公开(公告)号：US10435377B2

公开(公告)日：2019-10-08

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 ,  A61K31/505

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：US09896471B2

公开(公告)日：2018-02-20

申请号：US14498334

申请日：2014-09-26

Applicant: FUJIFILM Corporation

Inventor： Yasutaka Baba ,  Tatsuya Murakami ,  Junko Shintani

IPC: C07H19/06 ,  A61K31/7068 ,  C07H19/073 ,  C07C309/66 ,  C07C309/04

CPC classification number: C07H19/06 ,  A61K31/7068 ,  C07C309/04 ,  C07C309/66 ,  C07H19/073

Abstract: A superior antitumor agent is provided. A salt of 1-(2-deoxy-2-fluoro-4-thio-β-D-arabinofuranosyl)cytosine shows at least one or more of such characteristics as (1) it has superior antitumor activity, (2) it shows superior crystallinity, (3) it shows high water solubility, (4) it does not show deliquescent property, (5) it shows superior flowability, (6) it shows superior tableting property, (7) it can be manufactured with less environmental load, and (8) it can be manufactured in a large scale, and therefore it is useful as a bulk drug for medicaments.

公开(公告)号：US10562862B2

公开(公告)日：2020-02-18

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 ,  A61K31/505

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：US09624215B2

公开(公告)日：2017-04-18

申请号：US14440010

申请日：2013-10-30

Applicant: TOYAMA CHEMICAL CO., LTD. ,  FUJIFILM CORPORATION

Inventor： Tadashi Tanaka ,  Yoshitake Konishi ,  Daisuke Kubo ,  Masataka Fujino ,  Issei Doi ,  Daisuke Nakagawa ,  Tatsuya Murakami ,  Takayuki Yamakawa

IPC: A61K31/455 ,  A61K31/4709 ,  A61K31/497 ,  A61K31/501 ,  C07D235/26 ,  C07D403/04 ,  C07D413/12 ,  C07D417/04 ,  C07D241/44 ,  C07D263/58 ,  C07D209/08 ,  C07D277/68 ,  C07D471/04 ,  C07D403/12 ,  C07D401/14 ,  C07D405/14 ,  A61K31/4035 ,  A61K31/404 ,  A61K31/416 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/427 ,  A61K31/428 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4725 ,  A61K31/498 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/538 ,  C07D213/80 ,  C07D215/38 ,  C07D217/24 ,  C07D231/56 ,  C07D401/04 ,  C07D235/08 ,  C07D401/06 ,  C07D401/12 ,  C07D417/06 ,  C07D417/12 ,  C07D209/12 ,  C07D209/34 ,  C07D209/38 ,  C07D209/42 ,  C07D209/46 ,  C07D209/48 ,  C07C211/45 ,  C07D209/04 ,  C07D215/227 ,  C07D239/88 ,  C07D265/36 ,  C07D401/10 ,  C07D407/14 ,  C07D413/06 ,  C07D413/10 ,  C07D413/14

CPC classification number: C07D471/04 ,  A61K31/4035 ,  A61K31/404 ,  A61K31/416 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/427 ,  A61K31/428 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/455 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/497 ,  A61K31/498 ,  A61K31/501 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/538 ,  C07C211/45 ,  C07D209/04 ,  C07D209/08 ,  C07D209/12 ,  C07D209/34 ,  C07D209/38 ,  C07D209/42 ,  C07D209/46 ,  C07D209/48 ,  C07D213/80 ,  C07D215/227 ,  C07D215/38 ,  C07D217/24 ,  C07D231/56 ,  C07D235/08 ,  C07D235/26 ,  C07D239/88 ,  C07D241/44 ,  C07D263/58 ,  C07D265/36 ,  C07D277/68 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/14 ,  C07D407/14 ,  C07D413/06 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  Y02P20/55

Abstract: A novel amine derivative expressed by general formula (1) (in the formula: G1, G2, and G3 are the same or different and represent CH or a nitrogen atom; R1 represents a chlorine atom, an optionally-substituted C3-8 cycloalkyl group, or the like; R2 represents —COOR5 (in the formula, R5 represents a hydrogen atom or a carboxyl protective group), or the like; R3 represents a hydrogen atom, or the like; and R4 represents an optionally-substituted condensed bicyclic hydrocarbon group, an optionally-substituted bicyclic heterocyclic group, or the like), or a salt thereof is useful in procedures such as the treatment or prevention of conditions related to excessive keratinocyte proliferation.

