Tricyclic prodrugs

A compound according to formula (Ia),

• wherein
• R1 is halo;
• R1′ is selected from the group consisting of H, C1-5 alkyl, C1-5 fluoroalkyl, halo, C3-8 non-aromatic carbocycle, C0-5 alkyleneOC0-5 alkyl, C0-3 alkyleneOC1-5 fluoroalkyl, C0-3 alkyleneOC(O)C1-5 alkyl, OC2-3 alkyleneN(C0-5 alkyl)2 in which the C0-5 alkyl may be the same or different, C0-3 alkyleneNHC0-5 alkyl, C0-3 alkyleneN(C1-5 alkyl)2 in which the C1-5 alkyl may be the same or different, C0-3 alkyleneN(C0-5 alkyl)C(O)C1-5 alkyl, C0-3 alkyleneNHaryl, wherein the aryl is unsubstituted or substituted with a one or several substituents independently selected from the group consisting of C1-5 alkyl, C1-5 fluoroalkyl, halo, C0-5 alkyleneOC0-5 alkyl, nitro, cyano and N(C0-5 alkyl)2 in which the C0-5 alkyl may be the same or different, C0-3 alkyleneNHheteroaryl, wherein said heteroaryl is a 5- or 6-membered heteroaryl, said heteroaryl being unsubstituted or substituted with a one or several independently selected C1-5 alkyl groups, C0-3 alkyleneC(O)NHC0-5 alkyl, C0-3 alkyleneC(O)N(C1-5 alkyl)2 in which the C1-5 alkyl may be the same or different, C0-3 alkyleneC(O)N(C4-5 alkylene), C0-3 alkyleneC(O)OC0-5 alkyl, a 3- to 8-membered non-aromatic heterocycle, C0-3 alkylene aryl, wherein the aryl is unsubstituted or substituted with a one or several substituents independently selected from the group consisting of C1-5 alkyl, C1-5 fluoroalkyl, halo, C0-5 alkyleneOC0-5 alkyl, nitro, cyano and N(C0-5 alkyl)2 in which the C0-5 alkyl may be the same or different, C0-3 alkylene heteroaryl, wherein said heteroaryl is a 5- or 6-membered heteroaryl, said heteroaryl being unsubstituted or substituted with a one or several independently selected C1-5 alkyl groups, halo, C0-1 alkylene cyano, SC0-5 alkyl, C0-3 alkyleneSO2C0-5 alkyl, nitro, C(O)C0-C5 alkyl, C(O)C1-C5 fluoroalkyl, N(C0-C3 alkyl)SO2C1-C5 alkyl, and N(C0-C5 alkyl)SO2C1-5 fluoroalkyl;
• R2 and R2′ are independently selected from the group consisting of H, C1-5 alkyl, C1-5 fluoroalkyl, halo, C3-8 non-aromatic carbocycle, C0-5 alkyleneOC0-5 alkyl, C0-3 alkyleneOC1-5 fluoroalkyl, C0-3 alkyleneOC(O)C1-5 alkyl, OC2-3 alkyleneN(C0-5 alkyl)2 in which the C0-5 alkyl may be the same or different, C0-3 alkyleneNHC0-5 alkyl, C0-3 alkyleneN(C1-5 alkyl)2 in which the C1-5 alkyl may be the same or different, C0-3 alkyleneN(C0-5 alkyl)C(O)C1-5 alkyl, C0-3 alkyleneNHaryl, wherein the aryl is unsubstituted or substituted with a one or several substituents independently selected from the group consisting of C1-5 alkyl, C1-5 fluoroalkyl, halo, C0-5 alkyleneOC0-5 alkyl, nitro, cyano and N(C0-5 alkyl)2 in which the C0-5 alkyl may be the same or different, C0-3 alkyleneNHheteroaryl, wherein said heteroaryl is a 5- or 6-membered heteroaryl, said heteroaryl being unsubstituted or substituted with a one or several independently selected C1-5 alkyl groups, C0-3 alkyleneC(O)NHC0-5 alkyl, C0-3 alkyleneC(O)N(C1-5 alkyl)2 in which the C1-5 alkyl may be the same or different, C0-3 alkyleneC(O)N(C4-5 alkylene), C0-3 alkyleneC(O)OC0-5 alkyl, a 3- to 8-membered non-aromatic heterocycle, C0-3 alkylene aryl, wherein the aryl is unsubstituted or substituted with a one or several substituents independently selected from the group consisting of C1-5 alkyl, C1-5 fluoroalkyl, halo, C0-5 alkyleneOC0-5 alkyl, nitro, cyano and N(C0-5 alkyl)2 in which the C0-5 alkyl may be the same or different, C0-3 alkylene heteroaryl, wherein said heteroaryl is a 5- or 6-membered heteroaryl, said heteroaryl being unsubstituted or substituted with a one or several independently selected C1-5 alkyl groups, halo, C0-1 alkylene cyano, SC0-5 alkyl, C0-3 alkyleneSO2C0-5 alkyl, nitro, C(O)C0-C5 alkyl, C(O)C1-C5 fluoroalkyl, N(C0-C3 alkyl)SO2C1-C5 alkyl, and N(C0-C5 alkyl)SO2C1-5 fluoroalkyl;
