Abstract: Novel crystalline forms of 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyi-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyljbenzamide free base and 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyi-N-{4-[(4-methyl piperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide mono hydrochloride, pharmaceutical compositions thereof and methods of their preparation and use are disclosed herein. The instant application is directed to novel crystalline forms of 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyi-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl}phenyl}benzamide and 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyi-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide mono hydrochloride, compositions comprising such crystalline forms, and to methods of their preparation and use.
Type:
Grant
Filed:
December 12, 2013
Date of Patent:
November 15, 2016
Assignee:
ARIAD PHARMACEUTICALS, INC.
Inventors:
Christopher K. Murray, Leonard W. Rozamus, John J. Chaber, Pradeep Sharma
Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
Type:
Grant
Filed:
June 4, 2014
Date of Patent:
March 8, 2016
Assignee:
ARIAD Pharmaceuticals, Inc.
Inventors:
Dong Zou, Wei-Sheng Huang, R. Mathew Thomas, Jan Antoinette C. Romero, Jiwei Qi, Yihan Wang, Xiaotian Zhu, William C. Shakespeare, Rajeswari Sundaramoorthi, Chester A. Metcalf, III, David C. Dalgarno, Tomi K. Sawyer
Abstract: The invention features compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use as protein kinase inhibitors.
Type:
Grant
Filed:
March 15, 2013
Date of Patent:
March 1, 2016
Assignee:
ARIAD Pharmaceuticals, Inc.
Inventors:
Yihan Wang, Wei-Sheng Huang, Shuangying Liu, William C. Shakespeare, R. Mathew Thomas, Jiwei Qi, Feng Li, Xiaotian Zhu, Anna Kohlmann, David C. Dalgarno, Jan Antoinette C. Romero, Dong Zou
Abstract: Novel crystalline forms of 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyi-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyljbenzamide free base and 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyi-N-{4-[(4-methyl piperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide mono hydrochloride, pharmaceutical compositions thereof and methods of their preparation and use are disclosed herein. The instant application is directed to novel crystalline forms of 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyi-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl}phenyl}benzamide and 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyi-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide mono hydrochloride, compositions comprising such crystalline forms, and to methods of their preparation and use.
Type:
Application
Filed:
December 12, 2013
Publication date:
November 5, 2015
Applicant:
ARIAD PHARMACEUTICALS, INC.
Inventors:
Christopher K. Murray, Leonard W. Rozamus, John J. Chaber, Pradeep Sharma
Abstract: The invention features compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
Type:
Application
Filed:
April 20, 2015
Publication date:
August 13, 2015
Applicant:
ARIAD PHARMACEUTICALS, INC.
Inventors:
Yihan Wang, Wei-Sheng Huang, Shuangying Liu, William C. Shakespeare, Ranny M. Thomas, Jiwei Qi, Feng Li, Xiaotian Zhu, Anna Kohlmann, David C. Dalgarno, Jan Antoinette C. Romero, Dong Zou
Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
Type:
Grant
Filed:
September 13, 2012
Date of Patent:
July 28, 2015
Assignee:
ARIAD Pharmaceuticals, Inc.
Inventors:
Yihan Wang, Xiaotian Zhu, Rajeswari Sundaramoorthi, Wei-Sheng Huang, Dong Zou, R. Mathew Thomas, Jiwei Qi, Jan Antoinette C. Romero, David C. Dalgarno, William C. Shakespeare, Tomi K. Sawyer, Chester A. Metcalf, III
Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
Type:
Grant
Filed:
March 13, 2013
Date of Patent:
May 12, 2015
Assignee:
ARIAD Pharmaceuticals, Inc.
Inventors:
Dong Zou, Wei-Sheng Huang, R. Mathew Thomas, Jan Antoinette C. Romero, Jiwei Qi, Yihan Wang, Xiaotian Zhu, William C. Shakespeare, Rajeswari Sundaramoorthi, Chester A. Metcalf, III, David C. Dalgarno, Tomi K. Sawyer
Abstract: This disclosure concerns a new family of phosphorus-containing compounds of Formula (I): and pharmaceutically acceptable derivatives thereof. Compositions containing such compounds and uses thereof are also provided.
Type:
Grant
Filed:
November 14, 2011
Date of Patent:
May 5, 2015
Assignee:
Ariad Pharmaceuticals, Inc.
