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公开(公告)号：US5969090A
公开(公告)日：1999-10-19
申请号：US185157
申请日：1998-11-03
IPC分类号： A61K31/785 , A61K31/787 , C08F8/00 , C08F8/02 , C08F8/44 , C08F26/02 , C08F220/34 , C08F220/60 , C08G67/02
CPC分类号： A61K31/785 , A61K31/787 , C08F220/34 , C08F220/60 , C08F26/02 , C08F8/00 , C08F8/02 , C08F8/44
摘要： The present invention relates to a poly(allylamine) polymer and, more generally, a hydrocarbon amine polymer. Preferably, these polymers are crosslinked. The present invention also relates to methods of forming these polymers and methods for their use. Further, the present invention relates to alkylating agents that can be employed to form the polymers and to methods for forming the alkylating agents. Generally, the polymer sequestrant includes a substituent bound to an amine of the polymer. The substituent includes a quaternary amine-containing moiety having one, two or three terminal hydrophobic substituents. A method of preparing quaternary amine-containing alkylating agents includes reacting an unsymmetrical dihalide with a tertiary amine having at least one hydrophobic substituent. A method for binding bile salts of bile acids in a mammal includes orally administering to the mammal a therapeutically-effective amount of the polymer sequestrant.
摘要翻译： 本发明涉及聚（烯丙胺）聚合物，更一般地，涉及烃胺聚合物。 优选地，这些聚合物是交联的。 本发明还涉及形成这些聚合物的方法及其使用方法。 此外，本发明涉及可用于形成聚合物的烷基化剂和形成烷基化剂的方法。 通常，聚合物螯合剂包括与聚合物的胺结合的取代基。 取代基包括具有一个，两个或三个末端疏水取代基的含季胺的部分。 制备含季铵烷基化剂的方法包括使不对称二卤化物与具有至少一个疏水取代基的叔胺反应。 用于结合哺乳动物胆汁酸胆汁的方法包括向哺乳动物口服给予治疗有效量的聚合物螯合剂。
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2.发明授权Hydrophilic nonamine-containing and amine-containing copolymers and their use as bile acid sequestrants 失效含亲水性非胺和含胺共聚物及其作为胆汁酸螯合剂的用途
公开(公告)号：US5929184A
公开(公告)日：1999-07-27
申请号：US999029
申请日：1997-12-29
IPC分类号： A61K31/785 , B01D15/00 , B01J39/00 , C08F6/00
CPC分类号： A61K31/785 , C08F6/008
摘要： The present invention relates to polymer compositions and methods of using said compositions for sequestering bile acids in a patient. The polymer compositions of this invention comprise a copolymer characterized by one or more hydrophilic nonamine-containing monomers or repeat units and one or more amine-containing monomers or repeat units. The amine-containing monomers or repeat units of the polymer compositions have one or more substituents bound to a portion of the amine nitrogens. The substituent or substituents which are bound to the amine nitrogens of the polymer composition can include a hydrophobic moiety and/or a quaternary amine-containing moiety. Suitable amine-containing monomers or repeat units include, but are not limited to, for example, vinylamine, allylamine, diallylamine, diallylmethylamine, and ethyleneimine, which are appropriately substituted, as described above.The hydrophilic nonamine-containing monomer can be, but is not limited to, for example, allyl alcohol, vinyl alcohol, ethylene oxide, propylene oxide, hydroxyethylacrylate, hydroxyethylmethacrylate, hydroxypropylacrylate, hydroxypropylmethacrylate, poly(propyleneglycol) monomethacrylate, poly(ethyleneglycol) monomethacrylate, acrylic acid, carbon dioxide, and sulfur dioxide. Typically, the hydrophilic nonamine-containing monomer or repeat unit comprises from about 10 to about 90 mole percent of the polymer composition.
摘要翻译： 本发明涉及聚合物组合物和使用所述组合物在患者体内螯合胆汁酸的方法。 本发明的聚合物组合物包含一种共聚物，其特征在于一种或多种含亲水性非胺的单体或重复单元和一种或多种含胺单体或重复单元。 聚合物组合物的含胺单体或重复单元具有一个或多个与一部分胺氮结合的取代基。 与聚合物组合物的胺氮键合的取代基或取代基可以包括疏水部分和/或含季胺的部分。 合适的含胺单体或重复单元包括但不限于如上所述的适当取代的乙烯胺，烯丙胺，二烯丙基胺，二烯丙基甲胺和乙烯亚胺。 含亲水非胺的单体可以是但不限于例如烯丙醇，乙烯醇，环氧乙烷，环氧丙烷，丙烯酸羟乙酯，甲基丙烯酸羟乙酯，丙烯酸羟丙酯，甲基丙烯酸羟丙酯，单（甲基）丙烯酸聚（乙二醇），单甲基丙烯酸聚（乙二醇） 丙烯酸，二氧化碳和二氧化硫。 通常，含亲水非胺的单体或重复单元包含约10至约90摩尔％的聚合物组合物。
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公开(公告)号：US08377428B2
公开(公告)日：2013-02-19
申请号：US12427127
申请日：2009-04-21
IPC分类号： A61K31/74
CPC分类号： A61K31/765 , A61K31/785
摘要： Disclosed is a pharmaceutical composition comprising a stable polyallylamine hydrochloride polymer in which between about 4% to about 12% by weight of the polymer is a chloride anion and a pharmaceutically acceptable carrier or diluent.
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公开(公告)号：US20100068167A1
公开(公告)日：2010-03-18
申请号：US12427127
申请日：2009-04-21
IPC分类号： A61K31/74
CPC分类号： A61K31/765 , A61K31/785
摘要： Disclosed is a pharmaceutical composition comprising a stable polyallylamine hydrochloride polymer in which between about 4% to about 12% by weight of the polymer is a chloride anion and a pharmaceutically acceptable carrier or diluent.
摘要翻译： 公开了包含稳定的聚烯丙胺盐酸盐聚合物的药物组合物，其中约4％至约12％重量的聚合物是氯化物阴离子和药学上可接受的载体或稀释剂。
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公开(公告)号：US07541024B2
公开(公告)日：2009-06-02
申请号：US10125684
申请日：2002-04-17
IPC分类号： A61K31/74
CPC分类号： A61K31/765 , A61K31/785
摘要： Disclosed is a pharmaceutical composition comprising a stable polyallylamine hydrochloride polymer in which between about 4% to about 12% by weight of the polymer is a chloride anion and a pharmaceutically acceptable carrier or diluent.
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公开(公告)号：US07125547B2
公开(公告)日：2006-10-24
申请号：US10647665
申请日：2003-08-25
IPC分类号： A61K31/787 , A61P3/06
CPC分类号： B82Y5/00 , A61K31/785 , A61K31/787 , A61K31/795 , A61K47/6949 , C08G61/12 , Y10S514/824
摘要： The present invention relates to a method for removing bile acids from a patient and certain polymers of use in the method. The method comprises the step of administering to the patient a therapeutically effective amount of a polymer composition which includes a a poly(diallylamine) polymer which is substituted with hydrophobic groups. The hydrophobic groups can be a substituted or unsubstituted, straight chain or branched C3–C24-alkyl group, an aralkyl group or an aryl group.
摘要翻译： 本发明涉及一种从患者中除去胆汁酸的方法和本方法中使用的某些聚合物。 该方法包括向患者施用治疗有效量的聚合物组合物的步骤，该聚合物组合物包括被疏水基团取代的聚（二烯丙基胺）聚合物。 疏水基团可以是取代或未取代的直链或支链C 3 -C 24 - 烷基，芳烷基或芳基。
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公开(公告)号：US06203785B1
公开(公告)日：2001-03-20
申请号：US08777408
申请日：1996-12-30
IPC分类号： A61K31787
CPC分类号： B82Y5/00 , A61K31/785 , A61K31/787 , A61K31/795 , A61K47/6949 , C08G61/12 , Y10S514/824
摘要： The present invention relates to a method for removing bile acids from a patient and certain polymers of use in the method. The method comprises the step of administering to the patient a therapeutically effective amount of a polymer composition which includes a a poly(diallylamine) polymer which is substituted with hydrophobic groups. The hydrophobic groups can be a substituted or unsubstituted, straight chain or branched C3-C24-alkyl group, an aralkyl group or an aryl group.
