21st week of 2013 patent applcation highlights part 58 |
Patent application number | Title | Published |
20130130988 | MACROMOLECULAR COMPLEX OF BACTERIAL ORIGIN AND USE OF SAID MACROMOLECULAR COMPLEX FOR PREVENTING AND TREATING INFLAMMATORY RHEUMATISM - A bacterial macromolecular complex produced by bacteria belonging to the | 2013-05-23 |
20130130989 | EIF4E BINDING PEPTIDES - The present invention relates to modified eIF4G1 peptides, uses thereof and pharmaceutical compositions comprising the modified eIF4G1 peptides. | 2013-05-23 |
20130130990 | USE OF SPINK6 GENE AND ITS ENCODED PROTEIN FOR THE PREPARATION OF AN ANTI-TUMOR DRUG - The present invention describes use of spink6 gene and the encoded protein in the manufacture of an anti-tumor drug. spink6 gene has a nucleotide sequence designated as SEQ ID NO:1, and the protein encoded by spink6 gene has an amino acid sequence designated as SEQ ID NO:2. The protein encoded by spink6 gene and its derivatives can be used as potential drugs for treatment of human diseases caused by dysregulation of the cell cycle control, such as various malignant tumors, cell abnormal proliferation, and the like. | 2013-05-23 |
20130130991 | USE OF A PEPTIDE ENHANCING THE ABILITY OF RADIATION THERAPY TO KILL CANCER CELLS - The present invention relates to a peptide consisting essentially of the N2 sequence of the RasGAP protein, a bio logically active fragment thereof, or a variant thereof, which is useful for the preparation of a medicament for the treatment of cancer. Furthermore, it relates to a method of treatment of cancer comprising administering to a subject in need thereof, a therapeutically effective amount of the peptide of the invention. | 2013-05-23 |
20130130992 | DIPEPTIDE DERIVATIVE FOR THE TREATMENT OF CANCER - This invention relates to purified compound of formula (1). The invention includes all isomeric forms and all tautomeric forms of the compound of formula (1) and pharmaceutically acceptable salts thereof. The present invention further relates to processes for the production of the compound of formula (1) by fermentation of the fungal strain of sterile mycelium (PM0509732/MTCC5544) and to pharmaceutical compositions containing the compound as active ingredient and its use in medicines for treatment of cancer. | 2013-05-23 |
20130130993 | PIMAP39 MODULATES INFLAMMATORY RESPONSE - The present invention relates to a novel peptide sequence named PIMAP39 (herein referred to as SEQ ID NO.: 1) and methods of use of the novel sequence and functional variants thereof. The present invention also relates to methods for reducing and/or modulating inflammatory responses by administration of the peptide of the present invention. Furthermore, the present invention relates to the modulation of the expression of cytokines effected as part of an inflammatory response by administration of the peptide of the present invention. | 2013-05-23 |
20130130994 | ANTIMICROBIAL PEPTIDES AND PEPTIDE DERIVATIVES DERIVED FROM ONCOPELTUS FASCIATUS - The present invention relates to a antimicrobial peptide or peptide derivative comprising the following sequence: Sub | 2013-05-23 |
20130130995 | Treatments for Gastrointestinal Disorders - Described herein are peptides, compositions, and related methods for treating upper gastrointestinal disorders and conditions (e.g., dyspepsia, gastroparesis, post-operative gastric ileus, a functional esophageal disorder, a functional gastroduodenal disorder, gastroesophageal reflux disease (GERD), or a duodenal or stomach ulcer) as well as other conditions and disorders that are described herein. | 2013-05-23 |
20130130996 | PEPTIDES FOR INHIBITING CHEMOKINE BINDING TO CHEMOKINE RECEPTORS - Novel peptidic or peptidomimetic agents or small molecules for modulating the biological effect of a chemokine. According to the present invention, the therapeutic agents preferably are endowed with the capacity to bind to certain chemokines in order to modulate the biological interaction between the target ligand, chemokine, and the respective target receptor, chemokine receptor. These peptides may be described as agonist ligands or antagonists. Next, preferably certain peptides share consensus sequences are described which characterize the families or categories of these modulator peptides. | 2013-05-23 |
20130130997 | C-ARYL GLUCOSIDE DERIVATIVES, PREPARATION PROCESS AND PHARMACEUTICAL USE THEREOF - C-aryl glucoside derivatives, preparation processes and pharmaceutical uses thereof are disclosed. In particular, C-aryl glucoside derivatives represented by formula (I), with each substituent defined in the application, pharmaceutically acceptable salts or stereoisomers thereof, their preparation methods, and pharmaceutical compositions containing the derivatives as well as their uses as therapeutic agents, particularly as sodium-dependent glucose cotransporter (SGLT)-1 inhibitors, are disclosed. | 2013-05-23 |
