2381044-50-2Relevant academic research and scientific papers
PYRIDAZINONES AS PARP7 INHIBITORS
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Page/Page column 44-46, (2021/05/07)
The present invention relates to pyridazinones and related compounds which are inhibitors of PARP7 and are useful in the treatment of cancer.
PYRIDAZINONES AS PARP7 INHIBITORS
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Page/Page column 29-30, (2021/05/07)
The present invention relates to pyridazinones and related compounds which are inhibitors of PARP7 and are useful in the treatment of cancer.
SOLID FORMS OF A PARP7 INHIBITOR
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Page/Page column 29, (2020/11/13)
The present invention relates to solid forms of the poly(ADP-ribose) polymerase 7 (PARP7) inhibitor 5-[[(2S)-1-(3-oxo-3-[4-[5-(trifluoromethyl)pyrimidin-2-yl]piperazin-1-yl]propoxy)propan-2-yl]amino]-4-(trifluoromethyl)-2,3-dihydropyridazin-3-one, and salts thereof, including methods of preparation thereof, where the inhibitor is useful in the treatment of cancer.
PYRIDAZINONES AS PARP7 INHIBITORS
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Paragraph 0633, (2019/11/11)
The present invention relates to pyridazinones and related compounds which are inhibitors of PARP7 and are useful in the treatment of cancer.
3-[(5-Chloro-2-hydroxyphenyl)methyl]-5-[4-(trifluoromethyl)phenyl]-1,3, 4-oxadiazol-2(3H)-one, BMS-191011: Opener of large-conductance Ca 2+-activated potassium (maxi-K) channels, identification, solubility, and SAR
Romine, Jeffrey L.,Martin, Scott W.,Meanwell, Nicholas A.,Gribkoff, Valentin K.,Boissard, Christopher G.,Dworetzky, Steven I.,Natale, Joanne,Moon, Sandra,Ortiz, Astrid,Yeleswaram, Swamy,Pajor, Lorraine,Gao, Qi,Starrett Jr., John E.
, p. 528 - 542 (2007/10/03)
Compound 8a (BMS-191011), an opener of the cloned large-conductance, Ca2+-activated potassium (maxi-K) channel, demonstrated efficacy in in vivo stroke models, which led to its nomination as a candidate for clinical evaluation. Its maxi-K channel opening properties were consistent with its structural topology, being derived by combining elements from other known maxi-K openers. However, 8a suffered from poor aqueous solubility, which complicated elucidation of SAR during in vitro evaluation. The activity of 8a in in vivo stroke models and studies directed toward improving its solubility are reported herein. Enhanced solubility was achieved by appending heterocycles to the 8a scaffold, and a notable observation was made that inclusion of a simple amino group (anilines 8k and 8l) yielded excellent in vitro maxi-K ion channel opening activity and enhanced brain-to-plasma partitioning compared to the appended heterocycles.
