Back to results
US 12,686,657 B2Granted
Anti-inflammatory carboxamide derivatives
AssigneeBiomedcode Hellas SA
InventorsGeorge Kollias, Niki Karagianni, Maria C. Denis, Alexios N. Matralis, Dimitra Papadopoulou, Eleni Karkoulia
Life of this patent
Estimating the term…
Abstract
A compound of formula (I) or a pharmaceutically acceptable salt, hydrate, or isomer thereof. Pharmaceutical compositions comprising the compounds of formula (I) as well as their use in therapy, particularly in the treatment of inflammatory conditions. Advantageously, the compounds show a broad and robust anti-inflammatory effect, and are therapeutically safe.
Claims14
A compound of formula (I):
- or a pharmaceutically acceptable salt, hydrate, or isomer thereof,
- wherein:
- R1 represents halogen;
- —OR4;
- (C1-C10)alkyl;
- or (C1-C10)alkyl substituted with one or more substituents, the same or different, selected from OH, halogen, (C1-C6)alkyl, —O—(C1-C6)alkyl, nitro, cyano, and halogen;
- or, alternatively,
- R1 together with X2 forms an aromatic, saturated or partially saturated known ring, the ring having 5 or 6 members selected from the group consisting of:
- —C(Rx)2—, —CRx—, —N—, —NRx—, S, and O;
- represents a single bond or a double bond;
- R2 represents —OH;
- halogen;
- (C1-C10)alkyl;
- (C1-C10)alkyl substituted with one or more substituents, the same or different, selected from OH, halogen, (C1-C6)alkyl, —O—(C1-C6)alkyl, nitro, cyano, and halogen;
- —S(O)2R4;
- an aromatic known ring system comprising 5 or 6 members selected from —CRa—, and —N—;
- R3 represents —NR5R6, being R5 and R6 the same or different and being selected from —H, (C1-C10)alkyl, (C3-C10)cycloalkyl, and an aromatic known ring system comprising 5 or 6 members selected from —CRb—, and —N—;
- or, alternatively,
- R2 together with R3 form an aromatic, saturated or partially saturated known ring, the ring having 5 or 6 members selected from —C(Ry)2—, —CRy—, —N—, —NRy, —S—, and —O—;
- A is a known ring system having from 1 to 3 rings and comprising from 4 to 14 members, each one of the members being selected from, —C(Rz)2—, —CRz—, —N—, —NR′z—, —S—, —Se—, —SO2, —SeO2, and —O—;
- the rings being saturated, partially unsaturated, or aromatic;
- and being fused or isolated;
- or, alternatively,
- A represents —NRc-A′, wherein
- Rc represents —H or (C1-C10)alkyl, and
- A′ is a known ring system having from 1 to 3 rings and comprising from 4 to 14 members, each one of the members being selected from, —C(Rz)2—, —CRz—, —N—, —NRz—, —S—, —Se—, —SO2, —SeO2, and —O—;
- the rings being saturated, partially unsaturated, or aromatic;
- and being fused or isolated;
- n represents a enter value comprised from 1 to 7;
- X1 and X2 are the same or different and represent C or N atom;
- R4 represents —H;
- (C1-C10) alkyl;
- or (C1-C10) alkyl substituted with one or more substituents, the same or different, selected from OH, halogen, (C1-C6)alkyl, —O—(C1-C5)alkyl, nitro, cyano, and halogen;
- the term “(C3-C10)cycloalkyl” refers to a saturated carbocyclic ring containing from 3 to 10 carbon atoms;
- each one of Ra is independently selected from the group consisting of —H, —OH, halogen, (C1-C6)alkyl, and (C1-C6)alkyl substituted with one or more substituents, the same or different, selected from:
- OH, halogen, (C1-C6)alkyl, —O—(C1-C6)alkyl, nitro, cyano, and halogen;
- each one of Rb is independently selected from the group consisting of —H, —OH, halogen, (C1-C6)alkyl, and (C1-C6)alkyl substituted with one or more substituents, the same or different, selected from:
- OH, halogen, (C1-C6)alkyl, —O—(C1-C6)alkyl, nitro, cyano, and halogen;
- Rt represents (C1-C10) alkyl;
- each one of the Rx is independently selected from the group consisting of —H, —OH, (C1-C6)alkyl, (C1-C6)haloalkyl, —O—(C1-C6)alkyl, nitro, —NR7—, —NR8R9, and halogen;
- each one of the Ry is independently selected from the group consisting of —H, —OH, (C1-C6)alkyl, (C1-C5)haloalkyl, —O—(C1-C6)alkyl, nitro, —NR10—, —NR11R12, and halogen;
- each one of the Rz is independently selected from the group consisting of —H, —OH, (C1-C6)alkyl, (C1-C6)haloalkyl, —O—(C1-C6)alkyl, —O—(C1-C6)haloalkyl, nitro, —NR13—, —NR12R15, and halogen;
- R′z is selected from the group consisting of (C1-C6)alkyl and (C1-C6)haloalkyl;
- and
- each one of R7 to R15 is independently selected from the group consisting of H, (C1-C6)alkyl, (C1-C6)haloalkyl, and —O—(C1-C6)alkyl.
42 more elements
Dependencies are inferred from the claim text.