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1. 发明申请

US20160250277A1 PERIPHERAL KAPPA OPIOID RECEPTOR AGONISTS FOR PREVENTING, INHIBITING OR TREATING NAUSEA AND VOMITING 审中-公开
标题翻译：外用KAPPA OPIOID受体激素预防，抑制或治疗鼻炎和感冒
公开(公告)号：US20160250277A1
公开(公告)日：2016-09-01
申请号：US15032351
申请日：2014-10-27
申请人： CARA THERAPEUTICS, INC.
发明人： Derek T. CHALMERS , James B. JONES
IPC分类号： A61K38/07 , A61K31/40 , A61K31/485 , A61K9/00
CPC分类号： A61K38/07 , A61K9/0019 , A61K31/40 , A61K31/485 , A61K38/06 , C07K5/1016
摘要： A method for preventing, inhibiting or treating nausea and/or vomiting in a mammalian subject, the method comprising administering an effective amount of a peripherally-restricted kappa opioid receptor agonist to the subject. The nausea and/or vomiting can be associated with use of an opioid, such as morphine or fentanyl. The peripherally-restricted kappa opioid receptor agonist can be an L-amino acid-containing peptide, a D-amino acid-containing peptide, or a synthetic peptide amide, such as for instance, D-Phe-D-Phe-D-Leu-D-Lys-[ω(4-aminopiperidine-4-carboxylic acid)]-OH (CR845).
摘要翻译：一种用于预防，抑制或治疗哺乳动物受试者的恶心和/或呕吐的方法，所述方法包括向所述受试者施用有效量的外周受限的κ阿片受体激动剂。恶心和/或呕吐可能与阿片类药物（如吗啡或芬太尼）的使用有关。外周受限制的κ阿片受体激动剂可以是含L-氨基酸的肽，含有D-氨基酸的肽或合成肽酰胺，例如D-Phe-D-Phe-D-Leu -D-Lys- [ω（4-氨基哌啶-4-羧酸）] -OH（CR845）。

2. 发明申请

US20160310558A1 USES OF KAPPA OPIOID SYNTHETIC PEPTIDE AMIDES 审中-公开
标题翻译： KAPPA OPIOID合成肽类药物的使用
公开(公告)号：US20160310558A1
公开(公告)日：2016-10-27
申请号：US15137033
申请日：2016-04-25
申请人： Cara Therapeutics, Inc.
发明人： Claudio D. SCHTEINGART , Frédérique MENZAGHI , Guangcheng JIANG , Roberta Vezza ALEXANDER , Javier SUEIRAS-DIAZ , Robert H. SPENCER , Derek T. CHALMERS , Robert Zhiyong LUO
IPC分类号： A61K38/07 , A61K38/08
CPC分类号： A61K38/07 , A61K38/08 , C07K5/101 , C07K5/1016 , C07K5/1019 , C07K7/02
摘要： The invention relates to methods of use of synthetic peptide amides that are ligands of the kappa opioid receptor in the treatment and prevention of kappa opioid receptor-associated diseases and conditions; and particularly to uses of these agonists in the prophylaxis, inhibition and treatment of pain, inflammation and pruritis associated with a variety of diseases, disorders and conditions. Inflammatory conditions preventable or treatable by the methods of the invention include diseases and conditions associated with elevated levels of a proinflammatory cytokines, such as TNF-α, IL-1β, IL-6, MMP-1 and MMP-3. Such diseases and conditions include cardiovascular inflammation, neurological inflammation, skeletal inflammation, muscular inflammation, gastrointestinal inflammation, ocular inflammation, otic inflammation, inflammation due to insect bites and inflammation due to wound healing; atherosclerosis, ischemia, restenosis and vasculitis; of asthma, Sjogren's syndrome, pulmonary inflammation, chronic airway inflammation and chronic obstructive pulmonary disease (COPD), allergy, psoriasis, psoriatic arthritis, eczema, scleroderma, atopic dermatitis and systemic lupus erythematosus, arthritis, synovitis, osteomyelitis, rheumatoid arthritis, osteoarthritis and ankylosing spondylitis; septicemia and septic shock, diabetes, glucose intolerance, insulin resistance and obesity, colitis, ulcerative colitis, Crohn's disease, IBD and IBS, and the inflammatory diseases and conditions due to tumor proliferation, tumor metastasis or transplantation rejection.
摘要翻译：本发明涉及使用作为κ阿片样物质受体的配体的合成肽酰胺在治疗和预防κ阿片受体相关疾病和病症中的使用方法; 特别是这些激动剂在预防，抑制和治疗与各种疾病，病症和病症相关的疼痛，炎症和瘙痒症中的用途。通过本发明的方法可预防或治疗的炎症状态包括与升高的促炎细胞因子如TNF-α，IL-1β，IL-6，MMP-1和MMP-3水平相关的疾病和病症。这些疾病和病症包括心血管炎症，神经炎症，骨骼炎症，肌肉炎症，胃肠道炎症，眼部炎症，耳炎，由于昆虫叮咬引起的炎症和由于伤口愈合引起的炎症; 动脉粥样硬化，局部缺血，再狭窄和血管炎; 哮喘，干燥综合征，肺部炎症，慢性气道炎症和慢性阻塞性肺病（COPD），过敏，牛皮癣，银屑病关节炎，湿疹，硬皮病，特应性皮炎和系统性红斑狼疮，关节炎，滑膜炎，骨髓炎，类风湿性关节炎，骨关节炎和强直性脊柱炎; 败血病和败血性休克，糖尿病，葡萄糖不耐受，胰岛素抵抗和肥胖，结肠炎，溃疡性结肠炎，克罗恩病，IBD和IBS，以及由于肿瘤增殖，肿瘤转移或移植排斥引起的炎症疾病和病症。

