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US 2025/0243148 A1Published application
Multifunctional linker compounds
Assignee20Bloc, Inc.
InventorsAlexander LEPAK, Skylar J. FERRARA, Kai LU, David ROZZELL, Erik S. GOEBEL
Life of this patent
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Abstract
Provided herein are compounds of formula (I), or salt, stereoisomer, or deuterated form thereof, wherein X, R1, and R2 are defined herein. Also provided herein are conjugated compositions comprising reacted units of a molecule (e.g., a protein) and a compound of formula (I), or salt, stereoisomer, or deuterated form thereof.
Claims30
A compound of formula (I-1)
- or a salt, a stereoisomer, or a deuterated form thereof,
- wherein:
- X1 is arylene or heteroarylene, wherein X1 is optionally substituted with 1 or 2 R3 as permitted by valency;
- R1 and R2 are each independently a leaving group;
- each R3 is independently —OH, —CN, —NO2, halogen, oxo, —C1-6 alkyl, —C1-6 haloalkyl, —O(C1-6 alkyl), —S(C1-6 alkyl), —SO(C1-6 alkyl), —SO2(C1-6 alkyl), —(C1-12 alkylene)-N3, —(C1-12 alkylene)-(OCH2CH2)m—(CH2)n—N3, —C(O)NH—(C1-12 alkylene)-(OCH2CH2)m—(CH2)n—N3, —NHC(O)—(C1-12 alkylene)-(OCH2CH2)m—(CH2)n—N3, —O—(C1-12 alkylene)-(OCH2CH2)m—(CH2)n—N3, —S—(C1-12 alkylene)-(OCH2CH2)m—(CH2)n—N3, or —C(O)—R1, wherein each alkyl or alkylene is optionally and independently substituted with —C1-6 alkyl, —OH, —CN, —NO2, or halogen;
- each m is independently an integer of 1-200;
- and
- each n is independently an integer of 0-50,
- with the proviso that:
- if X1 is
- then the leaving group is not
- and
- if X1 is an arylene substituted with 1 R3, then R3 is different from —C(O)—R1 or —C(O)—R2.
10 more elements
A compound of formula (I-2)
- or a salt, a stereoisomer, or a deuterated form thereof,
- wherein:
- X2 is -L1-NRA-L2-,
- R1 and R2 are each independently a leaving group;
- RA is H, —C1-6 alkyl, aryl, —C(O)-aryl, —SO2(C1-6 alkyl), —SO2-aryl, or —(C1-6 alkylene)-(OCH2CH2)m—(CH2)n—N3, wherein each alkyl, aryl, or alkylene is optionally and independently substituted with —C1-6 alkyl, —OH, —CN, —NO2, or halogen;
- L1 and L2 are each independently C1-12 alkylene, C2-12 alkenylene, C2-12 alkynylene, C3-9 cycloalkylene, C3-9 cycloalkenylene, arylene, or heteroarylene, wherein L1 and L2 are optionally and independently substituted with 1-3 R3 as permitted by valency;
- each R3 is independently —OH, —CN, —NO2, halogen, oxo, —C1-6 alkyl, —C1-6 haloalkyl, —O(C1-6 alkyl), —S(C1-6 alkyl), —SO(C (alkyl), —SO2(C1-6 alkyl), —(C1-12 alkylene)-N3, —(C1-12 alkylene)-(OCH2CH2)m—(CH2)n—N3, —C(O)NH—(C1-12 alkylene)-(OCH2CH2)m—(CH2)n—N3, —NHC(O)—(C1-12 alkylene)-(OCH2CH2)m—(CH2)n—N3, —O—(C1-12 alkylene)-(OCH2CH2)m—(CH2)n—N3, —S—(C1-12 alkylene)-(OCH2CH2)m—(CH2)n—N3, or —C(O)—R1, wherein each alkyl or alkylene is optionally and independently substituted with —C1-6 alkyl, —OH, —CN, —NO2, or halogen;
- each m is independently an integer of 1-200;
- and
- each n is independently an integer of 0-50.
7 more elements
-26. (canceled)
A compound of formula (I-3)
- or a salt, a stereoisomer, or a deuterated form thereof,
- wherein:
- X3 is C1-24 alkylene, C2-24 alkenylene, or C2-24 alkynylene, wherein X2 is optionally substituted with 1-6 R3 as permitted by valency;
- R1 and R2 are each independently a leaving group, with the proviso that when X3 is unsubstituted, then the leaving group is not
- each R3 is independently —OH, —CN, —NO2, halogen, oxo, —C1-6 alkyl, —C1-6 haloalkyl, —O(C1-6 alkyl), —S(C1-6 alkyl), —SO(C1-6 alkyl), —SO2(C1-6 alkyl), —(C1-12 alkylene)-N3, —(C1-12 alkylene)-(OCH2CH2)m—(CH2)n—N3, —C(O)NH—(C1-12 alkylene)-(OCH2CH2)m—(CH2)n—N3, —NHC(O)—(C1-12 alkylene)-(OCH2CH2)m—(CH2)n—N3, —O—(C1-12 alkylene)-(OCH2CH2)m—(CH2)n—N3, —S—(C1-12 alkylene)-(OCH2CH2)m—(CH2)n—N3, or —C(O)—R1, wherein each alkyl or alkylene is optionally and independently substituted with —C1-6 alkyl, —OH, —CN, —NO2, or halogen;
- each m is independently an integer of 1-200;
- and
- each n is independently an integer of 0-50.
5 more elements
-41. (canceled)
A compound of formula (I-4)
- or a salt, a stereoisomer, or a deuterated form thereof,
- wherein:
- X4 is C3-9 cycloalkylene, C3-9 cycloalkenylene, 5-12 membered heterocyclylene containing 1 or 2 heteroatoms selected from N, S, or O, wherein X4 is optionally substituted with 1-6 R3 as permitted by valency;
- R1 and R2 are each independently a leaving group;
- each R3 is independently —OH, —CN, —NO2, halogen, oxo, —C1-6 alkyl, —C1-6 haloalkyl, —O(C1-6 alkyl), —S(C1-6 alkyl), —SO(C1-6 alkyl), —SO2(C1-6 alkyl), —(C1-12 alkylene)-N3, —(C1-12 alkylene)-(OCH2CH2)m—(CH2)n—N3, —C(O)NH—(C1-12 alkylene)-(OCH2CH2)m—(CH2)n—N3, —NHC(O)—(C1-12 alkylene)-(OCH2CH2)m—(CH2)n—N3, —O—(C1-12 alkylene)-(OCH2CH2)m—(CH2)n—N3, —S—(C1-12 alkylene)-(OCH2CH2)m—(CH2)n—N3, or —C(O)—R1, wherein each alkyl or alkylene is optionally and independently substituted with —C1-6 alkyl, —OH, —CN, —NO2, or halogen;
- each m is independently an integer of 1-200;
- and
- each n is independently an integer of 0-50.
5 more elements
-52. (canceled)
-70. (canceled)
Dependencies are inferred from the claim text.