公开(公告)号：US09388161B2

公开(公告)日：2016-07-12

申请号：US14546775

申请日：2014-11-18

Applicant: Forma Therapeutics, Inc.

Inventor： Kenneth W. Bair ,  Torsten Herbertz ,  Goss S. Kauffman ,  Katherine J. Kayser-Bricker ,  George P. Luke ,  Matthew W. Martin ,  David S. Millan ,  Shawn E. R. Schiller ,  Adam C. Talbot

IPC: C07D401/14 ,  A61K31/4709 ,  C07D401/04 ,  A61K31/5377 ,  A61K31/517 ,  C07D487/04 ,  A61K31/519 ,  A61K45/06

CPC classification number: C07D487/04 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/52 ,  A61K31/5377 ,  A61K45/06 ,  C07D215/20 ,  C07D215/48 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/10 ,  C07D417/14 ,  C07D471/04 ,  C07D473/28 ,  A61K2300/00

Abstract: The present invention relates to inhibitors of bromo and extra terminal (BET) bromodomains that are useful for the treatment of cancer, inflammatory diseases, diabetes, and obesity, having Formula I: wherein W, X, Y, Z, R1, R2, R5, and R8 are as described herein.

Abstract translation: 本发明涉及可用于治疗癌症，炎性疾病，糖尿病和肥胖症的溴和额外末端（BET）溴结构域的抑制剂，其具有式I：其中W，X，Y，Z，R 1，R 2，R 5 ，和R8如本文所述。

公开(公告)号：US20140163005A1

公开(公告)日：2014-06-12

申请号：US13949666

申请日：2013-07-24

Applicant: Forma Therapeutics, Inc.

Inventor： KRISHNA MURTHI ,  REBECCA CASAUBON ,  ARTHUR F. KLUGE ,  CHASE SMITH ,  JOACHIM VOGT

IPC: C07D471/04

CPC classification number: C07D471/04 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/551 ,  A61K45/06

Abstract: The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are kinase inhibitors, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.

公开(公告)号：US08232283B2

公开(公告)日：2012-07-31

申请号：US13105957

申请日：2011-05-12

Applicant: Andreas Schoop ,  Alexander Backes ,  Joachim Vogt ,  Lars Neumann ,  Jan Eickhoff ,  Stefan Hannus ,  Kerrin Hansen ,  Peter Amon ,  Igor Ivanov ,  Matthias Borgmann ,  Chase Smith ,  Arthur F. Kluge ,  Krishan Murthi ,  Rebecca Casaubon

Inventor： Andreas Schoop ,  Alexander Backes ,  Joachim Vogt ,  Lars Neumann ,  Jan Eickhoff ,  Stefan Hannus ,  Kerrin Hansen ,  Peter Amon ,  Igor Ivanov ,  Matthias Borgmann ,  Chase Smith ,  Arthur F. Kluge ,  Krishan Murthi ,  Rebecca Casaubon

IPC: C07D471/04 ,  A61K31/505 ,  A61P35/00

CPC classification number: C07D471/04

Abstract: The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are inhibitors or kinases such as Raf, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.

Abstract translation: 本发明提供吡啶并[2,3-d]嘧啶-7-酮的衍生物。 这些化合物是抑制剂或激酶如Raf，包括显示抗增殖活性的化合物，包括抗肿瘤细胞，并且可用于治疗包括癌症在内的疾病。

公开(公告)号：US20240148718A1

公开(公告)日：2024-05-09

申请号：US18220779

申请日：2023-07-11

Applicant: FORMA Therapeutics, Inc.

Inventor： Susan ASHWELL ,  Blythe THOMSON ,  Patrick F. KELLY ,  Alan COLLIS ,  Jeff DAVIS ,  Duncan WALKER ,  Wei LU

IPC: A61K31/4709 ,  A61K31/706 ,  A61P35/00 ,  A61P35/02

CPC classification number: A61K31/4709 ,  A61K31/706 ,  A61P35/00 ,  A61P35/02

Abstract: Patients diagnosed with a cancer harboring an IDH-1 mutation can be treated by the administration of a therapeutically effective amount of a pharmaceutical composition comprising Compound 1, a selective inhibitor of 2-HG production from mIDH-1 enzymes including the R132 mutations R132C, R132H, R132L, R132G, and R132S.

公开(公告)号：US20240016795A1

公开(公告)日：2024-01-18

申请号：US18371621

申请日：2023-09-22

Applicant: FORMA Therapeutics, Inc.

