155058-02-9Relevant articles and documents
INDOLE COMPOUNDS AS ANDROGEN RECEPTOR MODULATORS
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Page/Page column 40; 46, (2022/02/05)
Provided herein are compounds of formula (V) that bind to BF3 of an androgen receptor (AR), which can modulate the AR for the treatment of Kennedy's disease.
INHIBITOR OF BTK AND MUTANTS THEREOF
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, (2020/09/12)
The disclosure includes compounds of Formula (I) (1) wherein Q0, Q1, Q2, Q3, Q4, Z, W, i, j, m, n, Warhead, R0, R1, R3, R4, R5, R6, and R7, are defined herein. Also disclosed is a method for treating a neoplastic disease, autoimmune disease, and inflammatory disorder with these compounds.
PRMT5 INHIBITORS AND USES THEREOF
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, (2016/04/20)
Described herein are compounds of Formula (A), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof:wherein Y1 is of formula (?) or formula (y):Ring Y is a 5- to 6-membered heteroaryl ring; and V4, V5, Rx, x, y, and n are as defined herein. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
Identification of a sirtuin 3 inhibitor that displays selectivity over sirtuin 1 and 2
Galli, Ubaldina,Mesenzani, Ornella,Coppo, Camilla,Sorba, Giovanni,Canonico, Pier Luigi,Tron, Gian Cesare,Genazzani, Armando A.
, p. 58 - 66,9 (2020/07/31)
As part of an effort to identify novel selective modulators of sirtuins, we synthesized and tested several isosteres and constrained analogues of nicotinamide. Biological data suggest that compound 2 is selective for Sirt3 over Sirt1 and Sirt2.
Efficacy switching SAR of mGluR5 allosteric modulators: Highly potent positive and negative modulators from one chemotype
Sams, Anette Graven,Mikkelsen, Gitte Kobber?e,Brodbeck, Robbin M.,Pu, Xiaosui,Ritzén, Andreas
, p. 3407 - 3410 (2011/07/07)
A series of metabotropic glutamate 5 receptor (mGluR5) allosteric ligands with positive, negative or no modulatory efficacy is described. The ability of this series to yield both mGluR5 PAMs and NAMs with single-digit nanomolar potency is unusual, and the
Ready access to 7,8-dihydro- and 1,2,3,4-tetrahydro-1,6-naphthyridine-5(6H) -ones from simple pyridine precursors
Showalter, H. D. Hollis
, p. 1311 - 1317 (2007/10/03)
Short pathways are described for the synthesis of a representative example of each of the 7,8-dihydro- and 1,2,3,4-tetrahydro-1,6-naphthyridine-5(6H)-one ring systems from simple pyridine precursors. An attempted synthesis of the related 4,6-dihydro-1,6-naphthyridin-5(1H)-one ring system from a common intermediate was unsuccessful.
Dihydro- and tetrahydronaphthyridines
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, (2008/06/13)
This invention concerns novel dihydro- and tetrahydronaphthyridines useful for enhancing the lethal effects on tumor cells to treatment causing DNA-damaging activity as with ionizing radiation or with a chemotherapeutic agent.