| US 7,414,060 B2 | ||
| Pyridine-2-carboxyamide derivatives | ||
| Georg Jaeschke, Basel (Switzerland); Sabine Kolczewski, Rheinfelden (Germany); Richard Hugh Philip Porter, Reinach (Switzerland); and Eric Vieira, Frenkendorf (Switzerland) | ||
| Assigned to Hoffmann-La Roche Inc., Nutley, N.J. (US) | ||
| Filed on Feb. 23, 2006, as Appl. No. 11/360,085. | ||
| Claims priority of application No. 05101701 (EP), filed on Mar. 04, 2005. | ||
| Prior Publication US 2006/0199960 A1, Sep. 07, 2006 | ||
| Int. Cl. C07D 401/14 (2006.01); A61K 31/4436 (2006.01) | ||
| U.S. Cl. 514—256 [514/332; 514/333; 514/336; 514/341; 514/342; 514/354; 544/328; 546/256; 546/262; 546/270.4; 546/275.4; 546/280.4; 546/323] | 19 Claims |
19. A pharmaceutical composition comprising a therapeutically effective amount of a compound selected from the group consisting
of
 R2 is H, C1-C7-alkyl, C3-C6-cycloalkyl, or —(CH2)m—Ra;
R3 is aryl or a 5- or 6-membered heteroaryl each of which is optionally substituted by:
CN, Cl, F, Br, CF3, CHF2, —O—C1-C7-alkyl, —(CO)—Rb, —(CH2)m—Rc, —NH—(CO)—C1-C7-alkyl, —O—CH2F, —O—CHF2, —O—CF3, —S(O)2—Rd, C3-C6-cycloalkyl, or heteroaryl which is optionally substituted by C1-C7-alkyl; and
R4 is H, —OH, Cl, F, Br, CN, —CHF2, CF3, C1-C7-alkyl, —O—(CO)—C1-C7-alkyl, C3-C6-cycloalkyl, or —(CH2)m—Re;
 R2 is H, C1-C7-alkyl, C3-C6-cycloalkyl, or —(CH2)m—Ra;
R3 is aryl or a 5- or 6-membered heteroaryl each of which is optionally substituted by:
CN, Cl, F, Br, CF3, CHF2, —O—C1-C7-alkyl, —(CO)—Rb, —(CH2)m—Rc, —NH—(CO)—C1-C7-alkyl, —O—CH2F, —O—CHF2, —O—CF3, —S(O)2—Rd, C3-C6-cycloalkyl, or heteroaryl which is optionally substituted by C1-C7-alkyl; and
R4 is H, —OH, Cl, F, Br, CN, —CHF2, CF3, C1-C7-alkyl, —O—(CO)—C1-C7-alkyl, C3-C6-cycloalkyl, or —(CH2)m—Re;
 R2 is H or C1-C7-alkyl;
R3 is phenyl or a 5- or 6-membered heteroaryl each of which is optionally substituted by:
CN, Cl, F, Br, CF3, CHF2, —O—C1-C7-alkyl, —(CO)—Rb, —(CH2)m—Rc, —NH—(CO)—C1-C7-alkyl, O—CH2F, —O—CHF2, —O—CF3, —S(O)2—Rd, or heteroaryl which is optionally substituted by C1-C7-alkyl; and
R5 is C1-C7-alkyl, C1-C7-alkyl-C3-C6-cycloalkyl, —(CH2)n—O—Rf, C3-C8-alkenyl-O—Rf, —(CH2)n—NRgRh, or —C2-C6-alkenyl-NRgRh, or —(CH2)n—Re;
 R2 is H or C1-C7-alkyl;
R3 is phenyl or a 5- or 6-membered heteroaryl each of which is optionally substituted by:
CN, Cl, F, Br, CF3, CHF2, —O—C1-C7-alkyl, —(CO)—Rb, —(CH2)m—Rc, —NH—(CO)—C1-C7-alkyl, —O—CH2F, —O—CHF2, —O—CF3, —S(O)2—Rd, or heteroaryl which is optionally substituted by C1-C7-alkyl; and
R4 is H, —OH, Cl, F, Br, CN, —CHF2, CF3, C1-C7-alkyl, —O—(CO)—C1-C7-alkyl, or —(CH2)m—Re;
 R2 is H or C1-C7-alkyl;
R3 is phenyl or a 5- or 6-membered heteroaryl each of which is optionally substituted by:
CN, Cl, F, Br, CF3, CHF2, —O—C1-C7-alkyl, —(CO)—Rb, —(CH2)m—Rc, —NH—(CO)—C1-C7alkyl, —O—CH2F, —O—CHF2, —O—CF3, —S(O)2—Rd, or heteroaryl which is optionally substituted by C1-C7-alkyl; and
R4 is H, —OH, Cl, F, Br, CN, —CHF2, CF3, C1-C7-alkyl, —O—(CO)—C1-C7-alkyl, or —(CH2)m—Re;
 R2 is H, C1-C7-alkyl;
R3 is phenyl or a 5- or 6-membered heteroaryl each of which is optionally substituted by:
CN, Cl, F, Br, CF3, CHF2, —O—C1-C7-alkyl, —(CO)—Rb, —(CH2)m—Rc, —NH—(CO)—C1C7alkyl, —O—CH2F, —O—CHF2, —O—CF3, —S(O)2—Rd, or heteroaryl which is optionally substituted by C1-C7-alkyl; and
R4 is H, —OH, Cl, F, Br, CN, —CHF2, CF3, C1-C7-alkyl, —O—(CO)—C1-C7-alkyl, or —(CH2)m—Re;
and
 R2 is H or C1-C7-alkyl;
R3 is phenyl or a 5- or 6-membered heteroaryl each of which is optionally substituted by:
CN, Cl, F, Br, CF3, CHF2, —O—C1-C7-alkyl, —(CO)—Rb, —(CH2)m—Rc, —NH—(CO)—C1-C7alkyl, —O—CH2F, —O—CHF2, —O—CF3, —S(O)2—Rd, or heteroaryl which is optionally substituted by C1-C7-alkyl; and
R4 is H, —OH, Cl, F, Br, CN, —CHF2, CF3, C1-C7-alkyl, —O—(CO)—C1-C7-alkyl, or —(CH2)m—Re;
or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.
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