Quinolizines (including Hydrogenated) Patents (Class 514/306)
  • Patent number: 11219616
    Abstract: Methods of treating a dengue virus (DENV) infection in a human subject, comprising administering to the human subject a compound of Formula (I), or pharmaceutical composition comprising a compound of Formula (I): A compound of Formula (I) can be administered within onset of fever to 72 hours of fever onset due to dengue infection and then every 6 to 12 hours until there is an improvement in the infection or between from about 1 day to about 10 days. The methods of the invention can be used to treat primary and secondary DENV1-4 viral infections.
    Type: Grant
    Filed: December 23, 2019
    Date of Patent: January 11, 2022
    Assignees: 60 Degrees Pharmaceuticals, LLC, National University of Singapore, Singapore Health Services PTE Ltd.
    Inventors: Geoffrey S. Dow, Subhash Vasudevan, Mark Reid, Glynn Morrish, Cynthia Sung, Abhay Rathore, Satoru Watanabe, Eng Eong Ooi, Jenny Low
  • Patent number: 11000516
    Abstract: Methods of preventing a disease resulting from a dengue virus (DENV) infection in a human subject, comprising administering to the human subject a compound of Formula (I), or pharmaceutical composition comprising a compound of Formula (I); a compound of Formula (I) can be first administered to an asymptomatic human subject followed by subsequent doses administered at least once daily. The methods of the invention can be used to prevent a disease resulting from primary and secondary DENV 1-4 viral infections.
    Type: Grant
    Filed: December 9, 2016
    Date of Patent: May 11, 2021
    Assignees: 60 Degrees Pharmaceuticals, LLC, National University of Singapore, Singapore Health Services PTE Ltd.
    Inventors: Subhash Vasudevan, Geoffrey S. Dow, Satoru Watanabe, Eng Eong Ooi, Jenny Low, Kitti Wing Ki Chan
  • Patent number: 10407408
    Abstract: Provided is a novel low-molecular-weight compound that suppresses production of induction type MMPs, particularly MMP-9, rather than production of hemostatic type MMP-2. The present invention relates to a compound represented by the following formula (I): wherein each symbol is as described in the DESCRIPTION. The compound has a selective MMP-9 production suppressive action, and is useful as a drug for the prophylaxis and/or treatment of autoimmune diseases such as rheumatoid arthritis and the like, inflammatory bowel diseases (ulcerative colitis, Crohn's disease) or osteoarthritis.
    Type: Grant
    Filed: July 8, 2016
    Date of Patent: September 10, 2019
    Assignee: MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Seigo Ishibuchi, Kunio Saruta, Maiko Hamada, Nobuatsu Matoba, Tetsuji Matsudaira, Maki Seki, Akiko Tarao, Takashi Honjo, Shingo Ogata, Atsushi Kawata, Kenji Morokuma, Naoto Fujie, Yukio Aoyama
  • Patent number: 10328061
    Abstract: The present invention concerns the use of castanospermine or other alpha-glucosidase inhibitors for the treatment or prevention of Zika virus infections. Aspects of the invention include methods for treating or preventing Zika virus infection by administering an alpha-glucosidase inhibitor (e.g., an alpha-glucosidase I inhibitor) to a subject in need thereof; methods for inhibiting a Zika virus infection in a cell in vitro or in vivo; pharmaceutical compositions; packaged dosage formulations; and kits for treating or preventing Zika virus infection.
    Type: Grant
    Filed: May 2, 2017
    Date of Patent: June 25, 2019
    Assignee: FLORIDA STATE UNIVERSITY RESEARCH FOUNDATION, INC.
    Inventors: Eric Holmes, Gary Ostrander
  • Patent number: 10046005
    Abstract: A composition and associated method for treating a hepatitis C virus (HCV) infection in a subject who is human being. The composition includes: an anti-viral agent and/or a protease inhibitor; a polymerase inhibitor; one or more viral entry inhibitors; and one or more anti-fibrotic agents and/or anti-hemolytic agents including one or more Polyphenols and/or one or more Thiols. The composition may also include one or more sulfated oligosaccharide or non-anticoagulant glycosaminoglycans (GAGs). The method administers, to the subject, a therapeutic dose of the composition to treat the subject for the HCV infection.
