1,2,4-benzothiadiazines Patents (Class 544/12)
  • Patent number: 11198689
    Abstract: The invention encompasses compounds having formula I-V and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, may be therapeutically useful.
    Type: Grant
    Filed: August 26, 2019
    Date of Patent: December 14, 2021
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Hui Li, Sambaiah Thota, David Carroll, Ankush Argade, Kin Tso, Arvinder Sran, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Vanessa Taylor, Robin Cooper, Rajinder Singh, Brian Wong
  • Patent number: 10421752
    Abstract: The invention encompasses compounds having formula I-V and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, may be therapeutically useful.
    Type: Grant
    Filed: June 29, 2017
    Date of Patent: September 24, 2019
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Hui Li, Sambaiah Thota, David Carroll, Ankush Argade, Kin Tso, Arvinder Sran, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Vanessa Taylor, Robin Cooper, Rajinder Singh, Brian Wong
  • Patent number: 9381202
    Abstract: Provided are immediate or prolonged administration of certain salts of KATP channel openers such as diazoxide to a subject to achieve novel pharmacodynamic, pharmacokinetic, therapeutic, physiological, metabolic and compositional outcomes in the treatment of diseases or conditions involving KATP channels. Also provided are pharmaceutical formulations, methods of administration and dosing of the salts that achieve these outcomes and reduce the incidence of adverse effects in treated individuals. Further provided are method of co-administering the salts with other drugs to treat diseases of humans and animals.
    Type: Grant
    Filed: March 18, 2013
    Date of Patent: July 5, 2016
    Assignee: ESSENTIALIS, INC.
    Inventors: Neil M. Cowen, Khaled A. Yamout
  • Patent number: 9315478
    Abstract: The invention relates to compounds of Formula I: and its pharmaceutical acceptable salts, solvates, enantiomers, stereoisomers and hydrates thereof. Compounds of Formula I and and compositions comprising Formula I are used to treat patients with metabolic syndrome and may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, or parenteral administration, as a syrup, or for injection.
    Type: Grant
    Filed: February 3, 2013
    Date of Patent: April 19, 2016
    Assignee: CELLIX BIO PRIVATE LIMITED
    Inventor: Mahesh Kandula
  • Patent number: 9156832
    Abstract: The invention is directed to 5,6-dihydro-1H-pyridin-2-one compounds and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.
    Type: Grant
    Filed: June 10, 2014
    Date of Patent: October 13, 2015
    Assignee: Anadys Pharmaceuticals, Inc.
    Inventors: Peter Dragovich, Douglas E. Murphy
  • Publication number: 20150126497
    Abstract: The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of metabolic syndrome may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection.
    Type: Application
    Filed: February 3, 2013
    Publication date: May 7, 2015
    Inventor: Mahesh Kandula
  • Publication number: 20150126498
    Abstract: The disclosures herein relate to novel compounds of formula wherein W, X and Y1, Y2, Y3 and Y4 are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of neurological or psychiatric disorders associated with orexin receptors.
    Type: Application
    Filed: July 3, 2013
    Publication date: May 7, 2015
    Inventors: Miles Stuart Congreve, John Andrew Christopher, Benjamin Gerald Tehan, Sukhbinder Singh Klair, Sarah Joanne Aves
  • Publication number: 20140364414
    Abstract: Disclosed are compounds, compositions and methods for treating Type II diabetes. Such compounds are represented by Formula (I) as follows: wherein R1, R2, L, and Q are defined herein.
    Type: Application
    Filed: June 9, 2014
    Publication date: December 11, 2014
    Applicant: JANSSEN PHARMACEUTICA, NV
    Inventors: Mark R. Player, Sanath K. Meegalla, Carl R. Illig, Jinsheng Chen, Kenneth J. Wilson, Yu-Kai Lee, Daniel J. Parks, Hui Huang, Sharmila Patel, Tianbao Lu
  • Publication number: 20140357626
    Abstract: Inhibitors of HCV replication of formula I, including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R and R? have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in HCV therapy.
    Type: Application
    Filed: December 27, 2012
    Publication date: December 4, 2014
    Inventors: Koen Vandyck, Wim Gaston Verschueren, Pierre Jean-Marie Bernard Raboisson
  • Patent number: 8815848
    Abstract: The invention encompasses compounds having formula I-V and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, may be therapeutically useful.
