PYRROLO CARBOXAMIDES AS MODULATORS OF ORPHAN NUCLEAR RECEPTOR RAR-RELATED ORPHAN RECEPTOR-GAMMA (RORy, NR1F3) ACTIVITY AND FOR THE TREATMENT OF CHRONIC INFLAMMATORY AND AUTOIMMUNE DISEASES

A compound represented by Formula (1)

• an enantiomer, diastereomer, tautomer, N-oxide, solvate, formulation and pharmaceutically acceptable salt thereof,
• wherein
• R1 is selected from H, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-6-cycloalkyl, O3-6-heterocycloalkyl, C1-10-alkylene-C3-10-cycloalkyl, C1-10-alkylene-C3-10-heterocycloalkyl, C1-10-alkylene-(5-membered monocyclic heteroaryl), SO2—C1-10-alkyl, wherein alkyl, alkenyl, alkynyl, alkylene, cycloalkyl, heterocycloalkyl and heteroaryl is unsubstituted or substituted with 1 to 7 substituents independently selected from oxo, CN, OR11, O—C2-6-alkylene-OR11, C1-6-alkyl, halo-C1-6-alkyl, halogen, CO2R11, CONR11R12, COR11, SOyR11, SO3H, SO2NR11R12, NR11COR11, NR11SO2R11, NR11—CO—NR11R12, NR11—SO2—NR11R12, C3-6-cycloalkyl, O—C3-6-cycloalkyl, C3-6-heterocycloalkyl, O—C3-6-heterocycloalkyl and NR11R12;
• and
• R3 is pyridinone, a 6- to 10-membered mono- or bicyclic aryl, a 5- to 10-membered mono- or bicyclic heteroaryl containing 1 to 4 heteroatoms independently selected from the group consisting of N, O and S or a 6- to 12-membered partially saturated spiroheterocycle containing 1 to 4 heteroatoms independently selected from the group consisting of N, O and S,
• wherein pyridinone and spiroheterocycle is optionally substituted with 1 to 4 groups independently selected from halogen, C1-6-alkyl, halo-C1-6-alkyl, OH, O—C1-6-alkyl, O-halo-C1-6-alkyl, oxo, ═N—OR32, N(R32), C0-6-alkylene-C3-10-cycloalkyl, C0-6-alkylene-C3-10-heterocycloalkyl, C0-6-alkylene-(5- or 6-membered monocyclic heteroaryl), C1-6-alkylene-O—R31, C0-6-alkylene-CN, O—C3-10-cycloalkyl, O—C1-6-alkylene-O—R32, O—C3-10-heterocycloalkyl, C0-6-alkylene-COOR31, C0-6-alkylene-C(O)R31, C0-6-alkylene-C(O)N(R31)2, C0-6-alkylene-N(R31)C(O)R31, C0-6-alkylene-SO—R31, C0-6-alkylene-SO2—R31, C0-6-alkylene-SO2—N(R31)2, C0-6-alkylene-N(R31)SO2—R31, C0-6-alkylene-SO2—O3-10-heterocycloalkyl and C0-6-alkylene-SO2—O3-10-heterocycloalkyl,
• wherein alkylene, cycloalkyl, heterocycloalkyl and heteroaryl is optionally substituted by 1 to 4 substituents independently selected from the group consisting of halogen, CN, C1-3-alkyl, halo-C1-3-alkyl, OH, oxo, O—C1-3-alkyl and O-halo-C1-3-alkyl;
• wherein aryl and heteroaryl is substituted with at least one group selected from C3-10-cycloalkyl, C4-heterocycloalkyl, C1-4-alkylene-C3-10-cycloalkyl, C1-4-alkylene-(C3-10-heterocycloalkyl), carbon atom linked 5- or 6-membered monocyclic heteroaryl, C1-6-alkylene-(5- or 6-membered monocyclic heteroaryl), C1-4-alkylene-O—R31, C1-4-alkylene-CN, O—C3-10-cycloalkyl, O—C1-6-alkylene-O—R32, O—C3-10-heterocycloalkyl, C0-6-alkylene-COOR31, C0-6-alkylene-C(O)R31, C0-6-alkylene-C(O)N(R31)2, C0-6-alkylene-N(R31)C(O)R31, C0-6-alkylene-SO—R31, C1-6-alkylene-SO2—R31, C0-6-alkylene-SO2—N(R31)2, C0-6-alkylene-N(R31)SO2—R31, SO2—C3-10-heterocycloalkyl, SO2—C3-10-cycloalkyl, C0-6-alkylene-SO—R31 and two adjacent substituents completing a 3- to 8-membered saturated or partially unsaturated ring containing carbon atoms and optionally containing 1 to 3 heteroatoms selected from O, S or N, wherein the ring is unsubstituted or substituted with 1 to 6 substituents independently selected from halogen, C1-6-alkyl, halo-C1-6-alkyl, C3-6-cycloalkyl, C3-6-heterocycloalkyl, oxo, ═N—OR32, OH, O—C1-6-alkyl and O-halo-C1-6-alkyl,
