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| Number | Title | Issue Date |
| 7893279 | Cyclohexanecarboxylic acid compound The present invention provides a VLA-4 inhibitor having high water-solubility and excellent long-term stability; i.e., sodium trans-4-[1-[2,5-dichloro-4-[(1-methyl-1H-3-indolylcarbonyl)amino]phenylacetyl]-(4S)-methoxy-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylate ... | 02/22/2011 |
| 7847106 | Process for the preparation of macrocyclic compounds The present invention relates to a new process for the preparation of tripeptides of formula I wherein R1 is an amino protecting group and X is a halogen atom and wherein the tipeptide contains two olefinic moiet... | 12/07/2010 |
| 7842819 | Derivatives for modulation of ion channels Sulfonamide derivatives act as ion channel antagonists. The compositions are useful for treating or relieving pain-related conditions. ... | 11/30/2010 |
| 7619094 | Ketoamides with cyclic P4's as inhibitors of NS3 serine protease of hepatitis C virus The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of us... | 11/17/2009 |
| 7579483 | Process for preparing 7-(acryloyl)indoles The present invention involves a process for preparing substituted indoles, such as DTSI involving two sequential cross-coupling reactions. ... | 08/25/2009 |
| 7566790 | Intermediates and the synthesis of modified carbocyanine dyes and their conjugates Chemically reactive carbocyanine dyes incorporating an indolium ring moiety that is substituted at the 3-position by a reactive group or by a conjugated substance, and their uses, are described. Conjugation through this position results in spectral properties that a... | 07/28/2009 |
| 7528262 | Indole derivatives as histamine 3 receptor inhibitors for the treatment of cognitive and sleep disorders, obesity and other CNS disorders This invention relates to compounds having pharmacological activity, to compositions containing these compounds, and to a method of treatment employing the compounds and compositions. More particularly, this invention concerns certain indole derivatives and their sa... | 05/05/2009 |
| 7442805 | Substituted sulfonamide-indoles The present invention relates generally to substituted sulfonamide indoles such as substituted sulfonamide indoles, and methods of using them. ... | 10/28/2008 |
| 7439371 | Indol kinase inhibitors The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation. ... | 10/21/2008 |
| 7435832 | Crystals including a malic acid salt of a 3-pyrrole substituted 2-indolinone, and compositions thereof The present invention provides crystals, and compositions thereof, wherein the crystals include a malic acid salt of N-[2-(diethylamino)ethyl]-5-[(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide. Methods of preparing such ... | 10/14/2008 |
| 7429611 | Indole inhibitors of 15-lipoxygenase The present invention provides indole inhibitors of 15-LO, pharmaceutical compositions containing such inhibitors and methods for treating diseases related to the 15-LO cascade using such compounds and compositions. ... | 09/30/2008 |
| 7429661 | Intermediates for linezolid and related compounds The present invention provides a novel process for preparation of 5 aminomethyl substituted oxazolidinones, key intermediates for oxazolidinone antibacterials including linezolid. Thus, the key intermediate of linezolid is prepared by a) reacting N-[3-Chloro-2-(R)-h... | 09/30/2008 |
| 7405306 | 3-Heteroaryl-3,5-dihydro-4-oxo-4H-pyridazino[4,5-b]indole-1-acetamide derivatives, their preparation and their application in therapeutics The invention discloses and claims therapeutic uses of compounds of general formula (I) Wherein X, R1, R2 and R3 are as described herein. The invention further discloses processes for prepar... | 07/29/2008 |
| 7405300 | Substituted indoles as inhibitors of poly (ADP-ribose) polymerase (PARP) The present invention relates to a series of substituted indole derivatives of the formula I: wherein R, R1, R2, R3, R4, X and Y are as defined herein. Th... | 07/29/2008 |
| 7375118 | Phenyl-indole compounds for modulating IgE and Inhibiting cellular proliferation The present invention is directed to small molecule inhibitors of the IgE response to allergens, which are useful in the treatment of allergy and/or asthma or any diseases where IgE is pathogenic. This invention also relates to phenyl-indole molecules that are cellu... | 05/20/2008 |
| 7358364 | Substituted carboxylic acids The present invention relates to compounds and pharmaceutically acceptable salts of formula (I): which are useful in the treatment of metabolic disorders related to insulin resistance or hyperglycemia. These compounds inclu... | 04/15/2008 |
| 7358014 | Electrophotographic organophotoreceptors with novel charge transport compounds A novel charge transport compound, a novel process using that novel compound and an organophotoreceptor includes: (a) a novel charge transport compound having the formula | 04/15/2008 |
| 7348351 | Substituted 3-alkyl and 3-arylalkyl -indol-1yl acetic acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1) The invention formula substituted 3-alkyl and 3-arylalkyl 1H indol-1yl acetic acid derivatives which are useful as inhibitors of plasminogen activator inhibitor (PAI-1) useful for treating fibrinolytic disorders, the compounds having the structure ... | 03/25/2008 |
| 7345081 | Azabicyclo-octane inhibitors of IAP The invention provides novel inhibitors of IAP that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: X1 and X2 are independently O or S; L is... | 03/18/2008 |
