36155-78-9Relevant academic research and scientific papers
New pyrazolyl and thienyl aminohydantoins as potent BACE1 inhibitors: Exploring the S2′ region
Malamas, Michael S.,Erdei, Jim,Gunawan, Iwan,Barnes, Keith,Hui, Yu,Johnson, Matthew,Robichaud, Albert,Zhou, Ping,Yan, Yinfa,Solvibile, William,Turner, Jim,Fan, Kristi Yi,Chopra, Rajiv,Bard, Jonathan,Pangalos, Menelas N.
scheme or table, p. 5164 - 5170 (2011/10/09)
The proteolytic enzyme β-secretase (BACE1) plays a central role in the synthesis of the pathogenic β-amyloid in Alzheimer's disease. SAR studies of the S2′ region of the BACE1 ligand binding pocket with pyrazolyl and thienyl P2′ side chains are reported. These analogs exhibit low nanomolar potency for BACE1, and demonstrate >50- to 100-fold selectivity for the structurally related aspartyl proteases BACE2 and cathepsin D. Small groups attached at the nitrogen of the P2′ pyrazolyl moiety, together with the P3 pyrimidine nucleus projecting into the S3 region of the binding pocket, are critical components to ligand's potency and selectivity. P2′ thiophene side chain analogs are highly potent BACE1 inhibitors with excellent selectivity against cathepsin D, but only modest selectivity against BACE2. The cell-based activity of these new analogs tracked well with their increased molecular binding with EC50 values of 0.07-0.2 μM in the ELISA assay for the most potent analogs.
Amino-5-(5-membered)hetero-arylimidazolone compounds and the use thereof for beta-secretase modulation
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Page/Page column 39-40, (2008/06/13)
The present invention provides a 2-amino-5-heteroaryl-5-phenylimidazolone compound of formula I The present invention also provides methods for the use thereof to inhibit β-secretase (BACE) and treat β-amyloid deposits and neurofibrillary tangles
Vitamin D analogues
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Page column 25, (2010/02/09)
The present invention relates to novel triaromatic compounds having the general formula (I): as well as to a method for preparing them and to their use in pharmaceutical compositions intended for use in human or veterinary medicine (in dermatology, in car
Vitamin D analogues
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Page column 22, (2010/02/05)
The invention relates to novel bicyclic compounds having the general formula (I): as well as to a method for preparing them and to their use in pharmaceutical compositions intended for use in human or veterinary medicine (in dermatology, in carcinology and in the field of autoimmune diseases and that of organ or tissue transplants in particular), or alternatively in cosmetic compositions.
An efficient enantioselective synthesis of the D1 agonist (5aR,11bS)-4,5,5a,6,7,11b-hexahydro-2-propyl-3-thia-5-azacyclopenta[c] phenanthrene-9,10-diol (A-86929)
Ehrlich, Paul P.,Ralston, Jeffrey W.,Michaelides, Michael R.
, p. 2782 - 2785 (2007/10/03)
(5aR,11bS)-4,5,5a,6,7,11b-Hexahydro-2-propyl-3-thia-5-azacyclopenta[c] phenanthrene-9,10-diol (A86929, 1), a potent selective dopamine D1 agonist, was synthesized enantioselectively from D-aspartic acid. Key features of the 10-step synthesis are the follo
PROCESS FOR PREPARING CHIRAL TETRACYCLIC DOPAMINERGIC COMPOUNDS
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, (2008/06/13)
A process for preparing a chiral tetracyclic compound of formula: STR1 wherein R is hydrogen or a C 1-C 6-alkyl group and Z is oxygen, sulfur or--CH=CH--, the compounds having uses as dopamine agonists. The process involves reacting a chiral starting mate
