Entries |
Document | Title | Date |
20080242663 | NOVEL PYRIMIDINE DERIVATIVES 698 - The invention concerns compounds of Formula I, or a pharmaceutically acceptable salt thereof, | 10-02-2008 |
20080287431 | Heterocyclic Compound and Anti-Malignant-Tumor Agent Containing the Same as Active Ingredient - Heterocyclic compounds represented by the formula I and anti-malignant-tumor agents containing the heterocyclic compounds as effective components: | 11-20-2008 |
20090036440 | NOVEL PYRIMIDINE DERIVATIVES - 816 - The invention concerns pyrimidine compounds of Formula I, or a pharmaceutically acceptable salt thereof, | 02-05-2009 |
20090054428 | NOVEL PYRIMIDINE DERIVATIVES 965 - The invention concerns compounds of Formula I, or a pharmaceutically acceptable salt thereof, | 02-26-2009 |
20090215765 | Neuroprotective compounds for treating optic neuropathies - Neuroprotective compounds for treating optic neuropathies and screening methods for identifying neuroprotective compounds. | 08-27-2009 |
20100016298 | Theramutein 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. | 01-21-2010 |
20100063045 | NOVEL PYRIDINECARBOXYLIC ACID (2-AMINOPHENYL) AMIDE DERIVATIVE HAVING UREA STRUCTURE - Objects of the present invention are to study the synthesis of a novel pyridinecarboxylic acid (2-aminophenyl)amide derivative having a novel urea structure and to find a pharmacological effect of the derivative. The invention provides a compound represented by the formula (1) or a salt thereof. In the formula, R | 03-11-2010 |
20100105674 | Chemical Compounds - The present invention relates to dianilinopyrimidine derivatives, compositions and medicaments containing the same, as well as processes for the preparation and use of such compounds, compositions and medicaments. Such dianilinopyrimidine derivatives are useful in the treatment of diseases associated with inappropriate Wee1 kinase activity. | 04-29-2010 |
20100204219 | AROMATIC 1,4-DI-CARBOXYLAMIDES AND THEIR USE - The invention relates to novel compounds of formula (I) wherein X, Y, Z represent independently from one another C or N, n stands for 1, 2, 3, m is 0 or 1, p stands for 0 or an integer from 1 to 6, R | 08-12-2010 |
20100227858 | TRISUBSTITUTED PYRIMIDINE DERIVATIVES FOR THE TREATMENT OF PROLIFERATIVE DISEASES - A compound of formula (I) or a pharamaceutically acceptable salt thereof, processes for their preparation, pharmaceutical compositions containing them and their use intherapy, for example in the treatment of proliferative disease such as cancer and particularly in disease mediated by an mTOR kinase and/or one or more PI3K enzyme. | 09-09-2010 |
20100249126 | PYRIMIDINE DERIVATIVES USED AS PI-3-KINASE INHIBITORS - Phosphatidylinositol (PI) 3-kinase inhibitor compounds (I), their pharmaceutically acceptable salts, and prodrugs thereof; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of proliferative diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, and phospholipid kinases. | 09-30-2010 |
20100267716 | METHODS OF TREATING INFLAMMATIONS AND INFECTIONS WITH PYRIDINIUM SALTS - Compounds of pyridinium salts and methods of their use in medicine, particularly in the prophylaxis and treatment of inflammatory conditions, infectious conditions, as well as immune disorders are disclosed. The present invention also relates to methods of controlling fungi and/or bacteria. | 10-21-2010 |
20100298312 | SUBSTITUTED PYRIMIDINYL-AMINES AS PROTEIN KINASE INHIBITORS - The present invention provides novel substituted pyrimidinyl-amines that are useful as inhibitors of protein kinases, especially c-Jun N-terminal kinases (JNK) and pharmaceutical compositions thereof and methods of using the same for treating conditions responsive to the inhibition of the JNK pathway. | 11-25-2010 |
