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1. WO2000043374 - POLYAZANAPHTHALENONE DERIVATIVES USEFUL AS ALPHA 1A ADRENOCEPTOR ANTAGONISTS

Publication Number WO/2000/043374
Publication Date 27.07.2000
International Application No. PCT/US2000/001775
International Filing Date 24.01.2000
IPC
C07D 239/82 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
239Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
70condensed with carbocyclic rings or ring systems
72Quinazolines; Hydrogenated quinazolines
78with hetero atoms directly attached in position 2
80Oxygen atoms
82with an aryl radical attached in position 4
C07D 401/12 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
C07D 401/14 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
14containing three or more hetero rings
C07D 403/12 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
403Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
CPC
C07D 239/82
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
239Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
70condensed with carbocyclic rings or ring systems
72Quinazolines; Hydrogenated quinazolines
78with hetero atoms directly attached in position 2
80Oxygen atoms
82with an aryl radical attached in position 4
C07D 401/12
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
C07D 401/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
14containing three or more hetero rings
C07D 403/12
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
403Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
Applicants
  • MERCK & CO., INC. [US/US]; 126 East Lincoln Avenue Rahway, NJ 07065-0907, US (AllExceptUS)
  • BOCK, Mark, G. [US/US]; US (UsOnly)
  • PATANE, Michael, A. [US/US]; US (UsOnly)
  • STEELE, Thomas, G. [US/US]; US (UsOnly)
Inventors
  • BOCK, Mark, G.; US
  • PATANE, Michael, A.; US
  • STEELE, Thomas, G.; US
Common Representative
  • MERCK & CO., INC.; 126 East Lincoln Avenue Rahway, NJ 07065-0907, US
Priority Data
60/117,25526.01.1999US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) POLYAZANAPHTHALENONE DERIVATIVES USEFUL AS ALPHA 1A ADRENOCEPTOR ANTAGONISTS
(FR) DERIVES DE POLYAZANAPHTHALENONE EN TANT QU'ANTAGONISTES DU RECEPTEUR ADRENERGIQUE ALPHA 1A
Abstract
(EN)
Dihydro-polyazanaphthalen-2-one compounds (e.g., dihydroquinazolin-2-one and dihydropteridin-2-one derivatives) and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.
(FR)
L'invention concerne des composés dihydro-polyazanaphthalén-2-one (p. ex. des dérivés de dihydroquinazolin-2-one et de dihydroptéridin-2-one) et des sels pharmaceutiquement acceptable de ces composés. L'invention concerne également la synthèse de ces composés et leur utilisation en tant qu'antagonistes du récepteur adrénergique alpha 1a. L'une des applications de ces composés est le traitement de l'hyperplasie prostatique bénigne. Ces composés ont une capacité sélective de relaxer le tissu d'un muscle lisse contenant une concentration accrue de récepteur du sous-type alpha 1-a, sans provoquer simultanément une hypotension. Un tissu de ce type entoure la muqueuse urétrale. C'est pourquoi l'une des utilités de ces composés est de soulager dans une mesure importante les patients de sexe masculins souffrant d'une hyperplasie bénigne de la prostate en assurant un écoulement urinaire amélioré. La seconde utilité de ces composés réside dans leur combinaison avec des composé inhibiteurs de la réductase 5 alpha, cette combinaison permettant d'assurer la fois un soulagement des symptômes aigus et un soulagement à long terme des symptômes de l'hyperplasie prostatique bénigne.
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