发明授权
US5100873A Irreversible peptide ligands for bombesin receptors, their use, and
process for making the same
失效
BOMBESIN受体的不可逆肽配体，其使用及其制备方法
- 专利标题： Irreversible peptide ligands for bombesin receptors, their use, and process for making the same
- 专利标题（中）： BOMBESIN受体的不可逆肽配体，其使用及其制备方法
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申请号： US380539申请日： 1989-07-17
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公开(公告)号： US5100873A公开(公告)日： 1992-03-31
- 发明人: Roberto de Castiglione , Mauro Galantino , Fabio Corradi , Luigia Gozzini , Marina Ciomei , Isabella Molinari
- 申请人： Roberto de Castiglione , Mauro Galantino , Fabio Corradi , Luigia Gozzini , Marina Ciomei , Isabella Molinari
- 申请人地址： ITX Milan
- 专利权人： Farmitalia Carlo Erba
- 当前专利权人： Farmitalia Carlo Erba
- 当前专利权人地址： ITX Milan
- 优先权： GBX8817379 19880721; GBX8906900 19890328
- 主分类号： A61K38/00
- IPC分类号： A61K38/00 ; A61P35/00 ; C07K1/02 ; C07K7/06 ; C07K7/08
摘要：
A peptide of formula (I):A-B-C-D-Gln-Trp-Ala-Val-X-Y-T-W (I)wherein either:(i) A represents a hydrogen atom, a Boc group or an acetyl group, one of B and C represents a pMel or mMel residue, and the other of B and C represents a sigma bond or a Gly, Leu-Gly, E-Leu-Gly or Gln-E-Leu-Gly, E, or E-Gly residue with E=Arg(A), arg(A), Lys(A), lys(A), Orn(A) and orn(A); or(ii) A represents a hydrogen atom;B represents a Glp-Arg-Leu-Gly residue;C represents a pMel or mMel residue;D represents a sigma bond or an Asn or Thr residue;X represents a Gly or ala residue;Y represents a sigma bond or a His(R.sub.1);his(R.sub.1), Phe, phe, Ser, ser, Ala or ala residue,T represents a sigma bond or a Leu, leu, Phe or phe residue;W represents an OH, amino, pentylamino or phenethyl-amino group or a Met-R.sub.2, Leu-R.sub.2, Ile-R.sub.2 or Nle-R.sub.2 residue;R.sub.1 represents a hydrogen atom or a Tos, Dnp or Bzl group; andR.sub.2 represents an amino, hydroxy, methoxy or hydrazino group;and its pharmaceutically acceptable salts are disclosed.
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