Some content of this application is unavailable at the moment.
If this situation persist, please contact us atFeedback&Contact
1. (WO1997018209) ALPHA 1a ADRENERGIC RECEPTOR ANTAGONISTS
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1997/018209 International Application No.: PCT/US1996/018346
Publication Date: 22.05.1997 International Filing Date: 12.11.1996
Chapter 2 Demand Filed: 16.06.1997
IPC:
C07D 275/06 (2006.01) ,C07D 295/13 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
275
Heterocyclic compounds containing 1, 2-thiazole or hydrogenated 1,2-thiazole rings
04
condensed with carbocyclic rings or ring systems
06
with hetero atoms directly attached to the ring sulfur atom
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
295
Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
04
with substituted hydrocarbon radicals attached to ring nitrogen atoms
12
substituted by singly or doubly bound nitrogen atoms
125
with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
13
to an acyclic saturated chain
Applicants:
MERCK & CO., INC. [US/US]; 126 East Lincoln Avenue Rahway, NJ 07065, US (AllExceptUS)
BOCK, Mark, G. [US/US]; US (UsOnly)
PATANE, Michael, A. [US/US]; US (UsOnly)
Inventors:
BOCK, Mark, G.; US
PATANE, Michael, A.; US
Common
Representative:
MERCK & CO., INC.; 126 East Lincoln Avenue Rahway, NJ 07065, US
Priority Data:
60/007,96415.11.1995US
9605165.112.03.1996GB
Title (EN) ALPHA 1a ADRENERGIC RECEPTOR ANTAGONISTS
(FR) ANTAGONISTES DE RECEPTEURS ADRENERGIQUES 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 concerne de nouveaux composés, et des dérivés de ces derniers, leur synthèse et leur utilisation comme antagonistes de récepteurs adrénergiques alpha 1a sélectifs. Une des applications de ces composés est leur utilisation dans le traitement de l'hypertrophie de la prostate. Ces composés présentent une capacité sélective pour relâcher les tissus des muscles lisses dont la teneur en sous-types de récepteurs alpha 1a est enrichie, sans induire en même temps de syndrome orthostatique. Un tissu de ce type entoure la muqueuse urétrale. Par conséquent, l'intérêt de ces composés instantanés est d'assurer un soulagement rapide chez l'homme souffrant d'hypertrophie de la prostate, en évitant l'obstruction de l'écoulement urinaire. Un autre intérêt de ces composés est leur association à un composé inhibiteur de la réductase 5-alpha humaine, permettant d'obtenir des soulagements rapides et à long terme des effets de l'hypertrophie de la prostate.
Designated States: AL, AM, AU, AZ, BA, BB, BG, BR, BY, CA, CN, CU, CZ, EE, GE, HU, IL, IS, JP, KG, KR, KZ, LC, LK, LR, LT, LV, MD, MG, MK, MN, MX, NO, NZ, PL, RO, RU, SG, SI, SK, TJ, TM, TR, TT, UA, US, UZ, VN
African Regional Intellectual Property Organization (ARIPO) (KE, LS, MW, SD, SZ, UG)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, CH, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
AU1996077344