911372-80-0Relevant academic research and scientific papers
ANTIBODY-CONJUGATED CHEMICAL INDUCERS OF DEGRADATION OF BRM AND METHODS THEREOF
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Page/Page column 159-161, (2022/02/05)
The subject matter described herein is directed to antibody-CIDE conjugates (Ab-CIDEs) that target BRM for degradation, to pharmaceutical compositions containing them, and to their use in treating diseases and conditions where BRM degradation is beneficial.
3-AZABICYCLO(3.1.0)HEXANE DERIVATIVES HAVING KDM5 INHIBITORY ACTIVITY AND USE THEREOF
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, (2021/11/13)
The present invention provides KDM5 inhibitor. The compound disclosed herein represented by the general formula (I) : wherein all symbols have the same meanings as the definitions described in the specification; or a salt thereof is useful as a prophylact
Synthesis of α-Substituted Primary Benzylamines through Copper-Catalyzed Cross-Dehydrogenative Coupling
Kramer, S?ren
supporting information, p. 65 - 69 (2019/01/04)
A copper-catalyzed route to α-substituted, primary benzylamines by C-H functionalization of alkylarenes is described. The method directly affords the amine hydrochloride salt. Catalyst loadings down to 0.1 mol % in combination with scalability, insensitivity to air and moisture, and no need for column chromatography makes the procedure highly practical. The facile synthesis of the racemate of a blockbuster drug highlights the relevance for the development of pharmaceuticals. Preliminary mechanistic data are also included.
MODULATORS OF ESTROGEN RECEPTOR PROTEOLYSIS AND ASSOCIATED METHODS OF USE
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Paragraph 00434, (2018/08/20)
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 a cereblon, Von Hippel-Lindau ligase-binding moiety, Inhibitors of Apotosis Proteins, or mouse double-minute homolog 2 ligand, 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.
PYRROLOPYRIMIDIN-7-ONE DERIVATIVES AND THEIR USE AS PHARMACEUTICALS
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Page/Page column 177, (2009/01/20)
Compounds of formula (I) or pharmaceutically acceptable salts thereof wherein R1, R2, R3, R4, and R5 and are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
Reversal of diastereofacial selectivity in hydride reductions of N-tert-butanesulfinyl imines
Colyer, John T.,Andersen, Neil G.,Tedrow, Jason S.,Soukup, Troy S.,Faul, Margaret M.
, p. 6859 - 6862 (2007/10/03)
A variety of N-tert-butanesulfinyl imines were reduced with NaBH 4 in THF containing 2% water to provide the corresponding secondary sulfinamides in high yield and diastereoselectivity. By using the same sulfinyl imine starting materials and changing the reductant to L-Selectride, the stereoselectivity could be efficiently reversed to afford the opposite product diastereomer in high yield and selectivity.
