	US 7,468,380 B2
	Nitrogen-containing aromatic derivatives
Akihiko Tsuruoka, Tsukuba (Japan); Tomohiro Matsushima, Ushiku (Japan); Masayuki Matsukura, Tsukuba (Japan); Kazuki Miyazaki, Tsukuba (Japan); Keiko Takahashi, Ushiku (Japan); Junichi Kamata, Tsukuba (Japan); and Yoshio Fukuda, Tsukuba (Japan)
Assigned to Eisai R&D Management Co., Ltd., Bunkyo-ku, Tokyo (Japan)
Filed on Aug. 18, 2006, as Appl. No. 11/507,082.
Application 11/507082 is a division of application No. 10/651496, filed on Aug. 29, 2003, granted, now 7,109,219.
Claims priority of provisional application 60/464690, filed on Apr. 22, 2003.
Claims priority of application No. 2002-253123 (JP), filed on Aug. 30, 2002.
Prior Publication US 2007/0004764 A1, Jan. 04, 2007
Int. Cl. A61K 31/4439 (2006.01); C07D 401/12 (2006.01)

U.S. Cl. 514—339 [546/277.4]

27 Claims

1. A compound represented by the general formula:

or a salt or hydrate thereof, wherein:

X₁represents a group represented by the formula —CR₁₀═;

X₂represents a group represented by the formula —CR₁₁═;

Y represents an oxygen atom, a sulfur atom, a sulfinyl group, a sulfonyl group, or a group represented by the formula —NR_Y— (wherein R_Yrepresents a hydrogen atom or a C_1-6alkyl group);

R₁represents an optionally substituted C_1-6alkoxy group, an optionally substituted C_6-10aryloxy group, a group represented by the formula —NR_12aR_12b, a group represented by formula (VIII):

(wherein Y_A1and Y_A2each independently represents a group represented by the formula -A₁₀-A₁₁-A₁₂(wherein A₁₀represents a single bond or an optionally substituted C1-6 alkylene; A₁₁represents a single bond, an oxygen atom, a carbonyl group or a sulfonyl group; and A₁₂represents a hydrogen atom, a C_1-6alkyl group, a C_2-6alkenyl group, a C_2-6alkynyl group, a C_3-8cycloalkyl group, a C_6-10aryl group, a 5- to 10-membered heteroaryl group, a group represented by the formula —NR_A10R_A11, a group represented by the formula —OR_A12(wherein R_A10, R_A11and R_A12each independently represents a hydrogen atom, a C1-6 alkyl group or C_3-8cycloalkyl group) or a group represented by the formula:

(wherein e represents 1 or 2; Z represents an oxygen atom, a group represented by the formula —CR_X7R_X8— or a group represented by the formula —NR_X9—; R_X7, R_X8and R_X9each independently represents a hydrogen atom, a hydroxyl group or a C_1-6alkyl group)); and Y_A3represents a hydrogen atom or an optionally substituted C_1-6alkyl group) or a group represented by the formula:

(wherein T1 represents an optionally substituted 5- to 10-membered aromatic heterocycle which may have X in the ring or an optionally substituted 3- to 10-membered heterocycle which may have X in the ring);

R₂, R₃, R₄, R₅, R₆and R₈each represents a hydrogen atom;

R₇represents a halogen atom, a cyano group, an optionally substituted C_1-6alkyl group, an optionally substituted C_2-6alkenyl group, an optionally substituted C_2-6alkynyl group, an optionally substituted C_3-8cycloalkyl group, a group represented by the formula —CO—R₁₃, a group represented by the formula —NR₁₄—CO—R₁₃, a group represented by the formula —SO₂—R₁₅, a group represented by the formula —NR₁₄—SO₂—R₁₅, or a group represented by the formula —NR_16aR_16b;

R₁₀and R₁₁each independently represents a hydrogen atom, a halogen atom, a cyano group, an optionally substituted C_1-6alkyl group, an optionally substituted C_2-6alkenyl group, an optionally substituted C_2-6alkynyl group, an optionally substituted C_3-8cycloalkyl group, a group represented by the formula —CO—R₁₃, a group represented by the formula —NR₁₄—CO—R₁₃, a group represented by the formula —SO₂—R₁₅, a group represented by the formula —NR₁₄—SO₂—R₁₅, or a group represented by the formula —NR_16aR_16b;

R₉represents a group represented by the formula —NR_16aR_16b;

R_12aand R_12beach independently represents a hydrogen atom, an optionally substituted C_1-6alkyl group, an optionally substituted C_3-6alkenyl group, an optionally substituted C_3-6alkynyl group, an optionally substituted C_3-8cycloalkyl group, an optionally substituted 3- to 10-membered heterocyclic group, or an optionally substituted C_1-6alkoxy group;

R₁₃represents a hydrogen atom, an optionally substituted C_1-6alkyl group, an optionally substituted C_2-6alkenyl group, an optionally substituted C_2-6alkynyl group, an optionally substituted C_3-8cycloalkyl group, an optionally substituted C_6-10aryl group, an optionally substituted 5- to 10-membered heteroaryl group, an optionally substituted 3- to 10-membered heterocyclic group, an optionally substituted C_1-6alkoxy group, an optionally substituted C_6-10aryloxy group, a group represented by the formula —NR_12aR_12b, or a group represented by the formula:

(wherein T2 represents an optionally substituted 5- to 10-membered aromatic heterocycle or an optionally substituted 3- to 10-membered heterocycle);

R₁₄represents a hydrogen atom, an optionally substituted C_1-6alkyl group, an optionally substituted C_2-6alkenyl group, an optionally substituted C_2-6alkynyl group, an optionally substituted C_3-8cycloalkyl group, or a group represented by the formula —CO—R₁₃;

R₁₅represents an optionally substituted C_1-6alkyl group, an optionally substituted C_2-6alkenyl group, an optionally substituted C_2-6alkynyl group, an optionally substituted C_3-8cycloalkyl group, an optionally substituted C_6-10aryl group, an optionally substituted 5- to 10-membered heteroaryl group, or an optionally substituted 3- to 10-membered heterocyclic group;

R_16aand R_16beach independently represents a hydrogen atom, an optionally substituted C_1-6alkyl group, an optionally substituted C_3-6alkenyl group, an optionally substituted C_3-6alkynyl group, an optionally substituted C_3-8cycloalkyl group, an optionally substituted C_6-10aryl group or an optionally substituted C_1-6alkoxy group; and

X represents an oxygen atom, a sulfur atom, a carbonyl group, a sulfonyl group, a group represented by the formula —CR_X1R_X2—, or a group represented by the formula —NR_X3— (wherein R_X1, R_X2and R_X3each independently represents a hydrogen atom or a group represented by the formula -A₁-A₂-A₃(wherein A₁and A₂each independently represents a single bond, an optionally substituted C_1-6alkylene group or a carbonyl group; and A₃represents a hydrogen atom, a C_3-8cycloalkyl group, a group represented by the formula —NR_A1R_A2, or the formula —OR_A3(wherein, R_A1, R_A2and R_A3each independently represents a hydrogen atom or a C_1-6alkyl group), or an optionally substituted group represented by the formula:

(wherein a represents 1 or 2))).