1174512-81-2Relevant academic research and scientific papers
Fused tricyclic indoles as S1P1 agonists with robust efficacy in animal models of autoimmune disease
Buzard, Daniel J.,Han, Sangdon,Lopez, Luis,Kawasaki, Andrew,Moody, Jeanne,Thoresen, Lars,Ullman, Brett,Lehmann, Juerg,Calderon, Imelda,Zhu, Xiuwen,Gharbaoui, Tawfik,Sengupta, Dipanjan,Krishnan, Ashwin,Gao, Yinghong,Edwards, Jeff,Barden, Jeremy,Morgan, Michael,Usmani, Khawja,Chen, Chuan,Sadeque, Abu,Thatte, Jayant,Solomon, Michelle,Fu, Lixia,Whelan, Kevin,Liu, Ling,Al-Shamma, Hussien,Gatlin, Joel,Le, Minh,Xing, Charles,Espinola, Sheryll,Jones, Robert M.
, p. 4404 - 4409 (2012)
Two series of fused tricyclic indoles were identified as potent and selective S1P1 agonists. In vivo these agonists produced a significant reduction in circulating lymphocytes which translated into robust efficacy in several rodent models of autoimmune disease. Importantly, these agonists were devoid of any activity at the S1P3 receptor in vitro, and correspondingly did not produce S1P3 mediated bradycardia in telemeterized rat.
DIHYDRO- 1H- PYRROLO [1,2-A] INDOL-1-YL CARBOXYLIC DERIVATIVES WHICH ACT AS S1P1 AGONISTS
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Page/Page column 78, (2009/09/05)
The present invention relates to certain (1,2,4-oxadiazol-3-yl)-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl carboxylic 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 associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, sepsis, myocardial infarction, ischemic stroke, acne, microbial infections or diseases and viral infections or diseases.