| 7342005 | Antibiotic compounds The present invention relates to carbapenems and provides a compound of the formula (I): or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof wherein: R1 ... | 03/11/2008 |
| 7332487 | Nitrogen-containing 5-membered ring compound The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: wherein symbols in the formula have the following meanings; ... | 02/19/2008 |
| 7332515 | Indole-amid derivatives which possess glycogen phosphorylase inhibitory activity Heterocyclic amides of formula (1) and pharmaceutically acceptable salts or pro-drugs thereof wherein variable groups are as described herein; which possess glycogen phosphorylase inhibitory activity and accordin... | 02/19/2008 |
| 7323488 | Chromogenic enzyme substrates This invention provides novel chromogenic enzyme substrates which are indoxyl β-D-ribofuranosides. A process for their production is provided. Methods for detecting β-D-ribofuranosidase activity are given. The advantages of these novel compounds includes: detectin... | 01/29/2008 |
| 7317025 | Non-peptidic NPY Y2 receptor inhibitors The invention provides novel non-peptidic NPY Y2 receptor inhibitors useful in treating or preventing: anxiolytic disorders or depression; injured mammalian nerve tissue; conditions responsive to treatment through administration of a neurotrophic factor; neurologica... | 01/08/2008 |
| 7300928 | Benzimidazolidinone derivatives as muscarinic agents Benzimidazolidinone derivative compounds, which increase acetylcholine signaling or effect in the brain, and highly selective muscarinic agonists, particularly for the M1 and/or M4 receptor subtypes, pharmaceutical compositions comprising the s... | 11/27/2007 |
| 7291644 | Indole derivatives Compounds represented by formula (I) wherein all symbols represent the same meanings as described in specification and salts thereof. Since the compound represented by the formula (I) binds and antagonize... | 11/06/2007 |
| 7288662 | Process for the preparation of eletriptan The present invention provides an improved process for the preparation of the anti-migraine drug, (R)-5-(2-benzenesulphonylethyl)-3-N-methylpyrrolidin-2-ylmethyl)-1H-indole (eletriptan), available commercially as the hydrobromide salt, and an intermediate and dimer-... | 10/30/2007 |
| 7288563 | Substituted bicycloalkylamine derivatives as modulators of chemokine receptor activity The present application describes modulators of MCP-1 of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein X, Z, a, b, c, d, bond g, n, s, R1, R2, R4 | 10/30/2007 |
| 7282510 | Small molecule inhibitors of rotamase enzyme activity This invention relates to neurotrophic N-glyoxyl-prolyl ester compounds having an affinity for FKBP-type immunophilins, their preparation and use as inhibitors of the enzyme activity associated with immunophilin proteins, and particularly inhibitors of peptidyl-prol... | 10/16/2007 |
| 7273885 | Inhibitors of serine proteases, particularly HCV NS3-NS4A protease The present invention relates to compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents.... | 09/25/2007 |
| 7271265 | Cyanine compounds and their application as quenching compounds The present invention provides methods and non-fluorescent carbocyanine quencher compounds having the general formula: Wherein the A moiety is a substituted pyridinium, unsubstituted pyridinium, substituted quino... | 09/18/2007 |
| 7271192 | Substituted 2-pyrrolidine-2-yl-1H-indole compounds Novel 2-pyrrolidin-2-yl-1H-indole compounds corresponding to formula (I) wherein R1, R2, R3 and R4 have the meanings given in the description, and pharmaceutical compos... | 09/18/2007 |
| 7265148 | Substituted pyrrole-indoles The present invention relates generally to substituted pyrrole-indoles such as substituted pyrrole-indoles, and methods of using them. ... | 09/04/2007 |
| 7256188 | 3-aminoalkyl-2-aryl-indole derivatives and their use as GnRH antagonists The present invention relates to compounds of formula I which are antagonists of gonadotropin releasing hormone (GnRH) activity. The invention also relates to pharmaceutical formulations, the use of a compound of the present invention in the manufacture of a medicam... | 08/14/2007 |
| 7232906 | Substituted pyrrolines as kinase inhibitors The present invention is directed to novel substituted pyrroline compounds useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase or dual-kinase mediated disorder. ... | 06/19/2007 |
| 7223783 | Indolinone derivatives Compounds of formula (I) in which R1, R2, R3 and R4 have the meanings given in the specification, are receptor tyrosine kinase inhibitors useful in the treatment of pro... | 05/29/2007 |
| 7214700 | (2-Oxindol-3-ylidenyl) acetic acid derivatives and their use as protein kinase inhibitors The present invention relates to (2-oxindol-3-ylidenyl)acetic acid derivatives which modulate the activity of protein kinases and are therefore useful in the prevention and treatment of protein kinase related cellular disorders such as cancer. ... | 05/08/2007 |
| 7208566 | Imide-linked maleimide and polymaleimide compounds The invention is based on the discovery that a remarkable improvement in the performance of maleimide thermosets can be achieved through the incorporation of imide-extended mono-, bis-, or polymaleimide compounds. These imide-extended maleimide compounds are readily... | 04/24/2007 |
| 7192957 | Compounds as inhibitors of hepatitis C virus NS3 serine protease The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of us... | 03/20/2007 |
| 7186739 | Stabilized activated derivatives of carbamic acid, their process of preparation and their use for the preparation of ureas A carbamate compound is disclosed. ... | 03/06/2007 |