Class / Patent application number | Description | Number of patent applications / Date published |
514266400 | Nitrogen bonded directly to ring carbon of the 1,3-diazine ring of the quinazoline ring system | 87 |
20080214586 | 2-Amino-4-Phenylquinazoline Derivatives and the Use Thereof as Hsp90 Modulators - Novel phenylquinazoline derivatives of the formula (I), in which R | 09-04-2008 |
20080221138 | Method of using SAHA and Erlotinib for treating cancer - The present invention relates to a method of treating cancer in a subject in need thereof, by administering to a subject in need thereof a first amount of a histone deacetylase (HDAC) inhibitor such as suberoylanilide hydroxamic acid (SAHA), or a pharmaceutically acceptable salt or hydrate thereof, and a second amount of one or more anti-cancer agents, including Erlotinib. The HDAC inhibitor and the anti-cancer agent may be administered to comprise therapeutically effective amounts. In various aspects, the effect of the HDAC inhibitor and the anti-cancer agent may be additive or synergistic. | 09-11-2008 |
20080249117 | METHODS FOR STIMULATING OR INDUCING THE GROWTH AND/OR REDUCING THE LOSS OF KERATINOUS FIBERS - The invention relates to a cosmetic composition containing at least one 15-hydroxy-prostaglandin dehydrogenase inhibitor and cosmetically acceptable excipients. It also relates to a method of cosmetic treatment for promoting the growth and/or preventing or delaying the loss of hair, and the use of a 15-hydroxyprostaglandin dehydrogenase inhibitor for the preparation of a composition intended for controlling hair loss and/or for promoting hair regrowth. | 10-09-2008 |
20080269262 | Therameutin Modulators - This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein. | 10-30-2008 |
20080287474 | Antiproliferative Pyrimidyl, Fused Pyrimidyl and Pyrimidyl Hydrazones - The present invention is related to a novel series of pyrimidyl or fused pyrimidyl hydrazones. Compounds of Formula (I) wherein A is selected from the group consisting of Formulas (A1), (A2), (A3), (A4), (A5) are useful for the treatment and/or prevention of a proliferative disease. | 11-20-2008 |
20080312260 | Biological markers predictive of anti-cancer response to kinase inhibitors - The present invention provides diagnostic and prognostic methods for predicting the effectiveness of treatment of a cancer patient with inhibitors of EGFR kinase, PDGFR kinase, or FGFR kinase. Based on the surprising discovery that tumors cells after having undergone an EMT, while being mesenchymal-like, still express characteristics of both epithelial and mesenchymal cells, and that such cells have altered sensitivity to inhibition by receptor protein-tyrosine kinase inhibitors, in that they have become relatively insensitive to EGFR kinase inhibitors, but have frequently acquired sensitivity to inhibitors of other receptor protein-tyrosine kinases such as PDGFR or FGFR, methods have been devised for determining levels of specific epithelial and mesenchymal biomarkers that identify such “hybrid” tumor cells (e.g. determination of co-expression of vimentin and epithelial keratins), and thus predict the tumor's likely sensitivity to inhibitors of EGFR kinase, PDGFR kinase, or FGFR kinase. Improved methods for treating cancer patients with EGFR, PDGFR or FGFR kinase inhibitors that incorporate such methodology are also provided. | 12-18-2008 |
20090048278 | Novel Quinazoline-2,4-Diamine Derivatives and Their Use as Modulators of Small-Conductance Calcium-Activated Potassium Channels - This invention relates to novel quinazoline-2,4-diamine derivatives useful as modulators of small-conductance calcium-activated potassium channels (SK channels). In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention. | 02-19-2009 |
20090048279 | QUINAZOLINE ANALOGS AS RECEPTOR TYROSINE KINASE INHIBITORS - This invention provides quinazoline analogs of Formula I: | 02-19-2009 |
20090069350 | PHARMACEUTICAL COMPOSITIONS AND USE THEREOF - The present invention relates to pharmaceutical compositions and dosage compositions of compounds, including injectable formulations for the parenteral delivery of such compounds into patients in need of such treatment. Also featured are methods of making and using the compositions, including methods for the treatment of neoplastic diseases. | 03-12-2009 |
20090076042 | DEUTERIUM-ENRICHED ERLOTINIB - The present application describes deuterium-enriched erlotinib, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 03-19-2009 |
20090082371 | Treatment of Viral Disease and Cancer With Nf-kappaB Inhibitors - A method using quinazoline derivatives, celastrol, cape, BAY 11-7082, rocaglamide, and 7-Methoxy-5,11,12-trihydroxy-coumestan is administered to a mammal for the treatment and prevention of viral diseases and cancers. The chemical compounds are targeted to inhibit NF-κB transcriptional activity. These treatments for viral diseases, especially for infection caused by HIV, and cancers may be accomplished utilizing quinazoline derivatives, celastrol, cape, BAY 11-7082, rocaglamide, 7-Methoxy-5,11,12-trihydroxy-coumestan, and compounds similar to them alone or in combination with prior art other therapy. | 03-26-2009 |