• R3 and R3′ are independently selected from the group consisting of H, C1-5 alkyl, C1-5 fluoroalkyl, halo, C3-8 non-aromatic carbocycle, C0-5 alkyleneOC0-5 alkyl, C0-3 alkyleneOC1-5 fluoroalkyl, C0-3 alkyleneOC(O)C1-5 alkyl, OC2-3 alkyleneN(C0-5 alkyl)2 in which the C0-5 alkyl may be the same or different, C0-3 alkyleneNHC0-5 alkyl, C0-3 alkyleneN(C1-5 alkyl)2 in which the C1-5 alkyl may be the same or different, C0-3 alkyleneN(C0-5 alkyl)C(O)C1-5 alkyl, C0-3 alkyleneNHaryl, wherein the aryl is unsubstituted or substituted with a one or several substituents independently selected from the group consisting of C1-5 alkyl, C1-5 fluoroalkyl, halo, C0-5 alkyleneOC0-5 alkyl, nitro, cyano and N(C0-5 alkyl)2 in which the C0-5 alkyl may be the same or different, C0-3 alkyleneNHheteroaryl, wherein said heteroaryl is a 5- or 6-membered heteroaryl, said heteroaryl being unsubstituted or substituted with a one or several independently selected C1-5 alkyl groups, C0-3 alkyleneC(O)NHC0-5 alkyl, C0-3 alkyleneC(O)N(C1-5 alkyl)2 in which the C1-5 alkyl may be the same or different, C0-3 alkyleneC(O)N(C4-5 alkylene), C0-3 alkyleneC(O)OC0-5 alkyl, a 3- to 8-membered non-aromatic heterocycle, C0-3 alkylene aryl, wherein the aryl is unsubstituted or substituted with a one or several substituents independently selected from the group consisting of C1-5 alkyl, C1-5 fluoroalkyl, halo, C0-5 alkyleneOC0-5 alkyl, nitro, cyano and N(C0-5 alkyl)2 in which the C0-5 alkyl may be the same or different, C0-3 alkylene heteroaryl, wherein said heteroaryl is a 5- or 6-membered heteroaryl, said heteroaryl being unsubstituted or substituted with a one or several independently selected C1-5 alkyl groups, halo, C0-1 alkylene cyano, SC0-5 alkyl, C0-3 alkyleneSO2C0-5 alkyl, nitro, C(O)C0-C5 alkyl, C(O)C1-C5 fluoroalkyl, N(C0-C3 alkyl)SO2C1-C5 alkyl, and N(C0-C5 alkyl)SO2C1-5 fluoroalkyl;
• and
• R4 and R4′ are independently selected from the group consisting of H, C1-5 alkyl, C1-5 fluoroalkyl, halo, C3-8 non-aromatic carbocycle, C0-5 alkyleneOC0-5 alkyl, C0-3 alkyleneOC1-5 fluoroalkyl, C0-3 alkyleneOC(O)C1-5 alkyl, OC2-3 alkyleneN(C0-5 alkyl)2 in which the C0-5 alkyl may be the same or different, C0-3 alkyleneNHC0-5 alkyl, C0-3 alkyleneN(C1-5 alkyl)2 in which the C1-5 alkyl may be the same or different, C0-3 alkyleneN(C0-5 alkyl)C(O)C1-5 alkyl, C0-3 alkyleneNHaryl, wherein the aryl is unsubstituted or substituted with a one or several substituents independently selected from the group consisting of C1-5 alkyl, C1-5 fluoroalkyl, halo, C0-5 alkyleneOC0-5 alkyl, nitro, cyano and N(C0-5 alkyl)2 in which the C0-5 alkyl may be the same or different, C0-3 alkyleneNHheteroaryl, wherein said heteroaryl is a 5- or 6-membered heteroaryl, said heteroaryl being unsubstituted or substituted with a one or several independently selected C1-5 alkyl groups, C0-3 alkyleneC(O)NHC0-5 alkyl, C0-3 alkyleneC(O)N(C1-5 alkyl)2 in which the C1-5 alkyl may be the same or different, C0-3 alkyleneC(O)N(C4-5 alkylene), C0-3 alkyleneC(O)OC0-5 alkyl, a 3- to 8-membered non-aromatic heterocycle, C0-3 alkylene aryl, wherein the aryl is unsubstituted or substituted with a one or several substituents independently selected from the group consisting of C1-5 alkyl, C1-5 fluoroalkyl, halo, C0-5 alkyleneOC0-5 alkyl, nitro, cyano and N(C0-5 alkyl)2 in which the C0-5 alkyl may be the same or different, C0-3 alkylene heteroaryl, wherein said heteroaryl is a 5- or 6-membered heteroaryl, said heteroaryl being unsubstituted or substituted with a one or several independently selected C1-5 alkyl groups, halo, C0-1 alkylene cyano, SC0-5 alkyl, C0-3 alkyleneSO2C0-5 alkyl, nitro, C(O)C0-C5 alkyl, C(O)C1-C5 fluoroalkyl, N(C0-C3 alkyl)SO2C1-C5 alkyl, and N(C0-C5 alkyl)SO2C1-5 fluoroalkyl;
• as a free base, an acid in its non-charged protonated form, a pharmaceutically acceptable addition salt, solvate, solvate of a salt thereof, a pure diastereomer, a pure enantiomer, a diastereomeric mixture, a racemic mixture, a scalemic mixture, a corresponding tautomeric form resulting from a hydrogen shift between two hetero-atoms and/or the corresponding tautomeric form resulting from a keto-enol tautomerization.