Eisai Company, Limited

Eisai R&d Management Co., Ltd.

Mercian Corporation

Merican Corporation

Yoshihiko Kotake

Jun Niijima

Norihiro Ueda

Kyosuke Kitoh

Takeshi Nagasu

Nozomu Koyanagi

Hiroshi Yoshino

Kentaro Yoshimatsu

Tatsuo Watanabe

Toshimi Okada

Mitsuo Nagai

Takashi Nakashima

Kappei Tsukahara

Toshio Tsuchida

Hiroyuki Sugumi

Makoto Asada

Atsumi Iijima

Regina Mikie Kanada

Toru Haneda

Yoshio Fukuda

Takashi Sakai

Naoki Asai

John JianShi Wang

Guo Zhu Zheng

Gregg F Keaney

Hitoshi Harada

Kazunobu Kira

Parcharee Tivitmahaisoon

Sudeep Prajapati

Norio Murai

Masashi Yoshida

Baudouin Gerard

Tomohiro Sameshima

Xiang Liu

Toshimitsu Uenaka

Susumu Takeda

Satoshi Nagao

Masahiro Yasuda

Naoko Tsukahara

Masayuki Miyano

Kenzo Arai

Nicholas C Gearhart

Regina Mikie Kanada Sonobe

Masahi Yoshida

Kiyoshi Okamoto

Shuhei Miyazawa

Hiroaki Nomura

Masato Ueda

Atsushi Endo

Osamu Asano

Satoshi Yamamoto

Peter G Smith

Silvia Buonamici

Nobuyuki Yasuda

Kazuyuki Dobashi

Lihua Yu

Yoshiharu Mizui

Ermira Pazolli

Naoto Kawamura

Takao Yamori

Masanori Fujita

Motoko Matsufuji

Kian Huat Lim

Eunice Sun Park

Tomonari Yamada

Daisuke Ito

Akifumi Okuda

Michael P Thomas

Koji Norihisa

Betty Chan

Keisuke Komeda

Kumiko Kishi

Masao Iwata

Seiichi Kobayashi

Ming-Hong Hao

Dominic J Reynolds

Hisashi Shibata

Andrew Cook

Junichi Nagakawa

Takayuki Hida

Yasuhiro Kabasawa

Marta Nevalainen

Arani Chanda

Jason T Lowe

James Palacino

Daisuke Iida

Shelby Ellery

Kokichi Harada

Kyosuke Kito

Atsumi Yamaguchi

Katsuji Nakamura

Makoto Nakagawa

Lisa A Marcaurelle

Hirovuki Sugumi

Jun-ichi Kamata

Morgan Welzel O'shea

Tuoping Luo

Regina Mikie Kanada Sonabe

Regina Kanada Sonobe

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 relates to a compound represented by the formula (I): (wherein, R, R, Rand Rare the same as or different from one another and each represents a hydroxyl group etc.), a pharmacologically acceptable salt thereof or a hydrate of them. The compound (I) of the present invention suppresses angiogenesis, in particular, suppresses VEGF production in a hypoxic condition and is useful as a therapeutic agent for treating solid cancer.

Physiologically active substances

Process for producing compound of Formula: wherein P, Pand Rare the same as defined below, characterized by comprising reacting a compound represented by Formula (7): wherein Pmeans a protecting group for hydroxy group; and Het means a 1-phenyl-1H-tetrazol-5-yl group, with a compound represented by Formula (8): wherein Pmeans a protecting group for hydroxy group; and Rmeans a phenyl group which may be substituted, in the presence of a base.

Process for total synthesis of pladienolide B and pladienolide D

A process for producing a compound represented by Formula (11): wherein P, P, P, Pand Rare the same as defined herein, characterized by including reacting a compound represented by Formula (12): with a compound represented by Formula (13): in the presence of a catalyst.

The present invention provides a novel bioactive substance having an antitumor activity and a process for producing it, and a medical use thereof. Namely, it provides a 12-membered ring macrolide compound represented by the following formula obtained from the incubation solution ofsp. Mer. 11107 or a variant thereof, a pharmacologically acceptable salt thereof or a hydrate of them, and a process for producing it. 

Bioactive substance

A compound having excellent adenosine receptor (A, A, Areceptor) antagonistic action, of the following formula, a salt thereof or a solvate of them: wherein, Rand R, same or different, each represents a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a cycloalkenyl group, an aromatic hydrocarbon cyclic group, an acyl group or an alkylsulfonyl group, which groups may be substituted (except the hydrogen atom); Rrepresents a hydrogen atom, a halogen atom, a cyano group, an alkyl group, an alkenyl group, an alkynyl group, an aromatic hydrocarbon cyclic group, a nitrogen atom, an oxygen atom or a sulfur atom, which groups may be substituted (except the hydrogen atom, the halogen atom and the cyano group); Rrepresents an aromatic hydrocarbon cyclic group which may be substituted, and Rrepresents an aromatic hydrocarbon cyclic group which may be substituted.

Pyrimidine compound and medicinal composition thereof

Compounds represented by the following general formula (I), pharmacologically acceptable salts thereof or hydrates of the same: (I) wherein W represents and R, R, R, R, R, Rand Rare the same or different and each represents hydrogen, etc. Because of inhibiting angiogenesis and inhibiting the production of VEGF particularly in hypoxia, the compounds (I) are useful as remedies for solid cancer.

The present invention provides a medicament having a gentle but strong defecation-promoting action without causing diarrhea. That is, it provides a defecation-promoting agent comprising a compound having an adenosine Areceptor antagonism, preferably an adenosine Areceptor antagonism, or a salt thereof.

Medicinal compositions promoting bowel movement

The invention provides novel pyrimidone compounds exhibiting excellent antagonism against adenosine receptors (A, A, and Areceptors), particularly, compounds represented by the general formula (1), salts thereof, or solvates of both: (1) wherein Rand Rare each independently hydrogen, Calkyl, Calkenyl, Calkynyl, Ccycloalkyl, Ccycloalkenyl, a 5- to 14-membered nonaromatic heterocyclic group, a Caromatic hydrocarbon group, a 5- to 14-membered aromatic heterocyclic group, Cacyl, or Calkylsulfonyl; Ris hydrogen, Calkyl, Calkenyl, or Calkynyl; Ris a Caromatic hydrocarbon group; a 5- to 14-membered aromatic heterocyclic group, or a 5- to 14-membered nonaromatic heterocyclic group having at least one unsaturated bond; and Ris a Caromatic hydrocarbon group or a 5- to 14-membered aromatic heterocyclic group (with the proviso that every group except hydrogen may be substituted).

Pyrimidone compounds and pharmaceutical compositions containing the same

The present invention provides a novel bioactive substance having an antitumor activity and a process for producing it, and a medical use thereof. Namely, it provides a 12-membered ring macrolide compound represented by the following formula obtained from the incubation solution ofsp. Mer. 11107 or a variant thereof, a pharmacologically acceptable salt thereof or a hydrate of them, and a process for producing it

Fused polycyclic heterocycle derivatives

Growing community of inventors

Ibaraki, Japan

Yoshihiko Kotake