The invention is concerned with novel N-(4-carbamimidoyl-phenyl)-glycine derivatives of the formula:
1
wherein R
1
, E, X
1
to X
4
and G
1
and G
2
are as defined in the description and the claims, as well as hydrates or solvates and physiologically usable salts thereof.
An object of the present invention is to provide a medicinal drug much improved in anti tumor activity and excellent in safety. According to the present invention, there is provided a medicinal drug containing a compound represented by the following general formula (1) or a salt thereof as an active ingredient: [Formula 1] wherein X
1
represents a nitrogen atom or a group —CH═, R
1
represents a group -Z-R
6
, in which Z represents a group —CO—, a group —CH(OH)— or the like, R
6
represents a 5- to 15-membered monocyclic, dicyclic or tricyclic saturated or unsaturated heterocyclic group having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms, R
2
represents a hydrogen atom or a halogen atom, Y represents a group —O—, a group —CO—, a group —CH(OH)— or a lower alkylene group, and A represents [Formula 2] wherein R
3
represents a hydrogen atom, a lower alkoxy group or the like, p represents 1 or 2, R
4
represents an imidazolyl lower alkyl group or the like.
A highly enantioselective Friedel–Craftsreaction of activatedphenols with (E)-4-oxo-4-arylbutenoates has been developed with the N,N′-dioxide-scandium(III) complex as the catalyst. A variety of (E)-4-oxo-4-arylbutenoates were found to be suitable substrates for the reaction. The desired products were obtained in moderate to high yields (up to 98%) and excellent enantioselectivities (up to 97% ee)
The invention is concerned with novel N-(4-carbamimidoyl-phenyl)-glycine derivatives of the formula:
1
wherein R
1
, E, X
1
to X
4
and G
1
and G
2
are as defined in the description and the claims, as well as hydrates or solvates and physiologically usable salts thereof.
The present invention provides a novel compound, which has an excellent effect of suppressing the generation of collagen and less side effects, with being excellent in terms of safety. The compound of the present invention is represented by the following general formula (1):
[wherein X
1
represents a nitrogen atom or a group —CH═; R
1
represents a group -Z-R
6
, wherein Z represents a group —CO—, a group —CH(OH)—, or the like, and R
6
represents a 5- to 15-membered monocyclic, dicyclic, or tricyclic, saturated or unsaturated heterocyclic group having 1 to 4 nitrogen atoms, oxygen atoms, or sulfur atoms; R
2
represents a hydrogen atom, a halogen atom or a lower alkylene group; Y represents a group —O—, a group —CO—, a group —CH(OH)—, a lower alkylene group, or the like; and A represents a group
or the like, wherein R
3
represents a hydrogen atom, a lower alkoxy group, or the like, p represents 1 or 2, and R
4
represents an imidazolyl lower alkyl group or the like.