Benzothiadiazines Patents (Class 544/11)
  • Patent number: 11945813
    Abstract: Disclosed herein are 5-Substituted 4-amino-1H-benzo[c][1,2,6]thiadiazine 2,2-dioxide compounds useful as sweet flavor modifiers. Also disclosed herein are ingestible compositions that include one or more of these compounds in combination with a natural or artificial sweetener.
    Type: Grant
    Filed: August 6, 2019
    Date of Patent: April 2, 2024
    Assignee: FIRMENICH INCORPORATED
    Inventors: Joseph R. Fotsing, Catherine Tachdjian, Guy Servant, Brett Weylan Ching, Timothy Davis
  • Patent number: 10626111
    Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTC”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Grant
    Filed: November 21, 2018
    Date of Patent: April 21, 2020
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara S. Hadida Ruah, Matthew M. Hamilton, Mark Miller, Peter D. J. Grootenhuis
  • Patent number: 10087154
    Abstract: The present invention includes methods/processes and intermediates for preparing compounds having structural Formula (I): wherein X is alkyl, substituted alkyl, alkenyl, substituted alkenyl, heteroalkyl, substituted heteroalkyl, heteroalkenyl, or substituted heteroalkenyl.
    Type: Grant
    Filed: July 31, 2017
    Date of Patent: October 2, 2018
    Assignee: Senomyx, Inc.
    Inventors: Catherine Tachdjian, Donald S. Karanewsky, Xiao-Qing Tang, Qing Chen, Peter Leeming, Tayyab Rashid, Daniel Levin
  • Patent number: 9732052
    Abstract: The present invention includes methods/processes and intermediates for preparing compounds having structural Formula (I): wherein X is alkyl, substituted alkyl, alkenyl, substituted alkenyl, heteroalkyl, substituted heteroalkyl, heteroalkenyl, or substituted heteroalkenyl.
    Type: Grant
    Filed: June 16, 2016
    Date of Patent: August 15, 2017
    Assignee: Senomyx, Inc.
    Inventors: Catherine Tachdjian, Donald S. Karanewsky, Xiao-Qing Tang, Qing Chen, Peter Leeming, Tayyab Rashid, Daniel Levin
  • Patent number: 9603848
    Abstract: The present invention provides screening methods for identifying modifiers of chemosensory receptors and their ligands, e.g., by determining whether a test entity is suitable to interact with one or more interacting sites within the Venus flytrap domains of the chemosensory receptors as well as modifiers capable of modulating chemosensory receptors and their ligands.
    Type: Grant
    Filed: June 8, 2007
    Date of Patent: March 28, 2017
    Assignee: Senomyx, Inc.
    Inventors: Guy Servant, Xiaodong Li, Feng Zhang, Haitian Liu, Catherine Tachdjian, Xiao-Qing Tang, Sara Werner, Marketa Rinnova, Qing Chen, Albert Zlotnik, Mark Zoller, Boris Klebansky, Richard Fine, Xinshan Kang
  • Patent number: 9475803
    Abstract: The present invention includes compounds having structural formula (Ia): or salts or solvates thereof. These compounds are useful as sweet flavor modifiers. The present invention also includes compositions comprising the present compounds and methods of enhancing the sweet taste of compositions.
    Type: Grant
    Filed: February 19, 2014
    Date of Patent: October 25, 2016
    Assignee: Senomyx, Inc.
    Inventors: Sara Adamski-Werner, Vincent Darmohusodo, Catherine Tachdjian, Donald Karanewsky, Goran Petrovic, Rachel Kimmich, Joseph Fotsing
  • Patent number: 9181276
    Abstract: The present invention includes methods for identifying modifiers of chemosensory receptors and their ligands, e.g., by determining whether a test entity is suitable to interact with one or more interacting sites within the Venus flytrap domains of the chemosensory receptors, and modifiers capable of modulating chemosensory receptors and their ligands. The present invention also includes modifiers of chemosensory receptors and their ligands having Formula (I), its subgenus, and specific compounds. Furthermore, the present invention includes ingestible compositions comprising the modifiers of chemosensory receptors and their ligands and methods of using the modifiers of chemosensory receptors and their ligands to enhance the sweet taste of an ingestible composition or treat a condition associated with a chemosensory receptor. In addition, the present invention include processes for preparing the modifiers of chemosensory receptors and their ligands.
    Type: Grant
    Filed: November 12, 2013
    Date of Patent: November 10, 2015
    Assignee: Senomyx, Inc.
