1174512-52-7Relevant 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.
scheme or table, p. 4404 - 4409 (2012/07/17)
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.
DISUBSTITUTED OXADIAZOLE DERIVATIVES USEFUL IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISORDERS
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Page/Page column 50-51, (2011/02/24)
The present invention relates to certain disubstituted oxadiazole derivatives of Formula (Ia) and pharmaceutically acceptable salts, solvates, and hydrates 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.
DIHYDRO- 1H- PYRROLO [1,2-A] INDOL-1-YL CARBOXYLIC DERIVATIVES WHICH ACT AS S1P1 AGONISTS
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Page/Page column 81, (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.
