Nitrogen Bonded Directly To Ring Carbon Of The Hetero Ring Patents (Class 514/245)
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Patent number: 7335672Abstract: Substituted pyridines and pyrimidines and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenType: GrantFiled: September 13, 2005Date of Patent: February 26, 2008Assignee: Amgen Inc.Inventors: Mark H. Norman, Liping H. Pettus, Xianghong Wang, Jiawang Zhu
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Publication number: 20080045477Abstract: A series of new 4,6-diamino-1,2-dihydro-1-aryl-2-(-tricyclo[3.3.1.13,7]decyl]-1,3,5-triazines where the aryl group is a substituted or unsubstituted phenyl, or naphthyl-group, as pharmaceutically accepted salts or as free bases. The phenyl group substituents are halides, alkyls, alkoxyls or nitro group. One or more of the above substituents are found one or more times each one, and in various positions of the phenyl group. The corresponding isomers, stereoisomers, enantiomers, free bases and their complexes with various natural macromolecules and synthetic derivatives of them. The invention refers to new and prototype compounds inhibiting the proliferation of unwanted cells that belong to pathogenic microorganisms, to human tissues, to pathological cells, or any pathological cell proliferation. It also refers to the synthesis and the method of synthesis of the above mentioned compounds.Type: ApplicationFiled: June 14, 2002Publication date: February 21, 2008Inventors: Ekaterini Antoniadou-Vyza, Polyvxeni Tsitsa, Christos Roussakis
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Patent number: 7332489Abstract: The present invention relates to methods and compositions comprising compounds that treat pathophysiological conditions arising from inflammatory responses. In particular, the present invention is directed to compounds that inhibit or block glycated protein produced induction of the signaling-associated inflammatory response in endothelial cells. The present invention relates to compounds that inhibit smooth muscle proliferation. In particular, the present invention is directed to compounds that inhibit smooth muscle cell proliferation by modulating HSPGs such as Perlecan. The present invention further relates to the use of compounds to treat vascular occlusive conditions characterized by smooth muscle proliferation such as restenosis and atherosclerosis.Type: GrantFiled: March 26, 2003Date of Patent: February 19, 2008Assignee: Reddy US Therapeutics, Inc.Inventors: Richard T. Timmer, Christopher W. Alexander, Sivaram Pillarisetti, Uday Saxena, Koteswar Rao Yeleswarapu, Manojit Pal, Jangalgar Tirupathy Reddy, Velagala Venkata Rama Murali Krishna Reddy, Sesha Sridevi Alluri, Potlapally Rajender Kumar, Gaddam Om Reddy
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Patent number: 7332490Abstract: The present invention relates to methods and compositions comprising compounds that treat pathophysiological conditions arising from inflammatory responses. In particular, the present invention is directed to compounds that inhibit or block glycated protein produced induction of the signaling-associated inflammatory response in endothelial cells. The present invention relates to compounds that inhibit smooth muscle proliferation. In particular, the present invention is directed to compounds that inhibit smooth muscle cell proliferation by modulating HSPGs such as Perlecan. The present invention further relates to the use of compounds to treat vascular occlusive conditions characterized by smooth muscle proliferation such as restenosis and atherosclerosis.Type: GrantFiled: May 25, 2006Date of Patent: February 19, 2008Assignee: Reddy US Therapeutics, Inc.Inventors: Richard T. Timmer, Christopher W. Alexander, Sivaram Pillarisetti, Uday Saxena, Koteswar Rao Yeleswarapu, Manojit Pal, Jangalgar Tirupathy Reddy, Velagala Venkata Rama Murali Krishna Reddy, Sesha Sridevi Alluri, Potlapally Rajender Kumar, Gaddam Om Reddy
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Patent number: 7332488Abstract: The present invention relates to methods and compositions comprising compounds that treat pathophysiological conditions arising from inflammatory responses. In particular, the present invention is directed to compounds that inhibit or block glycated protein produced induction of the signaling-associated inflammatory response in endothelial cells. The present invention relates to compounds that inhibit smooth muscle proliferation. In particular, the present invention is directed to compounds that inhibit smooth muscle cell proliferation by modulating HSPGs such as Perlecan. The present invention further relates to the use of compounds to treat vascular occlusive conditions characterized by smooth muscle proliferation such as restenosis and atherosclerosis.Type: GrantFiled: August 28, 2006Date of Patent: February 19, 2008Assignee: Reddy US Therapeutics, Inc.Inventors: Richard T. Timmer, Christopher W. Alexander, Sivaram Pillarisetti, Uday Saxena, Koteswar Rao Yeleswarapu, Manojit Pal, Jangalgar Tirupathy Reddy, Velagala Venkata Rama Murali Krishna Reddy, Sesha Sridevi Alluri, Potlapally Rajender Kumar, Gaddam Om Reddy
