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公开(公告)号：US20090156508A1
公开(公告)日：2009-06-18
申请号：US12119311
申请日：2008-05-12
申请人： Claudio D. Schteingart , Frederique Menzaghi , Guangcheng Jiang , Roberta Vezza Alexander , Javier Sueiras-Diaz , Robert H. Spencer , Derek T. Chalmers , Zhiyong Luo
发明人： Claudio D. Schteingart , Frederique Menzaghi , Guangcheng Jiang , Roberta Vezza Alexander , Javier Sueiras-Diaz , Robert H. Spencer , Derek T. Chalmers , Zhiyong Luo
CPC分类号： C07K5/1016 , C07K7/02
摘要： The invention relates to synthetic peptide amides that are ligands of the kappa opioid receptor and particularly to agonists of the kappa opioid receptor that exhibit low P450 CYP inhibition and low penetration into the brain. The synthetic peptide amides of the invention conform to the structure: wherein Xaa is a D-amino acid and G is selected from the following three groups: The compounds are useful in the prophylaxis and treatment of pain, pruritis and inflammation associated with a variety of diseases and conditions.
摘要翻译： 本发明涉及作为κ阿片受体的配体的合成肽酰胺，特别是涉及低P450 CYP抑制和低渗透入脑的κ阿片样物质受体的激动剂。 本发明的合成肽酰胺符合以下结构：其中Xaa是D-氨基酸，G选自以下三组：所述化合物可用于预防和治疗与各种各样的相关的疼痛，瘙痒和炎症 疾病和病症。
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公开(公告)号：US20090075907A1
公开(公告)日：2009-03-19
申请号：US12176279
申请日：2008-07-18
申请人： Claudio D. Schteingart , Frederique Menzaghi , Guangcheng Jiang , Roberta Vezza Alexander , Javier Sueiras-Diaz , Robert H. Spencer , Derek T. Chalmers , Zhiyong Luo
发明人： Claudio D. Schteingart , Frederique Menzaghi , Guangcheng Jiang , Roberta Vezza Alexander , Javier Sueiras-Diaz , Robert H. Spencer , Derek T. Chalmers , Zhiyong Luo
CPC分类号： C07K5/1016 , A61K38/00 , A61K38/07 , C07K5/10 , C07K5/1008 , C07K5/101 , C07K7/02
摘要： The invention relates to synthetic peptide amide ligands of the kappa opioid receptor and particularly to agonists of the kappa opioid receptor that exhibit low P450 CYP inhibition and low penetration into the brain. The synthetic peptide amides of the invention conform to the structure of formula I: Pharmaceutical compositions containing these compounds are useful in the prophylaxis and treatment of pain and inflammation associated with a variety of diseases and conditions. Such treatable pain includes visceral pain, neuropathic pain and hyperalgesia. Inflammation associated with conditions such as IBD and IBS, ocular and otic inflammation, other disorders and conditions such as pruritis, edema, hyponatremia, hypokalemia, ileus, tussis and glaucoma are treatable or preventable with the pharmaceutical compositions of the invention.
摘要翻译： 本发明涉及κ阿片样物质受体的合成肽酰胺配体，特别是涉及低P450 CYP抑制和低渗透入脑的κ阿片受体激动剂。 本发明的合成肽酰胺符合式I的结构：含有这些化合物的药物组合物可用于预防和治疗与多种疾病和病症相关的疼痛和炎症。 这种可治疗的疼痛包括内脏痛，神经性疼痛和痛觉过敏。 与IBD和IBS等条件相关的炎症，眼部和耳部炎症，其他疾病和病症如瘙痒症，水肿，低钠血症，低钾血症，肠梗阻，肠炎和青光眼均可用本发明的药物组合物治疗或预防。
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公开(公告)号：US20110118186A1
公开(公告)日：2011-05-19
申请号：US12773992
申请日：2010-05-05
申请人： Claudio D. Schteingart , Frederique Menzaghi , Guangcheng Jiang , Roberta Vezza Alexander , Javier Sueiras-Diaz , Robert H. Spencer , Derek T. Chalmers , Zhiyong Luo
发明人： Claudio D. Schteingart , Frederique Menzaghi , Guangcheng Jiang , Roberta Vezza Alexander , Javier Sueiras-Diaz , Robert H. Spencer , Derek T. Chalmers , Zhiyong Luo
IPC分类号： A61K38/07 , C07K7/06 , A61K38/08 , C07K5/11 , C07K7/56 , A61K38/12 , C07K7/02 , A61P17/04 , A61P27/06 , A61P3/12 , A61P9/10 , A61P29/00 , A61P11/14
CPC分类号： C07K5/1016 , C07K7/02
摘要： The invention relates to synthetic peptide amides that are ligands of the kappa opioid receptor and particularly to agonists of the kappa opioid receptor that exhibit low P450 CYP inhibition and low penetration into the brain. The synthetic peptide amides of the invention conform to the structure: wherein Xaa is a D-amino acid and G is selected from the following three groups: The compounds are useful in the prophylaxis and treatment of pain, pruritis and inflammation associated with a variety of diseases and conditions.
