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    PRODUCTION METHOD OF THIENOPYRIMIDINE DERIVATIVE
    2.
    发明申请
    PRODUCTION METHOD OF THIENOPYRIMIDINE DERIVATIVE 有权

    公开(公告)号：US20220135585A1

    公开(公告)日：2022-05-05

    申请号：US17349584

    申请日：2021-06-16

    Applicant: Takeda Pharmaceutical Company Limited

    Inventor： Kazuhiro MIWA

    IPC: C07D495/04 ,  C07D333/38 ,  C07D409/12

    Abstract: The present invention provides a production method of a thienopyrimidine derivative or a salt thereof which has a gonadotropin releasing hormone (GnRH) antagonistic action with high quality in high yield. The present invention provides a method of producing a thienopyrimidine derivative, which comprises reacting 6-(4-aminophenyl)-1-(2,6-difluorobenzyl)-5-dimethylaminomethyl-3-(6-methoxypyridazin-3-yl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione or salt thereof, 1,1′-carbonyldiimidazole or a salt thereof and methoxyamine or a salt thereof, and the like.

    PRODUCTION METHOD OF THIENOPYRIMIDINE DERIVATIVE
    5.
    发明申请
    PRODUCTION METHOD OF THIENOPYRIMIDINE DERIVATIVE 审中-公开

    公开(公告)号：US20180319816A1

    公开(公告)日：2018-11-08

    申请号：US16034002

    申请日：2018-07-12

    Applicant: Takeda Pharmaceutical Company Limited

    Inventor： Kazuhiro MIWA ,  Tsuyoshi SASAKI ,  Fumiya KOMURA

    IPC: C07D495/04 ,  C07D409/12 ,  C07D333/38

    Abstract: The present invention provides a production method of a thienopyrimidine derivative or a salt thereof which has a gonadotropin releasing hormone (GnRH) antagonistic action with high quality in high yield. The present invention provides a method of producing a thienopyrimidine derivative, which comprises reacting 6-(4-aminophenyl)-1-(2,6-difluorobenzyl)-5-dimethylaminomethyl-3-(6-methoxypyridazin-3-yl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione or salt thereof, 1,1′-carbonyldiimidazole or a salt thereof and methoxyamine or a salt thereof, and the like.

    THIENOPYRIMIDINE COMPOUNDS AND USE THEREOF
    6.
    发明申请
    THIENOPYRIMIDINE COMPOUNDS AND USE THEREOF 有权
    噻吗啉化合物及其用途

    公开(公告)号：US20140221381A1

    公开(公告)日：2014-08-07

    申请号：US14251119

    申请日：2014-04-11

    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

    Inventor： Nobuo CHO ,  Takashi IMADA ,  Takenori HITAKA ,  Kazuhiro MIWA ,  Masami KUSAKA ,  Nobuhiro SUZUKI

    IPC: C07D495/04

    CPC classification number: C07D495/04 ,  A61K31/519

    Abstract: The present invention provides a compound represented by the formula: wherein R1 is a C1-4 alkyl; R2 is (1) a 5- to 7-membered nitrogen-containing heterocyclic group which may have a substituent selected from the group consisting of (1′) a halogen, (2′) a hydroxy group, (3′) a C1-4 alkyl and (4′) a C1-4 alkoxy, (2) a phenyl which may have a substituent selected from the group consisting of (1′) a halogen, (2′) a C1-4 alkoxy-C1-4 alkyl, (3′) a mono-C1-4 alkyl-carbamoyl-C1-4 alkyl, (4′) a C1-4 alkoxy and (5′) a mono-C1-4 alkylcarbamoyl-C1-4 alkoxy, or the like; R3 is a C1-4 alkyl; R4 is a C1-4 alkoxy, or the like; n is an integer of 1 to 4; or a salt thereof, as a thienopyrimidine compound having gonadotropin-releasing hormone antagonistic activity.

