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US 10,668,047 B2Granted
Aziridine containing DNA alkylating agents
AssigneeMolecular Templates, Inc.
InventorsMark Matteucci, Xiaohong Cai, Yeyu Cao, Hailong Jiao, Jing Yuan Ma, Jian-Xin Duan
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Abstract
Provided herein are compounds of formula (I)-(VI): wherein the variables are defined herein, processes of making them, and methods of treating cancer comprising administering such compounds.
Claims11
A compound selected from:
- or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of each thereof, wherein
- R1 is hydrogen, —N3, CN, NR21R22, —OR23, —SO2(C1-C6 alkyl), C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C8 cycloalkyl, C6-C10 aryl, 4-15 membered heterocycle, 5-15 membered heteroaryl, or ether;
- each R21 and R22 independently is hydrogen, hydroxy, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C8 cycloalkyl, C6-C10 aryl, 4-15 membered heterocycle, 5-15 membered heteroaryl, or —SO2(C1-C6 alkyl);
- or R21 and R22 together with the nitrogen atom they are bonded to form a 4-15 membered heterocycle or a 5-15 membered heteroaryl;
- R23 is hydrogen or C1-C6 alkyl;
- R2 is hydrogen or halo;
- R3 is hydrogen;
- R4 is hydrogen, halo, C1-C6 alkoxy, C1-C6 alkyl, or C6-C10 aryl,
- R5 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C8 cycloalkyl, C6-C10 aryl, 4-15 membered heterocycle, 5-15 membered heteroaryl;
- or R4 and R5 together with the intervening carbon atoms between them form a C5-C6 cycloalkyl ring;
- wherein the alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocycle, heteroaryl, alkoxy and ether groups are optionally substituted.
8 more elements
Dependencies are inferred from the claim text.