| 09th week of 2011 patent applcation highlights part 63 |
| Patent application number | Title | Published |
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| 20110053875 | Macrolide synthesis process and solid-state forms - This invention relates to a method for making macrolides, and, in particular, a method for making optionally substituted 20,23-dipiperidinyl-5-O-mycaminosyl-tylonolide and derivatives thereof, as well as uses of macrolides to make medicaments, methods of treatment using macrolides, and methods for making intermediates that, inter alia, may be used to make macrolides. This invention also relates to solvated and non-solvated crystalline forms of 20,23-dipiperidinyl-5-O-mycaminosyl-tylonolide, as well as methods for making such crystalline forms, medicaments comprising (or derived from) such crystalline forms, methods for making medicaments comprising (or derived from) such crystalline forms, methods of treatment using such crystalline forms, and kits comprising such crystalline forms. | 2011-03-03 |
| 20110053876 | MACROLIDES AND THEIR USE - The invention relates to macrolide compounds of formula (I), the use of said compounds as medicaments, in particular for the treatment or prevention of inflammatory and allergic diseases, pharmaceutical compositions containing said compounds and to processes for their preparation. The invention relates in particular to macrolide compounds with anti-inflammatory activity mediated primarily through inhibition of phosphodiesterase 4 (PDE4) which makes them useful for the treatment and/or prevention of inflammatory and allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rheumatoid arthritis, atopic dermatitis or inflammatory bowel disease or proliferative diseases such as cancer. | 2011-03-03 |
| 20110053877 | NIMESULIDE AND MUSCLE RELAXANT COMBINATIONS THEREOF - A topical pharmaceutical formulation made up of nimesulide or a pharmaceutically acceptable derivative of nimesulide, together with thiocolchicoside or a pharmaceutically acceptable derivative of thiocolchicoside. The present invention more particularly relates to pharmaceutical combinations of nimesulide and thiocolchicoside, in the form of topical gels, ointments, cream, sprays, or lotions with anti-inflammatory, analgesic, and myorelaxant activities. | 2011-03-03 |
| 20110053878 | ACID-SENSITIVE LINKERS FOR DRUG DELIVERY - The invention is in general directed to acid-sensitive linkers, and methods of use thereof, such as, for example, in drug delivery methods. | 2011-03-03 |
| 20110053879 | PICOPLATIN AND AMRUBICIN TO TREAT LUNG CANCER - A method for treatment of lung cancer comprising administration of picoplatin and amrubicin, or comprising radiation therapy and picoplatin is provided. A use of picoplatin in conjunction with amrubicin for treatment of lung cancer is provided. The lung cancer can be SCLC or NSCLC. The cancer can be resistant or refractory to treatment or that progresses following cessation of first-line organoplatinum chemotherapy. The treatment can include the administration of picoplatin and amrubicin, optionally in conjunction with a regimen of best supportive care. Multiple doses of the drug or drug combination can be administered. | 2011-03-03 |
| 20110053880 | COMPOSITION FOR TREATMENT OF TUBERCULOSIS - The invention relates to a pharmaceutical composition comprising a compound preventing EthR from binding to the ethA promoter, for example a compound of formula 1 wherein R | 2011-03-03 |
| 20110053881 | 6-Disubstituted Or Unsaturated Bicyclic Nucleic Acid Analogs - The present disclosure describes 6-disubstituted bicyclic nucleosides, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, the 6-disubstituted bicyclic nucleosides each comprise a 2′-O—C(Ri)(R2)-4′ or 2′-O—C=(R3)(R.4)-4′ bridge wherein each R is, independently a substituent group and Ri and R2 include H. The 6-disubstituted bicyclic nucleosides are useful for enhancing properties of oligomeric compounds including nuclease resistance. In certain embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA. | 2011-03-03 |
| 20110053882 | METHODS AND COMPOUNDS FOR PREVENTING AND TREATING A TUMOUR - The invention relates to a method of preventing, inhibiting, arresting or reversing tumourigenesis in a cell as well as a method of inducing apoptosis in a tumour cell. The method includes increasing the amount and/or the activity of a DACT protein, or a functional fragment thereof, in the cell. Also provided is a pharmaceutical composition that comprises a compound of general formula (I), wherein A is CH or N, R | 2011-03-03 |
| 20110053883 | AGENT THAT MODULATES PHYSIOLOGICAL CONDITION OF PESTS, INVOLVED IN INSECT C-JUN AMINO-TERMINAL KINASE ACTIVITY - The present invention provides an agent that modulates physiological condition of pests, wherein the agent has an ability to modulate the activity of an insect c-Jun NH | 2011-03-03 |
