Class / Patent application number | Description | Number of patent applications / Date published |
514252190 | Five-membered nitrogen hetero ring attached directly or indirectly to the 1,3-diazine ring by nonionic bonding | 70 |
20080214559 | COMPOUNDS WITH A COMBINATION OF CANNABINOID CB1 ANTAGONISM AND SEROTONIN REUPTAKE INHIBITION - Compounds with a combination of cannabinoid CB | 09-04-2008 |
20080214560 | Use of Pyrimidine Derivatives in the Manufacture of a Medicament for Prevention and/or Treatment of Alzheimer's Disease - Pyrimidine derivatives of formula I, | 09-04-2008 |
20080280920 | Plasminogen Activator Inhibitor-1 Inhibitors - Inhibitors of plasminogen activator inhibitor-1 (PAI-I) are provided, which may also act as anti cancer agents, of formulae (I-V). | 11-13-2008 |
20090005396 | Use of Pyrazolyl-Pyrimidine Derivatives in the Treatment of Pain - This invention relates to the use of a pyrazolyl-pyrimidine of the formula (I). n=0, 1, 2 or 3 (I) in the manufacture of a medicament for use in the treatment or prophylaxis of pain. and to their pharmaceutical formulations and to their methods of use. | 01-01-2009 |
20090030009 | Heterobicyclic Carboxamides as Inhibitors for Kinases - The invention relates to novel organic compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula (I) and to the use of a compound of formula (I) for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in particular tumour diseases. | 01-29-2009 |
20090054450 | COMPOSITIONS AND METHODS OF USE FOR TREATING OR PREVENTING LIPID RELATED DISORDERS - Disclosed herein are novel compositions and methods for treating or preventing a variety of disorders and conditions associated with lipid metabolism. The methods generally include administering to a patient in need thereof a therapeutically effective amount of a pharmaceutical composition comprising one or more fibric acid or statin derivative compositions alone or in combination with one or more lipid altering agents and/or PDE inhibitors. | 02-26-2009 |
20090062302 | Jak2 Tyrosine Kinase Inhibition - The present invention provides methods for inhibiting JAK2 tyrosine kinase. Further, the present invention also provides methods of treating or preventing myeloproliferative disorders. | 03-05-2009 |
20090076025 | DEUTERIUM-ENRICHED DASATINIB - The present application describes deuterium-enriched dasatinib, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 03-19-2009 |
20090099197 | Methods of Identifying and Treating Individuals Exhibiting MDR-1 Overexpression With Protein Tyrosine Kinase Inhibitors and Combinations Thereof - The invention described herein relates to diagnostic and treatment methods and compositions useful in the management of disorders, for example cancers, involving cells that overexpress MDR-1, and methods of decreasing the incidence of CNS complications that are often associated with CML patients that have been administered imatinib or other protein tyrosine kinase inhibitors. | 04-16-2009 |
20090105270 | Kinase inhibition and anticancer therapy - This invention relates to novel uses for Compound E in the treatment of diseases, in particular cancer, associated with aberrant kinase expression. | 04-23-2009 |
20090118297 | POLYMORPHS OF DASATINIB AND PROCESS FOR PREPARATION THEREOF - Provided is dasatinib, solvates thereof and their crystalline forms, methods for their preparation, and pharmaceutical compositions thereof. | 05-07-2009 |
20090143401 | Pyridine and Pyrimidine Derivatives as Inhibitors of Histone Deacetylase - This invention comprises the novel compounds of formula (I) | 06-04-2009 |
20090149469 | Phenyl-[4-(3-phenyl-1h-pyrazol-4-yl)-pyrimidin-2-yl]-amine derivatives as igf-ir inhibitors - The present invention relates to a compound of formula I | 06-11-2009 |
20090156609 | TREATMENT OF POST-TRAUMATIC STRESS DISORDER WITH TETRAHYDROINDOLONE ARYLPIPERZAINE COMPOUNDS - Tetrahydroindolone and aryl piperazine derivatives for use in treating post-traumatic stress disorder and acute stress disorder. | 06-18-2009 |
