Patents Represented by Attorney Genomics Institute of the Novartis Research Foundation
  • Patent number: 8101608
    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, cSrc, TPR-Met, Tie2, MET, FGFR3, Aurora, Axl, Bmx, BTK, c-kit, CHK2, Flt3, MST2, p70S6K, PDGFR, PKB, PKC, Raf, ROCK-II, Rsk1, SGK, TrkA, TrkB and TrkC kinases.
    Type: Grant
    Filed: November 7, 2005
    Date of Patent: January 24, 2012
    Assignee: IRM LLC, a Delware Limited Corporation
    Inventors: Yongqin Wan, Yuan Mi, Yi Fan, Dai Cheng, Yi Liu, Nathanael S. Gray, Pamela Albaugh
  • Patent number: 8039479
    Abstract: The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof.
    Type: Grant
    Filed: November 20, 2007
    Date of Patent: October 18, 2011
    Assignee: IRM LLC
    Inventors: Pierre-Yves Michellys, Wei Pei, Thomas H. Marsilje, Bei Chen, Tetsuo Uno
  • Patent number: 7964592
    Abstract: Novel pyrimidine derivatives of formula I to process for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.
    Type: Grant
    Filed: March 12, 2004
    Date of Patent: June 21, 2011
    Assignee: Novartis AG
    Inventors: Carlos Garcia-Echeverria, Takanori Kanazawa, Eiji Kawahara, Keiichi Masuya, Naoko Matsuura, Takahiro Miyake, Osamu Ohmori, Ichiro Umemura
  • Patent number: 7951823
    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: Grant
    Filed: May 16, 2007
    Date of Patent: May 31, 2011
    Assignee: IRM LLC
    Inventors: David C. Tully, Arnab K. Chatterjee, Agnes Vidal, Hank Michael James Petrassi, Zhiwei Wang, Badry Bursulaya, Glen Spraggon
  • Patent number: 7939547
    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: Grant
    Filed: May 15, 2007
    Date of Patent: May 10, 2011
    Assignee: IRM LLC
    Inventors: David C. Tully, Arnab K. Chatterjee, Hank Michael James Petrassi, Badry Bursulaya, Glen Spraggon
  • Patent number: 7928133
    Abstract: The invention provides a method for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula I.
    Type: Grant
    Filed: July 24, 2007
    Date of Patent: April 19, 2011
    Assignee: IRM LLC
    Inventors: Dai Cheng, Dong Han, Wenqi Gao, Jiqing Jiang, Shifeng Pan, Yongqin Wan, Qihui Jin
  • Patent number: 7893074
    Abstract: Novel pyrimidine derivatives of formula I to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.
    Type: Grant
    Filed: August 13, 2004
    Date of Patent: February 22, 2011
    Assignees: Novartis AG, IRM LLC
    Inventors: Carlos Garcia-Echeverria, Takanori Kanazawa, Eiji Kawahara, Keiichi Masuya, Naoko Matsuura, Takahiro Miyake, Osamu Ohmori, Ichiro Umemura, Ruo Steensma, Greg Chopiuk, Jiqing Jiang, Yongqin Wan, Qiang Ding, Qiong Zhang, Nathanael Schiander Gray, Donald Karanewsky
  • Patent number: 7868018
    Abstract: The invention provides compounds of Formula I: wherein R1-R6 are described in the Summary of the Invention; the 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, BTK, CHK2, b-RAF, c-RAF, CSK, c-SRC, Fes, FGFR3, Flt3, IKK?, IKK?, JNK2?2, Lck, Met, MKK4, MKK6, MST2, NEK2, p70S6K, PDGFR?, PKA, PKB?, PKD2, Rsk1, SAPK2?, SAPK2?, SAPK3, SGK, Tie2 and TrkB kinases.
    Type: Grant
    Filed: August 9, 2006
    Date of Patent: January 11, 2011
    Assignee: IRM LLC
    Inventors: Yongping Xie, Guobao Zhang, Xing Wang, Nathanael S. Gray, Yi Liu
  • Patent number: 7846923
    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, Bcr-Abl(T315I), ALK, BLK, BMX, BRK, C-kit, c-RAF, CSK, c-SRC, EGFR, Fes, FGFR3, Flt3, Fms, Fyn, IGF-1R, IR, JAK(2), JAK(3), KDR, Lck, NLK, p70S6K, PDGFR?, Ros, SAPK2?, SGK, SIK, Syk, Tie2 and TrkB kinases.
