Heteroaromatic and thioheteroaromatic substituted sulfonamide th

Details Heteroaromatic and thioheteroaromatic substituted sulfonamide th Heteroaromatic and thioheteroaromatic substituted sulfonamide th

1992-12-24

1994-07-26

Ivy, C. Warren

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

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

540467, 540470, 540450, 540544, 540553, 540575, 544 3, 544 53, 544 88, 544 98, 544238, 544242, 546166, 546256, 546275, 548146, 548206, 548215, 5483641, 5483111, 548517, C07D21536, C07D21558, C07D21502

Patent

active

053328221

ABSTRACT:
Sulfonamide thrombin inhibitors are provided which have the structure ##STR1## including all stereoisomers thereof, wherein X is S or --CH.sub.2 --; m is 0, 1 or 2 when X is --S-- or m is 0 when X is --CH.sub.2 --; n is 1, 2 or 3; R.sup.1 and R.sup.2 are independently H, lower alkyl, cyclo-alkyl, aryl, heteroaryl or heteroarylalkyl, or R.sup.1 and R.sup.2 can be taken together with the N atom to which they are attached to form a 5- to 8-membered ring which may optionally contain an additional N, O or S atom in the ring; R.sup.3 is heteroaryl; and R.sup.4 is alkyl, cycloalkyl, aryl, heteroaryl, quinolinyl or tetrahydroquinolinyl, and pharmaceutically acceptable salts thereof.

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J. Indian Chem. Soc., 53(3), pp. 274-278, Mar. 1976.
CA 62:2434f, "Screening of Antipolio . . . " by Otaki et al., 1965.
Merck Index, 9th Edition, #7770, p. 7767, 1976.
Angliker, Herbert et al., "Pseudoarginine: synthesis and properties of derivatives of .delta.-(1-imidazolyl)norvaline", Biochem. J. (1990) 266, 829-834.
Hijikata-Okunomiya, Akiko et al., "A Strategy for a Rational Approach to Designing Synthetic Selective Inhibitors", Seminars in Thrombosis and Hemostasis-vol. 18, No. 1, 1992, pp. 135-149.

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