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US 2026/0125378 A2Published application
Heterocyclic Compounds
AssigneeBeOne Medicines I GmbH
InventorsGuoliang Zhang, Zhikun Ni, Jianzhuang Miao, Zhi Zhang, Ce Wang
Life of this patent
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Abstract
Disclosed herein is a compound of Formula (I) having the following structure for activating T cells, promoting T cell proliferation, and/or exhibiting antitumor activity, a method of using the compounds disclosed herein for treating cancer, and a pharmaceutical composition comprising the same.
Claims32
A compound of formula (I),
- or a pharmaceutically acceptable salt, a tautomer, a stereoisomer, an enantiomer, an isotopologue, or a prodrug thereof,
- wherein
- X1 is C or N,
- each of X2 and X3 is independently selected from —N— or —CH—;
- X4 is N, O or S;
- R1 is hydrogen, deuterium, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkoxyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, or substituted or unsubstituted heteroaryl;
- R2 is hydrogen, halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted alkoxyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, or substituted or unsubstituted heteroaryl, provided that R2 is absent when X1 is N;
- R4 is hydrogen, halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted alkoxyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, or substituted or unsubstituted heteroaryl, provided that R4 is absent when X4 is O or S;
- R5 is hydrogen, halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted alkoxyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, or substituted or unsubstituted heteroaryl, R5a—C(O)—, R5a—C(O)O—, R5a—O—C(O)—, R5a—C(O)NR5b—, R5a—NR5b—C(O)—, or R5a—SO2—, wherein R5a and R5b are each independently hydrogen, alkyl, or cycloalkyl;
- each of R7, R9, R8, and R10 is independently hydrogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted alkoxyl, substituted or unsubstituted cycloalkyl, —C(O)R7a, or -alkyl-C(O)R7a, and wherein R7a is hydrogen, alkyl, or alkoxy, provided that at least one of R7 and R9 is not hydrogen;
- or R7 and R9 are each hydrogen and R8 and R10 together form a bridge containing at least one —CH2-moiety in addition to the two bridgehead atoms;
- or R8 and R10 are each hydrogen and R7 and R9 together form a bridge containing at least one —CH2-moiety in addition to the two bridgehead atoms;
- L1 is a direct bond, —O—, —N(RL)—, substituted or unsubstituted alkyl, -alkylene or —C(O)—, wherein RL is hydrogen or alkyl;
- Cy1 is unsubstituted or substituted cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted heterocyclyl, or unsubstituted or substituted heteroaryl, wherein Cy1 is optionally substituted with 1 to 5 substituents R3a,
- wherein R3a is selected from deuterium, alkoxy, alkyl, halogen, oxo, R3b—SO2—, cycloalkyl, cyano, R3b—C(O)—N(R3c)—, N(R3bR3c)—C(O)—, N(R3bR3c), R3b—O—C(O)—, cycloalkyl or heterocyclyl;
- optionally wherein two R3a connect to the same carbon and together form a spirocyclic ring;
- optionally wherein two R3a form a fused ring with Cy1, wherein R3a is unsubstituted or substituted with cyano, alkoxy, alkyl, halogen, or hydroxy;
- and
- wherein R3b and R3c are each independently hydrogen or alkyl.
16 more elements
Dependencies are inferred from the claim text.