US 12,577,201 B2Granted

Glutamine analogs

AssigneeJacobio Pharmaceuticals Co., Ltd.

InventorsRunze Li, Cunbo Ma, Zhenchang Lian, Jing Xiong, Yanping Wang, Wei Long

Life of this patent

Estimating the term…

Abstract

The invention relates to novel glutamine analogs, a composition containing the glutamine analogs and the use thereof.

Claims4

Dependent claims

A compound or a pharmaceutically acceptable salt thereof, a stereoisomer thereof, a tautomer thereof, and an isotopic substitution thereof, wherein the compound is selected from:

1
isopropyl (S)-6-diazo-2-((S)-2-methoxypropanamido)-5-oxohexanoate
2
methyl (S)-6-diazo-2-((S)-2-methoxypropanamido)-5-oxohexanoate
3
(S)-6-diazo-2-((S)-2-methoxypropanamido)-5-oxohexanoic acid
4
ethyl (S)-6-diazo-2-((S)-2-methoxypropanamido)-5-oxohexanoate
5
isopropyl (S)-6-diazo-2-(2-methoxyacetamido)-5-oxohexanoate
6
isopropyl (S)-6-diazo-2-(2-ethoxyacetamido)-5-oxohexanoate
7
isopropyl (S)-6-diazo-2-((S)-2-hydroxypropanamido)-5-oxohexanoate
8
isopropyl (S)-6-diazo-2-((S)-2-hydroxy-4-methylpentanamido)-5-
oxohexanoate
9
isopropyl (S)-6-diazo-2-((S)-2-ethoxypropanamido)-5-oxohexanoate
10
isopropyl (S)-6-diazo-2-((S)-2-isopropoxypropanamido)-5-
oxohexanoate
11
isopropyl (S)-6-diazo-2-(2-hydroxyacetamido)-5-oxohexanoate
12
isopropyl (S)-6-diazo-2-((S)-2-hydroxybutanamido)-5-oxohexanoate
13
isopropyl (S)-6-diazo-2-((S)-2-methoxybutanamido)-5-oxohexanoate
14
isopropyl (S)-6-diazo-2-((S)-2-ethoxybutanamido)-5-oxohexanoate
15
isopropyl (S)-6-diazo-2-((S)-2-isopropoxybutanamido)-5-oxohexanoate
16
isopropyl (S)-6-diazo-2-((S)-2-hydroxy-3-methylbutanamido)-5-
oxohexanoate
17
isopropyl (S)-6-diazo-2-((S)-2-methoxy-3-methylbutanamido)-5-
oxohexanoate
18
isopropyl (S)-6-diazo-2-((S)-2-ethoxy-3-methylbutanamido)-5-
oxohexanoate
19
isopropyl (S)-6-diazo-2-((S)-2-isopropoxy-3-methylbutanamido)-5-
oxohexanoate
20
isopropyl (S)-6-diazo-2-((2S,3R)-2-hydroxy-3-methylpentanamido)-5-
oxohexanoate
21
isopropyl (S)-6-diazo-2-((2S,3R)-2-methoxy-3-methylpentanamido)-5-
oxohexanoate
22
isopropyl (S)-6-diazo-2-((2S,3R)-2-ethoxy-3-methylpentanamido)-5-
oxohexanoate
23
isopropyl (S)-6-diazo-2-((2S,3R)-2-isopropoxy-3-methylpentanamido)-
5-oxohexanoate
24
isopropyl (S)-6-diazo-2-((S)-2-hydroxypentanamido)-5-oxohexanoate
25
isopropyl (S)-6-diazo-2-((S)-2-methoxypentanamido)-5-oxohexanoate
26
isopropyl (S)-6-diazo-2-((S)-2-ethoxypentanamido)-5-oxohexanoate
27
isopropyl (S)-6-diazo-2-((S)-2-isopropoxypentanamido)-5-
oxohexanoate
28
isopropyl (S)-6-diazo-2-((S)-2-methoxy-4-methylpentanamido)-5-