20130130998 | Analogues of Etoposide for the Treatment of Tumours - Compounds for treatment of a patient having a tumour that is metastatic and/or that reduces an organ function, wherein the compounds are of the general formula: | 2013-05-23 |
20130130999 | METHOD OF DETERMINING ACUTE MYELOID LEUKEMIA RESPONSE TO TREATMENT WITH FARNESYLTRANSFERASE INHIBITORS - The disclosed method rapidly identifies with desired accuracy AML patients, including elderly AML patients, likely to respond to treatment with a combination of a farnesyltransferase inhibitor and one or more of etoposide, teniposide, tamoxifen, sorafenib, paclitaxel, temozolomide, topotecan, trastuzumab and cisplatinum. In an embodiment, the improvements include the use of whole blood rather than the customary bone marrow sample, thus making the assay more accurate, rapid, less intrusive, less expensive as well as less painful. The method includes evaluation of a two-gene expression ratio (RASGRP1:APTX), which with a corresponding threshold, provides sufficient accuracy for predicting the response to the combination treatment. In the preferred embodiment the combination treatment combines tipifarnib (R115777, ZARNESTRA®) with etoposide. Further, the elderly AML patients identified as being likely responsive to the combination treatment with tipinifarb and etoposide have a complete recovery rate comparable to the best therapy available for younger patients. | 2013-05-23 |
20130131000 | Composition Comprising Ligustroflavone, Rhoifolin and Hyperin and Its Pharmaceutical Application - Disclosed is a composition comprising ligustroflavone, rhoifolin and hyperin, which is prepared according to rational weight ratio: 40% to 80% ligustroflavone, 5% to 45% rhoifolin and 1% to 40% hyperin. The composition can be used as a neuraminidase inhibitor for preventing and treating influenza, and can be formulated into pharmaceutically acceptable dosage forms. | 2013-05-23 |
20130131001 | Epirubicin Derivatives - Disclosed are compounds represented by formula (I), pharmaceutically acceptable salts thereof, solvates thereof, and solvates of the pharmaceutically acceptable salts thereof, | 2013-05-23 |
20130131002 | COMPOSITIONS AND METHODS FOR TREATING PULMONARY HYPERTENSION - The present invention relates to methods of treating pulmonary hypertension in a subject including administering to the subject a therapeutically effective dose of at least one anthracycline. | 2013-05-23 |
20130131003 | ORALLY DISINTEGRATING TABLET CONTAINING ACARBOSE - It was an object of the present invention to provide an orally disintegrating tablet (ODT) for the glycosidase inhibitor acarbose. The object is achieved with an orally disintegrating tablet containing 1-30% acarbose and 40-90% water-soluble carrier. In order to obtain the desired properties, the ingredients have to be precompacted and to be premixed with an insoluble carrier. | 2013-05-23 |
20130131004 | PROLIFERATION INHIBITOR OF HELICOBACTER PYLORI BACTERIA - A method for directly inhibiting proliferation of | 2013-05-23 |
20130131005 | METHODS AND COMPOSITIONS FOR PROVIDING CARDIAC PROTECTION - The invention provides a method of reducing infarct size and/or limiting, decreasing and/or inhibiting reperfusion injury and/or ameliorating heart failure in a patient comprising administering a pharmaceutically effective amount of at least one compound capable of inhibiting AC5 to the patient. The compound capable of inhibiting AC5 is particularly effective when administered during or after reperfusion in patients suffering from an ischemic injury. | 2013-05-23 |
20130131006 | METHOD FOR INHIBITING THE INDUCTION OF CELL DEATH BY INHIBITING THE SYNTHESIS OR SECRETION OF AGE-ALBUMIN IN CELLS OF THE MONONUCLEAR PHAGOCYTE SYSTEM - The present invention relates to a method for inhibiting the induction of cell death by inhibiting the synthesis or secretion of AGE-albumin in cells of the mononuclear phagocyte system, to an AGE-albumin synthesis inhibitor, and to a pharmaceutical composition comprising the AGE-albumin synthesis inhibitor for preventing or treating degenerative disease and autoimmune disease. The AGE-albumin of the present invention is synthesized and secreted in human microglia or human macrophages in an Alzheimer's model, stroke model, Parkinson's disease model and rheumatoid arthritis model. The AGE-albumin synthesis and secretion are caused by oxidative stress. The expression of RAGE increases in first-order human neurons or cartilage cells to which AGE-albumin is administered, whereupon a MAPK signaling pathway is activated and the expression of Bax increases to induce an increase in calcium in mitochondria, thus finally inducing cell death. Therefore, the AGE-albumin synthesis inhibitor of the present invention can be valuably used in the diagnosis or treatment of degenerative diseases or autoimmune diseases such as Alzheimer's disease, strokes, Parkinson's disease, amyotrophic lateral sclerosis, rheumatoid arthritis, diabetic retinopathy, AIDS, aging, pulmonary fibrosis, spinal cord injuries, etc. | 2013-05-23 |
