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Additional six-membered hetero ring consisting of five ring carbons and one ring nitrogen attached directly or indirectly to the 1,3-diazine by nonionic bonding

Subclass of:

514 - Drug, bio-affecting and body treating compositions

514001000 - DESIGNATED ORGANIC ACTIVE INGREDIENT CONTAINING (DOAI)

514183000 - Heterocyclic carbon compounds containing a hetero ring having chalcogen (i.e., O,S,Se or Te) or nitrogen as the only ring hetero atoms DOAI

514247000 - Hetero ring is six-membered consisting of two nitrogens and four carbon atoms (e.g., pyridazines, etc.)

514252100 - 1,4 diazines

514252120 - Piperazines (i.e., fully hydrogenated 1,4-diazines)

514252130 - Additional hetero ring attached directly or indirectly to the piperazine ring by nonionic bonding

514252140 - The additional hetero ring is a 1,3 diazine ring

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DocumentTitleDate
20130085145IMATINIB MESILATE PHARMACEUTICAL TABLET - The present invention provides a pharmaceutical tablet, comprising Imatinib in an amount of 50-75% w/w of the total tablet weight and comprising at least one pharmaceutically acceptable excipient without a binding agent and the process for preparation of the same.04-04-2013
20100113470BCR-ABL VARIANTS - A splice variant of bcr-abl mRNA that produces BCR-ABL protein with a truncated C-terminus and its role in resistance to treatment with kinase inhibitors is disclosed. Vectors for expressing the truncated gene product are provided as well as recombinant cells that express the truncated gene product from a cDNA construct. Also provided are methods compositions and kits for detecting the BCR-ABL splice variant. Additionally, methods for screening BCR-ABL kinase domain inhibitors which rely on the recombinant cells and methods of predicting likelihood for resistance of a CML patient with a BCR/ABL translocation respond to treatment with one or more BCR-ABL kinase inhibitors are also disclosed.05-06-2010
20090281112ADATANSERIN AND METABOLITES THEREOF FOR TREATMENT OF ATTENTION DEFICIT DISORDER, ANXIETY, DEPRESSION, SEXUAL DYSFUNCTION, AND OTHER DISORDERS - The present invention relates to a method for alleviation, prevention, and treatment of attention deficit disorder, anxiety, depression, sexual dysfunction, aggressive behavior, alcohol dependency, psychoses, and related conditions by administering adatanserin and/or metabolites of adatanserin. The present invention also relates to a method of weight loss by administering adatanserin and/or metabolites of adatanserin.11-12-2009
20130040958IMATINIB MESYLATE PREPARATION PROCEDURE - Methods for making Imatinib mesylate of formula (I):02-14-2013
20100144750Use of N-Phenyl-2-Pyrimidineamine Derivatives Against Mast Cell-Based Diseases Like Allergic Disorders - Use of the N-phenyl-2-pyrimidine-amine derivatives of formula I,06-10-2010
20100041666Use of N-Phenyl-2-pyrimidineamine Derivativea Against Mast Cell-based Diseases Like Allergic Disorders - Use of the N-phenyl-2-pyrimidine-amine derivatives of formula I,02-18-2010
20090203709Pharmaceutical Dosage Form For Oral Administration Of Tyrosine Kinase Inhibitor - A pharmaceutical dosage form comprises a solid dispersion product of at least one tyrosine kinase inhibitor, at least one pharmaceutically acceptable polymer, and at least one pharmaceutically acceptable solubilizer.08-13-2009
20090093496PREPARATION OF PHARMACEUTICAL SALTS OF PIPERAZINE COMPOUNDS - The present invention is generally directed to a process to directly prepare pharmaceutically acceptable salts enriched with respect to selected rotameric salts of a basic compound, by creative choice of an acid and a solvent medium. The process is particularly useful in preparing specific rotamers of pharmaceutically useful salts in desired preponderance of a rotamer.04-09-2009
20080312250Combination Comprising a Bcrp Inhibitor and 4- (4-Methylpiperazin-1-Ylmethyl)-N-[4-Methyl-3- (4-Pyridin-3-Yl) Pyrimidin-2-Ylamino) Phenyl] -Benzamide - The present invention relates to a combination which comprises a BCRP inhibitor and Compound I of formula (I),12-18-2008
20110294820N-Oxides of n-Phenyl-2-pyrimidine-amine Derivatives - The invention relates to N-phenyl-2-pyrimidine-amine derivatives derivatives in which at least one nitrogen atom carries an oxygen atom to form the corresponding N-oxides, to processes for the preparation thereof, to pharmaceutical compositions comprising those compounds, and to the use thereof in the preparation of pharmaceutical compositions for the therapeutic treatment of warm-blooded animals, including humans.12-01-2011
20080275055IMATINIB PRODUCTION PROCESS - Provided is a process for producing imatinib and salts thereof, e.g., imatinib mesylate. The process includes reacting4-(4-methyl-piperazin-1-ylmethyl)-benzoic acid with N-(5-amino-2-methylphenyl)-4-(3-pyridyl)-2-pyrimidine-amine in the presence of a carboxylic acid coupling reagent, to produce imatinib, and optionally converting the imatinib into a salt.11-06-2008
20100022553Therapeutic Combination Comprising an Aurora Kinase Inhibitor and Imatinib - The present invention provides a therapeutic combination comprising (a) a compound 1 of formula (A) as set forth in the specification and (b) a BCR-ABL kinase inhibitor selected from the group consisting of Imatinib, Dasatinib, Nilotinib, Bosutinib and Inno-406, wherein the active ingredients are present in each case in free form or in the form of a pharmaceutically acceptable salt or any hydrate thereof.01-28-2010
20090181977Anhydrous Amorphous Imatinib Mesylate - Described is a highly stable amorphous form of imatinib mesylate having a water content of less than 0.5 percent by weight, based on the total weight of the amorphous imatinib mesylate, (anhydrous amorphous imatinib mesylate), a process for preparation thereof, and pharmaceutical compositions.07-16-2009