20110028470 | Detection and Treatment of Schizophrenia - The present invention provides a method for diagnosing schizophrenia, and a schizophrenia diagnostic reagent or device for use in the method. The present invention further provides a therapeutic or ameliorating agent for schizophrenia, which is effective for the treatment or amelioration of schizophrenia. The therapeutic or ameliorating agent for schizophrenia contains a carbonyl scavenger or a carbonyl-modified protein formation inhibitor as an active ingredient. The method for diagnosing schizophrenia according to the present invention includes measuring at least one parameter in a subject, the parameter being selected from the group consisting of: (1) a genetic abnormality of glyoxalase I gene; (2) the expression level or activity of glyoxalase I in a biological sample; (3) the amount of a carbonyl compound or a carbonyl-modified protein that is a protein modified with the carbonyl compound; and (4) the amount of pyridoxal in a biological sample. | 02-03-2011 |
20110136799 | PROLINE DERIVATIVES - Compounds of formula (I): | 06-09-2011 |
20110237579 | INHIBITORS OF HCV NS5A - The invention relates to non-macrocyclic, non-peptidic, substituted heterocyclic compounds useful for inhibiting hepatitis C virus (“HCV”) replication, particularly functions of the non-structural 5A (“NS5A”) protein of HCV | 09-29-2011 |
20110294798 | IL-12 MODULATORY COMPOUNDS - The invention relates to cyclic hydrazone compounds, compositions including the cyclic hydrazone compounds and methods of using and methods of making thereof. The compounds (and compositions) are useful, inter alia, in modulating IL-12 production and processes mediated by IL-12. | 12-01-2011 |
20110312955 | TRIAZINE COMPOUNDS AS PI3 KINASE AND MTOR INHIBITORS - Compounds of formula I | 12-22-2011 |
20120015941 | Antibacterial Amide and Sulfonamide Substituted Heterocyclic Urea Compounds - The present invention provides novel amide and sulfonamide substituted heterocyclic urea compounds having useful antibacterial activity. Use of these compounds as pharmaceutical compositions and method of their production are also provided. | 01-19-2012 |
20120040977 | INHIBITORS OF HCV NS5A - Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C. | 02-16-2012 |
20120077807 | NIACIN MIMETICS, AND METHODS OF USE THEREOF - Disclosed are 6-(morpholinoalkyl)-substituted pyridines, and pharmaceutically acceptable salts and prodrugs thereof, that are active against a range of mammalian therapeutic indications. | 03-29-2012 |
20120077808 | Niacin Mimetics, and Methods of Use Thereof - Disclosed are heterocyclylalkyl-substituted and heteroaralkyl-substituted pyridines, and pharmaceutically acceptable salts and prodrugs thereof, that are active against a range of mammalian therapeutic indications. | 03-29-2012 |
20120202806 | Novel Pyrimidine- And Triazine-Hepcidine Antagonists - The present invention relates to new hepcidin antagonists, pharmaceutical compositions containing them and the use thereof as a drug, in particular for the treatment of iron metabolism disorders such as, in particular, iron deficiency diseases and anaemia, in particular anaemia associated with chronic inflammatory disease (ACD: anaemia of chronic disease and AI: anaemia of inflammation). | 08-09-2012 |
20120252802 | (ALPHA-SUBSTITUTED ARALKYLAMINO AND HETEROARYLALKYLAMINO) PYRIMIDINYL AND 1,3,5-TRIAZINYL BENZIMIDAZOLES, PHARMACEUTICAL COMPOSITIONS THEREOF, AND THEIR USE IN TREATING PROLIFERATIVE DISEASES - Provided herein are (alpha-substituted aralkylamino or heteroarylalkylamino) pyrimidinyl and 1,3,5-triazinyl benzimidazoles, e.g., a compound of Formula I, and their pharmaceutical compositions, preparation, and use as agents or drugs for treating proliferative diseases. | 10-04-2012 |
20120264749 | MORPHOLINE-SPIROCYCLIC PIPERIDINE AMIDES AS MODULATORS OF ION CHANNELS - The invention relates to morpholine spirocyclic piperidine amide compounds useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. | 10-18-2012 |
20130053378 | TETRA-O-SUBSTITUTED BUTANE-BRIDGE MODIFIED NDGA DERIVATIVES, THEIR SYNTHESIS AND PHARMACEUTICAL USE - The present invention relates to nordihydroguaiaretic acid derivative compounds, namely, butane bridge modified nordihydroguaiaretic acid (NDGA) compounds and butane bridge modified tetra-O-substituted NDGA compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, metabolic diseases, such as diabetes and hypertension, or a proliferative disease, such as diverse types of cancers. | 02-28-2013 |
