Amidinopyrroline derivatives, processes for their production and pharmaceutical agents containing these compounds

A compound of formula (I) ##STR21## wherein R.sub.1, R.sub.2 and Y are each independently selected from the group consisting of:

• (1) hydrogen;
• (2) C1-C6 alkyl which is unsubstituted or substituted with phenyl which is unsubstituted or substituted with O--(C1-C6 alkyl) which is unsubstituted or substituted by a 5- or 6-membered heterocyclic ring having 1-2 heteroatoms and having 1-2 substituents which is unsubstituted or has 1-2 substituents each independently selected from the group consisting of .dbd.O and (C1-C6 alkyl)--C(.dbd.O)--OH;
• (3) a 5- or 6-membered heterocyclic ring having 1-2 heteroatoms which is unsubstituted or substituted with
• (A) (C1-C6 alkyl)--C(.dbd.O)-phenyl which is unsubstituted or substituted in the phenyl with 1-2 O--(C1-C6 alkyl)--C(.dbd.O)--OH groups, or
• (B) a 5- or 6-membered heterocyclic ring having 1-2 heteroatoms which is unsubstituted or substituted with (C1-C6 alkyl)--C(.dbd.O)--OH;
• (4) a 5- or 6- membered carbocyclic ring which is unsubstituted or substituted with (C1-C6 alkyl)--C(.dbd.O)--OH;
• and
• (5) --V--C(.dbd.O)--X where V is a chemical bond or C1-C6 alkyl and X is selected from the group consisting of
• (A) C1-C6 alkyl which is unsubstituted or substituted 1-2 times by
• (i) N(--R.sub.3)--R.sub.4, where R.sub.3 and R.sub.4 are each independently selected from the group consisting of hydrogen, a 5- or 6-membered carbocyclic ring and C(.dbd.O)--R.sub.5 where R.sub.5 is selected from the group consisting of (1) C1-C6 alkyl which is unsubstituted or has 1-2 substituents selected from the group consisting of phenyl, N(--H)--(C1-C6 alkyl) and N(--H)-(sulfonyl C1-C6 alkyl) and (2) a 1-2 ring heterocycle having 1-3 heteroatoms, or R.sub.3 and R.sub.4, together with the N atom to which they are attached, form a 5-7 membered heterocyclic ring which is unsubstituted or has 1-2 substituents each independently selected from the group consisting of .dbd.O, N(--H)--(C1-C6 alkyl) and N(--H)-(sulfonyl C1-C6 alkyl), (ii) C(.dbd.O)--N(--H)--(C1-C6 alkyl) where the alkyl is unsubstituted or has 1-3 substitutents each independently selected from the group consisting of C1-C6 alkyl, .dbd.O, --OH, phenyl, a 5- or 6-membered heterocyclic ring having 1-2 heteroatoms, and .dbd.CH, and
• (iii) a 5- or 6-membered carbocyclic ring,
• (B) a 5- or 6-membered heterocyclic ring having 1-2 heteroatoms and which is unsubstituted or has 1-2 C1-C6 alkyl substituents each of which is unsubstituted or substituted with 1-3 substituents each independently selected from the group consisting of .dbd.O, --OH, --O--CH3, a 5- or 6-membered carbocyclic ring, a 1-2 ringed heterocyclic ring having 1-3 heteroatoms and N(--H)--(C1-C6 allyl) where the alkyl is unsubstituted or has 1-2 substitutents each independently selected from .dbd.O, --OH, SO2 and 5- or 6-membered heterocyclic ring having 1-2 heteroatoms;
• (C) phenyl which is unsubstituted or is substituted with --O--(C1-C6 alkyl) wherein the alkyl is unsubstituted or has 1-2 substituents each independently selected from the group consisting of .dbd.O and --OH, or the phenyl forms one ring of a bicyclic heterocycle containing 1-2 heteroatoms which is unsubstituted or has 1-3 substituents each independently selected from the group consisting of .dbd.O and C1-C6 alkyl which is unsubstituted or has 1-2 substituents selected from the group consisting of phenyl, .dbd.O and --OH;
• and
• (D) N(--H)--(C1-C6 alkyl) which is unsubstituted or substituted by 1-4 substituents each independently selected from the group consisting of .dbd.O, --OH and N(--H)--(C1-C6 alkyl) wherein the alkyl is unsubstituted or has 1-3 substituents each independently selected from the group consisting of phenyl, .dbd.O and --OH;
• or
• two of R.sub.1, R.sub.2 and Y, together with the N to which they are bound, form a 1-2 ring heterocycle with 0-1 additional heteroatoms, which is unsubstituted or substituted by 1-3 substituents independently selected from the group consisting of .dbd.O, C1-C6 alkyl wherein the allyl is unsubstituted or has 1-2 substituents each independently selected from the group consisting of (A) .dbd.O, (B) N(--H)--(C1-C6 alkyl) which is unsubstituted or substituted by 1-2 substituents each independently selected from the group consisting of .dbd.O and --OH, (C) --O-- phenyl which is unsubstituted or substituted in the phenyl with C1-C6 alkyl which is unsubstituted or substituted by 1-2 substituents each independently selected from the group consisting of .dbd.O and --OH, (D) carbocycle which is unsubstituted or substituted with C1-C6 alkyl which is unsubstituted or substituted by 1-2 substituents each independently selected from the group consisting of .dbd.O and --OH, (E) C1-C6 alkyl which is unsubstituted or substituted with 1-2 substituents each independently selected from the group consisting of (i) .dbd.O, (ii) N(--H)--(C1-C6 alkyl) which is unsubstituted or substituted by 1-2 substituents each independently selected from the group consisting of .dbd.O and --OH and (iii) a 5- or 6-membered heterocyclic ring having 1-2 heteroatoms which is unsubstituted or substituted with C1-C6 alkyl which is unsubstituted or substituted by 1-2 substituents each independently selected from the group consisting of .dbd.O and --OH,
• and the third of R.sub.1, R.sub.2 and Y is selected from the group consisting of groups (1)-(5) as noted above.