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Patent number: 7329658Abstract: Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein.Type: GrantFiled: January 21, 2004Date of Patent: February 12, 2008Assignee: Pfizer IncInventor: David A. Griffith
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Patent number: 7319099Abstract: The invention relates to compounds of formula wherein the substituents are described herein. The compounds may be used in the treatment of illnesses based on the glycine uptake inhibitor, such as psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.Type: GrantFiled: August 4, 2004Date of Patent: January 15, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Synese Jolidon, Robert Narquizian, Matthias Heinrich Nettekoven, Roger David Norcross, Emmanuel Pinard, Henri Stadler
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Publication number: 20080009497Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's Disease.Type: ApplicationFiled: July 5, 2007Publication date: January 10, 2008Inventors: Mark D. Wittman, Harold Mastalerz, Kurt Zimmermann, Mark G. Saulnier, Upender Velaparthi, Dolatrai M. Vyas, Guifen Zhang, Walter Lewis Johnson, David B. Frennesson, Xiaopeng Sang, Peiying Liu, David R. Langley
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Publication number: 20070299076Abstract: The invention provides compounds of formula (1), and the pharmaceutically acceptable salt thereof, wherein R1, n and R2 are as described herein; compositions thereof; and uses thereof.Type: ApplicationFiled: June 18, 2007Publication date: December 27, 2007Inventors: David W. Piotrowski, Yu Hui, John W. Benbow
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Patent number: 7307079Abstract: The invention relates to a group of novel triazine derivatives which are ligands for human adenosine-A3 receptors, as well as to pharmaceutical compositions containing a pharmacologically active amount of at least one of these compounds as an active ingredient. The invention relates to compounds of the general formula (1) wherein Y represents a group of the general formula (A), (B) or (C) and all other symbols have the meanings as given in the description.Type: GrantFiled: May 30, 2003Date of Patent: December 11, 2007Assignees: Solvay Pharmaceuticals, B.V., Arqule, Inc.Inventors: Jacobus A.J. Den Hartog, Jan H. Reinders, Guustaaf J.M. Van Scharrenburg, Maria L. Pras-Raves, Gary R. Gustafson
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Patent number: 7291616Abstract: The invention relates to aryl triazines and uses thereof, including to inhibit lysophosphatidic acid acyltransferase ? (LPAAT-?) activity and/or proliferation of cells such as tumor cells.Type: GrantFiled: October 30, 2002Date of Patent: November 6, 2007Assignee: Cell Therapeutics, Inc.Inventors: Rama Bhatt, Baoqing Gong, Feng Hong, Scott A. Jenkins, J. Peter Klein, Anil M. Kumar, John Tulinsky
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Patent number: 7285550Abstract: The invention is based on the discovery that compounds of formula (I) possess unexpectedly high affinity for the A2a adenosine receptor, and can be useful as antagonists thereof for preventing and/or treating numerous diseases, including Parkinson's disease.Type: GrantFiled: April 9, 2004Date of Patent: October 23, 2007Assignee: Biogen Idec MA Inc.Inventors: Chi Vu, Russell C. Petter, Gnanasambandam Kumaravel
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Patent number: 7265114Abstract: The present invention relates to methods and compositions comprising compounds that treat pathophysiological conditions arising from inflammatory responses. In particular, the present invention is directed to compounds that inhibit or block glycated protein produced induction of the signaling-associated inflammatory response in endothelial cells. The present invention relates to compounds that inhibit smooth muscle proliferation. In particular, the present invention is directed to compounds that inhibit smooth muscle cell proliferation by modulating HSPGs such as Perlecan. The present invention further relates to the use of compounds to treat vascular occlusive conditions characterized by smooth muscle proliferation such as restenosis and atherosclerosis.Type: GrantFiled: November 22, 2005Date of Patent: September 4, 2007Assignee: Reddy US Therapeutics, Inc.Inventors: Richard T. Timmer, Christopher W. Alexander, Sivaram Pillarisetti, Uday Saxena, Yeleswarapu Koteswar Rao, Manojit Pal, Jangalgar Tirupathy Reddy, Velagala Venkata Rama Murali Krishna Reddy, Sesha Sridevi Alluri, Potlapally Rajender Kumar, Gaddam Om Reddy
