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US 2026/0224720 A1Published application
Ecteinascidin derivative antibody drug conjugates
AssigneeAdcytherix SAS
InventorJulia GAVRILYUK
Life of this patent
Estimating the term…
Abstract
Provided herein are compounds, methods, and pharmaceutical compositions for use in treatment of cancer. In certain embodiments, ecteinascidin derivative antibody drug conjugate compounds are provided which display remarkable efficacy and bioavailability for the treatment of, for example, cancer in a human.
Claims19
A compound of Formula (I), or a pharmaceutically acceptable salt, ester, stereoisomer, or tautomer thereof:
- wherein R1 and R2 form at least one aromatic ring or bicyclic heterocyclic ring, optionally substituted with one to six substituents, independently in each instance, selected from the group consisting of C1-10-alkoxy, C1-10-alkyl, amino, hydroxyl, halogen, nitro, —P(O)(OH)2, thiol, and —SO3H;
- wherein R20 is either:
- (a) selected from the group consisting of H, C1-10-alkyl, C1-10-aryl, C3-10-heterocycle, C(O)R5, C(O)OR5, C(O)NHR5, SO2R5, and SO2NHR5, wherein the C1-10-alkyl and C6-10-aryl are each, individually, substituted, or unsubstituted;
- or
- (b) L1, wherein L1 is a reactive linker group;
- wherein, R20 is optionally substituted by 1-3 substituents, independently in each instance, selected from the group consisting of OH, F, Cl, Br, C1-5-alkyl, C3-6-cycloalkyl, and C3-6-heterocycle;
- wherein R30 is either:
- (c) selected from the group consisting of H, C1-10-alkyl, C6-10-aryl, phosphate, thiophosphate, phosphoramide, C(O)R6, C(O)OR6, and C(O)NHR6, sulfonyl, sulfonylamide,
- wherein the C1-10-alkyl and C6-10-aryl are each, individually, substituted, or unsubstituted;
- or
- (d) L2, wherein L2 is a reactive linker group;
- wherein the phosphate and thiophosphate are optionally substituted with one to two substituents independently, in each instance, selected from the group consisting of H, C1-6-alkyl, C3-10-cycloalkyl, (poly(ethylene) glycol)y ([PEG]y), C6-10-aryl, and C5-10-heteroaryl,
- wherein C1-6-alkyl is optionally substituted with one to three substituents independently selected from the group consisting of methyl, ethyl, propyl, fluoro, chloro, bromo, iodo, amino, nitro, —P(O)(OH)2, thiol, —OH, and —SO3H;
- and
- wherein the substituent on the phosphate and thiophosphate is optionally terminated with a protecting group;
- wherein R5 and R6 are each, independently in each instance, selected from the group consisting of C1-6-alkyl, C3-10-cycloalkyl, [PEG]y, C6-10-aryl, and C6-10-heteroaryl,
- wherein C1-6-alkyl is optionally substituted with one to three substituents independently selected from the group consisting of methyl, ethyl, propyl, fluoro, chloro, bromo, iodo, amino, nitro, —P(O)(OH)2, thiol, —OH, and —SO3H;
- wherein at least one of R20 or R30 is not H;
- wherein is either a single or a double bond;
- and
- wherein subscript y is an integer selected from 0 to 32.
18 more elements
A compound of Formula (II) or a pharmaceutically acceptable salt, ester, stereoisomer, or tautomer thereof, comprising:
- wherein one of L1 or L2 is a reactive linker.
16-43. (canceled)
46-91. (canceled)
Dependencies are inferred from the claim text.