Eisai R&d Management Co., Ltd.

Norio Murai

Keigo Tanaka

Shuji Shirotori

Satoshi Inoue

Masayuki Matsukura

Shinya Abe

Kazutaka Nakamoto

Satoshi Nagao

John JianShi Wang

Guo Zhu Zheng

Yoshihiko Kotake

Gregg F Keaney

Kazunobu Kira

Parcharee Tivitmahaisoon

Sudeep Prajapati

Baudouin Gerard

Xiang Liu

Masayuki Miyano

Kenzo Arai

Nicholas C Gearhart

Regina Mikie Kanada Sonobe

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

Marta Nevalainen

Hiroshi Azuma

Arani Chanda

Shinsuke Hirota

Jason T Lowe

James Palacino

Yoshiaki Ohashi

Shuichi Suzuki

Shelby Ellery

Daisuke Iida

Yuzo Watanabe

Takashi Fukuyama

Daisuke Ito

Wataru Itano

Lisa A Marcaurelle

Yosuke Kaburagi

Morgan Welzel O'shea

Tuoping Luo

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

A compound represented by the formula (I) or a salt thereof: wherein a ring Z is a 5 to 6-membered heteroaromatic ring having one or two heteroatoms in the ring; Xis a hydrogen atom, a hydroxy group, a hydroxy Calkyl group, &#x2014;B(OH), a boronate ester group, a cyclic boronate ester group, a boranyl group, a cyclic boranyl group, &#x2014;BFM, &#x2014;Sn(R)(R)(R), a leaving group, a carboxy group, a formyl group, or &#x2014;NRR; and Xis a hydrogen atom or &#x2014;COR.

Hetero-fused cyclic compound

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

An object of the present invention is to provide an antifungal agent which has excellent antifungal effects and is superior in terms of its physical properties, safety and metabolic stability. According to the present invention, there is disclosed a compound represented by the following formula (I), or a salt thereof: wherein R, R, X, Y, ring A, Z, Rand Rare as defined in the specification.

Heterocycles substituted pyridine derivatives and antifungal agent containing thereof

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

The present invention provides an antifungal agent that has excellent antifungal action, and is also excellent in terms of its properties, safety, and metabolic stability. The present invention discloses a compound represented by the following formula I or a salt thereof, and an antifungal agent comprising the compound or the salt: wherein Rrepresents a hydrogen atom, a halogen atom, an amino group, a Calkyl group, a Calkoxy group, or a C-alkoxy-C-alkyl group; Rrepresents a hydrogen atom or an amino group; X, Y, Z, and W independently represent a nitrogen atom, an oxygen atom, a sulfur atom, or &#x2014;CH&#x2014;, provided that at least two among X, Y, and W are nitrogen atoms; the ring A represents a 5- or 6-membered heteroaryl ring or a benzene ring; Q represents a methylene group, an oxygen atom, &#x2014;CHO&#x2014;, &#x2014;OCH&#x2014;, &#x2014;NH&#x2014;, &#x2014;NHCH&#x2014;, or &#x2014;CHNH&#x2014;; and Rrepresents a Calkyl group, a Ccycloalkyl group, a Caryl group, or a 5- or 6-membered heteroaryl group, each of which may have one or two substituents.

Pyridine derivative substituted by heteroaryl ring, and antifungal agent comprising the same

An object of the present invention is to provide an antifungal agent which has excellent antifungal effects and is superior in terms of its physical properties, safety and metabolic stability. According to the present invention, there is disclosed a compound represented by the following formula (I), or a salt thereof: wherein Rrepresents a hydrogen atom, a halogen atom, an amino group, a Calkyl group, a Calkoxy group or a Calkoxy Calkyl group; Rrepresents a hydrogen atom, a Calkyl group, an amino group or a di Calkylamino group; one of X and Y is a nitrogen atom while the other is a nitrogen atom or an oxygen atom; ring A represents a 5- or 6-member heteroaryl ring or a benzene ring which may have a halogen atom, or 1 or 2 Calkyl groups; Z represents a single bond, a methylene group, an ethylene group, an oxygen atom, a sulfur atom, &#x2014;CHO&#x2014;, &#x2014;OCH&#x2014;, &#x2014;NH&#x2014;, &#x2014;CHNH&#x2014;, &#x2014;NHCH&#x2014;, &#x2014;CHS&#x2014;, or &#x2014;SCH&#x2014;; Rrepresents a hydrogen atom, a halogen atom, a Calkyl group, a Ccycloalkyl group, a Caryl group, a 5- or 6-member heteroaryl group, or 5- or 6-member non-aromatic heterocyclic group which may have 1 or 2 substituents; and Rrepresents a hydrogen atom or a halogen atom.

The present invention provides compounds which are useful as safe substitutes for the organotin reagent used in coupling reaction for the oxymethylation of aromatic rings, such as alkoxymethylation or hydroxymethylation, with a palladium catalyst and which can dispense with chromatographic purification with silica gel in the production and are suitable for mass production; and compounds applicable even to the oxymethylation of aromatic ring substrates which do not permit coupling reaction by conventional technique or have low reactivity.

Oxymethyl boron compounds

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Tsukuba, Japan

Norio Murai