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| Number | Title | Issue Date |
| 8106213 | Sulfur substituted sulfonylaminocarboxylic acid N-arylamides, their preparation, their use and pharmaceutical preparations comprising them The present invention relates to compounds of the formula I wherein A1, A2, R1, R2, R3, X and n are as defined in the claims, which are valuable pharmaceutically active... | 01/31/2012 |
| RE42890 | Furazanobenzimidazoles The invention relates to compounds of formula (I) wherein R represents aryl or heteroaryl, X is oxygen, a carbonyl group, an oxime derivative of a carbonyl group or an α,β-unsaturated carbonyl group, and the substituents R1 to R6 have the mea... | 11/01/2011 |
| 8034953 | Modulators of indoleamine 2,3-dioxygenase and methods of using the same The present invention is directed to modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof. ... | 10/11/2011 |
| 7645882 | Inhibitor of protein modification products formation To provide a inhibitor of protein modification products formation capable of inhibiting of vitamin B6 deficiency disease as a side effect, especially a renal protective agent. There is provided a use, as an active ingredient, of any of free or salt-form compo... | 01/12/2010 |
| 7432293 | Heterocyclic compounds useful as Nurr-1 activators The present invention relates to compounds of formula (I): wherein R1 is hydroxy, C1-4 alkoxy, amino, C1-4 alkyl-amino, di C1-4alkylamino, benzyloxy or C2-C7 alkanoyl, R2 is C1-4 | 10/07/2008 |
| 7425555 | Heteroaryl substituted biphenyl derivatives as p38 kinase inhibitors Compounds of formula (I): are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38. ... | 09/16/2008 |
| 7419991 | 3-[5-(2-fluoro-phenyl)-[1,2,4]oxadiazol-3-yl]-benzoic acid, compositions, and methods for the use thereof Novel 1,2,4-oxadiazole benzoic acid compounds, methods of using and pharmaceutical compositions comprising an 1,2,4-oxadiazole benzoic acid derivative are disclosed. The methods include methods of treating or preventing a disease ameliorated by modulation of prematu... | 09/02/2008 |
| 7414048 | 4,5-dihydro-isoxazole derivatives and their pharmaceutical use The present invention is concerned with the compounds of formula wherein m, n and p are each independently 0 or 1 and q is 0, 1, 2, 3, 4 or 5; -A1=A2-A3=A4- is a pyridinylidene, p... | 08/19/2008 |
| 7385061 | Furazanobenzimidazoles The invention relates to compounds of formula (I) wherein R represents aryl or heteroaryl, X is oxygen, a carbonyl group, an oxime derivative of a carbonyl group or an α,β-unsaturated carbonyl group, and the substituents R1 to R6 have the mea... | 06/10/2008 |
| 7378529 | Heteroaryl, heterocyclic and aryl compounds which inhibit leukocyte adhesion mediated by VLA-4 Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, su... | 05/27/2008 |
| 7375123 | 1,2,4-thiadiazole derivatives as melanocortin receptor modulators The present invention is directed to novel 1,2,4-thiadiazole derivatives useful as agonists or antagonists of the melanocortin receptor. More particularly, the compounds of the present invention are useful for the treatment of metabolic, CNS and dermatological disor... | 05/20/2008 |
| 7371875 | Cytotoxic agents and methods of use Disclosed are compounds that inhibit proteasomic activity in cells. Also disclosed are pharmaceutical compositions comprising such compounds as well as methods to treat conditions, particularly cell proliferative conditions, such as cancer and inflammatory condition... | 05/13/2008 |
| 7368470 | Substituted 3-pyrrolidine-indole derivatives Substituted 3-pyrrolidine-indole derivatives and methods for their production. Also pharmaceutical compositions containing these compounds and the use of these substances in methods of treatment, in particular treatment of pain and/or depression. ... | 05/06/2008 |
| 7361675 | 1,2,4-thiadiazole compounds and use thereof 1,2,4-Thiadiazole compounds represented by the formula (1) have excellent control activities against harmful arthropods: wherein R1 represents C3-C7 alkynyl group optionally substituted one or more halogen atom(s... | 04/22/2008 |
| 7358266 | Cyclopropyl and cyclobutyl epothilone analogs The invention relates to cis- and trans-12, 13-cyclopropyl and 12,13-cyclobutyl epothilones of formula I to IV wherein Ar is a radical represented by the following structure: and ... | 04/15/2008 |
| 7348440 | Mitotic kinesin inhibitors The present invention relates to dihydropyrrole 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 comp... | 03/25/2008 |
| 7342031 | Thiadiazole compound and use thereof The thiadiazole compound represented by the formula (A): wherein R1 represents a C1-C7 alkyl group, a C3-C7 alkenyl group, a C3-C7 alkynyl group and the like; R2 represents a C1-C4 alkyl group substituted with a ... | 03/11/2008 |
| 7342039 | Substituted indole oximes The present invention relates to substituted indole oximes and methods of using them. ... | 03/11/2008 |
