Patent ID: 6136805
Filing Date: 2000-10-24
Classification: A61P,C07D,C07F

Abstract:
A compound of formula I ##STR6## wherein R.sup.1 is --(CH.sub.2).sub.n --CR.sup.2 H--(CH.sub.2).sub.m --ZR.sup.5, R.sup.6, R.sup.7 and R.sup.8 are the same or different and are hydrogen; C.sub.1-6 alkyl, in which optionally one or more hydrogen atoms are replaced by halogen atoms; nitro; halogen; NR.sup.9 R.sup.10 ; SO.sub.p R.sup.11 ; SO.sub.2 NR.sup.12 R.sup.13 ; SO.sub.3 H; SO.sub.3 C.sub.1-6 -alkyl or OR.sup.14,R.sup.2 is hydrogen or --(CH.sub.2).sub.q --R.sup.3,R.sup.3 is hydrogen, hydroxy, C.sub.1-6 -alkoxy or NR.sup.15 R.sup.16, n, m and q each are 0, 1, 2 or 3,Z is POXY, OPOXY, SO.sub.2 R.sup.17, CO.sub.2 R.sup.18, halogen, cyano or tetrazole,R.sup.11 is H, C.sub.1-6 -alkyl or phenyl,p is 0, 1, or 2,R.sup.12 and R.sup.13, independently of one another, are hydrogen or C.sub.1-4 -alkyl,R.sup.14 is A--R.sup.19 or a C.sub.6-12 -aryl or 5- or 6-membered hetaryl radical having 1-3 N, O and/or S atoms, optionally substituted with halogen C.sub.1-6 -alkoxy, hydroxy, cyano, NR.sup.20 R.sup.21, C.sub.1-6 -alkyl optionally substituted with halogen, and/or COR.sup.22,A is straight-chain or branched, saturated or unsaturated C.sub.1-10 -alkylene, wherein one or more carbon atoms is optionally replaced by O, S and/or NR.sup.26 and optionally substituted in one or more places with halogen,R.sup.19 is hydrogen; NR.sup.24 R.sup.25 ; halogen; C.sub.1-6 -alkyl, optionally substituted in one or more places with halogen; C.sub.1-6 -alkoxy; COR.sup.23 ; CN or a C.sub.6-12 -aryl or 5- or 6-membered hetaryl radical having 1-3 N, O and/or S atoms, optionally substituted with halogen, C.sub.1-6 -alkoxy, hydroxy, cyano, NR.sup.20 R.sup.21, C.sub.1-6 -alkyl optionally substituted with halogen, and/or COR.sup.22,R.sup.18 is hydrogen, C.sub.1-4 -alkyl, hydroxy, C.sub.1-6 -alkoxy or NR.sup.27 R.sup.28,R.sup.17, R.sup.22 and R.sup.23 are hydroxy, C.sub.1-6 alkoxy or NR.sup.29 R.sup.30,R.sup.26 is hydrogen, C.sub.1-4 -alkyl or C.sub.1-6 -alkanoyl,X and Y are the same or different and are hydroxy, C.sub.1-6 -alkoxy, C.sub.1-4 -alkyl or NR.sup.27 R.sup.28,R.sup.9 and R.sup.10, R.sup.20 and R.sup.21 and or R.sup.25 and R.sup.24 are the same or different and are hydrogen; CO--C.sub.1-6 -alkyl, phenyl or C.sub.1-6 -alkyl, optionally substituted with C.sub.1-4 -alkoxy or an amino group optionally mono- or disubstituted with C.sub.1-4 -alkyl; or together with the nitrogen atom form a saturated 5- or 7-membered saturated heterocycle optionally having another N, S or O atom and optionally substituted 1-3 times with C.sub.1-4 -alkyl or a phenyl, benzyl or benzoyl radical optionally substituted by halogen, or form an unsaturated 5-membered heterocycle having 1-3 N atoms and optionally substituted once or twice with cyano, C.sub.1-4 -alkyl, phenyl or CO--C.sub.1-6 -alkyl,R.sup.15 and R.sup.16, R.sup.27 and R.sup.28 and/or R.sup.29 and R.sup.30 are the same or different and are hydrogen, C.sub.1-4 -alkyl, phenyl or together with the nitrogen atom form a saturated 5- or 7-membered saturated heterocycle optionally having another oxygen, sulfur or nitrogen atom and optionally substituted 1-3 times with C.sub.1-4 -alkyl or a phenyl, benzyl or benzoyl radical optionally substituted by halogen, or form an unsaturated 5-membered heterocycle optionally having 1-3 N atoms and optionally substituted once or twice with cyano, C.sub.1-4 -alkyl, phenyl or CO.sub.2 C.sub.1-6 -alkyl,with the provisos thatone of the radicals R.sup.5 -R.sup.8 always is OR.sup.14, and R.sup.14 does not mean H or C.sub.1-6 -alkyl optionally substituted in 1-3 places with halogens, andif Z is CO.sub.2 R.sup.18 and one of the radicals R.sup.5 -R.sup.8 is OR.sup.14, at least one other radical R.sup.5 -R.sup.8 is C.sub.1-4 -alkyl substituted by halogen.