• wherein alkylene, cycloalkyl, heterocycloalkyl and the 5- or 6-membered monocyclic heteroaryl is optionally substituted by 1 to 4 substituents independently selected from the group consisting of halogen, CN, C1-3-alkyl, halo-C1-3-alkyl, OH, oxo, ═N—OR32, O—C1-3-alkyl and O-halo-C1-3-alkyl;
• and
• wherein aryl and heteroaryl are optionally substituted by 1 to 4 substituents independently selected from the group consisting of halogen, CN, C1-3-alkyl, halo-C1-3-alkyl, OH, O—C1-3-alkyl and O-halo-C1-3-alkyl;
• or
• R1 is selected from
• a 4-membered heterocycloalkyl group containing one heteroatom selected from the group consisting of N, O and S, or
• C1-10-alkyl substituted with a group selected from halogen, CN, OR11, SOyR11, SO3H, NR11SO2R11, SO2NR11R12, CO2R11, CONR11R12, NR11—CO—R11, NR11—CO—NR11R12, NR11—SO2—NR11R12, NR11R12 and a 4-membered heterocycloalkyl group containing one heteroatom selected from the group consisting of N, O and S, or
• C0-1-alkylene-C3-10-cycloalkyl substituted with a group selected from halogen, CN, SOyR11, NR11SO2R11, SO2NR11R12, CO2R11, CONR11R12, NR11—CO—R11, NR11—CO—NR11R12, NR11—SO2—NR11R12 and NR11R12, or
• C2-10-alkylene-C3-10-cycloalkyl, C2-10-alkylene-O—C3-10-cycloalkyl, C2-10-alkylene-C5-10-heterocycloalkyl, C2-10-alkylene-O—C6-10-heterocycloalkyl and SO2—C1-10-alkyl,
• wherein alkyl, alkylene, cycloalkyl and heterocycloalkyl are optionally substituted with 1 to 7 substituents independently selected from the group consisting of OH, oxo, CN, O—C1-6-alkyl, O-halo-C1-6-alkyl, C1-6-alkyl, halo-C1-6-alkyl, halogen, CO2R11, CONR11R12, COR11, SO2R11, SO2NR11R12, NR11COR11, NR11SO2R11, C3-6-cycloalkyl, O—C3-6-cycloalkyl, C3-6-heterocycloalkyl, O—C3-6-heterocycloalkyl, O—C2-6-alkylene-OR11 and NR11R12;
• and
• R3 is pyridinone, a 6- to 10-membered mono- or bicyclic aryl, a 5- to 10-membered mono- or bicyclic heteroaryl containing 1 to 4 heteroatoms independently selected from the group consisting of N, O and S or a 6- to 12-membered partially saturated spiroheterocycle containing 1 to 4 heteroatoms independently selected from the group consisting of N, O and S,
• wherein pyridinone, aryl and heteroaryl and spiroheterocycle is optionally substituted with 1 to 4 groups independently selected from halogen, C1-6-alkyl, halo-C1-6-alkyl, OH, O—C1-6-alkyl, O-halo-C1-6-alkyl, oxo, ═N—OR32, N(R32), C0-6-alkylene-C3-10-cycloalkyl, C0-6-alkylene-C3-10-heterocycloalkyl, C0-6-alkylene-(5- or 6-membered monocyclic heteroaryl), C1-6-alkylene-O—R31, C0-6-alkylene-CN, O—C3-10-cycloalkyl, O—C1-6-alkylene-O—R32, O—C3-10-heterocycloalkyl, C0-6-alkylene-COOR31, C0-6-alkylene-C(O)R31, C0-6-alkylene-C(O)N(R31)2, C0-6-alkylene-N(R31)C(O)R31, C0-6-alkylene-SO—R31, C0-6-alkylene-SO2—R31, C0-6-alkylene-SO2—N(R31)2 and C0-6-alkylene-N(R31)SO2—R31, and two adjacent substituents completing a 3- to 8-membered saturated or partially unsaturated ring containing carbon atoms and optionally containing 1 to 3 heteroatoms selected from O, S or N, wherein the ring is unsubstituted or substituted with 1 to 6 substituents independently selected from halogen, C1-6-alkyl, halo-C1-6-alkyl, C3-6-cycloalkyl, C3-6-heterocycloalkyl, oxo, ═N—OR32, OH, O—C1-6-alkyl and O-halo-C1-6-alkyl,
• wherein alkylene, cycloalkyl, heterocycloalkyl and the 5- or 6-membered monocyclic heteroaryl is optionally substituted by 1 to 4 substituents independently selected from the group consisting of halogen, CN, C1-3-alkyl, halo-C1-3-alkyl, OH, oxo, ═N—OR32, O—C1-3-alkyl and O-halo-C1-3-alkyl;
• and
• R2 is selected from the group consisting of H, C1-6-alkyl, halo-C1-6-alkyl and hydroxy-C1-6-alkyl,
