191425-55-5Relevant articles and documents
Traversal of the Blood-Brain Barrier by Cleavable l -Lysine Conjugates of Apigenin
Wong, Tsung-Yun,Tsai, Ming-Shian,Hsu, Lih-Ching,Lin, Shu-Wha,Liang, Pi-Hui
, p. 8124 - 8131 (2018)
Apigenin, a flavone abundant in parsley and celery, is known to act on several CNS receptors, but its very poor water solubility (a temporary sedative effect on the mice within 5 min of intraperitoneal administration (single dose of 0.4 mg/g) and could be detected in the mice brain tissues at a concentration of 0.82 μg/g of intact Lys-apigenin carbamate 10 and 0.42 ug/g of apigenin at 1.5 h. This study accomplished the delivery of apigenin across the BBB in a manner that might be applicable to other congeners, which should inform the future development of BBB-crossing flavonoids.
CYCLIC TETRAMER COMPOUNDS AS PROPROTEIN CONVERTASE SUBTILISIN/KEXIN TYPE 9 (PCSK9) INHIBITORS FOR THE TREATMENT OF METABOLIC DISORDERS
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Paragraph 0866; 0870, (2020/06/16)
The disclosure relates to inhibitors of PCSK9 useful in the treatment of cholesterol lipid metabolism, and other diseases in which PCSK9 plays a role, having the Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, N-oxide, or tautomer thereof, wherein R1, R1, R1, R1, R1, R1, R1, R1, R1, X1, X2, and X3 are described herein.
Heterocyclic derivatives with immunomodulatory effects
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Paragraph 0175; 0176; 0178, (2018/03/24)
The invention relates to novel heterocyclic derivatives with immunomodulatory effects capable of inhibiting therapeutic agents in a programmed cell death (PD1) signal path. The compounds disclosed bythe invention are capable of enhancing antitumor activit