The Five-membered Hetero Ring Is One Of The Cyclos In A Bicyclo Ring System Patents (Class 544/143)
  • Publication number: 20100016314
    Abstract: Derivatives of azabicyclo octane presented by formula (I), the method of making them, and the compositions containing the same and the uses thereof as inhibitors of dipeptidyl peptidase IV (DPP-IV), wherein the substitutes in formula (I) have the same meanings as what is mentioned in the descriptions.
    Type: Application
    Filed: October 30, 2007
    Publication date: January 21, 2010
    Inventors: Pengcho Tang, Zhigang Lin, Hejun Lü, Fuqiang Zhao, Li Li
  • Publication number: 20100016312
    Abstract: This application discloses compounds of generic Formula I: or pharmaceutically acceptable salts thereof, wherein A, R1, R2, R3, R4, Q, X, Y, m, p, and q are defined as described herein, useful for treatment of diseases associated with monoamine reuptake inhibitors. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.
    Type: Application
    Filed: July 15, 2009
    Publication date: January 21, 2010
    Inventors: Eun Kyung Lee, Ryan Craig Schoenfeld, Robert James Weikert
  • Publication number: 20100016308
    Abstract: Tetrahydroindole derivatives of formula (I): are disclosed. These compounds modulate the activity of gamma-secretase and hence find use in treatment or prevention of Alzheimer's disease.
    Type: Application
    Filed: November 3, 2006
    Publication date: January 21, 2010
    Inventors: Frank Burkamp, Graham David Checksfield, Stephen Robert Fletcher, Stephen John Lewis, Edward Giles Meiver, Paul Joseph Oakley, Martin Richard Teall
  • Publication number: 20100009986
    Abstract: The invention relates to substituted heteroaryl derivatives, to methods for the production thereof, to medicaments containing said compounds and to the use of substituted heteroaryl derivatives for producing medicaments.
    Type: Application
    Filed: July 17, 2007
    Publication date: January 14, 2010
    Applicant: GRUNENTHAL GmbH
    Inventors: Saskia Zemolka, Stefan Schunk, Werner Englberger, Babette-Yvonne Kögel, Klaus Link, Hans Schick, Helmut Sonnenschein, Heinz Graubaum, Claudia Hinze
  • Patent number: 7635694
    Abstract: 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: Grant
    Filed: February 24, 2005
    Date of Patent: December 22, 2009
    Assignee: Schering Corporation
    Inventors: Stephane L. Bogen, Weidong Pan, Sumie Ruan, F. George Njoroge
  • Publication number: 20090297476
    Abstract: The embodiments provide compounds of the general Formula I, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments provide compounds of the general Formula II, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.
    Type: Application
    Filed: May 9, 2008
    Publication date: December 3, 2009
    Applicants: InterMune, Inc., Array Biopharma Inc.
    Inventors: SCOTT SEIWERT, STEVEN W. ANDREWS, LEONID BEIGELMAN, LAWRENCE M. BLATT, BRAD BUCKMAN, Kevin R. Condroski, Yutong Jiang, Robert J. Kaus, April L. Kennedy, Timonthy S. Kercher, Michael A. Lyon, Bin Wang
  • Patent number: 7618967
    Abstract: The invention provides novel indane compounds which are useful in the treatment of affective disorders, pain disorders, attention deficit hyperactivity disorder (ADHD), cognitive disorders, substance abuse, smoking cessation and stress urinary incontinence.
    Type: Grant
    Filed: August 30, 2007
    Date of Patent: November 17, 2009
    Assignee: H. Lundbeck A/S
    Inventors: Jan Kehler, Karsten Juhl, Ask Püschl
  • Publication number: 20090281069
    Abstract: The present invention relates to compounds of the formula; and their use in therapy.
    Type: Application
    Filed: April 10, 2007
    Publication date: November 12, 2009
    Inventors: Daniel Kaspar Baeschlin, Garry Fenton, Kenji Namoto, Nils Ostermann, Richard Sedrani, Finton Sirockin
  • Patent number: 7612065
    Abstract: The present invention relates to inhibitors of JNK, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. 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: Grant
    Filed: March 28, 2007
    Date of Patent: November 3, 2009
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jeremy Green, Susanne Wilke, Francesco Salituro, Edmund Harrington, Jingrong Cao, Guy Bemis, Huai Gao
  • Publication number: 20090264414
    Abstract: The use of substituted amides for modulating the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11?HSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.
