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31. 发明授权

US6129910A Water-insoluble noncrosslinked bile acid sequestrants 失效
标题翻译：水不溶性非交联胆汁酸螯合剂
公开(公告)号：US6129910A
公开(公告)日：2000-10-10
申请号：US999351
申请日：1997-12-29
申请人： Stephen Randall Holmes-Farley , W. Harry Mandeville, III
发明人： Stephen Randall Holmes-Farley , W. Harry Mandeville, III
IPC分类号： A61K31/785
CPC分类号： A61K31/785 , C08F8/44
摘要： The present invention relates to a method for sequestering bile acids in a patient and to particular polymers for use in the method. The method comprises the step of orally administering to a mammal, such as a human, a therapeutically effective amount of a new class of water-insoluble noncrosslinked amine polymers.The water-insoluble noncrosslinked amine polymer comprises an amine-containing monomer or repeat unit which has one or more substituents bound to an amine nitrogen of the amine polymer. The substituent or substituents which are bound to the amine nitrogens of the amine polymer include a hydrophobic moiety and/or a quaternary amine-containing moiety.
摘要翻译：本发明涉及一种用于隔离患者中胆汁酸的方法和用于该方法的特定聚合物。该方法包括向哺乳动物（例如人）口服施用治疗有效量的新类型的不溶于水的非交联胺聚合物的步骤。水不溶性非交联胺聚合物包含含胺单体或具有一个或多个与胺聚合物的胺氮结合的取代基的重复单元。与胺聚合物的胺氮键合的取代基或取代基包括疏水部分和/或含季胺的部分。

32. 发明授权

US5969090A Hydrophobic sequestrant for cholesterol depletion 有权
标题翻译：疏水性螯合剂用于胆固醇消耗
公开(公告)号：US5969090A
公开(公告)日：1999-10-19
申请号：US185157
申请日：1998-11-03
申请人： W. Harry Mandeville, III , Stephen Randall Holmes-Farley , John S. Petersen
发明人： W. Harry Mandeville, III , Stephen Randall Holmes-Farley , John S. Petersen
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。

33. 发明授权

US5703188A Process for removing bile salts from a patient and compositions therefor 失效
标题翻译：从患者中除去胆汁盐的方法及其组合物
公开(公告)号：US5703188A
公开(公告)日：1997-12-30
申请号：US482969
申请日：1995-06-07
申请人： W. Harry Mandeville, III , Stephen Randall Holmes-Farley
发明人： W. Harry Mandeville, III , Stephen Randall Holmes-Farley
IPC分类号： A61K31/785 , A61K31/787 , A61K31/795 , C08F8/00 , C08F8/02 , C08F8/44 , C08F220/34 , C08F220/60 , C08F10/00 , C08F12/00 , C08F30/00 , C08F110/00
CPC分类号： C08F220/60 , A61K31/785 , A61K31/787 , A61K31/795 , C08F220/34 , C08F8/00 , C08F8/02 , C08F8/44
摘要： A method for removing bile salts from a patient by ion exchange by administering to the patient a therapeutically effective amount of one or more highly crosslinked polymers characterized by a repeat unit having the formula ##STR1## or copolymer thereof, where n is an integer; R.sup.1 is H or a C.sub.1 -C.sub.8 alkyl group: M is ##STR2## Z is O, NR.sup.3, S, or (CH.sub.2).sub.m ; m=0-10; R.sup.3 is H or a C.sub.1 -C.sub.8 alkyl group; and R.sup.2 is ##STR3## where p=0-10, and each R.sup.4, R.sup.5, and R.sup.6, independently is H, a C.sub.1 -C.sub.8 alkyl group, or an aryl group.
摘要翻译：一种通过离子交换从患者中除去胆汁盐的方法，其通过向患者施用治疗有效量的一种或多种高度交联的聚合物，其特征在于具有式“IMAGE”或其共聚物的重复单元，其中n为整数; R 1是H或C 1 -C 8烷基：M是O，NR 3，S或（CH 2）m; m = 0-10; R3是H或C1-C8烷基; 并且R 2是，其中p = 0-10，并且每个R 4，R 5和R 6独立地是H，C 1 -C 8烷基或芳基。