20130131007 | VITAMIN B12 COMPOSITIONS - This disclosure provides compositions of vitamin B | 2013-05-23 |
20130131008 | LIPOPHILIC MONOPHOSPHORYLATED DERIVATIVES AND NANOPARTICLES - There are provided, inter alia, lipophilic monophosphorylated derivatives of gemcitabine. There are further provided nanoparticles compositions incorporating lipophilic monophosphorylated derivatives of gemcitabine, pharmaceutical compositions thereof, and a method of treating cancer or a viral infection in a subject in need thereof, which method includes administration of a pharmaceutical composition disclosed herein. | 2013-05-23 |
20130131009 | Compositions Comprising High Molecular Weight Hyaluronic Acid and Methods For Producing Same - This invention provides cell culture compositions which produce significant quantities of high molecular weight hyaluronic acid. The cell cultures are obtained from cells of mole rats, such as naked mole rats and blind mole rats. The high molecular weight hyaluronic acid can be collected in the conditioned media of these cell cultures. These cell cultures provide a convenient source of large quantities of high molecular weight hyaluronic acid. | 2013-05-23 |
20130131010 | GALACTOSE-PRONGED POLYSACCHARIDES IN A FORMULATION FOR ANTIFIBROTIC THERAPIES - Methods and compositions for reducing fibrosis and cirrhosis are provided in which an effective dose of an admixture of a polysaccharide compound and, for example, a compound selected from the group consisting of antibodies specific to intracellular or cell-surface: (i) beta-PDGF receptors; (ii) synaptophysin; (iii) zvegf3; (iv) CCR1 receptors; (v) connective tissue growth factor; (vi) alpha 1-smooth muscle actin; (vii) matrix metalloproteinases MMP 2 and MMP9; (viii) matrix metalloproteinase inhibitors TIMP1 and TMP2; (ix) integrins; (x) TFG-β1; (xi) endothelin receptor antagonists; and (xii) collagen synthesis and degradation modulating compounds; (xiii) actin synthesis and degradation modulating compounds; and (xiv) tyrosine kinases is administered to an animal in order to treat fibrosis. | 2013-05-23 |
20130131011 | HYALURONIC ACID-BASED GELS INCLUDING LIDOCAINE - Disclosed herein are cohesive soft tissue fillers, for example, dermal and subdermal fillers, based on hyaluronic acids and pharmaceutically acceptable salts thereof. In one aspect, hyaluronic acid-based compositions described herein include a therapeutically effective amount of at least one anesthetic agent, for example, lidocaine. The present hyaluronic acid-based compositions including lidocaine have an enhanced stability and cohesivity, relative to conventional compositions including lidocaine, for example when subjected to sterilization techniques or when stored for long periods of time. Methods and processes of preparing such hyaluronic acid-based compositions are also provided. | 2013-05-23 |
20130131012 | PROCESS FOR OBTAINING CITRUS FIBER FROM CITRUS PULP - A process is disclosed for obtaining citrus fiber from citrus pulp. Citrus fiber is obtained having a c* close packing concentration value of less than 3.8. The citrus fiber can be obtained having a viscosity of at least 1000 mPa·s, wherein said citrus fiber is dispersed in standardized water at a mixing speed of from 800 rpm to 1000 rpm, to a 3 w/w % citrus fiber/standardized water solution, and wherein said viscosity is measured at a shear rate of 5 s−1 at 20° C. Citrus fiber can be obtained having a CIELAB L* value of at least 90. The citrus fiber can be used in food products, feed products, beverages, personal care products, pharmaceutical products or detergent products. | 2013-05-23 |
20130131013 | CYCLODEXTRIN-BASED POLYMERS FOR THERAPEUTICS DELIVERY - The present invention relates to novel compositions of therapeutic cyclodextrin containing polymeric compounds designed as a carrier for small molecule therapeutics delivery and pharmaceutical compositions thereof. These cyclodextrin-containing polymers improve drug stability and solubility, and reduce toxicity of the small molecule therapeutic when used in vivo. Furthermore, by selecting from a variety of linker groups and targeting ligands the polymers present methods for controlled delivery of the therapeutic agents. The invention also relates to methods of treating subjects with the therapeutic compositions described herein. The invention further relates to methods for conducting pharmaceutical business comprising manufacturing, licensing, or distributing kits containing or relating to the polymeric compounds described herein. | 2013-05-23 |
20130131014 | PREVENTION AND TREATMENT OF SECONDARY INFECTIONS FOLLOWING VIRAL INFECTION - This invention relates to a synthetic nutritional composition suitable for use in the prevention of secondary infections following a viral infection characterised by neuraminidase activity comprising a sialylated oligosaccharide and N-acetyl-lactosamine and/or an oligosaccharide containing N-acetyl-lactosamine. The invention further extends to the use of such a composition in the prevention of secondary infections such as otitis media. | 2013-05-23 |
