Dihydroimidazo[1,2-a]pyrimidine derivatives

Details Dihydroimidazo[1,2-a]pyrimidine derivatives Dihydroimidazo[1,2-a]pyrimidine derivatives

C - Chemistry, Metallurgy

07

D

167/220, 260/242

C07D 487/04 (2006.01) A61K 31/505 (2006.01)

Patent

CA 1271751

Y0-1-38736C/NK/85 Abstract of the Disclosure A dihydroimidazo[1,2-.alpha.]pyrimidine derivative of the formula: Image wherein R is hydrogen, C1-5 alkyl, heteroaryl, 2,1,3-benz- oxadiazolyl or phenyl which may be substituted by a substi- tuent selected from halogen, C1-4 alkyl, trifluoromethyl, C1-4 alkoxy, nitro and cyano; R1 is cyano, C1-4 alkoxy-carbonyl or -COOCH(R5)CH2R6 [wherein R5 is hydrogen or aryl and R6 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 heterocycle)]; R2 is C1-4 alkyl, hydroxymethyl, acetoxymethyl, di-C1-4 alkoxy-methyl, C1-4 alkyl-carbamoyloxymethyl or hydroxyimino- methyl; R3 is C1-4 alkyl, formyl, carboxyl, nitro, -N(R7)(R8) (wherein each of R7 and R8 is hydrogen, C1-8 alkyl, aryl, aralkyl or acyl, or R7 and R8 together with the adjacent nitrogen atom form a heterocycle), -OR9 or -SR10 (wherein each of R9 and R10 is hydrogen, C1-8 alkyl, aralkyl or acyl); R4 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 heterocycle and m is 1 to 3; n is 0 or 1 to 3 inclusive or an optical isomer thereof, a diastereomer thereof and compounds selected from the group consisting of pharma- ceutically 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 derivatives are useful as drugs for the treatment of coronary and cerebral circulatory diseases.

481703

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