- Ruthenium-Catalyzed Decarboxylative C-H Alkenylation in Aqueous Media: Synthesis of Tetrahydropyridoindoles
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We disclose herein a Ru(II)-catalyzed decarboxylative and oxidative coupling of N-substituted indolyl carboxylic acids with broad substrate scope in an aqueous solution. This method provides a sustainable and efficient access to synthesize various indole-fused cyclohexanyl acetic acids under mild conditions.
- Jin, Xiao-Yang,Xie, Li-Jun,Cheng, Hou-Ping,Liu, An-Di,Li, Xue-Dong,Wang, Dong,Cheng, Liang,Liu, Li
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- Design and synthesis of new tricyclic indoles as potent modulators of the S1P1 receptor
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Modulators of S1P1 have proven utility for the treatment of autoimmune disease and efforts to identify new agents with improved safety and pharmacokinetic parameters are ongoing. Several new S1P1 chemotypes were designed and optimize
- Buzard, Daniel J.,Schrader, Thomas O.,Zhu, Xiuwen,Lehmann, Juerg,Johnson, Ben,Kasem, Michelle,Kim, Sun Hee,Kawasaki, Andrew,Lopez, Luis,Moody, Jeanne,Han, Sangdon,Gao, Yinghong,Edwards, Jeff,Barden, Jeremy,Thatte, Jayant,Gatlin, Joel,Jones, Robert M.
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p. 659 - 663
(2015/01/30)
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- SUBSTITUTED TRICYCLIC ACID DERIVATIVES AS S1P1 RECEPTOR AGONISTS USEFUL IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISORDERS
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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.
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