oxohexanoate
29
isopropyl (S)-6-diazo-2-((S)-2-ethoxy-4-methylpentanamido)-5-
oxohexanoate
30
isopropyl (S)-6-diazo-2-((S)-2-isopropoxy-4-methylpentanamido)-5-
oxohexanoate
31
isopropyl (S)-6-diazo-2-((S)-2-hydroxy-3,3-dimethylbutanamido)-5-
oxohexanoate
32
isopropyl (S)-6-diazo-2-((S)-2-methoxy-3,3-dimethylbutanamido)-5-
oxohexanoate
33
isopropyl (S)-6-diazo-2-((S)-2-ethoxy-3,3-dimethylbutanamido)-5-
oxohexanoate
34
isopropyl (S)-6-diazo-2-((S)-2-isopropoxy-3,3-dimethylbutanamido)-5-
oxohexanoate
35
isopropyl (S)-6-diazo-2-((S)-2-hydroxyhexanamido)-5-oxohexanoate
36
isopropyl (S)-6-diazo-2-((S)-2-methoxyhexanamido)-5-oxohexanoate
37
isopropyl (S)-6-diazo-2-((S)-2-ethoxyhexanamido)-5-oxohexanoate
38
isopropyl (S)-6-diazo-2-((S)-2-isopropoxyhexanamido)-5-oxohexanoate
39
isopropyl (S)-6-diazo-2-(3-methoxy-2-oxopropanamido)-5-
oxohexanoate
40
isopropyl (S)-6-diazo-2-(3-hydroxy-2-oxopropanamido)-5-
oxohexanoate
41
isopropyl (S)-6-diazo-2-(3-hydroxypropanamido)-5-oxohexanoate
42
isopropyl (S)-6-diazo-2-((S)-3-hydroxybutanamido)-5-oxohexanoate
43
isopropyl (S)-6-diazo-2-(3-methoxypropanamido)-5-oxohexanoate
44
isopropyl (S)-6-diazo-2-((S)-3-methoxybutanamido)-5-oxohexanoate
45
isopropyl (S)-6-diazo-2-((S)-3-hydroxy-2-methylpropanamido)-5-
oxohexanoate
46
isopropyl (S)-6-diazo-2-((S)-3-methoxy-2-methylpropanamido)-5-
oxohexanoate
47
isopropyl (S)-6-diazo-2-((2S,3R)-3-hydroxy-2-methylbutanamido)-5-
oxohexanoate
48
isopropyl (S)-6-diazo-2-((2S,3R)-3-methoxy-2-methylbutanamido)-5-
oxohexanoate
49
isopropyl (S)-6-diazo-2-((2R,3R)-3-hydroxy-2-methylbutanamido)-5-
oxohexanoate
50
isopropyl (S)-6-diazo-2-((2R,3R)-3-methoxy-2-methylbutanamido)-5-
oxohexanoate
51
isopropyl (S)-6-diazo-2-((2R,3S)-3-hydroxy-2-methylbutanamido)-5-
oxohexanoate
52
isopropyl (S)-6-diazo-2-((2R,3S)-3-methoxy-2-methylbutanamido)-5-
oxohexanoate
53
isopropyl (S)-6-diazo-2-((R)-3-hydroxybutanamido)-5-oxohexanoate
54
isopropyl (S)-6-diazo-2-((2S,3S)-3-hydroxy-2-methylbutanamido)-5-
oxohexanoate
55
isopropyl (S)-6-diazo-2-((2S,3S)-3-methoxy-2-methylbutanamido)-5-
oxohexanoate
56
isopropyl (S)-6-diazo-2-((R)-3-methoxybutanamido)-5-oxohexanoate
57
isopropyl (S)-6-diazo-2-((R)-3-hydroxy-2-methylpropanamido)-5-
oxohexanoate
58
isopropyl (S)-6-diazo-2-((R)-3-methoxy-2-methylpropanamido)-5-
oxohexanoate
59
tert-butyl (S)-6-diazo-2-((S)-2-methoxypropanamido)-5-oxohexanoate
60
tert-butyl (S)-6-diazo-2-((R)-2-methoxypropanamido)-5-oxohexanoate
61
isopropyl (S)-6-diazo-2-((S)-2-methoxy-4-(methylthio)butanamido)-5-
oxohexanoate
62
isopropyl (S)-6-diazo-2-(2-hydroxy-2-methylpropanamido)-5-
