Abstract: The invention provides a compound of Formula I, Pharmaceutical compositions comprising such compounds and the use of such compounds in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.
Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function by contacting the cell with a hedgehog antagonist, such as a small molecule, in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize hedgehog activity.
Abstract: The present invention relates to tyrosine kinase inhibitors that contain a zinc-binding moiety and their use in the treatment of tyrosine related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors.
Type:
Grant
Filed:
March 18, 2013
Date of Patent:
October 27, 2015
Assignee:
Curis, Inc.
Inventors:
Xiong Cai, Changgeng Qian, Stephen Gould, Haixiao Zhai
Abstract: This invention relates to the discovery of novel forms of Compound 1, including solvates, hydrates, and other crystalline forms. These novel forms of Compound 1 may impart advantages in pharmaceutical formulations incorporating them, including improved stability and bioavailability.
Type:
Grant
Filed:
September 23, 2013
Date of Patent:
October 6, 2015
Assignee:
Curis, Inc.
Inventors:
Noel Hamill, James Moody, Sébastien Chabaud, Arnaud Hamel
Abstract: The present invention relates to quinazoline containing zinc-binding moiety based derivatives of formula I that have enhanced and unexpected properties as inhibitors of epidermal growth factor receptor tyrosine kinase (EGFR-TK) and their use in the treatment of EGFR-TK related diseases and disorders such as cancer.
Abstract: The emergence of mutations in tyrosine kinases following treatment of cancer patients with molecular-targeted therapy represents a major mechanism of acquired drug resistance. Here, we describe a mutation in the serpentine receptor, Smoothened (SMO), which results in resistance to a Hedgehog (Hh) pathway inhibitor in medulloblastoma. A single amino acid substitution in a conserved glutamic acid residue of SMO maintains Hh signaling, but results in the inability of the Hh pathway inhibitor, GDC-0449, to bind SMO and suppress the pathway. The invention provides screening methods to detect SMO mutations and methods to screen for drugs that specifically modulate mutant SMO exhibiting drug resistance.
Type:
Grant
Filed:
July 3, 2013
Date of Patent:
August 4, 2015
Assignees:
Genentech, Inc., Curis, Inc.
Inventors:
Frederic J. de Sauvage, Gerrit J. P. Dijkgraaf
Abstract: The present invention relates to HSP90 inhibitors containing fused amino pyridine core that are useful as inhibitors of HSP90 and their use in the treatment of HSP90 related diseases and disorders such as cancer, an autoimmune disease, or a neurodegenerative disease.
Abstract: The present invention relates to quinazoline containing zinc-binding moiety based derivatives of Formula (IV) below. These compounds have enhanced and unexpected properties as inhibitors of epidermal growth factor receptor tyrosine kinase (EGFR-TK) and are useful in the treatment of EGFR-TK related diseases and disorders such as cancer. These compounds may further act as HDAC inhibitors.
Type:
Grant
Filed:
November 25, 2013
Date of Patent:
May 5, 2015
Assignee:
Curis, Inc.
Inventors:
Changgeng Qian, Xiong Cai, Stephen Gould, Haixiao Zhai
Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.
Type:
Application
Filed:
December 24, 2014
Publication date:
April 23, 2015
Applicants:
CURIS, INC., GENENTECH, INC.
Inventors:
Janet L. GUNZNER, Daniel P. SUTHERLIN, Mark S. STANLEY, Liang BAO, Georgette M. CASTANEDO, Rebecca L. LALONDE, Shumei WANG, Mark E. REYNOLDS, Scott J. SAVAGE, Kimberly MALESKY, Michael S. DINA, Michael F.T. KOEHLER
Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.
Type:
Application
Filed:
December 18, 2014
Publication date:
April 16, 2015
Applicants:
CURIS, INC., GENENTECH, INC.
