Abstract: Provided herein are Pyrrolopyrimidine Compounds having the following structure: wherein R1, R2, R3, and L are as defined herein, compositions comprising an effective amount of a Pyrrolopyrimidine Compound, and methods for treating or preventing breast cancer, more particularly triple negative breast cancer, comprising administering an effective amount of such Pyrrolopyrimidine Compounds to a subject in need thereof.
Type:
Grant
Filed:
July 21, 2016
Date of Patent:
October 24, 2017
Assignee:
Signal Pharmaceuticals, LLC
Inventors:
Andrew Antony Calabrese, Brandon Jeffy, Dale Robinson, Dan Zhu, Dehua Huang, Jan Elsner, John Boylan, Lida Tehrani, Mark A. Nagy, Raj Kumar Raheja, Paul Erdman, Rama K. Narla, Roy L. Harris, Tam Minh Tran, Jennifer Riggs, Yuhong Ning, Shuichan Xu
Abstract: Provided herein are methods for treating or preventing a cancer, comprising administering an effective amount of a TOR kinase inhibitor having the following formula (I): and an effective amount of a cytidine analog, such as 5-azacytidine, to a patient having a cancer.
Abstract: Provided herein are diaminopyrimidyl Compounds having the following structures: wherein X, L, R1, and R2 are as defined herein, compositions comprising an effective amount of a Diaminopyrimidyl Compound, and methods for treating or preventing PKC-theta-mediated disorders, or a condition treatable or preventable by inhibition of a kinase, for example, PKC-theta.
Type:
Grant
Filed:
August 19, 2016
Date of Patent:
October 10, 2017
Assignee:
Signal Pharmaceuticals, LLC
Inventors:
Patrick Papa, Brian Edwin Cathers, Andrew Antony Calabrese, Brandon Wade Whitefield, Brydon Bennett, Daniel Cashion, Deborah Mortensen, Dehua Huang, Eduardo Torres, Jason Parnes, John Sapienza, Joshua Hansen, Katerina Leftheris, Matthew Correa, Maria Mercedes Delgado, Raj K. Raheja, Sogole Bahmanyar, Sayee Hegde, Stephen Norris, Veronique Plantevin-Krenitsky
Abstract: Provided herein are Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions, comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.
Type:
Grant
Filed:
October 5, 2015
Date of Patent:
September 26, 2017
Assignee:
Signal Pharmaceuticals, LLC
Inventors:
Jan Elsner, Roy L. Harris, Branden Gingsee Lee, Deborah Mortensen, Garrick K. Packard, Patrick Papa, Jason Parnes, Sophie Perrin-Ninkovic, Jennifer Riggs, John Sapienza, Graziella I. Shevlin, Lida Tehrani, Jingjing Zhao
Abstract: Provided herein are methods for treating or preventing a cancer, comprising administering an effective amount of a TOR kinase inhibitor and an effective amount a second active agent to a patient having a cancer, wherein the TOR kinase inhibitor is a compound of formula (I): and pharmaceutically acceptable salts, clathrates, solvates, stereoisomers, tautomers, metabolites, isotopologues and prodrugs thereof.
Type:
Grant
Filed:
April 15, 2015
Date of Patent:
August 22, 2017
Assignee:
Signal Pharmaceuticals, LLC
Inventors:
Kimberly Elizabeth Fultz, Tam Minh Tran, Shuichan Xu, Weiming Xu
Abstract: Provided herein are Aminopurine Compounds having the following structures: wherein R1, R2, and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound, and methods for treating or preventing a cancer, for example, melanoma.
