PROCESS FOR PRODUCING 6-MEMBER HETEROAROMATIC COMPOUNDS COMPRISING 1-3 NITROGEN ATOMS AND PHARMACEUTICAL COMPOSITIONS COMPRISING SAME

• Main Authors: SASAKI,TADAYUKI,JP, MIZUCHI,AKIRA,JP, KITAHARA,TAKUMI,JP, TOMINO,IKUO,JP, HORIKOMI,KAZUTOSHI,JP, TAKESUE,MITSUYUKI,JP, KIHARA,NORIAKI,JP, AWAYA,AKIRA,JP
• Format: Patent
• Language: English
• Published: 28.12.1992
• Edition: 5
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES

2-X-4-Y-5-Z-6-R1- Pyrimidine derivs. of formula (I) and their pharmaceutically acceptable salts are new: R1=H or lower alkyl; X=morpholino, 4-R2-piperazino, NR4R5 or a gp. of formula (a)-(e) R2=H, lower alkyl, phenyl, benzyl or alpha-(p-chlorophenyl)benzyl; x=1 or at least 2; each R3=lower alkyl, OH, phenyl opt. substd. by NO2, benzyl, benzoyloxy, benzoylamino, mono- or di-lower alkylamino, C(Ph)2OH, piperidino, lower hydroxyalkyl, PhSO2O, benzoyl opt. substd. by halo, lower alkylsulphonamido or lower alkoxycarbonyl; n=4-7; R4=H lower alkyl or benzyl; R5=lower alkyl, lower acyl, 2-fluroyl, benzyl, 4-piperidyl opt. substd. by benzoyl, phenethyl, a gp. of formula (g) or benzoyl opt. substd. by halo or NO2. Y= CH2R9, NR6R7 or a gp. of formula (g)-(j); R9=H, lower alkyl, lower alkoxy, lower alkylthio or di-lower alkylamino; R6=H, lower alkyl, phenyl, benzyl, lower alkoxy or 2-(N, N-dimethyl amino)ethyl; R7 = lower alkyl, lower acyl, cyclohexylcarbonyl, 2-fueoyl, lower alkoxycarbonyl, cinnamoyl, benzyl, benzylcarbonyl, tosyl, phenoxyacetyl, di-lower alkylcarbamoyl, 2-thienyl, COQ, CONHPh, COOPh, 4-lower alkyl piperazyl or benzoyl opt. substd. by halo, NO2, lower alkyl, lower alkoxy, NH2, benzoylamino or phenyl; provided that when R6=H, R7=benzoyl; Q=4-pyridyl, 1-piperidinyl or morpholino; R8=H, lower alkyl, phenyl or benzyl; m=4-7; Z=H halo, lower alkyl or lower alkoxycarbonyl; provided that (1) Y=CH2R9 only when Z=lower alkoxycarbonyl; (2) R4=H only when R5=lower alkyl, lower acyl, 2-furoyl, benzyl, phenethyl or benzoyl opt. substd. by halo or NO2 Y=CH2R9 and Z=lower alkoxycarbonyl or (3) Y=(g), (i) or (j) only when X=NR4R5 and R4= lower alkyl.