    Type: Application
    Filed: June 29, 2009
    Publication date: October 22, 2009
    Applicant: High Point Pharmaceuticals, LLC
    Inventors: Henrik Sune Andersen, Gita Camilla Tejlgaard Kampen, Inge Thoger Christensen, John Patrick Mogensen, Annette Rosendal Larsen, John Paul Kilburn
  • Patent number: 7605156
    Abstract: This invention provides methods for the use of substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof. The invention provides methods for the use of the compounds as inhibitors of the activity of various phospholipase enzymes, particularly phospholipase A2 enzymes, and for the medical treatment, prevention and inhibition diseases and disorders including asthma, stroke, atherosclerosis, multiple sclerosis, Parkinson's disease, arthritic disorders, rheumatic disorders, central nervous system damage resulting from stroke, central nervous system damage resulting from ischemia, central nervous system damage resulting from trauma, inflammation caused or potentiated by prostaglandins, inflammation caused or potentiated by leukotrienes, inflammation caused or potentiated by platelet activation factor, pain caused or potentiated by prostaglandins, pain caused or potentiated by leukotrienes, and pain caused or potentiated by platelet activation factor.
    Type: Grant
    Filed: May 27, 2005
    Date of Patent: October 20, 2009
    Assignee: Wyeth
    Inventors: John C. McKew, Steve Y. Tam, Katherine L. Lee, Lihren Chen, Paresh Thakker, Fuk-Wah Sum, Mark L. Behnke, Baihua Hu, James D. Clark, Wei Li, Valerie Clerin, Suzana Marusic, Kevin Pong
  • Patent number: 7601751
    Abstract: There is provided a series of substituted acyl guanidines of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, and R8 as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by ?-secretase and, more specifically, inhibit the production of A?-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to ?-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
    Type: Grant
    Filed: August 23, 2006
    Date of Patent: October 13, 2009
    Assignee: Bristol-Myers Squibb Company
    Inventors: Lorin A. Thompson, III, Jianliang Shi, F. Christopher Zusi, Michael F. Dee, John E. Macor
  • Patent number: 7598360
    Abstract: A bisstyryl compound. The bisstyryl compound has formula (I): wherein Z1 and Z2 are benzene, naphthalene, or heterocyclic ring, R1 is H, C1-5 alkyl, hydroxyl, halogen atoms, or alkoxy, R2 is H, halogen atoms, C1-5 alkyl, nitro, ester, carboxyl, sulfo, sulfonamide, sulfuric ester, amide, C1-3 alkoxy, amino, alkylamino, cyano, C1-6 alkylsulfonyl, or C2-7 alkoxy carbonyl, R3, R4, R5, and R6 are H, halogen atoms, alkyl, aralkyl, or heterocyclic ring containing O, S, or N, or R3 and R4 are joined to a nitrogen atom or R5 and R6 are joined together to form a ring, R7 and R8 are H or alkyl, W is nitrogen with or without Z1 and Z2 or aromatic group without Z1 and Z2, Y is carbon, oxygen, sulfur, selenium, —NR, or —C(CH3)2, m is 1-3, n is 1-18, and X1 and X2 are anionic groups or anionic organometallic complexes.
    Type: Grant
    Filed: October 21, 2005
    Date of Patent: October 6, 2009
    Assignee: Industrial Technology Research Institute
    Inventors: Shin-Shin Wang, Chien-Wen Chen, Jong-Lieh Yang, Chii-Chang Lai, Hui-Ping Tsai, Wen-Ping Chu, Wen-Yih Liao, Chien-Liang Huang, Tzuan-Ren Jeng, Ching-Yu Hsieh, An-Tse Lee
  • Publication number: 20090233901
    Abstract: There is provided a VLA-4 inhibitory drug having good oral absorbability and exhibiting sufficient anti-inflammatory effects when administered orally.
