Chalcogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 514/309)
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Patent number: 7402673Abstract: The invention provides novel ?2 adrenergic receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with ?2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.Type: GrantFiled: June 2, 2005Date of Patent: July 22, 2008Assignee: Theravance, Inc.Inventor: Martin S. Linsell
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Patent number: 7402596Abstract: Bicycloheteroaryl compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.Type: GrantFiled: March 17, 2006Date of Patent: July 22, 2008Assignee: Renovis, Inc.Inventors: Michael G. Kelly, John Kincaid
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Patent number: 7402595Abstract: A JNK inhibitor containing a compound having an isoquinolinone skeleton or a salt thereof, such as a compound represented by the formula wherein ring A and ring B are each an optionally substituted benzene ring, X is —O—, —N?, —NR3— or —CHR3—, R2 is an acyl group, an optionally esterified or thioesterified carboxyl group, an optionally substituted carbamoyl group or an optionally substituted amino group and the like, a broken line shows a single bond or a double bond, and R1 is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group and the like, and the like.Type: GrantFiled: February 12, 2003Date of Patent: July 22, 2008Assignee: Takeda Pharmaceutical Company LimitedInventors: Fumio Itoh, Hiroyuki Kimura, Hideki Igata, Tomohiro Kawamoto, Mitsuru Sasaki, Shuji Kitamura
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Publication number: 20080161347Abstract: Substituted aryl and heteroaryl derivatives are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.Type: ApplicationFiled: March 17, 2006Publication date: July 3, 2008Applicant: MERCK & CO., INC.Inventors: John E. Stelmach, Keith G. Rosauer, Emma R. Parmee, James R. Tata
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Publication number: 20080161297Abstract: Disclosed are novel substituted 2H-isoquinolin-1-one and 3H-quinazolin-4-one derivatives useful as inhibitors of Rho kinase and for treating a variety of diseases and disorders that are mediated or sustained through the activity of Rho kinase, including cardiovascular diseases, pharmaceutical compositions comprising such compounds, methods for using such compounds and processes for making such compounds.Type: ApplicationFiled: September 18, 2007Publication date: July 3, 2008Inventors: Todd Bosanac, John David Ginn, Eugene Richard Hickey, Thomas Martin Kirrane, Weimin Liu, Anthony S. Prokopowicz, Sabine K. Schlyer, Cheng-Kon Shih, Roger John Snow, Michael Robert Turner, Frank Wu, Erick Richard Young
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Patent number: 7390820Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: August 24, 2004Date of Patent: June 24, 2008Assignee: Amgen Inc.Inventor: Christopher Tegley
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Patent number: 7390798Abstract: The present invention is directed to compounds of Formula I: I (where variables A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache.Type: GrantFiled: February 9, 2005Date of Patent: June 24, 2008Assignee: Merck & Co., Inc.Inventors: Theresa M. Williams, Christopher S. Burgey, Thomas J. Tucker, Craig A. Stump, Ian M. Bell
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Publication number: 20080146566Abstract: The invention concerns a compound of the Formula I (A chemical formula should be inserted here—please see paper copy enclosed herewith) wherein m is 0-2 and each R1 is a group such as hydroxy, halogeno, trifluoromethyl heterocyclyl and heterocyclyloxy; R2 is halogeno, trifluoromethyl or (1-6C)alkyl; R3 is hydrogen, halogeno or (1-6C)alkyl; and R4 is (3-6C)cycloalkyl; or pharmaceutically-acceptable salts thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.Type: ApplicationFiled: December 22, 2005Publication date: June 19, 2008Inventors: Ian Alun Nash, Kenneth Mark Page, Paul Allen Bethel
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Publication number: 20080139605Abstract: The present invention relates to new substituted prolinamides of general formula (I) wherein D, L, E, G, J, M, R3, R4, R5 and R13 are defined as in the specification, the tautomers, the enantiomers, the diastereomers, the mixtures, and the salts thereof.Type: ApplicationFiled: May 16, 2007Publication date: June 12, 2008Inventors: Kai Gerlach, Georg Dahmann, Herbert Nar, Roland Pfau, Henning Priepke, Annette Schuler-Metz, Wolfgang Wienen
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Publication number: 20080132499Abstract: Compounds are provided which are useful as platelet ADP receptor inhibitors, for treating thrombosis and for reducing the likelihood and/or severity of a secondary ischemic event in a patient.Type: ApplicationFiled: September 17, 2007Publication date: June 5, 2008Applicant: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Carroll Anna Crew Scarborough, Shawn M. Bauer, Anjali Pandey
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Publication number: 20080132521Abstract: Compounds of formula (I): wherein n, R1, R2, R3 and R7 are disclosed herein, are useful in treating disease-states associated with nuclear receptor activity. Pharmaceutical compositions comprising and methods of using said compounds are also disclosed herein.Type: ApplicationFiled: July 27, 2007Publication date: June 5, 2008Applicant: EXELIXIS, INC.Inventors: Alan T. Johnson, Satoru Kaneko, Raju Mohan, Kozo Oda, Edwin J. Schweiger
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Publication number: 20080119461Abstract: Hepatitis C virus inhibitors having the general formula are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.Type: ApplicationFiled: November 5, 2007Publication date: May 22, 2008Inventors: Ny Sin, Brian Lee Venables, Li-Qiang Sun, Sing-Yuen Sit, Yan Chen, Paul Michael Scola
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Publication number: 20080113969Abstract: The present invention provides synergistic combinations for the treatment of conditions associated with pain including acute pain, e.g., postoperative pain, chronic pain, inflammatory pain, neuropathic pain and pain associated with migraine. In particular, the present invention relates to the use of an allosteric adenosine A1 receptor enhancer in conjunction with opioid analgesics or 2-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA)/kainate antagonists for alleviating pain, e.g., postoperative pain.Type: ApplicationFiled: October 16, 2007Publication date: May 15, 2008Inventor: James Conrad Eisenach
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Patent number: 7348433Abstract: This invention encompasses a method for treating a prostaglandin E mediated disease or condition comprising administering to a mammalian patient in need of such treatment a compound of Formula (A) in an amount that is effective to treat the prostaglandin E mediated disease or conditionType: GrantFiled: December 11, 2002Date of Patent: March 25, 2008Assignee: Merck Frosst Canada & Co.Inventors: Daniel Dube, Denis Deschenes, Rejean Fortin, Yves Girard
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Publication number: 20080045566Abstract: The present invention relates to 6-substituted isoquinoline derivatives having the general Formula I wherein X is O, S or NH; Y is OH or NH2; m is 0, 1 or 2; n is 0 or 1; o is 0 or 1; R1 is H, when Y is NH2; or R1 is H, (C1-4)alkyl or halogen, when Y is OH; R2 and R3 are independently H, (C1-4)alkyl or halogen; R4 is H or (C1-6)alkyl, optionally substituted with halogen, (C3-7)cycloalkyl, (C6-10)aryl or a saturated 5- or 6-membered heterocyclic ring comprising 1-3 heteroatoms independently selected from O, S and N, the (C6-10)aryl and heterocyclic ring being optionally substituted with (C1-4)alkyl, (C1-4)alkyloxy or halogen; R5 is H or (C1-4)alkyl; or a pharmaceutically acceptable salt thereof, with the proviso that the compounds of Formula I wherein X is O, Y is OH , n is 0 and m+o=2 are excluded, to pharmaceutical compositions comprising the same, as well as to the use of said 6-substituted isoquinoline derivatives for the preparation of a medicament for the treatment of ROCK-I related disorders such asType: ApplicationFiled: August 16, 2007Publication date: February 21, 2008Applicant: N.V. OrganonInventors: Peter Christopher Ray, Steven Laats, John Richard Morphy, Brad Sherborne
