- Peptide deformylase inhibitors
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The present invention relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods directed to bacterial infections and inhibition of bacterial peptide deformylase (PDF) activity.
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Page/Page column
(2014/12/09)
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- PEPTIDE DEFORMYLASE INHIBITORS
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The present invention relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods directed to bacterial infections and inhi-bition of bacterial peptide deformylase (PDF) activity
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Page/Page column
(2014/02/15)
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- Synthesis of a novel tricyclic 1,2,3,4,4a,5,6,10b-octahydro-1,10-phenanthroline ring system and CXCR4 antagonists with potent activity against HIV-1
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Stereorandom and diastereoselective syntheses of a novel 1,2,3,4,4a,5,6,10b-octahydro-1,10-phenanthroline ring system are described. Derivatives of all four diastereomers were prepared and isolated in >98% ee. The pure enantiomers were compared in order t
- Catalano, John G.,Gudmundsson, Kristjan S.,Svolto, Angilique,Boggs, Sharon D.,Miller, John F.,Spaltenstein, Andrew,Thomson, Michael,Wheelan, Pat,Minick, Doug J.,Phelps, Dean P.,Jenkinson, Stephen
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experimental part
p. 2186 - 2190
(2010/07/05)
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- Kilogram-scale synthesis of the CXCR4 antagonist GSK812397
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An improved, scalable synthesis of the CXCR4 antagonist GSK812397 is described. This new route was recently scaled up in 50 L fixed equipment to afford 1.2 kg of drug substance in five steps with an overall yield of 20% and >99% chemical and enantiomeric
- Boggs, Sharon,Elitzin, Vassil I.,Gudmundsson, Kristjan,Martin, Michael T.,Sharp, Matthew J.
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scheme or table
p. 781 - 785
(2010/04/22)
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- 7-Azaindole derivatives as potential partial nicotinic agonists
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We have investigated a series of 7-azaindoles as potential partial agonists of the α4β2 nicotinic acetylcholine receptor (nAChR). Three series of 7-azaindole derivatives have been synthesized and evaluated for rat brain neuronal nicotinic receptor affinity and functional activity. Compound (+)-51 exhibited the most potent nAChR binding (Ki = 10 nM). Compound 30A demonstrated both moderate binding affinity and partial agonist potency, thus representing a promising lead for the indications of cognition and smoking cessation.
- Stoit, Axel R.,den Hartog, Arnold P.,Mons, Harry,van Schaik, Sjoerd,Barkhuijsen, Nynke,Stroomer, Cees,Coolen, Hein K.A.C.,Reinders, Jan Hendrik,Adolfs, Tiny J.P.,van der Neut, Martina,Keizer, Hiskias,Kruse, Chris G.
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p. 188 - 193
(2008/12/23)
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- CHEMICAL COMPOUNDS
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The present invention provides compounds that demonstrate protective effects on target cells from HIV infection in a manner as to bind to chemokine receptor, and which affect the binding of the natural ligand or chemokine to a receptor such as CXCR4 of a
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Page/Page column 35
(2008/06/13)
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- CHEMICAL COMPOUNDS
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The present invention provides compounds that demonstrate protective effects on target cells from HIV infection in a manner as to bind to chemokine receptor, and which affect the binding of the natural ligand or chemokine to a receptor such as CXCR4 of a
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Page/Page column 44; 59
(2010/11/28)
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- CHEMICAL COMPOUNDS
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There is provided novel compounds that demonstrate protective effects on target cells from HIV infection in a manner as to bind specifically to the chemokine receptor, and which affect the binding of the natural ligand or chemokine to a receptor such as C
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Page/Page column 39-40
(2008/06/13)
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- CHEMCIAL COMPOUNDS
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The present invention provides novel compounds that demonstrate protective effects on target cells from HIV infection in a manner as to bind specifically to the chemokine receptor, and which affect the binding of the natural ligand or chemokine to a receptor such as CXCR4 and/or CCR5 of a target cell.
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Page/Page column 59-60
(2010/10/20)
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- CHEMICAL COMPOUNDS
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The present invention provides novel compounds that demonstrate protective effects on target cells from HIV infection in a manner as to bind specifically to the chemokine receptor, and which affect the binding of the natural ligand or chemokine to a recep
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Page/Page column 64-65
(2010/11/08)
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- CHEMICAL COMPOUNDS
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The present invention provides compounds of Formula (I) comprising: including salts, solvates, and physiologically functional derivatives thereof, pharmaceutical formulations containing them, processes for their preparation, and methods of treatment using them.
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Page/Page column 14.B.A
(2008/06/13)
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- Large-scale synthesis of new cyclazines, 5-thia-1,8b-diazaacenaphthylene-3-carboxylic acid derivatives having the peripheral 12π-electron ring system
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The 5-thia-1,8b-diazaacenaphthylenes (2 and its ester, 8) are new cyclazines, in which a paramagnetic ring is present in the peripheral 12π-electron ring system. Three convenient methods of preparing 8 have been developed. One involved thioglycolation of a new compound, 5-fluoroimidazo[1,2-a]pyridine (6b), followed by the Duff reaction gave 8 in 64% yield without chromatographic purification.
- Ikemoto, Tomomi,Kawamoto, Tetsuji,Wada, Hiroki,Ishida, Toru,Ito, Tatsuya,Isogami, Yasushi,Miyano, Yoshiko,Mizuno, Yukio,Tomimatsu, Kiminori,Hamamura, Kazumasa,Takatani, Muneo,Wakimasu, Mitsuhiro
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p. 489 - 493
(2007/10/03)
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- Fused imidazopyridine derivatives as antihyperlipidemic agents
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A novel compound of the formula: wherein ring Q is an optionally substituted pyridine ring; One of R0, R1and R2is —Y0—Z0, and the other tow groups are a hydrogen, a halogen, an optionally substituted hydroxy group, a hydrocarbon group that may be an optionally substituted hydrocarbon group or an acyl group; Y0is a bond or an optionally substituted bivalent hydrocarbon group; Z0is a basic group which may be bonded via oxygen, nitrogen, —CO—, —CS—, —SO2N(R3)— (where R3is hydrogen or an optionally substituted hydrocarbon group), or S(O)n(wherein n is to 0, 1 or 2); .........is a single bond or a double bond, or a salt thereof, which has an excellent LDL receptor up-regulating, blood-lipids lowering, blood-sugar lowering and diabetic complication-ameliorating activity.
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- Condensation of substituted 2-aminopyridine with β-ketocarboxylic esters: 4H-pyrido[1,2-a]pyrimidin-4-ones and pyridin-2-ones
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We report the condensation of substituted 2-aminopyridines 5 with β- ketocarboxylic esters in polyphosphoric acid. In this reaction were obtained together with the target compounds, 4H-pyrido[1,2-a]pyrimidin-4-ones 6 also the pyridin-2-ones 7. All the compounds 7 were tested for their calcium- antagonistic activity but failed to evoke any vasorelaxant response.
- Ferrarini, Pier Luigi,Mori, Claudio,Manera, Clementina,Mori, Filippo,Calderone, Vincenzo,Martinotti, Enrica
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p. 1123 - 1127
(2007/10/03)
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- Benzothiazine derivative
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N-(6-fluoro-2-pyridyl)-3,4-dihydro-2-methyl-4-oxo-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide that is a novel benzothiazine derivative. The compound is characterized by a low degree of toxicity and a low incidence of gastric disorders and useful as an anti-inflammatory agent.
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