20130131015 | SYNTHESIS AND REGIOSELECTIVE SUBSTITUTION OF 6-HALO- AND 6-ALKOXY NICOTINE DERIVATIVES - The present invention provides active compounds for modulating nicotinic acetylcholine receptors and methods of making the same. The methods of preparing the active compounds utilize different intermediate compounds. | 2013-05-23 |
20130131016 | BORON-CONTAINING SMALL MOLECULES - This invention provides novel compounds, methods of using the compounds, and pharmaceutical formulations comprising the compounds. | 2013-05-23 |
20130131017 | BORON-CONTAINING SMALL MOLECULES - This invention provides novel compounds, methods of using the compounds, and pharmaceutical compositions containing the compounds. | 2013-05-23 |
20130131018 | SUBSTITUTED ISOQUINOLINES AND THEIR USE AS TUBULIN POLYMERIZATION INHIBITORS - The present invention relates generally to substituted isoquinolines and their use as tubulin polymerization inhibitors. In particular, the invention relates to substituted isoquinolines which possess useful therapeutic activity, use of these compounds in methods of therapy and the manufacture of medicaments as well as compositions containing these compounds. | 2013-05-23 |
20130131019 | CHIRAL COMPOUNDS SUBSTITUTED WITH PHOSPHONIC ACID ESTER FUNCTIONS OR PHOSPHONIC ACID FUNCTIONS - The present invention relates to novel compounds that contain PNA units substituted with phosphonic acid ester functions or phosphonic acid functions, and have at least one chiral center. The compounds may be used for the treatment of viral diseases, such as AIDS. | 2013-05-23 |
20130131020 | SYNERGISTIC COMPOSITION - A synergistic composition comprising a THP salt and a biopenetrant, in which the biopenetrant comprises a polymer of an unsaturated carboxylic acid or a copolymer of an unsaturated carboxylic acid with a sulphonic acid, said polymer or copolymer being terminated by a mono- or diphosphonated unsaturated carboxylic acid group or having such monomers incorporated into the polymer backbone. This composition acts synergistically to enhance the biocidal efficacy of the THP salt against both planktonic (free-swimming) and sessile (attached) bacteria, and also acts synergistically to enhance the efficacy of the THP salt in the dissolution of iron sulphide scale. | 2013-05-23 |
20130131021 | ANALOGUES OF CILOSTAZOL - This invention relates to novel compounds which are derivatives of the phosphodiesterase inhibitor, cilostazol and pharmaceutically acceptable salts thereof. This invention also provides pyrogen-free compositions comprising one or more compounds of the invention and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are treated by administration of a phosphodiesterase inhibitor, such as cilostazol. The invention also relates to the use of the disclosed compounds and compositions as reagents in analytical studies involving cilostazol. | 2013-05-23 |
20130131022 | Methods for Controlled Release Oral Dosage of a Vitamin D Compound - A stable, controlled release formulation for oral dosing of vitamin D compounds is disclosed. The formulation is prepared by incorporating one or more vitamin D compounds into a solid or semi-solid mixture of waxy materials. Oral dosage forms can be prepared by melt-blending the components described herein and filling gelatin capsules with the formulation. | 2013-05-23 |
20130131023 | NEW POLYMORPHIC FORM OF A CALCIMIMETIC COMPOUND - The present invention relates to the crystalline, polymorphic Form C of the calcimimetic compound {4-[(1R,3S)-3-((R)-1-Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid, to methods of preparation thereof, to methods of characterization thereof by single crystal X-Ray crystallography (XRC), X-Ray Powder diffractometry, attenuated total reflectance Fourier transform infrared (ATR-FTIR) spectroscopy, Solid State NMR spectroscopy and Differential Scanning Calorimetry (DSC), and to its use. The invention also relates to the preparation of Form C by crystallization from a saturated solution of {4-[(1R,3S)-3-((R)-1-Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid in the presence of crystallization seeds of Form C, or alternatively by conversion of an amorphous starting material into the different crystalline polymorphic Form X by crystallization of {4-[(1R,3S)-3-((R)-1-Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid, followed by a solid solution transformation thereof into the desired polymorphic Form C. | 2013-05-23 |
20130131024 | METHODS AND COMPOSITIONS FOR THE TREATMENT OF FLUID ACCUMULATION IN AND/ OR UNDER THE RETINA - The present invention provides methods and compositions for the treatment of fluid accumulation in and/or under the retina. | 2013-05-23 |
