Global patent index - EP 1003734 A2

EP 1003734 A2 2000-05-31 - ALPHA 1a ADRENERGIC RECEPTOR ANTAGONIST

Title (en)

ALPHA 1a ADRENERGIC RECEPTOR ANTAGONIST

Title (de)

ALFA 1A ADRENERGISCH REZEPTOR ANTAGONIST

Title (fr)

ANTAGONISTE DE RECEPTEUR ADRENERGIQUE ALPHA 1a

Publication

EP 1003734 A2 (EN)

Application

EP 98938234 A

Priority

  • GB 9719706 A
  • GB 9719708 A
  • US 9816011 W
  • US 5481597 P
  • US 5490297 P
  • US 12230198 A

Abstract (en)

[origin: WO9907695A2] 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.

IPC 1-7 (main, further and additional classification)

C07D 401/00

IPC 8 full level (invention and additional information)

A61K 31/513 (2006.01); A61P 13/08 (2006.01); C07D 239/22 (2006.01); C07D 401/04 (2006.01); C07D 401/14 (2006.01)

CPC (invention and additional information)

C07D 239/22 (2013.01); C07D 401/04 (2013.01); C07D 401/14 (2013.01)

Citation (search report)

See references of WO 9907695A3

Designated contracting state (EPC)

AT BE CH DE DK ES FI FR GB GR IE IT LI LU NL PT SE

EPO simple patent family

WO 9907695 A2 19990218; WO 9907695 A3 19990617; AU 8680598 A 19990301; CA 2297889 A1 19990218; EP 1003734 A2 20000531; JP 2001512724 A 20010828

INPADOC legal status

2001-07-25 [18D] DEEMED TO BE WITHDRAWN

- Ref Legal Event Code: 18D

- Effective date: 20010201

2000-05-31 [17P] REQUEST FOR EXAMINATION FILED

- Ref Legal Event Code: 17P

- Effective date: 20000306

2000-05-31 [AK] DESIGNATED CONTRACTING STATES:

- Ref Legal Event Code: AK

- Designated State(s): AT BE CH DE DK ES FI FR GB GR IE IT LI LU NL PT SE