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| Number | Title | Issue Date |
| 8183245 | Pyrazine substituted pyrrolopyridines as inhibitors of JAK and PDK1 The present invention relates to pyrazine substituted pyrrolopyridines having formula (I) useful as inhibitors of JAK kinases (JAK1, JAK2, JAK3 and/or TYK2) and/or PDK1 and for the treatment of myeloproliferative disorders ... | 05/22/2012 |
| 8168658 | Inhibitors of histone deacetylase The present invention relates to a novel class of compounds. These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting... | 05/01/2012 |
| 8168652 | Inhibitors of AKT activity The instant invention provides for substituted naphthyridine compounds 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 compo... | 05/01/2012 |
| 8158825 | Modified malonate derivatives The present invention relates to a novel class of modified malonate derivatives. The modified malonate compounds can be used to treat cancer. The modified malonate compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing termin... | 04/17/2012 |
| 8153778 | RNA interference mediated inhibition of vascular cell adhesion molecule (VCAM) gene expression using short interfering nucleic acid (siNA) This invention relates to compounds, compositions, and methods useful for modulating vascular cell adhesion molecule gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for... | 04/10/2012 |
| 8119685 | Disubstituted aniline compounds The present invention relates to a novel class of disubstituted aniline compounds. These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cel... | 02/21/2012 |
| 8119652 | Aryl-fused spirocyclic compounds The present invention relates to a novel class of aryl-fused spirocyclic compounds. These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic ce... | 02/21/2012 |
| 8101621 | Aminopyridine derivatives having aurora a selective inhibitory action The present invention relates to a compound of general formula I: wherein: n1 and n2 are the same or different, and are 0 or 1; R is aryl, heteroaryl, etc.; Re | 01/24/2012 |
| 8101603 | Tyrosine kinase inhibitors The present invention relates to 5H-benzo[4,5]cyclohepta[1,2-b]pyridine 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... | 01/24/2012 |
| 8093295 | Formulations of suberoylanilide hydroxamic acid and methods for producing the same The present invention provides a pharmaceutical composition or crystalline composition with a specific dissolution profile, which comprises suberoylanilide hydroxamic acid or a pharmaceutically acceptable salt or hydrate thereof as an active ingredient. The present ... | 01/10/2012 |
| 8080573 | Heterocycle substituted amide and sulfur amide derivatives as histone deacetylase (hdac) inhibitors The present invention related to compounds of formula (I): or a pharmaceutically acceptable salt, stereoisomer or tautomer thereof. Compounds of the present invention are inhibitors of histone deacetylase (HDAC) and are useful for treating cellular proliferative dis... | 12/20/2011 |
| 8076479 | Process and intermediates for the synthesis of (3-alkyl-5-piperidin-1-yl-3,3a-dihydro-pyrazolo[1,5-a]pyrimidin-7-yl)-amino derivatives and intermediates Disclosed is a process for the synthesis of compounds of Formula I by sequentially aminating, first with a primary amine and then with a secondary amine, an intermediate compound of the structure of Formula E1, | 12/13/2011 |
| 8076472 | RNA interference mediated inhibition of muscarinic colinergic receptor gene expression using short interfering nucleic acid (siNA) The present invention relates to compounds, compositions, and methods useful for modulating the expression of genes associated with respiratory and pulmonary disease, such as cholinergic muscarinic receptor genes, using short interfering nucleic acid (siNA) molecule... | 12/13/2011 |
| 8071623 | Amide substituted indazoles as poly(ADP-ribose)polymerase(PARP) inhibitors The present invention relates to compounds of formula I: and pharmaceutically acceptable salts, stereoisomers or tautomers thereof which are inhibitors of poly (ADP-ribose) polymerase (PARP) and thus useful for the treatmen... | 12/06/2011 |
| 8034772 | Inhibitor of vascular endothelial cell growth factor The vascular endothelial cell growth factor (VEGF) inhibitors of the present invention are naturally occurring or recombinantly engineered soluble forms with or without a C-terminal transmembrane region of the receptor for VEGF, a very selective growth factor for en... | 10/11/2011 |
| 8030327 | Fused imidazole derivative The present invention relates to a compound represented by the Formula [I]: Wherein: the A ring is a 5-membered aromatic heterocyclic group containing at least one hetero atom selected fro... | 10/04/2011 |
| 8026265 | Heterocycle substituted ketone derivatives as histone deacetylase (HDAC) inhibitors The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts and tautomers thereof. Compounds of the present invention are inhibitors of histone deacetylase (HDAC) and are useful for treating cellular proliferative diseases, inclu... | 09/27/2011 |
| 8026260 | Histone deacetylase inhibitors with aryl-pyrazolyl-motifs The present invention relates to a novel class of histone deacetylase inhibitors with aryl-pyrazolyl motifs. The compounds of this invention can be used to treat cancer. The compounds of this invention are suitable for use in selectively inducing terminal differenti... | 09/27/2011 |
| 8017765 | RNA interference mediated treatment of alzheimer's disease using short interfering nucleic acid (siNA) The present invention concerns methods and reagents useful in modulating BACE gene expression in a variety of applications, including use in therapeutic, diagnostic, target validation, and genomic discovery applications. Specifically, the invention relates to small ... | 09/13/2011 |
| 8017761 | RNA interference mediated inhibition of Stearoyl-CoA desaturase (SCD) gene expression using short interfering nucelic acid (siNA) This invention relates to compounds, compositions, and methods useful for modulating Stearoyl-CoA desaturase (SCD) gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for m... | 09/13/2011 |
