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    • 100. 发明授权
    • [((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-异丙基-5-甲基 - 环己烷羰基) - 氨基] - 乙酸异丙酯和相关化合物及其在治疗中的用途
    • US08426463B2
    • 2013-04-23
    • US13065971
    • 2011-04-04
    • Edward T. Wei
    • Edward T. Wei
    • A61K31/223A61K31/196A61K9/20A61K9/68A61P11/02A61P11/04
    • A61K9/0056A61K9/0048A61K9/2018A61K31/24
    • 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).
    • 本发明一般涉及冷却剂和药物治疗领域。 更具体地,本发明涉及某些抗伤害感受剂,例如[((1R,2S,5R)-2-异丙基-5-甲基 - 环己烷羰基) - 氨基] - 乙酸异丙酯,其是有效的和长的 与角质化的上皮组织相比,对非角质化上皮组织的作用和选择性冷却,并且可用于例如非角质化分层上皮的治疗(例如,减轻症状,改善)感觉不适 (NKSE)组织; 因此用于治疗:眼表面,眼睑,眼睑边缘,眼球前部,结膜,泪液系统,角膜前角膜或角膜的感觉不适, 口腔,嘴唇的内部,咽表面,食管表面或肛门表面; 由眼睛疲劳和/或疲劳,空气污染物,过度暴露于阳光,结膜炎,干眼综合征引起的眼睛不适; 与口腔粘膜炎相关的感觉不适; 呼吸道(例如喉,气管和/或支气管)紧张,气道不适(例如喉,气管和/或支气管),窒息,咳嗽和/或呼吸困难,例如与哮喘和/或慢性相关 阻塞性肺疾病(COPD)。