摘要翻译： 本发明涉及作为κ阿片受体的配体的合成肽酰胺，特别是涉及低P450 CYP抑制和低渗透入脑的κ阿片样物质受体的激动剂。 本发明的合成肽酰胺符合以下结构：其中Xaa是D-氨基酸，G选自以下三组：所述化合物可用于预防和治疗与各种各样的相关的疼痛，瘙痒和炎症 疾病和病症。
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公开(公告)号：US20100075910A1
公开(公告)日：2010-03-25
申请号：US12480059
申请日：2009-06-08
申请人： Claudio D. Schteingart , Frederique Menzaghi , Guangcheng Jiang , Roberta Vezza Alexander , Javier Sueiras-Diaz , Robert H. Spencer , Derek T. Chalmers , Zhiyong Luo
发明人： Claudio D. Schteingart , Frederique Menzaghi , Guangcheng Jiang , Roberta Vezza Alexander , Javier Sueiras-Diaz , Robert H. Spencer , Derek T. Chalmers , Zhiyong Luo
CPC分类号： C07K5/1016 , C07K7/02
摘要： The invention relates to synthetic peptide amides that are ligands of the kappa opioid receptor and particularly to agonists of the kappa opioid receptor that exhibit low P450 CYP inhibition and low penetration into the brain. The synthetic peptide amides of the invention conform to the structure: wherein Xaa is a D-amino acid and G is selected from the following three groups: The compounds are useful in the prophylaxis and treatment of pain, pruritus and inflammation associated with a variety of diseases and conditions.
摘要翻译： 本发明涉及作为κ阿片受体的配体的合成肽酰胺，特别是涉及低P450 CYP抑制和低渗透入脑的κ阿片样物质受体的激动剂。 本发明的合成肽酰胺符合以下结构：其中Xaa是D-氨基酸，G选自以下三组：所述化合物可用于预防和治疗与各种各样的相关的疼痛，瘙痒和炎症 疾病和病症。
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公开(公告)号：US08906859B2
公开(公告)日：2014-12-09
申请号：US12868790
申请日：2010-08-26
申请人： Claudio D. Schteingart , Frederique Menzaghi , Guangcheng Jiang , Roberta Vezza Alexander , Javier Sueiras-Diaz , Robert H. Spencer , Derek T. Chalmers , Robert Zhiyong Luo
发明人： Claudio D. Schteingart , Frederique Menzaghi , Guangcheng Jiang , Roberta Vezza Alexander , Javier Sueiras-Diaz , Robert H. Spencer , Derek T. Chalmers , Robert Zhiyong Luo
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-β, 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-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。
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公开(公告)号：US20140221277A1
公开(公告)日：2014-08-07
申请号：US14087142
申请日：2013-11-22
CPC分类号： A61K38/07 , A61K31/00 , A61K38/095 , A61K45/06
摘要： Methods for elevating and stabilizing prolactin levels in a mammal including methods of treating disorders and conditions associated with reduced serum levels of prolactin are provided. Also provided are methods of using certain synthetic tetrapeptide amides which are peripherally selective kappa opioid receptor agonists to elevate or stabilize serum prolactin levels.