    Type: Grant
    Filed: January 25, 2013
    Date of Patent: August 26, 2014
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Hui Li, Sambaiah Thota, David Carroll, Ankush Argade, Kin Tso, Arvinder Sran, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Vanessa Taylor, Robin Cooper, Rajinder Singh, Brian Wong
  • Patent number: 8815849
    Abstract: Inhibitors of HCV replication of formula I including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R and R? have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in HCV therapy.
    Type: Grant
    Filed: July 26, 2011
    Date of Patent: August 26, 2014
    Assignee: Janssen R&D Ireland
    Inventors: Koen Vandyck, Wim Gaston Verschueren, Pierre Jean-Marie Bernard Raboisson
  • Publication number: 20130343992
    Abstract: Compounds of formula (I) are disclosed Compounds of formula (I) are useful in treating conditions and disorders prevented by or ameliorated by PDE10A ligands. Radiolabeled compounds of formula (I) are also useful as diagnostic tools as PDE10A positron emission tomography ligands. Also disclosed are pharmaceutical compositions comprising compound of formula (I), methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).
    Type: Application
    Filed: December 21, 2012
    Publication date: December 26, 2013
    Applicant: AbbVie Inc.
    Inventor: AbbVie Inc.
  • Publication number: 20130338151
    Abstract: The present invention relates to arylcarbonyl and heteroarylcarbonyl anthranilate compounds that may be useful as anti-fibrotic agents. The present invention also relates to methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment disorders.
    Type: Application
    Filed: October 21, 2010
    Publication date: December 19, 2013
    Applicant: Fibrotech Therapeutics Pty Ltd
    Inventors: Spencer John Williams, Steven Zammit, Darren James Kelly
  • Patent number: 8586578
    Abstract: The invention is directed to deuterated 5,6-dihydro-1H-pyridin-2-one compounds of Formula I and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.
    Type: Grant
    Filed: October 27, 2010
    Date of Patent: November 19, 2013
    Assignee: Anadys Pharmaceuticals, Inc.
    Inventor: Stephen E. Webber
  • Publication number: 20130225806
    Abstract: Provided are immediate or prolonged administration of certain salts of KATP channel openers such as diazoxide to a subject to achieve novel pharmacodynamic, pharmacokinetic, therapeutic, physiological, metabolic and compositional outcomes in the treatment of diseases or conditions involving KATP channels. Also provided are pharmaceutical formulations, methods of administration and dosing of the salts that achieve these outcomes and reduce the incidence of adverse effects in treated individuals. Further provided are method of co-administering the salts with other drugs to treat diseases of humans and animals.
    Type: Application
    Filed: March 18, 2013
    Publication date: August 29, 2013
    Applicant: Essentialis, Inc.
    Inventors: Neil M. Cowen, Khaled A. Yamout
  • Publication number: 20130123244
    Abstract: Inhibitors of HCV replication of formula I including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R and R? have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in HCV therapy.
    Type: Application
    Filed: July 26, 2011
    Publication date: May 16, 2013
    Applicant: JANSSEN R&D IRELAND
    Inventors: Koen Vandyck, Wim Gaston Verschueren, Pierre Jean-Marie Bernard Raboisson
  • Publication number: 20120270863
    Abstract: The present invention relates to arylcarbonyl and heteroarylcarbonyl anthranilate compounds that may be useful as anti-fibrotic agents. The present invention also relates to methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment disorders.
    Type: Application
    Filed: October 21, 2010
    Publication date: October 25, 2012
    Applicant: Fibrotech Therapeutics Pty Ltd
    Inventors: Spencer John Williams, Steven Zammit, Darren James Kelly
  • Publication number: 20120238554
    Abstract: Provided are immediate or prolonged administration of certain salts of KATP channel openers such as diazoxide to a subject to achieve novel pharmacodynamic, pharmacokinetic, therapeutic, physiological, metabolic and compositional outcomes in the treatment of diseases or conditions involving KATP channels. Also provided are pharmaceutical formulations, methods of administration and dosing of the salts that achieve these outcomes and reduce the incidence of adverse effects in treated individuals. Further provided are method of co-administering the salts with other drugs to treat diseases of humans and animals.
    Type: Application
    Filed: February 27, 2012
    Publication date: September 20, 2012
    Inventor: Neil M. Cowen
  • Patent number: 8236948
    Abstract: The invention is directed to 5,6-dihydro-1H-pyridin-2-one compounds of Formula I wherein X is N, and A is and compounds used to synthesize the compounds of Formula I.
