Patent application number | Description | Published |
20110046121 | INHIBITORS OF FOCAL ADHESION KINASE - The invention provides inhibitors of focal adhesion kinase, an enzyme involved in the attachment of the cytoskeleton of a cell to an extracellular matrix, which has been implicated in processes such as cell migration, cell proliferation, and cell survival. The inhibitors are derivatives of a 5-substituted 2,4-diaminopyridine wherein the substituents are as defined herein. The invention also provides a method of using the inhibitors in treatment of cancer, and methods of preparation of the inhibitors by use of coupling reactions. | 02-24-2011 |
20120309757 | N-BIPHENYLMETHYLINDOLE MODULATORS OF PPARG - The invention provides molecular entities that bind with high affinity to PPARG (PPARγ), inhibit kinase-mediated, e.g., cdk5-mediated, phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes, insulin resistance, impaired glucose tolerance, pre-diabetes, hyperglycemia, hyperinsulinemia, obesity, or inflammation. In methods of treatment of these conditions using a compound of the invention, the compound can avoid producing side effects of significant weight gain, edema, impairment of bone growth or formation, or cardiac hypertrophy, or any combination thereof, in the patient receiving the compound. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided. | 12-06-2012 |
20120309769 | N-BENZYLINDOLE MODULATORS OF PPARG - The invention provides molecular entities that bind with high affinity to PPARG (PPARγ), and inhibit kinase-mediated (e.g., cdk5-mediated) phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes, insulin resistance, impaired glucose tolerance, pre-diabetes, hyperglycemia, hyperinsulinemia, obesity, or inflammation. Side effects such as significant weight gain, edema, impairment of bone growth or formation, or cardiac hypertrophy, or any combination thereof, can be avoided in the mammal receiving the compound. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided. | 12-06-2012 |
20130281443 | INHIBITORS OF FOCAL ADHESION KINASE - The invention provides inhibitors of focal adhesion kinase, an enzyme involved in the attachment of the cytoskeleton of a cell to an extracellular matrix, which has been implicated in processes such as cell migration, cell proliferation, and cell survival. The inhibitors are derivatives of a 5-substituted 2,4-diaminopyridine wherein the substituents are as defined herein. The invention also provides a method of using the inhibitors in treatment of cancer, and methods of preparation of the inhibitors by use of coupling reactions. | 10-24-2013 |
20140187554 | MODULATORS OF THE NUCLEAR HORMONE RECEPTOR ROR - The invention provides small molecule modulators of retinoic acid receptor-related orphan receptors such as RORα, RORβ, or RORγ. Compounds of the invention can be effective modulators at concentrations ineffective to act on LXR receptors, or on other nuclear receptors, or other biological targets. Methods of modulation the RORs and methods of treating metabolic disorders, immune disorders, cancer, and CNS disorders wherein modulation of an ROR is medically indicated are also provided. | 07-03-2014 |
20140364432 | SUBSTITUTED PROLINES / PIPERIDINES AS OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as OX | 12-11-2014 |
20140364433 | SUBSTITUTED PROLINES / PIPERIDINES AS OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as OX | 12-11-2014 |
Patent application number | Description | Published |
20090056331 | HIGH EFFICIENCY INTEGRATED HEAT ENGINE (HEIHE) - The present invention is a High Efficient Integrated Heat Engine, or HEIHE for short. HEIHE is a reciprocal combustion engine integrated with both compound cycle and combined cycle. HEIHE comprises twin compound cylinder structure, with the first cylinder being the primary combustion and/or expansion cylinder; the second cylinder being the secondary combustion and/or expansion cylinder. Power strokes driven by expansions of different working fluids such as air-fuel combustion products, steam and compressed air, are integrated into one engine block. Twin cylinder structure provides compound expansions of three (3) different fluids as to recover the energies that would be lost with the exhaust fluids or during braking. All of these make HEIHE work around six (6) periods with twelve (12) operation strokes. Among six (6) working periods involved, four (4) periods contain four (4) different power strokes but only one of the power strokes consumes the fuel. Thus the fuel conversion efficiency could be greatly increased, or even be doubled comparing with the conventional internal combustion engine (ICE). | 03-05-2009 |
20090056670 | HIGH EFFICIENCY INTEGRATED HEAT ENGINE-2 (HEIHE-2) - The present invention is a second kind of High Efficiency Integrated Heat Engine, or HEIHE-2 for short. HEIHE-2 is a reciprocal combustion engine integrated with both compound cycle and combined cycle. HEIHE-2 comprises triple compound cylinder structure, with the first cylinder and the second cylinder being the primary combustion and/or expansion cylinders; and the third cylinder being the secondary combustion and/or expansion cylinder. Power strokes driven by expansions of different working fluids such as air-fuel combustion products, steam and compressed air, are integrated into one engine block. Triple cylinder structure provides compound expansions of three (3) different fluids as to recover the energies that would be lost with the exhaust fluids or during braking. All of these make HEIHE-2 work around four (4) periods with six (6) different operation strokes. All four (4) working periods contain four (4) different power strokes but only two (2) of them consume the fuel. Thus the fuel conversion efficiency could be greatly increased, or even be doubled comparing with the conventional internal combustion engine (ICE). | 03-05-2009 |