Class / Patent application number | Description | Number of patent applications / Date published |
514217060 | The additional hetero ring is a 1,3 diazine (including hydrogenated) | 74 |
20080293697 | Pyrazolo[4,3-D]Pyrimidines - This invention relates to compounds of formula (I). | 11-27-2008 |
20090012059 | DIPEPTIDYL PEPTIDASE INHIBITORS - Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound comprising: | 01-08-2009 |
20090042863 | Therapeutic Agent for Diabetes - The present invention relates to an agent for pancreas protection which contains a combination of a blood glucose lowering drug that does not stimulate insulin secretion and a compound represented by the formula (I) | 02-12-2009 |
20090069298 | Pyrazolo[1,5-A]Pyrimidine Compounds - The present invention relates to a novel pyrazolo[1,5-a]pyrimidine compound of the formula [I]: | 03-12-2009 |
20090082336 | mGluR1 Antagonists as Therapeutic Agents - In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J | 03-26-2009 |
20090118261 | QUINAZOLINONE DERIVATIVES AND THEIR USE AS B-RAF INHIBITORS - The invention relates to chemical compounds of the formula (I): or pharmaceutically acceptable salts thereof, which possess B Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man. | 05-07-2009 |
20090124599 | Fungicidal Mixtures - Fungicidal mixtures comprising, as active components
| 05-14-2009 |
20090124600 | N-Alkyl-Azacycloalkyl NMDA/NR2B Antagonists - Compounds represented by Formula (I): and/or pharmaceutically acceptable salts, individual enantiomers and stereoisomers thereof, are effective as NMDA/NR2B antagonists useful for treating conditions such as pain, Parkinson's disease, Alzheimer's disease, epilepsy, depression, anxiety, ischemic brain injury including stroke. | 05-14-2009 |
20090176763 | Azaindoles useful as inhibitors of JAK and other protein kinases - The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. | 07-09-2009 |
20090186875 | COMPOUNDS FOR THE TREATMENT OF INFLAMMATORY DISEASES - Dihydrothienopyrimidines of formula 1 | 07-23-2009 |
20090203673 | 4-HETEROCYCLOALKYLPYRI(MI)DINES, PROCESS FOR THE PREPARATION THEREOF AND THEIR USE AS MEDICAMENTS - The present invention encompasses compounds of general Formula (I) wherein X and R | 08-13-2009 |
20090203674 | PYRIMIDINE COMPOUND AND PESTS CONTROLLING COMPOSITION CONTAINING THE SAME - The present invention relates to a pyrimidine compound of the formula (I): | 08-13-2009 |
20090209518 | PYRIMIDINE COMPOUND AND PESTS CONTROLLING COMPOSITION CONTAINING THE SAME - The present invention relates to a pyrimidine compound of the formula (I): | 08-20-2009 |
20090209519 | PYRIMIDINE COMPOUND AND PESTS CONTROLLING COMPOSITION CONTAINING THE SAME - The present invention relates to a pyrimidine compound of the formula (I): | 08-20-2009 |
20090221555 | FUSED BICYCLIC DERIVATIVES OF 2,4-DIAMINOPYRIMIDINE AS ALK AND c-MET INHIBITORS - The present invention provides a compound of formula I or II or a pharmaceutically acceptable salt form thereof, wherein R | 09-03-2009 |
20090318424 | NOVEL COMPOUNDS - Novel substituted 1,5,7-trisubstituted-3,4-dihydro-pyrimido[4,5-d]pyrimidin-2-(1H)-one compounds and compositions, and their use in therapy as CSBP/RK/p38 kinase inhibitors. | 12-24-2009 |
20090325933 | Pyrimidinone Derivatives and Their Use as a Drug - The present application relates to new pyrimidinone derivatives. These products have a good affinity for certain sub-types of cannabinoid receptors, especially the CB2 receptors. They are particularly attractive for treating pathological conditions and diseases in which one or more cannabinoid receptors are involved. The invention also relates to pharmaceutical compositions containing said products and their use for the preparation of a drug. | 12-31-2009 |
20100016289 | Compounds Useful as Antagonists of CCR2 - The present invention provides compounds of general formula I: (I) or a pharmaceutically acceptable salt thereof, wherein X, n, Y, and R | 01-21-2010 |
20100022516 | 4,5-Disubstituted-2-aryl pyrimidines - 4,5-disubstituted-2-arypyrimidines of Formula I and Formula II are provided: | 01-28-2010 |
20100048539 | COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to beat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of c-kit, PDGFRα and PDGFRβ kinases. Formula (I). | 02-25-2010 |
20100093702 | METHYLENE AMINES OF THIENO[2,3-d]PYRIMIDINE AND THEIR USE AS ADENOSINE A2a RECEPTOR ANTAGONISTS - This invention relates to a novel thieno[2,3-d]pyrimidine, A, and its therapeutic and prophylactic uses, wherein R | 04-15-2010 |
