184906-29-4Relevant academic research and scientific papers
SUBSTITUTED BICYCLIC COMPOUNDS
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Page/Page column 169; 170, (2016/03/13)
Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V) and/or a salt thereof, wherein R1 is OH or OP(O)(OH)2, and X1, X2, X3, R2, R2a, Ra, Rb, and Rc are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
NEW COMPOUNDS
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Page/Page column 32-33, (2010/07/10)
The present invention encompasses compounds of general formula (1) wherein A, B, X, R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and t
Design, synthesis, and in vitro evaluation of cyclic nitrones as free radical traps for the treatment of stroke
Fevig, Thomas L.,Bowen, S. Marc,Janowick, David A.,Jones, Bryan K.,Munson, H. Randall,Ohlweiler, David F.,Thomas, Craig E.
, p. 4988 - 4996 (2007/10/03)
Analogs of the cyclic nitrone free radical trap 1 (3,3-dimethyl-3,4- dihydroisoquinoline N-oxide, a cyclic analog of phenyl-tert-butylnitrone (PBN)) were prepared in which (1) the fused phenyl ring was replaced with a naphthalene ring, an electron rich heterocycle, or a dimethylphenol, (2) the nitrone-containing ring comprised five, six, or seven atoms, and (3) the gem- dimethyl group was replaced with spirocyclic groups. The most active antioxidant, which bears a dimethylphenol fused to a 7-membered ring nitrone (compound 6h), inhibited lipid peroxidation in vitro with an IC50 of 22 μM, a 75-fold improvement over that of 1. The previously observed correlation between lipophilicity and activity vs lipid peroxidation in vitro has been further substantiated and refined by this study. Moreover, certain classes of compounds (namely, dimethylphenols 6g, h and furan 6j) have now been found which are considerably more active in vitro than expected on the basis of their log k'(w) values.
