- BICYCLIC ARYL AND HETEROARYL COMPOUNDS FOR THE TREATMENT OF METABOLIC DISORDERS
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Compounds of formula (I): or pharmaceutically acceptable salts thereof, are opioid receptor modulators, e.g. mu- opioid receptor antagonists, neutral antagonists or inverse agonists, and are useful for the treatment of metabolic disorders including obesity.
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Page/Page column 25
(2009/01/20)
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- Novel 8-substituted dipyridodiazepinone inhibitors with a broad-spectrum of activity against HIV-1 strains resistant to non-nucleoside reverse transcriptase inhibitors
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A series of novel 8-substituted dipyridodiazepinone-based inhibitors were investigated for their antiviral activity against wild type human immunodeficiency virus (HIV-1) and the clinically prevalent K103N/Y181C mutant virus. Our efforts have resulted in a series of benzoic acid analogues that are potent inhibitors of HIV-1 replication against a panel of HIV-1 strains resistant to non-nucleoside reverse transcriptase inhibitors (NNRTIs). Furthermore, the combination of good antiviral potency, a broad spectrum of activity, and an excellent pharmacokinetic profile provides strong justification for the further development of compound 7 as a potential treatment for wild type and NNRT1-resistant HIV-1 infection.
- O'Meara, Jeff A.,Yoakim, Christiane,Bonneau, Pierre R.,B?s, Michael,Cordingley, Michael G.,Déziel, Robert,Doyon, Louise,Duan, Jianmin,Garneau, Michel,Guse, Ingrid,Landry, Serge,Malenfant, Eric,Naud, Julie,Ogilvie, William W.,Thavonekham, Bounkham,Simoneau, Bruno
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p. 5580 - 5588
(2007/10/03)
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- Palladium(II)-catalyzed sequential hydroxylation-carboxylation of biphenyl using formic acid as a carbonyl source
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(Equation Presented) A simultaneous hydroxylation-carboxylation of biphenyl occurred to give 4′-hydroxy-4-biphenylcarboxylic acid, which has wide potential application as a polyester monomer.
- Shibahara, Fumitoshi,Kinoshita, Shinsuke,Nozaki, Kyoko
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p. 2437 - 2439
(2007/10/03)
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- Hydroxylation of ionized aromatics including carboxylic acid or amine using recombinant Streptomyces lividans cells expressing modified biphenyl dioxygenase genes
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The bphA1(2072)A2A3A4 gene cluster codes for a shuffled biphenyl dioxygenase holoenzyme with broad substrate specificity. These bphA1(2072)A2A3A4 genes were expressed in the actinomycetes Streptomyces lividans using a thiostrepton-inducible promoter PtipA. Biotransformation experiments of various aromatics including carboxylic acid or amine in their molecular structure, such as 1-naphthoic acid, 2-(1-naphthyl)acetic acid, diphenylamine, and 1-benzyl-4-piperidone, were performed using the recombinant S.lividans cells. These ionized aromatics were converted to the corresponding 1,2-dihydrodiol, mono- or tri-hydroxy forms in 48h. The structure of the converted products was determined by their EI-MS, 1H- and 13C NMR analysis, and several products were found to be novel compounds.
- Shindo, Kazutoshi,Nakamura, Ryoko,Chinda, Ikuko,Ohnishi, Yasuo,Horinouchi, Sueharu,Takahashi, Haruko,Iguchi, Kazuo,Harayama, Shigeaki,Furukawa, Kensuke,Misawa, Norihiko
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p. 1895 - 1900
(2007/10/03)
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