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1. 发明申请

WO2002085378A1 LOW SALT FORMS OF POLYALLYLAMINE 审中-公开
标题翻译：聚氨酯的低盐形式
公开(公告)号：WO2002085378A1
公开(公告)日：2002-10-31
申请号：PCT/US2002/011408
申请日：2002-04-10
申请人： GELTEX PHARMACEUTICALS, INC.
发明人： PETERSEN, John, S. , BURKE, Steven, Keith , HOLMES-FARLEY, Stephen, Randall
IPC分类号： A61K31/785
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。

2. 发明申请

WO1998012203A1 ACID-FUNCTIONALIZED SACCHARIDES AS POLYVALENT ANTI-INFECTIVES 审中-公开
标题翻译：作为多重抗感染剂的酸功能化的食物
公开(公告)号：WO1998012203A1
公开(公告)日：1998-03-26
申请号：PCT/US1997016545
申请日：1997-09-18
申请人： GELTEX PHARMACEUTICALS, INC. , MANDEVILLE, W., Harry, III , GARIGAPATI, Venkata, R.
发明人： GELTEX PHARMACEUTICALS, INC.
IPC分类号： C07H13/04
CPC分类号： A61K31/785 , C08F20/28 , C08F20/38 , C08F20/58 , Y02A50/481
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包含一个或多个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。

3. 发明申请

WO2002085383A1 METHOD FOR REDUCING COPPER LEVELS AND TREATING COPPER TOXICOSIS 审中-公开
标题翻译：减少铜含量和治疗铜毒素的方法
公开(公告)号：WO2002085383A1
公开(公告)日：2002-10-31
申请号：PCT/US2002/011496
申请日：2002-04-10
申请人： GELTEX PHARMACEUTICALS, INC.
发明人： HOLMES-FARLEY, Stephen, Randall
IPC分类号： A61K31/785
CPC分类号： A61K31/785
摘要： A method for reducing copper levels in a patient and for treatin copper toxicosis and Wilson's Disease is disclosed that includes administering to the patient a therapeutically effective amount of an amine polymer, wherein the amine polymer is substantially water-insoluble or non-aborbent in the gastrointestinal tract. In one embodiment, the amine polymer is aliphatic. Examples of polmers that are useful in an embodiment of the invention includes sevelamer hydrogen chloride and colesevelam. The invention includes the use of amine polymers such as a cross-linked polymer characterized by a repeat unit having the formula (1) and salts and copolmers thereof, where n is a positive and x is zero or an integer between 1 and about 4. Also described is a use, for the manufacture of a medicament, of a polymer that reduces copper levels in a patient.
摘要翻译：公开了一种用于降低患者中铜含量和治疗铜毒中毒和威尔逊氏病的方法，其包括向患者施用治疗有效量的胺聚合物，其中胺聚合物在胃肠中基本上不溶于水或不吸收道。在一个实施方案中，胺聚合物是脂族的。在本发明的一个实施方案中有用的聚合物的实例包括赛维拉姆氯化氢和大肠杆菌素。本发明包括使用胺聚合物，例如交联聚合物，其特征在于具有式（1）的重复单元及其盐和共聚物，其中n为正，x为0或1至约4之间的整数。还描述了用于制造药物的用于降低患者中铜含量的聚合物的用途。