| 20110053884 | POTENT COMBINATIONS OF ZIDOVUDINE AND DRUGS THAT SELECT FOR THE K65R MUTATION IN THE HIV POLYMERASE - Combinations of antiretroviral nucleoside reverse transcriptase inhibitors, and methods for their use in treating retroviral infections, are provided. In one embodiment, the combinations include non-thymidine nucleoside antiretroviral agents, such as tenofovir-DF, abacavir, APD and DAPD, that select for the K65R mutation and relatively low doses of zidovudine (AZT) or other thymidine nucleoside antiretroviral agents. The thymidine nucleoside antiretroviral agents retard development of the K65R mutation, and at the low doses, are less likely to produce side effects. In another embodiment, the combinations include DAPD and AZT. DAPD retards the development of TAMs, and AZT retards the development of the K65R mutation. In a third embodiment, the combinations include adenine, cytosine, thymidine, and guanine nucleoside antiviral agents, in further combination with at least one additional antiviral agent that works via a different mechanism than a nucleoside analog. This combination has the potential to eliminate the presence of HIV in an infected patient. | 2011-03-03 |
| 20110053885 | PHARMACEUTICAL AGENT HAVING LONG-LASTING EFFECT OF TREATING ARTHRITIC DISORDERS - The present invention relates to an injection solution for intra-articular administration for treating arthritic disorders comprising a cross-linked hyaluronic acid derivative wherein part of functional groups of a hyaluronic acid are cross-linked with a cross-linking group to the extent of 0.6 to 15% of cross-linking extent as an active ingredient in an amount having a long-lasting analgesic effect and a pharmaceutically acceptable carrier, and an analgesic composition for suppressing a cartilage degeneration caused by arthritic disorders or a composition for suppressing a cartilage degeneration or an inflammation of synovium caused by arthritic disorders each comprising the cross-linked hyaluronic acid derivative and a pharmaceutically acceptable carrier. | 2011-03-03 |
| 20110053886 | Delayed Self-Gelling Alginate Systems and Uses Thereof - Dispersions that comprise insoluble alginate/gelling ion particles in an alginate solution, wherein the dispersion exhibits less than 10% of final gel storage modulus after one minute in the absence of addition of non-gelling cations are disclosed. Kits and compositions for making such dispersions are disclosed and methods for making and using the dispersions, and the components used in the dispersions are also disclosed. | 2011-03-03 |
| 20110053887 | SOCS3 EXPRESSION PROMOTER, DRUG AND FOOD CONTAINING THE SAME AND METHOD OF PROMOTING THE EXPRESSION OF SOCS3 - A SOCS3 expression promoter includes hyaluronic acid having an average molecular weight of 500,000 or more and/or a salt thereof as an active ingredient. | 2011-03-03 |
| 20110053888 | Mixture Of Carboyhydrates And Its Use In The Preparation Of A Product Intended For Oral Or Enteral Nutrition - The present invention is related to a new mixture of carbohydrates and its usage for the preparation of a food product intended for oral or enteral nutrition, particularly for the nutrition of the diabetic patient and in particular for the nutrition of the diabetes type II patient and their associated comorbidity. The carbohydrate mixture of the present invention is formed by type IV or RS IV (modified maltodextrins) resistant starch, maltodextrin of low dextrose equivalent DE=5-8, preferably DE equal to 6, insulin and cellulose and is exempt from fructose. | 2011-03-03 |
| 20110053889 | Prenatal and postnatal screening and treatment of critical monosaccharide deficiencies for neurologic and immunologic function - A method for determining the effect of critical glyconutrient dietary supplements in premature and term infants on growth, health, and brain function during early childhood development is described. The method comprises determining a critical target nutrient profile in typical samples of preterm and mother's milk, developing a supplement of the missing critical target nutrients to simulate mother's milk, performing an evaluation of early child development by correlating physiologic brain function with cognitive/behavioral brain function in low birth weight premature and term infants, assessing family influence and home environment on developmental outcome on infants under treatment, and comparing term siblings of low birth weight premature vs. term babies. A composition having the critical nutrients, an algorithm for screening and treatment, and a useful kit for employing the above are also described. | 2011-03-03 |
| 20110053890 | SYNTHETIC ANALOGS OF BACTERIAL QUORUM SENSORS - Bacterial quorum-sensing molecule analogs having the following structures: | 2011-03-03 |
| 20110053891 | 5-FLUOROPYRIMIDINONE DERIVATIVES - This present disclosure is related to the field of 5-fluoropyrimidinones and their derivatives and to the use of these compounds as fungicides. | 2011-03-03 |
| 20110053892 | Imidazo[4,5-d]Pyridazine Compounds For Treating Viral Infections - Disclosed are compounds and compositions of Formula (I), pharmaceutically acceptable salts and solvates thereof, and their preparation and uses for treating viral infections mediated at least in part by a virus in the Flaviviridae family of viruses: | 2011-03-03 |
| 20110053893 | COMPOUNDS AND COMPOSITIONS AS TLR ACTIVITY MODULATORS - The invention provides a novel class of compounds, immunogenic compositions and pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with Toll-Like Receptors 7. In one aspect, the compounds are useful as adjuvants for enhancing the effectiveness of a vaccine. | 2011-03-03 |
| 20110053894 | Broad Spectrum Antiviral and Methods of Use - A method for the prevention or treatment of Influenza virus infection or Adenovirus infection by administering an effective amount of a compound of Formula (I), Formula (II), or similar compound to an individual in need is provided. | 2011-03-03 |