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Patent number: 7314937Abstract: The present invention discloses novel substituted aryl alkylamine compounds of Formula (I) or pharmaceutically acceptable salts thereof which have selective histamine-H3 receptor antagonist activity as well as methods for preparing such compounds.Type: GrantFiled: March 21, 2002Date of Patent: January 1, 2008Assignee: Eli Lilly and CompanyInventors: Lisa Selsam Beavers, Robert Alan Gadski, Philip Arthur Hipskind, Craig William Lindsley, Karen Lynn Lobb, James Arthur Nixon, Richard Todd Pickard, John Mehnert Schaus, Takako Takakuwa, Brian Morgan Watson
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Patent number: 7309708Abstract: Hepatitis C virus inhibitors are disclosed having the general formula: wherein R1, R2, R3, R?, B, Y and X are described in the description. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.Type: GrantFiled: November 18, 2004Date of Patent: December 18, 2007Assignee: Birstol-Myers Squibb CompanyInventors: Yong Tu, Paul Michael Scola, Andrew Charles Good, Jeffrey Allen Campbell
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Patent number: 7304053Abstract: Substituted heterocyclic compounds for treating multidrug resistance are disclosed. Compositions and methods of use for the substituted heterocyclic compounds are disclosed.Type: GrantFiled: December 19, 2003Date of Patent: December 4, 2007Assignee: H. Lee Moffitt Cancer Center & Research Institute, Inc.Inventors: Charles Raymond Degenhardt, David Joseph Eickhoff
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Patent number: 7294635Abstract: Isoquinolinone compounds are provided that are useful for the inhibition of ADP-platelet aggregation, particularly in the treatment of thrombosis and thrombosis related conditions or disorders.Type: GrantFiled: September 29, 2004Date of Patent: November 13, 2007Assignee: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Kim A. Kane-MaGuire, Charles K. Marlowe, Mark S. Smyth, Xiaoming Zhang
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Publication number: 20070259851Abstract: 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 vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.Type: ApplicationFiled: May 1, 2007Publication date: November 8, 2007Inventors: Prasad V. Chaturvedula, Stephen E. Mercer, Haiquan Fang, Xiaojun Han, Guanglin Luo, Gene M. Dubowchik, Graham S. Poindexter
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Patent number: 7265130Abstract: The present invention provides a pharmaceutical composition for use as an NPY Y5 receptor antagonist comprising a compound of the formula (I): wherein R1 is lower alkyl, cycloalkyl or the like, R2 is hydrogen, lower alkyl or the like, n is 1 or 2, X is lower alkylene, lower alkenylene, arylene, cycloalkylene or the like, Y is CONR7, CSNR7, NR7CO, NR7CS or the like, Z is lower alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl or the like and R7 is hydrogen or lower alkyl, prodrug, pharmaceutically acceptable salt or solvate thereof.Type: GrantFiled: December 30, 2003Date of Patent: September 4, 2007Assignee: Shionogi & Co., Ltd.Inventors: Yasuyuki Kawanishi, Hideyuki Takenaka, Kohji Hanasaki, Tetsuo Okada
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Patent number: 7265131Abstract: Compounds of formula (I): wherein n, R1, R2, R3 and R7 are disclosed herein, are useful in treating disease-states associated with nuclear receptor activity. Pharmaceutical compositions comprising and methods of using said compounds are also disclosed herein.Type: GrantFiled: December 17, 2003Date of Patent: September 4, 2007Assignee: Exelixis, Inc.Inventors: Alan T Johnson, Satoru Kaneko, Raju Mohan, Kozo Oda, Edwin J Schweiger