4. 发明申请

WO2002085380A1 METHOD FOR TREATING GOUT AND REDUCING SERUM URIC ACID 审中-公开
标题翻译：用于治疗GOUT并减少血清尿酸的方法
公开(公告)号：WO2002085380A1
公开(公告)日：2002-10-31
申请号：PCT/US2002/011491
申请日：2002-04-10
申请人： GELTEX PHARMACEUTICALS, INC.
发明人： HOLMES-FARLEY, Stephen, Randall , BURKE, Steven, K.
IPC分类号： A61K31/785
CPC分类号： A61K31/785
摘要： A method for treating gout and/or reducing serum uric acid levels in a patient is disclosed that includes administering to the patient a therapeutically effective amount of an amine polymer; for example, an alipathic amine polymer. Examples of polymers useful in the invention are sevelamer hydrogen chloride and colesevelam. The invention includes the use of amine polymers such as a cross-linked polymer characterized by a repeat unit having the formula (I): and salts and copolymers thereof, where n is a positive integer and x is zero or an integer between 1 and about 4. Also described is a use, for the manufacture of a medicament, of a polymer that reduces serum uric acid levels in a patient.
摘要翻译：公开了一种用于治疗患者痛风和/或降低血清尿酸水平的方法，其包括向患者施用治疗有效量的胺聚合物; 例如，酰胺类聚合物。可用于本发明的聚合物的实例是赛维默氯化氢和考布威兰。本发明包括使用胺聚合物，例如交联聚合物，其特征在于具有式（I）的重复单元：及其盐和共聚物，其中n为正整数，x为0或1与约1之间的整数还描述了用于制造药物的用于降低患者血清尿酸水平的聚合物的用途。

5. 发明申请

WO1998029107A2 POLY(DIALLYLAMINE)-BASED BILE ACID SEQUESTRANTS 审中-公开
标题翻译：多（氨基甲酸） - 双酯酸序列
公开(公告)号：WO1998029107A2
公开(公告)日：1998-07-09
申请号：PCT/US1997023899
申请日：1997-12-29
申请人： GELTEX PHARMACEUTICALS, INC. , HOLMES-FARLEY, Stephen, Randall , DHAL, Pradeep, K. , PETERSEN, John, S.
发明人： GELTEX PHARMACEUTICALS, INC.
IPC分类号： A61K31/00
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 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包含被疏水基团取代的聚（二烯丙基胺）聚合物的聚合物组合物的步骤。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。

6. 发明申请

WO1995034585A1 PROCESS FOR REMOVING BILE SALTS FROM A PATIENT AND ALKYLATED COMPOSITIONS THEREFOR 审中-公开
标题翻译：从患者和其中的烷基化组合物中移除双性盐的方法
公开(公告)号：WO1995034585A1
公开(公告)日：1995-12-21
申请号：PCT/US1995007181
申请日：1995-06-05
申请人： GELTEX PHARMACEUTICALS, INC. , MANDEVILLE, W., Harry, III. , HOLMES-FARLEY, Stephen, Randall
发明人： GELTEX PHARMACEUTICALS, INC.
IPC分类号： C08F08/02
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： A method for removing bile salts from a patient that includes administering to the patient a therapeutically effective amount of the reaction product of: a) one or more highly cross-linked polymers characterized by a repeat unit selected from the group consisting essentially of: (1), (2), (3): (NR-CH2 -CH2)n, (4): (NR-CH2CH2-NR-CH2CH2-NR-CH2CHOH-CH2)n and salts and copolymers thereof, where n is an integer and each R, independently, is H or a C1-C8 alkyl group; and b) at least one alkylating agent. The reaction product is characterized in that: (i) at least some of the nitrogen atoms in said repeat units are unreacted with said alkylating agent; (ii) less than 10 mol% of the nitrogen atoms in the repeat units that react with the alkylating agent form quaternary ammonium units; and (iii) the reaction product is non-toxic and stable once ingested.
摘要翻译：一种从患者中除去胆汁盐的方法，包括向患者施用治疗有效量的以下物质的反应产物：a）一种或多种高度交联的聚合物，其特征在于重复单元，所述重复单元主要包括：（1 ），（2），（3）：（NR-CH2-CH2）n，（4）：（NR-CH2CH2-NR-CH2CH2-NR-CH2CHOH-CH2）n及其盐和共聚物，其中n是整数并且每个R独立地是H或C 1 -C 8烷基; 和b）至少一种烷基化剂。反应产物的特征在于：（i）所述重复单元中的至少一些氮原子与所述烷基化剂未反应; （ii）与烷基化剂反应形成季铵单元的重复单元中少于10mol％的氮原子; 和（iii）一旦摄入，反应产物是无毒的和稳定的。

