US 7,612,108 B2
2-phenylthiophene derivative
Junji Miyata, Chuo-ku (Japan); Masaki Yokota, Chuo-ku (Japan); Ryo Naito, Chuo-ku (Japan); Akio Kamikawa, Chuo-ku (Japan); Masakatsu Kawakami, Chuo-ku (Japan); and Kazuyuki Hattori, Chuo-ku (Japan)
Assigned to Astellas Pharma Inc., Tokyo (Japan)
Appl. No. 11/661,294
PCT Filed Aug. 26, 2005, PCT No. PCT/JP2005/015550
§ 371(c)(1), (2), (4) Date Feb. 27, 2007,
PCT Pub. No. WO2006/022375, PCT Pub. Date Mar. 02, 2006.
Claims priority of application No. 2004-249276 (JP), filed on Aug. 27, 2004.
Prior Publication US 2008/0027048 A1, Jan. 31, 2008
Int. Cl. A61K 31/381 (2006.01); C07D 333/16 (2006.01)
U.S. Cl. 514—445  [549/62] 17 Claims
 
1. A compound represented by the following general formula (I) or a salt thereof:

OG Complex Work Unit Drawing
wherein the symbols have the following meanings:
R1: —CO2H, —CO2-lower alkyl, or a tetrazolyl group,
R2: H, halogen, lower alkyl, or —O-lower alkyl,
R3: H, lower alkyl, or halogen,
R4: —CN, —NO2, —Br, halogeno-lower alkyl, or —(CO)-lower alkyl,
R5: H, lower alkyl, —O-lower alkyl, halogen, —NO2, or —CN,
X: —O—, —N(R7)—, or —S—,
wherein the group represented by R4 is bonded to the phenyl group at the meta- or para- position relative to the thienyl group and the group represented by —X—R6 is bonded to the phenyl group at the meta- or para- position relative to the thienyl group,
R7: H or lower alkyl,
R6: linear or branched alkyl having 1 to 8 carbon atoms, linear or branched alkenyl having 3 to 8 carbon atoms, —Y-(cycloalkyl which may contain an oxygen atom), —Y-phenyl, or —Y-heteroaryl,
where the linear or branched alkyl having 1 to 8 carbon atoms, linear or branched alkenyl having 3 to 8 carbon atoms, cycloalkyl which may contain an oxygen atom, phenyl, and heteroaryl may be substituted with a group selected from the group consisting of hydroxy, —CN, —O-lower alkyl, —S-lower alkyl, —NR9(R9), and —(CO)NR9(R9),
Y: a bond, lower alkylene, or lower alkenylene,
R8 and R9: the same or different from each other, H or lower alkyl,
where, when X is a group represented by —N(R7)—, R7 and R6 may be combined together with the nitrogen atom to form a nitrogen-containing saturated heterocycle and the nitrogen-containing saturated heterocycle may be substituted with an lower alkyl.