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1. 发明申请

US20140155350A1 Prodrugs of Neuraminidase Inhibitors 有权
标题翻译：神经氨酸酶抑制剂的前药
公开(公告)号：US20140155350A1
公开(公告)日：2014-06-05
申请号：US14091004
申请日：2013-11-26
申请人： John Hilfinger , Gordon Amidon
发明人： John Hilfinger , Gordon Amidon
IPC分类号： C07F7/12 , C07C279/16 , C07D307/89 , C07D231/14 , C07D309/28
CPC分类号： C07F7/12 , A61K31/155 , A61K31/167 , A61K31/351 , C07C279/16 , C07D231/14 , C07D307/89 , C07D309/28
摘要： A new class of neuramidase inhibitor prodrugs is provided characterized by a prodrug moiety of a carboxyl group modified to form a carbonyl ethoxy amino acid, a carbonyl ethoxy dipeptide or a carbonyl ethoxy tripeptide, a guanidine group modified to form a carbonyl ethoxy amino acid, a carbonyl ethoxy dipeptide, a carbonyl ethoxy tripeptide; a primary alcohol modified to form an esterified single amino acid, dipeptide or tripeptide of zanavimir of the unaltered therapeutic agent. Exemplary therapeutic agents so modified to form prodrugs include zanavimir, oseltamivir and peramivir. The prodrug has increased oral bioavailability relative to the unaltered neuraminidase inhibitor and is effective in the inhibition of viral infections involving neuraminidase in the viral reproductive cycle.
摘要翻译：提供了一类新的神经酰胺酶抑制剂前药，其特征在于被修饰以形成羰基乙氧基氨基酸的羧基的前药部分，羰基乙氧基二肽或羰基乙氧基三肽，修饰形成羰基乙氧基氨基酸的胍基，羰基乙氧基二肽，羰基乙氧基三肽; 改性以形成未改变的治疗剂的酯化单一氨基酸，二肽或三肽的三乙胺的伯醇。如此修饰以形成前药的示例性治疗剂包括扎那韦咪，奥司他韦和帕拉莫韦。前药相对于未改变的神经氨酸酶抑制剂具有增加的口服生物利用度，并且在病毒繁殖周期中有效抑制涉及神经氨酸酶的病毒感染。

2. 发明申请

US20120058937A9 Prodrugs of Neuraminidase Inhibitors 审中-公开
标题翻译：神经氨酸酶抑制剂的前药
公开(公告)号：US20120058937A9
公开(公告)日：2012-03-08
申请号：US12937624
申请日：2009-04-15
申请人： John Hilfinger , Gordon Amidon
发明人： John Hilfinger , Gordon Amidon
IPC分类号： A61K38/06 , C07C229/48 , C07K5/08 , A61P31/16 , A61K31/351 , A61K31/215 , A61P31/12 , C07D309/28 , A61K38/05
CPC分类号： C07F7/12 , A61K31/155 , A61K31/167 , A61K31/351 , C07C279/16 , C07D231/14 , C07D307/89 , C07D309/28
摘要： A new class of neuramidase inhibitor prodrugs is provided characterized by a prodrug moiety of a carboxyl group modified to form a carbonyl ethoxy amino acid, a carbonyl ethoxy dipeptide or a carbonyl ethoxy tripeptide, a guanidine group modified to form a carbonyl ethoxy amino acid, a carbonyl ethoxy dipeptide, a carbonyl ethoxy tripeptide; a primary alcohol modified to form an esterified single amino acid, dipeptide or tripeptide of zanavimir of the unaltered therapeutic agent. Exemplary therapeutic agents so modified to form prodrugs include zanavimir, oseltamivir and peramivir. The prodrug has increased oral bioavailability relative to the unaltered neuraminidase inhibitor and is effective in the inhibition of viral infections involving neuraminidase in the viral reproductive cycle.
摘要翻译：提供了一类新的神经酰胺酶抑制剂前药，其特征在于被修饰以形成羰基乙氧基氨基酸的羧基的前药部分，羰基乙氧基二肽或羰基乙氧基三肽，修饰形成羰基乙氧基氨基酸的胍基，羰基乙氧基二肽，羰基乙氧基三肽; 改性以形成未改变的治疗剂的酯化单一氨基酸，二肽或三肽的三乙胺的伯醇。如此修饰以形成前药的示例性治疗剂包括扎那韦咪，奥司他韦和帕拉莫韦。前药相对于未改变的神经氨酸酶抑制剂具有增加的口服生物利用度，并且在病毒繁殖周期中有效抑制涉及神经氨酸酶的病毒感染。

