21st week of 2015 patent applcation highlights part 61 |
Patent application number | Title | Published |
20150141395 | BENZOFURAN DERIVATIVES FOR THE TREATMENT OF HEPATITIS C - The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV. | 2015-05-21 |
20150141396 | PYRIMIDINE PYRAZOLYL DERIVATIVES - The present invention provides compounds of Formula (I) for the treatment of cancer, rheumatoid arthritis and other diseases. | 2015-05-21 |
20150141397 | SUBSTITUTED ANILINES AS CCR(4) ANTAGONISTS - Aniline compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer. | 2015-05-21 |
20150141398 | NAMPT INHIBITORS - Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed. | 2015-05-21 |
20150141399 | MEK Inhibitors And Methods Of Their Use - Disclosed are compounds of Formula I: | 2015-05-21 |
20150141400 | QUINAZOLINEDIONE DERIVATIVE - The present invention relates to quinazolinedione derivatives represented by formula (I) or pharmaceutically acceptable salts thereof. | 2015-05-21 |
20150141401 | NOVEL BETA-LACTAMASE INHIBITOR AND PROCESS FOR PREPARING THE SAME - A diazabicyclooctane compound, which is a beta-lactame inhibitor, represented by the following formula (I): | 2015-05-21 |
20150141402 | PURINE DERIVATIVES - The present invention relates to compounds of formula (I) | 2015-05-21 |
20150141403 | 1,2,4-Triazolo [4,3-A] Pyridine Derivatives and Their Use For The Treatment of Prevention of Neurological and Psychiatric Disorders - The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) | 2015-05-21 |
20150141404 | NON-IONIC VESICLE FORMULATIONS OF CALCIUM CHANNEL BLOCKERS - Disclosed are non-ionic surfactant vesicle formulations of calcium channel blockers, such as diltiazem, and methods of using the formulations for treating anal disorders. | 2015-05-21 |
20150141405 | TREATMENT OF RESPIRATORY DEPRESSION - Tricyclic dibenzothiazepine compounds for use in the treatment of respiratory depression. | 2015-05-21 |
20150141406 | HETEROCYCLIC COMPOUND - The present invention provides a compound having a superior JAK inhibitory action, which is useful as an agent for the prophylaxis or treatment of autoimmune diseases (rheumatoid arthritis, psoriasis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus, etc.), cancer (leukemia, uterine leiomyosarcoma, prostate cancer, multiple myeloma, cachexia, myelofibrosis, etc.) and the like, or a salt thereof. | 2015-05-21 |
20150141407 | N-Aryl Unsaturated Fused Ring Tertiary Amine Compounds, Preparation Method and Anti-Tumor Applications Thereof - The present invention relates to a compound of Formula I or a pharmaceutically acceptable salt thereof, its preparation method, a pharmaceutical composition comprising the compound, and its use in manufacture of a medicament for treatment of a disease or disorder, wherein R | 2015-05-21 |
20150141408 | TRICYCLIC PYRROLO DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS - The present invention relates to tricyclic pyrrolo derivatives which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them. | 2015-05-21 |
20150141409 | NOVEL REVAMIPIDE PRODRUGS, PREPARATION METHOD AND USE THEREOF - Disclosed are a novel rebamipide prodrug, a method for preparing the same, and use thereof. Also, a pharmaceutical composition comprising the novel rebamipide prodrug as an active ingredient is provided. The rebamipide prodrug is increased 25-fold in absorption rate compared to rebamipide itself, and can be applied to the prophylaxis or therapy of gastric ulcer, acute gastritis, chronic gastritis, xerophthalmia, cancer, osteoarthritis, rheumatoid arthritis, or obesity. | 2015-05-21 |
20150141410 | GPR17 Receptor Modulators - Chemical compounds are provided which act on GPR17 receptors and are useful in the treatment or amelioration of chronic and/or acute neurodegenerative diseases, such as multiple sclerosis, inflammatory diseases, pathologies involving the immune system, cardiovascular diseases, and renal diseases. | 2015-05-21 |
20150141411 | SUBSTITUTED 3,4-DIHYDRO-2H-PYRIDO[1,2-A]PYRAZINE-1,6-DIONE DERIVATIVES USEFUL FOR THE TREATMENT OF (INTER ALIA) ALZHEIMER'S DISEASE - The present invention is concerned with novel substituted 3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-dione derivatives of Formula (I) wherein R | 2015-05-21 |
20150141412 | PRODUCTION OF STERILE ACTIVE PHARMACEUTICAL INGREDIENTS - The invention refers to a process for preparing sterile active pharmaceutical ingredients (APIs) useful in the preparation of sterile product for ophthalmic use. The process comprises the gamma-ray sterilization treatment of the APIs powder in a protective atmosphere. | 2015-05-21 |
20150141413 | 5-AMINO[1,4]THIAZINES AS BACE 1 INHIBITORS - The present invention provides a compound of formula I having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease. | 2015-05-21 |
