发明名称 Antidiabetic compounds
摘要 The present invention provides novel peptidomimetics, of formula (I), which primarily act as glucose dependent insulin secretagogues. Furthermore, it was found that these peptidomimetics showed glucagon receptor antagonistic activity, along with the GLP-1 receptor agonistic activity. A-Z1—Z2—Z3—Z4—Z5—Z6—Z7—Z8—Z9—Z10—Z11—B  (I)
申请公布号 US8841413(B2) 申请公布日期 2014.09.23
申请号 US200712311448 申请日期 2007.09.28
申请人 Cadila Healthcare Limited 发明人 Bahekar Rajesh H.;Lohray Braj Bhushan;Lohray Vidya Bhushan;Jain Mukul R.;Banerjee Kaushik M.;Patel Pankaj Ramanbhai
分类号 C07K7/08;C07K7/06;C07K14/605 主分类号 C07K7/08
代理机构 Ladas & Parry LLP 代理人 Ladas & Parry LLP
主权项 1. An isolated peptidomimetic having a sequence of Formula (I), or a tautomer or solvate thereof; A-Z1—Z2—Z3—Z4—Z5—Z6—Z7—Z8—Z9—Z10—Z11—B  (I) wherein, A represents the groups —NH—R1, R3—CO— or R3—SO2—, wherein R1 represents hydrogen, or optionally substituted linear or branched (C1-C10) alkyl chain; R3 is selected from linear or branched (C1-C10) alkyl, (C3-C6) cycloalkyl, aryl, heteroaryl or arylalkyl groups; B represents the groups —COOR2, —CONHR2 or CH2OR2 or a tetrazole, wherein R2 represents H, optionally substituted groups selected from linear or branched (C1-C10) alkyl, aryl or aralkyl groups; Z1 represents Histidine; Z2 represents a naturally or unnaturally occurring amino acid selected from the group comprising L-Serine, D-Serine, L-alanine, D-alanine, α-amino-isobutyric acid, and 1-amino cyclopropane carboxyl acid; Z3 represents glutamine (Gln; Q) or compounds of formula II; Z4 represents glycine or the group 1-amino cyclopropane carboxylic acid; Z3 represents a naturally or non-naturally occurring amino acid comprising a hydroxyl side chain; Z6 represents, a naturally of unnaturally occurring amino acid having a disubstituted alpha carbon having two side chains, wherein each of them are independently selected from an optionally substituted alkyl, aryl or an aralkyl group wherein the substituents are selected from one or more alkyl groups or one or more halo groups;Z7 and Z8 independently represents a naturally or non-naturally occurring amino acid comprising a hydroxyl side chain; Z9 independently represents a naturally or non-naturally occurring amino acid having an amino acid side chain comprising an acidic group;Z10 represents a naturally or unnaturally occurring amino acid of formula IV and Z11 represents a naturally or unnaturally occurring amino acid of formula V(a-d)
地址 Amedadabad IN