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| Number | Title | Issue Date |
| 8022058 | Agents for preventing and treating disorders involving modulation of the RyR receptors The present invention provides novel compounds of Formula I and salts, hydrates, solvates, complexes, and prodrugs thereof. The present invention further provides methods for synthesizing compounds of Formula I. The inventi... | 09/20/2011 |
| 7981879 | HIV integrase inhibitors Compounds of Formula I are inhibitors of FHV integrase and inhibitors of FHV replication (I), wherein m, n, X, R1, R2, R3, R4, R5, R6, R7; R8, R9 and R10 ar... | 07/19/2011 |
| 7956049 | Melanin concentrating hormone receptor-1 antagonists The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R1a, R1b, R1c, Q, A, ... | 06/07/2011 |
| 7943607 | Heteroaryl benzamide derivatives for use as GLK activators in the treatment of diabetes Compounds of formula (I), wherein R1, R4, HET-1 and HET-2 are as described in the specification, and their salts and pro-drugs, are activators of glucokinase (GLK) and are thereby useful in the treatment of, for example, type 2 diabetes. Proces... | 05/17/2011 |
| 7879840 | Agents for preventing and treating disorders involving modulation of the RyR receptors The present invention provides compounds of Formula I and salts, hydrates, solvates, complexes, and prodrugs thereof. The present invention further provides methods for synthesizing compounds of Formula I. The invention add... | 02/01/2011 |
| 7718644 | Anti-arrhythmic and heart failure drugs that target the leak in the ryanodine receptor (RyR2) and uses thereof The present invention provides methods for limiting or preventing a decrease in the level of RyR2-bound FKBP12.6 in a subject. The present invention further provides methods for treating and preventing atrial and ventricular cardiac arrhythmias, heart failure, and e... | 05/18/2010 |
| 7718645 | Substituted bicyclolactam compounds The invention provides compounds of formula (1), and the pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5a, R5b, R5c, R5d... | 05/18/2010 |
| 7704990 | Agents for preventing and treating disorders involving modulation of the RyR receptors The present invention provides novel compounds of Formula I and salts, hydrates, solvates, complexes, and prodrugs thereof. The present invention further provides methods for synthesizing compounds of Formula I. The inventi... | 04/27/2010 |
| 7625886 | Selected CGRP antagonists, processes for preparing them and their use as pharmaceutical compositions The present invention relates to the CGRP antagonists of general formula I wherein R1, R2, R3 and R4 are defined as in claim 1, the tautomers, the isomers, the diastereomer... | 12/01/2009 |
| 7435728 | Pyrazole derivatives This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivative thereofs, wherein R1 to R4 are defined in the description, and to processes for the preparation ther... | 10/14/2008 |
| 7390798 | Carboxamide spirolactam CGRP receptor antagonists The present invention is directed to compounds of Formula I: I (where variables A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in... | 06/24/2008 |
| 7323455 | 7-aryl 1,5-dihydro-4,1-benzoxazepin-2(3)-one derivatives and their use as progesterone receptor modulators This invention provides progesterone receptor modulators having the structure: wherein R1 to R7, X, and Q are as defined in the specification; or a pharmaceutically acceptable salt thereof. ... | 01/29/2008 |
| 7220739 | Therapeutic application of pro-apoptotic benzodiazepines Benzodiazepine compounds, and methods for using those compounds are provided. Some of the benzodiazepine compounds include 1,4-benzodiazepine-2-one and 1,4-benzodiazepine-2,5-dione compounds of the following structures: | 05/22/2007 |
| 7196108 | Bicyclic heterocycles for the treatment of diabetes and other diseases The invention relates to certain bicyclic heterocycles havng the structure shown below which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, and atherosclerosis. | 03/27/2007 |