20150141414 | Formulation of Stable Recombinant Alpha-Fetoprotein Conjugated with Anti-Tumor Substance in Target-Delivery System for Treatment of Cancer and Autoimmune Disease - Disclosed is a stable formulation based on rAFP conjugated with drug delivery system of various classes of pharmacological agents such as dactinomycin, cardionolide, and bufadinolide, among others. In another embodiment, the invention discloses a method of producing rAFP in a strain of methylotrophic | 2015-05-21 |
20150141415 | Methionine Aminopeptidase Inhibitors for Treating Infectious Diseases - The present invention relates to methods for treating an infectious disease in a subject in need thereof via administration of a therapeutically effective amount of compounds described herein. The methods may utilize particular compounds, for example, a quinoline, a hydrazone, a quinone, or a pyrimidine derivatives thereof or a pharmaceutical salts thereof. | 2015-05-21 |
20150141416 | HYDROXYBUPROPION ANALOGUES FOR TREATING DRUG DEPENDENCE - The invention provides hydroxybupropion analogues capable of inhibiting the reuptake of one or more monoamines and/or acting as antagonists at nicotinic acetylcholine receptors. The compounds may selectively bind to one or more monoamine transporters, including those for dopamine, norepinephrine, and serotonin and/or may selectively bind to one or more nicotinic acetylcholine receptor subtypes. Such compounds may be used to treat conditions that are responsive to modification of monoamine levels and/or antagonism of nicotinic acetylcholine receptors, including drug dependency, depression, and obesity. | 2015-05-21 |
20150141417 | TETRA-SUBSTITUTED NDGA DERIVATIVES VIA ETHER BONDS AND CARBAMATE BONDS AND THEIR SYNTHESIS AND PHARMACEUTICAL USE - Disclosed are nordihydroguaiaretic acid derivative compounds including various end groups bonded by a carbon atom or heteroatom though a side chain bonded to the respective hydroxy residue O groups by an ether bond or a carbamate bond, pharmaceutical compositions, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, a metabolic disease, such as diabetes, a vascular disease, such as hypertension and macular degeneration, or a proliferative disease, such as diverse types of cancers. | 2015-05-21 |
20150141418 | TETRAHYDROCARBAZOLES AS ACTIVE AGENTS FOR INHIBITING VEGF PRODUCTION BY TRANSLATIONAL CONTROL - The present invention relates to methods, compounds, and compositions for inhibiting angiogenesis. More particularly, the present invention relates to methods, compounds, and compositions for inhibiting VEGF production. | 2015-05-21 |
20150141419 | DIARYL[A, G]QUINOLIZIDINE COMPOUND, PREPARATION METHOD THEREFOR, PHARMACEUTICAL COMPOSITION, AND USES THEREOF - The present invention relates to a diarylo[a,g]quinolizidine compound of formula (I), enantiomer, diastereoisomer, racemate, mixture, pharmaceutically acceptable salt, crystalline hydrate or solvate thereof; the preparation method thereof, and uses thereof in preparing an experimental model drugs related to dopamine receptors and 5-HT receptors or a medicament for treating or preventing a disease related to dopamine receptors and 5-HT receptors. | 2015-05-21 |
20150141420 | USE OF SUBSTITUTED 2, 3-DIHYDROIMIDAZO[1,2-C]QUINAZOLINES FOR THE TREATMENT OF MYELOMA - The present invention relates to the use of 2,3-dihydroimidazo[1,2-c]quinazoline compounds, and of pharmaceutical compositions containing such compounds, for the treatment or prophylaxis of multiple myeloma, as a sole agent or in combination with other one or more other active ingredients. | 2015-05-21 |
20150141421 | 6,7-DIALKOXY QUINAZOLINE DERIVATIVES AND METHODS OF TREATING DRUG RESISTANT AND OTHER TUMORS - Compounds of formula (I) | 2015-05-21 |
20150141422 | HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK - Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus. | 2015-05-21 |
20150141423 | PESTICIDALLY ACTIVE PYRIDYL- AND PYRIMIDYL- SUBSTITUTED THIAZOLE DERIVATIVES - Disclosed are pesticidally active pyridyl- and pyrimidyl-substituted thiazole derivatives, processes for their preparation, compositions comprising those compounds, and their use for controlling insects. | 2015-05-21 |
20150141424 | IRE-1alpha INHIBITORS - Compounds which directly inhibit IRE-1α activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) and can be used as single agents or in combination therapies. | 2015-05-21 |
20150141425 | C5aR ANTAGONISTS - Compounds are provided that are modulators of the C5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of C5a receptors. | 2015-05-21 |
20150141426 | DOSAGE REGIMEN FOR A PI-3 KINASE INHIBITOR - The present invention relates to a dosage regimen for a phosphatidylinositol 3-kinase (PI3K) inhibitor compound of formula (I) or a pharmaceutically acceptable salt thereof. More specifically, the present invention relates to a dosage regimen for the treatment of patients suffering from a proliferative disease, such as, for example, cancer, with a phosphatidylinositol 3-kinase (PI3K) inhibitor compound of formula (I) or a pharmaceutically acceptable salt thereof. | 2015-05-21 |