20130131025 | HYPERLIPEMIA-AMELIORATING AGENT, ANEMIA-AMELIORATING COMPOSITION, URIC-ACID-LEVEL-REDUCING COMPOSITION, AND FOOD OR BEVERAGE - A neutral-fat-level-regulating agent, a cholesterol-level-regulating agent, a free-fatty-acid-level-regulating agent or an anti-obesity agent, including: at least one of protopanaxatriol, panaxatriol, protopanaxadiol and panaxadiol which are aglycons of dammarane-type saponins and a hyperlipemia-ameliorating agent including: at least one of the neutral-fat-level-regulating agent, the cholesterol-level-regulating agent, the free-fatty-acid-level-regulating agent and the anti-obesity agent. | 2013-05-23 |
20130131026 | COMPOSITIONS AND METHODS FOR TREATING SYMPTOMS OF INFLAMMATORY RELATED CONDITIONS USING A COMBINATION OF AN ANTIHISTAMINE AND A STIMULANT - The present invention relates to compositions containing stimulant and anti-histamine compounds, to methods for treating symptoms related to inflammation using the combination compounds, and to a method for preparing the compositions. | 2013-05-23 |
20130131027 | PARENTERAL PHARMACEUTICAL FORM WHICH RELEASES AROMATSE INHIBITOR AND GESTAGENS, FOR THE TREATMENT OF ENDOMETRIOSIS - The present invention for the treatment of endometriosis relates to providing a parenteral dosage form (delivery system) for the controlled release of an aromatase inhibitor (AI) in a daily release rate that does not induce stimulation of the ovaries by negative feed-back of the pituitary-ovarian-axis (which would cause secretion of gonadotropins and stimulation of ovarian follicular growth) and a gestagen in a daily release rate below the ovulation inhibition dose that provides contraceptive efficacy based on local effects (e.g. reducing and thickening of the cervical mucus impairing sperm ascension, effects on the endometrium and on tubal motility impairing implantation and egg transport). | 2013-05-23 |
20130131028 | METHODS FOR TREATMENT OF SLEEP-RELATED BREATHING DISORDERS - Described herein are methods for modulation of the activity of the carotid body that afford therapeutic benefit for sleep-related breathing disorders and related conditions. | 2013-05-23 |
20130131029 | ANTISOLVENT SOLIDIFICATION PROCESS - The present invention relates to a antisolvent solidification process wherein a liquid medium comprising at least one organic or inorganic compound which is to be solidified is forced through a membrane into one or more antisolvents, or wherein one or more antisolvents are forced through a membrane into a liquid medium comprising at least one organic or inorganic compound which is to be solidified, yielding a composition comprising solid particles comprising said organic and/or inorganic compound(s). | 2013-05-23 |
20130131030 | OPTIMIZING MIFEPRISTONE ABSORPTION - The present invention provides a method for altering the pharmacokinetics of mifepristone upon oral administration. Mifepristone absorption into the blood is increased upon administration with meals. The method of the invention can benefit patients suffering from conditions including psychiatric illnesses and hormonal disorders. | 2013-05-23 |
20130131031 | METHOD OF TREATING REFRACTORY CANCER - Therapeutic methods for treating refractory cancers are disclosed comprising administering to a patient in need of treatment a ruthenium complex salt. | 2013-05-23 |
20130131033 | PHARMACEUTICAL COMPOSITION FOR TREATMENT OF RESPIRATORY TRACT INFECTIONS - The present invention relates to a pharmaceutical composition comprising ciprofloxacin or salts of thereof and amoxycillin or salts of thereof and other pharmaceutical excipients. The present invention provides more reliable effect against all bacteria, including the most commonly causative | 2013-05-23 |
20130131034 | DERIVATIVES OF AMINOINDANES, THEIR PREPARATION AND THEIR APPLICATION IN THERAPEUTICS - The instant invention relates to derivatives of formula (I) | 2013-05-23 |
20130131035 | CARBOXAMIDES AS INHIBITORS OF VOLTAGE-GATED SODIUM CHANNELS - The present invention provides compounds that are inhibitors of voltage-gated sodium channels (Nav), in particular Nav 1.7, and are therefore useful for the treatment of diseases treatable by inhibition of these channels, in particular, chronic pain disorders. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds. | 2013-05-23 |
20130131036 | NOVEL TRPV3 MODULATORS - Disclosed herein are modulators of TRPV3 of formula (II): | 2013-05-23 |
20130131037 | 2-(HETEROCYCLYLBENZYL)PYRIDAZINONE DERIVATIVES - Compounds of the formula (I), in which R | 2013-05-23 |
20130131038 | N-CONTAINING HETEROARYL DERIVATIVES AS JAK3 KINASE INHIBITORS - N-containing heteroaryl derivatives of formula I or II, wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as JAK, particularly JAK3, kinase inhibitors. | 2013-05-23 |
20130131039 | 5,7-SUBSTITUTED-IMIDAZO[1,2-C]PYRIMIDINES AS INHIBITORS OF JAK KINASES - Compounds of Formula I: (Formula should be inserted here) and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R | 2013-05-23 |
20130131040 | PYRAZINE KINASE INHIBITORS - Provided are pyrazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibition Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity. | 2013-05-23 |