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Patent number: 7244732Abstract: The present invention provides hydrophobic prodrugs of bases, nucleosides, and nucleotides as well as methods of using the prodrugs as antiviral and anti-cancer chemotherapeutic agents.Type: GrantFiled: March 31, 2004Date of Patent: July 17, 2007Assignee: Koronis Pharmaceuticals, IncorporatedInventors: Richard Daifuku, Alexander Gall, Dmitri Sergueev, Dina Sologub, Kevin Harris
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Patent number: 7238692Abstract: The present invention relates to methods and compositions comprising compounds that treat pathophysiological conditions arising from inflammatory responses. In particular, the present invention is directed to compounds that inhibit or block glycated protein produced induction of the signaling-associated inflammatory response in endothelial cells. The present invention relates to compounds that inhibit smooth muscle proliferation. In particular, the present invention is directed to compounds that inhibit smooth muscle cell proliferation by modulating HSPGs such as Perlecan. The present invention further relates to the use of compounds to treat vascular occlusive conditions characterized by smooth muscle proliferation such as restenosis and atherosclerosis.Type: GrantFiled: September 27, 2004Date of Patent: July 3, 2007Assignee: Reddy US Therapeutics, Inc.Inventors: Richard T. Timmer, Christopher W. Alexander, Sivaram Pillarisetti, Uday Saxena, Koteswar Rao Yeleswarapu, Manojit Pal, Jangalgar Tirupathy Reddy, Velagala Venkata Rama Murali Krisha Reddy, Sesha Sridevi Alluri, Potlapally Rajender Kumar, Gaddam Om Reddy
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Patent number: 7223759Abstract: The invention relates to antibacterial 3,5-diaminopiperidine-substituted aromatic and heteroaromatic compounds and pharmaceutical compositions thereof. This invention also relates to a method of using such compounds in the treatment of bacterial infections in mammals, especially humans.Type: GrantFiled: September 15, 2004Date of Patent: May 29, 2007Assignee: Anadys Pharmaceuticals, Inc.Inventors: Yuefen Zhou, Dionisios Vourloumis, Vlad E. Gregor, Geoffrey C. Winters, Thomas Hermann, Benjamin Ayida, Zhongxiang Sun, Douglas Murphy, Klaus B. Simonsen
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Patent number: 7217821Abstract: Cosmetic/dermatological sunscreen compositions, suited for photoprotecting, e.g., the skin, lips, scalp and/or hair against the damaging effects of UV-radiation, contain thus effective amounts of at least one novel s-triazine compound tri-substituted with para-aminobenzalmalonate substituents.Type: GrantFiled: April 22, 2004Date of Patent: May 15, 2007Assignee: L'OrealInventor: Hervé Richard
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Patent number: 7214701Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ?in which W, X, Y, Z, A, B, D and G are each as defined in the disclosure, and (b) specified agonists or antagonists of nicotinic acetylcholine receptors.Type: GrantFiled: June 25, 2004Date of Patent: May 8, 2007Assignee: Bayer CropScience AGInventors: Reiner Fischer, Christoph Erdelen
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Patent number: 7208597Abstract: Triazine derivatives of formula (1) wherein R1 is C1–C20alkyl; C3–C7cycloalkyl; or C1–C20perfluoroalkyl; R2 is hydrogen; C1–C20alkyl; or C3–C7cycloalkyl; and R3 is hydrogen; C1–C20alkyl; C3–C7cycloalky; C1–C20perfluoroalky; C1C20alkyl-carbonyl; C3–C7cycloalkyl-carbonyl; C1–C20perfluoroalkyl-carbonyl; or phenylcarbonyl; are described. The compounds exhibit pronounced action against gram-positive and gram-negative bacteria and also against yeasts and moulds.Type: GrantFiled: July 22, 2003Date of Patent: April 24, 2007Assignee: Ciba Specialty Chemicals CorporationInventors: Werner Hölzl, Gabriele Eichacker, Andrea Preuss
