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| Number | Title | Issue Date |
| 7630838 | Method for identifying agents that interact with beta-site APP cleaving enzyme (BACE) This invention is directed to the three dimensional crystal structure of Beta-site APP Cleaving Enzyme (BACE), and to the use of this structure in rational drug design methods to identify agents that may interact with active sites of BACE. Such agents may represent ... | 12/08/2009 |
| 7157568 | Human estrogen receptor-β The present invention provides isolated nucleic acids encoding full-length human estrogen receptor-β (hERβ), which comprises 530 amino acids. The invention also provides isolated hERβ polypeptides and hERβ-reactive antibodies, including those that specifically r... | 01/02/2007 |
| 6787319 | β-amyloid peptide-binding proteins and polynucleotides encoding the same Novel proteins which bind human β-amyloid peptide, polynucleotides which encode these proteins, and methods for producing these proteins are provided. Diagnostic, therapeutic, and screening methods employing the polynucleotides and polypeptides of the present inven... | 09/07/2004 |
| 6689781 | Phenylalanine derivatives as alpha 4 integrin inhibitors Disclosed are a series of phenylalanine derivatives, to compositions containing them, to processes for their preparation, and to their use in medicine.... | 02/10/2004 |
| 6559127 | 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.... | 05/06/2003 |
| 6545003 | Fused ring heteroaryl and heterocyclic 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.... | 04/08/2003 |
| 6524592 | Veterinary vaccines The invention relates to vaccines which are suitable for the prevention of clostridial diseases of sheep (and lambs), providing an effective immunity for up to a year or more following a single injection or dose.... | 02/25/2003 |
| 6525026 | Carbamyloxy 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.... | 02/25/2003 |
| 6509334 | Cyclocarbamate derivatives as progesterone receptor modulators This invention provides compounds of Formula (I): ##STR1## wherein R1 and R2 may be single substituents or fused to form spirocyclic or hetero-spirocyclic rings; R3 is H, OH, NH2, C1 to C6 ... | 01/21/2003 |
| 6492372 | 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.... | 12/10/2002 |
| 6492421 | Substituted phenylalanine type compounds which inhibit leukocyte adhesion mediated by VLA-4 Disclosed are compounds which bind VLA-4. Certain of these compounds aslo 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.... | 12/10/2002 |
| 6465523 | 4-substituted-3-substituted-amino-cyclobut-3-ene-1,2-diones and analogs thereof as novel potassium channel openers 4-Substituted-3-substituted-amino-cyclobutyl-3-ene-1,2-diones having the Formula (I): ##STR1## wherein R1, R2, R3, R4, R5, A and W are as defined in the specification which compounds relaxes smooth mu... | 10/15/2002 |
| 6462059 | 4-substituted-3-substituted-amino-cyclobut-3-ene-1,2-diones and analogs thereof as novel potassium channel openers 4-Substituted-3-substituted-amino-cyclobut-3-ene-1,2-diones having the Formula (I): ##STR1## wherein R1, R2, R3, R4, R5, A and W are as defined in the specification which compounds relaxes smooth musc... | 10/08/2002 |
| 6462073 | N-hydroxy-2-(alkyl, aryl, or heteroaryl sulfanyl, sulfinyl or sulfonyl)-3-substituted alkyl, aryl or heteroarylamides as matrix metalloproteinase inhibitors Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenase... | 10/08/2002 |
| 6459996 | Crystal structure of E. coli GDP-fucose synthetase (and complexes thereof) and methods of identifying agonists and antagonists using same The present invention provides for crystalline GFS. The crystal structure of GFS has also been solved using such material. Models based upon such crystal structure are also provided. Methods of identifying inhibitors of GFS activity using such models are ... | 10/01/2002 |
| 6444704 | N-hydroxy-2-(alkyl, aryl, or heteroaryl sulfanyl, sulfinyl or sulfonyl)-3-substituted alkyl, aryl or heteroarylamides as matrix metalloproteinase inhibitors Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenase... | 09/03/2002 |
| 6441023 | N-hydroxy-2-(alkyl, aryl, or heteroaryl sulfanyl, sulfinyl or sulfonyl)-3-substituted alkyl, aryl or heteroarylamides as matrix metalloproteinase inhibitors Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenase... | 08/27/2002 |
| 6436904 | Compounds which inhibit leukocyte adhesion mediated by VLA-4 Disclosed are compounds which bind VAL-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.... | 08/20/2002 |
| 6426355 | Heterocyclic carboxamide-containing thiourea inhibitors of herpes viruses containing phenylenediamine group Compounds having the formula: ##STR1## wherein R1 -R5, X and G are described herein and which are useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Bar... | 07/30/2002 |
| 6423699 | Combination therapies using benzimidazolones This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds which are antagonists of the progesterone receptor having the general structure: ##STR1## wherein: A is O, S, or NR4 ; B is ... | 07/23/2002 |
| 6423688 | Dipeptide and related compounds which inhibit leukocyte adhesion mediated by VLA-4 Disclosed are compounds which bind VLA-4. Certain of these compounds aslo 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.... | 07/23/2002 |
| 6420137 | Nucleic acid encoding human neurotensin subtype 2 receptor Nucleic acids encoding the long form and shorter isoform of the neurotensin receptor subtype 2, referred to as HNT2R (long) and HNT2R (short), are described. Polypeptides having amino acid sequences of the HNT2R and HNT2RS isolated proteins are also provi... | 07/16/2002 |
