25th week of 2013 patent applcation highlights part 58 |
Patent application number | Title | Published |
20130157970 | NOVEL GLYCOSIDE COMPOUNDS - Compounds of formula (I): | 2013-06-20 |
20130157971 | 2'-FLUORONUCLEOSIDES - 2′-Fluoro-nucleoside compounds are disclosed which are useful in the treatment of hepatitis B infection, hepatitis C infection, HIV and abnormal cellular proliferation, including tumors and cancer. The compounds have the general formulae: | 2013-06-20 |
20130157972 | COMPOSITIONS INCLUDING TRICIRIBINE AND BORTEZOMIB AND DERIVATIVES THEREOF AND METHODS OF USE THEREOF - This application relates to combination therapies including triciribine and related compounds and bortezomib and derivatives thereof analogs and compositions with reduced toxicity for the treatment and prevention of tumors, cancer, and other disorders associated with abnormal cell proliferation. | 2013-06-20 |
20130157973 | PHARMACEUTICAL COMPOSITIONS AND METHODS FOR TREATING GASTROINTESTINAL INFECTIONS AND DISORDERS - Methods of treating gastrointestinal disorders, in a patient in need thereof, including disorders of the liver and pancreas, using an amount of an orally dosed TLR-7 compound in an amount sufficient to increase IFN in the gastrointestinal area, including the liver, but not significantly increasing systemic IFN. | 2013-06-20 |
20130157974 | Preparation Comprising Iron(III) Complex Compounds And Redox-Active Substance(s) - A preparation is disclosed that comprises one or more iron(III) complex compounds which have a redox potential at pH 7 of from −324 mV to −750 mV relative to a normal hydrogen electrode (NHE), and one or more redox-active substances, wherein the carbohydrates are selected from the group consisting of dextrans and hydrogenated dextrans, dextrins, oxidised or hydrogenated dextrins, as well as pullulan, oligomers thereof and/or hydrogenated pullulans, and wherein the redox-active substance(s) is/are selected from the group consisting of ascorbic acid; vitamin E; cysteine; physiologically acceptable phenols/polyphenols selected from the group consisting of quercetin, rutin, flavones, flavonoids, hydroquinones; and glutathione, and in particular is ascorbic acid. | 2013-06-20 |
20130157975 | AGENT FOR SUPPRESSING ELEVATION OF BLOOD ALCOHOL CONCENTRATION - An object of the present invention is to provide an agent for suppressing elevation of blood alcohol concentration and a method for suppressing elevation of blood alcohol concentration, the agent and the method enabling prevention of an intoxication state upon drinking and further prevention of hepatic dysfunctions due to drinking such as fatty liver. Provided are an agent for suppressing elevation of blood alcohol concentration, comprising a dextrin as an active ingredient, and a method for suppressing elevation of blood alcohol concentration, comprising, when alcohol is ingested, ingesting 0.5 parts by mass or more of a digestible dextrin and/or an indigestible dextrin relative to 1 part by mass of the ingested alcohol. | 2013-06-20 |
20130157976 | NOVEL PYRIDOPYRAZINES AND THEIR USE AS MODULATORS OF KINASES - The invention relates to novel pyrido[2,3-b]pyrazine derivatives of the general formulae (I) and (II), and to their preparation and use as medicaments, especially for the treatment of malignant disorders and other disorders based on pathological cell proliferations. | 2013-06-20 |
20130157977 | Benzimidazole Boronic Acid Derivatives As PI3 Kinase Inhibitors - This invention relates to the use of benzimidazole boronic acid derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3′ OH kinase family (hereinafter PI3 kinases), suitably, PI3Kα, PI3Kδ, PI3Kβ, and/or PI3Kγ. Suitably, the present invention relates to the use of benzimidazole boronic acids in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3Kβ selective benzimidazole boronic acid compounds for treating cancer. | 2013-06-20 |
20130157978 | PREPARATION FOR THE PREVENTION AND/OR TREATMENT OF VASCULAR DISORDERS - The present invention relates to a preparation suitable for the prevention and/or treatment of vascular disorders, comprising the following fractions:
| 2013-06-20 |
20130157979 | PHOSPHATE ESTERS OF GYRASE AND TOPOISOMERASE INHIBITORS - The present invention relates to phosphate esters of compounds that inhibit bacterial gyrase and/or Topoisomerase IV and pharmaceutical compositions thereof. These phosphate esters are useful for treating bacterial infections. | 2013-06-20 |
20130157980 | SUBSTITUTED INDOLE DERIVATIVES - The present invention relates to substituted indole derivatives, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them. | 2013-06-20 |
20130157981 | HETEROCYCLIC COMPOUNDS, MEDICAMENTS CONTAINING SAID COMPOUNDS, USE THEREOF AND PROCESSES FOR THE PREPARATION THEREOF - The present invention relates to compounds of general formula (I) | 2013-06-20 |
