Abstract: This invention provides methods for identifying novel SHMT modulators. The methods comprise first screening test agents for modulators of p38 activity and then further screening the identified modulating agents for modulators of SHMT enzyme activity. The invention further provides methods and pharmaceutical compositions for modulating cellular proliferation and for treating tumors using the novel SHMT modulators.
Abstract: The present invention relates to immunosuppressants, processes 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:
July 19, 2007
Applicant:
IRM LLC
Inventors:
Shifeng Pan, Wenqi Gao, Nathanael Gray, Yuan Mi
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:
Application
Filed:
September 26, 2006
Publication date:
June 28, 2007
Applicants:
IRM LLC, Novartis, AG
Inventors:
Valentina Molteni, Xiaolin Li, Donatella Chianelli, Jon Loren, Shuli You, Juliet Nabakka, Xiadong Liu, Shifeng Pan, Yi Liu, Donald Karanewsky, Pascal Furet, Vito Guagnano
Abstract: The present invention provides universal G protein-coupled receptor (GPCR) reporter constructs. The constructs comprise a serum response element, a cAMP response element, and a multiple response element. These reporter constructs are able to detect activities of all GPCRs examined. Further provided by the present invention are host cells harboring a universal GPCR reporter construct of the invention, as well as assays for detecting modulators of GPCRs using the host cells.
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:
January 5, 2007
Publication date:
May 31, 2007
Applicant:
IRM LLC
Inventors:
Hong Liu, David Tully, Phillip Alper, Robert Epple, Arnab Chatterjee, Michael Roberts
Abstract: High throughput and automated cellular disruption systems that substantially uniformly disrupt cells as part of cellular motility assays as wells as other assay types are provided. In addition, various system components, including holding blocks, holding block loading devices, and system software, are also provided. Moreover, related methods that utilize these systems and system components are additionally provided.
Type:
Application
Filed:
November 9, 2005
Publication date:
May 10, 2007
Applicants:
IRM, LLC, THE SCRIPPS RESEARCH INSTITUTE
Inventors:
Kenneth Micklash, Jiyong Hong, James Mainquist, Sheng Ding, Robert Downs, Peter Schultz
Abstract: The present invention relates to inhibition of viruses, e.g., HIV using oxindoles and compounds related to oxindoles. 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:
April 17, 2007
Assignee:
IRM LLC
Inventors:
Yun He, Tao Jiang, Kelli L. Kuhen, David Archer Ellis, Baogen Wu, Tom Yao-Hsiang Wu, Badry Bursulaya
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, EGF-R, c-erbB2 kinase (HER-2), CHK2, FGFR3, p70S6K, PKC, PDGF-R, p38, TGF?, KDR, c-Kit, b-RAF, c-RAF, FLT1 and/or FLT4 kinases.
Type:
Grant
Filed:
September 30, 2004
Date of Patent:
March 13, 2007
Assignee:
IRM LLC
Inventors:
Greg Chopiuk, Pascal Furet, Nathanael Schiander Gray, Patricia Imbach, Yi Liu, Joseph Schoepfer, Ruo Steensma
Abstract: This invention provides methods of screening for compounds that inhibit herpesviral transcription and replication. The methods comprise screening test compounds for ability to enhance the activity of homeodomain transcription factor PDX1 in repressing transcription of herpesviral genes (e.g., the IE gene of cytomegalovirus). Transcriptional repression by PDX1 can be monitored using an expression vector comprising a reporter gene operably linked to a PDX1-binding, upstream transcription regulatory sequence of the herpesvirus. The invention further provides methods and pharmaceutical compositions for stimulating PDX1-mediated transcriptional repression in a subject and for treating diseases and conditions associated with herpesviral infection.
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:
Grant
Filed:
October 12, 2002
Date of Patent:
February 13, 2007
Assignees:
The Scripps Research Institute, IRM LLC
Inventors:
Sheng Ding, Qiang Ding, Nathanael S. Gray
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:
June 10, 2004
Date of Patent:
February 6, 2007
Assignee:
IRM, LLC
Inventors:
Hong Liu, David Tully, Phillip Alper, Robert Epple, Arnab Chatterjee, Michael Roberts
Abstract: The present invention relates to biphenylyl derivatives, processes for their production, their uses and pharmaceutical compositions containing them. Compounds according to the present invention are based upon the chemical formula: wherein the substituents have the values mentioned herein.
Type:
Grant
Filed:
May 27, 2003
Date of Patent:
January 30, 2007
Assignee:
IRM LLC
Inventors:
Shifeng Pan, Nathanael S. Gray, Wenqui Gao, Klaus Hinterding, Sophie Lefebvre, Yuan Mi, Peter Nussbaumer, Wei Wang, Federic Zecri, Fan Yi, Lawrence Blas Perez, Kenneth Richad la Montagne, Peter Ettmayer
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.
Abstract: The invention provides a novel class of cyclic compounds, pharmaceutical compositions comprising such cyclic compounds and methods of using such compounds to treat or prevent diseases and disorders associated with cyclin-dependent kinases (CDKs) activity, particularly diseases associated with the activity of CDK2 and CDK5.
Type:
Grant
Filed:
March 5, 2004
Date of Patent:
December 19, 2006
Assignee:
IRM LLC
Inventors:
Pingda Ren, Francisco Adrian, Nathanael S. Gray, Xia Wang
Abstract: The invention provides efficiently automated incubation devices that reduce the number of powered moving parts in the devices and the amount of air transfer between environments that are internal and external to the devices. Related systems are also provided.
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:
Application
Filed:
March 20, 2006
Publication date:
November 9, 2006
Applicants:
IRM LLC, Novartis AG
Inventors:
Stuart Bevan, Pamposh Ganju, Peter McIntyre, Ardem Patapoutian, Andrea Peier, Chuanzheng Song
Abstract: The invention is directed to novel biaryl derivatives, to the uses of these compounds in various medicinal applications, including the treatment, prevention and control of proliferative diseases such as tumors, and to pharmaceutical compositions comprising these compounds. Compounds of the invention can be used to treat or prevent diseases or disorders that involve the activity of MIF-1 and/or adenosine kinase.
Type:
Grant
Filed:
December 18, 2003
Date of Patent:
October 24, 2006
Assignee:
IRM LLC
Inventors:
Jason Chyba, Quinn Devereax, Garret Hampton, Fred King
Abstract: This invention provides novel genes and polypeptides of the VR family, identification of trkA+ pain specific genes expressed in the DRG, 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:
June 13, 2002
Date of Patent:
October 3, 2006
Assignees:
IRM LLC, A Delaware Corp., Novartis AG
Inventors:
Stuart Bevan, Pamposh Ganju, Peter McIntyre, Ardem Patapoutian, Andrea Peier, Chuanzheng Song