Patent ID: 6180637
Filing Date: 2001-01-30
Classification: A61P,C07D

Abstract:
1,2,5-trisubstituted 1,2-dihydroindazol-3-ones of formula (I) ##STR53##whereinX is --SO.sub.2 --, --SO--, (CH.sub.2).sub.p --, --(CH.sub.2).sub.p --O--, --(CH.sub.2).sub.p --(C.dbd.O)--, --(CH.sub.2).sub.p --(C.dbd.O)--NH--, --(CH.sub.2).sub.p --CHOH--, --CHOH--(CH.sub.2).sub.p --, --(CH.sub.2).sub.p --CH.dbd.CH--, --CH.dbd.CH--(CH.sub.2).sub.p --,Y is --(C.dbd.O)--, --(C.dbd.O)--NH--, --(C.dbd.O)--NH--(CH.sub.2).sub.p --, --(C.dbd.O)--(CH.sub.2).sub.p --, --(CH.sub.2).sub.p --, --(CH.sub.2).sub.p --(C.dbd.O)--, --(CH.sub.2).sub.p --(C.dbd.O)--NH--, --(CH.sub.2).sub.p --(C.dbd.O)--NH--(CH.sub.2).sub.p --, --(CH.sub.2).sub.p --CHOH--, --CHOH--(CH.sub.2).sub.p --, --(CH.sub.2).sub.p --CH.dbd.CH--, --CH.dbd.CH--(CH.sub.2).sub.p --,Z is --O--, --O--(CH.sub.2).sub.p --, --NH--, --NH--(C.dbd.O)--, --NH--(C.dbd.O)--NH--, --NH--(C.dbd.O)--O--, --NH--CH.sub.2 --(C.dbd.O)-- and --NH--(C.dbd.O)--CH.sub.2 --,P is a cardinal number from 1 to 4,R.sup.1, R.sup.2 and R.sup.3 are the same or different and are:mono-, bi- or tricyclic saturated or mono- or polyunsaturated carbocycles having from 5 to 14 ring members; or mono-, bi- or tricyclic saturated or mono- or polyunsaturated heterocycles having from 5 to 15 ring members and from 1 to 6 heteroatoms,in which the carbocycles and the heterocycles can be mono- or polysubstituted by:--C.sub.1-6 -alkyl, --O--C.sub.1-6 -alkyl, --O--C.sub.3-7 -cycloalkyl, mono-, bi- or tricyclic saturated or mono- or polyunsaturated carbocycles having from 3 to 14 ring members, mono-, bi- or tricyclic saturated or mono- or polyunsaturated heterocycles having from 5 to 15 ring members and from 1 to 6 heteroatoms,R.sup.1 is also H, provided that when X is (CH.sub.2).sub.p, then R.sup.1 is not H,R.sup.3 --Z is also NO.sub.2,and their pharmaceutically acceptable salts,but excluding compounds of formula (I) in whichif Z is --NH--(C.dbd.O)--, --NH--(C.dbd.O)--NH--, --NH--(C.dbd.O)--O--, --NH--(C.dbd.O)--CH.sub.2 -- and at the same time R.sup.1 is phenyl, monosubstituted or polysubstituted by --COOH, --COOC.sub.1-6 -alkyl, --(CH.sub.2).sub.p --COOH, --(CH.sub.2).sub.p --COOC.sub.1-6 -alkyl --CONHC.sub.1-6 -alkyl, --CONHC.sub.6-14 -aryl, --CONHSO.sub.2 C.sub.1-6 -alkyl, --CONHSO.sub.2 C.sub.6-14 -aryl, 1H-tetrazol-5-yl, then R.sup.2 is not phenyl, monosubstituted or polysubstituted by CN, halogen, C.sub.1-4 -alkyl, C.sub.1-4 -alkyloxy, CF.sub.3 ; and if R.sup.3 --Z is NO.sub.2, then R.sup.1 --X is not benzyl or 4-methoxybenzyl, and R.sup.2 --Y is not benzyl or 2-picolyl at the same time.