公开(公告)号：US5114709A

公开(公告)日：1992-05-19

申请号：US713875

申请日：1991-06-12

申请人： Leon E. St. Pierre ,  George R. Brown ,  Gaoming Wu ,  Youlu Yu

发明人： Leon E. St. Pierre ,  George R. Brown ,  Gaoming Wu ,  Youlu Yu

IPC分类号： A61K31/785 ,  A61K31/80

CPC分类号： A61K31/80 ,  A61K31/785 ,  Y10S514/892 ,  Y10S514/911

摘要： The invention is concerned with a metal ion coordinated polyamine resin in which a non-toxic, pharmaceutically acceptable chelating metal ion is coordinated with a cross-linked and non-digestible polymeric amine selected from the group consisting of: (a) polyamine resins with a hydrophilic backbone, of the formula: ##STR1## wherein P represents a hydrophilic, cross-linked and non-digestible homopolymer backbone, m is an integer varying from 1 to 10 inclusive, and n, o and p are, independently, integers varying from 2 to 12 inclusive; (b) polyamine resins with a hydrophobic backbone, of the formula:P'--[NH(CH.sub.2).sub.n ].sub.m NH.sub.2 (II)wherein P' represents a hydrophobic, cross-linked and non-digestible homopolymer backbone, m is an integer varying from 0 to 6 inclusive and n is an integer varying from 2 to 12 inclusive; and (c) cross-linked copolymers of a polyethylenepolyamine containing from 2 to 6 ethylene units and epichlorohydrin. The metal ion coordinated polyamine resins of the invention are highly efficient sorbents for bile acids and salts and can thus be used for reducing hypercholesterolemia in affected humans.

摘要翻译： 本发明涉及金属离子配位聚胺树脂，其中无毒的药学上可接受的螯合金属离子与交联和不可消化的聚合胺配位，所述交联和不可消化的聚合胺选自：（a）多胺树脂与 亲水性骨架，其具有下式：其中P表示亲水性，交联和不消化的均聚物主链，m是从1到10的整数，包括端值在内，n，o和p独立地是从 2到12包含; （b）具有下式的疏水主链的聚胺树脂：P' - [NH（CH 2）n] m NH 2（II）其中P'表示疏水性，交联和不消化的均聚物主链，m是整数 0〜6，n为2〜12的整数， 和（c）含有2-6个乙烯单元的聚亚乙基多胺和表氯醇的交联共聚物。 本发明的金属离子配位聚胺树脂是胆汁酸和盐的高效吸附剂，因此可用于降低受影响人体中的高胆固醇血症。

公开(公告)号：US5366724A

公开(公告)日：1994-11-22

申请号：US652004

申请日：1991-02-07

申请人： Leon E. St. Pierre ,  George R. Brown ,  Gaoming Wu

发明人： Leon E. St. Pierre ,  George R. Brown ,  Gaoming Wu

IPC分类号： A61K31/785 ,  A61K31/74

CPC分类号： A61K31/785

摘要： The invention is concerned with novel ingestible polymeric amines in linear or branched form of the formula: ##STR1## and their pharmaceutically acceptable salts of the formulae: ##STR2## wherein P represents a hydrophilic, cross-linked and digestable polymer backbone; R is a hydrogen atom or a lower alkyl radical; X.sup.- is a pharmaceutically acceptable anion; m is an integer varying from 1 to 10 inclusive; and n, o and p are, independently, integers varying from 2 to 12 inclusive. The polymeric amines of the invention are highly efficient adsorbents for bile acids and salts and can thus be used for reducing hypercholesterolemia in affected humans.

摘要翻译： 本发明涉及以下结构式的直链或支链形式的新颖的可摄取聚合胺：其具有下式的其药学上可接受的盐：其中P代表亲水的，交联和可消化的聚合物主链; R是氢原子或低级烷基; X-是药学上可接受的阴离子; m为1〜10的整数， 并且n，o和p独立地为从2到12的整数。 本发明的聚合胺是胆汁酸和盐的高效吸附剂，因此可用于降低受影响人体的高胆固醇血症。

公开(公告)号：US5236701A

公开(公告)日：1993-08-17

申请号：US381988

申请日：1989-07-19

申请人： Leon E. St. Pierre ,  George R. Brown ,  Gaoming Wu

发明人： Leon E. St. Pierre ,  George R. Brown ,  Gaoming Wu

IPC分类号： A61K31/785

CPC分类号： A61K31/785

摘要： The invention is concerned with novel ingestible cross-linked homopolymers having functional groups consisting of linear or branched amines, of the formula: ##STR1## and their pharmaceutically acceptable salts of the formulae: ##STR2## wherein P represents a hydrophilic, cross-linked and non-digestible homopolymer backbone; R is a hydrogen atom or a lower alkyl radical; X.sup.- is a pharmaceutically acceptable anion; m is an integer varying from 1 to 10 inclusive; and n, o and p are, independently, integers varying from 2 to 12 inclusive. The amine functionalized and cross-linked homopolymers of the invention are highly efficient adsorbents for bile acids and salts and can thus be used for reducing hypercholesterolemia in affected humans.

