Tetrahydronaphthalene and tetrahydroisoquinoline derivatives as estrogen receptor degraders

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
CN110291087APending Publication Date: 2019-09-27ARVINAS OPERATIONS INC
37 Cites 14 Cited by

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
ARVINAS OPERATIONS INC
Publication Date
2019-09-27

Smart Images

  • Figure 1
    Figure 1
  • Figure 2
    Figure 2
  • Figure 3
    Figure 3
Patent Text Reader

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.
Need to check novelty before this filing date? Find Prior Art

Description

[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...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More