20130143876 | New piperidine derivatives, pharmaceutical compositions and uses thereof - The invention relates to new piperidine derivatives of the formula I | 06-06-2013 |
20130150358 | THERAMUTEIN 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. | 06-13-2013 |
20130225571 | MANUFACTURING PROCESS FOR PYRIMIDINE DERIVATIVES - The invention relates to new crystalline forms of processes for manufacturing a compound of formula 5, | 08-29-2013 |
20130231336 | SUBSTITUTED PYRIMIDINYL-AMINES AS PROTEIN KINASE INHIBITORS - The present invention provides novel substituted pyrimidinyl-amines that are useful as inhibitors of protein kinases, especially c-Jun N-terminal kinases (JNK) and pharmaceutical compositions thereof and methods of using the same for treating conditions responsive to the inhibition of the JNK pathway. | 09-05-2013 |
20130274254 | INHIBITORS OF CYTOCHROME P450 (CYP3A4) - The present application provides for a compound of formula I, and related compounds, or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods that include the administration of such compounds with at least one additional therapeutic agent. | 10-17-2013 |
20140018359 | Niacin Mimetics, and Methods of Use Thereof - Disclosed are 6-(morpholinoalkyl)-substituted pyridines, and pharmaceutically acceptable salts and prodrugs thereof, that are active against a range of mammalian therapeutic indications. | 01-16-2014 |
20140051694 | Aminooxazole Inhibitors of Cyclin Dependent Kinases - Oxazole derivatives are described. The inventive compounds are useful as kinase inhibitors, and may be used in the treatment of cancer, such as prostate cancer, lung cancer, breast cancer, colon cancer, leukemia, CNS cancer, melanoma, ovarian cancer, and renal cancer. | 02-20-2014 |
20140057904 | Combination of (a) a phosphoinositide 3-kinase inhibitor and (b) a modulator of RAS/RAF/MEK pathway - The invention relates to a pharmaceutical combination which comprises (a) a phosphoinositide 3-kinase inhibitor compound and (b) a compound which modulates the Ras/Raf/Mek pathway for the treatment of a proliferative disease, especially a solid tumor disease; a pharmaceutical composition comprising such a combination; the use of such a combination for the preparation of a medicament for the treatment of a proliferative disease; a commercial package or product comprising such a combination as a combined preparation for simultaneous, separate or sequential use; and to a method of treatment of a warm-blooded animal, especially a human. | 02-27-2014 |
20140107114 | Combination Therapy Comprising A CDK4/6 Inhibitor and a P13K Inhibitor for Use in the Treatment of Cancer - A combination of a CDK4/6 inhibitor and a P3Kinase inhibitor for the treatment of cancer. | 04-17-2014 |
20140135322 | NOVEL COMPOUNDS AND THEIR USE IN THERAPY - The present invention relates to novel chemical compounds formula (I) (C) | 05-15-2014 |
20140213583 | PI3K Inhibitor for Use in the Treatment of Bone Cancer or for Preventing Metastatic Dissemination Primary Cancer Cells into the Bone - Provided herein are methods for the treatment of bone cancer and prevention of the metastatic spread of cancer. | 07-31-2014 |
20140221366 | Substituted Azaheterocycles for the Treatment of Cancer - The invention provides novel substituted azaheterocyclic compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer. | 08-07-2014 |
20140235630 | COMPOSITIONS AND METHODS FOR THE TREATMENT OF PROLIFERATIVE DISEASES - The present invention relates to pharmaceutical compositions that contain PI3K inhibitors (e.g., PBKa-specific inhibitors) and PARP inhibitors. The invention also provides methods for the treatment of proliferative diseases such as cancer (e.g., breast cancer) by administering the composition(s) to a subject. | 08-21-2014 |
20140288067 | CARM1 INHIBITORS AND USES THEREOF - Provided herein are compounds of Formula (I): | 09-25-2014 |
