申请人:Hoffmann-La Roche Inc.
公开号:US05084476A1
公开(公告)日:1992-01-28
The compounds of the formula ##STR1## wherein X and Y are independently --CH.sub.2 -- or >C(CH.sub.3).sub.2 ; Z is --CHR.sup.8 --, >CO, >CR.sup.8 OR.sup.7, --CHR.sup.8 --CHR.sup.8 --, --CHOR.sup.7 --CH.sub.2 --, --CO--CHOR.sup.7 or --CHOR.sup.7 --CHOR.sup.7 --; R.sup.1 is a 5- or 6-membered, monocyclic heterocyclic group which optionally can be C-substituted by halogen, lower-alkyl, lower-alkoxy, acyloxy, nitro, hydroxy, amino, lower-alkylamino or di-lower-alkylamino and/or which can be substituted on a ring --NH-- group by lower-alkyl; R.sup.2 and R.sup.3 are independently hydrogen, lower-alkyl, trifluoromethyl or halogen and one of R.sup.2 and R.sup.3 always is trifluoromethyl or lower-alkyl; R.sup.4 and R.sup.5 are independently hydrogen, alkyl, alkoxy or halogen; R.sup.6 is hydrogen, lower-alkyl or --OR.sup.7 ; R.sup.7 is hydrogen, lower-alkyl or acyl; R.sup.8 is hydrogen or lower-alkyl; and R.sup.7 and R.sup.8 can be the same or different from one another, are useful for the treatment of neoplasms and dermatoses in mammals. The compounds can be manufactured from a corresponding bicyclic component and a heterocyclic component containing the residue R.sup.1 by a Wittig, Horner or Grignard reaction and the optional subsequent transformation of reactive groups.
式为##STR1##的化合物,其中X和Y独立地为--CH.sub.2--或>C(CH.sub.3).sub.2;Z为--CHR.sup.8--,>CO,>CR.sup.8OR.sup.7,--CHR.sup.8--CHR.sup.8--,--CHOR.sup.7--CH.sub.2--,--CO--CHOR.sup.7或--CHOR.sup.7--CHOR.sup.7--;R.sup.1为5-或6-成员的,单环杂环基团,可选择性地被卤素,低烷基,低烷氧基,酰氧基,硝基,羟基,氨基,低烷基氨基或二低烷基氨基取代,和/或可在环上--NH--基团上被低烷基取代;R.sup.2和R.sup.3独立地为氢,低烷基,三氟甲基或卤素,其中R.sup.2和R.sup.3中的一个总是三氟甲基或低烷基;R.sup.4和R.sup.5独立地为氢,烷基,烷氧基或卤素;R.sup.6为氢,低烷基或--OR.sup.7;R.sup.7为氢,低烷基或酰基;R.sup.8为氢或低烷基;并且R.sup.7和R.sup.8可以相同或不同,对于哺乳动物的肿瘤和皮肤病的治疗有用。这些化合物可以通过Wittig,Horner或Grignard反应以及可选的反应基团转化,从相应的双环组分和含有残基R.sup.1的杂环组分制备。