Aromatic heterocyclic derivatives as enzyme inhibitors

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

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C07D21172

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active

060111585

ABSTRACT:
The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.

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Bernstein et al., "Nonpeptide Inhibitors of Human Leukocyte Elastase. 3. Design, Synthesis, X-ray Crystallographic Analysis, and Structure-Activity Relationships for a Series of Orally Active 3-Amino-6-phenylpyridin-2-one Trifluoromethyl Ketones," Journal of Medicinal Chemistry 37(20):313-326 (1994).
Damewood, et al., "Nonpeptidic Inhibitors of Human Leukocycte Elastase. 2. Design, Synthesis and in vitro Activity of a Series of 3-Amino-6arylopyridine-2-one Trifluoromethyl Ketones, " J. Med Chem. 37:3303-3323 (1994).
Maybridge Chemical Co. Ltd., Intermediates Catalogue 6, 1994/95, Trevillett, Tintagel, Cornwall, PL34 OHW, U.K.
Bernstein et al., "Nonpeptidic Inhibitors . . . Trifluoromethyl Ketones", J. Med. Chem., vol. 37, No. 20 (Sep. 30, 1994), pp. 3313-3326.

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