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公开(公告)号:US20120190695A1
公开(公告)日:2012-07-26
申请号:US13439511
申请日:2012-04-04
IPC分类号: A61K31/506 , A61P37/08 , A61P29/00 , A61P11/06 , A61P27/02 , A61P11/00 , C07C259/18 , C07D271/06 , C07D401/14 , C07D413/14 , A61P11/02
CPC分类号: A61K31/506 , C07D217/06 , C07D271/06 , C07D413/14
摘要: This invention is directed to a compound of formula (I): wherein R1, R2 and R3 are as defined herein, a pharmaceutical composition comprising the compound, intermediates and processes for making said compounds, and the use of the compound to treat allergic and/or inflammatory disorders, particularly disorders such as allergic rhinitis, asthma, chronic obstructive pulmonary disease (COPD) and age-related macular degeneration (AMD).
摘要翻译: 本发明涉及式(I)化合物:其中R1,R2和R3如本文所定义,药物组合物包含化合物,中间体和制备所述化合物的方法,以及该化合物用于治疗过敏和/ 特别是诸如过敏性鼻炎,哮喘,慢性阻塞性肺病(COPD)和年龄相关性黄斑变性(AMD)的疾病。
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公开(公告)号:US20100081618A1
公开(公告)日:2010-04-01
申请号:US12553649
申请日:2009-09-03
申请人: Paul A. Wender , Jonathan B. Rothbard , Lee Wright , Erik L. Kreider , Christopher L. VanDeusen
发明人: Paul A. Wender , Jonathan B. Rothbard , Lee Wright , Erik L. Kreider , Christopher L. VanDeusen
CPC分类号: A61K47/64
摘要: The present invention provides compositions and methods for enhancing transport of biologically active compounds across biological membranes and across and into animal epithelial or endothelial tissues. The composition includes a biologically active agent and a transport moiety. The transport moiety includes a structure selected from the group consisting of (ZYZ)nZ, (ZY)nZ, (ZYY)nZ and (ZYYY)nZ. Subunit “Z” is L-arginine or D-arginine, and subunit “Y” is an amino acid that does not comprise an amidino or guanidino moiety. Subscript “n” is an integer ranging from 2 to 10. The method for enhancing transport involves the administration of the aforementioned composition.
摘要翻译: 本发明提供用于增强生物活性化合物跨越生物膜并跨越动物上皮细胞或内皮组织的转运的组合物和方法。 组合物包括生物活性剂和运输部分。 运输部分包括选自(ZYZ)nZ,(ZY)nZ,(ZYY)nZ和(ZYYY)nZ的结构。 亚基“Z”是L-精氨酸或D-精氨酸,亚基“Y”是不包含脒基或胍基部分的氨基酸。 下标“n”是从2到10的整数。用于增强转运的方法涉及上述组合物的给药。
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公开(公告)号:US07585834B2
公开(公告)日:2009-09-08
申请号:US10078247
申请日:2002-02-14
申请人: Paul A. Wender , Jonathan B. Rothbard , Lee Wright , Erik L. Kreider , Christopher L. VanDeusen
发明人: Paul A. Wender , Jonathan B. Rothbard , Lee Wright , Erik L. Kreider , Christopher L. VanDeusen
CPC分类号: A61K47/64
摘要: The present invention provides compositions and methods for enhancing transport of biologically active compounds across biological membranes and across and into animal epithelial or endothelial tissues. The composition includes a biologically active agent and a transport moiety. The transport moiety includes a structure selected from the group consisting of (ZYZ)nZ, (ZY)nZ, (ZYY)nZ and (ZYYY)nZ. Subunit “Z” is L-arginine or D-arginine, and subunit “Y” is an amino acid that does not comprise an amidino or guanidino moiety. Subscript “n” is an integer ranging from 2 to 10. The method for enhancing transport involves the administration of the aforementioned composition.
