Taiho Pharmaceutical Company Limited

Chihoko Yoshimura

Shuichi Ohkubo

Makoto Kitade

Takao Uno

Hiromi Oshiumi

Takashi Mizutani

Satoshi Yamashita

Yuichi Kawai

Hitomi Kondo

Yasuo Kodama

A pyrrolopyrimidine compound or a salt thereof and compositions, NAE inhibitors and anti-tumor agents containing the pyrrolopyrimidine compound or a salt thereof. The pyrrolopyrimidine compound or a salt thereof has an NAE inhibitory action and a cell growth inhibitory effect and is represented by Formula (A): 

Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof

An object to be solved by the present invention is to identify patients resistant to known HSP90 inhibitors, and to provide a novel therapeutic agent for treating the patients who have become resistant to known HSP90 inhibitors. As a means for solving the above problems, the present invention provides identification of the patients based on a protein, which is an HSP90 family protein having a mutation in the site corresponding to F138 of HSP90&#x3b1; class A consisting of the amino acid sequence of SEQ ID NO: 1, and use of a substance that inhibits the protein as an active ingredient of a therapeutic agent.

Resistant mutant 90 kDa heat shock protein

It is intended to provide a novel azabicyclo compound which exhibits both HSP90 inhibitory activity and cell proliferation inhibitory effect. Specifically disclosed is a compound represented by the following general formula (I) or a salt thereof: wherein Xrepresents CH or N; any one of X, Xand Xrepresents N, and the others represent CH; any one or two of Y, Y, Yand Yrepresent C&#x2014;R, and the others are the same or different and represent CH or N; Rrepresents an optionally substituted monocyclic or bicyclic unsaturated heterocyclic group having 1 to 4 heteroatoms selected from N, S and O; Rrepresents an alkyl group having 1 to 6 carbon atoms, or the like; and Rand Rrepresent &#x2014;CO&#x2014;Ror the like.

Azabicyclo compound and salt thereof

The invention provides an indazole compound of formula (I) which is capable of inhibiting HSP90 and shows a cytostatic effect on cancer cells: 

Growing community of inventors

Tsukuba, Japan

Chihoko Yoshimura