| 7338956 | Acylamino-substituted heteroaromatic compounds and their use as pharmaceuticals The present invention relates to acylamino-substituted heteroaromatic compounds of formula I, wherein R1, R2, R3, R4 and R5 and X are as defined herein, to pharmaceutic... | 03/04/2008 |
| 7335653 | Bis-aryl sulfonamides Compounds are provided that act as potent antagonists of chemokine receptors. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of chemokine receptor-mediated diseases, and as controls i... | 02/26/2008 |
| 7312337 | Oxadiazoles and their manufacture An oxadiazole compound and process of making same, is represented by Formula I: wherein R1 represents a substituted or unsubstituted straight, branched, or cyclo-alkyl group having at least two... | 12/25/2007 |
| 7301028 | Mitotic kinesin inhibitors The present invention relates to dihydropyrazole 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 com... | 11/27/2007 |
| 7297797 | Pyrrolines The invention relates to novel Δ1-pyrrolines of the formula (I) in which R1, R2, R3, R4, A1, A2, R5, R6, R7, R | 11/20/2007 |
| 7288567 | Inhibitors of histone deacetylase The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and cond... | 10/30/2007 |
| 7285558 | Pyrazolo[3,4-d]pyrimidines inhibiting infections Compounds having the general formula and pharmaceutical compositions containing them, and their use in the treatment or prophylaxis of H. pylori infection. ... | 10/23/2007 |
| 7268235 | Method for preparation of N-pyrazolylamidoximes A method for the preparation of N-pyrazolylamidoximes of the general formula I R1 and R2 independently represent an alkyl, aryl, or heteroaryl group, comprises ... | 09/11/2007 |
| 7259179 | Kinase inhibitors A compound of the general formula: or pharmaceutically acceptable salts, hydrates, solvates, crystal forms or diastereomers thereof is described. A method of treating protein kinase-associated disease states usin... | 08/21/2007 |
| 7253200 | Imidazole compounds Imidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor expression, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions. | 08/07/2007 |
| 7244851 | Inhibitors of IAP The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R... | 07/17/2007 |
| 7241755 | Epothilone derivatives The present invention relates to compounds of the formula in which the variables G, W, Q, X, Y, B1, B2, Z1, Z2, and R1–R7 are as defined herein,... | 07/10/2007 |
| 7214800 | Compounds, compositions, and methods Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed. ... | 05/08/2007 |
| 7205321 | Peroxisome proliferator activated receptor alpha agonists The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts, solvates and hydrates thereof, R1 is selected from the group consisting of hydrogen, substituted or unsubstituted group selected fr... | 04/17/2007 |
| 7189680 | 5-halo-6-aryl[1,2,4]triazolo[1,5-a]pyrimidin-7-amines The invention relates to novel triazolopyrimidines of the formula in which R1, R2, R3 and X have the meanings given in the disclosure, and acid addition s... | 03/13/2007 |
| 7189755 | Pyrrolidine melanocortin-specific compounds Melanocortin receptor-specific pyrrolidine compounds having the structure: and stereoisomer and pharmaceutically acceptable salts thereof, where R1, R2, and R3 are as described in... | 03/13/2007 |
| 7189856 | Non-peptide somatostatin receptor ligands Non-peptide somatostatin receptor ligands with conformationally restricted side chains exhibiting high binding affinity toward somatostatin receptors are provided. The compounds exhibit a high selectivity and act as agonists at human subtype 2 somatostatin receptors... | 03/13/2007 |
| 7186831 | 5-halo-2-alkyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amines This invention relates to novel triazolopyrimidines of the formula in which R1, R2, R3, R4and X have the meanings given in the disclosure, to a... | 03/06/2007 |
| 7183300 | Inhibitors of HIV-1 capsid formation: substituted aryl aminomethyl thiazole ureas and analogues thereof Substituted aryl aminomethyl thiazole ureas and analogues thereof that act as inhibitors of viral capsid formation, including HIV capsid formation, are provided here. Generally the virus capsid formation inhibitors described herein are compounds of Formula I ... | 02/27/2007 |
| 7183414 | Processes for the preparation of benzoimidazole derivatives The present invention relates to a process for preparing a compound of the formula I or a pharmaceutically acceptable salt, prodrug, hydrate or solvate thereof, wherein R1, R2, R3 | 02/27/2007 |
| 7173030 | Inhibitors of 11-β-hydroxy steroid dehydrogenase type 1 The present invention relates to compounds with the formula (I) and also to pharmaceutical compositions comprising the compounds, as well as to the use of the compounds in medicine and fo... | 02/06/2007 |
| 7166622 | Substituted phenylsulfonamide inhibitors of beta amyloid production Compounds of Formula I, wherein R1–R8 are defined herein are provided, together with pharmaceutically acceptable salts, hydrates, metabolites, and/or prodrugs ther... | 01/23/2007 |