7. 发明申请

WO2002085382A1 METHODS OF TREATING SYNDROME X WITH ALIPHATIC POLYAMINES 审中-公开
标题翻译：用ALIPHATIC POLYAMINES处理综合征X的方法
公开(公告)号：WO2002085382A1
公开(公告)日：2002-10-31
申请号：PCT/US2002/011495
申请日：2002-04-10
申请人： GELTEX PHARMACEUTICALS, INC.
发明人： BURKE, Steven, K. , DONOVAN, Joanne, M.
IPC分类号： A61K31/785
CPC分类号： A61K31/015 , A61K31/355 , A61K31/375 , A61K31/4415 , A61K31/714 , A61K31/785 , A61K2300/00
摘要： The invention relates to a method for treating Syndrome X, or inhibiting the onset of symptoms of Syndrome X in a patient, and includes administering a therapeutically effective amount of a salt of at least one alkylated and cross-linked polymer, or a copolymer thereof, the polymer salt formed as a product of the reaction of one or more polymers, or salts and copolymers thereof, having a repeat unit that is essentially (1) or (2); where n is a positive integer and each R, independently, is H or C 1 -C 8 alkyl group; at least one aliphatic alkylating agent; and a cross-linking agent. Long term administration of the cross-linked polyamine salts of the invention increases HDL levels and decreases LDL levels in patients. The invention also provides for administration of the polymer salt colesevelam, in combination with an HMG-CoA reductase inhibitor; the combined administration is effective in further lowering serum total-cholesterol and LDL-cholesterol levels beyond that achieved by either agent alone.
摘要翻译：本发明涉及一种治疗综合征X或抑制患者综合症X症状发作的方法，包括给予治疗有效量的至少一种烷基化和交联聚合物或其共聚物的盐，形成为具有基本上为（1）或（2）的重复单元的一种或多种聚合物或其盐和共聚物的反应产物的聚合物盐; 其中n是正整数，每个R独立地是H或C 1 -C 8烷基; 至少一种脂族烷基化剂; 和交联剂。本发明的交联多胺盐的长期给药增加了患者的HDL水平并降低了LDL水平。本发明还提供了与HMG-CoA还原酶抑制剂组合的聚合物盐考布单抗的施用; 联合给药有效地进一步降低血清总胆固醇和低密度脂蛋白胆固醇水平超过单独任一药物所达到的水平。

8. 发明申请

WO1998042355A1 PHOSPHATE-BINDING POLYMERS COMBINED WITH A CALCIUM SUPPLEMENT FOR ORAL ADMINISTRATION 审中-公开
标题翻译：与用于口腔管理的钙补充剂组合的磷酸酯结合聚合物
公开(公告)号：WO1998042355A1
公开(公告)日：1998-10-01
申请号：PCT/US1997005780
申请日：1997-04-08
申请人： GELTEX PHARMACEUTICALS, INC. , GOLDBERG, Dennis, I. , BURKE, Steven, K. , MANDEVILLE, W., Harry, III , HOLMES-FARLEY, Stephen, Randall , WHITESIDES, George, M.
发明人： GELTEX PHARMACEUTICALS, INC.
IPC分类号： A61K31/785
CPC分类号： C08G73/02 , A61K31/785 , A61K33/06 , A61K33/14 , A61K31/7004 , A61K31/19 , A61K2300/00
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。聚合物经口给药，可用于治疗高磷血症。

9. 发明申请

WO1996021454A1 PHOSPHATE-BINDING POLYMERS FOR ORAL ADMINISTRATION 审中-公开
标题翻译：用于口服管理的磷酸酯结合聚合物
公开(公告)号：WO1996021454A1
公开(公告)日：1996-07-18
申请号：PCT/US1995000482
申请日：1995-01-12
申请人： GELTEX PHARMACEUTICALS, INC. , HOLMES-FARLEY, Stephen, Randall , MANDEVILLE, Harry, W., III , WHITESIDES, George, McClelland
发明人： GELTEX PHARMACEUTICALS, INC.
IPC分类号： A61K31/785
CPC分类号： A61K31/785
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。

