Patents Represented by Attorney Genomics Institute of the Novartis Research Foundation
  • Patent number: 8338417
    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 c-kit, PDGFR and PDGFR kinases.
    Type: Grant
    Filed: May 2, 2008
    Date of Patent: December 25, 2012
    Assignees: IRM LLC, Novartis AG
    Inventors: Xiaolin Li, Xiaodong Liu, Valentina Molteni, Donatella Chianelli, Jon Loren, Juliet Nabakka, Timothy Ramsey, Werner Breitenstein
  • Patent number: 8338469
    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: April 19, 2011
    Date of Patent: December 25, 2012
    Assignee: IRM LLC
    Inventors: David C. Tully, Amab K. Chatterjee, Agnes Vidal, Hank Michael James Petrassi, Zhiwei Wang, Badry Bursulaya, Glen Spraggon
  • Patent number: 8334288
    Abstract: The present invention provides compounds of Formula I, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent; diseases or disorders associated with the activity of GPR119.
    Type: Grant
    Filed: July 9, 2009
    Date of Patent: December 18, 2012
    Assignee: IRM LLC
    Inventors: Robert Epple, Gerald Lelais, Victor Nikulin, Lucas Westcott-Baker
  • Patent number: 8293915
    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: January 7, 2008
    Date of Patent: October 23, 2012
    Assignee: IRM LLC
    Inventors: David C. Tully, Arnab K. Chatterjee, Zhiwei Wang
  • Patent number: 8293757
    Abstract: The invention provides compounds of formula (1) 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, AbI, BCR-AbI, CSK, JNK1, JNK2, p38, p70S6K, TGF?, SRC, EGFR, trkB, FGFR3. Fes, Lck, Syk, RAF, MKK4, MKK6, SAPK2?, BRK, Fms, KDR, c-rapor b-raf kinases.
    Type: Grant
    Filed: August 19, 2008
    Date of Patent: October 23, 2012
    Assignee: IRM LLC
    Inventors: Valentina Molteni, Xiaolin Li, Xiaodong Liu, Donatella Chianelli, Juliet Nabakka, Jon Loren, Shuli You
  • Patent number: 8288540
    Abstract: The invention provides compounds of Formula (I) 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, Fes, Lck, Syk, RAF, MKK4, MKK6, SAPK2?, BRK, Fms, KDR, c-raf or b-raf kinases.
    Type: Grant
    Filed: August 18, 2008
    Date of Patent: October 16, 2012
    Assignee: IRM LLC
    Inventors: Donatella Chianelli, Valentina Molteni, Xiaolin Li, Xiaodong Liu, Juliet Nabakka, Jon Loren
  • Patent number: 8278452
    Abstract: The invention provides a novel class of compounds of Formula I: (I) pharmaceutical compositions comprising 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 c-kit, PDGFR? and PDGFR? kinases.
    Type: Grant
    Filed: February 20, 2009
    Date of Patent: October 2, 2012
    Assignee: IRM LLC
    Inventors: Donatella Chianelli, Xiaolin Li, Xiaodong Liu, Jon Loren, Valentina Molteni, Juliet Nabakka, Vince Yeh
  • Patent number: 8268996
    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 Cathepsin S.
    Type: Grant
    Filed: June 16, 2011
    Date of Patent: September 18, 2012
    Assignee: IRM LLC
    Inventors: Hong Liu, David C. Tully, Arnab Chatterjee, Phillip B. Alper, David H. Woodmansee, Daniel Mutnick
  • Patent number: 8268850
    Abstract: The invention provides a novel class of pyrimidine derivatives, 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 c-kit, PDGFR? and PDGFR? kinases.
    Type: Grant
    Filed: May 1, 2008
    Date of Patent: September 18, 2012
    Assignee: IRM LLC
    Inventors: Xiaolin Li, Xiaodong Liu, Valentina Molteni
  • Patent number: 8263590
    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: April 27, 2011
    Date of Patent: September 11, 2012
    Inventors: Carlos Garcia-Echeverria, Takanori Kanazawa, Eiji Kawahara, Keiichi Masuya, Naoko Matsuura, Takahiro Miyake, Osamu Ohmori, Ichiro Umemura
  • Patent number: 8258156
    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 GPR119.
    Type: Grant
    Filed: May 23, 2011
    Date of Patent: September 4, 2012
    Assignee: IRM LLC
    Inventors: Phillip B. Alper, Mihai Azimioara, Christopher N. Cow, Robert Epple, Pierre-Yves Michellys, Victor Nikulin
  • Patent number: 8202876
    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, ARG, BCR-Abl, BRK, EphB, Fms, Fyn, KDR, c-Kit, LCK, PDGF-R, b-Raf, c-Raf, SAPK2, Src, Tie2 and TrkB kinases.
