Patents Represented by Attorney Genomics Institute of the Novartis Research Foundation
  • Patent number: 7678792
    Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit, PDGFR?, PDGFR?, CSF1R, Abl, BCR-Abl, CSK, JNK1, JNK2, p38, p70S6K, TGF?, SRC, EGFR, trkB, FGFR3, FLT3, Fes, Lck, Syk, RAF, MKK4, MKK6, SAPK2?, BRK, KDR, c-raf or b-raf kinase, or mutant forms thereof.
    Type: Grant
    Filed: October 16, 2007
    Date of Patent: March 16, 2010
    Assignee: IRM LLC
    Inventors: Donatella Chianelli, Christopher Cow, Yun He, Songchun Jiang, Xiaolin Li, Xiaodong Liu, Zuosheng Liu, Jon Loren, Valentina Molteni, Juliet Nabakka, Pingda Ren, Taebo Sim, Xiaodong Wang, Shuli You
  • Patent number: 7642255
    Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, BCR-Abl, Bmx, c-Raf, Csk, Fes, FGFR, Flt3, Ikk, IR, JNK, Lck, Mkk, PKC, PKD, Rsk, SAPK, Syk, Trk, BTK, Src, EGFR, IGF, Mek, Ros and Tie2 kinases.
    Type: Grant
    Filed: April 8, 2008
    Date of Patent: January 5, 2010
    Assignee: IRM LLC
    Inventors: Taebo Sim, Hyun Soo Lee, Pingda Ren, Qiang Ding, Yi Liu, Bing Li, Lintong Li, Xia Wang, Tetsuo Uno, Guobao Zhang, Nathanael Schiander Gray, Shuli You
  • Patent number: 7638523
    Abstract: Described herein are compounds that include a diarylamine structural feature. Also described herein are methods for making such compounds, methods for using such compounds to modulate the activity of c-kit receptors, and pharmaceutical compositions and medicaments comprising such compounds. Also described herein are methods of using such compounds, pharmaceutical compositions and medicaments to treat and/or prevent and/or inhibit and/or ameliorate the pathology and/or symptomology diseases or conditions associated with the activity of c-kit receptors.
    Type: Grant
    Filed: October 31, 2007
    Date of Patent: December 29, 2009
    Assignees: IRM LLC, Novartis AG
    Inventors: Valentina Molteni, Shuli You, Juliet Nabakka, Yi Liu, Xiaolin Li, Donatella Chianelli, Jon Loren, Xiaodong Liu, Shifeng Pan, Donald S. Karanewsky, Pascal Furet, Vito Guagnano
  • Patent number: 7638601
    Abstract: This invention provides novel genes and polypeptides of the transient receptor potential channel family, and use of these genes and polypeptides for the treatment of pain and identification of agents useful in the treatment of pain.
    Type: Grant
    Filed: March 21, 2006
    Date of Patent: December 29, 2009
    Assignees: IRM LLC, Novartis AG
    Inventors: Stuart Bevan, Pamposh Ganju, Peter McIntyre, Ardem Patapoutian, Andrea Peier, Chuanzheng Song
  • Patent number: 7604977
    Abstract: This invention provides novel methods for identifying agents that inhibit HIV infection. The anti-HIV agents are identified by screening test compounds for ability to modulate a biological activity of isopeptidase T (IsoT), e.g., its isopeptidase activity or its binding to another molecule such as viral protein R (Vpr). Such IsoT modulators can be further examined for their activity in inhibiting an activity indicative of HIV infection or HIV replication. These novel anti-HIV agents are useful in the prevention or treatment of HIV infection and conditions associated with or caused by HIV infection.
    Type: Grant
    Filed: April 21, 2006
    Date of Patent: October 20, 2009
    Assignee: IRM LLC
    Inventors: Kelli L. Kuhen, Jeremy S. Caldwell
  • Patent number: 7601742
    Abstract: The present invention relates to inhibition of viruses, e.g., HIV using pyrrolidones and compounds related to pyrrolidones. The invention further relates to methods for identifying and using agents, including small molecule chemical compositions that inhibit HIV in a cell; as well as to methods of prophylaxis, and therapy related to HIV infection and related disease states such as AIDS.