20130157982 | NOVEL COMPOUNDS AS RECEPTOR MODULATORS WITH THERAPEUTIC UTILITY - The present invention relates to novel amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. | 2013-06-20 |
20130157983 | Compounds for Use in the Treatment of Cancer - Pharmaceutical compositions comprise a first compound of Formula I or a physiologically acceptable salt thereof, and a cyto-protective amount of a manganese chelate of N,N′-dipyridoxyl ethylenedianiine-N,N′-diacetic acid (MnPLED): | 2013-06-20 |
20130157984 | PROSTAGLANDIN-BISPHOSPHONATE CONJUGATE COMPOUNDS, METHODS OF MAKING SAME, AND USES THEREOF - The invention provides in part, conjugate compounds. The invention also provides synthesis methods for making the compounds, and uses of the compounds. | 2013-06-20 |
20130157985 | PAIN RELIEF COMPOSITIONS, MANUFACTURE AND USES - The present invention relates to TRPV1 selective agonist topical compositions including capsaicinoid and analgesic agent compositions and methods of manufacture and methods of providing pain relief as well as treating a variety of disorders with such compositions. | 2013-06-20 |
20130157986 | NOVEL METHYLENEDIOXY PHENOLIC COMPOUNDS AND THEIR USE TO TREAT DISEASE - Pharmaceutical compounds and compositions are provided which are methylenedioxy phenolic compounds and their derivatives, along with methods of making them and methods of using them for therapeutic purposes. The compounds and compositions are advantageous in that they can be used to treat or prevent cardiovascular disease, vascular disease and/or inflammatory disease, as well as Type I and Type II Diabetes and Dyslipidemia patients at risk for hypertension, stroke, cardiovascular and renal disease. | 2013-06-20 |
20130157987 | 1-DEOXY ANALOGS OF 1,25-DIHYDROXYVITAMIN D3 COMPOUNDS - This present disclosure is directed to novel prodrugs of activated vitamin D3 compounds. The prodrugs can be designed to have one or more beneficial properties, such as selective inhibition of the enzyme CYP24, low calcemic activity, and anti-proliferative activity. Specifically, these prodrugs are 1-deoxy prohormones of active Vitamin D analogs, e.g. analogs of calcitriol. This disclosure is also directed to pharmaceutical and diagnostic compositions containing the prodrugs of the invention, and to their medical use, particularly as prodrugs in the treatment and/or prevention of diseases. | 2013-06-20 |
20130157988 | SUBSTITUTED ANDROST-4-ENE DIONES - The disclosure relates to novel C4 and C6 substituted androst-4-ene diones as well as andros-1,4-diene diones and derivatives thereof, their process of preparation, pharmaceutical compounds containing them, and the use of said compounds for the treatment of hormone-related disorders in mammals. This includes hormone-dependent cancers, particularly those caused by elevated levels of estrogen and its intermediates. These compounds can also be used in the treatment of other hormone-related disorders, including benign prostatic hyperplasia, cardiovascular disease, and neurodegenerative disorders. | 2013-06-20 |
20130157989 | 7-AZONIABICYCLO[2.2.1]HEPTANE DERIVATIVES, METHODS OF PRODUCTION, AND PHARMACEUTICAL USES THEREOF - Muscarinic acetylcholine receptor antagonists and methods of using them for the treatment of muscarinic acetylcholine receptor-mediated diseases, such as pulmonary diseases, are provided. | 2013-06-20 |
20130157990 | METHOD OF DRUG DETOXIFICATION - A method of detoxifying a patient addicted to at least one drug comprises the step of administering a first-medication component to the patient for mitigating drug withdrawal symptoms of the patient. The method further comprises the step of administering an anesthetic component to the patient for putting the patient in a sedated state. The method further comprises the step of administering a detoxification component to the patient for detoxifying the patient of the drug(s) while the patient is in the sedated state. The detoxification component can comprise naloxone. The method further comprises the step of administering a second-medication component to the patient for further mitigating drug withdrawal symptoms of the patient while the patient is in the sedated state. The second-medication component can comprise naltrexone. The method further comprises the step of terminating administration of the anesthetic component to the patient for reviving the patient from the sedated state. | 2013-06-20 |
