Racemates, diastereoisomers and optical isomers of a compound of formula
(I):
##STR1##
wherein
B is H, a C.sub.6 or C.sub.10 aryl, C.sub.7-16 aralkyl; Het or (lower
alkyl)-Het, all of which optionally substituted with C.sub.1-6 alkyl;
C.sub.1-6 alkoxy; C.sub.1-6 alkanoyl; hydroxy; hydroxyalkyl; halo;
haloalkyl; nitro; cyano; cyanoalkyl; amino optionally substituted with
C.sub.1-6 alkyl; amido; or (lower alkyl)amide; or
B is an acyl derivative of formula R.sub.4 --C(O)--; a carboxyl of formula
R.sub.4 --O--C(O)--; an amide of formula R.sub.4 --N(R.sub.5)--C(O)--; a
thioamide of formula R.sub.4 --N(R.sub.5)--C(S)--; or a sulfonyl of
formula R.sub.4 --SO.sub.2 ; R.sub.5 is H or C.sub.1-6 alkyl; and
Y is H or C.sub.1-6 alkyl;
R.sup.3 is C.sub.1-8 alkyl, C.sub.3-7 cycloalkyl, or C.sub.4-10
alkylcycloalkyl, all optionally substituted with hydroxy, C.sub.1-6
alkoxy, C.sub.1-6 thioalkyl, amido, (lower alkyl)amido, C.sub.6 or
C.sub.10 aryl, or C.sub.7-16 aralkyl;
R.sub.2 is CH.sub.2 --R.sub.20, NH--R.sub.20, O--R.sub.20 or S--R.sub.20,
wherein R.sub.20 is a saturated or unsaturated C.sub.3-7 cycloalkyl or
C.sub.4-10 (alkylcycloalkyl), all of which being optionally mono-, di- or
tri-substituted with R.sub.21,
or R.sub.20 is a C.sub.6 or C.sub.10 aryl or C.sub.7-14 aralkyl optionally
substituted, or R.sub.20 is Het or (lower alkyl)-Het, both optionally
substituted, Het or (lower alkyl)-Het; carboxyl;
carboxy(lower alkyl); C.sub.6 or C.sub.10 aryl, C.sub.7-14 aralkyl or Het,
said aryl, aralkyl or Het being optionally substituted; and
R.sup.1 is H; C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.2-6 alkenyl, or
C.sub.2-6 alkynyl, all optionally substituted with halogen; or a
pharmaceutically acceptable salt or ester thereof.
Racemates, diastereoisomers en optische isomeren van een samenstelling van formule (I): ## STR1 ## waarin B is H, C.sub.6 of C.sub.10 aryl, aralkyl C.sub.7-16; Het of (lagere alkyl)-het, die naar keuze met alkyl c.sub.1-6 substitueerde; alkoxy c.sub.1-6; alkanoyl c.sub.1-6; hydroxy; hydroxyalkyl; halo; haloalkyl; nitro; cyano; cyanoalkyl; amino naar keuze gesubstitueerd met alkyl c.sub.1-6; amido; of (lagere alkyl)amide; of B is een acyl derivaat van formule R.sub.4 -- C (O); carboxyl van formule R.sub.4 -- O -- C (O); een amide van formule R.sub.4 -- N (R.sub.5) -- C (O) - -; een thioamide van formule R.sub.4 -- N (R.sub.5) -- C (S) - -; of sulfonyl van formule R.sub.4 -- SO.sub.2; R.sub.5 is H of alkyl c.sub.1-6; en Y is H of alkyl c.sub.1-6; R.sup.3 is alkyl c.sub.1-8, cycloalkyl c.sub.3-7, of c.sub.4-10 alkylcycloalkyl, allen naar keuze gesubstitueerd met hydroxy, alkoxy c.sub.1-6, amido thioalkyl c.sub.1-6, (lagere alkyl)amido, aryl C.sub.6 of C.sub.10, of aralkyl C.sub.7-16; R.sub.2 is CH.sub.2 -- R.sub.20, NH -- R.sub.20, O -- R.sub.20 of S -- R.sub.20, waarin R.sub.20 een verzadigde of onverzadigde c.sub.3-7 cycloalkyl of c.sub.4-10 is (alkylcycloalkyl), die is zijn naar keuze mono -, Di - of tri-substituted met R.sub.21, of R.sub.20 naar keuze gesubstitueerde aryl C.sub.6 of C.sub.10 of aralkyl C.sub.7-14, of R.sub.20 is Het of (lagere alkyl)-het, naar keuze gesubstitueerd allebei, Het of (lagere alkyl)-het; carboxyl ub.6 or C.sub.10 aryl or C.sub.7-14 aralkyl optionally substituted, or R.sub.20 is Het or (lower alkyl)-Het, both optionally substituted, Het or (lower alkyl)-Het; carboxyl; carboxy(lower alkyl); C.sub.6 of aryl C.sub.10, aralkyl C.sub.7-14 of Het, zeiden aryl, aralkyl of Het die naar keuze worden gesubstitueerd; en R.sup.1 is H; c.sub.1-6 substitueerden alkyl, cycloalkyl c.sub.3-7, alkenyl c.sub.2-6, of c.sub.2-6 alkynyl, allen naar keuze met halogeen; of een farmaceutisch aanvaardbare zout of een ester daarvan.
