US 7,612,114 B2
Selective estrogen receptor modulator
Shinichi Hamaoka, Tsukuba (Japan); Noritaka Kitazawa, Tsukuba (Japan); Kazumasa Nara, Tsukuba (Japan); Atsushi Sasaki, Tsukuba (Japan); Atsushi Kamada, Tsukuba (Japan); and Tadashi Okabe, Tsukuba (Japan)
Assigned to Eisai R&D Management Co., Ltd., Tokyo (Japan)
Filed on Jun. 22, 2005, as Appl. No. 11/158,245.
Application 11/158245 is a continuation in part of application No. PCT/JP03/16808, filed on Dec. 25, 2003.
Claims priority of application No. 2002-378729 (JP), filed on Dec. 26, 2002.
Prior Publication US 2006/0116364 A1, Jun. 01, 2006
Int. Cl. A61K 31/136 (2006.01); C07C 211/44 (2006.01)
U.S. Cl. 514—647  [564/308; 564/307] 12 Claims
 
1. A compound represented by the following formula (I);

OG Complex Work Unit Drawing
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;

OG Complex Work Unit Drawing
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:

OG Complex Work Unit Drawing
is

OG Complex Work Unit Drawing
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.