公开(公告)号：US20220153706A1

公开(公告)日：2022-05-19

申请号：US17356389

申请日：2021-06-23

Applicant: CELGENE QUANTICEL RESEARCH, INC.

Inventor： Young K. Chen ,  Toufike Kanouni ,  Stephen W. Kaldor ,  Jeffrey Alan Stafford ,  James Marvin Veal

IPC: C07D239/47 ,  A61K31/4545 ,  A61K31/513 ,  C07D401/14 ,  C07D405/14 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D401/04 ,  C07D471/10 ,  C07B59/00 ,  C07D239/36 ,  C07D403/14 ,  A61K31/5377 ,  A61K31/551

Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer.

公开(公告)号：US10703739B2

公开(公告)日：2020-07-07

申请号：US16436541

申请日：2019-06-10

Applicant: Celgene Quanticel Research, Inc.

Inventor： Young K. Chen ,  Toufike Kanouni ,  Stephen W. Kaldor ,  Jeffrey Alan Stafford ,  James Marvin Veal ,  Paula Alessandra Tavares-Greco ,  Matthew Michael Kreilein

IPC: C07D239/36 ,  C07D401/04 ,  A61K31/4545 ,  A61K31/506 ,  A61P35/00

Abstract: Described herein are amorphous and crystalline forms of pharmaceutically acceptable salts of the lysine specific demethylase-1 inhibitor 4-[2-(4-aminopiperidin-1-yl)-5-(3-fluoro-4-methoxy-phenyl)-1-methyl-6-oxo-1,6-dihydropyrimidin-4-yl]-2-fluorobenzonitrile. Also described are pharmaceutical compositions suitable for administration to a mammal that include the lysine specific demethylase-1 inhibitor, and methods of using the lysine specific demethylase-1 inhibitor for treating diseases or conditions that are associated with lysine specific demethylase-1 activity.

公开(公告)号：US10131664B2

公开(公告)日：2018-11-20

申请号：US15900737

申请日：2018-02-20

Applicant: Celgene Quanticel Research, Inc.

Inventor： Young K. Chen ,  Toufike Kanouni ,  Stephen W. Kaldor ,  Jeffrey Alan Stafford ,  James Marvin Veal

IPC: C07D471/04 ,  C07D401/14 ,  C07D401/04 ,  C07D403/12 ,  C07D405/14 ,  C07D413/14 ,  C07D401/12 ,  C07D403/14 ,  C07D413/12 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C07D491/107 ,  C07D498/18 ,  C07D519/00 ,  C07D401/06 ,  C07D498/08

Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.

公开(公告)号：US20170349555A1

公开(公告)日：2017-12-07

申请号：US15684886

申请日：2017-08-23

Applicant: CELGENE QUANTICEL RESEARCH, INC.

Inventor： Young K. Chen ,  Toufike Kanouni ,  Stephen W. Kaldor ,  Jeffrey Alan Stafford ,  James Marvin Veal

IPC: C07D239/47 ,  C07D405/14 ,  C07D403/14 ,  C07D403/12 ,  C07D403/04 ,  A61K31/513 ,  A61K31/4545 ,  C07D401/04 ,  C07D239/36 ,  C07D401/12 ,  C07B59/00 ,  C07D471/10 ,  C07D401/14

CPC classification number: A61K31/513 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/551 ,  C07B59/002 ,  C07B2200/05 ,  C07D239/36 ,  C07D239/47 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D471/10

Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer.

公开(公告)号：US20160304516A1

公开(公告)日：2016-10-20

申请号：US15103024

申请日：2014-12-10

Applicant: CELGENE QUANTICEL RESEARCH, INC.

Inventor： Young K. Chen ,  Toufike Kanouni ,  Stephen W. Kaldor ,  Jeffrey Alan Stafford ,  James Marvin Veal

IPC: C07D471/04 ,  C07D487/04 ,  C07D401/12 ,  C07D413/12 ,  C07D487/10 ,  C07D498/08 ,  C07D401/14 ,  C07D401/04 ,  C07D405/14 ,  C07D471/10 ,  C07D471/08 ,  C07D519/00 ,  C07D403/14 ,  C07D491/107 ,  C07D401/06 ,  C07D403/12

CPC classification number: C07D471/04 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C07D491/107 ,  C07D498/08 ,  C07D498/18 ,  C07D519/00

Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.

