公开(公告)号：US09346822B2

公开(公告)日：2016-05-24

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: A61K31/519 ,  A61P15/02 ,  A61P15/08 ,  C07D495/04 ,  A61P15/18

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。

公开(公告)号：US10668260B2

公开(公告)日：2020-06-02

申请号：US14774385

申请日：2014-03-11

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Yoshihiro Omachi ,  Yasuhiro Hiraishi ,  Masami Kusaka ,  Shigehiro Asano ,  Masao Nagao

IPC: A61M37/00 ,  A61K9/00 ,  A61K9/70 ,  B29C45/00 ,  B29C45/16 ,  B29K101/12 ,  B29L9/00 ,  B29L31/00

Abstract: The present invention provides a microneedle patch which can solve the problem that microneedle production is difficult and requires high accuracy, the problem that time and mental burdens on a health professional and a patient are large, and the problem caused by compounding a plurality of drugs. The microneedle patch comprises a large number of drug-carrying microprojections 4 erected on one support sheet, each microprojection 4 having a drug layer 5 soluble in vivo at its top part and having an intermediate layer 6 under the drug layer 5, the intermediate layer 6 containing a polymeric substance for adhesion of the drug layer 5 to the support sheet, the drug layer 5 at the top part of the microprojection 4 containing a single drug, the microprojections 4 holding difference types of drugs being arranged together on the support sheet 2.