20090124642 | Crystalline forms of Erlotinib HCI and formulations thereof - The invention provides a novel crystalline form of Erlotinib HCl, processes for its preparation, and formulations thereof. | 05-14-2009 |
20090170880 | Methods and Means for the Treatment of Cancer - Provided are Breast Cancer Resistance Protein (BCRP) inhibitors, P-glycoprotein (P-gp) inhibitors and chemotherapeutic agents for use in the treatment of cancer by combination therapy of the BCRP inhibitor and/or P-gp inhibitor with the chemotherapeutic agent. The chemotherapeutic agent is an imidazotetrazine, e.g. temozolomide. | 07-02-2009 |
20090203718 | CANCER TREATMENT METHOD - The present invention relates to a method of treating cancer in a mammal and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering an erb family inhibitor and an IGF-1R inhibitor to a mammal suffering from a cancer. | 08-13-2009 |
20090233949 | ISOSERINE DERIVATIVES FOR USE AS COAGULATION FACTOR IXA INHIBITORS - The invention relates to the compounds of formula (I) | 09-17-2009 |
20090253719 | CRYSTALLINE SALT FORMS OF ANTIFOLATE COMPOUNDS AND METHODS OF MANUFACTURING THEREOF - The present invention provides methods of preparing antifolate compounds. The inventive methods can particularly be use for preparing compounds exhibiting improved bioavailability, making the compound particularly useful in pharmaceutical compositions. The compounds prepared according to the inventive methods are useful in the treatment of multiple conditions, including abnormal cell proliferation, inflammatory diseases, asthma, and arthritis. | 10-08-2009 |
20090253720 | ANTIFOLATE COMPOSITIONS - The present invention provides pharmaceutical compositions comprising an antifolate compound. The composition exhibit improved bioavailability, and they particularly incorporate beneficial excipients that increase solubility and bioavailability, such as cyclodextrins or compounds formed of fatty acid esters of glycerol and polyethylene glycol esters. The pharmaceutical compositions are useful in the treatment of multiple conditions, including abnormal cell proliferation, inflammatory diseases, asthma, and arthritis. | 10-08-2009 |
20090253721 | Combined treatment with radiation and an epidermal growth factor receptor kinase inhibitor - The present invention provides a method for treating tumors or tumor metastases in a patient, comprising administering to the patient a therapeutically effective amount of an EGFR kinase inhibitor, combined with treating the patient simultaneously or sequentially with radiation therapy, with or without additional agents or treatments, such as other anti-cancer drugs. A preferred example of an EGFR kinase inhibitor that can be used in practicing this invention is the compound erlitinib HCl (also known as Tarceva™). | 10-08-2009 |
20090281129 | CDKI PATHWAY INHIBITORS AND USES THEREOF - The invention relates to the inhibition of the Cyclin-Dependent Kinase Inhibitor (CDKI) pathway. More particularly, the invention relates to methods for inhibiting the CDKI pathway for studies of and intervention in senescence-related and other CDKI-related diseases. | 11-12-2009 |
20090306101 | COMBINATION TREATMENT OF CANCER COMPRISING EGFR/HER2 INHIBITORS - The invention relates to a therapy of cancer comprising co-administration to a person in need of such treatment and/or co-treatment of a person in need of such treatment with effective amounts of: (1) a compound 1 of formula (I), wherein the groups R | 12-10-2009 |
20100022566 | QUINAZOLINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF - The present invention relates to novel quinazoline derivatives with less skin irritation and an excellent action of strongly suppressing scratching behavior, and pharmaceutical compositions containing a quinazoline derivative as an active ingredient. The present invention is directed to the quinazoline derivatives represented by the general formula [1] or pharmaceutically acceptable salts thereof. In the general formula [1], R | 01-28-2010 |
20100087457 | DOSAGES AND METHODS FOR THE TREATMENT OF CANCER - In general, the invention relates to a pharmaceutical dose having (4-Methoxy-phenyl)-methyl-(2-methyl-quinazolin-4-yl)-amine hydrochloride as the active ingredient that upon administration to a subject provides a C | 04-08-2010 |
20100087458 | METHOD OF TREATING MELANOMA - Disclosed is (4-Methoxy-phenyl)-methyl-(2-methyl-quinazolin-4-yl)-amine hydrochloride effective as a cytotoxic agent. (4-Methoxy-phenyl)-methyl-(2-methyl-quinazolin-4-yl)-amine hydrochloride is useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs, and in particular to its use in treating melanoma. | 04-08-2010 |
