| abstract |
New pharmacologically active amidino derivatives as muscarinic receptor nblocking agents which are useful for the treatment of gastrointestinal ndisorders of the following formula nA― n = N―R₁ (I) n nwherein nR represents hydrogen atom, C₁₋₅ alkyl, aryl, an amino group optionally nsubstituted by one or two C₁₋₅ alkyl; nR₁ represents hydrogen atom, C₁₋₈ alkyl, aralkyl; nA represents nC₁₋₅ alkyl substituted by 2 or 3 radicals, which may be identical nor different from each other, selected from aryl, cycloalkyl, carbonxamide; nor a saturated 6-membered heterocyclic ring containing one nitrogen natom N-substituted by COR₂ where R₂ is a methyl substituted by 2 or n3 radicals, which may be identical or different from each other, nselected from aryl, cycloalkyl, hydroxy; nor n nwhere R₃ is hydrogen atom and R₄ is C₁₋₅ alkyl substitued nby 2 or 3 radicals, which may be identical or different from each nother, selected from aryl, cycloalkyl, carboxamide, or by hydroxy noptionally esterified with a cycloalkylcarboxylic acid, or R₃ and nR₄, together with the nitrogen atom to which they are attached, nform a saturated 5- to 7-membered heterocyclic ring, optionally ncontaining one or two nitrogen atoms or an endocyclic carboxamido ngroup optionally comprising in its inside -CH₂-CH₂- or n nbeing the heterocyclic ring substituted by a C₁₋₅ alkyl substituted n n nin turn by 2 or 3 radicals, which may be identical or different from neach other, selected from C₁₋₅ alkyl, aryl, cycloalkyl or hydroxy, or nbyarylalkylene, or by -OR₅ where R₅ is -OCR₆ where R₆ is methyl substintuted by 2 or 3 radicals, which may be identical or different from each nother, selected from a saturated or unsaturated C₁₋₅ alkyl, aryl, cyclonalkyl, hydroxy C₁₋₅ alkyl, hydroxy, or unsaturated 6-membered heteroncyclic ring, provided that at least one between R and A is amino group nor n n The tautomers and the acid addition salts of these compounds, as well as nthe process for the preparation of the compounds of formula (I) and npharmaceutical compositions containing them are also described. |