| US 7,544,709 B2 | ||
| Derivatives of andrimide and moiramide B having antibacterial properties | ||
| Nina Brunner, Essen (Germany); Christoph Freiberg, Wuppertal (Germany); Thomas Lampe, Düsseldorf (Germany); Ben Newton, Bucks (United Kingdom); Michael Otteneder, Arlesheim (Austria); Josef Pernerstorfer, Hilden (Germany); Jens Pohlmann, Wuppertal (Germany); Guido Schiffer, Wuppertal (Germany); and Mitsuyuki Shimada, Nara (Japan) | ||
| Assigned to Bayer Healthcare AG, Leverkusen (Germany) | ||
| Appl. No. 10/496,058 PCT Filed Nov. 07, 2002, PCT No. PCT/EP02/12428 § 371(c)(1), (2), (4) Date Dec. 06, 2004, PCT Pub. No. WO03/043982, PCT Pub. Date May 30, 2003. |
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| Claims priority of application No. 101 56 894 (DE), filed on Nov. 20, 2001. | ||
| Prior Publication US 2005/0080129 A1, Apr. 14, 2005 | ||
| Int. Cl. A61K 31/4015 (2006.01); C07D 207/40 (2006.01) | ||
| U.S. Cl. 514—425 [548/546] | 14 Claims |
1. A compound of formula (I)
 R1 is a group
 where
R1-1 is alkyl, cycloalkyl or aryl,
where
R1-1 can optionally be substituted by from 1 to 3 substituents R1-1-1, R1-1-1 being selected independently at each occurrence from the group consisting of halogen, alkyl, aryl, alkoxy, phenoxy, amino,
monoalkylamino, dialkylamino, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, carboxyl, alkoxycarbonyl, alkylcarbonyl,
heteroaryl and heterocyclyl,
R1-2 and R1-3 are identical or different and are hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl or heterocyclyl,
where
R1-2 can optionally be substituted by from 1 to 3 substituents R1-2-1, R1-2-1 being selected independently at each occurrence from the group consisting of halogen, trifluoromethyl, trifluoromethoxy, nitro,
amino, alkyl, monoalkylamino, dialkylamino, cycloalkyl, aryl, heteroaryl, heterocyclyl, hydroxyl, alkoxy, phenoxy, carboxyl,
alkoxycarbonyl, ailkylcarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, aminosulfonyl, alkylamino-sulfonyl,
dialkylaminosulfonyl, arylaminosulfonyl, heterocyclylaminosulfonyl, heteroarylaminosulfonyl, aminocarbonylamino, hydroxycarbonylamino
and alkoxycarbonylamino, it being possible for aryl and heteroaryl to be substituted by from 1 to 2 substituents selected
independently of one another from the group consisting of halogen, hydroxyl, alkyl, alkoxy, trifluoromethyl, trifluoromethoxy,
nitro, amino, cyano, monoalkylamino and dialkylamino,
or
R1-2 and R1-3 together with the nitrogen atom to which they are attached form a heterocycle which can optionally be benzo-fused,
R1-4 is alkyl, alkenyl, alkynyl, cycloalkyl or aryl,
where
R1-4 can optionally be substituted by from 1 to 3 substituents R1-4-1, R1-4-1 being selected independently at each occurrence from the group consisting of halogen, alkyl, aryl, amino, monoalkylamino,
dialkylamino, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, carboxyl, alkoxycarbonyl, alkylcarbonyl, heteroaryl
and heterocyclyl,
R2 is hydrogen or methyl,
R3 is hydrogen or C1-C3-alkyl,
R4 is hydrogen or C1-C3-alkyl,
R5 is selected from the group consisting of halogen, trifluoromethyl, trifluoromethoxy, nitro, amino, monoalkylamino, dialkylamino,
hydroxyl, alkyl, alkoxy, carboxyl, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, aryl and heteroaryl,
or
two substituents R5 together with the carbon atoms to which they are attached form a cycloalkyl or heterocyclyl,
it being possible for this cycloalkyl or heterocyclyl to be substituted by 0, 1 or 2 substituents R5-1, the substituents R5-1 being selected independently of one another from the group consisting of halogen, alkyl, nitro, amino, trifluoromethyl, hydroxyl
and alkoxy,
n is 0, 1, 2 or 3,
where if n is 2 or 3 the radicals R5 can be identical or different,
R6 is alkyl, cycloalkyl or heterocyclyl,
it being possible for R6 to be substituted by 0, 1 or 2 substituents R6-1, the substituents R6-1 being selected independently of one another from the group consisting of halogen, nitro, amino, trifluoromethyl, hydroxyl,
alkyl and alkoxy,
or a pharmaceutically acceptable salt thereof.
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