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1. (WO1997017967) ALPHA 1a ADRENERGIC RECEPTOR ANTAGONISTS
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1997/017967 International Application No.: PCT/US1996/018321
Publication Date: 22.05.1997 International Filing Date: 12.11.1996
Chapter 2 Demand Filed: 12.06.1997
IPC:
A61K 31/451 (2006.01) ,A61K 31/495 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
435
having six-membered rings with one nitrogen as the only ring hetero atom
44
Non-condensed pyridines; Hydrogenated derivatives thereof
445
Non-condensed piperidines, e.g. piperocaine
451
having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
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)
PONTICELLO, Rose, Ann [US/US]; US (UsOnly)
Inventors:
BOCK, Mark, G.; US
PATANE, Michael, A.; US
PONTICELLO, Rose, Ann; US
Common
Representative:
MERCK & CO., INC.; 126 East Lincoln Avenue Rahway, NJ 07065, US
Priority Data:
60/006,76515.11.1995US
9603423.619.02.1996GB
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 componds 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 are achieved.
(FR) L'invention concerne certains nouveaux composés et leur dérivés, leur synthèse et leur utilisation en tant qu'antagonistes du récepteur adrénergique alpha 1a. Le traitement de l'adénome prostatique constitue l'une des applications desdits composés. Ces composés sont sélectifs dans leur capacité à relaxer les tissus des muscles lisses enrichis en sous-type du récepteur alpha 1a sans pour autant provoquer une hypotension. L'un de ces tissus entoure la muqueuse urétrale. Par conséquent, ces composés peuvent servir par exemple à soulager de façon aiguë les hommes souffrant d'adénome prostatique, en permettant un flux urinaire moins entravé. En combinant ces composés avec un composé inhibiteur de la réductase 5-alpha humaine, on peut également les utiliser pour atténuer de façon chronique et aiguë les effets de l'adénome prostatique.
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:
EP0865280US5922722JPH11507395CA2235370AU1996077343