Abstract: N-phosphonomethylamines are produced by reaction of an amine substrate with a halomethylphosphonic acid or salt thereof, a hydroxymethylphosphonic acid or salt thereof, or a dehydrated self-ester dimer, trimer or oligomer of hydroxymethylphosphonic acid. Among the products that may be prepared according to the process are N-phosphonomethylaminocarboxylic acids such as (e.g.) glyphosate, N-phosphonomethylaminoalkanols such as (e.g.) hydroxyethlaminomethylphosphonic acid, and N-acylaminomethylphosphonic acids such as (e.g.) N-carbamylaminomethylphosphonic acid. Certain reactions are conducted with a substantial excess of amine reactant in order to drive the conversion while avoiding excessive formation of bis(N-phosphonomethyl)amine by-products.

Abstract: This invention provides a method of preparing a polymeric delivery system for active ingredients. The delivery system is formed either by attaching the active ingredient to a linker through a hydrolyzable covalent bond, then forming a covalent bond between the linker and a portion of the subunits of a cross-linked polymer, or by attaching a linker to a portion of the subunits of a cross-linked polymer, then attaching the active ingredient to the polymer-linker combination through a hydrolyzable covalent bond. The invention also provides a delivery system comprising an active ingredient covalently bonded through a hydrolyzale covalent bond to a linker, which is in turn covalently bonded to a portion of subunits of a cross-linked polymer.

Abstract: Thiepine apical sodium co-dependent bile acid transport (ASBT) inhibitors are disclosed together with methods of making the same, methods of using the same to treat hyperlipidemic conditions as well as pharmaceutical compositions containing the same compounds.

Abstract: Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals.

Abstract: Among its several embodiments, the present invention provides an improved process for the preparation of tetrahydrobenzothiepine-1,1-dioxide compounds; the provision of a process for preparing a diastereomeric mixture of tetrahydrobenzothiepine-1,1-dioxide compounds from a single diastereomer of such compounds; the provision of a process for the preparation of 3-bromo-2-substituted propionaldehyde compounds; and the provision of a process for the preparation of 3-thio-2-substituted propionaldehyde compounds.

Abstract: Mono-fluorinated and di-fluorinated benzothiepine apical sodium co-dependent bile acid transport (ASBT) inhibitors are disclosed together with methods of making the same, methods of using the same to treat hyperlipidemic conditions as well as pharmaceutical compositions containing the same compounds.

Abstract: Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals.

Abstract: Novel methods and combinations for the treatment and/or prophylaxis of a hyperlipidernic condition or disorder in a subject, wherein the methods comprise the administration of one or more HMG Co-A reductase inhibitors and one or more ASBT inhibitors selected from the specific group of compounds described herein, and the combinations comprise one or more HMG Co-A reductase inhibitors and one or more of said apical sodium co-dependent bile acid transport inhibitors.

Abstract: Among its several embodiments, the present invention provides an improved process for the preparation of tetrahydrobenzothiepine-1,1-dioxide compounds; the provision of a process for preparing a diastereomeric mixture of tetrahydrobenzothiepine-1,1-dioxide compounds from a single diastereomer of such compounds; the provision of a process for the preparation of 3-bromo-2-substituted propionaldehyde compounds; and the provision of a process for the preparation of 3-thio-2-substituted propionaldehyde compounds.

Abstract: Compounds, pharmaceutical compositions, and methods for the treatment of a hyperlipidemic condition in a subject.

Abstract: Mono-fluorinated and di-fluorinated benzothiepine apical sodium co-dependent bile acid transport (ASBT) inhibitors are disclosed together with methods of making the same, methods of using the same to treat hyperlipidemic conditions as well as pharmaceutical compositions containing the same compounds.

