Thrombin inhibitors

A compound having the formula:

• ##STR14## wherein R.sup.1 and R.sup.2 are independently
• hydrogen,
• phenyl unsubstituted, mono- or di-substituted with OH, C.sub.1-4 alkyl, oxo, or halo,
• naphthyl,
• biphenyl,
• a 5-to 7-membered mono- or bicyclic heterocyclic ring or bicyclic heterocyclic ring system any ring of which may be saturated or unsaturated, and which consists of carbon atoms and from one to three heteroatoms selected from the group consisting of N, O and S, C.sub.1-4 alkyl,
• branched C.sub.1-4 alkyl,
• C.sub.3-7 cycloalkyl,
• C.sub.5-12 bicyclic alkyl,
• C.sub.11-16 tricyclic alkyl,
• R.sup.4 (CH.sub.2).sub.n,
• (R.sup.4).sub.2 CH, wherein R.sup.4 is the same or different,
• (R.sup.4)(R.sup.4 O)CH, wherein R.sup.4 is the same or different,
• R.sup.4 O(CH.sub.2).sub.n, or
• R.sup.2 may be joined with R.sup.1 to form a four- to seven membered carbon ring in which zero to two carbon atoms may be substituted with heteroatoms independently selected from the list N, O, and S,
• where n is 1, 2, 3 or 4;
• and
• R.sup.3 is
• H,
• HO(CH.sub.2).sub.p, where p is 0, 1, 2, 3 or 4;
• or ##STR15## wherein Z is C, O or a bond;
• provided that when R.sup.3 is hydrogen and either one of R.sup.1 or R.sup.2 is hydrogen, the other of R.sup.1 and R.sup.2 is not
• phenyl,
• mono-hydroxy substituted phenyl
• a 5-to 7-membered mono- or bicyclic heterocyclic ring or bicyclic heterocyclic ring system any ring of which may be saturated or unsaturated, and which consists of carbon atoms and from one to three heteroatoms selected from the group consisting of N,O and S.
• C.sub.3-7 cycloalkyl,
• C.sub.5-12 bicyclic heterocyclic, or
• R.sup.4 (CH.sub.2).sub.n, where n is 1, 2, 3, or 4, and R.sup.4 is
• phenyl,
• mono-hydroxy substituted phenyl,
• a 5-to 7-membered mono or bicyclic heterocyclic ring or bicyclic heterocyclic ring system any ring of which may he saturated or unsaturated, and which consists of carbon atoms and from one to three heteroatoms selected from the group consisting of N, O and S,
• C.sub.3-7 cycloalkyl, or
• C.sub.5-12 bicyclic alkyl;
• R.sup.4 is
• phenyl unsubstituted, mono- or di-substituted with OH, OMe, C.sub.1-4 alkyl, oxo, or halo,
• naphthyl,
• biphenyl,
• 1-dibenzocycloheptene,
• a 5-to 7-membered mono- or bicyclic heterocyclic ring or bicyclic heterocyclic ring system any ring of which may be saturated or unsaturated, and which consists of carbon atoms and from one to three heteroatoms selected from the group consisting of N, O and S,
• C.sub.1-4 alkyl,
• branched C.sub.1-4 alkyl,
• C.sub.3-7 cycloalkyl,
• C.sub.5-12 bicyclic alkyl, or
• C.sub.11-16 tricyclic alkyl;
• and,
• X is
• (CH.sub.2)q where q is 1 or 2,
• NR.sup.1 CH.sub.2, or
• SCH.sub.2,
• or a pharmaceutically acceptable salt thereof.