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| Number | Title | Issue Date |
| 7754892 | Processes for the preparation of N-(2-acetyl-4,6-dimethylphenyl)-3-{[(3,4 dimethyl-5-isoxazolyl)amino]sulfonyl}-2-thiophenecarboxamide Provided are processes for the preparation of N-(2-acetyl-4,6-dimethylphenyl)-3-{[(3,4 dimethyl-5-isoxazolyl)amino]sulfonyl}-2-thiophenecarboxamide, a compound useful for the treatment of endothelin-mediated disorders. ... | 07/13/2010 |
| 7390908 | Compounds effecting glucokinase The invention relates to the use of a compound of Formula (I) or a salt, solvate or prodrug thereof, wherein R1, R2, R3, n and m are as described in the specification, in the preparation of a medicament for the treatment or preventio... | 06/24/2008 |
| 7354919 | Isoxazole compositions useful as inhibitors of ERK Described herein are compounds that are useful as protein kinase inhibitors, especially inhibitors of ERK, having the formula: where A, B, R1, R2, T and Ht are described in the specification. The compo... | 04/08/2008 |
| 7329670 | Inhibition of RAF kinase using aryl and heteroaryl substituted heterocyclic ureas The compounds are aryl and heteroaryl substituted heterocyclic ureas of the formula A—NH—C(O)—NH—B where A is the aryl or hetaryl substituted heterocyclic group and B is an aryl or heteroaryl moiety. The compounds inhibit raf kinase and are useful in the tre... | 02/12/2008 |
| 7241786 | Isoxazole and isothiazole compounds for the treatment of neurodegenerative disorders The present invention relates to compounds of the Formula wherein R1, R1a, R1b, R2, R3, R4, R5, R6, R7, R8 | 07/10/2007 |
| 7220865 | Isoxazole-and isothiazole-amine compounds for the treatment of neurodegenerative disorders The present invention relates to compounds of the Formula I wherein R1, R3, R5, R6, R7, X and Y are as defined. Compounds of the Formula I have activity inhi... | 05/22/2007 |
| 7173129 | Sulfonamide-substituted chalcone derivatives and their use to treat diseases The invention relates to compounds, pharmaceutical compositions and methods of using compounds of the general formula or its pharmaceutically acceptable salt or ester, wherein the substituents are defined in the ... | 02/06/2007 |
| 7151113 | Pyrazole-amine compounds useful as kinase inhibitors The present invention provides pyrazole derived compounds of formula (I) useful for treating p38 kinase-associated conditions, where W, X, R1, R2, R3, R4, R5... | 12/19/2006 |
| 6972292 | Certain substituted polyketides, pharmaceutical compositions containing them and their use in treating tumors The present invention relates to certain substituted polyketides of formula I, wherein A, B, C, D, E, F and m are as defined herein, pharmaceutical compositions containing said compounds, and the use of said compounds ... | 12/06/2005 |
| 6949550 | Substituted amino methyl factor Xa inhibitors The present application describes substituted-aminomethyl substituted compounds and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa. ... | 09/27/2005 |
| 6903104 | Indol-3-YL-2-oxoacetamide compounds and methods of use thereof The invention is based on the discovery that certain 3-oxoacetamideindolyl compounds have potent anticancer and anti-angiogenic activity. The 3-oxoacetamideindolyl compounds are of the following formula. In this formul... | 06/07/2005 |
| 6852745 | Biphenyl sulfonamides as dual angiotensin endothelin receptor antagonists Novel biphenyl sulfonamide compounds which are combined angiotensin and endothelin receptor antagonists are claimed along with methods of using such compounds in the treatment of conditions such as hypertension and other diseases, as well as pharmaceutical compositi... | 02/08/2005 |
| 6835842 | 3-nitroisoxazoles and their use in the protection of materials The 3-nitroisoxazoles of the formula (I) in which R1 and R2 are each as defined in the description, some of which are known, are highly suitable for use as biocides for pr... | 12/28/2004 |
| 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 |
| 6716850 | Non-nucleoside reverse transcriptase inhibitors Compounds of the formula I: where; R1 is O, S; R2 is an optionally substituted nitrogen-containing heterocycle, wherein the nitrogen is located at the 2 position relative to the (thio)... | 04/06/2004 |
| 6680317 | IL-8 receptor antagonists This invention relates to novel compounds of Formula (I), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).... | 01/20/2004 |
| 6677360 | Biphenyl and biphenyl-analogous compounds as integrin antagonists The present invention relates to biphenyl and biphenyl-analogous compounds, their preparation and use as pharmaceutical compositions, as integrin antagonists and in particular for the production of pharmaceutical compositions for the treatment and prophyl... | 01/13/2004 |
| 6653330 | Amide-type triazole compounds A compound of formula (I) or a pharmacologically acceptable prodrug or salt thereof which exhibits excellent antifungal activity: ##STR1## wherein Ar1 represents a phenyl group or the like; Ar2 represents a phenylene group or the lik... | 11/25/2003 |
| 6638958 | 3-nitroisoxazoles and their use in the protection of materials The 3-nitroisoxazoles of the formula (I) ##STR1## in which R1 and R2 are each as defined in the description, some of which are known, are highly suitable for use as biocides for protecting industrial materials.... | 10/28/2003 |
| 6624167 | Pharmaceutical compositions and methods for use Pharmaceutical compositions incorporate compounds that are capable of affecting nicotinic cholinergic receptors. A wide variety of conditions and disorders, and particularly conditions and disorders associated with dysfunction of the central and autonomic... | 09/23/2003 |
