Ono Pharmaceutical Co., Ltd.

Gilead Sciences, Inc.

Ono Pharmaceuticals Co., Ltd.

Shingo Yamamoto

Toshio Yoshizawa

Masakuni Kurono

Shingo Hotta

Hisao Nakai

Shingo Nakatani

Tomomi Hirosaki

Hiroshi Tokura

Yoshinori Nomura

Atsushi Yoshida

Seung H Lee

The purinone derivative 6-amino-9-[(3R)-1-(2-butynoyl)-3-pyrrolidinyl]-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one hydrochloride has Btk-selective inhibitory activity and, in addition to having excellent metabolic stability, it is a compound that exhibits a high level of solubility and absorption with respect to the free base and can be crystallized, hence it can serve as a therapeutic agent for diseases involving B cells and mast cells.

Purinone derivative hydrochloride

The present invention relates to a compound represented by general formula (I) (wherein, all symbols represent the same meanings as the symbols set forth in the specification), a salt thereof, a solvate thereof, an N-oxide thereof, or a prodrug of any of these. Since the compound has a Brk inhibitory activity, the compound is useful as a drug ingredient for the prevention and/or treatment of Brk-related diseases such as cancer, for example. 

BRK inhibitory compound

The present invention relates to a Brk inhibitory compound represented by general formula (I) (wherein, all symbols represent the same meanings as the symbols set forth in the specification), a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug of any of these. 

Compounds represented by general formula (I) (all of the symbols in the formula conform to the definitions in the Description) are compounds that, in addition to having a Btk-selective inhibitory activity, exhibit an excellent metabolic stability and can avoid hepatotoxicity or the like, and as a consequence can provide safe therapeutic agents for diseases in which B cells or mast cells participate.

Purinone derivative

Brk inhibitory compound

Inhibitors for Bruton's Tyrosine Kinase (BTK) are disclosed as are compositions thereof, methods for their preparation, and methods for their use.

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Osaka, Japan

Shingo Yamamoto