摘要翻译： 本发明涉及具有下列通式的直链或支链胺官能团的新颖可摄取的交联均聚物：其[P（（CH 2）n NRR）m R（Ia）或者（Ib））及其药学上可接受的盐 式：P [（CH2）nN +（R）2] mR.mX-（Ic）和（IMA）其中P表示亲水的，交联和不消化的均聚物主链; R是氢原子或低级烷基; X-是药学上可接受的阴离子; m为1〜10的整数， 并且n，o和p独立地为从2到12的整数。 本发明的胺官能化和交联的均聚物是胆汁酸和盐的高效吸附剂，因此可用于降低受影响人体的高胆固醇血症。

公开(公告)号：US5374422A

公开(公告)日：1994-12-20

申请号：US674150

申请日：1991-03-25

申请人： Leon E. St. Pierre ,  George R. Brown ,  Gaoming Wu

发明人： Leon E. St. Pierre ,  George R. Brown ,  Gaoming Wu

IPC分类号： A61K31/785 ,  A61K31/74 ,  C08F112/08

CPC分类号： A61K31/785

摘要： The invention is concerned with novel ingestible cross-linked homopolymers having functional groups consisting of linear or branched amines, of the formula: ##STR1## and their pharmaceutically acceptable salts of the formulae: ##STR2## wherein P(or POLYMER .parallel.-) represents a hydrophobic, cross-linked and non-digestible homopolymer backbone; R is a hydrogen atom or a lower alkyl radical; X.sup.- is a pharmaceutically acceptable anion; m is an integer varying from 1 to 6 inclusive; and n, o and p are, independently, integers varying from 2 to 12 inclusive. The amine functionalized and cross-linked homopolymers of the invention are highly efficient adsorbents for bile acids and salts and can thus be used for reducing hypercholesterolemia in affected humans.

摘要翻译： 本发明涉及具有下列通式的直链或支链胺官能团的新型可摄取的交联均聚物：式中：P [NR（CH 2）n] m N（R）2或（Ia） 式（I）其中P（或聚合物平行 - - ）代表的式（I）的可接受的盐：P [N +（R）2（CH 2）n] m N +（R） 疏水，交联和不消化的均聚物骨架; R是氢原子或低级烷基; X-是药学上可接受的阴离子; m为1〜6的整数， 并且n，o和p独立地为从2到12的整数。 本发明的胺官能化和交联的均聚物是胆汁酸和盐的高效吸附剂，因此可用于降低受影响人体的高胆固醇血症。

公开(公告)号：US5427777A

公开(公告)日：1995-06-27

申请号：US856184

申请日：1992-03-23

申请人： Leon E. St. Pierre ,  George R. Brown ,  Zhanjie Tan ,  Sophie-Dorothee Clas

发明人： Leon E. St. Pierre ,  George R. Brown ,  Zhanjie Tan ,  Sophie-Dorothee Clas

IPC分类号： A61K31/80 ,  A61K31/74

CPC分类号： A61K31/80

摘要： Novel ingestible polymeric phosphonium salts have the formula: ##STR1## wherein P' represents a cross-linked and non-digestible polymer backbone; R is a lower alkyl radical; X.sup.- is a pharmaceutically acceptable anion; n, n.sub.1 and n.sub.2 are, independently, integers varying from 0 to 6 inclusive, with the proviso that when m.sub.1 .gtoreq.1, n.sub.2 .gtoreq.1; and o.sub.1, o.sub.2, p.sub.1 p.sub.2, q.sub.1 and q.sub.2 are, independently, integers varying from 1 to 6 inclusive. The polymeric phosphonium salts of the invention are highly efficient sorbents for bile acids and salts and can thus be used for reducing hypercholesterolemia in affected humans.

摘要翻译： 新颖的可摄取聚合鏻盐具有下式：P'[（CH 2）n1P +（R）2] m1 [（CH2）n2P +（R）2] m2R。（m1 + m2）X-（Ia）P' （Ib）或P'（CH 2）n（Ic）其中P'表示交联和不消化的聚合物主链; R是低级烷基; X-是药学上可接受的阴离子; n，n1和n2独立地为0至6的整数，包括1和1，条件是当m1> = 1时，n2> / = 1; 而o1，o2，p1，p2，q1和q2独立地为从1到6的整数。 本发明的聚合鏻盐是胆汁酸和盐的高效吸附剂，因此可用于降低受影响人体中的高胆固醇血症。