34. 发明授权

US5700458A Acid-functionalized saccharides as polyvalent anti-infectives 失效
标题翻译：酸官能化糖作为多价抗感染药
公开(公告)号：US5700458A
公开(公告)日：1997-12-23
申请号：US717264
申请日：1996-09-20
申请人： W. Harry Mandeville, III , Venkata R. Garigapati
发明人： W. Harry Mandeville, III , Venkata R. Garigapati
IPC分类号： C07H15/04 , A61K31/785 , C08F12/14 , C08F16/26 , C08F20/26 , C08F20/28 , C08F20/38 , C08F20/58 , C08F26/02 , C08F220/56 , A61K31/765
CPC分类号： A61K31/785 , C08F20/28 , C08F20/38 , C08F20/58
摘要： The present invention includes polymerizable monomers comprising an acid-functionalized glycoside moiety. In one embodiment, the monomer has a polymerizable functional group, such as an olefinic bond, to which the acid-functionalized glycoside moiety is attached by a spacer group, for example, an alkylene group, or an alkylene group wherein one or more carbon atoms are substituted by heteroatoms, such as oxygen, nitrogen or sulfur atoms. The present invention also includes polymers comprising one or more acid-functionalized glycoside moieties, such as pendant acid-functionalized glycoside moieties, which can inhibit or prevent rotavirus infection in a mammal. Such a polymer can comprise, for example, a monomer of the present invention. The polymer can be a homopolymer or a copolymer, and can have, for example, a polyacrylamide, polyacrylate or polystyrene backbone. In another embodiment, the present invention comprises a method for treating a rotaviral infection in a mammal, for example, a human, by administering to the mammal a therapeutically effective amount of a polymer comprising one or more glycoside moieties, such as pendant glycoside moieties. The polymer can be a homopolymer or a copolymer. In one embodiment, the polymer is a copolymer which comprises an acid-functionalized glycoside-bearing monomer and acrylamide.
摘要翻译：本发明包括包含酸官能化的糖苷部分的可聚合单体。在一个实施方案中，单体具有可聚合官能团，例如烯键，酸官能化糖苷部分通过间隔基团连接到其上，例如亚烷基或其中一个或多个碳原子被杂原子，如氧，氮或硫原子所取代。本发明还包括可以抑制或预防哺乳动物轮状病毒感染的一种或多种酸官能化糖苷部分的聚合物，例如侧酸官能化糖苷部分。这样的聚合物可以包括例如本发明的单体。聚合物可以是均聚物或共聚物，并且可以具有例如聚丙烯酰胺，聚丙烯酸酯或聚苯乙烯主链。在另一个实施方案中，本发明包括通过向哺乳动物施用治疗有效量的包含一个或多个糖苷部分的聚合物，例如侧链糖苷部分，来治疗哺乳动物例如人类的轮状病毒感染的方法。聚合物可以是均聚物或共聚物。在一个实施方案中，聚合物是包含酸官能化的含糖单体和丙烯酰胺的共聚物。

35. 发明申请

US20090226392A1 Phosphate-Binding Polymers for Oral Administration 审中-公开
标题翻译：用于口服给药的磷酸酯结合聚合物
公开(公告)号：US20090226392A1
公开(公告)日：2009-09-10
申请号：US12256615
申请日：2008-10-23
申请人： Stephen Randall Holmes-Farley , W. Harry Mandeville, III , George M. Whitesides
发明人： Stephen Randall Holmes-Farley , W. Harry Mandeville, III , George M. Whitesides
IPC分类号： A61K31/785 , A61P39/04
CPC分类号： A61K31/662 , A61K31/785 , A61K31/795
摘要： Phosphate-binding polymers are provided for removing phosphate from the gastrointestinal tract. The polymers are orally administered, and are useful for the treatment of hyperphosphatemia.
摘要翻译：提供磷酸盐结合聚合物用于从胃肠道除去磷酸盐。口服聚合物，可用于治疗高磷血症。