公开(公告)号：US20150299189A1

公开(公告)日：2015-10-22

申请号：US14440010

申请日：2013-10-30

Applicant: TOYAMA CHEMICAL CO., LTD. ,  FUJIFILM CORPORATION

Inventor： Tadashi Tanaka ,  Yoshitake Konishi ,  Daisuke Kubo ,  Masataka Fujino ,  Issei Doi ,  Daisuke Nakagawa ,  Tatsuya Murakami ,  Takayuki Yamakawa

IPC: C07D471/04 ,  C07D215/227 ,  C07D217/24 ,  C07D213/80 ,  C07D263/58 ,  C07C211/45 ,  C07D241/44 ,  C07D239/88 ,  C07D265/36 ,  C07D401/10 ,  C07D413/10 ,  C07D401/12 ,  C07D413/06 ,  C07D417/04 ,  C07D413/12 ,  C07D403/04 ,  C07D401/04 ,  C07D413/14 ,  C07D403/12 ,  C07D407/14 ,  C07D401/14 ,  C07D417/12 ,  C07D209/04

CPC classification number: C07D471/04 ,  A61K31/4035 ,  A61K31/404 ,  A61K31/416 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/427 ,  A61K31/428 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/455 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/497 ,  A61K31/498 ,  A61K31/501 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/538 ,  C07C211/45 ,  C07D209/04 ,  C07D209/08 ,  C07D209/12 ,  C07D209/34 ,  C07D209/38 ,  C07D209/42 ,  C07D209/46 ,  C07D209/48 ,  C07D213/80 ,  C07D215/227 ,  C07D215/38 ,  C07D217/24 ,  C07D231/56 ,  C07D235/08 ,  C07D235/26 ,  C07D239/88 ,  C07D241/44 ,  C07D263/58 ,  C07D265/36 ,  C07D277/68 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/14 ,  C07D407/14 ,  C07D413/06 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  Y02P20/55

Abstract: A novel amine derivative expressed by general formula (1) (in the formula: G1, G2, and G3 are the same or different and represent CH or a nitrogen atom; R1 represents a chlorine atom, an optionally-substituted C3-8 cycloalkyl group, or the like; R2 represents —COOR5 (in the formula, R5 represents a hydrogen atom or a carboxyl protective group), or the like; R3 represents a hydrogen atom, or the like; and R4 represents an optionally-substituted condensed bicyclic hydrocarbon group, an optionally-substituted bicyclic heterocyclic group, or the like), or a salt thereof is useful in procedures such as the treatment or prevention of conditions related to excessive keratinocyte proliferation.

Abstract translation: 由通式（1）表示的新型胺衍生物（式中，G1，G2和G3相同或不同，表示CH或氮原子; R1表示氯原子，任意取代的C3-8环烷基 等; R 2表示-COOR 5（式中，R5表示氢原子或羧基保护基）等; R3表示氢原子等; R4表示任选取代的稠合双环烃 基团，任选取代的双环杂环基等）或其盐可用于诸如治疗或预防与过度角质形成细胞增殖相关的病症的过程。

公开(公告)号：US11382927B2

公开(公告)日：2022-07-12

申请号：US16114457

申请日：2018-08-28

Applicant: FUJIFILM Corporation

Inventor： Hiroki Tanisaka ,  Tatsuya Murakami

IPC: A61K31/7068 ,  A61K47/10 ,  A61K9/08 ,  A61P35/00 ,  A61K9/00 ,  A61K47/02 ,  A61K47/26

Abstract: An object of the present invention is to provide a liquid medicinal preparation which does not generate precipitates and is suitable for mass production. According to the present invention, provided is a liquid medicinal preparation that contains 1-(2-deoxy-2-fluoro-4-thio-β-D-arabinofuranosyl)cytosine or a salt thereof, a polyhydric alcohol having a molecular weight of 100 or less, and water. The polyhydric alcohol is preferably glycerin, propylene glycol, or butanediol.