摘要翻译: 本发明提供用于增强生物活性化合物跨越生物膜并跨越动物上皮细胞或内皮组织的转运的组合物和方法。 组合物包括生物活性剂和运输部分。 运输部分包括选自(ZYZ)nZ,(ZY)nZ,(ZYY)nZ和(ZYYY)nZ的结构。 亚基“Z”是L-精氨酸或D-精氨酸,亚基“Y”是不包含脒基或胍基部分的氨基酸。 下标“n”是从2到10的整数。用于增强转运的方法涉及上述组合物的给药。
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公开(公告)号:US20100048568A1
公开(公告)日:2010-02-25
申请号:US12570355
申请日:2009-09-30
申请人: Suzanne C. Aldous , Michael W. Fennie , John Z. Jiang , Stanly John , Lan Mu , Brian Pedgrift , James R. Pribish , Barbara Rauckman , Jeffrey S. Sabol , Grzegorz T. Stoklosa , Sukanthini Thurairatnam , Christopher L. Vandeusen
发明人: Suzanne C. Aldous , Michael W. Fennie , John Z. Jiang , Stanly John , Lan Mu , Brian Pedgrift , James R. Pribish , Barbara Rauckman , Jeffrey S. Sabol , Grzegorz T. Stoklosa , Sukanthini Thurairatnam , Christopher L. Vandeusen
IPC分类号: A61K31/5377 , C07D401/14 , A61K31/506 , A61P29/00 , A61P37/00 , A61P37/08 , A61P11/06 , A61P11/00 , C07D403/12 , A61K31/496 , C07D413/14 , A61K31/53 , C07D417/14 , C07D403/14
CPC分类号: C07D239/28 , C07D403/12 , C07D403/14 , C07D413/12 , C07D417/14
摘要: This invention is directed to a compound of formula (I): wherein R1, R2, R3, R4 and L1 are as defined herein, a pharmaceutical composition comprising the compound, and the use of the compound to treat allergic and/or inflammatory disorders, particularly disorders such as allergic rhinitis, asthma and/or chronic obstructive pulmonary disease (COPD).
摘要翻译: 本发明涉及式(I)化合物:其中R 1,R 2,R 3,R 4和L 1如本文所定义,包含该化合物的药物组合物和该化合物用于治疗过敏和/或炎症性疾病的用途, 尤其是过敏性鼻炎,哮喘和/或慢性阻塞性肺病(COPD)等疾病。
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公开(公告)号:US07067698B2
公开(公告)日:2006-06-27
申请号:US10211986
申请日:2002-08-02
申请人: Paul A. Wender , Christopher L. VanDeusen , Kanaka Pattabiraman , Erin T. Pelkey , Theodore C. Jessop
发明人: Paul A. Wender , Christopher L. VanDeusen , Kanaka Pattabiraman , Erin T. Pelkey , Theodore C. Jessop
IPC分类号: C07C277/00
CPC分类号: C07C271/22 , C07K1/006
摘要: Synthesis routes that can be adapted to large scale synthesis of oligoguanidine compounds such as oligoarginine compounds are described which use a perguanidinylation step to convert a group of ω-amino groups to the corresponding guanidinyl groups. These compounds find utility as transport agents. Modified oligoguanidine compounds are also described.
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公开(公告)号:US09469627B2
公开(公告)日:2016-10-18
申请号:US13439511
申请日:2012-04-04
IPC分类号: C07D413/14 , A61K31/506 , C07D271/06
CPC分类号: A61K31/506 , C07D217/06 , C07D271/06 , C07D413/14
摘要: This invention is directed to a compound of formula (I): wherein R1, R2 and R3 are as defined herein, a pharmaceutical composition comprising the compound, intermediates and processes for making said compounds, and the use of the compound to treat allergic and/or inflammatory disorders, particularly disorders such as allergic rhinitis, asthma, chronic obstructive pulmonary disease (COPD) and age-related macular degeneration (AMD).
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