| 7151097 | Bicyclic pyrazolyl and imidazolyl compounds and uses thereof Compounds of Formula (I) are described herein. The compounds have been shown to act as cannabinoid receptor ligands and are therefore useful in the treatment of diseases linked to the mediation of the cannabinoid... | 12/19/2006 |
| 7060698 | Benzoxazepinone derivatives The invention relates to benzoxazepinone derivatives of formula wherein R1, R2, R3, R4, and n are as defined in the specification and... | 06/13/2006 |
| 7053081 | Cyclic malonamides as inhibitors of A-β protein production This invention relates to novel cyclic malonamides having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor prote... | 05/30/2006 |
| 7030107 | Fused bicyclic pyridine derivatives as tachykinin receptor antagonists A novel fused bicyclic pyridine derivative or a salt thereof that acts as a tachykinin receptor antagonist, in particular as an NK1 receptor antagonist, is represented by the following general formula (1): ... | 04/18/2006 |
| 7026309 | Fused bicyclic pyridine derivative as tachykinin receptor antagonist A fused bicyclic pyridine derivative represented by the following general formula (1), or a salt thereof: wherein the rings A and B are each a benzene ring, which may have 1 to 3 substituents (a... | 04/11/2006 |
| 6995153 | Fused bicyclic pyrimidine derivatives A novel fused bicyclic pyrimidine derivative or a salt thereof that acts as a tachykinin receptor antagonist and, in particular, as an NK1 receptor antagonist is represented by the following general formula (1): wherein... | 02/07/2006 |
| 6977252 | Use of 1,4-benzothiazepine derivatives as drugs for overcoming resistance to anticancer drugs The present invention relates to use of compounds represented by the following general formula [1] or salts or prodrugs thereof: [where R1 represents hydrogen atom or lower alkoxy group; R2 represe... | 12/20/2005 |
| 6946459 | CRYSTALLINE FORMS OF 1S-[1ALPHA(2S*,3R*), 9ALPHA]6, 10-DIOXO-N-(2-ETHOXY-5-OXO-TETRAHYDRO-3-FURANYL)-9[[(1-ISOQUINOLYL) CARBONYL]AMINO]OCTAHYDRO-6H-PIRIDAZINO[1,2-A][1,2]DIAZEPIN-1-CARBOXAMIDE Two new crystalline forms of 1S-[1alpha(2S*, 3R*), 9alpha]6, 10-dioxo-N-(2-ethoxy-5-oxo-tetrahydro-3-furany1)-9 [[(1-isoquinolyl) carbony1]amino]octahydro-6H-pyridazino [1,2-a][1,2]diazepin-1-carboxamide (anhydrous or hydrated), their preparation process and the pha... | 09/20/2005 |
| 6924277 | Cyclized benzamide neurokinin antagonists for use in therapy Compounds having the general formula wherein R1a, R1b, R1c, X1, X2, R2, R3, R4, R5, R6, n, Y and Z are as de... | 08/02/2005 |
| 6897305 | Calcium channel drugs and uses Novel multibinding compounds are disclosed. The compounds of this invention comprise 2-10 ligands covalently connected, each of the ligands being capable of binding to a ligand binding site in a Ca++ channel , thereby modulating the biological activities ... | 05/24/2005 |
| 6890918 | Pharmaceutical compositions including ACE/NEP inhibitors and bioavailability enhancers A pharmaceutical composition comprising an inhibitor of angiotensin converting enzyme and neutral endopeptidase, such as sampatrilat, and at least one bioavailability enhancer such as an organic acid, e.g., ascorbic acid. Such a composition has improved systemic bio... | 05/10/2005 |
| 6797504 | Inhibitors of serine protease activity of matriptase or MTSP1 The present invention provides compounds which inhibit serine protease activity of matriptase or MTSP1. Also provided are pharmaceutical compositions comprising those compounds and methods of using the compounds and pharmaceutical compositions to treat conditions am... | 09/28/2004 |
| 6759404 | Cyclic malonamides as inhibitors of aβ protein production Novel cyclic malonamides having the formula (I): and their pharmaceutical compositions. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-pept... | 07/06/2004 |