    Type: Application
    Filed: December 13, 2006
    Publication date: September 17, 2009
    Applicant: Daiichi Sankyo Company, Limited
    Inventors: Nobuo Machinaga, Shin Iimura, Yoshiyuki Yoneda, Jun Chiba, Fumihito Muro, Hideko Hoh, Atsushi Nakayama
  • Publication number: 20090227538
    Abstract: The invention relates to compounds of the general formula (I) wherein R1, R2, R3, R4, R5, R6, A, X, m and n have the significances given in claim 1, and optionally the enantiomers thereof. The active ingredients have advantageous pesticidal properties. They are especially suitable for controlling parasites on warm-blooded animals and plants.
    Type: Application
    Filed: November 2, 2006
    Publication date: September 10, 2009
    Inventors: Jörg Früchtel, Noëlle Gauvry, Sandra Schorderet Weber, Jacques Bouvier
  • Publication number: 20090221578
    Abstract: There are provided according to the invention compounds of formula (I) in free or salt form, wherein R1, R2, R4, R5, R6, D, X, W, m and n are as described in the specification, process for preparing them, and their use as pharmaceuticals.
    Type: Application
    Filed: December 7, 2006
    Publication date: September 3, 2009
    Inventor: David Andrew Sandham
  • Publication number: 20090203665
    Abstract: The present invention relates to compounds of formula I wherein R1, R2, and are defined in the specification and to pharmaceutically acceptable acid addition salts thereof.
    Type: Application
    Filed: April 13, 2009
    Publication date: August 13, 2009
    Inventors: Synese Jolidon, Robert Narquizian, Roger David Norcross, Emmanuel Pinard
  • Patent number: 7560481
    Abstract: The present invention provides novel compounds of Formula (I) which are CB2 selective ligands useful for the treatment of pain.
    Type: Grant
    Filed: December 21, 2005
    Date of Patent: July 14, 2009
    Assignee: Abbott Laboratories
    Inventors: Jennifer M. Frost, Karin R. Tietje, Michael J. Dart, Michael D. Meyer
  • Publication number: 20090163492
    Abstract: The invention relates to novel oxindol derivative of general formula (I), wherein substituents R1, R2, A, B and Y are such as defined in a claim 1. Drugs containing said derivatives and the use thereof for preventing and/or treating vassopress- and/or oxytocin-dependent-diseases are also disclosed.
    Type: Application
    Filed: March 23, 2006
    Publication date: June 25, 2009
    Inventors: Thorsten Oost, Wilfried Lubisch, Wolfgang Wernet, Wilfried Hornberger, Liliane Unger
  • Publication number: 20090163495
    Abstract: There are provided according to the invention, novel compounds of formula (I) wherein R1, R2, R3, R4, R5, X, a, b and Z are as defined in the specification, processes for preparing them, formulations containing them and their use in therapy for the treatment of inflammatory diseases.
    Type: Application
    Filed: February 24, 2009
    Publication date: June 25, 2009
    Applicant: GLAXO GROUP LIMITED
    Inventors: Rachael Anne Ancliff, Simon Teanby Hodgson, Suzanne Elaine Keeling, Xiao Qing Lewell, Graeme Michael Robertson
  • Publication number: 20090137800
    Abstract: A compound represented by the following general formula (I), wherein ring A and ring B each independently represent a benzene, naphthalene, or heterocyclic ring which may be substituted; R1 and R2 each independently represent an alkyl group having 1 to 8 carbon atoms which may be substituted; R1 and R2 may be linked together to form a ring; a methylene group of the alkyl group having 1 to 8 carbon atoms may be replaced by —O— or —CH?CH—; Anq- represents a q-valent anion, where q is 1 or 2; p represents a coefficient to keep the charge neutral.
    Type: Application
    Filed: March 5, 2007
    Publication date: May 28, 2009
    Inventor: Satoshi Yanagisawa
  • Publication number: 20090137570
    Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.
