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    • 29. 发明授权
    • Bradykinin antagonist peptides
    • 缓激肽拮抗肽
    • US4693993A
    • 1987-09-15
    • US744207
    • 1985-06-13
    • John M. StewartRaymond J. Vavrek
    • John M. StewartRaymond J. Vavrek
    • A61K38/00C07K7/18C07K7/06C07K7/08
    • C07K7/18A61K38/00
    • The substitution of the L-Pro at the 7-position of the peptide hormone bradykinin or other substituted analogs of bradykinin with an aromatic amino acid or the D-configuration converts bradykinin agonists into a bradykinin antagonist. The invention further includes additional modifications at other positions within the novel 7-position modified bradykinin antagonists which increase enzyme resistance, antagonist potency and/or specificity of the new bradykinin antagonists. The analogs produced are useful in treating conditions and diseases of the mammal and human body in which an excess of bradykinin or related kinins are produced or injected as by bites into the body.
    • 使用芳香族氨基酸或D-构型将肽激素缓激肽或其他取代的缓激肽类似物的L-Pro取代成缓激肽拮抗剂。 本发明进一步包括增加新的缓冲肽拮抗剂的抗酶性,拮抗剂效能和/或特异性的新型7-位修饰的缓激肽拮抗剂中的其它位置的其它修饰。 所产生的类似物可用于治疗哺乳动物和人体的状况和疾病,其中过量的缓激肽或相关激肽通过叮咬产生或注射到体内。