79069-52-6Relevant academic research and scientific papers
NOVEL AZAPEPTIDE OR AZAPEPTIDOMIMETIC COMPOUNDS INHIBITING BCRP AND/OR P-GP
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Page/Page column 15, (2012/01/15)
The present invention relates to compounds of azapeptide or azapeptidomimetic type of formula (I): in which R1, R2, R3, X1, X2, X3, X4 and Y are as defined in claim 1, to pharmaceutical compositions containing them and to such compounds as adjuvant for an anticancer or anti-infectious medicament.
DIPEPTIDYL PEPTIDASE-IV INHIBITING COMPOUNDS, METHODS OF PREPARING THE SAME, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME AS AN ACTIVE AGENT
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Page/Page column 37, (2010/11/24)
The present invention relates to novel compounds exhibiting good inhibitory activity versus Dipeptidyl Peptidase-IV(DPP-IV), methods of preparing the same and pharmaceutical compositions containing the same as an active agent.
Arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 2: Optimization of P1 and N-aryl
Alper, Phillip B.,Liu, Hong,Chatterjee, Arnab K.,Nguyen, Khanhlinh T.,Tully, David C.,Tumanut, Christine,Li, Jun,Harris, Jennifer L.,Tuntland, Tove,Chang, Jonathan,Gordon, Perry,Hollenbeck, Thomas,Karanewsky, Donald S.
, p. 1486 - 1490 (2007/10/03)
A systematic study of anilines led to the discovery of a metabolically robust fluoroindoline replacement for the alkoxy aniline toxicophore in 1. Investigations of the P1 pocket resulted in the discovery of a wide tolerance of functionality leading to the discovery of 11 as a potent and selective inhibitor of cathepsin S.
Synthesis of densely functionalized pyrrolidinone templates by an intramolecular oxo-Diels-Alder reaction
Murray, William V.,Mishra, Pranab K.,Sun, Sengen,Maden, Amy
, p. 7389 - 7392 (2007/10/03)
Preparation of densely functionalized pyrrolidinone templates, is a challenge for synthetic chemists. These templates are important building blocks for novel conformationally constrained natural products or for library generation of highly functionalized
N-nitrosoanilines: A new class of caspase-3 inhibitors
Guo, Zhengmao,Xian, Ming,Zhang, Wei,McGill, Andrea,Wang, Peng George
, p. 99 - 106 (2007/10/03)
Caspases are a family of cysteine proteases activated during apoptosis. In cultured human endothelial cells, physiological levels of NO prevent apoptosis and interfere with the activation of the caspase cascade. Previous studies have demonstrated that NO
Design of a potent combined pseudopeptide endothelin-a/endothelin-b receptor antagonist, ac-dBhg16-Leu-Asp-IIe-[NMe]IIe-Trp21 (PD 156252): Examination of its pharmacokinetic and spectral properties
Cody, Wayne L.,He, John X.,Reily, Michael D.,Haleen, Stephen J.,Walker, Donnelle M.,Reyner, Eric L.,Stewart, Barbra H.,Doherty, Annette M.
, p. 2228 - 2240 (2007/10/03)
The endothelins (ETs) are a family of bicyclic 21-amino acid peptides that are potent and prolonged vasoconstrictors. It has been shown that highly potent combined ET(A)/ET(B) receptor antagonists can be developed from the C- terminal hexapeptide of ET (H
