IP Library Granted Patent US 12662473
Granted Patent B2
US 12662473 · App. 17/455,807 · Granted Jun 23, 2026

Inhibitors for programmed cell necrosis and preparation method therefor and use thereof

Inventors: Li Tan (Shanghai, CN); Ying Qin (Shanghai, CN)
Assignee: SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES
C07D413/04C07D207/06C07D207/08C07D207/09C07D231/04C07D231/06C07D401/04C07D401/12C07D403/04C07D403/06C07D403/12C07D417/04C07D417/12C07B2200/05
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Quick Facts
Patent No.
US 12662473
App. No.
17/455,807
Granted
Jun 23, 2026
Kind
B2
Abstract

Provided in the present invention are inhibitors for programmed cell necrosis, a preparation method therefor and a use thereof. Specifically, provided in the present invention are a compound represented by formula I and a composition comprising same. The described compound may be used to prepare a pharmaceutical composition for the prevention and/or treatment of diseases involving cell death and/or inflammation.

Claims (165)

1 . A compound represented by the following Formula (I-c), or pharmaceutically acceptable salts thereof,

wherein:

dashed line is a chemical bond or none;

X is selected from the group consisting of CR 2 , NR, O, S, CR, and N;

R is selected from the group consisting of H, D, and C1-C4 alkyl;

R 1 and R 2 are each independently selected from the group consisting of H and C1-C4 alkyl; or R 1 and R 2 together form a structure of substituted or unsubstituted —(CH 2 ) n —; wherein, n is 1, 2, 3, or 4;

ring A is selected from the group consisting of substituted or unsubstituted C6-C10 aryl, and substituted or unsubstituted 5-12 membered heteroaryl;

ring B is selected from the group consisting of substituted or unsubstituted C6-C10 aryl, and substituted or unsubstituted 5-12 membered heteroaryl,

wherein the substituted means that at least one hydrogen atom in a group is substituted by one or more substituents selected from the group consisting of halogen, deuterium, C1-C6 alkoxy, halogenated C1-C6 alkoxy, methyl sulfonyl, —S(═O) 2 NH 2 , oxo(═O), —CN, hydroxyl, —NH 2 , carboxyl, C2-C6 amido (—C(—O)—N(Rc) 2 or—NH—C(—O)(Rc), wherein Rc is H or C1-C5 alkyl), C1-C6 alkyl-(C2-C6 amido), and substituted or unsubstituted groups selected from the group consisting of C1-C6 alkyl, C3-C8 cycloalkyl, C1-C6 amino, C6-C10 aryl, 5-10 membered heteroaryl having 1-3 heteroatoms selected from N, S and O, 5-12 membered heterocyclyl having 1-3 heteroatoms selected from N, S and O, —(CH 2 )—C6-C10 aryl, and —(CH 2 )-(5-10 membered heteroaryl having 1-3 heteroatoms selected from N, S and O), and the substituents are selected from the group consisting of halogen, C1-C6 alkyl, C1-C6 alkoxy, oxo, —CN, —NH 2 , —OH, C6-C10 aryl, C1-C6 amino, C2-C6 amido, and 5-10 membered heteroaryl having 1-3 heteroatoms selected from N, S and O.

2 . The compound according to claim 1 , wherein the compound of Formula (I-c) has a structure selected from the group consisting of I-a and I-b:

3 . The compound according to claim 1 , wherein the ring A is selected from the group consisting of substituted or unsubstituted phenyl and substituted or unsubstituted 5-7 membered heteroaryl; and/or

ring B is selected from the group consisting of substituted or unsubstituted phenyl and substituted or unsubstituted 5-7 membered heteroaryl.

