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| Number | Title | Issue Date |
| 8188098 | GPR119 receptor agonists Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositi... | 05/29/2012 |
| 8183247 | Boron compounds useful in BNCT The present invention relates to novel boron comprising compounds, to pharmaceutical compositions comprising said compounds, to the therapeutic use of said compounds, and to a process for preparation of said compounds. The compounds are useful in boron neutron captu... | 05/22/2012 |
| 8173662 | Fused pyrimidines as inhibitors of nucleoside phosphorylases and nucleosidases The present invention relates to compounds of the general formula (I) which are inhibitors of purine muclioside phosphorylases (PNP), purine phosphoribosyltransferases (PPRT), 5′-methylthioadenosine phosphorylases (MTAP), 5′-methylthioadenosine mucliosidases (MT... | 05/08/2012 |
| 8158633 | Phenyl-substituted pyrazolopyrimidines The invention relates to novel phenyl-substituted pyrazolopyrimidines, process for their preparation, and their use for producing medicaments for improving perception, concentration, learning and/or memory. ... | 04/17/2012 |
| 8158634 | Compounds and compositions as inhibitors of cannabinoid receptor 1 activity The invention provides compounds having Formula Ia, or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4 and Y are as defined in the specification; as well as pha... | 04/17/2012 |
| 8148386 | Agent for the prevention and treatment of prostatic hyperplasia comprising pyrazolopyrimidinone compound The present invention relates to an agent for preventing and treating benign prostatic hyperplasia (BPH) and lower urinary tract symptoms (LUTS) associated with BPH and a relaxant for relaxing urethral smooth muscle or prostatic smooth muscle comprising a pyrazolopy... | 04/03/2012 |
| 8148387 | AKT and P70 S6 kinase inhibitors The present invention provides AKT and p70 S6 kinase inhibitors of the formula: The present invention also provides pharmaceutical compositions comprising compounds of Formula I, uses of compounds of Formula I and methods of ... | 04/03/2012 |
| 8143262 | 7-(3′,4′-Dialkoxyphenyl)[1,2,4]-triazolo[1,5-A]pyrimidine compounds, process for preparing thereof, and pharmaceutical composition for treating or preventing asthma, chronic obstructive pulmonary disease, arthritis, atopic dermatitis, tumor and degenerative brain diseases comprising the same The present invention relates to novel {7-(3′,4′-dialkoxyphenyl)-[1,2,4]-triazolo[1,5-a]pyrimidine compounds or pharmaceutically acceptable salts thereof, a process for preparing the same, and pharmaceutical compositions for treating or preventing inflammatory d... | 03/27/2012 |
| 8143263 | Therapeutic agents A compound of Formula (I): is useful in the treatment or prevention of a disease or medical condition mediated through glucokinase (GLK or GK), leading to a decreased glucose threshold for insulin secretion. ... | 03/27/2012 |
| 8088781 | Inhibitors of brutons tyrosine kinase Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include th... | 01/03/2012 |
| 8071608 | Therapeutic agents (2S)-2-[1-(2-Chloro-6-cyano-phenyl)pyrazolo[4,5-e]pyrimidin-4-yl]oxy-3-[(1R)-2-hydroxy-1-methyl-ethoxy]-N-(5-methylpyrazin-2-yl)propanamide or a pharmaceutically acceptable salt thereof is useful in the treatment or prevention of a disease or medical condition media... | 12/06/2011 |
| 8071607 | Mnk1 or Mnk2 inhibitors The present invention relates to the use of pyrazolopyrimidine compounds for the production of pharmaceutical compositions for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a... | 12/06/2011 |
| 8044060 | 6-cyclylmethyl- and 6-alkylmethyl pyrazolo[3,4-D]pyrimidines, methods for their preparation and methods for their use to treat impairments of perception, concentration learning and/or memory Described are 6-cyclylmethyl- and 6-alkylmethyl-substituted pyrazolo[3,4-d]pyrimidines of the formula (I): as defined herein, processes for their preparation and their use for producing medicaments for treating impairment o... | 10/25/2011 |
| 8039477 | Substituted pyrazolo[3,4-d]pyrimidin-4-one compounds as phosphodiesterase inhibitors The invention relates to novel alkyl-substituted pyrazolopyrimidines, process for their preparation, and the use thereof for producing medicaments for improving perception, concentration, learning and/or memory with compounds of formula (I): | 10/18/2011 |
| 8008309 | Inhibitors of bruton's tyrosine kinase Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include th... | 08/30/2011 |
| 7973046 | Use of allopurinol for the treatment of palmar plantar erythrodysesthesia Allopurinol or a pharmaceutically acceptable salt thereof can be used for the treatment or prevention of palmar plantar erythrodysesthesia induced by chemotherapy. The allopurinol or its salt may be administered topically to the affected areas, palms and soles, pref... | 07/05/2011 |
| 7968554 | Pyrazolo[3,4-d]pyrimidine derivatives Disclosed are novel pyrazolo[3,4-d]pyrimidine derivatives that are inhibitors of Raf kinase. These compounds and their pharmaceutically-acceptable salts and esters are anti-proliferative agents useful in the treatment or control of proliferative disorders such as so... | 06/28/2011 |
| 7964607 | Pyrazolo[3,4-d]pyrimidine compounds The invention provides PDE9-inhibiting compounds of Formula (I), and pharmaceutically acceptable salts thereof, wherein R, R1, R2 and R3 are as defined herein. Pharmaceutical compositions co... | 06/21/2011 |
| 7960396 | Inhibitors of Bruton's tyrosine kinase Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include th... | 06/14/2011 |
