Analogs of substance P and eledoisin
    7.
    发明授权
    Analogs of substance P and eledoisin 失效
    物质P和eledoisin的类似物

    公开(公告)号:US4680283A

    公开(公告)日:1987-07-14

    申请号:US898274

    申请日:1986-08-20

    CPC分类号: C07K7/22 A61K38/00

    摘要: Analogs of substance P and eledoisin which are conformationally constrained by the presence of a lactam in the peptide chain demonstrate greater selectivity and increased protease stability and are useful as analgesic, anti-inflammatory, antihypertensive, central nervous system agents, and stimulants of lachrymal secretion. The compounds are prepared by standard peptide synthetic procedures.

    摘要翻译: 由肽链中存在内酰胺构象约束的物质P和eledoisin的类似物表现出更大的选择性和增加的蛋白酶稳定性,并且可用作止痛,抗炎,抗高血压,中枢神经系统药物和泪液分泌的兴奋剂。 化合物通过标准肽合成方法制备。

    Cyclic hexapeptide somatostatin analogs
    8.
    发明授权
    Cyclic hexapeptide somatostatin analogs 失效
    循环六肽生长抑素类似物

    公开(公告)号:US4611054A

    公开(公告)日:1986-09-09

    申请号:US728353

    申请日:1985-04-29

    申请人: Roger Freidinger

    发明人: Roger Freidinger

    IPC分类号: C07K14/655 C07K7/26 A61K37/24

    摘要: Cyclic hexapeptide somatostatin analogs are prepared wherein a peptide surrogate replaces eight of the ring amino acids of somatostatin. The cyclic hexapeptides are easier to synthesize, have a longer duration of activity, and many have a greater level of activity than somatostatin. The compounds have the properties of inhibiting the release of glucagon, growth hormone and insulin. Certain of the compounds also are capable of inhibiting the release of gastric acid secretions. The compounds are particularly useful in the treatment of acromegaly, diabetes, diabetic retinopathy and peptic ulcers. These cyclic hexapeptides are prepared by the solid phase method.

    摘要翻译: 制备环状六肽生长抑素类似物,其中肽替代物取代生长抑素的八个环氨基酸。 环状六肽更容易合成,具有较长的活性持续时间,并且许多具有比生长抑素更高的活性水平。 该化合物具有抑制胰高血糖素,生长激素和胰岛素释放的性质。 某些化合物还能够抑制胃酸分泌物的释放。 该化合物特别可用于治疗肢端肥大症,糖尿病,糖尿病性视网膜病变和消化性溃疡。 这些环状六肽通过固相法制备。

    Cyclic hexapeptide somatostatin analogs
    9.
    发明授权
    Cyclic hexapeptide somatostatin analogs 失效
    循环六肽生长抑素类似物

    公开(公告)号:US4486415A

    公开(公告)日:1984-12-04

    申请号:US523224

    申请日:1983-08-15

    申请人: Roger Freidinger

    发明人: Roger Freidinger

    摘要: Somatostatin analogs are prepared wherein a cyclic hexapeptide contains a secondary amino acid which replaces seven of the ring amino acids of somatostatin. The cyclic hexapeptides are easier to synthesize, have a longer duration of activity, and many have a greater level of activity than somatostatin. The compounds have the properties of inhibiting the release of glucagon, growth hormone and insulin. Certain of the compounds also are capable of inhibiting gastric acid secretions. The compounds are particularly useful in the treatment of acromegaly, diabetes, diabetic retinopathy and peptic ulcers. These cyclic hexapeptides are prepared by the solid phase method.

    摘要翻译: 制备生长抑素类似物,其中环状六肽含有替代生长抑素的七个环氨基酸的仲氨基酸。 环状六肽更容易合成,具有较长的活性持续时间,并且许多具有比生长抑素更高的活性水平。 该化合物具有抑制胰高血糖素,生长激素和胰岛素释放的性质。 某些化合物还能够抑制胃酸分泌。 该化合物特别可用于治疗肢端肥大症,糖尿病,糖尿病性视网膜病变和消化性溃疡。 这些环状六肽通过固相法制备。