| 6593349 | Bisarylamines as potassium channel openers Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides bisarylamines, compositions... | 07/15/2003 |
| 6586433 | Substituted N-heteroaryl-N-phenyl aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating... | 07/01/2003 |
| 6545030 | 1-heterocycle substituted diarylamines 1-Heterocycle substituted diarylamines, methods of making and using them, and compositions containing them.... | 04/08/2003 |
| 6525196 | 5HT1 antagonists for antidepressant therapy The present invention relates to compounds of formula 1, ##STR1## wherein R1, R2, R3 and R4 are defined as in the specification. These compounds are useful as psychotherapeutic agents.... | 02/25/2003 |
| 6432994 | Sulfonamides for treatment of endothelin-mediated disorders Thienyl-, furyl- and pyrrolyl-sulfonamides, pharmaceutically-acceptable salts of sulfonamides, formulations of salts and the sulfonamides, and methods for modulating or altering the activity of the endothelin family of peptides using the formulations and ... | 08/13/2002 |
| 6376523 | Benzenesulfonamides and the use thereof to modulate the activity of endothelin N-(5-isoxazolyl)benzenesulfonamides and N-(3-isoxazolyl)benzenesulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(5-isoxazolyl)biphenylsulfonamides and N-(3-isoxazolyl... | 04/23/2002 |
| 6271248 | Substituted biphenysulfonamide endothelin antagonists Compounds of the formula ##STR1## wherein X, Y, R1, R2, R3, R4 and R5 are as described herein, inhibit the activity of endothelin.... | 08/07/2001 |
| 6248767 | Formulation of sulfonamides for treatment of endothelin-mediated disorders Formulations of pharmaceutically-acceptable salts of thienyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides using the formulations are provided. In particular, formulations of so... | 06/19/2001 |
| 6159973 | Aromatic amides, their preparation process, the compositions containing them and their use as pesticides The subject of the invention is the compounds of formula (I): Q(CH2)a --(X1)b --Q1 --Q2 --C(X2)--N(R1)(R2) (I) in which: Q represents an aryl ... | 12/12/2000 |
| 6107320 | Phenyl sulfonamide endothelin antagonists Compounds of the formula ##STR1## inhibit the activity of endothelin. The symbols are defined as follows: R1, R2 and R3 are each independently (a) hydrogen, except that R1 is other than hydrogen; (b) alkyl, alke... | 08/22/2000 |
| 6080774 | Substituted biphenylsulfonamide endothelin antagonists Compounds of the formula ##STR1## inhibit the activity of endothelin. The symbols are defined as follows: ##STR2## R2 and R3 are each independently (a) hydrogen; (b) alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, cycloalkylalkyl, ... | 06/27/2000 |
| 6022977 | Dynamic resolution of isoxazoline thioesters to isoxazoline carboxylic acids The present invention relates generally to a novel method for preparation of substituted isoxazolin-5-yl acetic acid in high optical purity from a stereoisomeric mixture of an esterified substituted isoxazolin-5-yl acetate. The products are useful in the ... | 02/08/2000 |
| 6013655 | Thieno-pyridine sulfonamides derivatives thereof and related compounds that modulate the activity of endothelin Methods, compositions, and compounds for modulating the activity of an endothelin pepuide are provided. The methods use compositions that contain compounds that include those of the formula: ##STR1## where X is selected from groups that include O, S,... | 01/11/2000 |
| 5939446 | Heteroaryl substituted phenyl isoxazole sulfonamide endothelin antagonists Compounds of the formula ##STR1## inhibit the activity of endothelin.... | 08/17/1999 |
| 5935973 | Heterocyclcarboxamide derivatives and their use as therapeutic agents Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which A is methylene or O; B is methylene or O; g is 0,1,2,3 or 4; R1 is an optional substituent; U is an alkylene chain optionally substituted by one or more... | 08/10/1999 |
| 5856507 | Methods for the preparation of biphenyl isoxazole sulfonamides Methods for the preparation of biphenyl isoxazole sulfonamides and intermediates thereof. The present invention also relates to the novel intermediates prepared by these methods. The biphenyl isoxazole sulfonamides prepared by the present methods are endo... | 01/05/1999 |
| 5846985 | Substituted biphenyl isoxazole sulfonamides Compounds of the formula ##STR1## inhibit the activity of endothelin. The symbols R1, R2, Q, K, J, , ଲ, p, R11, R12, R13 R14, X, Y, R3 and R4 are def... | 12/08/1998 |
| 5843937 | DNA-binding indole derivatives, their prodrugs and immunoconjugates as anticancer agents The present invention relates to novel DNA alkylating agents and the prodrugs of these agents which are useful as antitumor agents and DNA labelling agents. The compounds are hydroxy dihydrobenzindole oligopeptides and prodrugs thereof wherein the monomer... | 12/01/1998 |
| 5804585 | Thieno-pyridine sulfonamides derivatives thereof and related compounds that modulate the activity of endothelin Methods, compositions, and compounds for modulating the activity of an endothelin peptide are provided. The methods use compositions that contain compounds that include those of the formula: ##STR1## where X is selected from groups that include O, S,... | 09/08/1998 |
| 5783705 | Process of preparing alkali metal salys of hydrophobic sulfonamides A process of preparing an alkali metal salt of a hydrophobic sulfonamide is provided. The process includes the step of dissolving a free sulfonamide in an organic solvent in the presence of a saturated alkali metal salt solution and recovering the formed ... | 07/21/1998 |
