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Exploratory drug safety: a discovery strategy to reduce attrition in development.
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Discovery of Narlaprevir (SCH 900518): A Potent, Second Generation HCV NS3 Serine Protease Inhibitor.
TLDR
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.
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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).
TLDR
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.
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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).
TLDR
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.
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High-performance liquid chromatographic analysis of pilocarpine hydrochloride, isopilocarpine, pilocarpic acid and isopilocarpic acid in eye-drop preparations.
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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)
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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…
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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…
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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…
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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
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