Patent application number | Description | Published |
20080207572 | Use of Dual C-Kit/Fgfr3 Inhibitors for Treating Multiple Myeloma - The present invention relates to a method for treating Multiple Myeloma (MM), FGFR3+ myeloma, especially relapsed or refractory multiple myeloma (4/14) expressing FGFR3, comprising administering a dual C-KIT/FGFR3 inhibitor, such as 2-aminoarylthiazoles and 2-aminoaryloxazoles. | 08-28-2008 |
20080242704 | Substituted Oxazole Derivatives and their Use as Tyrosine Kinase Inhibitors - The present invention relates to novel compounds selected from substituted oxazole derivatives of formula (I) that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant tyrosine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic, and degenerative disorders. More particularly, these compounds are potent and selective c-kit, bcr-abl and Fit-3 inhibitors. | 10-02-2008 |
20080255141 | 2-(3-AMINOARYL) AMINO-4-ARYL-THIAZOLES AND THEIR USE AS C-KIT INHIBITORS - Novel compounds selected from 2-(3-aminoaryl)amino-4-aryl-thiazoles of formula (I) that selectively modulate, regulate, and/or inhibit signal transductions mediated by certain native and/or mutant tyrosine kinases implicated in a variety of human and animal diseases such as cell proliferation metabolic, allergic and degenerative disorders. More particularly, these compounds are potent and selective c-kit inhibitors. | 10-16-2008 |
20090082360 | Use of tyrosine kinase inhibitors for treating CNS disorders - The present invention relates to a method for treating CNS disorders, more particularly selected from the group consisting of depression, schizophrenia, anxiety, migraine, memory loss, pain and neurodegenerative diseases, comprising administering a compound capable of depleting mast cells to a human in need of such treatment. Such compounds can be chosen from tyrosine kinase inhibitors and more particularly non-toxic, selective and potent c-kit inhibitors. Preferably, said inhibitor is unable to promote death of IL-3 dependent cells cultured in presence of IL-3. | 03-26-2009 |
20100093750 | COMBINATION TREATMENT OF SOLID CANCERS WITH ANTIMETABOLITES AND TYROSINE KINASE INHIBITORS - The present invention relates to a method for treating solid cancers including non-small 5 cell lung cancer, pancreatic, bladder, breast and ovarian cancer as well as advanced biliary tract cancers comprising administering at least one antineoplasticagent such as a nucleotide analog, for example gemcitabine, or an antimitotic such as docetaxel, in combination with a tyrosine kinase inhibitor selected from 2-aminoarylthiazoles and 2-aminoaryloxazoles. | 04-15-2010 |
20100113471 | 2-Aminoaryloxazole compounds as tyrosine kinase inhibitors - The present invention relates to novel compounds selected from 2-aminoaryloxazoles that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant tyrosine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic and degenerative disorders. More particularly, these compounds are potent and selective c-kit, bcr-abl, FGFR3 and/or Flt-3 inhibitors. | 05-06-2010 |
20100121063 | PROCESS FOR THE SYNTHESIS OF 2-AMINOTHIAZOLE COMPOUNDS AS KINASE INHIBITORS - The present invention relates to an industrial process of preparing pharmaceutical compounds having the formula (1) which are useful as certain tyrosine kinase inhibitors and more particularly as c-kit and bcr-abl inhibitors. The groups R1 and R2, identical or different, represent each a hydrogen, halogen atom, an alkyl, an alkoxy, a trifluoromethyl, an amino, an alkylamino, a dialkylamino, a solubilising group; m is 0-5 and n is 0-4; the group R3 represents an aryl or an heteroaryl group as described in claims herein. | 05-13-2010 |
20110201620 | 2-(3-AMINOARYL) AMINO-4-ARYL-THIAZOLES AND THEIR USE AS C-KIT INHIBITORS - The present invention relates to the use of masitinib or a pharmaceutically acceptable salt thereof, and in particular of masitinib mesylate, for the preparation of a medicament for the treatment of GIST, to the use of this therapy for the treatment of GIST, and a method of treating mammals, including humans, suffering from GIST by administering to said mammal in need of such treatment an effective dose of masitinib, and in particular masitinib mesylate. | 08-18-2011 |
