845305-83-1Relevant academic research and scientific papers
BIFUNCTIONAL MOLECULES CONTAINING AN E3 UBIQUITINE LIGASE BINDING MOIETY LINKED TO A BCL6 TARGETING MOIETY
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, (2021/04/23)
Bifunctional compounds, which find utility as modulators of B-cell lymphoma 6 protein (BCL6; target protein), are described herein. In particular, the bifunctional compounds of the present disclosure contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand that 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 bifunctional compounds of the present disclosure exhibit 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.
BRD9 BIFUNCTIONAL DEGRADERS AND THEIR METHODS OF USE
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Page/Page column 187; 188, (2021/04/01)
The disclosure provides BRD9 bifunctional compounds of Formula (A) or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, to their preparation, to pharmaceutical compositions comprising them, and to their use in the treatment of diseases and disorders mediated by a bromodomain-containing protein, such as bromodoma in-containing protein 9 (BRD9)
IRAK DEGRADERS AND USES THEREOF
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Paragraph 005203; 005206-005207, (2020/06/19)
The present invention provides compounds, compositions thereof, and methods of using the same.
N-(3-(7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL)PHENYL)BENZAMIDE DERIVATIVES
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Page/Page column 81, (2019/10/23)
The invention relates to compounds of the formula (I) (I) or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to use of the compounds in the treatment of disease.
3-HYDROXY-N-(3-(7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL)PHENYL)PYRROLIDINE-1-CARBOXAMIDE DERIVATIVES
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Page/Page column 83, (2019/10/23)
The invention relates to compounds of the formula (I) or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions compris
OXYPIPERIDINE DERIVATIVES AND METHODS OF USE THEREOF
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Page/Page column 43-44, (2009/05/29)
The present invention relates to novel Oxypiperidine Derivatives, pharmaceutical compositions comprising the Oxypiperidine Derivatives and the use of the Oxypiperidine Derivatives for treating or preventing treating allergy, an allergy-induced airway resp
A practical synthesis of differentially protected 4,4′-dipiperidinyl ethers: Novel ligands of pharmaceutical interest
Bailey, James M.,Bruton, Gordon,Huxley, Anthony,Johnstone, Vicky,Milner, Peter H.,Orlek, Barry S.,Stemp, Geoffrey
experimental part, p. 1051 - 1054 (2009/09/06)
An efficient four-step synthesis (requiring no purification) of Boc-protected 4,4′-dipiperidinyl ethers is described. Georg Thieme Verlag Stuttgart.
A two-step procedure for the preparation of mono-protected bis-N-heterocyclic alkyl ether systems
Chao, Jianhua,Israiel, Mariam,Zheng, Junying,Aki, Cynthia
, p. 791 - 794 (2007/10/03)
A two-step convenient sequence for the synthesis of previously inaccessible mono-Boc-protected bis-N-heterocyclic alkyl substituted ether derivatives 4 is described. Mitsunobu protocol was applied to the preparation of pyridinyl ether precursor 5. The reduction of the electron rich pyridinyl system 5 has been achieved catalytically using the combination of PtO2-H2SO4 or PtO2-pTsOH under a hydrogen atmosphere maintained by a gas balloon at ambient temperature.
Novel compounds useful for bradykinin B1 receptor antagonism
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Page/Page column 37, (2010/11/25)
Disclosed are compounds that are bradykinin B1 receptor antagonists and are useful for treating diseases, or relieving adverse symptoms associated with disease conditions, in mammals mediated by bradykinin B1 receptor.
SUBSTITUTED PIPERIDINES AS HISTAMINE H3 RECEPTOR LIGANDS
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Page/Page column 18-19, (2010/02/10)
The present invention relates to novel piperidine ether derivatives having affinity for the histamine H3 receptor, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.
