Fujifilm Corporation

Shinsuke Mizumoto

Takashi Tamura

Hiyoku Nakata

Tatsuya Murakami

Tomoyuki Tanaka

Yasutaka Baba

Kimihiko Sato

Mari Yamamoto

Yohei Kubo

Hideyasu Fujiwara

Yusuke Nagato

Masaru Takasaki

Daisuke Terada

Atsushi Hirai

Hidenobu Kuniyoshi

Shinji Hagiwara

Takuya Matsumoto

Yuichiro Sato

Tomoyuki Mashiko

Hideki Kurihara

Shinsuke Inuki

Megumi Ookubo

Atsush Hirai

Shintarou Tanabe

Toshiaki Tsujino

An object of the present invention is to provide a method for industrially manufacturing a nitrogen-containing heterocyclic compound which shows excellent FLT3 inhibitory activity and is useful as a pharmaceutical active ingredient of pharmaceutical products. The present invention provides a manufacturing method of a compound represented by General Formula [14] or a salt thereof (in the formula, Rrepresents a Calkyl group which may be substituted; and Rrepresents a leaving group or the like). 

Method for manufacturing nitrogen-containing heterocyclic compound and intermediate of same

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

The object is to provide an Fms-like tyrosine kinase 3 (FLT3) inhibitor useful as a therapeutic agent for acute myeloid leukemia (AML). A novel nitrogen-containing heterocyclic compound represented by the general formula [1] or a salt thereof is provided. The compound or a salt thereof of the present invention can be used as an active ingredient of a pharmaceutical composition for a treatment of a disease or condition relating to FLT3, such as acute myeloid leukemia (AML) and acute promyelocytic leukemia (APL).

Nitrogen-containing heterocyclic compound or salt thereof

The object of the present invention is to provide a compound and a pharmaceutical composition having excellent Syk inhibitory activity. According to the present invention, a nicotinamide derivative represented by the following formula (I) or a salt thereof is provided, wherein (wherein R, R, R, n, and Xhave the same definitions as those described in the specification), and Ris a pyridyl, indazolyl, phenyl, pyrazolopyridyl, benzisoxazolyl, pyrimidinyl, or quinolyl group, each of which optionally has at least one substituent.

Nicotinamide derivative or salt thereof

An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. The present invention provides a nicotinamide derivative represented by the following formula (I) (wherein Rrepresents a halogen atom; Rrepresents a Calkyl group, a Calkenyl group, a Calkynyl group, a Ccycloalkyl group, an aryl group, an ar-Calkyl group or a heterocyclic group, each optionally having at least one substituent; Rrepresents an aryl group or a heterocyclic group each optionally having at least one substituent; and Rand Reach independently represent a hydrogen atom; and Rand Rmay form a cyclic amino group optionally having at least one substituent together with the nitrogen atom to which they bind) or a salt thereof, and a pharmaceutical composition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.

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Ashigarakami-gun, Japan

Shinsuke Mizumoto