发明申请
- 专利标题: Somatostatin agonists
-
申请号: US11973954申请日: 2007-10-11
-
公开(公告)号: US20080090756A1公开(公告)日: 2008-04-17
- 发明人: David Coy , Walajapet Rajeswaran
- 申请人: David Coy , Walajapet Rajeswaran
- 申请人地址: US LA New Orleans
- 专利权人: The Administrators of the Tulane Educational Fund
- 当前专利权人: The Administrators of the Tulane Educational Fund
- 当前专利权人地址: US LA New Orleans
- 主分类号: A61K38/12
- IPC分类号: A61K38/12 ; A61P1/00 ; A61P3/00 ; A61P35/00 ; A61P5/00 ; C07K7/50
摘要:
Claimed are a series of somatostatin agonists typically characterized by alkylation of the amide nitrogen, and uses thereof. Examples of claimed compounds are those according to formula (I), A1-cyclo{Cys-A2-D-Trp-A3-A4-Cys}-A5-Y1, (I) wherein: A1 is an optionally substituted D- or L-aromatic α-amino acid or optionally substituted D- or L-cyclo(C3-6)alkylalanine; A2 is an optionally substituted aromatic α-amino acid or optionally substituted cyclo(C3-6)alkylalanine; A3 is Lys or Orn; A4 is β-Hydroxyvaline, Ser, hSer, or Thr; A5 is β-Hydroxyvaline, Ser, hSer, or Thr; and Y1 is OH, NH2 or NHR1, where R1 is (C1-6)alkyl; wherein each said optionally substituted aromatic α-amino acid and each said optionally substituted cyclo(C3-6)alkylalanine is optionally substituted with one or more substituents each independently selected from the group consisting of halogen, NO2, OH, CN, (C1-6)alkyl, (C2-6)alkenyl, (C2-6)alkynyl, (C1-6)alkoxy, Bzl, O-Bzl, and NR9R10, where R9 and R10 each is independently H or (C1-6) alkyl; and wherein the amine nitrogen of each peptide bond and the amino group of A1 of formula (I) is optionally substituted with a methyl group, provided that there is at least one said methyl group; and further provided that said compound is not D-Phe-cyclo{Cys-Phe-D-Trp-Lys-(N-Me-Thr)-Cys}-Thr-NH2; or a pharmaceutically acceptable salt thereof.
信息查询
IPC分类: