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Cereblon ligands and bifunctional compounds comprising the same

A compound and cerebellar technology, applied in drug combination, organic chemistry, pharmaceutical formulation, etc.

Pending Publication Date: 2019-12-24
ARVINAS OPERATIONS INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, nonspecific effects and the complete inability to target and regulate certain classes of proteins, such as transcription factors, remain obstacles to the development of effective anticancer agents

Method used

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  • Cereblon ligands and bifunctional compounds comprising the same
  • Cereblon ligands and bifunctional compounds comprising the same
  • Cereblon ligands and bifunctional compounds comprising the same

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Experimental program
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Embodiment

[2217] abbreviation:

[2218] ACN: Acetonitrile

[2219] ADDP: 1,1'-(Azodicarbonyl)dipiperidine

[2220] BAST: N,N-bis(2-methoxyethyl)aminosulfur trifluoride

[2221] BPO: Benzoyl Peroxide

[2222] Cbz: Carbonylbenzyloxy

[2223] DAST: Diethylaminosulfur trifluoride

[2224] DBE: 1,2-dibromoethane

[2225] DCM: dichloromethane

[2226] DEAD: Diethyl azodicarboxylate

[2227] DIAD: Diisopropyl azodicarboxylate

[2228] DIBAL: Diisobutylaluminum hydride

[2229] DIEA or DIPEA: Diisopropylethylamine

[2230] DMA: N,N-Dimethylacetamide

[2231] DMF: N,N-Dimethylformamide

[2232] DMP: Dess-Martin periodinane

[2233] EA: ethyl acetate

[2234] EDCI: 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide

[2235] HBTU: N,N,N’N’-tetramethyl-O-(1H-benzotriazol-1-yl)uronium hexafluorophosphate

[2236] HMDS: Bis(trimethylsilyl)amine

[2237] HMPA: Hexamethylphosphoramide

[2238] LDA: lithium diisopropylamide

[2239] MCPBA: m-chloroperoxybenzoic acid

[2240] MsCl: methanesul...

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Abstract

The description relates to cereblon E3 ligase binding compounds, including bifunctional compounds comprising the same, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and / or otherwise inhibited by bifunctional compounds according to the present disclosure. In particular, the description provides compounds, which contain on one end a ligand which binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. Compounds can be synthesized that exhibit a broad range of pharmacological activities consistent with the degradation / inhibition of targeted polypeptides of nearly any type.

Description

[0001] Cross References to Related Applications [0002] This disclosure claims priority to US Provisional Application No. 62 / 452,972, filed January 31, 2017, which is hereby incorporated by reference in its entirety. [0003] incorporated by reference [0004] U.S. Patent Application Serial No. 15 / 230,354, filed August 5, 2016, published as U.S. Patent Application Publication No. 2017 / 0065719; U.S. Patent Application Serial No. 15 / 801,243, filed November 1, 2017; July 11, 2016 U.S. Patent Application Serial No. 15 / 206,497 filed on July 13, 2016; U.S. Patent Application Serial No. 15 / 730,728 filed on October 11, 2017; U.S. Patent Application Serial No. 15 / 829,541; U.S. Patent Application Serial No. 15 / 881,318 filed January 26, 2018; U.S. Patent Application Serial No. filed April 14, 2015 published as U.S. Patent Application Publication No. 2015 / 0291562 14 / 686,640; U.S. Patent Application Serial No. 14 / 792,414, filed July 6, 2015, published as U.S. Patent Application Publicatio...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/04A61K31/454A61K31/4725A61P35/00
CPCC07D401/14C07D417/14C07D471/04A61P35/02C07D487/04C07D495/14C07D498/04C07D471/10C07D401/04A61K31/454A61K31/4725A61P35/00
Inventor 安德鲁·P·克鲁斯迈克尔·贝尔林H·董基特·R·霍恩伯格Y·钱劳伦斯·B·斯奈德J·王库尔特·齐默尔曼
Owner ARVINAS OPERATIONS INC
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