    Type: Grant
    Filed: January 23, 2012
    Date of Patent: August 7, 2012
    Assignee: Anadys Pharmaceuticals, Inc.
    Inventors: Chinh V. Tran, Frank Ruebsam, Douglas E. Murphy, Peter Dragovich
  • 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
  • Patent number: 8222404
    Abstract: The invention is directed to a [7-methanesulfonylamino-methyl)-1,1-dioxo-1,4-dihydro-1?6-thieno[2,3-e][1,2,4]thiadiazin-3-yl]-acetic acid compound and to methods of making the same.
    Type: Grant
    Filed: January 13, 2012
    Date of Patent: July 17, 2012
    Assignee: Anadys Pharmaceuticals, Inc.
    Inventors: Peter Dragovich, Douglas Eric Murphy
  • Publication number: 20120165321
    Abstract: Invented is a method of inhibiting the activity/function of PI3 kinases using quinoline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinoline derivatives.
    Type: Application
    Filed: March 5, 2012
    Publication date: June 28, 2012
    Inventors: Nicholas D. Adams, Joelle Lorraine Burgess, Michael Gerrard Darcy, Carla A. Donatelli, Steven David Knight, Kenneth Allen Newlander, Lance Ridgers, Martha A. Sarpong, Stanley J. Schmidt
  • Patent number: 8138347
    Abstract: Invented is a method of inhibiting the activity/function of PI3 kinases using quinoline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinoline derivatives.
    Type: Grant
    Filed: May 16, 2008
    Date of Patent: March 20, 2012
    Assignee: GlaxoSmithKline LLC
    Inventors: Steven David Knight, Stanley J. Schmidt
  • Patent number: 8101800
    Abstract: The invention is directed to a 5,6-dihydro-1H-pyridin-2-one compound selected from:
    Type: Grant
    Filed: March 8, 2011
    Date of Patent: January 24, 2012
    Assignee: Anadys Pharmaceuticals, Inc.
    Inventors: Chinh V. Tran, Frank Ruebsam, Douglas E. Murphy, Peter Dragovich, Yuefen Zhou, Lijian Chen, David Kucera, Fritz Blatter, Martin Viertelhaus
  • Patent number: 8097613
    Abstract: The invention is directed to [1,2,4]thiadiazine 1,1-dioxide compounds of formula I wherein A is B is and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.
    Type: Grant
    Filed: June 9, 2009
    Date of Patent: January 17, 2012
    Assignee: Anadys Pharmaceuticals, Inc.
    Inventors: Frank Ruebsam, Peter Dragovich, Stephen E. Webber, Douglas Eric Murphy, Chinh Viet Tran
  • Patent number: 8022066
    Abstract: The present invention relates to novel compounds that act as chemical uncouplers. Compounds of the invention are useful, inter alia, in the treatment, including prevention, of obesity, diabetes and a number of diseases or conditions associated therewith.
    Type: Grant
    Filed: November 15, 2007
    Date of Patent: September 20, 2011
    Assignee: High Point Pharmaceuticals, LLC
    Inventors: Anders Klarskov Petersen, Preben Houlberg Olesen, Lise Brown Christiansen, Holger Claus Hansen, Flemming Elmelund Nielsen
  • Patent number: 7939524
    Abstract: The invention is directed to 5,6-dihydro-1H-pyridin-2-one compounds of Formula I wherein X is N, and A is and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.
    Type: Grant
    Filed: April 2, 2008
    Date of Patent: May 10, 2011
    Assignee: Anadys Pharmaceuticals, Inc.
    Inventors: Chinh V. Tran, Frank Ruebsam, Douglas E. Murphy, Peter Dragovich, Yuefen Zhou, Lijian Chen, David Kucera
  • 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
  • Publication number: 20110033417
    Abstract: The present invention relates to 2,3-Substituted Indole Derivatives, compositions comprising at least one 2,3-Substituted Indole Derivative, and methods of using the 2,3-Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Application
    Filed: August 27, 2008
    Publication date: February 10, 2011
    Inventors: Gopinadhan N. Anilkumar, Frank Bennett, Tin-Yau Chan, Kevin X. Chen, Mousumi Sannigrahi, Francisco Velazquez, Srikanth Venkatraman, Qingbei Zeng, Jose S. Duca, Charles A. Lesburg, Joseph A. Kozlowski, F. George Njoroge, Stuart B. Rosenblum, Neng-Yang Shih, Stephen J. Gavalas, Yueheng Jiang, Patrick A. Pinto, Haiyan Pu, Oleg B. Selyutin, Bancha Vibulbhan, Li Wang, Wanli Wu, Weiying Yang, Yuhua Huang, Hsueh-Cheng Huang, Robert Palermo, Boris Feld
  • Publication number: 20100324029
    Abstract: The invention encompasses 2-[4-(imidazolyl)-phenyl]vinyl-heterocycle derivatives which selectively attenuate production of Abeta(1-42) and are useful in the treatment of Alzheimer's disease. Pharmaceutical compositions and methods of use are also encompassed.
