| 30th week of 2011 patent applcation highlights part 45 |
| Patent application number | Title | Published |
|---|
| 20110183940 | CHEMICAL COMPOUNDS - The present invention features compounds that are prodrugs of HIV integrase inhibitors and therefore are useful in the delivery of compounds for the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC. | 2011-07-28 |
| 20110183941 | Herbicide consisting of a glyphosate formulation containing a surfactant consisting in a branched alkyl alcohol polyethoxylated or polypropoxylated and a mixture of alkylamines - Linear alkyl amine polyethoxylated containing in the alkyl chain 16 to 20 carbon atoms are worldwide used as surfactants for herbicides based on glyphosate. | 2011-07-28 |
| 20110183942 | Methods and Compositions for Treating Alzheimer's Disease - A method is disclosed for inhibiting the build-up of amyloid plaques in the brain of a patient with at least one risk factor for, or a diagnosis of, Alzheimer's Disease by administering to the patient an amount of one or more compounds effective to inhibit the phosphorylative activity of eEF2K, thereby inhibiting amyloid plaque deposition. | 2011-07-28 |
| 20110183943 | CONCURRENT THERAPY REGIME/REGIMEN FOR THE TREATMENT OF ACNE RELATED DISEASES - A novel therapy regime/regimen for the treatment of acne related diseases includes administering a topical fixed-dose combination of a retinoid and an anti-bacterial agent, such as BPO, to a course of oral antibiotic therapy. | 2011-07-28 |
| 20110183944 | SUSTAINED-RELEASE NSAID/HMG CoA REDUCTASE INHIBITOR COMPOSITIONS - Compositions for controlled release of one or more therapeutic agents where the composition is essentially free of excipients are disclosed. In particular, compositions comprising a HMG-CoA reductase inhibitor, particularly simvastatin, and a NSAID, such as a COX-2 inhibitor, particularly celecoxib, in which greater than 90% of the weight of the composition is made up of the HMG-CoA reductase inhibitor and NSAID are provided. | 2011-07-28 |
| 20110183945 | LONG ACTING CURCUMIN DERIVATIVE, PREPARATION METHOD AND PHARMACEUTICAL USE THEREOF - The invention provides a long acting curcumin derivative, preparation method and pharmaceutical use thereof, wherein said long acting curcumin derivative having the general structural formula disclosed herein, wherein R1 and R2 are hydrogen or methoxyl; R3 and R4 are each independently selected from C1-C50 alkyl. Compared with cuminoids, the inventive long acting curcumin derivative has a better release effect, a higher bioavailability and pharmaceutical activity, and thus can be useful for the treatment of diseases such as depression and cancer. | 2011-07-28 |
| 20110183946 | Complexes Comprising alpha2-Adrenergic Receptor Agonists and Methods of Providing Neuroprotection or Treating or Inhibiting Progression of Glaucoma - A complex comprises at least an α | 2011-07-28 |
| 20110183947 | ALPHA-KETO HETEROCYCLES AS FAAH INHIBITORS - The invention provides a series of -αketoheterocyclic compounds, for example, compounds of formula (I). The compounds can inhibit fatty acid amide hydrolase and can be useful for treatment of malconditions modulated by fatty acid amide hydrolase. The invention further provides methods of making compounds of formula (I), useful intermediates for the preparation of compounds of formula (I), and methods of using compounds of formula (I) and compositions thereof. | 2011-07-28 |
| 20110183948 | TREATMENT OF FIBROTIC CONDITIONS USING HEDGEHOG INHIBITORS - Provided is a method of treating a fibrotic condition with a hedgehog inhibitor. | 2011-07-28 |
| 20110183949 | Use of Fulvestrant in the Treatment of Resistant Breast Cancer - The invention relates to the use of fulvestrant in the treatment of breast cancer in patients who have previously been treated with a Selective Estrogen Receptor Modulator (SERM) and an aromatase inhibitor. | 2011-07-28 |
| 20110183950 | TREATMENT OF VAGINAL ATROPHY IN WOMEN WITH TUMOR 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 developing an estrogen-dependent tumor or suffering or having suffered from an estrogen-dependent tumor. | 2011-07-28 |
| 20110183951 | Copper (1) Complex - A Copper (I) chloride complex of pyrazinic acid having the empirical formula C | 2011-07-28 |
| 20110183952 | NEW CHEMICAL COMPOUNDS - The present invention encompasses compounds of general formula (1), wherein the groups R | 2011-07-28 |
| 20110183953 | SELECTIVE HETEROCYCLIC SPHINGOSINE 1 PHOSPHATE RECEPTOR MODULATORS - Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds is provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated. | 2011-07-28 |
| 20110183954 | TRICYCLIC 2,4-DIAMINO-L,3,5-TRIAZINE DERIVATIVES USEFUL FOR THE TREATMENT OF CANCER AND MYELOPROLIFERATIVE DISORDERS - The present invention relates to compounds of Formula (I): (I) and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds provide a treatment for myeloproliferative disorders and cancer. | 2011-07-28 |
| 20110183955 | 2-Aminocarbonyl Substituted Piperazine or Diaza-Cyclic Compounds as Apoptosis Protein Inhibitors (Iap) Modulators - The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts, solvates, hydrates or pharmaceutically acceptable formulations thereof. These compounds may be used to modulate cellular proliferation and to prevent and/or treat proliferative diseases. | 2011-07-28 |
| 20110183956 | PROCESS FOR THE SYNTHESIS OF EZETIMIBE AND INTERMEDIATES USEFUL THEREFOR - The present invention discloses novel and useful intermediates for the synthesis of ezetimibe (EZT), which intermediates share a characteristic Z-isomeric structure. Based on Z-5-(4-fluorophenyl)-pent-4-enoic acid, and proceeding the synthesis through further Z-intermediates, a total synthesis is presented to obtained final ezetimibe in high yields. | 2011-07-28 |
| 20110183957 | CERTAIN KYNURENINE-3-MONOOXYGENASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF - Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity. | 2011-07-28 |
| 20110183958 | AZETIDINE DERIVATIVES AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE - Azetidine derivatives of structural formula I are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD). 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; atherosclerosis; obesity; diabetes; neurological disease; Metabolic Syndrome; insulin resistance; cancer; liver steatosis; and non-alcoholic steatohepatitis. | 2011-07-28 |
| 20110183959 | P38 KINASE INHIBITING AGENTS - Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: | 2011-07-28 |
| 20110183960 | THIOPHENE-2-CARBOXAMIDE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The subject matter of the invention is compounds corresponding to formula (I), in which: R | 2011-07-28 |
| 20110183961 | AZETIDINE POLYSUBSTITUTED COMPOUNDS, PREPARATION THEREOF, AND THERAPEUTIC APPLICATION THEREOF - The invention relates to compounds of the formula (I) where: R is a (C | 2011-07-28 |
| 20110183962 | SMOOTHENED ANTAGONISM FOR THE TREATMENT OF HEDGEHOG PATHWAY-RELATED DISORDERS - The invention provides methods for modulating, e.g., antagonizing, the activity of the Hedgehog signaling pathway, and for treating Hedgehog related disorders such as cancers (e.g., medulloblastoma). In particular, the invention provides methods for inhibiting aberrant growth states resulting from phenotypes such as Ptch loss-of-function, Hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function by administering to a mammal combinations of Smoothened inhibitors (e.g., a compound of Formula I, Formula II, or Formula III, or any of the compounds listed herein or incorporated by reference) and cholesterol biosynthesis pathway inhibitors (e.g., statins), Gli inhibitors, and/or Phosphatidylinositol 3-kinase (PI3K) inhibitors. | 2011-07-28 |
| 20110183963 | Amino Acid Conjugates of Quetiapine, Process for Making and Using the Same - The presently described technology provides a novel class of prodrugs of quetiapine that can be synthesized by chemically conjugating amino acids to quetiapine. The present technology also provides methods of treating patients, pharmaceutical compositions and methods of synthesizing conjugates of the present technology. | 2011-07-28 |
| 20110183964 | HYDROXAMATE-BASED INHIBITORS OF DEACETYLASES B - The present teachings relate to compounds of Formula I: | 2011-07-28 |
| 20110183965 | 6-AMINOISOQUINOLINE COMPOUNDS - 6-Amino isoquinoline compounds are provided that influence, inhibit or reduce the action of a kinase. Pharmaceutical compositions including therapeutically effective amounts of the 6-aminoisoquinoline compounds and pharmaceutically acceptable carriers are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions such as cancer, obesity and glaucoma are also provided. | 2011-07-28 |
| 20110183966 | AMINOPYRIDINE KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. | 2011-07-28 |
| 20110183967 | BENZOXAZOLE COMPOUNDS AND METHODS OF USE - The present invention provides benzoxazole compounds and pharmaceutically acceptable salts thereof and pharmaceutical compositions including the same. The present invention further provides methods of use as described herein. | 2011-07-28 |
| 20110183968 | ANTIFUNGAL COMPOUNDS CONTAINING BENZOTHIAZINONE, BENZOXAZINONE OR BENZOXAZOLINONE AND PROCESS THEREOF - The present invention discloses novel compounds of the Formula (1), comprising benzothiazinone, benzoxazinone or benzoxazolinone moieties having antifungal activity, method for preparing these compounds and the use of these compounds as antifungal agents in prevention and treatment of fungal infections, and pharmaceutical preparations containing these novel compounds. | 2011-07-28 |