    Type: Grant
    Filed: April 22, 2008
    Date of Patent: October 13, 2009
    Assignee: IRM LLC
    Inventors: Baogen Wu, Yun He, Truc Ngoc Nguyen, Kelli L. Kuhen, David Archer Ellis, Tao Jiang, Xiaohui He, Kunyong Yang, Badry Bursulaya
  • Patent number: 7595148
    Abstract: This invention provides novel methods and compositions for modulating T cell differentiation and T cell responses. The modulators are identified by screening test compounds for ability to modulate an inositol 1,4,5-trisphosphate 3-kinase (IP3K). The IP3K modulators can be further examined for their activity in modulating development of progenitor T cells (e.g., CD4+/CD8+ double positive T cells) into mature CD4+ or CD8+ single positive T cells. Pharmaceutical compositions comprising these T cell modulators can be administered to a subject to modulate T cell immune responses, to suppress inflammations, and to treat disease conditions such as autoimmune diseases, graft rejection or allergies.
    Type: Grant
    Filed: January 23, 2004
    Date of Patent: September 29, 2009
    Assignee: IRM LLC
    Inventors: Michael P. Cooke, Karsten Sauer, Tim Wiltshire, Lisa Tarantino, Colin Fletcher, Ben Wen
  • Patent number: 7592349
    Abstract: Described herein are compounds that include a diarylamine structural feature. Also described herein are methods for making such compounds, methods for using such compounds to modulate the activity of c-kit receptors, and pharmaceutical compositions and medicaments comprising such compounds. Also described herein are methods of using such compounds, pharmaceutical compositions and medicaments to treat and/or prevent and/or inhibit and/or ameliorate the pathology and/or symptomology diseases or conditions associated with the activity of c-kit receptors.
    Type: Grant
    Filed: October 31, 2007
    Date of Patent: September 22, 2009
    Assignees: IRM LLC, Novartis AG
    Inventors: Valentina Molteni, Shuli You, Juliet Nabakka, Yi Liu, Xiaolin Li, Donatella Chianelli, Jon Loren, Xiaodong Liu, Shifeng Pan, Donald S. Karanewsky, Pascal Furet, Vito Guagnano
  • Patent number: 7589101
    Abstract: The invention provides a novel class of compounds of formula I, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the AbI, Bcr-AbI, Aurora-A, SGK, Tie-2, Trk-B, FGFR3, c-kit, b-RAF, c-RAF, DYRK2, Fms, Fyn and PDGFRalpha and PDGFR&bgr; kinases.
    Type: Grant
    Filed: August 15, 2006
    Date of Patent: September 15, 2009
    Assignees: IRM LLC, The Scripps Research Institute
    Inventors: Barun Okram, Pingda Ren, Nathanael S. Gray
  • Patent number: 7578206
    Abstract: A method and system to deposit rapidly, accurately and efficiently liquid droplets onto a sample plate. A liquid from which the droplet is formed contains sample molecules, matrix molecules or a mixture of both sample and matrix molecules. A sample plate is positioned with respect to a position below a portion of the liquid, such as a droplet. A power supply forms an electric field between the sample plate and the liquid, which pulls the droplet to a target location on the sample plate. A plurality of capillary columns is provided for simultaneous or successive multiple depositions via application of one or more high voltage pulses between the liquid sample array and a sample plate.
    Type: Grant
    Filed: June 20, 2005
    Date of Patent: August 25, 2009
    Assignee: IRM LLC
    Inventors: Ansgar Brock, Christopher M. Shaw, Robert C Downs
  • Patent number: 7579363
    Abstract: This invention is directed to novel bicyclic compounds, to the uses of these compounds in various medicinal applications, including treating disorders amenable to treatment by peptidyl deformylase inhibitors such as treatment of bacterial infections, and to pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: June 27, 2007
    Date of Patent: August 25, 2009
    Assignee: IRM LLC
    Inventors: Valentina Molteni, Xiaohui He, Yun He, Andreas Kreusch, Juliet Nabakka, Kunyong Yang
  • Patent number: 7572811
    Abstract: The present invention relates to immunosuppressant, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction.
    Type: Grant
    Filed: February 24, 2005
    Date of Patent: August 11, 2009
    Assignee: IRM LLC
    Inventors: Shifeng Pan, Thomas Marsilje, Wenshuo Lu, Wenqi Gao, Nathanael Schiander Gray, Yun He, Yahua Liu, Yuan Mi, Yongping Xie
  • Patent number: 7569593
    Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, BCR-Abl, PDGF-R, lck, SAPK2?, p38, TGF?, KDR, c-Kit, b-RAF, c-RAF, FLT1 and FLT4 kinases.
