| Class / Patent application number | Description | Number of patent applications / Date published |
|---|
| 514264110 | Nitrogen bonded directly to ring carbon of the 1,3-diazine ring of the bicyclo ring system | 50 |
| 20080207651 | Heterocyclic compounds useful in treating diseases and conditions - The present invention relates to compounds of formula (I) | 08-28-2008 |
| 20080207652 | Novel inhibitors of folic acid-dependent enzymes - The invention relates to compounds of the formula I, or pharmaceutically acceptable salts thereof: | 08-28-2008 |
| 20080255162 | Pyrrolyl Substituted Pyrido[2,3-D]Pyrimidin-7-Ones and Derivatives Thereof as Therapeutic Agents - The present invention provides pyrimidines of Formula I: | 10-16-2008 |
| 20080255163 | Use of Modified Pyrimidine Compounds to Promote Stem Cell Migration and Proliferation - This invention provides cells and methods for stimulating proliferation and migration of endogenous and exogenous mammalian stem cells in vivo and in vitro. The invention provides reagents and methods for efficiently proliferating mammalian stem cells in an animal in need thereof and producing stem cells that can be re-introduced into an animal in need thereof to alleviate neurological and corporal disorders. | 10-16-2008 |
| 20090036472 | AZABICYCLO DERIVATIVES AS ANTI-INFLAMMATORY AGENTS - The present invention relates to novel azabicyclo derivatives of Formula (I) as anti-inflammatory agents which are useful for inhibition and prevention of inflammation and associated pathologies including inflammatory and autoimmune diseases such as sepsis, rheumatoid arthritis, inflammatory bowel disease, type-1 diabetes, asthma, chronic obstructive pulmonary disorder, organ transplant rejection and psoriasis. | 02-05-2009 |
| 20090048277 | PYRIDOPYRIMIDONE DERIVATIVES, PREPARATION THEREOF, THERAPEUTIC USE THEREOF - The disclosure relates to pyrido[2,3-d]pyrimidone compounds, to the preparation thereof and to the therapeutic use thereof, wherein said compounds are of general formula (I): | 02-19-2009 |
| 20090062316 | DEUTERIUM-ENRICHED PELITREXOL - The present application describes deuterium-enriched pelitrexol, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 03-05-2009 |
| 20090118310 | Activated Cdc42-associated kinase (ACK) as a therapeutic target for Ras-induced cancer - Methods for preventing or treating Ras-induced cancer in a patient by (a) detecting v-Ha-Ras-transformed cells in a patient and (b) administering to the patient a therapeutically effective amount of a chemotherapeutic composition comprising an effective amount of an inhibitor for activated Cdc42-associated kinase (ACK) kinase. | 05-07-2009 |
| 20090118311 | DHFR Enzyme Inhibitors - Compounds of formula (I) or (II) are dihydrofolate reductase inhibitors, useful for the treatment of, for example, cell proliferative diseases: | 05-07-2009 |
| 20090131460 | PYRIDO[2,3-D]PYRIMIDINES USEFUL AS HCV INHIBITORS, AND METHODS FOR THE PREPARATION THEREOF - The present invention relates to the use of pyrido[2,3-d]pyrimidines as inhibitors of HCV replication as well as their use in pharmaceutical compositions aimed to treat or combat HCV infections. In addition, the present invention relates to pyrido-[2,3-d]pyrimidines compounds per se and their use as medicines. The present invention also concerns processes for the preparation of such compounds, pharmaceutical compositions comprising them, and combinations of said compounds with other anti-HCV agents. | 05-21-2009 |
| 20090176811 | Substituted 5,6,7,8-Tetrahydro-pyrido[4,3-d]pyrimidine-2-yl Compounds and 5,6,7,8-Tetrahydro-quinazoline-2-yl Compounds - Substituted 5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-2-yl and 5,6,7,8-tetrahydro-quinazolin-2-yl compounds, corresponding to formula I | 07-09-2009 |
| 20090186910 | COMPOSITIONS AND METHODS FOR REDUCING CELLULAR FAT AND FOR PREDICTING CARDIAC TOXICITY AND UPON TREATMENT WITH TYROSINE KINASE INHIBITORS - Methods are disclosed for determining whether organ toxicity, particularly cardiotoxicity, will occur in a patient selected for treatment with various kinase inhibitors, such as tyrosine kinase inhibitors, more particularly erbB inhibitors such as Herceptin. In addition, methods are disclosed for determining whether a potential drug is likely to produce a cardiotoxic effect. The methods involve analyzing lipid levels or the expression fatty acid oxidation enzymes, pAMP activated protein kinase, glucose uptake, to determine whether a fatty acid oxidation disorder is present. The identification of a fatty acid oxidation disorder can be used as a predictor of toxicity, especially cardiac toxicity, and as an indication that organ function should be carefully monitored if a drug such as a tyrosine kinase inhibitor is administered. Methods are also disclosed for protecting organs from metabolic stress and for the treatment of cells, such as adipocytes, to reduce their lipid content. | 07-23-2009 |
