US 7,538,123 B2
Indole derivative having piperidine ring
Yuichi Suzuki, Tsukuba (Japan); Koichi Ito, Tsukuba (Japan); Atsushi Sasaki, Tsukuba (Japan); Koshi Ueno, Tsukuba (Japan); Miyuki Sakai, Tsukuba (Japan); Hiroki Ishihara, Tsukuba (Japan); and Atsuhiko Kubota, Tsukuba (Japan)
Assigned to Eisai R & D Management Co., Ltd., Tokyo (Japan)
Appl. No. 11/579,903
PCT Filed May 11, 2005, PCT No. PCT/JP2005/008632
§ 371(c)(1), (2), (4) Date Nov. 08, 2006,
PCT Pub. No. WO2005/108389, PCT Pub. Date Nov. 17, 2005.
Claims priority of application No. 2004-142437 (JP), filed on May 12, 2004.
Prior Publication US 2007/0219179 A1, Sep. 20, 2007
Int. Cl. A61K 31/454 (2006.01)
U.S. Cl. 514—323  [514/300; 514/370] 29 Claims
 
1. A compound represented by the following formula (I) or a pharmacologically acceptable salt thereof:

OG Complex Work Unit Drawing
wherein R1 and R2 are substituents adjacent to each other, and together with two carbon atoms to each of which they attach, form:
(1) a 5- to 7-membered non-aromatic carbocyclic group,
(2) a 5- to 7-membered non-aromatic heterocyclyl group,
(3) a 6-membered aromatic carbocyclic group, or
(4) a 5- or 6-membered aromatic heterocyclyl group,
which may be substituted by 1 to 4 substituents selected from the following substituent group B1;
R3 represents a hydrogen atom or a methyl group; and
R6 represents a substituent selected from the following substituent group A1,
Substituent group A1: (1) a hydrogen atom, (2) a halogen atom, (3) a cyano group, (4) a hydroxyl group, (5) a nitro group, (6) a carboxyl group, (7) a C3-C8 cycloalkyl group, (8) a C2-C6 alkenyl group, (9) a C2-C6 alkynyl group, (10) a C1-C6 alkylthio group, (11) a C1-C6 alkoxycarbonyl group, (12) a C1-C6 alkylsulfonyl group, (13) a C1-C6 alkyl group (wherein said C1-C6 alkyl group may be substituted by 1 to 3 substituents selected from the group consisting of a halogen atom, a hydroxyl group, and a C1-C6 alkoxy group), (14) a C1-C6 alkoxy group (wherein said C1-C6 alkoxy group may be substituted by 1 to 3 halogen atoms), (15) an amino group (wherein said amino group may be substituted by a substituent selected from the group consisting of a C1-C6 alkyl group, a formyl group, a C1-C6 alkanoyl group, and a C1-C6 alkylsulfonyl group), and (16) a carbamoyl group (wherein said carbamoyl group may be substituted by one or two C1-C6 alkyl groups);
Substituent group B1: (1) a hydrogen atom, (2) a halogen atom, (3) a cyano group, (4) a hydroxyl group, (5) a nitro group, (6) an oxo group, (7) a carboxyl group, (8) a C3-C8 cycloalkyl group, (9) a C2-C6 alkenyl group, (10) a C2-C6 alkynyl group, (11) a C1-C6 alkylthio group, (12) a C1-C6 alkoxycarbonyl group, (13) a C1-C6 alkylsulfonyl group, (14) a C1-C6 alkyl group (wherein said C1-C6 alkyl group may be substituted by a halogen atom, a hydroxyl group, or a C1-C6 alkoxy group), (15) a C1-C6 alkoxy group (wherein said C1-C6 alkoxy group may be substituted by 1 to 3 halogen atoms), (16) an amino group (wherein said amino group may be substituted by a substituent selected from the group consisting of a C1-C6 alkyl group, a formyl group, a C1-C6 alkanoyl group, and a C1-C6 alkylsulfonyl group), (17) a carbamoyl group (wherein said carbamoyl group may be substituted by one or two C1-C6 alkyl groups), (18) a C1-C6 alkoxyimino group, (19) a C5-C6 cycloalkyl group formed by two C1-C3 alkyl groups attaching to the same carbon atom, and (20) a tetrahydropyranyl group formed by two C1-C3 alkyl group attaching to the same carbon atom, together with an oxygen atom and said carbon atom.