38th week of 2014 patent applcation highlights part 158 |
Patent application number | Title | Published |
20140274994 | STABILIZING CEFTOLOZANE - Pharmaceutical compositions can include an amount of a ceftolozane and a stabilizing agent in a formulation for parenteral administration. | 2014-09-18 |
20140274995 | PARENTERAL CEFTOLOZANE ANTIBIOTIC COMPOSITIONS - Parenteral pharmaceutical compositions including ceftolozane and tazobactam can be formulated to provide desired levels of osmolality, pH and ceftolozane stability. | 2014-09-18 |
20140274996 | TAZOBACTAM AND CEFTOLOZANE ANTIBIOTIC COMPOSITIONS - This disclosure provides pharmaceutical compositions comprising ceftolozane, pharmaceutical compositions comprising ceftolozane and tazobactam, methods of making those compositions, and related methods and uses of these compositions. | 2014-09-18 |
20140274997 | CEPHALOSPORIN PHARMACEUTICAL COMPOSITIONS - Pharmaceutical compositions including a cephalosporin disclosed herein as having the structure of formula (III). | 2014-09-18 |
20140274998 | CEFTOLOZANE-TAZOBACTAM PHARMACEUTICAL COMPOSITIONS - Pharmaceutical compositions can include ceftolozane lyophilized in the absence of tazobactam. | 2014-09-18 |
20140274999 | CEPHALOSPORIN COMPOSITIONS AND METHODS OF MANUFACTURE - Provided herein is a method for the synthesis of cephalosporin antibiotic compounds comprising the conversion of a protected 7-amino group into a 7-carboxamide moiety in a single step. | 2014-09-18 |
20140275000 | CEFTOLOZANE PHARMACEUTICAL COMPOSITIONS - Pharmaceutical compositions can include an amount of sodium chloride effective to stabilize ceftolozane in an antibiotic formulation. | 2014-09-18 |
20140275001 | CRYSTALLINE FORM OF A BETA-LACTAMASE INHIBITOR - This disclosure provides compositions containing solid forms of sodium (2S,5R)-2-(1,3,4-oxadiazol-2-yl)-7-oxo-1,6-diazabicyclo[3.2.1]octan-6-yl sulfate, and methods of manufacturing and using these compositions. | 2014-09-18 |
20140275002 | AZETIDINYLOXYPHENYLPYRROLIDINE COMPOUNDS - The invention provides certain azetidinyloxyphenylpyrrolidine compounds, particularly compounds of formula I wherein R is hydrogen or methyl, and pharmaceutical compositions thereof. The invention further provides methods of using a compound of formula I to treat overactive bladder. | 2014-09-18 |
20140275003 | BIARYL AMIDE COMPOUNDS AS KINASE INHIBITORS - The present invention provides compounds of Formula (I) | 2014-09-18 |
20140275004 | PYRROLOPYRIMINDINE CDK9 KINASE INHIBITORS - Disclosed are compound of Formula (Ia), | 2014-09-18 |
20140275005 | SUBSTITUTED PHENYL CYCLOALKYL PYRROLIDINE (PIPERIDINE) SPIROLACTAMS AND AMIDES, PREPARATION AND THERAPEUTIC USE THEREOF - The present disclosure relates to a series of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and formula (Ib). | 2014-09-18 |
20140275006 | AZOLE DERIVATIVE - The present invention provides agents for treating or preventing diseases such as mood disorder, anxiety disorder, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal disease, drug addiction, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head injury, inflammation, immune-related disease, alopecia, and so forth. | 2014-09-18 |
20140275007 | OXAMAZIN ANTIBIOTICS - Disclosed herein are oxamazin monobactam compounds and their use as antibiotics resistant to degradation by β-lactamases. Also disclosed are pharmaceutical compositions containing the compounds and methods of synthesis. | 2014-09-18 |
20140275008 | 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. | 2014-09-18 |
20140275009 | COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE - The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. | 2014-09-18 |
20140275010 | QUATERNARY SALTS - The present invention provides quaternary salts, such as those of Formula I: | 2014-09-18 |
20140275011 | PYRIDINE CDK9 KINASE INHIBITORS - Disclosed are compound of Formula (Ia), | 2014-09-18 |
20140275012 | HETEROAROMATIC COMPOUNDS AS BTK INHIBITORS - The present invention encompasses compounds of the formula (I) | 2014-09-18 |
20140275013 | COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF PARASITIC DISEASES - The present invention provides compounds of formula I: | 2014-09-18 |
