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| Number | Title | Issue Date |
| 8088923 | Cyclic-fused beta-lactones and their synthesis The present invention provides a concise synthetic method for generating lactam-fused beta-lactones that feature, in some embodiments, a tertiary fused carbinol, quaternary carbons, and a reactive beta-lactone moiety available for further reactions. The present inve... | 01/03/2012 |
| 7576213 | Vinylogous 4-pyrones and their use in promoting plant growth A hitherto unknown class of chemical compounds, 2H-furo[2,3-c]pyran-2-ones including derivatives and analogues thereof are disclosed herein. Methods for making compounds within said class are disclosed herein and includes, without limitation, at least the intermedia... | 08/18/2009 |
| 7498438 | Fused ring NKantagonists A compound having the general structure shown in Formula 1: or pharmaceutically acceptable salts and/or solvates thereof are useful in treating diseases or conditions mediated by NK1 receptors, for example variou... | 03/03/2009 |
| 7439247 | Bicyclic pyridine and pyrimidine P38 kinase inhibitors The present invention discloses compounds corresponding to formula wherein A, R, X, Y, R, R1 and R2 are as defined above, pharmaceutical formulations, methods of making and uses thereof. ... | 10/21/2008 |
| 7423152 | Process for the manufacture of intermediates in camptothecin production The present invention provides a process for the manufacture of the compound of formula (1): which is a key intermediate in the manufacture of camptothecin (CPT). This compound continues to serve as an attractive and promis... | 09/09/2008 |
| 7407972 | Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade The present invention provides compounds of Formula (I): wherein A, B, C, G, and W1 have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful to treat thro... | 08/05/2008 |
| 7371863 | Method for manufacture of THIP The present invention relates to a new method of preparing gaboxadol (THIP), which is useful for treating sleep disorders. In particular a method of preparing THIP comprising reacting a compound of formula (8b) or a salt thereof with an acid, typically a mineral aci... | 05/13/2008 |
| 7371752 | Aryl fused substituted 4-oxy-pyridines Disclosed are compounds of the formula: wherein X, Q, W and are as defined herein. These compounds are agonists, antagonists or inverse agonists for GABAA brain recepto... | 05/13/2008 |
| 7365079 | Azole derivatives The present invention relates to a compound of the formula (I): wherein Az is a group comprising a monocyclic azole or a bicyclic aromatic ring of the same or different fused azoles; T, U, V and W are independently methine ... | 04/29/2008 |
| 7323494 | Compounds and methods Disclosed is a compound of having the formula: pharmaceutically acceptable salts or solvates thereof and pharmaceutical compositions containing the same, wherein the structural variables ... | 01/29/2008 |
| 7304072 | Spiro compounds Compounds represented by the general formula (I) wherein Ar1 represents an aryl or heteroaryl which may be substituted; n represents 0 or 1; T, U, V and W each independently represent a nitrogen atom o... | 12/04/2007 |
| 7262300 | Polymorphic forms of a GABAagonist Two new crystalline monhydrates and two new crystalline anhydrates of gaboxadol are disclosed together with methods for preparing them. ... | 08/28/2007 |
| 7230009 | Pyridoxal analogues and methods of treatment Pyridoxal analogues can be useful for treating B6 deficiency and related diseases; cardiovascular and related diseases; melanoma and related diseases; and symptoms thereof. One such analogue is a compound of the formula: | 06/12/2007 |
| 7220868 | Process for the preparation of novel dyes for use in imaging members There are described novel rhodamine dye compounds and imaging members and imaging methods, including thermal imaging members and imaging methods, utilizing the compounds. The dye compounds exhibit a first color when in the crystalline form and a second color, differ... | 05/22/2007 |
| 7220860 | Camptothecin analogs and methods of preparation thereof A compound has the formula in racemic form, enantiomerically enriched form or enantiomerically pure form. R6 is preferably —Si(R8R9R10) or —(R7)Si(R... | 05/22/2007 |
| 7205401 | Compositions and methods for separating amines and amino acids from their counter-enantiomers Diketo- and pyridine-containing chiral crown ligands having at least two chiral bulky groups attached to two different chiral carbon atoms of the crown that are covalently bonded to or coated on suitable solid supports, and further coated by hydrophobic organic solv... | 04/17/2007 |
| 7196093 | Reversible inhibitors of SAH hydrolase and uses thereof 1. The present invention provides compositions and methods for reversibly inhibiting S-adenosyl-L-homocysteine (SAH) hydrolase. The compounds of the present invention can be used as an anti-hemorrhagic viral infection agent, an immunosuppressant, a homocysteine lowe... | 03/27/2007 |
| 7132418 | Peptidyl heterocyclic ketones useful as tryptase inhibitors The present invention relates to a series of peptidyl heterocyclic ketones which are inflammatory cell serine protease inhibitors and their compositions and methods for the prevention and treatment of a variety of immunomediated inflammatory disorders. More particul... | 11/07/2006 |
| 7087756 | Isoxazolopyridinones The invention provides compounds of formula I, wherein X, Y, R1, R2, and R3 are as defined in the description, and the preparation thereof. The compounds of formula I are useful as pharmaceuticals. ... | 08/08/2006 |
