公开(公告)号：US5144011A

公开(公告)日：1992-09-01

申请号：US308960

申请日：1989-02-06

申请人： Wei C. Shen ,  Hugues J.-P. Ryser

发明人： Wei C. Shen ,  Hugues J.-P. Ryser

IPC分类号： A61K47/48

CPC分类号： A61K47/48715 ,  A61K47/48692

摘要： A method for controlling the release of durgs or other passenger molecules form carrier conjugates, and a class of conjugates that releases drugs when ingested by a cell or subjected to acidic conditions, are disclosed. These conjugates contain a passenger molecule which is attached to a spacer molecule through an acidic bonding group, such as carboxyl, that is in a "cis" configuration with another acidic group, and a carrier molecule that is bonded to the spacer molecule at another site. When subjected to a mild increase in acidity, such as occurs within a lysosome of a cell, the drug or other passenger molecule is hydrolyzed from the the conjugate and released in unmodified, active form.

摘要翻译： 公开了一种用于控制杜氏或其他乘客分子的释放形成载体缀合物的方法，以及一类在被细胞摄取或经受酸性条件时释放药物的缀合物。 这些缀合物含有通过酸性键合基团（例如羧基）与间隔基分子连接的乘客分子，其与另一个酸性基团呈“顺式”构型，并且载体分子在另一位置与间隔基分子键合 。 当经历轻度的酸性增加，例如在细胞的溶酶体内发生时，药物或其他乘客分子从缀合物中水解并以未改变的活性形式释放。

公开(公告)号：US4847240A

公开(公告)日：1989-07-11

申请号：US106129

申请日：1987-10-07

申请人： Hugues J. P. Ryser ,  Wei-Chiang Shen

发明人： Hugues J. P. Ryser ,  Wei-Chiang Shen

IPC分类号： A61K39/44 ,  A61K47/48 ,  C12N11/08

CPC分类号： C12N11/08 ,  A61K39/44 ,  A61K47/48176 ,  A61K47/48238 ,  A61K47/48315

摘要： A method of effecting cellular uptake of molecules which are either excluded from cells or poorly transported into cells is disclosed wherein such molecules are covalently bonded to a cationic polymer which serves as a transport carrier to transport the molecules into cells.

摘要翻译： 公开了一种影响细胞从细胞中排出或运送到细胞中的分子的细胞摄取的方法，其中这样的分子共价键合到阳离子聚合物上，该阳离子聚合物用作将分子转运到细胞中的转运载体。