Monsanto Company

G.d. Searle & Company

Pharmacia Corporation

G.d. Searle LLC

Monsanto Technology LLC

Galera Labs, LLC

Galera Therapeutics, LLC

Monsato Company

Samuel J Tremont

Alex N Williamson

Martin P McGrath

Len F Lee

David B Reitz

Horng-Chih Huang

Jinglin J Li

Shyamal C Banerjee

Raymond E Miller

Robert A Keppel

Kevin J Koeller

George D Davis

Arthur J Solodar

Emerson H Lee

Paul Waddell Collins

Denis Forster

William L Neumann

Kishore Udipi

Mark John Pozzo

Daniela Salvemini

Jon P Lawson

Claire A Przybyla

James C Peterson

Erik D Sall

Amruta Reddy Poreddy

Payman N Farid

Kevin Babiak

Pierre-Jean Colson

Robert Hett

Grace Mary Wagner

Benxin Zhi

Ricky L Fenton

Jay S Trivedi

Andrew Carpenter

Eduardo K Mar

Vladislav Orlovski

Lawrence M Miller

Shine Chou

Christian H Huber

Gerald A Weisenburger

Martin P Mcgrath

Aubert Y Coran

James P Coleman

Jerry R Ebner

Patrick J Lennon

James J Li

Frederick Ignatz-Hoover

Eric A Haupfear

Terry M Balthazor

Leonard Harris Davis

Serge G Wolfson

Yinong Ma

Philip H Brodsky

Peter Hadley Jones

William Eldredge Perkins

James Li

Joseph A Schaper

Compounds and methods for utilizing compounds comprising a superoxide dismutase mimetic covalently linked to polyethylene glycol. Methods are also provided for preparing a superoxide dismutase mimetic covalently linked to a polyethylene glycol, the methods comprising reacting an activated polyethylene glycol with a superoxide dismutase mimetic, or alternatively, reacting a superoxide dismutase mimetic with an activated polyethylene glycol. A method is also provided for preventing or treating a disease or disorder in which superoxide anions are implicated, comprising administering to a subject in need thereof, a therapeutically effective amount of a compound comprising a superoxide dismutase mimetic covalently linked to a polyethylene glycol. Methods of determining the safety and efficacy of the compounds are also provided. Methods for determining the safety and efficacy can include methods in lab animals and humans.

Polyethylene glycolated superoxide dismutase mimetics

Compounds and methods for utilizing compounds comprising a superoxide dismutase mimetic covalently linked to polyethylene glycol. Methods are also provided for preparing a superoxide dismutase mimetic covalently linked to a polyethylene glycol, the methods comprising reacting an activated polyethylene glycol with a superoxide dismutase mimetic, or alternatively, reacting a superoxide dismutase mimetic with an activated polyethylene glycol. A method is also provided for preventing or treating a disease or disorder in which superoxide anions are implicated, comprising administering to a subject in need thereof, a therapeutically effective amount of a compound comprising a superoxide dismutase mimetic covalently linked to a polyethylene glycol. Methods of determining the safety and efficacy of the compounds ere also provided. Methods for determining the safety and efficacy can include methods in lab animals and humans.

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. Other reactions use a secondary amine substrate (such as iminodiacetic acid) and can be conducted at substantial equimolar ratios of halomethylaminomethylphosphonic acid or hydroxyaminomethylphosphonic acid to secondary amine reactant without significant formation of bis(phosphonomethyl)amine by-products. Further disclosed is a process for the preparation of hydroxymethylphosphonic acid self-ester dimers, trimers and oligomers by azeotropic dehydration.

Process for the preparation of N-phosphonomethylglycine and derivatives thereof

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.

Hydrolyzable delivery system using cross-linked polymeric resins as vehicles

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.

Alkyl/aryl hydroxy or keto thiepine compounds as inhibitors of apical sodium co-dependent bile acid transport (ASBT) and taurocholate uptake

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.

Method for the preparation of tetrahydrobenzothiepines

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.

Benzothiepines having activity as inhibitors of ileal bile acid transport and taurocholate uptake

Mono-flourinated 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.

Mono- and di-fluorinated benzothiepine compounds as inhibitors of apical sodium co-dependent bile acid transport (ASBT) and taurocholate uptake

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. The invention further provides a method for treatment or prevention of gastric ulcers using a delivery system capable of delivering prostaglandin or prostacyclin drugs, especially misoprostol.

Ph-selective delivery system using crosslinked polymeric resins as vehicles

Gastro-specific prodrugs

Intermediates and processes for the preparation of benzothiepines having activity as inhibitors of ileal bile acid transport and taurocholate uptake

Substituted 5-aryl-benzothiepines having activity as inhibitors of ileal

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 crosslinked polymer, or by attaching a linker to a portion of the subunits of a crosslinked 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 hydrolyzable covalent bond to a linker, which is in turn covalently bonded to a portion of subunits of a crosslinked polymer.

Hydrolyzable delivery system using crosslinked polymeric resins as

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Manchester, MO, United States of America

Samuel J Tremont