Polyamidic acid derivatives with antigastrin activity, a method for their preparation, and their pharmaceutical use

A compound represented by Formula (I):

• ##STR27## wherein s is 1 or 2, wherein R.sub.1 is a member selected from the group consisting of an unsubstituted or mono- or di-substituted phenyl group, wherein the substituents of the mono- or di-substituted phenyl group are selected from the group consisting of a chloro group, a fluoro group, a bromo group, a trifluoromethyl group, a linear or branched C.sub.1 -C.sub.4 alkyl group, a nitro group, a cyano group, and a methoxy group;
• a 2-naphthyl group, a 2-(or 3-)indolyl group;
• and a 2-(or 3-)quinolinyl group;
• wherein R.sub.2 is:
• a.sub.1) a group represented by:
• ##STR28## wherein m and n are each an integer of from 1 to 3, provided that the ring formed consists of at least 5 atoms, X and Y are each selected from the group consisting of (CH--R.sub.3).sub.z, TCH.sub.2 and CH.sub.2 T, where T is O or S, wherein R.sub.3 is a member selected from the group consisting of H, CH.sub.3 and C.sub.2 H.sub.5, and wherein z is 0 or an integer of from 1 to 3, provided that the ring formed consists of at least 3 atoms,
• wherein R.sub.3a, R.sub.3b and R.sub.3d are H or CH.sub.3,
• wherein R.sub.3c and R.sub.3e are H or Ch.sub.3,
• wherein r.sub.1, r.sub.2 and r.sub.3 are each 0 or an integer of from 1 to 2,
• wherein W is a member selected from the group consisting of H, a linear or branched C.sub.1 -C.sub.6 alkyl group, OH, OCH.sub.3, SH, a benzyloxyl group, a thiomethyl group (CH.sub.3 --S--), or W is a member selected from the group consisting of a cycloalkane group, a heterocyclic group, a mono- or dicyclic aromatic or hydro-aromatic group having up to 10 carbon atoms, which is unsubstituted or substituted with a substituent selected from the group consisting of a fluoro group, a chloro group, a methyl group, a ethyl group, a trifluoromethyl group, a methoxy group, a cyano group, and a nitro group, or W is a CO-R.sub.6 group, where R.sub.6 is selected from the group consisting of:
• a.sub.2) a linear or branched amino group represented by:
• ##STR29## wherein R.sub.7 is selected from the group consisting of H and a linear or branched C.sub.1 -C.sub.5 alkyl group and an alkoxyalkyl group;
• and R.sub.8 is selected from the group consisting of H, a C.sub.1 -C.sub.5 alkyl group and a (CH.sub.2).sub.z -Ar group, wherein z has the meaning given above and Ar is an unsubstituted phenyl group or mono- or di-substituted phenyl group, wherein the substituents of the mono- or di-substituted phenyl group are selected from the group consisting of a fluoro group, a chloro group, a methyl group, an ethyl group, a trifluoromethyl group and a methoxy group;
• or a 1 (or 2)-naphthyl group;
• b.sub.2) a monocyclic aminoalkyl group represented by:
• ##STR30## wherein z, R.sub.3 and R.sub.7 have the meanings given above, z.sub.1 and z.sub.2 are each an integer of from 1 to 4, provided that the ring formed consist of 4 to 10 carbon atoms;
• c.sub.2) a dicyclic aminospiro group represented by:
• ##STR31## wherein R.sub.3, R.sub.7, s, z.sub.1 and z.sub.2 have the meanings given above;
• d.sub.2) a dicyclic (orthofused) amino group, represented by:
• ##STR32## wherein R.sub.3, R.sub.7, s, z.sub.1 and z.sub.2 have the meanings given above;
• e.sub.2) a dicyclic amino group represented by:
• ##STR33## wherein R.sub.3, R.sub.7, s, z, z.sub.1 and z.sub.2 have the meanings given above;
• f.sub.2) an azacycloalkyl group represented by:
• ##STR34## wherein R.sub.3, z.sub.1 and z.sub.2 have the meanings given above;
• g.sub.2) an azadicyclic (orthofused) group, represented by:
• ##STR35## wherein R.sub.3, s, z.sub.1 and z.sub.2 have the meanings given above;
• h.sub.2) a dicyclic azaspiro group represented by:
• ##STR36## wherein R.sub.3, s, z.sub.1 and z.sub.2 have the meanings given above;
• i.sub.2) an azadicyclic group represented by:
• ##STR37## wherein R.sub.3, s, z.sub.1 and z.sub.2 have the meanings given above;
• l.sub.2) an azacycloalkyl group represented by:
• ##STR38## wherein R.sub.3, z.sub.1, z.sub.2 and T have the meanings given above;
• and m.sub.2) an aminoalkyl adamantyl group represented by:
• ##STR39## wherein R.sub.3 and z have the meanings given above and Ad is adamantyl (1- or 2-yl);
• wherein the stereochemistry of the chiral center marked by (*) in Formula (I) is in the R configuration;
• and the stereochemistry of the carbon atom marked by (**), which may be asymmetrical according to the substituents bonded thereto, may be R, RS or S.