formula: Compound (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising Compound (I) in combination with a suitable carrier, diluent, or excipient; and methods for treating physiological disorders, particularly congestive heart failure, hypertension, diabetic nephropathy, or chronic kidney disease, comprising administering Compound (I), or a pharmaceutically acceptable salt thereof. | 2011-12-22 |
20110312955 | TRIAZINE COMPOUNDS AS PI3 KINASE AND MTOR INHIBITORS - Compounds of formula I | 2011-12-22 |
20110312956 | ARYLINDENOPYRIMIDINES WITH REDUCED hERG CHANNEL BINDING - This invention provides novel arylindenopyrimidines of the Formula (I), | 2011-12-22 |
20110312957 | IMIDAZOPYRIDINES AND IMIDAZOPYRIMIDINES AS HIV-I REVERSE TRANSCRIPTASE INHIBITORS - The invention provides compounds of formula A or B which are useful in the treatment of a subject infected with HIV. | 2011-12-22 |
20110312958 | MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS - Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention. | 2011-12-22 |
20110312959 | Derivatives of Azaindoles as Inhibitors of Protein Kinases ABL and SRC - The present invention relates to compounds of general formula I and use thereof as inhibitors of protein kinases AbI and Src and the method of production thereof. The present invention also relates to pharmaceutical compositions and medici-nal products comprising these compounds. | 2011-12-22 |
20110312960 | PYRAZINE DERIVATIVES AND USE AS PI3K INHIBITORS - The present invention is related to pyrazine derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries. | 2011-12-22 |
20110312961 | 2,5-Disubstituted Morpholine Orexin REceptor Antagonists - The present invention relates to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS). | 2011-12-22 |
20110312962 | NOVEL 2-MORPHOLINO-3-AMIDO-PYRIDINE DERIVATIVES AND THEIR MEDICAL USE - The present application discloses novel 2-morpholino-3-amido-pyhcline derivatives and their use as modulators of the voltage gated K | 2011-12-22 |
20110312963 | P38 MAP KINASE INHIBITORS - The present disclosure relates to compounds of formula (I): | 2011-12-22 |
20110312964 | CYSTEINE PROTEASE INHIBITORS - Compounds of the formula I | 2011-12-22 |
20110312965 | RETINOID DERIVATIVES ENDOWED WITH CYTOTOXIC AND/OR ANTIANGIOGENIC PROPERTIES - The present invention relates to new retinoid derivatives of formula I and to pharmaceutical compositions containing them for the treatment of patients affected by pathologies such as arthritic conditions, tumours, metastatic cancer, diabetic retinopathy, psoriasis, chronic inflammatory diseases or atherosclerosis. | 2011-12-22 |
20110312966 | Dithiinopyridazinone Derivates - The present invention relates to new dithiinopyridazinone derivatives, to processes for preparing them, to their use for controlling unwanted microorganisms, more particularly phytopathogenic fungi, in crop protection, in the household and hygiene sector and in the protection of materials, and also to crop protection compositions comprising these dithiinopyridazinone derivatives. | 2011-12-22 |
20110312967 | BRIDGED AND FUSED ANTIDIABETIC COMPOUNDS - This invention provides for certain bridged and fused compounds of the formula G-L-A I or a pharmaceutically acceptable salt, ester of solvate thereof wherein: A is: (I) and the other variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders. | 2011-12-22 |
20110312968 | METHOD FOR OPTIMIZING THE TREATMENT OF CHRONIC MYELOID LEUKEMIA WITH ABL TYROSINE KINASE INHIBITORS - The present invention relates to a method tor evaluating patterns to help-optimizing the treatment of chronic myeloid leukemia (CML) in a human patient population. Specifically, present invention relates to SHP1 and/or SHP2 as a biomarker for CML patients. | 2011-12-22 |
20110312969 | COMPOUNDS FOR TREATING CANCER - Compounds of general formula (I): wherein R | 2011-12-22 |
20110312970 | PYRIDINE DERIVATIVES FOR THE TREATMENT OF METABOLIC DISORDERS RELATED TO INSULIN RESISTANCE OR HYPERGLYCEMIA - The present invention provides novel compounds represented by the general formula (I): | 2011-12-22 |