20140275014 | HETEROAROMATIC COMPOUNDS AS BTK INHIBITORS - The present invention encompasses compounds of the formula (I) | 2014-09-18 |
20140275015 | P2X7 MODULATORS - The present invention is directed to compounds of Formulas (I, IIa and IIb): | 2014-09-18 |
20140275016 | N-Acyl-N'-(pyridin-2-yl) Ureas and Analogs Exhibiting Anti-Cancer and Anti-Proliferative Activities - Described are compounds of Formula 1 | 2014-09-18 |
20140275017 | CGRP RECEPTOR ANTAGONISTS - Compounds of Formula I: | 2014-09-18 |
20140275018 | NITROGEN CONTAINING COMPOUNDS - Compounds of Formula (I), their preparation and use in preventing or treating bacterial infection is disclosed. | 2014-09-18 |
20140275019 | TETRAHYDROPYRIDINE DERIVATIVES AS FABI INHIBITORS - The present invention relates to tetrahydropyridine derivatives of formula (1) which may be therapeutically useful as anti-bacterial agents, more particularly FabI inhibitors. | 2014-09-18 |
20140275020 | INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL - This invention relates to compounds of Formula I having the following general structure: | 2014-09-18 |
20140275021 | COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE - The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. | 2014-09-18 |
20140275022 | SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF - The invention provides compounds for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc. | 2014-09-18 |
20140275023 | Substituted Tricyclic Pyrazolo-Pyrimidine Compounds - The present invention relates to substituted tricyclic pyrazolo-pyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted tricyclic pyrazolo-pyrimidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof. | 2014-09-18 |
20140275024 | DNA-PK INHIBITORS - The present invention relates to compounds useful as inhibitors of DNA-PK. 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. | 2014-09-18 |
20140275025 | SUBSTITUTED 2-AZA-BICYCLO[2.2.1]HEPTANE-3-CARBOXYLIC ACID (BENZYL-CYANO-METHYL)-AMIDES INHIBITORS OF CATHEPSIN C - This invention relates to 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid(benzyl-cyano-methyl)-amides of formula 1 | 2014-09-18 |
20140275026 | DIHYDRO-PYRROLOPYRIDINONE INHIBITORS - The present invention provides for compounds of formula (I) | 2014-09-18 |
20140275027 | PYRROLO[2,3-B]PYRIDINE CDK9 KINASE INHIBITORS - Disclosed are compounds of Formula (IIIa), | 2014-09-18 |
20140275028 | 1,2,5-SUBSTITUTED BENZIMIDAZOLES AS FLAP MODULATORS - The present invention relates to compounds of Formula (I), | 2014-09-18 |
20140275029 | 1,2,6-SUBSTITUTED BENZIMIDAZOLES AS FLAP MODULATORS - The present invention relates to compounds of Formula (I), | 2014-09-18 |
20140275030 | TRICYCLIC HETEROCYCLES AS BET PROTEIN INHIBITORS - The present invention relates to tricyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer. | 2014-09-18 |
20140275031 | PIPERIDIN-4-YL AZETIDINE DERIVATIVES AS JAK1 INHIBITORS - The present invention provides piperidin-4-yl azetidine derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase 1 (JAK1) and are useful in the treatment of diseases related to the activity of JAK1 including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases. | 2014-09-18 |
20140275032 | ARYL SULFAMIDE AND SULFAMATE DERIVATIVES AS RORc MODULATORS - Compounds of the formula I: | 2014-09-18 |
20140275033 | INHIBITORS OF KINASES AND CANCER STEM CELLS, AND METHODS OF PREPARATION AND USE THEREOF - The invention provides novel inhibitors of cancer stem cells as well as cancer stem cell pathway kinase and other related kinases, pharmaceutical compositions and uses thereof in the treatment of cancer or a related disorder in a mammal, and methods of making such compounds and compositions. | 2014-09-18 |
20140275034 | Methods and Compositions Utilizing Lactams Derived from Camphor, Verbenone or Cat Thyme Oil for Repelling Blood-Sucking and Biting Insects, Ticks and Mites - A method for repelling blood-sucking and biting insects, ticks and mites involving treating an object or area with a blood-sucking and biting insects, ticks and mites repelling effective amount of camphor lactams, verbenone lactams, dolicholactams, dolicholactone, and their precursors, and mixtures thereof, and optionally a carrier. | 2014-09-18 |
