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| Number | Title | Issue Date |
| 8153821 | Compounds The present invention related to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to novel salts thereof, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to met... | 04/10/2012 |
| 8076493 | 3-carboxy-2-oxo-1-pyrrolidine derivatives and their uses The present invention relates to 3-carboxy-2-oxo-1-pyrrolidine derivatives of formula (I), geometrical isomers, enantiomers, diastereoisomers, pharmaceutically acceptable salts and all possible mixtures thereof, and processes using them. | 12/13/2011 |
| 8030501 | Process for producing optically active 3-amino nitrogen-containing compounds Aiming at production of an optically active 3-amino nitrogen-containing compound which is useful as an intermediate in synthesis of medicines and pesticides, in particular, an optically active 1-protected-3-aminopyrrolidine derivative, from an inexpensive and readil... | 10/04/2011 |
| 8003808 | 3-hydrazino-2,5-dioxopyrrolidine-3-carboxylates, process for production of the same, and use of the same The present invention provides 3-hydrazino-2,5-dioxopyrrolidine-3-carboxylates of the formula (I): wherein R1 is a C1-6 alkyl group, etc., R2 is a hydrogen atom or a COOR3 group, ... | 08/23/2011 |
| 7838686 | Preparation of pregabalin and related compounds Materials and Methods for preparing (S)-(+)-3-aminomethyl-5-methyl-hexanoic acid and structurally related compounds via enzymatic kinetic resolution are disclosed. ... | 11/23/2010 |
| 7807846 | Method for producing succinimide compound There is provided a method for producing a succinimide compound. The method for producing a succinimide compound of formula (3) comprises reacting an aminomalonic ester compound of formula (1) with a compound of formula (2) in a solvent in the presence of a base, wh... | 10/05/2010 |
| 7626042 | O-substituted hydroxyaryl derivatives A medicament having inhibitory activity against NF-κB activation which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, a... | 12/01/2009 |
| 7439257 | Aryloxyalkylcarbamate-type derivatives, preparation method thereof and use of same in therapeutics The invention relates to a compound of formula (I): Wherein m, n, X, Y, R1, R2, R3 and R4 are as defined herein. The invention also relates to the use of same in therapeutics. | 10/21/2008 |
| 7405297 | Process for preparing inhibitors of nucleoside metabolism A process of preparing a compound of the formula (I) wherein B is chosen from OH, NH2, NHR, H or halogen; D is chosen from OH, NH2, NHR, H halogen or SCH3; R is an optionally substituted alk... | 07/29/2008 |
| 7335680 | Pyrrolidine derivatives as prostaglandin modulators Substituted pyrrolidine compounds are provided, and methods of treatment and pharmaceutical composition that utilize or comprise one or more such compounds. Compounds of the invention are useful for a variety of therapies, including treating or preventing preterm la... | 02/26/2008 |
| 7323447 | Hepatitis C virus inhibitors The present disclosure is generally directed to antiviral compounds, and more specifically directed to compounds which inhibit the function of the NS3 protease (also referred to herein as “serine protease”) encoded by Hepatitis C virus (HCV), compositions compri... | 01/29/2008 |
| 7268236 | Method of heightening optical purity of 1-benzyl-3-aminopyrrolidine and salt for used therein The present invention provides a method to improve the optical purity of 1-benzyl-3-aminopyrrolidine having a low optical purity using an inexpensive agent via a simple procedure. The present invention provides a method for improving the optical purity of 1-benzyl-3... | 09/11/2007 |
| 7256257 | Pentapeptide compounds and uses related thereto Pentapeptide compounds are disclosed. The compounds have biological activity, e.g., cytotoxicity. Prodrugs having targeting groups and pentapeptide moieities, as well as precursors thereof are also disclosed. For example, precursors having a reactive linker that can... | 08/14/2007 |
| 7253169 | Aza compounds, pharmaceutical compositions and methods of use The present invention relates to N-substituted cyclic aza compounds, pharmaceutical compositions comprising such compounds, and methods of their use for effecting neuronal activities. ... | 08/07/2007 |
| 7241757 | Amidino derivatives and their use as thrombin inhibitors There is provided compounds of formula I wherein R1, Rx, Y, Ry, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases... | 07/10/2007 |
| 7211677 | Process for preparing inhibitors of nucleoside metabolism A process of preparing a compound of the formula (I) wherein B is chosen from OH, NH2, NHR, H or halogen; D is chosen from OH, NH2, NHR, H halogen or SCH3; R is an optionally subs... | 05/01/2007 |
| 7199243 | Piperidine compounds useful as PPAR activators PPAR alpha activators, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol ... | 04/03/2007 |
| 7169937 | Dithiocarbamic esters The present invention relates to dithiocarbamic esters, their preparation and their use for regulating the degree of polymerization during the polymerization of monomers, such as during the polymerization of chloroprene to give polychloroprene, and during the polyme... | 01/30/2007 |
| 7166600 | Thiocarbamate inhibitors of alpha-4 integrins The invention provides novel thiocarbamate alpha-4 inhibitors of the general formula (I) that are resistant to metabolism having improved half-life and/or clearance properties compared to corresponding carbamate compounds wherein substituents L, X, Y, Z, R1 | 01/23/2007 |
| 7157585 | Serine protease inhibitors Compounds of formula (I) where R5, R6a, each X, L, Cy and Lp are as defined in the specification, are tryptase inhibitors useful as antiinflammatory agents. ... | 01/02/2007 |