20080312251Aminopyrimidine Compounds and Their Salts, Process for Preparation and Pharmaceutical Use Thereof - The present invention provides aminopyrimidine compounds of formula (I) and their salts, wherein R12-18-2008
20090082361DEUTERIUM-ENRICHED IMATINIB - The present application describes deuterium-enriched imatinib, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-26-2009
20090076024Episomal Fusion Gene - The present invention relates to an episomal structure expressing a functional oncogene, whereby said oncogene is a fusion gene of two chromosomal gene fragments. More specifically, the invention relates to a NUP214-ABL1 fusion product, important in the development of T-cell acute lymphoblastic leukemia, to methods to detect the fusion and to methods to prevent the oncogenic activity of said fusion product.03-19-2009
20090149468Substituted heterocyclic compounds and methods of use - The present invention relates to therapeutic diazobicyclo pyridines and their use in the treatment of arthritis, rheumatoid arthritis, psoriatic arthritis or osteoarthritis, organ transplant, acute transplant or heterograft and homograft rejection, ischemic and reperfusion injury, transplantation tolerance induction, multiple sclerosis, inflammatory bowel disease, ulcerative colitis, Crohn's disease, lupus, graft vs. host diseases, T-cell mediated hypersensitivity diseases, contact hypersensitivity, delayed-type hypersensitivity, gluten-sensitive enteropathy, Type 1 diabetes, psoriasis, contact dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Graves' Disease, Addison's disease, autoimmune polyglandular disease, autoimmune alopecia, pernicious anemia, vitiligo, autoimmune hypopituatarism, Guillain-Barre syndrome, autoimmune diseases, glomerulonephritis, serum sickness, uticaria, respiratory allergies, asthma, hayfever, allergic rhinitis, skin allergies, scleracielma, mycosis fungoides, acute inflammatory responses, acute respiratory distress syndrome, dermatomyositis, alopecia areata, chronic actinic dermatitis, eczema, Behcet's disease, Pustulosis palmoplanteris, Pyoderma gangrenum, Sezary's syndrome, atopic dermatitis, systemic schlerosis, morphea, Type II diabetes and cancers where PKC theta or other PKC-family kinases are activated, overexpressed or facilitate tumor growth or survival of tumor cells, T cell leukemia, thymoma, T and B cell lymphoma, colon carcinoma, breast carcinoma and lung carcinoma or provides resistance to chemotherapeutic drugs.06-11-2009
20090149467Tyrosine Kinase Inhibitors - The present invention relates to pyridinyloxy- and pyrimidinyloxyindole derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.06-11-2009
20080312252Combination of Organic Compounds - The invention provides a pharmaceutical combination comprising: 12-18-2008
20110195975MATERIALS AND METHODS FOR SUPPRESSING AND/OR TREATING NEUROFIBROMA AND RELATED TUMORS - Germline mutations in the NF1 tumor suppressor gene cause Von Recklinghausen's neurofibromatosis type 1 (NF1), a common genetic disorder of the nervous system characterized by plexiform neurofibroma development. Using adoptive transfer of hematopoietic cells, we establish that NF1 heterozygosity of bone marrow derived cells in the tumor microenvironment is sufficient to allow neurofibroma progression in the context of Schwann cell nullizygosity. Further, genetic or pharmacologic attenuation of the c-kit signaling pathway in hematopoietic cells greatly diminishes neurofibroma initiation and progression. These studies identify haploinsufficient hematopoietic cells and the c-kit receptor as therapeutic targets for preventing plexiform neurofibromas and implicate mast cells as critical mediators of tumor initiation. Administering therapeutically effective doses of a tyrosine kinase inhibitor such as the compound imatinib mesylate to a patient in need thereof to treat tumors in a human patient afflicted with plexiform neurofibroma.08-11-2011
20100120787MODIFICATION OF AMYLOID-BETA LOAD IN NON-BRAIN TISSUE - The present invention relates to methods and compositions for modulating levels of amyloid-β peptide (Aβ) exhibited by non-neuronal (i.e., peripheral) cells, fluids, or tissues. The invention also relates to modulation of Aβ levels via selective modulation (e.g., inhibition) of γ-secretase activity. The invention also relates to methods of preventing, treating or ameliorating the symptoms of a disorder, including but not limited to an Aβ-related disorder, by administering a compound that result in the modulation of γ-secretase in a non-neuronal tissue, either directly or indirectly to prevent, treat or ameliorate the symptoms of a brain Aβ disorder, such as Alzheimer's disease.05-13-2010
20110201619Use of N-Phenyl-2-pyrimidineamine Derivatives Against Mast Cell-based Diseases Like Allergic Disorders - Use of the N-phenyl-2-pyrimidine-amine derivatives of formula I,08-18-2011
200902811113-HYDROXY GEPIRONE FOR THE TREATMENT OF ATTENTION DEFICIT DISORDER AND SEXUAL DYSFUNCTION - The present invention relates to a method for alleviation, prevention, and treatment of attention deficit disorder, sexual dysfunction, and related conditions by administering certain bioactive metabolites of the known anti-depressant compound gepirone. In a preferred embodiment, the compound is 4,4,-dimethyl-3-hydroxy-1-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-2,6-piperidinedione (3-OH gepirone).11-12-2009
