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Compounds comprising cleavable linkers and uses thereof
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A technology of compounds and conjugates, applied in the field of compounds containing cleavable linkers, which can solve problems such as low activity
Pending Publication Date: 2022-04-12
INTOCELL INC
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The linker component of an ADC is an important feature for the development of targeted anticancer agents with desirable target specificity, i.e. high activity in tumor cells but low activity in healthy cells
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Embodiment 1
[1202] [Example 1] Preparation of Int-TG
[1203]
[1204] in N 2 β-D-Galactose pentaacetate (Alfa, CAS 4163-60-4, 5.0 g, 12.81 mmol) was dissolved in 33% HBr in AcOH (20 mL) at 0 °C under atmosphere. The mixture was warmed to room temperature. After stirring at room temperature for 4 hours, the mixture was concentrated under reduced pressure, and then EA (1000 mL) and saturated sodiumbicarbonate (1000 mL) were added. The organic layer was washed with anhydrous Na 2 SO 4 Dry, filter, and concentrate under reduced pressure. The residue was purified by column chromatography to provide compound Int-TG (5.2 g, 99%).
[1206] [Example 2] Preparation of compound Int-TG1
[1207]
[1208] Preparation of compound Int-TG1-1
[1209] in N 2 To a solution of salicylaldehyde (Aldrich, CAS 90-02-8, 148 mg, 1.22 mmol) and compound Int-TG (0.5 g, 1.22 mmol) in acetonitrile (10 mL) was added under atmosphere Dry molecular sieves (2.5g) and Ag 2 O (845 mg, 3.65 mmol). After stirring at room temperature for 1 hour, distilled water (50 mL) and EA (50 mL X2) were added. The organic layer was washed with anhydrous Na 2 SO 4 Dry, filter and concentrate under reduced pressure. The residue was purified by column chromatography to provide compound Int-TG1-1 (441 mg, 81%).
[1212] at 0°C in N 2 To a solution of compound Int-TG...
Embodiment 3
[1220] [embodiment 3] preparation of compound Int-TG2
[1221]
[1222] Preparation of compound Int-TG2-1
[1223] at 0°C in N 2 Under atmosphere, 3-formyl-4-hydroxybenzoic acid (3g, 18.06mmol) and 11-azido-3,6,9-trioxaundecane-1-amine (Aldrich Company, CAS 134179 -38-7, 5.98g, 23.48mmol) in DMF (20mL) were added EDCI (5.19g, 27.09mmol), HOBt (4.15g, 27.09mmol) and Et 3 N (10.1 mL, 72.24 mmol). The mixture was heated at room temperature under N 2 Stir overnight under atmosphere. The reaction was quenched with EA (60 mL x 2) and citric acid (60 mL). The organic layer was extracted with aqueous sodiumbicarbonate (80 mL). The obtained organic layer was subjected to anhydrous Na 2 SO 4 Dry, filter, and concentrate under reduced pressure. The residue was purified by column chromatography to provide compound Int-TG2-1 (2.56 g, 39%).
[1224] 1 H NMR (400MHz, CDCl 3 )δ11.26(s,1H),9.96(s,1H),8.16(s,1H),7.98-7.96(d,J=8.4Hz,1H),7.04-7.02(d,J=9.2Hz,1H ),6.91(s,1H),3.68...
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Abstract
The present invention relates to compounds comprising cleavable linkers and uses thereof. The present invention provides a compound comprising a cleavable linker, a use thereof, and an intermediate compound for preparing the compound, and more particularly, the compound comprising a cleavable linker of the present invention may comprise an active agent having a specific function or activity (e.g., a drug, a toxin, a ligand, a probe for detection, etc. In some embodiments, the active agent may include-S (= O) (= N-)-functional groups capable of selectively releasing the active agent, and functional groups that trigger chemical reactions, physical-chemical reactions, and / or biological reactions by external stimuli, and may also include ligands (e.g., oligopeptides, polypeptides, antibodies, etc.) having binding specificity for a desired target receptor.
Description
[0001] This application is a PCT international application PCT / IB2020 / 000019 submitted on January 2, 2020, which entered the Chinese national phase on July 1, 2021. The Chinese patent application number is 202080007805.2, and the title of the invention is "Compounds comprising Uses" is a divisional application of the invention patent application. [0002] related application [0003] This application claims the benefit of U.S. Provisional Patent Application No. 62 / 788,039, filed January 3, 2019, the contents of which are hereby incorporated by reference in their entirety. technical field [0004] The present invention relates to compounds comprising a cleavable linker and uses thereof. Background technique [0005] Antibody-drug conjugates (ADCs) are emerging as a powerful class of antineoplastic agents with efficacy against a range of cancers. ADCs generally consist of three distinct features: a cell-binding agent or targeting moiety; a linker; and a cytotoxic agent. The...
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