- POLYCYCLIC COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF RAPIDLY ACCELERATED FIBROSARCOMA POLYPEPTIDES
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The present disclosure relates to bifunctional compounds, ULM— L—PTM, which find utility as modulators of Rapidly Accelerated Fibrosarcoma (RAF, such as c-RAF, A- RAF and/or B-RAF; the target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, 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 RAF, 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, or the constitutive activation of the target protein, are treated or prevented with compounds and compositions of the present disclosure.
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Paragraph 2097; 2098
(2020/03/29)
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- NOVEL THIAZOLOPYRAZOLES AND METHODS OF THEIR USE
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This invention concerns novel thiazolopyrazole compounds of formula (I) and compositions comprising them. Methods of using these compounds for the treatment, prevention and management of various diseases and disorders are also encompassed by the invention.
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Page/Page column 55
(2008/06/13)
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- 4,7-dihydropyrazolo(3,4-b) pyridine derivatives
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Novel Ca-blockers, 4,7-dihydropyrazolo[3,4-b]pyridine derivatives having potent antihypertensive and coronary vasodilating actions and useful in treatment for diseases in circulatory system, but without systole inhibitory action.
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