Patents Assigned to IRM LLC
  • FLAVIVIRUS PROTEASE SUBSTRATES AND INHIBITORS
    Publication number: 20080032917
    Abstract: The invention provides substrate specificity profiles for flaviviral proteases (e.g., dengue proteases or West Nile protease). Optimal flaviviral protease substrate sequences, both to the prime side and non-prime side of the flaviviral protease recognition site, are disclosed herein. The flaviviral protease substrate sequences are used in designing substrates, inhibitors, and prodrugs. Flaviviral protease inhibitors based on substrate specificity are also provided.
    Type: Application
    Filed: January 2, 2007
    Publication date: February 7, 2008
    Applicant: IRM LLC, A DELAWARE LIMITED LIABILITY COMPANY
    Inventors: Jun Li, Jennifer Harris, Christine Tumanut
  • Inhibitors of cathepsin S
    Patent number: 7314872
    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 morpholinyl; and A, R5, R6, R7, R8, R9 and Ar are substituents.
    Type: Grant
    Filed: August 18, 2004
    Date of Patent: January 1, 2008
    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
  • Compounds and Compositions as Lxr Modulators
    Publication number: 20070293547
    Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of liver X receptors (LXRs).
    Type: Application
    Filed: February 11, 2005
    Publication date: December 20, 2007
    Applicant: IRM LLC
    Inventors: Valentina Molteni, Xiaolin Li, Fang Liang, Juliet Nabakka, Enrique Saez, John Wityak
  • Inhibitors of cathepsin S
    Patent number: 7307095
    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: January 5, 2007
    Date of Patent: December 11, 2007
    Assignee: IRM LLC
    Inventors: Hong Liu, David Tully, Phillip Alper, Robert Epple, Arnab Chatterjee, Michael Roberts
  • Compounds and Compositions as Channel Activating Protease Inhibitors
    Publication number: 20070276002
    Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating channel activating proteases, and methods for using such compounds to treat, ameliorate or prevent a condition associated with a channel activating protease, including but not limited to prostasin, PRSS22, TMPRSS11 (e.g., TMPRSS11B, TMPRSS11E), TMPRSS2, TMPRSS3, TMPRSS4 (MTSP-2), matriptase (MTSP-1), CAP2, CAP3, trypsin, cathepsin A, or neutrophil elastase.
    Type: Application
    Filed: May 15, 2007
    Publication date: November 29, 2007
    Applicant: IRM LLC
    Inventors: David Tully, Arnab Chatterjee, Hank Michael Petrassi, Badry Bursulaya, Glen Spraggon
  • Compounds and Compositions as Channel Activating Protease Inhibitors
    Publication number: 20070275906
    Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating channel activating proteases, and methods for, using such compounds to treat, ameliorate or prevent a condition associated with a channel activating protease, including but not limited to prostasin, PRSS22, TMPRSS11 (e.g., TMPRSS11B, TMPRSS11E), TMPRSS2, TMPRSS3, TMPRSS4 (MTSP-2), matriptase (MTSP-1), CAP2, CAP3, trypsin, cathepsin A, or neutrophil elastase.
    Type: Application
    Filed: May 16, 2007
    Publication date: November 29, 2007
    Applicant: IRM LLC
    Inventors: David Tully, Arnab Chatterjee, Agnes Vidal, Hank Petrassi, Zhiwei Wang, Badry Bursulaya, Glen Spraggon
  • Inhibitors of cathepsin S
    Patent number: 7297714
    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: October 20, 2004
    Date of Patent: November 20, 2007
    Assignee: IRM LLC
    Inventors: Hong Liu, Phillip Alper, Daniel Mutnick, Donald Karanewsky
  • INHIBITORS OF CATHEPSIN S
    Publication number: 20070259873
    Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.
    Type: Application
    Filed: July 13, 2007
    Publication date: November 8, 2007
    Applicant: IRM LLC
    Inventors: Hong Liu, Phillip Alper, Donald Karanewsky
  • Compounds and Compositions as Ppar Modulators
    Publication number: 20070244130
    Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of the Peroxisome Proliferator-Activated Receptor (PPAR) families, particularly the activity of PPAR.
    Type: Application
    Filed: May 24, 2005
    Publication date: October 18, 2007
    Applicant: IRM LLC
    Inventors: Robert Epple, Yongping Xie, Xing Wang, Christopher Cow, Ross Russo
  • METHODS OF SCREENING FOR ANTITUMOR AGENTS
    Publication number: 20070226813
    Abstract: This invention provides cellular regulators of antitumor agent apratoxin A. The invention also provides methods for identifying novel antitumor compounds using these cellular regulators of apratoxin A. The methods comprise first screening test agents for modulators of a cellular regulator of apratoxin A and then further screening the identified modulating agents for antitumor activities. The invention further provides methods and pharmaceutical compositions for treating tumors in a subject.
    Type: Application
    Filed: January 30, 2007
    Publication date: September 27, 2007
    Applicants: IRM LLC, THE SCRIPPS RESEARCH INSTITUTE
    Inventors: Hendrik Luesch, Sumit Chanda
  • Compounds and Compositions as Protein Kinase Inhibitors
    Publication number: 20070225306
    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 FAK, Abl, BCR-Abl, PDGF-R, c-Kit, NPM-ALK, Flt-3, JAK2 and c-Met kinases.
