3418-69-7Relevant articles and documents
(7-Benzyloxy-2,3-dihydro- 1H -pyrrolo[1,2-a]indol-1-yl)acetic acids as S1P1 functional antagonists
Buzard, Daniel J.,Lopez, Luis,Moody, Jeanne,Kawasaki, Andrew,Schrader, Thomas O.,Kasem, Michelle,Johnson, Ben,Zhu, Xiuwen,Thoresen, Lars,Kim, Sun Hee,Gharbaoui, Tawfik,Sengupta, Dipanjan,Calvano, Lorene,Krishnan, Ashwin,Gao, Yinghong,Semple, Graeme,Edwards, Jeff,Barden, Jeremy,Morgan, Michael,Usmani, Khawja,Chen, Chuan,Sadeque, Abu,Chen, Weichao,Christopher, Ronald J.,Thatte, Jayant,Fu, Lixia,Solomon, Michelle,Whelan, Kevin,Al-Shamma, Hussien,Gatlin, Joel,Gaidarov, Ibragim,Anthony, Todd,Le, Minh,Unett, David J.,Stirn, Scott,Blackburn, Anthony,Behan, Dominic P.,Jones, Robert M.
, p. 1334 - 1339 (2015/02/02)
S1P1 is a validated target for treatment of autoimmune disease, and functional antagonists with superior safety and pharmacokinetic properties are being sought as second generation therapeutics. We describe the discovery and optimization of (7-benzyloxy-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic acids as potent, centrally available, direct acting S1P1 functional antagonists, with favorable pharmacokinetic and safety properties.
SUBSTITUTED TRICYCLIC ACID DERIVATIVES AS S1P1 RECEPTOR AGONISTS USEFUL IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISORDERS
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Page/Page column 32, (2011/07/08)
The present invention relates to certain substituted tricyclic acid derivatives of Formula (I) 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-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, myocardial ischemia-reperfusion injury, hypertensive nephropathy, glomerulosclerosis, gastritis, polymyositis, thyroiditis, vitiligo, hepatitis, biliary cirrhosis, microbial infections and associated diseases, viral infections and associated diseases, diseases and disorders mediated by lymphocytes, auto immune diseases, inflammatory diseases, and cancer.