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: ##STR00001## wherein R.sup.1 is a C.sub.1-4 alkyl; R.sup.2 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 C.sub.1-4 alkyl and (4') a C.sub.1-4 alkoxy, (2) a phenyl which may have a substituent selected from the group consisting of (1') a halogen, (2') a C.sub.1-4 alkoxy-C.sub.1-4 alkyl, (3') a mono-C.sub.1-4 alkyl-carbamoyl-C.sub.1-4 alkyl, (4') a C.sub.1-4 alkoxy and (5') a mono-C.sub.1-4 alkylcarbamoyl-C.sub.1-4 alkoxy, or the like; R.sup.3 is a C.sub.1-4 alkyl; R.sup.4 is a C.sub.1-4 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):	Cho; Nobuo (Fujisawa, JP), Imada; Takashi (Fujisawa, JP), Hitaka; Takenori (Fujisawa, JP), Miwa; Kazuhiro (Osaka, JP), Kusaka; Masami (Osaka, JP), Suzuki; Nobuhiro (Mino, JP)
Assignee:	Takeda Pharmaceutical Company Limited (Osaka-Shi, JP)
Application Number:	14/251,119
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): ##STR00157## wherein R.sup.1 is a C.sub.1-4 alkyl; R.sup.2 is (1) a C.sub.1-6 alkyl which may have a substituent selected from the group consisting of (1') a hydroxy group, (2') a C.sub.1-4 alkoxy, (3') a C.sub.1-4 alkoxy-carbonyl, (4') a di-C.sub.1-4 alkyl-carbamoyl, (5') a 5- to 7-membered nitrogen-containing heterocyclic group, (6') a C.sub.1-4 alkyl-carbonyl and (7') a halogen, (2) a C.sub.3-8 cycloalkyl which may have (1') a hydroxy group or (2') a mono-C.sub.1-4 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 C.sub.1-4 alkyl and (4') a C.sub.1-4 alkoxy, (4) a phenyl which may have a substituent selected from the group consisting of (1') a halogen, (2') a C.sub.1-4 alkoxy-C.sub.1-4 alkyl, (3') a mono-C.sub.1-4 alkyl-carbamoyl-C.sub.1-4 alkyl, (4') a C.sub.1-4 alkoxy and (5') a mono-C.sub.1-4 alkyl-carbamoyl-C.sub.1-4 alkoxy, or (5) a C.sub.1-4 alkoxy; R.sup.3 is a C.sub.1-4 alkyl; R.sup.4 is (1) a hydrogen atom, (2) a C.sub.1-4 alkoxy, (3) a C.sub.6-10 aryl, (4) a N--C.sub.1-4 alkyl-N--C.sub.1-4 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 C.sub.1-4 alkyl, (3') a hydroxy-C.sub.1-4 alkyl, (4') a C.sub.1-4 alkoxy-carbonyl, (5') a mono-C.sub.1-4 alkyl-carbamoyl and (6') a C.sub.1-4 alkylsulfonyl; n is an integer of 1 to 4; provided that when R.sup.2 is a phenyl which may have a substituent, R.sup.4 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-C.sub.1-4 alkyl, (3) a C.sub.1-4 alkoxy-carbonyl, (4) a mono-C.sub.1-4 alkyl-carbamoyl and (5) a C.sub.1-4 alkylsulfonyl; or a salt thereof; to a mammal in need thereof. 2. The method according to claim 1, wherein R.sup.2 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 C.sub.1-4 alkyl and (4') a C.sub.1-4 alkoxy. 3. The method according to claim 1, wherein R.sup.4 is a hydrogen atom. 4. The method according to claim 1, wherein R.sup.1 is methyl. 5. The method according to claim 1, wherein R.sup.3 is methyl. 6. The method according to claim 1, wherein n is 1. 7. The method according to claim 1, wherein R.sup.3 is methyl; R.sup.4 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-pyr- idazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-- N'-methoxyurea, or a salt thereof.