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    Kappa receptor opioid peptides
    2.
    发明授权
    Kappa receptor opioid peptides 失效
    卡帕受体阿片样肽

    公开(公告)号：US5965701A

    公开(公告)日：1999-10-12

    申请号：US997208

    申请日：1997-12-23

    申请人： Jean Louis Junien ,  Pierre J.M. Riviere ,  Claudio D. Schteingart ,  Javier Sueiras Diaz ,  Jerzy A. Trojnar ,  Todd W. Vanderah

    发明人： Jean Louis Junien ,  Pierre J.M. Riviere ,  Claudio D. Schteingart ,  Javier Sueiras Diaz ,  Jerzy A. Trojnar ,  Todd W. Vanderah

    IPC分类号： A61K38/00 ,  A61K38/07 ,  A61P1/04 ,  A61P13/00 ,  A61P13/10 ,  A61P25/04 ,  C07K5/10 ,  C07K5/107 ,  C07K5/117 ,  C07K5/00

    CPC分类号： C07K5/1027 ,  C07K5/1016 ,  C07K5/1024 ,  A61K38/00

    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.

    摘要翻译： 产生对κ阿片样物质受体（KOR）具有高选择性且长期持续的外周作用而不显着进入脑的肽是具有C末端的四个D-异构体氨基酸残基的序列，其是单或二 - 取代的酰胺。 对KOR具有至少1,000次对μ阿片受体的亲和力和不大于约0.5mg / kg的ED 50的亲和力的代表性化合物包括H-D-Phe-D-Phe-D-Nle-D- Arg-NHEt，HD-Phe-D-Phe-D-Nle-D-Arg-吗啉基，HD-Phe-D-Phe-D-Nle-D-Arg-NH-4-吡啶甲基，HD-Phe- Phe-D-Nle-D-Arg-NHPr，HD-Phe-D-Phe-D-Nle-D-Arg-硫代吗啉基，HD-Phe-D-Phe-D-Nle-D-Arg-NEt2， Phe-D-Phe-D-Nle-D-Arg-NHMe，HD-Phe-D-Phe-D-Leu-D-Orn-吗啉基，HD-Phe-D-Phe-D-Nle-D-Arg- NHhEt，HD-Phe-D-Phe-D-Nle-D-Arg-NH-环丙基，HD-Ala（2Thi）-D-4Cpa-D-Leu-D-Arg-吗啉基，HD-Phe-D-Phe -D-Nle-D-Arg-哌啶基，HD-Phe-D-Phe-D-Leu-D-Orn-NHEt，HD-Phe-D-Phe-D-Leu-D-Lys-吗啉基和H-D -Phe-D-Phe-D-Nle-D-Arg-哌嗪基。

    Vasotocin derivatives
    3.
    发明授权
    Vasotocin derivatives 失效
    血管生成衍生物

    公开(公告)号：US4504469A

    公开(公告)日：1985-03-12

    申请号：US561920

    申请日：1983-12-15

    申请人： Per O. R. Melin ,  Jerzy A. Trojnar

    发明人： Per O. R. Melin ,  Jerzy A. Trojnar

    IPC分类号： C07K7/16 ,  A61K38/00 ,  A61K38/095 ,  A61P5/00 ,  A61P13/02 ,  A61P15/00 ,  C07K14/575 ,  A61K37/00 ,  C07C103/52

    CPC分类号： C07K7/16 ,  A61K38/00 ,  Y10S930/15

    摘要： Novel vasotocin derivatives having an inhibitory effect on uterine contractions, pharmaceutical compositions containing these derivatives, and the use thereof in the therapeutical treatment of excessive muscle contractions in the uterus and described. The derivatives differ from vasotocin in that the structure of the original hormone has been modified at positions 1, 2 and, optionally, 4 and/or 8. The vasotocin derivatives thus have the formula ##STR1## wherein Mpa is a 3-mercaptopropionoyl residue (--S--CH.sub.2 --CH.sub.2 --CO--);A is the peptide residue of L- or D-tyrosine-O-ethyl ether (in other words, 4-ethoxy-L or D-phenyl alanine, i.e. L- or D-Tyr(Et)), or of a hydrophobic D-amino acid, such as D-tyrosine(D-Tyr) or D-tryptophane(D-Trp);Ile is the peptide residue of isoleucine;B is the peptide residue of glutamine (Gln), treonine (Thr) or valine (Val);Asn is the peptide residue of asparagin;Cys is the peptide residue of cysteine;Pro is the peptide residue of proline;C is the peptide residue of L- or D-arginine (Arg), ornithine (Orn) or citrullin (Cit); andGly--NH.sub.2 is the peptide residue of glycine amide.

    摘要翻译： 具有对子宫收缩的抑制作用的新型血管生成物衍生物，含有这些衍生物的药物组合物及其在治疗性治疗子宫中过度肌肉收缩的用途及其用途。 衍生物不同于血管生成素，因为原始激素的结构已经在1,2和任选的4和/或8位被修饰。因此，血管生成物衍生物具有式“IMAGE”，其中Mpa是3-巯基丙酰基残基（ -S-CH 2 -CH 2 -CO-）; A是L-或D-酪氨酸-O-乙基醚的肽残基（换句话说，4-乙氧基-L或D-苯基丙氨酸，即L-或D-Tyr（Et））或疏水性D - 氨基酸，如D-酪氨酸（D-Tyr）或D-色氨酸（D-Trp）; Ile是异亮氨酸的肽残基; B是谷氨酰胺（Gln），枸橼酸（Thr）或缬氨酸（Val）的肽残基; Asn是天冬酰胺的肽残基; Cys是半胱氨酸的肽残基; Pro是脯氨酸的肽残基; C是L-或D-精氨酸（Arg），鸟氨酸（Orn）或瓜氨酸（Cit）的肽残基; Gly-NH2是甘氨酰胺的肽残基。