20100298336PYRIMIDINES AS NOVEL THERAPEUTIC AGENTS - The present invention features compounds having the Formula (Ia) and (Ib) (e.g., a compound of any of Formulas ((Ia-2)-(Ia-21)), including other tautomers, stereoisomers, E/Z stereoisomers, prodrugs, pharmaceutically acceptable salts, and compositions thereof. The invention also features methods for treating or preventing pain (e.g., neuropathic pain), inflammation, or epilepsy in a patient by administering an effective amount of a compound of Formula (Ia) or (Ib). The invention also features a method for treating or preventing pain (e.g., neuropathic pain), inflammation, or epilepsy in a patient that includes administering to a patient in need thereof an effective amount of a compound of Formula (IIa) or (IIb) (e.g., a compound of any of Formulas ((IIa-2)-(IIa-6)). The compounds described herein (e.g., a compound of Formulas (Ia), (Ib), (IIa), or (IIb)) can also be used as anticonvulsants.11-25-2010
20100120786Piperazine Derivatives - This invention relates to novel compounds that are piperazine derivatives, and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel piperazine compounds that are derivatives of the chemokine CCR5 receptor antagonist, vicriviroc. This invention also provides pyrogen-free compositions comprising one or more compounds of the invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are treated by administering chemokine CCR5 receptor antagonists, such as vicriviroc. The invention also relates to the use of one or more of the disclosed compounds as reagents in analytical studies involving vicriviroc.05-13-2010
20080280919QUINOLINE AND QUINAZOLINE DERIVATIVES HAVING AFFINITY FOR 5HT1-TYPE RECEPTORS - Disclosed are methods for use of compounds of formula (I) in combination with other active substances in the treatment of CNS disorders such as depression or anxiety.11-13-2008
20120295917IMATINIB DICHLOROACETATE AND ANTI-CANCER AGENT COMPRISING THE SAME - The present invention relates to imatinib dichloroacetate and an anti-cancer agent comprising the same. The imatinib dichloroacetate of the present invention can inhibit tyrosine kinase as well as induce cancer cells to kill themselves via apoptosis, thereby inhibit growth of cancer cells and lead to their destruction, and show significantly enhanced anti-cancer effects by synergy between imatinib and dichloroacetic acid.11-22-2012
20090264439Combination of a) N--4-(3-pyridyl)-2-pyrimidine-amine and b) a histone deacetylase inhibitor for the treatment of leukemia - The invention pertains to a combination of a histone deacetylase inhibitor and N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine or a pharmaceutically acceptable salt thereof for simultaneous, separate or sequential use for the treatment of leukemia and especially N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-resistant leukemia.10-22-2009
20090264438Polymorphic forms of imatinib mesylate and processes for preparation of novel crystalline forms as well as amorphous and form alpha - Solvates and crystalline forms of imatinib mesylate are described. Further, methods for preparing such solvates and crystalline forms of imatinib mesylate are described.10-22-2009
200902644374-Piperazinyl-Pyrimidine Compounds Suitable for Treating Disorders that Respond to Modulation of the Dopamine D3 Receptor - The present invention relates to novel 4-piperazinylpyrimidine compounds. The compounds possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of the dopamine D10-22-2009
20120196870COMBINATION THERAPY AND CANCER - The disclosure relates to methods of treating tuberous sclerosis in a subject, comprising administering a composition comprising an mTOR inhibitor and a tyrosine kinase inhibitor to a subject that is diagnosed with, suspected of, or exhibiting symptoms of cancer. In some embodiments, the cancer is tuberous sclerosis. In some embodiments, the mTOR inhibitor is sirolimus and the tyrosine kinase inhibitor is imatinib. In some embodiments, the disclosure relates to a composition comprising an mTOR inhibitor and a tyrosine kinase inhibitor. In some embodiments, the disclosure relates to a composition comprising sirolimus and imatinib.08-02-2012
20090054449Substituted N-heterocyclic Compounds and Their Use as Dopamine D3 Receptor Ligands - The invention relates to substituted N-heterocyclic compounds of general formula (I.A)02-26-2009
20120142696SUBSTITUTED INDOLE/INDAZOLE-PYRIMIDINYL COMPOUNDS - The present disclosure provides indole/indazole-pyrimidinyl compounds useful in the treatment of p38 kinase mediated diseases, such as lymphoma and auto-inflammatory disease, having the structure of Formula (I):06-07-2012
20090325977CANCER COMBINATION THERAPY COMPRISING AZD2171 AND IMATINIB - The present invention relates to a method for the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionizing radiation, particularly a method for the treatment of a cancer, particularly a cancer involving a solid tumor or a leukaemia, which comprises the administration of AZD2171 in combination with imatinib; to a pharmaceutical composition comprising AZD2171 and imatinib; to a combination product comprising AZD2171 and imatinib for use in a method of treatment of a human or animal body by therapy; to a kit comprising AZD2171 and imatinib; to the use of AZD2171 and imatinib in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionizing radiation.12-31-2009
20120095014AMINOPYRIMIDINES USEFUL AS KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.04-19-2012
20110224223MTOR Modulators and Uses Thereof - The present invention provides methods and compositions for selective modulation of certain protein kinases, and especially mTor complexes. The methods and compositions are particularly useful in inhibiting mTor selectively for therapeutic applications.09-15-2011
20090093495COMBINATION OF A SRC KINASE INHIBITOR AND A BCR-ABL INHIBITOR FOR THE TREATMENT OF PROLIFERATIVE DISEASES - A combination and methods are disclosed which are useful for the treatment of cancer and/or leukemia.04-09-2009
20080261992Pyridin-2-One Compounds and Their Use as Modulators of the Dopamine D3 Receptor - The invention relates to pyridin-2-one compounds of general formula (I)10-23-2008
