公开(公告)号：US20180319834A1

公开(公告)日：2018-11-08

申请号：US16037375

申请日：2018-07-17

Applicant: FUJIFILM Corporation

Inventor： Hidenobu KUNIYOSHI ,  Daisuke NAKAGAWA ,  Takuya MATSUMOTO ,  Yuji YOSHIMITSU

IPC: C07H19/10 ,  A61P35/02 ,  A61K31/7068 ,  A61P35/00

CPC classification number: C07H19/10 ,  A61K31/7068 ,  A61P35/00 ,  A61P35/02

Abstract: 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, R1 represents a hydroxyl group which may be protected, a C1-20 alkoxy group which may be substituted, or the like; R2 represents a C1-20 alkoxy group which may be substituted, a C3-8 cycloalkoxy group which may be substituted, or the like; and R3 represents 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.

公开(公告)号：US20160168139A1

公开(公告)日：2016-06-16

申请号：US15052252

申请日：2016-02-24

Applicant: FUJIFILM Corporation

Inventor： Yohei KUBO ,  Makoto ANDO ,  Hidehiko TANAKA ,  Shuhei OSAKA ,  Takuya MATSUMOTO ,  Hiyoku NAKATA ,  Daisuke TERADA ,  Tatsuya NITABARU

IPC: C07D413/14 ,  C07D409/14 ,  C07D498/08 ,  C07D491/048 ,  C07D411/14 ,  C07D498/04 ,  C07D405/14 ,  C07D491/052 ,  C07D411/04 ,  C07D409/04 ,  C07D405/04

CPC classification number: C07D413/14 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/55 ,  A61K31/553 ,  C07D401/14 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D411/04 ,  C07D411/14 ,  C07D417/14 ,  C07D491/048 ,  C07D491/052 ,  C07D491/056 ,  C07D491/107 ,  C07D498/04 ,  C07D498/08

Abstract: There is provided a morpholine derivative represented by General Formula [1A] or a salt thereof. (In the formula, a ring A represents a ring represented by General Formula [I]; * represents a bonding position; Z2 represents CH or the like; Z1 represents CR6 or the like; R6 represents a hydrogen atom or the like; X1 represents CHR7 or the like; R7 represents a hydrogen atom or the like; X2 represents CH2 or the like; R1 and R2 are the same as or different from each other, and each of R1 and R2 represents a hydrogen atom or the like; R3, R4, and R5 are the same as or different from each other, and each of R3, R4, and R5 represents a hydrogen atom, NRaRb, or the like; and each of Ra and Rb represents a hydrogen atom, a C1-8 alkyl group which may have a substituent, or the like.)

Abstract translation: 提供由通式[1A]表示的吗啉衍生物或其盐。 （式中，环A表示通式[I]表示的环; *表示键合位置，Z 2表示CH等，Z1表示CR 6等，R 6表示氢原子等; X 1表示 CHR 7等; R 7表示氢原子等; X 2表示CH 2等; R 1和R 2相同或不同，R 1和R 2各自表示氢原子等; R 3， R 4和R 5彼此相同或不同，R 3，R 4和R 5各自表示氢原子，NR a R b等; R a和R b分别表示氢原子，C 1-8烷基 可以具有取代基的基团等）

公开(公告)号：US20180327377A1

公开(公告)日：2018-11-15

申请号：US16045047

申请日：2018-07-25

Applicant: FUJIFILM Corporation

Inventor： Kouki NAKAMURA ,  Satoshi SHIMAMURA ,  Junichi IMOTO ,  Motomasa TAKAHASHI ,  Katsuyuki WATANABE ,  Kenji WADA ,  Yuuta FUJINO ,  Takuya MATSUMOTO ,  Makoto TAKAHASHI ,  Hideki OKADA ,  Takehiro YAMANE ,  Takayuki ITO

