Patent · US Expired

2-benzyl-polycyclic guanine derivatives and process for preparing them

US5939419A · kind A · utility

59Cited by
7References
9Claims
0Family size

Assignee

Inventors

Key dates

Filing dateAug 23, 1995
Grant dateAug 17, 1999
Priority date
Expiry dateAug 23, 2015

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07D473/40
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

Antihypertensive and bronchodilating compounds of the formula or a pharmaceutically acceptable salt thereof, and a process for preparing them are disclosed, wherein: PA0 R.sub.1, R.sub.2, R.sub.3, R.sup.a, R.sup.b and R.sup.c as defined in the disclosure; PA1 pharmaceutical compositions containing said compounds; PA1 methods of treatment using said compounds; and PA1 a process for preparing polycyclic guanines comprising PA2 a) reducing a nitrosopyrimidine, and treating the reduced nitrosopyrimidine with an acylating reagent to give the amidopyrimidine; PA2 b) reacting the amidopyrimidine with a halogenating/cyclizing reagent to give a halopurine; PA2 c) reacting, in the presence of a base, the halopurine with an amine to give the substituted aminopurine; and PA2 d) closing the ring of the substituted aminopurine with a suitable dehydrating agent.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.