Ring Sulfur In The Polycyclo Ring System Patents (Class 514/324)
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Patent number: 7462630Abstract: The invention relates to a compound represented by the following general formula (1) or its analogue, which selectively inhibit N-type calcium channels or its analogue, and to a method for treating pain etc. comprising the compound represented by the following general formula (1) or its analogue to a patient in need of such treatment: wherein, A represents CH?CH, etc., a, b, c and d represents CH etc., R1, R2, R3, R4, R5 and R6 represents H etc., V—W represents C?C, etc., n represents 0 to 3, Y1 represents O etc., B represents —(CH2)vCHR21 wherein v is 0 to 3, R21 represents H, a lower alkyl group or the like, etc., G represents —CO—, a covalent bond, etc., m is 0 to 6, R7 and R8 represents H, a lower alkyl group, —COR18a, —COOR20 wherein R18a and R20 each represents a lower alkyl group or the like, etc.Type: GrantFiled: February 27, 2004Date of Patent: December 9, 2008Assignee: Ajinomoto Co., Inc.Inventors: Takashi Yamamoto, Seiji Niwa, Kayo Otani, Seiji Ohno, Hajime Koganei, Satoshi Iwayama, Akira Takahara, Yukitsugu Ono, Tomoko Takeda, Shinichi Fujita, Keiko Moki
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Publication number: 20080300277Abstract: The present invention describes in particular a method for stabilizing a pharmaceutical composition by contacting said composition with a polymeric material comprising in particular an ethylene oxide sterilization step.Type: ApplicationFiled: January 18, 2008Publication date: December 4, 2008Inventors: Andrea Fetz, Georg Ludwig Kis, Michel Pepiot
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Publication number: 20080287498Abstract: Racemic norketotifen, racemic 10-hydroxy-ketotifen, racemic 10-hydroxy-nor-ketotifen and optically active isomers of ketotifen, norketotifen, 10-hydroxy-ketotifen and 10-hydroxy-norketotifen were found to have antiallergic and anti-inflammatory effects while being devoid of the severe dose-limiting sedative side effects of Ketotifen.Type: ApplicationFiled: April 30, 2007Publication date: November 20, 2008Inventors: A.K. Gunnar Aberg, George E. Wright, Jan L. Chen, Andrew T. Maioli
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Patent number: 7449483Abstract: The present invention relates to heteroaromate OSC inhibitors. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.Type: GrantFiled: December 6, 2006Date of Patent: November 11, 2008Assignee: Hoffman-La Roche Inc.Inventors: Johannes Aebi, Jean Ackermann, Henrietta Dehmlow, Hans-Peter Maerki, Olivier Morand
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Patent number: 7449453Abstract: A method of prevention or treatment of a cholesterol-associated tumor is provided which comprises administering a therapeutically effective amount of an azetidinone-based cholesterol absorption inhibitor, preferably ezetimibe (SCH 58235) and/or its phenolic glucuronide, or at least one ezetimibe analog, e.g., SCH 48461 and SCH 58053, to a patient wherein the patient is either at risk of developing a cholesterol-associated tumor or already exhibits a cholesterol-associated tumor. Formulations of ezetimibe are also provided for the prevention or treatment of a cholesterol-associated tumor further comprising at least one other anticancer agent.Type: GrantFiled: July 13, 2006Date of Patent: November 11, 2008Assignees: Karykion Inc., Children's Medical Center CorporationInventors: Carl P. Schaffner, Keith R. Solomon, Michael R. Freeman
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Publication number: 20080227814Abstract: The present invention relates to a selective estrogen receptor modulator selected from the group consisting of: (I) or a pharmaceutical salt thereof; useful, e.g., for treating endometriosis and uterine leiomyoma.Type: ApplicationFiled: January 18, 2005Publication date: September 18, 2008Inventors: Jeffrey Alan Dodge, Scott Alan Frank, Ronald Jay Hinklin, Owen Brendan Wallace
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Publication number: 20080207692Abstract: Ophthalmic compositions comprising ketotifen and a source of hydrogen peroxide providing an amount of hydrogen peroxide of from about 0.001 to about 0.1% (w/v) of hydrogen peroxide, and methods for the treatment and prevention of allergic conjunctivitis using these compositions are provided herein.Type: ApplicationFiled: April 15, 2008Publication date: August 28, 2008Inventors: Fu-Pao Tsao, Michelle Wong, Shau-Fong Yen
