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| Number | Title | Issue Date |
| 8138209 | Substituted picolinamides as MAO-B inhibitors useful for treating obesity The invention provides novel compounds of formula I: that are monoamine oxidase-B inhibitors, which can be useful in treating obesity, diabetes, and/or cardiometabolic disorders (e.g., hypertension, dyslipidemias, high bloo... | 03/20/2012 |
| 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 |
| 8124645 | LPA receptor antagonist A compound of the general formula (I): (wherein the symbols are as defined in the description), or a non-toxic salt thereof. This compound engages in LPA receptor bonding and antagonism and hence is useful in the prevention... | 02/28/2012 |
| 8119636 | Pyrrolopyrazine kinase inhibitors The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q and R are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-i... | 02/21/2012 |
| 8110576 | Substituted pyrrolo[2,3b]pyrazines and methods for treatment of raf protein kinase-mediated indications Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described, wherein the compounds have the formula: In certain aspects and embodiments, the descr... | 02/07/2012 |
| 8106059 | Substituted pyrazines that inhibit protease cathepsin S and HCV replication The present invention is directed to compounds of formula I, below, that have the dual property of acting as cathepsin S inhibitors and of inhibiting HCV replication. Such compounds are therefore useful in treating disease states that include hepatitis C, Alzheimer'... | 01/31/2012 |
| 8101620 | Heterocyclic sulfonamides Provided is a compound of the following formula: wherein: R3 is an aryl or heteroaryl group, which is optionally substituted with a halogen, lower alkoxy, aryl or heteroaryl gro... | 01/24/2012 |
| 8101611 | Substituted pyridazines inhibitors of MEK Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8 and R9, W, X and Y are as defined in the spe... | 01/24/2012 |
| 8093382 | Dipeptidyl peptidase inhibitors Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a member selected from the group consisting of: wherein E is CH or N, Q is selected from the group consistin... | 01/10/2012 |
| 8080536 | Phosphorus-containing prodrugs Novel cyclic phosphoramidate prodrugs of drugs of formula I their use in delivery of drugs to the liver, their use in enhancing oral bioavailability, and their method of preparation are described. ... | 12/20/2011 |
| 8076480 | Process of preparing optically active allyl compound Disclosed is a process of preparing an optically active allyl compound, e.g., as represented by formula (III): comprising asymmetrically coupling an allyl compound with an organic nucleophilic compound in the presence of a ... | 12/13/2011 |
| 8071598 | 3,9-diazabicyclo[3.3.1]nonane derivatives and their use as monoamine neurotransmitter re-uptake inhibitors 3,9-diazabicyclo[3.3.1]nonane derivatives, useful as monoamine neurotransmitter re-uptake inhibitors. Also, use of these compounds in a method for therapy and in pharmaceutical compositions comprising the compounds. The 3,9-diazabicyclo[3.3.1]nonane derivatives have... | 12/06/2011 |
| 8067423 | Polymorphs of dasatinib isopropyl alcohol and process for preparation thereof The invention provides crystalline forms of isopropyl alcohol solvate of dasatinib, methods for their preparation, and pharmaceutical compositions thereof. ... | 11/29/2011 |
| 8058456 | Optically active 3-amino-2,5-dioxopyrrolidine-3-carboxylate, process for production of the compound, and use of the compound The present invention provides a compound of the formula (III): wherein R is a C1-6 alkyl group, as a novel optically active intermediate for preparing tetrahydropyrrolo[1,2-a]pyrazin-4-spiro-3′-pyrro... | 11/15/2011 |
| 8044052 | Biaryl ether urea compounds The present invention relates to compounds of Formula (I) or a pharmaceutically acceptable salt thereof; processes for the preparation of the compounds; intermediates used in the preparation of the compounds; compositions c... | 10/25/2011 |
| 8039471 | Aza spiro alkane derivatives as inhibitors of metalloproteases The present invention provides a compound of Formula I or Formula II: enantiomer, diastereomer, prodrug, solvate, metabolite, or pharmaceutically acceptable salt thereof, wherein constituent variables are provided herein. T... | 10/18/2011 |
| 8034955 | Therapeutic compounds and methods of use Compounds and methods useful for chemopreventative treatment of diseases such as cancer, Alzheimer's disease, Parkinson's disease, inflammatory bowel diseases, and multiple sclerosis. ... | 10/11/2011 |
| 8012974 | Pyrrolopyrazinyl urea kinase inhibitors The present invention relates to the use of novel pyrrolopyrazinyl urea derivatives of Formula I, wherein the variables R1, R2, R3, R4, and R5 are defined as described ... | 09/06/2011 |
| 8012969 | 11C-labeled benzyl-lactam compounds and their use as imaging agents The invention relates to “C-labeled compounds, their preparation, compositions comprising an effective amount of a “C-labeled compound, and the use of a “C-labeled compound as a radiopharmaceutical for positron emission tomography. ... | 09/06/2011 |
| 8008491 | Substituted AZA-indoles as inhibitors of poly(ADP-ribose) polymerase (PARP) The present invention relates to a series of substituted aza-indole derivatives of the formula I: wherein R, R1, R2, R3, R4, X and Y are as defined herein. This invention also rel... | 08/30/2011 |
| 8003654 | N-glycinsulfonamide derivatives and uses as orexin receptor antagonists The invention relates to novel sulfonamide compounds of the formula (I) and their use as orexin receptor antagonists. ... | 08/23/2011 |
