公开(公告)号：US07541339B2

公开(公告)日：2009-06-02

申请号：US10517803

申请日：2003-06-10

申请人： Robert Ramage ,  Robin Plevin ,  Kevin Thomas Shaw ,  Lu Jiang ,  Louise Claire Young ,  Alan Lang Harvey ,  Pu Wang ,  Toru Kanke ,  Junichi Kawagoe ,  Mototsugu Kabeya

发明人： Robert Ramage ,  Robin Plevin ,  Kevin Thomas Shaw ,  Lu Jiang ,  Louise Claire Young ,  Alan Lang Harvey ,  Pu Wang ,  Toru Kanke ,  Junichi Kawagoe ,  Mototsugu Kabeya

IPC分类号： A61K38/08 ,  C07K7/06

CPC分类号： C07K14/705 ,  A61K38/00 ,  C07K7/06

摘要： The present invention relates to a peptide derivative represented by the general formula (I) or a salt thereof: Z-(CH2)n—CO—NH-Leu-Ile-Gly-AA1-AA2-CO—R (I) wherein Z represents an aryl group which may or may not have a substituent or a heteroaryl group which may or may not have a substituent; n represents 0, 1 or 2: AA1-AA2 represents Lys-Val or Arg-Leu; and R represents —OH or —NH2, and relates to a pharmaceutical composition comprising a peptide derivative represented by the general formula (I) or a salt thereof, and a pharmaceutically acceptable carrier thereof. The peptide derivative is useful as a prophylactic and therapeutic agent of dysfunction of masticatory, dysphagia, dysgeusia, ozostomia, intra-oral cavity dysphoria, intra-oral cavity infections, intra-oral cavity inflammations, dry eye, ectocornea detachment, keratitis, corneal ulcer, conjunctivitis, stomach ulcer, duodenal ulcer, gastritis, diarrhea, enteritis or Sjogren's syndrome.

摘要翻译： 本发明涉及由通式（I）表示的肽衍生物或其盐：Z-（CH2）n-CO-NH-Leu-Ile-Gly-AA1-AA2-CO-R（Ⅰ）其中Z 表示可以具有也可以不具有取代基的芳基或可以具有取代基的杂芳基; n表示0,1或2：AA1-AA2表示Lys-Val或Arg-Leu; 和R表示-OH或-NH 2，并且涉及包含由通式（I）表示的肽衍生物或其盐及其药学上可接受的载体的药物组合物。 肽衍生物可用作咀嚼，吞咽困难，发重症，口臭，口腔内烦躁，口腔内感染，口腔内炎症，干眼症，异位角脱落，角膜炎，角膜溃疡功能障碍的预防和治疗剂 ，结膜炎，胃溃疡，十二指肠溃疡，胃炎，腹泻，肠炎或干燥综合征。