Abstract: The present invention provides combinations of cardiovascular therapeutic compounds for the prophylaxis or treatment of cardiovascular disease including hypercholesterolemia and atherosclerosis. Combinations disclosed include an ileal bile acid transport inhibitor combined with a cholesteryl ester transport protein (CETP) inhibitor, a fibric acid derivative, a nicotinic acid derivative, a microsomal triglyceride transfer protein inhibitor, a cholesterol abosrption antagonist, a phytosterol, a stanol, an antihypertensive agent, or others. Further combinations include a CETP inhibitor with a fibric acid derivative, a nicotinic acid derivative, a bile acid sequestrant, a microsomal triglyceride transfer protein inhibitor, a cholesterol abosrption antagonist, or others.

Abstract: Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals.

Abstract: Among its several embodiments, the present invention provides an improved process for the preparation of tetrahydrobenzothiepine-1,1-dioxide compounds; the provision of a process for preparing a diastereomeric mixture of tetrahydrobenzothiepine-1,1-dioxide compounds from a single diastereomer of such compounds; the provision of a process for the preparation of 3-bromo-2-substituted propionaldehyde compounds; and the provision of a process for the preparation of 3-thio-2-substituted propionaldehyde compounds.

Abstract: A method of treatment of a host with a cellular proliferative disease, comprising contacting the host with a cephalotaxine and an antiproliferative agent, each in an amount sufficient to modulate said cellular proliferative disease, is described. In some embodiments, the cephalotaxine comprises homoharringtonine (cephalotaxine, 4-methyl-2-hydroxy-2-(4-hydroxy-4-methyl pentyl) butanediocate ester). Antiproliferative agents of the invention comprise alkylating agents, intercalating agents, metal coordination complexes, pyrimidine nucleosides, purine nucleosides, inhibitors of nucleic acid associated enzymes and proteins, and agents affecting structural proteins and cytoplasmic enzymes.

Abstract: Thiepine apical sodium co-dependent bile acid transport (ASBT) inhibitors are disclosed together with methods of making the same, methods of using the same to treat hyperlipidemic conditions as well as pharmaceutical compositions containing the same compounds.

Abstract: Among its several embodiments, the present invention provides an improved process for the preparation of tetrahydrobenzothiepine-1,1-dioxide compounds; the provision of a process for preparing a diastereomeric mixture of tetrahydrobenzothiepine-1,1-dioxide compounds from a single diastereomer of such compounds; the provision of a process for the preparation of 3-bromo-2-substituted propionaldehyde compounds; and the provision of a process for the preparation of 3-thio-2-substituted propionaldehyde compounds.

Abstract: Compounds, pharmaceutical compositions, and methods for the treatment of a hyperlipidemic condition in a subject. The compounds of the present invention are apical sodium co-dependent bile acid transport inhibitors and are 1,4-benzothiazepine and 1,5-benzothiazepine compounds corresponding to Formula I: 1 wherein j, m, Y, Z, R1A, R1B, R2A, R2B and R6 are as defined in the specification.

Abstract: This invention provides a method of preparing a polymeric delivery system for active ingredients having enhanced site specific release performance characteristics. The delivery system is formed either by attaching the active ingredient to a linker through an acid-sensitive covalent bond, then forming a covalent bond between the linker and a portion of the subunits of a crosslinked polystyrene polymer, or by attaching a linker to a portion of the subunits of a crosslinked polystyrene polymer, then attaching the active ingredient to the polymer-linker combination through an acid-sensitive covalent bond. The invention also provides a delivery system comprising an active ingredient covalently bonded through an acid-sensitive covalent bond to a linker, which is in turn covalently bonded to a portion of subunits of a crosslinked polystyrene polymer.

Abstract: A compound is disclosed havin the formula AW—SiR1R2R3 wherein R1 and R2 are independently alkyl, cycloalkyl, alkenyl, alkynyl, aryl, aralkyl, alkaryl, or a hydrophilic group; R3 is a hydrophilic group; and AW is the covalently bonded form of a drug AWH, wherein W is O, NH, S, or an enolate group. The hydrophilic group may be either non-neutral, or may be a polyol. This compound serves as a prodrug for the drug AWH. A method for preparing these compounds is also disclosed. Also disclosed is a method of treatment or prevention of gastric ulcers by administering the prodrug compounds.