3. 发明申请

US20150152138A1 USES OF KAPPA OPIOID SYNTHETIC PEPTIDE AMIDES 审中-公开
标题翻译： KAPPA OPIOID合成肽类药物的使用
公开(公告)号：US20150152138A1
公开(公告)日：2015-06-04
申请号：US14557576
申请日：2014-12-02
申请人： Cara Therapeutics, Inc.
发明人： Claudio D. SCHTEINGART , Frédérique MENZAGHI , Guangcheng JIANG , Roberta Vezza ALEXANDER , Javier SUEIRAS-DIAZ , Robert H. SPENCER , Derek T. CHALMERS , Robert Zhiyong LUO
IPC分类号： C07K5/11
CPC分类号： A61K38/07 , A61K38/08 , C07K5/101 , C07K5/1016 , C07K5/1019 , C07K7/02
摘要： The invention relates to methods of use of synthetic peptide amides that are ligands of the kappa opioid receptor in the treatment and prevention of kappa opioid receptor-associated diseases and conditions; and particularly to uses of these agonists in the prophylaxis, inhibition and treatment of pain, inflammation and pruritis associated with a variety of diseases, disorders and conditions. Inflammatory conditions preventable or treatable by the methods of the invention include diseases and conditions associated with elevated levels of a proinflammatory cytokines, such as TNF-α, IL-1β, IL-6, MMP-1 and MMP-3. Such diseases and conditions include cardiovascular inflammation, neurological inflammation, skeletal inflammation, muscular inflammation, gastrointestinal inflammation, ocular inflammation, otic inflammation, inflammation due to insect bites and inflammation due to wound healing; atherosclerosis, ischemia, restenosis and vasculitis; of asthma, Sjogren's syndrome, pulmonary inflammation, chronic airway inflammation and chronic obstructive pulmonary disease (COPD), allergy, psoriasis, psoriatic arthritis, eczema, scleroderma, atopic dermatitis and systemic lupus erythematosus, arthritis, synovitis, osteomyelitis, rheumatoid arthritis, osteoarthritis and ankylosing spondylitis; septicemia and septic shock, diabetes, glucose intolerance, insulin resistance and obesity, colitis, ulcerative colitis, Crohn's disease, IBD and IBS, and the inflammatory diseases and conditions due to tumor proliferation, tumor metastasis or transplantation rejection.
摘要翻译：本发明涉及使用作为κ阿片样物质受体的配体的合成肽酰胺在治疗和预防κ阿片受体相关疾病和病症中的使用方法; 特别是这些激动剂在预防，抑制和治疗与各种疾病，病症和病症相关的疼痛，炎症和瘙痒症中的用途。通过本发明的方法可预防或治疗的炎性病症包括与升高的促炎细胞因子如TNF-α，IL-1和bgr，IL-6，MMP-1和MMP-3水平相关的疾病和病症。这些疾病和病症包括心血管炎症，神经炎症，骨骼炎症，肌肉炎症，胃肠道炎症，眼部炎症，耳炎，由于昆虫叮咬引起的炎症和由于伤口愈合引起的炎症; 动脉粥样硬化，局部缺血，再狭窄和血管炎; 哮喘，干燥综合征，肺部炎症，慢性气道炎症和慢性阻塞性肺病（COPD），过敏，牛皮癣，银屑病关节炎，湿疹，硬皮病，特应性皮炎和系统性红斑狼疮，关节炎，滑膜炎，骨髓炎，类风湿性关节炎，骨关节炎和强直性脊柱炎; 败血病和败血性休克，糖尿病，葡萄糖不耐受，胰岛素抵抗和肥胖，结肠炎，溃疡性结肠炎，克罗恩病，IBD和IBS，以及由于肿瘤增殖，肿瘤转移或移植排斥引起的炎症疾病和病症。