    Inventors: Catherine Tachdjian, Donald S. Karanewsky, Xiao-Qing Tang, Xiaodong Li, Feng Zhang, Guy Servant, Qing Chen, Vincent Darmohusodo, Richard Fine, Joseph R. Fotsing, Jeffrey Robert Hammaker, Xinshan Kang, Rachel D. A. Kimmich, Boris Klebansky, Haitian Liu, Goran Petrovic, Marketa Rinnova, Sara Adamski-Werner, Jeffrey Yamamoto, Hong Zhang, Albert Zlotnik
  • Patent number: 9000151
    Abstract: The present invention includes compounds having structural formula (I): or salts or solvates thereof. These compounds are useful as sweet flavor modifiers. The present invention also includes compositions comprising the present compounds and methods of enhancing the sweet taste of compositions.
    Type: Grant
    Filed: February 19, 2014
    Date of Patent: April 7, 2015
    Assignee: Senomyx, Inc.
    Inventors: Sara L. Adamski-Werner, Vincent Darmohusodo, Catherine Tachdjian, Donald S. Karanewsky
  • Publication number: 20150031684
    Abstract: The present invention includes compounds having structural formula (I), or salts or solvates thereof. These compounds are useful as sweet flavor modifiers. The present invention also includes compositions comprising the present compounds and methods of modulating the sweet taste of compositions.
    Type: Application
    Filed: August 1, 2014
    Publication date: January 29, 2015
    Inventors: Catherine TACHDJIAN, Donald KARANEWSKY, Sara WERNER, Vincent DARMOHUSODO, Jeff YAMAMOTO
  • Patent number: 8877922
    Abstract: The present invention includes compounds having structural formula (I): or salts or solvates thereof. These compounds are useful as sweet flavor modifiers. The present invention also includes compositions comprising the present compounds and methods of modulating the sweet taste of compositions.
    Type: Grant
    Filed: December 4, 2013
    Date of Patent: November 4, 2014
    Assignee: Senomyx, Inc.
    Inventors: Catherine Tachdjian, Donald Karanewsky, Sara Werner, Vincent Darmohusodo, Jeff Yamamoto
  • Publication number: 20140235624
    Abstract: The present invention includes compounds having structural formula (I), or salts or solvates thereof. These compounds are useful as sweet flavor modifiers. The present invention also includes compositions comprising the present compounds and methods of enhancing the sweet taste of compositions.
    Type: Application
    Filed: February 19, 2014
    Publication date: August 21, 2014
    Inventors: SARA L. ADAMSKI-WERNER, VINCENT DARMOHUSODO, CATHERINE TACHDJIAN, DONALD S. KARANEWSKY
  • Publication number: 20140094453
    Abstract: The present invention includes compounds having structural formula (I), or salts or solvates thereof. These compounds are useful as sweet flavor modifiers. The present invention also includes compositions comprising the present compounds and methods of modulating the sweet taste of compositions.
    Type: Application
    Filed: December 4, 2013
    Publication date: April 3, 2014
    Inventors: Catherine TACHDJIAN, Donald KARANEWSKY, Sara WERNER, Vincent DARMOHUSODO, Jeff YAMAMOTO
  • Patent number: 8633186
    Abstract: The present invention includes methods for identifying modifiers of chemosensory receptors and their ligands, e.g., by determining whether a test entity is suitable to interact with one or more interacting sites within the Venus flytrap domains of the chemosensory receptors, and modifiers capable of modulating chemosensory receptors and their ligands. The present invention also includes modifiers of chemosensory receptors and their ligands having Formula (I), its subgenus, and specific compounds. Furthermore, the present invention includes ingestible compositions comprising the modifiers of chemosensory receptors and their ligands and methods of using the modifiers of chemosensory receptors and their ligands to enhance the sweet taste of an ingestible composition or treat a condition associated with a chemosensory receptor. In addition, the present invention include processes for preparing the modifiers of chemosensory receptors and their ligands.
    Type: Grant
    Filed: June 3, 2008
    Date of Patent: January 21, 2014
    Assignee: Senomyx Inc.