20090163510 | Methods of Identifying and Treating Individuals Exhibiting Mutant SRC Kinase Polypeptides - The invention described herein relates to mutant SRC kinase proteins, and to diagnostic and therapeutic methods and compositions useful in the management of disorders, for example cancers, involving cells that express such mutant SRC kinase proteins. | 06-25-2009 |
20090170866 | MOESIN, CAVEOLIN 1 AND YES ASSOCIATED PROTEIN 1 AS PREDICTIVE MARKERS OF RESPONSE TO DASATINIB IN BREAST CANCERS - The invention described herein relates to methods and compositions useful in the diagnosis, treatment and management of cancers that express particular genes, including the moesin, caveolin 1, and/or yes-associated protein 1 genes. | 07-02-2009 |
20090197893 | Methods of Identifying and Treating Individuals Exhibiting Complex Karyotypes - The invention described herein relates to diagnostic and therapeutic methods and compositions useful in the management of disorders, for example cancers, involving cells that harbor complex karyotypes. The present invention also related to mutant BCR-ABL kinase proteins, and to diagnostic and therapeutic methods and compositions useful in the management of disorders, for example cancers, involving cells that express such mutant BCR-ABL kinase proteins. | 08-06-2009 |
20090215792 | METHOD OF TREATING CHRONIC MYELOGENOUS LEUKEMIA CELLS - Here, the inventors disclose the treatment of imatinib mesylate resistant chronic myelogenous leukemia cells with a cotreatment of vorinostat (SAHA, suberoylanilide hydroxamic acid) and dasatinib, a dual Abl/Src kinase (TK) inhibitor. Combined treatment of cultured human CML and BaF3 cells with vorinostat and dasatinib induced more apoptosis than either agent alone, as well as synergistically induced loss of clonogenic survival, which was associated with greater depletion of Bcr-Abl, p-CrkL and p-STAT5 levels. Co-treatment with dasatinib and vorinostat also attenuated the levels of Bcr-AblE255K and Bcr-AblT315I and induced apoptosis of BaF3 cells with ectopic expression of the mutant forms of Bcr-Abl. Finally, co-treatment of the primary CML cells with vorinostat and dasatinib induced more loss of cell viability and depleted Bcr-Abl or Bcr-AblT315I, p-STAT5 and p-CrkL levels than either agent alone. | 08-27-2009 |
20090221601 | Methods of identifying and treating individuals exhibiting mutant kit protein - The invention described herein relates to methods of identifying and treating individuals with protein tyrosine kinase associated disorders that have, or may, become resistant to treatment with a kinase inhibitor such as imatinib due to a gain-of-function mutation in KIT tyrosine kinase. | 09-03-2009 |
20090221602 | PROCESSES FOR PREPARING SUBSTITUTED PYRIMIDINES - The present invention provides a facile process for the preparation of tri- and tetra-substituted pyrimidines. The process is useful for preparing inhibitors of protein kinases, especially Aurora kinase. These inhibitors are useful for treating or lessening the severity of Aurora-mediated diseases or conditions. | 09-03-2009 |
20090286803 | COMBINATION COMPRISING A) A PYRIMIDYLAMINOBENZAMIDE COMPOUND, AND B) A THR315LLE KINASE INHIBITOR - The invention provides a pharmaceutical combination comprising:
| 11-19-2009 |
20090298844 | ABL KINASE INHIBITION - The present invention relates to inhibition of AbI kinase. | 12-03-2009 |
20090306094 | Methods Of Identifying And Treating Individuals Exhibiting Mutant Bcr/Abl Kinase Polypeptides - The present invention relates to mutant BCR-ABL kinase proteins, and to diagnostic and therapeutic methods and compositions useful in the management of disorders, for example cancers, involving cells that express such mutant BCR-ABL kinase proteins. | 12-10-2009 |