Inventors:
David L. Berstein, Leonard W. Rozamus, Yihan Wang, Chester A. Metcalf, III
Abstract: The invention features methods and compositions for the synthesis of multimerizing agents. An exemplary method for producing AP20187 may comprise: (a) coupling 2-N,Ndimethylaminomethyl-1,3-diaminopropane with AP20792 to produce the dimeric alcohol, AP20793; and (b) coupling the AP20793 so produced with API7362 to yield AP20187. In particular embodiments, the method further includes the step of producing API7362 by coupling API7360 with methyl-L-pipecolic acid, or a salt thereof.
Abstract: The invention features compounds of the general formula (I) in which the variable groups are as defined herein, and to their preparation and use.
Type:
Grant
Filed:
May 21, 2009
Date of Patent:
April 21, 2015
Assignee:
Ariad Pharmaceuticals, Inc.
Inventors:
Yihan Wang, Wei-Sheng Huang, Shuangying Liu, William C. Shakespeare, R. Mathew Thomas, Jiwei Qi, Feng Li, Xiaotian Zhu, Anna Kohlman, David C. Dalgarno, Jan Antoinette C. Romero, Dong Zou
Abstract: This invention relates to compounds of the general formula (I) in which the variable groups are as defined herein, and to their preparation and use.
Type:
Grant
Filed:
December 11, 2009
Date of Patent:
December 16, 2014
Assignee:
ARIAD Pharmaceuticals, Inc.
Inventors:
Jiwei Qi, Yihan Wang, Feng Li, William C. Shakespeare, Anna Kohlmann, David C. Dalgarno, Xiaotian Zhu
Abstract: The instant invention provides a method of treating a cancer selected from the group consisting of non-small cell lung cancer and breast cancer with an mTOR inhibitor and an ?v62 3 integrin antagonist, wherein the mTOR inhibitor is ridaforolimus, everolimus, temsirolimus or a combination thereof.
Type:
Application
Filed:
April 30, 2014
Publication date:
November 27, 2014
Applicants:
ARIAD Pharmaceuticals, Inc., Merck
Inventors:
Jennifer O'Neil, Yair Benita, Shane Marine, Brian Haines
Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
Type:
Grant
Filed:
March 13, 2013
Date of Patent:
July 15, 2014
Assignee:
ARIAD Pharmaceuticals, Inc.
Inventors:
Dong Zou, Wei-Sheng Huang, R. Mathew Thomas, Jan Antoinette C. Romero, Jiwei Qi, Yihan Wang, Xiaotian Zhu, William C. Shakespeare, Rajeswari Sundaramoorthi, Chester A. Metcalf, III, David C. Dalgarno, Tomi K. Sawyer
Abstract: The invention features methods and compositions for the synthesis of multimerizing agents. An exemplary method for producing AP20187 may comprise: (a) coupling 2-N,Ndimethylaminomethyl-1,3-diaminopropane with AP20792 to produce the dimeric alcohol, AP20793; and (b) coupling the AP20793 so produced with API7362 to yield AP20187. In particular embodiments, the method further includes the step of producing API7362 by coupling API7360 with methyl-L-pipecolic acid, or a salt thereof.
Abstract: The invention discloses methods and compositions for treating or preventing Parkinson's disease by administering a compound of Formula (I): or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the variables are defined as herein.
Abstract: The invention features compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
Abstract: The invention discloses methods and compositions for treating or preventing neurodegenerative disease by administering a compound of Formula I: or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the variables are defined as herein.
Type:
Application
Filed:
April 6, 2012
Publication date:
February 13, 2014
Applicant:
ARIAD PHARMACEUTICALS, INC.
Inventors:
William C. Shakespeare, Frank G. Haluska
Abstract: The invention features a method for treating patients who have an EGFR-driven cancer, which is, or has become, refractory to a tyrosine kinase inhibitor, such as eriotinib and gefitinib, by administering a compound of formula (I) to the patient. The invention also features treating EGFR-driven cancers having an EGFR mutation identified herein.
Type:
Application
Filed:
October 14, 2011
Publication date:
January 23, 2014
Applicant:
ARIAD PHARMACEUTICALS, INC.
Inventors:
David C. Dalgarno, William C. Shakespeare, Xiaotian Zhu, Victor M. Rivera, Juan J. Miret