Bradykinin-antagonists for the treatment of acute pancreatitis
    2.
    发明授权
    Bradykinin-antagonists for the treatment of acute pancreatitis 失效
    缓激肽拮抗剂治疗急性胰腺炎

    公开(公告)号:US5670619A

    公开(公告)日:1997-09-23

    申请号:US232338

    申请日:1994-04-22

    CPC分类号: A61K38/043 A61K38/08

    摘要: The invention relates to the use of bradykinin-antagonists of the formula R.sup.1 -A-B-C-E-F-G-J-K-R.sup.2 wherein R.sup.1 represents hydrogen, C.sub.1 -C.sub.4 -alkanoyl which can be substituted by mercapto, hydroxyphenyl, (4-benzoyl)phenoxy or represents (4-benzoyl)benzoyl-Lys; A represents D-Arg or D-Lys or stands for a direct bond; B represents Arg which can be substituted by NO.sub.2 or toluol-4-sulfonyl or represents Lys which can be substituted by toluol-4-sulfonyl or CO--NH--C.sub.6 H.sub.5, or stands for a direct bond; C represents Hyp-Pro-Gly, Pro-Hyp-Gly, Pro-Pro-Gly or dehydroPro-Hyp-Gly; E represents Thi, Phe, Leu or Cha; F represents Ser or Cys; G represents D-Tic, D-Phe or D-Hyp substituted by C.sub.1 -C.sub.4 -alkoxy; J represents Tic, Aoc or Oic; K represents Arg or Ahx or stands for a direct bond; R.sup.2 is hydroxy or amino; and the physiologically tolerable salts thereof for the treatments of acute pancreatitis, to pharmaceutical agents containing them and to the use thereof for the preparation of appropriate pharmaceutical compositions.

    摘要翻译: 本发明涉及式R1-ABCEFGJK-R2的缓激肽拮抗剂的用途,其中R1表示氢,可被巯基,羟基苯基,(4-苯甲酰基)苯氧基取代的C 1 -C 4 - 烷酰基或代表(4-苯甲酰基)苯甲酰基 - 赖氨酸 A代表D-Arg或D-Lys或代表直接键; B表示可被NO 2或甲苯-4-磺酰基取代的Arg,或表示可被甲苯-4-磺酰基或CO-NH-C6H5取代的Lys,或代表直接键; C代表Hyp-Pro-Gly,Pro-Hyp-Gly,Pro-Pro-Gly或脱氢Pro-Hyp-Gly; E代表Thi,Phe,Leu或Cha; F代表Ser或Cys; G表示被C 1 -C 4 - 烷氧基取代的D-Tic,D-Phe或D-Hyp; J代表Tic,Aoc或Oic; K代表Arg或Ahx或代表直接键; R2是羟基或氨基; 及其用于治疗急性胰腺炎的生理上可耐受的盐,以及含有它们的药物及其用于制备合适的药物组合物的用途。