10. 发明申请

WO2003002570A1 ARYL BORONIC ACIDS FOR TREATING OBESITY 审中-公开
公开(公告)号：WO2003002570A1
公开(公告)日：2003-01-09
申请号：PCT/US2002/020923
申请日：2002-07-01
申请人： GELTEX PHARMACEUTICALS, INC.
发明人： HOLMES-FARLEY, Stephen, Randall , MANDEVILLE, W., Harry, III , HUVAL, Chad, Cori , LI, Xinhua , DHAL, Pradeep, K.
IPC分类号： C07F5/02
CPC分类号： C07F5/025 , A61K31/74 , A61K31/785
摘要： Disclosed is a phenyl boronic acid compound represented by Structural Formula (I): Ar is a substituted or unsubstituted aryl group. Z and Z' are independently -O-. -NH- or -S-. X is an electron withdrawing group. R is a substituted or unsubstituted straight chained hydrocarbyl group optionally comprising one or more amine, ammonium, ether, thioether or phenylene linking groups and Y is -H, an amine, -[NH-(NH 2 ) q ]-NH 2 , halogen, -CF 3 , thiol, ammonium, alcohol, -COOH, -SO 3 H, -OSO 3 H or phosphonium group covalently bonded to the terminal position of R. Each -NH- in -[NH-)CH 2 ) q ] r -NH 2 is optionally N -alkylated or N,N -dialkylated and -NH 2 in -[NH-(CH 2 ) q ] r -NH 2 is optionally N -alkylated, N,N -dialkylated or N,N,N -triakylated. q is an integer from 2 to about 10 and r is an integer from 1 to about 5. R 1 and R 1' are independently -H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group, or, taken together, are a C2-C5 substituted or unsubstituted alkylene group optionally comprising an amine linking group [-N + (R 1a )-]. Each R 1 , is Structural Formula (I) is preferably -H. R 1a is-H, alkyl, substituted alkyl, phenyl or substituted phenyl. Also disclosed is a method of treating obesity in a subject by administering an effective amount of a compound represented by Structural Formula (I) and a pharmaceutical composition comprising the compound and a pharmaceutically acceptable carier or diluent.
摘要翻译：公开了由结构式（I）表示的苯基硼酸化合物：Ar是取代或未取代的芳基。 Z和Z'独立地为-O-。 -NH-或-S-。 X是吸电子基团。 R是任选包含一个或多个胺，铵，醚，硫醚或亚苯基连接基团的取代或未取代的直链烃基，Y是-H，胺， - [NH-（NH 2）q] -NH 2，卤素， CF 3，硫醇，铵，醇，-COOH，-SO 3 H，-OSO 3 H或共价键合到R的末端的鏻基。每个-NH-在 - [NH-）CH 2）q] r -NH 2任选地N-烷基化或-N，N-二烷基化和-NH 2在 - [NH-（CH 2）q] r -NH 2中的任选被N-烷基化，N，N-二烷基化或N，N，N-三烷基化。 q为2至约10的整数，r为1至约5的整数.R 1和R 1'独立地为-H，脂族基团，取代的脂族基团，芳基或取代的芳基，或被取代一起是任选地包含胺连接基团[-N +（R 1a）] - 的C 2 -C 5取代或未取代的亚烷基。每个R 1，结构式（I）优选为-H。 R 1a是-H，烷基，取代的烷基，苯基或取代的苯基。还公开了通过施用有效量的由结构式（I）表示的化合物和包含该化合物和药学上可接受的卡里尔或稀释剂的药物组合物来治疗受试者的肥胖症的方法。

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