20090209549Analogs of Benzoquinone-Containing Ansamycins and Methods of Use Thereof - The present invention provides analogs of benzoquinone-containing ansamycins and uses thereof for treating and modulating disorders associated with hyperproliferation, such as cancer. The present invention provides analogs of benzoquinone-containing ansamycins where the benzoquinone is reduced to a hydroquinone and trapped by reaction with a suitable acid, preferably ones that increase the solubility and air stability of the resulting 17-ammonium hydroquinone ansamycin analog.08-20-2009
20090239878COMBINATIONS OF (A) AN ATP-COMPETITIVE INHIBITOR OF C-ABL KINASE ACTIVITY WITH (B) TWO OR MORE OTHER ANTINEOPLASTIC AGENTS - The invention relates to combinations of (a) an ATP-competitive inhibitor of c-abl kinase activity with (b) two or more other antineoplastic agents for simultaneous, separate or sequential use, in particular for the delay of progression or treatment of a proliferative disease09-24-2009
20090239879N-OXIDES OF N-PHENYL-2-PYRIMIDINE-AMINE DERIVATIVES - The invention relates to N-phenyl-2-pyrimidine-amine derivatives derivatives in which at least one nitrogen atom carries an oxygen atom to form the corresponding N-oxides, to processes for the preparation thereof, to pharmaceutical compositions comprising those compounds, and to the use thereof in the preparation of pharmaceutical compositions for the therapeutic treatment of warm-blooded animals, including humans.09-24-2009
20090298843TREATMENT OF HEMATOLOGICAL MALIGNANCIES WITH FTS AND A BCR-ABL TYROSINE KINASE INHIBITOR - Disclosed are methods of treating a hematological malignancy by administering to a human in need thereof effective amounts of FTS (Farnesylthiosalicylic Acid), or various analogs thereof, or a pharmaceutically acceptable salt thereof, optionally in combination with a Bcr-Abl tyrosine kinase inhibitor. Also disclosed are pharmaceutical compositions comprising FTS, or various analogs thereof, or a pharmaceutically acceptable salt thereof, a Bcr-Abl tyrosine kinase inhibitor, preferably Imatinib and a pharmaceutically acceptable carrier.12-03-2009
20100160340PROTEIN KINASE INHIBITORS - The present invention provides a compound of formula (I):06-24-2010
20100160339TREATING PANCREATITIS - This document provides methods and materials related to treating pancreatitis. For example, methods and materials relating to the use of a tyrosine kinase inhibitor to pancreatitis are provided.06-24-2010
201001791642,4-PYRIMIDINEDIAMINE COMPOUNDS FOR TREATMENT OF INFLAMMATORY DISORDERS - 2,4-Pyrimidinediamine compounds represented by formula (I), methods for preparing the same and methods for treating an inflammatory disorder and for inhibiting the production of IL-23 and/or stimulating the production of IL-10 using the same:07-15-2010
20100184779METHOD FOR OPTIMIZING THE TREATMENT OF CHRONIC MYELOID LEUKEMIA WITH ABL TYROSINE KINASE INHIBITORS - The present invention relates to a method for evaluating patients to help optimizing the treatment of chronic myeloid leukemia (CML) in a human patient population. More specifically, the method comprises the steps of (a) determining the OCT-1 Activity in pre-therapy blood of a warm-blooded animal suffering from CML, and (b) administering a daily dose between about 500 and 1200 mg of Imatinib mesylate to the warm-blooded animal suffering from CML showing an OCT-1 Activity corresponding to Imatinib intracellular concentration to below about 6.0 to 10.0 ng/200,000 cells, especially about 8.0 to 8.5 ng/200,000 cells.07-22-2010
20100184778NOVEL HETEROCYCLE COMPOUNDS AND USES THEREOF - The invention relates to chemical compounds, or pharmaceutically acceptable salts thereof of the formula (Q) or (I), which penetrate the blood-brain barrier, inhibit the formation and accumulation of beta-amyloid, and are useful in the treatment of neurodegenerative diseases, particularly Alzheimer's disease. Further, the compounds of the present invention inhibit certain kinases, thereby being useful for the treatment of cancers of the central nervous system.07-22-2010
20120142697Salt forms of 4-(4-Methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl) pyrimidin-2-ylamino)phenyl]-benzamide - The present invention relates to acid addition salts of 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]-benzamide, which are selected from the group consisting of a tartrate salt, such as a (D)(−) tartrate salt or a (L)(+) tartrate salt, a hydrochloride salt, a citrate salt, a malate salt, a fumarate salt, a succinate salt, a benzoate salt, a benzenesulfonate salt, a pamoate salt, a formate salt, a malonate salt, a 1,5-naphthalenedisulfonate salt, a salicylate salt, a cyclohexanesulfamate salt, a lactate salt, a mandelate salt, aq glutarate salt, an adipate salt, a squarate salt, a vanillate salt, an oxaloacetate salt, an ascorbate salt and a sulfate salt.06-07-2012
20100240673EML4-ALK Fusion Gene - The present inventors found that a fusion gene present in some cancer patients is an oncogene. The present invention relates to a polypeptide as a novel fusion protein, a polynucleotide encoding the polypeptide, a vector comprising the polynucleotide, a transformed cell comprising the vector, a method for detecting the fusion protein or polynucleotide, a method for screening a therapeutic agent for cancer, and a method for treating cancer that is shown to be positive for the fusion gene. Further, the present invention relates kit, primer set, and probe useful in the detection of cancer that is shown to be positive for the fusion gene.09-23-2010
20100144749TREATMENT OF CANCERS WITH ACQUIRED RESISTANCE TO KIT INHIBITORS - The present invention provides compositions and methods for treating cancers which have acquired resistance to a KIT inhibitor by administering effective amounts of sorafenib.06-10-2010