20100093773 | METHODS OF TREATING CANCER - Disclosed is (4-Methoxy-phenyl)-methyl-(2-methyl-quinazolin-4-yl)-amine hydrochloride effective as a vascular disrupting agent. (4-Methoxy-phenyl)-methyl-(2-methyl-quinazolin-4-yl)-amine hydrochloride is useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs, and in particular to its use in treating cancer. | 04-15-2010 |
20100120803 | 3,4-DIHYDROQUINAZOLINE DERIVATIVES - The present invention relates to 3,4-dihydroquinazoline derivatives, a process of preparing them and a pharmaceutical composition including them. The 3,4-dihydroquinazoline derivatives of the present invention have excellent T-type calcium channel blocking effect and anti-cancer activity. | 05-13-2010 |
20100168142 | SALTS OF 4-ANILINE QUINAZOLINE DERIVATIVE - The present invention relates to salt forms of N-{4-[3-chloro-4-(3-fluoro-benzyloxy)phenylamino]-quinazolin-6-yl}-acrylamide, methods for preparation thereof, pharmaceutical compositions comprising the same and their use thereof. The salt forms of the present invention, which possess excellent tumor inhibitory activity, good bioavailability and low toxicity in an animal body, are suitable for the use of preparation of anti-tumor medicaments. | 07-01-2010 |
20100190807 | CDKI Pathway inhibitors and uses thereof to regulate expression to TAU protein - The invention relates to the inhibition of the Cyclin-Dependent Kinase Inhibitor (CDKI) pathway. More particularly, the invention relates to methods for inhibiting increases in MAPT expression induced by the CDKI pathway for studies of and intervention in senescence-related and other CDKI-related diseases. | 07-29-2010 |
20100222371 | PREVENTION OF SURGICAL ADHESIONS - The present invention relates to methods for treatment (particularly the prevention or suppression) of formation or reformation of adhesions, particularly in the peritoneal or pelvic cavities resulting from wound, surgery, infection, inflammation or trauma. The invention provides methods useful for inhibiting, suppressing or ameliorating adhesion formation in mammals, including humans wherein an individual is administered a compound selected from the group consisting of sunitinib malate, axitinib, semaxanib, sorafenib, ZD1839, and erlotinib. The invention applies to human and veterinary applications. The inventive method has been shown to be especially effective in preventing adhesion formation in the peritoneum following surgery. | 09-02-2010 |
20100261738 | NOVEL POLYMORPHS OF ERLOTINIB HYDROCHLORIDE AND METHOD OF PREPARATION - The present invention relates to three novel crystalline forms of Erlotinib hydrochloride and method of preparation thereof. Erlotinib hydrochloride is N-(3-ethynylphenyl)-6,7-bis(2-methoxy ethoxy)-4-quinazolinamine hydrochloride of formula-(I). The present invention provides stable novel crystalline forms of Erlotinib hydrochloride designated as Form-M, Form-N and Form-P, and processes for the preparation of the same. Erlotinib hydrochloride can be used as medicament for the treatment of hyperproliferative disorders, such as cancers, in humans. | 10-14-2010 |
20100261739 | Method of Treating Non-Small Cell Lung Cancer - A method of treating non-small cell lung cancer (NSCLC), and especially NSCLC that has metastasized to brain is disclosed. | 10-14-2010 |
20110021545 | NOVEL PREPARATION FOR EXTERNAL USE - A compound represented by the formula (I), salt thereof, or hydrate thereof has an excellent anti-pruritic effect and an excellent effect in terms of metabolism. The topical formulation of the present invention has excellent skin absorption properties of the compound represented by the formula (I), salt thereof, or hydrate thereof. Furthermore, the topical formulation of the present invention is excellent in stability because ingredients are hardly bled after long-term storage. | 01-27-2011 |
20110021546 | Gene Defects And Mutant ALK Kinase In Human Solid Tumors - In accordance with the invention, novel gene deletions and translocations involving chromosome 2 resulting in fusion proteins combining part of Anaplastic Lymphoma Kinase (ALK) kinase with part of a secondary protein have now been identified in human solid tumors, e.g. non-small cell lung carcinoma (NSCLC). Secondary proteins include Echinoderm Microtubule-Associated Protein-Like 4 (EML-4) and TRK-Fusion Gene (TFG). The EML4-ALK fusion protein, which retains ALK tyrosine kinase activity, was confirmed to drive the proliferation and survival of NSCLC characterized by this mutation. The invention therefore provides, in part, isolated polynucleotides and vectors encoding the disclosed mutant ALK kinase polypeptides, probes for detecting it, isolated mutant polypeptides, recombinant polypeptides, and reagents for detecting the fusion and truncated polypeptides. The disclosed identification of this new fusion protein enables new methods for determining the presence of these mutant ALK kinase polypeptides in a biological sample, methods for screening for compounds that inhibit the proteins, and methods for inhibiting the progression of a cancer characterized by the mutant polynucleotides or polypeptides, which are also provided by the invention. | 01-27-2011 |