20140275035 | THIENYLINDOLE AZEPINES AS SEROTONIN 5-HT2C RECEPTOR LIGANDS AND USES THEREOF - The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are thienylindole azepines. These compounds are serotonin receptor (5-HT | 2014-09-18 |
20140275036 | 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. | 2014-09-18 |
20140275037 | SULFONYL SEMICARBAZIDES, SEMICARBAZIDES AND UREAS, PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS FOR TREATING HEMORRHAGIC FEVER VIRUSES, INCLUDING INFECTIONS ASSOCIATED WITH ARENAVIRUSES - Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel semicarbazides, sulfonyl carbazides, ureas and related compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to Arenaviridae (Junin, Machupo, Guanavito, Sabia and Lassa), Filoviridae (ebola and Marburg viruses), Flaviviridae (yellow fever, omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever). | 2014-09-18 |
20140275038 | ABUSE DETERRENT COMPOSITIONS AND METHODS OF USE - Orally administrable pharmaceutical compositions, methods of administration, and methods of making the same are provided. The pharmaceutical compositions provide abuse deterrent properties. | 2014-09-18 |
20140275039 | ABUSE DETERRENT COMPOSITIONS AND METHODS OF USE - Orally administrable pharmaceutical compositions, methods of administration, and methods of making the same are provided. The pharmaceutical compositions provide abuse deterrent properties. | 2014-09-18 |
20140275040 | NEW COMPOUNDS - The present invention relates to compounds which are inhibitors of SSAO activity. The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment or prevention of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases, immune disorders and the inhibition of tumor growth. | 2014-09-18 |
20140275041 | OXAZOLE TYROSINE KINASE INHIBITORS - The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar | 2014-09-18 |
20140275042 | TRICYCLIC AND TETRACYCLIC SYSTEMS ACTING UPON THE VASCULAR AND CENTRAL NERVOUS SYSTEMS - Tricyclic and tetracyclic derivatives of benzodiazepine, pyridodiazepine, and pyrimidodiazepine fused with 1,4-dihydropyridine derivatives are disclosed. The present derivatives can be obtained from derivatives containing a dihydropyridine ring reacting with compounds of the ortho-phenyldiamine, ortho-diaminopyridine, and ortho-diaminopyrimidine type, as well as some subsequent transformations and, tricyclic and tetracyclic derivatives can be obtained with a diazepine or diazepinone nucleus fused to a 1,4-dihydropyridine nucleus, having a substituted or unsubstituted ring of benzene, pyridine or pyrimidine. The present derivatives exhibit vascular and central nervous system therapeutic activity. | 2014-09-18 |
20140275043 | SUBSTITUTED 3-PHENYLPROPYLAMINE DERIVATIVES FOR THE TREATMENT OF OPHTHALMIC DISEASES AND DISORDERS - The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are substituted 3-phenylpropylamine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease. | 2014-09-18 |
20140275044 | TETRAHYDROPYRROLOTHIAZINE COMPOUNDS - The present invention provides a compound of Formula I: | 2014-09-18 |
20140275045 | PHENAZINE-3-ONE AND PHENOTHIAZINE-3-ONE DERIVATIVES FOR TREATMENT OF OXIDATIVE STRESS DISORDERS - Disclosed herein are phenazine-3-one and phenothiazine-3-one derivative compounds and methods of using such compounds for treating or suppressing oxidative stress disorders, including mitochondrial disorders, impaired energy processing disorders, neurodegenerative diseases and diseases of aging. | 2014-09-18 |
20140275046 | COMPOSITIONS OF A POLYORTHOESTER AND AN APROTIC SOLVENT - Delivery systems and compositions comprised of a biodegradable polyorthoester polymer, an aprotic solvent, and a drug are described. The solvent is selected to modulate release of drug from the composition, where, in some embodiments, the solvent is rapidly released after administration and provides a corresponding rapid rate of drug release. Alternatively, in other embodiments, the solvent is slowly released from the composition after its administration, and provides a correspondingly slow rate of drug release. | 2014-09-18 |