    Type: Application
    Filed: February 5, 2008
    Publication date: December 23, 2010
    Inventors: Christian Fischer, Benito Munoz, Alexey A. Rivkin
  • Patent number: 7834009
    Abstract: The invention is directed to 4-hydroxy-5,6-dihydro-1H-pyridin-2-one compounds of Formula I and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus: wherein R6 is X is N, Ring A is a 5- or 6-membered aryl, optionally substituted by 1-3 R8 moieties, n is 2, and R1-R6 and R8 are defined herein.
    Type: Grant
    Filed: August 27, 2007
    Date of Patent: November 16, 2010
    Assignee: Anadys Pharmaceuticals, Inc.
    Inventors: David Ellis, Liansheng Li, Chinh V. Tran, Frank Ruebsam, Yuefen Zhou
  • Publication number: 20100273784
    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, maintaining bladder control or treating urinary incontinence) 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: April 9, 2010
    Publication date: October 28, 2010
    Applicant: Icagen, Inc.
    Inventors: Grant Andrew McNaughton-Smith, George Salvatore Amato, James Barnwell Thomas, JR.
  • Patent number: 7799777
    Abstract: Provided are immediate or prolonged administration of certain salts of KATP channel openers such as diazoxide to a subject to achieve novel pharmacodynamic, pharmacokinetic, therapeutic, physiological, metabolic and compositional outcomes in the treatment of diseases or conditions involving KATP channels. Also provided are pharmaceutical formulations, methods of administration and dosing of the salts that achieve these outcomes and reduce the incidence of adverse effects in treated individuals. Further provided are method of co-administering the salts with other drugs to treat diseases of humans and animals.
    Type: Grant
    Filed: December 20, 2006
    Date of Patent: September 21, 2010
    Assignee: Essentialis, Inc.
    Inventors: Neil M. Cowen, Khaled A. Yamout
  • Publication number: 20100160300
    Abstract: Methods for treatment of depression-related mood disorders in mammals, particularly humans are disclosed. The methods of the invention include administration of compounds capable of enhancing glutamate transporter activity in the brain of mammals suffering from depression. ATP-sensitive K+ channel openers and ?-lactam antibiotics are used to enhance glutamate transport and to treat depression-related mood disorders and depressive symptoms.
    Type: Application
    Filed: December 18, 2009
    Publication date: June 24, 2010
    Applicant: Brookhaven Science Associates, LLC
    Inventor: Fritz Henn
  • Patent number: 7741320
    Abstract: Compounds of formula (I): wherein: RCy represents an unsubstituted or substituted cycloalkyl group or cycloalkylalkyl group, R1, R2, R3 and R4, which may be the same or different, each represent a hydrogen or halogen atom or a nitro group; a cyano group; a hydroxy group; an alkoxy group; an alkyl group; an unsubstituted or substituted amino group; a carboxy group; an alkoxycarbonyl group; an aryloxycarbonyl group; an unsubstituted or substituted aminocarbonyl group. Medicinal products containing the same which are useful in treating or preventing conditions treatable by an AMPA receptor modulator.
    Type: Grant
    Filed: July 9, 2009
    Date of Patent: June 22, 2010
    Assignee: Les Laboratoires Servier
    Inventors: Pierre Francotte, Pascal De Tullio, Bernard Pirotte, Laurence Danober, Pierre Lestage, Daniel-Henri Caignard
  • Publication number: 20100035866
    Abstract: The present invention relates to compounds of substituted-1,1-dioxo-benzo[1,2,4]thiadiazin-3-ones acting as a 5HT6 receptor antagonist, a preparation method thereof, and a pharmaceutical composition containing the same for treatment of the central nervous system disorders. The compounds of substituted-1,1-dioxo-benzo[1,2,4]thiadiazin-3-ones according to the present invention have excellent binding affinity for the 5HT6 receptor and excellent selectivity for the 5HT6 receptor over other receptors. Also, the compounds reverse a disruption of PPI by apomorphine and don't show rotatod deficit in mice. Therefore the compounds according to the present invention may be valuably used for treatment of a 5HT6 receptor relating disorders.