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Patent number: 7205298Abstract: The present invention provides substituted 1,3,5-triazine compounds as kinase inhibitors and a method for treating or ameliorating a kinase mediated disorder.Type: GrantFiled: July 18, 2003Date of Patent: April 17, 2007Assignee: Janssen Pharmaceutica N.V.Inventors: Gee-Hong Kuo, Alan DeAngelis, Aihua Wang, Yan Zhang, Stuart L. Emanuel, Steve Middleton
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Patent number: 7205302Abstract: The present invention provides a compound which is useful as a PGI2 receptor agonist, and a pharmaceutical composition. The present invention is directed to a pharmaceutical composition comprising a compound represented by the following formula [1]: (R1 and R2 are the same or different and each represents optionally substituted aryl, Y represents N or CH, Z represents N or CH, A represents NH, NR5, O, S, or ethylene, R5 represents alkyl, D represents alkylene or alkenylene, E represents phenylene or single bond, G represents O, S, or CH2, R3 and R4 are the same or different and each represents hydrogen or alkyl, Q represents carboxy, alkoxycarbonyl, tetrazolyl, carbamoyl, or N-(alkylsulfonyl)carbamoyl), or a pharmaceutically acceptable salt thereof as an active ingredient.Type: GrantFiled: April 25, 2002Date of Patent: April 17, 2007Assignee: Nippon Shinyaku Co., Ltd.Inventors: Tetsuo Asaki, Taisuke Hamamoto, Keiichi Kuwano
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Patent number: 7189720Abstract: This invention is directed to triazine derivatives, bicyclic compounds and tricyclic compounds which are selective antagonists for a NPY (Y5) receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of this invention and a pharmaceutically acceptable carrier. This invention provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The invention further provides the use of a compound of the invention for the preparation of a pharmaceutical composition for treating an abnormality, wherein the abnormality is alleviated by decreasing the activity of a human Y5 receptor.Type: GrantFiled: April 6, 2005Date of Patent: March 13, 2007Assignee: H. Lundbeck A/SInventors: Mohammad R. Marzabadi, Stewart A. Noble, Mahesh N. Desai
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Patent number: 7173032Abstract: The present invention relates to methods and compositions comprising compounds that treat pathophysiological conditions arising from inflammatory responses. In particular, the present invention is directed to compounds that inhibit or block glycated protein produced induction of the signaling-associated inflammatory response in endothelial cells. The present invention relates to compounds that inhibit smooth muscle proliferation. In particular, the present invention is directed to compounds that inhibit smooth muscle cell proliferation by modulating HSPGs such as Perlecan. The present invention further relates to the use of compounds to treat vascular occlusive conditions characterized by smooth muscle proliferation such as restenosis and atherosclerosis.Type: GrantFiled: March 17, 2003Date of Patent: February 6, 2007Assignee: Reddy US Therapeutics, Inc.Inventors: Richard T. Timmer, Christopher W. Alexander, Sivaram Pillarisetti, Uday Saxena, Karen A. Campbell
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Patent number: 7173038Abstract: The invention relates to quinazoline derivatives of formula (I), wherein m is an integer from 1 to 3; R1 represents halogeno or C1-3alkyl; X1 represents —O—; R2 is selected from one of the following three groups: 1) C1-5alkylR3 (wherein R3 is piperidin-4-yl which may bear one or two substituents selected from hydroxy, halogeno, C1-4hydroxyalkyl and C1-4alkoxy; 2) C2-5alkenylR3 (wherein R3 is as defined hereinbefore); 3) C2-5alkynylR3 (wherein R3 is as defined hereinbefore); and wherein any alkyl, alkenyl or alkynyl group may bear one or more substituents selected from hydroxy, halogeno and amino; and salts thereof, processes for their preparation, pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as a active ingredient. The compounds of formula (I) and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of number of disease states including cancer and rheumatoid arthritis.Type: GrantFiled: November 1, 2000Date of Patent: February 6, 2007Assignee: AstraZeneca ABInventors: Andrew Peter Thomas, Elaine Sophie Elizabeth Stokes, Laurent Francois Andre Hennequin
