Patent application number | Description | Published |
20080287457 | Inhibitors of Akt Activity - The present invention is directed to compounds which contain substituted naphthyridines which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention. These substituted naphthyridines have unexpected advantageous properties when compared to other naphthyridines reported in PCT publication WO2003/086394, such unexpected advantageous properties may include increased cellular potency/solubility, greater selectivity, enhanced pharmacokinetic properties, lack of off target activity and so on. | 11-20-2008 |
20100160309 | INHIBITORS OF JANUS KINASES AND/OR 3-PHOSPHOINOSITIDE-DEPENDENT PROTEIN KINASE-1 - The instant invention provides for compounds that inhibit JAK2 tyrosine kinase and/or PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting JAK2 tyrosine kinase activity and/or PDK1 kinase inhibitory activity by administering the compound to a patient in need of treatment or prevention of myeloproliferative disorders or cancer. | 06-24-2010 |
20100197634 | INHIBITORS OF JANUS KINASES - The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer. | 08-05-2010 |
20100267707 | Tyrosine Kinase Inhibitors - The present invention relates to 4-indol-3-yl-N-phenylpyrimidin-2-amine 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. | 10-21-2010 |
20110082136 | INHIBITORS OF JANUS KINASES - The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3, TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer. | 04-07-2011 |
20110245205 | AMINOPYRIMIDINES AS SYK INHIBITORS - The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis. | 10-06-2011 |
20120004240 | INHIBITORS OF AKT ACTIVITY - The instant invention provides for substituted fused naphthyridine derivatives that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer. | 01-05-2012 |
20120220624 | PYRAZOLO [3,4-B] PYRIDIN-4-ONE KINASE INHIBITORS - The present invention is directed to novel kinase inhibitors of general formula (I) and pharmaceutically acceptable salts thereof, and to the use of the kinase inhibitors of general formula (I) for treating diseases or disorders in which tau phosphorylation and cell cycle regulation is implicated, such as Alzheimer's Disease and cancer. | 08-30-2012 |
20120277192 | AMINOPYRIMIDINES AS SYK INHIBITORS - The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis. | 11-01-2012 |
20130040933 | AZAINDOLES AS JANUS KINASE INHIBITORS - The present invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof. Compounds of formula I are inhibitors of Janus kinases and as such are useful for the treatment of various diseases and conditions mediated by said enzymes, such as rheumatoid arthritis, asthma, COPD, ALS, and the like. | 02-14-2013 |
20130225591 | IMIDOTHIAZOLE KINASE INHIBITORS - The present invention is directed to novel kinase inhibitors of general formula (I) and pharmaceutically acceptable salts thereof, and to the use of the kinase inhibitors of general formula (I) for treating diseases or disorders in which tau phosphorylation and cell cycle regulation is implicated, such as Alzheimer's Disease and cancer. | 08-29-2013 |
20140235641 | PYRAZOLE CARBOXAMIDES AS JANUS KINASE INHIBITORS - The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer. | 08-21-2014 |
20140243290 | Aminopyrimidines as SYK Inhibitors - The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis. | 08-28-2014 |
20140243309 | CYCLOALKYLNITRILE PYRAZOLE CARBOXAMIDES AS JANUS KINASE INHIBITORS - The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer. | 08-28-2014 |