Global Patent Index - EP 0853479 A4

EP 0853479 A4 20010411 - ALPHA 1b ADRENERGIC RECEPTOR ANTAGONISTS

Title (en)

ALPHA 1b ADRENERGIC RECEPTOR ANTAGONISTS

Title (de)

ALPHA 1B ADRENERGISCHER REZEPTORANTAGONISTEN

Title (fr)

ANTAGONISTES DU RECEPTEUR ADRENERGIQUE ALPHA 1b

Publication

EP 0853479 A4 20010411 (EN)

Application

EP 96933093 A 19960924

Priority

  • GB 9604288 A 19960229
  • US 9615223 W 19960924
  • US 450195 P 19950929

Abstract (en)

[origin: WO9711698A1] This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as selective alpha 1b adrenergic receptor antagonists. These compounds display submicromolar affinity for the human alpha 1b adrenergic receptor subtype while displaying at least five-fold lower affinity for the human alpha 1d and alpha 1a adrenergic receptor subtypes, and many other G-protein coupled human receptors. One application of these compounds is in the treatment of hypertension. More specifically, these compounds display selectivity for lowering blood pressure without, for example, substantially affecting urethral pressure.

IPC 1-7

A61K 31/495; C07D 403/04

IPC 8 full level

A61K 31/00 (2006.01); A61K 31/505 (2006.01); A61K 31/517 (2006.01); A61K 31/529 (2006.01); A61P 9/00 (2006.01); A61P 9/12 (2006.01); A61P 13/00 (2006.01); A61P 13/08 (2006.01); A61P 43/00 (2006.01); C07D 403/04 (2006.01); C07D 405/14 (2006.01)

CPC (source: EP)

A61P 9/00 (2017.12); A61P 9/12 (2017.12); A61P 13/00 (2017.12); A61P 13/08 (2017.12); A61P 43/00 (2017.12); C07D 403/04 (2013.01); C07D 405/14 (2013.01)

Citation (search report)

  • [X] GB 2171977 A 19860910 - EMI PLC THORN
  • [X] US 4101548 A 19780718 - CRENSHAW RONNIE R, et al
  • [X] US 4026894 A 19770531 - WINN MARTIN, et al
  • [X] VALERIE A. ALABASTER, SIMON F.CAMPBELL, JOHN C. DANILEWICZ, COLIN W.GREENGRASS, AND RHONA M. PLEWS: "2,4-Diamino-6,7-dimethoxyquinazolines. 2. 2-(4-Carbamoylpiperidino) Derivatives as alpha1-Adrenoceptor Antagonists and Antihypertensive Agents", J.MED.CHEM., vol. 30, 1987, pages 999 - 1003, XP002159406
  • [X] I.TAKAYANAGI, F.KONNO, H.ARAI, K. CHIMOTO AND T. KITADA: "Newly synthesized alpha1-adrenoceptor blockers (SM911 and SM2470) and characterization of alpha-adrenoceptors in rat aortic strips, rat vas deferens preparations and rabbit aortic strips", GEN.PHARMACOL., vol. 16, no. 6, 1985, pages 613 - 615, XP000973937
  • See references of WO 9711698A1

Designated contracting state (EPC)

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

DOCDB simple family (publication)

WO 9711698 A1 19970403; CA 2232138 A1 19970403; EP 0853479 A1 19980722; EP 0853479 A4 20010411; JP H11512710 A 19991102

DOCDB simple family (application)

US 9615223 W 19960924; CA 2232138 A 19960924; EP 96933093 A 19960924; JP 51353297 A 19960924