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Publication number: 20080207593Abstract: A once daily formulation containing the combination of a non-sedating or selective antihistamine (Loratadine) with a sedating or non-selective antihistamine (Chlorpheniramine) administered at bed-time has demonstrated greater efficacy in relieving allergic symptoms than Loratadine alone.Type: ApplicationFiled: August 20, 2007Publication date: August 28, 2008Inventors: Michael Heffernan, Jane C. Hirsh, Roman V. Rariy
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Publication number: 20080207691Abstract: The present invention provides compounds of formula I that are useful as potent and selective inhibitors of 11-beta hydroxysteroid dehydrogenase 1. The present invention further provides a pharmaceutical composition which comprises a compound of Formula I, or a pharmaceutical salt thereof, and a pharmaceutically acceptable carrier, diluent, or excipient. In addition, the present invention provides compositions comprising compounds of formula I for the treatment of metabolic syndrome, diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, other symptoms associated with hyperglycemia, and related disorders. Formula (I) wherein, Ru0 is (II), or (III) G1 is methylene or ethylene; L is a divalent linking group selected from —(C1-C4) alkylene-, —S—, —CH(OH)—, or —O—; A is methylene, —S—, —O—, or —NH—; and the other substituents are as defined in the claims.Type: ApplicationFiled: December 16, 2005Publication date: August 28, 2008Inventors: Thomas Daniel Aicher, Mark Joseph Chicarelli, Ronald Jay Hinklin, Hongqi Tian, Owen Brendan Wallace
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Publication number: 20080206194Abstract: A method for inducing ER? expression in cancer cells in a subject affected with cancer cells which are ER? (?) is disclosed. The method involves administering to the subject an effective amount of a PPAR? antagonist alone or in combination with anti-estrogen therapy.Type: ApplicationFiled: February 12, 2008Publication date: August 28, 2008Inventors: Robert I. Glazer, Yuzhi Yin, Levy Kopelovich
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Publication number: 20080207530Abstract: The invention provides a method for the treatment of COPD and/or gastrointestinal disease conditions ameliorated by histamine management in a subject, comprising administering to the subject an effective amount of a histidine decarboxylase inhibitor.Type: ApplicationFiled: February 12, 2008Publication date: August 28, 2008Inventors: Michalis Nicolaou, Emile Loria, Gaetan Terrasse, Yves Trehin
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Patent number: 7393864Abstract: The present invention provides methods for the modulation of vascular tone in a patient having compromised vascular tissue, which methods comprise the administration of a chloride channel blocking agent or a pharmaceutically acceptable salt thereof.Type: GrantFiled: August 15, 2001Date of Patent: July 1, 2008Assignee: University of Iowa Research FoundationInventors: Fred S. Lamb, Brian C. Schutte, Baoli Yang
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Publication number: 20080139513Abstract: A composition for transdermal delivery of a non-traditional active agent is described. The compositions comprise: (a) a non-traditional transdermal active agent; (b) a solvent; (c) a non-miscible liquid; (d) a stabilizer; and (e) water, wherein the composition is formulated into an emulsion.Type: ApplicationFiled: September 26, 2007Publication date: June 12, 2008Inventors: Robert Lee, Dinesh Shenoy, Steve Bandak
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Patent number: 7381721Abstract: 3,4-Disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.Type: GrantFiled: March 17, 2003Date of Patent: June 3, 2008Assignee: Adolor CorporationInventors: Roland Ellwood Dolle, Bertrand Le Bourdonnec
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Publication number: 20080124402Abstract: Compounds of structural formula (I) are modulators of the androgen receptor (AR) in a tissue selective manner.Type: ApplicationFiled: October 25, 2005Publication date: May 29, 2008Applicant: MERCK & CO., INC.Inventors: Yuntae Kim, Joshua Close, Mark E. Duggan, Barbara Hanney, Robert S. Meissner, Jeffrey Musselman, James J. Perkins, Jiabing Wang