20150141427 | COMPOUNDS AND COMPOSITIONS FOR INHIBITING THE ACTIVITY OF ABL1, ABL2 AND BCR-ABL1 - The present invention relates to compounds of formula I: in which Y, Y | 2015-05-21 |
20150141428 | TrkA Kinase Inhibitors, Compositions and Methods Thereof - The present invention is directed to benzyl urea compounds, which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence may be useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor Trk-A, Trk-B and/or Trk-C. | 2015-05-21 |
20150141429 | PARP INHIBITOR COMPOUNDS, COMPOSITIONS AND METHODS OF USE - The present invention relates to tetraaza phenalen-3-one compounds which inhibit poly (ADP-ribose) polymerase (PARP) and are useful in the chemosensitization of cancer therapeutics. The induction of peripheral neuropathy is a common side-effect of many of the conventional and newer chemotherapies. The present invention further provides means to reliably prevent or cure chemotherapy-induced neuropathy. The invention also relates to the use of the disclosed PARP inhibitor compounds in enhancing the efficacy of chemotherapeutic agents such as temozolomide. The invention also relates to the use of the disclosed PARP inhibitor compounds to radiosensitize tumor cells to ionizing radiation. The invention also relates to the use of the disclosed PARP inhibitor compounds for treatment of cancers with DNA repair defects. | 2015-05-21 |
20150141430 | METHOD FOR MODULATING CANONICAL WNT PATHWAY USING FOLATE AND INOSITOL - The canonical Wnt signaling pathway is implicated in wound healing. Administration of a composition having myo-inositol and folic acid upregulates fibronectin and provides the greatest protection in an additive/synergistic manner against adverse Wnt/β-catenin-mediated effects on cell processes relating to cell differentiation, proliferation, and migration that relate to wound healing. | 2015-05-21 |
20150141431 | PYRAZINOISOQUINOLINE COMPOUNDS - This invention in one embodiment is directed to a compound of Formula Ia; | 2015-05-21 |
20150141432 | PIPERIDIN-4-YL-PYRIDAZIN-3-YLAMINE DERIVATIVES AS FAST DISSOCIATING DOPAMINE 2 RECEPTOR ANTAGONISTS - The present invention relates to compounds that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects. | 2015-05-21 |
20150141433 | N-ARYLMETHYL SULFONAMIDE NEGATIVE MODULATORS OF NR2A - Compounds that selectively negatively modulate NMDA receptors containing an NR2A subunit, pharmaceutical compositions comprising the compounds, and methods of treating a disease using the compounds are disclosed. | 2015-05-21 |
20150141434 | PYRIDINE AND PIPERIDINE DERIVATIVES AND USE THEREOF - The invention provides compounds that are useful as sodium channel blockers. In one aspect, the invention provides compounds of Formula I: | 2015-05-21 |
20150141435 | 2-PYRIDONE ANTIMICROBIAL COMPOSITIONS - Disclosed herein are compounds of Formula I | 2015-05-21 |
20150141436 | INDOLES - Herein are disclosed indoles of formula (I) | 2015-05-21 |
20150141437 | AMIDOPHENOXYPROPANOLAMINES - The use of compounds of formula wherein R | 2015-05-21 |
20150141438 | METHODS FOR DELAYING OR PREVENTING THE ONSET OF TYPE 1 DIABETES - Described herein are methods for preventing or delaying the onset of Type 1 Diabetes, or inhibiting the maturation of anti-insulin B cells, in an individual in need thereof. The methods include administering to an individual in need thereof ibrutinib, alone or in combination with other Type 1 Diabetes treatments. | 2015-05-21 |
20150141439 | PHARMACEUTICAL COMPOSITION FOR THE PREVENTION OR TREATMENT OF BRAIN TUMOR OR TEMODAL RESISTANT GLIOBLASTOMA MULTIFORM COMPRISING AZATHIOPRINE AS AN ACTIVE INGREDIENT - The present invention relates to a pharmaceutical composition for the prevention or treatment of cancer or Temodal resistant glioblastoma multiform comprising azathioprine as an active ingredient. The azathioprine of the present invention is not only effective in inhibiting the growth of glioblastoma multiform, a kind of brain tumor, but also excellent in treating glioblastoma multiform that displays resistance against Temodal (temozolomide), the conventional therapeutic agent for glioblastoma multiform, so that it can be effectively used as an active ingredient of a pharmaceutical composition for the prevention or treatment of such cancer as brain tumor (particularly, glioblastoma multiform) and particularly Temodal resistant glioblastoma multiform. | 2015-05-21 |
20150141440 | Pharmaceutical Composition for Headache Relief - A pharmaceutical composition for headache relief combines a vasoconstricting agent, a pain relief agent, and a disposition altering agent for a three-pronged approach to headache or migraine relief. | 2015-05-21 |