    Type: Grant
    Filed: May 11, 2007
    Date of Patent: December 7, 2010
    Assignee: IRM LLC
    Inventors: Pingda Ren, Baogen Wu, Guobao Zhang, Yongping Xie, Barun Okram, Victor Nikulin, Xia Wang, Ha-Soon Choi
  • Patent number: 7846949
    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: Grant
    Filed: February 11, 2005
    Date of Patent: December 7, 2010
    Assignee: IRM LLC
    Inventors: Valentina Molteni, Xiaolin Li, Fang Liang, Juliet Nabakka, Enrique Saez, John Wityak
  • Patent number: 7820705
    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: Grant
    Filed: May 12, 2005
    Date of Patent: October 26, 2010
    Assignee: IRM LLC
    Inventors: Robert Epple, Ross Russo, Mihai Azimioara, Yongping Xie
  • Patent number: 7816542
    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 TPO activity, particularly diseases or disorders that involve thrombocytopenia.
    Type: Grant
    Filed: August 15, 2006
    Date of Patent: October 19, 2010
    Assignee: IRM LLC
    Inventors: Thomas Marsilje, Wenshuo Lu, Phillip B. Alper, Daniel Mutnick, Yun He
  • Patent number: 7807841
    Abstract: Described herein are compounds that have a spiro structural feature. Also described herein are methods for making such compounds, methods for using such compounds to modulate the activity of steroid hormone nuclear 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 diseases or conditions associated with the activity of steroid hormone nuclear receptors.
    Type: Grant
    Filed: February 16, 2006
    Date of Patent: October 5, 2010
    Assignee: IRM LLC
    Inventors: Pierre-Yves Michellys, Chi Ching Mak, Wei Pei
  • Patent number: 7750032
    Abstract: The invention provides trisubstituted pyrazoles and imidazoles of Formula I: wherein L2, q, R13, R14, R15, R16, Z1 and Z2 are as described in the Summary of the Invention; 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: Grant
    Filed: February 3, 2006
    Date of Patent: July 6, 2010
    Assignee: IRM LLC
    Inventors: Christopher Cow, Robert Epple, Xing Wang, Yongping Xie, Hans Martin Seidel
  • Patent number: 7750021
    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: July 25, 2008
    Date of Patent: July 6, 2010
    Assignee: IRM LLC
    Inventors: Yuan Mi, Shifeng Pan, Nathanael Schiander Gray, Wenqi Gao, Yi Fan, Tao Jiang
  • Patent number: 7745437
    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, trkB, c-SRC, BMX, FGFR3, b-RAF, ??K, T??2, ???, ?NK2?2, MKK4, c-RAF, MKK6, SAPK2? and SAPK2? kinases.
    Type: Grant
    Filed: June 9, 2005
    Date of Patent: June 29, 2010
    Assignee: IRM LLC
    Inventors: Pingda Ren, Xia Wang, Guobao Zhang, Qiang Ding, Shuli You, Qiong Zhang, Greg Chopiuk, Pamela A. Albaugh, Taebo Sim, Nathanael Schiander Gray
  • Patent number: 7745445
    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: Grant
    Filed: May 13, 2005
    Date of Patent: June 29, 2010
    Assignee: IRM LLC
    Inventors: Robert Epple, Mihai Azimioara
  • Patent number: 7732449
    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 1: wherein Q is an optionally substituted piperazinyl; and A, R5, R6, R7, R8, R9 and Ar are substituents.
    Type: Grant
    Filed: January 28, 2009
    Date of Patent: June 8, 2010
    Assignee: IRM LLC
    Inventors: Hong Liu, Arnab K. Chatterjee, David C. Tully, Phillip B. Alper, David H. Woodmansee
  • Patent number: 7718704
    Abstract: The invention provides a novel class of cyclic oximes of Formula I: wherein A, X, Y, Z, W, R1, R2, R3 and n are as described in the summary of the invention; 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: May 18, 2010
    Assignee: IRM LLC
    Inventors: Shifeng Pan, Wenqi Gao, Nathanael Schiander Gray, Yuan Mi
  • Patent number: 7713958
    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 and disorders associated with kinase activity, particularly diseases associated with the activity of CDK1, CDK2, CDK4, CDK5, GSK3?, Bcr-abl, Flt-3, c-Kit, PDGFR?, Src, Mek1 and CK1.
    Type: Grant
    Filed: August 6, 2008
    Date of Patent: May 11, 2010
    Assignee: IRM LLC
    Inventors: Yongqin Wan, Nathanael S. Gray