Fujifilm Corporation

Mitsui Chemicals Asahi Life Materials Co., Ltd.

Takuya Matsumoto

Takayuki Ito

Satoru Okamoto

Makoto Ando

Kenji Wada

Katsuyuki Watanabe

Makoto Takahashi

Hideki Okada

Kouki Nakamura

Satoshi Shimamura

Yuuta Fujino

Motomasa Takahashi

Junichi Imoto

Daisuke Nakagawa

Manabu Kitazawa

Daisuke Terada

Takehiro Yamane

Hidenobu Kuniyoshi

Yuji Yoshimitsu

Kazufumi Kato

Rumina Obi

Hiyoku Nakata

Yoko Kuriyama

Shinsuke Mizumoto

Nao Sugimoto

Chie Okamura

Yohei Kubo

Shuhei Osaka

Hidehiko Tanaka

Tatsuya Nitabaru

Yusuke Yamada

A compound represented by a formula [1D] as shown below (wherein R, R, R, R, Rand Rrepresent a hydrogen atom, an optionally substituted Calkyl group, and the like) is useful as an intermediate for producing a thionucleoside, and the production method of the present invention is useful as a method for producing a thionucleoside. 

Synthetic intermediate of 1-(2-deoxy-2-fluoro-4-thio-&#x3b2;-D-arabinofuranosyl)cytosine, synthetic intermediate of thionucleoside, and method for producing the same

Disclosed are a compound and a pharmaceutical composition that exhibit an excellent drug efficacy against a tumor, in particular a tumor which has acquired resistance to gemcitabine. Specifically, provided is a thionucleoside derivative represented by General (in the formula, Rrepresents a hydroxyl group which may be protected, a Calkoxy group which may be substituted, or the like; Rrepresents a Calkoxy group which may be substituted, a Ccycloalkoxy group which may be substituted, or the like; and Rrepresents a hydrogen atom or the like); or a salt thereof. Further, provided is a pharmaceutical composition containing such a thionucleoside derivative or a salt thereof.

Thionucleoside derivative or salt thereof, and pharmaceutical composition

Disclosed are a compound and a pharmaceutical composition that exhibit an excellent drug efficacy against a tumor, in particular a tumor which has acquired resistance to gemcitabine. Specifically, provided is a thionucleoside derivative represented by General Formula [1] 

An object of the present invention is to provide a compound and pharmaceutical composition showing superior stability and/or solubility, etc. and having superior FLT3 inhibitory activity. The present invention provides a salt of (S,E)-N-(1-((5-(2-((4-cyanophenyl)amino)-4-(propylamino)pyrimidin-5-yl)pent-4-yn-1-yl)amino)-1-oxopropan-2-yl)-4-(dimethylamino)-N-methylbut-2-enamide, or a crystal thereof. Since the salt or a crystal thereof has superior FLT3 inhibitory activity and shows superior physicochemical properties as drugs, such as storage stability, solubility, and so forth, it is useful for treatments of diseases or conditions relating to FLT3. The present invention also provides a pharmaceutical composition and FLT3 inhibitor containing the salt or a crystal thereof. 

Salt of nitrogen-containing heterocyclic compound or crystal thereof, pharmaceutical composition, and FLT3 inhibitor

Synthetic intermediate of 1-(2-deoxy-2-fluoro-4-thio-&#x3b2;-D-arabinofuranosyl) cytosine, synthetic intermediate of thionucleoside, and method for producing the same

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Ashigarakami-gun, Japan

Takuya Matsumoto