Type:
Grant
Filed:
October 27, 2016
Date of Patent:
August 22, 2017
Assignee:
Signal Pharmaceuticals, LLC
Inventors:
Matthew Alexander, Sogole Bahmanyar, Joshua Hansen, Dehua Huang, Robert Hubbard, Brandon Jeffy, Jim Leisten, Mehran Moghaddam, Raj K. Raheja, Heather Raymon, Kimberly Schwarz, Marianne Sloss, Eduardo Torres, Tam Minh Tran, Shuichan Xu, JingJing Zhao, John Frederick Boylan
Abstract: Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing cancer, a cardiovascular disease, a renal disease, an autoimmune condition, an inflammatory condition, macular degeneration, ischemia-reperfusion injury, pain and related syndromes, disease-related wasting, an asbestos-related condition, pulmonary hypertension or a condition treatable or preventable by inhibition of the JNK pathway comprising administering an effective amount of an Aminopurine Compound to a patient in need thereof.
Type:
Grant
Filed:
October 21, 2015
Date of Patent:
August 8, 2017
Assignee:
Signal Pharmaceuticals, LLC
Inventors:
Steven Clareen, Veronique Plantevin-Krenitsky, Moorthy Palanki, Yoshitaka Satoh
Abstract: Provided herein are formulations, processes, solid forms and methods of use relating to 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one.
Abstract: Provided herein are Diaminopyrimidine Compounds having the following structures: wherein R1, R2, R3, and R4 are as defined herein, compositions comprising an effective amount of a Diaminopyrimidine Compound, and methods for treating or preventing liver fibrotic disorders or a condition treatable or preventable by inhibition of a JNK pathway.
Type:
Grant
Filed:
July 31, 2015
Date of Patent:
July 11, 2017
Assignee:
Signal Pharmaceuticals, LLC
Inventors:
Brydon L. Bennett, Mercedes Delgado, Jan Elsner, Paul Erdman, Robert Hilgraf, Laurie Ann LeBrun, Meg McCarrick, Mehran F. Moghaddam, Mark A. Nagy, Stephen Norris, David A. Paisner, William J. Romanow, Yoshitaka Satoh, Marianne Sloss, Jayashree Tikhe, Won Hyung Yoon
Abstract: Provided herein are methods for treating or preventing glioblastoma multiforme (GBM) characterized by O6-methylguanine-DNA methyltransferase (MGMT) expression and/or promoter methylation status, comprising administering an effective amount of a Dihydropyrazino-Pyrazine Compound to a patient having glioblastoma multiforme (GBM) characterized by O6-methylguanine-DNA methyltransferase (MGMT) expression and/or promoter methylation status.
Abstract: Provided herein are methods for treating or preventing a cancer, in particular solid tumors and hematological cancers, comprising administering to a subject in need thereof an effective amount of a compound of formula (I):
Type:
Grant
Filed:
July 13, 2015
Date of Patent:
April 18, 2017
Assignee:
Signal Pharmaceuticals, LLC
Inventors:
Dan Zhu, John Boylan, Shuichan Xu, Jennifer Riggs, Tao Shi, Andrew Wurmser, David Mikolon, Gordafaried Deyanat-Yazdi
Abstract: Provided herein are compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one, solid forms, isotopologs and metabolites thereof, and methods of their use for the treatment of a disease, disorder, or condition.
Type:
Grant
Filed:
May 28, 2014
Date of Patent:
March 28, 2017
Assignee:
Signal Pharmaceuticals, LLC
Inventors:
Marie Georges Beauchamps, Antonio Christian Ferretti, Juan Antonio Gamboa, Kevin Klopfer, William Edward Konnecke, Matthew Michael Kreilein, Anil Menon, Amanda Nicole Miklos, John Fitzgerald Traverse
Abstract: Provided herein are methods for treating and/or preventing a cancer or a tumor syndrome in a patient, comprising administering an effective amount of a TOR kinase inhibitor to a patient having cancer or a tumor syndrome, characterized by a LKB1 and/or AMPK gene or protein loss or mutation.
Abstract: Provided herein are diaminopyrimidyl Compounds having the following structures: wherein X, L, R1, and R2 are as defined herein, compositions comprising an effective amount of a Diaminopyrimidyl Compound, and methods for treating or preventing PKC-theta-mediated disorders, or a condition treatable or preventable by inhibition of a kinase, for example, PKC-theta.
