Celgene Quanticel Research, Inc.

Takeda Pharmaceutical Company Limited

Agouron Pharmaceuticals, Inc.

Takeda San Diego, Inc.

Quanticel Pharmaceuticals, Inc.

Other

Astrazeneca Ab

Michael Brennan Wallace

Jeffrey Alan Stafford

James Marvin Veal

Toufike Kanouni

Young K Chen

Zhe Nie

Amogh Boloor

Stephen L Gwaltney

Zhiyuan Zhang

Jun Feng

Qing Dong

Siegfried Heinz Reich

Stephen W Kaldor

Nicholas Scorah

Theodore Otto Johnson, Jr

Bheema Rao Paraselli

Min Teng

Robert Steven Kania

Cynthia Louise Palmer

Michael D Varney

Steven Lee Bender

Michael Raymond Collins

Juan Manuel Betancort

Allen Borchardt

Ted Michael Bleckman

Susan Elizabeth Kephart

Stephan James Cripps

Hiep The Luu

William Henry Romines, Iii

Ye Hua

Michael David Johnson

Christine Thomas

John David Lawson

Lynnie Lin Trzoss

Xiao-Yi Xiao

Edcon Chang

David J Hosfield

Anna Maria Tempczyk-Russell

Anna Marie Tempczyk-Russell

Zhlyuan Zhang

Laurence Edward Burgess

Ellen Ruth Laird

Jason W Brown

Christopher Ronald Smith

Xiaolun Wang

Sheldon Cao

Andrew John Jennings

Jerome C Bressi

Michael John Bennett

Scott D Cowen

Yi Yang

Lily Kwok

Mallareddy Komandla

Wesley Kwan Mung Chong

Mark E Adams

Shao Song Chu

Rohit Kumar Duvadie

Shaosong Chu

Philip Erickson

Lin Li

Larry Andrew Alegria

Wolfgang Reinhard Ludwig Notz

Marc E Navre

Hasanthi Wijesekera

Sanjib Das

Toufiko Kanounl

Stephen S Gonzales

Xiaodong Wang

Christopher L Caster

Yiqin Wu

Feng Zhou

Xianchang Gong

The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyrido[3,4-d]pyrimidin-4-one derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase. 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.

Histone demethylase inhibitors

The present embodiments relate to substituted heterocyclic derivative therapeutic 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 diseases mediated by aberrant cell signalling, such as inflammatory disorders, cancer and neoplastic disease. Particular compounds described herein exhibit selective inhibitory activity against CBP compared with BRD4.

Therapeutic compounds

The present embodiments provide for substituted triazolylpyridine derivative compounds, and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for modulating the activity of histone demethylase enzymes. Additionally, the subject compounds and compositions are useful for the treatment of cancer or other neoplastic diseases, or maladies associated with abnormal histone demethylase activity. Accordingly, the substituted triazolylpyridine derivative compounds described herein are useful in methods and medicaments for treating cancer.

The present disclosure relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyridine derivative compounds, and compositions (including pharmaceutical compositions) that include these compounds. The subject compounds and compositions are useful for inhibition of at least one histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer or neoplastic disease, such as prostate cancer, breast cancer, bladder cancer, lung cancer, melanoma, retinoblastoma, or multiple endocrine neoplasia type 1.

The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted amidopyridine or amidopyridazine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. 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.

Growing community of inventors

San Diego, CA, United States of America

Michael Brennan Wallace