发明授权
- 专利标题: Kappa receptor opioid peptides
- 专利标题(中): 卡帕受体阿片样肽
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申请号: US997208申请日: 1997-12-23
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公开(公告)号: US5965701A公开(公告)日: 1999-10-12
- 发明人: Jean Louis Junien , Pierre J.M. Riviere , Claudio D. Schteingart , Javier Sueiras Diaz , Jerzy A. Trojnar , Todd W. Vanderah
- 申请人: Jean Louis Junien , Pierre J.M. Riviere , Claudio D. Schteingart , Javier Sueiras Diaz , Jerzy A. Trojnar , Todd W. Vanderah
- 申请人地址: NLX
- 专利权人: Ferring BV
- 当前专利权人: Ferring BV
- 当前专利权人地址: NLX
- 主分类号: A61K38/00
- IPC分类号: A61K38/00 ; A61K38/07 ; A61P1/04 ; A61P13/00 ; A61P13/10 ; A61P25/04 ; C07K5/10 ; C07K5/107 ; C07K5/117 ; C07K5/00
摘要:
Peptides which exhibit high selectivity for the kappa opioid receptor (KOR) and long duration of peripheral action without significant entry into the brain are created which are sequences of four D-isomer amino acid residues having a C-terminus which is a mono or di-substituted amide. Representative compounds, which have an affinity for the KOR at least 1,000 times their affinity for the mu opioid receptor and an ED.sub.50 of not greater than about 0.5 mg/kg, includeH-D-Phe-D-Phe-D-Nle-D-Arg-NHEt,H-D-Phe-D-Phe-D-Nle-D-Arg-morpholinyl,H-D-Phe-D-Phe-D-Nle-D-Arg-NH-4-picolyl,H-D-Phe-D-Phe-D-Nle-D-Arg-NHPr,H-D-Phe-D-Phe-D-Nle-D-Arg-thiomorpholinyl,H-D-Phe-D-Phe-D-Nle-D-Arg-NEt.sub.2,H-D-Phe-D-Phe-D-Nle-D-Arg-NHMe,H-D-Phe-D-Phe-D-Leu-D-Orn-morpholinyl,H-D-Phe-D-Phe-D-Nle-D-Arg-NHhEt,H-D-Phe-D-Phe-D-Nle-D-Arg-NH-cyclopropyl,H-D-Ala(2Thi)-D-4Cpa-D-Leu-D-Arg-morpholinyl,H-D-Phe-D-Phe-D-Nle-D-Arg-piperidinyl,H-D-Phe-D-Phe-D-Leu-D-Orn-NHEt,H-D-Phe-D-Phe-D-Leu-D-Lys-morpholinyl,andH-D-Phe-D-Phe-D-Nle-D-Arg-piperazinyl.
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