20140309221 | METHOD OF INHIBITING HAMARTOMA TUMOR CELLS - Dimorpholinopyrimidines are useful for inhibiting growth or proliferation of hamartoma tumor cells. Because the Dimorpholinopyrimidines inhibit the growth and proliferation of hamartoma tumor cells they are also useful in treating PTEN hamartoma tumor syndromes. The therapeutic and prophylactic treatments provided by this invention are practiced by administering to a patient in need thereof an amount of a compound of dimorpholinopyrimidine derivative that is effective to inhibit growth or proliferation of the hamartoma tumor cells. | 10-16-2014 |
20140329812 | ARYL TRIAZOLE COMPOUNDS WITH ANTITUMOURAL ACTIVITY - The present invention relates to aryl triazole derivatives of Formula I having antitumoural activity through, as one possible biological target, the molecular chaperone heat shock protein 90 (Hsp90) inhibition. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an inhibition of Hsp90 is responsive, and the pharmaceutical composition containing such compounds. | 11-06-2014 |
20150072980 | Substituted 2,3-dihydro-1H-inden-1-one Retinoic acid-related orphan nuclear receptor Antagonists for Treating Multiple Sclerosis - The present invention is directed to compounds, their synthesis, and their use as antagonists, inverse agonists, modulators and or inhibitors of the Retinoic acid-related orphan nuclear receptor γt (RORγt)/RORγ. The compounds of the present invention are useful for modulating RORγt)/RORγ activity and for treating diseases or conditions mediated by RORγt)/RORγ such as for example, disease states associated with immunopathology of human autoimmune diseases such as Multiple Sclerosis (MS), Rheumatoid Arthritis (RA), Inflammatory Colitis, Psoriasis, COPD, Pain, Obesity, Diabetes, Dyslipidemia, Osteoporosis, Asthma, Neurodegenerative diseases and Cancer. | 03-12-2015 |
20150094303 | Niacin Mimetics, and Methods of Use Thereof - Disclosed are heterocyclylalkyl-substituted and heteroaralkyl-substituted pyridines, and pharmaceutically acceptable salts and prodrugs thereof, that are active against a range of mammalian therapeutic indications. | 04-02-2015 |
20150133441 | THERAMUTEIN 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. | 05-14-2015 |
20150315144 | ARYL DIHYDROPYRIDINONES AND PIPERIDINONE MGAT2 INHIBITORS - The present invention provides compounds of Formula (I): | 11-05-2015 |
20150352076 | MOLECULARLY TARGETED COMBINATION DRUG FOR TUMOR TREATMENT AND PREVENTION - To provide means for treating and preventing a wide variety of cancers and tumors, including cancer in which there is PI3K/Akt pathway activation or p53 deactivation, or tumors for which chemotherapy, radiation therapy, hormone therapy, and other such conventional treatment methods have low effectiveness, different molecularly targeted drugs such as OBP-801 and PI3K inhibitor—preferably LY294002, BKM120, GDC-0941, BEZ235, BYL719, or CH5132799—are used in combination. This makes it possible to simultaneously obtain a plurality of different marked pharmaceutical benefits which are synergistic, not being obtainable through use of a formulation with either of the respective molecularly targeted drugs alone, such as caspase pathway activation, enhanced expression of Bim, increased accumulation of intracellular reactive oxygen species, and suppressed expression of survivin and XIAP protein, and makes it possible to provide new and clinically effective tumor treatment/prevention strategies. | 12-10-2015 |
20150353524 | PYRIDINE COMPOUNDS USED AS PI3 KINASE INHIBITORS - The present invention is directed to novel pyridines, their derivatives, pharmaceutically acceptable salts, solvates and hydrates thereof. The present invention discloses compounds of Formulas I and II. The compounds and compositions of the present invention have protein kinases inhibitory activities and are expected to be useful for the treatment of protein kinases mediated diseases and conditions. | 12-10-2015 |
20160002205 | SUBSTITUTED 2-AMINOPYRIDINE PROTEIN KINASE INHIBITOR - Disclosed are a | 01-07-2016 |