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Publication number: 20080124376Abstract: Described herein are stable ocular devices that immobilize and deliver bioactive agents to the eye over sustained periods of time. Also described herein are methods of making and using the ocular devices.Type: ApplicationFiled: November 5, 2007Publication date: May 29, 2008Applicant: NOVARTIS AGInventors: John Dallas PRUITT, Lynn Cook WINTERTON, John Martin LALLY
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Patent number: 7345060Abstract: The invention is directed to compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7a, R7b, W, G1, G2, a, b, c, d and m are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: GrantFiled: November 19, 2004Date of Patent: March 18, 2008Assignee: Theravance, Inc.Inventors: Mathai Mammen, Sarah Dunham
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Patent number: 7326716Abstract: The present invention provides a method of treating inflammatory bowel disease which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a piperidinyl prostaglandin E analog.Type: GrantFiled: November 29, 2004Date of Patent: February 5, 2008Assignee: Allergan, Inc.Inventors: David W. Old, Danny T. Dinh, Karen M. Kedzie, Daniel W. Gil, Wha Bin Im
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Patent number: 7319104Abstract: Compounds of formula (1) or a pharmaceutically acceptable salt, solvate, acid isostere, or hydrolyzable ester thereof, are disclosed. Methods of making and using the compounds are also disclosed.Type: GrantFiled: February 25, 2003Date of Patent: January 15, 2008Assignee: SmithKline Beecham CorporationInventors: Rodolfo Cadilla, Brad Richard Henke, Millard H. Lambert, III, Guangcheng Kevin Liu, Jennifer Susan Smith
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Patent number: 7312222Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.Type: GrantFiled: March 25, 2004Date of Patent: December 25, 2007Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Soo S. Ko, George V. Delucca, John V. Duncia, Joseph B. Santella, III, Dean A. Wacker
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Patent number: 7309691Abstract: The invention relates to a pharmaceutical combined preparation of LHRH analogues and anti-oestrogens having tissue-selective oestrogen activity and also to its use for the treatment of gynaecological disorders, especially for the treatment of endometrioses and myomas.Type: GrantFiled: January 29, 1997Date of Patent: December 18, 2007Assignee: Achering AktiengesellschaftInventors: Klaus Stöckemann, Peter Muhn
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Patent number: 7282497Abstract: The invention relates to compounds of formula (Ic) processes for their preparation, pharmaceutical compositions containing them and to their use in medicine, particularly use in the amelioration of a clinical condition for which a Factor Xa inhibitor is indicated.Type: GrantFiled: March 17, 2006Date of Patent: October 16, 2007Assignee: Glaxo Group LimitedInventors: Chuen Chan, Julie Nicole Hamblin, Henry Anderson Kelly, Nigel Paul King, Andrew McMurtrie Mason, Vipulkumar Kantibhai Patel, Stefan Senger, Gita Punjabhai Shah, Nigel Stephen Watson, Helen Elisabeth Weston, Caroline Whitworth, Robert John Young
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Patent number: 7241789Abstract: The present invention relates to novel substituted indole compounds that are antagonists of alpha V (?v) integrins, for example ?v?3 and ?v?5 integrins, their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. The compounds may be used in the treatment of pathological conditions mediated by ?v?3 and ?v?5 integrins, including such conditions as tumor growth, metastasis, restenosis, osteoporosis, inflammation, macular degeneration, diabetic retinopathy, and rheumatoid arthritis. The compounds have the general formula: where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, D, X, W, a, m, n, i, j, k and v are defined herein.Type: GrantFiled: December 6, 2004Date of Patent: July 10, 2007Assignee: 3-Dimensional Pharmaceutical, Inc.Inventors: Tianbo Lu, Bruce E. Tomczuk, Louis V. LaFrance, Thomas P. Markotan, Juan J. Marugan Sanchez, Victor J. Marder, David C. U'Prichard, Beth M. Anaclerio, Zihong Guo, Wenzi Pan, Kristi A. Leonard
