Carna Biosciences, Inc.

Academia Sinica

Gilead Sciences, Inc.

National Cancer Center

Sbi Biotech Co., Ltd.

The Kitasato Institute

Crystalgenomics, Inc.

Mychunter Therapeutics, Inc.

Masaaki Sawa

Tokiko Asami

Takayuki Irie

Chi-Huey Wong

Tsui-Ling Hsu

Sarah R Hanson

Chika Tanaka

Yoko Funakoshi

Hirokazu Matsumoto

Yuko Uno

Ayako Sawa

Takao Kiyoi

Tetsuya Kobayashi

Jonathan William Medley

Leena Patel

Tesshi Yamada

Qingming Zhu

Hideki Moriyama

Shigeki Kashimoto

Ryoko Nakai

Mai Arai

Yuko Asamitsu

Wataru Kawahata

Michael Graupe

Satoshi Omura

Juan A Guerrero

Suet Chung Yeung

Jie Xu

Julian Andrew Codelli

Yasamin Moazami

Takahiro Miyake

Seong Gu Ro

Kazuhiko Otoguro

Jesse M Jacobsen

Masato Iwatsuki

Heath A Weaver

Stephen D Holmbo

Koichi Yokota

Miki Shitashige

Aki Ishiyama

Choul Hong Park

Sayuri Ito

Yusuke Kawase

Rei Hokari

Catherine Pugh

Eric Hu

Latesh Lad

Will Watkins

Shiori Takamatsu

The present disclosure provides diacylglycerol kinase modulating compounds, and pharmaceutical compositions thereof, for treating cancer, including solid tumors, and viral infections, such as HIV or hepatitis B virus infection. The compounds can be used alone or in combination with other agents.

Diacylglycerol kinase modulating compounds

Provided herein are novel compounds having an inhibitory effect on the activation of a STING pathway. The provided compounds are 1,2-diaminobenzimidazole derivatives represented by a compound formula (I) or a pharmaceutically acceptable salt thereof: wherein A, A, R, R, R, R, and Rare defined in the specification.

1,2-diaminobenzimidazole derivative

An oxoisoquinoline compound of the following formula: or a pharmaceutically acceptable salt thereof; a pharmaceutical composition comprising the oxoisoquinoline compound or salt; and a method for treating B-cell lymphoma comprising administering the oxoisoquinoline compound or salt to a patient.

Oxoisoquinoline derivatives

To provide a novel furanone derivative, and a medicine including the same. The furanone derivative is represented by the formula (I): wherein A represents &#x2014;COOR1 or a hydrogen atom; R1 represents a hydrogen atom, an optionally substituted hydrocarbon group, or an optionally substituted heterocycle; R2 and R3 are the same or different and each independently represent a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted phenyl group, an optionally substituted heterocycle, an optionally substituted heterocyclic fused ring, or an optionally substituted amino group; or alternatively, R2 and R3, taken together with the nitrogen atom to which they are attached, may form an optionally substituted heterocycle or an optionally substituted heterocyclic fused ring; and R4 represents a hydrogen atom or a halogen atom; with the proviso that when A represents &#x2014;COOR1, R2 and R3 are not optionally substituted amino groups at the same time, and when A represents a hydrogen atom, R3 represents a hydrogen atom.

Furanone derivative

The present invention provides a novel 2,4,6-substituted pyrimidine derivative, which is a compound represented by formula (I) (in the formula, ring A is a 6-membered heteroaryl group having at least one N atom optionally substituted with R1, R2, and R3; Z is an optionally substituted alkoxy group, an optionally substituted amino group, an optionally substituted heterocycloalkyl group, or an optionally substituted heteroaryl group; and R1, R2, and R3 are each independently selected from the group consisting of a hydrogen atom, a halogen atom, an optionally substituted alkyl group, an optionally substituted cycloalkyl group, an optionally substituted alkoxy group, an optionally substituted cycloalkyloxy group, an optionally substituted heterocycloalkyloxy group, an optionally substituted phenoxy group, an optionally substituted amino group, a nitro group, and a hydroxy group) or a pharmaceutically acceptable salt thereof.

