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    • 8. 发明申请
    • PEPTIDE DERIVATIVES CORRESPONDING TO THE CARBOXY TERMINAL SEQUENCE OF HIRUDIN
    • 针对呼吸道的羧基末端序列的肽衍生物
    • WO1993022344A1
    • 1993-11-11
    • PCT/EP1993000908
    • 1993-04-15
    • CIBA-GEIGY AGUCP GEN-PHARMA AGBRUNDISH, Derek, EdwardRINK, HansGRÜTTER, MarkusPRIESTLE, John, PeterSCHMITZ, Albert
    • CIBA-GEIGY AGUCP GEN-PHARMA AG
    • C07K15/00
    • C07D295/185A61K38/00C07D211/34C07D211/62C07K14/815
    • Novel compounds of formula (I) in which R and R are hydrogen, C1-C4 alkyl or are linked to form C3-C7 cycloalkyl and R , R and R are the same or different and are hydrogen, C1-C4 alkyl, hydroxy, OR , SR , halogen, NR R , NO2, CN, CONR R or CO2R wherein R is C1-C4 alkyl or C7-C10 aralkyl and R , R and R are the same or different and are hydrogen, C1-C4 alkyl or C7-C10 aralyl or R and R together with the nitrogen atom to which they are bound form 5 or 6 membered azacyloalkyl or oxazacyloalkyl; Arg is arginine [NH-CH(CH2CH2CH2NH-C(=NH)-NH2)-CO]; X is methine CH or nitrogen; n is an integer from 0 to 7; L is a peptide linker, and H is the carboxy terminal end of hirudin, and salts thereof, are provided. The novel compounds are useful for the medical treatment or prevention of thrombosis or diseases caused by thrombosis or can be used for the determination of thrombin in blood as diagnostic reagents.
    • 式(I)的新型化合物,其中R 1和R 2为氢,C 1 -C 4烷基或连接形成C 3 -C 7环烷基且R 3,R 4和R 5为 相同或不同的是氢,C 1 -C 4烷基,羟基,OR 6,SR 6,卤素,NR 7 R 8,NO 2,CN,CONR 7 R 8或CO 2 R 其中R 6为C 1 -C 4烷基或C 7 -C 10芳烷基,R 7,R 8和R 9相同或不同,为氢,C 1 -C 4烷基或C 7 -C 10 芳酰基或R 7和R 8与它们所连接的氮原子一起形成5或6元氮杂烷基或恶唑烷基烷基; Arg是精氨酸[NH-CH(CH 2 CH 2 CH 2 NH-C(= NH)-NH 2)-CO]; X是次甲基CH或氮; n为0〜7的整数; L是肽接头,H是水蛭素的羧基末端及其盐。 该新型化合物可用于治疗或预防由血栓引起的血栓形成或疾病,或可用于测定血液中的凝血酶作为诊断试剂。