Patent ID: 6251909
Filing Date: 2001-06-26
Classification: A61P,C07D

Abstract:
An arylglycinamide derivative of formula I: ##STR97##or the pharmaceutically acceptable salts thereof, whereinAr is unsubstituted or mono- to penta-substituted phenyl, wherein the substituents are independently selected from the group consisting of halogen, hydroxy, (C.sub.1-4)alkyl, O--(C.sub.1-4)alkyl, CF.sub.3, OCF.sub.3 and NR.sup.9 R.sup.10, wherein R.sup.9 and R.sup.10 are independently selected from the group consisting of hydrogen, methyl and acetyl, orAr is phenyl having a substituent selected from the group consisting of --OCH.sub.2 O-- and --O(CH.sub.2).sub.2 O--;R.sup.1 and R.sup.2 together with the N to which they are bound form a ring of the formula ##STR98##whereinp is 2or 3;X is N(CH.sub.2).sub.n R.sup.6 ;n is 0, 1 or 2,R.sup.6 is (C.sub.3-7)cycloalkyl, phenyl or naphthyl, wherein the phenyl is optionally mono- to tri-substituted by halogen, (C.sub.1-4)alkyl, O--(C.sub.1-4)alkyl, CF.sub.3, OCF.sub.3 or NR.sup.9 R.sup.10, wherein R.sup.9 and R.sup.10 are independently selected from the group consisting of hydrogen, methyl and acetyl;R.sup.3 is hydrogen, (C.sub.1-4)alkyl, unsubstituted or mono- to tri-substituted phenyl, wherein the substituents are independently selected from the group consisting of halogen, (C.sub.1-4)alkyl, O--(C.sub.1-4)alkyl, CF.sub.3, OCF.sub.3 and NR.sup.9 R.sup.10, wherein R.sup.9 and R.sup.10 are independently selected from the group consisting of hydrogen, methyl and acetyl;R.sup.4 is phenyl(C.sub.1-4)alkyl or naphthyl(C.sub.1-4)alkyl, wherein phenyl is optionally substituted by 1 to 3 substituents, wherein the substituents are independently selected from the group consisting of halogen, (C.sub.1-4)alkyl, O--(C.sub.1-4)alkyl, CF.sub.3, OCF.sub.3 and NR.sup.11 R.sup.12, wherein R.sup.11 and R.sup.12 are independently selected from the group consisting of hydrogen, methyl and acetyl; andR.sup.5 is hydrogen, (C.sub.1-4)alkyl, (C.sub.3-6)cycloalkyl, CH.sub.2 COOH, CH.sub.2 C(O)NH.sub.2, hydroxy, or phenyl(C.sub.1-4)alkyl.