Pyrimidine-and nitrogen-containing bicyclic compound
AssigneesAsahi Kasei Pharma Corporation, Vernalis (R&D) Ltd
InventorsKoichiro Arai, Kenichiro Takaba, Masakazu Atobe, Misato Takashima, Naomi Aono, Andrew John Potter, Daniel Paul Maddox
Life of this patent
Estimating the term…
Abstract
A compound represented by the general formula (1) or a salt thereof, which has a superior IRAK-4 inhibitory activity, and is useful as active ingredients of medicaments for prophylactic treatment and/or therapeutic treatment of diseases relating to IRAK-4 inhibition.
Claims35
A compound represented by the following general formula (1):
- [in the formula (1),
- Rg is a group represented by the following general formula (1-1):
- or
- the following general formula (1-2):
- (a and b represent direction of bonding),
- R1 is —H, —F, —Cl, methyl, or C1-3 alkoxy, the C1-3 alkoxy may be substituted with the same or different 1 to 3 substituents selected from the group G1;
- the group G1 is a group consisting of —F, hydroxy, cyano, halogeno-C1-6 alkyl, C1-4 alkoxy, phenyl, 5- or 6-membered heteroaryl, and a 3- to 7-membered saturated ring group, the phenyl and 5- or 6-membered heteroaryl included in the group G1 may be substituted with the same or different 1 to 3 substituents selected from the group GM;
- the group GAr is a group consisting of —F, —Cl, hydroxy, cyano, C1-6 alkyl, halogeno-C1-6 alkyl, and —NH2;
- R2 is C1-6 alkyl, halogeno-C1-6 alkyl, or a 3- to 7-membered saturated ring group, R2 may be substituted with the same or different 1 to 3 substituents selected from the group G2;
- the group G2 is a group consisting of —F, hydroxy, halogeno-C1-3 alkyl, and C1-4 alkoxy;
- Cy is a group represented by the following general formula (2-1):
- in the formula (2-1),
- k is an integer of 0 or 1;
- RCy1 and RCy2 are independently —H, —F, hydroxy, cyano, C1-6 alkyl, halogeno-C1-6 alkyl, C1-6 alkoxy, —NR11R12, phenyl, 5- or 6-membered heteroaryl, or a 3- to 7-membered saturated ring group, the phenyl and 5- or 6-membered heteroaryl as RCy1 and RCy2 may be substituted with the same or different 1 to 3 substituents selected from the group GAr, RCy1 and RCy2 may be substituted with the same or different 1 to 3 substituents selected from the group G1;
- R11 and R12 are independently —H, C1-6 alkyl, halogeno-C1-6 alkyl, hydroxy-C1-6 alkyl, C1-6 alkoxy-C1-6 alkyl, a 3- to 7-membered saturated ring group, phenyl, or 5- or 6-membered heteroaryl, and R11 and R12 may be substituted with the same or different 1 to 3 substituents selected from the group G1;
- or
- R11 and R12 combine to form a 4- to 10-membered saturated ring or a 7- to 11-membered spiro ring, the 4- to 10-membered saturated ring and 7- to 11-membered spiro ring may contain the same or different 1 or 2 heteroatoms selected from the group consisting of O and N, or —S(O2)—, in addition to N, the 4- to 10-membered saturated ring and 7- to 11-membered spiro ring may be substituted with the same or different 1 to 3 substituents selected from the group G3;
- the group G3 is a group consisting of —F, hydroxy, C1-6 alkyl, halogeno-C1-6 alkyl, hydroxy-C1-6 alkyl, C1-6 alkoxy, C1-6 alkoxy-C1-6 alkyl, halogeno-C1-6 alkoxy, —C(O)R14, —NR13C(O)R14, —C(O)NR13R14, —C(O)NH2, —NR13S(O2)R14, —S(O2)NR13R14, —S(O2)NH2, —S(O2)R14, phenyl, 5- or 6-membered heteroaryl, and a 3- to 7-membered saturated ring group, the phenyl and 5- or 6-membered heteroaryl included in the group G3 may be substituted with the same or different 1 to 3 substituents selected from the group GA;
- R13 is —H, C1-6 alkyl, halogeno-C1-6 alkyl, C1-6 alkoxy-C1-6 alkyl, halogeno-C1-6 alkoxy-C1-6 alkyl, phenyl, 5- or 6-membered heteroaryl, or a 3- to 7-membered saturated ring group, the phenyl and 5- or 6-membered heteroaryl as R13 may be substituted with the same or different 1 to 3 substituents selected from the group GAr;
- R14 is C1-6 alkyl, halogeno-C1-6 alkyl, C1-6 alkoxy-C1-6 alkyl, halogeno-C1-6 alkoxy-C1-6 alkyl, phenyl, 5- or 6-membered heteroaryl, or a 3- to 7-membered saturated ring group, and the phenyl and 5- or 6-membered heteroaryl as R14 may be substituted with the same or different 1 to 3 substituents selected from the group GAr;
- or
- R13 and R14 combine to form a 4- to 7-membered saturated ring or a 7- to 11-membered spiro ring, and the 4- to 7-membered saturated ring and 7- to 11-membered spiro ring may contain the same or different 1 or 2 heteroatoms selected from the group consisting of O and N, or —S(O2)—, in addition to N;
- or
- RCy1 and RCy2 combine to form a 4- to 7-membered saturated ring, the 4- to 7-membered saturated ring may contain the same or different 1 or 2 heteroatoms selected from the group consisting of O and N, or —S(O2)—, and the 4- to 7-membered saturated ring may be substituted with the same or different 1 to 3 substituents selected from the group G1], or
- a salt thereof.
A compound represented by the following formula:
- or a salt thereof.
A compound represented by the following formula:
- or a salt thereof.
A compound represented by the following formula:
- or a salt thereof.
A compound represented by the following formula:
- or a salt thereof.
A compound represented by the following formula:
- or a salt thereof.
A compound represented by the following formula:
- or a salt thereof.
A compound represented by the following formula:
- or a salt thereof.
A compound represented by the following formula:
- or a salt thereof.
A compound represented by the following formula:
- or a salt thereof.
A compound represented by the following formula:
- or a salt thereof.
A compound represented by the following formula:
- or a salt thereof.
A compound represented by the following formula:
- or a salt thereof.
A compound represented by the following formula:
- or a salt thereof.
A compound represented by the following formula:
- or a salt thereof.
Dependencies are inferred from the claim text.