| 20110183969 | ANTIFUNGAL COMBINATION THERAPY - The invention provides pharmaceutical combinations comprising a combination of an antifungal indolizine compound of formula (I) or a pharmaceutically acceptable salt thereof and a second antifungal agent: wherein: R1, R2, R3, R4, R5, R6, R7, X and X | 2011-07-28 |
| 20110183970 | Insecticide Compositions And Process - A synergistic insecticide composition comprising:
| 2011-07-28 |
| 20110183971 | 3,4-DIHYDRO-2H-PYRAZINO[1,2-A]INDOL-1-ONE DERIVATIVES ACTIVE AS KINASE INHIBITORS, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM - Compounds which are 3,4-dihydro-2H-pyrazino[1,2-a]indol-1-one derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them. | 2011-07-28 |
| 20110183972 | AROMATIC RING FUSED TRIAZINE DERIVATIVES AND USES THEREOF - The invention belongs to pharmaceutical field. The invention relates to the compounds according to Formula I, including their optically active forms, pharmaceutically acceptable salts or hydrates, and the pharmaceutical composition comprising thereof as active ingredient; uses in the preparation of vascular endothelial growth factor receptor tyrosine kinase inhibitors, and uses in the preparation of medicament for the treatment and/or prevention of cancer. | 2011-07-28 |
| 20110183973 | Novel Compounds - The invention is directed to certain novel compounds directed to compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity. | 2011-07-28 |
| 20110183974 | 1,2,4-OXADIAZOLE SUBSTITUTED PIPERIDINE AND PIPERAZINE DERIVATIVES AS SMO ANTAGONISTS - The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts, stereoisomers or tautomers thereof which are inhibitors of the Sonic Hedgehog pathway, in particular Smo antagonists. Thus the compounds of this invention are useful for the treatment of diseases associated with abnormal hedgehog pathway activation, including cancer, for example basal cell carcinoma, medulloblastoma, prostate, pancreatic, breast, colon, bone and small cell lung cancers, and cancers of the upper GI tract. | 2011-07-28 |
| 20110183975 | NOVEL 6-AZAINDOLE AMINOPYRIMIDINE DERIVATIVES HAVING NIK INHIBITORY ACTIVITY - The present invention relates to a compound of formula I: wherein: R | 2011-07-28 |
| 20110183976 | 5- AND 6-MEMBERED HETEROCYCLIC COMPOUNDS - 5- and 6-membered heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. Also described is the treatment of neurological, neurodegenerative and psychiatric disorders including but not limited to those comprising cognitive deficits or schizophrenic symptoms. | 2011-07-28 |
| 20110183977 | BENZENE, PYRIDINE, AND PYRIDAZINE DERIVATIVES - Disclosed are compounds and pharmaceutically acceptable salts of Formula I | 2011-07-28 |
| 20110183978 | Phenylpyri(mi)dinylazoles - Phenylpyri(mi)dinylazoles of the formula [I-a] and [I-b], | 2011-07-28 |
| 20110183979 | NITROGEN-CONTAINING HETEROARYL DERIVATIVES - The invention is concerned with novel nitrogen-containing heteroaryl derivatives of formula (I) | 2011-07-28 |
| 20110183980 | O-BENZYL NICOTINAMIDE ANALOGS AS MGLUR5 POSITIVE ALLOSTERIC MODULATORS - In one aspect, the invention relates to O-benzyl nicotinamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 2011-07-28 |
| 20110183981 | HETEROCYCLIC INHIBITORS OF MEK AND METHODS OF USE THEREOF - Disclosed are compounds of the Formula I | 2011-07-28 |
| 20110183982 | PHENOXY ACETIC ACIDS AS PPAR DELTA ACTIVATORS - The present invention describes phenoxy-acetic acids and pharmaceutical compositions containing the same and methods of using the same. The phenoxy-acetic acids are activators of PPAR-δ and should be useful for treating conditions mediated by the same. | 2011-07-28 |
| 20110183983 | HETEROCYCLIC COMPOUND AS PROTEIN KINASE INHIBITOR - Provided are novel heterocyclic compounds useful as anti-cancer drugs by suppressing protein kinase activities of growth factor receptors such as c-Met, pharmaceutical compositions containing the same, and methods for using the compound. | 2011-07-28 |
| 20110183984 | SMALL MOLECULE INHIBITORS OF LCK SH2 DOMAIN BINDING - The present invention provides materials and methods for modulating an immune response. The materials and methods may be used to treat diseases associated with an aberrant immune response. In some embodiments, materials and methods of the invention may be used to treat autoimmune diseases, for example, rheumatoid arthritis. | 2011-07-28 |
| 20110183985 | SUBSTITUTED FUSED ARYL AND HETEROARYL DERIVATIVES AS PI3K INHIBITORS - The present invention provides fused aryl and heteroaryl derivatives of Formula I: | 2011-07-28 |
| 20110183986 | POLYCYCLIC ARYL SUBSTITUTED TRIAZOLES AND POLYCYCLIC HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS - Polycyclic aryl and polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl catalytic activity are also disclosed. | 2011-07-28 |