20100004257 | Identification of Biomarkers Predictive of Dasatinib Effects in Cancer Cells - A method of predicting response to treatment with inhibitors of EGFR and SRC by screening for status of key biomarkers such as EGFR. Dasatinib is a drug that can inhibit a group of proteins called SRC proteins. In addition, other experiments have suggested that other important signaling proteins are affected by dasatinib. Early phase trials of dasatinib are ongoing in cancer patients. It will be important to determine which patients receive a clinical benefit of dasatinib. Predetermination of treatment benefit can be performed by assessing biomarkers in patients tumors prior to treatment with dasatinib or other inhibitors of EGFR and SRC. Patients that have positive biomarkers for treatment could then be treated with higher confidence of benefit while those not possessing these predictive biomarkers would avoid ineffective and potentially toxic therapy. Additionally, treatment can be tailored according to predetermined sensitivity by evaluating indicated biomarkers correlating with sensitivity to one or more agents. | 01-07-2010 |
20100029676 | T315A AND F317I MUTATIONS OF BCR-ABL KINASE DOMAIN - The present invention relates to mutant BCR-ABL kinase proteins, and to diagnostic and therapeutic methods and compositions useful in the management of disorders, for example cancers, involving cells that express such mutant BCR-ABL kinase proteins. | 02-04-2010 |
20100081666 | SRC ACTIVATION FOR DETERMINING CANCER PROGNOSIS AND AS A TARGET FOR CANCER THERAPY - Methods of cancer diagnosis and prognosis using biomarkers. | 04-01-2010 |
20100120788 | IDENTIFICATION OF POLYNUCLEOTIDES FOR PREDICTING ACTIVITY OF COMPOUNDS THAT INTERACT WITH AND/OR MODULATE PROTEIN TYROSINE KINASES AND/OR PROTEIN TYROSINE KINASE PATHWAYS IN PROSTATE CELLS - The present invention describes polynucleotides that have been discovered to correlate to the relative intrinsic sensitivity or resistance of cells, e.g., prostate cell lines, to treatment with compounds that interact with and modulate, e.g., inhibit, protein tyrosine kinases, such as, for example, members of the Src family of tyrosine kinases, e.g., Src, Fgr, Fyn, Yes, Blk, Hck, Lck and Lyn, as well as other protein tyrosine kinases, including, Bcr-abl, Jak, PDGFR, c-kit and Eph receptors. These polynucleotides have been shown to have utility in predicting the resistance and sensitivity of prostate cell lines to the compounds. The expression level or phosphorylation status of some polynucleotides is regulated by treatment with a particular protein tyrosine kinase inhibitor compound, thus indicating that these polynucleotides are involved in the protein tyrosine kinase signal transduction pathway, e.g., Src tyrosine kinase. Such polynucleotides, whose expression levels correlate highly with drug sensitivity or resistance and which are modulated by treatment with the compounds, comprise polynucleotide predictor or marker sets useful in methods of predicting drug response, and as prognostic or diagnostic indicators in disease management, particularly in those disease areas, e.g., prostate cancer, in which signaling through the protein tyrosine kinase pathway, such as the Src tyrosine kinase pathway, is involved with the disease process. | 05-13-2010 |
20100152198 | USE OF C-SRC INHIBITORS IN COMBINATION WITH A PYRIMIDYLAMINOBENZAMIDE COMPOUND FOR THE TREATMENT OF LEUKEMIA - The invention relates to a combination which comprises (a) at least one compound decreasing the c-Src activity and (b) a pyrimidylaminobenzamide compound; to pharmaceutical compositions comprising said combinations; and to a method of treating a warm-blooded animal having leukemia, especially chronic myelogenous leukemia, comprising administering to the animal at least one compound inhibiting the activity of a member of the Src kinase family, the Btk kinase family, the Tec kinase family or a Raf kinase inhibitor, in particular inhibiting the c-Src protein tyrosine kinase activity or inhibiting simultaneously the c-Src protein tyrosine kinase activity and the Bcr-Abl tyrosine kinase activity, in combination with a pyrimidylaminobenzamide compound, in particular 4-Methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-N-[5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)phenyl]benzamide. | 06-17-2010 |