20140275047 | MOLECULES HAVING CERTAIN PESTICIDAL UTILITIES, AND INTERMEDIATES, COMPOSITIONS, AND PROCESSES RELATED THERETO - This disclosure relates to the field of molecules having pesticidal utility against pests in phyla Nematoda, Arthropoda, and/or Mollusca, processes to produce such molecules and intermediates used in such processes, compositions containing such molecules, and processes of using such molecules against such pests. These molecules may be used, for example, as nematicides, acaricides, insecticides, miticides, and/or molluscicides. This document discloses molecules having the following formula (“Formula One”). | 2014-09-18 |
20140275048 | PRODRUGS OF FUMARATES AND THEIR USE IN TREATING VARIOUS DISEASES - The present invention provides compounds of formula (I), and pharmaceutical compositions thereof. | 2014-09-18 |
20140275049 | SUBSTITUTED PYRAZOLE ANALOGS As RAR ANTAGONISTS - The present invention provides compounds of Formula I or a pharmaceutical salt thereof; methods of treating osteoarthritis and the pain associated with osteoarthritis using the compounds; and processes for preparing the compounds. | 2014-09-18 |
20140275050 | 2,5-DISUBSTITUTED THIOMORPHOLINE OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to 2,5-disubstituted thiomorpholine amide compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2,5-disubstituted thiomorpholine amide compounds described herein in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved. | 2014-09-18 |
20140275051 | COMPOSITION AND METHOD FOR CONTROLLING PLANT DISEASES - The present invention provides a composition for controlling plant diseases having an excellent control efficacy on plant diseases. A composition for controlling plant diseases comprising an amide compound represented by a formula (I): wherein each of symbols are the same as defined in the Description; or salts thereof and at least one kind of compounds selected from the group (A) consisting of kresoxim-methyl, azoxystrobin, pyraclostrobin, picoxystrobin, enestrobin, trifloxystrobin, dimoxystrobin, fluoxastrobin, orysastrobin, famoxadone, fenamidone, metominostrobin, a compound represented by a formula (II): and pyribencarb shows an excellent controlling efficacy on plant diseases. | 2014-09-18 |
20140275052 | COMPOSITION AND METHOD FOR CONTROLLING PLANT DISEASES - The present invention provides a composition for controlling plant diseases having an excellent control efficacy on plant diseases. A composition for controlling plant diseases comprising an carboxylic acid compound represented by a formula (I): wherein each of symbols are the same as defined in the Description; or salts thereof and at least one kind of compounds selected from the group (A) consisting of kresoxim-methyl, azoxystrobin, pyraclostrobin, picoxystrobin, enestrobin, trifloxystrobin, dimoxystrobin, fluoxastrobin, orysastrobin, famoxadone, fenamidone, metominostrobin, a compound represented by a formula (II): and pyribencarb shows an excellent controlling efficacy on plant diseases. | 2014-09-18 |
20140275053 | COMPOSITION AND METHOD FOR CONTROLLING PLANT DISEASES - The present invention provides a composition for controlling plant diseases having an excellent control efficacy on plant diseases. A composition for controlling plant diseases comprising an amide compound represented by a formula (I); wherein each of symbols are the same as defined in the Description; or salts thereof and at least one kind of compounds selected from the group (A) consisting of kresoxim-methyl, azoxystrobin, pyraclostrobin, picoxystrobin, enestrobin, trifloxystrobin, dimoxystrobin, fluoxastrobin, orysastrobin, famoxadone, fenamidone, metominostrobin, a compound represented by a formula (II) and pyribencarb: shows an excellent controlling efficacy on plant diseases. | 2014-09-18 |
20140275054 | RESORUFIN DERIVATIVES FOR TREATMENT OF OXIDATIVE STRESS DISORDERS - Disclosed herein are resorufin derivative compounds and methods of using such compounds for treating or suppressing oxidative stress disorders, including mitochondrial disorders, impaired energy processing disorders, neurodegenerative diseases and diseases of aging. | 2014-09-18 |
