695215-92-0Relevant articles and documents
Cyanobacterial peptides as a prototype for the design of potent β-secretase inhibitors and the development of selective chemical probes for other aspartic proteases
Liu, Yanxia,Zhang, Wei,Li, Li,Salvador, Lilibeth A.,Chen, Tiantian,Chen, Wuyan,Felsenstein, Kevin M.,Ladd, Thomas B.,Price, Ashleigh R.,Golde, Todd E.,He, Jianhua,Xu, Yechun,Li, Yingxia,Luesch, Hendrik
, p. 10749 - 10765 (2013/02/23)
Inspired by marine cyanobacterial natural products, we synthesized modified peptides with a central statine-core unit, characteristic for aspartic protease inhibition. A series of tasiamide B analogues inhibited BACE1, a therapeutic target in Alzheimer's
COMPOUNDS FOR THE TREATMENT OF ALZHEIMER'S DISEASE
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Page/Page column 66, (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
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 33-34, (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.]
Substituted 1,2-ethylenediamines, Methods for Preparing Them and Uses Thereof
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Page/Page column 133; 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.
BENZYLETHER AND BENZYLAMINO BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE
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Page/Page column 24, (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 of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed t
Structure-based design of potent and selective cell-permeable inhibitors of human β-secretase (BACE-1)
Stachel, Shawn J.,Coburn, Craig A.,Steele, Thomas G.,Jones, Kristen G.,Loutzenhiser, Elizabeth F.,Gregro, Alison R.,Rajapakse, Hemaka A.,Lai, Ming-Tain,Crouthamel, Ming-Chih,Xu, Min,Tugusheva, Katherine,Lineberger, Janet E.,Pietrak, Beth L.,Espeseth, Amy S.,Shi, Xiao-Ping,Chen-Dodson, Elizabeth,Holloway, M. Katharine,Munshi, Sanjeev,Simon, Adam J.,Kuo, Lawrence,Vacca, Joseph P.
, p. 6447 - 6450 (2007/10/03)
We describe the development of cell-permeable β-secretase inhibitors that demonstratively inhibit the production of the secreted amino terminal fragment of an artificial amyloid precursor protein in cell culture. In addition to potent inhibition in a cell
PHENYLCARBOXAMIDE BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE
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Page 21, (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