Patent ID: 6294556
Filing Date: 2001-09-25
Classification: A61P,C07D

Abstract:
An arylglycinamide derivative of formula I: ##STR100##or the pharmaceutically acceptable salts thereof, whereinAr is unsubstituted or mono- to penta-substituted phenyl, or unsubstituted or mono- or di-substituted naphthyl, in which the substituents of the phenyl and naphthyl 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 substituted by --O--CH.sub.2 --O or --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 ##STR101##whereinp is 2 or 3,X is CR.sup.7 R.sup.8, wherein R.sup.7 and R.sup.8 have one of the following meanings:(a) R.sup.7 and R.sup.8 are each hydrogen when R.sup.3 is unsubstituted or substituted phenyl;(b) R.sup.7 is phenyl,phenyl 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 and OCF.sub.3,piperidinyl,1-methylpiperidinyl, ##STR102##when R.sup.8 is hydrogen, --CONH.sub.2, --NHC(O)CH.sub.3, --N(CH.sub.3)C(O)CH.sub.3, CN, --C(O)NH(C.sub.1-3)alkyl, or --C(O)N((C.sub.1-3)alkyl).sub.2 ; or(c) R.sup.7 and R.sup.8 together form the group ##STR103##R.sup.3 is hydrogen, (C.sub.1-4)alkyl, unsubstituted phenyl 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, 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; 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.