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Exploratory drug safety: a discovery strategy to reduce attrition in development.
Discovery of Narlaprevir (SCH 900518): A Potent, Second Generation HCV NS3 Serine Protease Inhibitor.
- A. Arasappan, F. Bennett, F. G. Njoroge
- Biology, ChemistryACS medicinal chemistry letters
- 15 February 2010
Detailed investigations toward a second generation protease inhibitor culminated in the discovery of narlaprevir, 37, with improved potency (∼10-fold over 1), pharmacokinetic profile and physicochemical characteristics, currently in phase II human trials.
Posaconazole (Noxafil, SCH 56592), a new azole antifungal drug, was a discovery based on the isolation and mass spectral characterization of a circulating metabolite of an earlier lead (SCH 51048).
H-SCH 51048 was administered to a large group of mice, the serum was harvested and the metabolite was isolated by extraction and semipreparative HPLC, and SCH 56592 emerged as the candidate with the best overall profile.
Synthesis of [(3) H], [(13) C3 , (15) N], and [(14) C]SCH 900567: an inhibitor of TNF-α (tumor necrosis factor alpha) converting enzyme (TACE).
- S. Ren, D. Hesk, P. Mcnamara, D. Koharski, S. Borges
- Chemistry, BiologyJournal of labelled compounds…
- 31 August 2014
Stable isotope-labeled SCH 900567 was requested by the bioanalytical group as an internal standard for Liquid chromatography-tandem mass spectrometry (LC-MS/MS) method development as well as by the drug metabolism and pharmacokinetics group for a potential microdose study.
High-performance liquid chromatographic analysis of pilocarpine hydrochloride, isopilocarpine, pilocarpic acid and isopilocarpic acid in eye-drop preparations.
Amino acid derivatives that stabilize secondary structures of polypeptides : II. The most stable conformation of peptides containing 3-amino-2-piperidone-6-carboxylic acid (Acp)
An efficient synthesis of ethyl LL-3-amino-2-piperidone-6-carboxylate
Synthese a partir de cycloglycylhomoseryle via la bromo-2' ethyl-2 diethoxy-3,6 dihydro-2,5 pyrazine, le diethoxy-3,6 diaza-2,5bicyclo [2.2.2] octadiene-2,5 et le dichlorhydrate du diamino-2,5…
Tritium labelling of pharmaceuticals by metal‐catalysed exchange methods
Metal-catalysed exchange with tritiated water and tritium gas has been extensively used to prepare a wide range of tritium-labelled compounds in support of pharmaceutical research. Examples of the…
Synthesis of isotopically labelled compounds at Schering-Plough, an historical perspective
The use of isotopically labelled compounds at Schering-Plough (S-P) has substantially increased over the past 30 years. Since the formation of the S-P Radiochemistry section in the early 1970s, the…
Conformationally restricted cyclic nonapeptides derived from L-cysteine and LL-3-amino-2-piperidone-6-carboxylic acid (LL-Acp), a potent .beta.-turn-inducing dipeptide analog
Synthese de cyclo-(Gly-Cys-Gly) 3 , cyclo-(Pro-Gly-Cys) 3 et cyclo-(Cys-Acp) 3 pontes sur les 3 atomes de soufre par mesitylenetriyl. Conformations