Publication number: 20200069656
Abstract: Disclosed are methods of treating hyperproliferative disorders such as cancer, methods of arresting the cell cycle in cancer cells, methods of inhibiting glutathione synthesis in cancer cells, and associated compounds for use and uses in medicaments. In certain embodiments, the methods, uses and compounds are provided with reference to compounds of the structural formula (I), in which X1, X2, Z1, Z2, the ring system denoted by “a”, R1, L1, L2, Q, L3, R3, L4, R4, L5, and R5 are as described herein. In certain embodiments, compounds disclosed herein are especially active against cancers having a mutant KRAS gene.
Type:
Application
Filed:
November 29, 2017
Publication date:
March 5, 2020
Inventors:
Arshad M. Siddiqui, Stephane Ciblat, Lea Constantineau-Forget, Chantal Grand-Maitre, Xiangyu Guo, Jr., Sanjay Srivastava, Gerald W. Shipps, Alan B. Cooper, Vibha Oza, Matthew W. Kostura, Michael Luther, Jedd Levine
Patent number: 10537558
Abstract: Disclosed are pyrazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure (I) and pharmaceutically acceptable salts and/V-oxides thereof, wherein X1, X2, Z1, Z2, the ring system denoted by “a”, R1, A1A, L1B, A1B, L1A, L2, Q, L3, R3, A4A, L4B, A4B, L4A, R4, L5, and R5 are as described herein. In certain embodiments, compounds disclosed herein disrupt the eIF4E/eiF4G interaction, and can be used to treat hyperproliferative disorder, a neurological disease or disorder, or autism.
Type:
Grant
Filed:
June 1, 2016
Date of Patent:
January 21, 2020
Assignee:
Bantam Pharmaceutical, LLC
Inventors:
M. Arshad Siddiqui, Stephane Ciblat, Martin Dery, Lea Constantineau-Forget, Chantal Grand-Maitre, Xiangyu Guo, Sanjay Srivastava, Gerald W. Shipps, Alan B. Cooper, Nicolas Bruneau-Latour, Vu Linh Ly
Patent number: 10519135
Abstract: The present invention provides novel compounds of Formula (I) and Formula (II) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of cyclin-dependent kinase 7 (CDK7), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.
Type:
Grant
Filed:
July 10, 2018
Date of Patent:
December 31, 2019
Assignee:
Syros Pharmaceuticals, Inc.
Inventors:
Kevin Sprott, Jason J. Marineau, Darby Schmidt, Michael Bradley, Stephane Ciblat, M. Arshad Siddiqui, Anzhelika Kabro, Melissa Leblanc, Serge Leger, Stephanie Roy, Dana K. Winter, Tom Miller, Amy Ripka, Dansu Li
Publication number: 20190345152
Abstract: Disclosed are compounds useful, for example, in methods of treating hyperproliferative disorders such as cancer, methods of arresting the cell cycle in cancer cells, methods of inhibiting glutathione synthesis in cancer cells, and associated compounds for use and uses in medicaments. In certain embodiments, the methods, uses and compounds are provided with reference to compounds of the structural formulae (Ia), (Ib), (Ic), (Id) and (Ie), in which R1, L1, L2, Q, L3, R3, L4, R4, L5, and R5 are as described herein. In certain embodiments, compounds disclosed herein are especially active against cancers having a mutant KRAS gene.
Type:
Application
Filed:
November 29, 2017
Publication date:
November 14, 2019
Inventors:
Arshad M. Siddiqui, Stephane Ciblat, Martin Dery, Lea Constantineau-Forget, Chantal Grand-Maitre, Nicolas Bruneau-Latour, Gerald W. Shipps, Alan B. Cooper, Vibha Oza, Matthew W. Kostura, Michael Luther, Jedd Levine
Publication number: 20190292167
Abstract: The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of cyclin-dependent kinase 7 (CDK7), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.
Type:
Application
Filed:
December 21, 2018
Publication date:
September 26, 2019
Inventors:
Stephane Ciblat, Patrick Deroy, Melissa Leblanc, Jason J. Marineau, Joel Moore, Stephanie Roy, M. Arshad Siddiqui, Kevin Sprott, Dana K. Winter, Anzhelika Kabro, Serge Leger, Tom Miller, Darby Schmidt, Michael Bradley
Publication number: 20190241541
Abstract: The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g., cyclin-dependent kinase 7 (CDK7)), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.
Type:
Application
Filed:
December 5, 2018
Publication date:
August 8, 2019
Inventors:
Stephane Ciblat, Patrick Deroy, Nathanael Gray, Melissa Leblanc, Jason J. Marineau, Joel Moore, Kevin Sprott, Tinghu Zhang, M. Arshad Siddiqui, Anzhelika Kabro, Serge Leger, Stephanie Roy, Darby Schmidt, Dana K. Winter, Michael Bradley, Tom Miller
Patent number: 10308648
Abstract: The present invention provides novel compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of cyclin-dependent kinase (e.g., CDK7), and therefore induce cellular apoptosis and/or inhibit transcription in the subject.
Type:
Grant
Filed:
October 15, 2015
Date of Patent:
June 4, 2019
Assignee:
Syros Pharmaceuticals, Inc.
Inventors:
Stephane Ciblat, Anzhelika Kabro, Melissa Leblanc, Serge Leger, Jason J. Marineau, Tom Miller, Stephanie Roy, Darby Schmidt, Arshad M. Siddiqui, Kevin Sprott, Dana K. Winter, Amy Ripka, Dansu Li, Guoli Zhang
Publication number: 20190048019
Abstract: The present invention provides novel compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases, e.g., cancers (e.g., breast cancer, prostate cancer, lymphoma, lung cancer, pancreatic cancer, ovarian cancer, neuroblastoma, or colorectal cancer), benign neoplasms, angiogenesis, inflammatory diseases, fibrosis (e.g., polycystic kidney disease), autoinflammatory diseases, and autoimmune diseases in a subject.
Type:
Application
Filed:
September 8, 2017
Publication date:
February 14, 2019
Inventors:
Jason J. Marineau, Kevin Sprott, Stephane Ciblat, Christopher Roberts, Yi Zhang, Francis Beaumier, Luce Lépissier, Boubacar Sow, Peter B. Rahl, Robin Larouche-Gauther, Lauren Berstler
Publication number: 20190031642
Abstract: The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, lymphoma, melanoma, multiple myeloma, breast cancer, Ewing's sarcoma, osteosarcoma, brain cancer, neuroblastoma, lung cancer), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g.
Type:
Application
Filed:
August 1, 2018
Publication date:
January 31, 2019
Inventors:
Nathanael Gray, Tinghu Zhang, Stephane Ciblat, Melissa Leblanc, Jason J. Marineau, Joel Moore, Kevin Sprott, M. Arshad Siddiqui, Anzhelika Kabro, Tom Miller, Stephanie Roy, Darby Schmidt, Dana K. Winter, Michael Bradley
Publication number: 20180354972
Abstract: The present invention provides novel compounds of Formulas (I) and (II) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases, e.g., cancers (e.g., breast cancer, prostate cancer, lymphoma, lung cancer, pancreatic cancer, ovarian cancer, neuroblastoma, or colorectal cancer), benign neoplasms, angio genesis, inflammatory diseases, fibrosis (e.g., polycystic kidney disease), autoinflammatory diseases, and autoimmune diseases in a subject.
Type:
Application
Filed:
June 3, 2016
Publication date:
December 13, 2018
Inventors:
Jason J. Marineau, Peter B. Rahl, Kevin Sprott, Stephane Ciblat, Boubacar Sow, Robin Larouche-Gauthier, Lauren Berstler, Christopher Roberts, Zhang Yi, Francis Beaumier, Luce Lépissier
Publication number: 20180311218
Abstract: Disclosed are pyrazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure (I) and pharmaceutically acceptable salts and/V-oxides thereof, wherein X1, X2, Z1, Z2, the ring system denoted by “a”, R1, A1A, L1B, A1B, L1A, L2, Q, L3, R3, A4A, L4B, A4B, L4A, R4, L5, and R5 are as described herein. In certain embodiments, compounds disclosed herein disrupt the elF4E/eiF4G interaction, and can be used to treat hyperproliferative disorder, a neurological disease or disorder, or autism.
Type:
Application
Filed:
June 1, 2016
Publication date:
November 1, 2018
Inventors:
M. Arshad Siddiqui, Stephane Ciblat, Martin Dery, Lea Constantineau-Forget, Chantal Grand-Maitre, Xiangyu Guo, Sanjay Srivastava, Gerald W. Shipps, Alan B. Cooper, Nicolas Bruneau-Latour, Vu Linh Ly