Inventor： Sylvie GUICHARD ,  Maureen CALIGIURI ,  Anna ERICSSON ,  Qunli XU ,  Hesham MOHAMED

IPC: A61K31/4745 ,  A61P35/00

CPC classification number: A61K31/4745 ,  A61P35/00

Abstract: Methods for treating certain androgen receptor-positive forms of cancer using inhibitors of the CREB binding protein bromodomain are disclosed. In some methods, the AR-positive forms of cancer may be breast cancer, including triple negative forms, hormone receptor positive forms, and HER2-positive forms. In other methods, the AR-positive forms of cancer may be prostate cancer, including metastatic castration resistant prostate cancer. In some embodiments, methods of treating prostate cancer comprise the step of administering to a patient in need thereof the compound (1R,3R)-3-[(7S)-2-[(R)-(5-fluoro-2-methoxyphenyl)(hydroxy)methyl]-6-(methoxycarbonyl)-7-methyl-3H,6H,7H,8H,9H-imidazo[4,5-f]quinolin-3-yl]cyclohexane-1-carboxylic acid, or a pharmaceutically acceptable salt thereof.

公开(公告)号：US11814386B2

公开(公告)日：2023-11-14

申请号：US18048079

申请日：2022-10-20

Applicant: FORMA Therapeutics, Inc.

Inventor： Alex J. Buckmelter ,  Justin Andrew Caravella ,  Hongbin Li ,  Matthew W. Martin ,  Steven Mischke ,  David James Richard ,  Angela V. West

IPC: C07D471/18 ,  C07D403/12 ,  C07D471/08 ,  C07D487/08 ,  C07D487/18 ,  C07D491/107

CPC classification number: C07D471/18 ,  C07D403/12 ,  C07D471/08 ,  C07D487/08 ,  C07D487/18 ,  C07D491/107

Abstract: The disclosure relates to USP30 Inhibitor Compounds, pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising same, and medical uses involving same.

公开(公告)号：US20230126252A1

公开(公告)日：2023-04-27

申请号：US18048079

申请日：2022-10-20

Applicant: FORMA Therapeutics, Inc.

Inventor： Alex J. Buckmelter ,  Justin Andrew Caravella ,  Hongbin Li ,  Matthew W. Martin ,  Steven Mischke ,  David James Richard ,  Angela V. West

IPC: C07D471/18 ,  C07D403/12 ,  C07D471/08 ,  C07D487/08 ,  C07D487/18 ,  C07D491/107

Abstract: The disclosure relates to USP30 Inhibitor Compounds, pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising same, and medical uses involving same.

公开(公告)号：US20230066088A1

公开(公告)日：2023-03-02

申请号：US17700027

申请日：2022-03-21

Applicant: FORMA Therapeutics, Inc.

Inventor： Patrick F. Kelly ,  Susan Ashwell ,  Blythe Thomson ,  Alan Collis ,  Jeff Davis ,  Duncan Walker ,  Wei Lu

IPC: A61K31/4709 ,  A61P35/00

Abstract: Patients diagnosed with a cancer harboring an IDH-1 mutation can be treated by the administration of a therapeutically effective amount of a pharmaceutical composition comprising Compound 1, a selective inhibitor of 2-HG production from mIDH-1 enzymes including the R132 mutations R132C, R132H, R132L, R132G, and R132S.

公开(公告)号：US20230065368A1

公开(公告)日：2023-03-02

申请号：US17277500

申请日：2019-09-19

Applicant: FORMA Therapeutics, Inc.

Inventor： Bruce FOLLOWS ,  Katherine J. KAYSER-BRICKER ,  Adam Charles TALBOT ,  Scot MENTE ,  Tatiana SHELEKHIN ,  Anna ERICSSON

IPC: C07D519/00 ,  A61P35/00 ,  C07D487/04

Abstract: The disclosure provides novel chemical compounds useful as inhibitors of ubiquitin specific peptidase 9X (USP9X). USP9X inhibiting compounds are useful in the treatment of disease and disorders associated with modulation of USP9X, such as cancer.

公开(公告)号：US11566013B1

公开(公告)日：2023-01-31

申请号：US16953112

申请日：2020-11-19

Applicant: FORMA Therapeutics, Inc.

Inventor： Jian Lin ,  George P. Luke ,  Madhu Mondal

IPC: C07D401/12 ,  A61K9/00 ,  A61K9/20 ,  A61K9/48 ,  A61K31/706

Abstract: This disclosure relates to compositions and methods for inhibiting mutant IDH1, useful in treatment of mIDH1 cancers including AML, as well as mIDH1-positive solid tumors such as glioma.