Claims for Patent: 7,612,114

Summary for Patent: 7,612,114

Title:	Selective estrogen receptor modulator
Abstract:	The present invention provides a compound represented by the following formula (I); [wherein T represents a single bond, a C1-C4 alkylene group which may have a substituent and the like; formula (I-1) represents a single bond or a double bond; A represents a single bond, a bivalent 5- to 14-membered heterocyclic group which may have a substituent and the like; Y represents a single bond and the like; Z represents a methylene group and the like; ring G represents a phenylene group and the like which may condense with a 5- to 6-membered ring and may have a heteroatom; Ra and Rb are the same as or different from each other and represent a hydrogen atom and the like; W represents a single bond and the like; R′ represents 1 to 4 independent hydrogen atoms and the like; and R″ represents 1 to 4 independent hydrogen atoms and the like] or a salt thereof, or a hydrate thereof.
Inventor(s):	Shinichi Hamaoka, Noritaka Kitazawa, Kazumasa Nara, Atsushi Sasaki, Atsushi Kamada, Tadashi Okabe
Assignee:	Eisai R&D Management Co Ltd
Application Number:	US11/158,245
Patent Claims:	1. A compound represented by the following formula (I); wherein TZ represents a C1-C4 alkylene group or —CRf′Rg′—CH2—O— wherein Rf′ and Rg′ independently represent a C1-C6 alkyl group; A represents a 5- to 14-membered heteroarylene group which may have a substituent or a C6-C14 arylene group which may have a substituent; Y represents —CH2—NRc— wherein Rc represents a C1-C6 alkyl group which may have a substituent; ring G represents the following formula; R′ represents 1 to 4 substituents independently selected from a hydrogen and a C1-C6 alkoxy group; a partial structure in formula (I) represented by the following formula: is R″ represents a hydroxyl group that may be further protected by a protecting group or a C1-C6 alkoxy group which may have a substituent; and Ra and Rb are the same as or different from each other and each represents a hydrogen atom, a C1-C6 alkyl group which may have a substituent, or a C3-C8 cycloalkyl group which may have a substituent, or when Ra and Rb are bonded together, they may form, together with the nitrogen atom that is adjacent to Ra and Rb, a 4- to 10-membered single ring which may have a substituent; and L represents a single bond, or a salt thereof. 2. The compound or the salt thereof, according to claim 1, wherein Ra and Rb independently represent a hydrogen atom, a methyl group, an ethyl group, an n-propyl group, an iso-propyl group, an n-butyl group, an iso-butyl group, or a tert-butyl group. 3. The compound or the salt thereof, according to claim 1, wherein -T-Z represents —CH2CH2 or —C(CH3)2CH2O—. 4. The compound or the salt thereof, according to claim 1, wherein Y represents —CH2—N(CH2CH3)— or —CH2—N(CH2CH2OH)—. 5. The compound or the salt thereof, or the hydrate thereof according to claim 1, wherein each of R″ independently represents a hydrogen atom or a methoxy group. 6. The compound or the salt thereof according to claim 1, wherein R″ represents a hydroxyl group. 7. The compound or the salt thereof, according to claim 1, wherein A represents a phenylene group. 8. A compound selected from the group consisting of (R)-6-{2-{ethyl[4-(2-ethylaminoethyl)benzyl]amino }-4-methoxyphenyl }-5,6,7,8-tetrahydronaphthalen-2-ol, (R)-6-{2-{ethyl [4-(2-ethylaminoethyl)benzyl]amino }-4,5-dimethoxyphenyl }-5,6,7,8-tetrahydronaphthalen-2-ol, (R)-6-{2-{ethyl [4-(2-methylaminoethyl)benzyl]amino }-4-methoxyphenyl }-5,6,7,8-tetrahydronaphthalen-2-ol, (R)-6-{2-[[4-(2-dimethylamino-2-methylpropoxy)benzyl](2-hydroxyethyl)amino]-4-methoxyphenyl }-5 ,6,7,8-tetrahydronaphthalen-2-ol, (R)-6-{2-{ethyl[4-(2-propylaminoethyl)benzyl]amino }-4-methoxyphenyl }-5,6,7,8-tetrahydronaphthalen-2-ol, (R)-6-{2-{[4-(2-butylaminoethyl)benzyl]ethylamino }-4-methoxyphenyl }-5,6,7,8-tetrahydronaphthalen-2-ol, (R)-6-{2-{ethyl [4-(2-isopropylaminoethyl)benzyl]amino }-4-methoxyphenyl }-5,6,7,8-tetrahydronaphthalen-2-ol, (R)-6-{2-{[4-(2-tert-butylaminoethyl)benzyl]ethylamino }-4-methoxyphenyl }-5,6,7,8-tetrahydronaphthalen-2-ol, and (R)-6-{2-{[4-(2-cyclohexylaminoethyl)benzyl]ethylamino }-4-methoxyphenyl }-5,6,7,8-tetrahydronaphthalen-2-ol, or a salt of any of the foregoing. 9. The compound (R)-6-{2-{ethyl [4-(2-ethylaminoethyl)benzyl]amino }-4-methoxyphenyl}-5,6,7,8-tetrahydronaphthalen-2-ol, or a salt thereof. 10. The compound (R)-6-{2-[[4-(2-dimethylamino-2-methylpropoxy)benzyl](2-hydroxyethyl)amino]-4-methoxyphenyl}-5,6,7,8-tetrahydronaphthalen-2-ol, or a salt thereof. 11. A pharmaceutical composition comprising the compound or the salt thereof according to any one of claims 1, 2, and 3-10 and a pharmaceutically acceptable carrier. 12. A method for treating osteoporosis, or breast cancer, which are estrogen-dependent, comprising administering to a mammalian animal an effective amount of the compound or the salt thereof, according to any one of claims 1, 2, and 3-10.