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Patent number: 7238713Abstract: Compounds and methods are provided for the treatment of disease conditions in which modification of cholinergic, especially muscarinic m1, m4, or both m1 and m4, receptor activity has a beneficial effect. In the method, an effective amount of a compound is administered to a patient in need of such treatment.Type: GrantFiled: July 17, 2003Date of Patent: July 3, 2007Assignee: Acadia Pharmaceuticals, Inc.Inventors: Carl-Magnus A. Anderson, Bo Lennart M. Friberg, Niels Skjaerbaek, Tracy A. Spalding, Allan K. Uldam
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Patent number: 7226934Abstract: Racemic norketotifen, racemic 10-hydroxy-ketotifen, racemic 10-hydroxy-nor-ketotifen and optically active isomers of ketotifen, norketotifen, 10-hydroxy-ketotifen and 10-hydroxy-norketotifen were found to have antiallergic and anti-inflammatory effects while being devoid of the severe dose-limiting sedative side effects of ketotifen.Type: GrantFiled: September 12, 2000Date of Patent: June 5, 2007Assignee: Bridge Pharma, Inc.Inventors: A. K. Gunnar Aberg, George E. Wright, Jan L. Chen, Andrew T. Maioli
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Patent number: 7214692Abstract: The present invention relates to the use of tachykinin antagonists, including substance P antagonists and other neurokinin antagonists, in the treatment of emesis. Also described are novel tachykinin antagonists of formula (I), processes for their preparation, pharmaceutical compositions containing them and their medical use. wherein R represents the ring A or 2-pyridinyl or 2-pyridinyl-N-oxide; R1 is selected from halogen atoms and C1-4alkyl, C1-4alkoxy, trifluoromethyl, and S(O)nC1-4alkyl groups; R2 and R3, which may be the same or different, each independently are selected from hydrogen and halogen atoms and C1-4alkyl, C1-4alkoxy, trifluoromethyl and cyano groups; n represents zero, 1 or 2; and pharmaceutically acceptable salts and solvates thereof.Type: GrantFiled: November 5, 2001Date of Patent: May 8, 2007Assignee: Glaxo Group LimitedInventors: Russell Michael Hagan, Keith Thomas Bunce
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Patent number: 7189757Abstract: The invention is directed to compositions used for treating Central Nervous System (CNS) disorders. In addition, the invention provides convenient methods of treatment of a CNS disorder. Furthermore, the invention provides methods of treating sleep disorders using compositions that remain active for a discrete period of time to reduce side effects. More specifically, the invention is directed to the compositions and use of derivatized, e.g., ester or carboxylic acid derivatized, antihistamine antagonists for the treatment of sleep disorders.Type: GrantFiled: October 16, 2002Date of Patent: March 13, 2007Assignee: Hypnion, Inc.Inventors: Dale M. Edgar, David G. Hangauer, Harry Jefferson Leighton, Emmanuel J. M. Mignot
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Patent number: 7169768Abstract: A method of decreasing atherosclerosis and its complications including but not limited to myocardial infarction, stroke and peripheral vascular disease wherein the method involves administering to a human or an animal an amount of an inhibitor of the release of LHRH or GnRH.Type: GrantFiled: June 3, 1998Date of Patent: January 30, 2007Inventors: Kenneth M. Weisman, Michael Goldberg
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Patent number: 7153868Abstract: The present invention provides a method of treatment of a subject suffering from a disease, such as schizophrenia, for which the administration of an NK-3 antagonist is indicated which comprises administering to that subject a therapeutically effective amount of a compound of formula I: wherein, generally, Q is R1 is benzyl, phenyl, thiophene or imidazolyl optionally substituted with C1-4alkyl or halogen, such as methyl, fluorine or bromine; R2 is hydrogen or C1-4alkyl such as methyl; R3 is phenyl; R4 is hydrogen; R5 is hydrogen or C1-6alkylcarbonyl such as methylcarbonyl; X is —SO2— or —C(O)N(R2)SO2— where R2 is preferably hydrogen; Y is a bond, CH2 or Z1 where Z1 is —N(Rf)— in which Rf is C1-6alkylcarbonyl such as ethylcarbonyl; and R6 is phenyl, pyrazolyl, pyridyl, pyrimidinyl or benzimidazolonyl optionally substituted with one or two groups chosen from C1-6alkyl and benzyl, such as methyl, ethyl and benzyl; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: April 16, 2003Date of Patent: December 26, 2006Assignee: Merck Sharp & Dohme Ltd.Inventors: Mark Stuart Chambers, Philip Jones, Helen Jane Szekeres
