| US 7,531,532 B2 | ||
| Pyridine derivative and pyrimidine derivative | ||
| Tomohiro Matsushima, Tsukuba (Japan); Keiko Takahashi, Tsukuba (Japan); Setsuo Funasaka, Tsukuba (Japan); and Hiroshi Obaishi, Tsukuba (Japan) | ||
| Assigned to Eisai R&D Management Co., Ltd., Tokyo (Japan) | ||
| Filed on Feb. 25, 2005, as Appl. No. 11/65,631. | ||
| Claims priority of application No. P2004-054451 (JP), filed on Feb. 27, 2004; and application No. P2004-370801 (JP), filed on Dec. 22, 2004. | ||
| Prior Publication US 2005/0277652 A1, Dec. 15, 2005 | ||
| Int. Cl. C07D 213/75 (2006.01); C07D 239/48 (2006.01); C07D 239/47 (2006.01); A61K 31/44 (2006.01) | ||
| U.S. Cl. 514—218 [514/235.8; 514/252.14; 514/252.18; 514/269; 540/575; 544/122; 544/319] | 25 Claims |
1. A compound represented by the following formula, or a salt thereof:
 wherein R1 represents C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 cycloalkyl, C6-10 aryl, C1-6 alkoxy, 5- to 10-membered heteroaryl, a 3- to 10-membered non-aromatic heterocyclic group or a group represented by the formula
—NR11aR11b, and R1 may be substituted with a substituent selected from the group consisting of Substituent Group A and Substituent Group B, wherein
R11a and R11b may be the same or different and each represents hydrogen, C1-6 alkyl, C3-6 alkenyl, C3-6 alkynyl, C3-10 cycloalkyl, C6-10 aryl, C1-6 alkoxy, 5- to 10-membered heteroaryl or a 4- to 10-membered non-aromatic heterocyclic group, and R11a and R11b may be substituted with a substituent selected from the group consisting of Substituent Group A and Substituent Group B;
R2 and R3 represent hydrogen;
R4, R5, R6 and R7 may be the same or different and each represents hydrogen, halogen, hydroxyl, cyano, trifluoromethyl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkoxy, amino, mono-C1-6 alkylamino, di-C1-6 alkylamino or a group represented by the formula —CO—R12, wherein R12 represents hydrogen, hydroxyl, C1-6 alkyl, C1-6 alkoxy, amino, mono-C1-6 alkylamino or di-C1-6 alkylamino;
R8 represents hydrogen or C1-6 alkyl;
R9 represents C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 cycloalkyl, C6-10 aryl, C3-10 cycloalkyl-C1-6 alkyl, C6-10 aryl-C1-6 alkyl, C1-6 alkoxy, 5- to 10-membered heteroaryl, a 3- to 10-membered non-aromatic heterocyclic group, 5- to 10-membered heteroaryl-C1-6 alkyl, 3- to 10-membered non-aromatic heterocyclic-C1-6 alkyl or a group represented by the formula —NR11aR11b, and R9 may be substituted with a substituent selected from the group consisting of Substituent Group A and Substituent Group B, wherein
R11a and R11b represent the same meaning as recited above;
V1 and V2 may be the same or different and each represents oxygen or sulfur;
W represents a group represented by the formula —N(RW3)—, wherein RW3 represents hydrogen or C1-6 alkyl;
X represents nitrogen; and
Y represents oxygen, sulfur, sulfinyl, sulfonyl or a group represented by the formula —N(RY)—, wherein RY represents hydrogen or C1-6 alkyl,
wherein Substituent Group A is selected from the group consisting of halogen, hydroxyl, mercapto, nitro, cyano and oxo;
wherein Substituent Group B is selected from the group consisting of C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 cycloalkyl, C6-10 aryl, 5- to 10-membered heteroaryl, a 3- to 10-membered non-aromatic heterocyclic group, C1-6 alkoxy, C3-6 alkenyloxy, C3-6 alkynyloxy, C3-10 cycloalkoxy, C6-10 aryloxy, 5- to 10-membered heteroaryloxy, 4- to 10-membered non-aromatic heterocyclicoxy, C1-6 alkylthio, C3-6 alkenylthio, C3-6 alkynylthio, C3-10 cycloalkylthio, C6-10 arylthio, 5- to 10-membered heteroarylthio, 4- to 10-membered non-aromatic heterocyclicthio and a group represented by the
formula -T1-T2-T3, and each group in Substituent Group B may be substituted with a substituent selected from the group consisting of Substituent
Group C, wherein T1 represents a direct bond or C1-6 alkylene, T2 represents carbonyl, sulfinyl, sulfonyl, a group represented by the formula —C(═O)—O—, a group represented by the formula
—O—C(═O)—, a group represented by the formula —SO2—O—, a group represented by the formula —O—SO2—, a group represented by the formula —NRT1—, a group represented by the formula —C(═O)—NRT1—, a group represented by the formula —NRT1—C(═O)—, a group represented by the formula —SO2—NRT1— or a group represented by the formula —NRT1—SO2—, T3 represents hydrogen, C1-6 alkyl, C3-6 alkenyl, C3-6 alkynyl, C3-10 cycloalkyl, C6-10 aryl, 5- to 10-membered heteroaryl or a 4- to 10-membered non-aromatic heterocyclic group, and RT1 represents hydrogen or C1-6 alkyl; and
wherein Substituent Group C is selected from the group consisting of halogen, hydroxyl, mercapto, nitro, cyano, oxo, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 cycloalkyl, C6-10 aryl, 5- to 10-membered heteroaryl, a 3- to 10-membered non-aromatic heterocyclic group, C1-6 alkoxy and C1-6 alkylthio.
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