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| Number | Title | Issue Date |
| 8076479 | Process and intermediates for the synthesis of (3-alkyl-5-piperidin-1-yl-3,3a-dihydro-pyrazolo[1,5-a]pyrimidin-7-yl)-amino derivatives and intermediates Disclosed is a process for the synthesis of compounds of Formula I by sequentially aminating, first with a primary amine and then with a secondary amine, an intermediate compound of the structure of Formula E1, | 12/13/2011 |
| 7998958 | Substituted N-arylsulfonylheterocyclic amines as gamma-secretase inhibitors Disclosed are novel gamma secretase inhibitors of the formula: Also disclosed are methods for inhibiting gamma secretase, for treating one or more neurodegenerative diseases, for inhibiting the deposition of beta amyloid prot... | 08/16/2011 |
| 7964646 | 3,4-DI-substituted cyclobutene-1,2-diones as CXC-chemokine receptor ligands There are disclosed compounds of the formula or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and ca... | 06/21/2011 |
| 7947720 | 3,4-di-substituted cyclobutene-1,2-diones as CXC-chemokine receptor ligands There are disclosed compounds of the formula or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and ca... | 05/24/2011 |
| 7897606 | 5,6-di-substituted oxadiazolopyrazines and thiadiazolopyrazines as CXC-chemokine receptor ligands Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof. The compounds are useful for the treatment of chemokine-mediated diseases such as COPD. ... | 03/01/2011 |
| 7807672 | Compounds that are ERK inhibitors Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a do... | 10/05/2010 |
| 7786149 | Thiadiazoles as CXC- and CC- chemokine receptor ligands Disclosed are novel compounds of the formula: and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl... | 08/31/2010 |
| 7763613 | Substituted N-arylsulfonylheterocyclic amines as gamma-secretase inhibitors Disclosed are novel gamma secretase inhibitors of the formula: Also disclosed are methods for inhibiting gamma secretase, for treating one or more neurodegenerative diseases, for inhibiting the deposition of beta amyloid prot... | 07/27/2010 |
| 7718678 | Di-substituted oxadiazoles as CXC-chemokine receptor ligands Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof. X is N or N+O−, and Y is N or N+O−, provided that at least X or Y is N. The compounds... | 05/18/2010 |
| 7700601 | Substituted indazoles of formula 1.0 that are kinase inhibitors Disclosed is a compound of the formula: and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating protein kinase mediated diseases using the compound of formula 1.0. Also disclosed are method... | 04/20/2010 |
| 7691856 | Thiadiazoledioxides and thiadiazoleoxides as CXC- and CC-chemokine receptor ligands Disclosed are novel compounds of the formula: and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl... | 04/06/2010 |
| 7671212 | Isothiazole dioxides as CXC- and CC-chemokine receptor ligands Disclosed are novel compounds of the formula: and the pharmaceutically acceptable salts and solvates thereof. D and E are different groups wherein one is N and the other is CR50. Examples of groups comprising Sub... | 03/02/2010 |
| 7638526 | Azetidine derivatives useful in treating pain, diabetes and disorders of lipid metabolism Disclosed are compounds of the formula: and compounds of the formula: wherein R1, R2, R3, R4, R5, u and v are as defined her... | 12/29/2009 |
| 7635697 | Farnesyl protein transferase inhibitors and methods for treating proliferative diseases Disclosed are compounds of the Formula: wherein the substituents are as defined herein. Also disclosed are uses of the compounds of formula 1.0 for the manufacture of a medicament for treating cancer and for inhibiting farn... | 12/22/2009 |
| 7585864 | Farnesyl protein transferase inhibitors and their use to treat cancer Disclosed are compounds of the formula: wherein R8 represents a cyclic and acyclic moiety to which is bound an imidazolylalkyl group; R9 represents a carbamate, urea, amide or sulfonamide group; and th... | 09/08/2009 |
| 7557107 | Farnesyl protein transferase inhibitors as antitumor agents Disclosed are novel tricyclic compounds of the formula: and a pharmaceutically acceptable salts or solvates thereof. The compounds are useful for inhibiting farnesyl protein transferase. Also disclosed are pharmaceutical co... | 07/07/2009 |
| 7368457 | Bridged N-arylsulfonylpiperidines as gamma-secretase inhibitors In an embodiment, this invention discloses novel gamma secretase inhibitors of Formulae I: wherein the various moieties are described herein. Also disclosed is a method of treating Alzheimer's disease using a compound of Fo... | 05/06/2008 |
| 7342016 | Farnesyl protein transferase inhibitors as antitumor agents Disclosed are novel tricyclic compounds represented by the formula (1.0): and a pharmaceutically acceptable salt or solvate thereof. The compounds are useful for inhibiting farnesyl protein transferase. Also disclosed are p... | 03/11/2008 |
| 7338968 | Thiadiazoles AS CXC- and CC- chemokine receptor ligands Disclosed are novel compounds of the formula: and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl... | 03/04/2008 |
| 7326729 | CXCR1 and CXCR2 chemokine antagonists The present invention is directed to a compound having the general structure of formula (1): useful for the treatment, prevention or amelioration of a CXCR1 or CXCR2 chemokine-mediated disease. ... | 02/05/2008 |