36. 发明授权

US06784254B2 Process for removing bile salts from a patient and alkylated compositions therefor 有权
标题翻译：从患者中除去胆汁盐的方法及其烷基化组合物
公开(公告)号：US06784254B2
公开(公告)日：2004-08-31
申请号：US10264350
申请日：2002-10-03
申请人： W. Harry Mandeville, III , Stephen Randall Holmes-Farley
发明人： W. Harry Mandeville, III , Stephen Randall Holmes-Farley
IPC分类号： C08F11600
CPC分类号： C08F220/60 , A61K31/785 , A61K31/787 , C08F8/00 , C08F8/02 , C08F8/44 , C08F26/00 , C08F220/34 , C08L39/02 , C08F220/00 , C08F226/02 , C08F26/02
摘要： The invention relates to a method for removing bile salts from a patient in need thereof and compositions useful in the method. The method comprises administering to the patient a therapeutically effective amount of a salt of an alkylated and crosslinked polymer. The alkylated and crosslinked polymer salt comprises the reaction product of crosslinked polymers, or salts and copolymers thereof having amine containing repeat units, with at least one aliphatic alkylating agent.
摘要翻译：本发明涉及从有需要的患者中除去胆汁盐的方法和用于该方法的组合物。该方法包括向患者施用治疗有效量的烷基化和交联聚合物的盐。烷基化和交联的聚合物盐包括具有含有重复单元的胺的交联聚合物或其盐和共聚物与至少一种脂族烷基化剂的反应产物。

37. 发明授权

US06767549B2 Ionic polymers as anti-infective agents 有权
标题翻译：离子聚合物作为抗感染剂
公开(公告)号：US06767549B2
公开(公告)日：2004-07-27
申请号：US10374014
申请日：2003-02-25
申请人： W. Harry Mandeville, III , Thomas X. Neenan , Stephen Randall Holmes-Farley
发明人： W. Harry Mandeville, III , Thomas X. Neenan , Stephen Randall Holmes-Farley
IPC分类号： A61K3114
CPC分类号： A61K31/785 , Y02A50/473 , Y02A50/475 , Y02A50/481 , Y02A50/491
摘要： A method for treating a microbial infection in a mammal, such as a human, comprising treating the mammal with a therapeutically effective amount of a polymer comprising an amino group or an ammonium group attached to the polymer backbone via an aliphatic spacer group. The polymer can be a homopolymer or a copolymer. In one embodiment, the polymer is a copolymer comprising a monomer having a pendant ammonium group and a hydrophobic monomer.
摘要翻译：一种用于治疗哺乳动物例如人的微生物感染的方法，包括用治疗有效量的包含通过脂肪族间隔基连接到聚合物主链的氨基或铵基团的聚合物来治疗哺乳动物。聚合物可以是均聚物或共聚物。在一个实施方案中，聚合物是包含具有侧铵基团和疏水单体的单体的共聚物。

38. 发明授权

US06726906B1 Fat-binding polymers 失效
标题翻译：脂肪结合聚合物
公开(公告)号：US06726906B1
公开(公告)日：2004-04-27
申请号：US09721310
申请日：2000-11-22
申请人： Thomas Jozefiak , Stephen Randall Holmes-Farley , W. Harry Mandeville, III , Chad Cori Huval , Venkata R. Garigapati , Keith K. Shackett , Danny Concagh
发明人： Thomas Jozefiak , Stephen Randall Holmes-Farley , W. Harry Mandeville, III , Chad Cori Huval , Venkata R. Garigapati , Keith K. Shackett , Danny Concagh
IPC分类号： A61K31785
CPC分类号： A61K45/06 , A61K31/785 , A61K2300/00
摘要： The present invention relates to a method for treating obesity, a method for reducing the absorption of dietary fat, and a method for treating hypertriglyceridemia in a patient and to particular polymers for use in the methods or in a manufacture of a medicament. The methods comprise the step of orally administering to a mammal, such as a human, a therapeutically effective amount of one or more fat-binding polymers. The administration of the fat-binding polymer of the invention facilitates the removal of fat from the body prior to digestion, with minimal side effects and low toxicity. In a preferred embodiment, the one or more fat-binding polymers are administered in combination with one or more lipase inhibitors, for example, lipstatin and tetrahydrolipstatin.
摘要翻译：本发明涉及一种治疗肥胖症的方法，一种减少膳食脂肪吸收的方法，以及用于治疗患者中的高甘油三酯血症的方法以及用于该方法或用于制备药物的具体聚合物。所述方法包括向哺乳动物（例如人）口服施用治疗有效量的一种或多种脂肪结合聚合物的步骤。本发明的脂肪结合聚合物的施用有利于在消化之前从身体去除脂肪，具有最小的副作用和低毒性。在一个优选的实施方案中，一种或多种脂肪结合聚合物与一种或多种脂肪酶抑制剂，例如脂抑素和四氢脂抑素组合施用。