20140275055 | Protein Kinase C Inhibitors and Uses Thereof - This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes. | 2014-09-18 |
20140275056 | P2X7 MODULATORS - The present invention is directed to a compound of Formula (I): | 2014-09-18 |
20140275057 | NOVEL COMPOUNDS AND COMPOSITIONS FOR THE INHIBITION OF NAMPT - The present invention relates to compounds and composition for inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below. | 2014-09-18 |
20140275058 | PERFLUORINATED CYCLOPROPYL FUSED 1,3-OXAZIN-2-AMINE COMPOUNDS AS BETA-SECRETASE INHIBITORS AND METHODS OF USE - The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: | 2014-09-18 |
20140275059 | DNA-PK INHIBITORS - The present invention relates to compounds useful as inhibitors of DNA-PK. 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. | 2014-09-18 |
20140275060 | COMPOUNDS FOR THE TREATMENT OF NEUROLOGIC DISORDERS - Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of certain neurologic disorders, including disorders related to NMDA receptor activity, including neuropsychiatric disorders, neurodegenerative disorders and other neurologic diseases, disorders and conditions including stroke, brain injury, epilepsy, neuropsychiatric disorders, mood disorders, chronic pain and related conditions. | 2014-09-18 |
20140275061 | SUBSTITUTED TETRAHYDROISOQUINOLINE COMPOUNDS AS FACTOR XIA INHIBITORS - The present invention provides compounds of Formula (I): or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor XIa and/or plasma kallikrein which may be used as medicaments. | 2014-09-18 |
20140275062 | DIIMIDE COMPOUNDS - The invention relates to novel compounds which are naphthalene diimides of general formula (I): | 2014-09-18 |
20140275063 | NEW ENZYME INHIBITOR COMPOUNDS - Compounds of formula (I) are inhibitors of Semicarbazide-sensitive amine oxidase | 2014-09-18 |
20140275064 | DYRK1 INHIBITORS AND USES THEREOF - The present invention relates to novel thiazolo[5,4-f]quinazoline compounds and methods that are useful in the amelioration, treatment or control of Down's syndrome or early Alzheimer's disease or in the amelioration, treatment or control of cancers, especially solid tumors. More specifically, the invention relates to DYRK1A and/or DYRK1B inhibitors and to methods for preparing such compounds. | 2014-09-18 |
20140275065 | SUBSTITUTED 7-AZABICYLES AND THEIR USE AS OREXIN RECEPTOR MODULATORS - The present invention is directed to compounds of Formula I: | 2014-09-18 |
20140275066 | Transient Protection of Normal Cells During Chemotherapy - This invention is in the area of improved compounds, compositions and methods of transiently protecting healthy cells, and in particular hematopoietic stem and progenitor cells (HSPC) as well as renal cells, from damage associated with DNA damaging chemotherapeutic agents. In one aspect, improved protection of healthy cells is disclosed using disclosed compounds that act as highly selective and short, transiently-acting cyclin-dependent kinase 4/6 (CDK 4/6) inhibitors when administered to subjects undergoing DNA damaging chemotherapeutic regimens for the treatment of proliferative disorders. | 2014-09-18 |
20140275067 | Transient Protection of Normal Cells During Chemotherapy - This invention is in the area of improved compounds, compositions and methods of transiently protecting healthy cells, and in particular hematopoietic stem and progenitor cells (HSPC) as well as renal cells, from damage associated with DNA damaging chemotherapeutic agents. In one aspect, improved protection of healthy cells is disclosed using disclosed compounds that act as highly selective and short, transiently-acting cyclin-dependent kinase 4/6 (CDK 4/6) inhibitors when administered to subjects undergoing DNA damaging chemotherapeutic regimens for the treatment of proliferative disorders. | 2014-09-18 |
20140275068 | PRO-DRUG COMPOUNDS - The present invention provides neuronal gap junction blocking compounds according to formula (I) or a hydrate, solvate, or pharmaceutically acceptable salt thereof: | 2014-09-18 |