| 20110053895 | USE OF MITOCHONDRIALLY-ADDRESSED COMPOUNDS FOR PREVENTING AND TREATING CARDIOVASCULAR DISEASES - The invention relates to pharmacology and medicine, in particular to a class of mitochondrially-addressed compounds which can be used in the pharmaceutical compositions of medicinal agents (preparations) for preventing and treating cardiovascular diseases and diseases and pathological conditions caused by disturbed blood circulation or oxygen supply to tissues and organs. | 2011-03-03 |
| 20110053896 | OSMOLYTES FOR THE TREATMENT OF ALLERGIC OR VIRAL RESPIRATORY DISEASES - The present invention relates to the use of osmolytes for treating allergic or viral respiratory diseases, e.g. allergic rhinitis (hay fever) as well as rhinovirus and/or adenovirus infections. The invention also relates to a medicament preparation containing one or more compounds from the group of osmolytes. The group of osmolytes used in the invention comprises various low-molecular substances , more specifically ectoine, 4,5,6,7-tetrahydro-2-methyl-1H-[1, 3]-diazepine-4-S-carboxylic acid (homoectoine), hydroxyectoine, di-myo-inositol-phosphate (DIP), to cyclic 2,3-diphosphoglycerate (cDPG), 1,1-diglycerol phosphate (DGP), β-mannosylglycerate (firoin), β-mannosylglyceramide (firoin-A), dimannosyl-diinositol phosphate (DMIP), glucosylglycerol, taurine, betaine, citrulline, and/or a derivative, e.g. an acid, salt, or ester of said compounds. | 2011-03-03 |
| 20110053897 | COMPOUNDS AND COMPOSITIONS AS SYK KINASE INHIBITORS - Provided herein area novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated Syk kinase activity. | 2011-03-03 |
| 20110053898 | TOPICAL COMPOSITION COMPRISING VITAMIN D ANALOGUE AND CORTICOSTEROIDS - A topical pharmaceutical composition comprising therapeutically effective amounts of vitamin D or vitamin D analogues, corticosteroid and a straight chain C | 2011-03-03 |
| 20110053899 | USE OF LANOSTANE AND PORIA EXTRACT IN TREATING DIABETES - A pharmaceutical composition for treating diabetes is provided in this invention. The composition contains a lanostane compound as a potent component. A suitable source of the lanostane compound is a | 2011-03-03 |
| 20110053900 | PROGESTERONE ANTAGONISTS SUCH AS CDB-4124 IN THE TREATMENT OF BREAST CANCER - The subject matter of the instant invention is pertinent to the field of cancer treatment. In particular, the instant invention is relevant to the treatment and/or prevention of breast cancer in a patient. Compositions for practicing the methods, comprising selective progesterone receptor modulators, which function as progesterone agonists in the uterus and as progesterone antagonists in the breast tissue and exhibit only low affinity for glucocorticoid and estrogen receptors, are also disclosed. Embodiments of the instant invention also disclose methods for preventing the development of breast cancer in patients undergoing hormone replacement therapy or estrogen therapy. | 2011-03-03 |
| 20110053901 | ACETYL MIMIC COMPOUNDS FOR THE INHIBITION OF ISOPRENYL-S-CYSTEINYL METHYLTRANSFERASE - Among other things, the present invention provides novel compounds capable of effectively inhibiting inflammatory responses that are mediated by G-proteins or GPCRs in neutrophils, macrophages and platelets. In particular, compounds of the present invention act as inhibitors of edema, inhibitors of erythema and inhibitors of MPO (myeloperoxidase), pharmaceutical compositions containing the same compounds and the use thereof for the treatment of diseases that may benefit from edema, erythema and MPO inhibition, such as inflammation (acute or chronic), asthma, autoimmune diseases, and chronic obstructive pulmonary disease (COPD) (e.g., emphysema, chronic bronchitis and small airways disease, etc.), inflammatory responses of the immune system, skin diseases (e.g., reducing acute skin irritation for patients suffering from rosacea, atopic dermatitis, seborrheic dermatitis, psoriasis), irritable bowel syndrome (e.g., Chron's disease and ulcerative colitis, etc.), and central nervous system disorders (e.g., Parkinson's disease). | 2011-03-03 |
| 20110053902 | AMINO DERIVATIVES OF ANDROSTANES AND ANDROSTENES AS MEDICAMENTS FOR CARDIOVASCULAR DISORDERS - Compounds of formula (I) wherein: the groups are as defined in the description, are useful for the preparation of medicaments for the treatment of cardiovascular disorders, in particular heart failure and hypertension. The compounds are inhibitors of the enzymatic activity of the Na | 2011-03-03 |
| 20110053903 | PHARMACEUTICAL COMPOSITIONS BASED ON AZETIDINE DERIVATIVES - A stable pharmaceutical composition comprising azetidine compound of formula (Ib): | 2011-03-03 |
| 20110053904 | CARBOCYCLIC GLYT1 RECEPTOR ANTAGONISTS - The present invention relates to the use of a compound of formula I | 2011-03-03 |
| 20110053905 | COMPOUNDS AS TYROSINE KINASE MODULATORS - The present invention is directed to novel compounds of Formula I. The compounds of the present invention are potent tyrosine kinase modulators, and are suitable for the treatment and prevention of diseases and conditions related to abnormal activities of tyrosine kinase receptors. | 2011-03-03 |
