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| Number | Title | Issue Date |
| 8124600 | 5-HTreceptor modulators, methods of making, and use thereof Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these co... | 02/28/2012 |
| 8110568 | 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, R3, R | 02/07/2012 |
| 7998952 | Thiolactams and uses thereof This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, and R6 are as described in the specification. The compou... | 08/16/2011 |
| 7968536 | Heterocyclic compounds useful as RAF kinase inhibitors The present invention provides compounds useful as inhibitors of protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases. ... | 06/28/2011 |
| 7968535 | Use of azapaullones for preventing and treating pancreatic autoimmune disorders This invention relates to the use of azapaullones, particularly in combination with immunomodulating agents, in the prevention, and/or treatment of pancreatic autoimmune disorders, e.g. type I diabetes or LADA and neurodegenerative disorders. ... | 06/28/2011 |
| 7951795 | Constrained spirocyclic compounds as CGRP receptor antagonists Compounds of formula I: (wherein variables A1, A2, A3, G1, G2, G3, J, m, n, p, R1, R2, R3, R4 and Y are as descri... | 05/31/2011 |
| 7947677 | Spirolactam tricyclic CGRP receptor antagonists Compounds of formula I: (wherein variables A1, A2, A3, A4, A5, A6, A7, B1, B2, B3, B4, D1, ... | 05/24/2011 |
| 7935694 | Lactam compounds useful as protein kinase inhibitors The present invention provides novel compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases. ... | 05/03/2011 |
| 7897595 | Pyridoazepine derivatives The present invention relates to pyridoazepine derivatives that act as 5-HT ligands, e.g., 5-HT2 C. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds. | 03/01/2011 |
| 7888344 | Fused thiazole derivatives as kinase inhibitors A series of 5,6-dihydro-1,3-benzothiazol-7(4H)-one derivatives, and analogues thereof, which are substituted in the 2-position by an optionally substituted morpholin-4-yl moiety, being selective inhibitors of PD kinase enzymes, are accordingly of benefit in medicine... | 02/15/2011 |
| 7858612 | Therapeutic agent for inflammatory bowel diseases The present invention relates to a method for maintaining the remission of or treating inflammatory bowel diseases, which comprises administering a maintenance therapeutically effective amount or a therapeutically effective amount of 7,8-dimethoxy-4(5H),10-dioxo-1H-... | 12/28/2010 |
| 7838517 | Compounds useful as protein kinase inhibitors The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, o... | 11/23/2010 |
| 7732436 | Preparation of hymenialdisine derivatives and use thereof The synthesis and biological activity of indoloazepines and acid amine salts thereof which are structurally related to naturally-occurring hymenialdisine is disclosed. Naturally-occurring hymenialdisine obtained from the sponge is a potent inhibitor of production of... | 06/08/2010 |
| 7713958 | Compounds and compositions as protein kinase inhibitors The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases and disorders associated with kinase activity, particularly diseases associated with the activit... | 05/11/2010 |
| 7601710 | Preparation of hymenialdisine derivatives and use thereof The synthesis and biological activity of indoloazepines and acid amine salts thereof which are structurally related to naturally-occurring hymenialdisine is disclosed. Naturally-occurring hymenialdisine obtained from the sponge is a potent inhibitor of production of... | 10/13/2009 |
| 7531530 | Therapeutic compounds The invention relates to trycyclic lactam indole derivatives and triacyclic lactam benzimodole derivatives and their use in inhibiting the activity of PARP enzyme. The invention also relates to the use of these compounds in the preparation of medicaments. ... | 05/12/2009 |
| 7470679 | Constrained compounds as CGRP-receptor antagonists The invention encompasses constrained bicyclic and tricyclic CGRP-receptor antagonists, methods for identifying them, pharmaceutical compositions comprising them, and methods for their use in therapy for treatment of migraine and other headaches, neurogenic vasodila... | 12/30/2008 |
| 7470680 | Constrained compounds as CGRP-receptor antagonists The invention encompasses constrained bicyclic and tricyclic CGRP-receptor antagonists, methods for identifying them, pharmaceutical compositions comprising them, and methods for their use in therapy for treatment of migraine and other headaches, neurogenic vasodila... | 12/30/2008 |
| 7459448 | Lactam compounds useful as protein kinase inhibitors The present invention provides novel compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases. ... | 12/02/2008 |
| 7423031 | Compounds and compositions as protein kinase inhibitors The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases and disorders associated with kinase activity, particularly diseases associated with the activit... | 09/09/2008 |
| 7419967 | Sulfonamide inhibitors of aspartyl protease The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. T... | 09/02/2008 |
| 7384931 | Constrained compounds as CGRP-receptor antagonists The invention encompasses constrained bicyclic and tricyclic CGRP-receptor antagonists, methods for identifying them, pharmaceutical compositions comprising them, and methods for their use in therapy for treatment of migraine and other headaches, neurogenic vasodila... | 06/10/2008 |