20140275069 | Novel inhibitor compounds of phosphodiesterase type 10A - The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof: | 2014-09-18 |
20140275070 | COMPOSITIONS COMPRISING THIENOPYRIMIDINE AND THIENOPYRIDINE COMPOUNDS AND METHODS OF USE THEREOF - The present invention relates generally to thienopyrimidine and thienopyridine class compounds and methods of use thereof. In particular embodiments, the present invention provides compositions comprising thienopyrimidine class compounds and methods of use to inhibit the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins (e.g., for the treatment of leukemia, solid cancers and other diseases dependent on activity of MLL1 and MLL2 or menin). | 2014-09-18 |
20140275071 | SUBSTITUTED XANTHINES AND METHODS OF USE THEREOF - Compounds, compositions and methods are described for inhibiting the TRPC5 ion channel and disorders related to TRPC5. | 2014-09-18 |
20140275072 | MORPHOLINYLBENZOTRIAZINES FOR USE IN CANCER THERAPY - The invention relates to compounds of the formula (I) in which R1, L and m have the meaning indicated in the claims, and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. | 2014-09-18 |
20140275073 | METHODS OF TREATING CANCER SENSITIVE TO ANTI-EGFR THERAPY AND MODIFYING TREATMENT USING BLOOD BIOMARKERS - The present disclosure provides methods of treating cancer and modifying a cancer treatment for a cancer with an anti-EGFR drug by creating PRDX6 expression profiles and using the profiles to evaluate and optionally modify treatment. The present disclosure also provides assays and systems for assessing sensitivity of a cancer to an anti-EGFR therapy. | 2014-09-18 |
20140275074 | HETEROCYCLIC DERIVATIVE HAVING PGD2 RECEPTOR ANTAGONIST ACTIVITY - The present invention is related to a compound represented by formula (I), | 2014-09-18 |
20140275075 | ISATIN COMPOUNDS, COMPOSITIONS AND METHODS FOR TREATMENT OF DEGENERATIVE DISEASES AND DISORDERS - Provided herein are compounds of the formula (I): | 2014-09-18 |
20140275076 | HETEROCYCLIC SUBSTITUTED-3-HETEROARYLIDENYL-2-INDOLINONE DERIVATIVE - Disclosed is a compound represented by formula (1) or a pharmacologically acceptable salt thereof. (In the formula, R | 2014-09-18 |
20140275077 | URACIL DERIVATIVES AS AXL AND C-MET KINASE INHIBITORS - The present application provides compounds of Formula I | 2014-09-18 |
20140275078 | COMPOSITIONS AND METHODS FOR TREATING CANCER USING PI3KB INHIBITOR AND MAPK PATHWAY INHIBITOR, INCLUDING MEK AND RAF INHIBITORS - The present invention relates to compositions comprising at least one MAPK pathway inhibitor including MEK and RAF inhibitors and at least one PI3Kβ inhibitor, and also to uses thereof for the treatment of cancer. | 2014-09-18 |
20140275079 | PYRROLE AMIDE INHIBITORS - The present invention provides for compounds of formula (I) | 2014-09-18 |
20140275080 | N-Acyl-N'-(pyridin-2-yl) Ureas and Analogs Exhibiting Anti-Cancer and Anti-Proliferative Activities - Described are compounds of Formula I | 2014-09-18 |
20140275081 | INHIBITORS OF HUMAN EZH2, AND METHODS OF USE THEREOF - The invention relates to inhibition of wild-type and certain mutant forms of human histone methyltransferase EZH2, the catalytic subunit of the PRC2 complex which catalyzes the mono- through tri-methylation of lysine 27 on histone H3 (H3-K27). In one embodiment the inhibition is selective for the mutant form of the EZH2, such that trimethylation of H3-K27, which is associated with certain cancers, is inhibited. The methods can be used to treat cancers including follicular lymphoma and diffuse large B-cell lymphoma (DLBCL). Also provided are methods for identifying small molecule selective inhibitors of the mutant forms of EZH2 and also methods for determining responsiveness to an EZH2 inhibitor in a subject. | 2014-09-18 |
20140275082 | APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE AND AUTOIMMUNE DISEASES - Disclosed herein are compounds that inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases using the compounds. | 2014-09-18 |
20140275083 | 3-PYRIMIDIN-4-YL-OXAZOLIDIN-2-ONES AS INHIBITORS OF MUTANT IDH - The invention is directed to a formula (I): | 2014-09-18 |
