Patent ID: 6063800
Filing Date: 2000-05-16
Classification: C07D,C07F

Abstract:
A compound of formula (I)(L).sub.n --Ar.sub.1 --R.sub.1 --Awhereinn is 1, 2, 3, 4, or 5 and (L).sub.n represents up to five (5) substituents which independently of each other are hydrogen, C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy, hydroxy, halogen, trihalogenomethyl, hydroxy-C.sub.1-6 -alkyl, amino-C.sub.1-6 -alkyl, --COR.sub.2, --NO.sub.2, --CN, --CHO, C.sub.1-6 -alkanoyloxy, carbamoyl, --NR.sub.5 R.sub.6, aryloxy optionally substituted;R.sub.2 is C.sub.1-6 -alkyl, aryl optionally substituted, aralkyl optionally substituted, --OH, --NR.sub.3 R.sub.4 wherein R.sub.3 and R.sub.4 independently of each other are hydrogen, C.sub.1-6 -alkyl, aryl optionally substituted, aralkyl optionally substituted;R.sub.5 and R.sub.6 are independently of each other hydrogen or C.sub.1-6 -alkyl, aryl optionally substituted, aralkyl optionally substituted or --COZ.sub.1 wherein Z.sub.1 is C.sub.1-6 -alkyl, aryl optionally substituted, aralkyl optionally substituted;or L is A.sub.1 --Y.sub.1 --(W.sub.1)--X--(W.sub.2)--Y.sub.2 -- wherein X is a chemical bond, --CO, --CONR.sub.7, --NR.sub.7 CO, --NR.sub.7, --O--, --S--, --SO, or --SO.sub.2 ;Y.sub.1 and Y.sub.2 are independently a chemical bond, --O--, --S--, or --NR.sub.7 ;R.sub.7 is hydrogen, C.sub.1-6 -alkyl, aryl optionally substituted, aralkyl optionally substituted, thiazole and isothiazole optionally substituted, --COZ.sub.2 wherein Z.sub.2 is C.sub.1-6 -alkyl, aryl optionally substituted, aralkyl optionally substituted;W.sub.1 and W.sub.2 are independently a chemical bond or saturated or unsaturated C.sub.1-6 -alkylene;A.sub.1 is aryl optionally substituted, thiazole or isothiazole optionally substituted, biaryl optionally substituted, --NR.sub.8 R.sub.9 wherein R.sub.8 and R.sub.9 independently are hydrogen, C.sub.1-6 -alkyl, aryl optionally substituted, aralkyl optionally substituted, thiazole or isothiazole optionally substituted, --COZ.sub.3 wherein Z.sub.3 is C.sub.1-6 -alkyl, aryl optionally substituted, aralkyl optionally substituted, thiazole or isothiazole optionally substituted orwhen R.sub.8 and R.sub.9 together with the nitrogen atoms forms a ring system, A.sub.1 is a thiazole or isothiazole ring system optionally substituted with C.sub.1-6 -alkyl, aryl optionally substituted, aralkyl optionally substituted, --OH, C.sub.1-6 -alkoxy, hydroxy-C.sub.1-6 -alkyl, amino-C.sub.1-6 -alkyl, --COZ.sub.4wherein Z.sub.4 is --OH, C.sub.1-6 -alkyl, NR.sub.10 R.sub.11 wherein R.sub.10 and R.sub.11 independently are hydrogen, C.sub.1-6 -alkyl;R.sub.1 is a linker selected from a chemical bond, --C.sub.1-6 -alkyl--, --O(CH.sub.2).sub.m --, --NR.sub.12 --, --CONR.sub.12 --, --NR.sub.13 CO--, --SO.sub.2 NR.sub.14 --, --NR.sub.15 SO.sub.2 --, --CR.sub.16 .dbd.CR.sub.17 --, --CH.dbd.--, --CHR.sub.17, --CH.sub.2 --, --CHF--, --CF.sub.2 --, --SO.sub.2 --;R.sub.12, R.sub.13, R.sub.14, R.sub.15 R.sub.16 and R.sub.17 are hydrogen, C.sub.1-6 -alkyl, aralkyl and m is 1, 2, or 3;A is a heterocycle as shown in scheme 1 wherein the point of attachment is indicated with a single bond ##STR33## optionally substituted by hydrogen, halogen, C.sub.1-6 -alkyl optionally substituted by phenyl optionally substituted by C.sub.1-6 -alkoxy, C.sub.1-6 -alkylthio; --COOX.sup.1 wherein X.sup.1 is C.sub.1-6 -alkyl optionally substituted by phenyl or benzyl optionally substituted;R.sub.18, and R.sub.19, are C.sub.1-6 -alkyl, phenyl, benzyl;R.sub.20 is hydrogen, --OH, C.sub.1-6 -alkoxy, --SH, C.sub.1-6 -alkylthio, --COR.sub.21, --SOR.sub.22, --SO.sub.2 R.sub.23, --NR.sub.24 R.sub.25, --NHCN, halogen, trihalogenomethyl;R.sub.21, R.sub.22, and R.sub.23 are --OR.sub.26, C.sub.1-6 -alkyl, --NR.sub.24 R.sub.25, trihalogenomethyl;R.sub.24 and R.sub.25 independently are hydrogen, C.sub.1-6 -alkyl, --SO.sub.2 R.sub.26, --COZ.sub.5 wherein Z.sub.5 is C.sub.1-6 -alkyl, trihalogenomethylR.sub.26 is hydrogen, C.sub.1-6 -alkyl, trihalogenomethyl;nn is 1 or 2;and Ar.sub.1 is aryl, thiazole or isothiazole;or a pharmaceutically acceptable salt thereof.