20130131041 | SPIROCYCLIC COMPOUNDS - The present invention relates to a novel class of substituted spirocyclic compounds. These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the compounds of the instant invention and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of these compounds in vivo. | 2013-05-23 |
20130131042 | SPIROXAZOLIDINONE COMPOUNDS - Substituted spirocyclic amines of structural formula (I) are selective antagonists of the somatostatin subtype receptor 5 (SSTR5) and are useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as Type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, Metabolic Syndrome, depression, and anxiety. | 2013-05-23 |
20130131043 | PYRAZOLE COMPOUNDS AS JAK INHIBITORS - The invention relates to compounds of formula (I) | 2013-05-23 |
20130131044 | SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF - The invention provides compounds of Formula (I) for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc. | 2013-05-23 |
20130131045 | BENZAZEPINE COMPOUND - An object of the present invention is to provide a novel benzazepine compound or a salt thereof, which has excellent vasopressin antagonistic activity. | 2013-05-23 |
20130131046 | NORIBOGAINE COMPOSITIONS - Disclosed are noribogaine compositions comprising a very high level of the 2(R), 4(S), 5(S), 6(S) and 18(R) enantiomer and not more than 0.5 wt % of ibogaine relative to the total amount of noribogaine. | 2013-05-23 |
20130131047 | PHARMACOKINETICALLY IMPROVED COMPOUNDS - The present invention relates to inhibitors of ROCK1 and ROCK2 and methods of modulating the pharmacokinetic and/or pharmacodynamic properties of such compounds. Also provided are methods of inhibiting ROCK1 and or ROCK2 that are useful for the treatment of disease. | 2013-05-23 |
20130131048 | NOVEL PSYCHOTROPIC AGENTS HAVING GLUTAMATE NMDA ACTIVITY - The invention provides novel compounds and pharmaceutical compositions for the treatment of psychological and/or psychiatric diseases or disorders. | 2013-05-23 |
20130131049 | COMPOUNDS FOR THE REDUCTION OF BETA-AMYLOID PRODUCTION - Compounds of formula (I), including pharmaceutically acceptable salts thereof, are set forth herein: | 2013-05-23 |
20130131050 | FUSED HETEROCYCLIC COMPOUND AND APPLICATION THEREOF - The present invention provides a compound useful for the prophylaxis or treatment of eicosanoid-associated diseases such as atherosclerosis, atherothrombosis, diabetes, obesity, asthma, fever, pain, cancer, rheumatism, osteoarthritis, atopic dermatitis and the like, and having superior pharmacological action, physicochemical properties and the like. | 2013-05-23 |
20130131051 | COMPOUNDS FOR THE REDUCTION OF BETA-AMYLOID PRODUCTION - Compounds of formula (I), including pharmaceutically acceptable salts thereof, are set forth herein: | 2013-05-23 |
20130131052 | Amelioration Of The Development Of Cataracts And Other Ophthalmic Diseases - Ophthalmically acceptable compositions used in arresting the development of cataracts or macular degeneration comprising a pharmaceutically acceptable carrier or diluent and a compound having the formula: | 2013-05-23 |
20130131053 | ISOXAZOLINE DERIVATIVES AS PESTICIDES - The invention relates to new isoxazoline compounds of formula | 2013-05-23 |
20130131054 | TETRACYCLIC COMPOUNDS - This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic[4,3-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. | 2013-05-23 |
20130131055 | FUROPYRIDINYL-SUBSTITUTED 1,4-DIHYDROPYRIDINE DERIVATIVES AND METHODS OF USE THEREOF - This invention relates to novel 4-(furo[3,2-c]pyridin-2-yl)-1,4-dihydropyridine derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly cancer and other proliferative disorders. | 2013-05-23 |
20130131056 | POSITIVE ALLOSTERIC MODULATORS (PAM) - The present invention relates to phenylethynyl compounds of formula I | 2013-05-23 |
20130131057 | NEW BICYCLIC COMPOUNDS AS PI3-K AND MTOR INHIBITORS - There is provided compounds of formula (I), wherein A | 2013-05-23 |
20130131058 | 2-SUBSTITUTED-8-ALKYL-7-OXO-7,8-DIHYDROPYRIDO[2,3-D] PYRIMIDINE-6-CARBONITRILES AND USES THEREOF - Compounds according to Formula (I), as well salts thereof: wherein R | 2013-05-23 |
20130131059 | METHOD FOR TREATING OPHTHALMIC DISEASES USING KINASE INHIBITOR COMPOUNDS IN PRODRUG FORMS - This invention is directed to prodrugs of rho kinase (ROCK) inhibitors. These prodrugs are in general the ester or the amide derivatives of the parent compounds. These prodrugs are often weak inhibitors of ROCK, but their parent compounds have good activities. Upon instillation into the eyes, the ester or the amide group of these prodrugs is rapidly hydrolyzed into alcohol, amine, or acid, and the prodrugs are converted into the active base compounds. The prodrugs of ROCK inhibitors provide several advantages such as delivery of higher concentrations of the active species into the target site and reduction of ocular discomfort. The invention is also directed to a method of treating ophthalmic diseases such as glaucoma, allergic conjunctivitis, macular edema, macular degeneration, and blepharitis, by administering an effective amount of a ROCK prodrug compound of Formula I to the eyes of the patient in need of. | 2013-05-23 |
