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

A technology of cyclohexane carbonyl and isopropyl acetate, which can be used in medical preparations containing active ingredients, drug combinations, organic chemistry, etc., and can solve the problems of restricting applications due to irritating effects and nauseating taste of lozenges, etc.

Active Publication Date: 2013-10-02
AXALBION SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, on nonkeratinizing epithelial cells, menthol's irritating effects limit its

Method used

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

[0029] Compound

[0030] The inventors have discovered that certain compounds are surprisingly and unexpectedly effective cooling agents for non-keratinized stratified epithelial (NKSE) tissues. Compared with keratinized epithelial tissues, these compounds are effective and long-lasting and selective cooling for non-keratinized epithelial tissues.

[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

[0033] [((1R,2S,5R)-2-isopropyl-5-methyl-cyclohexanecarbonyl)-methyl-amino]-isopropyl acetate ("N-Gly-O-iPr");

[0034] And its pharmaceutically acceptable salts, hydrates, and solvates.

[0035] Thus, one aspect of the present invention is the following compound:

[0036] [((1R,2S,5R)-2-isopropyl-5-methyl-cyclohexanecarbonyl)-amino]-isopropyl acetate ("Gly-O-iPr") or

[0037] [((1R,2S,5R)-2-isopropyl-5-methyl-cyclohexa...

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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,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 ...

Claims

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Application Information

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IPC IPC(8): C07C233/63A61K31/223A61P11/00A61P27/02
CPCA61P11/00A61P11/14A61P17/04A61P27/02C07B2200/07C07C233/63C07C2601/14A61K31/223
Inventor 魏德烽
Owner AXALBION SA
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