20160015643 | FORMULATIONS OF ORGANIC COMPOUNDS - The present invention relates to solid pharmaceutical compositions comprising the phosphatidylinositol 3-kinase inhibitor compound 4-(trifluoromethyl)-5-(2,6-dimorpholinopyrimidin-4-yl)pyridin-2-amine or a pharmaceutically acceptable salt thereof, sodium stearyl fumarate, and optionally at least one additional pharmaceutically acceptable carrier. The present invention also relates to the processes for their preparation and to their use as medicaments for the treatment of cancer. | 01-21-2016 |
20160030441 | NIACIN MIMETICS, AND METHODS OF USE THEREOF - Disclosed are 6-(morpholinoalkyl)-substituted pyridines, and pharmaceutically acceptable salts and prodrugs thereof, that are active against a range of mammalian therapeutic indications. | 02-04-2016 |
20160082012 | Combination of a PI3 Kinase Inhibitor with Pacitaxel for Use in the Treatment or Prevention of a Cancer of the Head and Neck - A pharmaceutical combination comprising (a) a phosphatidylinositol-3-kinase (PI3K) inhibitor compound of formula (I), as defined herein, or a pharmaceutically acceptable salt thereof and (b) paclitaxel or a pharmaceutically acceptable salt thereof for simultaneous, separate or sequential use, for the treatment of a cancer of the head and neck; a pharmaceutical composition comprising said combination; the use of said combination for the preparation of a medicament for the treatment of a cancer of the head and neck; a method of treating or preventing a cancer of the head and neck comprising administering a jointly therapeutically effective amount of such a combination to a subject in need thereof; and a commercial package thereof. | 03-24-2016 |
20160120871 | PHARMACEUTICAL COMBINATIONS OF A PI3K INHIBITOR AND A MICROTUBULE DESTABILIZING AGENT - The present invention relates to a combination comprising (a) a phosphatidylinositol 3-kinase inhibitor selected from 5-(2,6-di-morpholin-4-yl-pyrimidin-4-yl)-4-trifluoromethyl-pyridin-2-ylamine, (S)-Pyrrolidine-1,2-dicarboxylic acid 2-amide 1-({4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethyl-ethyl)-pyridin-4-yl]-thiazol-2-yl}-amide) or a pharmaceutically acceptable salts thereof, and (b) a microtubule destabilizing agent for simultaneous, separate or sequential use for the treatment of a tumor disease; a pharmaceutical composition comprising such combination; a method of treating a subject having a tumor disease comprising administration of said combination to a subject in need thereof; use of such combination for preparation of a medicament for the treatment of a tumor disease; and a commercial package thereto. | 05-05-2016 |
20160122361 | PYRIMIDINE COMPOUNDS AS KINASE INHIBITORS - This disclosure relates to compounds, methods for their preparation, pharmaceutical compositions including these compounds and methods for the treatment of cellular proliferative disorders, including, but not limited to, cancer. | 05-05-2016 |
20160129003 | Pharmaceutical Combinations - A pharmaceutical combination comprising: (a) a phosphatidylinositol-3-kinase inhibitor selected from 2-methyl-2-[4-(3-methyl-2-oxo-8-quinolin-3-yl-2,3-dihydro-imidazo[4,5-c]quinolin-1-yl)-phenyl]-propionitrile, 5-(2,6-di-morpholin-4-yl-pyrimidin-4-yl)-4-trifluoromethyl-pyridin-2-ylamine, (S)-Pyrrolidine-1,2-dicarboxylic acid 2-amide 1-({4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethyl-ethyl)-pyridin-4-yl]-thiazol-2-yl}-amide) or any pharmaceutically acceptable salt thereof, and (b) an anaplastic lymphoma kinase inhibitor, particularly for use in the treatment or prevention of a proliferative disease; uses of such a combination in the treatment or prevention of proliferative diseases; to pharmaceutical compositions of the combination of said therapeutic agents and methods of treating a proliferative disease in a subject comprising administering to said subject a therapeutically effective amount of such a combination. | 05-12-2016 |
20160136171 | Combination Therapy Comprising A CDK4/6 Inhibitor and a PI3K Inhibitor for Use in the Treatment of Cancer - A combination of a CDK4/6 inhibitor and a P3Kinase inhibitor for the treatment of cancer. | 05-19-2016 |
20170231997 | Tablet Formulation Of 2-Fluoro-N-Methyl-4-[ 7- ( Quinolin-6-Ylmethyl) Imidazo [1,2-B] [1,2,4] Triazin-2-YL] Benzamide | 08-17-2017 |