20100160342 | Compositions of Topical Ocular Solutions to Deliver Effective Concentrations of Active Agent to the Posterior Segment of the Eye - The present invention relates to development of efficacious pharmaceutical compositions comprising an active agent, such as the free base or hydrochloride salt of tandospirone, for topical delivery to the eye for the treatment of retinal disorders. | 06-24-2010 |
20100324063 | JAK2 TYROSINE KINASE INHIBITION - The present invention provides methods for inhibiting JAK2 tyrosine kinase. Further, the present invention also provides methods of treating or preventing myeloproliferative disorders. | 12-23-2010 |
20110028489 | Pyrimidine Derivatives and Their Use for Treating Bone-Related Disorders - The present invention relates to a new use of pyrimidine derivatives of formula I, as a free base or a pharmaceutically acceptable salt thereof in the manufacture of a medicament in the treatment and/or prophylaxis of Alzheimer's Disease: | 02-03-2011 |
20110166154 | IDENTIFICATION OF PREDICTIVE MARKERS OF RESPONSE TO DASATINIB IN HUMAN COLON CANCER - Methods and compositions are provided useful in the diagnosis, treatment and management of cancers wherein cancer cells express certain polynucleotides and/or polypeptides that are differentially expressed in colon cancer subtypes that are sensitive to therapy with abl kinase inhibitors and src kinase inhibitors. In particular, PTK-7, PLK-2 and PLK-3 could be identified as markers for determining the responsiveness of cancer to dasatinib. | 07-07-2011 |
20110172242 | TREATMENT OF ORGANOPHOSPHATE EXPOSURE WITH TETRAHYDROINDOLONE ARYLPIPERAZINE COMPOUNDS - A method of treating exposure to organophosphate agents through the use of compounds comprising tetrahydroindolone and arylpiperazine moieties. | 07-14-2011 |
20110178095 | TYROSINE KINASE INHIBITORS CONTAINING A ZINC BINDING MOIETY - The present invention relates to tyrosine kinase inhibitors that contain a zinc-binding moiety and their use in the treatment of tyrosine related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors. | 07-21-2011 |
20110263609 | Methods of Identifying and Treating Individuals Exhibiting NUP214-ABL1 Positive T-Cell Malignancies with Protein Tyrosine Kinase Inhibitors and Combinations Thereof - The invention described herein relates to diagnostic and treatment methods and compositions useful in the management of disorders, for example cancers, involving NUP214-ABL1 positive T-cell malignancies and methods for treating an individual suffering from a NUP214-ABL1 positive T cell malignancy. | 10-27-2011 |
20120015956 | DEUTERIUM-ENRICHED DASATINIB - The present application describes deuterium-enriched dasatinib, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 01-19-2012 |
20120028989 | 6-(3-AZA-BICYCLO[3.1.0]HEX-3-YL)-2-PHENYL-PYRIMIDINES - The present invention relates to 6-(3-aza-bicyclo[3.1.0]hex-3-yl)-2-phenyl-pyrimidine derivatives and their use as P2Y | 02-02-2012 |
20120035183 | Cancer Treatment Method - The present invention relates to a method of treating cancer in a mammal by administration of 4-quinazolinamines and at least one additional anti-neoplastic compound. In particular, the method relates to a methods of treating cancers by administration of N-{3-chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methanesulphonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine and salts and solvates thereof in combination with at least one additional anti-neoplastic compound. | 02-09-2012 |