20130131060 | 3-(INDOLYL)- OR 3-(AZAINDOLYL)- 4-ARYLMALEIMIDE COMPOUNDS AND THEIR USE IN TUMOR TREATMENT - The present invention relates to a compound of formula (I) wherein R | 2013-05-23 |
20130131061 | Novel Estrogen Receptor Ligands - The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, carbamate, solvate or salt thereof, including a salt of such an ester, amide or carbamate, and a solvate of such an ester, amide, carbamate or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity, wherein R | 2013-05-23 |
20130131062 | PYRIDAZINONES AND FURAN-CONTAINING COMPOUNDS - The present invention is directed to pyridazinone compounds of formula (I) and furan compounds of formula (II), pharmaceutical compositions of compounds of formula (I) and (II), kits containing these compounds, methods of syntheses, and a method of treatment of a proliferative disease in a subject by administration of a therapeutically effective amount of a compound of formulae (I) or (II). Both classes of compounds were identified through screening of a collection of small molecule libraries. | 2013-05-23 |
20130131063 | Compounds and Methods for Inhibiting the Interaction of BCL Proteins with Binding Partners - The invention relates to isoxazolidine containing compounds that bind to bcl proteins and inhibit Bcl function. The compounds may be used for treating and modulating disorders associated with hyperproliferation, such as cancer. | 2013-05-23 |
20130131064 | Quinuclidine Compounds as Alpha-7 Nicotinic Acetylcholine Receptor Ligands - The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic α7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders. | 2013-05-23 |
20130131065 | TREATMENT OF TYPE 2 DIABETES - The present invention relates to triazine derivatives of Formula I for their use in the treatment of Type 2 diabetes, and to compositions comprising said triazine derivatives. | 2013-05-23 |
20130131066 | TREATMENT OF TYPE 1 DIABETES - The present invention relates to triazine derivatives of formula (I) for their use in the treatment of type 1 diabetes mellitus, and to compositions comprising said triazine derivatives. | 2013-05-23 |
20130131067 | PLANT DISEASE CONTROLLING COMPOSITION AND USE THEREOF - A plant disease controlling composition, containing a carboxamide compound represented by formula (I): | 2013-05-23 |
20130131068 | PHTHALAZINONE KETONE DERIVATIVE, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL USE THEREOF - A phthalazinone ketone derivative as represented by formula (I), a preparation method thereof, a pharmaceutical composition containing the derivative, a use thereof as a poly (ADP-ribose) polymerase (PARP) inhibitor, and a cancer treatment method thereof are described. | 2013-05-23 |
20130131069 | METHOD FOR TREATMENT OF SOLID MALIGNANCIES INCLUDING ADVANCED OR METASTATIC SOLID MALIGNANCIES - The present invention relates to the use of Volasertib or a salt thereof or the hydrate thereof for treating patients suffering from solid malignancies including advanced or metastatic solid malignancies comprising a high frequency administration of Volasertib according to a specific dosage schedule. | 2013-05-23 |
20130131070 | 1-Aryl or 1- Heteroaryl-Pyrido(B)indoles and Uses Thereof - Provided are 1-aryl or 1-heteroaryl substituted beta-carboline compounds or indole analogs thereof having the structure: | 2013-05-23 |
20130131071 | USE OF PTERIDINE DERIVATIVES FOR THE TREATMENT OF INCREASED INTRACRANIAL PRESSURE, SECONDARY ISCHEMIA, AND DISORDERS ASSOCIATED WITH AN INCREASED LEVEL OF CYTOTOXIC REACTIVE OXYGEN SPECIES - The present invention relates to the use of pteridine derivatives for the treatment of increased intracranial pressure, secondary ischemia, and disorders associated with an increased level of cytotoxic reactive oxygen species. | 2013-05-23 |
20130131072 | Methods for Optimizing Clinical Responsiveness to Methotrexate Therapy Using Metabolite Profiling and Pharmacogenetics - The present invention provides methods for optimizing clinical responsiveness to chemotherapy in an individual through genotypic analysis of polymorphisms in at least one gene. The methods of the present invention may further comprise determining the level of at least one long-chain methotrexate polyglutamate (MTXPG) in a sample obtained from the individual. The present invention also provides methods for generating a pharmacogenetic index for predicting clinical responsiveness to chemotherapy in an individual through genotypic analysts of polymorphisms in at least one gene. In addition, the present invention provides methods for optimizing therapeutic efficacy of chemotherapy in an individual by calculating the level of at least one long-chain MTXPG in a sample obtained from the individual. | 2013-05-23 |
