Search Results - "ROSSI, Tino"
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Discovery Process and Pharmacological Characterization of 2-(S)-(4-Fluoro-2-methylphenyl)piperazine-1-carboxylic Acid [1-(R)-(3,5-Bis-trifluoromethylphenyl)ethyl]methylamide (Vestipitant) as a Potent, Selective, and Orally Active NK1 Receptor Antagonist
Published in Journal of medicinal chemistry (28-05-2009)“…In an effort to discover novel druglike NK1 receptor antagonists a new series of suitably substituted C-phenylpiperazine derivatives was identified by an…”
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2
Quality by Design in lead optimization: a new strategy to address productivity in drug discovery
Published in Current opinion in pharmacology (01-10-2011)“…Highlights ► High attrition has put the entire Pharma R&D business model under pressure. ► The selection of quality candidates is key to achieve efficiency and…”
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3
Stereoselective Synthesis of a Key Intermediate of Sanfetrinem by Means of a Chelated Tin(IV) Enolate
Published in Journal of organic chemistry (21-03-1997)“…(2S)-2-Methoxycyclohexanone [(2S)-6], reacts with the 4-acetoxyazetidinone 3a in the presence of SnCl4 and a tertiary amine base (such as…”
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4
Solution phase library of perhydrooxazin-4-ones
Published in Tetrahedron letters (01-09-1998)“…A general approach to the solution phase parallel synthesis of perhydrooxazin-4-ones, which allows the preparation of milligram quantities of each individual…”
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5
The synthesis of a key intermediate of tricyclic beta-lactam antibiotics
Published in Tetrahedron letters (12-06-1995)“…By employing an intramolecular Sakurai-type olefination it was possible to obtain the olefin 5, a key intermediate in the synthesis of the broad spectrum…”
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6
1,2,4-Triazol-3-yl-thiopropyl-tetrahydrobenzazepines: A Series of Potent and Selective Dopamine D 3 Receptor Antagonists
Published in Journal of medicinal chemistry (18-10-2007)Get full text
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7
Analogues of 4,5-bis(3,5-dichlorophenyl)-2-trifluoromethyl-1H-imidazole as potential antibacterial agents
Published in Bioorganic & medicinal chemistry letters (05-04-1999)“…A preliminary exploration of analogues of 4,5-bis(3,5-dichlorophenyl)-2-trifluoromethyl-1H-imidazole, 1, as novel antibacterial agents was carried out to…”
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8
Dopamine D 3 receptor antagonists: The quest for a potentially selective PET ligand. Part 3: Radiosynthesis and in vivo studies
Published in Bioorganic & medicinal chemistry letters (01-09-2009)“…Radiosynthesis and in vivo testing for a potential Dopamine D 3 PET ligand are reported. Compound 1 is a potent and selective antagonist of the dopamine D 3…”
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9
Application of LC-NMR to the identification of bulk drug impurities in NK1 antagonist GW597599 (vestipitant)
Published in Magnetic resonance in chemistry (01-07-2010)“…Liquid chromatography‐NMR (LC–NMR) spectroscopy was used to obtain detailed information regarding the structure of the major bulk drug impurities present in…”
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10
Dopamine D3 receptor antagonists: The quest for a potentially selective PET ligand. Part 3: Radiosynthesis and in vivo studies
Published in Bioorganic & medicinal chemistry letters (01-09-2009)“…Compound 1 is a potent and selective antagonist of the dopamine D(3) receptor. With the aim of developing a carbon-11 labeled ligand for the dopamine D(3)…”
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11
1,2,4-Triazol-3-yl-thiopropyl-tetrahydrobenzazepines: A Series of Potent and Selective Dopamine D3 Receptor Antagonists
Published in Journal of medicinal chemistry (18-10-2007)“…The discovery of new highly potent and selective dopamine D3 receptor antagonists has recently permitted characterization of the role of the dopamine D3…”
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12
Dopamine D sub(3) receptor antagonists: The quest for a potentially selective PET ligand. Part 3: Radiosynthesis and in vivo studies
Published in Bioorganic & medicinal chemistry letters (01-09-2009)“…Compound 1 is a potent and selective antagonist of the dopamine D sub(3) receptor. With the aim of developing a carbon-11 labeled ligand for the dopamine D…”
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13
Discovery Process and Pharmacological Characterization of 2-( S )-(4-Fluoro-2-methylphenyl)piperazine-1-carboxylic Acid [1-( R )-(3,5-Bis-trifluoromethylphenyl)ethyl]methylamide (Vestipitant) as a Potent, Selective, and Orally Active NK 1 Receptor Antagonist
Published in Journal of medicinal chemistry (28-05-2009)Get full text
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14
1,2,4-triazol-3-yl-thiopropyl-tetrahydrobenzazepines: a series of potent and selective dopamine D(3) receptor antagonists
Published in Journal of medicinal chemistry (18-10-2007)“…The discovery of new highly potent and selective dopamine D3 receptor antagonists has recently permitted characterization of the role of the dopamine D3…”
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15
Nitrate ester derivatives from epoxides using CAN: Efficient preparation of key intermediates in the synthesis of 4-alkoxytrinems
Published in Tetrahedron letters (19-05-1997)“…A regio and stereoselective opening reaction of epoxide with CAN (0.5 equivalents) in aprotic solvents is descried. This novel reaction allowed the preparation…”
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16
Solid-phase/solution-phase combinatorial synthesis of neuroimmunophilin ligands
Published in Bioorganic & medicinal chemistry letters (15-05-2000)“…A novel solid-phase/solution-phase strategy for the synthesis of neuroimmunophilin ligands based on GPI 1046 was developed. The synthesis employs a solid-phase…”
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17
The stereoselective synthesis of 4-formyltrinem, a key intermediate for novel trinems
Published in Tetrahedron letters (19-05-1997)“…The stereoselective synthesis of a protected 4-formyltrinem 8 was accomplished in good yield. This compound is a potential intermediate in the synthesis of a…”
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18
Novel Amidoalkylation of 4-Acetoxyazetidinones with Allylic Boranes. A Stereoselective Entry into the Tribactams
Published in Journal of the American Chemical Society (01-09-1995)Get full text
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19
Highly Diastereoselective Synthesis of 4- N-Methylformamidino Trinem (GV129606), a Potent Antibacterial Agent
Published in Tetrahedron (28-07-2000)“…In this paper a highly diastereoselective synthesis of 4- N-methylformamidino trinem 3 is reported. The route offers advantages compared to that previously…”
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20
Synthesis of polymer-bound fischer chromium alkoxy and aminocarbene complexes
Published in Tetrahedron letters (30-04-1999)“…A series of polymer-bound Fischer chromium alkoxy and amino carbene type I complexes were synthesized by the thermal exchange of a CO ligand in chromium…”
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