- MANUFACTURE PROCESS OF ORGANIC COMPOUNDS
-
The present invention relates to a method of preparing N-substituted salicylamides or derivatives thereof and their derivatives, e.g. their salts. In particular, the present invention relates to a method of preparing (N-(5-chlorosalicyloyl)-8-aminocapryli
- -
-
Page/Page column 5
(2009/09/28)
-
- MANUFACTURE PROCESS OF N-SUBSTITUTED SALICYLAMIDES
-
The present invention relates to a method of preparing N-substituted salicylamides or derivatives thereof, and their salts, hydrates and solvates. In particular, the present invention relates to a method of preparing N-(5-chlorosalicyloyl)-8-aminocaprylic
- -
-
Page/Page column 34-35
(2008/06/13)
-
- Compositions for delivering parathyroid hormone and calcitonin
-
The present invention relates to a composition comprising a delivery agent, parathyroid hormone, and calcitonin. This composition exhibits increased delivery of parathyroid hormone and/or calcitonin and is useful for the treatment of osteoporosis. The com
- -
-
-
- Use of oligosalicylates in the preparation of phenolic amido acids
-
A simplified methodology has been developed for preparing salicylamides from the corresponding acids via oligosalicylates which both protect the phenolic group and, at the same time, activate the carboxyl for coupling. Copyright Taylor & Francis, Inc.
- Gschneidner, David,Corvino, JoAnne,Freeman, John,O'Toole, Doris,Shields, Lynn,Wang, Eric
-
p. 1567 - 1575
(2007/10/03)
-
- Method of preparing salicylamides
-
The present invention provides a fast, high yield method for preparing salicylamide intermediates. The method comprises reacting a C4 or higher alkyl ester of salicylic acid or derivative thereof with at least one amine selected from the group consisting of monoalkylamines, dialkylamines, ammonia, and any combination of any of the foregoing in alcohol to yield the sali-cylamide. The C4 or higher alkyl ester of salicylic acid or a derivative thereof is preferably prepared by reacting salicylic acid or a derivative thereof with a C4 or higher alcohol in presence of at least one of sulfuric acid, a sulfonic acid, and a mineral acid. This process for preparing salicylamide intermediates from salicylic acid or derivative thereof generally has a cycle time of about 2 days, and yields about 95% of a 99% pure material. In comparison, when a C3 or lower alkyl ester is used in lieu of the C4 or higher alkyl ester, the process generally has a cycle time of 7-9 days and yields about 60% of a 95% pure material. Methods of preparing an alkylated salicylamide are also provided.
- -
-
Page/Page column 8-9
(2008/06/13)
-
- Method of preparing alkylated salicylamides
-
The present invention relates to a method of preparing an alkylated salicylamide from a protected and activated salicylamide (hereinafter referred to as a “protected/activated salicylamide”). The method comprises the steps of (a) alkylating the protected/
- -
-
-
- Synthesis and evaluation of compounds that facilitate the gastrointestinal absorption of heparin
-
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.
-
p. 1163 - 1171
(2007/10/03)
-