20120071492 | Oligomer-Protein Tyrosine Kinase Inhibitor Conjugates - The invention relates to (among other things) oligomer-PTK inhibitor conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over PTK inhibitor compounds lacking a water soluble, non peptidic oligomer. | 03-22-2012 |
20120095015 | TRIAZOLE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECEPTOR - The invention relates to compounds of formula (I), wherein n is 1 or 2, Ar is a C-bound 1,2,4-triazol radical which carries a radical R | 04-19-2012 |
20120122882 | Substituted Pyrrolo-Pyrimidine Derivatives, Process for Their Preparation and Their Use as Kinase Inhibitors - Substituted pyrrolo-pyrimidine derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a dysregulated protein kinase activity, like cancer. | 05-17-2012 |
20120129870 | PIPERAZINYL DERIVATIVES USEFUL AS MODULATORS OF THE NEUROPEPTIDE Y2 RECEPTOR - The present invention is directed to piperidinyl and piperazinyl derivatives of formula (II) useful as inhibitors of the NPY Y2 receptor, pharmaceutical compositions comprising said compounds, processes for the preparation of said compounds and the use of said compounds for the treatment and/or prevention of disorders, diseases and conditions mediated by the NPY Y2 receptor. | 05-24-2012 |
20120142698 | MICROBIOCIDAL HETEROCYCLES - The present invention relates to heterocyclic compounds of formula I which have microbiocidal activity, in particular fungicidal activity as well as methods of using the compounds of formula (I) to control microbes: wherein A is x-C(R | 06-07-2012 |
20120165340 | PTEN PHOSPHORYLATION-DRIVEN RESISTANCE TO CANCER TREATMENT AND ALTERED PATIENT PROGNOSIS - Indicators that can guide clinical decisions in cancer, particularly posttranslational modification of proteins which result in altered prognosis and differential sensitivity to targeted cancer therapy, are provided. In particular, monitoring of phosphorylation of PTEN may be utilized to predict or assess drug response, drug sensitivity, and clinical outcome. Modulation of PTEN phosphorylation may be utilized to alter sensitivity and outcome in cancer patients. Posttranslational modification of PTEN, particularly phosphorylation, is correlated with resistance to targeted cancer therapy, including EGFR inhibitors, and with reduced survival prognosis. Methods and assays for determining phosphorylation of PTEN, particularly Y240 phosphorylation, are provided. Methods for sensitizing tumors to inhibition and targeted therapy by modulating PTEN phosphorylation are provided. | 06-28-2012 |
20120184560 | MOLECULAR DIAGNOSTIC METHODS FOR PREDICTING BRAIN METASTASIS OF BREAST CANCER - Disclosed are molecular diagnostic compositions and methods for predicting brain metastasis of breast cancer, as well as methods for drug repositioning to identify existing and new therapeutics for use in developing individualized, patient-specific treatment regimens for improving diagnoses and patient outcomes in individuals at risk for brain metastasis of breast cancer. | 07-19-2012 |
20120302578 | Aminooxazole Inhibitors of Cyclin Dependent Kinases - Oxazole derivatives are described. The inventive compounds are useful as kinase inhibitors, and may be used in the treatment of cancer, such as prostate cancer, lung cancer, breast cancer, colon cancer, leukemia, CNS cancer, melanoma, ovarian cancer, and renal cancer. | 11-29-2012 |
20130012519 | Biomarker Identifying the Reactivation of STAT3 After Src Inhibition - A method of identifying cancer or an associated disorder comprising identifying and quantifying STAT3 occurring in a biological sample taken from a subject after administering a SFK inhibitor to said subject. | 01-10-2013 |
20130030004 | Gyrase inhibitors and uses thereof - The present invention relates to compounds of formula I: | 01-31-2013 |