20100144705 | EGFR KINASE KNOCKDOWN VIA ELECTROPHILICALLY ENHANCED INHIBITORS - Provided herein are electrophilically enhanced kinase inhibitors. Also provided herein are methods of making and utilizing the same. | 06-10-2010 |
20100144706 | Compounds - The present invention encompasses compounds of general formula (1) wherein R | 06-10-2010 |
20100152167 | PYRIMIDINE DERIVATIVES - The present invention relates to trisubstituted pyrimidines of formula (I) | 06-17-2010 |
20100184746 | LINCOSAMIDE DERIVATIVES AND ANTIMICROBIAL AGENTS COMPRISING THE SAME AS ACTIVE INGREDIENT - An objective of the present invention is to provide compounds of formula (I) or their pharmacologically acceptable salts or solvates wherein A represents aryl while R | 07-22-2010 |
20100227853 | INHIBITORS OF CYCLIC AMP PHOSPHODIESTERASES - Recombinant fission yeast cells and methods of using them are described, which provide for identification of chemical and biological inhibitors or activators of a target exogenous phosphodiesterase (PDE). The invention provides, in some aspects, compounds that inhibit cAMP PDE activity and compositions that include such compounds. The invention, in part, also includes methods of using cAMP PDE-inhibiting compounds in the treatment of cAMP PDE-associated diseases and/or disorders. | 09-09-2010 |
20100234354 | PYRIDAZINONE DERIVATIVES - Compounds of the formula (I), in which R | 09-16-2010 |
20100298297 | Tetrahydropyridothienopyrimidine Compounds and Methods of Use Thereof - This invention relates to compounds of Formula (I), | 11-25-2010 |
20100298298 | QUINAZOLINEDIONE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USES THEREOF - The invention relates to quinazolinedione derivatives, processes for the preparation thereof and their therapeutic applications. | 11-25-2010 |
20110098279 | USE OF TRIAZOLOPYRIMIDINE DERIVATIVES AS MICROBICIDES - Use of compounds of the formula (I) | 04-28-2011 |
20110098280 | 2,4-PYRIMIDINEDIAMINES USEFUL IN THE TREATMENT OF NEOPLASTIC DISEASES, INFLAMMATORY AND IMMUNE SYSTEM DISORDERS - Novel pyrimidine derivatives of formula I | 04-28-2011 |
20110144095 | Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions - The present invention relates to substituted xanthines of general formula | 06-16-2011 |
20110195956 | Heterocyclic Kinase Inhibitors - New compounds, compositions and methods of inhibition of Provirus Integration of Maloney Kinase (PIM kinase) activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one PIM kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer. | 08-11-2011 |
20110201599 | CDK Modulators - A compound according to Formula I: or a pharmaceutically-acceptable salt thereof, wherein R1, R3, A, B and D are as defined in the specification; pharmaceutical compositions thereof, and methods of use thereof. | 08-18-2011 |
20110218189 | PYRROLO[2,3-d]PYRIMIDIN-2-YL-AMINE DERIVATIVES AS PKC-THETA INHIBITORS - The present invention relates to a pyrrolo[2,3-d]pyrimidin-2-yl-amine derivative according to formula (I) wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising one or more of said pyrrolo[2,3-d]pyrimidine-2-ylamine derivatives and to their use in therapy, for instance in the treatment of PKCθ mediated disorders. | 09-08-2011 |
20110263570 | PYRIMIDINE DERIVATIVES AS GPCR MODULATORS FOR USE IN THE TREATMENT OF OBESITY AND DIABETES - The present invention relates to Pyriraidine Derivatives of formula (I), compositions comprising a Pyrimidine Derivative, and methods of using the Pyrimidine Derivatives for treating or preventing obesity, diabetes, a diabetic complication, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G protein-coupled receptor (GPCR) in a patient. | 10-27-2011 |
20110306602 | 4, 6-DISUBSTITUTED AMINOPYRIMIDINE DERIVATIVES AS INHIBITORS OF PROTEIN KINASES - The present invention relates to inhibitors of general Formula (I) of cyclin-dependent kinases and therapeutic applications thereof. Furthermore, the invention relates to compounds for preventing and/or treating any type of pain, inflammatory disorders, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases and neurodegenerative diseases. | 12-15-2011 |
20120004210 | SUBSTITUTED QUINAZOLINE COMPOUNDS - The invention is directed to certain novel compounds, methods for producing them and methods for treating or ameliorating a kinase-mediated disorder. More particularly, this invention is directed to substituted quinazoline compounds useful as selective kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase-mediated disorder, In particular, the methods relate to treating or ameliorating a kinase-mediated disorder including cardiovascular diseases, diabetes, diabetes-associated disorders, inflammatory diseases, immunological disorders, cancer and diseases of the eye such as retinopathies or macular degeneration or other vitreoretinal diseases, and the like. | 01-05-2012 |