20110053963 | TARTRATE SALTS OF QUINAZOLINE BASED EGFR INHIBITORS CONTAINING A ZINC BINDING MOIETY - The present invention relates to tartrate salts of quinazoline containing zinc-binding moiety based derivatives of Formula II, below. | 03-03-2011 |
20110065734 | NOVEL BIFUNCTIONAL COMPOUNDS WHICH INHIBIT PROTEIN KINASES AND HISTONE DEACETYLASES - The present invention relates to a bifunctional compound of formula I or its pharmaceutically acceptable salts or solvates A-L-B (I) wherein A is a histone deacetylase (HDAC) inhibitory moiety, L is a single bond or a linker group and B is a protein kinase inhibitory moiety. The bifunctional compound according to formula (I) is useful for the treatment of malignant and non-malignant neoplasia and diseases related to abnormal cell growth. | 03-17-2011 |
20110065735 | SUBSTITUTED QUINAZOLINES - This invention relates to the discovery of substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim | 03-17-2011 |
20110112118 | 2,4-Diaminoquinazolines for Spinal Muscular Atrophy - 2,4-Diaminoquinazolines of formulae I-IV and VI | 05-12-2011 |
20110130413 | SUBSTITUTED QUINAZOLINES - This invention relates to the discovery of prodrugs of substituted analogues of the selective platelet lowering agent anagrelide which have reduced potential for cardiovascular side-effects and which should therefore lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to prodrugs of certain imidazoquinazoline derivatives which have the general formula (I) shown below wherein the substituents have the meanings defined in claim | 06-02-2011 |
20110184004 | PREDICTIVE MARKER FOR EGFR INHIBITOR TREATMENT - The present invention provides biomarkers which are predictive for the clinical benefit of EGFR inhibitor treatment in cancer patients. | 07-28-2011 |
20110184005 | PREDICTIVE MARKER FOR EGFR INHIBITOR TREATMENT - The present invention provides a biomarker which is predictive for the clinical benefit of EGFR inhibitor treatment in cancer patients. | 07-28-2011 |
20110190321 | PREDICTIVE MARKER FOR EGFR INHIBITOR TREATMENT - The present invention provides a biomarker that is predictive for the response to treatment with an EGFR inhibitor in cancer patients. | 08-04-2011 |
20110195982 | PREDICTIVE MARKER FOR EGFR INHIBITOR TREATMENT - The present invention provides a biomarker that is predictive for the response to treatment with an EGFR inhibitor in cancer patients | 08-11-2011 |
20110212979 | PREDICTIVE MARKER FOR EGFR INHIBITOR TREATMENT - The present invention provides a biomarker which is predictive for the clinical benefit of EGFR inhibitor treatment in cancer patients. | 09-01-2011 |
20110218212 | PREDICTIVE MARKERS FOR EGFR INHIBITORS TREATMENT - The present invention provides biomarkers that are predictive for the response to treatment with an EGFR inhibitor in cancer patients. The markers are the genes GBAS, APOH, SCYL3, PMS2CL, PRODH, SERF1A, URG4A and LRRC31. | 09-08-2011 |
20110224240 | METHODS OF TREATING CANCER AND RELATED DISEASES - Disclosed are orally bioavailable compounds effective as cytotoxic agents. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs, such as in cancer and related diseases. | 09-15-2011 |
20110230506 | PREDICTIVE MARKER FOR EGFR INHIBITOR TREATMENT - The present invention provides a biomarker (RAPGEF5) that is predictive for the response to treatment with an EGFR inhibitor in cancer patients. | 09-22-2011 |
20110237609 | ANTIFOLATE COMPOSITIONS - The present invention provides pharmaceutical compositions comprising an antifolate compound. The compositions can be prepared such that unit dosages of the composition exhibit excellent API content uniformity, such as by wet granulation or hot melt granulation. The pharmaceutical compositions are useful in the treatment of multiple conditions, including abnormal cell proliferation, inflammatory diseases, asthma, and arthritis. | 09-29-2011 |
20110245279 | PREDICTIVE MARKER FOR EGFR INHIBITOR TREATMENT - The present invention provides a biomarker which is predictive for the clinical benefit of EGFR inhibitor treatment in cancer patients | 10-06-2011 |
20110312981 | PREDICTIVE MARKER FOR EGFR INHIBITOR TREATMENT - The present invention provides a biomarker SFRS7 which is predictive for the clinical benefit of EGFR inhibitor treatment in cancer patients. | 12-22-2011 |
20120004249 | The polymorph forms of 4-anilinoquinazoline derivatives, the preparation methods and uses thereof - The present invention relates to polymorphic forms of N-{4-[3-chloro-4-(3-fluoro-benzyloxy)phenylamino]-quinazolin-6-yl}-acrylamide p-toluenesulfonate with the characteristic X-ray powder diffraction data as stated in the description, preparation methods thereof, pharmaceutical compositions comprising the same and the use thereof. | 01-05-2012 |