| 20110053906 | PROTEIN KINASE INHIBITORS AND USE THEREOF - Disclosed are benzonaphthyridinyl derivative 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 kinase signal transduction inhibition, regulation or modulation. | 2011-03-03 |
| 20110053907 | SUBSTITUTED PYRIMIDINES AND TRIAZINES AND THEIR USE IN CANCER THERAPY - Provided herein are substituted pyrimidine and triazine derivatives, including bicyclic pyrimidine derivatives, their pharmaceutical compositions, their preparation, and their use as agents or drugs for cancer therapy, either alone or in combination with radiation and/or other anticancer drugs. In one embodiment, the pyrimidine and triazine derivatives are morpholino-pyrimidine, morpholino-triazine, pyridyl-pyrimidine, and pyridyl-triazine derivatives which are selective irreversible inhibitors of the p110α isoform of PI3K. | 2011-03-03 |
| 20110053908 | AZETIDINE-DERIVED COMPOUNDS, PREPARATION METHOD THEREFOR AND THERAPEUTIC USE OF SAME - This disclosure relates to compounds of formula (I): | 2011-03-03 |
| 20110053909 | Compounds - 801 - Spirocyclic amide derivatives of formula I | 2011-03-03 |
| 20110053910 | 2 -HETEROCYCLYLOXYBENZOYL AMINO HETEROCYCLYL COMPOUNDS AS MODULATORS OF GLUCOKINASE FOR THE TREATMENT OF TYPE 2 DIABETES - Compounds of formula (I) | 2011-03-03 |
| 20110053911 | TRICYCLIC DERIVATIVES AS INHIBITORS OF POLY(ADP-RIBOSE) POLYMERASE (PARP) - The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts or tautomers thereof which are inhibitors of poly(ADP-ribose)polymerase (PARP) and thus useful for the treatment of cancer, inflammatory diseases, reperfusion injuries, ischaemic conditions, stroke, renal failure, cardiovascular diseases, vascular diseases other than cardiovascular diseases, diabetes mellitus, neurodegenerative diseases, retroviral infections, retinal damage, skin senescence and UV-induced skin damage, and as chemo- or radiosensitizers for cancer treatment. | 2011-03-03 |
| 20110053912 | PYRIMIDINE COMPOUND - A novel and excellent method for preventing and/or treating diseases related to a cannabinoid type 2 receptor, based on an agonistic action on a cannabinoid type 2 receptor. It was found that a hetero ring derivative mainly having two substituents, for example, a pyrimidine-5-carboxamide derivative having a substituent amino group at the 2-position, exhibits a potent agonistic action on a cannabinoid type 2 receptor, and can be an agent for preventing and/or treating diseases related to a cannabinoid type 2 receptor such as inflammatory diseases, pain, and the like. | 2011-03-03 |
| 20110053913 | Methods and Therapies for Alleviating Pain - A method for alleviating or delaying onset of pain in a subject via administration of an ultra low dose of alpha-2 receptor antagonist which does not significantly block or inhibit alpha-2 receptor activity is provided. A non-selective alpha-2 receptor antagonist or a selective alpha-2A receptor antagonist may be administered. | 2011-03-03 |
| 20110053914 | Pharmaceutical Combination Comprising 6-Dimethylaminomethyl-1-(3-methoxy-phenyl)-cyclohexane-1,3-diol or 6-Dimethylaminomethyl-1-(3-hydroxy-phenyl)-cyclohexane-1,3-diol and an Antiepileptic - A pharmaceutical combination comprising: | 2011-03-03 |
| 20110053915 | HETEROCYCLIC INHIBITORS OF AN Hh-SIGNAL CASCADE, MEDICINAL COMPOSITIONS BASED THEREON AND METHODS FOR TREATING DISEASES CAUSED BY THE ABERRANT ACTIVITY OF AN Hh-SIGNAL SYSTEM - The invention relates to novel heterocyclic compounds and to the use thereof, to pharmaceutical compositions containing said chemical compounds as an active ingredient and to the use thereof for producing medicinal preparations for the human being and warm-blood animals for treating diseases caused by the aberrant activity of an Hedgehog (Hh)-signal system, in particular oncological diseases. The invention also relates to the use of the above-mentioned compounds in the form of ‘molecular pharmacological tools’ for examining (in vitro and in vivo) the biochemical features of the Hh-signal system, in particular, the interaction of Hh protein and transmembrane proteins, namely, suppressor Patched (Ptc) and protooncogenic proteins. The eight groups of the claimed compounds comprise the derivatives of 2,6-dihydro-7H-pyrazolo[3,4-d]pyridazine-7-one and 1,4-dihydropyrazolo[3,4-b][1,4]thiazine-5-one; N-acidylated 4-imidazo[1,2-a]pyrimidine-2-il-anilines; ([4H-thino[3,2-b]pyrrol-5-il) carbonyl]piperidine-4-carbonic acid amides; 2-(4carbomoilpyperidine-1-il)-isonicotinic acid amides; N-sylphonyl-1,2,3,4-tetrahydroquinoline-6-carbonic acid amides; and pyridine 2-amino-4,5,6,7-tetrahydrothieno[2,3-c] N-acidylated 3-azole derivatives. | 2011-03-03 |
| 20110053916 | PYRIMIDINE COMPOUNDS AS TUBERCULOSIS INHIBITORS - The present invention relates to compounds useful as inhibitors of treating tuberculosis. The invention also provides processes for preparing compounds of the inventions and | 2011-03-03 |
| 20110053917 | Allosteric Modulators of the A1 Adenosine Receptor - The present invention provides compounds of formula (I) | 2011-03-03 |
| 20110053918 | GAMMA SECRETASE MODULATORS - In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions. | 2011-03-03 |
| 20110053919 | Active Compound Combinations Having Insecticidal and Acaricidal Properties - The novel active compound combinations comprising a compound of the formula (I) or (II) and the active compounds (1) to (6) listed in the description have very good insecticidal and acaricidal properties. | 2011-03-03 |