20130131076METHODS AND COMPOSITIONS RELATED TO WRAPPING OF DEHYDRONS - This application describes a novel technology in drug discovery and drug-based imaging/detection: the wrapping technology. This technology is based on identified singularities in the structure of soluble proteins. In contrast with drug-design approaches based on standard structural considerations, the packing of a protein, or more precisely, its dehydron pattern, may be used as a selectivity filter to design small-molecule inhibitors. The wrapping technology described herein is a novel form of rational drug design for avoiding side effects in drug therapy and sharpening the inhibitory impact of drugs on the oncokinome.05-23-2013
20100222360Treatment of Malignant Peripheral Nerve Sheath Tumors - The present invention pertains to a combination comprising (a) at least one c-Jun N-terminal kinase (JNK) inhibitor and (b) 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide or a pyrimidylaminobenzamide of formula I09-02-2010
20110245266PYRIDIN-2-ONE COMPOUNDS AND THEIR USE AS MODULATORS OF THE DOPAMINE D3 RECEPTOR - The invention relates to novel pyridin-2-one compounds of general formula (I), in which A represents a 4- to 6-membered hydrocarbon chain that can have 1 or 2 methyl groups as substituents, wherein 1 or 2 carbon atoms can be replaced by oxygen, a carbonyl group or sulfur, and the hydrocarbon chain can have a double bond or a triple bond; R10-06-2011
20130150375GEPIRONE-ER TREATMENT OF MAJOR DEPRESSION IN PATIENTS TAKING NON-STEROIDAL ANTI-INFLAMMATORY DRUGS (NSAIDs) - A method of treatment of depression in a person also taking non-Steroidal anti-inflammatory drugs (NSAIDs) by administering gepirone as either a short term or long term therapy.06-13-2013
20100179165METHODS FOR TREATING INFLAMMATORY DISORDERS USING 2,4-PYRIMIDINEDIAMINE COMPOUNDS - Methods for treating an inflammatory disorder and for inhibiting the production of IL-23 using 2,4-pyrimidinediamine compounds represented by formula (I):07-15-2010
20100160341HETEROARYL, HETEROCYCLIC AND ARYL COMPOUNDS WHICH INHIBIT LEUKOCYTE ADHESION MEDIATED BY VLA-4 - Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.06-24-2010
20100069398Combination therapy - The present invention relates to a method for the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation, particularly a method for the treatment of a cancer, particularly a cancer involving a solid tumour or a leukaemia, which comprises the administration of ZD6474 in combination with imatinib; to a pharmaceutical composition comprising ZD6474 and imatinib; to a combination product comprising ZD6474 and imatinib for use in a method of treatment of a human or animal body by therapy; to a kit comprising ZD6474 and imatinib; to the use of ZD6474 and imatinib in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation.03-18-2010
20080318971TREATMENT OF IMATINIB RESISTANT LEUKEMIA - The present invention provides 4-anilino-3-quinolinecarbonitriles compounds useful for treating a subject having an BcrAbl positive leukemia that is resistant to imatinib.12-25-2008
20110251210MODIFIED CHLOROQUINES WITH SINGLE RING MOIETY OR FUSED RING MOIETY - The disclosure provides modified chloroquine compounds having single ring or fused ring moieties. Also provided are pharmaceutical compositions comprising such compounds, methods of using such compounds to inhibit or treat diseases or conditions caused by chloroquine-resistant (CQ10-13-2011
20080249104Salt Forms of 4- (4-Methylpiperazin-1-Ylmethyl) -N- [4-Methyl-3- (4-Pyridin-3-Yl) Pyrimidin-2-Ylamino) Phenyl]- Benzamide - The present invention relates to acid addition salts of 4-[(4-methyl-1-piperazinyl)methyl]-N-(4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]-benzamide, which are selected from the group consisting of a tartrate salt, such as a (D)(−) tartrate salt or a (L)(+) tartrate salt, a hydrochloride salt, a citrate salt, a malate salt, a fumarate salt, a succinate salt, a benzoate salt, a benzenesulfonate salt, a pamoate salt, a formate salt, a malonate salt, a 1,5-naphthalenedisulfonate salt, a salicylate salt, a cyclohexanesulfamate salt, a lactate salt, a mandelate salt, aq glutarate salt, an adipate salt, a squarate salt, a vanillate salt, an oxaloacetate salt, an ascorbate salt and a sulfate salt.10-09-2008
20080214558PYRIMIDINE-2,4-DIAMINE DERIVATIVES AND THEIR USE AS JAK2 KINASE INHIBITORS - Pyrimidine-2,4-diamines derivatives having activity as JAK2 kinase inhibitors are disclosed, as well as pharmaceutical compositions and methods for using the same in the treatment of cancer and other JAK2 kinase-associated conditions.09-04-2008
20080255139Use Of 4- (4-Methylpiperazin-1-Ylmethyl)-N-[4-Methyl-3-(4-(Pyridin-3-Yl)Pyrimidin-2-Ylamino)Phenyl]-Benzamide to Inhibit the Tyrosine Kinase Receptor C-Fms - This invention relates to the use of 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-(pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide (also known as imatinib, gleevec, glivec, cgp57148b or STI571), or a pharmaceutically acceptable salt thereof, for the manufacture of a medicament for the treatment of c-fms-associated diseases including; choriocarcinoma, malignant histiocytosis, embryonal carcinoma, endometrial carcinoma, brain microglial tumours, sarcoidosis, microglial cell involvement in normal and variant Creutzfeld-Jacob disease, and amyotrophic lateral sclerosis.10-16-2008
201100539522-HETEROARYLAMINO-PYRIMIDINE DERIVATIVES AS KINASE INHIBITORS - The invention provides compounds of Formula (I) and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit, PDGFRα, PDGFRβ, CSF1R, Abl, BCR-Abl, CSK, JNK1, JNK2, p38, p70S6K, TGFβ, SRC, EGFR, trkB, FGFR3, Fes, Lck, Syk, RAF, MKK4, MKK6, SAPK2β, BRK, Fms, KDR, c-raf or b-raf kinases.03-03-2011
20120302577TREATMENT 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