    Inventors: Catherine Tachdjian, Donald S. Karanewsky, Xiao-Qing Tang, Xiaodong Li, Feng Zhang, Guy Servant, Qing Chen, Vincent Darmohusodo, Richard Fine, Joseph R. Fotsing, Jeffrey Robert Hammaker, Xinshan Kang, Rachel D. A. Kimmich, Boris Klebansky, Haitian Liu, Goran Petrovic, Marketa Rinnova, Sara Adamski-Werner, Jeffrey Yamamoto, Hong Zhang, Albert Zlotnik, Karen Zoller
  • Publication number: 20140011796
    Abstract: The present invention provides MDM2 inhibitor compounds of Formula I, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.
    Type: Application
    Filed: September 12, 2013
    Publication date: January 9, 2014
    Applicant: AMGEN INC.
    Inventors: Michael David BARTBERGER, Ana Gonzalez Buenrostro, Hilary Plake Beck, Xiaoqi Chen, Richard Victor Connors, Jeffrey Deignan, Jason Duquette, John Eksterwicz, Benjamin Fisher, Brian Matthew Fox, Jiasheng Fu, Zice Fu, Felix Gonzalez Lopez De Turiso, Michael William Gribble, Dann James Gustin, Julie Anne Heath, Xin Huang, Xianyun Jiao, Michael Johnson, Frank Kayser, David John Kopecky, Sujen Lai, Yihong Li, Zhihong Li, Jiwen Liu, Jonathan Dante Low, Brian Stuart Lucas, Zhihua Ma, Lawrence R. McGee, Joel McIntosh, Dustin McMinn, Julio Cesar Medina, Jeffrey Thomas Mihalic, Steven Howard Olson, Yosup Rew, Philip Marley Roveto, Daqing Sun, Xiaodong Wang, Yingcai Wang, Xuelei Yan, Ming Yu, Jiang Zhu
  • Publication number: 20130338095
    Abstract: Provided herein are methods for treating conditions associated with a chemosensory receptor, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administering a composition comprising a chemosensory receptor ligand. Also provided herein are chemosensory receptor ligand compositions and methods for the preparation thereof for use in the methods of the present invention.
    Type: Application
    Filed: October 18, 2011
    Publication date: December 19, 2013
    Applicant: ELCELYX THERAPEUTICS, INC.
    Inventors: Alain D. Baron, Martin R. Brown, Christopher R.G. Jones, Nigel R.A. Beeley
  • Patent number: 8586733
    Abstract: The present invention includes methods/processes and intermediates for preparing compounds having structural Formula (I): wherein X is alkyl, substituted alkyl, alkenyl, substituted alkenyl, heteroalkyl, substituted heteroalkyl, heteroalkenyl, or substituted heteroalkenyl.
    Type: Grant
    Filed: July 29, 2009
    Date of Patent: November 19, 2013
    Assignee: Senomyx, Inc.
    Inventors: Catherine Tachdjian, Donald S. Karanewsky, Xiao-Qing Tang, Qing Chen, Peter Leeming, Tayyab Rashid, Daniel Levin
  • Patent number: 8222405
    Abstract: Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to ?4 integrin. They are used as therapeutic agents for various diseases concerning ?4 integrin.
    Type: Grant
    Filed: November 22, 2010
    Date of Patent: July 17, 2012
    Assignee: Ajinomoto Co., Inc.
    Inventors: Shingo Makino, Tatsuya Okuzumi, Toshihiko Yoshimura, Yuko Satake, Nobuyasu Suzuki, Hiroyuki Izawa, Kazuyuki Sagi, Akira Chiba, Eiji Nakanishi, Masahiro Murata, Takashi Tsuji
  • Publication number: 20110319378
    Abstract: The present invention provides MDM2 inhibitor compounds of Formula I, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.
    Type: Application
    Filed: June 3, 2011
    Publication date: December 29, 2011
    Applicant: AMGEN INC.
    Inventors: Michael David BARTBERGER, Ana GONZALEZ BUENROSTRO, Hilary Plake BECK, Xiaoqi CHEN, Richard Victor CONNORS, Jeffrey DEIGNAN, Jason DUQUETTE, John EKSTEROWICZ, Benjamin FISHER, Brian Matthew FOX, Jiasheng FU, Zice FU, Felix GONZALEZ LOPEZ DE TURISO, Michael GRIBBLE, JR., Darin James GUSTIN, Julie Anne HEATH, Xin HUANG, Xianyun JIAO, Michael G. JOHNSON, Frank KAYSER, David John KOPECKY, Sujen LAI, Yihong LI, Zhihong LI, Jiwen LIU, Jonathan Dante LOW, Brian Stuart LUCAS, Zhihua MA, Lawrence McGEE, Joel McINTOSH, Dustin McMINN, Julio Cesar MEDINA, Jeffrey Thomas MIHALIC, Steven Howard Olson, Yosup REW, Philip Marley ROVETO, Daqing SUN, Xiaodong WANG, Yingcai WANG, Xuelei YAN, Ming YU, Jiang ZHU
  • Publication number: 20110245494
    Abstract: The present invention includes methods/processes and intermediates for preparing compounds having structural Formula (I): wherein X is alkyl, substituted alkyl, alkenyl, substituted alkenyl, heteroalkyl, substituted heteroalkyl, heteroalkenyl, or substituted heteroalkenyl.