| 20110053920 | SUBSTITUTED BICYCLIC PYRIMIDINES - The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions that include substituted heterobicyclic pyrimidines of Formula (I): | 2011-03-03 |
| 20110053921 | HEXAHYDROOXAZINOPTERINE COMPOUNDS - The present invention provides mTOR inhibitors of the formula | 2011-03-03 |
| 20110053922 | Spiro (Piperidine-4,2'-Pyrrolidine)-1-(3,5-Trifluoromethyl Phenyl) Methylcarboxamides As NK1 Tachikynin Receptor Antagonists - Compounds of formula (I) or a pharmaceutically acceptable salt thereof | 2011-03-03 |
| 20110053923 | CHEMICAL COMPOUNDS 610 - There is provided pyrimidinyl indole compounds of Formula (I), | 2011-03-03 |
| 20110053924 | SUBSTITUTED PIPERIDINES AS RENIN INHIBITORS - The present invention relates to compounds of the general formula (I) and the salts thereof, preferably the pharmaceutically acceptable salts thereof; in which R has the meaning explained in the description, a process for their preparation and the use of these compounds as medicines, especially as renin inhibitors. | 2011-03-03 |
| 20110053925 | Hydroxamate-Based Inhibitors of Deacetylases - The present teachings relate to compounds of Formula I: | 2011-03-03 |
| 20110053926 | New Pharmaceutically-Active Compounds for the Treatment of Respiratory Diseases - The present invention relates to the use of the compounds of general formula 1 | 2011-03-03 |
| 20110053927 | NANOPARTICLE FORMATION VIA RAPID PRECIPITATION - The invention encompasses a method for making nano-sized particles of water-insoluble pharmaceuticals comprising: (1) dissolving the water-insoluble pharmaceutical in a water-miscible solvent, optionally with water and inactive pharmaceutical ingredients, to make a solution; (2) rapidly mixing the solution with an anti-solvent which creates a high level of supersaturation, wherein the anti-solvent is water with optional inactive pharmaceutical ingredients; (3) simultaneously applying energy to the resulting mixture during the mixing of solution and anti-solvent as nano-sized drug particles precipitate out and form a slurry mixture under supersaturation; and (4) optionally isolating the nano-sized particles of water-insoluble pharmaceuticals from the slurry mixture. | 2011-03-03 |
| 20110053928 | PYRIMIDOTHIENOINDAZOLES - The invention relates to novel pyrimidothienoindazoles of formula (I), processes for their preparation and their use for preparing medicaments for the treatment or prophylaxis of disorders, especially of hyperproliferative disorders. | 2011-03-03 |
| 20110053929 | IMIDAZO-, PYRAZOLOPYRAZINES AND IMIDAZOTRIAZINES AND THEIR USE - The invention relates to substituted imidazo-, pyrazolopyrazines and imidazotriazines and processes for their preparation, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, in particular of hematological disorders, preferably of leukopenias and neutropenias. | 2011-03-03 |
| 20110053930 | INHIBITORS OF THE BMP SIGNALING PATHWAY - The present invention provides small molecule inhibitors of BMP signaling. These compounds may be used to modulate cell growth, differentiation, proliferation, and apoptosis, and thus may be useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation. | 2011-03-03 |
| 20110053931 | QUINOLINE COMPOUNDS AND METHODS OF USE - Compounds of Formula (I), and stereoisomers, geometric isomers, tautomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof, are useful for inhibiting receptor tyrosine kinases and for treating hyperproliferative disorders mediated thereby. Methods of using compounds of Formula (I), and stereoisomers, geometric isomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed. | 2011-03-03 |
| 20110053932 | Protein Kinase Inhibitors and Methods for Using Thereof - The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, and methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of Alk, Abl, Aurora-A, B-Raf, C-Raf, Bcr-Abl, BRK, Blk, Bmx, BTK, C-Kit, C-Raf, C-Src, EphB1, EphB2, EphB4, FGFR1, FGFR2, FGFR3, FLT1, Fms, Flt3, Fyn, FRK3, JAK2, KDR, Lck, Lyn, PDGFRα, PDGFRβ, PKCα, p38, Src, SIK, Syk, Tie2 and TrkB kinases. | 2011-03-03 |
| 20110053933 | HYDROXYQUINOXALINECARBOXAMIDE DERIVATIVE - The present invention provides a novel hydroxyquinoxaline carboxamide derivative that is useful for preventing and/or treating blood coagulation disorders. A compound represented by formula (i), or a pharmacologically acceptable salt thereof: | 2011-03-03 |
| 20110053934 | COMPOUNDS AND METHODS OF TREATMENT - A derivative, which is useful as a ret kinase inhibitor is described herein. The described invention also includes methods of using the same in the treatment of diseases mediated by inappropriate ret kinase activity. | 2011-03-03 |
| 20110053935 | FUSED PYRIDINES ACTIVE AS INHIBITORS OF C-MET - Fused pyridines of formula (I) and the pharmaceutically acceptable salts thereof have activity as inhibitors of c-Met and may thus be used to treat various diseases and disorders including cancer. Processes for synthesizing the compounds are also described. | 2011-03-03 |
| 20110053936 | SUBSTITUTED SPIRO[CYCLOALKYL-1,3'-INDOL]-2'(1'H)-ONE DERIVATIVES AND THEIR USE AS P38 MITOGEN-ACTIVATED KINASE INHIBITORS - The present disclosure is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I), processes for preparation thereof, pharmaceutical compositions thereof, and methods of use thereof. | 2011-03-03 |
