公开(公告)号：EP2043627A2

公开(公告)日：2009-04-08

申请号：EP07796408.8

申请日：2007-06-25

申请人： GENZYME CORPORATION

发明人： HUVAL, Chad, C. ,  DHAL, Pradeep, K. ,  HOLMES-FARLEY, Stephen, Randall

IPC分类号： A61K31/295 ,  A61K33/26 ,  A61K9/14

CPC分类号： A61K33/26 ,  A61K9/145 ,  A61K9/146 ,  A61K31/295 ,  A61K31/785 ,  A61K45/06 ,  A61K2300/00

摘要： A pharmaceutical composition comprises a pharmaceutically acceptable ferrous iron compound; an amine polymer or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. Alternatively, a pharmaceutica composition comprises a pharmaceutically acceptable ferrous iron compound and pharmaceutically acceptable carrier, wherein the ferrous iron compound is selecte from the group consisting of iron(II) acetate, iron(II) citrate, iron(II) ascorbate, iron(II) oxalate, iron(II) oxide, iron(II) carbonate, iron(II) carbonate saccharated, iron(II) formate, iron(II) sulfate, iron(II) chloride, iron(II) acetylacetonate and combinations thereof. A method of treating a subject with hyperphosphatemia comprises administering to the subject an effective amount of a pharmaceutical composition as described above.

公开(公告)号：EP1578816A1

公开(公告)日：2005-09-28

申请号：EP03768974.2

申请日：2003-11-19

申请人： GENZYME CORPORATION

发明人： HUVAL, Chad Cori ,  LI, Xinhua ,  HOLMES-FARLEY, Stephen, Randall ,  DHAL, Pradeep, K.

IPC分类号： C08F20/00

CPC分类号： C08F230/06 ,  A61K31/69 ,  A61K45/06 ,  C08F30/06 ,  C08F220/56 ,  C08F220/60 ,  C08F226/10 ,  C08F265/00 ,  C08F289/00 ,  C08F290/06 ,  C08F290/14 ,  C08F291/00 ,  C08F293/005 ,  C08F297/00 ,  C08F297/02 ,  C08F2438/02

摘要： Human obesity is a health problem affecting a significant proportion of the American population. Numerous methods of treating obesity have been developed, but all have serious drawbacks. The present invention discloses a novel class of polymers with either a sulfur atom or an electron withdrawing group between a polymer backbone and pendant aryl boronic acid group. Polymers having such an electron withdrawing group have been found to be particularly effective in inhibiting lipase in vitro and in vivo. Methods of treating obesity and reducing absorption of fat are also disclosed.

公开(公告)号：EP1416942A1

公开(公告)日：2004-05-12

申请号：EP02726732.7

申请日：2002-04-10

申请人： GENZYME CORPORATION

发明人： HOLMES-FARLEY, Stephen, Randall ,  BURKE, Steven, K.

IPC分类号： A61K31/785 ,  A61P3/00

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 aliphatic amine polymer. In one embodiment, the polymer binds to uric acid or a precursor thereof. Examples of polymers useful in an embodiment of the invention include sevelamer hydrochloride and colesevelam. The invention includes the use of amine polymers such as a cross-linked polymer characterized by a repeat unit having the formula: 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 binds serum uric acid in a patient.

公开(公告)号：EP1404349A1

公开(公告)日：2004-04-07

申请号：EP02744787.9

申请日：2002-07-01

申请人： GENZYME CORPORATION

发明人： HOLMES-FARLEY, Stephen, Randall

IPC分类号： A61K31/785

CPC分类号： A61K31/785 ,  A61K31/74

摘要： The present invention provides fat-binding polymers, which comprise dialkanolamine, dialkanolammonium, aminoalkylpolyol, and ammoniumalkylpolyol pendant groups for subjects in need of fat removal from the gastrointestinal tract, particularly subjects suffering from steatorrhea and/or experiencing side effects from lipase inhibitors. Patients being administered with lipase inhibitors are typically being treated for Type II Diabetes, streatorrhea, and hypertriglyceridemia. The fat binding polymers of this invention are also suitable for use with obese subjects.