IPC: C07D333/32 ,  C07F7/18 ,  A61K31/7068 ,  C07C47/277 ,  C07C251/40 ,  C07C309/66 ,  C07H19/06 ,  C07H7/04 ,  C07H1/00 ,  C07C303/28 ,  C07C45/00 ,  C07B53/00 ,  C07C309/73 ,  C07C249/04 ,  C07C251/38 ,  C07H13/04 ,  C07H13/08 ,  C07H15/04 ,  C07H15/18 ,  C07H15/203 ,  C07H17/02 ,  C07H19/067 ,  C07H19/073 ,  C07H23/00 ,  C07C69/96 ,  C07C69/92 ,  C07C69/76 ,  C07C69/618 ,  C07C69/28 ,  C07C68/06 ,  C07C67/29 ,  C07C69/78

Abstract: A compound represented by a formula [1D] as shown below (wherein R1A, R1B, R2A, R2B, R3A and R3B represent a hydrogen atom, an optionally substituted C1-6 alkyl 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.

公开(公告)号：US20170233429A1

公开(公告)日：2017-08-17

申请号：US15581834

申请日：2017-04-28

Applicant: FUJIFILM Corporation

Inventor： Hidenobu KUNIYOSHI ,  Daisuke NAKAGAWA ,  Takuya MATSUMOTO ,  Yuji YOSHIMITSU

IPC: C07H19/10

CPC classification number: C07H19/10 ,  A61K31/7068 ,  A61P35/00 ,  A61P35/02

Abstract: 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] (in the formula, R1 represents a hydroxyl group which may be protected, a C1-20 alkoxy group which may be substituted, or the like; R2 represents a C1-20 alkoxy group which may be substituted, a C3-8 cycloalkoxy group which may be substituted, or the like; and R3 represents 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.

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：US20160362389A1

公开(公告)日：2016-12-15

申请号：US15246177

申请日：2016-08-24

Applicant: FUJIFILM Corporation

Inventor： Kouki NAKAMURA ,  Satoshi SHIMAMURA ,  Junichi IMOTO ,  Motomasa TAKAHASHI ,  Katsuyuki WATANABE ,  Kenji WADA ,  Yuuta FUJINO ,  Takuya MATSUMOTO ,  Makoto TAKAHASHI ,  Hideki OKADA ,  Takehiro YAMANE ,  Takayuki ITO

IPC: C07D333/32 ,  C07C309/73 ,  C07C47/277 ,  C07H7/04 ,  C07H13/04 ,  C07C309/66 ,  C07C69/78 ,  C07C69/618 ,  C07C69/76 ,  C07C69/28 ,  C07C69/96 ,  C07F7/18 ,  C07C251/38 ,  C07C251/40

CPC classification number: C07D333/32 ,  A61K31/7068 ,  C07B53/00 ,  C07C45/00 ,  C07C47/277 ,  C07C67/29 ,  C07C68/06 ,  C07C69/28 ,  C07C69/618 ,  C07C69/76 ,  C07C69/78 ,  C07C69/92 ,  C07C69/96 ,  C07C249/04 ,  C07C251/38 ,  C07C251/40 ,  C07C303/28 ,  C07C309/66 ,  C07C309/73 ,  C07F7/1804 ,  C07H1/00 ,  C07H7/04 ,  C07H13/04 ,  C07H13/08 ,  C07H15/04 ,  C07H15/18 ,  C07H15/203 ,  C07H17/02 ,  C07H19/06 ,  C07H19/067 ,  C07H19/073 ,  C07H23/00 ,  Y02P20/55

Abstract: A compound represented by a formula [1D] as shown below (wherein R1A, R1B, R2A, R2B, R3A and R3B represent a hydrogen atom, an optionally substituted C1-6 alkyl 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.

