Claims for Patent: 8,058,280

Summary for Patent: 8,058,280

Title:	Substituted thieno[2,3-d]pyrimidin-2,4-dione compounds and uses 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:	US11/848,939
Patent Claims:	1. A compound of the formula (I): wherein R1 is a C1-4 alkyl; 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; 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; or a salt thereof. 2. The compound as claimed in claim 1, wherein R4 is (1) a C1-4 alkoxy, (2) a C6-10 aryl, (3) a N—C1-4 alkyl-N—C1-4 alkylsulfonylamino, or (4) 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 alkoxycarbonyl, (4′) a mono-C1-4 alkyl-carbamoyl and (5′) a C1-4 alkylsulfonyl. 3. The compound as claimed in claim 1, wherein R1 is methyl. 4. The compound as claimed in claim 1, wherein R3 is methyl. 5. The compound as claimed in claim 1, wherein R4 is a C1-4 alkoxy. 6. The compound as claimed in claim 1, wherein n is 2. 7. The compound as claimed in claim 1, wherein R3 is methyl, R4 is a hydrogen atom and n is 1. 8. N-(4-(1-(2,6-difluorobenzyl)-5(((2-methoxyethyl)(methyl)amino)methyl)-2,4-dioxo-3-(2-pyridinyl)-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea, N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxypyridin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea, or a salt thereof. 9. A pharmaceutical composition which comprises the compound compound of claim 1 or a salt thereof with a pharmacologically acceptable carrier, excipient or diluent. 10. A method for manufacturing a pharmaceutical composition for antagonizing gonadotropin-releasing hormone which comprises mixing the compound of claim 1 or a salt thereof with a pharmacologically acceptable carrier, excipient or diluent. 11. N-(4-(1-(2,6-difluorobenzyl)-5(((2-methoxyethyl)(methyl)amino)methyl)-2,4-dioxo-3-(2-pyridinyl)-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea or a salt thereof. 12. N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxypyridin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea or a salt thereof.