公开(公告)号：US20180127382A1

公开(公告)日：2018-05-10

申请号：US15867122

申请日：2018-01-10

Applicant: FUJIFILM Corporation

Inventor： Yusuke NAGATO ,  Shinsuke MIZUMOTO ,  Tatsuya MURAKAMI ,  Tomoyuki TANAKA

IPC: C07D239/48 ,  C07D403/06

Abstract: 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, R1 represents a C1-6 alkyl group which may be substituted; and R8 represents a leaving group or the like).

公开(公告)号：US20150045339A1

公开(公告)日：2015-02-12

申请号：US14516337

申请日：2014-10-16

Applicant: FUJIFILM Corporation

Inventor： Masaru TAKASAKI ,  Toshiaki TSUJINO ,  Shintarou TANABE ,  Megumi OOKUBO ,  Kimihiko SATO ,  Atsushi HIRAI ,  Daisuke TERADA ,  Shinsuke INUKI ,  Shinsuke MIZUMOTO

IPC: C07D471/04 ,  C07D401/14 ,  C07D239/48 ,  C07D403/12 ,  C07D413/04 ,  C07D403/14 ,  C07D413/14 ,  C07D405/12 ,  C07D401/06 ,  C07D403/04 ,  C07D417/12 ,  C07D409/12 ,  C07D401/12 ,  C07D413/12

CPC classification number: C07D471/04 ,  A61K31/44 ,  A61K31/505 ,  C07D213/74 ,  C07D239/48 ,  C07D239/49 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D409/12 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

Abstract: 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).

Abstract translation: 目的是提供可用作急性骨髓性白血病（AML）治疗剂的Fms样酪氨酸激酶3（FLT3）抑制剂。 提供了由通式[1]表示的新型含氮杂环化合物或其盐。 本发明的化合物或其盐可以用作治疗与FLT3有关的疾病或病症的药物组合物的活性成分，例如急性骨髓性白血病（AML）和急性早幼粒细胞白血病（APL）。

公开(公告)号：US20190169133A1

公开(公告)日：2019-06-06

申请号：US16272263

申请日：2019-02-11

Applicant: FUJIFILM Corporation

Inventor： Yusuke NAGATO ,  Shinsuke MIZUMOTO ,  Tatsuya MURAKAMI ,  Tomoyuki TANAKA

IPC: C07D239/48 ,  C07D403/06

Abstract: 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, R1 represents a C1-6 alkyl group which may be substituted; and R8 represents a leaving group or the like).

公开(公告)号：US20160229812A1

公开(公告)日：2016-08-11

申请号：US15130168

申请日：2016-04-15

Applicant: FUJIFILM Corporation

Inventor： Shinsuke MIZUMOTO ,  Takuya MATSUMOTO

IPC: C07D239/48 ,  C07C309/29 ,  C07C65/11 ,  C07C55/10 ,  C07C57/15

CPC classification number: C07D239/48 ,  A61K31/505 ,  C07B2200/13 ,  C07C55/10 ,  C07C57/15 ,  C07C65/11 ,  C07C309/29 ,  C07D239/42

Abstract: 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.

Abstract translation: 本发明的目的是提供显示出优异的稳定性和/或溶解性等并且具有优异的FLT3抑制活性的化合物和药物组合物。 本发明提供了（S，E）-N-（1 - （（5-（2 - （（4-氰基苯基）氨基）-4-（丙基氨基）嘧啶-5-基）戊-4-炔 -1-基）氨基）-1-氧代丙-2-基）-4-（二甲基氨基）-N-甲基丁-2-烯酰胺或其结晶。 由于盐或其结晶具有优异的FLT3抑制活性，并且作为药物，例如储存稳定性，溶解度等，具有优异的物理化学性质，因此可用于治疗与FLT3有关的疾病或病症。 本发明还提供含有盐或其结晶的药物组合物和FLT3抑制剂。

公开(公告)号：US20140309225A1

公开(公告)日：2014-10-16

申请号：US14317001

申请日：2014-06-27

Applicant: FUJIFILM Corporation

Inventor： Hideyasu FUJIWARA ,  Shinsuke MIZUMOTO ,  Yohei KUBO ,  Hiyoku NAKATA ,  Shinji HAGIWARA ,  Yasutaka BABA ,  Takashi TAMURA ,  Hidenobu KUNIYOSHI ,  Tomoyuki MASHIKO ,  Mari YAMAMOTO

IPC: C07D413/12 ,  C07D213/82 ,  C07D401/12 ,  C07D401/14

CPC classification number: C07D413/12 ,  C07D213/82 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/14 ,  C07D409/14 ,  C07D471/04

Abstract: 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 R1 is a substituent represented by the following formula (II-1), (III-1), or (IV-1) (wherein R3, R4, R5, n, and X1 have the same definitions as those described in the specification), and R2 is a pyridyl, indazolyl, phenyl, pyrazolopyridyl, benzisoxazolyl, pyrimidinyl, or quinolyl group, each of which optionally has at least one substituent.

Abstract translation: 本发明的目的是提供具有优异的Syk抑制活性的化合物和药物组合物。 根据本发明，提供由下式（I）表示的烟酰胺衍生物或其盐，其中R 1为下式（II-1），（III-1）或（IV- 1）（其中R3，R4，R5，n和X1具有与说明书中描述的相同的定义），R2是吡啶基，吲唑基，苯基，吡唑并吡啶基，苯并异恶唑基，嘧啶基或喹啉基， 具有至少一个取代基。