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1.发明公开CYCLOBUTYL SULFONES AS NOTCH SPARING GAMMA SECRETASE INHIBITORS 有权CYCLOBUTYL SULFONES作为NOTCH SPARING GAMMA SECRETASE抑制剂
公开(公告)号：EP2273877A1
公开(公告)日：2011-01-19
申请号：EP09734395.8
申请日：2009-04-17
发明人： HEIDEBRECHT, Richard, W. , LI, Chaomin , MUNOZ, Benito , ROSENAU, Andrew , SURDI, Laura, M. , TEMPEST, Paul , SILIPHAIVANH, Phieng , BRUBAKER, Jason
CPC分类号： C07C317/30 , C07C2601/04 , C07D309/12
摘要： The invention encompasses a novel class of cyclobutyl sulfone derivatives which inhibit the processing of APP by the putative γ-secretase while sparing Notch signaling pathway, and thus are useful in the treatment or prevention of Alzheimer's disease without the development of Notch inhibition mediated gastrointestinal issues. Pharmaceutical compositions and methods of use are also included.
摘要翻译： 本发明包括一类新的环丁基砜衍生物，其抑制由推定的γ-分泌酶加工APP而同时保留Notch信号传导途径，因此可用于治疗或预防阿尔茨海默氏病而不发展Notch抑制介导的胃肠问题。 药物组合物和使用方法也包括在内。
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2.发明授权CYCLOBUTYL SULFONES AS NOTCH SPARING GAMMA SECRETASE INHIBITORS 有权CYCLOBUTYL SULFONES作为NOTCH SPARING GAMMA SECRETASE抑制剂
公开(公告)号：EP2273877B1
公开(公告)日：2014-04-16
申请号：EP09734395.8
申请日：2009-04-17
发明人： HEIDEBRECHT, Richard, W. , LI, Chaomin , MUNOZ, Benito , ROSENAU, Andrew , SURDI, Laura, M. , TEMPEST, Paul , SILIPHAIVANH, Phieng , BRUBAKER, Jason
CPC分类号： C07C317/30 , C07C2601/04 , C07D309/12
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公开(公告)号：EP2378879A1
公开(公告)日：2011-10-26
申请号：EP09833803.1
申请日：2009-12-07
发明人： FISCHER, Christian , METHOT, Joey , ZHOU, Hua , SCHELL, Adam, J. , MUNOZ, Benito , RIVKIN, Alexey, A. , AHEARN, Sean, P. , CHICHETTI, Stephanie , MACCOSS, Rachel, N. , KATTAR, Sam, D. , CHRISTOPHER, Matthew , LI, Chaomin , ROSENAU, Andrew , BROWN, William Colby
CPC分类号： A61K31/41 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： According to the invention there is provided a compound of formula I or a pharmaceutically acceptable salt or hydrate thereof; wherein the variables are as defined herein. The compounds selectively attenuate the production of Aß42 and hence are useful in treatment of Alzheimer's disease and related conditions.
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