20120108616 | SUBSTITUTED OXAZOLE DERIVATIVES AND THEIR USE AS TYROSINE KINASE INHIBITORS - The present invention relates to novel compounds selected from substituted oxazole derivatives of formula (I) that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant tyrosine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic, and degenerative disorders. More particularly, these compounds are potent and selective c-kit, bcr-abl and Flt-3 inhibitors. | 05-03-2012 |
20120196871 | PROCESS FOR THE SYNTHESIS OF 2-AMINOTHIAZOLE COMPOUNDS AS KINASE INHIBITORS - The present invention relates to an industrial process of preparing pharmaceutical compounds having the formula I: | 08-02-2012 |
20120302577 | TREATMENT OF GIST WITH MASITINIB - The present invention relates to the use of masitinib or a pharmaceutically acceptable salt thereof, and in particular of masitinib mesylate, for the preparation of a medicament for the treatment of GIST, to the use of this therapy for the treatment of GIST, and a method of treating mammals, including humans, suffering from GIST by administering to said mammal in need of such treatment an effective dose of masitinib, and in particular masitinib mesylate. | 11-29-2012 |
20120309706 | COMBINED TREATMENT OF PANCREATIC CANCER WITH GEMCITABINE AND MASITINIB - The present invention relates to the combined treatment of pancreatic cancers, especially in patients with metastasis and in patients whose cancer is developing resistance to first line treatment with gemcitabine, comprising administration of masitinib and gemcitabine, both in appropriate dosage regimens allowing resensitisation of cancer cells to gemcitabine. | 12-06-2012 |
20130035331 | THIAZOLE AND OXAZOLE KINASE INHIBITORS - The present invention is concerned with substituted azole derivatives that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant proteine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic, and degenerative disorders. In particular, several of these compounds are potent and selective Flt-3 inhibitors or/and syk inhibitors. | 02-07-2013 |
20130072474 | TREATMENT OF DEMENTIA OF ALZHEIMER'S TYPE WITH MASITINIB - The present invention relates to the use of masitinib or a pharmaceutically acceptable salt thereof, for the preparation of a medicament for the treatment of dementia of Alzheimer's type, at appropriate dosage regimen. | 03-21-2013 |
20130202555 | TREATMENT OF MULTIPLE SCLEROSIS WITH MASITINIB - The present invention relates to a tyrosine kinase inhibitor or a mast cell inhibitor, and in particular masitinib or a pharmaceutically acceptable salt thereof, for the treatment of human multiple sclerosis. | 08-08-2013 |
20130267484 | TREATMENT OF RHEUMATOID ARTHRITIS WITH MASITINIB - The present invention relates to a tyrosine kinase inhibitor or a mast cell inhibitor, and in particular masitinib or a pharmaceutically acceptable salt thereof, for the treatment of human rheumatoid arthritis. | 10-10-2013 |
20130289045 | AMINOTHIAZOLE COMPOUNDS AS KINASE INHIBITORS AND METHODS OF USING THE SAME - The present invention relates to an industrial process of preparing pharmaceutical compounds having the formula I: | 10-31-2013 |
20140046063 | TREATMENT OF SERVICE PERSISTANT ASTHMA WITH MASITINIB - The present invention relates to the treatment of severe persistent asthma, and in particular severe persistent corticosteroid-dependent or corticosteroid-resistant asthma, comprising administration a tyrosine kinase inhibitor or a mast cell inhibitor, especially masitinib or a pharmaceutically acceptable salt thereof. | 02-13-2014 |
20140051662 | TREATMENT OF MULTIPLE MYELOMA WITH MASITINIB - The present invention relates to the treatment of multiple myeloma, especially for the treatment of those patients with refractory or first relapsed multiple myeloma, and in particular patients with t(4;14) multiple myeloma, comprising administration of a tyrosine kinase inhibitor or a mast cell inhibitor, especially masitinib or a pharmaceutically acceptable salt thereof, administered in association with an additional care in multiple myeloma; for example, autologous stem-cell transplantation, targeted therapies, anti-myeloma agents such as alkylating agents, corticosteroids, or immunomodulatory agents, including bortezomib, lenalidomide, and dexamethasone. | 02-20-2014 |