39. 发明授权

US06692732B2 Ionic polymers as toxin-binding agents 有权
标题翻译：离子聚合物作为毒素结合剂
公开(公告)号：US06692732B2
公开(公告)日：2004-02-17
申请号：US10324623
申请日：2002-12-19
申请人： Richard Fitzpatrick , Chad Cori Huval , Caroline Isabelle Bacon Kurtz , W. Harry Mandeville, III , Thomas X. Neenan
发明人： Richard Fitzpatrick , Chad Cori Huval , Caroline Isabelle Bacon Kurtz , W. Harry Mandeville, III , Thomas X. Neenan
IPC分类号： A61K3174
CPC分类号： A61K31/785 , Y02A50/465 , Y02A50/473 , Y02A50/475 , Y02A50/481
摘要： A method for treating pathogenic toxins in a mammal, such as a human, comprising treating the mammal with a therapeutically effective amount of a polymer comprising a cationic group attached to the polymer backbone. The polymer can be a homopolymer or a copolymer. In one embodiment, the polymer is a copolymer comprising a monomer having a pendant ammonium group and a hydrophobic monomer.
摘要翻译：一种用于治疗哺乳动物（例如人）中致病性毒素的方法，包括用治疗有效量的包含连接到聚合物主链上的阳离子基团的聚合物来治疗哺乳动物。聚合物可以是均聚物或共聚物。在一个实施方案中，聚合物是包含具有侧铵基团和疏水单体的单体的共聚物。

40. 发明授权

US06565895B2 Bismuth compounds for the treatment and prevention of mucositis 有权
公开(公告)号：US06565895B2
公开(公告)日：2003-05-20
申请号：US09877723
申请日：2001-06-08
申请人： Philip J. Goddard , Jeffrey D. Klinger , Pradeep K. Dhal , W. Harry Mandeville, III , Richard J. Fitzpatrick , Thomas X. Neenan
发明人： Philip J. Goddard , Jeffrey D. Klinger , Pradeep K. Dhal , W. Harry Mandeville, III , Richard J. Fitzpatrick , Thomas X. Neenan
IPC分类号： A61K3324
CPC分类号： A61K33/12 , A61K31/28 , A61K31/60 , A61K33/24 , A61K33/245 , Y10S514/901 , Y10S514/902 , Y10S514/925 , Y10S514/928 , A61K31/715 , A61K31/00 , A61K2300/00
摘要： The invention relates to the unexpected discovery that bismuth-containing compounds are effective in the treatment of oral mucositis in a mammal. Thus, the invention relates, in one aspect to a method of treating oral mucositis comprising administering an effective amount of a pharmaceutically acceptable bismuth-containing compound, such as a bismuth salt or bismuth complex. In a preferred embodiment, the bismuth compound is an organic or inorganic salt such as, bismuth subsalicylate, bismuth subgallate, bismuth aluminate, bismuth citrate, bismuth subcitrate, bismuth carbonate, bismuth subcarbonate, tripotassium dicitrato bismuthate, bismuth nitrate, bismuth subnitrate, bismuth tartrate and mixtures thereof, preferably, bismuth subsalicylate and bismuth subgallate.

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