20120095029 | IPP COMPLEX AS MARKER FOR ERLOTINIB TREATMENT - The present invention provides biomarkers which are predictive for the clinical benefit of erlotinib hydrochloride treatment in cancer patients. | 04-19-2012 |
20120157480 | Biological markers predictive of anti-cancer response to epidermal growth factor receptor kinase inhibitors - The present invention provides diagnostic and prognostic methods for predicting the effectiveness of treatment of a cancer patient with an EGFR kinase inhibitor. Methods are provided for predicting the sensitivity of tumor cell growth to inhibition by an EGFR kinase inhibitor, comprising assessing whether the tumor cell has undergone an epithelial to mesenchymal transition (EMT), by determining the expression level of epithelial and/or mesenchymal biomarkers, wherein tumor cells that have undergone an EMT are substantially less sensitive to inhibition by EGFR kinase inhibitors. Improved methods for treating cancer patients with EGFR kinase inhibitors that incorporate the above methodology are also provided. Additionally, methods are provided for the identification of new biomarkers that are predictive of responsiveness of tumors to EGFR kinase inhibitors. Furthermore, methods for the identification of agents that restore the sensitivity of tumor cells that have undergone EMT to inhibition by EGFR kinase inhibitors are also provided. | 06-21-2012 |
20120214828 | DETERMINING SENSITIVITY OF CELLS TO B-RAF INHIBITOR TREATMENT BY DETECTING KRAS MUTATION AND RTK EXPRESSION LEVELS - The present invention relates to prognostic methods for identifying tumors that are not susceptible to B-Raf inhibitor treatment by detecting mutations in a K-ras gene or protein or by detecting overexpression of RTKs and/or their ligands. Kits are also disclosed for carrying out the methods. | 08-23-2012 |
20120214829 | Molecular Predictors of Therapeutic Response to Specific Anti-Cancer Agents - Herein is described the use of a collection of 50 breast cancer cell lines to match responses to 77 conventional and experimental therapeutic agents with transcriptional, proteomic and genomic subtypes found in primary tumors. Almost all compounds produced strong differential responses across the cell lines produced responses that were associated with transcriptional and proteomic subtypes and produced responses that were associated with recurrent genome copy number abnormalities. These associations can now be incorporated into clinical trials that test subtype markers and clinical responses simultaneously. | 08-23-2012 |
20120214830 | BIOLOGICAL MARKERS PREDICTIVE OF ANTI-CANCER RESPONSE TO INSULIN-LIKE GROWTH FACTOR-1 RECEPTOR KINASE INHIBITORS IN HEPATOCELLULAR CARCINOMA - The present invention provides diagnostic methods for predicting the effectiveness of treatment of an hepatocellular carcinoma (HCC) patient with an IGF-1R kinase inhibitor by assessing whether the HCC tumor cells express a high level of AFP, or whether serum levels of AFP protein are high. The present invention also provides diagnostic methods for predicting the effectiveness of treatment of cancer patients with IGF-1R kinase inhibitors, based on a determination of the expression level of IR, IGF-2, IGFBP3 or IGFBP7 in tumor cells, or a 4-gene index calculated using the expression vales for each of these four genes, which can be used to identify tumors that will be sensitive to IGF-1R kinase inhibitors, and also those that will be insensitive. Improved methods for treating cancer patients with IGF-1R kinase inhibitors that incorporate the above methods are also provided. | 08-23-2012 |
20120316187 | MOLECULAR BIOMARKERS FOR PREDICTING RESPONSE TO TYROSINE KINASE INHIBITORS IN LUNG CANCER - The invention relates to a method for predicting the response to the treatment with an EGFR tyrosine kinase inhibitor of a patient suffering lung cancer an carrying a mutation in the EGFR gene based on the expression levels in a sample of said patient of the BRCA1 gene wherein low BRCA1 expression levels are indicative of a positive response of a patient. This positive response is also observed in patients showing the T790M mutation in the EGFR gene which is usually associated with resistance to EGFR tyrosine kinase inhibitors. | 12-13-2012 |
20130012528 | NOVEL DERIVATIVES OF ERLOTINIB - This invention relates to novel compounds and hydrochloric acid salts thereof. More specifically, this invention relates to novel compounds and hydrochloric acid salts thereof derived from erlotinib. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering an epidermal growth factor receptor tyrosine kinase (EGFR) inhibitor, such as erlotinib. | 01-10-2013 |
