| US 7,585,878 B2 | ||
| Benzamide derivative or salt thereof | ||
| Takahiro Kuramochi, Chuo-ku (Japan); Norio Asai, Chuo-ku (Japan); Kazuhiro Ikegai, Chuo-ku (Japan); Seijiro Akamatsu, Chuo-ku (Japan); Hironori Harada, Chuo-ku (Japan); Noriko Ishikawa, Chuo-ku (Japan); Shohei Shirakami, Chuo-ku (Japan); Satoshi Miyamoto, Chuo-ku (Japan); Toshihiro Watanabe, Chuo-ku (Japan); and Tetsuo Kiso, Chuo-ku (Japan) | ||
| Assigned to Astellas Pharma Inc., Tokyo (Japan) | ||
| Appl. No. 10/560,282 PCT Filed Jun. 10, 2004, PCT No. PCT/JP2004/008479 § 371(c)(1), (2), (4) Date Dec. 12, 2005, PCT Pub. No. WO2004/110986, PCT Pub. Date Dec. 23, 2004. |
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| Claims priority of application No. 2003-167865 (JP), filed on Jun. 12, 2003; and application No. 2003-405086 (JP), filed on Dec. 03, 2003. | ||
| Prior Publication US 2007/0167444 A1, Jul. 19, 2007 | ||
| Int. Cl. C07D 413/02 (2006.01); C07D 403/02 (2006.01); A61K 31/538 (2006.01); A61K 31/404 (2006.01) | ||
| U.S. Cl. 514—313 [546/159; 546/175; 546/176; 514/314] | 17 Claims |
1. A benzamide derivative represented by formula (I):
  L: a lower alkylene;
D ring: a bicyclic heteroaromatic ring selected from the group consisting of quinoline, dihydroquinoline, and tetrahydroquinoline;
E ring: a monocyclic or bicyclic hydrocarbon ring, or a 5- to 12-membered monocyclic or bicyclic heteroaromatic ring containing
1 to 4 atoms selected from the group consisting of N, S, and O;
G ring: a 4- to 12-membered monocyclic or bicyclic heterocycle containing 1 to 4 atoms selected from the group consisting
of N, S, and O;
R1 to R9: the same or different, a hydrogen atom, a halogen atom, a lower alkyl, a halogen-substituted lower alkyl, —OH, —SH, —O-lower
alkyl, —O-lower alkyl-NH-lower alkyl, —O-lower alkyl-N(lower alkyl)2, ═O, —NH2, —NH-lower alkyl, —N(lower alkyl)2, —S-lower alkyl, —SO-lower alkyl, —SO2-lower alkyl, —CN, —COOH, —C(═O)—O-lower alkyl, —C(═O)—NH2, —C(═O)—NH-lower alkyl, —C(═O)—N(lower alkyl)2, —NH—C(═O)—O-lower alkyl, —NH—SO2-lower alkyl, —SO2—NH2, —SO2—NH-lower alkyl, —C(═O)-lower alkyl, —NO2 or a nitrogen-containing saturated heterocycle,
R10: a hydrogen atom or a lower alkyl,
R11 to R15: the same or different, a hydrogen atom, a halogen atom, a lower alkyl, a halogen-substituted lower alkyl, —OH, —O-lower
alkyl, —S-lower alkyl, —SO-lower alkyl, —SO2-lower alkyl, ═O, —C(═O)H, —C(═O)-lower alkyl, —COOH, —CN, —NH2, —NH-lower alkyl, —N(lower alkyl)2, —C(═O)—NH2, —C(═O)—NH-lower alkyl, —C(═O)—N(lower alkyl)2, —C(═O)-aryl, —C(═O)—NH-aryl, —NH—C(═O)-lower alkyl, —NH—C(═O)-aryl, —NH—SO2-lower alkyl, —N(lower alkyl)-SO2-lower alkyl, -lower alkylene-NH—SO2-lower alkyl, -lower alkylene-NH—SO2-aryl, —C(═O)—O-lower alkyl, -lower alkylene-OH, -lower alkylene-C(═O)—NH-lower alkyl, -lower alkylene-C(═O)—N(lower alkyl)2, -lower alkylene-C(═O)—NH2, -lower alkylene-C(═O)—OH, -lower alkylene-O-lower alkyl, -lower alkylene-S-lower alkyl, -lower alkylene-O—C(═O)-lower alkyl,
-lower alkylene-NH-lower alkyl, -lower alkylene-N(lower alkyl)2, -lower alkylene-aryl, a cycloalkyl, an aryl,
-(4- to 12-membered monocyclic or bicyclic heterocycle containing 1 to 4 atoms selected from the group consisting of N, S,
and O),
—O-(4- to 12-membered monocyclic or bicyclic heterocycle containing 1 to 4 atoms selected from the group consisting of N,
S, and O),
-lower alkylene-(4- to 12-membered monocyclic or bicyclic heterocycle containing 1 to 4 atoms selected from the group consisting
of N, S, and O),
—C(═O)-(4- to 12-membered monocyclic or bicyclic heterocycle containing 1 to 4 atoms selected from the group consisting of
N, S, and O),
-lower alkylene-N(lower alkyl)-(4- to 12-membered monocyclic or bicyclic heterocycle containing 1 to 4 atoms selected from
the group consisting of N, S, and O), or
—C(═O)—NH-(4- to 12-membered monocyclic or bicyclic heterocycle containing 1 to 4 atoms selected from the group consisting
of N, S, and O),
and the above monocyclic or bicyclic heterocycle may be substituted by halogen atom(s), lower alkyl(s), —O-lower alkyl, or
—OH;
or a salt thereof.
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