| 20090270430 | Pyridopyrimidinone Inhibitors of Pl3Kalpha - The invention is directed to Compounds of Formula I: | 10-29-2009 |
| 20090312349 | ANTI-INFLAMMATORY MEDICAMENTS - Novel compounds and methods of using those compounds for the treatment of inflammatory conditions, hyperproliferative diseases, cancer, and diseases characterized by hyper-vascularization are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein, abl kinase protein, bcr-abl kinase protein, braf kinase protein, VEGFR kinase protein, or PDGFR kinase protein comprises the step of contacting said kinase protein with the novel compounds. | 12-17-2009 |
| 20100041680 | PIPERIDINE DERIVATIVES - Compounds of formula I: I selectively inhibit production of Ab(1-42) and hence find use in treatment of Alzheimer's disease and other conditions associated with deposition of A(b) in the brain. | 02-18-2010 |
| 20100087456 | PYRIDOPYRIMIDINONE INHIBITORS OF PI3K-ALPHA and mTOR - The invention is directed to Compounds of Formula I: | 04-08-2010 |
| 20100099691 | PYRIMIDINYL PYRIDONE INHIBITORS OF JNK - This application discloses novel pyrimidinyl pyridone derivatives according to Formula I, | 04-22-2010 |
| 20100113487 | PYRIMIDINONE DERIVATIVES AND METHODS OF USE THEREOF - The present invention relates to Pyrimidinone Derivatives, compositions comprising a Pyrimidinone Derivative, and methods of using the Pyrimidinone Derivatives for treating or preventing obesity, diabetes, a metabolic disease, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient. | 05-06-2010 |
| 20100130518 | MAPK/ERK KINASE INHIBITORS - Compounds of the following formula are provided for use with MEK (I): wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds. | 05-27-2010 |
| 20100160355 | Anti-Viral Compounds - Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection. | 06-24-2010 |
| 20100179174 | SUBSTITUTED AZAQUINAZOLINES HAVING AN ANTIVIRAL ACTION - This invention relates to substituted azaquinazolines, to a process for their preparation, to pharmaceutical compositions containing them, and to their use for the treatment and/or prophylaxis of diseases, especially for use as antiviral agents, in particular against cytomegaloviruses. | 07-15-2010 |
| 20100317676 | Fused heterocyclic compounds, and compositions and uses thereof - Fused heterocyclic compounds are disclosed that have formula 1: | 12-16-2010 |
| 20110009432 | PYRID-2YL FUSED HETEROCYCLIC COMPOUNDS, AND COMPOSITIONS AND USES THEREOF - Fused heterocyclic compounds are provided according to formula 1a or 1b: | 01-13-2011 |
| 20110077256 | MEDIATORS OF HEDGEHOG SIGNALING PATHWAYS, COMPOSITIONS AND USES RELATED THERETO - The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from | 03-31-2011 |
| 20110136838 | CHEMICAL COMPOUNDS - The invention is directed to pyrido[4,3-d]pyrimidin-5(6H)-one derivatives. Specifically, the invention is directed to compounds according to Formula I: | 06-09-2011 |
| 20110172254 | FOLATE RECEPTOR BINDING CONJUGATES OF ANTIFOLATES - Conjugates of antifolates, releasable linkers, and drugs, and pharmaceutical compositions containing them are described. The conjugates are useful for treating diseases arising from pathogenic cell populations. Methods for treating such diseases are also described. | 07-14-2011 |
| 20110237608 | Pyridopyrimidinone Inhibitors of PI3Kalpha - The invention is directed to Compounds of Formula I: | 09-29-2011 |
| 20110257207 | RAF INHIBITORS - The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are inhibitors or kinases such as Raf, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer. | 10-20-2011 |
| 20120101115 | Compounds For Inducing Cellular Apoptosis - The present invention provides isoquinoline, tetrahydroisoquinoline and tetrahydropyridopyrimidine compounds that induce cell death by apoptosis and uses of the compounds in medicine, especially their use for treating cancer and other diseases. | 04-26-2012 |
| 20120136012 | AMINO TETRAHYDRO-PYRIDOPYRIMIDINE PDE10 INHIBITORS - The present invention is directed to amino tetrahydro-pyridopyrimidine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction. | 05-31-2012 |
| 20120202831 | Pharmaceutical Formulation - The invention relates to a pharmaceutical formulation including, as an active principle, the compound of formula (I) | 08-09-2012 |
| 20120202832 | KINASE INHIBITORS, PRODRUG FORMS THEREOF AND THEIR USE IN THERAPY - The invention provides kinase inhibitors of Formula I: | 08-09-2012 |