20130085152 | Method For Assay On The Effect Of Vascularization Inhibitor - The present invention provides a method of predicting the antitumor effect of an angiogenesis inhibitor. It is possible to predict the antitumor effect of an angiogenesis inhibitor by evaluating the EOF dependency of a tumor cell for proliferation and/or survival and using the EGF dependency as an indicator. Since the antitumor effect of an angiogenesis inhibitor correlates with the EGF dependency of a tumor cell for proliferation and/or survival, the angiogenesis inhibitors is capable of producing excellent antitumor effect when combined with a substance having EGF inhibitory activity. | 04-04-2013 |
20130137711 | POLYMORPH FORMS OF 4-ANILINOQUINAZOLINE DERIVATIVES, THE PREPARATION METHODS AND USES THEREOF - The present invention relates to polymorphic forms of N-{4-[3-chloro-4-(3-fluoro-benzyloxy)phenylamino]-quinazolin-6-yl}-acrylamide p-toluenesulfonate with the characteristic X-ray powder diffraction data as stated in the description, preparation methods thereof, pharmaceutical compositions comprising the same and the use thereof. | 05-30-2013 |
20130150385 | CANCER THERAPY USING A COMBINATION OF A HSP90 INHIBITORY COMPOUNDS AND A EGFR INHIBITOR - A pharmaceutical combination comprising an EGFR inhibitor and an Hsp90 inhibitor according to the following formulae (I) or (Ia) a tautomer, or a pharmaceutically acceptable salt thereof, wherein the variables in the structural formulae are defined herein. Also provided are methods for treating a proliferative disorder in a subject in need thereof using pharmaceutical combinations disclosed herein. | 06-13-2013 |
20130150386 | METHODS FOR THE TREATMENT OF LUNG CANCER - Described herein are methods for the treatment of lung cancer in a subject. In particular, methods are provided for the treatment of resistant lung cancer with a combination of entinostat and an EGFR inhibitor. | 06-13-2013 |
20130203788 | EGFR AND KRAS MUTATIONS - The present invention relates to mutations in Epidermal Growth Factor Receptor (EGFR) and KRAS and methods of detecting such mutations as well as prognostic methods for identifying tumors that are susceptible to anticancer therapy such as chemotherapy and/or kinase inhibitor treatment. The methods involve determining the presence of a mutated EGFR gene or mutated EGFR protein and/or a mutated KRAS gene or mutated KRAS protein in a tumor sample. | 08-08-2013 |
20130210842 | PURE ERLOTINIB - The present invention relates to processes for the preparation of erlotinib and salts and polymorphs thereof, preferably of high purity. The present invention also relates to erlotinib and salts and polymorphs thereof preparable by said processes, to medical uses of said erlotinib, salts and polymorphs, and to pharmaceutical compositions comprising the same. | 08-15-2013 |
20130210843 | PREDICTIVE MARKER FOR EGFR INHIBITOR TREATMENT - The present invention provides a biomarker which is predictive for the clinical benefit of EGFR inhibitor treatment in cancer patients. | 08-15-2013 |
20130217712 | PREDICTIVE MARKER FOR EGFR INHIBITOR TREATMENT - The present invention provides a biomarker that is predictive for the response to treatment with an EGFR inhibitor in cancer patients. | 08-22-2013 |
20130217713 | PREDICTIVE MARKER FOR EGFR INHIBITOR TREATMENT - The present invention provides a biomarker which is predictive for the clinical benefit of EGFR inhibitor treatment in cancer patients. | 08-22-2013 |
20130225613 | QUINAZOLINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF - The present invention relates to novel quinazoline derivatives with less skin irritation and an excellent action of strongly suppressing scratching behavior, and pharmaceutical compositions containing a quinazoline derivative as an active ingredient. The present invention is directed to the quinazoline derivatives represented by the general formula [1] or pharmaceutically acceptable salts thereof. In the general formula [1], R | 08-29-2013 |
20130252978 | Novel Hydrated Form of Erlotinib Free Base and a Process For Preparation Of Erlotinib Hydrochloride Polymorph Form A Substantially Free of Polymorph Form B - The present invention provides a novel and stable hydrated form of erlotinib free base, and a process for its preparation thereof. The present invention also provides a process for preparation of erlotinib hydrochloride crystalline polymorph a substantially free of polymorph B. The present invention further relates to erlotinib hydrochloride crystalline particles having mean particle size (D | 09-26-2013 |
20140011821 | EGFR MUTATIONS - The present invention relates to mutations in Epidermal Growth Factor Receptor (EGFR) and methods of detecting such mutations as well as prognostic methods method for identifying a tumors that are susceptible to anticancer therapy such as chemotherapy and/or kinase inhibitor treatment. The methods involve determining the presence of a mutated EGFR gene or mutated EGFR protein in a tumor sample whereby the presence of a mutated EGFR gene or protein indicates the tumor is susceptible to treatment. | 01-09-2014 |