摘要翻译： 本发明涉及一种从患者中除去胆汁酸的方法和本方法中使用的某些聚合物。 该方法包括向患者施用治疗有效量的聚合物组合物的步骤，该聚合物组合物包括被疏水基团取代的聚（二烯丙基胺）聚合物。 疏水基团可以是取代或未取代的直链或支链C 3 -C 24 - 烷基，芳烷基或芳基。
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公开(公告)号：US5900475A
公开(公告)日：1999-05-04
申请号：US659264
申请日：1996-06-06
IPC分类号： A61K31/785 , A61K31/787 , C08F8/00 , C08F8/02 , C08F8/44 , C08F26/02 , C08F220/34 , C08F220/60 , C08G67/02 , C08G79/02
CPC分类号： A61K31/785 , A61K31/787 , C08F220/34 , C08F220/60 , C08F26/02 , C08F8/00 , C08F8/02 , C08F8/44
摘要： The present invention relates to a poly(allylamine) polymer and, more generally, a hydrocarbon amine polymer. Preferably, these polymers are crosslinked. The present invention also relates to methods of forming these polymers and methods for their use. Further, the present invention relates to alkylating agents that can be employed to form the polymers and to methods for forming the alkylating agents Generally, the polymer sequestrant includes a substituent bound to an amine of the polymer. The substituent includes a quaternary amine-containing moiety having one, two or three terminal hydrophobic substituents. A method of preparing quaternary amine-containing alkylating agents includes reacting an unsymmetrical dihalide with a tertiary amine having at least one hydrophobic substituent. A method for binding bile salts of bile acids in a mammal includes orally administering to the mammal a therapeutically-effective amount of the polymer sequestrant.
摘要翻译： 本发明涉及聚（烯丙胺）聚合物，更一般地，涉及烃胺聚合物。 优选地，这些聚合物是交联的。 本发明还涉及形成这些聚合物的方法及其使用方法。 此外，本发明涉及可用于形成聚合物的烷基化剂和形成烷基化剂的方法。通常，聚合物螯合剂包括与聚合物的胺结合的取代基。 取代基包括具有一个，两个或三个末端疏水取代基的含季胺的部分。 制备含季铵烷基化剂的方法包括使不对称二卤化物与具有至少一个疏水取代基的叔胺反应。 用于结合哺乳动物胆汁酸胆汁的方法包括向哺乳动物口服给予治疗有效量的聚合物螯合剂。
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公开(公告)号：US20100266526A1
公开(公告)日：2010-10-21
申请号：US12590511
申请日：2009-11-09
IPC分类号： A61K31/785 , A61P3/06 , A61K31/787
CPC分类号： A61K31/785 , Y10S514/824
摘要： The invention relates to methods for treating hypercholesterolemia and atherosclerosis, and reducing serum cholesterol in a mammal. The methods of the invention comprise administering to a mammal a first amount of a bile acid sequestrant compound which is an unsubstituted polydiallylamine polymer and a second amount of a cholesterol-lowering agent. The first and second amounts together comprise a therapeutically effective amount.The invention further relates to pharmaceutical compositions useful for the treatment of hypercholesterolemia and atherosclerosis, and for reducing serum cholesterol. The pharmaceutical compositions comprise a combination of a first amount of an unsubstituted polydiallylamine polymer compound and a second amount of a cholesterol-lowering agent. The first and second amounts comprise a therapeutically effective amount. The pharmaceutical compositions of the present invention may optionally contain a pharmaceutically acceptable carrier.
摘要翻译： 本发明涉及治疗高胆固醇血症和动脉粥样硬化以及降低哺乳动物血清胆固醇的方法。 本发明的方法包括向哺乳动物施用第一量的胆汁酸多价螯合剂化合物，其是未取代的聚二烯丙基胺聚合物和第二量的降胆固醇剂。 第一和第二量一起包括治疗有效量。 本发明还涉及可用于治疗高胆固醇血症和动脉粥样硬化以及降低血清胆固醇的药物组合物。 药物组合物包含第一量的未取代的聚二烯丙基胺聚合物化合物和第二量的降胆固醇剂的组合。 第一和第二量包括治疗有效量。 本发明的药物组合物可任选地含有药学上可接受的载体。
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公开(公告)号：US07638524B2
公开(公告)日：2009-12-29
申请号：US10025184
申请日：2001-12-19
IPC分类号： A61K9/14 , A61K9/00 , A61K31/785 , A61K31/795 , A01N43/40 , A61K31/435 , A01N43/64 , A61K31/41
CPC分类号： A61K31/785 , Y10S514/824
摘要： The invention relates to methods for treating hypercholesterolemia and atherosclerosis, and reducing serum cholesterol in a mammal. The methods of the invention comprise administering to a mammal a first amount of a bile acid sequestrant compound which is an unsubstituted polydiallylamine polymer and a second amount of a cholesterol-lowering agent. The first and second amounts together comprise a therapeutically effective amount.The invention further relates to pharmaceutical compositions useful for the treatment of hypercholesterolemia and atherosclerosis, and for reducing serum cholesterol. The pharmaceutical compositions comprise a combination of a first amount of an unsubstituted polydiallylamine polymer compound and a second amount of a cholesterol-lowering agent. The first and second amounts comprise a therapeutically effective amount. The pharmaceutical compositions of the present invention may optionally contain a pharmaceutically acceptable carrier.
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