Patent · US Expired

Enzymatic process of making alpha 1a adrenergic receptor antagonists using protease

US6207444A · kind A · utility

2Cited by
1References
19Claims
0Family size

Assignee

Inventors

Key dates

Filing dateJul 24, 1998
Grant dateMar 27, 2001
Priority date
Expiry dateJul 24, 2018

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07D401/14
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

This invention relates to crystalline pharmaceutically acceptable salts of an alpha 1a adrenergic receptor antagonist, Compound A, which are useful in the treatment of benign prostatic hyperplasia. Pharmaceutical compositions employing the crystalline salts, and processes for making and using the crystalline salts and pharmaceutical compositions of Compound A are also disclosed. This invention further relates to a process for obtaining enantiomerically pure intermediate useful for the synthesis of end product alpha 1a adrenergic receptor antagonists. The end product compounds are useful for the treatment of benign prostatic hyperplasia and for relaxing lower urinary tract tissue. The invention also relates to a process for preparing a class of dihydropyrimidinone compounds of which Compound A is a member, wherein the process involves deprotonating a dihydropyrimidinone compound and then coupling the deprotonated derivative with a primary amine.

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