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Patent number: 7169785Abstract: The present invention relates to methods and compositions comprising compounds that treat pathophysiological conditions arising from inflammatory responses. In particular, the present invention is directed to compounds that inhibit or block glycated protein produced induction of the signaling-associated inflammatory response in endothelial cells. The present invention relates to compounds that inhibit smooth muscle proliferation. In particular, the present invention is directed to compounds that inhibit smooth muscle cell proliferation by modulating HSPGs such as Perlecan. The present invention further relates to the use of compounds to treat vascular occlusive conditions characterized by smooth muscle proliferation such as restenosis and atherosclerosis.Type: GrantFiled: March 26, 2003Date of Patent: January 30, 2007Assignee: Reddy US Therapeutics, Inc.Inventors: Richard T. Timmer, Christopher W. Alexander, Sivaram Pillarisetti, Uday Saxena, Koteswar Rao Yeleswarapu, Manojit Pal, Jangalgar Tirupathy Reddy, Velagala Venkata Rama Murali Krishma Reddy, Sesha Sridevi Alluri, Potlapally Rajender Kumar, Gaddam Om Reddy
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Patent number: 7166602Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]triazine compounds as inhibitors of kinases such as, for example, cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the kinases using such compounds or pharmaceutical compositions.Type: GrantFiled: January 19, 2006Date of Patent: January 23, 2007Assignee: Schering CorporationInventors: Timothy J. Guzi, Kamil Paruch
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Patent number: 7157078Abstract: This invention relates to devices, kits, and methods for eliminating termite colonies. The kits, devices, and methods employ a termiticidal bait matrix containing a) a termiticide selected such that the termiticide causes death to about 50 to about 100% of termites within about 24 to about 84 days after the termites begin to ingest the termiticide or the bait matrix comprising the termiticide, b) a cellulose containing material, and c) water. The termiticidal bait matrix can be used in a bait station installed in the ground. The kits are suitable to be used by consumers in their homes.Type: GrantFiled: February 2, 2004Date of Patent: January 2, 2007Assignee: The University of Florida Research Foundation, Inc.Inventors: Philip Frederick Brode, III, Garry Steven Garren, Leo Timothy Laughlin, Randall Stryker Matthews, Dale Edwin Barker, Daniel James Kinne, Gary Eugene McKibben, Christopher Miles Miller, Timothy Robert Probst
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Patent number: 7148221Abstract: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, dType: GrantFiled: August 1, 2005Date of Patent: December 12, 2006Assignee: Amgen Inc.Inventors: Elizabeth M. Doherty, Jiawang Zhu, Markian Stec, Mark H. Norman, Hui-Ling Wang, Christopher H. Fotsch, Ning Chen, Partha P. Chakrabarti, Celia Dominguez, James Richard Falsey, Christopher Hulme, Jodie Katon, Thomas Nixey, Vassil I. Ognyanov, Liping H. Pettus, Robert Michael Rzasa
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Patent number: 7132448Abstract: A topical insecticide is provided which can be safe to use and avoids many common deleterious side effects of conventional topical insecticides. The insecticide contains an insecticide and an insect growth regulator effective for killing fleas, flea larvae and flea eggs. The insecticide is formulated by dissolving an insecticidal (tetrahydro-3-furanyl) methylamine derivative or a chloronicotinyl insecticide and an insect growth regulator (IGR) in a solvent containing a quaternary ammonium salt to increase the solvency of the IGR component, thereby providing an insecticide having high insecticidal activity.Type: GrantFiled: August 3, 2004Date of Patent: November 7, 2006Assignee: The Hartz Mountain CorporationInventors: Ian W. Cottrell, Albert Ahn, Richard Fisher, Christine M. Monro, Pierre R. Joseph
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Patent number: 7132423Abstract: The present invention relates to methods and compositions comprising compounds that treat pathophysiological conditions arising from inflammatory responses. In particular, the present invention is directed to compounds that inhibit or block glycated protein produced induction of the signaling-associated inflammatory response in endothelial cells. The present invention relates to compounds that inhibit smooth muscle proliferation. In particular, the present invention is directed to compounds that inhibit smooth muscle cell proliferation by modulating HSPGs such as Perlecan. The present invention further relates to the use of compounds to treat vascular occlusive conditions characterized by smooth muscle proliferation such as restenosis and atherosclerosis.Type: GrantFiled: March 26, 2003Date of Patent: November 7, 2006Assignee: Reddy US Therapeutics, Inc.Inventors: Richard T. Timmer, Christopher W. Alexander, Sivaram Pillarisetti, Uday Saxena, Koteswar Rao Yeleswarapu, Manojit Pal, Jangalgar Tirupathy Reddy, Velagala Venkata Rama Murali Krishna Reddy, Sesha Sridevi Alluri, Potlapally Rajender Kumar, Gaddam Om Reddy