20120022048 | Anti-proliferative substituted pyrazolo[3,4-d]pyrimidines derivatives (SPP) to inhibit immune activation, virus replication and tumor growth - A family of pyrazolo[3,4-d]pyrimidine derivatives (SPPs) with different substituents on the pyrimidine and pyrazolo rings have been characterized with a panel of tests demonstrating their effects in cell proliferation, toxicity, apoptosis and inhibition of virus replication. We have identified compounds and molecular structures suitable for the treatment of viral infection because they have antiviral activity, anti-proliferative activity or, preferably, both so that, as a single molecule, they both limit T cell hyperactivation and inhibit virus replication. These compounds are not toxic at effective concentrations and are poorly apoptotic. Other nontoxic compounds within this family with excellent anti-proliferative and apoptotic features are potentially effective as anti-cancer drugs. | 01-26-2012 |
20120028962 | FUSED HETEROCYCLIC RING COMPOUND - A compound represented by the following formula or a salt thereof, which has an GPR119 agonist action, is useful for the prophylaxis or treatment of diabetes, obesity and the like, and shows superior efficacy: | 02-02-2012 |
20120035158 | Xanthine Derivatives, the Preparation Thereof and Their Use as Pharmaceutical Compositions - The present invention relates to substituted xanthines of general formula | 02-09-2012 |
20120088750 | ANTIBACTERIAL COMPOUNDS - The present invention provides a compound of the following formula and salts thereof: | 04-12-2012 |
20120129840 | NOVEL VIRAL REPLICATION INHIBITORS - The present invention relates to a series of novel compounds having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to methods for the preparation of such compounds, as well as to novel intermediates useful in one or more steps of such syntheses. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutical amount of such compounds, optionally combined with one or more other drugs having antiviral activity. | 05-24-2012 |
20120142673 | Pyrido-, Pyrazo- and Pyrimido-Pyrimidine Derivatives as mTOR Inhibitors - There is provided a compound of formula I: | 06-07-2012 |
20120178742 | METABOTROPIC GLUTAMATE RECEPTOR MODULATORS - The invention relates to heterocyclic derivatives as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are mGluR5 modulators and are therefore useful for the control and prevention of acute and/or chronic neurological disorders. | 07-12-2012 |
20120178743 | NOVEL ADENINE COMPOUND AND USE THEREOF - An antiallergic agent for topical administration containing an adenine compound of general formula (1): | 07-12-2012 |
20120202792 | Antimicrobial Compounds and Methods of Making and Using the Same - The present invention relates generally to the field of antimicrobial compounds and to methods of making and using them. These compounds are useful for treating, preventing, and/or reducing the risk of microbial infections in humans and animals. | 08-09-2012 |
20120208797 | PYRIMIDONE DERIVATIVES - A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: | 08-16-2012 |
20120252790 | Amino-Derivatives As Novel Inhibitors Of Histone Deacetylase - This invention comprises the novel compounds of formula (I) | 10-04-2012 |
20120252791 | Heterocyclic GTP Cyclohydrolase 1 Inhibitors For the Treatment of Pain - The present invention relates to the field of small molecule heterocyclic inhibitors of GTP cyclohydrolase (GCH-I), or a tautomer, prodrug, or pharmaceutically acceptable salt thereof. The invention also features pharmaceutical compositions of the compounds and the medical use of these compounds for the treatment or prevention of pain (e.g., inflammatory pain, nociceptive pain, functional pain, or neuropathic pain). | 10-04-2012 |
20120258958 | AZAINDOLES USEFUL AS INHIBITORS OF JAK AND OTHER PROTEIN KINASES - The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. | 10-11-2012 |
20120258959 | PYRIDONE GPR119 G PROTEIN-COUPLED RECEPTOR AGONISTS - Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure Formula I or Formula IA. | 10-11-2012 |
20120270858 | Isoquinoline, quinoline, and quinazoline derivatives as inhibitors of hedgehog signaling - The invention provides isoquinoline, quinoline, and quinazoline derivatives to treat a variety of disorders, diseases and pathologic conditions, and more specifically to the use of isoquinoline, quinoline, and quinazoline derivatives to inhibit the hedgehog signaling pathway and to the use of those compounds to the treatment of hyperproliferative diseases and pathologic angiogenesis. | 10-25-2012 |
