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1. WO1996040135 - ALPHA 1a ADRENERGIC RECEPTOR ANTAGONISTS

Publication Number WO/1996/040135
Publication Date 19.12.1996
International Application No. PCT/US1996/009363
International Filing Date 04.06.1996
Chapter 2 Demand Filed 04.11.1996
IPC
A61K 31/58 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
56Compounds containing cyclopentahydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
58containing heterocyclic rings, e.g. aldosterone, danazol, stanozolol, pancuronium, digitogenin
C07D 211/60 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
211Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
04with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
06having no double bonds between ring members or between ring members and non-ring members
36with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
60Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 417/06 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
417Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
02containing two hetero rings
06linked by a carbon chain containing only aliphatic carbon atoms
CPC
A61K 31/58
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives, e.g. steroids
58containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
A61P 11/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
C07D 211/60
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
211Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
04with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
06having no double bonds between ring members or between ring members and non-ring members
36with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
60Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 417/06
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
417Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
02containing two hetero rings
06linked by a carbon chain containing only aliphatic carbon atoms
Applicants
  • MERCK & CO., INC. [US]/[US] (AllExceptUS)
  • PATANE, Michael, A. [US]/[US] (UsOnly)
  • BOCK, Mark, G. [US]/[US] (UsOnly)
  • FREIDINGER, Roger, M. [US]/[US] (UsOnly)
Inventors
  • PATANE, Michael, A.
  • BOCK, Mark, G.
  • FREIDINGER, Roger, M.
Common Representative
  • MERCK & CO., INC.
Priority Data
08/488,26707.06.1995US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) ALPHA 1a ADRENERGIC RECEPTOR ANTAGONISTS
(FR) ANTAGONISTES DU RECEPTEUR ADRENERGIQUE ALPHA 1a
Abstract
(EN)
This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as selective alpha-1a adrenergic receptor antagonists. 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 orthostatic 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 are achieved.
(FR)
L'invention porte sur certains nouveaux composés, leurs dérivés, leur synthèse, et leur utilisation comme antagonistes sélectifs du récepteur adrénergique alpha-1a, et dont l'une des applications est le traitement de l'hyperplasie prostatique bénigne. Ces composés ont une capacité sélective de relaxation des tissus des muscles lisses riches en sous-types de récepteurs alpha-1a, sans entraîner par la même occasion d'hypotension orthostatique. Un tissu de ce type entoure la muqueuse urétrale. En conséquence, l'une des applications des composés selon l'invention est de fournir un intense soulagement aux hommes souffrant d'hyperplasie prostatique bénigne en réduisant les obstacles s'opposant au passage de l'urine. Une autre application de ces composés résulte de leur association avec un composé inhibiteur de la 5-alpha réductase humaine, association qui permet d'apporter à la fois un soulagement instantané intense et un soulagement permanent des effets de l'hyperplasie prostatique bénigne.
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