| 20120258975 | Potent Small Molecule Inhibitors of Autophagy, and Methods of Use Thereof - Certain aspects of the invention relates to small molecule autophagy inhibitors of the formula (I), and their use for treatment and prevention of cancers and acute pancreatitis. As disclosed herein, a small molecule inhibitor of autophagy was been identified from an image-based screen in a known bioactive library. It was found that this autophagy inhibitor functions by promoting the degradation of type III PI3 kinase complex which is required for initiating autophagy. Medicinal chemistry studies led to small molecular autophagy inhibitors with improved potency and selectivity. (I) | 10-11-2012 |
| 20120309775 | 4-METHYLPYRIDOPYRIMIDINONE COMPOUNDS - The present invention is directed to novel 4-methylpyridopyrimidinone compounds of Formula (I), | 12-06-2012 |
| 20130045983 | HSP90 INHIBITORS FOR THERAPEUTIC TREATMENT - The use of a Hsp90 inhibitor for the treatment of cancer of the bladder, the colon, the liver, the lung, the breast, the vagina, the ovaries, the pancreas, the kidney, the stomach, the gastrointestinal tract, the prostate, the head and neck, the peritoneal cavity, the thyroid, the bone, the brain, the central nervous system and/or the blood and/or for the treatment of myelodysplastic syndrome, systemic mastocytosis, von Hippel-Lindau syndrome, multicentric Castleman disease and/or psoriasis. | 02-21-2013 |
| 20130172371 | Methods of Treating Cancer Using Pyridopyrimidinone Inhibitors of PI3K and mTOR in Combination with Autophagy Inhibitors - The invention provides compounds of Formula I: | 07-04-2013 |
| 20130172372 | RING-FUSED 4-AMINOPYRIMIDINES AND USE THEREOF AS STIMULATORS OF SOLUABLE GUANYLATE CYCLASES - The present application relates to novel fused 4-aminopyrimidines, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for the treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of cardiovascular disorders. | 07-04-2013 |
| 20130252977 | Raf Inhibitor Compounds - The present invention provides a pyrido[2,3-d]pyrimidine compound, or a pharmaceutically acceptable salt thereof, that inhibits Raf and, therefore, may be useful in treating cancer. | 09-26-2013 |
| 20130274274 | SUBSTITUTED PYRIDOPYRIMIDINE COMPOUNDS AND THEIR USE AS FLT3 INHIBITORS - Compounds of Formula (I) and methods for inhibiting kinases, including spleen tyrosine kinases, are disclosed. Also disclosed are methods for treating a kinase-mediated disease or condition by administering to a subject a therapeutically effective amount of the compound of Formula (I). | 10-17-2013 |
| 20140038991 | Protein Kinase Inhibitors - The present invention is directed to compounds of the Formula I | 02-06-2014 |
| 20140200231 | Bicyclic Pyrimidine Compounds - The present invention provides compounds of the Formula I: | 07-17-2014 |
| 20140213601 | ANTI-VIRAL COMPOUNDS - Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection. | 07-31-2014 |
| 20140296265 | Method of Treating Lymphoma Using Pyridopyrimidinone Inhibitors of PI3K/mTOR - The invention provides a method for treating cancers including hematologic malignancies comprising administering a compound of formula I: | 10-02-2014 |
| 20140378481 | INHIBITORS OF THE FIBROBLAST GROWTH FACTOR RECEPTOR - Described herein are inhibitors of FGFR, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions to inhibit the activity of tyrosine kinases. | 12-25-2014 |
| 20150126534 | ENZYME AND RECEPTOR MODULATION - Covalent conjugation of an alpha amino acid ester to a modulator of the activity of a target intracellular enzyme or receptor, wherein the ester group of the conjugate is hydrolysable by one or more intracellular carboxylesterase enzymes to the corresponding acid, leads to accumulation of the carboxylic acid hydrolysis product in the cell and enables improved or more prolonged enzyme or receptor modulation relative to the unconjugated modulator. | 05-07-2015 |
| 20160031877 | KINASE INHIBITORS, PRODRUG FORMS THEREOF AND THEIR USE IN THERAPY - The invention provides kinase inhibitors of Formula I: | 02-04-2016 |
| 20160096832 | KINASE INHIBITORS - The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation. | 04-07-2016 |
| 20160102088 | PIPERIDYLPYRIMIDINE DERIVATIVES AS MODULATORS OF PROTEIN KINASE INHIBITORS AND OF VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR 2 - This invention is directed to a compound of Formula I | 04-14-2016 |
| 20160251347 | FUSED PYRIMIDINE COMPOUNDS | 09-01-2016 |
| 20160375025 | HUMAN PAPILLOMA VIRUS AS PREDICTOR OF CANCER PROGNOSIS - Methods of treating a head and neck cancer are disclosed. | 12-29-2016 |