    Type: Application
    Filed: January 28, 2009
    Publication date: May 28, 2009
    Applicant: IRM LLC
    Inventors: Hong LIU, Arnab K. CHATTERJEE, David C. TULLY, Phillip B. ALPER, Badry BURSULAYA, Jianhua GUO, David H. WOODMANSEE, Daniel MUTNICK, Donald S. KARANEWSKY, Yun HE
  • Publication number: 20090124608
    Abstract: Compositions for the treatment of neurodegenerative diseases are disclosed. Methods of treating and monitoring progression of a neurodegenerative disease are disclosed. According to the present invention, a selective CB2 receptor modulator may be administered to a mammal for the treatment of a neurodegenerative disease.
    Type: Application
    Filed: October 5, 2007
    Publication date: May 14, 2009
    Applicant: Board of Trustees of the University of Arkansas
    Inventors: Paul L. Prather, John P. Crow
  • Publication number: 20090124616
    Abstract: Compounds which inhibit the activity of anti-apoptotic Mcl-1 protein, compositions containing the compounds, and methods of treating diseases involving overexpressed or unregulated Mcl-1 protein are disclosed.
    Type: Application
    Filed: April 16, 2008
    Publication date: May 14, 2009
    Applicant: Abbott Laboratories
    Inventors: Xiaohong Song, Hong Ding, Steven W. Elmore, Milan Bruncko, David J. Madar, Andrew J. Souers, Cheol-Min Park, Zhi-Fu Tao, Xilu Wang, Aaron R. Kunzer
  • Publication number: 20090124598
    Abstract: The use of substituted amides for modulating the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11?HSD1 and may be useful in the treatment of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.
    Type: Application
    Filed: November 1, 2006
    Publication date: May 14, 2009
    Inventors: Henrik Sune Andersen, Anker Steen Jorgensen, John Paul Kilburn, Gita Camilla Tejlgaard Kampen, Soren Ebdrup
  • Patent number: 7531535
    Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
    Type: Grant
    Filed: December 13, 2007
    Date of Patent: May 12, 2009
    Assignee: Bristol-Meyers Squibb Company
    Inventors: Donald J. P. Pinto, Jennifer X. Qiao
  • Publication number: 20090118503
    Abstract: Indole derivatives that are useful for treating pain, inflammation and other conditions are described. Certain of the compounds are benzyl derivatives and others are benzoyl derivatives. The compounds are substituted at least at the 3 position of the indole.
    Type: Application
    Filed: June 20, 2008
    Publication date: May 7, 2009
    Inventors: Kevin Sprott, John Jeffrey Talley, James Philip Pearson, G. Todd Milne
  • Publication number: 20090093469
    Abstract: The present invention is directed to phenylaminopropanol derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.
    Type: Application
    Filed: December 15, 2008
    Publication date: April 9, 2009
    Applicant: WYETH
    Inventors: Callain Younghee Kim, Paige Erin Mahaney, Eugene John Trybulski, Puwen Zhang, Eugene Anthony Terefenko, Casey Cameron McComas, Michael Anthony Marella, Richard Dale Coghlan, Gavin David Heffernan, Stephen Todd Cohn, An Thien Vu, Joseph Peter Sabatucci, Fei Ye
  • Publication number: 20090076004
    Abstract: There is provided compounds of formula (I), wherein X1, Q, T, Y, R1, R2, R3, R4 and R5 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation.
    Type: Application
    Filed: December 22, 2005
    Publication date: March 19, 2009
    Inventors: Benjamin Pelcman, Kristofer Olofsson, Martins Katkevics, Vita Ozola, Edgars Suna, Ivars Kalvins, Peteris Trapencieris, Dace Katkevica, Wesley Schaal
  • Publication number: 20090069321
    Abstract: The present invention relates to cyanomethyl substituted N-acyl tryptamines of the formula I in which R1, R2, R3, R4, R5, Q, X and W have the meaning as defined in the description. The compounds according to the invention are effective FSH antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.
    Type: Application
    Filed: July 29, 2008
    Publication date: March 12, 2009
    Inventors: Lars WORTMANN, Marcus Koppitz, Florian Peter Liesener, Thomas Frenzel, Hans-Peter Muhn, Anna Schrey, Ronald Kuehne
  • Publication number: 20090054402
    Abstract: Compounds which inhibit the activity of anti-apoptotic Mcl-1 protein, compositions containing the compounds, and methods of treating diseases involving overexpressed or unregulated Mcl-1 protein are disclosed.
