发明名称 |
USE OF SELECTIVE ANTAGONISTS OF THE alpha 1b-ADRENERGIC RECEPTOR FOR IMPROVEMENT OF SEXUAL DYSFUNCTION |
摘要 |
Compounds (I) (A=2-furyl, substituted 2-furyl, 2-tetrahydrofuryl, substituted alkoxy or substituted phenoxyalkyl; B=B1, B2 or B3, but if B=B1 then A=substituted phenoxyalkyl) and their enantiomers, diastereoisomers and pharmaceutically acceptable salts are useful for the preparation of a medicament for the treatment of sexual dysfunction in males and females. Compounds II (I:B=B3, A ≠ 2-furyl) are novel and are claimed per se. Pharmaceutical compositions containing compounds II are also claimed, as are pharmaceutical compositions containing compounds I and one or more of a prostaglandin, a direct vasodilator and a 5 cGMP phosphodiesterase inhibitor (e.g. sildenafil). Compounds which bind to mammalian alpha 1b adrenergic receptors with an affinity of at least about 10-<8> M and which bind to mammalian alpha 1b adrenergic receptors with an affinity at least 10-fold higher than the affinity with which the compound binds to mammalian alpha 1a or alpha 1d alpha 1L adrenergic receptors are also useful for the preparation of a medicament for the treatment of sexual dysfunction in males and females. A method of identifying such compounds is also disclosed and claimed.
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申请公布号 |
WO0067735(A2) |
申请公布日期 |
2000.11.16 |
申请号 |
WO2000EP04308 |
申请日期 |
2000.05.08 |
申请人 |
RECORDATI INDUSTRIA CHIMICA E FARMACEUTICA SPA;RECORDATI S.A., CHEMICAL AND PHARMACEUTICAL COMPANY |
发明人 |
LEONARDI, AMEDEO;MOTTA, GIANNI;TESTA, RODOLFO;SIRONI, GIORGIO |
分类号 |
C07D239/88;A61K31/496;A61K31/498;A61K31/517;A61K31/519;A61K31/557;A61K31/5575;A61K45/00;A61K45/06;A61P15/00;A61P15/10;A61P43/00;C07D239/95;C07D403/04;C07D405/12;C07D405/14;G01N33/94;(IPC1-7):A61K31/00 |
主分类号 |
C07D239/88 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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