3. 发明申请

US20110160127A1 Prodrugs of Neuraminidase Inhibitors 审中-公开
标题翻译：神经氨酸酶抑制剂的前药
公开(公告)号：US20110160127A1
公开(公告)日：2011-06-30
申请号：US12937624
申请日：2009-04-15
申请人： John Hilfinger , Gordon Amidon
发明人： John Hilfinger , Gordon Amidon
IPC分类号： A61K38/06 , C07D309/28 , C07C229/48 , C07K5/08 , A61K38/05 , A61K31/351 , A61K31/215 , A61P31/12 , A61P31/16
CPC分类号： C07F7/12 , A61K31/155 , A61K31/167 , A61K31/351 , C07C279/16 , C07D231/14 , C07D307/89 , C07D309/28
摘要： A new class of neuramidase inhibitor prodrugs is provided characterized by a prodrug moiety of a carboxyl group modified to form a carbonyl ethoxy amino acid, a carbonyl ethoxy dipeptide or a carbonyl ethoxy tripeptide, a guanidine group modified to form a carbonyl ethoxy amino acid, a carbonyl ethoxy dipeptide, a carbonyl ethoxy tripeptide; a primary alcohol modified to form an esterified single amino acid, dipeptide or tripeptide of zanavimir of the unaltered therapeutic agent. Exemplary therapeutic agents so modified to form prodrugs include zanavimir, oseltamivir and peramivir. The prodrug has increased oral bioavailability relative to the unaltered neuraminidase inhibitor and is effective in the inhibition of viral infections involving neuraminidase in the viral reproductive cycle.
摘要翻译：提供了一类新的神经酰胺酶抑制剂前药，其特征在于被修饰以形成羰基乙氧基氨基酸的羧基的前药部分，羰基乙氧基二肽或羰基乙氧基三肽，修饰形成羰基乙氧基氨基酸的胍基，羰基乙氧基二肽，羰基乙氧基三肽; 改性以形成未改变的治疗剂的酯化单一氨基酸，二肽或三肽的三乙胺的伯醇。如此修饰以形成前药的示例性治疗剂包括扎那韦咪，奥司他韦和帕拉莫韦。前药相对于未改变的神经氨酸酶抑制剂具有增加的口服生物利用度，并且在病毒繁殖周期中有效抑制涉及神经氨酸酶的病毒感染。

4. 发明授权

US09181281B2 Prodrugs of neuraminidase inhibitors 有权
标题翻译：神经氨酸酶抑制剂的前药
公开(公告)号：US09181281B2
公开(公告)日：2015-11-10
申请号：US14091004
申请日：2013-11-26
申请人： John Hilfinger , Gordon Amidon
发明人： John Hilfinger , Gordon Amidon
IPC分类号： C07C279/16 , C07F7/12 , A61K31/155 , A61K31/167 , A61K31/351 , C07D231/14 , C07D307/89 , C07D309/28
CPC分类号： C07F7/12 , A61K31/155 , A61K31/167 , A61K31/351 , C07C279/16 , C07D231/14 , C07D307/89 , C07D309/28
摘要： A new class of neuramidase inhibitor prodrugs is provided characterized by a prodrug moiety of a carboxyl group modified to form a carbonyl ethoxy amino acid, a carbonyl ethoxy dipeptide or a carbonyl ethoxy tripeptide, a guanidine group modified to form a carbonyl ethoxy amino acid, a carbonyl ethoxy dipeptide, a carbonyl ethoxy tripeptide; a primary alcohol modified to form an esterified single amino acid, dipeptide or tripeptide of zanavimir of the unaltered therapeutic agent. Exemplary therapeutic agents so modified to form prodrugs include zanavimir, oseltamivir and peramivir. The prodrug has increased oral bioavailability relative to the unaltered neuraminidase inhibitor and is effective in the inhibition of viral infections involving neuraminidase in the viral reproductive cycle.
摘要翻译：提供了一类新的神经酰胺酶抑制剂前药，其特征在于被修饰以形成羰基乙氧基氨基酸的羧基的前药部分，羰基乙氧基二肽或羰基乙氧基三肽，修饰形成羰基乙氧基氨基酸的胍基，羰基乙氧基二肽，羰基乙氧基三肽; 改性以形成未改变的治疗剂的酯化单一氨基酸，二肽或三肽的三乙胺的伯醇。如此修饰以形成前药的示例性治疗剂包括扎那韦咪，奥司他韦和帕拉莫韦。前药相对于未改变的神经氨酸酶抑制剂具有增加的口服生物利用度，并且在病毒繁殖周期中有效抑制涉及神经氨酸酶的病毒感染。

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