| 20110053937 | Inhibitors of the Interaction Between MDM2 and P53 - The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I) | 2011-03-03 |
| 20110053938 | Compounds and Compositions For Treating Cancer - The invention relates to compounds and composition for the treatment and prevention of cancer. The invention also covers all diseases that may be treated by selective modulation of levels of reactive oxygen species in diseased cells versus normal cells. Methods for the preparation and administration of such compositions are also disclosed. | 2011-03-03 |
| 20110053939 | NOVEL AROMATIC NITRO COMPOUNDS - Pharmaceutical compositions comprising at least one compound of e.g. the formulas (Ie) and a pharmaceutically acceptable carrier which is useful in a medicine wherein the symbols and substituents have the following meaning—X— is e.g. and Y is e.g. or the pharmaceutically acceptable salts, esters or amides and prodrugs of the above identified compounds can be applied to modulate the in-vitro and in-vivo binding processes mediated by E-, P- or L-selectin binding. | 2011-03-03 |
| 20110053940 | 3,4-SUBSTITUTED PIPERIDINE DERIVATIVES AS RENIN INHIBITORS - The present invention relates to 3,4-substituted piperidinyl-based renin inhibitor compounds bearing at 4-position oxopyridine and having the formula (I). The invention further relates to pharmaceutical compositions containing said compounds, as well as their use in treating cardiovascular events and renal insufficiency. | 2011-03-03 |
| 20110053941 | IDO Inhibitors - Presently provided are methods for (a) modulating an activity of indoleamine 2,3-dioxygenase comprising contacting an indoleamine 2,3-dioxygenase with a modulation effective amount of a compound as described in one of the aspects described herein; (b) treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression in a subject in need thereof, comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (c) treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (d) enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent and a compound as described in one of the aspects described herein; (e) treating tumor-specific immunosuppression associated with cancer comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; and (f) treating immunosuppression associated with an infectious disease, e.g., HIV-I infection, comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount a compound as described in one of the aspects described herein. | 2011-03-03 |
| 20110053942 | ORALLY DISINTEGRATING TABLETS - The present invention relates to an orally disintegrating tablet containing (1) an active ingredient, (2) mannitol, (3) crystalline cellulose and (4) at least two kinds of particular ingredients selected from the group consisting of low-substituted hydroxypropylcellulose, cornstarch and carmellose, wherein the blending ratio of each ingredient relative to 100 wt % of the disintegrating tablet is (1) 0.01 to 50 wt %, (2) 20 to 86 wt %, (3) 10 to 30 wt %, and (4) 1 to 20 wt % for each particular ingredient and 3 to 60 wt % as the total of the particular ingredients to be blended, and an assembly of (3) crystalline cellulose to be blended has a bulk density of not more than 0.18 g/cm | 2011-03-03 |
| 20110053943 | CARBAMATE AND UREA INHIBITORS OF 11 -HYDROXYSTEROID DEHYDROGENASE 1 - This invention relates to novel compounds of the invention pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell. | 2011-03-03 |
| 20110053944 | SUBSTITUTED DIHYDROPTERIDIN-6-ONE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS - Dihydropteridin-6-one derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, 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 disregulated protein kinase activity, like cancer. | 2011-03-03 |
| 20110053945 | SALTS OF 6-(5-CHLORO-2-PYRIDYL)-5-[(4-METHYL-1-PIPERAZINYL)CARBONYLOXY]-7-- OXO-6,7-DIHY-DRO-5H-PYRROLO[3,4-B]PYRAZINE - Novel mesylate, (R)-mandelate, succinate, citrate, fumarate, D-malate, D-tartrate, sulfate and L-tartrate salts of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) are provided. | 2011-03-03 |
| 20110053946 | Aryl-Quinolyl Compounds and Their Use - The present invention pertains generally to the field of therapeutic compounds for treating proliferative disorders, cancer, etc., and more specifically to certain aryl-quinolyl compounds, as described herein, which, inter alia, inhibit RAF (e.g., B-RAF) activity. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., BRAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and disorders that are ameliorated by the inhibition of RAF, RTK, etc., proliferative disorders such as cancer (e.g., colorectal cancer, melanoma), etc. | 2011-03-03 |
| 20110053947 | Arylchalcogenoarylalkyl-substituted imidazolidine-2,4-diones, process for preparation thereof, medicaments comprising these compounds and use thereof - The invention relates to compounds of formula (I) wherein the groups R and R′, A, D, E, G, L, p and R1 to R10 have the stated meanings and to their physiologically compatible salts. Said compounds are suitable, for example, as anti-obesity drugs. | 2011-03-03 |
| 20110053948 | PYRROLIDINES AS NK3 RECEPTOR ANTAGONISTS - The present invention relates to a compounds of formula I | 2011-03-03 |