    Type: Application
    Filed: April 16, 2008
    Publication date: February 26, 2009
    Applicant: Abbott Laboratories
    Inventors: Xilu Wang, Xiaohong Song, Steven W. Elmore, Milan Bruncko, David J. Madar, Andrew J. Souers, Lisa A. Hasvold, Le Wang, Zhi-Fu Tao, Aaron R. Kunzer
  • Publication number: 20090042882
    Abstract: The present invention relates to substituted acetamides of the general formula I, process for their preparation, and the use thereof for the manufacture of pharmaceutical compositions for the treatment of disorders and indications connected with the EP2 receptor.
    Type: Application
    Filed: June 12, 2008
    Publication date: February 12, 2009
    Inventors: Bernd BUCHMANN, Nico Braeuer, Olaf Peters, Knut Eis, Marcus Koppitz, Bernhard Lindenthal, Gernot Langer, Tim Wintermantel, Antonius Ter Laak
  • Publication number: 20090041722
    Abstract: Indole indane amides which are CB2 agonists are provided which have the structure wherein R1, R2, R3, R4 and R5 are as defined herein, which compounds are useful in treating autoimmune diseases, inflammation, pain, cardiovascular disorders and other diseases mediated by CB2 receptors. A method for preventing or treating such diseases employing the compounds of the invention is also provided.
    Type: Application
    Filed: July 22, 2008
    Publication date: February 12, 2009
    Inventors: Chunjian Liu, Stephen T. Wrobleski, Katerina Leftheris, Gang Wu, Philip M. Sher, Bruce A. Ellsworth
  • Publication number: 20090036443
    Abstract: The present invention relates to thienopyrrole compounds of formula (I); wherein A, B, Y, Ar, n, Z and X1 are as defined herein, and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepatitis C infections.
    Type: Application
    Filed: September 7, 2004
    Publication date: February 5, 2009
    Inventors: Barbara Attenni, Jose Ignacio Martin Hernando, Savina Malancona, Frank Narjes, Jesus Maria Ontoria Ontaria, Michael Rowley
  • Publication number: 20090036444
    Abstract: The present invention relates to a fused ring compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable a salt thereof, and a hepatitis C virus (HCV) polymerase inhibitor and a therapeutic agent for hepatitis C containing this compound. The compound of the present invention shows an anti-HCV activity based on the HCV polymerase inhibitory activity, and useful as an agent for the prophylaxis or treatment of hepatitis C.
    Type: Application
    Filed: May 18, 2006
    Publication date: February 5, 2009
    Applicant: Japan Tobacco Inc.
    Inventors: Ryo Mizojiri, Shintaro Hirashima, Takahiro Oka, Kenta Aoki, Satoru Noji, Izuru Ando, Toshihiro Sato, Yasushi Niwa
  • Publication number: 20080318902
    Abstract: The present invention relates to novel Triheterocyclic Compounds, compositions comprising a Triheterocyclic Compound, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering a Triheterocyclic Compound. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a cancer cell or neoplastic cell, treating or preventing a viral infection, or inhibiting the replication and/or infectivity of a virus.
    Type: Application
    Filed: July 18, 2008
    Publication date: December 25, 2008
    Applicant: Gemin X Pharmaceuticals Canada Inc.
    Inventors: Giorgio Attardo, Jean-Francois Lavallee, Elise Rioux, Sasmita Tripathy, Terrence W. Doyle
  • Patent number: 7452881
    Abstract: The present invention relates to new derivatives of sulphonamides, with the general formula (I), as well as to their physiologically acceptable salts, the processes for their preparation, their application as medicaments in human and/or veterinary therapy and the pharmaceutical compositions that contain them.
    Type: Grant
    Filed: February 16, 2007
    Date of Patent: November 18, 2008
    Assignee: Laboratories Del Dr. Esteve, S.A.