oxohexanoate
63
methyl (S)-6-diazo-2-((S)-2-methoxy-4-(methylthio)butanamido)-5-
oxohexanoate
64
methyl (S)-6-diazo-2-((S)-2-hydroxy-3-methylbutanamido)-5-
oxohexanoate
65
methyl (S)-6-diazo-2-(2-isopropoxyacetamido)-5-oxohexanoate
66
(S)-6-diazo-2-((S)-2-hydroxypropanamido)-5-oxohexanoic acid
67
isopropyl (S)-6-diazo-2-(2-isopropoxyacetamido)-5-oxohexanoate
68
methyl (S)-6-diazo-2-(2-methoxyacetamido)-5-oxohexanoate
69
S-isopropyl (S)-6-diazo-2-((S)-2-methoxypropanamido)-5-
oxohexanethioate
70
(S)-6-diazo-2-((S)-2-methoxy-4-(methylthio)butanamido)-5-
oxohexanoic acid
71
isopropyl (S)-6-diazo-2-((S)-2-(methoxy-d3)propanamido)-5-
oxohexanoate
72
(S)-6-diazo-2-((S)-2-(methoxy-d3)propanamido)-5-oxohexanoic acid
73
methyl (S)-6-diazo-2-((S)-2-(methoxy-d3)propanamido)-5-
oxohexanoate
74
ethyl (S)-6-diazo-2-((S)-2-(methoxy-d3)propanamido)-5-oxohexanoate
75
S-isopropyl (S)-6-diazo-2-((S)-2-(methoxy-d3)propanamido)-5-
oxohexanethioate
76
isopropyl (S)-6-diazo-2-((S)-2-(methoxy-d3)-4-(methylthio)
butanamido)-5-oxohexanoate
77
methyl-d3 (S)-6-diazo-2-((S)-2-methoxypropanamido)-5-oxohexanoate
78
ethyl-2,2,2-d3 (S)-6-diazo-2-((S)-2-methoxypropanamido)-5-
oxohexanoate
79
isopropyl (S)-6-diazo-2-(2-(ethoxy-2,2,2-d3)acetamido)-5-
oxohexanoate
80
isopropyl (S)-6-diazo-2-(2-(ethoxy-d5)acetamido)-5-oxohexanoate
81
ethyl-d5 (S)-6-diazo-2-((S)-2-methoxypropanamido)-5-oxohexanoate
82
propan-2-yl-d7 (S)-6-diazo-2-((S)-2-methoxypropanamido)-5-
oxohexanoate
83
propan-2-yl-d7 (S)-6-diazo-2-((S)-2-hydroxypropanamido)-5-
oxohexanoate
84
propan-2-yl-d7 (S)-6-diazo-2-((S)-2-hydroxy-3-methylbutanamido)-5-
oxohexanoate
85
propan-2-yl-d7 (S)-6-diazo-2-(2-ethoxyacetamido)-5-oxohexanoate
86
S-(propan-2-yl-d7) (S)-6-diazo-2-((S)-2-methoxypropanamido)-5-
oxohexanethioate
87
propan-2-yl-d7 (S)-6-diazo-2-((S)-2-methoxy-4-(methylthio)
butanamido)-5-oxohexanoate
88
methyl-d3 (S)-6-diazo-2-((S)-2-(methoxy-d3)propanamido)-5-
oxohexanoate
89
ethyl-2,2,2-d3 (S)-6-diazo-2-((S)-2-(methoxy-d3)propanamido)-5-
oxohexanoate
90
ethyl-d5 (S)-6-diazo-2-((S)-2-(methoxy-d3)propanamido)-5-
oxohexanoate
91
propan-2-yl-d7 (S)-6-diazo-2-((S)-2-(methoxy-d3)propanamido)-5-
oxohexanoate
92
propan-2-yl-d7 (S)-6-diazo-2-(2-(ethoxy-2,2,2-d3)acetamido)-5-
oxohexanoate
93
S-(propan-2-yl-d7) (S)-6-diazo-2-((S)-2-(methoxy-d3)propanamido)-5-
oxohexanethioate
94
propan-2-yl-d7 (S)-6-diazo-2-((S)-2-(methoxy-d3)-4-
(methylthio)butanamido)-5-oxohexanoate
95
propan-2-yl-d7 (S)-6-diazo-2-(2-(ethoxy-d5)acetamido)-5-
oxohexanoate
96