公开(公告)号：EP2968403A1

公开(公告)日：2016-01-20

申请号：EP14715503.0

申请日：2014-03-12

申请人： Genzyme Corporation

发明人： HOLMES-FARLEY, Stephen, Randall ,  DHAL, Pradeep ,  BESEV, Magnus ,  MILLER, Robert, J. ,  PAPOULIS, Andrew, T.

IPC分类号： A61K31/785 ,  A61P13/12 ,  A61P9/10 ,  A61P25/28 ,  A61P27/12

CPC分类号： C08F126/02 ,  A61K31/785

摘要： Sequestrants of AGE precursors comprise amines separated by 2, 3 or 4 carbons. Sequestrants of AGE precursors can be used as pharmaceutical agents and in pharmaceutical compositions. The sequestrants of AGE precursors are particularly useful binding AGE precursors and dietary dicarbonyls in mammals in the gastrointestinal tract for the treatment of ailments such as diabetic nephropathy, chronic renal disease, atherosclerosis, stroke, cataracts, and Alzheimer's disease.

摘要翻译： AGE前体的螯合剂包括被2,3或4个碳分隔的胺。 AGE前体的螯合剂可用作药剂和药物组合物。 AGE前体的多价螯合剂特别有用于结合AGE前体和膳食二羰基在哺乳动物在胃肠道中用于治疗诸如糖尿病肾病，慢性肾脏疾病，动脉粥样硬化，中风，白内障和阿尔茨海默氏病等疾病。

公开(公告)号：EP1404349B1

公开(公告)日：2008-10-22

申请号：EP02744787.9

申请日：2002-07-01

申请人： GENZYME CORPORATION

发明人： HOLMES-FARLEY, Stephen, Randall

IPC分类号： A61K31/785

CPC分类号： A61K31/785 ,  A61K31/74

摘要： The present invention provides fat-binding polymers, which comprise dialkanolamine, dialkanolammonium, aminoalkylpolyol, and ammoniumalkylpolyol pendant groups for subjects in need of fat removal from the gastrointestinal tract, particularly subjects suffering from steatorrhea and/or experiencing side effects from lipase inhibitors. Patients being administered with lipase inhibitors are typically being treated for Type II Diabetes, streatorrhea, and hypertriglyceridemia. The fat binding polymers of this invention are also suitable for use with obese subjects.

公开(公告)号：EP1465638A2

公开(公告)日：2004-10-13

申请号：EP02806234.7

申请日：2002-12-24

申请人： GENZYME CORPORATION

发明人： JOZEFIAK, Thomas, H. ,  BASTOS, Cecilia, M. ,  PAPOULIS, Andrew, T. ,  HOLMES-FARLEY, Stephen, Randall

IPC分类号： A61K31/63 ,  A61K31/166 ,  A61K31/415 ,  A61K31/17 ,  A61P13/12 ,  A61P19/10 ,  A61P3/14

CPC分类号： A61K45/06 ,  A61K31/166 ,  A61K31/17 ,  A61K31/18 ,  A61K31/415 ,  A61K31/63 ,  A61K33/38 ,  A61K2300/00

摘要： Disclosed are compounds, which have been identified as inhibitors of phosphate transport. Many of the compounds are represented by Structural Formula (I): Ar1-W-X-Y-Ar2; or a pharmaceutically acceptable salt thereof. Ar1 and Ar2 are independently a substituted or unsubstituted aryl group or an optionally substituted five membered or six membered non-aromatic heterocylic group fused to an optionally substituted monocylic aryl group. W and Y are independently a covalent bond or a C 1-C3 substituted or unsubstituted alkylene group. X is a heteroatom-containing functional group, an aromatic heterocyclic group, substituted aromatic heterocyclic group, non-aromatic heterocyclic group, substituted non-aromatic heterocyclic group, an olefin group or a substituted olefin group. Also disclosed are methods of treating a subject with a disease associated with hyperphosphatemia, as well as a disease mediated by phosphate-transport function. The methods comprise the step of administering an effective amount of the one of the compounds described above.