| 8013146 | RNA interference mediated inhibition of matrix metalloproteinase 13 (MMP13) gene expression using short interfering nucleic acid (siNA) This invention relates to compounds, compositions, and methods useful for modulating matrix metalloproteinase (e.g., MMP13) gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods use... | 09/06/2011 |
| 8013143 | RNA interference mediated inhibition of CXCR4 gene expression using short interfering nucleic acid (siNA) This invention relates to compounds, compositions, and methods useful for modulating chemokine receptor (CXCR) gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modul... | 09/06/2011 |
| 8008295 | Tyrosine kinase inhibitors The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating signal transduction of both receptor-type and non-receptor type tyrosine kinases. The compounds of the instant invention possess a core structure that comprises a... | 08/30/2011 |
| 8003643 | Inhibitors of Akt activity The present invention is directed to compounds which contain substituted pyridazines and pyrimidines moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the comp... | 08/23/2011 |
| 7981874 | Phosphorus derivatives as histone deacetylase inhibitors The present invention relates to a novel class of phosphorus derivatives. The phosphorus compounds can be used to treat cancer. The phosphorus compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, a... | 07/19/2011 |
| 7977374 | Thiophene and thiazole substituted trifluoroethanone derivatives as histone deacetylase (HDAC) inhibitors The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt or stereoisomer thereof. The compounds of the present invention are inhibitors of histone deacetylase (HDAC) and are useful for treating cellular proliferative diseases,... | 07/12/2011 |
| 7977336 | Aminopyrimidine derivatives as PLK1 inhibitors The present invention relates to a compound represented by Formula [I]: or a pharmaceutically acceptable salt or ester thereof, wherein R1 and R2, which may be the same or different, are each a hydroge... | 07/12/2011 |
| 7973037 | Cathepsin cysteine protease inhibitors This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, s... | 07/05/2011 |
| 7964578 | Conjugates and compositions for cellular delivery This invention features conjugates, degradable linkers, compositions, methods of synthesis, and applications thereof, including cholesterol, folate, galactose, galactosamine, N-acetyl galactosamine, PEG, phospholipid, peptide and human serum albumin (HSA) derived co... | 06/21/2011 |
| 7935812 | RNA interference mediated inhibition of hepatitis C virus (HCV) expression using short interfering nucleic acid (siNA) The present invention relates to compounds, compositions, and methods for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of hepatitis C virus (HCV) gene expression and/or activity. The present invention is also ... | 05/03/2011 |
| 7935724 | Thiophene and benzothiophene hydroxamic acid derivatives The present invention relates to a novel class of hydroxamic acid derivatives having a benzothiophene or thiophene backbone. The hydroxamic acid compounds can be used to treat cancer. The hydroxamic acid compounds can also inhibit historic deacetylase and are suitab... | 05/03/2011 |
| 7935708 | Dihydropyrazolopyrimidinone derivatives The invention relates to compounds of a general formula (I): wherein Ar1 is an optionally-substituted aryl or heteroaromatic group; R1 is an optionally-substituted lower alkyl, lower alkenyl, lower alk... | 05/03/2011 |
| 7928220 | RNA interference mediated inhibition of stromal cell-derived factor-1 (SDF-1) gene expression using short interfering nucleic acid (siNA) The present invention relates to compounds, compositions, and methods for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of stromal cell-derived factor-1 (SDF-1) gene expression and/or activity. The present inve... | 04/19/2011 |
| 7928219 | RNA interference mediated inhibition of placental growth factor gene expression using short interfering nucleic acid (SINA) This invention relates to compounds, compositions, and methods useful for modulating placental growth factor (e.g., PGF-1 or PlGF-1, PGF-2 or PlGF-2, and/or PGF-3 or PlGF-3) gene expression using short interfering nucleic acid (siNA) molecules. This invention also r... | 04/19/2011 |
| 7928218 | RNA interference mediated inhibition of polycomb group protein EZH2 gene expression using short interfering nucleic acid (siNA) This invention relates to compounds, compositions, and methods useful for modulating polycomb group protein EZH2 gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for mod... | 04/19/2011 |
| 7928091 | Cathepsin cysteine protease inhibitors This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, s... | 04/19/2011 |
| 7923549 | RNA interference mediated inhibition of interleukin and interleukin receptor gene expression using short interfering nucleic acid (siNA) This invention relates to compounds, compositions, and methods useful for modulating interleukin and/or interleukin receptor gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods us... | 04/12/2011 |
| 7919261 | Methods for predicting treatment response based on the expression profiles of protein and transcription biomarkers The invention disclosed herein describes novel biomarkers useful for risk assessment, screening, prognosis and selection and monitoring of therapy for HDAC mediated cell proliferative disorders. In particular, the invention provides the identities of three particula... | 04/05/2011 |
| 7915407 | Process for {3-[2(R)-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3(S)-(4-fluorophenyl)morpholin-4-yl]methyl]-5-oxo-4,5-dihydro-[1,2,4]-triazol-1-yl}phosphonic acid The present invention is concerned with a process for the preparation of the compound {3-[2(R)-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3(S)-(4-fluorophenyl) -morpholin-4-yl]methyl]-5-oxo-4,5-dihydro-[1,2,4]-triazol-1-yl}phosphonic acid, and pharmaceutically ... | 03/29/2011 |
| 7915400 | RNA interference mediated inhibition of hepatitis C virus (HCV) gene expression using short interfering nucleic acid (siNA) The present invention concerns methods and reagents useful in modulating hepatitis C virus (HCV) gene expression in a variety of applications, including use in therapeutic, diagnostic, target validation, and genomic discovery applications. Specifically, the inventio... | 03/29/2011 |