20130184288 | Aminooxazole Inhibitors of Cyclin Dependent Kinases - Oxazole derivatives are described. The inventive compounds are useful as kinase inhibitors, and may be used in the treatment of cancer, such as prostate cancer, lung cancer, breast cancer, colon cancer, leukemia, CNS cancer, melanoma, ovarian cancer, and renal cancer. | 07-18-2013 |
20130225599 | NOVEL PYRROLIDINE DERIVED BETA 3 ADRENERGIC RECEPTOR AGONISTS - The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of b3-adrenoceptor. Formula (I). | 08-29-2013 |
20130225600 | OXAZOLINE AND ISOXAZOLINE DERIVATIVES AS CRAC MODULATORS - The present invention relates to compounds of Formula (I) along with processes for their preparation that are useful for treating, preventing and/or managing the diseases, disorders, syndromes or conditions associated with the modulation of CRAC. The invention further relates to methods of treating, preventing managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of CRAC of Formula (I). | 08-29-2013 |
20140018368 | HEDGEHOG ANTAGONISTS HAVING ZINC BINDING MOIETIES - The present invention provides compounds which antagonize hedgehog signaling and inhibit HDAC activity. The compounds can be used in methods of treating proliferative diseases and disorders such as cancer. | 01-16-2014 |
20140051708 | PYRAZOLYL-PYRIMIDINE DERIVATIVES AS KINASE INHIBITORS - The present invention relates to pyrazolyl-pyrimidine 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 compounds or the pharmaceutical compositions containing them. | 02-20-2014 |
20140128406 | MICROBIOCIDAL HETEROCYCLES - The present invention relates to heterocyclic compounds of formula I which have microbiocidal activity, in particular fungicidal activity as well as methods of using the compounds of formula (I) to control microbes: wherein A is x-C(R | 05-08-2014 |
20140135341 | Pyridine And Pyrimidine Derivatives As Inhibitors Of Histone Deacetylase - This invention comprises the novel compounds of formula (I) | 05-15-2014 |
20140179711 | PROCESS FOR PREPARING 2-AMINOTHIAZOLE-5-AROMATIC CARBOXAMIDES AS KINASE INHIBITORS - The invention relates to processes for preparing compounds having the formula, | 06-26-2014 |
20140288087 | NICHE TARGETING OF QUIESCENT CANCER STEM CELLS - The disclosure provides methods for determining the self-renewal potential of a cancer stem cell (CSC), or for predicting the drugability (susceptibility to a drug) of a CSC, and/or for predicting the progression of a cancer that corresponds to the CSC. In alternative embodiments, the disclosure provides methods for determining whether a CSC in a niche is more pro-apoptotic or more anti-apoptotic in relation to a normal stem cell or a CSC from another niche. In alternative embodiments, the disclosure provides methods for determining the prognosis or malignant potential of a cancer. In alternative embodiments, the disclosure provides methods determining the anti-apoptotic versus a pro-apoptotic potential of a cancer stem cell (CSC). | 09-25-2014 |
20140303180 | METHODS OF DIAGNOSING AND TREATING aCML and CNL - Disclosed herein are methods and kits used in treating a cancer characterized by aberrant activity of CSF3R. These methods involve detecting a mutation in exon 14 of CSF3R such as a mutation of T615 or T618 and treating the subject with a JAK inhibitor and/or detecting a mutation in exon 17 of CSF3R and treating with dasatinib or tyrosine kinase inhibitor with one or more targets in common with dasatinib. | 10-09-2014 |
20140303181 | METHODS OF DIAGNOSING AND TREATING aCML and CNL - Disclosed herein are methods and kits used in treating a cancer characterized by aberrant activity of CSF3R. These methods involve detecting a mutation in exon 14 of CSF3R such as a mutation of T615 or T618 and treating the subject with a JAK inhibitor and/or detecting a mutation in exon 17 of CSF3R and treating with dasatinib or tyrosine kinase inhibitor with one or more targets in common with dasatinib. | 10-09-2014 |