| 7300941 | Non-imidazole compounds Disclosed are novel compounds of the formula Also disclosed are pharmaceutical compositions comprising the compounds of Formula I. Also disclosed are methods of treating various diseases or conditions, such ... | 11/27/2007 |
| 7256186 | Gamma secretase inhibitors This invention discloses novel gamma secretase inhibitors of the formula: wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 ... | 08/14/2007 |
| 7238688 | Piperidine compounds Disclosed are novel compounds of the formula Also disclosed are pharmaceutical compositions comprising the compounds of Formula I. Also disclosed are methods of treating various diseases or conditions, such ... | 07/03/2007 |
| 7049440 | Enantioselective process An enantioselective process for preparing intermediates useful in the preparation of the chiral tricyclic compound of formula I is disclosed. ... | 05/23/2006 |
| 6903131 | 3,4-di-substituted maleimide compounds as CXC chemokine receptor antagonists Disclosed are compounds of the formula (I) or a pharmaceutically acceptable salt or solvate thereof. The compounds are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory diso... | 06/07/2005 |
| 6878709 | 3,4-di-substituted pyridazinediones as CXC chemokine receptor antagonists Disclosed are compounds of the formula (I) or a pharmaceutically acceptable salt or solvate thereof. The compounds are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory diso... | 04/12/2005 |
| 6800636 | Farnesyl protein transferase inhibitors Disclosed are compounds of the formula: wherein R8 represents a cyclic moiety to which is bound an imodazolylalkyl group; R9 represents a carbamate, urea, amide or sulfonamide group; and the remaini... | 10/05/2004 |
| 6777415 | Methods of inducing cancer cell death and tumor regression Methods are provided for treating cancer, comprising administering (1) a farnesyl protein transferase inhibitor in conjunction with (2) an additional Ras signaling pathway inhibitor to induce cancer cell death and tumor regression. ... | 08/17/2004 |
| 6740661 | Farnesyl protein transferase inhibitors Disclosed are compounds of the formula: wherein R13 represents an imidazole ring; R14 represents a carbamate, urea, amide or sulfonamide group; R8 represents H when the alkyl chain betwee... | 05/25/2004 |
| 6706883 | Process for producing (8-chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-B]pyridin-11-YL)-1-piperdine A process for producing compounds of the formula: is disclosed. The compound of formula 1.0 is produced by: (1) separating the atropisomers of to obtain the atropis... | 03/16/2004 |
| 6703400 | Methods for treating multidrug resistance Methods are provided for treating multidrug resistance in refractory tumor cells comprising administering (1) a P-glycoprotein inhibitor in conjunction with (2) an antineoplastic agent.... | 03/09/2004 |
| 6699872 | N-substituted urea inhibitors of farnesyl-protein transferase Novel halo-N-substituted urea compounds and pharmaceutical compositions are disclosed which are inhibitors of the enzyme, farnesyl protein transferase. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of c... | 03/02/2004 |
| 6689789 | Compounds useful for inhibition of farnesyl protein transferase Novel compounds of the formula: ##STR1## or a pharmaceutically acceptable salt or solvate thereof, wherein: a represents N or NO- ; R1 and R3 are the same or different and each represents halo; R2 and R4 are th... | 02/10/2004 |
| 6683091 | Gamma Secretase inhibitors This invention discloses novel gamma secretase inhibitors of the formula: ##STR1## wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 group, alkyl, --X(CO)Y, --(CR32)1-4 | 01/27/2004 |
| 6399615 | Farnesyl protein transferase inhibitors Novel compounds of the formula: ##STR1## wherein a represents N or NO, R1 and R3 are halo, R2 and R4 are independently H or halo provided that at least one is H, X is C, CH or N, and T represents ##STR2## w... | 06/04/2002 |
| 6372747 | Farnesyl protein transferase inhibitors Disclosed are compounds of the formula: ##STR1## wherein R13 represents an imidazole ring; R14 represents a carbamate, urea, amide or sulfonamide group; R8 represents H when the alkyl chain between the amide group and the ... | 04/16/2002 |
| 6365588 | Tricyclic amide and urea compounds useful for inhibition of G-protein function and for treatment of proliferative diseases A method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells is disclosed. The method comprises the administration of a compound of Formula 1.0: ##STR1## to a biological system. In particular, the method inhibits the abnormal ... | 04/02/2002 |
| 6362188 | Farnesyl protein transferase inhibitors Disclosed are compounds of the formula: ##STR1## wherein R.sup.8 represents a cyclic moiety to which is bound an imodazolylalkyl group; R.sup.9 represents a carbamate, urea, amide or sulfonamide group; and the remaining substituents are as defined herein.... | 03/26/2002 |
| 6300338 | Tricyclic carbamate compounds useful for inhibition of g-protein function and for treatment of proliferative diseases A method of inhibiting Ras function and therefore inhibiting cellular growth is disclosed. The method comprises the administration of a compound of Formula 1.0 ##STR1## Also disclosed are novel compounds of the formulas: ##STR2## Also disclosed are p... | 10/09/2001 |
| 6277854 | Tricyclic antitumor farnesyl protein transferase inhibitors The invention relates to compounds of the formula ##STR1## wherein R1, R2, R3, R4, R5, R6, R7, R8, Y, A, B, X, a, b, c, d, v, and w are as described herein. The compou... | 08/21/2001 |
