Montefiore Medical Center

City of Hope

Albert Einstein College of Medicine

Research, Incorporated

Montefiore Hospital and Medical Center

Iraj Lalezari

Parviz Lalezari

Samuel Rahbar

Eli Seifter

Jacques Padawer

Francis F Foldes

The nonenzymatic glycation and crosslinking of proteins is a part of the aging process with the glycation endproducts and crosslinking of long-lived proteins increasing with age. This process is increased at elevated concentrations of reducing sugars in the blood and in the intracellular environment such as occurs with diabetes. The structural and functional integrity of the affected molecules become disturbed by these modifications and can result in severe consequences. The compounds of the present invention can be used to inhibit this process of nonenzymatic glycation and therefore to inhibit some of the ill effects caused by diabetes or by aging. The compounds are also useful for preventing premature aging, spoilage of proteins in food and can prevent discoloration of teeth.

Inhibitors of formation of advanced glycation endproducts (AGEs)

The nonenzymatic glycation and crosslinking of proteins is a part of the aging process with the glycation endproducts and crosslinking of long-lived proteins increasing with age. This process is increased at elevated concentrations of reducing sugars in the blood and in the intracellular environment such as occurs with diabetes. The structural and functional integrity of the affected molecules become perturbed by these modifications and can result in severe consequences. The compounds of the present invention can be used to inhibit this process of nonenzymatic glycation and therefore to inhibit some of the ill effects caused by diabetes or by aging. The compounds are also useful for preventing premature aging, spoilage of proteins in food and can prevent discoloration of teeth.

Inhibitors of formation of advanced glycation endproducts (AGES)

Derivatives of aryl and heterocyclic ureido and aryl and heterocyclic carboxamido phenoxy isobutyric acids have been found to inhibit the nonenzymatic glycation of proteins which often results in formation of advanced glycation endproducts and crosslinks. Many other phenoxyisobutyric acid derivatives as well as certain other compounds as set out in this disclosure also have been found to inhibit the nonenzymatic glycation of proteins. The nonenzymatic glycation and crosslinking of proteins is a part of the aging process with the glycation endproducts and crosslinking of long-lived proteins increasing with age. This process is increased at elevated concentrations of reducing sugars in the blood and in the intracellular environment such as occurs with diabetes. The structural and functional integrity of the affected molecules become perturbed by these modifications and can result in severe consequences. The compounds of the present invention can be used to inhibit this process of nonenzymatic glycation and therefore to inhibit some of the ill effects caused by diabetes or by aging. The compounds are also useful for preventing premature aging, spoilage of proteins in food and can prevent discoloration of teeth.

The present invention provides a chemically modified form of hemoglobin that is stabilized and can efficiently bind and release oxygen. In addition the chemically modified hemoglobin may be polymerized to increase its molecular weight and increase its stability so that it will have a longer half life in the circulatory system and may be used as a stable oxygen transport mediator which is useful as the basis of a blood substitute.

Compounds for preparing modified hemoglobin

Modified hemoglobin and its use as a component of an artificial blood

A new process is disclosed for the preparation of esters of polyhydroxy compounds having three or more hydroxy compounds. The process is based on the reaction with an alkyl chloroformate to form a mixed anhydride which is contacted with a polyol.

Method of synthesizing polyesters

The present invention is concerned with a method for treating hemoglobin or blood in vivo or in vitro to modify the affinity of hemoglobin for oxygen, said method comprising causing an effective amount of a substituted arylureidophenoxymethyl propionic acid to come in contact with hemoglobin.

Method of synthesis and novel compounds for pharmaceutical uses

A method for improving the quality of an aliment, such as an alcoholic liquor, by removing impurities such as carbamates, sulfites and bioamines, includes contacting an aliment containing the impurity with a container formed of a membrane permeable to the impurity. The container encloses a non-diffusible reactant such as binding agents, neutralizing agents, oxidizing agents, transesterifying agents and hydrolyzing agents. The container and the contents are separated from the aliment after a period of time sufficient for the reactants to react with the impurity.

Method and system for removing impurities from aliments

The present invention is concerned with a process for the synthesis of substituted arylureidophenoxymethyl propionic acids and an analogous benzamides series of compounds which have activity in the dissociation of oxygen from hemoglobin. In addition the process may be utilized to prepare compounds which are known.

Novel compounds are disclosed which have the formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 may be the same or different and independently selected from the group consisting of hydrogen, halogen, straight and branched chain alkyl of from 1-6 carbon atoms, aryl, cycloalkyl of 4 to 7 carbon atoms; and alkoxy of 1 to 6 carbon atoms; R.sub.5 and R.sub.6 may be the same or different and are selected from the group consisting of hydrogen, halogen, straight and branched chain alkyl groups of from 1-6 carbon atoms, aralkyl groups wherein the alkyl portion has from 1-6 carbon atoms cycloalkyl of from 4-7 carbon atoms and aryl; R.sub.7 is hydrogen or a straight or branched chain alkyl group of 1-6 carbon atoms and the pharmaceutically acceptable salts thereof. These compounds are useful for the treatment of hyperlipidemia and for the in vivo and in vitro treatment of hemoglobin or blood to modify the affinity of hemoglobin for oxygen.

Compound, composition and method for the reduction of lipids the

The present invention is concerned with a process for the synthesis of substituted arylureidophenexymethyl propionic acids and an analogous benzamides series of compounds which have activity in the dissociation of oxygen from hemoglobin. In addition the process may be utilized to prepare compounds which are known.

The present invention is concerned with a process for the synthesis of substituted arylureidophenexymethyl propionic acids and an analogous benzamides series of compounds which have activity in the dissociation of oxygen from hemoglobin. In addition, the process may be utilized to prepare compounds which are known.

The invention relates to the preparation of an ester or an amide from an anhydride with an alcohol or an amine, wherein the anhydride is first prepared by reacting an acid and an alkyl chloroformate in a 100% aqueous medium, that is, 100% water.

Process for the synthesis of esters and amides of carboxylic acids

This invention relates to a method for antagonizing induced the neuromuscular blocking effects of certain therapeutic agents and pathological disorders in mammals, which comprises administering to said mammal an antagonizing-effective amount of a compound of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each hydrogen, alkyl, alkenyl, alkynyl, aryl, aralkyl, cycloalkyl, cycloalkyl-lower alkyl or hydroxyalkyl, or, when taken together, form a heterocyclic ring with the nitrogen to which they are attached, with the proviso that both are not hydrogen;

Anti-curare agents

Mixed anhydrides products are described. These mixed anhydrides are produced by reaction of a carboxylic acid-containing steroid with a material having the formula: ##STR1## wherein: X is a halogen

Growing community of inventors

Scarsdale, NY, United States of America

Iraj Lalezari