| 20110183987 | Stereoselective Synthesis of Bicyclic Heterocycles - The present invention relates to a process for the stereoselective preparation of compounds of formulae (1A) and (1B) | 2011-07-28 |
| 20110183988 | COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR - Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on each of B-Raf, B-Raf V600E and c-Raf-1 protein kinase. In certain aspects and embodiments, the described compounds are active in inhibiting proliferation of a Ras mutant cell line. Also described are methods of use thereof to treat diseases and conditions, including melanoma, glioma, glioblastoma, pilocytic astrocytoma, liver cancer, biliary tract cancer, cholangiocarcinoma, colorectal cancer, lung cancer, bladder cancer, gallbladder cancer, breast cancer, pancreatic cancer, thyroid cancer, kidney cancer, ovarian cancer, adrenocortical cancer, prostate cancer, gastrointestinal stromal tumors, medullary thyroid cancer, tumor angiogenesis, acute myeloid leukemia, chronic myelomonocytic leukemia, childhood acute lymphoblastic leukemia, plasma cell leukemia, and multiple myeloma. | 2011-07-28 |
| 20110183989 | SATURATED BICYCLIC HETEROCYCLIC DERIVATIVES AS SMO ANTAGONISTS - The present invention relates to compounds of formula I: and pharmaceutically acceptable salts or tautomers thereof which are inhibitors of the Sonic Hedgehog pathway, in particular Smoantagonists. Thus the compounds of this invention are useful for the treatment of diseases associated with abnormal hedgehog pathway activation, including cancer, for example basal cell carcinoma, medulloblastoma, prostate, pancreatic, breast, colon, bone and small cell lung cancers, and cancers of the upper GI tract. | 2011-07-28 |
| 20110183990 | METHOD OF TREATING ATRIAL FIBRILLATION - The present invention relates to a method for the treatment or prevention of atrial fibrillation and/or atrial flutter comprising coadministration of a synergistically therapeutic amount of dronedarone or a pharmaceutically acceptable salt or salts thereof and a synergistically therapeutic amount of ranolazine or a pharmaceutically acceptable salt or salts thereof. Also provided are methods for modulating ventricular and atrial rhythm and rate. This invention also relates to pharmaceutical formulations that are suitable for such combined administration. | 2011-07-28 |
| 20110183991 | 5HT7 RECEPTOR LIGANDS AND COMPOSITIONS COMPRISING THE SAME - The present invention relates to compounds having pharmacological activity towards the 5-HT | 2011-07-28 |
| 20110183992 | THERAPEUTIC AGENT FOR MIGRAINE - Provided are therapeutic and/or preventive agents for migraine which comprise, as an active ingredient, a compound having a selective adenosine A | 2011-07-28 |
| 20110183993 | CYCLOALKANE DERIVATIVE - The present invention relates to a novel cycloalkane derivative which has an excellent psychotropic action. | 2011-07-28 |
| 20110183994 | 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-cyanoin-dol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine, crystalline modification of the dihydrochloride of 1-[4-(5-cyanoin-dol-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. | 2011-07-28 |
| 20110183995 | ELTOPRAZINE FOR SUPPRESSION OF L-DOPA INDUCED DYSKINESIAS - This invention relates to the use of the drug Eltoprazine for combating dyskinesias arising from chronic Levodopa (L-DOPA) therapy in patients suffering from Parkinson's disease. | 2011-07-28 |
| 20110183996 | THE 1-BUTYL-2-HYDROXYARALKYL PIPERAZINE DERIVATIVES AND THE USES AS ANTI-DEPRESSION MEDICINE THEREOF - The invention discloses 1-butyl-2-hydroxyl aralkyl piperazine derivatives and their use as antidepressants. The derivatives of the present invention have triple inhibition effect on the reuptake of 5-HT, NA and DA, and can be administrated to the patients in need thereof in form of composition by route of oral administration, injection and the like. Compared with clinically currently used dual targets antidepressants (such as venlafaxine), said derivatives may have stronger antidepression effect, broader indications, faster onset and lower neurotoxicity and side reaction; and said derivatives have stronger antidepression activity, lower toxicity, higher bioavailability, longer half life and better druggablity, compared with aryl alkanol piperazine derivatives and optical isomers thereof disclosed in prior art. The 1-butyl-2-hydroxyl aralkyl piperazine derivative is the free alkali or its salt of a compound of formula below: | 2011-07-28 |
| 20110183997 | HETEROCYCLIC COMPOUNDS AND COMPOSITIONS AS C-KIT AND PDGFR KINASE INHIBITORS - The invention provides a novel class of compounds of Formula I: (I) pharmaceutical compositions comprising such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of c-kit, PDGFRα and PDGFRβ kinases. | 2011-07-28 |
| 20110183998 | HETEROCYCLIC COMPOUNDS, PROCESSES FOR THEIR PREPARATION, MEDICAMENTS COMPRISING THESE COMPOUNDS, AND THE USE THEREOF - Heterocyclic derivatives, processes for their preparation, medicaments comprising these compounds, and the use thereof. The invention relates to compounds of the formula I in which the radicals R1, R2, R3, R4, W, A, B, D, E, G, L, M, R, T and Y have the stated meanings, and to the physiologically tolerated salts thereof. The compounds are suitable for example for the treatment of the metabolic syndrome, insulin resistance, obesity and diabetes. | 2011-07-28 |
| 20110183999 | NOVEL POLYMORPHIC FORMS OF METHYL CARBAMATE - The invention relates to novel forms of methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}carbamate of the formula (I), in particular to the modification I, to processes for their preparation, to medicaments comprising them and to their use for fighting diseases. | 2011-07-28 |
| 20110184000 | 1-HETEROCYCLYL-1,5-DIHYDRO-PYRAZOLO[3,4-D] PYRIMIDIN-4-ONE DERIVATES AND THEIR USE AS PDE9A MODULATORS - The invention relates to novel 1,6-disubstituted pyrazolopyrimidinones, Formula (I) with is a mono-, bi- or tri-cyclic heterocyclyl group, the ring members of which are carbon atoms and at least 1, preferably 1, 2 or 3, heteroatom(s), which are selected from the group of nitrogen, oxygen and sulphur, which is in the form of —S(O) | 2011-07-28 |
| 20110184001 | INHIBITORS OF BRUTON'S TYROSINE KINASE - Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. | 2011-07-28 |
| 20110184002 | METHOD OF TREATING HEPATIC DISEASE USING A2B ADENOSINE RECEPTOR ANTAGONISTS - The invention is related to methods of preventing and treating hepatic fibrosis using A | 2011-07-28 |
| 20110184003 | COMPOUNDS AND METHODS FOR THE TREATMENT OF VIRAL INFECTION - The invention relates to compounds and methods for treating or preventing a viral infection, by administering a monophosphorylated prodrug of acyclovir or monophosphorylated derivative of an acyclovir prodrug to a subject suffering from or susceptible (to a viral infection, such as HIV infection. | 2011-07-28 |
| 20110184004 | PREDICTIVE MARKER FOR EGFR INHIBITOR TREATMENT - The present invention provides biomarkers which are predictive for the clinical benefit of EGFR inhibitor treatment in cancer patients. | 2011-07-28 |
| 20110184005 | PREDICTIVE MARKER FOR EGFR INHIBITOR TREATMENT - The present invention provides a biomarker which is predictive for the clinical benefit of EGFR inhibitor treatment in cancer patients. | 2011-07-28 |
| 20110184006 | METHOD AND COMPOSITION FOR THERMALLY STABILIZING VITAMIN C WITHIN NANO LAYERS OF MONTMORILLONITE CLAY - A thermally stable Vitamin C composition containing montmorillonite, an organic acid containing L-ascorbic acid or a derivative thereof, a divalent cation present within nanolayers of the montmorillonite, wherein the organic acid is combined with the divalent cation within the nanolayers to form an organic acid-montmorillonite chelate. | 2011-07-28 |
| 20110184007 | PHARMACEUTICAL COMPOSITIONS CONFIGURED TO DETER DOSAGE FORM SPLITTING - An oral pharmaceutical composition comprising a drug and one or more pharmaceutically acceptable excipients in a monolithic dosage form, wherein the dosage form is configured such that when the dosage form is divided into more than one piece and at least one of the pieces is administered to a subject the Cmax, AUC, and/or rate of drug released after administration is substantially the same or lower and the Tmax is higher than the Cmax, AUC, rate of drug released, and/or Tmax after administration of: (1) a comparable composition in intact dosage form of equal drug dosage of the administered at least one piece; (2) a bioequivalent drug composition in an intact dosage form of equal drug dosage to the administered at least one piece; and (3) a divided piece of a bioequivalent drug composition, wherein the divided piece comprises a drug dosage equal to the dosage of the administered piece of the oral composition. Methods of making the same and methods of using the same are also provided. | 2011-07-28 |
| 20110184008 | CRYSTALLINE FORMS OF AN 8-AZABICYCLO[3.2.1]OCTANE COMPOUND - The invention provides a crystalline sulfate salt of 3-endo-(8-{2-[cyclohexylmethyl-((S)-2,3-dihydroxy-propionyl)amino]ethyl}-8-aza-bicyclo[3.2.1]oct-3-yl)benzamide or a solvate thereof. The invention also provides pharmaceutical compositions comprising such crystalline salt forms, methods of using such crystalline salt forms to treat diseases associated with mu opioid receptor activity, and processes useful for preparing such crystalline salt forms. | 2011-07-28 |