20130157991 | Dry Powder Inhalation Drug Products Exhibiting Moisture Control Properties and Methods of Administering the Same - A drug product comprises a dry powder inhalation device containing one or more pharmaceutical compositions present therein, wherein the one or more pharmaceutical compositions comprise active ingredients (I) 4-{(1R)-2-[(6-{2-[(2,6-dichlorobenzyl)oxy]ethoxy}hexyl)amino]-1-hydroxyethyl}-2-(hydroxymethyl)phenol, or a salt thereof, and (II) (6α,11β,16α,17α)-6,9-difluoro-17-{[(fluoromethyl)thio]carbonyl}-11-hydroxy-16-methyl-3-oxoandrosta-1,4-dien-17-yl 2-furancarboxylate or a solvate thereof; a hygroscopic material; and a package which encompasses the dry powder inhalation device and the hygroscopic material defining an enclosed volume therein; wherein each of the active ingredients (I) and (II) are present in the same or different pharmaceutical compositions, and wherein the enclosed volume within the package exhibits a Relative Humidity of from 20% to 40%. | 2013-06-20 |
20130157992 | SUSTAINED DRUG RELEASE AND IMPROVED PRODUCT STABILITY USING NON-COVALENT PARTICLE COATING METHODS - The present invention relates to improved methods of making compositions and compositions made by these methods having improved stability and/or extended release of an active agent or drug upon administration. These compositions may generally comprise an active agent or drug non-covalently immobilized or bound to an excipient substrate. The active agent or drug may include a wide variety of drugs. Binding of the active agent or drug to the substrate may be achieved by evaporating a solvent containing the active agent dissolved therein or by triggering co-precipitation by addition of a precipitating solvent. Additional steps of vacuum removal of surrounding atmosphere and replacement with inert gas may provide additional stability. Present methods and compositions also facilitate manufacturing of drug products and may make these processes safer in some cases. The present invention further provides improved methods of treatment or administration, which may take advantage of improvements with present compositions. | 2013-06-20 |
20130157993 | USE OF 5ALPHA-ANDROSTANE (ALKYL)-3BETA,5,6BETA-TRIOL IN PREPARATION OF NEUROPROTECTIVE DRUGS - Disclosed is the use of 5α-androstane(alkyl)-3β,5,6β-triol in preparing neuroprotective drugs. The compound has significant protective effect against neuron injuries caused by cerebral ischemia, spinal cord isehemia or hypoxia and has no obvious toxic reaction within effective dose thereof. | 2013-06-20 |
20130157994 | HIGH-PURITY TEXAPHYRIN METAL COMPLEXES - Disclosed herein are the methods and compositions for the improved synthesis of texaphyrin metal complexes. The improved synthesis results in high-purity compositions of texaphyrin metal complexes in which more than about 98% of the texaphyrin metal complexes in the composition have the same structure and/or the same molecular weight. Further described herein are pharmaceutical compositions comprising such high-purity compositions, and the use of such high-purity compositions in the treatment of cancer and cardiovascular diseases and disorders. | 2013-06-20 |
20130157995 | NICOTINE COMPOUNDS AND ANALOGS THEREOF, SYNTHETIC METHODS OF MAKING COMPOUNDS, AND METHODS OF USE - Embodiments of the present disclosure provide for compounds such as those shown in FIG. | 2013-06-20 |
20130157996 | TRPM8 ANTAGONISTS AND THEIR USE IN TREATMENTS - Compounds of Formula I are useful as antagonists of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: | 2013-06-20 |
20130157997 | BENZIMIDAZOLE ANALOGUES FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS - Compounds represented by formula I: | 2013-06-20 |
20130157998 | HETEROCYCLIC INHIBITORS OF GLUTAMINASE - The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treatment using the novel heterocyclic compounds of the invention. | 2013-06-20 |
20130157999 | AMINOPYRIMIDINE DERIVATIVES AS LRRK2 MODULATORS - Specific Compounds of formula I: | 2013-06-20 |
20130158000 | Disubstituted benzothienyl-pyrrolotriazines and uses thereof - This invention relates to novel substituted 5-(1-benzothiophen-2-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives having protein tyrosine kinase inhibitory activities, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating proliferative disorders, in particular cancer and tumor diseases. | 2013-06-20 |
20130158001 | SUBSTITUTED 3-PHENYL-1,2,4-OXADIAZOLE COMPOUNDS - Disclosed are compounds of Formula (I): (I) or stereoisomers, salts, or prodrugs thereof, wherein: (i) R1 and R2 are independently C | 2013-06-20 |
20130158002 | POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 - The present invention is directed to 5-substituted 1,3-dihydro-2,1,3-benzothiadiazole 2,2-dioxide and 1,3-dihydro[1,2,5]thiadiazolo[3,4-b]pyridine 2,2,-dioxide derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved. | 2013-06-20 |
20130158003 | HETEROARYL COMPOUNDS AND METHODS OF USE THEREOF - Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes. | 2013-06-20 |
20130158004 | Azetidine Derivatives - Azetidine derivatives of which the following is exemplary | 2013-06-20 |