Inventors:
Janet L. GUNZNER, Daniel SUTHERLIN, Mark S. STANLEY, Liang BAO, Georgette M. CASTANEDO, Rebecca L. LALONDE, Shumei WANG, Mark E. REYNOLDS, Scott J. SAVAGE, Kimberly MALESKY, Michael S. DINA, Michael F.T. KOEHLER
Abstract: The present invention relates to quinazoline containing zinc-binding moiety based derivatives of Formula (I) below. These compounds have enhanced and unexpected properties as inhibitors of epidermal growth factor receptor tyrosine kinase (EGFR-TK) and are useful in the treatment of EGFR-TK related diseases and disorders such as cancer. These compounds may further act as HDAC inhibitors.
Type:
Grant
Filed:
May 15, 2013
Date of Patent:
March 10, 2015
Assignee:
Curis, Inc.
Inventors:
Changgeng Qian, Xiong Cai, Stephen Gould
Abstract: The instant application relates to deazapurines, thienopyrimidines and furopyrimidines with zinc-binding moiety based derivatives and their use in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.
Abstract: The present invention makes available methods and reagents for modulating proliferation or differentiation in a cell or tissue comprising contacting the cell with a hedgehog agonist, such as the compounds depicted in FIGS. 32 and 33. In certain embodiments, the methods and reagents may be employed to correct or inhibit an aberrant or unwanted growth state, e.g., by antagonizing a normal ptc pathway or agonizing smoothened or hedgehog activity.
Type:
Grant
Filed:
August 20, 2007
Date of Patent:
October 7, 2014
Assignee:
Curis, Inc.
Inventors:
Anthony David Baxter, Edward Andrew Boyd, Maria Frank-Kamenetsky, Oivin Guicherit, Jeffery Porter, Stephen Price, Lee Rubin, John Harry Alexander Stibbard
Abstract: The present invention relates to tartrate salts of quinazoline containing zinc-binding moiety based derivatives of Formula II, below: These compounds are inhibitors of epidermal growth factor receptor tyrosine kinase (EGFR-TK) and may further act as HDAC inhibitors. The invention further relates to the use of these tartrate salts in the treatment of EGFR-TK related diseases and disorders such as cancer.
Abstract: The invention provides a compound of Formula I, Pharmaceutical compositions comprising such compounds and the use of such compounds in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.
Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist of formula (I) in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity.
Type:
Grant
Filed:
March 16, 2012
Date of Patent:
August 26, 2014
Assignees:
Curis, Inc., Genentech, Inc.
Inventors:
Oivin M. Guicherit, Edward Andrew Boyd, Shirley Ann Brunton, Stephen Price, John Harry Alexander Stibbard, Colin H. Mackinnon
Abstract: The instant application relates to methods and reagents for modulating the Hedgehog signaling pathway using RNA interference technology (RNAi). The application provides potential targets of the Hedgehog RNAi, methods to identify additional Hedgehog signaling pathway components, methods to inhibit Hedgehog signaling targets using siRNA, and their uses in the treatment of a number of disease conditions.
Abstract: The present invention relates to quinazoline containing zinc-binding moiety based derivatives of Formula (IV) below. These compounds have enhanced and unexpected properties as inhibitors of epidermal growth factor receptor tyrosine kinase (EGFR-TK) and are useful in the treatment of EGFR-TK related diseases and disorders such as cancer. These compounds may further act as HDAC inhibitors.
Type:
Application
Filed:
November 25, 2013
Publication date:
August 7, 2014
Applicant:
Curis, Inc.
Inventors:
Changgeng Qian, Xiong Cai, Stephen Gould, Haixiao Zhai
Abstract: The present invention relates to HSP90 inhibitors containing fused amino pyridine core that are useful as inhibitors of HSP90 and their use in the treatment of HSP90 related diseases and disorders such as cancer, an autoimmune disease, or a neurodegenerative disease.
Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist, such as a small molecule, in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity.
Type:
Grant
Filed:
December 12, 2012
Date of Patent:
July 8, 2014
Assignee:
Curis, Inc.
Inventors:
Lee L. Rubin, Oivin Guicherit, Stephen Price, Edward Andrew Boyd