| 20110184009 | CAMPTOTHECIN DERIVATIVES AS CHEMORADIOSENSITIZING AGENTS - Camptothecin-based compounds are useful for treating a neoplasm in mammalian subjects by administering such compound to the subjects in combination with radiotherapy, i.e., the treatment of tumors with radioactive substances or radiation from a source external to the subject. Camptothecin-based compounds are modified by positioning at least one electron-affinic group around the camptothecin structure to enhance their value in combination with radiotherapy. New Camptothecin-based compounds are disclosed that are useful for treating cancer by administering the novel compounds alone or in combination with radiotherapy. | 2011-07-28 |
| 20110184010 | METHOD OF TREATING MANTLE CELL LYMPHOMA - This invention provides the use of rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid (CCI-779) in the treatment or inhibition of mantle cell lymphoma. | 2011-07-28 |
| 20110184011 | Compounds - The present invention relates to new therapeutic and prophylactic applications of known compounds of general formula (Ia), novel compounds of formula (Ia) | 2011-07-28 |
| 20110184012 | METHODS AND COMPOSITIONS FOR ALLEVIATING STUTTERING - Methods of treating stuttering include treating people with gamma-aminobutyric acid (GABA) receptor modulators, including cyclopyrrolones. A second active agent may be used with GABA receptor modulators. Active enantiomers, active metabolites, and pharmaceutically acceptable salts of garnma-aminobutyric acid receptor modulators, including cyclopyrrolones, are acceptable components of the compositions. The cyclopyrrolone class of modulators includes pagoclone, suriclone, zopiclone, 2-(7-chloro-2-naphthyridin-1,8-yl)-3-(5-methyl-2-oxohexy))isoindolin-1-one, 2-(7-chloro-2-naphthyridin-1,8-yl)isoindolin-1-yl-4- acetamidobutyrate, and 2-(7-chloro-1,8-naphthyridin-2y1)-3-(5-methyl-5-hydroxy-2-oxohexyl)-1-isoindolinone. | 2011-07-28 |
| 20110184013 | Imidazo[1,2-a]Pyridine Compounds As Receptor Tyrosine Kinase Inhibitors - Compounds of Formula I and II: I II having the chemical names cis-6-fluoro-8-(3-fluoropiperidin-4-yloxy)-2-(7-(2-methoxyethoxy)imidazo[1,2-a]pyridin-3-yl)quinoline and 6-fluoro-8-(trans-3-fluoropiperidin-4-yloxy)-2-(7-(2-methoxyethoxy)imidazo[1,2-a]pyridin-3-yl)quinoline, respectively, and enantiomers and pharmaceutically acceptable salts thereof, are receptor tyrosine inhibitors useful in the treatment of diseases mediated by class 3 and class 5 receptor tyrosine kinases. The compounds of this invention have also been found to be inhibitors of Pim-1. | 2011-07-28 |
| 20110184014 | NEW COMPOUNDS - The present invention relates to new mGluR1 and mGluR5 receptor subtype preferring ligands of formula (I); wherein Y represents a substituent selected from hydrogen, methyl, fluoro, chloro, bromo, methoxy; Z is hydrogen or methyl; R is an optionally substituted heteroaryl, and/or salts and/or hydrates and/or solvates thereof, to the processes for producing the same, to pharmaceutical compositions containing the same and to their use in therapy and/or prevention of pathological conditions which require the modulation of mGluR1 and mGluR5 receptors such as neurological disorders, psychiatric disorders, acute and chronic pain and neuromuscular dysfunctions of the lower urinary tract. | 2011-07-28 |
| 20110184015 | NOVEL DERIVATIVES OF PYRROLOINDOLE WHICH ARE INHIBITORS OF HSP90, COMPOSITIONS CONTAINING SAME, AND USE THEREOF - Pyrroloindoles of formula (I) are provided wherein Het is an aromatic or partially unsaturated, monocyclic or bicyclic heterocycle containing between 1 and 4 heteroatoms N, O or S, optionally substituted by R1 or R′1 which are the same or different; R is X-(A-B)n-CONH2, X-(A-B)n-O—CONH2, X-(A-B)n-NH—CONH2, X—(CH2)m-heterocycloalkyl, X(CH2)m-aryl and X—(CH2)m-heteroaryl wherein X is —O—C(O), —NH—C(O), NH—CS, —NH—CO—CH2-O—; —NH—COCH2-S—CH2-CO—NH—; —NH—CO—(CH2)2-SO2-; and —NH—CO—CH2-N(CH3)-CO—; A and B are the same or different and are each independently a single bond, CH2, CH-alkyl, and CH-aralkyl; n=1,2 and m=0, 1; R1 and/or R′1 are H, halogen, CF3, nitro, cyano, alkyle, hydroxy, mercapto, amino, alkylamino, dialkylamino, alkoxy, alkylthio, and carboxy, free or esterified by an alkyl, carboxamide, CONH(alkyl), CON(alkyl)2, NH—CO-alkyl, sulfonamide, NH—SO2-alkyl, S(O)2-NHalkyl, and S(O2)-N(alkyl)2 group, all of said alkyl, alcoxy and alkylthio groups being optionally substituted themselves, said products being in all isomer forms and salts, as medicaments. | 2011-07-28 |
| 20110184016 | PREVENTION AND TREATMENT OF ITCH WITH CYSTEINE PROTEASE INHIBITION - Embodiments of the invention relates to methods of preventing itch in a subject using a therapeutically effective amount of a cysteine protease inhibitor. The itch is not associated with psoriasis and atopic dermatitis. The itch is also a non-histamine mediated itch. The inhibitor are directed to the cathepsin selected from the group consisting of cathepsin B, C, F, J, K, H, L, P, Q, S, W, X, V, and Z. | 2011-07-28 |