20130158005 | PYRIMIDINE DERIVATIVES AS FAK INHIBITORS - Compounds of the formula (I), in which R | 2013-06-20 |
20130158006 | AMINOPYRIMIDINE DERIVATIVES AS LRRK2 MODULATORS - Compounds of the formula I: | 2013-06-20 |
20130158007 | Fatty 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 fatty acids to quetiapine. Pharmaceutical compositions and methods of synthesizing conjugates of the present technology are also provided. Methods of treating patients with the compositions of the present technology are also provided. | 2013-06-20 |
20130158008 | SOLID IVABRADINE-CONTAINING COMPOSITION - The present invention relates to a solid composition containing ivabradine or a pharmaceutically acceptable salt thereof. Further, the invention relates to a method for the preparation of such a composition as well as a pharmaceutical product comprising such a composition. | 2013-06-20 |
20130158009 | PIPERIDINYL-SUBSTITUTED LACTAMS AS GPR119 MODULATORS - Compounds of Formula (I): and pharmaceutically acceptable salts thereof in which X | 2013-06-20 |
20130158010 | METHODS FOR INCREASING THE STABILIZATION OF HYPOXIA INDUCIBLE FACTOR-1 ALPHA - Disclosed herein are methods for controlling the activity of hypoxia-inducible transcription factor 1-alpha (HIF-1α) and diseases, conditions, or syndromes related thereto, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia. Further disclosed are pharmaceutical compositions comprising HIF-1α prolyl hydroxylase inhibitors useful in treating diseases, conditions, and/or syndromes related thereto the activity of HIF-1α. | 2013-06-20 |
20130158011 | NOVEL COMPOUNDS - This invention relates to compounds of formula I | 2013-06-20 |
20130158012 | USE AND COMPOSITION FOR TREATING DEMENTIA - There is described a method for increasing the maximal tolerated dose and thus the efficacy of an acetyl choline esterase inhibitor (AChEI) in a patient suffering from an Alzheimer type dementia by decreasing concomitant adverse effects by administration of said AChEI in combination with a non-selective, peripheral anticholinergic agent, whereby an enhanced acetyl choline esterase inhibition in the CNS of said patient is achieved and alleviation of the symptoms of Alzheimer type dementia in said patient is thereby improved to a greater extent. The use of a non-selective, peripheral anticholinergic agent (nsPAChA) for the preparation of a pharmaceutical composition for increasing the maximal tolerated dose and thus the efficacy of an acetyl choline esterase inhibitor (AChEI) in a patient suffering from an Alzheimer type dementia and pharmaceutical compositions comprising a non-selective peripheral anticholinergic agent of formula II as illustrated in the description and an acetylcholine esterase inhibitor are also described. | 2013-06-20 |
20130158013 | PROCESSES FOR THE PREPARATION OF 5-HT2C RECEPTOR AGONISTS - Processes and intermediates for preparing salts of the 5-HT | 2013-06-20 |
20130158014 | METHOD FOR TREATING DISEASES ASSOCIATED WITH ALTERATIONS IN CELLULAR INTEGRITY USING RHO KINASE INHIBITOR COMPOUNDS - This invention is directed to methods of preventing or treating diseases or conditions associated with alterations in cellular integrity including alterations in endothelial permeability, excessive cell proliferation or tissue remodeling. Particularly, this invention is directed to methods of treating diabetic nephropathy, malaria, or cancer. The method comprises identifying a subject in need of the treatment, and administering to the subject an effective amount of a novel rho kinase inhibitor compound to treat the disease. | 2013-06-20 |
20130158015 | DUAL MECHANISM INHIBITORS FOR THE TREATMENT OF DISEASE - Provided are compounds that are inhibitors of both rho kinase and of a monoamine transporter (MAT) act to improve the disease state or condition. Further provided are compositions comprising the compounds. Further provided are methods for treating diseases or conditions, the methods comprising administering compounds according to the invention. One such disease may be glaucoma for which, among other beneficial effects, a marked reduction in intraocular pressure (IOP) may be achieved. | 2013-06-20 |
20130158016 | ANESTHETIC ASSOCIATION, ANESTHETIC COMPOSITION, AND ANESTHETIC MEDICAMENT FOR VETERINARY USE - The present invention relates to a new association of active ingredients working as anesthetic and pre-anesthetic formulated in a composition containing anesthetics and analgesics suitable for use in surgical and pre-surgical procedures and others which require sedation, tranquilization, chemical restraint and pre-anesthetic medication. More specifically the present invention relates to a new association comprising the active ingredients ketamine, preferably the isomer S-ketamine(+), midazolam and tramadol, formulated in true solution for parenteral use. The present invention also contemplates an anesthetic drug for veterinary use for parenteral use. | 2013-06-20 |