Type:
Grant
Filed:
December 19, 2014
Date of Patent:
January 31, 2017
Assignee:
Signal Pharmaceuticals, LLC
Inventors:
Patrick Papa, Brian Edwin Cathers, Andrew Antony Calabrese, Brandon Wade Whitefield, Brydon Bennett, Daniel Cashion, Deborah Mortensen, Dehua Huang, Eduardo Torres, Jason Parnes, John Sapienza, Joshua Hansen, Katerina Leftheris, Matthew Correa, Maria Mercedes Delgado, Raj K. Raheja, Sogole Bahmanyar, Sayee Hegde, Stephen Norris, Veronique Plantevin-Krenitsky
Abstract: Provided herein are methods for treating a cancer treatable by inhibition of phosphorylation of PRAS40, GSK3? or p70S6K1, comprising administering an effective amount of a TOR kinase inhibitor to a patient having a cancer treatable by inhibition of phosphorylation of PRAS40, GSK3? or p70S6K1.
Type:
Grant
Filed:
August 26, 2015
Date of Patent:
January 31, 2017
Assignee:
Signal Pharmaceuticals, LLC
Inventors:
Weiming Xu, Deborah Mortensen, Shuichan Xu, Kimberly Elizabeth Fultz
Abstract: Provided herein are methods for evaluating the effect of 2-(tert-butylamino)-4-((1R,3R,4R)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide or a pharmaceutically acceptable stereoisomer, tautomer, solid form, polymorph, salt, hydrate, clathrate, or solvate thereof in a patient with an assay based on UVB-irradiation and phosphorylated c-Jun expression. The analyzes allow for evaluation of dose-response and identification of patient populations who are sensitive to 2-(tert-butylamino)-4-((1R,3R,4R)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide or a pharmaceutically acceptable stereoisomer, tautomer, solid form, polymorph, salt, hydrate, clathrate, or solvate thereof.
Abstract: Provided herein are Aminopurine Compounds having the following structures: wherein R1, R2, and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound, and methods for treating or preventing a cancer, for example, melanoma.
Type:
Grant
Filed:
October 5, 2015
Date of Patent:
December 6, 2016
Assignee:
Signal Pharmaceuticals, LLC
Inventors:
Matthew Alexander, Sogole Bahmanyar, Joshua Hansen, Dehua Huang, Robert Hubbard, Brandon Jeffy, Jim Leisten, Mehran Moghaddam, Raj K. Raheja, Heather Raymon, Kimberly Schwarz, Marianne Sloss, Eduardo Torres, Tam Minh Tran, Shuichan Xu, JingJing Zhao, John Frederick Boylan
Abstract: Provided herein are formulations, processes, solid forms and methods of use relating to 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one.
Abstract: Provided herein are methods for treating or preventing chronic lymphocytic leukemia, comprising administering an effective amount of a Dihydropyrazino-Pyrazine Compound to a patient having chronic lymphocytic leukemia.
Type:
Grant
Filed:
April 16, 2014
Date of Patent:
November 29, 2016
Assignee:
Signal Pharmaceuticals, LLC
Inventors:
Heather Raymon, Shuichan Xu, Antonia Lopez-Girona, Toshiya Tsuji, Kristen Mae Hege
Abstract: Provided herein are methods for treating or preventing a solid tumor, non-Hodgkin lymphoma or multiple myeloma in a patient, comprising administering an effective amount of a TOR kinase inhibitor to a patient having a solid tumor, non-Hodgkin lymphoma or multiple myeloma.
Type:
Grant
Filed:
October 18, 2012
Date of Patent:
November 15, 2016
Assignee:
Signal Pharmaceuticals, LLC
Inventors:
Shuichan Xu, Kristen Mae Hege, Antonia Lopez-Girona, Heather Raymon, Rama K. Narla, Rajesh Chopra