20150141441 | AUGMENTED COGNITIVE TRAINING - The present invention provides methods of therapy of cognitive deficits associated with a central nervous system disorder or condition, methods of enhancing cognitive performance and methods for repeated stimulation of neuronal activity or a pattern of neuronal activity, such as that underlying a specific neuronal circuit(s). The methods comprise combining cognitive training protocols and a general administration of CREB pathway-enhancing agents. | 2015-05-21 |
20150141442 | CHEMICAL ENTITIES AND THERAPEUTIC USES THEREOF - Certain chemical entities that modulate PI3 kinase activity, and chemical entities, pharmaceutical compositions, and methods of treatments of diseases and conditions associated with PB kinase activity are described. | 2015-05-21 |
20150141443 | OPTICALLY ACTIVE PYRAZOLYLAMINOQUINAZOLINE, AND PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE THEREOF - Provided herein is an optically active pyrazolylaminoquinazoline, and pharmaceutical compositions thereof. Also provided herein is a method for treating, preventing, or ameliorating one or more symptoms of a JAK-mediated condition, disorder, or disease. Further provided herein is a method for treating, preventing, or ameliorating one or more symptoms of a proliferative disease, inflammatory disease, or renal disease. | 2015-05-21 |
20150141444 | N-METHYL TETRAHYDROQUINOLINE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS - The present invention is directed to N-methyl tetrahydroquinoline compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor. | 2015-05-21 |
20150141445 | Tricyclic Compounds Having Cytostatic and/or Cytotoxic Activity and Methods of Use Thereof - The present invention provides tricyclic compounds having cytostatic and cytotoxic activity in a single molecule having receptor tyrosine kinase(s), dihydrofolate reductase, thymidylate synthase and/or dihydroorotate dehydrogenase inhibitory activity, which are useful as anti-angiogenic and anti-tumor agents. Also provided are methods of utilizing these inhibitors to treat tumor cells and other proliferative diseases and disorders. | 2015-05-21 |
20150141446 | PESTICIDAL PYRIMIDINE COMPOUNDS - Pyrimidine compounds and their use in controlling pests such as insects and other invertebrates are provided. Further embodiments, forms, objects, features, advantages, aspects and benefits shall become apparent from the description. | 2015-05-21 |
20150141447 | SOLID PREPARATION - The present invention provides a solid preparation excellent in disintegration property and preservation stability. The present invention relates to a solid preparation containing (1) 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-4-fluorobenzonitrile (compound (A)) or a salt thereof, (2) a saccharide, and (3) sodium stearyl fumarate. In addition, the present invention relates to a solid preparation containing (1) compound (A) or a salt thereof, (2) a saccharide, and (3) stearic acid or talc in a naked tablet part. | 2015-05-21 |
20150141448 | Topical Ophthalmological Pharmaceutical Composition containing Pazopanib - The present invention relates to topical ophthalmological pharmaceutical compositions containing pazopanib, a hydrate, solvate or pharmaceutically acceptable salt thereof or a polymorph thereof and its process of preparation and its use for treating ophthalmological disorders. | 2015-05-21 |
20150141449 | KEY INTERMEDIATES FOR THE SYNTHESIS OF ROSUVASTATIN OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF - The present invention relates in general to the field of organic chemistry and in particular to the preparation of N-(4-(4-fluorophenyl)-6-isopropyl-5-methylpyrimidin-2-yl)-N-methylmethanesulfonamide (I), N-(4-(4-fluorophenyl)-5-(bromomethyl)-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide (II) and N-(4-(4-fluorophenyl)-5-(hydroxymethyl)-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide (III), key intermediates in preparation of Rosuvastatin. | 2015-05-21 |
20150141450 | METHODS OF TREATING TRAVELER'S DIARRHEA AND HEPATIC ENCEPHALOPATHY - Treatment of traveler's diarrhea using in subjects having hepatic encephalopathy using gastrointestinal specific antibiotics is disclosed. One example of a gastrointestinal specific antibiotic is rifaximin. | 2015-05-21 |
20150141451 | COMPOSITIONS AND METHODS FOR THE TREATMENT OF CHRONIC PAIN - The invention relates to the compounds of formula I and formula II or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I or formula II, and methods for treating chronic pain in a disease may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of acute pain (such as post-operative pain), palliative care to alleviate the severe, chronic, disabling pain of terminal conditions such as cancer, and degenerative conditions such as rheumatoid arthritis, non-malignant chronic pain, chemotherapy induced pain, musculoskeletal pain, sciatica, radiculopathy pain, migraine, neuropathic pain, post herpetic neuralgia, neuralgia pain, multiple sclerosis, multiple sclerosis, restless legs syndrome (RLS), cluster headache, depression, fibromyalgia and amyotrophic lateral sclerosis (ALS). | 2015-05-21 |
