专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO1994029349A1 TRIFUNCTIONAL ANTITHROMBIN AND ANTIPLATELET PEPTIDES 审中-公开
标题翻译：功能性抗血栓素和抗血小板肽
公开(公告)号：WO1994029349A1
公开(公告)日：1994-12-22
申请号：PCT/US1994005355
申请日：1994-05-13
申请人： MERRELL DOW PHARMACEUTICALS INC. , BROERSMA, Robert, J., Jr. , OWEN, Thomas, J. , KRSTENANSKY, John, L.
发明人： MERRELL DOW PHARMACEUTICALS INC.
IPC分类号： C07K15/00
CPC分类号： C07K14/815 , A61K38/00 , C07K14/75
摘要： Compounds of the formula: X-A-B-C-Y wherein X is an amino terminal residue selected from hydrogen, one or two alkyl groups of from 1 to 6 carbon atoms, one or two acyl groups of from 2 to 10 carbon atoms, carbobenzyloxy, H2NC(=NH)-, or a t-butyloxy carbonyl group; A is a peptide analog of the formula: A1-A2-A3 wherein A1 is (D)Phe, (D)Phg, (D)1-Tiq, (D)3-Tiq, N-Me- (D)Phe, (D)Cha, (D)Chg, (D)Nag, or (D)Thg; A2 is Pro, Pip, or Azt; A3 is Arg, Lys, Orn, or hArg; B is a peptide analog of formulae (3) or (4) wherein B1 is Gly, Ala, (D)Ala, Val, (D)Val, or Gly-Gly; B2 is Gly, Gly-Gly, Gly-Gly-Gly, Gly-Gly-Gly-Gly or any (D) amino acid; B2' is Arg-Ile-Pro or Lys-Ile-Pro; B3 is Arg, hArg, N-Me-Arg or Lys; B4 is Nle, Phe, Met or Cha; C is a peptide analog of the formula: Asp-C1-C2-C3-C4-C5-C6-C7-C8-C9 wherein C1 is Phe, pC1Phe, pNO2Phe, Tha, Npa, Tyr or Trp; C2 is Glu or Asp; C3 is any amino acid; C4 is Ile, Val, Leu or Phe; C5 is Pro, Hyp, Sar, NMePgl or D-Ala; C6 is any amino acid; C7 is any amino acid; C8 is Tyr, Glu, Pro, Ala-Cha, Tyr-Cha, Tyr-Leu and Ala-Tyr; C9 is a bond or is Glu, (D)Glu, Gln, Pro, Leu-Gln, Asp-Glu, or Leu-Pro; and Y is a carboxy terminal residue selected from OH, C1-C6 alkoxy, amino, mono- or di-(C1-C4) alkyl substituted amino, or benzylamino; or pharmaceutically acceptable salts thereof are useful anticoagulant agents. This invention also relates to the use of the above compounds in treating acute postangioplasty occlusion, extracorporeal circulation-induced cytopenia, developing myocardial infarction, and post fibrinolytic therapy occlusion.
摘要翻译：式XABCY的化合物，其中X是选自氢，一个或两个1-6个碳原子的一个或两个烷基，一个或两个2-10个碳原子的酰基，苄氧羰基，H 2 NC（= NH） - 或叔丁氧基羰基; A是下式的肽类似物：A1-A2-A3，其中A1是（D）Phe，（D）Phg，（D）1-Tiq，（D）3-Tiq，N-Me-（D）（D）Cha，（D）Chg，（D）Nag或（D）Thg; A2是Pro，Pip或Azt; A3是Arg，Lys，Orn或hArg; B是式（3）或（4）的肽类似物，其中B1是Gly，Ala，（D）Ala，Val，（D）Val或Gly-Gly; B2是Gly，Gly-Gly，Gly-Gly-Gly，Gly-Gly-Gly-Gly或任何（D）氨基酸; B2'是Arg-Ile-Pro或Lys-Ile-Pro; B3是Arg，hArg，N-Me-Arg或Lys; B4为Nle，Phe，Met或Cha; C是下式的肽类似物：Asp-C1-C2-C3-C4-C5-C6-C7-C8-C9，其中C1是Phe，pC1Phe，pNO2Phe，Tha，Npa，Tyr或Trp; C2是Glu或Asp; C3是任何氨基酸; C4是Ile，Val，Leu或Phe; C5是Pro，Hyp，Sar，NMePgl或D-Ala; C6是任何氨基酸; C7是任何氨基酸; C8是Tyr，Glu，Pro，Ala-Cha，Tyr-Cha，Tyr-Leu和Ala-Tyr; C9是Glu或Glu，（D）Glu，Gln，Pro，Leu-Gln，Asp-Glu或Leu-Pro; 和Y是选自OH，C 1 -C 6烷氧基，氨基，单 - 或二 - （C 1 -C 4）烷基取代的氨基或苄基氨基的羧基末端残基; 或其药学上可接受的盐是有用的抗凝血剂。本发明还涉及上述化合物在治疗急性血管成形术闭塞，体外循环诱导的血细胞减少，发展中的心肌梗死和纤维蛋白溶解治疗闭塞中的用途。

IPRDB

热门服务

关于我们

友情链接

联系方式