124880-31-5Relevant academic research and scientific papers
JAK Inhibitor with high oral bioavailability
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Paragraph 0081-0084, (2021/11/06)
The JAK inhibitor has high oral bioavailability, and is characterized in that the JAK inhibitor comprises a compound of the formula I, or a stereoisomer thereof. A geometric isomer, a tautomer, a hydrate, a solvate, and a pharmaceutically acceptable salt
Pharmaceutical compound used as JAK kinase inhibitor
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Paragraph 0056-0059, (2020/12/05)
The invention provides a pharmaceutical compound. The pharmaceutical compound is a compound shown in the following structural formula or a stereoisomer, a geometrical isomer, a tautomer, a racemate, ahydrate, a solvate, a metabolite and a pharmaceutically acceptable salt or prodrug thereof shown in the specification, wherein R represents 1 to 3 substituents on a benzene ring, and each of the 1 to3 substituents is independently selected from halogen or cyano. The pharmaceutical compound provided by the invention can inhibit JAK kinase, and more particularly can be used as a JAK1/Tyk2 dual inhibitor and a Tyk2 specific inhibitor. More specifically, the pharmaceutical compound provided by the invention can be used for preventing or treating autoimmune diseases such as rheumatoid arthritis,ankylosing spondylitis, ulcerative colitis, systemic lupus erythematosus, type I diabetes, sicca syndrome, vasculitis, alopecia areata, psoriasis, leucoderma and the like, or other inflammatory skin diseases such as atopic dermatitis, eczema, acne and hidradenitis suppurativa.
Synthesis and Biological Activity of trans-(+/-)-N-Methyl-2-(3-pirydyl)-2-tetrahydrothiopyrancarbothioamide 1-Oxide (RP 49356) and Analogues: A New Class of Potassium Channel Opener
Brown, Thomas J.,Chapman, Robert F.,Cook, David C.,Hart, Terance W.,McLay, Iain M.,et al.
, p. 3613 - 3624 (2007/10/02)
The synthesis and biological activity of trans-(+/-)-N-methyl-2-(3-pyridyl)-2-tetrahydrothiopyrancarbothioamide 1-oxide (8a, RP 49356) and analoques is reported.These compounds constitute a new structural class of K+-channel opener.The effects of changes in the pyridyl group, thioamide, and thiane ring on in vitro K+-channel opening activity are discussed.A 3-pyridyl or 3-quinolyl group, a small N-alkyl thioamide function, and a thiane oxide ring, in which the sulfoxide is in a trans relationship to thioamide, are preferred for activity.Selected compounds were tested intravenously in the normotensive anaesthetized rat for hypotensive effects, and the activities reflect their in vitro K+-channel opening activity.This led to further evaluation of compound 8a and the selection of the (-)-enantiomer 8b (RP 52891) for development as an antihypertensive and antianginal agent.