methyl 6-diazo-2-((S)-2-methoxypropanamido)-5-oxohexanoate-2-d
97
ethyl 6-diazo-2-((S)-2-methoxypropanamido)-5-oxohexanoate-2-d
98
isopropyl 6-diazo-2-((S)-2-methoxypropanamido)-5-oxohexanoate-2-d
99
isopropyl 6-diazo-2-(2-ethoxyacetamido)-5-oxohexanoate-2-d
100
S-isopropyl 6-diazo-2-((S)-2-methoxypropanamido)-5-
oxohexanethioate-2-d
101
isopropyl 6-diazo-2-((S)-2-methoxy-4-(methylthio)butanamido)-5-
oxohexanoate-2-d
102
isopropyl 6-diazo-2-((S)-2-hydroxypropanamido)-5-oxohexanoate-2-d
103
isopropyl 6-diazo-2-((S)-2-hydroxy-3-methylbutanamido)-5-
oxohexanoate-2-d
104
propan-2-yl-1,1,1,3,3,3-d6 (S)-6-diazo-2-((S)-2-(methoxy-
d3)propanamido)-5-oxohexanoate
105
propan-2-yl-1,1,1,3,3,3-d6 (S)-6-diazo-2-(2-(ethoxy-2,2,2-d3)
acetamido)-5-oxohexanoate
106
S-(propan-2-y1-1,1,1,3,3,3-d6) (S)-6-diazo-2-((S)-2-(methoxy-
d3)propanamido)-5-oxohexanethioate
107
propan-2-yl-1,1,1,3,3,3-d6 (S)-6-diazo-2-((S)-2-(methoxy-d3)-4-
(methylthio)butanamido)-5-oxohexanoate
108
propan-2-yl-1,1,1,3,3,3-d6 (S)-6-diazo-2-(2-(ethoxy-d5)acetamido)-5-
oxohexanoate
109
propan-2-yl-1,1,1,3,3,3-d6 (S)-6-diazo-2-((S)-2-hydroxypropanamido)-
5-oxohexanoate
110
propan-2-yl-1,1,1,3,3,3-d6 (S)-6-diazo-2-((S)-2-hydroxy-3-
methylbutanamido)-5-oxohexanoate
111
propan-2-yl-1,1,1-d3 (2S)-6-diazo-2-((S)-2-(methoxy-d3)
propanamido)-5-oxohexanoate
112
propan-2-yl-1,1,1-d3 (2S)-6-diazo-2-(2-(ethoxy-2,2,2-d3)acetamido)-5-
oxohexanoate
113
S-(propan-2-y1-1,1,1-d3) (2S)-6-diazo-2-((S)-2-(methoxy-
d3 )propanamido)-5-oxohexanethioate
114
propan-2-yl-1, 1,1-d3 (2S)-6-diazo-2-((S)-2-(methoxy-d3)-4-
(methylthio)butanamido)-5-oxohexanoate
115
propan-2-yl-1,1,1-d3 (2S)-6-diazo-2-(2-(ethoxy-d5)acetamido)-5-
oxohexanoate
116
propan-2-yl-1,1,1-d3 (2S)-6-diazo-2-((S)-2-hydroxypropanamido)-5-
oxohexanoate
117
propan-2-yl-1,1,1-d3 (2S)-6-diazo-2-((S)-2-hydroxy-3-
methylbutanamido)-5-oxohexanoate
118
propan-2-yl-1,1,1,3,3,3-d6 (S)-6-diazo-2-((S)-2-methoxypropanamido)-
5-oxohexanoate
119
propan-2-yl-1,1,1,3,3,3-d6 (S)-6-diazo-2-(2-ethoxyacetamido)-5-
oxohexanoate
120
S-(propan-2-y1-1,1,1,3,3,3-d6) (S)-6-diazo-2-((S)-2-
methoxypropanamido)-5-oxohexanethioate
121
propan-2-yl-1,1,1,3,3,3-d6 (S)-6-diazo-2-((S)-2-methoxy-4-
(methylthio)butanamido)-5-oxohexanoate
122
propan-2-yl-1,1,1-d3 (2S)-6-diazo-2-((S)-2-methoxypropanamido)-5-
oxohexanoate
123
propan-2-yl-1,1,1-d3 (2S)-6-diazo-2-(2-ethoxyacetamido)-5-
oxohexanoate
124
S-(propan-2-y1-1,1,1-d3) (2S)-6-diazo-2-((S)-2-methoxypropanamido)-
5-oxohexanethioate
125
propan-2-yl-1,1,1-d3 (2S)-6-diazo-2-((S)-2-methoxy-4-
(methylthio)butanamido)-5-oxohexanoate.