    Type: Grant
    Filed: October 1, 2004
    Date of Patent: August 4, 2009
    Assignee: IRM LLC
    Inventors: Nathanael Schiander Gray, Jiqing Jiang, Yi Liu, Ruo Steensma
  • Patent number: 7563894
    Abstract: Described herein are compounds that include a diarylamine structural feature. Also described herein are methods for making such compounds, methods for using such compounds to modulate the activity of c-kit receptors, and pharmaceutical compositions and medicaments comprising such compounds. Also described herein are methods of using such compounds, pharmaceutical compositions and medicaments to treat and/or prevent and/or inhibit and/or ameliorate the pathology and/or symptomology diseases or conditions associated with the activity of c-kit receptors.
    Type: Grant
    Filed: October 31, 2007
    Date of Patent: July 21, 2009
    Assignees: IRM LLC, Novartis AG
    Inventors: Valentina Molteni, Shuli You, Juliet Nabakka, Yi Liu, Xiaolin Li, Donatella Chianelli, Jon Loren, Xiaodong Liu, Shifeng Pan, Donald S. Karanewsky, Pascal Furet, Vito Guagnano
  • Patent number: 7514447
    Abstract: Described herein are compounds that include a diarylamine structural feature. Also described herein are methods for making such compounds, methods for using such compounds to modulate the activity of c-kit receptors, and pharmaceutical compositions and medicaments comprising such compounds. Also described herein are methods of using such compounds, pharmaceutical compositions and medicaments to treat and/or prevent and/or inhibit and/or ameliorate the pathology and/or symptomology diseases or conditions associated with the activity of c-kit receptors.
    Type: Grant
    Filed: September 26, 2006
    Date of Patent: April 7, 2009
    Assignees: IRM LLC, Novartis AG
    Inventors: Valentina Molteni, Xiaolin Li, Donatella Chianelli, Jon Loren, Juliet Nabakka, Xiadong Liu, Shifeng Pan, Yi Liu, Donald S. Karanewsky, Pascal Furet, Vito Guagnano, Shuli You
  • Patent number: 7507755
    Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.
    Type: Grant
    Filed: July 13, 2007
    Date of Patent: March 24, 2009
    Assignee: IRM LLC
    Inventors: Hong Liu, Phillip B. Alper, Donald S. Karanewsky
  • Patent number: 7501408
    Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S. More particularly, the present invention provides compounds having Formula (I): wherein Q is thiomorpholinyl; and A, R5, R6, R7, R8, R9 and Ar are substituents.
    Type: Grant
    Filed: October 31, 2007
    Date of Patent: March 10, 2009
    Assignee: IRM LLC
    Inventors: Hong Liu, Arnab Chatterjee, David C. Tully, Phillip Alper, Badry Bursulaya, Jianhua Guo, David H. Woodmansee, Daniel Mutnick, Donald S. Karanewsky, Yun He
  • Patent number: 7495016
    Abstract: The present invention relates to inhibition of viruses, e.g., HIV using pyrrolidones and compounds related to pyrrolidones. The invention further relates to methods for identifying and using agents, including small molecule chemical compositions that inhibit HIV in a cell; as well as to methods of prophylaxis, and therapy related to HIV infection and related disease states such as AIDS.
    Type: Grant
    Filed: October 21, 2003
    Date of Patent: February 24, 2009
    Assignee: IRM LLC
    Inventors: Baogen Wu, Yun He, Truc Ngoc Nguyen, Kelli L. Kuhen, David Archer Ellis, Tao Jiang, Xiaohui He, Kunyong Yang, Badry Bursulaya
  • Patent number: 7462629
    Abstract: The present invention relates to immunosuppressant, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction.
    Type: Grant
    Filed: May 19, 2004
    Date of Patent: December 9, 2008
    Assignee: IRM LLC
    Inventors: Shifeng Pan, Nathanael S. Gray, Yuan Mi, Yi Fan, Wenqi Gao
  • Patent number: 7449582
    Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, BCR-Abl, CSK, JNK1, JNK2, PDGF-R, p38, p70S6K, TGF?, SRC, EGFR, c-Kit, trkB, FGFR3, Fes, Lck, Syk, RAF, MKK4, MKK6 and SAPK2? kinases.
    Type: Grant
    Filed: October 8, 2004
    Date of Patent: November 11, 2008
    Assignee: IRM LLC
    Inventors: Qiang Ding, Yongping Xie, Nathanael S. Gray, Shuli You, Greg Chopiuk, Jiqing Jiang, Yi Liu, Ruo Steensma, Xing Wang, Taebo Sim