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    • 9. 发明授权
    • Effectors of dipeptidyl peptidase IV for topical use
    • 二肽基肽酶IV用于局部使用的作用
    • US07335645B2
    • 2008-02-26
    • US11069926
    • 2005-03-01
    • Hans-Ulrich DemuthTorsten HoffmannDagmar SchlenzigUlrich Heiser
    • Hans-Ulrich DemuthTorsten HoffmannDagmar SchlenzigUlrich Heiser
    • A61K38/00A61K31/33
    • C07K5/06078A61K38/00C07K5/06104C07K5/0806C07K7/08C08G65/329
    • The invention relates to compounds for topically influencing the activity of dipeptidyl peptidase of the general formula wherein A is an amino acid having at least one functional group in the side chain; B is a chemical compound covalently bound to a functional group of the side chain of A, chosen from the group consisting of (a) oligopeptides having a chain length of up to 20 amino acids, (b) homopolymers of glycine consisting of up to 6 glycine monomers, and (c) polyethylene glycols having molar masses of up to 20 000 g/mol; and C is a group amide-bonded to A chosen from the group consisting of thiazolidine, pyrrolidine, cyanopyrrolidine, hydroxyproline, dehydroproline or piperidine. The invention further relates to the use of said compounds for targeted intervention in local immunological processes (chemotaxis, inflammatory processes, autoimmune diseases), as well as effective and targeted treatment of pathophysiological and physiological processes related thereto (psoriasis, periodontitis, arthritis, allergies, inflammation), inter alia.
    • 本发明涉及用于局部影响以下通式的二肽基肽酶的活性的化合物:其中A是在侧链中具有至少一个官能团的氨基酸; B是与A的侧链官能团共价结合的化合物,选自(a)链长达20个氨基酸的寡肽,(b)由多达6个氨基酸组成的甘氨酸均聚物 甘氨酸单体,和(c)摩尔质量高达20 000g / mol的聚乙二醇; 和C是选自噻唑烷,吡咯烷,氰基吡咯烷,羟脯氨酸,脱氢脯氨酸或哌啶的酰胺键合的基团。 本发明进一步涉及所述化合物在局部免疫学过程(趋化性,炎性过程,自身免疫性疾病)中的靶向干预的用途,以及与之相关的病理生理和生理过程的有效和靶向治疗(牛皮癣,牙周炎,关节炎,过敏, 炎症),特别是。