20140018375 | BIOLOGICAL MARKERS PREDICTIVE OF ANTI-CANCER RESPONSE TO EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITORS - The present invention provides diagnostic and prognostic methods for predicting the effectiveness of treatment of a cancer patient with an EGFR kinase inhibitor. Methods are provided for predicting the sensitivity of tumor cell growth to inhibition by an EGFR kinase inhibitor, comprising assessing whether the tumor cell has undergone an epithelial to mesenchymal transition (EMT), by determining the expression level of epithelial and/or mesenchymal biomarkers, wherein tumor cells that have undergone an EMT are substantially less sensitive to inhibition by EGFR kinase inhibitors. Improved methods for treating cancer patients with EGFR kinase inhibitors that incorporate the above methodology are also provided. Additionally, methods are provided for the identification of new biomarkers that are predictive of responsiveness of tumors to EGFR kinase inhibitors. Furthermore, methods for the identification of agents that restore the sensitivity of tumor cells that have undergone EMT to inhibition by EGFR kinase inhibitors are also provided. | 01-16-2014 |
20140066465 | CANCER TREATMENT USING TYROSINE KINASE AND NF-kB INHIBITORS - A method of treating cancer by administering to a subject in need thereof a therapeutically effective amount of a tyrosine kinase inhibitor and an NF-κB inhibitor is described. The method is useful for treating subjects having cancer that has developed resistance to tyrosine kinase inhibitors. | 03-06-2014 |
20140080848 | ARYL AMINE SUBSTITUTED PYRIMIDINE AND QUINAZOLINE AND THEIR USE AS ANTICANER DRUGS - A series of mono- and di-substituted quinazoline and pyrimidine derivatives based on the skeleton of erlotinib (an EGFR inhibitor) were synthesized and their bioactivities against hepatocellular carcinoma and human lung adenocarcinoma were evaluated. | 03-20-2014 |
20150038520 | Molecular Biomarkers for Predicting Response to Tyrosine Kinase Inhibitors in Lung Cancer - The invention relates to methods for determining the clinical outcome of patients suffering lung cancer and being under treatment with an EGFR inhibitor. The methods are based on the detection of the presence of mutations in the EGFR gene conferring resistance to inhibitors of the EGFR tyrosine kinase activity, wherein the appearance of said mutations in the biofluid of the patient is indicative of a high probability that the patient suffers a relapse of the disease. The invention also provides therapeutic methods for said patients. | 02-05-2015 |
20150065526 | OVERCOMING ACQUIRED RESISTANCE TO CHEMOTHERAPY TREATMENTS THROUGH SUPPRESSION OF STAT3 - This disclosure relates to methods of treating cancer comprising administering an effective amount of a STAT3 inhibitor, prodrugs, or derivatives thereof, in combinations with an EGFR tyrosine kinase inhibitors, prodrugs, or derivatives thereof, to a subject in need thereof. In certain embodiments, the STAT3 inhibitor is niclosamide or salt thereof. In certain embodiments, the EGFR tyrosine kinase inhibitor is erlotinib or salt thereof. | 03-05-2015 |
20150105412 | COMBINATION THERAPY WITH MDM2 AND EFGR INHIBITORS - Provided is a method of treating a proliferative disease, condition, or disorder in a subject by administering a combination of an inhibitor of p53 and MDM2 binding and an EGFR inhibitor. Various embodiments of the disclosed methods provide a synergistic anti-proliferative or anti-apoptotic effect compared to administration of one agent alone. | 04-16-2015 |
20150111907 | EGFR AND PTEN GENE ALTERATIONS PREDICTS SURVIVAL IN PATIENTS WITH BRAIN TUMOR - The invention relates to methods of predicting the clinical outcome of brain cancer patients based on the LOH levels of the PTEN gene and on the expression levels or the polysomy/amplification levels of EGFR gene in a sample from said patients. | 04-23-2015 |
20150133476 | Polymorphic forms of 4-phenylamino quinazoline derivative, the preparation method and uses thereof - The present invention relates to polymorphic forms of N-{4-[3-chloro-4-(3-fluoro-benzyloxy)phenylamino]-quinazolin-6-yl}-acrylamide p-toluenesulfonate with the characteristic X-ray powder diffraction data as stated in the description, preparation methods thereof, pharmaceutical compositions comprising the same and the use thereof. | 05-14-2015 |
20150290196 | EGFR MUTATIONS - The present invention relates to mutations in Epidermal Growth Factor Receptor (EGFR) and methods of detecting such mutations as well as prognostic methods method for identifying a tumors that are susceptible to anticancer therapy such as chemotherapy and/or kinase inhibitor treatment. The methods involve determining the presence of a mutated EGFR gene or mutated EGFR protein in a tumor sample whereby the presence of a mutated EGFR gene or protein indicates the tumor is susceptible to treatment. | 10-15-2015 |