    Type: Application
    Filed: July 29, 2009
    Publication date: October 6, 2011
    Applicant: SENOMYX, INC.
    Inventors: Catherine Tachdjian, Donald S. Karanewsky, Xiao-Qing Tang, Qing Chen, Peter Leeming, Tayyab Rashid, Daniel Levin
  • Publication number: 20110224155
    Abstract: The present invention includes methods for identifying modifiers of chemosensory receptors and their ligands, e.g., by determining whether a test entity is suitable to interact with one or more interacting sites within the Venus flytrap domains of the chemosensory receptors, and modifiers capable of modulating chemosensory receptors and their ligands. The present invention also includes modifiers of chemosensory receptors and their ligands having Formula (I), its subgenus, and specific compounds. Furthermore, the present invention includes ingestible compositions comprising the modifiers of chemosensory receptors and their ligands and methods of using the modifiers of chemosensory receptors and their ligands to enhance the sweet taste of an ingestible composition or treat a condition associated with a chemosensory receptor. In addition, the present invention include processes for preparing the modifiers of chemosensory receptors and their ligands.
    Type: Application
    Filed: June 3, 2008
    Publication date: September 15, 2011
    Applicant: SENOMYX INC.
    Inventors: Catherine Tachdjian, Donald S. Karanewsky, Xiao-Qing Tang, Xiaodong Li, Feng Zhang, Guy Servant, Qing Chen, Vincent Darmohusodo, Richard Fine, Joseph R. Fotsing, Jeffrey Robert Hammaker, Xinshan Kang, Rachel D.A. Kimmich, Boris Klebansky, Haitian Liu, Goran Petrovic, Marketa Rinnova, Sara Adamski-Werner, Jeffrey Yamamoto, Hong Zhang, Albert Zlotnik, Mark Zoller, Karen Zoller
  • Publication number: 20110065918
    Abstract: Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to ?4 integrin. They are used as therapeutic agents for various diseases concerning ?4 integrin.
    Type: Application
    Filed: November 22, 2010
    Publication date: March 17, 2011
    Applicant: Ajinomoto Co., Inc.
    Inventors: Shingo MAKINO, Tatsuya Okuzumi, Toshihiko Yoshimura, Yuko Satake, Nobuyasu Suzuki, Hiroyuki Izawa, Kazuyuki Sagi, Akira Chiba, Eiji Nakanishi, Masahiro Murata, Takashi Tsuji
  • Patent number: 7902203
    Abstract: The present invention provides an HCV polymerase inhibiting compound having the formula (I) and a composition comprising a therapeutically effective amount of said compound. The present invention also provides a method for inhibiting hepatitis C virus (HCV) polymerase, a method for inhibiting HCV viral replication, and a method for treating or preventing HCV infection. Processes for making said compounds, and synthetic intermediates employed in said processes, are also provided.
    Type: Grant
    Filed: October 31, 2003
    Date of Patent: March 8, 2011
    Assignee: Abbott Laboratories, Inc.
    Inventors: John K. Pratt, David A. Betebenner, Pamela L. Donner, Brian E. Green, Dale J. Kempf, Keith F. McDaniel, Clarence J. Maring, Vincent S. Stoll, Rong Zhang, Hui-Ju Chen, William J. Flosi, Larry L. Klein, Allan C. Krueger, Dachun Liu, Darold L. Madigan, Laura M. Maymon, Todd W. Rockway, Kent D. Stewart, Ming C. Yeung, Qinghua Xie
  • Patent number: 7875618
    Abstract: The invention relates to imidazo[1,5-a]quinoxaline derivatives having Formula IIa: to processes for preparing them, to pharmaceutical preparations which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 10 (PDE10), as active compounds for treating central nervous system diseases of mammals, including humans.