| 20110184017 | STABLE AQUEOUS SOLUTION COMPOSITION CONTAINING SULFONAMIDE COMPOUND - An aqueous solution composition containing (S)-1-(4-chloro-5-isoquinolinesulfonyl)-3-aminopyrrolidine or (S)-1-(4-chloro-5-isoquinolinesulfonyl)-3-(methylamino)pyrrolidine as an active ingredient, and not containing citric acid or a salt thereof, which has high stability so as to be storable at room temperature. | 2011-07-28 |
| 20110184018 | METHOD FOR TREATING PERIPHERAL NEUROPATHIC PAIN - A method for the treatment of peripheral neuropathic pain in a mammal is provided. The method comprises administering to a mammal (e.g., a human) suffering from peripheral neuropathic pain a pain relieving amount of a diarylureido-dihalokynurenate compound. Preferred diarylureido-dihalokynurenate compounds are esters (e.g., ethyl esters). Particularly preferred are diphenylureido-dichlorokynurenate compounds. The diphenylureido-dihalokynurenate compounds are shown to be agonists of cannabinoid receptor 1 (CB1) and stimulate CB1 activity. | 2011-07-28 |
| 20110184019 | Long chain N-Alkyl compounds and oxa-derivatives thereof - Long chain N-alkyl amino and imino compounds, oxa-substituted derivatives thereof, and pharmaceutical compositions including such compounds are described. The long chain N-alkyl group is a C | 2011-07-28 |
| 20110184020 | Vanilloid Receptor Ligands, Pharmaceutical Compositions Containing Them, Process For Making Them, and Use Thereof For Treating Pain and Other Conditions - Vanilloid receptor ligand compounds corresponding to formula I: | 2011-07-28 |
| 20110184021 | 2-Acylaminopropoanol-Type Glucosylceramide Synthase Inhibitors - A compound for use in treating polycystic kidney disease is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating polycystic kidney disease in a subject in need thereof comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. Methods of treating in polycystic kidney disease in a subject in need thereof respectively comprise administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. | 2011-07-28 |
| 20110184022 | Organic Compounds - Compounds of formula (I), which are 14-O-{[(optionally substituted hydroxy)cyclohexyl)sulfanyl]acetyl}mutilins further substituted at the cyclohexyl group by an acylated amino group, salts and solvates thereof, pharmaceutical compositions comprising such compounds and their use as a pharmaceutical, e.g. for the treatment of diseases mediated by microbes and for the treatment of inflammation where microbese are mediating said inflammation. | 2011-07-28 |
| 20110184023 | THE SALTS OF N-[4-(1-CYANOCYCLOPENTYL)PHENYL]-2-(4-PYRIDYLMETHYL)AMINO-3-PYRIDINECARBO- XAMIDE - The present invention relates to the salts of N-[4-(1-cyanocyclopentyl)phenyl]-2-(4-pyridylmethyl) amino-3-pyridine carboxamide, especially hydrochloride and mesylate thereof, and the use of said salts in the preparation of an antineoplastic medicament. | 2011-07-28 |
| 20110184024 | Pharmaceutical Composition Containing Esomeprazole - The present invention relates to esomeprazole free base or its alkali salt-containing composition which stability is improved and is easy to manufacture. | 2011-07-28 |
| 20110184025 | Methods and Compositions Using Immunomodulatory Compounds for the Treatment and Management of Spirochete and Other Obligate Intracellular Bacterial Diseases - Methods of treating, preventing and/or managing a spirochete and/or other obligate intracellular bacterial disease or disorder are disclosed. Specific methods encompass the administration of an immunomodulatory compound alone or in combination with a second active agent. | 2011-07-28 |
| 20110184026 | C4-SUBSTITUTED ALPHA-KETO OXAZOLES - The invention provides a series of C4-substituted oxazole compounds having an alpha keto side chain at the 2 position, for example, compounds of formula I. The compounds can inhibit fatty acid amide hydrolase and can be useful for treatment of malconditions modulated by fatty acid amide hydrolase. The invention further provides methods of making compounds of formula I, useful intermediates in the preparation of compounds of formula I, and methods of using compounds of formula I and compositions thereof. | 2011-07-28 |
| 20110184027 | TISSUE SELECTIVE STEAROYL-COA DESATURASE 1 INHIBITORS AND CELL BASED SCREENING ASSAY FOR THEIR IDENTIFICATION - The present invention provides a method of treating a disorder treatable by administering a therapeutically effective amount of a tissue selective Stearoyl-CoA Desaturase 1 (SCD-1) modulator to a subject. In one embodiment, the present invention provides a method of treating a disorder treatable by administering a pharmaceutically effective amount of a tissue selective SCD-1 inhibitor to a subject. The invention also provides whole cell based screening assays to identify agents that selectively modulate the activity of SCD-1. This invention further provides whole cell based screening assays to identify agents that differentially inhibit SCD in different body tissues. | 2011-07-28 |