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Patent number: 7253160Abstract: The present invention discloses novel depeptidized compounds which have HCV protease inhibitory activity as well as pharmaceutical compositions comprising such compounds and methods of using them to treat disorders associated with the HCV protease.Type: GrantFiled: November 19, 2004Date of Patent: August 7, 2007Assignee: Schering CorporationInventors: F. George Njoroge, Srikanth Venkatraman, Viyyoor M. Girijavallabhan
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Publication number: 20070161670Abstract: The present disclosure generally relates to a process for the preparation of hydroxy-substituted heterocycles such as isoquinolines, naphthyridines, pyridopyridazines, and pyridopyrimidines.Type: ApplicationFiled: January 4, 2007Publication date: July 12, 2007Inventors: Andrew J. Staab, Ny Sin
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Patent number: 7220759Abstract: The present invention relates to an isoquinoline compound represented by the following formula (I), an optically active form thereof, a pharmaceutically acceptable salt thereof, a water adduct thereof, a hydrate thereof and a solvate thereof, as well as an agent for the prophylaxis and/or treatment of a disease caused by hyperreactivity of poly(ADP-ribose)polymerase, containing the compound, and a poly(ADP-ribose)polymerase inhibitor containing the compound. In addition, this compound is useful as an agent for the prophylaxis and/or treatment of cerebral infarction, particularly as an agent for the prophylaxis and/or treatment of acute cerebral infarction. Furthermore, this compound is useful as a prophylactic and/or therapeutic agent that improves neurological symptoms associated with cerebral infarction, particularly acute cerebral infarction. wherein the symbols are the same as defined in the description.Type: GrantFiled: April 30, 2004Date of Patent: May 22, 2007Assignee: Mitsubishi Pharma CorporationInventors: Masakazu Fujio, Hiroyuki Satoh, Shinya Inoue, Toshifumi Matsumoto, Yasuhiro Egi
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Patent number: 7205315Abstract: The present invention is directed to a compound of formula (I), or a stereoisomer or a mixture of stereoisomer thereof in any ratio, or its physiologically tolerable salt, which is useful as an inhibitor of matrix metalloproteinase. The present invention is also directed to a pharmaceutical preparation comprising a pharmaceutically effective amount of at least one compound of formula (I); processes for their preparation; the use of a compound of formula (I) having activity as an matrix metalloproteinase inhibitor; and for the prophylaxis and therapy of disease states that involve an increase in the activity of matrix metalloproteinase.Type: GrantFiled: September 27, 2004Date of Patent: April 17, 2007Assignee: Sanofi-Aventis Deutschland GmbHInventors: Manfred Schudok, Hans Matter, Armin Hofmeister
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Patent number: 7196088Abstract: The invention provides compounds of the formula: and pharmaceutically acceptable salts or prodrugs thereof, wherein, n, X, Y, R1, R2, R3, R4 and R5 are as defined herein. The subject compounds are useful for treatment of 5-HT6 receptor antagonist-mediated diseases. Also provides are methods for preparing, compositions comprising, and methods for using the subject compounds.Type: GrantFiled: March 2, 2004Date of Patent: March 27, 2007Assignee: Roche Palo Alto LLCInventor: David George Putman
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Patent number: 7173057Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.Type: GrantFiled: February 24, 2005Date of Patent: February 6, 2007Assignee: Schering CorporationInventors: Kevin X. Chen, F. George Njoroge, Mousumi Sannigrahi, Latha G. Nair, Weiying Yang, Bancha Vibulbhan, Srikanth Venkatraman, Ashok Arasappan, Stephane L. Bogen, Frank Bennett, Viyyoor M. Girijavallabhan
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Patent number: 7144894Abstract: The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts and solvates, their pharmaceutical compositions, and their uses in inhibiting ?-amyloid peptide (?-AP) productionType: GrantFiled: September 21, 2005Date of Patent: December 5, 2006Assignee: Bristol-Myers Squibb CompanyInventor: Paul J. Gilligan
