Thrombin inhibiting arylsulfonyl guanidinophenylalanine amides

Details Thrombin inhibiting arylsulfonyl guanidinophenylalanine amides Thrombin inhibiting arylsulfonyl guanidinophenylalanine amides

1983-06-14

1985-08-27

Jiles, Henry R.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514211, 514212, 514218, 514229, 514255, 514423, 514602, 514603, 260239B, 260239BC, 2603306, 544162, 544391, 546206, 546226, 548540, 564 84, 564 91, 564 86, A61K 31445, A61K 3116, C07D21116, C07C14713

Patent

active

045378967

ABSTRACT:
New thrombin inhibiting N.sup..alpha. -arylsulfonyl-p-guanidinophenylalanine amides of the formula ##STR1## wherein Ar is a substituted aryl and R.sub.1 and R.sub.2 are an alkyl group having 1-5 carbon atoms or together with the amine nitrogen form an heterocyclic ring, in racemate form as well as in form of optical active antipodes, theirs pharmaceutically acceptable salts, methods for their preparation, pharmaceutical composition and diagnostical preparation containing these compounds, use of the compounds in treatments of thrombosis and methods of treatment of thrombosis as well as methods for determination of thrombin concentration in blood.

REFERENCES:
patent: 3884896 (1975-05-01), Blomback et al.
patent: 3978045 (1976-08-01), Okamoto et al.
patent: 4069323 (1978-01-01), Okamoto et al.
Kikumoto et al., "Thrombin Indicators", J. Med. Chem., (1980), 23, pp. 830-836.
Klausner et al., "The Interaction of .alpha.-N-(p-Toluenesulphonyl)-p-Guanidino-L-Phenylalanine Methyl Ester with Thrombin and Trypsin", Biochem. J., (1978), 169, pp. 157-167.
Sturzebecher, J. et al., "Synthetische Inhibitoren der Serin proteinasen", Pharmazie, 36, H. 9, (1981), pp. 639-641.
Hauptmann, J. et al., "Anticoagulant and Antithrombotic Action of Novel Specific Inhibitors of Thrombin", Thromb. Haem., 43, (1980), pp. 118-123.
Elliot, D. et al., "Bacteriostasis in the Amino Acid Series", J. Chem. Soc., (1949), pp. 1374-1378.
Tsunematsu, H. et al., "Interactions of Derivatives of Guanidinophenylglycine and Guanidinophenylalanine with Trypsin and Related Enzymes, J. Biochem., 88, (1980), pp. 1773-1783.
Shinji Tonomura et al., Kobe J. Med. Sci., 26, 1-9, Mar. 1980, "A Novel Series of Synthetic Thrombin-Inhibitors".
Thrombosis Research, 29; 635-642, 1983, Pergamon Press Ltd., "Cyclic Amides of N-.alpha.-Arylsulfonyl-Aminoacylated 4-Amino-Phenylalanine-Tight Binding Inhibitors of Thrombin", J. Sturzebecher et al.
Moore, S. et al., "Synthesis of Analogues of Bradykinin with Replacement of the Arginine Residues by 4-Guanidinophenyl-L-alanine, J. Chem. Soc. Perkin I, (1977), pp. 2025-2030.
Blomback et al., Chemistry and Biology of Thrombin Ann Arbor Science Pub., Ann Arbor, Michigan, (1977) pp. 276-290.

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