- The [(Cp)M(CO)3] (M=Re, 99mTc) building block for imaging agents and bioinorganic probes: Perspectives and limitations
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Starting from asymmetric Thiele's acid derivatives, two different imaging probes [99mTc(CO)3(CpR)] (R=potential targeting vector) are generated simultaneously in one-pot and from one substrate. This extends the previously introduced
- Can, Daniel,Peindy N'Dongo, Harmel W.,Spingler, Bernhard,Schmutz, Paul,Alberto, Roger,Raposinho, Paula,Santos, Isabel
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p. 1849 - 1866,18
(2020/08/24)
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- ERYTHROMYCIN A 9-0-OXIME DERIVATIVES ENDOWED WITH ANTIBIOTIC ACTIVITY
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PCT No. PCT/EP95/04815 Sec. 371 Date May 16, 1997 Sec. 102(e) Date May 16, 1997 PCT Filed Dec. 7, 1995 PCT Pub. No. WO96/18633 PCT Pub. Date Jun. 20, 1996Erythromycin 9-oxime derivatives wherein a phenyl or heterocylic group is attached indirectly to the 9-position of erythromycin A through an alkylene diamine bridging member. These compounds exhibit broad spectrum antibiotic activity.
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- Studies directed at the use of a parallel synthesis matrix to increase throughput in an in vivo assay
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Heparin is the anticoagulant of choice for hospitalized patients, but it is dosed only by injection because it is not absorbed following oral administration. We have discovered and prepared compounds (delivery agents) that facilitate the gastrointestinal absorption of heparin in rats, monkeys, and humans when given orally. We are currently developing a parallel synthesis approach to increase our delivery agent screening throughput in vivo. This approach has been used to produce micromolar quantities of compounds for testing in rats in a 5 x 5 parallel synthesis array. Using an amine benzoylation reaction sequence, 10 mixtures were prepared. These mixtures contained equal weight quantities of five N-substituted, non-α, amino acid delivery agents. Each of these mixtures was orally administered to rats in combination with heparin, and plasma clotting times (APTT) were measured to determine activity. Deconvolution of the data accurately identified the most active individual components. Independent synthesis of these compounds verified their activity. This parallel synthesis approach is an effective tool for the screening of oral heparin delivery agents and has increased screening throughput significantly.
- Leone-Bay,Freeman,O'Toole,Rosario-Gray,Salo-Kostmayer,Tai,Mercogliano,Baughman
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p. 3573 - 3576
(2007/10/03)
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- Synthesis and evaluation of compounds that facilitate the gastrointestinal absorption of heparin
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A family of novel compounds (delivery agents) that promote the gastrointestinal absorption of USP heparin in rats and primates has been discovered. The delivery agents in combination with heparin were administered either orally or intracolonically in an aqueous propylene glycol solution and caused dramatic increases in both plasma heparin concentrations (anti-Factor Xa) and clotting times (APTT). Using one of the most effective delivery agents in this series, an estimated relative bioavailability of 8% can be achieved following oral administration to cynomolgus monkeys. To establish a correlation between the in vivo data and an in vitro parameter, immobilized artificial membrane (IAM) chromatography was performed. Log relative k' values were correlated to the efficiency of oral heparin delivery.
- Leone-Bay, Andrea,Paton, Duncan R.,Freeman, John,Lercara, Christine,O'Toole, Doris,Gschneidner, David,Wang, Eric,Harris, Elizabeth,Rosado, Connie,Rivera, Theresa,DeVincent, Aldonna,Tai, Monica,Mercogliano, Frank,Agarwal, Rajesh,Leipold, Harry,Baughman, Robert A.
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p. 1163 - 1171
(2007/10/03)
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- Composition containing a penem or carbapenem antibiotic and the use of the same
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Administration of an N-acylated amino acid in association with a penem or carbapenem antibiotic relieves or eliminates the renal problems associated with administration of the antibiotic alone. The amino acid derivative and antibiotic may be formulated together as a composition or administered separately, either simultaneously or sequentially.
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- Composition containing a penem or carbapenem antibiotic
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Administration of an N-acylated amino acid in association with a penem or carbapenem antibiotic relieves or eliminates the renal problems associated with administration of the antibiotic alone. The amino acid derivative and antibiotic may be formulated together as a composition or administered separately, either simultaneously or sequentially. The composition may be prepared by simple mixing.
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