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Patent number: 7148240Abstract: The invention relates to benzofuran or benzothiophene derivatives of general formula: These compounds are of use as medicinal products, in particular in the treatment of pathological syndromes of the cardiovascular system.Type: GrantFiled: August 23, 2001Date of Patent: December 12, 2006Assignee: Sanofi-AventisInventors: Jean-Louis Assens, Claude Bernhart, Frédérique Cabanel-Haudricourt, Dino Nisato
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Patent number: 7144883Abstract: The present invention relates to substituted sulfonamide compounds of the general formula (I), wherein P is sulfonamide or amide-substituted sulfonic acid, which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II diabetes and/or disorders of the central nervous systemType: GrantFiled: June 11, 2002Date of Patent: December 5, 2006Assignee: Biovitrum ABInventors: Patrizia Caldirola, Gary Johansson, Andrew Mott, Katarina Beierlien, Markus Thor, Lars Tedenborg, Ulf Bremberg, Annika Jenmalm Jensen
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Patent number: 7135483Abstract: Substituted heterocyclinc compounds are disclosed. The compounds are useful for treating multidrug resistance. The compounds can be formulated in compositions with a carrier and, optionally, a therapeutic agent.Type: GrantFiled: November 29, 2001Date of Patent: November 14, 2006Assignee: H. Lee Moffitt Cancer Center & Research Institute, Inc.Inventors: Charles Raymond Degenhardt, David Joseph Eickhoff
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Patent number: 7112594Abstract: Compounds represented by the following general formula (I) wherein ring A is benzene, cyclohexane, pyridine, piperidine, a derivative thereof, imidazole, a derivative thereof, etc.; the ring B represents benzene, cyclohexane, pyrrole or a derivative thereof, furan, thiophene, etc.; R1, R2 and R3 represent each hydrogen, alkyl, halogen, hydroxyl, alkoxy, etc.; W represents hydrogen, alkyl or hydroxycarbonylalkyl; X represents halogen, cyano, nitro, etc.; X? represents hydrogen, halogen, etc.; and Y represents alkyl, hydroxyalkyl, hydroxycarbonylalkyl, aminoalkyl, etc.; salt thereof, and drugs comprising these compounds. Because of having an exellent effect of inhibiting activated lymphocyte proliferation, these compounds are usefull as preventives or remedies for various autoimmune diseases.Type: GrantFiled: August 9, 2001Date of Patent: September 26, 2006Assignee: Mitsubishi Pharma CorporationInventors: Hiroyuki Ushio, Youichiro Naito, Naoki Sugiyama, Takafumi Kawaguchi, Makio Ohtsuki, Kenji Chiba
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Patent number: 7098198Abstract: A method of prevention or treatment of a cholesterol-associated tumor is provided which comprises administering a therapeutically effective amount of an azetidinone-based cholesterol absorption inhibitor, preferably ezetimibe (SCH 58235) and/or its phenolic glucuronide, or at least one ezetimibe analog, e.g., SCH 48461 and SCH 58053, to a patient wherein the patient is either at risk of developing a cholesterol-associated tumor or already exhibits a cholesterol-associated tumor. Formulations of ezetimibe are also provided for the prevention or treatment of a cholesterol-associated tumor further comprising at least one other anticancer agent.Type: GrantFiled: May 12, 2005Date of Patent: August 29, 2006Assignee: Karykion, Inc.Inventors: Carl P. Schaffner, Keith R. Solomon
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Patent number: 7078059Abstract: The invention provides a method for enhancing bone formation, inhibiting osteoclastic differentiation and/or activating osteoblastic differentiation whereby to manage, treat or achieve prophylaxis of bone disease which comprises administering to a human or animal subject suffering from, or susceptible to bone disease a therapeutically or prophylactically effective amount of a lanthanum compound.Type: GrantFiled: June 26, 2001Date of Patent: July 18, 2006Assignee: Shire Holdings AGInventors: Nigel D. Atherton, Joseph William Totten, Michael David Gaitonde