4. 发明申请

US20180078605A1 PERIPHERAL KAPPA OPIOID RECEPTOR AGONISTS FOR UREMIC PRURITUS IN DIALYSIS PATIENTS 审中-公开
公开(公告)号：US20180078605A1
公开(公告)日：2018-03-22
申请号：US15811199
申请日：2017-11-13
申请人： Cara Therapeutics, Inc.
发明人： Robert H. SPENCER , Frédérique MENZAGHI , Derek T. CHALMERS
IPC分类号： A61K38/07 , C07K7/02 , C07K5/107 , A61K38/08 , C07K5/11 , C07K5/103
CPC分类号： A61K38/07 , A61K9/0019 , A61K31/4453 , A61K38/08 , C07K5/0205 , C07K5/101 , C07K5/1016 , C07K5/1019 , C07K7/02
摘要： The invention provides a method of prevention, inhibition or treatment of uremic pruritus in a dialysis patient by administering an effective amount of a kappa opioid receptor agonist. Also provided is a method of inhibition or treatment of adverse symptoms associated with dialysis affecting the quality of life of dialysis patient, the method includes administering an effective amount of a kappa opioid receptor agonist. The adverse symptoms associated with dialysis addressable by the methods of the invention include uremic pruritus, sleep disruption, depression and other mood alterations.

5. 发明申请

US20170007574A1 PERIPHERAL KAPPA OPIOID RECEPTOR AGONISTS FOR UREMIC PRURITUS IN DIALYSIS PATIENTS 审中-公开
标题翻译：尿崩症患者外周血KAPPA OPIOID受体激素
公开(公告)号：US20170007574A1
公开(公告)日：2017-01-12
申请号：US15193837
申请日：2016-06-27
申请人： Cara Therapeutics, Inc.
发明人： Robert H. SPENCER , Frédérique MENZAGHI , Derek T. CHALMERS
IPC分类号： A61K31/40 , A61K9/00
CPC分类号： A61K9/0019 , A61K31/451 , A61K38/07
摘要： The invention provides a method of prevention, inhibition or treatment of uremic pruritus in a dialysis patient by administering an effective amount of a kappa opioid receptor agonist. Also provided is a method of inhibition or treatment of adverse symptoms associated with dialysis affecting the quality of life of dialysis patient, the method includes administering an effective amount of a kappa opioid receptor agonist. The adverse symptoms associated with dialysis addressable by the methods of the invention include uremic pruritus, sleep disruption, depression and other mood alterations.
摘要翻译：本发明提供了一种通过施用有效量的κ阿片受体激动剂来预防，抑制或治疗透析患者尿毒症瘙痒症的方法。还提供了抑制或治疗与影响透析患者的生活质量的透析相关的不良症状的方法，该方法包括施用有效量的κ阿片受体激动剂。与通过本发明的方法可寻址的透析相关的不良症状包括尿毒症瘙痒，睡眠中断，抑郁和其他情绪改变。

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