    Type: Application
    Filed: February 14, 2005
    Publication date: September 27, 2007
    Applicant: IRM LLC
    Inventors: Ha-Soon Choi, Zhicheng Wang, Nathanael Gay, Xiang-Ju Gu, Xiaohui He, Yun He, Toa Jiang, Yi Liu, Windy Richmond, Taebo Sim, Kunyong Yang
  • Flap Endonuclease (Fen1) Regulatory Sequences And Uses Thereof
    Publication number: 20070212675
    Abstract: FEN1 transcriptional regulatory sequences (TREs) are provided. FEN1 TREs provide for transcriptional regulation dependent upon transcription factors that are only active in cancer cells. The FEN1 TREs may be used as a vehicle for introducing new genetic capability, particularly associated with cytotoxicity, for selective expression in cancer cells.
    Type: Application
    Filed: April 15, 2004
    Publication date: September 13, 2007
    Applicants: NOVARTIS AG, IRM LLC
    Inventors: Paul Hallenbeck, Garret Hampton, Carl Hay, Ying Huang, John Jakubczak, Sandrina Phipps
  • Compounds And Compositions As Ppar Modulators
    Publication number: 20070203155
    Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of the Peroxisome Proliferator-Activated Receptor (PPAR) families, particularly the activity of PPAR.
    Type: Application
    Filed: May 24, 2005
    Publication date: August 30, 2007
    Applicant: IRM LLC
    Inventors: Robert Epple, Christopher Cow, Yongping Xie, Xing Wang, Ross Russo, Mihai Azimioara, Enrique Saez
  • Immunosuppressant Compounds and Compositions
    Publication number: 20070203100
    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: Application
    Filed: February 24, 2005
    Publication date: August 30, 2007
    Applicant: IRM LLC
    Inventors: Shifeng Pan, Thomas Marsilje, Wenshuo Lu, Gao Wenqi, Nathanael Gray, Yun He, Yahua Liu, Yuan Mi, Yongping Xie
  • Modulators of ion channel trpa1
    Publication number: 20070196866
    Abstract: This invention provides methods for modulating activities of noxious ion channel TRPAI and methods for screening for novel modulators of TRPAI. Compounds such as bradykinin, eugenol, gingerol, methyl salicylate, allicin, and cinnamaldehyde can be employed to activate cold themosensor TRPAI. These TRPAI agonists can be used in screenings methods to activate TRPA1 and therefore identify novel TRPAI antagonists that can inhibit the activated TRPAI. These TRPAI agonists also provide chemical backbones to synthesize and identify analogs with improved biological or pharmaceutical properties. Further, novel TRPAI modulators can be identified by screening test agents for ability in modulating enzymatic activity or cellular level of phospholipase C.
    Type: Application
    Filed: March 11, 2005
    Publication date: August 23, 2007
    Applicants: IRM LLC, The Scripps Research Institute
    Inventors: Ardem Patapoutian, Michael Bandell, Gina Story
  • KINASE INHIBITOR SCAFFOLDS AND METHODS FOR THEIR PREPARATION
    Publication number: 20070191380
    Abstract: General methods for the solution phase as well as solid phase synthesis of various substituted heteroaryls has been demonstrated. These substituted heteroaryls can be further elaborated by aromatic substitution with amines at elevated temperature or by anilines, boronic acids and phenols via palladium catalyzed cross-coupling reactions.
    Type: Application
    Filed: February 12, 2007
    Publication date: August 16, 2007
    Applicant: IRM LLC
    Inventors: Sheng Ding, Qiang Ding, Nathanael Gray
  • Bicyclic compounds and compositions
    Patent number: 7256206
    Abstract: The present invention relates to bicyclic derivatives, 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/S1P receptor mediated signal transduction.
    Type: Grant
    Filed: February 11, 2004
    Date of Patent: August 14, 2007
    Assignee: IRM LLC
    Inventors: Shifeng Pan, Nathanael S. Gray, Yuan Mi, Wenqi Gao, Yi Fan, Sophie Lefebvre
  • Inhibitors of cathepsin S
    Patent number: 7256207
    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: August 18, 2004
    Date of Patent: August 14, 2007
    Assignee: IRM LLC
    Inventors: Hong Liu, Phillip B. Alper, Donald S. Karanewsky
  • Bicyclic compounds and compositions as PDF inhibitors
    Patent number: 7253164
    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: July 30, 2004
    Date of Patent: August 7, 2007
    Assignee: IRM LLC
    Inventors: Valentina Molteni, Xiaohui He, Yun He, Andreas Kreusch, Juliet Nabakka, Kunyong Yang
  • 6-phenyl-7H-pyrrolo[2,3-d]pyrimidine compounds that induce neuronal differentiation in embryonic stem cells
    Patent number: 7253166
    Abstract: The invention provides a novel class of compounds and compositions of Formula I: in which R1, R2 and R3 are defined herein, that are useful in the treatment or prevention of diseases or disorders associated with kinases, particularly GSK-3?, c-Abl, HER-1, HER-2, KDR, Flt-3, c-Raf-1, PDGFR-?, c-Kit, Flt-4, Flt-1, Tek, c-src, CDK1, PDK1, FGFR-1, FGFR-2, Fer, MAP3K13, EPHA7 and c-Met kinases. The invention further relates to the use of the compounds of the invention as potent inducers of neurogenesis in embryonic stem cells.
    Type: Grant
    Filed: April 22, 2004
    Date of Patent: August 7, 2007
    Assignees: IRM LLC, The Scripps Research Institute
    Inventors: Sheng Ding, Tom Wu, Nathanael S. Gray, Peter Schultz