301225-52-5Relevant academic research and scientific papers
LINEAR GLYCOSIDASE INHIBITORS
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Page/Page column 92, (2019/03/14)
Compounds of formula (I) wherein A, R, W, Q, L, n and m have the meaning according to the claims can be employed, inter alia, for the treatment of tauopathies and Alzheimer's disease.
Two analogues of fenarimol show curative activity in an experimental model of chagas disease
Keenan, Martine,Chaplin, Jason H.,Alexander, Paul W.,Abbott, Michael J.,Best, Wayne M.,Khong, Andrea,Botero, Adriana,Perez, Catherine,Cornwall, Scott,Thompson, R. Andrew,White, Karen L.,Shackleford, David M.,Koltun, Maria,Chiu, Francis C. K.,Morizzi, Julia,Ryan, Eileen,Campbell, Michael,Von Geldern, Thomas W.,Scandale, Ivan,Chatelain, Eric,Charman, Susan A.
, p. 10158 - 10170 (2014/01/17)
Chagas disease, caused by the protozoan parasite Trypanosoma cruzi (T. cruzi), is an increasing threat to global health. Available medicines were introduced over 40 years ago, have undesirable side effects, and give equivocal results of cure in the chronic stage of the disease. We report the development of two compounds, 6 and (S)-7, with PCR-confirmed curative activity in a mouse model of established T. cruzi infection after once daily oral dosing for 20 days at 20 mg/kg 6 and 10 mg/kg (S)-7. Compounds 6 and (S)-7 have potent in vitro activity, are noncytotoxic, show no adverse effects in vivo following repeat dosing, are prepared by a short synthetic route, and have druglike properties suitable for preclinical development.
1,3,4 Trisubstituted pyrrolidine CCR5 receptor antagonists bearing 4-aminoheterocycle substituted piperidine side chains
Willoughby, Christopher A.,Rosauer, Keith G.,Hale, Jeffery J.,Budhu, Richard J.,Mills, Sander G.,Chapman, Kevin T.,MacCoss, Malcolm,Malkowitz, Lorraine,Springer, Martin S.,Gould, Sandra L.,DeMartino, Julie A.,Siciliano, Salvatore J.,Cascieri, Margaret A.,Carella, Anthony,Carver, Gwen,Holmes, Karen,Schleif, William A.,Danzeisen, Renee,Hazuda, Daria,Kessler, Joseph,Lineberger, Janet,Miller, Michael,Emini, Emilio A.
, p. 427 - 431 (2007/10/03)
A new class of 4-(aminoheterocycle)piperidine derived 1,3,4 trisubstituted pyrrolidine CCR5 antagonists is reported. Compound 4a is shown to have good binding affinity (1.8 nM) and antiviral activity in PBMC's (IC95=50 nM). Compound 4a also has improved PK properties relative to 1.
PYRROLIDINE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY
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, (2008/06/13)
The present invention is directed to pyrrolidine compounds of the formula I: (wherein R 1, R 2, R 3, R 4, R 5, R 6 and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.
