C - Chemistry – Metallurgy – 12 – N
Patent
C - Chemistry, Metallurgy
12
N
C12N 15/62 (2006.01) A61K 38/08 (2006.01) A61K 38/10 (2006.01) A61K 38/58 (2006.01) C07D 211/34 (2006.01) C07D 211/62 (2006.01) C07D 295/185 (2006.01) C07K 7/02 (2006.01) C07K 7/06 (2006.01) C07K 7/08 (2006.01) C07K 14/815 (2006.01) C12N 15/15 (2006.01) A61K 38/00 (2006.01)
Patent
CA 2133581
2133581 9322344 PCTABScor01 Novel compounds of formula (I) in which R1 and R2 are hydrogen, C1-C4 alkyl or are linked to form C3-C7 cycloalkyl and R3, R4 and R5 are the same or different and are hydrogen, C1-C4 alkyl, hydroxy, OR6, SR6, halogen, NR7R8, NO2, CN, CONR7R8 or CO2R9 wherein R6 is C1-C4 alkyl or C7-C10 aralkyl and R7, R8 and R9 are the same or different and are hydrogen, C1-C4 alkyl or C7-C10 aralyl or R7 and R8 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.
Brundish Derek E.
Grutter Markus
Priestle John P.
Rink Hans
Schmitz Albert
Ag Ciba-Geigy
Fetherstonhaugh & Co.
Ucp Gen-Pharma Ag
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