Patent number: 11192887
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:
Grant
Filed:
November 29, 2017
Date of Patent:
December 7, 2021
Assignee:
Bantam Pharmaceutical, LLC
Inventors:
M. Arshad Siddiqui, Stephane Ciblat, Martin Dery, Lea Constantineau-Forget, Chantal Grand-Maitre, Nicolas Bruneau-Latour, Gerald W. Shipps, Alan B. Cooper, Vibha Oza, Matthew J. Kostura, Michael Luther, Jedd Levine
Patent number: 11124527
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:
Grant
Filed:
June 3, 2016
Date of Patent:
September 21, 2021
Assignee:
Syros Pharmaceuticals, Inc.
Inventors:
Jason J. Marineau, Peter B. Rahl, Kevin Sprott, Stephane Ciblat, Boubacar Sow, Robin Larouche-Gauthier, Lauren Berstler, Christopher Roberts, Yi Zhang, Francis Beaumier, Luce Lépissier
Publication number: 20210221820
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:
November 30, 2020
Publication date:
July 22, 2021
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: 20210188833
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., 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:
June 26, 2020
Publication date:
June 24, 2021
Inventors:
Jason J. Marineau, Peter B. Rahl, Kevin Sprott, Stephane Ciblat, Boubacar Sow, Robin Larouche-Gauthier, Lauren Berstler, Christopher Roberts, Yi Zhang, Francis Beaumier, Luce Lépissier
Patent number: 11040957
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:
Grant
Filed:
December 5, 2018
Date of Patent:
June 22, 2021
Assignees:
Dana-Farber Cancer Institute, Inc., Syros Pharmaceuticals, Inc.
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: 10906889
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:
Grant
Filed:
August 1, 2018
Date of Patent:
February 2, 2021
Assignee:
Dana-Farber Cancer Institute, Inc.
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
Patent number: 10865206
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:
May 15, 2019
Date of Patent:
December 15, 2020
Assignee:
Syros Pharmaceuticals, Inc.
Inventors:
Stephane Ciblat, Anzhelika Kabro, Melissa Leblanc, Serge Leger, Jason J. Marineau, Tom Miller, Stephanie Roy, Darby Schmidt, M. Arshad Siddiqui, Kevin Sprott, Dana K. Winter, Amy Ripka, Dansu Li, Guoli Zhang
Patent number: 10787444
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., 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:
Grant
Filed:
June 5, 2016
Date of Patent:
September 29, 2020
Assignee:
Syros Pharmaceuticals, Inc.
Inventors:
Jason J. Marineau, Peter B. Rahl, Kevin Sprott, Stephane Ciblat, Boubacar Sow, Robin Larouche-Gauthier, Lauren Berstler, Christopher Roberts, Yi Zhang, Francis Beaumier, Luce Lépissier
Publication number: 20200261424
Abstract: Disclosed are pyrazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure and pharmaceutically acceptable salts and N-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:
Application
Filed:
January 21, 2020
Publication date:
August 20, 2020
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