4 . The compound according to claim 1 , wherein the compound is selected from the following table:

Com-

Com-

pound

pound

number

Chemical structure

number

Chemical structure

QY-1- 98

QY-4- 6

QY-2- 25

QY-4- 7

QY-2- 26

QY-4- 8

QY-2- 27

QY-4- 11

QY-2- 34

QY-4- 12

QY-2- 38

QY-4- 14

QY-2- 39

QY-4- 27

QY-2- 52

QY-4- 32

QY-2- 53

QY-4- 35

QY-2- 54

QY-4- 39

QY-2- 55

QY-4- 66

QY-2- 56

QY-4- 67

QY-2- 75

QY-4- 69

QY-2- 76

QY-4- 70

QY-2- 77

QY-4- 75

QY-2- 78

QY-4- 78

QY-2- 79

QY-4- 87

QY-2- 100

QY-4- 88

QY-2- 103

QY-4- 96

QY-2- 104

QY-4- 99

QY-3- 4

QY-5- 1

QY-3- 11

QY-5- 4

QY-3- 17

QY-5- 21

QY-3- 26

QY-5- 22

QY-3- 27

QY-5- 79

QY-3- 28

QY-5- 83

QY-3- 29

QY-5- 85

QY-3- 35

QY-6- 47

QY-3- 36

QY-6- 60

QY-3- 39

QY-6- 61

QY-3- 46

QY-6- 62

QY-3- 51

QY-6- 63

QY-3- 65

QY-6- 83

QY-3- 81

QY-6- 84

QY-3- 86

QY-7- 7

QY-3- 94

QY-7- 50

QY-3- 95

QY-7- 60

QY-3- 96

QY-7- 62

QY-3- 99

XHJ-3- 22

QY4-1

ZSQ-13- 56

QY4-2

ZSQ-13- 57

QY-7- 101

QY-8- 101

QY-9- 8

QY-9- 32

QY-9- 43

QY-10- 1

QY-10- 92

QY-10- 96

QY-10- 104

QY-11- 1

QY-11- 9A

QY-11- 9B

QY-11- 11A

QY-11- 11B

QY-11- 15B

QY-11- 16A

QY-11- 16B

QY-11- 36

QY-11- 44

QY-11- 45

QY-12- 11

QY-12- 14

QY-12- 32

QY-13- 42

QY-13- 68

QY-13- 70

QY-13- 86

QY-14- 8

QY-14- 9

QY-14- 17

QY-14- 24

QY-14- 25

QY-14- 27

QY-14- 29

QY-14- 30

QY-14- 31

QY-14- 33

QY-14- 34

QY-14- 35

QY-14- 40

QY-14- 44

QY-14- 59

QY-14- 60

QY-14- 68

QY-15- 11

QY-15- 12

QY-15- 31

QY-16- 60

QY-16- 61

QY-16- 66

QY-16- 75

QY-16- 76

QY-16- 77

QY-16- 82

and

QY-16- 84

.

5 . A pharmaceutical composition comprising: (a) a therapeutically effective amount of the compound according to claim 1 , or pharmaceutically acceptable salts, hydrates or solvates thereof; and (b) a pharmaceutically acceptable carrier.

6 . The pharmaceutical composition according to claim 5 , wherein diseases or conditions to be treated with the pharmaceutical composition are selected from the group consisting of inflammatory diseases, infectious diseases, ischemic or degenerative-related diseases, and tissue damage.

7 . The pharmaceutical composition according to claim 5 , wherein diseases or conditions to be treated with the pharmaceutical composition are related to programmed cell necrosis and/or the activity or expression levels of human receptor interacting protein 1 kinase (RIPK1).

8 . The pharmaceutical composition according to claim 7 , wherein the diseases or conditions are selected from the group consisting of inflammatory diseases, infectious diseases, ischemic or degenerative related diseases, and tissue damage.

9 . A method for treating diseases or conditions related to programmed cell necrosis and/or the activity or expression levels of human receptor interacting protein 1 kinase (RIPK1), comprising administering the compound of Formula (I-c) according to claim 1 to a subject in need thereof, wherein the diseases or conditions are selected from the group consisting of inflammatory diseases, infectious diseases, ischemic or degenerative related diseases, and tissue damage.