| 7956062 | Reactive oxygen generating enzyme inhibitor with nitric oxide bioactivity and uses thereof A reactive oxygen generating enzyme inhibitor with NO donor bioactivity, e.g., nitrated allopurinol, is useful to treat heart failure, stable angina, ischemic disorder, ischemic reperfusion injury, atherosclerosis, sickle cell disease, diabetes, Alzheimer's disease,... | 06/07/2011 |
| 7947695 | 5-membered annelated heterocyclic pyrimidines as kinase inhibitors This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, Q1, Q2, X1, X2, Y and... | 05/24/2011 |
| 7947694 | Substituted pyrazolo[3,4-D]pyrimidines as cell cycle kinase inhibitors This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, X1 and X2 have defined meanings, having cel... | 05/24/2011 |
| 7943624 | Pyridinylpyrazolopyrimidinone derivatives as PDE 7 inhibitors To provide the compounds inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic disease, inflammatory disease or immunologic disease. The compound is pyrid... | 05/17/2011 |
| 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 |
| 7932257 | Substituted pyrazolo[4,3-d]pyrimidines as aurora kinase inhibitors The present invention provides compounds having the formula: wherein A-B together represent one of the following structures: ... | 04/26/2011 |
| 7919498 | Substituted pyrazolo[3,4-d]pyrimidines as PI3K inhibitors Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psorias... | 04/05/2011 |
| 7910594 | Vitamin-mitomycin conjugates This invention relates to vitamin-mitomycin conjugates, to a method of using the conjugates to selectively eliminate a population of pathogenic cells in a host animal harboring the pathogenic cells, and to a method of preparation of the conjugates. The conjugate is ... | 03/22/2011 |
| 7829571 | Cyclic derivatives as modulators of chemokine receptor activity The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the treatment of rheumatoid arthritis, multiple sclerosis, atherosclerosis and asthma. ... | 11/09/2010 |
| 7799794 | Treatment for cardiovascular disease This invention relates to a method for treating and preventing hypertension by administering a therapeutically effective amount of an agent capable of reducing uric acid levels in a patient in need of such treatment. Additionally, the scope of the invention includes... | 09/21/2010 |
| 7786131 | Pyrimido[5,4-d]pyrimidines derivatives as irreversible inhibitors of tyrosine kinases The present invention relates to pyrimido [5,4-d] pyrimidine compounds of Formula II or a pharmaceutically acceptable salt thereof, wherein Q is and X, E1, E2 | 08/31/2010 |
| 7763624 | Substituted pyrazolo[3,4-d]pyrimidines as ACK-1 and LCK inhibitors The present invention relates to compounds of Formula I or a stereomer, a tautomer, a solvate, a pharmaceutically acceptable salt, or a prodrug thereof, pharmaceutical formulations containing the compounds, methods of treat... | 07/27/2010 |
| 7745450 | Pyrazolo[4,3-d]pyrimidines, processes for their preparation and methods for therapy The invention relates to 3-, 5-, 7-trisubstituted pyrazolo[4,3-d]pyrimidines represented by the general formula I and pharmaceutically acceptable salts thereof, wherein R3 is an optionally substituted alkyl, cyclo... | 06/29/2010 |
| 7741330 | Pyrazolo-pyrimidine inhibitors of Bruton's tyrosine kinase Described herein are kinase inhibitor compounds, methods for synthesizing such inhibitors, and methods for using such inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate inhibitor of a prot... | 06/22/2010 |
| 7737156 | Selective phosphodiesterase 9A inhibitors as medicaments for improving cognitive processes The invention relates to the use of selective phosphodiesterase 9A (PDE9A) inhibitors for producing medicaments for improving perception, concentration, cognitive processes, learning and/or memory. ... | 06/15/2010 |
| 7732454 | Inhibitors of Bruton's tyrosine kinase Disclosed herein are imidazo[1,5-f][1,2,4]triazine compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). The imidazo[1,5-f][1,2,4]triazine compounds described are irreversible inhibitors of Btk. Methods for the preparation of the imidazo[1,5-f][1,2... | 06/08/2010 |
| 7718662 | Pyrazolo-pyrimidine inhibitors of bruton's tyrosine kinase Described herein are kinase inhibitor compounds, methods for synthesizing such inhibitors, and methods for using such inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate inhibitor of a prot... | 05/18/2010 |
| 7642267 | Benzimidazole and pyridylimidazole derivatives This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I. The invention is particularly related to such compounds that bind with high selectivity and high affinity to the ben... | 01/05/2010 |
| 7629349 | Pyrazolo [3,4-d] pyrimidine derivatives and their use as purinergic receptor antagonists Pharmaceutical compositions and their uses comprising compounds of formula (I): wherein: R1 is selected from: alkyl, alkoxy, aryloxy, alkylthio, arylthio, aryl, halogen, CN, NR6R7, NR5 | 12/08/2009 |
| 7625906 | Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto The present invention relates to certain fused aryl and heteroaryl derivatives of Formula (I) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the prophylaxis or treatment of ... | 12/01/2009 |
| 7625907 | Reactive oxygen generating enzyme inhibitor with nitric oxide bioactivity and uses thereof A reactive oxygen generating enzyme inhibitor with NO donor bioactivity, e.g., nitrated allopurinol, is useful to treat heart failure, stable angina, ischemic disorder, ischemic reperfusion injury, atherosclerosis, sickle cell disease, diabetes, Alzheimer's disease,... | 12/01/2009 |