    Type: Application
    Filed: March 28, 2006
    Publication date: February 11, 2010
    Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
    Inventors: Churlmin Seong, Jinil Choi, Chul Min Park, Wookyu Park, Jaeyang Kong, Sunhee Kang, Chimin Park
  • Publication number: 20100009974
    Abstract: Compounds of formula (I): wherein: RCy represents an unsubstituted or substituted cycloalkyl group or cycloalkylalkyl group, R1, R2, R3 and R4, which may be the same or different, each represent a hydrogen or halogen atom or a nitro group; a cyano group; a hydroxy group; an alkoxy group; an alkyl group; an unsubstituted or substituted amino group; a carboxy group; an alkoxycarbonyl group; an aryloxycarbonyl group; an unsubstituted or substituted aminocarbonyl group. Medicinal products containing the same which are useful in treating or preventing conditions treatable by an AMPA receptor modulator.
    Type: Application
    Filed: July 9, 2009
    Publication date: January 14, 2010
    Applicant: LES LABORATOIRES SERVIER
    Inventors: Pierre FRANCOTTE, Pascal De Tullio, Bernard Pirotte, Laurence Danober, Pierre Lestage, Daniel-Henri Caignard
  • Patent number: 7642253
    Abstract: Compounds, pharmaceutical compositions, kits and methods useful for inhibiting HDAC, thereby treating a disease state for which HDAC possess activity that contributes to the pathology and/or symptomology of the disease state. The compound is selected from the group consisting of: wherein the variables are as defined herein.
    Type: Grant
    Filed: May 10, 2006
    Date of Patent: January 5, 2010
    Assignee: Takeda San Diego, Inc.
    Inventors: Jerome C. Bressi, Jason W. Brown, Anthony R. Gangloff, Jeffrey A. Stafford, Phong H. Vu
  • Publication number: 20090325941
    Abstract: The present invention relates to novel compounds that act as chemical uncouplers. Compounds of the invention are useful, inter alia, in the treatment, including prevention, of obesity, diabetes and a number of diseases or conditions associated therewith.
    Type: Application
    Filed: November 15, 2007
    Publication date: December 31, 2009
    Inventors: Anders Klarskov Petersen, Preben Houlberg Olesen, Lise Brown Christiansen, Holger Claus Hansen, Flemming Elmelund Nielsen
  • Publication number: 20090257979
    Abstract: The embodiments provide compounds of the general Formula I, 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: April 14, 2009
    Publication date: October 15, 2009
    Applicant: INTERMUNE, INC.
    Inventors: Leonid Beigelman, Guangyi Wang, Brad O. Buckman, Antitsa Dimitrova Stoycheva
  • Patent number: 7582626
    Abstract: The invention is directed to 5,6-dihydro-1H-pyridin-2-one compounds of Formula I and pharmaceutical compositions containing such compounds that are useful in treating hepatitis C virus infections: wherein Z is X is N or CR9; Y is ā€”(CR4R5)nā€”; n is 2, 3, 4, or 5; and R1 through R9 are defined herein.
    Type: Grant
    Filed: December 12, 2007
    Date of Patent: September 1, 2009
    Assignee: Anadys Pharmaceuticals, Inc.
    Inventors: Chinh V. Tran, Frank Ruebsam, Yuefen Zhou, Peter Dragovich, Alan X. Xiang
  • Patent number: 7572789
    Abstract: Provided are immediate or prolonged administration of certain salts of KATP channel openers such as diazoxide to a subject to achieve novel pharmacodynamic, pharmacokinetic, therapeutic, physiological, metabolic and compositional outcomes in the treatment of diseases or conditions involving KATP channels. Also provided are pharmaceutical formulations, methods of administration and dosing of the salts that achieve these outcomes and reduce the incidence of adverse effects in treated individuals. Further provided are method of co-administering the salts with other drugs to treat diseases of humans and animals.
    Type: Grant
    Filed: February 24, 2009
    Date of Patent: August 11, 2009
    Assignee: Essentialis, Inc.
    Inventors: Neil M. Cowen, Kenneth B. Kashkin, Khaled A. Yamout
  • Publication number: 20090148526
    Abstract: Provided are immediate or prolonged administration of certain salts of KATP channel openers such as diazoxide to a subject to achieve novel pharmacodynamic, pharmacokinetic, therapeutic, physiological, metabolic and compositional outcomes in the treatment of diseases or conditions involving KATP channels. Also provided are pharmaceutical formulations, methods of administration and dosing of the salts that achieve these outcomes and reduce the incidence of adverse effects in treated individuals. Further provided are method of co-administering the salts with other drugs to treat diseases of humans and animals.
