The present invention relates to N-acyl derivatives of amino acids and pharmaceutically acceptable salts thereof ##STR00001## wherein n is 2 or 3; and R.sub.1 represents ##STR00002## or pharmaceutically acceptable salts thereof, to novel processes for preparing the same, to use thereof as anti-allergic, anti-anaphylactic, anti-inflammatory and hypolipidemic agents as well as to a pharmaceutical composition comprising the indicated compounds in an efficient amount and to a method for treating allergic and inflammatory diseases and lipid metabolism disorders: bronchial asthma, allergic rhinitis, pollinoses, seasonal and year-round rhinitis, allergic pneumonitis, atopic dermatitis, psoriasis, urticaria, allergic (including anaphylactic) reactions to insect stings and medicaments, cold allergy, allergic conjunctivitis, atherosclerosis, obesity, ischemic heart and cerebral disease, myocardial infarction and stroke.

Otkrytoe Aktsionernoe Obschestvo-Otechestvennye Lekarstva

N-acyl amino acid derivatives, a method for the preparation thereof, a pharmaceutical composition and use thereof as anti-allergic, anti-inflammatory and hypolipidemic agents

Nebolsin; Vladimir Evgenievich

Kromova; Tatyana Alexandrovna

Zheltukhina; Galina Alexandrovna

Kovaleva; Violetta Leonidovna

Otkrytoe Aktsionernoe Obschestvo Otechestvennye Lekarstva

Vladimir Evgenievich Nebolsin

N-acylic aminoacid derivatives, method for the production thereof, pharmacological composition and the use in the form anti-allergic, anti-inflammatory and hypolipidemic agents

Provided herein is technology relating to deuterated amiexanox and particularly, but not exclusively, to compositions comprising deuterated amiexanox, methods of producing deuterated amiexanox, and uses of deuterated amiexanox. Provided herein are deuteratecl amiexanox compounds for the treatment of obesity, insulin resistance, diabetes, and steatosis. In addition, the deuterated compounds are anti-inflammatory antiallergic immunomodulators. e.g., for the treatment of diseases associated with inflammation. The deuterium kinetic isotope effect associated with placing deuterium at the site of metabolic derivatization slows metabolic derivatization and thus increases the lifetime of the active drug in vivo.

THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Deuterated amlexanox

anti allergic

obesity

anti allergic/obesity

N-acyl amino acid derivatives, a method for the preparation thereof, a pharmaceutical composition and use thereof as anti-allergic, anti-inflammatory and hypolipidemic agents

N-acylic aminoacid derivatives, method for the production thereof, pharmacological composition and the use in the form anti-allergic, anti-inflammatory and hypolipidemic agents

Deuterated amlexanox

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