Search Results - "Karig, Gunter"
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Discovery of Molidustat (BAY 85‐3934): A Small‐Molecule Oral HIF‐Prolyl Hydroxylase (HIF‐PH) Inhibitor for the Treatment of Renal Anemia
Published in ChemMedChem (23-05-2018)“…Small‐molecule inhibitors of hypoxia‐inducible factor prolyl hydroxylases (HIF‐PHs) are currently under clinical development as novel treatment options for…”
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Journal Article -
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C−H Activation and Palladium Migration within Biaryls under Heck Reaction Conditions
Published in Organic letters (05-09-2002)“…Biaryl bromides such as 1 (RNO2, H, OMe) undergo the Heck reaction to give both the expected products 3 (“retention”) as well as “crossover” products 4…”
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Front Cover: Discovery of Molidustat (BAY 85‐3934): A Small‐Molecule Oral HIF‐Prolyl Hydroxylase (HIF‐PH) Inhibitor for the Treatment of Renal Anemia (ChemMedChem 10/2018)
Published in ChemMedChem (23-05-2018)“…The Front Cover shows key elements of the pharmacological action of molidustat, a novel small‐molecule inhibitor of the hypoxia‐inducible factor prolyl…”
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New Solutions to the C-12,13 Stereoproblem of Epothilones B and D; Synthesis of a 12,13-Diol-Acetonide Epothilone B Analog
Published in European Journal of Organic Chemistry (01-08-2006)“…New approaches are described to the synthesis of epothilone B and a 12,13‐diol‐acetonide derivative. Specifically the (12Z) double bond is formed…”
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Book Review Journal Article -
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Directed Deprotonation−Transmetalation as a Route to Substituted Pyridines
Published in Organic letters (22-03-2001)“…Regioselective C-4 deprotonation of 3-bromopyridine, followed by Li/Zn transmetalation and Pd-mediated coupling processes, provides a flexible entry to…”
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Synthesis and Pharmacological Characterization of Novel Analogues of the Nicotinic Acetylcholine Receptor Agonist (±)-UB-165
Published in Journal of medicinal chemistry (18-07-2002)“…(±)-UB-165 (1) is a potent neuronal nicotinic acetylcholine receptor (nAChR) ligand, which displays functional selectivity between nAChR subtypes. Using UB-165…”
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A novel highly stereoselective total synthesis of epothilone B and of its (12 R,13 R) acetonide
Published in Tetrahedron letters (30-09-2000)“…Stereoselective syntheses of epothilone B ( 1) and its novel derivative 2 are described. Key steps are the formation of intermediate 3 via Sharpless…”
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Synthesis and nicotinic binding of novel phenyl derivatives of UB-165. Identifying factors associated with α7 selectivity
Published in Bioorganic & medicinal chemistry letters (01-09-2003)“…Four racemic phenyl-substituted analogues 3– 6 of the potent nicotinic agonist UB-165 1 have been synthesised and evaluated against the α 4β 2, α 3β 4, and α 7…”
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Journal Article -
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Synthesis and nicotinic binding of novel phenyl derivatives of UB-165. Identifying factors associated with alpha7 selectivity
Published in Bioorganic & medicinal chemistry letters (01-09-2003)“…Four racemic phenyl-substituted analogues 3-6 of the potent nicotinic agonist UB-165 1 have been synthesised and evaluated against the alpha(4)beta(2),…”
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Journal Article -
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δ-Peptide Analogues of Pyranosyl-RNA, Part 1, Nucleo-δ-peptides Derived from Conformationally Constrained Nucleo-δ-amino Acids: Preparation of Monomers
Published in Helvetica chimica acta (07-06-2000)“…Cyclic nucleo‐δ‐amino acids that constitute monomers of a conformationally constrained nucleo‐δ‐peptide base‐pairing system have been prepared. Their synthesis…”
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d-Peptide Analogues of Pyranosyl-RNA, Part 1 , Nucleo-d-peptides Derived from Conformationally Constrained Nucleo-d-amino Acids: Preparation of Monomers
Published in Helvetica chimica acta (07-06-2000)“…Cyclic nucleo-amino acids that constitute monomers of a conformationally constrained nucleo-peptide base-pairing system have been prepared. Their synthesis…”
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