| 6410571 | Heterocyclic carboxamide-containing thiourea inhibitors of herpes viruses containing a substituted phenylenediamine group Compounds of the formula: ##STR1## wherein the substituents are defined herein which are useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster ... | 06/25/2002 |
| 6407101 | Cyanopyrroles This invention provides a progesterone receptor antagonist of formula 1 having the structure ##STR1## wherein T is O, S, or absent; R1, and R2 are each, independently, hydrogen, alkyl, substituted alkyl; or R1 and R2 | 06/18/2002 |
| 6407066 | Pyroglutamic acid derivatives and related compounds which inhibit leukocyte adhesion mediated by VLA-4 Disclosed are pyroglutamic acid derivatives and related 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 inflamma... | 06/18/2002 |
| 6407249 | Heterocyclic carboxamide-containing thiourea inhibitors of herpes viruses containing a substituted phenylenediamine group Compounds of the formula: ##STR1## wherein R1 -R5 are independently selected from hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkynyl of 2 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl... | 06/18/2002 |
| 6407123 | Diaminopyridine-containing thiourea inhibitors of herpes viruses Compounds of the formula ##STR1## wherein R1 -R5 are independently selected from hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkynyl of 2 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl ... | 06/18/2002 |
| 6403617 | Diaminopyridine-containing thiourea inhibitors of herpes viruses Compounds of the formula ##STR1## Useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, humanherpesviruses-6 and -7, and Kaposi herpesvi... | 06/11/2002 |
| 6395762 | Phenyl amino squarate and thiadiazole dioxide beta-3 adrenergic receptor agonists This invention provides compounds of Formula I having the structure ##STR1## wherein, ##STR2## R1, R2, and X are as defined hereinbefore, or a pharmaceutically acceptable salt thereof, which are useful in treating or inhibiting ... | 05/28/2002 |
| 6395477 | Human potassium channel polynucleotide and polypeptides and uses thereof Novel human Kv4.3 polypeptides, polynucleotides which encode these polypeptides, and methods for producing these polypeptides are provided. Diagnostic, therapeutic, and screening methods employing the polynucleotides and polypeptides of the present invent... | 05/28/2002 |
| 6391902 | Substituted benzofuranoindoles and indenoindoles as novel potassium channel openers Compounds of the Formulae (I) and (II): ##STR1## wherein R1, R2, R3, X, Y and Z are as defined in the specification which compounds are useful in the treatment of disorders associated with smooth muscle contraction via pot... | 05/21/2002 |
| 6391897 | Biphenyl oxo-acetic acids useful in the treatment of insulin resistance and hyperglycemia This invention provides substituted compounds of the general formulae: ##STR1## wherein B and E are C or N; D, G and W are O, S, or N; or salt forms thereof, and methods and pharmaceutical compositions for their use in treating disorders related to insuli... | 05/21/2002 |
| 6391907 | Indoline derivatives This invention relates to substituted indoline derivative compounds which are antagonists of the progesterone receptor, their preparation and pharmaceutical utility, particularly including contraception and treatment of benign or malignant neoplastic dise... | 05/21/2002 |
| 6384058 | 2,4,6-trisubstituted pryridines with estrogenic activity and methods for the solid phase synthesis thereof The present invention relates to novel substituted pyridine compounds of Formula (I) ##STR1## wherein the moiety Z, R1, R2 and R3 are as herein defined, having estrogenic activity, to processes for their preparation, to a ... | 05/07/2002 |
| 6384057 | 2,4,6-trisubstituted pyridines with estrogenic activity and methods for the solid phase synthesis The present invention relates to novel substituted pyridine compounds of Formula (I) ##STR1## wherein the moiety Z, R1, R2 and R3 are as herein defined, having estrogenic activity, to processes for their preparation, to a ... | 05/07/2002 |
| 6383512 | Vesicular complexes and methods of making and using the same Composition comprising lamellar vesicles that comprise a local anesthetic and a nucleic acid molecule are disclosed. Methods of making such compositions are disclosed. Method of delivering proteins to cells of individuals are disclosed. Methods of inducin... | 05/07/2002 |
| 6384223 | Substituted quinazoline derivatives This invention provides a process for preparing compounds of formula 1: ##STR1## wherein: X is phenyl optionally substituted with one or more substituents selected from the group consisting of halogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms... | 05/07/2002 |
| 6384060 | 2,4,6-trisbstituted pyridines with estrogenic activity and methods for the solid phase synthesis thereof The present invention relates to novel substituted pyridine compounds of Formula (I) ##STR1## wherein the moiety Z, R1, R2 and R3 are as herein defined, having estrogenic activity, to processes for their preparation, to a ... | 05/07/2002 |
| 6379965 | Multifunctional complexes for gene transfer into cells comprising a nucleic acid bound to a polyamine and having an endosome disruption agent A method of delivering a multifunctional molecular complex for the transfer of a nucleic acid composition to a target cell is provided. The complex is comprised of a) said nucleic acid composition and b) a transfer moiety comprising 1) one or more cationi... | 04/30/2002 |
| 6380166 | Glucopyranosides conjugates of 2-(4-hydroxy-phenyl)-3-methyl-1-[4-(2-amin-1-yl-ethoxy)-benzyl]-1H-indol-5 -ols This invention provides tissue selective estrogens of formula I having the structure ##STR1## wherein: R1 and R2 are independently, hydrogen, alkyl chain of 1-6 carbon atoms, benzyl, acyl of 2-7 carbon atoms, benzoyl, ##STR2## X... | 04/30/2002 |
