695216-60-5Relevant academic research and scientific papers
Conformationally biased P3 amide replacements of β-secretase inhibitors
Stachel, Shawn J.,Coburn, Craig A.,Steele, Thomas G.,Crouthamel, Min-Chi,Pietrak, Beth L.,Lai, Ming-Tain,Holloway, M. Katharine,Munshi, Sanjeev K.,Graham, Samuel L.,Vacca, Joseph P.
, p. 641 - 644 (2006)
We have synthesized and evaluated a series of conformationally biased P3 amide replacements based on an isophthalamide lead structure. The studies resulted in the identification of the β-secretase inhibitor 7m which has an in vitro IC50 = 35 nM
β SECRETASE INHIBITOR
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Page/Page column 46-47, (2008/06/13)
Disclosed is a compound represented by the formula (1) below which is useful as a drug for treating Alzheimer's disease, or a pharmaceutically acceptable salt thereof. (1) [In the formula, R1 represents a group represented by the following formula (2): (2) (wherein X represents a nitrogen atom or a group expressed as C(R5); Y represents a nitrogen atom or a group expressed as C(R6); and R5 and R6 independently represent a hydrogen atom or the like) or the like; m represents an integer of 1-6; L1 represents a single bond or the like; R2 represents a hydrogen atom, a substituted or unsubstituted alkyl group or the like; R3 represents a hydrogen atom or the like; L2 represents a single bond or the like; and R4 represents a hydrogen atom, a substituted or unsubstituted aryl group or the like.]
PHENYLCARBOXAMIDE BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE
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Page 53, (2008/06/13)
The present invention is directed to compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment or prevention of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is a