• or R1 and R2 when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring containing carbon atoms and optionally containing 1 or 2 heteroatoms selected from O, S or N, wherein the ring is unsubstituted or substituted with 1 to 4 substitutents independently selected from halogen, oxo, CN, OR11, SOyR11, SO3H, NR11SO2R11, SO2NR11R12, C0-6-alkylene-CO2R11, CONR11R12, COR11, NR11—CO—R11, NR11—CO—NR11R12, NR11—SO2—NR11R12, NR11R12, C1-6-alkyl, halo-C1-6-alkyl, hydroxy-C1-6-alkyl, C3-6-cycloalkyl, O—C3-6-cycloalkyl, C3-6-heterocycloalkyl and O—C3-6-heterocycloalkyl,
• wherein cycloalkyl and heterocycloalkyl are unsubstituted or substituted with 1 to 4 substitutents independently selected from halogen, C1-3-alkyl, halo-C1-3-alkyl and oxo;
• R4 is SO2—(CR8R8)yR7, SO2—NR12R7, (CR8R8)x—R10 or C3-6-cycloalkyl, which is spirocyclic fused with C3-10-cycloalkyl;
• R5 is selected from H, C1-6-alkyl, halo-C1-6-alkyl, CHO, CON(R52)2 or halogen, wherein alkyl is unsubstituted or substituted with 1 to 3 substituents independently selected from the group consisting of O—C1-6-alkyl, O-halo-C1-6-alkyl and OH;
• R6 is selected from H, C1-6-alkyl, halo-C1-6-alkyl or halogen;
• R7 is selected from C3-10-cycloalkyl and C3-10-heterocycloalkyl,
• wherein cycloalkyl and heterocycloalkyl are unsubstituted or substituted with 1 to 3 substituents independently selected from the group consisting of halogen, OH, oxo, O—C1-6-alkyl, O-halo-C1-6-alkyl, C1-6-alkyl, halo-C1-6-alkyl, cycloalkyl and heterocycloalkyl;
• R8 is independently selected from H, F, C1-3-alkyl, halo-C1-3-alkyl or OH;
• R10 is C3-10-cycloalkyl, wherein cycloalkyl is unsubstituted or substituted with 1 to 6 substituents independently selected from halogen, OH, oxo, O—C1-6-alkyl, O-halo-C1-6-alkyl, C1-6-alkyl, halo-C1-6-alkyl, cycloalkyl, heterocycloalkyl, and optionally two adjacent substituents together complete a 6-membered aryl ring wherein the ring is unsubstituted or substituted with 1 to 3 substituents independently selected from halogen, C1-2-alkyl, halo-C1-2-alkyl;
• R11 is independently selected from H, C1-6-alkyl, C0-6-alkylene-C3-6-cycloalkyl, C0-6-alkylene-C3-6-heterocycloalkyl, wherein alkyl, alkylene, cyclolalkyl and heterocycloalkyl are unsubstituted or substituted with 1 to 6 substituents independently selected from halogen, OH, oxo, C1-3-alkyl, halo-C1-3-alkyl, O—C1-3-alkyl, O-halo-C1-3-alkyl and SO2—C1-3-alkyl;
• R12 is independently selected from H, C1-6-alkyl and halo-C1-6-alkyl;
• R31 is independently selected from H, C1-6-alkyl, halo-C1-6-alkyl, C0-6-alkylene-C3-6-cycloalkyl, C0-6-alkylene-C3-6-heterocycloalkyl, 5- or 6-membered heteroaryl and 6-membered aryl, wherein alkyl, alkylene, cyclolalkyl, heterocycloalkyl, aryl and heteroaryl are unsubstituted or substituted with 1 to 6 substituents independently selected from halogen, CN, OH, oxo, C1-3-alkyl, halo-C1-3-alkyl, O—C1-3-alkyl, O-halo-C1-3-alkyl and SO2—C1-3-alkyl;
• and optionally wherein two R31 when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring containing carbon atoms and optionally containing 1 or 2 heteroatoms selected from O, S or N, wherein the ring is unsubstituted or substituted with 1 to 4 substitutents independently selected from fluoro, OH, oxo, C1-4-alkyl and halo-C1-4-alkyl;
• R32 is independently selected from H, C1-6-alkyl and halo-C1-6-alkyl;
• R52 is independently selected from H, C1-3-alkyl and halo-C1-3-alkyl;
• x is independently selected from 1 and 2;
• y is independently selected from 0, 1 and 2;
• with the proviso that R3 is not an unsubstituted or substituted ring selected from