20100298338METHOD OF OPTIMIZING THE TREATMENT OF PROLIFERATIVE DISEASES MEDIATED BY THE TYROSINE KINASE RECEPTOR KIT - The invention relates to a method of treating proliferative diseases mediated by the tyrosine kinase receptor KIT, in particular GIST, in a human patient population.11-25-2010
20100216809PIPERIDINE/PIPERAZINE DERIVATIVES - The invention further relates to a DGAT inhibitor of formula (I), including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —NR08-26-2010
20100197702OPHTHALMIC COMPOSITION WITH NITRIC OXIDE DONOR COMPOUND AND METHOD OF FORMING AND USING SAME - The present invention is directed to the provision of ophthalmic compositions such as multi-dose, topical, ophthalmic compositions. The compositions include a nitric oxide (NO) donor compound.08-05-2010
20110190313Treatment of Pulmonary Arterial Hypertension - The present invention pertains to the use of 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide or a pharmaceutically acceptable salt thereof or a pyrimidylaminobenzamide of formula I08-04-2011
20100029674Methods of Using Phosphoantigen for the Treatment of Cancer - The present invention relates to compositions and methods useful for treating a cancer in mammals, including humans. The methods and compositions typically comprise use of a chemotherapeutic agent and a γδ T cell activator such that the composition is effective for treating a cancer. Preferably the composition enhances the effect of the γδ T cell activator and/or prevents or delays the escape of a tumor from control chemotherapy, particularly an anti-angiogenic chemotherapeutic agent.02-04-2010
200902919622-PHENYL-6-AMINOCARBONYL-PYRIMIDINE DERIVATIVES AND THEIR USE AS P2Y12 RECEPTOR - The invention relates to 2-phenyl-6-aminbcarbonyl-pyrimidinc derivatives and their use as P2Y11-26-2009
20110306618JNK Modulators - Compounds of formula (I) modulate JNK wherein X12-15-2011
20100029675Pyrimidine-2, 4-diamine JAK2 Kinase inhibiting anti-inflammation use - A method of treatment or prevention of Castleman's disease, atherosclerosis, coronary artery disease, peripheral edema, peripheral vascular disease, glaucoma, and wet or dry age-related macular degeneration (AMD), asthma; chronic bronchitis; chronic obstructive pulmonary disease; adult respiratory distress syndrome; infant respiratory distress syndrome; cough; chronic obstructive pulmonary disease in animals; adult respiratory distress syndrome; ulcerative colitis; Crohn's disease; hypersecretion of gastric acid; bacterial, fungal, or viral induced sepsis or septic shock; endotoxic shock; laminitis or colic in horses; spinal cord trauma; head injury; neurogenic inflammation; pain; reperfusion injury of the brain; psoriatic arthritis; rheumatoid arthritis; alkylosing spondylitis; osteoarthritis; inflammation; or cytokine-mediated chronic tissue degeneration comprises the step of administering a therapeutically effective amount, or a prophylactically effective amount, of a compound having the following structure (I):02-04-2010
20100240672MELT-PROCESSED IMATINIB DOSAGE FORM - The invention provides a dosage form, comprising a melt-processed mixture of (a) a pharmaceutically effective amount of imatinib or a salt thereof, (b) at least one polymeric binder, and (c) at least one pharmaceutically acceptable non-ionic surfactant. The invention provides imatinib dosage forms with high drug loading which can be prepared in a simple and efficient manner, imatinib dosage forms from which the active principle is released in an essentially pH-independent fashion, and extended release imatinib dosage forms.09-23-2010
20090105269Multifunctional Compounds and Methods of Use Thereof - Compositions comprising multifunctional agents and methods of use thereof are provided.04-23-2009
20090082360Use 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
20120015955F, G, H, I and K Crystal Forms of Imatinib Mesylate - The invention relates to the F-crystal form, G-crystal form, H-crystal form, I-crystal form and K-crystal form of the methanesulfonic acid addition salt of 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-(pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide, certain processes for their preparation, pharmaceutical compositions containing these crystal forms, their use in diagnostic methods or for the therapeutic treatment of warm-blooded animals, and their use as an intermediate or for the preparation of pharmaceutical preparations for use in diagnostic methods or for the therapeutic treatment of warm-blooded animals, especially humans.01-19-2012
20120022077NOVEL CYANOPYRIMIDINE DERIVATIVE - The present invention relates to a novel cyanopyrimidine compound and a pharmaceutical composition which have a safe and potent adenosine A2a receptor agonistic activity.01-26-2012
20120208824ROS Kinase in Lung Cancer - The invention provides the identification of the presence of polypeptides with ROS kinase activity in mammalian lung cancer. In some embodiments, the polypeptide with ROS kinase activity is the result of a fusion between a ROS-encoding polynucleotide and a polynucleotide encoding a second (non-ROS) polypeptide. Three different fusion partners of ROS are described, namely proteins encoded by the FIG gene, the SLC34A2 gene, and the CD74 gene. The invention enables new methods for determining the presence of a polypeptide with ROS kinase activity in a biological sample, methods for screening for compounds that inhibit the proteins, and methods for inhibiting the progression of a cancer (e.g., an lung cancer).08-16-2012
20120071491Oligomer-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
20090012097Polycyclic 1,2,3,4-Tetrahydro-Isoquinoline Derivatives and Compositions Comprising Them As Ppar Modulators - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of the Peroxisome Proliferator-Activated Receptor (PPAR) families.01-08-2009
