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    Synthetic peptide amide dimers
    8.
    发明授权
    Synthetic peptide amide dimers 有权
    合成肽酰胺二聚体

    公开(公告)号：US07842662B2

    公开(公告)日：2010-11-30

    申请号：US11938776

    申请日：2007-11-12

    申请人： Claudio D. Schteingart ,  Frédérique Menzaghi ,  Guangcheng Jiang ,  Roberta Vezza Alexander ,  Javier Sueiras-Diaz ,  Robert H. Spencer ,  Derek T. Chalmers ,  Zhiyong Luo

    发明人： Claudio D. Schteingart ,  Frédérique Menzaghi ,  Guangcheng Jiang ,  Roberta Vezza Alexander ,  Javier Sueiras-Diaz ,  Robert H. Spencer ,  Derek T. Chalmers ,  Zhiyong Luo

    IPC分类号： A61K38/00

    CPC分类号： C07K5/1016 ,  A61K38/00 ,  C07K5/1005 ,  C07K5/1008 ,  C07K5/1024 ,  C07K7/06

    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: 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以下结构：含有这些化合物的药物组合物可用于预防和治疗与各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。

    Synthetic peptide amides
    9.
    发明授权
    Synthetic peptide amides 有权
    合成肽酰胺

    公开(公告)号：US07727963B2

    公开(公告)日：2010-06-01

    申请号：US12176279

    申请日：2008-07-18

    申请人： Claudio D. Schteingart ,  Guangcheng Jiang ,  Roberta Vezza Alexander ,  Javier Sueiras-Diaz ,  Zhiyong Luo

    发明人： Claudio D. Schteingart ,  Guangcheng Jiang ,  Roberta Vezza Alexander ,  Javier Sueiras-Diaz ,  Zhiyong Luo

    IPC分类号： A61K38/07

    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 tetrapeptide 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. An exemplary synthetic tetrapeptide amide of the invention is D-Phe-D-Phe-D-Leu-(ε-Me) D-Lys-[4-Amidinohomopiperazine amide]: 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四肽酰胺配体，特别涉及表现出低P450 CYP抑制和低渗透入脑的κ阿片受体激动剂。 本发明的示例性合成四肽酰胺是D-Phe-D-Phe-D-Leu-（α-Me）D-Lys- [4-脒基高密度哌嗪酰胺]：含有这些化合物的药物组合物可用于预防和治疗 与各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。