| 7087601 | Metabotropic glutamate receptor-5 modulators Phenyl compounds substituted at the 1-position with a fused bicyclo moeity formed from a five-membered heterocycle fused to a six-membered carbocycle, to a six-membered aryl, or to a six-membered hetaryl, and further optionally substituted at the 3,4 positions, are ... | 08/08/2006 |
| 7067515 | Quinuclidines-substituted-multi-cyclic-heteroaryls for the treatment of disease The invention provides compounds of Formula I: where in W is These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or... | 06/27/2006 |
| 7053219 | Isoxazolopyridone derivatives and their use The invention relates to isoxazolopyridone derivatives of a formula (I-a): wherein R1a represents an optionally-substituted heteroaryl or phenyl group, R2a represents an optionally-substitut... | 05/30/2006 |
| 6982333 | Intermediates in the synthesis of camptothecin and related compounds and synthesis thereof The present invention provides a short, convergent total synthesis of camptothecin and related compounds which consists of a novel 4+1 radical annulation. The present invention also provides novel chemical intermediates for such 4+1 radical annulations. ... | 01/03/2006 |
| 6927293 | Tyrosine kinase inhibitors The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogen... | 08/09/2005 |
| 6911543 | Azabicyclic-substituted fused-heteroaryl compounds for the treatment of disease The invention provides compounds of Formula I: wherein Azabicyclo is These compounds may be in the form of pharmaceutical salts or co... | 06/28/2005 |
| 6878705 | 4-oxo-4,7-dihydrofuro[2,3-b]pyridine-5-carboxamide antiviral agents The invention provides a compound of formula I: wherein G, R2, R3, and R4 have any of the values defined in the specification, or a pharmaceutically acceptable salt thereof, as well as ... | 04/12/2005 |
| 6867217 | Substituted polycyclic aryl and heteroaryl pyridones useful for selective inhibition of the coagulation cascade The invention relates to substituted polycyclic aryl and heteroaryl pyridone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety... | 03/15/2005 |
| 6841559 | Pyridinones to treat and prevent bacterial infections Novel pyridinones and their derivatives which are effective in treating or preventing Gram-negative bacterial infections are provided. The pyridinones are stable and easily derivatized; the methods by which these derivatizations occur is described. Two regioselectiv... | 01/11/2005 |
| 6833370 | Heterocycle substituted aminoazacycles useful as central nervous system agents Heterocyclic substituted aminoazacyclic compounds of formula I Z—R3 I, wherein Z is a defined aminoazacycle and R3 is a defined heterocycle moiety, pharmaceutical compositions of these compounds, and use of said comp... | 12/21/2004 |
| 6809203 | Oxazolo, thiazolo and selenazolo [4,5-C]-quinolin-4-amines and analogs thereof Thiazolo-, oxazolo- and selenazolo[4,5-c]quinolin-4-amines and analogs thereof are described including methods of manufacture and the use of novel intermediates. The compounds are immunomodulators and induce cytokine biosynthesis, including interferon and/or tumor b... | 10/26/2004 |
| 6803372 | Spiro compounds Compounds of the general formula (I): wherein Ar1 represents optionally substituted aryl or heteroaryl; n represents 0 or 1; T, U, V, and W each independently represent nitrogen atom or o... | 10/12/2004 |
| 6797717 | Anilide compounds and drugs containing the same The invention relates to a novel anilide compound and a pharmaceutical composition comprising the same. The invention relates to a compound represented by the following general formula: represents a divalent residue of b... | 09/28/2004 |
| 6794393 | Tyrosine kinase inhibitors The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogen... | 09/21/2004 |
| 6762301 | Analogues of camptothecin, their use as medicaments and the pharmaceutical compositions containing them A process for the preparation of a compound of the formula wherein the substituents are defined as set forth in the specification comprising reacting a compound of the formula | 07/13/2004 |
| 6753331 | Heterocyclic derivatives which inhibit factor Xa The invention relates to heterocyclic derivatives of formula (I), or pharmaceutically-acceptable salts thereof, which possess antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals. The invention also rela... | 06/22/2004 |
| 6635633 | Substituted pyrazoles Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S are described.... | 10/21/2003 |
| 6620937 | Intermediates in the synthesis of camptothecin and related compounds and synthesis thereof The present invention provides a short, convergent total synthesis of camptothecin and related compounds which consists of a novel 4+1 radical annulation. The present invention also provides novel chemical intermediates for such 4+1 radical annulations.... | 09/16/2003 |
| 6583161 | Benzenesulfonamides and benzamides as therapeutic agents The invention provides compounds, compositions and methods relating to novel aromatic derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particul... | 06/24/2003 |
| 6545021 | Use of substituted-1,5-dideoxy-1,5-imino-D-glucitol compounds for treating hepatitis virus infections N-Substituted-1,5-dideoxy-1,5-imino-D-glucitol compounds of Formula I are effective in treatment of hepatitis infections, including hepatitis B and hepatitis C. In treating hepatitis infections, the compounds of Formula I may be used alone, or in combinat... | 04/08/2003 |
| 6525197 | Methods for preparing macrocyclic products by ring-closing diyne metathessis The present invention relates to methods for preparing macrocyclic products having 9 or more ring atoms by ring-closing diyne metathesis of suitable diyne substrates. The diyne substrates can be converted into cycloalkynes or into cycloalkadiynes by cyclo... | 02/25/2003 |