| 20110184028 | DERIVATIVES OF PYRIDOXINE FOR INHIBITING HIV INTEGRASE - The present invention relates to compounds of Formula I or pharmaceutically acceptable salts, solvates or formulations thereof. Compounds of Formula I inhibit HIV-integrase enzyme and are useful for preventing and treating of HIV infection and AIDS. | 2011-07-28 |
| 20110184029 | PYRIDONE DERIVATIVES AS NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS - The present invention relates to 2-pyridone derivatives of Formula I or IV | 2011-07-28 |
| 20110184030 | Pharmaceutically acceptable salt and polymorphic forms of flupirtine maleate - The present invention is concerned with new polymorphic forms of flupirtine maleate, processes for preparing the new polymorphic forms, pharmaceutical compositions containing them, therapeutic uses thereof and methods of treatment employing them. | 2011-07-28 |
| 20110184031 | G-Protein-Conjugated Receptor Agonist - Disclosed is a novel aralkyl carboxylic acid compound which has an agonistic activity on GPR-120 and/or GPR-40, particularly GPR-120, and is therefore useful as an appetite regulator, an anti-obesity agent, a therapeutic agent for diabetes, a pancreatic beta differentiating cell growth enhancer, a therapeutic agent for metabolic syndrome, a therapeutic agent for a gastrointestinal disease, a therapeutic agent for a neuropathy, a therapeutic agent for a mental disorder, a therapeutic agent for a pulmonary disease, a therapeutic agent for a pituitary hormone secretion disorder or a lipid flavoring/seasoning agent. The aralkyl carboxylic acid compound is represented by the general formula (I). (I) wherein the ring Q represents a pyridyl or the like; R | 2011-07-28 |
| 20110184032 | Novel Phenylamino Isonicotinamide Compounds - The invention provides novel compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. | 2011-07-28 |
| 20110184033 | Selective Ligands for the Dopamine 3 (D3) Receptor and Methods of using the Same - Potent and selective ligands for the dopamine 3 (D | 2011-07-28 |
| 20110184034 | Severe sepsis preventive therapeutic agent - The present invention provides an agent for the prophylaxis or treatment of severe sepsis, which contains a compound represented by the formula (I): | 2011-07-28 |
| 20110184035 | METHODS OF TREATING DEGENERATIVE DISEASES/INJURIES - Invented is a method of treating degenerative diseases/injuries, in a mammal, including a human, in need thereof which comprises the administration of a therapeutically effective amount of a non-peptide TPO receptor agonist to such mammal. | 2011-07-28 |
| 20110184036 | FORMULATIONS OF BENDAMUSTINE - Long term storage stable bendamustine-containing compositions are disclosed. The compositions can include bendamustine or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable fluid which can include in some embodiments PEG, PG or mixtures thereof and an antioxidant or chloride ion source. The bendamustine-containing compositions have less than about 5% total impurities, on a normalized peak area response (“PAR”) basis as determined by high performance liquid chromatography (“HPLC”) at a wavelength of 223 nm, after at least about 15 months of storage at a temperature of from about 5° C. to about 25° C. | 2011-07-28 |
| 20110184037 | METHODS FOR TREATING AN INTERVERTEBRAL DISC USING LOCAL ANALGESICS - Effective methods of treating back pain from an intervertebral disc are provided. The methods of treatment include administering an immediate release analgesic at or near the intervertebral disc; administering a bulking agent or sealing agent within the intervertebral disc; and administering a sustained release analgesic within the intervertebral disc, wherein the sustained release analgesic releases the analgesic over a period of at least one day. | 2011-07-28 |
| 20110184038 | METHODS AND COMPOSITIONS OF SMALL MOLECULE MODULATORS OF HEPATOCYTE GROWTH FACTOR (SCATTER FACTOR) ACTIVITY - The present invention provides compositions and formulations of compounds having formula (I) and pharmaceutically acceptable derivatives thereof, wherein p, R | 2011-07-28 |
| 20110184039 | PHARMACEUTICAL FORMULATION - A pharmaceutical composition comprising: a) a 5-HT1 agonist; b) an NSAID; and c) a disintegrant characterised in that the disintegrant comprises between about 15 to about 50% w/w based on the weight of the composition, said composition optionally comprising one or more other pharmaceutically acceptable excipients. | 2011-07-28 |