329 more elements

Dependencies are inferred from the claim text.

Facts

Application: 18/031,893Filed 14 Oct 2021
Priority: WO PCT/CN2020/12111415 Oct 2020
Published: US 2023/0399297 A114 Dec 2023
Granted: 17 Mar 2026
Term ends: Not estimatedThe source records don’t support an estimate.

Classification56 codes

C07D 209/20
Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals:…
A61P 35/00
Antineoplastic agents
C07C 245/18
Having diazo groups bound to acyclic carbon atoms of a carbon skeleton: the carbon skeleton being further substituted by carboxyl groups
C07C 255/14
Containing cyano groups and singly-bound oxygen atoms bound to the same saturated acyclic carbon skeleton: containing cyano groups and esterified…

Family

US 2023/0399297 A1Pre-grant publication · published 14 Dec 2023
US 12,577,201 B2This patent

From the US filing history. Foreign family members aren’t listed.

Timeline

Citations

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A compound or a pharmaceutically acceptable salt thereof, a stereoisomer thereof, a tautomer thereof, and an isotopic substitution thereof, wherein the compound is selected from:

1
isopropyl (S)-6-diazo-2-((S)-2-methoxypropanamido)-5-oxohexanoate
2
methyl (S)-6-diazo-2-((S)-2-methoxypropanamido)-5-oxohexanoate
3
(S)-6-diazo-2-((S)-2-methoxypropanamido)-5-oxohexanoic acid
4
ethyl (S)-6-diazo-2-((S)-2-methoxypropanamido)-5-oxohexanoate
5
isopropyl (S)-6-diazo-2-(2-methoxyacetamido)-5-oxohexanoate
6
isopropyl (S)-6-diazo-2-(2-ethoxyacetamido)-5-oxohexanoate
7
isopropyl (S)-6-diazo-2-((S)-2-hydroxypropanamido)-5-oxohexanoate
8
isopropyl (S)-6-diazo-2-((S)-2-hydroxy-4-methylpentanamido)-5-
oxohexanoate
9
isopropyl (S)-6-diazo-2-((S)-2-ethoxypropanamido)-5-oxohexanoate
10
isopropyl (S)-6-diazo-2-((S)-2-isopropoxypropanamido)-5-
oxohexanoate
11
isopropyl (S)-6-diazo-2-(2-hydroxyacetamido)-5-oxohexanoate
12
isopropyl (S)-6-diazo-2-((S)-2-hydroxybutanamido)-5-oxohexanoate
13
isopropyl (S)-6-diazo-2-((S)-2-methoxybutanamido)-5-oxohexanoate
14
isopropyl (S)-6-diazo-2-((S)-2-ethoxybutanamido)-5-oxohexanoate
15
isopropyl (S)-6-diazo-2-((S)-2-isopropoxybutanamido)-5-oxohexanoate
16
isopropyl (S)-6-diazo-2-((S)-2-hydroxy-3-methylbutanamido)-5-
oxohexanoate
17
isopropyl (S)-6-diazo-2-((S)-2-methoxy-3-methylbutanamido)-5-
oxohexanoate
18
isopropyl (S)-6-diazo-2-((S)-2-ethoxy-3-methylbutanamido)-5-
oxohexanoate
19
isopropyl (S)-6-diazo-2-((S)-2-isopropoxy-3-methylbutanamido)-5-
oxohexanoate
20
isopropyl (S)-6-diazo-2-((2S,3R)-2-hydroxy-3-methylpentanamido)-5-
oxohexanoate
21
isopropyl (S)-6-diazo-2-((2S,3R)-2-methoxy-3-methylpentanamido)-5-
oxohexanoate
22
isopropyl (S)-6-diazo-2-((2S,3R)-2-ethoxy-3-methylpentanamido)-5-
oxohexanoate
23
isopropyl (S)-6-diazo-2-((2S,3R)-2-isopropoxy-3-methylpentanamido)-
5-oxohexanoate
24
isopropyl (S)-6-diazo-2-((S)-2-hydroxypentanamido)-5-oxohexanoate