    Type: Grant
    Filed: November 25, 2008
    Date of Patent: January 25, 2011
    Assignees: Wyeth, elbion GmbH
    Inventors: Michael S. Malamas, Yike Ni, James Joseph Erdei, Norbert Höfgen, Hans Stange, Rudolf Schindler, Ute Egerland, Barbara Langen
  • Publication number: 20100190778
    Abstract: The present invention is related to new 3,4-dihydroberizo[1,2,3]thiadiazine-1,1-dioxide derivatives of the Formula (I), medicaments containing said new compounds, process for the preparation thereof and the use of said derivatives in the medicine. The compounds according to the present invention are suitable for the treatment or prevention of disorders of the central nervous system.
    Type: Application
    Filed: August 13, 2007
    Publication date: July 29, 2010
    Applicant: EGIS GYOGYSZERGYAR NYILVANOSAN MUKODO RESZVENTARSASAG
    Inventors: Marta Porcs-Makkay, Gyula Lukacs, Gabor Kapus, Istvan Gacsalyi, Gyula Simig, Gyoergy Levay, Tibor Mezei, Miklos Vegh, Szabolcs Kertesz, Jozsef Barkoczy, Csilla Leveleki, Laszlo Gabor Harsing
  • Publication number: 20100184749
    Abstract: Chemokine receptor antagonists, in particular, compounds of Formula (I) that act as antagonists of the chemokine CCR2 receptor, including pharmaceutical compositions and uses thereof to treat or prevent diseases associated with monocyte accumulation, lymphocyte accumulation or leukocyte accumulation are described herein.
    Type: Application
    Filed: October 12, 2007
    Publication date: July 22, 2010
    Applicant: EPIX Delaware ,Inc.
    Inventors: Merav Fichman, Rosa E. Melendez, Pradyumna Mohanty, Jian Lin, Dilara McCauley, Boaz Inbal, Mercedes Lobera, Pini Orbach, Ori Kalid, Dongli Chen, Yael Marantz, Michael Xie, Sharon Shacham, Oren Becker
  • Publication number: 20100168087
    Abstract: The present invention relates to new benzo[1,2,3]thiadiazine-1,1-dioxide derivatives of the general Formula (I), medicaments containing such compounds and the use thereof in the medicine. Benzo[1,2,3]thiadiazine-1,1-dioxide derivatives of the general Formula (I) are suitable for the prevention or treatment of the diseases of the central nervous system.
    Type: Application
    Filed: August 13, 2007
    Publication date: July 1, 2010
    Inventors: Marta Porcs-Makkay, Gyula Lukacs, Gabor Kapus, Istvan Gacsalyi, Gyula Simig, Gyoergy Levay, Tibor Mezei, Miklos Vegh, Szabolcs Kertesz, Jozsef Barkoczy, Csilla Leveleki, Laszlo Gabor Harsing
  • Patent number: 7718652
    Abstract: The present invention is directed to substituted benzothiadiazinedioxide derivatives of formula I: or a pharmaceutically acceptable salt, stereoisomer or tautomer thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, vasomotor symptoms, sexual dysfunction, gastrointestinal disorders and genitourinary disorder, depression disorders, endogenous behavioral disorders, cognitive disorders, diabetic neuropathy, pain, and other diseases or disorders.
    Type: Grant
    Filed: December 12, 2007
    Date of Patent: May 18, 2010
    Assignee: Wyeth LLC
    Inventors: Joel Adam Goldberg, Andrew Fensome, Casey Cameron McComas, Puwen Zhang
  • Publication number: 20090163480
    Abstract: The present invention relates to modified amino acids of general formula wherein A, Z, X, n, m, R, R2, R3, R4 and R11 are defined as in claims 1 to 5, their tautomers, their diastereomers, their enantiomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them as well as their use for the production and purification of antibodies and as labelled compounds in RIA- and ELISA assays and as diagnostic or analytical aids in neurotransmitter research.
    Type: Application
    Filed: December 17, 2008
    Publication date: June 25, 2009
    Applicant: Dr. Karl Thomae GmbH
    Inventors: Klaus RUDOLF, Wolfgang EBERLEIN, Wolfhard ENGEL, Helmut PIEPER, Henri DOODS, Gerhard HALLERMAYER, Michael ENTZEROTH, Wolfgang WIENEN
  • Patent number: 7476667
    Abstract: The invention relates to indole acetic acid compounds which function as antagonists of the CRTH2 receptor. The invention also relates to the use of these compounds to inhibit the binding of prostaglandin D2 and its metabolites or certain thromboxane metabolites to the CRTH2 receptor and to treat disorders responsive to such inhibition.
