Back to results
US 12,570,600 B2Granted
Multifunctional linker compounds
Assignee20Bloc, Inc.
InventorsAlexander Lepak, Skylar J. Ferrara, Kai Lu, David Rozzell, Erik S. Goebel
Life of this patent
Estimating the term…
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.
Claims42
A compound of formula (I-1)
- or a salt, a stereoisomer, or a deuterated form thereof,
- wherein:
- R1 and R2 are each independently a leaving group;
- X1 is:
- (i) C6-10 arylene substituted with —C(O)—R1, and wherein R1 is a leaving group which is
- or
- (ii) C6-10 arylene substituted with —C(O)NH—(C1-12 alkylene)-(OCH2CH2)m—(CH2)n—N3, or —NHC(O)—(C1-12 alkylene)-(OCH2CH2)m—(CH2)n—N3, and wherein each m is independently an integer of 1-200, and each n is independently an integer of 0-100;
- wherein X1 is optionally substituted with 1 or 2 R3 as permitted by valency, and 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
- if X1 is an arylene substituted with one R3, then R3 is different from —C(O)—R1 or —C(O)—R2;
- and
- the compound is not
14 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(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.
7 more elements
A compound which is:
- or a salt, a stereoisomer, or a deuterated form thereof.
Dependencies are inferred from the claim text.