20140329828 | Oligomer-Protein Tyrosine Kinase Inhibitor Conjugates - The invention relates to (among other things) oligomer-PTK inhibitor conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over PTK inhibitor compounds lacking a water-soluble, non-peptidic oligomer. | 11-06-2014 |
20140343073 | PROCESS FOR PREPARATION OF AMORPHOUS FORM OF DASATINIB - A stable amorphous form of dasatinib of Formula (I) wherein amorphous dasatinib after exposure to a relative humidity of 75% at 40° C. or 60% at 25° C. for a period of at least three months doesn't change to crystalline form and a process for the preparation of the amorphous form of dasatinib of Formula (I). | 11-20-2014 |
20150065518 | METHODS OF TREATING CANCER HAVING AN ACTIVE WNT/BETA-CATENIN PATHWAY - The present invention provides methods of treating a subject having a Wnt/beta-catenin active cancer by administering to said subject a compound that inhibits the expression or activity of YES1, BIRC5 or BCL2L1, a compound that inhibits YAP1-beta-catenin complex formation, a compound that inhibits YAP1-beta-catenin complex binding to DNA, a compound that inhibits YAP1-beta-catenin-TBX5 complex formation, or any combination thereof. The compound can be, for example, a nucleic acid, a peptide, an antibody or a small molecule. Methods of screening for therapeutic targets for treating cancer are included. | 03-05-2015 |
20150133464 | Injectable particle - The present invention generally relates to an novel injectable particle composition essentially consisting of: (a) a population of domains, wherein each domain essentially consists of a drug matrix and a population of subdomains, wherein the subdomains are evenly distributed in the drug matrix, wherein each subdomain essentially consists of an ionizable excipient, and (b) a rate controlling matrix comprising a biocompatible polymer and optionally an excipient. The particle is for the use of cancer therapy. | 05-14-2015 |
20160009690 | 2-Imidazolyl-Pyrimidine Scaffolds as Potent and Selective Inhibitors of Neuronal Nitric Oxide Synthase | 01-14-2016 |
20160095934 | DASATINIB AND NONLINEAR CONFIGURATION POLYETHYLENE GLYCOL CONJUGATE - A dasatinib and nonlinear configuration polyethylene glycol conjugate represented by formula I, wherein core is the core structure of a nonlinear configuration of polyethylene glycol, selected from a residue of pentaerythritol, methylglucoside, sucrose, diethylene glycol, propanediol, glycerol or polyglycerol removaed the hydrogen atom from the hydroxyl group; P is a polyethylene glycol residue with a number-average molecular weight of 300-60000 Da; X is selected from single bond, —CH | 04-07-2016 |
20160102367 | RECURRENT MUTATIONS IN EPIGENETIC REGULATORS, RHOA AND FYN KINASE IN PERIPHERAL T-CELL LYMPHOMAS - Whole exome sequencing of 12 tumor-normal DNA pairs, RNAseq analysis and targeted deep sequencing identified new genetic alterations in PTCL transformation. These analyses identified highly recurrent epigenetic factor mutations in TET2, DN-MT3A and IDH2 as well as a new highly prevalent RHOA p.Gly17Val (NM_001664) mutation present in 22/35 (67%) of angioimmunoblastic T-cell lymphomas (AITL) and in 8/44 (18%) not otherwise specified PTCL (PTCL NOS) samples. Mechanistically, the RHOA Gly17Val protein interferes with RHOA signaling in biochemical and cellular assays, an effect potentially mediated by the sequestration of activated Guanine Exchange Factor (GEF) proteins. In addition, new and recurrent, genetic defects are described including mutations in FYN, ATM, B2M and CD58 implicating SRC signaling, impaired DNA damage response and escape from immune surveillance mechanisms in the pathogenesis of PTCL. | 04-14-2016 |
20160168142 | SALTS OF DASATINIB IN AMORPHOUS FORM | 06-16-2016 |
20160168143 | SALTS OF DASATINIB IN CRYSTALLINE FORM | 06-16-2016 |
20160176862 | 1-(PIPERAZIN-1-YL)-2-([1,2,4]TRIAZOL-1-YL)-ETHANONE DERIVATIVES | 06-23-2016 |
20160195536 | Materials and Methods Relating to Pancreatic Cancer | 07-07-2016 |