| 20110053949 | 4-[3-(ARYLOXY)BENZYLIDENE]-3-METHYL PIPERIDINE ARYL CARBOXAMIDE COMPOUNDS USEFUL AS FAAH INHIBITORS - The present invention relates to compounds of Formula (I), wherein Ar is optionally substituted phenyl or heteroaryl and X, Y and Z are independently N or CH; or a pharmaceutically acceptable salt thereof; processes for the preparation of the compounds; intermediates used in the preparation of the compounds; compositions containing the compounds; and uses of the compounds in treating diseases or conditions associated with fatty acid amide hydrolase (FAAH) activity. | 2011-03-03 |
| 20110053950 | 4-BENZYLIDENE-3-METHYLPIPERIDINE ARYL CARBOXAMIDE COMPOUNDS USEFUL AS FAAH INHIBITORS - The present invention relates to compounds of Formula (I) wherein Ar is optionally substituted phenyl or heteroaryl; or a pharmaceutically acceptable salt thereof; processes for the preparation of the compounds; intermediates used in the preparation of the compounds; compositions containing the compounds; and uses of the compounds in treating diseases or conditions associated with fatty acid amide hydrolase (FAAH) activity. | 2011-03-03 |
| 20110053951 | METHODS FOR TREATING DISORDERS USING NMDA NR2B-SUBTYPE SELECTIVE ANTAGONIST - A method of treating, preventing or ameliorating a disease or condition by inhibiting NR2B subunit containing NMDA receptors using a compound according to formula (I) or a pharmaceutically acceptable salt thereof: | 2011-03-03 |
| 20110053952 | 2-HETEROARYLAMINO-PYRIMIDINE DERIVATIVES AS KINASE INHIBITORS - The invention provides compounds of Formula (I) and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit, PDGFRα, PDGFRβ, CSF1R, Abl, BCR-Abl, CSK, JNK1, JNK2, p38, p70S6K, TGFβ, SRC, EGFR, trkB, FGFR3, Fes, Lck, Syk, RAF, MKK4, MKK6, SAPK2β, BRK, Fms, KDR, c-raf or b-raf kinases. | 2011-03-03 |
| 20110053953 | AZA-Isoindolones and Their Use as Metabotropic Glutamate Receptor Potentiators - 613 - Compounds of formula I: wherein R | 2011-03-03 |
| 20110053954 | METHOD OF TREATMENT AND/OR PREVENTION OF BRAIN, SPINAL OR NERVE INJURY - The invention relates to a method of treatment and/or prevention of brain, spinal or nerve injury comprising administration to a person in need of such treatment, of a therapeutically effective amount of an NK-1 receptor antagonist compound of the formula | 2011-03-03 |
| 20110053955 | ANTI-CYTOKINE HETEROCYCLIC COMPOUNDS - Heterocyclic compounds which are inhibitors of Mitrogen-Activated Protein Kinase-Activated Protein Kinase-2 (MAPKAP-K2) as described, in addition to their use in the treatment of cytokine mediated diseases. | 2011-03-03 |
| 20110053956 | Treatment for Neurological and Mental Disorders - Methods for treating neurological or mental disorders in humans and the symptoms associated therewith are provided by administering eltoprazine and/or related compounds. In some embodiments, specific symptoms are treated by administering eltoprazine and/or a related compound in an effective amount to ameliorate the symptoms. Of particular significance are symptoms that are associated with cognitive dysfunction where eltoprazine will improve the symptoms and the disorder associated with that symptom. Of particular interest are non-ADHD-associated inattention, hyperactivity and impulsiveness. The methods provided herein are especially useful for improving functional recovery after CNS injury such as stroke where improved cognitive function will facilitate the acquisition of learning and memory of rehabilitative tasks. | 2011-03-03 |
| 20110053957 | MALONATE SALT OF 4-((1R,3S)-6-CHLORO-3-PHENYLINDAN-1-YL)-1,2,2-TRIMETHYLPIPERAZINE AND USES OF SAME - 4-((1R,35)-6-Chloro-3 -phenylindan-1-yl)-1,2,2-trimethylpiperazine hydrogen malonate salt and pharmaceutical comprising and uses of the same, including for the treatment of schizophrenia and other psychotic disorders are described. | 2011-03-03 |
| 20110053958 | MODULATORS OF THE PROSTACYCLIN (PGI2) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO - The present invention relates to amide derivatives of Formula (XIIIa) and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pulmonary arterial hypertension (PAH); idiopathic PAH; familial PAH; PAH associated with a collagen vascular disease, a congenital heart disease, portal hypertension, HIV infection, ingestion of a drug or toxin, hereditary hemorrhagic telangiectasia, splenectomy, pulmonary veno-occlusive disease (PVOD) or pulmonary capillary hemangiomatosis (PCH); PAH with significant venous or capillary involvement; platelet aggregation; coronary artery disease; myocardial infarction; transient ischemic attack; angina; stroke; ischemia-reperfusion injury; restenosis; atrial fibrillation; blood clot formation in an angioplasty or coronary bypass surgery individual or in an individual suffering from atrial fibrillation; atherosclerosis; atherothrombosis; asthma or a symptom thereof; a diabetic-related disorder such as diabetic peripheral neuropathy, diabetic nephropathy or diabetic retinopathy; glaucoma or other disease of the eye with abnormal intraocular pressure; hypertension; inflammation; psoriasis; psoriatic arthritis; rheumatoid arthritis; Crohn's disease; transplant rejection; multiple sclerosis; systemic lupus erythematosus (SLE); ulcerative colitis; ischemia-reperfusion injury; restenosis; atherosclerosis; acne; type 1 diabetes; type 2 diabetes; sepsis; and chronic obstructive pulmonary disorder (COPD). | 2011-03-03 |
