153993-80-7Relevant academic research and scientific papers
PYRAZINE DERIVATIVES
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Page/Page column 66, (2011/08/08)
The invention concerns pyrazine derivatives of the Formula (I) or pharmaceutically-acceptable salts thereof; wherein each of n, m and R has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of bone-related disorders or conditions
Design of peptide hydroxamate-based photoreactive activity-based probes of zinc-dependent metalloproteases
Geurink, Paul P.,Klein, Theo,Prely, Laurette,Paal, Krisztina,Leeuwenburgh, Michiel A.,Van Der Marel, Gijs A.,Kauffman, Henk F.,Overkleeft, Herman S.,Bischoff, Rainer
experimental part, p. 2100 - 2112 (2010/08/19)
Metalloproteases (ADAMs, MMPs) are multidomain proteins that play key roles in extracellular matrix remodelling and degradation, in cell-cell and cell-matrix interactions and in the proteolytic liberation of membrane-anchored proforms of cytokines and gro
Design and preparation of potent, nonpeptidic, bioavailable renin inhibitors
Bezen?on, Olivier,Bur, Daniel,Weller, Thomas,Richard-Bildstein, Sylvia,Remeň, Lubo?,Sifferlen, Thierry,Corminboeuf, Olivier,Grisostomi, Corinna,Boss, Christoph,Prade, Lars,Delahaye, Stéphane,Treiber, Alexander,Strickner, Panja,Binkert, Christoph,Hess, Patrick,Steiner, Beat,Fischli, Walter
supporting information; experimental part, p. 3689 - 3702 (2010/04/02)
Starting from known piperidine renin inhibitors, a new series of 3,9-diazabicyclo[3.3.1]nonene derivatives was rationally designed and prepared. Optimization of the positions 3, 6, and 7 of the diazabicyclonene template led to potent renin inhibitors. The substituents attached at the positions 6 and 7 were essential for the binding affinity of these compounds for renin. The introduction of a substituent attached at the position 3 did not modify the binding affinity but allowed the modulation of the ADME properties. Our efforts led to the discovery of compound (+)-26g that inhibits renin with an IC 50 of 0.20 nM in buffer and 19 nM in plasma. The pharmacokinetics properties of this and other similar compounds are discussed. Compound (+)-26g is well absorbed in rats and efficacious at 10 mg/kg in vivo.
Novel Piperidine Carboxylic Acid Amide Derivatives
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Page/Page column 9, (2008/12/08)
The invention relates to novel piperidine carboxylic acid amide derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of these
RENIN INHIBITORS
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Page/Page column 58, (2008/06/13)
The present invention relates to novel renin inhibitors of the general Formula (I), and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds. These novel renin inhibitors are used in treating cardiovascular events and renal insufficiency.
NOVEL DIAZABICYCLONONENE DERIVATIVE
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Page/Page column 15-16, (2010/11/08)
The invention relates to a novel 3,9-diazabicyclo[3.3.1]nonene derivative and the enantiomers thereof and the use thereof as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including proces
Design and synthesis of a potent biotinylated Smac mimetic
Sun, Haiying,Nikolovska-Coleska, Zaneta,Yang, Chao-Yie,Wang, Shaomeng
, p. 7015 - 7018 (2007/10/03)
A biotinylated Smac mimetic (2) was designed based upon our previously reported potent, conformationally constrained Smac mimetic (1). Smac mimetic (2) was synthesized and determined to bind to XIAP protein with a high-affinity (Ki value of 13
Fused pyridine derivatives
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Example 299, (2010/01/30)
The present provides a condensed pyridine compound (I) represented by the following formula: (wherein, R2represents ring A represents benzene ring, pyridine ring, thiophene ring or furan ring; and B represents its pharmaceutically acceptable salt or hydrates thereof, which is a clinically useful medicament having a serotonin antagonism, in particular, that for treating, ameliorating or preventing spastic paralysis or central muscle relaxants for ameliorating myotonia.
19-nor steroids substituted in position 11β, preparation method and intermediates, application as medicines and pharmaceutical compositions containing them
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, (2008/06/13)
A compound selected from the group consisting of the compounds of the formula wherein the substituents are defined as in the specification and their addition salts with non-toxic, pharmaceutically acceptable acids and bases having estrogenic activity at t
Synthesis of a photoaffinity-labeling analog of alternariolide (AM-toxin I), a host-specific phytotoxin
Hashimoto, Kimiko,Yoshioka, Takuya,Morita, Chikanori,Sakai, Mitsuru,Okuno, Toshikatsu,Shirahama, Haruhisa
, p. 203 - 204 (2007/10/03)
A photoaffinity-labeling analog of alternariolide (AM-toxin I) which contains L-2-amino-5-[4-(1-azi-2,2,2-trifluoro)ethyl-phenyl]pentanoic acid (10) was synthesized.
