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Machine translation
1. (WO2000029386) PYRIMIDINEDIONE DERIVATIVES USEFUL AS ALPHA 1A ADRENOCEPTOR ANTAGONISTS
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2000/029386    International Application No.:    PCT/US1999/026362
Publication Date: 25.05.2000 International Filing Date: 09.11.1999
IPC:
C07D 239/54 (2006.01), C07D 401/06 (2006.01), C07D 401/12 (2006.01)
Applicants: MERCK & CO., INC. [US/US]; 126 East Lincoln Avenue, Rahway, NJ 07065-0907 (US) (For All Designated States Except US).
NERENBERG, Jennie, B. [US/US]; (US) (For US Only).
BOCK, Mark, G. [US/US]; (US) (For US Only)
Inventors: NERENBERG, Jennie, B.; (US).
BOCK, Mark, G.; (US)
Common
Representative:
MERCK & CO., INC.; 126 East Lincoln Avenue, Rahway, NJ 07065-0907 (US)
Priority Data:
60/108,146 12.11.1998 US
Title (EN) PYRIMIDINEDIONE DERIVATIVES USEFUL AS ALPHA 1A ADRENOCEPTOR ANTAGONISTS
(FR) DERIVES DE LA PYRIMIDINEDIONE, ANTAGONISTES DE L'ADRENOCEPTEUR ALPHA 1A
Abstract: front page image
(EN)Novel pyrimidinedione compounds 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 porte sur des composés de pyrimidinédione et leurs sels pharmacocompatibles, la synthèse de ces composés, et leur utilisation comme antagonistes du récepteur adrénergique alpha 1a. L'une des applications de ces composés est le traitement de l'hyperplasie prostatique bénigne. Ces composés présentent en effet une capacité sélective de relâchement des tissus des muscles lisses enrichis en sous-types du récepteur alpha 1a, sans induction simultanée d'hypotension. L'un de ces tissus se trouvant autour de la muqueuse de l'urètre, ces composés à effet instantané procurent un soulagement immédiat aux hommes souffrant d'hyperplasie prostatique bénigne en réduisant les entraves à l'écoulement de l'urine. En outre, associés à un composé inhibiteur de la 5-alpha réductase humaine, ils peuvent procurer à la fois un soulagement instantané et prolongé aux effets de l'hyperplasie prostatique bénigne.
Designated States: AE, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, CA, CH, CN, CR, CU, CZ, DE, DK, DM, EE, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, TJ, TM, TR, TT, TZ, UA, UG, US, UZ, VN, YU, ZA, ZW.
African Regional Intellectual Property Organization (GH, GM, KE, LS, MW, SD, SL, SZ, TZ, UG, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, CH, CY, 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, GW, ML, MR, NE, SN, TD, TG).
Publication Language: English (EN)
Filing Language: English (EN)