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| Number | Title | Issue Date |
| 8158785 | 5,7-disubstituted[1.3]thiazolo [4,5-D] pyrimidin-2(3H)-amine derivatives and their use in therapy There are disclosed novel 5-substituted 7-amino-[1,3]thiazolo[4,5-d]pyrimidine derivatives of formula (I) wherein R1, R2, R3, R4 and n are as defined in the specification, and pharmaceutically acceptable salts thereof, tog... | 04/17/2012 |
| 7781581 | Process for the preparation of 5-amino-3H-thiazolo[4,5-d]pyrimidin-2-one The present invention relates to a process for the preparation of 5-amino-3H-thiazolo[4,5-d]pyrimidin-2-one which is a useful intermediate in the preparation of certain thiazolo[4,5-d]pyrimidine nucleosides. The process com... | 08/24/2010 |
| 7560552 | Thiopyrimidine and isothiazolopyrimidine kinase inhibitors Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using th... | 07/14/2009 |
| 7439246 | Fused heterocyclic kinase inhibitors In general, the instant invention comprises compounds of Formulas I and II including pharmaceutically acceptable salts thereof. The compounds of the invention are useful as protein kinase inhibitors and therefore are useful... | 10/21/2008 |
| 7427616 | Condensed pyridines and pyrimidines with tie2 (TEK) activity A compound of the Formula (I), wherein A together with the carbon atoms to which it is attached forms a fused 5-membered heteroaryl ring, wherein said heteroaryl ring contains 1 or 2 heteroatoms selected from O, N and S, and wherein the 5-membered ring containing G ... | 09/23/2008 |
| 7371766 | Curcumin analogs with anti-tumor and anti-angiogenic properties The present invention is directed to curcumin analogs exhibiting anti-tumor and anti-angiogenic properties, pharmaceutical formulations including such compounds and methods of using such compounds. ... | 05/13/2008 |
| 7351826 | Aryl acid pyrimidinyl methyl amides, pyridazinyl methyl amides and related compounds The invention provides compounds of Formula (I) that bind to GABAA receptors. In the above formula, variables are defined herein. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly... | 04/01/2008 |
| 7321033 | 3-B-D-ribofuranosylthiazolo [4,5-] pyrimidine nucleosides and uses thereof The invention is directed to 3-β-D-ribofuranosylthiazolo[4,5-d]pyridimine nucleosides and pharmaceutical compositions containing such compounds that have immunomodulatory activity. The invention is also directed to the therapeutic or prophylactic use of such compou... | 01/22/2008 |
| 7294633 | Oxazolo-and furopyrimidines and their use in medicaments against tumors The invention relates to pharmaceutically acceptable compounds of formula I, wherein the radicals have the significances given in the description. Compounds of formula I are useful against tumor diseases ... | 11/13/2007 |
| 7262186 | Substituted pyrazolo[3,4-d] pyrimidinones as a mitotic kinesin inhibitor The present invention relates to azolopyriniidinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which ... | 08/28/2007 |
| 7262187 | Substituted oxazolo- and thizaolopyrimidinones as a mitotic kinesin inhibitor The present invention relates to azolopyrimidinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which c... | 08/28/2007 |
| 7253154 | Substituted thiazolopyrimidines as xanthine oxidase inhibitors The invention relates to compounds of the following formula (I) or their salts: in which R1 represents OR4 or others, in which R4 is an alkyl group having 1-8 carbon atoms which m... | 08/07/2007 |
| 7244727 | Fused bicyclic nitrogen-containing heterocycles Compounds, pharmaceutical compositions and methods that are useful in the treatment or prevention of metabolic and cell proliferative diseases or conditions are provided herein. In particular, the invention provides compounds which modulate the activity of proteins ... | 07/17/2007 |
| 7179915 | Method for producing highly pure tris-ortho metalated organoiridium compounds The present invention describes a process for preparing highly pure tris-ortho-metalled organoiridium compounds and pure organometallic compounds of this type, especially compounds of the d8 metals, which may find use as coloring components in the near fu... | 02/20/2007 |
| 7176215 | Bicyclic oxopyridine and oxopyrimidine derivatives Compounds of formulae (1a) and (1b) are described: in which the dashed line represents an optional bond; A is a —N═ atom or a —N(Rb)—, —C(Rb)═ or —C(Rb)(RC)— group; Ra, Rb and Rc ... | 02/13/2007 |
| 7141564 | Nitrogen-containing bicyclic heterocycles for use as antibacterials Cyclohexane and cyclohexene derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly man. ... | 11/28/2006 |
| 7115739 | Triazole compounds useful as protein kinase inhibitors This invention describes novel triazole compounds of formula IX: wherein Z1 is nitrogen or CR9 and Z2 is nitrogen or CH, provided that at least one of Z1 and Z2 | 10/03/2006 |
| 7105524 | Pesticidal and parasiticidal di-and trifluorosubstituted alkene compounds Di- and trifluorosubstituted alkene compounds of formula I wherein X is hydrogen or fluorine; Y is oxygen, NR1 or S(O)m; R1 is hydro... | 09/12/2006 |
| 7067657 | Thiazolopyrimidine derivatives and use thereof as antagonists of the CXCR1 receptor Provided herein is a compound having the formula (Ia): wherein said compounds are useful for the treatment or prophylaxis of neurodegenerative disorders, demyelinating disease and pain. ... | 06/27/2006 |
| 7053214 | β-sheet mimetics and composition and methods relating thereto Compounds having the following structure: including pharmaceutically acceptable salts and stereoisomers thereof, wherein A, A′, B, X, Y, R2, R3, R4 and R5 are as defi... | 05/30/2006 |