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Patent number: 7125863Abstract: Compounds according to formula (1), wherein R1 is H or CN, X1 is S, O, SO2 or CH2, X2 is CO, CH2 or a covalent bond, Het is a nitrogen-containing heterocycle and n is 1–5 are new. The compounds of the invention are inhibitors of dipeptidyl peptidase IV.Type: GrantFiled: April 26, 2001Date of Patent: October 24, 2006Assignee: Ferring BVInventors: David Michael Evans, Gary Robert William Pitt
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Patent number: 7109212Abstract: The invention relates to quinoline and isoquinoline derivatives of general formula I and a process for their production, and their use as inflammation inhibitors.Type: GrantFiled: February 17, 2005Date of Patent: September 19, 2006Assignee: Schering AGInventors: Stefan Jaroch, Manfred Lehmann, Norbert Schmees, Markus Berger, Hartmut Rehwinkel, Konrad Krolikiewicz, Werner Skuballa, Heike Schaecke, Arndt. J. G. Schottelius
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Patent number: 7091356Abstract: Imido and Amido substituted alkanohydroxamic acids reduce the levels of TNFa and inhibit phosphodiesterase in a mammal. A typical embodiment is 3-(3-cyclopentyloxy-4-methoxyphenyl)-N-hydroxy-3-phthalimidopropionamide.Type: GrantFiled: June 16, 2003Date of Patent: August 15, 2006Inventors: George W. Muller, Hon-Wah Man
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Patent number: 7041676Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.Type: GrantFiled: June 12, 2003Date of Patent: May 9, 2006Assignees: Cytokinetics, Inc., Smithkline Beecham CorporationInventors: Andrew McDonald, Pu-Ping Lu, Gustave Bergnes, David J. Morgans, Jr., Dashyant Dhanak, Steven David Knight
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Patent number: 7030136Abstract: The use of phanquinone (4,7-phenanthroline-5,6-dione) for the treatment or prevention of memory impairment is suggested. Also a method for improving the learning or memory of a normal subject is suggested, said method comprising the administering of phanquinone, optionally together with one or more pharmaceutically acceptable carrier(s).Type: GrantFiled: March 15, 2002Date of Patent: April 18, 2006Assignee: Prana Biotechnology LimitedInventors: Michel Xilinas, Panayotis Nikolas Gerolymatos
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Patent number: 6998408Abstract: The present application describes 6–5, 6—6, or 6–7 heterobicycles of Formula I or pharmaceutically acceptable salt forms thereof: wherein ring P is a 6-membered heteroaromatic and ring M is a 5-, 6-, or 7-membered non-aromatic carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.Type: GrantFiled: March 22, 2002Date of Patent: February 14, 2006Assignee: Bristol-Myers Squibb Pharma CompanyInventor: Donald Joseph Philip Pinto
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Patent number: 6992084Abstract: The invention provides compounds and compositions of the formula: wherein, the subscript n is an integer of from 0 to 4; Ar is a member selected from the group consisting of substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl, R1 is a member selected from the group consisting of substituted or unsubstituted (C5–C15)alkyl and (C8–C14)acyl group; R2 is a member selected from the group consisting of substituted or unsubstituted (C1–C8)alkyl; each R3 is independently a substituent Y is a member selected from the group consisting of substituted or unsubstituted (C2–C8)alkylene and substituted or unsubstituted (C2–C8)heteroalkylene; Z is —NR4R5 R4 and R5 are independently selected from the group consisting of hydrogen and (C1–C8)alkyl or taken together with the nitrogen atom to which each is attached to form a heterocyclyl or heteroaryl; These compounds and compositions bind to the CXCR3 chemokine receptor and are useful for treating diseases and conditions responsive to the moType: GrantFiled: October 23, 2002Date of Patent: January 31, 2006Assignee: ChemoCentryx, Inc.Inventors: Thomas J. Schall, Daniel J. Dairaghi, Brian E. McMaster