    Abstract translation: 本发明提供由下式表示的化合物：其中R1是C1-4烷基; R2是（1）可以具有选自（1'）卤素，（2'）羟基，（3'），C 1〜C 6的取代基的5〜7元含氮杂环基， 4烷基和（4'）C 1-4烷氧基，（2）可具有选自（1'）卤素，（2'）C 1-4烷氧基-C 1-4烷基的取代基的苯基 ，（3'）单-C 1-4烷基 - 氨基甲酰基-C 1-4烷基，（4'）C 1-4烷氧基和（5'）单-C 1-4烷基氨基甲酰基-C 1-4烷氧基等 ; R3是C1-4烷基; R4是C1-4烷氧基等; n为1〜4的整数， 或其盐作为具有促性腺激素释放激素拮抗活性的噻吩并嘧啶化合物。

    COMPOSITIONS OF THIENOPYRIMIDINE DERIVATIVES
    7.
    发明申请
    COMPOSITIONS OF THIENOPYRIMIDINE DERIVATIVES 有权

    公开(公告)号：US20250051353A1

    公开(公告)日：2025-02-13

    申请号：US18927346

    申请日：2024-10-25

    Applicant: Takeda Pharmaceutical Company Limited

    Inventor： Kazuhiro MIWA

    IPC: C07D495/04 ,  C07D333/38 ,  C07D409/12

    Abstract: The present invention provides a production method of a thienopyrimidine derivative or a salt thereof which has a gonadotropin releasing hormone (GnRH) antagonistic action with high quality in high yield. The present invention provides a method of producing a thienopyrimidine derivative, which comprises reacting 6-(4-aminophenyl)-1-(2,6-difluorobenzyl)-5-dimethylaminomethyl-3-(6-methoxypyridazin-3-yl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione or salt thereof, 1,1′-carbonyldiimidazole or a salt thereof and methoxyamine or a salt thereof, and the like.

    COMPOSITIONS OF THIENOPYRIMIDINE DERIVATIVES
    8.
    发明申请
    COMPOSITIONS OF THIENOPYRIMIDINE DERIVATIVES 有权

    公开(公告)号：US20220204525A1

    公开(公告)日：2022-06-30

    申请号：US17694635

    申请日：2022-03-14

    Applicant: Takeda Pharmaceutical Company Limited

    Inventor： Koichiro FUKUOKA ,  Kazuhiro MIWA ,  Tsuyoshi SASAKI ,  Fumiya KOMURA

    IPC: C07D495/04 ,  C07D333/38 ,  C07D409/12

    Abstract: The present invention provides a production method of a thienopyrimidine derivative or a salt thereof which has a gonadotropin releasing hormone (GnRH) antagonistic action with high quality in high yield. The present invention provides a method of producing a thienopyrirnidine derivative, which comprises reacting 6-(4-aminophenyl)-1-(2,6-difluorobenzyl)-5-dimethylaminomethyl-3-(6-methoxypyridazin-3-yl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione or salt thereof, 1,1′-carbonyldiimidazole or a salt thereof and methoxyamine or a salt thereof, and the like.

    PRODUCTION METHOD OF THIENOPYRIMIDINE DERIVATIVE
    9.
    发明申请
    PRODUCTION METHOD OF THIENOPYRIMIDINE DERIVATIVE 审中-公开

    公开(公告)号：US20190055261A1

    公开(公告)日：2019-02-21

    申请号：US16116804

    申请日：2018-08-29

    Applicant: Takeda Pharmaceutical Company Limited

    Inventor： Kazuhiro MIWA

    IPC: C07D495/04 ,  C07D333/38 ,  C07D409/12

    Abstract: The present invention provides a production method of a thienopyrimidine derivative or a salt thereof which has a gonadotropin releasing hormone (GnRH) antagonistic action with high quality in high yield. The present invention provides a method of producing a thienopyrimidine derivative, which comprises reacting 6-(4-aminophenyl)-1-(2,6-difluorobenzyl)-5-dimethylaminomethyl-3-(6-methoxypyridazin-3-yl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione or salt thereof, 1,1′-carbonyldiimidazole or a salt thereof and methoxyamine or a salt thereof, and the like.

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