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Patent number: 7109329Abstract: This invention provides pharmacologically active compounds having neurological and other bio-active capability. These active compounds comprise the derivatives of guanidino, aminoguanidino, 2-imadazolino, 2-hydrazinoimidazolino or 2-guanidinobenzimidazolino groups.Type: GrantFiled: July 1, 2002Date of Patent: September 19, 2006Inventor: N. Eric Naftchi
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Patent number: 7084138Abstract: The invention relates to novel active compound combinations having very good insecticidal and acaricidal properties and containing (a) cyclic ketoenols having the formula in which the groups W, X, Y, Z, A, B, D, and G have the meanings given in the disclosure, and (b) the active compounds (1) to (22) listed in the disclosure.Type: GrantFiled: August 23, 2001Date of Patent: August 1, 2006Assignee: Bayer CropScience AGInventors: Reiner Fischer, Christoph Erdelen
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Patent number: 7064129Abstract: Compounds are provided which are represented by the formula: where the structural variables are defined herein. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers.Type: GrantFiled: August 18, 2004Date of Patent: June 20, 2006Assignee: Parion Sciences, Inc.Inventors: Michael R. Johnson, Bruce Molino, Jianzhong Zhang, Bruce Sargent
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Patent number: 7045495Abstract: This invention provides methods for screening a modulating agent which when combined with antitumor therapeutic agent increases apoptosis in tumor cells. This invention also provides methods for screening antitumor therapeutic agents suitable for combination therapy with a protein kinase C inhibitors capable of potentiating apoptosis in tumor cells. This invention further provides different combination therapies comprising the specific protein kinase C inhibitors and the antitumor therapeutic agents.Type: GrantFiled: August 7, 2002Date of Patent: May 16, 2006Assignee: Sloan-Kettering Institute for Cancer ResearchInventors: Gary K. Schwartz, Anthony P. Albino
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Patent number: 7034021Abstract: The invention concerns compounds of general formula (I) wherein: R1, R2, R3, R4, R5 and R6 are as defined in Claim 1. Said compounds are useful in the treatment of pathologies related to the insulin-resistance syndrome.Type: GrantFiled: January 25, 2001Date of Patent: April 25, 2006Assignee: LIPHAInventors: Gérard Moinet, Daniel Cravo, Liliane Doare, Micheline Kergoat, Didier Mesangeau
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Patent number: 7008903Abstract: The present invention provides a composition comprising synergistic amounts of a compound of the formula (I) wherein X, E, R, A and Z are as defined herein, and at least one fungicidal active compound as defined herein. The compositions of the present invention find use as pesticides.Type: GrantFiled: June 3, 2002Date of Patent: March 7, 2006Assignee: Bayer AktiengesellschaftInventors: Stefan Dutzmann, Christoph Erdelen, Wolfram Andersch, Heinz-Wilhelm Dehne, Jürgen Hartwig, Klaus Stenzel, Wolfgang Krämer
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Patent number: 7001903Abstract: The invention relates to insecticidal mixtures of spinosyns and agonists or antagonists of nicotinic acetylcholine receptors for protecting plants against attack by pests.Type: GrantFiled: December 12, 2003Date of Patent: February 21, 2006Assignee: Bayer AktiengesellschaftInventors: Wolfram Andersch, Hans-Jürgen Schnorbach, Detlef Wollweber
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Patent number: 6984662Abstract: A topical insecticide is provided which can be safe to use and avoids many common deleterious side effects of conventional topical insecticides. The insecticide contains an insecticide and an insect growth regulator effective for killing fleas, flea larvae and flea eggs. The insecticide is formulated by dissolving an insecticidal (tetrahydro-3-furanyl) methylamine derivative and an insect growth regulator (IGR) in a solvent containing a quaternary ammonium salt to increase the solvency of the IGR component, thereby providing an insecticide having high insecticidal activity.Type: GrantFiled: November 3, 2003Date of Patent: January 10, 2006Assignee: The Hartz Mountain CorporationInventors: Ian W. Cottrell, Christine M. Monro, Pierre R. Joseph, Albert Ahn, Richard Fisher