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Patent number: 6974822Abstract: This invention provides compounds defined by Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, Q, R2, R3, R4, and n are as defined in the specification. The invention also provides pharmaceutical compositions comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, as defined in the specification, together with a pharmaceutically acceptable carrier, diluent, or excipient. The invention also provides methods of inhibiting an MMP-13 enzyme in an animal, comprising administering to the animal a compound of Formula I, or a pharmaceutically acceptable salt thereof. The invention also provides methods of treating a disease mediated by an MMP-13 enzyme in a patient, comprising administering to the patient a compound of Formula I, or a pharmaceutically acceptable salt thereof, either alone or in a pharmaceutical composition.Type: GrantFiled: August 5, 2003Date of Patent: December 13, 2005Assignee: Warner-Lambert Company LLCInventors: Amy Mae Bunker, Drago Robert Sliskovic
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Patent number: 6964782Abstract: Disclosed are several preferred embodiments of hydrogen peroxide which are packaged with ease of use and extended shelf-life in mind. The embodiments include foam, mist, gel, and disposable towelette forms of H2O2. Optional ingredients of topical pain relievers and skin protectants are also disclosed, as are their methods of use.Type: GrantFiled: July 7, 2003Date of Patent: November 15, 2005Assignee: Tec Labs, Inc.Inventors: Robert Lee Smith, Steven Dale Smith, Wendy S. Langley, John Mark Christensen, Vernon W. Smith
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Patent number: 6962927Abstract: The specification discloses a method for enhancing the inhibiting action of drugs against multidrug resistant cells, apparently by reversing or inhibiting the glycoprotein “pumps” associated with such cells.Type: GrantFiled: June 7, 1995Date of Patent: November 8, 2005Assignee: Cancer Biologics of America, Inc.Inventor: Knox Van Dyke
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Patent number: 6949567Abstract: The invention relates to new diphenylurea having the formula (I) or a salt thereof, where Y is C?O, C?S, C?NH, (C?O)2 or SO2; and to processes for the preparation of these compounds and to their use in the treatment of protozoal diseases and to diseases where the inhibition of intracellular protein-degradation pathways is of benefit.Type: GrantFiled: February 26, 2002Date of Patent: September 27, 2005Assignee: 4SC AGInventors: Andrea Aschenbrenner, Katharina Aulinger Fuchs, Matthias Dormeyer, Gabriel Garcia, Bernd Kramer, Jürgen Kraus, Rolf Krauss, Johan Leban, Stefano Pegoraro, Wael Saeb, Kristina Wolf
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Patent number: 6943266Abstract: Novel polycyclic cannabinoid analogs are presented which have preferentially high affinities for the cannabinoid CB2 receptor sites. The improved receptor affinity makes these analogs therapeutically useful as medications in individuals and animals for treatment of pain, glaucoma, epilepsy, nausea associated with chemotherapy.Type: GrantFiled: October 18, 2000Date of Patent: September 13, 2005Assignee: University of ConnecticutInventors: Alexandros Makriyannis, Atmaram Khanolkar
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Patent number: 6939867Abstract: Sulfamide compounds having formula (I) are described as well as their use in the treatment of diseases dependent on the signaling pathways associated with ?-adrenergic receptors, such as obesity, diabetes, hypertension, gastrointestinal hypo- or hyper-motility and cardiovascular diseasesType: GrantFiled: February 28, 2002Date of Patent: September 6, 2005Assignee: Pfizer Inc.Inventors: Robert L. Dow, Ernest S. Paight
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Patent number: 6921756Abstract: The invention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.Type: GrantFiled: April 8, 2003Date of Patent: July 26, 2005Assignee: MethylGene, Inc.Inventors: Jeffrey M. Besterman, Jubrail Rahil, Arkadii Vaisburg
