US 7,320,977 B2 | ||
Substituted 2-phenyl-3(2h)-pyridazinones | ||
Rudolf Schohe-Loop, Wuppertal (Germany); Elmar Burchardt, Wuppertal (Germany); Christiane Faeste, Oslo (Norway); Claudia Hirth-Dietrich, Wuppertal (Germany); Jörg Keldenich, Wuppertal (Germany); Andreas Knorr, Erkrath (Germany); Thomas Lampe, Düsseldorf (Germany); Paul Naab, Wuppertal (Germany); Delf Schmidt, Wuppertal (Germany); and Gunter Schmidt, Wuppertal (Germany) | ||
Assigned to Bayer Healthcare AG, Leverkusen (Germany) | ||
Appl. No. 10/511,225 PCT Filed Apr. 08, 2003, PCT No. PCT/EP03/03628 § 371(c)(1), (2), (4) Date Jul. 11, 2005, PCT Pub. No. WO03/097612, PCT Pub. Date Nov. 27, 2003. |
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Claims priority of application No. 102 16 144 (DE), filed on Apr. 12, 2002. | ||
Prior Publication US 2006/0004015 A1, Jan. 05, 2006 | ||
Int. Cl. C07D 403/04 (2006.01); A61K 31/501 (2006.01) |
U.S. Cl. 514—252.02 [514/252.03; 514/227.8; 544/58.2; 544/114; 544/238] | 6 Claims |
1. A compound of the formula (I)
![]() in which
R1 is 5- to 7-membered, saturated or partially unsaturated heterocyclyl which is linked via a ring nitrogen atom and optionally
has a further heteroatom or hetero chain member from the series N, O, S, SO or SO2, and which may be substituted once or twice, identically or differently, by substitutents selected from the group of halogen,
(C1-C6)-alkyl, (C2-C6)-alkenyl, (C3-C8)-cycloalkyl, hydroxy, oxo, carboxyl, (C1-C6)-alkoxycarbonyl, (C1-C6)-alkanoyl, (C3-C8)-cycloalkylcarbonyl, (C1-C6)-alkylsulfonyl, aminocarbonyl,
![]() and (C1-C6)-alkylaminocarbonyl,
where (C1-C6)-alkyl and (C1-C6)-alkanoyl in turn may each be substituted by halogen, hydroxy, (C1-C4)-alkoxy, (C1-C4)-alkoxycarbonyl, amino, mono- or di-(C1-C4)-alkylamino, (C1-C4)-alkoxycarbonylamino or 5- or 6-membered heterocyclyl having up to two heteroatoms from the series N, O and/or S,
or
R1 is 5-membered heteroaryl which is linked via a ring nitrogen atom and has up to two further ring nitrogen atoms, and which
may be substituted once to three times, identically or differently, by halogen, (C1-C6)-alkoxycarbonyl or (C1-C6)-alkyl which is in turn optionally substituted by hydroxy or halogen,
R2 is (C6-C10)-aryl which may be substituted once or twice, identically differently, by substituents selected from the group of halogen,
nitro, cyano, (C1-C6)-alkyl, trifluoromethyl, (C1-C6)-alkanoyl, (C1-C6)-alkoxy, hydroxy, (C1-C6)-acyloxy, amino, (C1-C6)-acylamino, mono- and di-[(C1-C6)-alkylsulfonyl]amino,
where (C1-C6)-alkyl and (C1-C6)-alkoxy in turn may each be substituted by hydroxy, amino, (C1-C4)-alkoxy or (C1-C4)-acylamino,
or
R2 is 5- or 6-membered heteroaryl which has up to two ring nitrogen atoms and which may be substituted by amino, hydroxy, halogen,
(C1-C6)-alkyl or (C1-C6)-alkoxy,
and
R3 is hydrogen, halogen, (C1-C6)-alkyl, trifluoromethyl, nitro, cyano, carboxyl or (C1-C6)-alkoxycarbonyl,
or a salt, solvate or solvate of a salt thereof.
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