41014-27-1Relevant articles and documents
COMPOUND FOR INHIBITING PGE2/EP4 SIGNALING TRANSDUCTION INHIBITING, PREPARATION METHOD THEREFOR, AND MEDICAL USES THEREOF
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Paragraph 0214; 0218-0219, (2022/03/14)
A compound of formula (I), a preparation method therefor, a pharmaceutical composition containing a derivative thereof, and the therapeutic uses thereof, especially inhibiting PGE2/EP4 signalling transduction and the uses thereof for treating cancer, acute or chronic pain, migraine, osteoarthritis, rheumatoid arthritis, gout, bursitis, ankylosing spondylitis, primary dysmenorrhea, tumour or arteriosclerosis.
Immunomodulator
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, (2021/02/10)
The invention discloses an immunomodulator, and particularly relates to a compound shown as a formula I, or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof. Experiments prove that the compound has good IL-17A inhibitory activity, can be used for preparing an IL-17A inhibitor and drugs for preventing and/or treating IL-17A mediated diseases (such as inflammation, autoimmune diseases, infectious diseases, cancers and precancerous syndromes), and provides a new medical possibility for clinical treatment of diseases related to abnormal IL-17A activity.
Synthesis and Insecticidal Activity of Spinosyns with C9- O -Benzyl Bioisosteres in Place of the 2′,3′,4′-Tri- O -methyl Rhamnose
Oliver, M. Paige,Crouse, Gary D.,Demeter, David A.,Sparks, Thomas C.
, p. 5571 - 5577 (2015/06/25)
The spinosyns are fermentation-derived natural products active against a wide range of insect pests. They are structurally complex, consisting of two sugars (forosamine and rhamnose) coupled to a macrocyclic tetracycle. Removal of the rhamnose sugar results in a >100-fold reduction in insecticidal activity. C9-O-benzyl analogues of spinosyn D were synthesized to determine if the 2′,3′,4′-tri-O-methyl rhamnose moiety could be replaced with a simpler, synthetic bioisostere. Insecticidal activity was evaluated against larvae of Spodoptera exigua (beet armyworm) and Helicoverpa zea (corn earworm). Whereas most analogues were far less active than spinosyn D, a few of the C9-O-benzyl analogues, such as 4-CN, 4-Cl, 2-isopropyl, and 3,5-diOMe, were within 3-15 times the activity of spinosyn D for larvae of S. exigua and H. zea. Thus, although not yet quite as effective, synthetic bioisosteres can substitute for the naturally occurring 2′,3′,4′-tri-O-methyl rhamnose moiety.