20130131073 | FUSED-IMIDAZOYL COMPOUNDS USEFUL AS ANTIMICROBIAL AGENTS - Disclosed are methods of treating microbial infections, comprising administering a compound of Formula (I) Formula I wherein R | 2013-05-23 |
20130131074 | PYRIDONE AND PYRIDAZONE ANALOGUES AS GPR119 MODULATORS - Novel compounds of structure Formula I: | 2013-05-23 |
20130131075 | NEW COMPOUNDS - The present invention relates to the compounds of general formula I | 2013-05-23 |
20130131076 | METHODS AND COMPOSITIONS RELATED TO WRAPPING OF DEHYDRONS - This application describes a novel technology in drug discovery and drug-based imaging/detection: the wrapping technology. This technology is based on identified singularities in the structure of soluble proteins. In contrast with drug-design approaches based on standard structural considerations, the packing of a protein, or more precisely, its dehydron pattern, may be used as a selectivity filter to design small-molecule inhibitors. The wrapping technology described herein is a novel form of rational drug design for avoiding side effects in drug therapy and sharpening the inhibitory impact of drugs on the oncokinome. | 2013-05-23 |
20130131077 | PYRIDO[3,4-B]INDOLES AND METHODS OF USE - This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[3,4-b]indoles are described, as are pharmaceutical-compositions comprising the compounds and 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. | 2013-05-23 |
20130131078 | Carboxamide Compounds And Methods For Using The Same - Disclosed are carboxamide compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure | 2013-05-23 |
20130131079 | FLUFENOXINE DERIVATIVES FOR THE TREATMENT AND PREVENTION OF AMYLOID PATHOLOGIES - The present invention is directed to a compound of formula (I) for use in a method to treat or ameliorate amyloid or tau pathologies, such as Alzheimer's disease, or symptoms thereof. The invention is also directed to new compounds of formula (I), of subformula (II), (III), (IV), or (V). | 2013-05-23 |
20130131080 | Novel Compounds - The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): | 2013-05-23 |
20130131081 | PHARMACEUTICAL COMPOSITIONS INCLUDING CARBAMOYLOXY ARYLALKANOYL ARYLPIPERAZINE COMPOUND - A pharmaceutical composition that includes a carbamoyloxy arylalkanoyl arylpiperazine compound SERUM CHOLESTEROL and effectively prevents or treats diabetic nephropathy, diabetic neuropathy, diabetic vascular complications, hyperlipidemia, coronary artery disease, or inflammation. | 2013-05-23 |
20130131082 | Aminopyrazine Derivative and Medicine - The present invention relates to a compound represented by general formula [1] satisfying the following (I) or (II), or a pharmaceutically acceptable salt of the compound. | 2013-05-23 |
20130131083 | PEST CONTROL COMPOSITION - A pest control composition comprising a hydrazide compound shown by formula (1) below (in the formula, G, M, Q | 2013-05-23 |
20130131084 | USE OF DERIVATIVES OF INDOLES FOR THE TREATMENT OF CANCER - The present invention relates to the use of derivatives of indoles having a general formula (I) as follow: | 2013-05-23 |
20130131085 | CYTOCHROME P450 OXIDASE INHIBITORS AND USES THEREOF - The present invention features compounds of formula I | 2013-05-23 |
20130131086 | METHODS OF USING A G PROTEIN-COUPLED RECEPTOR TO IDENTIFY PEPTIDE YY (PYY) SECRETAGOGUES AND COMPOUNDS USEFUL IN THE TREATMENT OF CONDITIONS MODULATED BY PYY - The present invention relates to methods of using GPR119 receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditions modulated by PYY, such as conditions modulated by stimulation of NPY Y2 receptor (Y2R). Agonists of GPR119 receptor are useful as therapeutic agents for treating or preventing a condition modulated by PYY, such as a condition modulated by stimulation of Y2R. Conditions modulated by PYY such as may be a condition modulated by stimulation of Y2R include bone-related conditions, metabolic disorders, angiogenesis-related conditions, ischemia-related conditions, convulsive disorders, malabsorptive disorders, cancers, and inflammatory disorders. | 2013-05-23 |
20130131087 | Pharmaceutical Compositions - The present invention relates to pharmaceutical compositions and, more particularly, to a pharmaceutical composition containing the compound {1S-[1α, 2α, 3β(1S*,2R*),5β]}-3-(7-{[2-(3,4-difluorophenyl)cyclopropyl]amino}-5-(propylthio)-3H-1,2,3-triazolo[4,5-d]pyrimidin-3-yl)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol. | 2013-05-23 |
20130131088 | TREATING CANCER WITH STATINS AND COMPOUNDS HAVING DIPYRIDAMOLE ACTIVITY - The disclosure pertains to methods of treating a cancer comprising administering to a subject in need thereof an effective amount of a statin in combination with an effective amount of a dipyridamole and/or a compound that has dipyridamole activity. | 2013-05-23 |