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    Aryl boronic acids for treating obesity
    3.
    发明授权
    Aryl boronic acids for treating obesity 有权
    用于治疗肥胖症的芳基硼酸

    公开(公告)号：US06858592B2

    公开(公告)日：2005-02-22

    申请号：US10187397

    申请日：2002-06-27

    Applicant: Stephen Randall Holmes-Farley ,  W. Harry Mandeville, III ,  Pradeep K. Dhal ,  Chad Cori Huval ,  Xinhua Li

    Inventor： Stephen Randall Holmes-Farley ,  W. Harry Mandeville, III ,  Pradeep K. Dhal ,  Chad Cori Huval ,  Xinhua Li

    IPC: A61K31/69 ,  A61K31/74 ,  A61K31/785 ,  A61P3/04 ,  A61P3/06 ,  C07F5/02

    CPC classification number: C07F5/025 ,  A61K31/74 ,  A61K31/785

    Abstract: 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—(CH2)q]r—NH2, halogen, —CF3, thiol ammonium, alcohol, —COOH, —SO3H, —OSO3H or phosphonium group covalently bonded to the terminal position of R. Each —NH— in —[NH—(CH2)q]r—NH2 is optionally N-alkylated or N,N-dialkylated and —NH2 in —[NH—(CH2)q]r—NH2 is optionally N-alkylated, N,N-dialkylated or N,N,N-trialkylated. q is an integer from 2 to about 10 and r is an integer from 1 to about 5. R1 and R1′ 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+(R1a)—]. Each R1 is Structural Formula (I) is preferably —H. R1a 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 carrier or diluent.

    Abstract translation: 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'独立地是-O-。 -NH-或-S-X是吸电子基团.R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取代或未取代的直链烃基，Y是-H，胺， - [NH-（CH 2）q] r -NH 2，卤素，-CF 3，硫醇铵，醇，-COOH，-SO 3 H，-OSO 3 H或共价键合到R的末端的鏻基团。 NH-（CH 2）q] r -NH 2任选被N-烷基化或N，N-二烷基化，-NH 2在 - [NH-（CH 2）q] r -NH 2中任选地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.R1的整数，R1'独立地为-H，脂族基团，取代的脂族基团，芳基或 取代的芳基，或者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R1是结构式（I）优选-HR 1a是-H，烷基，取代的烷基，苯基或取代的苯基。还公开了通过给予有效量的由 结构式（I）和包含该化合物和药学上可接受的载体或稀释剂的药物组合物。

    Lipase inhibiting polymers
    5.
    发明授权
    Lipase inhibiting polymers 失效
    脂肪酶抑制聚合物

    公开(公告)号：US06352692B1

    公开(公告)日：2002-03-05

    申请号：US09226585

    申请日：1999-01-06

    Applicant: W. Harry Mandeville, III ,  Molly Kate Boie ,  Venkata R. Garigapati

    Inventor： W. Harry Mandeville, III ,  Molly Kate Boie ,  Venkata R. Garigapati

    IPC: A61K3174

    CPC classification number: A61K31/00 ,  Y10S514/909

    Abstract: The invention features a method for treating obesity in a patient by administering to the patient a polymer that has been substituted with one or more groups that inhibit lipases, which are enzymes responsible for the hydrolysis of fat. The invention further relates to the polymers employed in the methods described herein as well as novel intermediates and methods for preparing the polymers.

    Abstract translation: 本发明的特征在于通过向患者施用已经被一种或多种抑制脂肪酶的基团取代的聚合物来治疗患者的肥胖的方法，脂肪酶是负责脂肪水解的酶。 本发明还涉及本文所述方法中使用的聚合物以及新型中间体和制备聚合物的方法。

    Fat-binding polymers
    6.
    发明授权
    Fat-binding polymers 失效
    脂肪结合聚合物

    公开(公告)号：US06299868B1

    公开(公告)日：2001-10-09

    申请号：US09353329

    申请日：1999-07-14

    Applicant: Thomas Jozefiak ,  Stephen Randall Holmes-Farley ,  W. Harry Mandeville, III ,  Chad Cori Huval ,  Venkata R. Garigapati ,  Keith K. Shackett ,  Danny Concagh

    Inventor： Thomas Jozefiak ,  Stephen Randall Holmes-Farley ,  W. Harry Mandeville, III ,  Chad Cori Huval ,  Venkata R. Garigapati ,  Keith K. Shackett ,  Danny Concagh

    IPC: A61K31795

    CPC classification number: A61K45/06 ,  A61K31/785 ,  A61K2300/00

    Abstract: 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.

    Abstract translation: 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。

    Fat-binding polymers
    7.
    发明授权
    Fat-binding polymers 有权
    脂肪结合聚合物

    公开(公告)号：US06264937B1

    公开(公告)日：2001-07-24

    申请号：US09166453

    申请日：1998-10-05

    Applicant: W. Harry Mandeville, III ,  George M. Whitesides ,  Stephen Randall Holmes-Farley

    Inventor： W. Harry Mandeville, III ,  George M. Whitesides ,  Stephen Randall Holmes-Farley

    IPC: A61K31785

    CPC classification number: A61K31/765 ,  A61K31/78 ,  A61K31/785 ,  A61K2300/00

    Abstract: 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 inibitors, for example, lipstatin and tetrahydrolipstatin.

    Abstract translation: 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不孕症组合施用，例如，脂抑素和四氢孕激素。

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