20140275084 | HISTONE DEMETHYLASE INHIBITORS - The present invention relates generally to compositions and methods for treating cancer and neoplastic diseases. Provided herein are substituted imidazole-pyridine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase enzymes. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like. | 2014-09-18 |
20140275085 | 2-AMINOPYRIMIDIN-6-ONES AND ANALOGS EXHIBITING ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES - Described are compounds of Formula I | 2014-09-18 |
20140275086 | PYRROLIDINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY - The present invention relates to pyrrolidine derivatives of the formula (I), | 2014-09-18 |
20140275087 | PYRROLIDINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY - The present invention relates to pyrrolidine derivatives of the formula (I), | 2014-09-18 |
20140275088 | SMALL MOLECULE MALARIAL ALDOLASE-TRAP ENHANCERS AND GLIDEOSOME INHIBITORS - In one aspect, the present invention relates to a method of identifying compounds useful in modifying the activity of Aldolase. The method includes providing a first model comprising Aldolase or residues of the amino acid sequence corresponding to SEQ ID NO: 1 said residues being at amino acid positions selected from the group consisting of 10-13, 26, 27, 29, 30, 31, 32, 33, 37, 39, 40, 41, 43, 44, 47, 48, 51, 52, 60, 63, 66, 79, 84, 85, 92, 93, 103, 106-109, 112-117, 138, 142, 146, 148, 151, 153, 179, 182, 183, 185, 186, 194, 196, 197, 198, 199, 208, 226-228, 231-269, 270, 272, 277-283, 285-289, 294, 295, 297-299, 301-304, 306-310 312, 313, 316, 317, 319, 321, 323, 326, 330, 344, 345, and 347, providing one or more candidate compounds, evaluating contact between the candidate compounds and the first model to determine which of the one or more candidate compounds have an ability to bind to and/or fit in the first model, and identifying compounds which, based on said evaluating, have the ability to bind to and/or fit in the first model as compounds potentially useful for modifying the activity of Aldolase. The present invention also discloses compounds and compositions which modify the activity of Aldolase, or a complex between Aldolase and TRAP. Methods of treating or preventing malaria, or an infection by apicomplexan organisms are also disclosed. | 2014-09-18 |
20140275089 | 2-Carboxamide Cycloamino Urea Derivatives in Combination with HSP90 Inhibitors for the Treatment of Proliferative Diseases - The present invention relates to a pharmaceutical combination comprising a 2-carboxamide cycloamino urea derivative compound of formula (I) and inhibitors of Heat Shock Protein 90, and the uses of such combinations in the treatment of proliferative diseases, more specifically PI3K dependent diseases, more specifically PI3K-alpha dependent diseases. | 2014-09-18 |
20140275090 | BILE ACID RECYCLING INHIBITORS FOR TREATMENT OF PRIMARY SCLEROSING CHOLANGITIS AND INFLAMMATORY BOWEL DISEASE - Provided herein are methods of treating or ameliorating primary sclerosing cholangitis and inflammatory bowel disease by administering to an individual in need thereof a therapeutically effective amount of an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating primary sclerosing cholangitis comprising administering to an individual in need thereof a therapeutically effective amount of ASBTI or a pharmaceutically acceptable salt thereof. | 2014-09-18 |
20140275091 | Ocular formulations comprising geranylgeranylacetone derivatives for intraocular delivery - Provided herein is a pharmaceutical formulation comprising a GGA derivative in the form of an eye drop. Also provided herein are methods of treating neural diseases or disorders by administering such pharmaceutical formulations. | 2014-09-18 |
20140275092 | PYRAZOLO COMPOUNDS AND USES THEREOF - The present invention relates to compounds useful as inhibitors of one or more histone demethylses. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders. | 2014-09-18 |
20140275093 | SUBSTITUTED HYDROXAMIC ACIDS AND USES THEREOF - This invention provides compounds of formula (I): | 2014-09-18 |