Eisai R&d Management Co., Ltd.

Satoshi Nagao

Norio Murai

John JianShi Wang

Guo Zhu Zheng

Yoshihiko Kotake

Gregg F Keaney

Kazunobu Kira

Parcharee Tivitmahaisoon

Sudeep Prajapati

Baudouin Gerard

Xiang Liu

Masayuki Miyano

Regina Mikie Kanada Sonobe

Kenzo Arai

Nicholas C Gearhart

Keigo Tanaka

Atsushi Endo

Peter G Smith

Silvia Buonamici

Lihua Yu

Ermira Pazolli

Kian Huat Lim

Eunice Sun Park

Michael P Thomas

Betty Chan

Ming-Hong Hao

Dominic J Reynolds

Andrew Cook

Toshimi Okada

Shuji Shirotori

Arani Chanda

Jason T Lowe

James Palacino

Shelby Ellery

Yuzo Watanabe

Setsuo Funasaka

Isao Ohashi

Lisa A Marcaurelle

Tuoping Luo

Morgan Welzel O'shea

Yoshinobu Yamane

Yuki Karoji

Yusuke Nakatani

Regina Mikie Kanada Sonabe

Regina Kanada Sonobe

Sundeep Prajapati

The present disclosure provides novel pladienolide compounds, pharmaceutical compositions containing such compounds, and methods for using the compounds as therapeutic agents. These compounds may be useful in the treatment of cancers, particularly cancers in which agents that target the spliceosome and mutations therein are known to be useful. Also provided herein are methods of treating cancers by administering at least one compound disclosed herein and at least one additional therapy.

Certain pladienolide compounds and methods of use

The present disclosure provides a novel solid state form of pladienolide pyridine compounds having Formula I, compositions comprising at least one such solid state form, and methods of preparation and use and the same. The novel solid state form of pladienolide pyridine compounds may be useful in the treatment of cancer, such as, for example, cancers in which agents that target the spliceosome and mutations therein are known to be useful. 

Crystalline form of (2S,3S,6S,7R,10R,E)-7,10-dihydroxy-3,7-dimethyl-12-oxo-2-((R,2E,4E)-6-(piridin-2-yl)hepta-2,4-dien-2-yl)oxacyclododec-4-en-6-yl-4-methylpiperazine-1-carboxylate and methods of use thereof

The present invention provides novel pladienolide pyridine compounds, pharmaceutical compositions containing such compounds, and methods for using the compounds as therapeutic agents. These compounds may be useful in the treatment of cancer, particularly cancers in which agents that target the spliceosome and mutations therein are known to be useful.

Pladienolide pyridine compounds and methods of use

The present invention provides a novel compound having FGFR inhibitory activity or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same. Specifically, the present invention provides a compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof: wherein n represents 0 to 2; A represents an arylene group or a heteroarylene group; G represents a single bond, an oxygen atom or &#x2014;CH&#x2014;; E represents a nitrogen-containing non-aromatic heterocycle; Rrepresents an alkoxy group or the like; Rrepresents a hydrogen atom or the like; and Rrepresents a hydrogen atom, an alkyl group, an alkoxy group or the like, with the proviso that when E represents an azetidine ring and Ror Ris present on a nitrogen atom on the azetidine ring, the Ror Rdoes not represent a hydrogen atom.

Monocyclic pyridine derivative

Provided is a fluoroboron compound which is highly safe and stable and is capable of forming a cyclic ether-fused ring by the intramolecular alkoxymethylation reaction, or a salt thereof. The compound can be synthesized by the intramolecular alkoxymethylation reaction of a fluoroboron compound represented by the formula (I) or a salt thereof in the presence of a metal catalyst.  represents an aromatic ring; L represents a substituent such as a halogen atom; R represents a substituted or unsubstituted alkylene group having 1 or 2 carbon atoms; and M represents an alkali metal cation or the like, with the proviso that L and &#x2014;R&#x2014;OCHBFM are respectively located on contiguous carbon atoms on the aromatic ring, or in the case of a fused aromatic ring, on two carbon atoms adjacent to one carbon at the fused position).

Fluoroboron compound having aromatic ring or salt thereof, and method for producing compound having cyclic ether-fused aromatic ring using the same

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Tsukuba, Japan

Satoshi Nagao