    Type: Grant
    Filed: June 2, 2008
    Date of Patent: January 13, 2009
    Assignee: Wyeth
    Inventors: Youssef L. Bennani, Lawrence Nathan Tumey, Elizabeth Ann Gleason, Michael Joseph Robarge
  • Publication number: 20080306053
    Abstract: The present invention provides screening methods for identifying modifiers of chemosensory receptors and their ligands, e.g., by determining whether a test entity is suitable to interact with one or more interacting sites within the Venus flytrap domains of the chemosensory receptors as well as modifiers capable of modulating chemosensory receptors and their ligands.
    Type: Application
    Filed: August 8, 2007
    Publication date: December 11, 2008
    Applicant: SENOMYX, INC.
    Inventors: Catherine Tachdjian, Xiao-Qing Tang, Sara Werner, Marketa Rinnova, Qing Chen, Guy Servant, Xiaodong Li, Feng Zhang, Haitian Liu, Albert Zlotnik, Mark Zoller, Boris Klebansky, Richard Fine, Xinshan Kang
  • Publication number: 20080255100
    Abstract: The invention relates to indole acetic acid compounds which function as antagonists of the CRTH2 receptor. The invention also relates to the use of these compounds to inhibit the binding of prostaglandin D2 and its metabolites or certain thromboxane metabolites to the CRTH2 receptor and to treat disorders responsive to such inhibition.
    Type: Application
    Filed: June 2, 2008
    Publication date: October 16, 2008
    Applicant: Wyeth
    Inventors: Youssef L. Bennani, Lawrence Nathan Tumey, Elizabeth Ann Gleason, Michael Joseph Robarge
  • Patent number: 7410964
    Abstract: Compounds of formula I: inhibit gamma-secretase and hence find use in treatment or prevention of Alzheimer's disease.
    Type: Grant
    Filed: May 7, 2004
    Date of Patent: August 12, 2008
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Kevin Dinnell, Karl Richard Gibson, Timothy Harrison, Richard Alexander Jelley, Alan John Nadin, Paul Joseph Oakley, Andrew Pate Owens, Duncan Edward Shaw, Brian John Williams
  • Publication number: 20080176830
    Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.
    Type: Application
    Filed: April 13, 2006
    Publication date: July 24, 2008
    Inventors: Nicholas D. Adams, Michael Gerard Darcy, Dashyant Dhanak, Kevin J. Duffy, Duke M. Fitch, Steven David Knight, Kenneth Allen Newlander, Antony N. Shaw
  • Publication number: 20080161295
    Abstract: The present invention is directed to substituted benzothiadiazinedioxide derivatives of formula I: or a pharmaceutically acceptable salt, stereoisomer or tautomer thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, vasomotor symptoms, sexual dysfunction, gastrointestinal disorders and genitourinary disorder, depression disorders, endogenous behavioral disorders, cognitive disorders, diabetic neuropathy, pain, and other diseases or disorders.
    Type: Application
    Filed: December 12, 2007
    Publication date: July 3, 2008
    Applicant: Wyeth
    Inventors: Joel Adam Goldberg, Andrew Fensome, Casey Cameron McComas, Puwen Zhang
  • Patent number: 7365063
    Abstract: Compounds of the formula I: and pharmaceutically acceptable salts thereof wherein X is N, Y is S, Z is —(CRaRb)r—, A is —NR3, m is 2, n is 1, q is 2, R2 is optioinally substituted aryl or optionally substituted heteroaryl, and p, R1, R3, R4, R5, R6, R7, R8, R9, and R10, are as defined herein. The invention also provides methods for preparing, compositions comprising, and methods for using compounds of formula I for treatment of central nervous system diseases.
    Type: Grant
    Filed: February 7, 2007
    Date of Patent: April 29, 2008
    Assignee: Roche Palo Alto LLC
    Inventors: Nancy Elisabeth Krauss, Meng Sui, Shu-Hai Zhao
  • Patent number: 7358239
    Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is
    Type: Grant
    Filed: March 14, 2005
    Date of Patent: April 15, 2008
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
  • Patent number: 6982264
    Abstract: The invention relates to substituted alcohol compounds of the formula (I): wherein X, R1, R2, R3, RN, R20 and RC are defined herein. The compounds are useful in the treatment or prevention of Alzheimer's disease and more specifically to compounds that are capable of inhibiting beta-secretase, an enzyme that cleaves amyloid precursor protein to produce amyloid beta peptide (A-beta), a major component of the amyloid plaques found in the brains of Alzheimer's sufferers.
    Type: Grant
    Filed: June 27, 2002
    Date of Patent: January 3, 2006
    Assignee: Elan Pharmaceuticals, Inc.
    Inventors: Varghese John, Roy Hom, John Tucker
  • Patent number: 6900222
    Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereon wherein —Z1—Z2— is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is a
    Type: Grant
    Filed: May 23, 2000
    Date of Patent: May 31, 2005
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
  • Patent number: 6894043
    Abstract: Compound selected from those of formula (I): wherein: X represents flourine, bromine, iodine or methyl, each of R1 and R2, which may be identical or different, represents hydrogen or alkyl, its isomers when they exist, and addition salts thereof with a pharmaceutically acceptable acid Medicinal products containing the same which are useful as AMPA modulators.
    Type: Grant
    Filed: November 28, 2000
    Date of Patent: May 17, 2005
    Assignee: Les Laboratoires Servier
    Inventors: Bernard Pirotte, Pascal De Tullio, Stéphane Boverie, Isabelle Kempen, Pierre Lestage
  • Patent number: 6861421
    Abstract: A compound of the having the general formula (I) or general formula (II): wherein Z, A, B, C, R1, R2, Q, W, and n are as described herein.
    Type: Grant
    Filed: April 18, 2002
    Date of Patent: March 1, 2005
    Assignee: Euro-Celtique S.A
    Inventors: R. Richard Goehring, Zhengming Chen, John Whitehead, Parviz Gharagozloo, Sam Victory, Donald Kyle
  • Patent number: 6844338
    Abstract: A pharmaceutical compound of the formula (I) in which R1 and R2 are each hydrogen or C1-6 alkyl, R3 is —SR10, —SOR10, —SO2R10, —COR10, —CH2OH or —CONHR11, where R10 is C1-6 alkyl and R11 is hydrogen or C1-6 alkyl, R4, R5, R6 and R7 are each hydrogen or C1-6alkyl, provided that at least one of R4, R5, R6 and R7 is C1-6alkyl, R8 and R9 are each hydrogen, halo, C1-6 alkyl or cyano, n is 0 or 1 and m is 2 or 3, x is a (a) or (b), and y is (c) or (d), wherein R12 and R13 are each hydrogen, C1- alkyl, cyclopropyl or cyclopropyl-C1-6 alkyl; and salts thereof.
    Type: Grant
    Filed: May 4, 2001
    Date of Patent: January 18, 2005
    Assignee: Eli Lilly and Company
    Inventors: John Fairhurst, Peter Gallagher
  • Publication number: 20040198724
    Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides quinazolinone, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety and motor neuron diseases) and as neuroprotective agents (e.g., to prevent stroke and the like) by modulating potassium channels associated with the onset or recurrence of the indicated conditions.
    Type: Application
    Filed: December 23, 2003
    Publication date: October 7, 2004
    Applicant: ICAgen, Inc.
    Inventors: Grant A. McNaughton-Smith, James B. Thomas, George S. Amato
  • Publication number: 20040167123
    Abstract: The present invention provides an HCV polymerase inhibiting compound having the formula (I) 1
    Type: Application
    Filed: October 31, 2003
    Publication date: August 26, 2004
    Inventors: John K. Pratt, David A. Betebenner, Pamela L. Donner, Brian E. Green, Dale J. Kempf, Keith F. McDaniel, Clarence J. Maring, Vincent S. Stoll, Rong Zhang
  • Publication number: 20030225068
    Abstract: A pharmaceutical compound of the formula (I) in which R1 and R2 are each hydrogen or C1-6 alkyl, R3 is —SR10, —SOR10, —SO2R10, —COR10, —CH2OH or —CONHR11, where R10 is C1-6 alkyl and R11 is hydrogen or C1-6 alkyl, R4, R5, R6 and R7 are each hydrogen or C1-6 alkyl, provided that at least one of R4, R5, R6 and R7 is C1-6 alkyl, R8 and R9 are each hydrogen, halo, C1-6 alkyl or cyano, n is 0 or 1 and m is 2 or 3, x is a (a) or (b), and y is (c) or (d), wherein R12 and R13 are each hydrogen, C1- alkyl, cyclopropyl or cyclopropyl-C1-6 alkyl; and salts thereof.