    Type: Grant
    Filed: September 24, 2007
    Date of Patent: June 19, 2012
    Assignees: IRM LLC, Novartis AG
    Inventors: Pamela Albaugh, Gregory B. Chopiuk, Qiang Ding, Shenlin Huang, Zuosheng Liu, Shifeng Pan, Pingda Ren, Xia Wang, Xing Wang, Yongping Xie, Chengzhi Zhang, Qiong Zhang, Guobao Zhang, Daniel Poon, Paul Renhowe, Martin Sendzik
  • Patent number: 8183248
    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 Abl, Bcr-Abl, Bmx, BTK, b-RAF, c RAF, CSK, cSRC, Fes, FGFR3, Flt3, IKK?, IKK?, JNK1?1, JNK2?2, Lck, Met, MKK4, MKK6, p70S6K, PAK2, PDGFR?, PKA, PKC?, PKD2, ROCK-II, Ros, Rsk1, SAPK2?, SAPK2?, SAPK3, SAPK4, SGK, Syk, Tie2 and TrkB kinases.
    Type: Grant
    Filed: May 10, 2006
    Date of Patent: May 22, 2012
    Assignee: IRM LLC
    Inventors: Advait Nagle, Nathanael Schiander Gray, Yi Liu, Pingda Ren, Taebo Sim, Shuli You
  • Patent number: 8178563
    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: May 4, 2007
    Date of Patent: May 15, 2012
    Assignee: IRM LLC
    Inventors: Wenqi Gao, Jiqing Jiang, Yongqin Wan, Dai Cheng, Dong Han, Xu Wu, Shifeng Pan
  • Patent number: 8178526
    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 dysregulated B cell activities, particularly diseases or disorders that involve aberrant activation of inositol 1,4,5-trisphosphate 3-kinase B (ITPKb).
    Type: Grant
    Filed: June 12, 2008
    Date of Patent: May 15, 2012
    Assignee: IRM LLC
    Inventors: Badry Bursulaya, Dai Cheng, Jiqing Jiang, Donald S. Karanewsky, Yi Liu, Shifeng Pan, Yongqin Wan, Xia Wang, Yun Feng Xie, Yang Yang
  • Patent number: 8158662
    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: April 17, 2012
    Assignee: Hamilton
    Inventors: Valentina Molteni, Xiaolin Li, Juliet Nabakka, David Archer Ellis, Beth Anaclerio, Enrique Saez, John Wityak
  • Patent number: 8158634
    Abstract: The invention provides compounds having Formula Ia, or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4 and Y are as defined in the specification; as well as pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cannabinoid Receptor 1 (CB1).
    Type: Grant
    Filed: October 26, 2005
    Date of Patent: April 17, 2012
    Assignee: IRM LLC
    Inventors: Hong Liu, Xiaohui He, Ha-Soon Choi, Kunyong Yang, David Woodmansee, Zhicheng Wang, David Archer Ellis, Baogen Wu, Yun He, Truc Ngoc Nguyen
  • Patent number: 8153635
    Abstract: The invention provides compounds of Formula I: wherein A, L, m, q, Q, R1, R2, R3, R4 and R5 are defined in the Summary of the Invention. The invention further provides for pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.
    Type: Grant
    Filed: September 4, 2008
    Date of Patent: April 10, 2012
    Assignee: IRM LLC
    Inventors: Phillip B. Alper, Mihai Azimioara, Christopher Cow, Robert Epple, Songchun Jiang, Gerald Lelais, Pierre-Yves Michellys, Daniel Mutnick, Victor Nikulin
  • Patent number: 8153671
    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: July 14, 2006
    Date of Patent: April 10, 2012
    Assignee: IRM LLC
    Inventors: Phillip B. Alper, Thomas Marsilje, Arnab Chatterjee, Wenshuo Lu, Daniel Mutnick, Michael Roberts, Yun He
  • Patent number: 8106068
    Abstract: The invention provides compounds of Formula (2), and pharmaceutical compositions thereof, wherein R1, R2, R3, R4 and L are as described herein; 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: December 2, 2009
    Date of Patent: January 31, 2012
    Assignee: IRM LLC
    Inventors: Zuosheng Liu, Jon Loren, Valentina Molteni, Juliet Nabakka