20130158017 | METHODS FOR TREATING OR PREVENTING CANCER AND NEURODEGENERATIVE DISEASES - Provided are methods of treating or preventing a neurodegenerative disease comprising administering to a subject having a neurodegenerative disease an effective amount of a compound of Formula I: | 2013-06-20 |
20130158018 | Heteroaryl Nitrile Compounds Useful as Inhibitors of Cathepsin-S - Disclosed are Cathepsin-S reversible inhibitor compounds of the formula (I) which are useful in the treatment of autoimmune and other diseases. Also disclosed are pharmaceutical compositions containing the same, and methods of making and using the same. | 2013-06-20 |
20130158019 | PYRIMIDINE COMPOUNDS THAT INHIBIT ANAPLASTIC LYMPHOMA KINASE - Compounds of Formula I are useful inhibitors of anaplastic lymphoma kinase. Compounds of Formula I have the following structure: | 2013-06-20 |
20130158020 | INDAZOLE DERIVATIVES USEFUL AS ERK INHIBITORS - The present invention provides a compound of the Formula I: Formula I or a pharmaceutically acceptable salt, solvate or ester thereof, wherein R, R1, R2, R3, R4, X, m and n are as defined herein. The compounds are ERK inhibitors. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same. | 2013-06-20 |
20130158021 | AMINO ACID-, PEPTIDE-AND POLYPEPTIDE-LIPIDS, ISOMERS, COMPOSITIONS, AND USES THEREOF - Described herein are compounds and compositions characterized, in certain embodiments, by conjugation of various groups, such as lipophilic groups, to an amino or amide group of an amino acid, a linear or cyclic peptide, a linear or cyclic polypeptide, or structural isomer thereof, to provide compounds of the present invention, collectively referred to herein as “APPLs”. Such APPLs are deemed useful for a variety of applications, such as, for example, improved nucleotide delivery. Exemplary APPLs include, but are not limited to, compounds of Formula (I), (II), (III), (IV), (V), and (VI), and salts thereof, as described herein: | 2013-06-20 |
20130158022 | Acrylamide Compounds And Use Thereof For Inhibiting Apoptosis - The present invention relates to a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate of the compound, and to a composition comprising the compound of Formula I, or the isomer, pharmaceutically acceptable salt and solvate thereof, and a pharmaceutically acceptable carrier, excipient or diluents. The present invention also relates to use of the compound of Formula I, or the isomer, pharmaceutically acceptable salt and solvate thereof for combating apoptosis, preventing or treating a disease or disorder associated with apoptosis; and especially use for protecting cardiomyocyte, and for preventing or treating a disease or disorder associated with cardiomyocyte apoptosis. | 2013-06-20 |
20130158023 | IDENTIFICATION OF GENE EXPRESSION AS A PREDICTIVE BIOMARKER FOR LKB1 STATUS - Provided herein are methods for predicting the LKB1 status of a patient or a biological sample, comprising the measurement of particular gene expression levels relative to a set of reference levels that represent the gene expression level of a biological wild-type sample without LKB1 gene or protein loss or mutation and the gene expression level of a reference sample with LKB1 gene or protein loss or mutation. Further provided herein are methods for treating and/or preventing a cancer or a tumor syndrome in a patient, comprising administering an effective amount of a TOR kinase inhibitor to a patient having cancer or a tumor syndrome, characterized by particular gene expression levels. | 2013-06-20 |
20130158024 | TRICYCLIC NECROSTATIN COMPOUNDS - The present invention features compounds, pharmaceutical compositions, and methods for treating trauma, ischemia, stroke, degenerative diseases associated with cellular necrosis, and other conditions. Screening assays for identifying compounds useful for treating these conditions are also described. | 2013-06-20 |
20130158025 | NOVEL COMPOUND ACTING AS A CANNABINOID RECEPTOR-1 INHIBITOR - Disclosed is a novel compound acting as a cannabinoid receptor 1 inhibitor, a prodrug thereof, an isomer thereof, a pharmaceutically acceptable salt thereof, a hydrate thereof or a solvate thereof. The novel compound or the like is useful for preventing or treating diseases mediated by the cannabinoid receptor-1. | 2013-06-20 |
20130158026 | CHROMENONE DERIVATIVES - The invention concerns chromenone derivatives of Formula I | 2013-06-20 |
20130158027 | PYRAZOLO PYRIDINE DERIVATIVES AS NADPH OXIDASE INHIBITORS - The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase). | 2013-06-20 |
