1269260-00-5Relevant articles and documents
DIRECT THROMBIN INHIBITORS AND METHODS OF USE THEREOF
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Page/Page column 25; 28-29, (2021/10/22)
Novel direct thrombin inhibitors are provided herein, along with methods for their use as anticoagulants. The direct thrombin inhibitors described herein are useful in treating and/or preventing thromboembolism and bleeding or clotting disorders. Also provided herein are methods for inhibiting thrombin in a cell using the compounds and compositions described herein.
HETEROCYCLIC COMPOUNDS FOR MODULATING NR2F6
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Paragraph 00392; 00416, (2021/09/04)
The present disclosure relates to compounds capable of modulating the activity of NR2F6. The compounds of the disclosure may be used in methods for the prevention and/or the treatment of diseases and disorders associated with modulating NR2F6 activity.
Regio- and Stereoselective Palladium-Catalyzed C(sp3)-H Arylation of Pyrrolidines and Piperidines with C(3) Directing Groups
Antermite, Daniele,Affron, Dominic P.,Bull, James A.
, p. 3948 - 3952 (2018/07/22)
The selective synthesis of cis-3,4-disubstituted pyrrolidines and piperidines is achieved by a Pd-catalyzed C-H arylation with excellent regio- and stereoselectivity using an aminoquinoline auxiliary at C(3). The arylation conditions are silver free, use a low catalyst loading, and employ inexpensive K2CO3 as a base. Directing group removal is accomplished under new, mild conditions to access amide-, acid-, ester-, and alcohol-containing fragments and building blocks. This C-H arylation protocol enabled a short and stereocontrolled formal synthesis of (-)-paroxetine.
Design and syntheses of melanocortin subtype-4 receptor agonists. Part 2: Discovery of the dihydropyridazinone motif
Ujjainwalla, Feroze,Warner, Daniel,Snedden, Christine,Grisson, Ricky D.,Walsh, Thomas F.,Wyvratt, Matthew J.,Kalyani, Rubana N.,MacNeil, Tanya,Tang, Rui,Weinberg, David H.,Van Der Ploeg, Lex,Goulet, Mark T.
, p. 4023 - 4028 (2007/10/03)
Optimization of the biological activity of a new class of non-peptidyl, pyridazinone derived human melanocortin subtype-4 receptor agonists is disclosed.