    Type: Grant
    Filed: August 11, 2016
    Date of Patent: August 14, 2018
    Inventor: Shaker A. Mousa
  • Patent number: 9199939
    Abstract: The present invention is directed to quinoline amide compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Grant
    Filed: December 13, 2010
    Date of Patent: December 1, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Kelly-Ann S. Schlegel, Zhi-Qiang Yang
  • Publication number: 20150141435
    Abstract: Disclosed herein are compounds of Formula I wherein R1, R2, X, and Y are defined herein. These compounds are type II topoisomerase inhibitors and can be used in methods for treating infections caused by gram-positive pathogens, gram-negative pathogens, and drug-resistant strains thereof.
    Type: Application
    Filed: January 7, 2015
    Publication date: May 21, 2015
    Inventors: Patrick ROUSSEL, Jutta HEIM, Peter SCHNEIDER, Christian BARTELS, Yaoquan LIU, Glen DALE, Daniel MILLIGAN
  • Patent number: 8962842
    Abstract: Described are a series of 2-pyridone compounds as a potent and selective new class of type II topoisomerase inhibitors with broad-spectrum antimicrobial activity having the general formula (I); where R1, R2, X, and Y are defined herein Such compounds can be used in methods for treating an infection caused by a gram-positive pathogen, a gram-negative pathogen, or a drug-resistant strains thereof.
    Type: Grant
    Filed: September 16, 2011
    Date of Patent: February 24, 2015
    Assignee: Evolva SA
    Inventors: Patrick Roussel, Jutta Heim, Peter Schneider, Christian Bartels, Yaoquan Liu, Glen Dale, Daniel Milligan
  • Patent number: 8946446
    Abstract: The invention provides modulators for the orphan nuclear receptor RORy and methods for treating RORy mediated diseases by administrating these novel RORy modulators to a human or a mammal in need thereof. Specifically, the present invention provides pyrrolo sulfonamide compounds of Formula (1) and the enantiomers, diastereomers, tautomers, solvates and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: April 13, 2012
    Date of Patent: February 3, 2015
    Assignee: Phenex Pharmaceuticals AG
    Inventors: Christoph Steeneck, Olaf Kinzel, Christian Gege, Gerald Kleymann, Thomas Hoffmann
  • Patent number: 8835461
    Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.
    Type: Grant
    Filed: March 23, 2010
    Date of Patent: September 16, 2014
    Assignee: Shionogi & Co., Ltd.
    Inventors: Toshio Fujishita, Minako Mikamiyama, Makoto Kawai, Toshiyuki Akiyama
  • Patent number: 8796256
    Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalac
    Type: Grant
    Filed: May 24, 2011
    Date of Patent: August 5, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Gilles Bignan, Wing Cheung, Micheal Gaul, Hui Huang, Xun Li, Raymond Patch, Sharmila Patel, Mark Player, Guozhang Xu, Bao-Ping Zhao, Jian Liu
  • Publication number: 20140094450
    Abstract: The present invention relates to benzoimidazole-carboxylic acid amide compounds of the formula I, in which R?, R?, R??, R1, R2, R3, R4, R5, R6 and Z are defined as indicated below. The compounds of the formula I are APJ receptor modulators, and are useful for the treatment of diseases associated with increased blood pressure for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Application
    Filed: September 19, 2013
    Publication date: April 3, 2014
    Applicant: SANOFI
    Inventors: Stephanie HACHTEL, Paulus WOHLFART, John WESTON, Marco MUELLER, Elisabeth DEFOSSA, Katharina MERTSCH, Jian-Hui WENG, Robert Alan BINNIE, Farid ABDUL-LATIF, William Jerome BOCK, Armin WALSER
  • Patent number: 8623891
    Abstract: Disclosed herein are methods of treating a patient suffering from a cognitive disorder using compounds of Formulas (1) and (2) wherein the variables have the meaning disclosed in the specification.