| 7153883 | Carboxylic acids and carboxylic acid isosteres of N-heterocyclic compounds This invention relates to novel N-heterocyclic carboxylic acids and carboxylic acid isosteres, their preparation and use for treating neurological disorders including physically damaged nerves and neurodegenerative diseases, for treating alopecia and promoting hair ... | 12/26/2006 |
| 7148362 | Process for the preparation of enantiopure pyrrolidin-2-one derivatives The present invention relates to a process for the preparation of enantiopure intermediates useful in the synthesis of valuable pharmaceutically active compounds, e.g. MAOB inhibitors, and to novel intermediates of formulae I and II | 12/12/2006 |
| 7132551 | Ligands for monoamine receptors and transporters, and methods of use thereof One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine tra... | 11/07/2006 |
| 7109196 | 1,8 Naphthyridine derivatives and their use to treat diabetes and related disorders The invention relates generally to naphthyridine derivatives of the formula wherein one of U, X, Y and Z is nitrogen and the others are C—R, where R is hydrogen or a substituent. More specifically, the inventio... | 09/19/2006 |
| 7071211 | Small organic molecules that increase the activity of gelatinase a in ocular cells Small organic molecules capable of effecting a “pharmacological trabeculocanalotomy” in an eye by means of reducing juxtacanalicular meshwork as a barrier to outflow of aqueous. The small organic molecules increase Gelatinase A activity in ocular cells by increa... | 07/04/2006 |
| 7060719 | Glutaminyl based DPIV inhibitors The present invention provides compounds of the formula: wherein X=CH2 or S or pharmaceutical acceptable salts thereof useful for treating conditions mediated by DPIV or DPIV-like enzymes, such as arth... | 06/13/2006 |
| 7060697 | Immunosuppressant compounds and compositions The present invention relates to immunosuppressant, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by... | 06/13/2006 |
| 7056935 | Rotamase enzyme activity inhibitors This invention relates to methods of using neurotrophic compounds having an affinity for FKBP-type immunophilins to stimulate or promote neuronal growth or regeneration and to prevent neuronal degeneration. ... | 06/06/2006 |
| 7045532 | ACE-2 modulating compounds and methods of use thereof ACE-2 inhibitors for the treatment of body weight and related disorders are disclosed. ACE-2 inhibitors include peptides and small molecules. Examples of small molecule ACE-2 inhibitors include compounds of formula (I): Z-Λ (I) Wherein Z is... | 05/16/2006 |
| 7034163 | Synthesis of pyrroles An improved and highly efficient method for the preparation of 2-R(R=alkyl, aryl, H) pyrroles from nitrites (RCN, R=alkyl, aryl) is described using Lewis acid activated donor-acceptor cyclopropanes to react with aliphatic, aromatic, branched, α,β-unsaturated, or o... | 04/25/2006 |
| 7015323 | Thiocarbamate inhibitors of alpha-4 integrins The invention provides novel thiocarbamate alpha-4 inhibitors of the general formula (I) that are resistant to metabolism having improved half-life and/or clearance properties compared to corresponding carbamate compounds wherein substituents L, X, Y, Z, R1 | 03/21/2006 |
| 7001911 | Fused cyclic modulators of nuclear hormone receptor function The invention pertains to fused cyclic compounds having the formula, wherein G is an optionally substituted aryl or heterocyclo, L is an optional linker, M is a bond, O, CR7R7′ or NR10 | 02/21/2006 |
| 6992102 | Bicyclic modulators of androgen receptor function The invention provides compounds of the formula I wherein the substitutents are as described herein. Further provided are methods of using such compounds for the treatment of nuclear hormone receptor-associated con... | 01/31/2006 |
| 6946480 | Glutaminyl based DPIV inhibitors The present invention provides compounds of the formula: wherein X═CH2 or S or pharmaceutical acceptable salts thereof useful for treating conditions mediated by DPIV or DPIV-like enzymes, such as arthriti... | 09/20/2005 |
| 6946481 | Endothelin antagonists A compound of the formula (I): or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing endothelin. ... | 09/20/2005 |
| 6946468 | 3-mercaptopyrrolidines as farnesyl protein transferase inhibitors The present invention relates to inhibitors of ras farnesylation of the Formula I wherein: R1 is for example H and further values as defined in the specification; R2 | 09/20/2005 |
| 6872836 | Process for the manufacture of 3-amino-pyrrolidine derivatives The invention is concerned with a process for the manufacture of 3-amino-pyrrolidine derivatives of the formula wherein R1 signifies hydrogen or an amino protecting group; | 03/29/2005 |
| 6849743 | Synthesis of clasto-lactacystin β-lactone and analogs thereof The present invention is directed to an improved synthesis of clasto-lactacystin-β-lactone, and analogs thereof, that proceeds in fewer steps and in much greater overall yield than syntheses described in the prior art. The synthetic pathway relies upon a novel ster... | 02/01/2005 |
| 6797829 | Synthesis of a novel paramagnetic amino derivative (epm-5) for labelling chemical and biological macromolecules The present invention refers to the synthesis and application of 2,2,5,5-tetramethylpyrrolidine-N-oxyl-(9-fluorenylmethyloxycarbonyl)-3-amine-4-carboxylic acid, a novel paramagnetic amino acid derivative (spin label), denominated Fmoc-Poac. Fmoc-Poac can be coupled ... | 09/28/2004 |
| 6759430 | Piperidine and pyrrolidine derivatives comprising a nitric oxide donor for treating stress The present invention relates to chemical compounds comprising a nitric oxide (NO) donor and a superoxide ion (O2−) scavenger, their preparation and their use in the treatment of conditions associated with oxidative stress or endothelial dysf... | 07/06/2004 |
