[EN] INDAZOLES AND AZAINDAZOLES AS LRRK2 INHIBITORS<br/>[FR] INDAZOLES ET AZAINDAZOLES EN TANT QU'INHIBITEURS DE LRRK2
申请人:ESCAPE BIO INC
公开号:WO2021178780A1
公开(公告)日:2021-09-10
The present invention is directed to indazole and azaindazole compounds which are inhibitors of LRRK2 and are useful in the treatment of CNS disorders.
Treatment of di-endo- or di-exo-3-aminobicyclo[2.2.1]hept-5-ene-2-carbohydrazides (1a and 1b) with ethyl 2-(2-oxocyclopentyl)acetate (2) yields norbornene-condensed 9-amino-1,9-diazatricyclo[6.4.0.0(4.8)]dodecane -2,10-diones 3a and 3b; the condensed bis(lactams) 4a and 4b and (from 1b and 2) the cyclopenta[c]pyridazinone 5. After separation, 3a and 3b both decompose on heating by loss of cyclopentadiene to give 9-amino-1,9-diazatricyclo[6.4.0.0(4.8)]dodecane-2,10-dione (6).
REICHELT, I.;REISSIG, H. -U., SYNTHESIS, BRD, 1984, N 9, 786-787