695215-94-2Relevant 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
supporting information, 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
Design and synthesis of potent macrocyclic renin inhibitors
Sund, Christian,Belda, Oscar,Wiktelius, Daniel,Sahlberg, Christer,Vrang, Lotta,Sedig, Susanne,Hamelink, Elizabeth,Henderson, Ian,Agback, Tatiana,Jansson, Katarina,Borkakoti, Neera,Derbyshire, Dean,Eneroth, Anders,Samuelsson, Bertil
scheme or table, p. 358 - 362 (2011/02/27)
Two types of P1-P3-linked macrocyclic renin inhibitors containing the hydroxyethylene isostere (HE) scaffold just outside the macrocyclic ring have been synthesized. An aromatic or aliphatic substituent (P3sp) was introduced in the macrocyclic ring aiming
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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Page/Page column 52, (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
β SECRETASE INHIBITOR
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Page/Page column 32-33, (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.]
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
Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors
Lindsley, Stacey R.,Moore, Keith P.,Rajapakse, Hemaka A.,Selnick, Harold G.,Young, Mary Beth,Zhu, Hong,Munshi, Sanjeev,Kuo, Lawrence,McGaughey, Georgia B.,Colussi, Dennis,Crouthamel, Ming-Chih,Lai, Ming-Tain,Pietrak, Beth,Price, Eric A.,Sankaranarayanan, Sethu,Simon, Adam J.,Seabrook, Guy R.,Hazuda, Daria J.,Pudvah, Nicole T.,Hochman, Jerome H.,Graham, Samuel L.,Vacca, Joseph P.,Nantermet, Philippe G.
, p. 4057 - 4061 (2008/02/10)
This Letter describes the design and synthesis of tertiary carbinamine macrocyclic inhibitors of the β-secretase (BACE-1) enzyme. These macrocyclic inhibitors, some of which incorporate novel P2 substituents, display a 2- to 100-fold increase in potency r
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.
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.