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| Number | Title | Issue Date |
| 8183254 | Inhibitors of JNK The invention relates to prodrugs of JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses prodrugs of JNK inhibitors, as described below in formula I: | 05/22/2012 |
| 8183255 | N-pyrimidin-4-yl-3-amino-pyrrolo[3,4-c]pyrazole derivatives as PKC kinase inhibitors The present invention relates to compounds and pharmaceutically acceptable salts of Formulas A and B: (A) and (B) wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9 and ... | 05/22/2012 |
| 8183253 | Phenylaminopyrimidine derivatives as inhibitors of bcr-abl kinase The present invention relates to novel phenylaminopyrimidine derivatives, pharmaceutical compositions containing the novel phenylaminopyrimidine derivatives, and processes for their preparation. These compounds are candidates for the treatment of chronic myeloid leu... | 05/22/2012 |
| 8163764 | Skincare methods Disclosed are compositions and methods for skincare, e.g., reducing skin wrinkles and for treating skin disorders. ... | 04/24/2012 |
| 8163765 | Substituted indolyl-alkyl-amino-derivatives as inhibitors of histone deacetylase This invention comprises the novel compounds of formula (1) wherein R1, R2, R3, R4, R5, X and Y have defined meanings, having histone deacetylase inhibiting enzymatic a... | 04/24/2012 |
| 8158642 | Carbamate compounds which inhibit leukocyte adhesion mediated by VLA-4 Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, su... | 04/17/2012 |
| 8158641 | 2-anilino-4-aminoalkyleneaminopyrimidines The present invention relates to 2-arylamino-4-(aminoalkylene)aminopyrimidines inhibitors having the structure shown below: wherein R and R1 are as defined herein. The 2-arylamino-4 -(aminoalkylene)aminopyrimidin... | 04/17/2012 |
| 8148391 | 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 R1, R2, R3, R4, R5, A1, A2, A3, A4, and A... | 04/03/2012 |
| 8138199 | Use of bi-aryl meta-pyrimidine inhibitors of kinases The invention provides biaryl meta-pyrimidine compounds having the general structure (A). The pyrimidine compounds of the invention are capable of inhibiting kinases, such as members of the Jak kinase family, and various other specific receptor and non-receptor kina... | 03/20/2012 |
| 8138198 | Substituted aminopropenyl piperidine or morpholine derivatives as novel inhibitors of histone deacetylase This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, R4, X and Y have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them a... | 03/20/2012 |
| 8133901 | 3-heteroaryl (amino or amido)-1-(biphenyl or phenylthiazolyl) carbonylpiperidine derivatives as orexin receptor inhibitors The invention relates to piperidine compounds of formula (I): wherein X—R1 represents —N(H)-pyrimidinyl, wherein said pyrimidinyl is unsubstituted or mono-substituted wherein the substituent is selected from ... | 03/13/2012 |
| 8133900 | Use of bi-aryl meta-pyrimidine inhibitors of kinases The invention provides methods of treating a disease selected from systemic sclerosis, rheumatoid arthritis, mastocytosis, and chronic eosinophilic leukemia comprising administering biaryl meta-pyrimidine compounds having the general structure (A) to a subject in ne... | 03/13/2012 |
| 8124611 | Inhibitors of the mutant form of kit The present invention relates to the treatment of KIT dependent diseases that are characterized by a mutant form of KIT whereby the mutant KIT is identified and an appropriate inhibitor of the mutant KIT is administered. ... | 02/28/2012 |
| 8124610 | Sodium channel inhibitors Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-gated sodium channels. More particularly, the invention provides substituted sulfonamides, compositions comprisin... | 02/28/2012 |
| 8119650 | Aminophenyl derivatives as novel inhibitors of histone deacetylase This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X and Y have defined... | 02/21/2012 |
| 8114885 | Chemical compounds Pyrimidine derivatives, which are useful as VEGFR2 inhibitors are described herein. The described invention also includes methods of making such pyrimidine derivatives as well as methods of using the same in the treatment of hyperproliferative diseases. ... | 02/14/2012 |
| 8114884 | CXCR4 antagonists for the treatment of medical disorders The invention provides compounds, pharmaceutical compositions and methods of use of certain compounds that are antagonists of the chemokine CXCR4 receptor for the treatment of proliferative conditions mediated by CXCR4 receptors. The compounds provided interfere wit... | 02/14/2012 |
| 8101628 | Imidazolidinonyl aminopyrimidine compounds for the treatment of cancer The present invention provides novel imidazolidinonyl aminopyrimidine compounds believed to have clinical use for treatment of cancer through inhibiting Plk1. wherein: R1 hydrogen, hydroxy, halo, methyl, C1-C2 alkoxy, amino, or methy... | 01/24/2012 |
| 8101627 | Stereoisomerically enriched 3-aminocarbonyl bicycloheptene pyrimidinediamine compounds and their uses The present invention provides stereoisomers and stereoisomeric mixtures of 3-aminocarbonyl-bicycloheptene-2,4-pyrimidinediamine compounds having antiproliferative activity, compositions comprising the compounds and methods of using the compounds to inhibit cellular... | 01/24/2012 |
| 8101629 | Salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile The present invention relates to a pharmaceutical composition comprising as active ingredient the hydrochloric acid salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethyl-phenyl]amino]-2-pyrimidinyl]amino]benzonitrile and to processes for their preparation. ... | 01/24/2012 |
