Ergoline derivatives

A compound of formula I

• wherein
• either each of R1 and R2, independently, is H;
• optionally R10- and/or R11-substituted phenyl;
• optionally R10- and/or R11-substituted phenyl-C1-C4-alkyl;
• optionally R10- and/or R11-substituted heteroaryl-C1-C4-alkyl;
• optionally R10- and/or R11-substituted heteroaryl N-oxide;
• optionally R10-substituted C1-C8-alkyl;
• optionally R10-substituted C2-C8-alkenyl;
• optionally R10-substituted C2-C8-alkynyl;
• optionally R10-substituted C3-C8-cycloalkyl;
• or optionally R10-substituted C4-C8-cycloalkenyl;
• or R1 and R2 form, together with the nitrogen atom to which they are attached, an optionally R10-substituted 3-8-membered ring containing, in addition to the nitrogen atom, up to 2 other heteroatoms selected independently from N, O and S;
• where R10 represents 1-to-4 substituents independently selected from C1-C6-alkyl;
• C1-C6-hydroxyalkyl;
• C1-C6-alkoxyalkyl;
• C1-C6-halogenoalkyl;
• C3-C6-cycloalkyl;
• C2-C6-alkenyl;
• C3-C6-cycloalkenyl;
• C2-C6-alkynyl;
• phenyl;
• heteroaryl;
• heteroaryl N-oxide;
• F;
• Cl;
• Br;
• I;
• OH;
• OR9;
• OCOR9;
• OCOOR9;
• OCONHR9;
• OCONR9R9;OSO2R9;
• COR9;
• COOH;
• COOR9;
• CONH2;
• CONHR9;
• CONR9R9;
• CF3;
• CHF2;
• CH2F;
• C1-C4-alkylNH2;
• C1-C4-alkylNHR9;
• C1-C4-alkylNR9R9;
• CN;
• NO2;
• NH2;
• NHR9;
• NR9R9;
• NHCOR9;
• NR9COR9;
• NHCONHR9;
• NHCONH2;
• NR9CONHR9;
• NR9CONR9R9;
• NHCOOR9;
• NR9COOR9;
• NHSO2R9;
• N(SO2R9)2;
• NR9SO2R9;
• SR9;
• SOR9;
• SO2R9;
• SO2NH2;
• SO2NHR9;
• SO2NR9R9;
• or R10 is ═O attached to a carbon atom of phenyl or heteroaryl, or may be one or two ═O's attached to the same S atom of heteroaryl, if any;
• R11 represents two adjacent substituents which form an annulated 4-7-membered nonaromatic ring optionally containing up to two heteroatoms selected independently from N, O and S;
• and
• each R9, independently, is C1-C6-alkyl;
• hydroxyl-C1-C6-alkyl;
• C3-C6-cycloalkyl;
• C2-C6-alkenyl;
• C2-C6-alkynyl;
• phenyl;
• benzyl;
• heteroaryl;
• —CH2-heteroaryl;
• or CF3;
• or two R9's, together with the N-atom to which they are attached, form an optionally R10-substituted 4-8-membered ring containing, in addition to the N-atom, up to 2 other heteroatoms selected independently from N, O and S;
• R3 is H;
• OR1;
• CH2R1R2;
• CH2NR1R2;
• (CH2)2NR1R2;
• CH2—CH2—OR1;
• CH2—CO—NR1R2;
• or CO—CH2R1R2;
• R4 is F;
• Cl;
• Br;
• I;
• OR1;
• NR1R2;
• H;
• optionally R10- and/or R11-substituted phenyl;
• optionally R10- and/or R11-substituted phenyl-C1-C4-alkyl;
• optionally R10- and/or R11-substituted heteroaryl;
• optionally R10- and/or R11-substituted heteroaryl-C1-C4-alkyl;
• optionally R10- and/or R11-substituted heteroaryl N-oxide;
• optionally R10-substituted C1-C8-alkyl;
• optionally R10-substituted C2-C8-alkenyl;
• optionally R10-substituted C2-C8-alkynyl;
• optionally R10-substituted C3-C8-cycloalkyl;
• or optionally R10-substituted C4-C8-cycloalkenyl;
• and
• R5 is optionally R10- and/or R11-substituted phenyl;
• optionally R10- and/or R11-substituted phenyl-C1-C4-alkyl;
• optionally R10- and/or R11-substituted heteroaryl;
• optionally R10-and/or R11-substituted heteroaryl-C1-C4-alkyl;
• optionally R10- and/or R11-substituted heteroaryl N-oxide;
• optionally R10-substituted C1-C8-alkyl;
• optionally R10-substituted C2-C8-alkenyl;
• optionally R10-substituted C2-C8-alkynyl;
• optionally R10-substituted C3-C8-cycloalkyl;
• or optionally R10-substituted C4-C8-cycloalkenyl, in free form or in salt form.