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Patent number: 6911454Abstract: The specification discloses a method for enhancing the inhibiting action of drugs against multidrug resistant cells, apparently by reversing or inhibiting the glycoprotein “pumps” associated with such cells.Type: GrantFiled: August 22, 1994Date of Patent: June 28, 2005Assignee: Cancer Biologics of America, Inc.Inventor: Knox Van Dyke
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Patent number: 6906061Abstract: A Rho kinase inhibitor is provided as a novel pharmaceutical agent, particularly as a therapeutic agent of hypertension, a therapeutic agent of angina pectoris, a suppressive agent of cerebrovascular contraction, a therapeutic agent of asthma, a therapeutic agent of peripheral circulation disorder, a prophylactic agent of immature birth, a therapeutic agent of arteriosclerosis, an anti-cancer drug, an anti-inflammatory agent, an immunosuppressant, a therapeutic agent of autoimmune disease, an anti-AIDS drug, a contraceptive, a prophylactic agent of digestive tract infection, a therapeutic agent of osteoporosis, a therapeutic agent of retinopathy and a brain function improving drug. In addition, the Rho kinase inhibitor is provided as a reagent and a diagnostic.Type: GrantFiled: July 31, 2002Date of Patent: June 14, 2005Assignee: Mitsubishi Pharma CorporationInventors: Masayoshi Uehata, Takashi Ono, Hiroyuki Satoh, Keiji Yamagami, Toshio Kawahara
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Patent number: 6906063Abstract: Novel compounds of formulae (I) to (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.Type: GrantFiled: August 2, 2001Date of Patent: June 14, 2005Assignee: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Wolin Huang, Charles K. Marlowe, Kim A. Kane-MaGuire
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Patent number: 6884791Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.Type: GrantFiled: November 22, 2002Date of Patent: April 26, 2005Assignee: MethylGene, Inc.Inventors: Jeffrey M. Besterman, Jubrail Rahil, Arkadii Vaisburg
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Patent number: 6878706Abstract: Compounds according to the following formula (I): wherein the variables Q and R1 to R6 are as described herein, which reversibly inhibit the cysteine proteases, such as cathepsins K, S, F, L and B; pharmaceutical compositions containing such compounds, and method of treating diseases and pathological conditions exacerbated by these cysteine proteases such as, but not limited to rheumatoid arthritis, multiple sclerosis and other autoimmune diseases, osteoporosis, asthma, Alzheimer's disease, atherosclerosis and endometriosis.Type: GrantFiled: March 27, 2003Date of Patent: April 12, 2005Assignee: Boehringer Ingelheim Pharmaceuticals Inc.Inventors: Thomas A. Gilmore, Eugene Richard Hickey, Weimin Liu, Peter Allen Nemoto, Denice M. Spero
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Patent number: 6875761Abstract: Condensed pyridine compounds represented by formula (I): wherein: R1 and R3 are, independently, hydrogen, lower alkyl, or lower alkoxy; R2 represent an amino substituent; ring A is a benzene ring, pyridine ring, thiophene ring, or furan ring; and B represents a substituent containing a ring structure. Also, pharmaceutically acceptable salt and hydrates thereof. These compounds are clinically useful medicaments having serotonin antagonism, and in particular, for treating, ameliorating, or preventing spastic paralysis. They are also useful as central muscle relaxants for ameliorating myotonia.Type: GrantFiled: March 10, 2004Date of Patent: April 5, 2005Assignee: Eisai Co., Ltd.Inventors: Kohshi Ueno, Atsushi Sasaki, Koki Kawano, Tadashi Okabe, Noritaka Kitazawa, Keiko Takahashi, Noboru Yamamoto, Yuichi Suzuki, Manabu Matsunaga, Atsuhiko Kubota
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Patent number: RE39265Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: November 9, 2000Date of Patent: September 5, 2006Assignee: Aventis Pharmaceuticals Inc.Inventors: Joseph T. Strupczewski, Kenneth J. Bordeau, Edward J. Glamkowski, Yulin Chiang, Grover C. Helsley