1206123-37-6Relevant articles and documents
Compound for treating ulcerative colitis as well as preparation method and application thereof
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Paragraph 0049; 0051; 0056; 0075-0076, (2021/05/19)
The invention provides a compound for treating ulcerative colitis. The compound has a structure as shown in a formula I. The compound provided by the invention can significantly inhibit abnormal secretion of TNF-alpha, IL-1[beta], IL-6 and other proinflammatory factors in colon tissues when colitis happens, inhibit inflammatory cell infiltration, maintain the integrity of intestinal epithelium and crypt gland, effectively relieve inflammation, and improve the symptoms of colon shortening and intestinal wall thickening, has excellent potential application value in preparation of medicines for treating ulcerative colitis, and provides a new choice for clinic.
Discovery of APD334: Design of a clinical stage functional antagonist of the sphingosine-1-phosphate-1 receptor
Buzard, Daniel J.,Kim, Sun Hee,Lopez, Luis,Kawasaki, Andrew,Zhu, Xiuwen,Moody, Jeanne,Thoresen, Lars,Calderon, Imelda,Ullman, Brett,Han, Sangdon,Lehmann, Juerg,Gharbaoui, Tawfik,Sengupta, Dipanjan,Calvano, Lorene,Montalban, Antonio Garrido,Ma, You-An,Sage, Carleton,Gao, Yinghong,Semple, Graeme,Edwards, Jeff,Barden, Jeremy,Morgan, Michael,Chen, Weichao,Usmani, Khawja,Chen, Chuan,Sadeque, Abu,Christopher, Ronald J.,Thatte, Jayant,Fu, Lixia,Solomon, Michelle,Mills, David,Whelan, Kevin,Al-Shamma, Hussien,Gatlin, Joel,Le, Minh,Gaidarov, Ibragim,Anthony, Todd,Unett, David J.,Blackburn, Anthony,Rueter, Jaimie,Stirn, Scott,Behan, Dominic P.,Jones, Robert M.
, p. 1313 - 1317 (2015/01/09)
APD334 was discovered as part of our internal effort to identify potent, centrally available, functional antagonists of the S1P1 receptor for use as next generation therapeutics for treating multiple sclerosis (MS) and other autoimmune diseases
SUBSTITUTED 1,2,3,4- TETRAHYDROCYCLOPENTA[b]INDOL-3-YL) ACETIC ACID DERIVATIVES USEFUL IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISORDERS
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Page/Page column 57, (2010/04/03)
The present invention relates to certain substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1 receptor-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, microbial infections or diseases and viral infections or diseases.