- BRM TARGETING COMPOUNDS AND ASSOCIATED METHODS OF USE
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The present disclosure relates to bifunctional compounds, which find utility as modulators of SMARCA2 or BRM (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a ligand that binds to the Von Hippel-Lindau 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.
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Paragraph 1033-1034
(2019/10/23)
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- Synthesis and polarized photoluminescence of novel phosphorescent cyclometalated platinum dimer
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A novel phosphorescent cyclometalated platinum dimer with bis-[2-(p-dodecyloxyphenyl) pyridyl]-hexane-1,6-diol as ligand and 1,3-(1-n-hexyl,3-n-heptadecyl) diketone as ancillary ligand was synthesized. The chemical structure and liquid crystal property of
- Jiang, Shi Ping,Luo, Kai Jun,Wang, Ying Han,Wang, Xin,Jiang, Ying,Wei, Yan Yan
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scheme or table
p. 1005 - 1008
(2012/01/11)
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- A revised synthesis of the antitumour antibiotic L-azatyrosine via 2-iodo-5-methoxypyridine
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A revised synthesis of the antitumour antibiotic L-azatyrosine is reported, the main features of which are the unambiguous synthesis of the previously misinterpreted 2-iodo-5-methoxypyridine and subsequent palladium-catalysed coupling with an iodoalanine-derived zinc reagent.
- Seton, Alison W.,Stevens, Malcolm F. G.,Westwell, Andrew D.
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p. 546 - 548
(2007/10/03)
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- Compounds and compositions as anticoagulants
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The present invention relates to novel biheterocyclic derivatives which are factor Xa inhibitors; the pharmaceutically acceptable salts and N-oxides thereof; their uses as therapeutic agents and the methods of their making.
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- New water-soluble duocarmycin derivatives: Synthesis and antitumor activity of A-ring pyrrole compounds bearing β-heteroarylacryloyl groups
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A series of A-ring pyrrole compounds of duocarmycin bearing 4'-methoxy- β-heteroarylacryloyl groups were synthesized and evaluated for in vitro anticellular activity against HeLa S3 cells and in vivo antitumor activity against murine sarcoma 18
- Amishiro, Nobuyoshi,Nagamura, Satoru,Kobayashi, Eiji,Gomi, Katsushige,Saito, Hiromitsu
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p. 669 - 676
(2007/10/03)
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- DC-89 derivatives
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Provided are DC-89 derivatives represented by the formula: STR1 wherein X represents Cl or Br, R represents hydrogen or COR1, and W represents STR2 and pharmaceutically acceptable salts thereof. The compounds of the present invention have excellent anti-tumor activity and are useful as anti-tumor agents.
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- An Efficient and Selective Method for the Preparation of Iodophenols
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Direct iodination of a wide range of phenols may be achieved with unprecedented selectivity in aqueous alcohol solvents by the action of a reagent preparated in situ from sodium hypochlorite and sodium iodide.Para-substituted phenols (or ortho-substituted, when the para-position is already occupied) are obtained in fair to excellent yields by simple isolation techniques.The extent of iodination is easily controlled by stoichiometry.The technique is also useful with some anilines.
- Edgar, Kevin J.,Falling, Stephen N.
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p. 5287 - 5291
(2007/10/02)
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