| 8093259 | 4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-N-[5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)phenyl]-benzamide for treatment of melanoma The present invention relates to the use of pyrimidylaminobenzamide compounds for the preparation of a drug for the treatment of diseases that respond to modulation of Ephrin receptor kinase, especially EphB4, activity, especially for the curative and/or prophylacti... | 01/10/2012 |
| 8088784 | 4-(3-aminopyrazole) pyrimidine derivatives for use as tyrosine kinase inhibitors in the treatment of cancer This invention relates to novel compounds having the formula (I) and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment for cancer. ... | 01/03/2012 |
| 8063058 | Inhibitors of syk and JAK protein kinases The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk kinase. The present invention is also directed to intermediates used in making such com... | 11/22/2011 |
| 8048889 | 3,4-disubstituted coumarin and quinolone compounds The present invention relates to 3,4-disubstituted coumarin and quinolone derivatives and processes for their preparation. The invention also related to methods for treating infection of Hepatitis C virus by administering a 3,4-disubstituted coumarin or quinolone de... | 11/01/2011 |
| RE42889 | α- and β- amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors α- and β-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. ... | 11/01/2011 |
| 8044064 | Fused pyrrolocarbazoles The present invention relates generally to selected fused pyrrolocarbazoles, including pharmaceutical compositions thereof and methods of treating diseases therewith. The present invention is also directed to intermediates and processes for making these fused pyrrol... | 10/25/2011 |
| 8039479 | Compounds and compositions as protein kinase inhibitors The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condit... | 10/18/2011 |
| 8026248 | HIV inhibiting pyrimidine derivatives This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CR4 or N; n is 0 to 4; Q ... | 09/27/2011 |
| 8022079 | Methods of modulating PPAR gamma-type receptors Novel compounds having the general formula (I) below: are useful in a wide variety of applications in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or d... | 09/20/2011 |
| 8017621 | Inhibitors of the mutant form of kit The present invention relates to the treatment of KIT dependent diseases that are characterized by a mutant form of KIT whereby the mutant KIT is identified and an appropriate inhibitor of the mutant KIT selected form midostaurin, vatalanib and compound A is adminis... | 09/13/2011 |
| 8012989 | Substituted pyrimidine compounds and their utility as CETP inhibitors A compound represented by the following general formula (I), wherein R1, R2, R3, R4 and R5 represent hydrogen atom, a halogen atom, a lower alkyl group and the like, R6 represents an alkyl group, a cy... | 09/06/2011 |
| 8008312 | CXCR4 antagonists for the treatment of HIV infection The invention provides compounds, pharmaceutical compositions and methods of use of certain compounds that are antagonists of the chemokine CXCR4 receptor, and in particular to inhibit viral entry of certain viruses. Certain compounds in particular can reduce entry ... | 08/30/2011 |
| 8008313 | Methods of using diaminopyrimidine P2Xand P2Xreceptor modulators for treatment of respiratory and gastrointestinal diseases Methods for treating respiratory and gastrointestinal diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a compound of formula (I): | 08/30/2011 |
| 7994185 | Benzene sulfonamide thiazole and oxazole compounds The present invention provides thiazole sulfonamide and oxazole sulfonamide compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents. ... | 08/09/2011 |
| 7994184 | Small molecules that replace or agonize p53 function This invention provides a novel screening system for identifying p53 mimetics/agonists. Also provided are small organic molecules that act as effective p53 mimetics/agonists. ... | 08/09/2011 |
| 7985756 | Modulation of neurogenesis by PDE inhibition The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The disclosure includes compositions and methods based on use of a PDE agent, optionally in combinat... | 07/26/2011 |
| 7977348 | Polymorphic forms of imatinib mesylate and processes for preparation of novel crystalline forms as well as amorphous and form α Solvates and crystalline forms of imatinib mesylate are described. Further, methods for preparing such solvates and crystalline forms of imatinib mesylate are described. The structure diagram below shows the chemical structure of imatinib mesylate. | 07/12/2011 |
| 7968560 | Compounds that modulate PPARγ-type receptors and cosmetic/pharmaceutical compositions comprising said compounds Novel compounds having the general formula (I) below: are useful in a wide variety of applications in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or d... | 06/28/2011 |
| 7956063 | Salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile The present invention relates to a pharmaceutical composition comprising as active ingredient the hydrochloric acid salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethyl-phenyl]amino]-2-pyrimidinyl]amino]benzonitrile and to processes for their preparation. ... | 06/07/2011 |
| 7947699 | Anhydrous amorphous imatinib mesylate Described is a highly stable amorphous form of imatinib mesylate having a water content of less than 0.5 percent by weight, based on the total weight of the amorphous imatinib mesylate, (anhydrous amorphous imatinib mesylate), a process for preparation thereof, and ... | 05/24/2011 |