Pyrimidine derivative having antimalarial activity

Methods for metabolic oligosaccharide engineering that incorporates derivatized alkyne-bearing sugar analogs as 'tags' into cellular glycoconjugates are disclosed. Alkynyl derivatized Fuc and alkynyl derivatized ManNAc sugars are incorporated into cellular glycoconjugates. Chemical probes comprising an azide group and a visual or fluorogenic probe and used to label alkyne-derivatized sugar-tagged glycoconjugates are disclosed. Chemical probes bind covalently to the alkynyl group by Cu(I)-catalyzed [3+2] azide-alkyne cycloaddition and are visualized at the cell surface, intracellularly, or in a cellular extract. The labeled glycoconjugate is capable of detection by flow cytometry, SDS-PAGE, Western blot, ELISA, confocal microscopy, and mass spectrometry.

Alkynyl sugar analogs for labeling and visualization of glycoconjugates in cells

Provided is a pharmaceutical composition comprising a Cdc7 inhibitor and an M phase promoter. In particular, the Cdc7 inhibitor contained in the pharmaceutical composition is a furanone derivative represented by formula (I), or a pharmaceutically acceptable salt thereof. (In the formula, A is &#x2014;COOR1 or a hydrogen atom; R1 is a hydrogen atom, an optionally substituted hydrocarbon group, or an optionally substituted heterocycle; R2 and R3 are the same or different and are each a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted phenyl group, an optionally substituted heterocycle, an optionally substituted heterocyclic condensed ring, or an optionally substituted amino group. Alternatively, R2 and R3 may, together with the nitrogen atoms bonding the same, form an optionally substituted heterocycle or optionally substituted heterocyclic condensed ring. R4 is a hydrogen atom or halogen atom. However, if A is &#x2014;COOR1, R2 and R3 are not both simultaneously optionally substituted amino groups. When A is a hydrogen atom, R3 is a hydrogen atom.)

Anticancer agent composition

The present invention provides a quinazoline derivative represented by the following formula (I): wherein Rand Rrepresent a hydrogen atom, a halogen atom, or a lower alkyl group optionally having a substituent; Z represents a cycloalkyl group having a substituent or a cycloalkenyl group having a substituent; and Q represents a bicyclic heteroaryl group optionally having a substituent, or a pharmaceutically acceptable salt thereof. Since the compound has an inhibitory effect on the Wnt/&#x3b2;-catenin signaling pathway and exhibits an antitumor effect, it is useful as a medicine.

Quinazoline derivative

The purpose of the present invention is to provide a novel triazine derivative of the formula (I): wherein

Triazine derivative

The present invention relates to novel bicyclic thiazole compounds that inhibit Traf2- and Nck-interacting kinase (TNIK), and as such are useful as TNIK inhibitors administered to cancer patients, especially to solid cancer patients such as colorectal cancer, pancreatic cancer, non-small cell lung cancer, prostate cancer or breast cancer. The bicyclic thiazole compounds are showed by a next formula (I). (wherein R, R, Rand Q are as defined in the specification), or a pharmaceutically acceptable salt thereof. 

Bicyclic thiazole compounds

Methods are provided for labeling cellular glycans bearing azide groups via fluorescent labeling comprising Cu(I)-catalyzed [3+2] cycloaddition of a probe comprising alkynyl group. Generation of fluorescent probes from a nonfluorescent precursor, 4-ethynyl-N-ethyl-1,8-naphthalimide, by Cu(I)-catalyzed [3+2] cycloaddition of the alkyne group of the probe to an azido-modified sugar are provided. Incorporation of azido-containing fucose analog into glycoconjugates via the fucose salvage pathway are disclosed. Fluorescent visualization of fucosylated cells by flow cytometry of cells treated with 6-azidofucose labeled with click-activated fluorogenic probe or biotinylated alkyne is disclosed. Visualization of intracellular location of fucosylated glycoconjugates by fluorescence microscopy are disclosed.

Glycoproteomic probes for fluorescent imaging of fucosylated glycans in vivo

Growing community of inventors

Ibaraki, Japan

Masaaki Sawa