20110312971 | POLYMORPHIC FORMS OF 1-'4-(5-CYANOINDOL-3-YL) BUTYL-4-(2-CARBAMOYLBENZOFURAN-5-YL)PIPERAZINE HYDROCHLORIDE - The invention relates to new crystalline modifications of the hydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine, crystalline modification of the dihydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine and amorphous 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride which are suitable in particular for the preparation of solid medicaments for the treatment or prevention of depressive disorders, anxiety disorders, bipolar disorders, mania, dementia, substance-related disorders, sexual dysfunctions, eating disorders, obesity, fibromyalgia, sleeping disorders, psychiatric disorders, cerebral infarct, tension, for the therapy of side-effects in the treatment of hypogonadism, secondary amenorrhea, premenstrual syndrome and undesired puerperal lactation. | 2011-12-22 |
20110312972 | SUBSTITUTED 3-BENZOFURANYL-INDOL-2-ONE-3-ACETAMIDIDOPIPERAZINE DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF - The invention relates to disubstituted 3-benzofuranyl-indol-2-one-3-acetamidopiperazine derivatives of the general formula (I) where R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are such as defined in claim | 2011-12-22 |
20110312973 | SOLID COMPOSITIONS - The present invention features solid compositions comprising amorphous Compound I. A solid dispersion of the present invention also contains a pharmaceutically acceptable hydrophilic polymer and a pharmaceutically acceptable surfactant. Compound I may be formulated in an amorphous solid dispersion which comprises a pharmaceutically acceptable hydrophilic polymer and preferably a pharmaceutically acceptable surfactant. | 2011-12-22 |
20110312974 | HETEROARYL ANTAGONISTS OF PROSTAGLANDIN D2 RECEPTORS - Described herein are compounds that are antagonists of PGD | 2011-12-22 |
20110312975 | CERTAIN CHEMICAL ENTITIES, COMPOSITIONS AND METHODS - Provided are certain chemical entities, and methods of use to modulate skeletal myosin, skeletal actin, skeletal tropomyosin, skeletal troponin C, skeletal troponin I, skeletal troponin T, and skeletal muscle, including fragments and isoforms thereof, as well as the skeletal sarcomere, and methods of use in the treatment of neuromuscular disorders, conditions having muscle wasting, claudication, frailty, metabolic syndrome, muscle atrophy associated with disuse, and muscle fatigue, and other indications. | 2011-12-22 |
20110312976 | NOVEL ISOINDOLIN-1-ONE DERIVATIVE - The present invention relates to a compound represented by formula (I): (wherein R, R | 2011-12-22 |
20110312977 | PROCESS FOR THE PREPARATION OF VORICONAZOLE - The present invention provides a process for preparation of racemic voriconazole in a single reaction vessel. The present invention also provides a process for preparation of voriconazole using racemic voriconazole and the process of making it therewith. | 2011-12-22 |
20110312978 | PDE1 INHIBITORS FOR OPHTHALMIC DISORDERS - Compounds that inhibit phosphodiesterase 1 (PDE1) are useful to treat glaucoma or elevated intraocular pressure. The PDE1 inhibitors may be administered as monotherapy or in combination with additional intraocular-pressure lowering agents. In addition, the invention provides ophthalmic compositions comprising PDE 1 inhibitors and optionally one or more additional intraocular pressure-lowering agents. Topical and systemic therapy may be used. | 2011-12-22 |
20110312979 | FUSED PYRROLE DERIVATIVES AS PI3K INHIBITORS - The present invention provides fused pyrrole derivatives of Formula I: | 2011-12-22 |
20110312980 | Small-molecule Hsp90 Inhibitors - Purine scaffold Hsp90 inhibitors are useful in therapeutic applications and as radioimaging ligands. | 2011-12-22 |
20110312981 | PREDICTIVE MARKER FOR EGFR INHIBITOR TREATMENT - The present invention provides a biomarker SFRS7 which is predictive for the clinical benefit of EGFR inhibitor treatment in cancer patients. | 2011-12-22 |
20110312982 | Cancer Treatment Method - A method of treating cancer is described including administration of a 4-quinazolinamine and at least one other anti-neoplastic agent as well as a pharmaceutical combination including the 4-quinazolinamines. | 2011-12-22 |
20110312983 | DEUTERIUM-ENRICHED ALOGLIPTIN - The present application describes deuterium-enriched alogliptin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 2011-12-22 |
20110312984 | STAT3 INHIBITORS - Small molecule inhibitors of Stat3 and their derivatives are disclosed. Also described are methods to inhibit cell growth by use of Stat3 inhibitors, and the use of Stat3 inhibitors for the prevention and/or treatment of cancer. Further, inhibitors of Stat3 that also do not inhibit Stat1 are described as well as their derivatives. Methods of screening additional compounds for Stat3 inhibition activity and/or non-inhibition of Stat1 activity are also described herein. | 2011-12-22 |
20110312985 | NARINGENIN COMPLEXES AND METHODS OF USE THEREOF - The invention relates to methods of treatment of hepatitis C, dyslipidemia, insulin resistance, and inflammation, with flavonoid-sugar complexes. | 2011-12-22 |
20110312986 | Composition and Method for Treating Overactive Bladder - The present specification discloses compounds, compositions including such compounds, kits including such compounds and compositions, and methods of treating an individual suffering from overactive bladder and/or diabetes by administering such compounds or compositions to an individual in need thereof. | 2011-12-22 |
20110312987 | SALT OF NAPHTHYRIDINE CARBOXYLIC ACID DERIVATIVE - 7-(3-Aminomethyl-4-methoxyiminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid methanesulfonate and hydrates thereof, processes for their preparation, pharmaceutical compositions comprising them, and their use in antibacterial therapy. | 2011-12-22 |
20110312988 | SNS-595 AND METHODS OF USING THE SAME - The present invention relates to SNS-595 and methods of treating cancer using the same. | 2011-12-22 |
20110312989 | INDOLES, 1H-INDAZOLES, 1,2-BENZISOXAZOLES, AND 1,2-BENZISOTHIAZOLES, AND PREPARATION AND USES THEREOF - The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds for example, indoles, 1H-indazoles, 1,2-benzisoxazoles, and 1,2-benzisothiazoles, which act as ligands for the α7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof. | 2011-12-22 |
20110312990 | Diamine Derivatives - A compound represented by the general formula (1): | 2011-12-22 |
20110312991 | ACTIVATED BLOOD COAGULATION FACTOR INHIBITOR - An object of the present invention is to provide a novel salt form of a compound that exhibits an inhibitory effect on activated blood coagulation factor X, and is useful as a preventive and/or therapeutic drug for thrombotic diseases, and crystals thereof. The present invention provides N | 2011-12-22 |
20110312992 | Inhibitors of C-Kit and Uses Thereof - Compounds and methods useful as inhibitors of c-Kit are presented. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of c-Kit and processes for synthesizing these compounds are also described herein. | 2011-12-22 |
20110312993 | AMIDO-TROPANE DERIVATIVES - The present invention relates to a compound of formula I | 2011-12-22 |
20110312994 | BIPHENYL DERIVATIVES - This invention provides biphenyl derivatives of formula I: | 2011-12-22 |
20110312995 | BRIDGED AND FUSED HETEROCYCLIC ANTIDIABETIC COMPOUNDS - This invention provides for certain bridged and fused heterocyclic compounds of the formula (I) or a pharmaceutically acceptable salt, ester solvate or prodrug thereof wherein: L is: (II) and the other variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders. | 2011-12-22 |
20110312996 | NOVEL INHIBITORS OF HEPATITIS C VIRUS REPLICATION - The embodiments provide compounds of the general Formulae VI, VII, VIII, IX, X, XI, XII, XIII, XIV, and XV as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition. | 2011-12-22 |
20110312997 | Inhibition of WDR5 Interaction with Its Binding Partners - Peptidomimetics that inhibit the interaction between MLL1 and WDR5 are disclosed. Methods of inhibiting MLL1 activity and methods of treating cancers also are disclosed. | 2011-12-22 |
20110312998 | Methods of Making and Using Stable Pharmaceutical Compositions Comprising Ketotifen and Naphazoline - Stable compositions comprising ketotifen or a ketotifen salt and methods of preparing such compositions are provided. The pH of the compositions remains at less than about 5 during storage. The methods comprise preparing pharmaceutical compositions comprising ketotifen or a ketotifen salt, and adjusting their pH to less than 5, thus slowing the changes of the active ingredients. | 2011-12-22 |
20110312999 | Ketoheteroarylpiperidine and -Piperazine Derivatives as Fungicides - Ketoheteroarylpiperidine and -piperazine derivatives of the formula (I), | 2011-12-22 |