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公开(公告)号：EP1222183B1
公开(公告)日：2003-04-23
申请号：EP00975868.1
申请日：2000-10-16
申请人： RECORDATI INDUSTRIA CHIMICA E FARMACEUTICA S.p.a. , RECORDATI S.A. CHEMICAL and PHARMACEUTICAL COMPANY
发明人： LEONARDI, Amedeo , MOTTA, Gianni , RIVA, Carlo , SIRONI, Giorgio
IPC分类号： C07D311/24 , A61K31/496 , A61P9/00 , C07D311/30
CPC分类号： C07D311/24 , C07D311/30
摘要： Benzopyran derivatives (I) (R = phenyl, alkoxycarbonyl, alkylcarbonyl, CONH2, CONH(alkyl), CON(alkyl)2, CN or alkoxycarbonylamino; R2 = alkyl, alkoxy, polyfluoroalkoxy, OH or CF3SO2O; each of R4 and R5 independently = H, halogen, polyfluoroalkyl, polyfluoroalkoxy, CN or CONH2; n is 0, 1 or 2; but if R = Ph and both of R4 and R5 = H or hologen atoms, then R2 = polyfluoroalkoxy or CF3SO2O) and their N-oxides and pharmaceutically acceptable salts are endowed with adrenergic antagonist activity and, in particular, with high selectivity for the α1-adrenergic receptor as compared to the 5-HT1A receptor. This activity profile suggests the use of these benzopyran derivatives in the treatment of obstructive syndromes of the lower urinary tract, including BPH, without side-effects associated with hypotensive activity.
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2.发明公开USE OF SELECTIVE ANTAGONISTS OF THE ALPHA 1b-ADRENERGIC RECEPTOR FOR IMPROVEMENT OF SEXUAL DYSFUNCTION 有权选择性α肾上腺素能受体拮抗剂对性疾病的治疗用途
公开(公告)号：EP1177190A2
公开(公告)日：2002-02-06
申请号：EP00927199.0
申请日：2000-05-08
申请人： RECORDATI INDUSTRIA CHIMICA E FARMACEUTICA S.p.a. , RECORDATI S.A. CHEMICAL and PHARMACEUTICAL COMPANY
IPC分类号： C07D403/04 , C07D407/14 , A61K31/517 , A61P15/10
CPC分类号： C07D403/04 , A61K31/517 , A61K31/519 , A61K31/557 , A61K45/06 , C07D239/95 , C07D405/12 , C07D405/14 , G01N33/9433 , G01N2500/00 , A61K2300/00
摘要： Described is the use in the treatment of either male or female sexual dysfunction of selective antagonists of the alpha1B-adrenergic receptor and the pharmaceutical compositions containing them as compounds capable of helping the sexual act avoiding at the same time excessive side effects due to acute hypotension.
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3.发明授权USE OF SELECTIVE ANTAGONISTS OF THE ALPHA 1b-ADRENERGIC RECEPTOR FOR IMPROVEMENT OF SEXUAL DYSFUNCTION 有权选择性α肾上腺素能受体拮抗剂对性疾病的治疗用途
公开(公告)号：EP1177190B1
公开(公告)日：2005-11-02
申请号：EP00927199.0
申请日：2000-05-08
IPC分类号： C07D403/04 , C07D407/14 , A61K31/517 , A61P15/10
CPC分类号： C07D403/04 , A61K31/517 , A61K31/519 , A61K31/557 , A61K45/06 , C07D239/95 , C07D405/12 , C07D405/14 , G01N33/9433 , G01N2500/00 , A61K2300/00
摘要： Described is the use in the treatment of either male or female sexual dysfunction of selective antagonists of the alpha1B-adrenergic receptor and the pharmaceutical compositions containing them as compounds capable of helping the sexual act avoiding at the same time excessive side effects due to acute hypotension.
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公开(公告)号：EP1222183A1
公开(公告)日：2002-07-17
申请号：EP00975868.1
申请日：2000-10-16
申请人： RECORDATI INDUSTRIA CHIMICA E FARMACEUTICA S.p.a. , RECORDATI S.A.CHEMICAL and PHARMACEUTICAL COMPANY
发明人： LEONARDI, Amedeo , MOTTA, Gianni , RIVA, Carlo , SIRONI, Giorgio
IPC分类号： C07D311/24 , A61K31/496 , A61P9/00 , C07D311/30
CPC分类号： C07D311/24 , C07D311/30
摘要： Benzopyran derivatives (I) (R = phenyl, alkoxycarbonyl, alkylcarbonyl, CONH2, CONH(alkyl), CON(alkyl)2, CN or alkoxycarbonylamino; R2 = alkyl, alkoxy, polyfluoroalkoxy, OH or CF3SO2O; each of R4 and R5 independently = H, halogen, polyfluoroalkyl, polyfluoroalkoxy, CN or CONH2; n is 0, 1 or 2; but if R = Ph and both of R4 and R5 = H or hologen atoms, then R2 = polyfluoroalkoxy or CF3SO2O) and their N-oxides and pharmaceutically acceptable salts are endowed with adrenergic antagonist activity and, in particular, with high selectivity for the α1-adrenergic receptor as compared to the 5-HT1A receptor. This activity profile suggests the use of these benzopyran derivatives in the treatment of obstructive syndromes of the lower urinary tract, including BPH, without side-effects associated with hypotensive activity.
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