    Type: Application
    Filed: February 24, 2009
    Publication date: June 11, 2009
    Inventors: Neil M. Cowen, Kenneth B. Kashkin, Khaled A. Yamout
  • Patent number: 7541459
    Abstract: The present invention provides a method of producing a compound represented by the following formula (1) or a compound represented by the following formula (4) or a tautomer thereof, the method including reacting a compound represented by the following formula (2) or a compound represented by the following formula (5) or a tautomer thereof with a compound represented by the following formula (3) or a compound represented by the following formula (6) in the presence of an aluminum alkoxide compound.
    Type: Grant
    Filed: September 27, 2005
    Date of Patent: June 2, 2009
    Assignee: Fujifilm Corporation
    Inventors: Keizo Kimura, Katsuyoshi Yamakawa
  • Patent number: 7524841
    Abstract: The invention provides low molecular compounds having activity which inhibits binding of CCR3 ligands to CCR3 on target cells, i.e. CCR3 antagonists. The invention also provides 4,4-(disubstituted)piperidine derivatives represented by formula (I) below, pharmaceutically acceptable acid adducts thereof, or pharmaceutically acceptable C1-C6 alkyl adducts thereof, as well as pharmaceutical compositions comprising them as effective ingredients, which are useful for treatment or prevention of diseases associated with CCR3, such as asthma and allergic rhinitis.
    Type: Grant
    Filed: April 16, 2003
    Date of Patent: April 28, 2009
    Assignee: Teijin Limited
    Inventors: Yoshiyuki Matsumoto, Minoru Imai, Yoshiyuki Sawai, Susumu Takeuchi, Akinobu Nakanishi, Kunio Minamizono, Tomonori Yokoyama
  • Patent number: 7517876
    Abstract: Compounds having the formula are hepatitis C (HCV) polymerase inhibitors. Also disclosed are compositions and methods for inhibiting hepatitis C (HCV) polymerase, processes for making the compounds, and synthetic intermediates employed in the processes.
    Type: Grant
    Filed: February 27, 2006
    Date of Patent: April 14, 2009
    Assignee: Abbott Laboratories
    Inventors: Larry L. Klein, Peggy P. Huang, John T. Randolph, Douglas K. Hutchinson, Ming C. Yeung, Charles A. Flentge
  • Patent number: 7517875
    Abstract: The invention provides low molecular compounds having activity which inhibits binding of CCR3 ligands to CCR3 on target cells, i.e. CCR3 antagonists. The invention also provides compounds represented by formula (I) below, pharmaceutically acceptable acid adducts thereof, or pharmaceutically acceptable C1-C6 alkyl adducts thereof, as well as pharmaceutical compositions comprising them as effective ingredients, which are useful for treatment or prevention of diseases associated with CCR3, such as asthma and allergic rhinitis.
    Type: Grant
    Filed: April 16, 2003
    Date of Patent: April 14, 2009
    Assignee: Teijin Limited
    Inventors: Yoshiyuki Matsumoto, Minoru Imai, Yoshiyuki Sawai, Susumu Takeuchi, Akinobu Nakanishi, Kunio Minamizono, Tomonori Yokoyama
  • Patent number: 7498325
    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: Grant
    Filed: April 29, 2004
    Date of Patent: March 3, 2009
    Assignee: Karl Thomas GmbH
    Inventors: Klaus Rudolf, Wolfgang Eberlein, Wolfhard Engel, Helmut Pieper, Henri Doods, Gerhard Hallermayer, Michael Entzeroth, Wolfgang Wienen
  • Patent number: 7462611
    Abstract: The invention is directed to pyrro[1,2-b]pyridazinone compounds of Formula I and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus: wherein R4 is selected from Ring A is 5 or 6- membered aryl or heterocyclyl, and the remaining substituents are defined herein.
    Type: Grant
    Filed: June 21, 2007
    Date of Patent: December 9, 2008
    Assignee: Anadys Pharmaceuticals, Inc.
    Inventors: Frank Ruebsam, Martin Tran, Stephen E. Webber, Peter Dragovich, Liansheng Li, Douglas Murphy, David Kucera, Zhongxiang Sun, Chinh Viet Tran