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1. 发明申请

WO2006052229A1 AMINATED POLYAMINES 审中-公开
标题翻译：氨基聚氨酯
公开(公告)号：WO2006052229A1
公开(公告)日：2006-05-18
申请号：PCT/US2004/036485
申请日：2004-11-03
申请人： UNIVERSITY OF FLORIDA , BERGERON, Raymond, J., Jr
发明人： BERGERON, Raymond, J., Jr
IPC分类号： C07C211/13
CPC分类号： C07C211/13
摘要： An aminated polyamine having the formula (I), or its possible stereoisomers or a salt thereof with a pharmaceutically acceptable acid wherein, R 1 and R 4 may be the same or different and are alkyl, aryl, aryl alkyl or cycloalkyl, optionally having an alkyl chain interrupted by at least one etheric oxygen atom; R 2 and R 3 may be the same or different and are R 1 , R 4 or H; N 1 , N 2 , N 3 and N 4 are nitrogen atoms capable of protonation at physiological pH's; ALK 1 , ALK 2 AND ALK 3 may be the same or different and are straight or branched chain alkylene bridging groups having 1 to 4 carbon atoms which effectively maintain the distance between the nitrogen atoms such that the polyamine: (i) is capable of uptake by a target cell upon administration of the polyamine to a human or non-human animal or is capable of binding to at least one polyamine site of a receptor located within or on the surface of a cell upon administration of the polyamine to a human or non-human animal; and (ii) upon uptake by the target cell, competitively binds via an electrostatic interaction between the positively charged nitrogen atoms to biological counter-anions; the polyamine, upon binding to the biological counter-anion in the cell, functions in a manner biologically different than the intracellular polyamines; and further wherein at least one of said bridging groups ALK 1 , ALK 2 and ALK 3 contains at least one -CH(NRH)- group which is not alpha- to either of the nitrogen atoms and R is H, alkyl, acyl or sulfonyl.
摘要翻译：具有式（I）的胺化多胺或其可能的立体异构体或其药学上可接受的酸的盐，其中R 1和R 4可以相同或不同并且是烷基，芳基，芳基烷基或环烷基，任选地具有被至少一个醚氧原子间隔的烷基链; R 2和R 3可以相同或不同，为R 1，R 4或H; N 1，N 2，N 3和N 4是在生理pH下能够质子化的氮原子; ALK 1，ALK 2和AL 3 3可以相同或不同，并且是具有1至4个碳原子的直链或支链亚烷基桥连基团其有效地保持氮原子之间的距离，使得多胺：（i）在将多胺向人或非人动物施用时能够被靶细胞吸收或能够结合到至少一个多胺位点将多胺施用于人或非人动物时位于细胞表面内或细胞表面的受体; 和（ii）被靶细胞吸收后，通过带正电的氮原子之间的静电相互作用与生物反阴离子竞争结合; 多胺在与细胞中的生物反阴离子结合时以与细胞内多胺生物学不同的方式起作用; 并且其中所述桥连基团ALK 1，ALK 2和ALK 3 3中的至少一个含有至少一个-CH（NRH） - 基团其不是氮原子中的任一个，R是H，烷基，酰基或磺酰基。

2. 发明公开

EP0973726A1 METHOD FOR SYNTHESIS OF RHIZOFERRIN 失效
标题翻译：用于生产rhizoferrin
公开(公告)号：EP0973726A1
公开(公告)日：2000-01-26
申请号：EP98901671.2
申请日：1998-01-08
申请人： UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC.
发明人： BERGERON, Raymond, J., Jr
IPC分类号： C07C229/24 , C07C229/26
CPC分类号： C07C231/02 , Y02P20/55 , C07C235/10
摘要： A method of synthesizing rhizoferrin and analogues thereof comprising acylating a protected polyamine with a citric acid diester; hydrolyzing the resulting amide to produce an N-protected rhizoferrin or analogue thereof; and deprotecting the intermediate to produce rhizoferrin or the analogue thereof.

3. 发明公开

EP1812377A1 AMINATED POLYAMINES 审中-公开
标题翻译：胺化多胺
公开(公告)号：EP1812377A1
公开(公告)日：2007-08-01
申请号：EP04800606.8
申请日：2004-11-03
申请人： University of Florida
发明人： BERGERON, Raymond, J., Jr
IPC分类号： C07C211/13 , A61K31/13
CPC分类号： C07C211/13
摘要： An aminated polyamine having the formula (I), or its possible stereoisomers or a salt thereof with a pharmaceutically acceptable acid wherein, R1 and R4 may be the same or different and are alkyl, aryl, aryl alkyl or cycloalkyl, optionally having an alkyl chain interrupted by at least one etheric oxygen atom; R2 and R3 may be the same or different and are R1, R4 or H; N1, N2, N3 and N4 are nitrogen atoms capable of protonation at physiological pH's; ALK1, ALK2 AND ALK3 may be the same or different and are straight or branched chain alkylene bridging groups having 1 to 4 carbon atoms which effectively maintain the distance between the nitrogen atoms such that the polyamine: (i) is capable of uptake by a target cell upon administration of the polyamine to a human or non-human animal or is capable of binding to at least one polyamine site of a receptor located within or on the surface of a cell upon administration of the polyamine to a human or non-human animal; and (ii) upon uptake by the target cell, competitively binds via an electrostatic interaction between the positively charged nitrogen atoms to biological counter-anions; the polyamine, upon binding to the biological counter-anion in the cell, functions in a manner biologically different than the intracellular polyamines; and further wherein at least one of said bridging groups ALK1, ALK2 and ALK3 contains at least one -CH(NRH)- group which is not alpha- to either of the nitrogen atoms and R is H, alkyl, acyl or sulfonyl.

4. 发明授权

EP0973726B1 METHOD FOR SYNTHESIS OF RHIZOFERRIN 失效
标题翻译：用于生产rhizoferrin
公开(公告)号：EP0973726B1
公开(公告)日：2005-04-06
申请号：EP98901671.2
申请日：1998-01-08
申请人： UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC.
发明人： BERGERON, Raymond, J., Jr
IPC分类号： C07C235/10 , C07C231/02 , A61K31/195
CPC分类号： C07C231/02 , Y02P20/55 , C07C235/10
摘要： A method of synthesizing rhizoferrin and analogues thereof comprising acylating a protected polyamine with a citric acid diester; hydrolyzing the resulting amide to produce an N-protected rhizoferrin or analogue thereof; and deprotecting the intermediate to produce rhizoferrin or the analogue thereof.

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