    Type: Grant
    Filed: March 4, 2008
    Date of Patent: January 7, 2014
    Assignee: Allergan, Inc.
    Inventors: John E. Donello, Fabien J. Schweighoffer, Lauren M. Luhrs
  • Publication number: 20130310357
    Abstract: Provided herein are azolyl urea compounds for treatment of CSF-1R kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
    Type: Application
    Filed: May 26, 2011
    Publication date: November 21, 2013
    Applicant: AMBIT BIOSCIENCES CORPORATION
    Inventor: Gang Liu
  • Patent number: 8586570
    Abstract: Peptidyl sensors comprise a metal-binding peptide and one or two kinase recognition sequences with a hydroxyamino acid that can be phosphorylated in the presence of a kinase.
    Type: Grant
    Filed: April 27, 2011
    Date of Patent: November 19, 2013
    Assignee: Massachusetts Institute of Technology
    Inventors: Barbara Imperiali, Elvedin Lukovic, Dora Carrico-Moniz
  • Publication number: 20130296228
    Abstract: Novel compositions and methods of reducing microbial resistance to antimicrobial agents and treating infections are disclosed. In particular, compositions and methods of inhibiting efflux pump activity, treating infection and methods of enhancing antimicrobial activity of antimicrobial agents are provided.
    Type: Application
    Filed: April 22, 2013
    Publication date: November 7, 2013
    Inventors: Mahesh Vithalbhai PATEL, Sachin Subhash Bhagwat, Mohammad Alam Jafri
  • Patent number: 8546425
    Abstract: Conjugates of antifolates, releasable linkers, and drugs, and pharmaceutical compositions containing them are described. The conjugates are useful for treating diseases arising from pathogenic cell populations. Methods for treating such diseases are also described.
    Type: Grant
    Filed: September 17, 2009
    Date of Patent: October 1, 2013
    Assignees: Purdue Research Foundation, Endocyte, Inc.
    Inventors: Christopher Paul Leamon, Iontcho Radoslavov Vlahov, Philip Stewart Low
  • Publication number: 20130245035
    Abstract: Described are a series of 2-pyridone compounds as a potent and selective new class of type II topoisomerase inhibitors with broad-spectrum antimicrobial activity having the general formula (I); where R1, R2, X, and Y are defined herein Such compounds can be used in methods for treating an infection caused by a gram-positive pathogen, a gram-negative pathogen, or a drug-resistant strains thereof.
    Type: Application
    Filed: September 16, 2011
    Publication date: September 19, 2013
    Applicant: EVOLVA SA
    Inventors: Patrick Roussel, Jutta Heim, Peter Schneider, Christian Bartels, Yaoquan Liu, Glen Dale, Daniel Milligan
  • Publication number: 20130172335
    Abstract: The present invention relates to compounds of formula I wherein R1a to R1e, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.
    Type: Application
    Filed: February 22, 2013
    Publication date: July 4, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • Patent number: 8450313
    Abstract: The present invention relates to compounds of formula I wherein R1a to R1e, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.
    Type: Grant
    Filed: May 22, 2012
    Date of Patent: May 28, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
  • Patent number: 8399480
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.
    Type: Grant
    Filed: April 2, 2009
    Date of Patent: March 19, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Sookhee Nicole Ha, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Dong-Ming Shen, Liping Wang, Cheng Zhu
  • Patent number: 8389720
    Abstract: The present invention is directed to quinolone compounds which are antagonists of neuropeptide S receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which the neuropeptide S receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the neuropeptide S receptor is involved.
    Type: Grant
    Filed: November 3, 2009
    Date of Patent: March 5, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: James C. Barrow, Mark T. Bilodeau, Christopher D. Cox, John C. Hartnett, Nathan R. Kett, Yiwei Li, Peter J. Manley, Jeffrey Melamed, William D. Shipe, B. Wesley Trotter, Amy Zartman
  • Patent number: 8357692
    Abstract: Methods of reducing bone loss and treating degenerative bone diseases such as osteoporosis are disclosed. The methods comprise administration of an agent that inhibits signaling through the IL-17 pathway, such as an antibody or a quinazolinone analogue such as halofuginone.
    Type: Grant
    Filed: June 17, 2011
    Date of Patent: January 22, 2013
    Assignee: Washington University
    Inventors: Steven L. Teitelbaum, Carl J. DeSelm
  • Patent number: 8357686
    Abstract: The invention relates to aryl-substituted polycyclic amines of the formula I, especially bicyclic amines, and to the physiologically tolerated salts and physiologically functional derivatives thereof; where the symbols and radicals are explained in the description as well as to pharmaceutical compositions and medical treatments employing these compounds.
    Type: Grant
    Filed: June 23, 2009
    Date of Patent: January 22, 2013
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Gerhard Hessler, Petra Lennig
  • Patent number: 8334316
    Abstract: The present invention provides substituted di-, tri-, tetra- and penta-sulfide compounds and compositions, and methods of using the same for the treatment and/or prevention of a cell proliferative disorder. The present invention also provides methods for preparing trisulfide compounds and compositions.
    Type: Grant
    Filed: February 9, 2009
    Date of Patent: December 18, 2012
    Assignee: ACEA Biosciences, Inc.
    Inventors: Xiao Xu, Haoyun An, Xiaobo Wang
  • Patent number: 8278323
    Abstract: Certain quinolizidine and octahydropyridopyrazine compounds, pharmaceutical compositions, and methods of their use, inter alia, as opioid receptor antagonists are disclosed.
    Type: Grant
    Filed: May 11, 2009
    Date of Patent: October 2, 2012
    Assignee: Adolor Corporation
    Inventors: Roland E. Dolle, Bertrand Le Bourdonnec, Allan James Goodman
  • Patent number: 8278322
    Abstract: The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.
    Type: Grant
    Filed: July 28, 2006
    Date of Patent: October 2, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: M. Katharine Holloway, Nigel J. Liverton, John A. McCauley, Michael T. Rudd, Joseph P. Vacca, Steven W. Ludmerer, David B. Olsen
  • Patent number: 8268894
    Abstract: Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted ethylene diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis.
    Type: Grant
    Filed: November 11, 2010
    Date of Patent: September 18, 2012
    Assignees: The United States of America as Represented by the Secretary, Department of Health and Human Services, Sequella, Inc.
    Inventors: Marina Nikolaevna Protopopova, Elena Bogatcheva, Leo Einck, Richard Edward Lee, Richard Allan Slayden, Clifton E. Barry, III
  • Publication number: 20120232076
    Abstract: The present invention is directed to compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Application
    Filed: November 15, 2010
    Publication date: September 13, 2012
    Inventors: Scott D. Kuduk, Ronald K. Chang
  • Publication number: 20120232071
    Abstract: The present invention relates to compounds of formula I wherein R1a to R1e, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.
    Type: Application
    Filed: May 22, 2012
    Publication date: September 13, 2012
    Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
  • Patent number: 8258135
    Abstract: The present invention is directed to spiropiperidine compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Grant
    Filed: October 15, 2008
    Date of Patent: September 4, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ronald K. Chang, Scott D. Kuduk
  • Patent number: 8247415
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.
    Type: Grant
    Filed: April 2, 2009
    Date of Patent: August 21, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Sookhee Nicole Ha, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Dong-Ming Shen, Liping Wang, Cheng Zhu
  • Patent number: 8232265
    Abstract: Disclosed are ionic liquids and methods of preparing ionic liquid compositions of active pharmaceutical, biological, nutritional, and energetic ingredients. Also disclosed are methods of using the compositions described herein to overcome polymorphism, overcome solubility and delivery problems, to control release rates, add functionality, enhance efficacy (synergy), and improve ease of use and manufacture.