20140088108 | 2-(3-AMINOARYL) AMINO-4-ARYL-THIAZOLES AND THEIR USE AS C-KIT INHIBITIORS - Novel compounds selected from 2-(3-aminoaryl) amino-4-aryl-thiazoles of formula (I) that selectively modulate, regulate, and/or inhibit signal transductions mediated by certain native and/or mutant tyrosine kinases implicated in a variety of human and animal diseases such as cell proliferative metabolic, allergic and degenerative disorders. More particularly, these compounds are potent and selective c-kit inhibitors. | 03-27-2014 |
20140147415 | TREATMENT OF MASTOCYTOSIS WITH MASITINIB - The present invention relates to the treatment of mastocytosis, and in particular indolent forms of mastocytosis (including smoldering systemic, indolent systemic and cutaneous mastocytosis), comprising administration of a tyrosine kinase inhibitor or a mast cell inhibitor, especially masitinib or a pharmaceutically acceptable salt thereof, in particular in an appropriate dosage regimen. | 05-29-2014 |
20140179698 | SELECTIVE PROTEIN KINASE INHIBITORS - The present invention relates to compounds of formula I or pharmaceutically acceptable salts thereof: | 06-26-2014 |
20150272945 | USE OF MASITINIB FOR TREATMENT OF CANCER IN PATIENT SUBPOPULATIONS IDENTIFIED USING PREDICTOR FACTORS - A method for treating patients afflicted with cancer, wherein the patients are treated with a compound including tyrosine kinase inhibitor, mast cell inhibitor or c-Kit inhibitor, in particular masitinib, optionally in combination with at least one antineoplastic agent. The tyrosine kinase inhibitor, mast cell inhibitor or c-Kit inhibitor, and the optional at least one antineoplastic agent, are administered in a dosage regimen that includes a therapeutically effective amount. Also described are methods for predicting therapeutic response to the treatment in a given patient and therefore identification of applicable patient subpopulations based upon these predictor factors; sometimes referred to as biomarkers. One method is based upon the clinical marker of pain intensity. Another method is based upon gene expression predictive biomarkers assessed via RNA expression in peripheral blood cell samples collected prior to treatment with the compound, which is also used for treating patients afflicted with pancreatic cancer. | 10-01-2015 |
20150290235 | USE OF SMALL MOLECULE INHIBITORS/ACTIVATORS IN COMBINATION WITH (DEOXY)NUCLEOSIDE OR (DEOXY)NUCLEOTIDE ANALOGS FOR TREATMENT OF CANCER AND HEMATOLOGICAL MALIGNANCIES OR VIRAL INFECTIONS - A method for treating patients afflicted with cancer (including hematological malignancies) or viral infections, wherein the patients are under treatment or are to be treated with at least one anticancer or antiviral agent, and in particular (deoxy)nucleotide or (deoxy)nucleoside analog drugs, includes administering at least one small molecule inhibitor/activator (including ATP competitive inhibitors, signal transduction inhibitors/activators, protein kinase inhibitors/activators, and tyrosine kinase inhibitors/activators) in combination with the (deoxy) nucleotide or (deoxy)nucleoside analog, and wherein the small molecule inhibitor/activator is administered in sufficient amount to modulate deoxynucleotide or deoxynucleoside kinase activity (and in particular deoxycytidine kinase activity) to modulate activation of the (deoxy)nucleotide or (deoxy)nucleoside analog in vivo with a subsequent therapeutically beneficial anticancer or antiviral effect. The combined treatments together include a therapeutically effective amount. | 10-15-2015 |
20160022671 | TREATMENT OF MASTOCYTOSIS WITH MASITINIB - The treatment of mastocytosis, and in particular indolent forms of mastocytosis (including smoldering systemic, indolent systemic and cutaneous mastocytosis), including administration of a tyrosine kinase inhibitor or a mast cell inhibitor, especially masitinib or a pharmaceutically acceptable salt or solvate thereof, in particular in an appropriate dosage regimen. | 01-28-2016 |
20160089368 | TREATMENT OF MASTOCYTOSIS WITH MASITINIB - The treatment of mastocytosis, and in particular indolent forms of mastocytosis (including smoldering systemic, indolent systemic and cutaneous mastocytosis), including the administration of a tyrosine kinase inhibitor or a mast cell inhibitor, especially masitinib or a pharmaceutically acceptable salt or solvate thereof, in particular in an appropriate dosage regimen. | 03-31-2016 |