20130143871 | 4-AMINOQUINAZOLIN-2-YL-1-PYRRAZOLE-4-CARBOXYLIC ACID COMPOUNDS AS PROLYL HYDROXYLASE INHIBITORS - Aminoquinazolinyl compounds of formula (I) are described, which are useful as prolyl hydroxylase inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by prolyl hydroxylase activity. Thus, the compounds may be administered to treat, e.g., anemia, vascular disorders, metabolic disorders, and wound healing. | 06-06-2013 |
20130165427 | COMPOUNDS AND COMPOSITIONS FOR TREATING CHEMICAL WARFARE AGENT-INDUCED INJURIES - Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein. | 06-27-2013 |
20130165428 | XANTHINE DERIVATIVES, THE PREPARATION THEREOF AND THEIR USE AS PHARMACEUTICAL COMPOSITIONS - The present invention relates to substituted xanthines of general formula | 06-27-2013 |
20130184260 | PYRIDAZINONE DERIVATIVES - Compounds of the formula (I), in which R | 07-18-2013 |
20130184261 | PYRIDAZINONE DERIVATIVES - Compounds of the formula (I), in which R | 07-18-2013 |
20130210810 | Protein Kinase C Inhibitors and Uses Thereof - This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes. | 08-15-2013 |
20130231331 | Inhibitors of Human Immunodeficiency Virus Replication - The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection. | 09-05-2013 |
20130296305 | TRICYCLIC PYRROLO DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS - The present invention relates to tricyclic pyrrolo derivatives of Formula (I), which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them. | 11-07-2013 |
20130303521 | COMPOUNDS AND COMPOSITIONS FOR TREATING CHEMICAL WARFARE AGENT-INDUCED INJURIES - Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein. | 11-14-2013 |
20130331377 | DIAMINOPYRIMIDINE DERIVATIVES AND PROCESSES FOR THE PREPARATION THEREOF - The present invention provides a diaminopyrimidine derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, a pharmaceutical composition comprising the same, and a use thereof. The diaminopyrimidine derivative or its pharmaceutically acceptable salt functions as a 5-HT | 12-12-2013 |
20130338147 | 4,6-DISUBSTITUTED AMINOPYRIMIDINE DERIVATIVES AS INHIBITORS OF PROTEIN KINASES - The present invention relates to inhibitors of cyclin-dependent kinases and therapeutic applications thereof. Furthermore, the invention relates to methods of preventing and/or treating any type of pain, inflammatory disorders, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases and neurodegenerative diseases comprising the administration of an effective amount of at least one inhibitor of cyclin-dependent kinases. | 12-19-2013 |
20140057901 | XANTHINE DERIVATIVES, THE PREPARATION THEREOF AND THEIR USE AS PHARMACEUTICAL COMPOSITIONS - The present invention relates to substituted xanthines of general formula | 02-27-2014 |
20140135315 | Pyrido-, Pyrazo- and Pyrimido-Pyrimidine Derivatives as mTOR Inhibitors - There is provided a compound of formula I: | 05-15-2014 |
20140155386 | BRIDGED BICYCLIC ARYL AND BRIDGED BICYCLIC HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS - Bridged bicyclic aryl or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed. | 06-05-2014 |
20140303149 | PYRAZOLO[1,5a]PYRIMIDINE DERIVATIVES AS IRAK4 MODULATORS - Compounds of the formula I or II: | 10-09-2014 |
20140309215 | 4-AMINOQUINAZOLIN-2-YL-1-PYRRAZOLE-4-CARBOXYLIC ACID COMPOUNDS AS PROLYL HYDROXYLASE INHIBITORS - Aminoquinazolinyl compounds of formula (I) are described, | 10-16-2014 |
20150011534 | PYRIDAZINONE DERIVATIVES - Compounds of the formula (I), in which R | 01-08-2015 |
20150051195 | NOVEL VIRAL REPLICATION INHIBITORS - The present invention relates to a series of novel compounds having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to methods for the preparation of such compounds, as well as to novel intermediates useful in one or more steps of such syntheses. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutical amount of such compounds, optionally combined with one or more other drugs having antiviral activity. | 02-19-2015 |
20150141408 | TRICYCLIC PYRROLO DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS - The present invention relates to tricyclic pyrrolo derivatives which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them. | 05-21-2015 |
20160122319 | CYCLIC AMINOMETHYL PYRIMIDINE DERIVATIVE - The present invention provides a cyclic aminomethyl pyrimidine derivative and a pharmaceutically acceptable salt thereof with high selectivity for dopamine D | 05-05-2016 |
20170233411 | THIAZOLYL-CONTAINING COMPOUNDS FOR TREATING PROLIFERATIVE DISEASES | 08-17-2017 |