    Inventors: Ramón Merce-Vidal, Blas Andaluz-Mataro, Jordi Frigola-Constansa
  • Patent number: 7449459
    Abstract: The invention relates to compounds of general formula I as well as the production and use thereof as a medication.
    Type: Grant
    Filed: March 23, 2007
    Date of Patent: November 11, 2008
    Assignee: Bayer Schering Pharma AG
    Inventors: Bernd Buchmann, Dirk Kosemund, Bernd Menzenbach, Martin Fritsch
  • Publication number: 20080261944
    Abstract: The present invention relates to indole compounds of the formula (I): wherein R1, R2, R3, R4, A, E and X are as defined herein, and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepatitis C infections.
    Type: Application
    Filed: June 8, 2005
    Publication date: October 23, 2008
    Inventors: Stefania Colarusso, Immacolata Conte, Joerg Habermann, Frank Narjes, Simona Ponzi
  • Publication number: 20080249091
    Abstract: There is provided compounds of formula I, wherein X1, R1, R2, R3, R4, R5 and R6 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation.
    Type: Application
    Filed: December 22, 2005
    Publication date: October 9, 2008
    Inventors: Benjamin Pelcman, Kristofer Olofsson, Martins Katkevics, Vita Ozola, Edgars Suna, Ivars Kalvins, Peteris Trapencieris
  • Publication number: 20080234260
    Abstract: A compound of the formula II wherein one of R1 and R2 is halo and the other is H or halo; R3 is C1-C4 straight or branched chain, optionally fluorinated, alkyl; R4 is H; or R3 together with R4 and the adjoining backbone carbon defines: a spiro-C5-C7 cycloalkyl, optionally substituted with 1 to 3 substituents selected from halo, hydroxyl, C1-C4 alkyl or C1-C4 haloalkyl; or optionally bridged with a methylene group; or a C4-C6 saturated heterocycle having a hetero atom selected from O, NRa, S, S(?O)2; where Ra is H, C1-C4 alkyl or CH3C(?O); R5 is independently selected from H or methyl; E is —C(?O)—, —S(?O)m—, —NR5S(?O)m—, —NR5C(?O)—, —OC(?O)—, R6 is a stable, optionally substituted, monocyclic or bicyclic, carbocycle or heterocycle; m is independently 0,1 or 2; are inhibitors of cathepsin K and useful in the treatment or prophylaxis of osteoporosis.
    Type: Application
    Filed: January 6, 2005
    Publication date: September 25, 2008
    Inventors: Magnus Nilsson, Xiao-Xiong Zhou, Lourdes Oden, Bjorn Classon, Rolf Noren, Urszula Grabowska, Philip Jackson, Philip Fallon, Andrew Carr, Mark Liley, Matt Tozer, Tony Johnson, Victor Diaz, Laia Crespo, Jussi Kangasmetsa, Thierry Bonnaud
  • Patent number: 7423058
    Abstract: 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: Grant
    Filed: December 21, 2006
    Date of Patent: September 9, 2008
    Assignee: Schering Corporation
    Inventors: Stephane L. Bogen, Weidong Pan, Sumei Ruan, Kevin X. Chen, Ashok Arasappan, Srikanth Venkatraman, Latha G. Nair, Mousumi Sannigrahi, Frank Bennett, Anil K. Saksena, F. George Njoroge, Viyyoor M. Girijavallabhan
  • Patent number: 7414067
    Abstract: This invention relates to the use of potent potassium channel blockers or a formulation thereof in the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.
    Type: Grant
    Filed: March 24, 2004
    Date of Patent: August 19, 2008
    Assignees: Merck & Co. Inc., Evotec OAI
    Inventors: Edward Andrew Boyd, Michael H. Fisher, Maria L. Garcia, Gregory J. Kaczorowski, Peter T. Meinke, William H. Parsons, Stephen Price, John Stibbard
  • Publication number: 20080188473
    Abstract: There is provided a compound of formula: (I) wherein X, R1, R2, R3, R4, R5, R6, R7 and R8 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of microsomal prostaglandin E synthase-1 is desired and/or required, and particularly in the treatment of inflammation.
