Tetrahydronaphthalene and tetrahydroisoquinoline derivatives as estrogen receptor degraders
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A technology of solvates and stereoisomers, applied in the field of tetrahydronaphthalene and tetrahydroisoquinoline derivatives as estrogen receptor degraders, can solve problems such as increase in MDM2
Pending Publication Date: 2019-09-27
ARVINAS OPERATIONS INC
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In response to DNA damage or cellular stress, p53 levels increase and due to a feedback loop from the p53 / MDM2 autoregulatory system, this also leads to an increase in MDM2
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[2204] pass 1 All synthesized compounds were characterized by H-NMR and analyzed for purity by LC / MS at wavelengths of 214 and 254 nM with UV detection. The purity of each compound in Table 1 and Table 2 was over 90%. The molecular weights observed from LC / MS are listed in Table 1 (see Figure 5 ) and Table 2 (see Figure 6 ) as [M+H] + listed. The synthetic methods used to prepare the respective compounds are listed in Table 1 and Table 2. Some molecules in Tables 1 and 2 are available as salts such as hydrochloride, acetate, formate or triflate. Only the structure of the neutral form of each compound is listed. 代表性化合物的1 H-NMR is listed in Table 3 (see Figure 7 ). Although the chemical names listed in Table 3 are for the neutral forms of the exemplary compounds, the corresponding 1 H-NMR data include both neutral and salt forms.
[2205] All synthetic chimeric molecules were evaluated for target engagement in T47D cells using a commercial kit for the ERE luciferase...
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Abstract
The present disclosure relates to bifunctional compounds, which find utility as modulators of estrogen receptor (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end at least one of a Von Hippel-Lindau ligand, a cereblon ligand, Inhibitors of Apoptosis Proteins ligand, mouse double-minute homolog 2 ligand, or a combination thereof, which binds to the respective E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
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[0001] Cross References to Related Applications [0002] This disclosure claims U.S. Provisional Patent Application No. 62 / 429,041, filed December 1, 2016, and titled: TETRAHYDRONAPHTHALENE AND TETRAHYDROISOQUINOLINE DERIVATIVES AS ESTROGEN RECEPTOR DEGRADERS, and filed August 1, 2017, and titled: TETRAHYDRONAPHTHALENE ANDTETRAHYDROISOQUINOLINE DERIVATIVES AS ESTROGEN RECEPTOR DEGRADERS Priority to US Provisional Patent Application No. 62 / 540,049 to RECEPTOR DEGRADERS, the contents of which are hereby incorporated by reference in their entirety for all purposes. [0003] incorporated by reference [0004] U.S. Patent Application Serial No. 15 / 230,354, filed August 5, 2016; and U.S. Patent Application 15 / 206,497, filed July 11, 2016; and U.S. Patent Application 15 / 2016, filed July 13, 2016 209,648; and U.S. Patent Application Serial No. 15 / 730,728, filed October 11, 2017; and U.S. Patent Application Serial No. 14 / 686,640, filed April 14, 2015 and published as U.S. Patent Appl...
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