Aromatic hetherocyclic derivatives as enzyme inhibitors

Details Aromatic hetherocyclic derivatives as enzyme inhibitors Aromatic hetherocyclic derivatives as enzyme inhibitors

1995-12-18

1999-12-28

Shah, Mukund J.

Organic compounds -- part of the class 532-570 series

Organic compounds

Nitrogen attached directly or indirectly to the purine ring...

544311, 544320, 544321, C07D23902

Patent

active

060083514

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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Williams, et al., "1-(((7,7-Dimethyl-2(S)-(2(S)-amino-4-(methylsulfonyl)butyramido)biccylo[2 .2.1]-heptan-1(S)-yl)methyl)sulfonyl)-4(2-methylphenyl)piperazine(L-368,889 ): An Orally Bioavailable, Non-Peptide Oxytocin Antagonist with Potential Utility for Managing Preterm Labor," J. Med. Chem. 37:565-571 (1994).
Damewood, et al., "Nonpeptidic Inhibitors of Human Leukoycyte Elastase.2.Design, Synthesis, and in vitro Acitvity of a Series of 3-Amino-6arylopyrideni-2-one Trifluoromethyl Ketones," J. Med. Chem. 37:3303-3312 (1994).
Skiles, et al., "Elastase Inhibitors Containing Conformationally Restricted Lactams as P.sub.3 -P.sub.2 Dipeptide Replacements," Bioorg. Med. Chem. Lett. 3(4):773-779 (1993).
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).
Maybridge Chemical Co. Ltd., Intermediates Catalogue 6, 1994/95, Trevillett, Tintagel, Cornwall, PL34 OHW, U.K.

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