公开(公告)号：US06299868B1

公开(公告)日：2001-10-09

申请号：US09353329

申请日：1999-07-14

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： A61K31795

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。

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。

公开(公告)号：US20060280719A1

公开(公告)日：2006-12-14

申请号：US11438679

申请日：2006-05-22

申请人： Thomas Jozefiak ,  Cecilia Bastos ,  Chad Huval

发明人： Thomas Jozefiak ,  Cecilia Bastos ,  Chad Huval

IPC分类号： A61K31/79 ,  C08L85/02

CPC分类号： C07F9/65502 ,  C07F9/3821 ,  C07F9/4012 ,  C07F9/5537 ,  C08F8/40 ,  C08F30/02 ,  Y02P20/55

摘要： Disclosed is a phosphate transport inhibiting compound represented by Structural Formula (I): R1 and R2 are independently —H, an electron withdrawing group or a C1-C10 alkyl group. Y is a covalent bond, a substituted methylene group, an unsubstituted methylene group or —CR1R2P(O)(OH)—. R3 is a hydrocarbyl group optionally comprising one or more amine, ammonium, ether, thioether or phenylene linking groups, a substituted hydrocarbyl group optionally comprising one or more amine, ammonium, ether, thioether or phenylene linking groups, a heteroaryl group, a substituted heteroaryl group or a phenyl group substituted with one or more groups selected from —Cl, —Br, —F, —CN, —NO2, —ORa, —N(Ra)2, —COORa, —CON(Ra)2, —CORa, —S(O)Ra, —S(O)2Ra, —S(O)2N(Ra)2, —NRaS(O)2Ra, —NRaCORa, a halogenated lower alkyl group, an aryl group, a substituted aryl group, or a halogenated alkoxy group. Each Ra is independently —H, lower alkyl, substituted lower alkyl, aryl or substituted aryl. Each Rb is independently —H, a lower alkyl group, or a phosphate protecting group.

摘要翻译： 公开了由结构式（I）表示的磷酸盐转运抑制化合物：R1和R2独立地是-H，吸电子基团或C 1 -C 10烷基 。 Y是共价键，取代亚甲基，未取代的亚甲基或-CR 1 R 2 P（O）（OH） - 。 R3是任选地包含一个或多个胺，铵，醚，硫醚或亚苯基连接基团的烃基，任选地包含一个或多个胺，铵，醚，硫醚或亚苯基连接基团的取代的烃基，杂芳基，取代的杂芳基 基团或被一个或多个选自-Cl，-Br，-F，-CN，-NO 2 - 的基团取代的苯基，-OR a，-N（ -CON（R a）2 O 2， - CO 2， - CO 2， - CO 2， ，-S（O）R a，-S（O）2 R a，S（O）2， ，-S（O）2 N（R a）O 2，-NR a S（O） 卤代低级烷基，芳基，取代的芳基，取代的芳基，取代的芳基，取代的芳基， 基团或卤代烷氧基。 每个R a a独立地是-H，低级烷基，取代的低级烷基，芳基或取代的芳基。 每个R b独立地是-H，低级烷基或磷酸酯保护基。

公开(公告)号：US20070021509A1

公开(公告)日：2007-01-25

申请号：US11489286

申请日：2006-07-19

申请人： Thomas Jozefiak ,  Cecilia Bastos ,  Andrew Papoulis ,  Stephen Holmes-Farley

发明人： Thomas Jozefiak ,  Cecilia Bastos ,  Andrew Papoulis ,  Stephen Holmes-Farley

IPC分类号： A61K31/18

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 C1-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：<？in-line-formula description =“In-line Formulas”end =“lead”？> Ar -WXY-Ar _{2 <？in-line-formula description =“In-line Formulas”end =“tail”？>或其药学上可接受的盐。 Ar 1和Ar 2独立地是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独立地是共价键或C1-C3取代或未取代的亚烷基。 X为含杂原子的官能团，芳香族杂环基，取代芳香族杂环基，非芳香族杂环基，取代非芳香族杂环基，烯基或取代烯基。 还公开了治疗患有与高磷酸盐血症相关的疾病的受试者以及由磷酸盐转运功能介导的疾病的方法。 所述方法包括施用有效量的上述一种化合物的步骤。}

公开(公告)号：US07048917B1

公开(公告)日：2006-05-23

申请号：US09721291

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： A61K31/795 ,  A61K31/785 ,  A61K31/74

CPC分类号： A61K31/74 ,  A61K31/785 ,  A61K31/795 ,  Y10S514/909

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。