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Patent number: 7060711Abstract: The present invention relates to derivatives of 4-(Thio- or Selenoxanthene-9-ylidene)-piperidine or acridine and pharmaceutically acceptable salts thereof, use of these compounds as a medicament and for the manufacture of a medicament for treatment of a disease state which can be alleviated by treatment with a 5-HT2B antagonist.Type: GrantFiled: October 25, 2002Date of Patent: June 13, 2006Assignee: Biofrontera Bioscience GmbHInventors: Hermann Lubbert, Christoph Ullmer, Emile Bellott, Mark Froimowitz, Douglas Gordon
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Patent number: 6984637Abstract: This invention relates to certain cyclic amine derivatives of Formula (I) that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.Type: GrantFiled: November 21, 2003Date of Patent: January 10, 2006Assignee: Syntex (U.S.A.) LLCInventors: Leyi Gong, Denis John Kertesz, David Bernard Smith, Francisco Xavier Talamas, Robert Stephen Wilhelm
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Patent number: 6977263Abstract: Provided herein are novel and useful compounds having a tryptase inhibition activity, pharmaceutical compositions comprising such compounds, and methods treating subjects suffering from a condition, disease, or disorder that can be ameliorated by the administration of an inhibitor of tryptase, e.g., asthma and inflammatory diseases, to name only a few.Type: GrantFiled: April 26, 2001Date of Patent: December 20, 2005Assignee: Aventis Pharmaceuticals Inc.Inventors: Peter C. Astles, Paul R. Eastwood, Olivier Houille, Julian Levell, Heinz Pauls, Mark Czekaj, Guyan Liang, Yong Gong, James Pribish, Kent Neuenschwander
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Patent number: 6977260Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; wherein X, Y, Z, D and R3 are as defined in the specification.Type: GrantFiled: January 22, 2004Date of Patent: December 20, 2005Assignee: Allergan, Inc.Inventors: David W. Old, Danny T. Dinh
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Patent number: 6951873Abstract: Methods for the treatment of age-related behavioral disorders in companion animals are disclosed. These comprise administering to a companion animal in need of such treatment a therapeutically effective amount of an acetylcholinesterase inhibitor. A preferred acetylcholinesterase inhibitor is a compound of Formula 1: Pharmaceutical compositions and dosage forms comprising a compound of Formula 1 are also disclosed.Type: GrantFiled: March 3, 2000Date of Patent: October 4, 2005Assignee: Pfizer Inc.Inventor: Kristin M. Lundy
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Patent number: 6933292Abstract: A method of prevention or treatment of a cholesterol-associated tumor is provided which comprises administering a therapeutically effective amount of an azetidinone-based cholesterol absorption inhibitor, preferably ezetimibe (SCH 58235) and/or its phenolic glucuronide, or at least one ezetimibe analog, e.g., SCH 48461 and SCH 58053, to a patient wherein the patient is either at risk of developing a cholesterol-associated tumor or already exhibits a cholesterol-associated tumor. Formulations of ezetimibe are also provided for the prevention or treatment of a cholesterol-associated tumor further comprising at least one other anticancer agent.Type: GrantFiled: July 30, 2003Date of Patent: August 23, 2005Assignee: Children's Medical Center CorporationInventors: Carl P. Schaffner, Keith R. Solomon, Michael R. Freeman
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Patent number: 6894064Abstract: This invention provides compounds of formula I and pharmaceutically acceptable salts and solvates thereof, characterized that the compound is in particulate form and having a specific size range. The present invention further provides pharmaceutical compositions containing or formulated using compounds of formula I, and the use of such compounds for alleviating human pathologies, including osteoporosis, serum lipid lowering, and breast cancer.Type: GrantFiled: March 26, 2004Date of Patent: May 17, 2005Assignee: Eli Lilly and CompanyInventors: Gordon Nelson Arbuthnot, Brian Weston Dalder, Kerry John Hartauer, Wayne Douglas Luke, Robert Eugene Stratford, Jr.
