Dihydroimidazo¬1,2-a pyrimidine derivatives, methods of preparing said compounds and pharmaceutical compositions constaining said compounds

摘要

A dihydroimidazo [1, 2-a] pyrimidine derivative of the formula: <CHEM> wherein R is hydrogen, C1-5 alkyl, heteroaryl, 2, 1, 3-benzoxadiazol or phenyl which may be substituted by a substituent selected from halogen, C1-4 alkyl, trifluromethyl, C1-4 alkoxy, nitro and cyano; R<1> is cyano C1-4 alkoxy-carbonyl or -COOCH (R<5>) CH2R<6> [wherein R<5> is hydrogen or aryl and R<6> is C1-4 alkoxy or -N (Ra) (Rb) (wherein each of Ra and Rb is C1-4 alkyl or aralkyl, or Ra and Rb together with the adjacent nitrogen atom form a heteorcycle)]; R<2> is C1-4 alkyl, hydroxymethyl, acetoxymethyl, di-C1-4 alkoxy-methyl, C1-4 alkyl-carbamoyloxymethyl or hydroxyimino-methyl; R<3> is C1-4 alkyl, formyl, carboxyl, nitro, -N (R<7>) (R<8>) (wherein each of R<7> and R<8> is hydrogen, C1-8 alkyl, aryl, aralkyl or acyl, R<7> and R<8> together with the adjacent nitrogen atom form a heterocycle), -OR<9> or -SR<1><0> (wherein each of R<9> and R<1><0> is hydrogen, C1-8 alkyl, aralkyl or acyl); R<4> is hydrogen or -(CH2)mN (Rc) (Rd) (wherein each of Rc and Rd is C1-4 alkyl or aralkyl, or Rc and Rd together with the adjacent nitrogen atom form a heteorcycle and m is 1 to 3; n is 0 or 1 to 3, inclusive of an optical isomer thereof, a disastereomer thereof and compounds selected from the group consisting of pharmaceutically acceptable acid addition salt forms thereof, hydrate forms thereof and mixtures thereof, methods of preparing said compounds and pharmaceutical compositions containing said compounds are disclosed. The dihydroimidazo [1,2 -a] pyrimidine deriavitives are useful as drugs for the treatment of coronary and cerebral circulatory diseases.