| 7384930 | Constrained compounds as CGRP-receptor antagonists The invention encompasses constrained bicyclic and tricyclic CGRP-receptor antagonists, methods for identifying them, pharmaceutical compositions comprising them, and methods for their use in therapy for treatment of migraine and other headaches, neurogenic vasodila... | 06/10/2008 |
| 7378411 | Substituted thienopyrimidinones as a mitotic kinesin inhibitor The present invention relates to thienopyrimidinone 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 ... | 05/27/2008 |
| 7351701 | Therapeutic compounds The invention relates to trycyclic lactam indole derivatives and triacyclic lactam benzimodole derivatives and their use in inhibiting the activity of PARP enzyme. The invention also relates to the use of these compounds in the preparation of medicaments. ... | 04/01/2008 |
| 7279468 | Integrin ligands The invention relates to novel compounds which bind to integrin receptors, their use as ligands of integrin receptors, in particular as ligands of the αvβ3 integrin receptor, their use, and pharmaceutical preparations comprising these compoun... | 10/09/2007 |
| 7244723 | Substituted furopyrimidinones as a mitotic kinesin inhibitors The present invention relates to furanopyrimidinone 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 ... | 07/17/2007 |
| 7238719 | Process for producing 1,2,3-Triazole compounds Disclosed is a process for efficiently producing a compound represented by formula (I): wherein R1 represents aryl, amino, alkyl, or alkoxy; R2 represents a protective group of the carboxyli... | 07/03/2007 |
| 7232814 | Use of paullone derivatives for making medicines The invention concerns the use for producing of GSK-3β inhibiting medicines from paullone derivatives. The invention is useful for treating pathologies involving GSK-3β and CDK5. ... | 06/19/2007 |
| 7229985 | Amorphous substance of tricyclic triazolobenzazepine derivative Disclosed are 2-(1-isopropoxycarbonyloxy-2-methylpropyl)-7,8-dimethoxy-4(5H), 10-dioxo-2H-1,2,3-triazolo[4,5-c][1]benzazepine, which has been rendered amorphous and possesses improved absorption and dissoluvability, and a pharmaceutical composition com... | 06/12/2007 |
| 7192949 | Substituted bicyclic pyrimidinones as a mitotic kinesin KSP inhibitors The present invention relates to cycloalkylpyrimidinone 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 wh... | 03/20/2007 |
| 7132533 | Tricyclic compounds protein kinase inhibitors for enhancing the efficacy of anti-neoplastic agents and radiation therapy Protein kinase, such as CHK-1, inhibiting tricyclic compounds of the following formula (wherein R2, R3 and R4 are as defined in the specification) pharmaceutical compositions cont... | 11/07/2006 |
| 7125911 | Autonomic nerve regulating agent The autonomic nerve regulating agent of the present invention, which, has sedative action, sleep inducing action, and stress mitigating action in individuals, regardless of individual variation in sensitivity to or preference for fragrance, contains as an active ing... | 10/24/2006 |
| 7098204 | Hymenialdisine or derivatives thereof in the manufacture of medicaments The invention relates to the use of hymenialdisine or derivatives thereof of formula (I) in which R1 and R2, identical or different, represent H or Br, or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for use in inhibiting acceptable... | 08/29/2006 |
| 7081455 | Substituted heterocycle fused gamma-carbolines The present invention is directed to methods of treating addictive behavior and sleep disorders by administering compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, ... | 07/25/2006 |
| 7074920 | Process for the synthesis of 1,3-dihydro-2H-3-benzazepin-2-one compounds, and to the application thereof in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid Process for the synthesis of compounds of formula (I): wherein R1 and R2, which may be the same or different, each represent a linear or branched (C1–C8)alkoxy group ... | 07/11/2006 |
| 7002009 | Crystalline tricyclic triazolobenzazepine derivative Disclosed are novel crystalline 2-(1-isopropoxycarbonyloxy-2-methylpropyl)-7,8-dimethoxy-4(5H),10-dioxo-2H-1,2,3-triazolo[4,5-c][1]benzazepine and a pharmaceutical composition comprising the same. ... | 02/21/2006 |
| 6958330 | Polycyclic α-amino-ε-caprolactams and related compounds Disclosed are polycyclic α-amino-ε-caprolactams and related compounds which are useful as synthetic intermediates in the preparation of inhibitors of β-amyloid peptide release and/or its synthesis. ... | 10/25/2005 |
| 6660729 | Particle-forming compositions containing fused pyrrolocarbazoles A non-aqueous, particle-forming, fused pyrrolocarbazole-containing composition is disclosed. Upon contact with an aqueous medium, the particle-forming composition spontaneously disperses into suspended particles, thereby forming a stable suspension that p... | 12/09/2003 |
| 6610684 | Fused azepinone cyclin dependent kinase inhibitors A new class of cyclin dependent kinase inhibitors that also have antiproliferative activity in human tumor cell line assays are described. Most of these compounds satisfy the formula ##STR1## wherein A is oxygen or sulfur coupled to the right by a single ... | 08/26/2003 |