    Type: Grant
    Filed: October 10, 2006
    Date of Patent: July 31, 2012
    Assignee: Board of Trustees of the University of Alabama
    Inventors: Robin D. Rogers, Daniel T. Daly, Richard P. Swatloski, Whitney L. Hough, James Hilliard Davis, Jr., Marcin Smiglak, Juliusz Pernak, Scott K. Spear
  • Patent number: 8202910
    Abstract: Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted ethylene diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis. In certain embodiments, the present invention comprises compositions comprising novel substituted ethylene diamine compounds further comprising antitubercular agents such as rifampicin, isoniazid, pyrazinamide and ethambutol.
    Type: Grant
    Filed: October 22, 2008
    Date of Patent: June 19, 2012
    Assignee: Sequella, Inc.
    Inventors: Marina Nikolaena Protopopova, Leo Einck, Boris Nikonenko, Ping Chen
  • Patent number: 8178520
    Abstract: The present invention relates to macrocyclic compounds of formula (I): wherein W, n, R1, Ra, Rb, R3, R4, M, Z, ring A and ring B are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising them, and their use for the treatment or prevention of infection by hepatitis C virus.
    Type: Grant
    Filed: May 11, 2007
    Date of Patent: May 15, 2012
    Assignee: Istituto di Ricerche di Biologia Molecolare P. Angeletti SpA
    Inventors: Maria Emilia Di Francesco, Emanuela Nizi, Paola Pace, Vincenzo Summa
  • Patent number: 8173672
    Abstract: The present invention is directed to compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Grant
    Filed: March 11, 2009
    Date of Patent: May 8, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Ronald K. Chang, Christina Ng Di Marco
  • Patent number: 8163741
    Abstract: The invention relates to therapeutic use of aryl-substituted polycyclic amines of the formula I, especially bicyclic amines, and to the physiologically tolerated salts and physiologically functional derivatives thereof; where the symbols and radicals are explained in the description.
    Type: Grant
    Filed: June 23, 2009
    Date of Patent: April 24, 2012
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Gerhard Hessler, Petra Lennig
  • Publication number: 20120095010
    Abstract: The invention is directed to delta opioid receptor modulators. More specifically, the invention relates to tricyclic ?-opioid modulators. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described.
    Type: Application
    Filed: December 22, 2011
    Publication date: April 19, 2012
    Inventors: John R. Carson, Ellen Codd, Christine M. Razler, Andrea Works, Mark McDonnell, James J. McNally
  • Patent number: 8143273
    Abstract: The present invention relates to a compound of formula I-A or I-B wherein X, R1, R2 and R3 are defined herein; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer thereof. The compounds of formulas I-A and I-B are good inhibitors of the glycine transporter 1 (GlyT-1), and have a good selectivity to glycine transporter 2 (GlyT-2) inhibitors, suitable in the treatment of neurological and neuropsychiatric disorders.
    Type: Grant
    Filed: June 16, 2011
    Date of Patent: March 27, 2012
    Assignee: Hoffman-La Roche Inc.
    Inventors: Sabine Kolczewski, Emmanuel Pinard
  • Patent number: 8119640
    Abstract: The present disclosure provides for compounds, pharmaceutical preparations, kits and methods for the inhibition of the Hh pathway and the alleviation of cancer and developmental disorders associated with the Hh pathway.
    Type: Grant
    Filed: February 12, 2009
    Date of Patent: February 21, 2012
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: James K. Chen, Joel M. Hyman, Cory A. Ocasio
  • Publication number: 20110311519
    Abstract: Methods of reducing bone loss and treating degenerative bone diseases such as osteoporosis are disclosed. The methods comprise administration of an agent that inhibits signaling through the IL-17 pathway, such as an antibody or a quinazoline analogue such as halofuginone.