20130158028 | USE OF STIMULATORS AND ACTIVATORS OF SOLUBLE GUANYLATE CYCLASE FOR TREATING SICKLE-CELL ANEMIA AND CONSERVING BLOOD SUBSTITUTES - The present invention relates to the novel use of stimulators and activators of soluble guanylate cyclase for the treatment of sickle cell anemia and for the preservation of blood substitutes. The present invention furthermore relates to the use of stimulators and activators of soluble guanylate cyclase in combination with PDE5 inhibitors for the treatment of sickle cell anemia and for the preservation of blood substitutes. | 2013-06-20 |
20130158029 | SIGMA RECEPTOR INHIBITORS - The invention refers to compounds of general formula (I) | 2013-06-20 |
20130158030 | PYRROLYL SUBSTITUTED DIHYDROINDOL-2-ONE DERIVATIVES, PREPARATION METHODS AND USES THEREOF - Provided are pyrrolyl substituted dihydroindol-2-one derivatives represented by formula (I), pharmaceutically acceptable salts or solvates of said derivatives, or solvates of said salts, which are effective tyrosine kinase inhibitors. Also provided are the preparation methods of the above compounds, pharmaceutical compositions containing these compounds, and the use of these compounds in manufacturing drugs useful for the treatment or adjunctive treatment of tumors medicated by tyrosine kinases or proliferation or migration of tumor cells driven by tyrosine kinases in mammals (including human). | 2013-06-20 |
20130158031 | ALKYNE-BRIDGED HETERO-AROMATICS AND USES THEREOF - This invention relates to novel alkyne-bridged hetero-aromatics as described in the specification which are PDE10A inhibitors and useful for the treatment of neurological, psychiatric disorder, metabolic disorders, such as Schizophrenia, Parkinson's disease, Huntington's disease, Alzheimer's disease, learning memory disorder, drug addiction (abuse), sleeping disorder, depression, obesity, non-insulin dependent diabetes, bipolar disorder, obsessive compulsive disorder, or pain; to process for their preparation; to pharmaceutical compositions comprising them; and to methods of using them. | 2013-06-20 |
20130158032 | AMINOPYRIMIDINE DERIVATIVES AS LRRK2 MODULATORS - Compounds of the formula I: | 2013-06-20 |
20130158034 | TRPM8 ANTAGONISTS AND THEIR USE IN TREATMENTS - Compounds of Formula I are useful as antagonists of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: | 2013-06-20 |
20130158035 | ANTIMETASTATIC COMPOUNDS - Screening methods for identifying compounds and compounds and pharmaceutical compositions for treating and preventing cancer are disclosed. The compounds affect signal transduction downstream of the MET receptor. | 2013-06-20 |
20130158036 | N,N-DISUBSTITUTED AMINOALKYLBIPHENYL ANTAGONISTS OF PROSTAGLANDIN D2 RECEPTORS - Described herein are compounds that are antagonists of PGD | 2013-06-20 |
20130158037 | COMPOUNDS AND METHODS FOR TREATING TUBERCULOSIS INFECTION - The present invention provides compounds which are potent inhibitors against Lpd activity, PDH activity, and/or the growth of | 2013-06-20 |
20130158038 | NOVEL COMPOUNDS - This invention relates to compounds of formula I | 2013-06-20 |
20130158039 | N-((1R,2S,5R)-5-(TERT-BUTYLAMINO)-2-((S)-3-(7-TERT-BUTYLPYRAZOLO[1,5-A][1,- 3,5]TRIAZIN-4-YLAMINO)-2-OXOPYRROLIDIN-1-YL)CYCLOHEXYL)ACETAMIDE, A DUAL MODULATOR OF CHEMOKINE RECEPTOR ACTIVITY, CRYSTALLINE FORMS AND PROCESSES - The present invention provides a novel antagonist: N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide: | 2013-06-20 |
20130158040 | DIAZAINDOLE INHIBITORS OF CRAC - Disclosed are compounds of Formula (I): | 2013-06-20 |
20130158041 | Tyrosine Kinase Inhibitors - The present invention relates to pyridazinthione derivatives that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also relates to compositions which comprise these compounds, and methods of using them to treat cancer in mammals. | 2013-06-20 |
20130158042 | NOVEL COMPOUNDS - This invention relates to compounds of formula I | 2013-06-20 |
20130158043 | PAK INHIBITORS FOR THE TREATMENT OF CANCER - Provided herein are methods of utilizing PAK inhibitors for the treatment of cancer. Further provided herein are compounds and formulations utilized for the treatment of cancer. | 2013-06-20 |
20130158044 | PIPERAZINE-SUBSTITUTED BENZOTHIOPHENES FOR TREATMENT OF MENTAL DISORDERS - The present invention provides a heterocyclic compound represented by the general formula (1): The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety. | 2013-06-20 |
20130158045 | PROLYL HYDROXYLASE INHIBITORS - Disclosed herein are prolyl hydroxylase inhibitors that can stabilize hypoxia inducible factor-1 alpha (HIF-1α), as well as hypoxia inducible factor-2 (HIF-2). Also disclosed herein are pharmaceutical compositions comprising one or more of the disclosed compounds. Yet further disclosed are methods for stimulating the cellular immune response in a mammal such as increasing phagocytosis, for example, prolonging the life of phagocytes, inter alia, kerotyiocytes, neutrophils. As such the disclosed compounds provide methods for treating diseases that relate to the body's immune response. | 2013-06-20 |
