140700-64-7Relevant articles and documents
Discovery of novel triazolobenzazepinones as γ-secretase modulators with central Aβ42 lowering in rodents and rhesus monkeys
Fischer, Christian,Zultanski, Susan L.,Zhou, Hua,Methot, Joey L.,Shah, Sanjiv,Hayashi, Ikuo,Hughes, Bethany L.,Moxham, Christopher M.,Bays, Nathan W.,Smotrov, Nadya,Hill, Armetta D.,Pan, Bo-Sheng,Wu, Zhenhua,Moy, Lily Y.,Tanga, Flobert,Kenific, Candia,Cruz, Jonathan C.,Walker, Deborah,Bouthillette, Melanie,Nikov, George N.,Deshmukh, Sujal V.,Jeliazkova-Mecheva, Valentina V.,Diaz, Damaris,Michener, Maria S.,Cook, Jacquelynn J.,Munoz, Benito,Shearman, Mark S.
, p. 3488 - 3494 (2015/08/06)
Abstract Synthesis and SAR studies of novel triazolobenzazepinones as gamma secretase modulators (GSMs) are presented in this communication. Starting from our azepinone leads, optimization studies toward improving central lowering of Aβ42 led to the discovery of novel benzo-fused azepinones. Several benzazepinones were profiled in vivo and found to lower brain Aβ42 levels in Sprague Dawley rats and transgenic APP-YAC mice in a dose-dependent manner after a single oral dose. Compound 34 was further progressed into a pilot study in our cisterna-magna-ported rhesus monkey model, where we observed robust lowering of CSF Aβ42 levels.
HETEROCYCLIC AMIDES AS KINASE INHIBITORS
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Page/Page column 66, (2014/09/03)
Disclosed are compounds having the formula (I) wherein X, Y, Z1, Z2, Z3, Z4, R5, RA, m, A. L, and B are as defined herein, and methods of making and using the same.
A convergent asymmetric synthesis of a growth hormone secretagogue
Zheng, Nan,Armstrong III, Joseph D.,Eng, Kan K.,Keller, Jennifer,Liu, Tom,Purick, Robert,Lynch, Joseph,Hartner, Frederick W.,Volante
, p. 3435 - 3446 (2007/10/03)
Described herein is a convergent asymmetric synthesis of growth hormone secretagogue (GHS) suitable for large-scale preparations. Key features include: (1) an improved method for α-iodination of a lactam; (2) a novel synthesis of a disubstituted urea usin
Lactam inhibitors of factor Xa and method
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, (2008/06/13)
Lactam inhibitors are provided which have the structure including pharmaceutically acceptable salts thereof and all stereoisomers thereof, and prodrug esters thereof, wherein n is 1 to 5; and and R1, R2, R3, R4, R5 , R6, R7, R8, R9, R10, R10a, 1011 and R12 are as defined herein. These compounds are inhibitors of Factor Xa and thus are useful as anticoagulants. A method for treating cardiovascular diseases associated with thromboses is also provided.
Design, synthesis, and discovery of 3-piperazinyl-3,4-dihydro-2(1H)-quinolinone derivatives: A novel series of mixed dopamine D2/D4 receptor antagonists
Zhao, He,Thurkauf, Andrew,Braun, Julia,Brodbeck, Robin,Kieltyka, Andrzej
, p. 2119 - 2122 (2007/10/03)
3-Piperazinyl-3,4-dihydro-2(1H)-quinolinone derivatives (δ-lactams) were designed, synthesized, and identified as a new series of mixed dopamine D2/D4 receptor antagonists. To further the structure-activity relationship (SAR) study, 3-piperazinylindolin-2-ones (γ-lactams) and 3-piperazinyl-3H,4H,5H-benzo[f]azepin-2-ones (ε-lactams) were also prepared and examined. (C) 2000 Elsevier Science Ltd.
Napthoo-fused azepines as potent growth hormone secretagogues
Hansen, Thomas Kruse,Thogersen, Henning,Hansen, Birgit Sehested
, p. 2951 - 2954 (2007/10/03)
Computer guided improvements of known growth hormone secretagogues are reported. These are a new series of napthofused azepines. Structure-activity relationships are different than in the corresponding benzo-fused azepines.
Benzo-fused lactams promote release of growth hormone
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, (2008/06/13)
There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such benzo-fused lactams as the active ingredient therefore are also disclosed.
Benzo-fused lactams promote release of growth hormone
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, (2008/06/13)
There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. The compounds are prepared by substitution of an amino-lactam with a substituted amide function. Growth promoting compositions containing such bezno-fused lactams as the active ingredient thereof are also disclosed. STR1 where L is STR2
An Efficient Asymmetric Synthesis of (R)-3-Amino-2,3,4,5-tetrahydro-1H-benzazepin-2-one
Armstrong, Joseph D. III,Eng, Kan K.,Keller, Jennifer L.,Purick, Robert M.,Hartner, Frederick W. Jr.,et al.
, p. 3239 - 3242 (2007/10/02)
Two approaches for the asymmetric preparation of (-)- or (+)-α-aminobenzlactam 1 are described.One route is based on the asymmetric hydrogenation of enamide 5 and the other on the racemization/resolution of (+/-)-1.
Benzo-fused lactams promote release of growth hormone
-
, (2008/06/13)
There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. The compounds are prepared by substitution of an amino-lactam with a substituted amide function. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed. STR1 Where L is STR2