Polyazanaphthalenone derivatives useful as alpha 1a adrenoceptor antagonists
US6358959B1 · kind B1 · utility
Assignee
Inventors
Key dates
| Filing date | Jan 11, 2000 |
| Grant date | Mar 19, 2002 |
| Priority date | — |
| Expiry date | Jan 11, 2020 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D403/12
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
Dihydro-polyazanaphthalen-2-one compounds (e.g., dihydroquinazolin-2-one and dihydropteridin-2-one derivatives) 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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.