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Last Updated: May 9, 2024

Claims for Patent: 7,939,540


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Summary for Patent: 7,939,540
Title:4-(3-benzoylaminophenyl)-6,7-dimethoxy-2-methylaminoquinazoline derivatives
Abstract: A compound represented by the following formula (I), salt thereof, or hydrate thereof, can effectively relieve itch caused by atopic disease or the like: ##STR00001## wherein R represents hydroxyl, C.sub.1-6 alkoxy optionally substituted with C.sub.1-6 alkoxy, or amino optionally substituted with C.sub.1-6 alkyl.
Inventor(s): Miyazaki; Kazuki (Tokyo, JP), Kusano; Kazutomi (Tsukuba, JP), Takase; Yasutaka (Tsukuba, JP), Asano; Osamu (Tsukuba, JP), Shirato; Manabu (Tsukuba, JP), Wakita; Hisashi (Tsukuba, JP), Ishii; Naoto (Tsukuba, JP), Saeki; Takao (Tsukuba, JP), Saeki, legal representative; Tomoko (Moriya, JP), Saeki, legal representative; Mai (Moriya, JP)
Assignee: Eisai R&D Management Co., Ltd. (Tokyo, JP)
Application Number:11/707,904
Patent Claims:1. A compound represented by the formula (I), salt thereof, or hydrate thereof: ##STR00033## wherein R represents hydroxyl, C.sub.1-6 alkoxy optionally substituted with C.sub.1-6 alkoxy, or amino optionally substituted with C.sub.1-6 alkyl.

2. The compound, salt thereof, or hydrate thereof according to claim 1, wherein R--C(.dbd.O)-- where R represents hydroxyl, C.sub.1-6 alkoxy optionally substituted with C.sub.1-6 alkoxy, or amino optionally substituted with C.sub.1-6 alkyl is bonded at the meta or para position.

3. The compound, salt thereof, or hydrate thereof according to claim 1, wherein R represents hydroxyl, C.sub.1-3 alkoxy optionally substituted with C.sub.1-3 alkoxy, or amino optionally substituted with C.sub.1-3 alkyl.

4. The compound, salt thereof, or hydrate thereof according to claim 1, wherein R represents hydroxyl, methoxy, ethoxy, 1-propoxy, 2-propoxy, methoxyethoxy, amino, methylamino, dimethylamino, ethylamino, or diethylamino.

5. Methyl N-[3-(6,7-dimethoxy-2-methylaminoquinazolin-4-yl) phenyl]terephthalamic acid, salt thereof, or hydrate thereof, ethyl N-[3-(6,7-dimethoxy-2-methylaminoquinazolin-4-yl)phenyl]terephthalamic acid, salt thereof, or hydrate thereof, N-[3-(6,7-dimethoxy-2-methylaminoquinazolin-4-yl)phenyl]-N'-methylterepht- halamide, salt thereof, or hydrate thereof, isopropyl N-[3-(6,7-dimethoxy-2-methylaminoquinazolin-4-yl)phenyl]terephthalamic acid, salt thereof, or hydrate thereof, isopropyl N-[3-(6,7-dimethoxy-2-methylaminoquinazolin-4-yl)phenyl]isophthalic acid, salt thereof, or hydrate thereof, N-[3-(6,7-dimethoxy-2-methylaminoquinazolin-4-yl)phenyl]terephthalamic acid 2-methoxyethyl ester, salt thereof, or hydrate thereof, or N-[3-(6,7-dimethoxy-2-methylaminoquinazolin-4-yl)phenyl]isophthalamic acid 2-methoxyethyl ester, salt thereof, or hydrate thereof.

6. Methyl N-[3-(6,7-dimethoxy-2-methylaminoquinazolin-4-yl) phenyl]terephthalamic acid, salt thereof, or hydrate thereof.

7. Ethyl N-[3-(6,7-dimethoxy-2-methylaminoquinazolin-4-yl) phenyl]terephthalamic acid, salt thereof, or hydrate thereof.

8. N-[3-(6,7-Dimethoxy-2-methylaminoquinazolin-4-yl)phenyl]-N'-methyltere- phthalamide, salt thereof, or hydrate thereof.

9. Isopropyl N-[3-(6,7-dimethoxy-2-methylaminoquinazolin-4- yl) phenyl]terephthalamic acid, salt thereof, or hydrate thereof.

10. Isopropyl N-[3-(6,7-dimethoxy-2-methylaminoquinazolin-4-yl) phenyl]isophthalic acid, salt thereof, or hydrate thereof.

11. N-[3-(6,7-Dimethoxy-2-methylaminoquinazolin-4-yl) phenyl]terephthalamic acid 2-methoxyethyl ester, salt thereof, or hydrate thereof.

12. N-[3-(6,7-Dimethoxy-2-methylaminoquinazolin-4-yl) phenyl]isophthalamic acid 2-methoxyethyl ester, salt thereof, or hydrate thereof.

13. A method of relieving pruritus in a subject comprising administering the compound, salt thereof, or hydrate thereof according to claim 1.

14. The method according to claim 13, wherein the subject is suffering from atopic disease.

15. The method according to claim 14, wherein the atopic disease is atopic dermatitis.

16. The method according to claim 13, wherein the pruritus is not curable by a steroid drug and/or an anti-histamine agent.

17. The method according to claim 13, wherein the compound, salt thereof, or hydrate thereof is administered in the form of an external preparation.

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