20150141452 | COMPOSITIONS FOR AFFECTING WEIGHT LOSS - Disclosed are compositions for affecting weight loss comprising a first compound and a second compound, where the first compound is an opioid antagonist and the second compound causes increased agonism of a melanocortin 3 receptor (MC3-R) or a melanocortin 4 receptor (MC4-R) compared to normal physiological conditions. Also disclosed are methods of affecting weight loss, increasing energy expenditure, increasing satiety in an individual, or suppressing the appetite of an individual, comprising identifying an individual in need thereof and treating that individual to antagonize opioid receptor activity and to enhance α-MSH activity. | 2015-05-21 |
20150141453 | Trigger-Responsive Chain-Shattering Polymers - Disclosed are polymers containing a backbone comprising alternating N-protected hydroxymethylaniline units (“spacer”) and linker units. | 2015-05-21 |
20150141454 | LIQUID PHARMACEUTICAL FORMULATIONS OF PALONOSETRON - The present invention relates to shelf-stable liquid formulations of palonosetron for reducing chemotherapy and radiotherapy induced emesis with palonosetron. The formulations are particularly useful in the preparation of intravenous and oral liquid medicaments. | 2015-05-21 |
20150141455 | COMPLEMENT PATHWAY MODULATORS AND USES THEREOF - The present invention provides a compound of formula I: (I) a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition. | 2015-05-21 |
20150141456 | CYCLIC AMINO COMPOUNDS FOR USE IN THE TREATMENT OF CARDIAC DISORDERS - The present invention relates to tertiary amines of formula (I) for use in therapy, particularly for use in treating cardiovascular disorders. The compounds have been found to regulate phospholamban phosphorylation by interfering with the A-kinase anchor protein 18delta (AKAP18δ) binding to the PKA substrate phospholamban. The compounds share a tri(alkylaryl/alkylheteroaryl) amine structure. | 2015-05-21 |
20150141457 | ELVITEGRAVIR SOLID DISPERSION - The present invention provides a novel amorphous solid dispersion of elvitegravir in combination with a pharmaceutically acceptable carrier, process for its preparation and pharmaceutical compositions comprising it. In a preferred embodiment the process for the preparation of amorphous solid dispersion of elvitegravir in combination with a pharmaceutically acceptable carrier comprises: preparing a solution comprising a mixture of elvitegravir and one or more pharmaceutically acceptable carriers selected from copovidone, ethyl cellulose, hydroxypropyl methylcellulose, polyethylene glycol, span 20 or soluplus in a solvent; and removing the solvent from the solution obtained; adding hydrocarbon solvent to the residual solid; and isolating amorphous solid dispersion of elvitegravir in combination with a pharmaceutically acceptable carrier. | 2015-05-21 |
20150141458 | Treatment of Glaucoma Using Laquinimod - The subject invention provides a method of treating a subject afflicted with glaucoma, suffering from retinal ganglion cell (RGC) loss or damage, or elevated intraocular pressure (IOP), or of reducing RGC loss or damage, or reducing IOP in a subject, comprising administering to the subject an amount of laquinimod effective to treat the subject, to reduce RGC loss or damage, or to reduce IOP in the subject. Provide also is a pharmaceutical composition, a package and a therapeutic package for treating a subject afflicted with glaucoma. | 2015-05-21 |
20150141459 | PHARMACEUTICAL COMPOSITIONS AND ADMINISTRATIONS THEREOF - The present invention relates to pharmaceutical compositions comprising a compound of Formula I in combination with one or both of a Compound of Formula II and/or a Compound of Formula III. The invention also relates to solid forms and to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis. | 2015-05-21 |
20150141460 | Anti-inflammatory Compositions - The invention relates to 3-(2′,2′-dimethylpropanoylamino)-tetrahydropyridin-2-one, and its pharmaceutical compositions and their use as a medicament intended to prevent or treat inflammatory disorders. | 2015-05-21 |
20150141462 | PHARMACEUTICAL COMPOSITIONS AND METHODS FOR TREATING DRUG ADDICTION AND PREVENTING A DRUG RELAPSE - The present invention relates to pharmaceutical compositions comprising (a) a pharmaceutically effective amount of an mGluR5 positive allosteric modulator, derivative, prodrug or a pharmaceutically acceptable salt thereof; (b) a pharmaceutically effective amount of an agent selected from an NMDA partial agonist or a GlyT1 inhibitor, derivative, prodrug or a pharmaceutically acceptable salt thereof; and (c) a pharmaceutically acceptable carrier. The present invention also relates to methods for treating drug addiction and preventing a drug relapse in a patient. The methods comprise (a) administering to the patient a pharmaceutically effective amount of an mGluR5 positive allosteric modulator, derivative, prodrug or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition thereof; (b) administering to the patient a pharmaceutically effective amount of an agent selected from an NMDA partial agonist or a GlyT1 inhibitor, derivative, prodrug or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition thereof. | 2015-05-21 |
