Geltex Pharmaceuticals, Inc.

Genzyme Corporation

Hyperion Catalysis International, Inc.

Geltex, Inc.

Geltex Pharmaceutical, Inc.

W Harry Mandeville, Iii

Stephen Randall Holmes-Farley

Venkata R Garigapati

Thomas X Neenan

George M Whitesides

Chad Cori Huval

John S Petersen

Howard G Tennent

Larry K Truesdale

Molly Kate Boie

Pradeep K Dhal

Thomas Henry Jozefiak

Xinhua Li

Richard Fitzpatrick

Keith K Shackett

Danny Concagh

James J Barber

Caroline Isabelle Bacon Kurtz

Carl Snyder

Dennis I Goldberg

Steven K Burke

Steven C Polomoscanik

Jeffrey D Klinger

Philip J Goddard

Phosphate-binding polymers are provided for removing phosphate from the gastrointestinal tract. The polymers are orally administered, and are useful for the treatment of hyperphosphatemia.

Phosphate-binding polymers for oral administration

The invention relates to a method for removing bile salts from a patient in need thereof and compositions useful in the method. The method comprises administering to the patient a therapeutically effective amount of a salt of an alkylated and crosslinked polymer. The alkylated and crosslinked polymer salt comprises the reaction product of crosslinked polymers, or salts and copolymers thereof having amine containing repeat units, with at least one aliphatic alkylating agent.

Alkylated poly(allylamine) polymers and methods of use

The invention relates to a method for reducing serum cholesterol in a patient in need thereof and alkylated and crosslinked poly(allylamine) polymers useful in the method. The alkylated and crosslinked poly(allylamine) polymers are crosslinked with epichlorohydrin and comprise at least some n-decyl substituted nitrogen atoms and at least some hexyltrimethyl ammonium substituted nitrogen atoms.

Process for removing bile salts from a patient and alkylated compositions therefor

Disclosed is a phenyl boronic acid compound represented by Structural Formula (I):  Ar is a substituted or unsubstituted aryl group. Also disclosed is a method of treating obesity in a subject by administering an effective amount of a compound represented by Structural Formula (I) and a pharmaceutical composition comprising the compound and a pharmaceutically acceptable carrier or diluent.

Aryl boronic acids for treating obesity

The present invention relates to a method for treating obesity, a method for reducing the absorption of dietary fat, and a method for treating hypertriglyceridemia in a patient and to particular polymers for use in the methods or in a manufacture of a medicament. The methods comprise the step of orally administering to a mammal, such as a human, a therapeutically effective amount of one or more fat-binding polymers. The administration of the fat-binding polymer of the invention facilitates the removal of fat from the body prior to digestion, with minimal side effects and low toxicity. In a preferred embodiment, the one or more fat-binding polymers are administered in combination with one or more lipase inhibitors, for example, lipstatin and tetrahydrolipstatin.

Fat-binding polymers

Disclosed are polymers comprising one or more phenyl boronate ester, boronamide or boronate thioester groups. The phenyl boronate ester, boronamide and boronate thioester groups are represented by one of the following structural formulas:  Ar in Structural Formulas (I) and (II) is substituted or unsubstituted; and each Z is &#x2014;O&#x2014;, &#x2014;NH&#x2014; or &#x2014;S&#x2014; and is independently selected. Pharmaceutically acceptable salts of the polymer are also included. The aryl boronate ester, boronamide or boronate thioester can be cleaved to release the corresponding aryl boronic acid. Also disclosed are pharmaceutical compositions comprising the polymers of the present invention and a pharmaceutically acceptable carrier or diluent; and methods of treating a subject for obesity with the polymers of the present invention.

Aryl boronate functionalized polymers for treating obesity

The invention features a method for treating obesity in a patient by administering to the patient a polymer that has been substituted with one or more groups that inhibit lipases, which are enzymes responsible for the hydrolysis of fat. The invention further relates to the polymers employed in the methods described herein as well as novel intermediates and methods for preparing the polymers.

Lipase inhibiting polymers

Disclosed is a phenyl boronic acid compound represented by Structural Formula (I): Also disclosed is a method of treating obesity in a subject by administering an effective amount of a compound represented by Structural Formula (I) and a pharmaceutical composition comprising the compound and a pharmaceutically acceptable carrier or diluent.

Method of making phosphate-binding polymers for oral administration

A method for treating a microbial infection in a mammal, such as a human, comprising treating the mammal with a therapeutically effective amount of a polymer comprising an amino group or an ammonium group attached to the polymer backbone via an aliphatic spacer group. The polymer can be a homopolymer or a copolymer. In one embodiment, the polymer is a copolymer comprising a monomer having a pendant ammonium group and a hydrophobic monomer.

Ionic polymers as anti-infective agents

The present invention relates to a method for lowering the serum phosphate level of a patient. The method comprises the step of administering to the patient a therapeutically effective amount of a polymer characterized by a diallylamine monomer or repeat unit. The amino nitrogen atom of the diallylamine repeat unit can be substituted by one or two substituents independently selected from among substituted and unsubstituted, normal, branched and cyclic alkyl groups, and aryl groups. When the diallylamine repeat unit comprises an ammonium or quaternary ammonium group, the monomer will further comprise a suitable anion, such as a conjugate base of a pharmaceutically acceptable acid.

Poly (diallylamines)-based phosphate binders

A method for treating pathogenic toxins in a mammal, such as a human, comprising treating the mammal with a therapeutically effective amount of a polymer comprising a cationic group attached to the polymer backbone. The polymer can be a homopolymer or a copolymer. In one embodiment, the polymer is a copolymer comprising a monomer having a pendant ammonium group and a hydrophobic monomer.

Ionic polymers as toxin-binding agents

Iron binding polymers are provided for decreasing the absorption of iron from the gastrointestinal tract. The polymers are orally administered, and are useful for treatment of iron overload disorders.

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Lynnfield, MA, United States of America

W Harry Mandeville, Iii