Kosan Biosciences Incorporated

Olema Pharmaceuticals, Inc.

University of Pennsylvania

Pfizer Corporation

Bristol-myers Squibb Compnay

Chiron Corporation

Aurigene Oncology Limited

David C Myles

Peter J Kushner

Zong-Qiang Tian

Cyrus L Harmon

Yaoquan Liu

Zhan Wang

Simon James Shaw

Daniel V Santi

Yandong Li

Brian R Hearn

Amos B Smith, Iii

Christopher Carreras

Hong Fu

Mark A Burlingame

Kurt Frederick Sundermann

Yong Li

Steven D Dong

C Richard Hutchinson

Robert Johnson

Yi-Qing Zhou

Li Feng

Daniel T Chu

Chaitan Khosla

Paul A Renhowe

Gary W Ashley

Robert G McDaniel

Kirk William Johnson

Leonard Katz

Susanta Samajdar

Yan Zhu

David Duhl

Rustum S Boyce

Zhi-Jie Ni

Li Tang

Yue Chen

Chandregowda Venkateshappa

Brian Scott Freeze

Tomoyasu Hirose

Leslie Carol Hodges Gallagher

Ignació Brouard Martin

Kedar Gautam Patel

Misty Piagentini

Effie Tozzo

Kalisankar Bera

David Yeghikyan

Reena Chawla

Richard Sun

Leslie Hodges Gallagher

Suraj Tatyasaheb Gore

Raymond A Ng

Hao Zheng

The present disclosure describes acylsulfonamide compounds of Formula (J), and pharmaceutically acceptable salts, compositions, methods, and uses thereof. Such compounds are believed to be therapeutically useful as KAT6A inhibitors particularly in the treatment and/or prevention of diseases and disorders mediated by KAT6A in a subject.

Acylsulfonamide KAT6A inhibitors

Provided herein are methods of administering estrogen receptor antagonists for use in treatment of cancer. In some embodiments, estrogen receptor antagonists provided herein are tetrahydro pyrido[3,4-b] indole compounds. In some embodiments, provided antagonists are complete estrogen receptor antagonists.

Regimens of estrogen receptor antagonists

The present disclosure provides tetrahydro-1H-pyrido[3,4-b]indole compounds or a pharmaceutically acceptable salt, solvate, hydrate, prodrug, stereoisomer, tautomer, rotamer, N-oxide and/or substituted derivative or, optionally in a pharmaceutical composition, for the modulation of disorders mediated by estrogen, or other disorders as more fully described herein.

Tetrahydro-1H-pyrido [3,4-b]indole anti-estrogenic drugs

Tetrahydro-1H-pyrido[3,4-b]indole anti-estrogenic drugs

Benzopyran compounds with strong anti-estrogenic activity and essentially no estrogenic activity are provided, which are OP-1038, which is 3-(4-hydroxyphenyl)-4-methyl-2-(4-{2-[(3R)-3-methylpyrrolidin-1-yl]ethoxy}phenyl)-2H-chromen-7-ol, and OP-1074, which is (2S)-3-(4-hydroxyphenyl)-4-methyl-2-(4-{2-[(3R)-3-methylpyrrolidin-1-yl]ethoxy}phenyl)-2H-chromen-7-ol. OP-1074 is a pure anti-estrogen when tested in the agonist mode and a complete anti-estrogen when tested in the antagonist mode. These compounds are useful for the treatment or prevention of a variety of conditions that are modulated through the estrogen receptor in mammals including humans.

Benzopyran compounds, compositions and uses thereof

6- and 7-substituted coumarin and related 6- and 7-substituted 1H-quinolin-2-one compounds, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the 7-substituted coumarin and related 7-substituted 1H-quinolin-2-one compounds mimic or exceed the high level of pharmacological activity of discodermolide. In other embodiments, their preparation involves more readily available materials, higher yield processes and/or simpler synthetic sequences. In yet other embodiments, the compounds of the invention represent structurally simpler, therapeutically active analogues of discodermolide than heretofore known and may be useful as microtubule stabilizers and, inter alia, for treating and/or preventing cancer and other diseases, disorders, and/or conditions mediated by the stabilization of microtubules.

Discodermolide analogues and methods of their use

Compounds according to formula I wherein m is 0 or 1;X is and R, R, RR, and Rare as defined herein, are useful as anti-infective agents.

Ketolide anti-infective compounds

The present invention is directed to compounds, compositions thereof, and the use of the compounds and compositions for the treatment and prevention of breast cancer. In one embodiment, the present invention relates to the use of a substituted triphenyl butene or prodrug thereof for the treatment of breast cancer in mono-therapy or in combination therapy, or for a reduction in the recurrence rate of previously-treated breast cancer.

Substituted triphenyl butenes

Leptomycin-type compounds according to formula I wherein R, R, R, R, R, R, R, R, and m are as defined herein, exhibit anti-tumor activity.

Leptomycin compounds

Compounds having a structure according to formula (I) where R, R, R, R, R, and Rare as defined herein, are useful as prokinetic agents.

Motilide compounds

Leptomycin-type compounds according to Formula I wherein R, R, R, R, R, R, R, R, and m are as defined herein, exhibit anti-tumor activity.

The invention relates to benzoquinone ansamycin analogs useful for the treatment of cancer and other diseases or conditions characterized by undesired cellular proliferation or hyperproliferation. Therapies involving the administration of such benzoquinone ansamycin analogs, optionally in combination with an inhibitor of an HSP90 client protein, are useful to treat cancer and non-cancerous disease conditions.

Benzoquinone ansamycins

Compounds and methods useful for the synthesis of (+)-discodermolide, a naturally occurring microtubule stabilizing agent useful as an anti-cancer agent.

Compounds useful for the synthesis of (+)-discodermolide and methods thereof

Growing community of inventors

Kensington, CA, United States of America

David C Myles