25
isopropyl (S)-6-diazo-2-((S)-2-methoxypentanamido)-5-oxohexanoate
26
isopropyl (S)-6-diazo-2-((S)-2-ethoxypentanamido)-5-oxohexanoate
27
isopropyl (S)-6-diazo-2-((S)-2-isopropoxypentanamido)-5-
oxohexanoate
28
isopropyl (S)-6-diazo-2-((S)-2-methoxy-4-methylpentanamido)-5-
oxohexanoate
29
isopropyl (S)-6-diazo-2-((S)-2-ethoxy-4-methylpentanamido)-5-
oxohexanoate
30
isopropyl (S)-6-diazo-2-((S)-2-isopropoxy-4-methylpentanamido)-5-
oxohexanoate
31
isopropyl (S)-6-diazo-2-((S)-2-hydroxy-3,3-dimethylbutanamido)-5-
oxohexanoate
32
isopropyl (S)-6-diazo-2-((S)-2-methoxy-3,3-dimethylbutanamido)-5-
oxohexanoate
33
isopropyl (S)-6-diazo-2-((S)-2-ethoxy-3,3-dimethylbutanamido)-5-
oxohexanoate
34
isopropyl (S)-6-diazo-2-((S)-2-isopropoxy-3,3-dimethylbutanamido)-5-
oxohexanoate
35
isopropyl (S)-6-diazo-2-((S)-2-hydroxyhexanamido)-5-oxohexanoate
36
isopropyl (S)-6-diazo-2-((S)-2-methoxyhexanamido)-5-oxohexanoate
37
isopropyl (S)-6-diazo-2-((S)-2-ethoxyhexanamido)-5-oxohexanoate
38
isopropyl (S)-6-diazo-2-((S)-2-isopropoxyhexanamido)-5-oxohexanoate
39
isopropyl (S)-6-diazo-2-(3-methoxy-2-oxopropanamido)-5-
oxohexanoate
40
isopropyl (S)-6-diazo-2-(3-hydroxy-2-oxopropanamido)-5-
oxohexanoate
41
isopropyl (S)-6-diazo-2-(3-hydroxypropanamido)-5-oxohexanoate
42
isopropyl (S)-6-diazo-2-((S)-3-hydroxybutanamido)-5-oxohexanoate
43
isopropyl (S)-6-diazo-2-(3-methoxypropanamido)-5-oxohexanoate
44
isopropyl (S)-6-diazo-2-((S)-3-methoxybutanamido)-5-oxohexanoate
45
isopropyl (S)-6-diazo-2-((S)-3-hydroxy-2-methylpropanamido)-5-
oxohexanoate
46
isopropyl (S)-6-diazo-2-((S)-3-methoxy-2-methylpropanamido)-5-
oxohexanoate
47
isopropyl (S)-6-diazo-2-((2S,3R)-3-hydroxy-2-methylbutanamido)-5-
oxohexanoate
48
isopropyl (S)-6-diazo-2-((2S,3R)-3-methoxy-2-methylbutanamido)-5-
oxohexanoate
49
isopropyl (S)-6-diazo-2-((2R,3R)-3-hydroxy-2-methylbutanamido)-5-
oxohexanoate
50
isopropyl (S)-6-diazo-2-((2R,3R)-3-methoxy-2-methylbutanamido)-5-
oxohexanoate
51
isopropyl (S)-6-diazo-2-((2R,3S)-3-hydroxy-2-methylbutanamido)-5-
oxohexanoate
52
isopropyl (S)-6-diazo-2-((2R,3S)-3-methoxy-2-methylbutanamido)-5-
oxohexanoate
53
isopropyl (S)-6-diazo-2-((R)-3-hydroxybutanamido)-5-oxohexanoate
54
isopropyl (S)-6-diazo-2-((2S,3S)-3-hydroxy-2-methylbutanamido)-5-
oxohexanoate
55
isopropyl (S)-6-diazo-2-((2S,3S)-3-methoxy-2-methylbutanamido)-5-
oxohexanoate
56
isopropyl (S)-6-diazo-2-((R)-3-methoxybutanamido)-5-oxohexanoate
57
isopropyl (S)-6-diazo-2-((R)-3-hydroxy-2-methylpropanamido)-5-
oxohexanoate
58
isopropyl (S)-6-diazo-2-((R)-3-methoxy-2-methylpropanamido)-5-
oxohexanoate
59
tert-butyl (S)-6-diazo-2-((S)-2-methoxypropanamido)-5-oxohexanoate
60
tert-butyl (S)-6-diazo-2-((R)-2-methoxypropanamido)-5-oxohexanoate
61
isopropyl (S)-6-diazo-2-((S)-2-methoxy-4-(methylthio)butanamido)-5-
oxohexanoate
62
isopropyl (S)-6-diazo-2-(2-hydroxy-2-methylpropanamido)-5-
oxohexanoate
63
