[((1R,2S,5R)-2-isopropyl-5-methyl-cyclohexanecarbonyl)-amino]-acetic acid isopropyl ester and related compounds and their use in therapy

Abstract

The present invention pertains generally to the field of coolants and medical therapy. More particularly, the present invention relates to certain anti-nociceptive agents, such as [((1R,2S,5f?)-2-isopropyl-5-methyl-cyclohexanecarbonyl)-amino]-acetic acid isopropyl ester, that are potent and long-acting and selectively cooling for non-keratinized epithelial tissues as compared to keratinized epithelial tissues, and are useful, for example, for the treatment of (e.g., the alleviation of symptoms of; the amelioration of) sensory discomfort of non-keratinized stratified epithelial (NKSE) tissue; and so for treatment of: sensory discomfort of an ocular surface, an eyelid, a margin of an eyelid, an anterior part of an eyeball, a conjunctiva, a lachrymal system, a pre-corneal film, or a cornea, a lining of the oral cavity, an internal portion of the lips, a pharyngeal surface, an esophageal surface, or an anogenital surface; eye discomfort, e.g., caused by extended wear of contact lenses, by eye strain and / or fatigue, by air pollutants, by excessive exposure to the sun, by conjunctivitis, by dry eye syndrome; sensory discomfort associated with oral mucositis; airway (e.g., larynx, trachea, and / or bronchi) tightness, discomfort in the airways (e.g., larynx, trachea, and / or bronchi), choking, cough, and / or dyspnea, e.g., associated with asthma and / or chronic obstructive pulmonary diseases (COPD).

Description

[0001] related application [0002] This application is related to US Patent Application No. 12 / 928,184, filed December 06, 2010, which is hereby incorporated by reference in its entirety. technical field [0003] The present invention relates generally to the fields of coolants and medical treatments. More specifically, the present invention relates to certain anti-nociceptive agents (analgesics, anti-nociceptive agent), such as [((1R,2S,5R)-2-isopropyl-5-methyl-cyclohexanecarbonyl )-amino]-isopropyl acetate, which is effective, long-lasting and selectively cooling on non-keratinized epithelial tissue versus keratinized epithelial tissue, and for example, on non-keratinized stratified epithelial (NKSE) tissue Treatment (eg, relief of symptoms; improvement) of sensory discomfort is useful; so use for: ocular surface, eyelids, eyelid margins, anterior part of the eye, conjunctiva, lacrimal system, epicorneal membrane, or cornea, lining of the mouth, inside of the lips Partial...

AI Technical Summary

Problems solved by technology

However, on nonkeratinizing epithelial cells, menthol's irritating effects limit its use; for example, lozenges containing more than 8 mg menthol per unit taste disgusting

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