Hydrophobic sequestrant for cholesterol depletion
    41.
    发明授权
    Hydrophobic sequestrant for cholesterol depletion 失效
    疏水性螯合剂用于胆固醇消耗

    公开(公告)号:US5900475A

    公开(公告)日:1999-05-04

    申请号:US659264

    申请日:1996-06-06

    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。

    Phosphate transport inhibitors
    42.
    发明授权
    Phosphate transport inhibitors 有权
    磷酸盐转运抑制剂

    公开(公告)号:US07119120B2

    公开(公告)日:2006-10-10

    申请号:US10327627

    申请日:2002-12-20

    IPC分类号: A61K31/18 A61K31/16 A61K37/18

    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。

    Fat-binding polymers
    43.
    发明授权

    公开(公告)号:US07049345B2

    公开(公告)日:2006-05-23

    申请号:US10187315

    申请日:2002-06-27

    IPC分类号: A61K47/30

    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.