methyl (S)-6-diazo-2-((S)-2-methoxy-4-(methylthio)butanamido)-5-
oxohexanoate
64
methyl (S)-6-diazo-2-((S)-2-hydroxy-3-methylbutanamido)-5-
oxohexanoate
65
methyl (S)-6-diazo-2-(2-isopropoxyacetamido)-5-oxohexanoate
66
(S)-6-diazo-2-((S)-2-hydroxypropanamido)-5-oxohexanoic acid
67
isopropyl (S)-6-diazo-2-(2-isopropoxyacetamido)-5-oxohexanoate
68
methyl (S)-6-diazo-2-(2-methoxyacetamido)-5-oxohexanoate
69
S-isopropyl (S)-6-diazo-2-((S)-2-methoxypropanamido)-5-
oxohexanethioate
70
(S)-6-diazo-2-((S)-2-methoxy-4-(methylthio)butanamido)-5-
oxohexanoic acid
71
isopropyl (S)-6-diazo-2-((S)-2-(methoxy-d3)propanamido)-5-
oxohexanoate
72
(S)-6-diazo-2-((S)-2-(methoxy-d3)propanamido)-5-oxohexanoic acid
73
methyl (S)-6-diazo-2-((S)-2-(methoxy-d3)propanamido)-5-
oxohexanoate
74
ethyl (S)-6-diazo-2-((S)-2-(methoxy-d3)propanamido)-5-oxohexanoate
75
S-isopropyl (S)-6-diazo-2-((S)-2-(methoxy-d3)propanamido)-5-
oxohexanethioate
76
isopropyl (S)-6-diazo-2-((S)-2-(methoxy-d3)-4-(methylthio)
butanamido)-5-oxohexanoate
77
methyl-d3 (S)-6-diazo-2-((S)-2-methoxypropanamido)-5-oxohexanoate
78
ethyl-2,2,2-d3 (S)-6-diazo-2-((S)-2-methoxypropanamido)-5-
oxohexanoate
79
isopropyl (S)-6-diazo-2-(2-(ethoxy-2,2,2-d3)acetamido)-5-
oxohexanoate
80
isopropyl (S)-6-diazo-2-(2-(ethoxy-d5)acetamido)-5-oxohexanoate
81
ethyl-d5 (S)-6-diazo-2-((S)-2-methoxypropanamido)-5-oxohexanoate
82
propan-2-yl-d7 (S)-6-diazo-2-((S)-2-methoxypropanamido)-5-
oxohexanoate
83
propan-2-yl-d7 (S)-6-diazo-2-((S)-2-hydroxypropanamido)-5-
oxohexanoate
84
propan-2-yl-d7 (S)-6-diazo-2-((S)-2-hydroxy-3-methylbutanamido)-5-
oxohexanoate
85
propan-2-yl-d7 (S)-6-diazo-2-(2-ethoxyacetamido)-5-oxohexanoate
86
S-(propan-2-yl-d7) (S)-6-diazo-2-((S)-2-methoxypropanamido)-5-
oxohexanethioate
87
propan-2-yl-d7 (S)-6-diazo-2-((S)-2-methoxy-4-(methylthio)
butanamido)-5-oxohexanoate
88
methyl-d3 (S)-6-diazo-2-((S)-2-(methoxy-d3)propanamido)-5-
oxohexanoate
89
ethyl-2,2,2-d3 (S)-6-diazo-2-((S)-2-(methoxy-d3)propanamido)-5-
oxohexanoate
90
ethyl-d5 (S)-6-diazo-2-((S)-2-(methoxy-d3)propanamido)-5-
oxohexanoate
91
propan-2-yl-d7 (S)-6-diazo-2-((S)-2-(methoxy-d3)propanamido)-5-
oxohexanoate
92
propan-2-yl-d7 (S)-6-diazo-2-(2-(ethoxy-2,2,2-d3)acetamido)-5-
oxohexanoate
93
S-(propan-2-yl-d7) (S)-6-diazo-2-((S)-2-(methoxy-d3)propanamido)-5-
oxohexanethioate
94
propan-2-yl-d7 (S)-6-diazo-2-((S)-2-(methoxy-d3)-4-
(methylthio)butanamido)-5-oxohexanoate
95
propan-2-yl-d7 (S)-6-diazo-2-(2-(ethoxy-d5)acetamido)-5-
oxohexanoate
96
methyl 6-diazo-2-((S)-2-methoxypropanamido)-5-oxohexanoate-2-d
97
ethyl 6-diazo-2-((S)-2-methoxypropanamido)-5-oxohexanoate-2-d
98
isopropyl 6-diazo-2-((S)-2-methoxypropanamido)-5-oxohexanoate-2-d
99
isopropyl 6-diazo-2-(2-ethoxyacetamido)-5-oxohexanoate-2-d
100
S-isopropyl 6-diazo-2-((S)-2-methoxypropanamido)-5-
oxohexanethioate-2-d
101
isopropyl 6-diazo-2-((S)-2-methoxy-4-(methylthio)butanamido)-5-