公开(公告)号：US10807982B2

公开(公告)日：2020-10-20

申请号：US16673839

申请日：2019-11-04

Applicant: CELGENE QUANTICEL RESEARCH, INC.

Inventor： Michael John Bennett ,  Juan Manual Betancort ,  Amogh Boloor ,  Stephen W. Kaldor ,  Jeffrey Alan Stafford ,  James M. Veal

IPC: C07D473/34 ,  C07D491/04 ,  C07D401/14 ,  C07D413/14 ,  C07D401/04 ,  C07D405/04 ,  C07D413/04 ,  C07D417/04 ,  C07D471/04 ,  C07D471/06 ,  C07D498/04

Abstract: The present invention relates to substituted heterocyclic derivative compounds, compositions comprising said compounds, and the use of said compounds and compositions for epigenetic regulation by inhibition of bromodomain-mediated recognition of acetyl lysine regions of proteins, such as histones. Said compositions and methods are useful for the treatment of cancer and neoplastic disease.

公开(公告)号：US10316016B2

公开(公告)日：2019-06-11

申请号：US16032002

申请日：2018-07-10

Applicant: CELGENE QUANTICEL RESEARCH, INC.

Inventor： Young K. Chen ,  Toufike Kanouni ,  Stephen W. Kaldor ,  Jeffrey Alan Stafford ,  James Marvin Veal ,  Paula Alessandra Tavares-Greco ,  Matthew Michael Kreilein

IPC: C07D401/04 ,  C07D239/36 ,  A61K31/4545 ,  A61K31/506

Abstract: Described herein are amorphous and crystalline forms of pharmaceutically acceptable salts of the lysine specific demethylase-1 inhibitor 4-[2-(4-aminopiperidin-1-yl)-5-(3-fluoro-4-methoxy-phenyl)-1-methyl-6-oxo-1,6-dihydropyrimidin-4-yl]-2-fluorobenzonitrile. Also described are pharmaceutical compositions suitable for administration to a mammal that include the lysine specific demethylase-1 inhibitor, and methods of using the lysine specific demethylase-1 inhibitor for treating diseases or conditions that are associated with lysine specific demethylase-1 activity.

公开(公告)号：US20190055242A1

公开(公告)日：2019-02-21

申请号：US16166832

申请日：2018-10-22

Applicant: CELGENE QUANTICEL RESEARCH, INC.

Inventor： Young K. Chen ,  Toufike Kanouni ,  Stephen W. Kaldor ,  Jeffrey Alan Stafford ,  James Marvin Veal

IPC: C07D471/04 ,  C07D403/14 ,  C07D498/18 ,  C07D401/04 ,  C07D491/107 ,  C07D401/14 ,  C07D519/00 ,  C07D403/12 ,  C07D413/12 ,  C07D401/06 ,  C07D401/12 ,  C07D405/14 ,  C07D471/08 ,  C07D487/04 ,  C07D413/14 ,  C07D498/08 ,  C07D487/10 ,  C07D471/10

CPC classification number: C07D471/04 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C07D491/107 ,  C07D498/08 ,  C07D498/18 ,  C07D519/00

Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.

公开(公告)号：US10207999B2

公开(公告)日：2019-02-19

申请号：US15684886

申请日：2017-08-23

Applicant: CELGENE QUANTICEL RESEARCH, INC.

Inventor： Young K. Chen ,  Toufike Kanouni ,  Stephen W. Kaldor ,  Jeffrey Alan Stafford ,  James Marvin Veal

IPC: C07D401/04 ,  C07D401/14 ,  C07D239/47 ,  C07D405/14 ,  C07D403/04 ,  A61K31/4545 ,  A61K31/513 ,  C07D401/12 ,  C07D471/10 ,  C07B59/00 ,  C07D239/36 ,  C07D403/14 ,  C07D403/12

Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer.

公开(公告)号：US10023543B2

公开(公告)日：2018-07-17

申请号：US15687251

申请日：2017-08-25

Applicant: CELGENE QUANTICEL RESEARCH, INC.

Inventor： Young K. Chen ,  Toufike Kanouni ,  Stephen W. Kaldor ,  Jeffrey Alan Stafford ,  James Marvin Veal

IPC: C07D403/04 ,  C07D403/14 ,  C07D239/47 ,  C07D405/14 ,  C07D401/04 ,  C07D401/14 ,  A61K31/513 ,  A61K31/4545 ,  C07D403/12 ,  C07D239/36 ,  C07D471/10 ,  C07D401/12 ,  C07B59/00

Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer.