695215-93-1Relevant articles and documents
COMPOUNDS FOR THE TREATMENT OF ALZHEIMER'S DISEASE
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Page/Page column 63, (2010/06/19)
The invention relates to substituted 1,2-ethylenediamines of general formula (I), wherein the radicals R1-R13, A, B, L and i are as defined in the description and the claims. The invention also relates to the use thereof for treating Alzheimer's disease (AD) and similar diseases.
COMPOUNDS FOR THE TREATMENT OF ALZHEIMER'S DISEASE
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Page/Page column 46, (2010/07/08)
The invention relates to substituted 1,2-ethylenediamines of general formula (I), wherein the radicals R1-R13, A, B, L and i are as defined in the description and in the claims. The invention also relates to the use thereof for treat
ASPARTYL PROTEASE INHIBITORS
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, (2009/01/20)
The invention provides compounds of the formula (I) N-oxides, addition salts, quaternary amines, metal complexes, stereochemically isomeric forms and metabolites thereof, wherein G is-O-, -S(=O)r-, -CRdRd or -NRa-; W is H, C1-C6
Design, synthesis, and X-ray structure of potent memapsin 2 (β-secretase) inhibitors with isophthalamide derivatives as the P 2 P3-ligands
Ghosh, Arun K.,Kumaragurubaran, Nagaswamy,Hong, Lin,Kulkarni, Sarang S.,Xu, Xiaoming,Chang, Wanpin,Weerasena, Vajira,Turner, Robert,Koelsch, Gerald,Bilcer, Geoffrey,Tang, Jordan
, p. 2399 - 2407 (2008/02/06)
Structure-based design and synthesis of a number of potent and selective memapsin 2 inhibitors are described. These inhibitors were designed based upon the X-ray structure of memapsin 2-bound inhibitor 3 that incorporates methylsulfonyl alanine as the Ps
β SECRETASE INHIBITOR
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Page/Page column 32, (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.]
Phenylamide and pyridylamide beta-secretase inhibitors for the treatment of alzheimer's disease
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Page/Page column 27, (2008/06/13)
The present invention is directed to phenylamide and pyridylamide derivative compounds of which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
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 (2007/10/03)
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
Substituted 1,2-ethylenediamines, Methods for Preparing Them and Uses Thereof
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Page/Page column 132-133; 141-142, (2010/11/24)
The present invention relates to substituted 1,2-ethylenediamines of general formula (I) wherein the groups R1 to R15, A, B, L, i as well as X1-X4 are defined as in the specification and claims and the use thereof for the treatment of Alzheimer's disease (AD) and similar diseases.
COMPOUNDS WHICH INHIBIT BETA-SECRETASE ACTIVITY AND METHODS OF USE THEREOF
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Page/Page column 51-52, (2008/06/13)
The present invention provides novel beta-secretase inhibitors of the general formula (I), where the variables A1, A2, L1, L2, L3, R1, R2, R3, R4, R5, R6 and R7 are as defined in the claims, a method for their use in treating Alzheimer's disease, and methods for their use in reducing memapsin 2 catalytic activity.
PYRROLIDIN-3-YL COMPOUNDS USEFUL AS BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE
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Page/Page column 33, (2010/02/15)
The present invention is directed to pyrrolidin-3-yl derivative compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The i