| 20110053959 | PYRIMIDYL CYCLOPENTANES AS AKT PROTEIN KINASE INHIBITORS - The present invention provides compounds of Formula (I) including tautomers, resolved enantiomers, resolved diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Also provided are methods of using the compounds of this invention as Akt protein kinase inhibitors and for the treatment of Akt-mediated diseases, for example, hyperproliferative diseases such as cancer. | 2011-03-03 |
| 20110053960 | METHOD FOR TREATING PAIN SYNDROME AND OTHER DISORDERS - The present invention provides the use of certain compounds to treat peripheral or central pain syndrome and other disorders associated with the T-type calcium ion channels. | 2011-03-03 |
| 20110053961 | SUBSTITUTED XANTHINE DERIVATIVES - This invention relates to novel compounds that are substituted xanthine derivatives and pharmaceutically acceptable salts thereof. For example, this invention relates to novel substituted xanthine derivatives that are derivatives of pentoxifylline. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions for which pentoxifylline and related compounds are beneficial. | 2011-03-03 |
| 20110053962 | AZAINDOLE DERIVATIVES WITH A COMBINATION OF PARTIAL NICOTINIC ACETYL-CHOLINE RECEPTOR AGONISM AND DOPAMINE REUPTAKE INHIBITION - Azaindole derivatives of formula (I): | 2011-03-03 |
| 20110053963 | TARTRATE SALTS OF QUINAZOLINE BASED EGFR INHIBITORS CONTAINING A ZINC BINDING MOIETY - The present invention relates to tartrate salts of quinazoline containing zinc-binding moiety based derivatives of Formula II, below. | 2011-03-03 |
| 20110053964 | 4-AMINOQUINAZOLINE DERIVATIVES AND METHODS OF USE THEREOF - This invention relates to novel 4-aminoquinazolines and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering inhibitors of the EGFR and HER-2. | 2011-03-03 |
| 20110053965 | SULFONATED PRECURSORS OF THYMIDINE FOR THE TREATMENT OF EPITHELIAL HYPERPLASIAS - This invention relates to pharmaceutical compositions comprising a sulfonated biological precursor of thymidine, such as a precursor of 4-thiothymidine (4-TT), and their use in the photodynamic treatment of skin hyperplasias, including cancer, psoriasis, actinic keratosis and keloids, by topical or systemic administration. | 2011-03-03 |
| 20110053966 | SYNERGISTIC FUNGICIDAL COMPOSITIONS CONTAINING A 5-FLUOROPYRIMIDINE DERIVATIVE FOR FUNGAL CONTROL IN CEREALS - A fungicidal composition containing a fungicidally effective amount of a) a compound of Formula IA and/or IB and (b) at least one fungicide selected from the group consisting of epoxiconazole, prothioconazole, azoxystrobin, pyraclostrobin, penthiopyrad, isopyrazam, bixafen, boscalid, prochloraz, chlorothalanil, isobutyric acid (3S,6S,7R,8R)-8-benzyl-3-[(3-isobutyryloxymethoxy-4-methoxypyridine-2-carbonyl)-amino]-6-methyl-4,9-dioxo-[1,5]dioxonan-7-yl ester, and (5,8-difluoroquinazolin-4-yl)-{2-[2-fluoro-4-(4-trifluoromethylpyridin-2-yloxy)-phenyl]-ethyl}-amine provides synergistic control of selected fungi. | 2011-03-03 |
| 20110053967 | (POLY) AMINOACETAMIDE DERIVATIVES OF EPIPODOPHYLLOTOXIN THEIR PROCESS OF PREPARATION AND THEIR APPLICATIONS IN THERAPEUTICS AS ANTICANCER AGENTS - The present invention relates to novel podophyllotoxin derivatives substituted in the 4-position by a substituted (poly)aminoalkylaminoacetamide chain, to their process of preparation and to their use as medicament as anticancer agents. | 2011-03-03 |
| 20110053968 | AMINOPYRIMIDINE INHIBITORS OF TYROSINE KINASE - The present invention relates to new aminopyrimidine inhibitors of tyrosine kinase activity, pharmaceutical compositions thereof, and methods of use thereof | 2011-03-03 |
| 20110053969 | NOVEL DIAZASIPIROAKANES AND THEIR USE FOR TREATMENT OF CCR8 MEDIATED DISEASES - The invention provides compounds of general formula. (II) wherein R and | 2011-03-03 |
| 20110053970 | Spirocyclic Cyclohexane Compounds Useful To Treat Substance Dependency - Spirocyclic cyclohexane compounds useful in pharmaceutical compositions for use in the treatment of substance dependency. | 2011-03-03 |
| 20110053971 | NALMEFENE DI-ESTER PRODRUGS - The present invention relates to prodrugs of nalmefene of formula (I), pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of substance abuse disorders such as alcohol abuse and alcohol dependence and impulse control disorders such as pathological gambling and addiction to shopping. | 2011-03-03 |
| 20110053972 | INHIBITORS OF AKT ACTIVITY - Invented are novel heterocyclic carboxamide compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis. | 2011-03-03 |
| 20110053973 | COMPOUNDS AS TYROSINE KINASE MODULATORS - The present invention is directed to novel compounds of Formula I. The compounds of the present invention are potent tyrosine kinase modulators, and are suitable for the treatment and prevention of diseases and conditions related to abnormal activities of tyrosine kinase receptors. | 2011-03-03 |
| 20110053974 | CARBOXYLIC ACID COMPOUND - To find a therapeutic agent and/or a preventive agent for diabetes mellitus or the like having excellent activity and safety. A compound represented by the following general formula (I), or a pharmacologically acceptable salt thereof. In the formula, X represents ═C(R5)- or ═N—; Y represents —O— or —NH—; L represents a bond or a substitutable C1-C3 alkylene group; M represents a substitutable C3-C10 cycloalkyl group, a substitutable C6-C10 aryl group, or a substitutable heterocyclic group; R | 2011-03-03 |