公开(公告)号：US20160024132A1

公开(公告)日：2016-01-28

申请号：US14873966

申请日：2015-10-02

Applicant: FUJIFILM Corporation

Inventor： Kouki NAKAMURA ,  Satoshi SHIMAMURA ,  Junichi IMOTO ,  Motomasa TAKAHASHI ,  Katsuyuki WATANABE ,  Kenji WADA ,  Yuuta FUJINO ,  Takuya MATSUMOTO ,  Makoto TAKAHASHI ,  Hideki OKADA ,  Takehiro YAMANE ,  Takayuki ITO

IPC: C07H19/06 ,  C07H7/04 ,  C07H1/00 ,  C07D333/32

CPC classification number: C07D333/32 ,  A61K31/7068 ,  C07B53/00 ,  C07C45/00 ,  C07C47/277 ,  C07C67/29 ,  C07C68/06 ,  C07C69/28 ,  C07C69/618 ,  C07C69/76 ,  C07C69/78 ,  C07C69/92 ,  C07C69/96 ,  C07C249/04 ,  C07C251/38 ,  C07C251/40 ,  C07C303/28 ,  C07C309/66 ,  C07C309/73 ,  C07F7/1804 ,  C07H1/00 ,  C07H7/04 ,  C07H13/04 ,  C07H13/08 ,  C07H15/04 ,  C07H15/18 ,  C07H15/203 ,  C07H17/02 ,  C07H19/06 ,  C07H19/067 ,  C07H19/073 ,  C07H23/00 ,  Y02P20/55

Abstract: A compound represented by a formula [1D] as shown below (wherein R1A, R1B, R2A, R2B, R3A and R3B represent a hydrogen atom, an optionally substituted C1-6 alkyl 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.

Abstract translation: 由下式（其中R1A，R1B，R2A，R2B，R3A和R3B表示氢原子，任选取代的C 1-6烷基等）表示的由式[1D]表示的化合物可用作生产中间体 硫代核苷，本发明的制造方法可用作硫代核苷的制造方法。

公开(公告)号：US20150152131A1

公开(公告)日：2015-06-04

申请号：US14621119

申请日：2015-02-12

Applicant: FUJIFILM Corporation

Inventor： Kouki NAKAMURA ,  Satoshi SHIMAMURA ,  Junichi IMOTO ,  Motomasa TAKAHASHI ,  Katsuyuki WATANABE ,  Kenji WADA ,  Yuuta FUJINO ,  Takuya MATSUMOTO ,  Makoto TAKAHASHI ,  Hideki OKADA ,  Takehiro YAMANE ,  Takayuki ITO

IPC: C07H19/06 ,  C07C69/78 ,  C07C251/38 ,  C07C309/73 ,  C07H7/04 ,  C07H1/00

CPC classification number: C07D333/32 ,  A61K31/7068 ,  C07B53/00 ,  C07C45/00 ,  C07C47/277 ,  C07C67/29 ,  C07C68/06 ,  C07C69/28 ,  C07C69/618 ,  C07C69/76 ,  C07C69/78 ,  C07C69/92 ,  C07C69/96 ,  C07C249/04 ,  C07C251/38 ,  C07C251/40 ,  C07C303/28 ,  C07C309/66 ,  C07C309/73 ,  C07F7/1804 ,  C07H1/00 ,  C07H7/04 ,  C07H13/04 ,  C07H13/08 ,  C07H15/04 ,  C07H15/18 ,  C07H15/203 ,  C07H17/02 ,  C07H19/06 ,  C07H19/067 ,  C07H19/073 ,  C07H23/00 ,  Y02P20/55

Abstract: A compound represented by a formula [1D] as shown below (wherein R1A, R1B, R2A, R2B, R3A and R3B represent a hydrogen atom, an optionally substituted C1-6 alkyl 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.

Abstract translation: 由下式（其中R1A，R1B，R2A，R2B，R3A和R3B表示氢原子，任选取代的C 1-6烷基等）表示的由式[1D]表示的化合物可用作生产中间体 硫代核苷，本发明的制造方法可用作硫代核苷的制造方法。