Claims for Patent: 9,346,822

Summary for Patent: 9,346,822

Title:	Thienopyrimidine compounds and use thereof
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.
Inventor(s):	Nobuo Cho, Takashi Imada, Takenori Hitaka, Kazuhiro Miwa, Masami Kusaka, Nobuhiro Suzuki
Assignee:	Takeda Pharmaceutical Co Ltd
Application Number:	US14/251,119
Patent Claims:	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. 2. The method according to claim 1, wherein R2 is 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. 3. The method according to claim 1, wherein R4 is a hydrogen atom. 4. The method according to claim 1, wherein R1 is methyl. 5. The method according to claim 1, wherein R3 is methyl. 6. The method according to claim 1, wherein n is 1. 7. The method according to claim 1, wherein R3 is methyl; R4 is a hydrogen atom; and n is 1. 8. The method according to claim 1, wherein the compound is N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea, or a salt thereof.