20100240674USE OF COMPOUNDS DERIVED FROM BENZAMIDINE METHANESULPHONATE OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, FOR EXAMPLE IMATINIB MESYLATE, FOR THE PREPARATION O F A DRUG FOR THE TREATMENT OF NEURODEGENERATIVE NIEMANN-PICK C DISEASE (NPC) - This invention relates to the use of imatinib mesylate for the treatment of metabolism disorders characterized by neurodegeneration, in particular a metabolism disorder characterized by an inability to metabolize lipids such as in persons with Niemann-Pick Type C disease. More specifically, this invention relates to a method of treating neurodegenerative disease, comprising administering a therapeutically effective amount of a compound derived from imatinib mesylate or a pharmaceutically acceptable salt thereof.09-23-2010
20120309767PROCESS FOR THE PREPARATION OF ALPHA FORM OF IMATINIB MESYLATE - The present invention provides an improved process for the preparation of alpha form of imatinib mesylate with (long needle) and α-crystal form (small needle) in a consistent manner and novel alpha crystal forms of imatinib mesylate. The present invention in particular provides a reproducible and efficient process. In particular the present invention provides a efficient process which gives higher yields and consistent results.12-06-2012
20100179163NOL3 IS A PREDICTOR OF PATIENT OUTCOME - The present invention features a method for determining the prognosis for survival of a cancer patient. Methods for measuring the level of NOL3 expression in a cancer cell-containing sample from a patient, and comparing the level of NOL3 expression in the sample to a reference level of NOL3 expression are also included. A higher level of NOL3 relative to the reference level correlates with decreased survival of the patient, and an equivalent or lower level of NOL3 relative to the reference level correlates with increased survival of the patient.07-15-2010
20100087444IMATINIB MESYLATE - There is provided a solid dispersion of imatinib mesylate that includes imatinib mesylate and a pharmaceutically acceptable carrier, wherein said carrier is a cellulose derivative. Also provided is a process for making a solid dispersion and a process for making imatinib.04-08-2010
20120129869PHOSPHORYLATION AND MUTATIONS OF ANAPLASTIC LYMPHOMA KINASE AS A DIAGNOSTIC AND THERAPEUTIC TARGET IN LUNG CANCER - The invention related to the use of high-density loss of heterozygosity (LOH) mapping in lung adenocarcinoma to identify intragenic LOH and driver mutations in different domains of ALK resulted in enhanced tumor growth in xenografted mouse. Mutant (H694R and E1384K) ALKs showed activation of Y1604 ALK and downstream AKT, STAT3 and ERK signaling pathways. Increases of oncogenic signalings resulted in enhanced cell proliferation, colony-formation, cell-migration and tumor-growth in xenografted mouse. Western blot and immunohistochemistry analysis using antibody against phospho-Y1604 ALK on 11 lung cancer cell-lines and 263 cancer specimens indicated ALK activation in all lung cancers regardless of tumor stages. Treating mutant-bearing mice with ALK inhibitor WHI-P 154 resulted in tumor shrinkage, metastasis suppression, and improved survival. Hyperphosphorylation of Y1604 ALK occurred early and continuously throughout tumor progression and could be used as a biomarker to detect lung cancer. Oncogenic ALK point mutations could be treatment targets for lung cancer.05-24-2012
20120172371FLUOROQUINOLONE DERIVATIVES OR SULFONAMIDE MOIETY-CONTAINING COMPOUNDS AS INHIBITORS OF TYROSYL-DNAPHOSPHODIESTERASE (TDP1) - A method for treating cancer in a subject, comprising administering to a subject having cancer a therapeutically effective amount of (i) a fluoroquinolone derivative that inhibits tyrosyl-DNA-phosphodiesterase 1 (Tdp1) activity or (ii) a sulfonamide moiety-containing compound that inhibits tyrosyl-DNA-phosphodiesterase 1 (Tdp1) activity, thereby treating the cancer in the subject. In certain embodiments, the fluoroquinolone derivative or sulfonamide moiety-containing compound is co-administered with a topoisomerase I (TopI) inhibitor.07-05-2012
20120214819Use of N--4-(3-pyridyl)-2-pyridine-amine for the Treatment of Pulmonary Hypertension - The compound of 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-2-yl-amino)phenyl]-benzamide of the formula I08-23-2012
20100048581THIAZOLYL COMPOUNDS USEFUL AS KINASE INHIBITORS - The invention provides compounds of formula I [INSERT CHEMICAL STRUCTURE HERE] (I) and pharmaceutically acceptable salts thereof. The formula I thiazolyl compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's Disease.02-25-2010
20120220600N-Oxide of 3-(2,6-dichloro-3,5-dimethoxy-phenyl) -1--1-methyl-urea - An N-oxide of 3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea, pharmaceutically acceptable salts thereof, compositions including the compound and its pharmaceutically acceptable salts, and methods of preparing the compound and the compositions (such as, for example, by oxidizing 3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea with an oxidizing agent) are described. Further described herein are methods of using the compound and compositions of the present technology, alone and in combination with other suitable agents, to treat various diseases, including but not limited to, those that can be prevented, inhibited or ameliorated by inhibition of kinase activity selected from FGFR1, FGFR2, FGFR3 or FGFR4.08-30-2012
20100190800COMBINATON OF PYRIMIDYLAMINOBENZAMIDE COMPOUNDS AND IMATINIB FOR TREATING OR PREVENTING PROLIFERATIVE DISEASES - The invention provides a pharmaceutical combination comprising: 07-29-2010
20110039860SOLUBLE EPOXIDE HYDROLASE INHIBITORS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT - Compounds of the formula (I) or a pharmaceutically acceptable salt or solvate thereof is disclosed. The compounds are useful for treating diabetes, inflammation, atherosclerosis, hypertension, pain and the like. Pharmaceutical compositions and methods of use are also included.02-17-2011