20150141463 | SUBSTITUTED PYRAZOLONE COMPOUNDS AND METHODS OF USE - The present invention provides novel substituted pyrazolone compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans. | 2015-05-21 |
20150141464 | N-BIPHENYLMETHYLBENZIMIDAZOLE MODULATORS OF PPARG - The invention provides molecular entities that bind with high affinity to PPARG (PPARγ), inhibit cdk5 -mediated phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes or obesity. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided. | 2015-05-21 |
20150141465 | COMPOUNDS AND USES THEREOF FOR THE MODULATION OF HEMOGLOBIN - Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation. | 2015-05-21 |
20150141466 | Composition Containing Amino Acid Surfactants, Betaines And N-Methyl-N-Acylglucamines And Having Improved Foam Quality And Higher Viscosity - The invention relates to a composition which contains at least one N-acyl-amino acid surfactant, a betaine surfactant, an N-methyl-N-acylglucamine, said N-methyl-N-acylglucamine having a C | 2015-05-21 |
20150141467 | SOLID FORMS OF ACETIC ACID, COMPOSITIONS, AND USES THEREOF - Provided herein are solid forms comprising {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino}acetic acid, compositions comprising the solid forms, methods of making the solid forms and methods of their use for the treatment of various diseases and/or disorders. | 2015-05-21 |
20150141468 | COMPOSITIONS AND METHODS FOR THE TREATMENT OF METABOLIC DISORDERS - The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for treating or preventing metabolic disorders may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be also used to the treatment of diabetes, lipid peroxidation, hypertriglyceridemia, metabolic disorders, free radical generated due to reactive oxygen and carbonyl groups, ionizing radiation, advanced glycation end products, kidney disease, renal complications and kidney stone disease. | 2015-05-21 |
20150141469 | KIT FOR PRODUCING FOAMS CONTAINING BISPYRIDINIUM ALKANE - A kit for the production of an antimicrobial foam includes: a) a liquid composition which includes a1)one or more bispyridinium alkane and a2)one or more surfactants selected from non-ionic surfactants, amphoteric surfactants and cation-active surfactants, wherein the composition is formulated so that a foam can be produced therefrom, and b) a device for producing the foam from the composition. By using the bispyridinium alkanes the foam stability of liquid and surfactant-containing compositions is increased. | 2015-05-21 |
20150141470 | DIAGNOSTIC AND TREATMENT METHODS IN PATIENTS HAVING OR AT RISK OF DEVELOPING RESISTANCE TO CANCER THERAPY - A method of identifying a subject having cancer who is likely to benefit from treatment with a combination therapy with a MAPK pathway inhibitor, such as a RAF inhibitor, MEK inhibitor, or ERK inhibitor, and a GEF or HDAC inhibitor is provided. A method of treating cancer in a subject in need thereof is also provided and includes administering to the subject an effective amount of a MAPK inhibitor, such as a RAF inhibitor, MEK inhibitor, or ERK inhibitor, and an effective amount of a GEF or HDAC inhibitor. A method of identifying targets that confers resistance to a MAPK pathway inhibitor is also provided. | 2015-05-21 |
20150141471 | Pyridine Derivatives And Their Use In The Treatment Of Conditions Associated With Pathological Thrombus Formation - The present invention relates to compounds of the formula (I), wherein the residues R | 2015-05-21 |
20150141472 | Aryl-Phenyl-Sulfonamido-Cycloalkyl Compounds and Their Use - The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-phenyl-sulfonamido-cycloalkyl compounds of the following formula (collectively referred to herein as “APSAC compounds”). 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, in treatment, for example, of inflammation and/or joint destruction and/or bone loss; of disorders mediated by excessive and/or inappropriate and/or prolonged activation of the immune system; of inflammatory and autoimmune disorders, for example, rheumatoid arthritis, psoriasis, psoriatic arthritis, chronic obstructive pulmonary disease (COPD), atherosclerosis, inflammatory bowel disease, ankylosing spondylitis, and the like; of disorders associated with bone loss, such as bone loss associated with excessive osteoclast activity in rheumatoid arthritis, osteoporosis, cancer-associated bone disease, Paget's disease and the like, etc.; and of cancer, such as a haematological malignancy, a solid tumour, etc. | 2015-05-21 |
20150141473 | PHARMACEUTICAL DOSAGE FORMS OF TIZANIDINE AND ADMINISTRATION ROUTES THEREOF - A pharmaceutical composition in liquid dosage form which contains a tizanidine hydrocloride aqueous solution suitable for parenteral, intranasal and oral administration. | 2015-05-21 |
