Tuberculosis treatment using pleuromutilin derivatives
A method of preventing or treating diseases caused by Mycobacterium , comprising administering to a subject in need of such treatment an effective amount of a pleuromutilin.
1 . A compound selected from the group consisting of compounds of formulae as set out in TABLE 1:
TABLE 1
2 . A compound of formula
wherein
the dotted line is a bond (double bond between positions a=b), R 1A is hydrogen and R 2A is not present, or
the dotted line is no bond (single bond between positions a-b) and R 1A and R 2A independently of each other are hydrogen, halogen or deuterium,
R 3A is (C 1-6 )alkyl,
R 4A is hydrogen, (C 1-6 )alkyl, a group —C(═NH)—NH 2 , or the residue of an amino acid,
R 5A is hydrogen, or
R 4A and R 5A together are a group ═CH—NH 2 ,
R 6A is hydrogen or deuterium, and
m A is 0, 1, 2, 3, 4, or 5.
3 . A compound of formula
wherein
R 1C has the meaning of R 1A as defined in claim 2 ,
R 2C has the meaning of R 2A as defined in claim 2 ,
the dotted line has the meaning as defined in claim 2 ,
R 4C has the meaning of R 6A as defined in claim 2 , and
R 3C is amino, (C 1-4 )alkylamino, di(C 1-4 )alkylamino, the residue of an amino acid, hydroxy, or (C 1-4 )alkoxy.
4 . A compound of formula
wherein
R 1D has the meaning of R 1A as defined in claim 2 ,
R 2D has the meaning of R 2A as defined in claim 2 ,
R 4D has the meaning of R 6A as defined in claim 2 ,
the dotted line has the meaning as defined in claim 2 , and
R 3D is aliphatic heterocyclyl of 4 to 8 ring members, and comprising one nitrogen atom as the heteroatom, or (C 4-8 )cycloalkyl, which heterocyclyl or cycloalkyl is substituted by hydroxy or oxo.
5 . The compound of claim 2 in the form of a salt.
6 . The compound of claim 2 for use as a pharmaceutical.
7 . A pharmaceutical composition comprising a compound of claim 2 in association with at least one pharmaceutical excipient.
8 . The pharmaceutical composition according to claim 6 , further comprising another pharmaceutically active agent.
9 . A pharmaceutical composition comprising a pleuromutilin in association with at least one pharmaceutical excipient, and further comprising another pharmaceutically active agent useful in the treatment of Mycobacterium infections.
10 . The compound of claim 2 for use in the preparation of a medicament for the treatment of microbial diseases.
11 . A method of treatment of microbial diseases, wherein said method comprises administering to a subject in need of such treatment an effective amount of a compound of claim 2 .