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Patent number: 6962916Abstract: This invention concerns the compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein R1 and R2 are each independently selected from hydrogen; hydroxy; amino; optionally substituted C1-6alkyl; C1-6alkyloxy; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; Ar1; mono- or di(C1-6alkyl)amino; mono- or di(C1-6alkyl)aminocarbonyl; dihydro-2(3H)-furanone; or R1 and R2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C1-6alkyl)amino-C1-4alkylidene; R3 is hydrogen, Ar1, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl, C1-6alkyl substituted with C1-6alkyloxycarbonyl; and R4, R5, R6, R7 and R8 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl or trihalomethyloxy; L is optionally substituted C1-10alkyl; C3-10alkenyl; C3-10alkynyl; C3-7cycloalkyl; Ar1 is optionally substituted phenyl; for the manufacture of a medicine for the treatment of sType: GrantFiled: March 26, 2003Date of Patent: November 8, 2005Assignee: Janssen Pharmaceutica N.V.Inventors: Paul A. J. Janssen, Jan Heeres, Henri E. L. Moereels, Michael Joseph Kukla, Donald W. Ludovici
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Patent number: 6953798Abstract: Alkanoic acid derivatives of formula (1) are described: Ar1(Alka)rL1Ar2CH(R1)C(Ra)(Ra?)R??(1) Ar1 is an optionally substituted aromatic or heteroarotic group; L1 is a covalent bond or a linker atom or group; Ar2 is an optionally substituted phenylene or nitrogen-containing six-membered heteroarylene group; R is a carboxylic acid (—CO2H) or a derivative thereof; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of ?4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.Type: GrantFiled: November 29, 1999Date of Patent: October 11, 2005Assignee: Celltech R&D LimitedInventors: John Robert Porter, John Clifford Head, Graham John Warrellow, Sarah Catherine Archibald
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Patent number: 6949544Abstract: The present invention provide a compound of formula I or II: or a pharmaceutically acceptable derivative thereof, wherein R1, R2, R3, and R4 are as described in the specification. These compounds are inhibitors of protein kinase, particularly inhibitors of JNK, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli; and Src-family kinases, especially Src and Lck kinases. These compounds are also inhibitors of GSK3 and CDK2 kinases. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: GrantFiled: March 28, 2002Date of Patent: September 27, 2005Assignee: Vertex Pharmaceuticals IncorporatedInventors: Randy S. Bethiel, John Cochran, Young-Choon Moon, Suganthini Nanthakumar
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Patent number: 6919339Abstract: The present invention provides compounds that elevate cellular expression of the ABCA-1 gene, promoting cholesterol efflux from cells and increasing HDL levels in the plasma of a mammal, in particular humans. The compounds are useful for treating coronary artery disease.Type: GrantFiled: December 4, 2001Date of Patent: July 19, 2005Assignee: CV Theapeutics, Inc.Inventors: Michael Campbell, Prabha N. Ibrahim, Jeff A. Zablocki, Richard Lawn
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Patent number: 6894047Abstract: This invention is directed to sorbitol dehydrogenase inhibitory compounds of formula I wherein R1, R2 and R3 are as defined in the specification. This invention is also directed to pharmaceutical compositions containing these compounds and to methods of treating or preventing diabetic complications, particularly diabetic neuropathy, diabetic nephropathy, diabetic microangiopathy, diabetic macroangiopathy, diabetic cardiomyopathy and foot ulcers.Type: GrantFiled: March 26, 2002Date of Patent: May 17, 2005Assignee: Pfizer Inc.Inventor: Banavara L. Mylari
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Patent number: 6887873Abstract: The present invention relates to cancer therapy and to novel anticancer agents having a mechanism of action which is quite specific. It also relates to novel chemical compounds as well as their therapeutic application in humans.Type: GrantFiled: March 25, 2002Date of Patent: May 3, 2005Assignee: Aventis Pharma S.A.Inventors: Patrick Mailliet, Abdelazize Laoui, Jean-François Riou, Gilles Doerflinger, Jean-Louis Mergny, François Hamy, Thomas Caulfield