20110046150USE OF N--4-(3-PYRIDYL)-2-PYRIDINE-AMINE FOR THE TREATMENT OF PULMONARY HYPERTENSION - The present invention pertains to the use of 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide of the formula I02-24-2011
20110224224Method of Optimizing the Treatment of Philadelphia-Positive Leukemia with Imatinib Mesylate - The present invention relates to a method of treating Philadelphia-positive leukemia (Ph+ leukemia), in a particular chronic myeloid leukemia (CML), in a human patient population. More specifically, the present invention pertains to a method of treating Ph+ leukemia, such as CML or Ph+ ALL, in a human patient suffering from Ph+ leukemia comprising the steps of09-15-2011
20120329810IMATINIB MESYLATE ORAL PHARMACEUTICAL COMPOSITION AND PROCESS FOR PREPARATION THEREOF - The invention relates to an oral pharmaceutical composition comprising, greater than 80% of Imatinib, by weight based on the total weight of the composition and the process for preparation thereof.12-27-2012
20120101108Anaplastic 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.04-26-2012
20080255140Squaric Acid Derivatives as Inhibitors of Histone Deacetylase - This invention comprises the novel compounds of formula (I)10-16-2008
20080255138Novel Polymorphic Form Of Imatinib Mesylate And A Process For Its Preparation - This invention discloses a novel stable crystal form of imatinib mesylate, designated by us as α10-16-2008
20080234286STABLE AMORPHOUS IMATINIB MESYLATE AND PRODUCTION PROCESS THEREFOR - Provided herein is a spray dried stable amorphous imatinib mesylate as a free-flowing solid and process for producing the amorphous imatinib mesylate in highly pure form.09-25-2008
20080234285Combination of Organic Compounds - The invention relates to a combination, such as a combined preparation or pharmaceutical composition, respectively, comprising the renin inhibitor of formula (I) or a pharmaceutically acceptable salt thereof and at least one PDGF receptor tyrosine kinase inhibitor.09-25-2008
20120252818HEAT SHOCK PROTEIN BINDING COMPOUNDS, COMPOSITIONS, AND METHODS FOR MAKING AND USING SAME - The present subject matter relates to a compound represented by the general formula (I) or (I′) or a pharmacologically acceptable salt thereof; pharmaceutical compositions containing at least one of these compounds; methods of making at least one of these compounds; methods of using at least one of these compounds for treating and/or preventing various cancers and/or proliferation disorders; methods of using at least one of these compounds for monitoring the effectiveness of an anticancer therapy against various cancers. In one embodiment, the subject matter relates to compounds that bind with a level of specificity to heat shock protein 70 (Hsp70). In another embodiment, the subject matter relates to compounds that bind with a level of specificity to inhibit both heat shock protein 70 (Hsp70) and heat shock cognate protein 70 (Hsc70).10-04-2012
20130096134HETEROCYCLIC COMPOUNDS AND THEIR USES - Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with pi 105 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelodysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.04-18-2013
20120277246Use of N-Phenyl-2-pyrimidineamine Derivatives Against Mast Cell-based Diseases Like Allergic Disorders - Use of the N-phenyl-2-pyrimidine-amine derivatives of formula I,11-01-2012
20090281113METHOD OF OPTIMIZING THE TREATMENT OF PHILADELPHIA-POSITIVE LEUKEMIA WITH ABL TYROSINE KINASE INHIBITORS - The present invention provides a method of treating Philadelphia positive (Ph+) leukemia, such as Philadelphia chromosome positive acute lymphoblastic leukemia (Ph+ ALL) or chronic myeloid leukemia (CML), in a human patient population comprising the steps of 11-12-2009
20100298337Organic Compounds - Compounds of formula (I) in free or salt or solvate form, where T11-25-2010
20130184287INDAZOLE COMPOUNDS AND THEIR USES - The present application relates to therapeutic organic compounds, compositions comprising an effective amount of a therapeutic organic compound; and methods for treating and preventing disease comprising administering and effective amount of a therapeutic organic compound to a subject in need thereof.07-18-2013
20110288102IL-8 BIOMARKER FOR MONITORING CANCER TREATMENT - The present application includes methods for using IL-8 as a biomarker for, e.g., tumor size, for example, during course of treatment with an anti-cancer agent such as an ERK inhibitor.11-24-2011
20110312968METHOD FOR OPTIMIZING THE TREATMENT OF CHRONIC MYELOID LEUKEMIA WITH ABL TYROSINE KINASE INHIBITORS - The present invention relates to a method tor evaluating patterns to help-optimizing the treatment of chronic myeloid leukemia (CML) in a human patient population. Specifically, present invention relates to SHP1 and/or SHP2 as a biomarker for CML patients.12-22-2011
20120088776TREATMENT OF MAMMALIAN DISORDERS MEDIATED BY ALPHA-ANHYDRASE ISOFORMS - The present invention pertains to 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide or a pharmaceutically acceptable salt thereof, or 4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-N-[5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)phenyl] benzamide or a pharmaceutically acceptable salt thereof, for the treatment of disorders mediated by alpha-carbonic anhydrase isoforms selected from intraocular hypertension (glaucoma), epilepsy, Lennox-Gastaut syndrome, altitude sickness, headaches, neurological disorders and obesity.04-12-2012

Patent applications in class Additional six-membered hetero ring consisting of five ring carbons and one ring nitrogen attached directly or indirectly to the 1,3-diazine by nonionic bonding