[((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,5R)-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 relates to US Patent Application No. 12 / 928,184 filed on December 06, 2010, the entire content of which is incorporated herein by reference. Technical field [0003] The present invention generally relates to the field of coolants and drug therapy. More specifically, the present invention relates to certain anti-nociceptive agents (analgesics, anti-nociceptive agents), such as [((1R,2S,5R)-2-isopropyl-5-methyl-cyclohexanecarbonyl )-Amino]-isopropyl acetate, compared to keratinized epithelial tissue, this is effective, long-lasting and selective cooling for non-keratinized epithelial tissue, and for example, for non-keratinized stratified epithelial (NKSE) tissue The treatment of discomfort (such as symptom relief; improvement) is useful; therefore, it is used to treat: eye surface, eyelid, eyelid edge, front of eyeball, conjunctiva, lacrimal system, corneal membrane, or cornea, oral cavity, inner lips Discomfort on the surface ...

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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