20130158046 | BIOCOMPATIBLE BIODEGRADABLE FUMAGILLIN ANALOG CONJUGATES - Fumagillin analog polymer conjugates, methods of making fumagillin analog polymer conjugates, compositions comprising a polymer conjugate of a fumagillin analog, and methods for treating cancer, or treating angiogenic diseases comprising administering to a subject in need thereof an effective amount of a polymer conjugate of a fumagillin analog, are described. Also described are novel fumagillin analogs, methods of making fumagillin analogs, compositions comprising at least one fumagillin analog, and methods for treating cancer, or treating angiogenic diseases comprising administering to a subject in need thereof an effective amount of a fumagillin analog. | 2013-06-20 |
20130158047 | NOVEL HETEROCYCLIC COMPOUND, AND COMPOSITION FOR TREATING INFLAMMATORY DISEASES USING SAME - Provided are heterocyclic compounds, having effects of treating and preventing inflammatory diseases and treating skin wounds, and particularly, exhibiting effects of recovering disrupted skin barriers, mitigating inflammation, and pruritus. Also, a composition containing the compound as an effective component can be used to mitigate various inflammatory diseases and protease activated receptor-2 (PAR-2)-overexpressed diseases, and can be particularly used as a composition having an anti-inflammatory function in inflammatory skin diseases including atopic dermatitis and the like, by inhibiting PAR-2 activity. | 2013-06-20 |
20130158048 | Formulation Solution Adapted to Prolong Plasma Times of Drugs in Mammals Including Humans - In the method of administering rifampicin to a human subject, the improvement wherein a prolongation composition is also administered, said prolongation composition comprising: | 2013-06-20 |
20130158049 | 7-AZAINDOLE INHIBITORS OF CRAC - Disclosed are compounds of Formula (I): | 2013-06-20 |
20130158050 | PIPERIDINE DERIVATIVES - The present invention relates to a compound of formula I | 2013-06-20 |
20130158051 | HETEROCYCLIC CARBOXYLIC ACID DERIVATIVES HAVING A 2,5,7-SUBSTITUTED OXAZOLOPYRIMIDINE RING - The invention relates to oxazolopyrimidine compounds of formula (I), where A, R | 2013-06-20 |
20130158052 | PYRIMIDINE CLASSICAL CANNABINOID COMPOUNDS AND RELATED METHODS OF USE - Disclosed are compounds of the formula I: | 2013-06-20 |
20130158053 | CRYSTALLINE FORMS OF 3-[5-CHLORO-4-[(2,4-DIFLUOROBENZYL) OXY]-6-OXOPYRIMIDIN-1(6H)-YL]-N-(2-HYDROXYETHYL)-4-METHYLBENZAMIDE - Crystalline forms of the p38 kinase inhibitor 3-[5-chloro-4-[(2,4-difluorobenzyl)oxy]-6-oxopyrimidin-1(6H)-yl]-N-(2-hydroxyethyl)-4-methylbenzamide is provided. Also provided are combinations and pharmaceutical compositions comprising the crystalline forms, and methods for the prophylaxis and/or treatment of a p38 kinase-mediated condition comprising administering to a subject a therapeutically effective amount of the crystalline forms. | 2013-06-20 |
20130158054 | POLYMORPHS OF 3-(E)-2--3-METHOXYACRYLATE - The present invention relates to novel crystalline polymorphic and amorphous forms of the compound (E)-2-{2-[6-(2-cyanophenoxy)pyrimidin-4-yloxy]phenyl}-3-methoxy-acrylate (azoxystrobin). Infrared Raman spectra, X-ray powder diffraction pattern and differential scanning calorimetry thermogram of two polymorphs “A” and “B” are provided. Further, the present invention also provides methods for preparing the novel polymorphic forms “A” and “B”, as well as processes for producing mixtures of the polymorphs, and a process for preparing amorphous azoxystrobin. Yet further, the present invention provides anti-fungal compositions comprising the novel crystalline polymorphs “A” and “B” or amorphous azoxystrobin, which are useful for controlling and combating fungi grown on agricultural and horticultural crops and up-land, and methods of using the same as pesticidal agents for combating fungi on agricultural and horticultural crops. | 2013-06-20 |
20130158055 | Prevention Of Pancreatic Beta Cell Degeneration - The present invention relates to compounds and pharmaceutically acceptable salts thereof and formulations comprising the compounds or a pharmaceutically acceptable salts thereof that are useful in methods of preventing pancreatic beta cell degeneration or methods of treating a disorder associated with pancreatic beta cell degeneration, such as type I diabetes. | 2013-06-20 |
20130158056 | ALKOXY PYRIMIDINE PDE10 INHIBITORS - The present invention is directed to 2-alkoxy pyrimidine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction. | 2013-06-20 |
20130158057 | AMINOPYRIMIDINE DERIVATIVES AS LRRK2 MODULATORS - Compounds of the formula I: | 2013-06-20 |
