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US 11,530,234 B2Granted
CD73 inhibitors and pharmaceutical uses thereof
AssigneeRisen (Suzhou) Pharma Tech Co., Ltd.
InventorsJiasheng Lu, Jiamin Gu, Gang Chen, Feng Zhou, Qiguo Zhang, Xuli Wang, Xiang Ji, Lin Wang, Xianqi Kong
Life of this patent
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Abstract
CD73 (also known as ecto-5′-nucleotidase) inhibitor compounds are provided, as well as compositions and uses thereof for treating or preventing CD73-associated or related diseases, disorders and conditions, including cancer- and immune-related disorders. CD73 inhibitor compounds include compounds having the structure set forth in Formula I and pharmaceutically acceptable esters or salts thereof.
Claims21
A compound of Formula I, or a pharmaceutically acceptable ester or salt thereof:
- where:
- W is oxygen, sulfur, nitrogen, or a methylene group;
- X is a moiety selected from phosphonyl (—P(═O)(OR)—), sulfonyl (—S(═O)2—), and carbonyl (—C(═O)—), where R is a hydrogen, an ester-forming group, or a protecting group;
- or X and W together form —(CR7R8)n, where n is an integer from 0 to 3, and R7 and R8 are independently selected from a hydrogen, a halogen, a hydroxyl group, and a lower alkyl group having 1 to 4 carbon atoms;
- Y is selected from phosphonate (—PO3R2), sulfonate (—SO3R), and carboxylate (—CO2R), where R is a hydrogen, an ester-forming group, or a protecting group;
- R1 is a hydroxyl group or a hydrogen;
- R2 is a chlorine or a hydrogen;
- and
- R3 and R4 are independently selected from a hydrogen, an alkyl group, an alkenyl group and an alkynyl group, where at least one of R3 and R4 has 1 to 30 carbon atoms, wherein at least one of R3 and R4 has 11 to 30 carbon atoms when W is O or S;
- or
- R3 and R4 are independently selected from a hydrogen and a ring system which is a monocycle, bicycle, tricycle, spiral-ring, fused-ring, or bridged-ring containing carbocyclic or heterocyclic ring system, the carbocyclic ring system being aromatic or non-aromatic, provided that R3 and R4 are not both hydrogen, and provided that the ring system is not a monocycle when W is O or S;
- or
- R3, R4, and the nitrogen atom to which they are attached form a heterocyclic system which is independently selected from a monocycle, a bicycle, a tricycle, a spiral-ring, a fused-ring, and a bridged-ring system.
10 more elements
A compound which is:
- or a pharmaceutically acceptable salt or ester thereof.
Dependencies are inferred from the claim text.