| 7022850 | Bicyclicpyrimidones and their use to treat diseases The present invention is directed to dihydropyrimidones having formula I or II and methods of using them to induce mitotic arrest, thereby making them useful as anti-cancer agents and other diseases that can be treated by inducing mitotic arrest. | 04/04/2006 |
| 6969713 | Piperidine and piperazine acetamide derivatives The invention provides piperidine and piperazine derivatives of general formula (I), processes for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy | 11/29/2005 |
| 6958343 | Thiazolopyrimidines and their use as modulators of chemokine receptor activity Compounds of formula (I): are described herein. The compounds can be used, for example, in the treatment of chemokine mediated diseases, including inflammatory diseases such as psoriasis and COPD. ... | 10/25/2005 |
| 6949643 | Thiazolopytimidines and their use as modulators of chemokine receptor activity The invention provides certain thiazolopyrimidine compounds of formula (I) or a pharmaceutically acceptable salt or solvate thereof: in which: A is a group of formula (a) or (b): processes and intermediates used in their preparation, pharmaceutical compositions cont... | 09/27/2005 |
| 6930101 | Thiazolopyrimidines useful as TNFα inhibitors The invention provides derivatives of thiazolo[4,5-dl]pyrimidine and their use as inhibitors of proinflammatory cytokines. ... | 08/16/2005 |
| 6891043 | Inhibitors of fatty acid amide hydrolase Potent inhibitors of fatty acid amide hydrolase (FAAH) are constructed having K1's below 200 pM and activities 102-103 times more potent than the corresponding trifluoromethyl ketones. The potent inhibitors combine several features, ... | 05/10/2005 |
| 6841549 | Condensed imidazole compounds and a therapeutic agent for diabetes mellitus The present invention provides a preventive or therapeutic agent for diabetes mellitus and diabetic complications, which is a new type based on an adenosine A2 receptor antagonist action. That is, it provides a novel condensed imidazole compound which has an ... | 01/11/2005 |
| 6835726 | Pyrimidine derivatives Compounds and compositions are provided which are useful for the treatment of viral infections, particularly human Cytomegalovirus infection. The compounds include novel pyrimidine-based derivatives. ... | 12/28/2004 |
| 6828326 | Pyrimidinone fused bicyclic metalloproteinase inhibitors The present invention relates to fused bicyclic metalloproteinase inhibitors of the formula wherein A, B, X, Y, and R1 are as defined in the specification, and to pharmaceutical comp... | 12/07/2004 |
| 6790850 | Thiazolo(4,5-d)pyrimidine compounds The invention provides certain thiazolopyrimidine compounds of formula (I) or a pharmaceutically acceptable salt or solvate thereof; processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy. | 09/14/2004 |
| 6777416 | Isoxazolo pyrimidinones and the use thereof The invention relates to novel isoxazolo pyrimidinones of general formula (I), a method for producing the same and the pharmaceutical use thereof. ... | 08/17/2004 |
| 6734180 | NF-κB inhibitor comprising an indan derivative as an active ingredient An inhibitor of NF-κB comprising as an active ingredient an indan derivative represented by the general formula (I) or a salt thereof. ... | 05/11/2004 |
| 6617330 | Pyrimidin-4-enamine as fungicide Novel pyrimidine derivatives of formula I ##STR1## as well as possible isomers and mixtures of isomers thereof. The novel compounds have plant-protective properties and are suitable for protecting plants against infestations by phytopathogenic microorganisms ... | 09/09/2003 |
| 6589958 | Isoxazolo [4,5-d] pyrimidines as CRF antagonists The present invention describes novel isoxazolo[1,5-a]pyrimidines of formula: ##STR1## wherein R is an aromatic or heteroaromatic ring, or pharmaceutically acceptable salt form thereof, which are useful as CRF antagonists.... | 07/08/2003 |
| 6528513 | Pyrimidine derivatives Compounds and compositions are provided which are useful for the treatment of viral infections, particularly human Cytomegalovirus infection. The compounds include novel pyrimidine-based derivatives.... | 03/04/2003 |
| 6525056 | Heterocyclyl-substituted ring-fused pyridines and pyrimidines as corticotropin releasing hormone (CRH) antagonists, useful for treating cns and stress-related disorders Corticotropin releasing factor (CRF) antagonists of Formula (I): ##STR1## and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding disorders as wel... | 02/25/2003 |
| 6410628 | Photoactivatable nitrogen-containing bases based on alpha-amino ketones The invention relates to organic compounds having a molecular weight of less than 1000 comprising at least one structural unit of the formula (I) ##STR1## in which R1 is an aromatic or heteroaromatic radical which is capable of absorbing light ... | 06/25/2002 |
| 6376667 | Solid phase synthesis of heterocycles Methods and compounds for the synthesis of heterocycles, including pyrimidine-2,4-diones, are disclosed. Also disclosed are solid supports useful for solid phase synthesis, and methods for making the solid supports.... | 04/23/2002 |
| 6281227 | Sulfonic acid sulfonylamino n-(heteroaralkyl)-azaheterocyclylamide compounds The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibit... | 08/28/2001 |
| 6228867 | Antagonists of gonadotropin releasing hormone There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men an... | 05/08/2001 |
