3360-79-0Relevant articles and documents
Cu-Catalyzed C-H Allylation of Benzimidazoles with Allenes
Dong, Yaxi,Breit, Bernhard
, p. 6765 - 6769 (2021/09/11)
CuH-catalyzed intramolecular cyclization and intermolecular allylation of benzimidazoles with allenes have been described. The reaction proceeded smoothly with the catalytic system of Cu(OAc)2/Xantphos and catalytic amount of (MeO)2MeSiH. This protocol features mild reaction conditions and a good tolerance of substrates bearing electron-withdrawing, electron-donating, or electron-neutral groups. A new catalytic mechanism was proposed for this copper hydride catalytic system.
Lysophosphatidic acid receptor antagonists and preparation method thereof
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Paragraph 0681-0682; 0683-0685, (2020/07/29)
The invention belongs to the technical field of medicinal chemistry, and particularly relates to lysophosphatidic acid receptor antagonists and a preparation method thereof. The applicant surprisinglyfinds that compounds provided by the invention have high LPAR1 antagonistic activity and selectivity, low toxicity, good metabolic stability and good drug development prospect, and can be used for preventing or treating diseases or symptoms related to LPAR1. The applicant also accidentally finds that the IC50 value of part of the compounds can be as low as 300 nM or below and even 50 nM or below.Moreover, the compounds disclosed by the invention have better safety, and the CC50 range of the compounds can reach 200 [mu]M or above. In addition, the compounds of the present invention have goodmetabolic stability in humans, rats, and mice, such excellent inhibitory activity being very desirable for their use as LPAR1 inhibitors in the above diseases or disorders. In addition, the preparation method of the compounds is simple, mild in reaction condition, high in product yield and suitable for industrial production.
Development of a Selective Inhibitor of Protein Arginine Deiminase 2
Muth, Aaron,Subramanian, Venkataraman,Beaumont, Edward,Nagar, Mitesh,Kerry, Philip,McEwan, Paul,Srinath, Hema,Clancy, Kathleen,Parelkar, Sangram,Thompson, Paul R.
supporting information, p. 3198 - 3211 (2017/04/19)
Protein arginine deiminase 2 (PAD2) plays a key role in the onset and progression of multiple sclerosis, rheumatoid arthritis, and breast cancer. To date, no PAD2-selective inhibitor has been developed. Such a compound will be critical for elucidating the