[((1R,2S,5R)-2-isopropyl-5-methyl-cyclohexanecarbonyl)-amino]-acetic acid isopropyl ester and related compounds and their use in therapy
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A technology of cyclohexane carbonyl compound, which is applied in the field of coolant and drug therapy, can solve the problems of lozenge, nausea, irritation, limited application, etc.
Active Publication Date: 2015-06-17
AXALBION SA
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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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[0029] compound
[0030] The present inventors have discovered that certain compounds are surprising and unexpectedly effective cooling agents for non-keratinized stratified epithelial (NKSE) tissue. These compounds are effective and long-acting and selectively cooling on non-keratinized epithelial tissue compared to keratinized epithelial tissue.
[0031] These compounds are collectively referred to herein as "isopropyl ester compounds" or "IPE compounds" and are:
[0032] [((1R,2S,5R)-2-Isopropyl-5-methyl-cyclohexanecarbonyl)-amino]-isopropyl acetate ("Gly-O-iPr") and
[0034] And its pharmaceutically acceptable salts, hydrates, and solvates.
[0035] Thus, one aspect of the invention is the following compounds:
[0036] [((1R,2S,5R)-2-Isopropyl-5-methyl-cyclohexanecarbonyl)-amino]-isopropyl acetate ("Gly-O-iPr") or
[0037] [((1R,2S,5R)-2-Isopropyl-5-methyl-...
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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...
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