    Type: Application
    Filed: June 17, 2011
    Publication date: December 22, 2011
    Applicant: Washington University
    Inventors: Steven L. Teitelbaum, Carl J. DeSelm
  • Publication number: 20110301192
    Abstract: The present invention provides compounds that inhibit cyclin kinase inhibitor p21, such as compounds of formula I. The present invention also provides compositions including compounds of Formula I and a pharmaceutically acceptable excipient. In addition, the present invention provides methods of inhibiting cyclin kinase inhibitor p21 and of treating cancer.
    Type: Application
    Filed: September 29, 2009
    Publication date: December 8, 2011
    Applicant: The regents of the University of California
    Inventors: Robert Weiss, See-Hyoung Park, Kit S. Lam, Ruiwu Liu
  • Publication number: 20110294780
    Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalac
    Type: Application
    Filed: May 24, 2011
    Publication date: December 1, 2011
    Inventors: Gilles Bignan, Wing Cheung, Micheal Gaul, Hui Huang, Xun Li, Raymond Patch, Sharmila Patel, Mark Player, Guozhang Xu, Bao-Ping Zhao, Jian Liu
  • Publication number: 20110274648
    Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of Hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Application
    Filed: November 4, 2010
    Publication date: November 10, 2011
    Inventors: Rico Lavoie, John A. Bender, Zhong Yang, Makonen Belema, Omar D. Lopez, Qi Chen, Gan Wang, Piyasena Hewawasam
  • Publication number: 20110183959
    Abstract: Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: are inhibitors of p38 and are useful in the treatment of inflammation such as in the treatment of rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, gouty arthritis and other arthritic conditions; inflamed joints, eczema, psoriasis or other inflammatory skin conditions such as sunburn; inflammatory eye conditions including conjunctivitis; pyresis, pain and other conditions associated with inflammation.
    Type: Application
    Filed: January 25, 2011
    Publication date: July 28, 2011
    Inventors: Meng-Hsin Chen, James B. Doherty, Robert Tynebor, Swaminathan R. Natarajan, Zhen Li, Soumya P. Sahoo
  • Publication number: 20110178122
    Abstract: The present invention is directed to quinolizidinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Application
    Filed: September 29, 2009
    Publication date: July 21, 2011
    Inventors: Scott D. Kuduk, Christina Ng Di Marco
  • Publication number: 20110160238
    Abstract: This invention relates to octahydroquinolizines for pharmaceutical use with the following formula: (I), X=H, F; R=Methyl, Ethyl, nPropyl, nButyl.
    Type: Application
    Filed: June 29, 2009
    Publication date: June 30, 2011
    Applicant: 55PHARMA DRUG DISCOVERY & DEVELOPMENT AG
    Inventors: Immanuel Adorjan, Leonhardt Bauer, Klaus Frobel, Clemens Fuernsinn
  • Patent number: 7915287
    Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Grant
    Filed: December 19, 2007
    Date of Patent: March 29, 2011
    Assignee: Amgen Inc.
    Inventors: Steven Bellon, Shon Booker, Noel D'Angelo, Julie Germain, Jean-Christophe Harmange, Tae-Seong Kim, Matthew Lee, Longbin Liu, Mark H. Norman, Elizabeth Rainbeau, Ning Xi, Shimin Xu
  • Patent number: 7897634
    Abstract: This invention relates to compounds of the formulas (1), (2) and (3) having pharmacological activity, to compositions containing these compounds, and to methods of treatment employing the compounds and compositions.
    Type: Grant
    Filed: January 30, 2007
    Date of Patent: March 1, 2011
    Assignee: Athersys, Inc.
    Inventors: Youssef L. Bennani, Michael G. Campbell, David Dastrup, Emile Porter Huck
  • Publication number: 20110046145
    Abstract: The present invention is directed to compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Application
    Filed: March 11, 2009
    Publication date: February 24, 2011
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Ronald K. Chang, Christina Ng Di Marco