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Machine translation
1. (WO2000027827) OXAZOLIDINONES USEFUL AS ALPHA 1A ADRENOCEPTOR ANTAGONISTS
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2000/027827    International Application No.:    PCT/US1999/026437
Publication Date: 18.05.2000 International Filing Date: 09.11.1999
IPC:
C07D 413/12 (2006.01), C07D 521/00 (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).
SELNICK, Harold, G. [US/US]; (US) (For US Only).
PAYNE, Linda [US/US]; (US) (For US Only)
Inventors: NERENBERG, Jennie, B.; (US).
BOCK, Mark, G.; (US).
SELNICK, Harold, G.; (US).
PAYNE, Linda; (US)
Common
Representative:
MERCK & CO., INC.; 126 East Lincoln Avenue, Rahway, NJ 07065-0907 (US)
Priority Data:
60/107,839 10.11.1998 US
09/190,506 12.11.1998 US
Title (EN) OXAZOLIDINONES USEFUL AS ALPHA 1A ADRENOCEPTOR ANTAGONISTS
(FR) OXAZOLIDINONES UTILES EN TANT QU'ANTAGONISTES DU RECEPTEUR ALPHA 1A ADRENERGIQUE
Abstract: front page image
(EN)Novel oxazolidinone 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)Nouveaux composés oxazolidinone et sels pharmaceutiquement acceptables desdits composés, ainsi que synthèse de ces composés et leur utilisation en tant qu'antagonistes du récepteur alpha 1a adrénergique. L'une des applications de ces composés concerne le traitement de l'adénome prostatique. Ces composés sont sélectifs dans leur capacité à détendre les tissus musculaires lisses enrichis en récepteur du sous-type alpha 1a, sans induire parallèlement l'hypotension. Des tissus de ce type entourent la muqueuse urétrale. Par conséquent, une utilité desdits composés est de fournir un soulagement radical aux hommes qui souffrent d'adénome prostatique, en permettant un flux urinaire moins entravé. Une autre utilité desdits composés est leur combinaison avec un composé inhibiteur de 5-alpha réductase humaine, qui permet d'obtenir un soulagement des symptômes tant aigus que chroniques de l'adénome prostatique.
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)