摘要翻译： 提供了用于升高和稳定哺乳动物中的催乳素水平的方法，包括治疗与催乳素血清水平降低相关的疾病和病症的方法。 还提供使用某些合成四肽酰胺的方法，其是外周选择性κ阿片样物质受体激动剂以提升或稳定血清催乳素水平。
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公开(公告)号：US20130012431A1
公开(公告)日：2013-01-10
申请号：US13543128
申请日：2012-07-06
CPC分类号： A61K38/07 , A61K31/00 , A61K38/095 , A61K45/06
摘要： Methods for elevating and stabilizing prolactin levels in a mammal including methods of treating disorders and conditions associated with reduced serum levels of prolactin are provided. Also provided are methods of using certain synthetic tetrapeptide amides which are peripherally selective kappa opioid receptor agonists to elevate or stabilize serum prolactin levels.
摘要翻译： 提供了用于升高和稳定哺乳动物中的催乳素水平的方法，包括治疗与催乳素血清水平降低相关的疾病和病症的方法。 还提供使用某些合成四肽酰胺的方法，其是外周选择性κ阿片样物质受体激动剂以提升或稳定血清催乳素水平。
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公开(公告)号：US08236766B2
公开(公告)日：2012-08-07
申请号：US12480059
申请日：2009-06-08
申请人： Claudio D. Schteingart , Frederique Menzaghi , Guangcheng Jiang , Roberta Vezza Alexander , Javier Sueiras-Diaz , Robert H. Spencer , Derek T. Chalmers , Zhiyong Luo
发明人： Claudio D. Schteingart , Frederique Menzaghi , Guangcheng Jiang , Roberta Vezza Alexander , Javier Sueiras-Diaz , Robert H. Spencer , Derek T. Chalmers , Zhiyong Luo
IPC分类号： A61K38/07
CPC分类号： C07K5/1016 , C07K7/02
摘要： The invention relates to synthetic peptide amides that are ligands of the kappa opioid receptor and particularly to agonists of the kappa opioid receptor that exhibit low P450 CYP inhibition and low penetration into the brain. The synthetic peptide amides of the invention conform to the structure: wherein Xaa is a D-amino acid and G is selected from the following three groups: The compounds are useful in the prophylaxis and treatment of pain, pruritus and inflammation associated with a variety of diseases and conditions.
摘要翻译： 本发明涉及作为κ阿片受体的配体的合成肽酰胺，特别是涉及低P450 CYP抑制和低渗透入脑的κ阿片样物质受体的激动剂。 本发明的合成肽酰胺符合以下结构：其中Xaa是D-氨基酸，G选自以下三组：所述化合物可用于预防和治疗与各种各样的相关的疼痛，瘙痒和炎症 疾病和病症。
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公开(公告)号：US08217000B2
公开(公告)日：2012-07-10
申请号：US12300595
申请日：2007-05-22
摘要： Methods for elevating and stabilizing prolactin levels in a mammal including methods of treating disorders and conditions associated with reduced serum levels of prolactin are provided. Also provided are methods of using certain synthetic tetrapeptide amides which are peripherally selective kappa opioid receptor agonists to elevate or stabilize serum prolactin levels.
摘要翻译： 提供了用于升高和稳定哺乳动物中的催乳素水平的方法，包括治疗与催乳素血清水平降低相关的疾病和病症的方法。 还提供使用某些合成四肽酰胺的方法，其是外周选择性κ阿片样物质受体激动剂以提升或稳定血清催乳素水平。
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公开(公告)号：US20090312271A1
公开(公告)日：2009-12-17
申请号：US12300595
申请日：2007-05-22
IPC分类号： A61K38/07
摘要： Methods for elevating and stabilizing prolactin levels in a mammal including methods of treating disorders and conditions associated with reduced serum levels of prolactin are provided. Also provided are methods of using certain synthetic tetrapeptide amides which are peripherally selective kappa opioid receptor agonists to elevate or stabilize serum prolactin levels.
摘要翻译： 提供了用于升高和稳定哺乳动物中的催乳素水平的方法，包括治疗与催乳素血清水平降低相关的疾病和病症的方法。 还提供使用某些合成四肽酰胺的方法，其是外周选择性κ阿片样物质受体激动剂以提升或稳定血清催乳素水平。
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