| 6713470 | Method of treatment There is described a method of treatment of a patient requiring analgesia which comprises the separate, simultaneous or sequential administration of a therapeutically effective amount of an opioid analgesic, devazepide and a surfactant. There is also describe... | 03/30/2004 |
| 6645999 | Lactacystin analogs Compounds related to lactacystin and lactacystin Beta-lactone, pharmaceutical compositions containing the compounds, and methods of use.... | 11/11/2003 |
| 6613761 | Benzoxazepine compounds, their production and use This invention provides new benzoxazepine compounds represented by the formula: ##STR1## [wherein R stands for a lower alkyl group optionally substituted with a hydroxyl group, X stands for an optionally substituted carbamoyl group or an optionally s... | 09/02/2003 |
| 6583155 | Method for treating allergies using substituted pyrazoles A method for treating an allergic condition, including an atopic allergic condition, using substituted pyrazoles.... | 06/24/2003 |
| 6544977 | CRYSTALLINE FORMS OF 1S-[1-ALPHA(2S*,3R*), 9ALPHA]6, 10-DIOXO-N-(2-ETHOXY-5-OXO-TETRAHYDRO-3-FURANYL)-9[[(1-ISOQUINOLYL)CARBONY L]AMINO]OCTAHYDRO-6H-PYRIDAZINO [1,2-A] [1,2] DIAZEPIN-1-CARBOXAMIDE Two new crystalline forms of 1S-[1alpha(2S*,3R*), 9alpha]6,10-dioxo-N-(2-ethoxy-5-oxo-tetrahydro-3-furanyl)-9 [[(1-isoquiinolyl)carbonyl]amino]octahydro-6H-pyridazino[1,2-a][1,2]diazep in-1-carboxamide (anhydrous or hydrated), their preparation process and... | 04/08/2003 |
| 6537987 | 4,1-benzoxazepines or 4,1-benzothiazepines and their use as squalene synthetase inhibitors This invention relates to certain benzoxazepinones and benzothiazepinones useful as hypocholesterolemic agents, hypotriglyceridemic agents, antiatherosclerosis agents, antifungal agents, anti-Alzheimer's agents or anti-acne agents.... | 03/25/2003 |
| 6509328 | Glutamate receptor antagonists The present invention is a compound of formula ##STR1## wherein X is an ethynediyl group, R1, R2 and R3 are as defined in the specification.... | 01/21/2003 |
| 6506744 | Benzazepinone-derivatives Compounds of formula I ##STR1## as well as pharmaceutically usable salts and esters thereof, inhibit the binding of adhesive proteins to the surface of different types of cell and accordingly influence cell-cell and cell-matrix interactions. They can be ... | 01/14/2003 |
| 6489320 | 5, 5-disubstituted-1, 5-dihydro-4, 1-benzoxazepin-2 (3H)-ones useful as HIV reverse transcriptase inhibitors The present invention relates to benzoxazepinones of formula I: ##STR1## or stereoisomeric forms or mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical composition... | 12/03/2002 |
| 6489321 | Nonpeptide substituted benzothiazepines as vasopressin antagonists The invention is directed to nonpeptide substituted benzodiazepines of Formula I, ##STR1## wherein A, X, Z, Bp, W, n, R1 and R2 are as described in the specification, which are useful as vasopressin receptor antagonists for trea... | 12/03/2002 |
| 6468997 | Desmethylolanzapine compositions and methods Methods and compositions are disclosed utilizing N-desmethylolanzapine for the treatment of psychosis in humans. N-Desmethylolanzapine exhibits a lessened liability toward drug-drug interactions than olanzapine and a more predictable dosing regimen than o... | 10/22/2002 |
| 6403578 | Bicyclic fibrinogen antagonists This invention relates to compounds of the formulae: ##STR1## wherein A1 is O, S, N--R1 or CHR1 ; A4 is N--R4 or CHR4 ; R2 is a sidechain containing an acid or ester group; R1, ... | 06/11/2002 |
| 6352982 | 4,1-benzoxazepines, their analogues, and their use as somatostatin agonists The present invention provides a compound of the formula: ##STR1## wherein ring A is an optionally substituted aromatic hydrocarbon ring or aromatic heterocyclic ring; ring B is an optionally substituted aromatic hydrocarbon ring or aromatic heterocyclic ... | 03/05/2002 |