    Type: Application
    Filed: October 21, 2002
    Publication date: December 4, 2003
    Inventors: John Fairhurst, Peter Gallagher
  • Publication number: 20030144274
    Abstract: A compound of Formula I 1
    Type: Application
    Filed: October 4, 2002
    Publication date: July 31, 2003
    Inventors: Amy Mae Bunker, William Glen Harter, James Lester Hicks, Patrick Michael O'Brien, Ly Pham, Joseph Armand Picard, William Howard Roark
  • Patent number: 6495547
    Abstract: The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein Alk1 is C1-6alkanediyl optionally substituted with hydroxy, C1-4alkyloxy or C1-4alkylcarbonyloxy; —Z1—Z2— is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical; R4 is hydrogen or C1-6alkyl; A is a bivalent radical of formula —NR6—Alk2— (b-1), or —Npiperidinyl-(CH2)m (b-2) wherein m is 0 or 1; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen.
    Type: Grant
    Filed: August 18, 2000
    Date of Patent: December 17, 2002
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren, Marc Francis Josephine Schroven, Marcel Frans Leopold De Bruyn
  • Patent number: 6329366
    Abstract: A pharmaceutical compound of the formula in which R1 and R2 are each hydrogen, halo, cyano or methyl, the dotted line represents an optional double bond, where R4 and R5 are each hydrogen, C1-6 alkyl, cyclopropyl or cyclopropyl-C1-6 alkyl, n is 0 or 1, and R3 is —SR6, —SOR6, —SO2R6, —COR6, —CH2OH or —CONHR7, where R6 is C1-6 alkyl and R7 is hydrogen or C1-6 alkyl; provided that when one of R1 and R2 is hydrogen and the other is fluoro, R4 and R5 are each hydrogen or C1-6 alkyl, and n is 0, then R3 is not —COR6 or —CONHR7; and salts thereof.
    Type: Grant
    Filed: November 18, 1999
    Date of Patent: December 11, 2001
    Assignee: Eli Lilly and Company Limited
    Inventors: John Fairhurst, Peter Thaddeus Gallagher, Martin Victor Miles
  • Patent number: 6252069
    Abstract: A process for preparing 3-isopropyl-1H-2,1,3-benzothiadiazin-4 (3H)-one 2,2-dioxide (I) or a salt of I which comprises reacting anthranilic isopropylamide II simultaneously with sulfur trioxide or chlorosulfonic acid in the presence of an organic base or with adducts of sulfur trioxide and organic bases and phosphorus oxychloride at from 50° C. to the reflux temperature, followed, if appropriate, by conversion into its salts, is described.
    Type: Grant
    Filed: February 17, 2000
    Date of Patent: June 26, 2001
    Assignee: BASF Aktiengesellschaft
    Inventors: Hans Rupert Merkle, Otto Wörz, Erich Fretschner, Hanspeter Hansen, Albrecht Müller, Kurt Benz
  • Patent number: 6069114
    Abstract: Compounds of the formula (I) and their salts ##STR1## in which R.sup.1 to R.sup.6, Y.sup.1, to Y.sup.2, Y.sup.3, m and n are as defined in claim 1 are suitable as herbicides and plant growth regulators. They can be prepared analogously to known processes using intermediates of the formula (V) (cf. claim 6).
    Type: Grant
    Filed: February 25, 1997
    Date of Patent: May 30, 2000
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Klaus Lorenz, Klemens Minn, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
  • Patent number: 6011034
    Abstract: Insecticidal dihydrooxadiazine compounds having the formula: ##STR1## wherein X is O or S; R is a substituted or unsubstituted phenyl or heterocyclic group; R.sup.1 is halogen, haloalkyl or haloalkoxy; R.sup.2, R.sup.3 , and R.sup.4 are, independently, hydrogen, alkyl or alkoxy; R.sup.5 is nitro, cyano, alkoxy, alkyl, haloalkoxy, dialkylamino, alkylthio, phenoxy, phenylthio, or alkoxycarbonyl; R.sup.6 is hydrogen, alkyl, alkylthio, alkoxyalkyl, alkoxycarbonyl, acyl, or benzyl, wherein R.sup.3 and R.sup.5 together can form a ring.
    Type: Grant
    Filed: February 12, 1998
    Date of Patent: January 4, 2000
    Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Co./CIE.
    Inventors: Anupama Mishra, Mark Achiel Dekeyser, Paul Thomas McDonald