- DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHODS OF USE
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Bifunctional compounds formed by conjugating BTK inhibitor moieties with E3 ligase ligand moieties, which function to recruit targeted proteins to E3 ubiquitin ligase for degradation, and methods of preparation and uses thereof.
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- Porphyrin Donor and Tunable Push–Pull Acceptor Conjugates—Experimental Investigation of Marcus Theory
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We report on a series of electron donor–acceptor conjugates incorporating a ZnII–porphyrin-based electron donor and a variety of non-conjugated rigid linkers connecting to push–pull chromophores as electron acceptors. The electron acceptors comprize multicyanobutadienes or extended tetracyanoquinodimethane analogues with first reduction potentials ranging from ?1.67 to ?0.23 V vs. Fc+/Fc in CH2Cl2, which are accessible through a final-step cycloaddition–retroelectrocyclization (CA-RE) reaction. Characterization of the conjugates includes electrochemistry, spectroelectrochemistry, DFT calculations, and photophysical measurements in a range of solvents. The collected data allows for the construction of multiple Marcus curves that consider electron-acceptor strength, linker length, and solvent, with data points extending well into the inverted region. The enhancement of electron–vibration couplings, resulting from the rigid spacers and, in particular, multicyano-groups in the conformationally highly fixed push–pull acceptor chromophores affects the charge-recombination kinetics in the inverted region drastically.
- Reekie, Tristan A.,Sekita, Michael,Urner, Lorenz M.,Bauroth, Stefan,Ruhlmann, Laurent,Gisselbrecht, Jean-Paul,Boudon, Corinne,Trapp, Nils,Clark, Timothy,Guldi, Dirk M.,Diederich, Fran?ois
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supporting information
p. 6357 - 6369
(2017/05/12)
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- PYRROLOTRIAZINES AS ALK AND JAK2 INHIBITORS
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The present invention provides a compound of formula (I) or a salt form thereof, wherein Q1, Q2, Q3, and Q4 are as defined herein. The compound of formula (I) has ALK and/or JAK2 inhibitory activity, and may be used to treat proliferative disorders.
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Page/Page column 375
(2010/08/05)
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- RETROMETABOLIC COMPOUNDS
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The present invention relates to phenylaminopyrimidine compounds that are retrometabolic drugs or metabolites thereof. These compounds are also inhibitors of protein kinases including JAK kinases, in particular JAK2 kinases and can be used in the treatmen
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Page/Page column 57-58
(2009/04/25)
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- Thiohydantoins and use thereof for treating diabetes
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The invention relates to 2-thiohydantoin derivative compounds selected from compounds of general formula (I): as defined in the claims, and to their addition salts with an acid, notably pharmaceutically acceptable salts. The invention also relates to thei
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Page/Page column 8
(2010/02/07)
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