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Patent number: 6864256Abstract: The present invention provides methods for the control of insect pests in the vicinity of feces or manure of a domestic animal. Such methods comprise orally administering cyromazine, wherein said administering results in the presence of an insecticidal amount of cyromazine in the feces of the animal being treated. The present invention further provides methods for inhibiting the development of fly larvae on feces or manure of a domestic animal. Such methods also comprise orally administering cyromazine, wherein said administering results in the presence of an insecticidal amount of cyromazine in the feces of the animal being treated.Type: GrantFiled: August 29, 2002Date of Patent: March 8, 2005Assignee: Tria Specialty Products, LLCInventor: Kathleen G. Palma
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Patent number: 6858609Abstract: This invention concerns the compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein R1 and R2 are each independently selected from hydrogen; hydroxy; amino; optionally substituted C1-6alkyl; C1-6alkyloxy; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; Ar1; mono- or di(C1-6alkyl)amino; mono- or di(C1-6alkyl)-aminocarbonyl; dihydro-2(3H7)-furanone; or R1 and R2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C1-6alkyl)amino-C1-4alkylidene; R3 is hydrogen, Ar1, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxy-carbonyl, C1-6alkyl substituted with C1-6alkyloxycarbonyl; and R4, R5, R6, R7 and R8 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl or trihalomethyloxy; L is optionally substituted C1-10alkyl; C3-10alkenyl; C3-10alkynyl; C3-7cycloalkyl; Ar1 is optionally substituted phenyl; for the manufacture of a medicine for the treatment oType: GrantFiled: November 15, 2001Date of Patent: February 22, 2005Assignee: Janssen Pharmaceutica N.V.Inventors: Paul A. J. Janssen, Jan Heeres, Henri E. L. Moereels, Michael Joseph Kukla, Donald W. Ludovici
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Patent number: 6858599Abstract: This invention relates to tricyclic compounds having spiro union represented by the following formula (I) or its salt which is useful as a drug, and in particular, as an inhibitor for activated blood coagulation factor X, which can be administered orally and which exhibits strong anticoagulation action. The invention also relates to a pharmacophore which was derived from the compound and is useful in molecular designing of the FXa inhibitor.Type: GrantFiled: December 27, 2001Date of Patent: February 22, 2005Assignee: Mochida Pharmaceutical Co., Ltd.Inventors: Hidemitsu Nishida, Fumihiko Saitoh, Kousuke Harada, Ikuya Shiromizu, Takafumi Mukaihira
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Patent number: 6852717Abstract: Disclosed are compounds useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds.Type: GrantFiled: May 10, 2002Date of Patent: February 8, 2005Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Pier Francesco Cirillo, Daniel R. Goldberg, Abdelhakim Hammach, Neil Moss, John Robinson Regan
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Patent number: 6849627Abstract: The present invention relates to compounds which are capable of preventing the extracellular release of inflammatory cytokines, said compounds, including all enantiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, have the formula: wherein R1 is substituted aryl; R4 is substituted or unsubstituted aryl or heteroaryl.Type: GrantFiled: March 17, 2003Date of Patent: February 1, 2005Assignee: The Procter & Gamble CompanyInventors: Michael Philip Clark, Matthew John Laufersweiler, Adam Golebiowski, Mark Sabat, Todd Andrew Brugel
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Patent number: 6815459Abstract: The present invention provides novel seleno compounds containing nitrone moiety, a process for preparing the same, the use of the novel compounds as therapeutics for treating and/or preventing various medical dysfunctions and diseases arising from reactive oxygen species, in particular stroke, Parkinson's disease, Alzheimer's disease. The compounds of the invention have similar or superior lipid peroxidation (LPO) inhibition activity to the reference compounds. While showing lower toxicity and better water solubility, they also effectively inhibit the cerebral neuronal cell death caused by ROS and show neuroprotective effects against ischemic neuronal degeneration.Type: GrantFiled: June 6, 2003Date of Patent: November 9, 2004Assignee: Sam-Sung Electronics Co., Ltd.Inventors: Sung-Bo Ko, Eu-Gene Oh, Eon-Kyeom Kim, Won-Yeob Kim, Dennis W. Choi, Laura L. Dugan, Jae-Young Koh, Moo-Ho Won, Myung-Bok Wie