- IMIDAZOPYRIDAZINE DERIVATIVES AS MODULATORS OF THE GABAA RECEPTOR ACTIVITY.
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The present invention relates to imidazopyridazine derivatives. More particularly, it relates to 4-(biphenyl-3-yl)-7H-imidazo[4,5-c]pyridazine derivatives of formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R and R6 are as defined in the description. The imidazopyridazine derivatives of the present invention modulate the activity of the GABAA receptor. They are useful in the treatment of a number of conditions, including pain.
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Page/Page column 73-74
(2016/01/01)
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- Dihydroxylphenyl amides as inhibitors of the Hsp90 molecular chaperone
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Information from X-ray crystal structures were used to optimize the potency of a HTS hit in a Hsp90 competitive binding assay. A class of novel and potent small molecule Hsp90 inhibitors were thereby identified. Enantio-pure compounds 31 and 33 were potent in PGA-based competitive binding assay and inhibited proliferation of various human cancer cell lines in vitro, with IC50 values averaging 20 nM.
- Kung, Pei-Pei,Funk, Lee,Meng, Jerry,Collins, Michael,Zhou, Joe Zhongxiang,Catherine Johnson,Ekker, Anne,Wang, Jeff,Mehta, Pramod,Yin, Min-Jean,Rodgers, Caroline,Davies II, Jay F.,Bayman, Eileen,Smeal, Tod,Maegley, Karen A.,Gehring, Michael R.
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supporting information; experimental part
p. 6273 - 6278
(2009/08/15)
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- AMIDE RESORCINOL COMPOUNDS
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The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts and solvates thereof, their synthesis, and their use as HSP-90 inhibitors.
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Page/Page column 41; 115
(2008/06/13)
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