Granted Patent B2

US 7,960,412 · App. 12/544,965 · Granted Jun 14, 2011

Abstract

Claims (26)

1. A compound represented by the following formula (I)

wherein

TZ represents a C1-C4 alkylene group or —CR f′ R g′ —CH 2 —O— wherein R f′ and R g′ independently represent hydrogen or 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 —CH 2 —NR c — wherein R c represents hydrogen or 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 atom, a C1-C6 alkoxy group, and a hydroxyl group;

a partial structure in formula (I) represented by the following formula:

is

R″ represents hydrogen, a hydroxyl group that may be further protected by a protecting group or a C1-C6 alkoxy group which may have a substituent; and

R a and R b 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 R a and R b are bonded together, they may form, together with the nitrogen atom that is adjacent to R a and R b , 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 R a and R b independently represent a hydrogen atom, a methyl group, an ethyl group, a n-propyl group, an iso-propyl group, a 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 —CH 2 CH 2 — or —C(CH 3 ) 2 CH 2 O—.

4. The compound or the salt thereof according to claim 1 , wherein Y represents —CH 2 —N(CH 2 CH 3 )— or —CH 2 —N(CH 2 CH 2 OH)—.

5. The compound or the salt 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:

[5-methoxy-2-(6-methoxynaphthalen-2-yl)phenyl]methyl[4-(2-piperidin-1-ylethoxy)benzyl]amine;

6-{4-hydroxy-2-{methyl[4-(2-piperidin-1-ylethoxy)benzyl]amino}phenyl}naphthalene-2-ol;

6-{2-{ethyl[3-fluoro-4-(2-piperidin-1-ylethoxy)benzyl]amino}-4-hydroxyphenyl}naphthalene-2-ol;

6-{2-{ethyl[3-fluoro-4-(2-piperidin-1-ylethoxy)benzyl]amino}phenyl}naphthalene-2-ol, or a salt of any of the foregoing.

9. A pharmaceutical composition comprising the compound or the salt thereof according to any one of claims 1 and 2 - 8 .

10. A method for treating osteoporosis or breast cancer which are estrogen-dependent, said method comprising administering to a mammalian animal an effective amount of the compound or the salt thereof according to any one of claims 1 and 2 - 8 .

Assignments (9)