20130158058 | HYPERCHOLESTEROLEMIA AND TENDINOUS INJURIES - This invention provides compositions and methods of inhibiting, suppressing, or treating a tendinous or musculoskeletal soft tissue injury. The invention further provides a method of ameliorating symptoms associated with a tendinous or musculoskeletal soft tissue injury. Additionally, the invention provides methods for evaluating the risk of developing a tendinous or musculoskeletal soft tissue injury. | 2013-06-20 |
20130158059 | NILOTINIB SALTS AND CRYSTALLINE FORMS THEREOF - Nilotinib salts and crystalline forms thereof have been prepared and characterized. | 2013-06-20 |
20130158061 | CONTROLLED RELEASE HYDROCODONE - A solid oral controlled-release dosage form of hydrocodone is disclosed, the dosage form comprising an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof, and controlled release material. | 2013-06-20 |
20130158062 | MULTI-ARM POLYMER PRODRUGS - Provided herein are water-soluble prodrugs, compositions comprising such prodrugs, and related methods of making and administering the same. The prodrugs of the invention comprise a water-soluble polymer having three or more arms, at least three of which are typically covalently attached to an active agent, e.g., a small molecule. The conjugates of the invention provide an optimal balance of polymer size and structure for achieving improved drug loading, since the conjugates of the invention possess three or more active agents releasably attached to a multi-armed water-soluble polymer. The prodrugs of the invention are therapeutically effective, and exhibit improved properties in-vivo when compared to unmodified parent drug. | 2013-06-20 |
20130158063 | Compounds, Compositions and Methods Related to PPAR Antagonists - Disclosed are compounds, compositions and methods related PPAR antagonists. Certain compounds are effective at inhibiting PPARs. The compositions can be used to inhibit PPARs, treat cancer and treat metabolic disorders. | 2013-06-20 |
20130158064 | NOVEL ISO-ERGOLINE DERIVATIVES - Provided herein are novel iso-ergoline derivatives and compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT | 2013-06-20 |
20130158065 | 1,2,3,4,5,6,7,8-OCTOHYDRO-9-PHENYLACETAMIDOACRIDINE, THE PREPARATION METHOD AND MEDICAL USE THEREOF - Disclosed are 1,2,3,4,5,6,7,8-octohydro-9-phenylacetamidoacridine and the salt thereof, as well as the preparation method and medical use thereof. The compound can be useful for the preparation of medicaments for treating cardiovascular diseases, especially arrhythmia. | 2013-06-20 |
20130158066 | 4-AZAINDOLE INHIBITORS OF CRAC - Disclosed are compounds of Formula (I): | 2013-06-20 |
20130158067 | TRPV1 Antagonists - Disclosed herein are compounds of formula (I): | 2013-06-20 |
20130158068 | DICARBOXIMIDE DERIVATIVES OF BERBAMINE, THE PREPARATION AND USE THEREOF - The present invention relates to a novel dicarboximide derivative of berbamine represented by formula I, including, but not limited to, a phthalimide derivative of berbamine and an aromatic heterocyclic dicarboximide derivative of berbamine, or a pharmaceutically acceptable salt thereof, to a process for preparation of the same, to a pharmaceutical composition comprising said compound and to use thereof in manufacture of an antitumor medicament. | 2013-06-20 |
20130158069 | PREVENTIVE AND/OR THERAPEUTIC AGENT FOR THROMBOEMBOLISM IN THROMBOEMBOLISM PATIENT WITH SEVERE RENAL IMPAIRMENT - It is intended to provide a highly safe, orally administrable preventive and/or therapeutic agent for thrombosis and/or embolism that can be applied to a thrombosis and/or embolism patient with severe renal impairment. The present inventors have found that even for a thrombosis and/or embolism patient with severe renal impairment, use of edoxaban at a dose of 15 mg once a day can effectively prevent thrombosis and/or embolism while avoiding the risk of bleeding. The present inventors have also found that even for a thrombosis and/or embolism patient with severe renal impairment, edoxaban at a dose of 15 mg once a day can effectively prevent thrombosis and/or embolism with safety over a long period. | 2013-06-20 |
20130158070 | CONJUGATES OF POLYUNSATURATED FATTY ACIDS AND AMINE-CONTAINING COMPOUNDS AND USES THEREOF - Novel chemical conjugates derived from unsaturated fatty acids and therapeutically active agents, are disclosed. The chemical conjugates are designed and characterized as COX-2 and/or 5-LOX inhibitors and are useful in the treatment of inflammatory diseases and disorders such as Alzheimer's disease, Parkinson's disease, asthma, osteoarthritis, rheumatoid arthritis, pain, primary dysmenorrhea, Crohn's disease and ulcerative colitis. | 2013-06-20 |
20130158071 | 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. | 2013-06-20 |