| 7994169 | 3,4-diaminopyridine derivatives for use as catalysts The present invention relates to 3,4-diaminopyridine derivatives of formula (I) wherein R1 and R2 are, independently of each other, electron donors, wherein R2... | 08/09/2011 |
| 7989461 | Substituted quinazolinamine compounds for the treatment of cancer The present invention comprises a new class of compounds capable of modulating Raf kinase and, accordingly, useful for treatment of Raf kinase mediated diseases, including melanomas, tumors and other cancer-related conditions. The compounds have a general Formula I | 08/02/2011 |
| 7989621 | Method for producing substituted imidazo[1,2-A]pyrazines of (s)-1-(3-(2-sec-butyl-6-(1h-indol-3-yl)-3-oxo-3,7-dihydroimadazo[1,2-a]pyrazin-8-yl)propyl)guanidine The present invention relates to a method for producing marine ostracod crustacean luciferin or a derivative thereof represented by a general formula (4), characterized by reacting a compound represented by a general formula (2) with a compound represented by a gene... | 08/02/2011 |
| 7981889 | Phthalazinone derivatives Compounds of the formula (I): wherein A and B together represent an optionally substituted, fused aromatic ring; X can be NRX or CRXRY; if X═NRX then n is 1 or 2 and if X═CR | 07/19/2011 |
| 7981925 | Compounds that modulate intracellular calcium Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with othe... | 07/19/2011 |
| 7977346 | Spiro compounds and methods of use The present invention relates to spiro compounds of formula I, processes for their preparation, pharmaceutical compositions containing them as active ingredient, methods for the treatment of disease states such as cancers associated with protein tyrosine kinases, es... | 07/12/2011 |
| 7973045 | Anhydrous form of dasatinib and process for preparation thereof The invention provides anhydrous forms of dasatinib, methods for their preparation, and pharmaceutical compositions thereof. ... | 07/05/2011 |
| 7960545 | Process for the prepartion of erlotinib The present invention discloses an improved and novel process for the preparation of erlotinib (N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine) of formula (1), which comprises: (i) demethylation of commercially available 6,7-dimethoxy-4(3H)-quinazoli... | 06/14/2011 |
| 7947674 | Meso-substituted porphyrins Meso-substituted porphyrins of general formula (I) suitable for the use as photosensitizing agents, in particular in photodynamic therapy, are herein described. ... | 05/24/2011 |
| 7935836 | Compounds comprising a linear series of five fused carbon rings, and preparation thereof The present application discloses methods for the production of organic compounds comprising a linear series of five fused carbon rings. Such compounds are useful in the production of electronic components, devices and materials. For example the methods disclosed pe... | 05/03/2011 |
| 7932254 | Pyrrolopyrazine kinase inhibitors The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q1 and R are defined as described herein, which inhibit JAK and SYK and are useful for the treatme... | 04/26/2011 |
| 7928111 | Compounds including substituted thienopyrimidinone derivatives as ligands for modulating chemosensory receptors The present invention provides compounds including substituted thienopyrimidinone derivatives of Formula (IIc) as ligands for modulating chemosensory receptors: These compounds are useful as sweet taste enhancers in comesti... | 04/19/2011 |
| 7915274 | Nitrogen containing heterocyclic compounds and medicines containing the same Compounds represented by the following general formula: [wherein X1, X2, X3 and X4 each independently represent a single bond, C1-6 alkylene, etc.; A2 repres... | 03/29/2011 |
| 7910766 | Preparation of at least one partial oxidation and/or ammoxidation product of a hydrocarbon A process for preparing at least one partial oxidation and/or ammoxidation product of a hydrocarbon by partially dehydrogenating at least one saturated hydrocarbon H under heterogeneous catalysis and using the resulting product gas mixture A, which comprises the par... | 03/22/2011 |
| 7884110 | Fused heteroaryl pyridyl and phenyl benzenesuflonamides as CCR2 modulators for the treatment of inflammation Compounds are provided that act as potent antagonists of the CCR2 receptor. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases and as controls in assays for the ... | 02/08/2011 |
| 7863282 | Compositions useful as inhibitors of protein kinases A compound of formula Ia: or a pharmaceutically acceptable salt thereof. ... | 01/04/2011 |
| 7858614 | Therapeutic pyrazolonaphthyridine derivatives The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and negatively modulating the α5 subtype of GABAA, and use of the compound of formula I... | 12/28/2010 |
| 7851503 | Thrombopoetin receptor activator and process for producing the same A preventive, therapeutic or improving agent for diseases against which activation of the thrombopoietin receptor is effective or a platelet increasing agent, which contains a thrombopoietin receptor activator represented by the formula (1): | 12/14/2010 |
| 7851621 | Synthesis of deoxybiotinyl hexamethylenediamine-dota A process for the synthesis of deoxybiotinyl hexamethylenediamine0-DOTA is herein described. Said process comprises reacting biotinyl hexamithylenediamine with tri-t-butyl DOTA in the presence of benzotriazol-1-yl-oxytripyrrolidinophosphonium hexafluorophosphate, as... | 12/14/2010 |