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Patent number: 6887888Abstract: Aqueous compositions of nonsteroidal triphenylethylene antiestrogens for pharmaceutical use comprising as a solubility enhancing agent a pharmaceutically acceptable mono- or dicarboxylic acid having 1-5 carbon atoms, wherein the carbon chain may further contain 1-4 hydroxyl, 1-3 oxo, or one or several halogen substituents, or a corresponding anion thereof, or methanesulfonic acid or its corresponding anion, in molar excess with respect to the triphenylethylene antiestrogen, optionally together with an organic water miscible co-solvent such as polyethylene glycol (PEG), propylene glycol, ethanol or isopropanol.Type: GrantFiled: April 8, 2003Date of Patent: May 3, 2005Assignee: Orion CorporationInventors: Kaija AF Ursin, Jukka Salmia, Heikki Niskanen, Pirjo Kortesuo, Mikko Kananen, Gunilla Örn, Juha Kiesvaara
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Patent number: 6878725Abstract: Compounds of formula (I) in which R2, X, Y, Cy, L and Lp(D)n have the meanings given in the specification, are inhibitors of the serine protease, Factor Xa and are useful in the treatment of cardiovascular disorders.Type: GrantFiled: June 12, 2001Date of Patent: April 12, 2005Assignee: Eli Lilly and CompanyInventors: John Walter Liebeschuetz, Christopher William Murray, Stephen Clinton Young, Nicholas Paul Camp, Stuart Donald Jones, William Alexander Wylie, John Joseph Masters, Michael Robert Wiley, Scott Martin Sheehan, David Birenbaum Engel, Brian Morgan Watson
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Patent number: 6797719Abstract: This invention provides compounds of formula I and pharmaceutically acceptable salts and solvates thereof, characterized that the compound is in particulate form and having a specific size range. The present invention further provides pharmaceutical compositions containing or formulated using compounds of formula I, and the use of such compounds for alleviating human pathologies, including osteoporosis, serum lipid lowering, and breast cancer.Type: GrantFiled: September 5, 2002Date of Patent: September 28, 2004Assignee: Eli Lilly and CompanyInventors: Gordon Nelson Arbuthnot, Brian Weston Dalder, Kerry John Hartauer, Wayne Douglas Luke, Robert Eugene Stratford, Jr.
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Patent number: 6784180Abstract: The present invention provides compounds of formula (I): which are useful for treating depression, anxiety, and alleviating the symptoms caused by withdrawal or partial withdrawal from the use of tobacco or of nicotine.Type: GrantFiled: September 9, 2002Date of Patent: August 31, 2004Assignee: Eli Lilly and CompanyInventors: John Xiaoqiang He, Nicholas Allan Honigschmidt, Todd Jonathan Kohn, Vincent Patrick Rocco, Patrick Gianpietro Spinazze, Kumiko Takeuchi
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Patent number: 6777429Abstract: The present invention is related to an ophthalmic composition comprising ketotifen as a pharmaceutically active agent.Type: GrantFiled: July 19, 2000Date of Patent: August 17, 2004Assignee: Novartis AGInventors: Marcia Johanna Adam, Andrea Fetz, Gyorgy Lajos Kis
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Patent number: 6774137Abstract: The present invention is related to an ophthalmic composition comprising ketotifen as a pharmaceutically active agent.Type: GrantFiled: April 29, 2002Date of Patent: August 10, 2004Assignee: Novartis AGInventors: Marcia Johanna Adam, Andrea Fetz, Gyorgy Lajos Kis
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Patent number: 6767915Abstract: Certain novel 4-substituted piperidine compounds are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.Type: GrantFiled: January 27, 2003Date of Patent: July 27, 2004Assignee: Merck & Co., Inc.Inventors: Raman K. Bakshi, Khaled J. Barakat, Yingjie Lai, Ravi P. Nargund, Brenda L. Palucki, Min K. Park, Iyassu K. Sebhat, Zhixiong Ye, Arthur A. Patchett
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Patent number: 6756388Abstract: The invention is a compound of Formula (I): wherein R is —OH, R1 is —OH, R2 is —H, n is 2 or 3 and X is sulfur, or a pharmaceutically acceptable salt of a compound having Formula (1), or a pharmaceutical composition comprising a compound having Formula (1) or a pharmaceutically acceptable salt thereof, or methods of treating bone loss, breast cancer or prostate cancer comprising administering an effective amount of the compound having Formula (I) or a pharmaceutically acceptable salt thereof.Type: GrantFiled: July 1, 1996Date of Patent: June 29, 2004Assignee: Pfizer Inc.Inventors: Kimberly O. Cameron, Paul Da Silva-Jardine, Eric R. Larson, James R. Hauske, Robert L. Rosati