IP Library › Granted Patent US 12662474

Granted Patent B2

US 12662474 · App. 18/275,706 · Granted Jun 23, 2026

Fused ring derivatives containing 1,4-oxazepane

Inventors: Lingyun Wu (Shanghai, CN); Lele Zhao (Shanghai, CN); Deheng Chen (Shanghai, CN); Xiaoxuan Yan (Shanghai, CN); Shuhui Chen (Shanghai, CN)

Assignee: Shanghai Fosun Pharmaceutical Industrial Development Co., Ltd.

C07D413/12 C07D413/14 C07D471/04 C07D495/04

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Quick Facts

Patent No.: US 12662474
App. No.: 18/275,706
Granted: Jun 23, 2026
Kind: B2

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Abstract

The present invention relates to a series of fused ring derivatives containing 1,4-oxazepane and a preparation method therefor, and in particular relates to a compound as shown in formula (II) and a pharmaceutically acceptable salt thereof.

Claims (91)

1 . A compound of formula (II) or a pharmaceutically acceptable salt thereof,

wherein

Z is selected from N and C;

the structural moiety

is selected from

wherein the structure moiety

is selected from

each is independently selected from a single bond and a double bond, wherein when is selected from the double bond, R 2 is absent;

each T is independently selected from N and CR 3 ;

each R 1 is independently selected from H, F, Cl, Br, I, —OH, —NH 2 , —CN, and C 1-3 alkyl, wherein the C 1-3 alkyl is optionally substituted by 1, 2, or 3 R a ;

R 2 is selected from H, F, Cl, Br, I, ═O, —OH, —NH 2 , —CN, C 1-3 alkyl, and 5- to 6-membered heterocycloalkyl, wherein the C 1-3 alkyl and 5- to 6-membered heterocycloalkyl are each independently and optionally substituted by 1, 2, or 3 R b ;

R 3 is selected from H, F, Cl, Br, I, —OH, —NH 2 , —CN, and C 1-3 alkyl, wherein the C 1-3 alkyl is optionally substituted by 1, 2, or 3 R c ;

R 5 is selected from H, F, Cl, Br, I, —OH, —NH 2 , —CN, and C 1-3 alkyl, wherein the C 1-3 alkyl is optionally substituted by 1, 2, or 3 R e ;

R 6 is selected from H, F, Cl, Br, I, —OH, —NH 2 , —CN, and C 1-3 alkyl, wherein the C 1-3 alkyl is optionally substituted by 1, 2, or 3 R f ,

each R a is independently selected from F, Cl, Br, I, —O, —OH, —NH 2 , and —CN;

each R b is independently selected from F, Cl, Br, I, ═O, —OH, —NH 2 , —CN, and C 1-3 alkyl;

each R c is independently selected from F, Cl, Br, I, ═O, —OH, —NH 2 , and —CN;

each R d is independently selected from F, Cl, Br, I, ═O, —OH, —NH 2 , and —CN;

each R e is independently selected from F, Cl, Br, I, ═O, —OH, —NH 2 , and —CN;

each R f is independently selected from F, Cl, Br, I, ═O, —OH, —NH 2 , and —CN;

n is selected from 1, 2, 3, and 4;

the 5- to 6-membered heterocycloalkyl contains 1, 2, 3, or 4 heteroatoms or heteroatom groups independently selected from —O—, —NH—, —S—, and —N—.

2 . The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein the compound has a structure of formula (II′):

the carbon atoms with “*” and “#” are chiral carbon atoms, which exist in an (R) or(S) single enantiomer form or an (R) or(S) single enantiomer-rich form.

3 . The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein R b is selected from F, Cl, Br, and CH 3 ,

or R 1 is selected from H, F, Cl, and —CH 3 .

4 . The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein R 2 is selected from H, —CH 3 ,

wherein the —CH 3 ,

are each independently and optionally substituted by 1, 2, or 3 R b .

5 . The compound or the pharmaceutically acceptable salt thereof according to claim 4 , wherein R 2 is selected from H, —CH 3 ,

6 . The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein R 3 is selected from H, F, CI, and Br.

7 . The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein R 5 is selected from H and —CH 3 .

8 . The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein R 6 is selected from H, F, CI, and Br.

9 . The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein the structural moiety

is selected from

10 . The compound or the pharmaceutically acceptable salt thereof according to claim 9 , wherein the structural moiety

is selected from

11 . The compound or the pharmaceutically acceptable salt thereof according to claim 10 , wherein the structural moiety

is selected from

12 . The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein the compound has a structure of formula (II-1):

13 . The compound or the pharmaceutically acceptable salt thereof according to claim 12 , wherein the compound has a structure of formula (II′-1):

the carbon atoms with “*” and “#” are chiral carbon atoms, which exist in an (R) or(S) single enantiomer form or an (R) or(S) single enantiomer-rich form.

14 . The compound or the pharmaceutically acceptable salt thereof according to claim 12 , wherein the compound is a compound of formula (I):

wherein

the structural moiety

is selected from

each is independently selected from a single bond and a double bond, wherein when is selected from the double bond, R 2 is absent;

each T is independently selected from N and CR 3 ;

R 3 is selected from H, F, Cl, Br, I, —OH, —NH 2 , —CN, and C 1-3 alkyl, wherein the C 1-3 alkyl is optionally substituted by 1, 2, or 3 R c ;

R 5 is selected from H, F, Cl, Br, I, —OH, —NH 2 , —CN, and C 1-3 alkyl, wherein the C 1-3 alkyl is optionally substituted by 1, 2, or 3 R e ;

each R c is independently selected from F, Cl, Br, I, —O, —OH, —NH 2 , and —CN;

each R d is independently selected from F, Cl, Br, I, —O, —OH, —NH 2 , and —CN;

each Re is independently selected from F, Cl, Br, I, —O, —OH, —NH 2 , and —CN.

15 . The compound or the pharmaceutically acceptable salt thereof according to claim 14 , wherein the compound has a structure of formula (I-1) or (1-3):

16 . The compound or the pharmaceutically acceptable salt thereof according to claim 15 , wherein the compound has a structure of formula (I-1A), (I-1B), or (I-3A):

17 . The compound or the pharmaceutically acceptable salt thereof according to claim 16 , wherein the compound has a structure of formula (I′-1A), (I′-1B), or (I′-3A):

wherein the carbon atoms with “*” and “#” are chiral carbon atoms, which exist in an (R) or(S) single enantiomer form or an (R) or(S) single enantiomer-rich form.

18 . A compound of the following formula, or a pharmaceutically acceptable salt thereof, selected from:

19 . The compound or the pharmaceutically acceptable salt thereof according to claim 18 , wherein the compound is:

20 . A method for inhibiting DPP1 in a subject comprising administering the compound of claim 1 , or a pharmaceutically acceptable salt thereof, to the subject in need thereof.

21 . A method for inhibiting DPP1 in a subject comprising administering to the subject in need thereof the compound of claim 18 , or a pharmaceutically acceptable salt thereof.

22 . A compound of formula (II):

or a pharmaceutically acceptable salt thereof, wherein:

the structural moiety

R 1 is selected from H, F, Cl, and —CH 3 ;

R 2 is selected from H, —CH 3 ,

R 3 is selected from H, F, Cl, and Br;

R 6 is selected from H, F, Cl, and Br; and

n is 1.

23 . The compound of claim 22 , or a pharmaceutically acceptable salt thereof, wherein:

R 1 is selected from H and F;

R 2 is selected from H and —CH 3 ;

R 3 is H; and

R 6 is H.

24 . The compound of claim 22 , wherein the compound is selected from: