发明名称 Leptin agonist and methods of use
摘要 Peptides are provided having leptin receptor agonist activity. The peptides are useful for treating obesity, type II diabetes, appetite control after bariatric surgery, insulin resistance, lipodystrophy and hypothalamic amenorrhea, obesity-related infertility, among other diseases and conditions related to leptin deficiency and/or leptin resistance.
申请公布号 US8980843(B2) 申请公布日期 2015.03.17
申请号 US201013381576 申请日期 2010.06.25
申请人 Temple University—of the Commonwealth System of Higher Education 发明人 Otvos, Jr. Laszlo
分类号 A61K38/10;C07K7/02;A61K38/16;A61K38/00;A61K38/22;A61K49/00;C07K14/575 主分类号 A61K38/10
代理机构 Drinker Biddle & Reath LLP 代理人 Drinker Biddle & Reath LLP
主权项 1. A compound according to Formula (I): X1-M-SEQ ID NO:2  (I)or a salt thereof, wherein: SEQ ID NO:2 represents Xaa1-Xaa2-Xaa3-Glu-Val-Val-Ala-Leu-Ser-Xaa4-Xaa5, wherein: Xaa1 is Tyr, Tyr(Me), Tyr(N-Me), Tyr(Me, N-Me), Tyr(I) or Tyr(I2);Xaa2 is Ser or a saccharide-modified serine;Xaa3 is Thr or a saccharide-modified threonine;Xaa4 is Arg or Arg(N-Me);Xaa5 is a non-natural amino acid selected from the group consisting of a D-isomer of a natural amino acid, arginosuccinic acid, citrulline, cysteine sulfinic acid, 3,4-dihydroxyphenylalanine, homocysteine, homoserine, ornithine, 3-monoiodotyrosine, 3,5-diiodotyrosine, 3,5,5′-triiodothyronine, 3,3′,5,5′-tetraiodothyronine, hydroxylysine, 4-hydroxyproline, an N-Cbz-protected amino acid, 2,4-diaminobutyric acid, homoarginine, N-methyl-arginine, norleucine, N-methylaminobutyric acid, naphthylalanine, phenylglycine, beta-phenylproline, tert-leucine, 4-aminocyclohexylalanine, N-methyl-norleucine, 3,4-dehydroproline, N,N-dimethylaminoglycine, N-methylaminoglycine, 4-aminopiperidine-4-carboxylic acid, Acp, AcpNH2, bAla, bAlaNH2, trans-4-(aminomethyl)-cyclohexanecarboxylic acid, 2-(aminomethyl)-benzoic acid, 3-(aminomethyl)-benzoic acid, 4-(aminomethyl)-benzoic acid, 1-aminocyclopentanecarboxylic acid, 1-aminocyclopropanecarboxylic acid, and 2-benzyl-5-aminopentanoic acid; and, X1-M is an optional group comprising a tagging element conjugated to the N-terminus of the amino acid sequence SEQ ID NO:2, wherein: X1 is the tagging element, wherein the tagging element is selected from the group consisting of a transduction domain and a detection label; and, -M- is a single bond or an optional linking group forming a covalent linkage between the tagging element and the amino acid sequence SEQ ID NO:2.
地址 Philadelphia PA US