US 7,345,049 B2
Phenylalanine derivatives
Kazuyuki Sagi, Kawasaki (Japan); Tatsuya Okuzumi, Kawasaki (Japan); Tatsuhiro Yamada, Kawasaki (Japan); Shunsuke Kageyama, Kawasaki (Japan); Yoichiro Shima, Kawasaki (Japan); Tadakiyo Nakagawa, Kawasaki (Japan); Munetaka Tokumasu, Kawasaki (Japan); Masayuki Sugiki, Kawasaki (Japan); Hajime Ito, Kawasaki (Japan); Itsuya Tanabe, Kawasaki (Japan); Tamotsu Suzuki, Kawasaki (Japan); Akira Nakayama, Kawasaki (Japan); Kazuyuki Ubukata, Kawasaki (Japan); Kenji Shinkai, Kawasaki (Japan); Yasuhiro Tanaka, Kawasaki (Japan); Misato Noguchi, Kawasaki (Japan); Ayatoshi Andou, Kawasaki (Japan); Yoriko Yamamoto, Kawasaki (Japan); Noriyasu Kataoka, Kawasaki (Japan); and Koichi Fujita, Kawasaki (Japan)
Assigned to Ajinomoto Co., Inc., Tokyo (Japan)
Filed on Dec. 22, 2004, as Appl. No. 11/18,226.
Claims priority of provisional application 60/617026, filed on Oct. 12, 2004.
Claims priority of provisional application 60/539108, filed on Jan. 27, 2004.
Claims priority of application No. 2003-425347 (JP), filed on Dec. 22, 2003; application No. 2004-074943 (JP), filed on Mar. 16, 2004; application No. 2004-159919 (JP), filed on May 28, 2004; and application No. 2004-260319 (JP), filed on Sep. 07, 2004.
Prior Publication US 2005/0222141 A1, Oct. 06, 2005
Int. Cl. A61K 31/517 (2006.01); A61K 31/519 (2006.01); C07D 239/70 (2006.01); C07D 239/95 (2006.01)
U.S. Cl. 514—266.2  [514/266.22; 514/266.3; 514/267; 544/249; 544/250; 544/285] 71 Claims
 
1. A phenylalanine compound of the following formula (1) or pharmaceutically acceptable salts thereof:

OG Complex Work Unit Drawing
wherein R11 represents a hydroxyl group, an alkoxyl group having 1 to 6 carbon atoms which may have a substituent(s), a morpholinoethyloxy group or a benzyloxy group which may be substituted with one or more methyl groups or one or more methoxy groups, R12 and R13 each independently represent a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, an acetyl group or methyloxycarbonyl group, or N(R12)R13 represents 1-pyrrolidinyl group, 1-piperidinyl group, 4-morpholinyl group, 4-thiomorpholinyl group, 3-tetrahydrothiazolyl group or 1-piperazinyl group of which the fourth position may be substituted with an alkyl group having 1 to 3 carbon atoms,
R14 represents a methyl group or an ethyl group,
R1′ represents a hydrogen atom, a fluorine atom or a chlorine atom,
X1 represents —CH(R1a)-, —CH(R1a)CH(R1b)-, —CH(R1a)CH(R1b)CH(R1c)-, —CH(R1a)CH(R1b)CH(R1c)CH(R1d)-, —N(R1a)CH(R1b)CH(R1c)—, —OCH(R1a)CH(R1b)-, —OCH(R1a)CH(R1b)CH(R1c)- or 1,3-pyrrolidinylene, wherein R1a, R1b, R1c and R1d each independently represent a hydrogen atom or a methyl group, and
Y11 and Y12 represent either one of the combinations, (Cl, Cl), (Cl, Me), (Cl, F), (F, F) and (F, Me).