公开(公告)号：US11040957B2

公开(公告)日：2021-06-22

申请号：US16210264

申请日：2018-12-05

Applicant: Syros Pharmaceuticals, Inc. ,  Dana-Farber Cancer Institute, Inc.

Inventor： 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

IPC: C07D401/14 ,  A61K31/506 ,  A61K45/06

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.

公开(公告)号：US20230062491A1

公开(公告)日：2023-03-02

申请号：US17667288

申请日：2022-02-08

Applicant: Syros Pharmaceuticals, Inc.

Inventor： Jason J. Marineau ,  Robert Zahler ,  Stephane Ciblat ,  Dana K. Winter ,  Anzhelika Kabro ,  Stephanie Roy ,  Darby Schmidt ,  Claudio Chuaqui ,  Goran Malojcic ,  Henri Piras ,  Kenneth Matthew Whitmore ,  Kate-Lyn Lund ,  William Sinko ,  Kevin Sprott

IPC: C07F9/6558 ,  C07D417/14 ,  C07D471/08 ,  C07D413/14 ,  C07D401/14 ,  C07D471/04

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.

公开(公告)号：US20190337940A1

公开(公告)日：2019-11-07

申请号：US16412726

申请日：2019-05-15

Applicant: Syros Pharmaceuticals, Inc.

Inventor： 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

IPC: C07D471/04 ,  C07D401/14 ,  C07D401/04 ,  C07D403/04

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.

公开(公告)号：US20160264552A1

公开(公告)日：2016-09-15

申请号：US15030265

申请日：2014-10-17

Applicant: SYROS PHARMACEUTICALS, INC.

Inventor： 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

IPC: C07D401/14 ,  A61K45/06 ,  C07D417/14 ,  C07D403/04 ,  C07D413/14 ,  A61K31/5377 ,  C07D401/04 ,  C07D417/04 ,  C07D451/04 ,  C07D403/14 ,  A61K31/635 ,  A61K31/506 ,  C07D413/04

CPC classification number: C07D401/14 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/635 ,  A61K45/06 ,  C07D401/04 ,  C07D403/04 ,  C07D403/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14 ,  C07D451/04

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 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. (I)

公开(公告)号：US20160264551A1

公开(公告)日：2016-09-15

申请号：US15030249

申请日：2014-10-17

Applicant: SYROS PHARMACEUTICALS, INC. ,  DANA-FARBER CANCER INSTITUTE, INC.

Inventor： Stephane Ciblat ,  Patrick Deroy ,  Nathanael Gray ,  Melissa Leblanc ,  Jason J. Marineau ,  Joel Moore ,  Kevin Sprott ,  Tinghu Zhang ,  M. Arshad Siddiqui ,  Anzhelika Kabro ,  Serge Leger ,  Tom Miller ,  Stephanie Roy ,  Darby Schmidt ,  Dana K. Winter ,  Michael Bradley

IPC: C07D401/14 ,  A61K31/506 ,  A61K45/06

CPC classification number: C07D401/14 ,  A61K31/506 ,  A61K45/06

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, in duce cellular apoptosis and/or inhibit transcription in the subject.

Abstract translation: 本发明提供新的式（I）化合物及其药学上可接受的盐，溶剂合物，水合物，互变异构体，立体异构体，同位素标记的衍生物及其组合物。 还提供了涉及用于治疗或预防受试者的增殖性疾病（例如，癌症（例如白血病，黑素瘤，多发性骨髓瘤），良性肿瘤，血管生成，炎性疾病，自身炎性疾病和自身免疫性疾病）的化合物或组合物的方法和试剂盒 。 使用本发明的化合物或组合物治疗具有增殖性疾病的受试者可以抑制激酶例如细胞周期蛋白依赖性激酶（CDK）（例如细胞周期蛋白依赖性激酶7（CDK7））的异常活性，因此 ，诱导受试者的细胞凋亡和/或抑制转录。

公开(公告)号：US20190292167A1

公开(公告)日：2019-09-26

申请号：US16230353

申请日：2018-12-21

Applicant: Syros Pharmaceuticals, Inc.

Inventor： 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

IPC: C07D401/14 ,  C07D451/04 ,  C07D417/14 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/635 ,  C07D413/14 ,  C07D417/04 ,  C07D413/04 ,  C07D403/14 ,  C07D403/04 ,  C07D401/04 ,  A61K45/06

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.

公开(公告)号：US10059690B2

公开(公告)日：2018-08-28

申请号：US15799661

申请日：2017-10-31

Applicant: Syros Pharmaceuticals, Inc.

Inventor： Stephane Ciblat ,  Kevin Sprott ,  Dana K. Winter ,  Amy Ripka ,  Dansu Li ,  Michael Bradley ,  Anzhelika Kabro ,  Melissa Leblanc ,  Serge Leger ,  Jason J. Marineau ,  Tom Miller ,  Stephanie Roy ,  Darby Schmidt ,  M. Arshad Siddiqui

IPC: A01N43/54 ,  A61K31/505 ,  C07D401/14

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.

公开(公告)号：US20170183355A1

公开(公告)日：2017-06-29

申请号：US15301815

申请日：2015-04-03

Applicant: SYROS PHARMACEUTICALS, INC.

Inventor： 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

IPC: C07D487/10 ,  A61K31/506 ,  C07D403/04 ,  C07D401/14 ,  C07D471/10 ,  C07D487/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  A61K31/5377 ,  C07D451/04 ,  A61K31/551 ,  C07D405/04 ,  C07D409/04 ,  C07D417/04 ,  A61K45/06 ,  C07D403/14

CPC classification number: C07D401/14 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/551 ,  A61K45/06 ,  C07D403/04 ,  C07D403/14 ,  C07D405/04 ,  C07D409/04 ,  C07D411/14 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14 ,  C07D451/04 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C07D498/10

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.

公开(公告)号：US20240360165A1

公开(公告)日：2024-10-31

申请号：US18635402

申请日：2024-04-15

Applicant: Syros Pharmaceuticals, Inc.

Inventor： Jason J. MARINEAU ,  Robert Zahler ,  Stephane Ciblat ,  Dana K. Winter ,  Anzhelika Kabro ,  Stephanie Roy ,  Darby Schmidt ,  Claudio Chuaqui ,  Goran Malojcic ,  Henri Piras ,  Kenneth Matthew Whitmore ,  Kate-Lyn Lund ,  William Sinko ,  Kevin Sprott

IPC: C07F9/6558 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08

CPC classification number: C07F9/65583 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08

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.

公开(公告)号：US20210061803A1

公开(公告)日：2021-03-04

申请号：US17097913

申请日：2020-11-13

Applicant: Syros Pharmaceuticals, Inc.

Inventor： 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

IPC: C07D471/04 ,  C07D403/04 ,  C07D401/04 ,  C07D401/14

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.