20150353507 | 4-AMINO SUBSTITUTED CONDENSED PYRIMIDINE COMPOUNDS AS PDE4 INHIBITORS - The invention relates to novel substituted condensed pyrimidine compounds of general formula (I) | 12-10-2015 |
20150353508 | QUINOLINYL GLUCAGON RECEPTOR MODULATORS - The present invention provides a compound of Formula I | 12-10-2015 |
20150369810 | ANAPLASTIC LYMPHOMA KINASE IN KIDNEY CANCER - The invention provides methods to identify, diagnose, and treat kidney cancer through the detection of expression and/or activity of anaplastic lymphoma kinase (ALK). The detection of the presence of a polypeptide with ALK kinase activity (e.g., by detecting expression and/or activity of the polypeptide), identify those kidney cancers that are likely to respond to an ALK-inhibiting therapeutic. | 12-24-2015 |
20150374827 | SOLID DISPERSIONS OF LOW-WATER SOLUBILITY ACTIVES - Disclosed are compositions including a solid dispersion comprising a dispersion polymer, a basic low-water solubility active, and an anionic counterion, as well as methods of making and using the compositions. | 12-31-2015 |
20160033511 | METHODS AND COMPOSITIONS FOR DETECTING PANCREATIC CANCER - The present invention relates to non-invasive methods for the diagnosis and prognosis of pancreatic cancer. In some embodiments, such methods and compositions relate to particular pancreatic cancer biomarkers and combinations thereof. | 02-04-2016 |
20160115549 | Diagnosing and Monitoring CNS Malignancies Using MicroRNA - The use of specific microRNAs (miRNAs) present in CSF as biomarkers for particular brain malignancies and disease activity. | 04-28-2016 |
20160138112 | NON-INVASIVE BLOOD BASED MONITORING OF GENOMIC ALTERATIONS IN CANCER - The invention provides methods to monitor cell free nucleic acids. The method comprises obtaining a plasma sample from a subject known to have a cancer characterized by a pair of mutually exclusive mutations specific to the cancer; isolating cell free nucleic acids from the plasma sample obtained from the subject; measuring the amount a housekeeping gene and/or total DNA in the cell free nucleic acids isolated from the plasma sample to confirm that the amount of housekeeping gene and/or total DNA in the sample is within a selected range; measuring the amount of a first of the pair of mutually exclusive mutations specific to the cancer in the cell free nucleic acids isolated from the plasma sample; and indicating in a report that the subject has the first mutation when (a) the amount of the housekeeping gene and/or total DNA in the cell free nucleic acids isolated from the plasma sample is within the selected range and (b) the amount of the first mutation is increased as compared to a control amount, wherein the control amount is determined by measuring the apparent amount of the first mutation in control cell free nucleic acids isolated from plasma samples obtained from control subjects known to have the second of the pair of mutually exclusive mutations specific to the cancer using measuring conditions substantially the same as those used to measure the amount of the first mutation in the cell free nucleic acids isolated from the plasma sample from the subject. | 05-19-2016 |
20160158235 | BIOLOGICAL MARKERS PREDICTIVE OF ANTI-CANCER RESPONSE TO EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITORS - The present invention provides diagnostic and prognostic methods for predicting the effectiveness of treatment of a cancer patient with an EGFR kinase inhibitor. Methods are provided for predicting the sensitivity of tumor cell growth to inhibition by an EGFR kinase inhibitor, comprising assessing whether the tumor cell has undergone an epithelial to mesenchymal transition (EMT), by determining the expression level of epithelial and/or mesenchymal biomarkers, wherein tumor cells that have undergone an EMT are substantially less sensitive to inhibition by EGFR kinase inhibitors. Improved methods for treating cancer patients with EGFR kinase inhibitors that incorporate the above methodology are also provided. Additionally, methods are provided for the identification of new biomarkers that are predictive of responsiveness of tumors to EGFR kinase inhibitors. Furthermore, methods for the identification of agents that restore the sensitivity of tumor cells that have undergone EMT to inhibition by EGFR kinase inhibitors are also provided. | 06-09-2016 |
20160184309 | METHODS OF TREATING VARIOUS CANCERS USING AN AXL/cMET INHIBITOR ALONE OR IN COMBINATION WITH OTHER AGENTS - This application describes the use of the compound (I) or a salt thereof, either alone or in combination with other therapeutically active agents, for the treatment of particular cancers, including any solid or hematological cancer in which AXL or c-Met is over-expressed. | 06-30-2016 |
20160195532 | Targeted Covalent Probes and Inhibitors of Proteins Containing Redox-Sensitive Cysteines | 07-07-2016 |