发明名称 Thienopyrimidine compounds and use thereof
摘要 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.
申请公布号 US9346822(B2) 申请公布日期 2016.05.24
申请号 US201414251119 申请日期 2014.04.11
申请人 Takeda Pharmaceutical Company Limited 发明人 Cho Nobuo;Imada Takashi;Hitaka Takenori;Miwa Kazuhiro;Kusaka Masami;Suzuki Nobuhiro
分类号 A61K31/519;A61P15/02;A61P15/08;C07D495/04;A61P15/18 主分类号 A61K31/519
代理机构 Mintz Levin Cohn Ferris Glovsky and Popeo, P.C. 代理人 Mintz Levin Cohn Ferris Glovsky and Popeo, P.C. ;Conlin David G.;Lee Joohee
主权项 1. A method for treating hysteromyoma by antagonizing gonadotropin-releasing hormone, which comprises administering an effective amount of the compound represented by formula (I): wherein R1 is a C1-4 alkyl; R2 is (1) a C1-6 alkyl which may have a substituent selected from the group consisting of (1′) a hydroxy group, (2′) a C1-4 alkoxy, (3′) a C1-4 alkoxy-carbonyl, (4′) a di-C1-4 alkyl-carbamoyl, (5′) a 5- to 7-membered nitrogen-containing heterocyclic group, (6′) a C1-4 alkyl-carbonyl and (7′) a halogen, (2) a C3-8 cycloalkyl which may have (1′) a hydroxy group or (2′) a mono-C1-4 alkyl-carbonylamino, (3) 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, (4) 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 alkyl-carbamoyl-C1-4 alkoxy, or (5) a C1-4 alkoxy; R3 is a C1-4 alkyl; R4 is (1) a hydrogen atom, (2) a C1-4 alkoxy, (3) a C6-10 aryl, (4) a N—C1-4 alkyl-N—C1-4 alkylsulfonylamino, (5) a hydroxyl group, or (6) a 5- to 7-membered nitrogen-containing heterocyclic group which may have a substituent selected from the group consisting of (1′) oxo, (2′) a C1-4 alkyl, (3′) a hydroxy-C1-4 alkyl, (4′) a C1-4 alkoxy-carbonyl, (5′) a mono-C1-4 alkyl-carbamoyl and (6′) a C1-4 alkylsulfonyl; n is an integer of 1 to 4; provided that when R2 is a phenyl which may have a substituent, R4 is a 5- to 7-membered nitrogen-containing heterocyclic group which may have a substituent selected from the group consisting of (1) oxo, (2) a hydroxy-C1-4 alkyl, (3) a C1-4 alkoxy-carbonyl, (4) a mono-C1-4 alkyl-carbamoyl and (5) a C1-4 alkylsulfonyl; or a salt thereof; to a mammal in need thereof.
地址 Osaka-Shi JP