20150141474 | CYCLIC ETHER DGAT1 INHIBITORSCYCLIC ETHER DGAT1 INHIBITORS - The invention relates to compounds of formula (I): useful for treating disorders mediated by acyl coA-diacylglycerol acyl transferase 1 (DGAT1), e.g. metabolic disorders. The invention also provides methods of treating such disorders, and compounds and compositions etc. for their treatment. | 2015-05-21 |
20150141475 | THERAPEUTIC AGENT FOR FOOD COMPETENCE DISORDER IN STOMACH - A therapeutic agent for impaired gastric accommodation which contains as an active ingredient a compound represented by the general formula (1): | 2015-05-21 |
20150141476 | Use Of 2,5-Dihydroxybenzene Compounds And Derivatives For The Treatment Of Rosacea - The present invention relates to the use of a 2,5-dihydroxybenzene derivative of formula (I) or a pharmaceutically acceptable salt, solvate, isomer, or prodrug thereof for the treatment and/or prophylaxis of, inter alia, rosacea. | 2015-05-21 |
20150141477 | Pyrazole Derivatives And Their Use As LPAR5 Antagonists - The present invention relates to compounds of the formula (I), wherein the residues R | 2015-05-21 |
20150141478 | SERIES OF DRUGS USING PHOTOFRIN TO CATALYZE DECOMPOSITION OF HYDROGEN PEROXIDE - The present invention relates to a series of new drugs which refer to chemical series capable of catalyzing the decomposition of H | 2015-05-21 |
20150141479 | COMPOSITIONS AND METHODS FOR THE TREATMENT OF MODERATE TO SEVERE PAIN - The invention relates to the compounds of formula I and formula II or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I or formula II, and methods for treating or preventing or modulating moderate to severe pain in a disease may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of pain, severe pain, chronic pain, chemotherapy induced pain, epilepsy, glaucoma, arthritis, tooth aches, inflammation, musculoskeletal pain, sciatica, radiculopathy pain, migraine, neuropathic pain, post herpetic neuralgia, neuralgia pain, multiple sclerosis, multiple sclerosis, restless legs syndrome (RLS), cluster headache, depression, fibromyalgia, amyotrophic lateral sclerosis (ALS), convulsions, partial seizures, mood-stabilizing agent and bipolar disorder. | 2015-05-21 |
20150141480 | CARBOHYDRATE-SELECTIVE RECEPTORS - The present invention is directed to a new class of synthetic carbohydrate receptor compounds comprising Formula I as described herein: (I). Other aspects of the present invention relate to pharmaceutical compositions and pharmaceutical delivery vehicles comprising the compound of Formula (I) The present invention is also directed to methods of treatment and diagnosis that involve the administration of a compound of Formula (I). | 2015-05-21 |
20150141481 | Treatment of Chronic Obstructive Pulmonary Disease with Nebulized Beta 2-Agonist or Combined Nebulized Beta 2-Agonist and Anticholinergic Administration - Inhalation solutions for administration of beta 2-agonists or combinations of muscarinic antagonists and beta 2-agonists for the treatment of breathing disorders, such as COPD, are provided. The inhalation solutions are administered by nebulization, particularly with a high efficiency nebulizer. | 2015-05-21 |
20150141482 | 1-(p-tolyl)cyclopropyl substituted Bridged Spiro[2.4]Heptane Derivatives as ALX Receptor Agonists - The present invention relates to 1-(p-tolyl)cyclopropyl substituted bridged spiro[2.4]heptane derivatives of formula (I), | 2015-05-21 |
20150141483 | CRYSTALLINE FORMS OF A 3-[2-METHANESULFONYL-1-(4-TRIFLUOROMETHYL-PHENOXY)ETHYL]PYRROLIDINE COMPOUND - The invention provides crystalline hydrochloride salts of (S)-3-[(S)-2-methanesulfonyl-1-(4-trifluoromethylphenoxy)ethyl]pyrrolidine. This invention also provides pharmaceutical compositions comprising the crystalline salts, processes and intermediates for preparing the crystalline salts, and methods of using the crystalline salts to treat diseases. | 2015-05-21 |
20150141484 | Methods, Compositions and Drug Delivery Systems for Intraocular Delivery of siRNA Molecules - Biocompatible intraocular drug delivery systems in the form of an implant for intraocular administration of siRNA molecules. The drug delivery systems may be placed in an eye to treat or reduce the occurrence of one or more ocular conditions, such as retinal damage, including glaucoma and proliferative vitreoretinopathy among others. | 2015-05-21 |
20150141485 | PROGNOSIS AND TREATMENT OF LUNG CANCER USING miRNA-135b - The present invention provides a method for the prognosis of lung cancer patient based on the expression levels of miRNA-135b, LZTS1, LATS2 and nuclear TAZ. The invention also provides a method for treatment of lung cancer. | 2015-05-21 |
20150141486 | COMPOSITION COMPRISING miRNA FOR ENHANCING RADIATION SENSITIVITY - Provided are a method of enhancing radiation sensitivity by using miR-499b-5p and a method of treating a radiation resistant cancer including administering miR-499b-5p. | 2015-05-21 |