    Type: Application
    Filed: June 17, 2005
    Publication date: August 7, 2008
    Inventors: Kristofer Olofsson, Benjamin Pelcman, Wesley Schaal, Ivars Kalvins, Edgars Suna, Vita Ozola, Martins Katkevics
  • Publication number: 20080176849
    Abstract: The present invention provides hydroxamate compounds which are deacetylase inhibitors. The compounds are suitable for pharmaceutical compositions having anti-proliferative properties.
    Type: Application
    Filed: March 11, 2008
    Publication date: July 24, 2008
    Inventors: Stacy William Remiszewski, Kenneth Walter Bair, Richard William Versace, Lawrence Blas Perez, Michael Alan Green, Lidia Cristina Sambucetti, Sushil Sharma
  • Publication number: 20080171741
    Abstract: A compound of Formula I and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating conditions associated with the activity of p38 kinase.
    Type: Application
    Filed: October 25, 2007
    Publication date: July 17, 2008
    Inventors: Stephen T. Wrobleski, Jagabandhu Das, T.G. Murali Dhar, Alaric J. Dyckman, John Hynes, Katerina Leftheris, James Lin, Shuqun Lin
  • Publication number: 20080167306
    Abstract: A compound of the following formula (1), or its prodrug or pharmaceutically acceptable salt thereof, being useful as a diabetic medicine or preventive, or blood sugar regulator, or therapeutic agent for hyperlipemia, etc. wherein the ring Z is an optionally substituted heteroaryl, W4 is a single bond, lower alkylene, etc., Ar2 is an optionally substituted aryl, etc., W3 is a single bond, lower alkylene, etc., Ar1 is an optionally substituted arylene, etc., each of W1 and W2 is an optionally substituted lower alkylene, etc., and R1 is carboxyl, an alkoxycarbonyl.
    Type: Application
    Filed: January 12, 2006
    Publication date: July 10, 2008
    Inventors: Yoko Takahashi, Ryu Nagata, Kantaro Ushiroda
  • Patent number: 7393404
    Abstract: A pigment dispersant contains the following component (a) alone or the following components (a) and (b) in combination: Component (a): a composite pigment formed of a diketopyrrolopyrrole pigment having a sulfonic group and another diketopyrrolopyrrole pigment having no sulfonic group, wherein the number of sulfonic group per molecule of the diketopyrrolopyrrole pigments in the composite pigment is from 0.05 to 0.5; and Component (b): a pigment other than the component (a), wherein the pigment has a sulfonic group or its metal salt, ammonium salt or amine salt. Also disclosed are a colored composition for color filters, a process for the fabrication of a color filter, the color filter fabricated by the process, an image display device including the color filter, and an information communication equipment including the image display device.
    Type: Grant
    Filed: February 15, 2006
    Date of Patent: July 1, 2008
    Assignee: Dainichiseika Color & Chemicals Mfg. Co., Ltd.
    Inventors: Hiroaki Saikatsu, Hiromitsu Yanagimoto, Naoto Kamata, Kazuhito Ooki, Yutaka Miura, Shigeru Sakamoto, Akio Yoshida, Michiei Nakamura
  • Patent number: 7381738
    Abstract: The present application describes modulators of MCP-1 of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein X, Z, a, b, c, d, n, R1, R2, R3, R4, R5, R10, R10a, and R12, are as defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using modulators of formula (I) are disclosed.
    Type: Grant
    Filed: February 17, 2005
    Date of Patent: June 3, 2008
    Assignee: Bristol-Myers Squibb Company
    Inventors: Douglas G. Batt, Percy H. Carter
  • Patent number: 7375219
    Abstract: The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing conditions such as, for example, stroke, reperfusion injury, neurodegeneration, head trauma, CABG, migraine headache with and without aura, migraine with allodynia, central post-stroke pain (CPSP), neuropathic pain, morphine/opioid induced tolerance and hyperalgesia.
    Type: Grant
    Filed: April 13, 2006
    Date of Patent: May 20, 2008
    Assignee: NeurAxon, Inc.
    Inventors: Shawn Maddaford, Jailall Ramnauth, Suman Rakhit, Joanne Patman, Paul Renton, Subhash C. Annedi