摘要翻译： 公开了已被鉴定为磷酸盐转运抑制剂的化合物。 许多化合物由结构式（I）表示：Ar 1 -W-X-Y-Ar 2; 或其药学上可接受的盐。 Ar 1和Ar 2独立地为与任选取代的单环芳基稠合的取代或未取代的芳基或任选取代的五元或六元非芳族杂环基。 W和Y独立地为共价键或C 1 -C 3取代或未取代的亚烷基。 X是含有杂原子的官能团，芳香族杂环基，取代的芳香族杂环基，非芳香族杂环基，取代的非芳香族杂环基，烯烃基或取代烯烃基。 还公开了治疗患有高磷酸盐血症相关疾病的受试者以及由磷酸盐转运功能介导的疾病的方法。 该方法包括施用有效量的上述化合物之一的步骤。

公开(公告)号：EP2131820A1

公开(公告)日：2009-12-16

申请号：EP08726435.4

申请日：2008-03-05

申请人： Genzyme Corporation

发明人： DHAL, Pradeep, K. ,  HOLMES-FARLEY, Stephen, Randall ,  HUVAL, Chad, C. ,  POLOMOSCANIK, Steven, C.

IPC分类号： A61K9/48

CPC分类号： C08G75/20 ,  C08G65/24 ,  C08G73/0253

摘要： Sulfone-containing copolymers and copolymer networks and compositions including sulfone-containing copolymers and copolymer networks may be used to bind target ions, such as phosphorous-containing compounds in the gastrointestinal tract of animals. In some cases, sulfone-containing copolymers and copolymer networks may be derived from a multi- amine monomer and a multifunctional sulfonyl-containing monomer comprising two or more amine-reactive groups.

摘要翻译： 含砜共聚物和共聚物网络以及包含含砜共聚物和共聚物网络的组合物可用于结合目标离子，例如动物胃肠道中的含磷化合物。 在一些情况下，含砜共聚物和共聚物网络可以衍生自多胺单体和包含两个或更多个胺反应性基团的多官能磺酰基单体。

公开(公告)号：EP2068819A2

公开(公告)日：2009-06-17

申请号：EP07837624.1

申请日：2007-08-31

申请人： GENZYME CORPORATION

发明人： COOPER, Christopher ,  DHAL, Pradeep, K. ,  GIMI, Rayomand, H. ,  HARRIS, David, J. ,  HOLMES-FARLEY, Stephen, Randall ,  HUVAL, Chad, C. ,  LEE, Edward

IPC分类号： A61K8/72

CPC分类号： C07C217/08 ,  A61K31/785

摘要： Amine compounds, amine polymers, crosslinked amine polymers and pharmaceutical compositions comprising the same may include polyhydroxy-containing cores that may be substituted with amine groups and may be used to treat hyperphosphatemia or to remove ions from the gastrointestinal tract of animals, including humans.

公开(公告)号：EP2016114A2

公开(公告)日：2009-01-21

申请号：EP07776627.7

申请日：2007-05-02

申请人： GENZYME CORPORATION

发明人： HUVAL, Chad, C. ,  DHAL, Pradeep, K. ,  HOLMES-FARLEY, Stephen, Randall

IPC分类号： C08G73/02

CPC分类号： A61K31/785 ,  C08G73/02 ,  C08G73/0206

摘要： Disclosed is a polymer or physiologically acceptable salt thereof. The polymer comprises a polymerized multifunctional amine monomer. The amine monomer comprises at least two amine groups and at least two acyclic nitrogen atoms that are connected through a -CH2CH2- group, provided that the amine monomer is not ethylenediamine or diethylenetriamine. The disclosed polymers can be used to bind anions in subject in need of such treatment.

摘要翻译： 公开了一种聚合物或其生理学上可接受的盐。 该聚合物包含聚合的多官能胺单体。 胺单体包含至少两个胺基和至少两个通过-CH 2 CH 2 - 基连接的无环氮原子，条件是胺单体不是乙二胺或二亚乙基三胺。 所公开的聚合物可以用于结合需要这种治疗的受试者中的阴离子。