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US 12,741,957 B2Granted
N-heteroarylalkyl-2-(heterocyclyl and heterocyclylmethyl) acetamide derivatives as SSTR4 agonists
AssigneeTakeda Pharmaceutical Company Limited
InventorsZacharia Cheruvallath, Jason Green, Ben Johnson, Benjamin Jones, Kristin Schleicher, Huikai Sun, Mingnam Tang
Life of this patent
Estimating the term…
Abstract
Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein L, n, R1, R2, R6, R7, R8, R9, R10, X3, X4 and X5 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating diseases, disorders, and conditions associated with SSTR4.
Claims17
A compound of Formula 1,
- or a pharmaceutically acceptable salt thereof in which:
- (a) X3 is selected from NR3N and O, X4 is a single bond, and X5 is selected from N and CR5;
- and
- R1 and R2, together with the carbon atoms to which they are attached, form a fused ring which is benzene, wherein each non-fusion carbon atom of the fused ring is unsubstituted or is substituted with an optional substituent independently selected from:
- (i) halo, hydroxy, and cyano;
- and
- (ii) C1-4 alkyl, C3-6 cycloalkyl, and C1-4 alkoxy, each optionally substituted with up to 3 substituents independently selected from halo;
- or
- (b) X3 is CR3C, X4 is selected from N and CR4, and X5 is selected from N and CR5;
- and
- R1 and R2 are each independently selected from:
- (i) hydrogen, halo, hydroxy, and cyano;
- and
- (ii) C1-4 alkyl, C3-6 cycloalkyl, and C1-4 alkoxy, each optionally substituted with up to 3 substituents independently selected from halo;
- or
- R1 and R2, together with the carbon atoms to which they are attached, form a fused ring selected from furan, pyrazole, and benzene, wherein one of the nitrogen atoms of the pyrazole ring is substituted with hydrogen, C1-4 alkyl or C3-6 cycloalkyl, and each non-fusion carbon atom of the fused ring is unsubstituted or is substituted with an optional substituent independently selected from:
- (i) halo, hydroxy, and cyano;
- and
- (ii) C1-4 alkyl, C3-6 cycloalkyl, and C1-4 alkoxy, each optionally substituted with up to 3 substituents independently selected from halo;
- L is O and n is 1;
- or
- L is a single bond and n is 0 or 1;
- R3N is selected from hydrogen, C1-4 alkyl and C3-6 cycloalkyl;
- R3C and R4 are each independently selected from:
- (i) hydrogen, halo, hydroxy, and cyano;
- and
- (ii) C1-4 alkyl, C3-6 cycloalkyl, and C1-4 alkoxy, each optionally substituted with up to 3 substituents independently selected from halo;
- R5 is selected from:
- (i) hydrogen, halo, hydroxy, and cyano;
- and
- (ii) C1-4 alkyl and C1-4 alkoxy, each optionally substituted with up to 3 substituents independently selected from halo;
- and
- R6 is hydrogen;
- or
- R5 and R6 together form an ethane-1,2-diyl bridging the carbon atoms to which they are attached;
- R7 and R8 are each independently selected from hydrogen and C1-4 alkyl which is optionally substituted with up to 3 substituents independently selected from halo, wherein at least one of R7 and R8 is not hydrogen, or R7 and R8, together with the carbon atom to which they are attached, form a C3-6 cycloalkylidene;
- R9 is selected from hydrogen and C1-4 alkyl which is optionally substituted with up to 3 substituents independently selected from halo;
- and
- R10 is azetidin-1-ylmethyl.
36 more elements
Dependencies are inferred from the claim text.