oxohexanoate-2-d
102
isopropyl 6-diazo-2-((S)-2-hydroxypropanamido)-5-oxohexanoate-2-d
103
isopropyl 6-diazo-2-((S)-2-hydroxy-3-methylbutanamido)-5-
oxohexanoate-2-d
104
propan-2-yl-1,1,1,3,3,3-d6 (S)-6-diazo-2-((S)-2-(methoxy-
d3)propanamido)-5-oxohexanoate
105
propan-2-yl-1,1,1,3,3,3-d6 (S)-6-diazo-2-(2-(ethoxy-2,2,2-d3)
acetamido)-5-oxohexanoate
106
S-(propan-2-y1-1,1,1,3,3,3-d6) (S)-6-diazo-2-((S)-2-(methoxy-
d3)propanamido)-5-oxohexanethioate
107
propan-2-yl-1,1,1,3,3,3-d6 (S)-6-diazo-2-((S)-2-(methoxy-d3)-4-
(methylthio)butanamido)-5-oxohexanoate
108
propan-2-yl-1,1,1,3,3,3-d6 (S)-6-diazo-2-(2-(ethoxy-d5)acetamido)-5-
oxohexanoate
109
propan-2-yl-1,1,1,3,3,3-d6 (S)-6-diazo-2-((S)-2-hydroxypropanamido)-
5-oxohexanoate
110
propan-2-yl-1,1,1,3,3,3-d6 (S)-6-diazo-2-((S)-2-hydroxy-3-
methylbutanamido)-5-oxohexanoate
111
propan-2-yl-1,1,1-d3 (2S)-6-diazo-2-((S)-2-(methoxy-d3)
propanamido)-5-oxohexanoate
112
propan-2-yl-1,1,1-d3 (2S)-6-diazo-2-(2-(ethoxy-2,2,2-d3)acetamido)-5-
oxohexanoate
113
S-(propan-2-y1-1,1,1-d3) (2S)-6-diazo-2-((S)-2-(methoxy-
d3 )propanamido)-5-oxohexanethioate
114
propan-2-yl-1, 1,1-d3 (2S)-6-diazo-2-((S)-2-(methoxy-d3)-4-
(methylthio)butanamido)-5-oxohexanoate
115
propan-2-yl-1,1,1-d3 (2S)-6-diazo-2-(2-(ethoxy-d5)acetamido)-5-
oxohexanoate
116
propan-2-yl-1,1,1-d3 (2S)-6-diazo-2-((S)-2-hydroxypropanamido)-5-
oxohexanoate
117
propan-2-yl-1,1,1-d3 (2S)-6-diazo-2-((S)-2-hydroxy-3-
methylbutanamido)-5-oxohexanoate
118
propan-2-yl-1,1,1,3,3,3-d6 (S)-6-diazo-2-((S)-2-methoxypropanamido)-
5-oxohexanoate
119
propan-2-yl-1,1,1,3,3,3-d6 (S)-6-diazo-2-(2-ethoxyacetamido)-5-
oxohexanoate
120
S-(propan-2-y1-1,1,1,3,3,3-d6) (S)-6-diazo-2-((S)-2-
methoxypropanamido)-5-oxohexanethioate
121
propan-2-yl-1,1,1,3,3,3-d6 (S)-6-diazo-2-((S)-2-methoxy-4-
(methylthio)butanamido)-5-oxohexanoate
122
propan-2-yl-1,1,1-d3 (2S)-6-diazo-2-((S)-2-methoxypropanamido)-5-
oxohexanoate
123
propan-2-yl-1,1,1-d3 (2S)-6-diazo-2-(2-ethoxyacetamido)-5-
oxohexanoate
124
S-(propan-2-y1-1,1,1-d3) (2S)-6-diazo-2-((S)-2-methoxypropanamido)-
5-oxohexanethioate
125
propan-2-yl-1,1,1-d3 (2S)-6-diazo-2-((S)-2-methoxy-4-
(methylthio)butanamido)-5-oxohexanoate.

329 more elements

Facts

Application

18/031,893Filed 14 Oct 2021

Priority

WO PCT/CN2020/12111415 Oct 2020

Published

US 2023/0399297 A114 Dec 2023

Granted

17 Mar 2026

Term ends

Not estimatedThe source records don’t support an estimate.

Classification56 codes

C07D 209/20
Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals:…
A61P 35/00
Antineoplastic agents
C07C 245/18
Having diazo groups bound to acyclic carbon atoms of a carbon skeleton: the carbon skeleton being further substituted by carboxyl groups
C07C 255/14
Containing cyano groups and singly-bound oxygen atoms bound to the same saturated acyclic carbon skeleton: containing cyano groups and esterified…