| US 7,572,801 B2 | ||
| Pyridopyrimidinone derivatives which are HM74A agonists | ||
| Aurelia Conte, Basel (Switzerland); Henrietta Dehmlow, Grenzach-Wyhlen (Germany); Uwe Grether, Efringen-Kirchen (Germany); Nicole A. Kratochwil, Sool (Switzerland); Holger Kuehne, Grenzach-Wyhlen (Germany); Robert Narquizian, St. Louis (France); Constantinos Panousis, Bottmingen (Switzerland); Jens-Uwe Peters, Grenzach-Wyhlen (Germany); Fabienne Ricklin, Hombourg (France); and Stephan Roever, Inzlingen (Germany) | ||
| Assigned to Hoffmann-La Roche Inc., Nutley, N.J. (US) | ||
| Filed on May 11, 2007, as Appl. No. 11/801,863. | ||
| Prior Publication US 2007/0275987 A1, Nov. 29, 2007 | ||
| Int. Cl. A61K 31/519 (2006.01); C07D 471/04 (2006.01); A61P 9/10 (2006.01); A61P 3/00 (2006.01); A61P 3/10 (2006.01) | ||
| U.S. Cl. 514—264.1 [514/264.11; 544/279; 546/316] | 39 Claims |
1. A compound of formula (I):
 (a) X is selected from the group consisting of:
(1) a single bond,
(2) O,
(3) N(R9)C(O),
(4) N(R9)C(O)O,
(5) OC(O)NR9,
(6) N(R9)C(O)NR10,
(7) N(R9)SO2, and
(8) C(O)NR9 if m is 1, 2 or 3;
(b) Y is selected from the group consisting of:
(1) a single bond, and
(2) O if n is 1, 2, 3, 4, 5 or 6;
(c) R1, R2 and R3 are independently from each other selected from the group consisting of:
(1) hydrogen,
(2) halogen,
(3) lower-alkyl,
(4) fluoro-lower-alkyl,
(5) lower-alkoxy,
(6) fluoro-lower-alkoxy, and
(7) cycloalkyl;
(d) R4, R5, R6 and R7 are independently from each other selected from the group consisting of:
(1) hydrogen,
(2) fluoro,
(3) lower-alkyl, and
(4) fluoro-lower-alkyl; or alternatively,
R4 and R5 are bound together to form a ring together with the carbon atom to which they are attached wherein —R4—R5— is —(CH2)2-6—, or R6 and R7 are bound together to form a ring together with the carbon atom to which they are attached wherein —R6—R7— is —(CH2)2-6—;
(e) R8 is aryl or heteroaryl, wherein said aryl or heteroaryl is optionally substituted with 1 to 3 substituents independently from
each other selected from the group consisting of:
(1) halogen,
(2) lower-alkyl,
(3) lower-alkoxy,
(4) fluoro-lower-alkyl,
(5) fluoro-lower-alkoxy,
(6) cycloalkyl,
(7) fluoro-cycloalkyl,
(8) cycloalkyl-oxy,
(9) C(O)OH,
(10) lower-alkoxy-C(O),
(11) NH2C(O),
(12) N(H,lower-alkyl)C(O),
(13) N(lower-alkyl)2C(O),
(14) OH,
(15) lower-alkyl-C(O)O,
(16) NH2,
(17) N(H,lower-alkyl),
(18) N(lower-alkyl)2,
(19) lower-alkyl-C(O)NH,
(20) lower-alkyl-C(O)N(lower-alkyl),
(21) NH2SO2,
(22) N(H,lower-alkyl)SO2,
(23) N(lower-alkyl)2SO2,
(24) lower-alkyl-SO2—NH,
(25) lower-alkyl-SO2—N(lower-alkyl),
(26) cyano, and
(27) phenyl which is optionally substituted with 1 to 3 substituents independently selected from the group consisting of halogen,
lower-alkyl, lower-alkoxy and fluoro-lower-alkyl;
(f) R9 and R10 independently from each other are selected from the group consisting of:
(1) hydrogen,
(2) lower-alkyl, and
(3) fluoro-lower-alkyl; and
(g) m is 0, 1, 2 or 3; and n is 0, 1, 2, 3, 4, 5 or 6; wherein m+n is ≧1.
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