Alteon Incorporated

The Picower Institute for Medical Research

Other

The United States of America As Represented by the Department of Health

The United States of America

Synvista Therapeutics, Inc.

John J Egan

Dilip R Wagle

Sara Vasan

Anthony Cerami

Peter C Ulrich

San-Bao Hwang

Taikyun Rho

Sheng-Ding Fang

Constantine Londos

Edmond Joseph LaVoie

Stanley Charles Bell

Martin Gall

Sheng Ding Fang

John Resek

Ihor Terleckyj

Alan R Kimmel

Andrew S Greenberg

Provided is a method of treating or ameliorating or preventing glaucoma, decreasing intraocular pressure or improving or amemliorting ocular accommodation in an animal, including a human comprising administering an intraocular pressure decreasing or accommodation improving amount of a compound of the formula I: 

Method for treating glaucoma IC

Provided, among other things, is a method of treating or ameliorating or preventing an indication of the invention in an animal, including a human comprising administering an effective amount of a compound of the formula I: 

Method for treating fibrotic diseases and other indications

The present invention relates to compositions and methods for inhibiting and reversing nonenzymatic cross-linking (protein aging). Accordingly, compositions are disclosed which comprise an agent capable of inhibiting the formation of advanced glycosylation endproducts of target proteins, and which additionally reverse pre-formed crosslinks in the advanced glycosylation endproducts by cleaving alpha-dicarbonyl-based protein crosslinks present in the advanced glycosylation endproducts. Certain useful agents are thiazolium salts. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated. A novel immunoassay for detection of the reversal of the nonenzymatic crosslinking is also disclosed.

Preventing and reversing the formation of advance glycosylation endproducts

The present invention relates to compositions and methods for reversing advanced glycosylation end product-mediated cross-linking and protein aging. Accordingly, compositions are described which comprise thiazolium compounds substituted with heterocyclic groups which are capable of reversing the formation of advanced glycosylation end product cross-links. Both industrial and therapeutic applications for the invention are disclosed, as food spoilage and animal protein aging can be treated. Such compounds have particular application in the treatment of protein aging such as is responsible for the complications of aging and diabetes.

Reversing advanced glycosylation cross-links using heterocyclic-substituted thiazolium compounds

Glucose and lipid lowering compounds

The present invention relates to compositions and methods for inhibiting and reversing nonenzymatic cross-linking (protein aging). Accordingly, compositions are disclosed which comprise an agent capable of inhibiting the formation of advanced glycosylation endproducts of target proteins, and which additionally reverse pre-formed crosslinks in the advanced glycosylation endproducts by cleaving alpha-dicarbonyl-based protein crosslinks present in the advanced glycosylation endproducts. Certain agents useful are thiazolium salts. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated. A immunoassay for detection of the reversal of the nonenzymatic crosslinking is also disclosed.

Method of treating certain indications associated with hyperglycemia

Provided are, among other things, lipid-lowering or glucose-lowering methods and compounds, particularly lipid-lowering or glucose-lowering compounds, with an A-B ring structure as follows:

Reversing advanced glycosylation cross-links using

The present invention provides isolated nucleic acid sequences, i.e., polynucleotides, which encode a family of perilipin proteins. The present invention also provides isolated, substantially purified perilipin proteins which are useful as markers for differentiating true adipocytes from non-adipocyte cells which, as a result of pathophysiological conditions, assume adipocyte characteristics and become lipid-laden. The present invention further provides methods for producing a substantially purified perilipin protein and methods for detecting the presence of such perilipin proteins in a biological samples.

Cloning of perilipin proteins

The present invention relates to compositions and methods for inhibiting and reversing nonenzymatic cross-linking (protein aging). Accordingly, compositions are disclosed which comprise an agent capable of inhibiting the formation of advanced glycosylation endproducts of target proteins, and which additionally reverse pre-formed crosslinks in the advanced glycosylation endproducts by cleaving alpha-dicarbonyl-based protein crosslinks present in the advanced glycosylation endproducts. Certain agents useful are thiazolium salts. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated. A novel immunoassay for detection of the reversal of the nonenzymatic crosslinking is also disclosed.

Reversing the formation of advanced glycosylation endproducts

Preventing and reversing the formation of advanced glycosylation

The present invention relates to compositions and methods for inhibiting and reversing nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises a thiazolium compound capable of inhibiting, and to some extent reversing, the formation of advanced glycosylation endproducts of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated. A novel immunoassay for detection of the reversal of the nonenzymatic crosslinking is also disclosed.

Preventing and reversing advanced glycosylation endproducts

A method for assaying protein kinases that phosphorylate peptides such as Kemptide, such as cAMP-dependent protein kinase, or a glycogen synthase peptide, which is an excellent substrate for protein kinase C. Upon sequentially processing of reaction mixtures through tandem columns of cation and anion exchange resins improved separation of ATP from phosphorylated peptides is achieved such that radioactivity in background samples is nearly nil and the yield of phosphorylated peptides is high. This method is generally applicable to any protein kinase so long as the substrate peptide is appropriately structured such that the peptide retains a net positive charge when fully phosphorylated so that the peptide will adhere to the cation exchange resin and pass through the anion exchange resin. This method reduces labor, radioactivity, enzyme requirements, and costs of assaying protein kinases.

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New York, NY, United States of America

John J Egan