20150141487 | OLIGORIBONUCLEOTIDES AND METHODS OF USE THEREOF FOR TREATMENT OF ALOPECIA, ACUTE RENAL FAILURE AND OTHER DISEASES - The invention relates to a double-stranded compound, preferably an oligoribonucleotide, which down-regulates the expression of a human p53 gene. The invention also relates to a pharmaceutical composition comprising the compound, or a vector capable of expressing the oligoribonucleotide compound, and a pharmaceutically acceptable carrier. The present invention also contemplates a method of treating a patient suffering from alopecia or acute renal failure or other diseases comprising administering to the patient the pharmaceutical composition in a therapeutically effective dose so as to thereby treat the patient. The alopecia may be induced by chemotherapy or radiotherapy, and the patient may be suffering from cancer, in particular breast cancer. | 2015-05-21 |
20150141488 | SMALL MOLECULE INHIBITORS OF RNA BINDING MOTIF (RBM) PROTEINS FOR THE TREATMENT OF ACUTE CELLULAR INJURY - A method of treating a cellular injury in a subject comprising administering to a subject in need thereof, a therapeutically effective amount of a compound of formula I: | 2015-05-21 |
20150141489 | METHODS OF TREATING AND DIAGNOSING DISEASES USING AGENTS THAT REGULATE THE ALTERNATIVE SPLICING PATHWAY - A method of determining a treatment for an inflammatory disorder in a subject, is disclosed. The method comprises determining an amount of SRSF6 in a sample from the subject, wherein an amount of the SRSF6 is indicative of the treatment. Methods of diagnosing inflammatory disorders and treating same are also disclosed. | 2015-05-21 |
20150141490 | PYRAZOLOTRIAZOLYL NUCLEOSIDE ANALOGUES AND OLIGONUCLEOTIDES COMPRISING THEM - The present invention relates to pyrazolotriazolyl nucleoside analogues, oligonucleotide comprising them, and uses thereof. Further the invention relates to a method for reducing gene expression in a cell comprising transfecting the cell with such an oligonucleotide. It has been found, in accordance with the present invention, that certain pyrazolotriazolyl-based nucleoside analogues such as 8-[3′-(2-cyanoethyl)-(N,Ndiisopropyl)]-phosphoramidite-(2′-deoxy-5′-dimethoxytrity 1-13-D-ribofuranozyl)-4-{N-benzoylamino)-pyrazolo[1,5a]-1,3,5-triazine, can be incorporated into oligonucleotides, substituting natural purine nucleosides and imparting acid stability and nuclease stability to the oligonucleotide. Furthermore, oligonucleotides comprising one or more such nucleoside analogues are capable of hybridizing with oligonucleotides having complementary sequences thereto in which no such analogues are incorporated. | 2015-05-21 |
20150141491 | Therapeutic Targets for Alzheimer's Disease - The present invention relates to novel methods for the prevention, treatment and diagnosis of Alzheimer's disease. In addition, the invention relates to methods for assessing an individual's susceptibility or pre-disposition to Alzheimer's disease. The methods of the present invention involve the use of therapeutic targets and diagnostic and/or predictive markers within the mTOR signalling pathway. The methods also involve screening subjects for genetic polymorphisms associated with rapamycin-sensitive genes. | 2015-05-21 |
20150141492 | RNA INTERFERENCE MEDIATING SMALL RNA MOLECULES - Double-stranded RNA (dsRNA) induces sequence-specific post-transcriptional gene silencing in many organisms by a process known as RNA interference (RNAi). Using a | 2015-05-21 |
20150141493 | ANTISENSE MODULATION OF GCCR EXPRESSION - Provided herein are methods, compounds, and compositions for reducing expression of GCCR mRNA and protein in an animal. Such methods, compounds, and compositions are useful to treat, prevent, delay, or ameliorate metabolic disease, for example, diabetes, or a symptom thereof. | 2015-05-21 |
20150141494 | TREATEMENT OF VASCULAR ENDOTHELIAL GROWTH FACTOR (VEGF) RELATED DISEASES BY INHIBITION OF NATURAL ANTISENSE TRANSCRIPT TO VEGF - Oligonucleotide compounds modulate expression and/or function of Vascular Endothelial Growth Factor (VEGF) polynucleotides and encoded products thereof. Methods for treating diseases associated with Vascular Endothelial Growth Factor (VEGF) comprise administering one or more Oligonucleotide compounds designed to inhibit the VEGF natural antisense transcript to patients. | 2015-05-21 |
20150141495 | DIFFERENTIAL EXPRESSION OF MICRORNAS IN NONFAILING VERSUS FAILING HUMAN HEARTS - The present invention discloses specific miRNAs as novel biomarkers and therapeutic targets in the treatment of heart failure. Methods of treating or preventing heart failure in a subject by administering mimics or inhibitors of these particular miRNAs are disclosed. A method of diagnosing or prognosing heart failure in a subject by determining the level of expression of one or more miRNAs is also described. | 2015-05-21 |