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    Combination therapy for treating hypercholestrolemia
    1.
    发明授权
    Combination therapy for treating hypercholestrolemia 有权
    联合治疗高胆固醇血症

    公开(公告)号：US06264938B1

    公开(公告)日：2001-07-24

    申请号：US09311402

    申请日：1999-05-13

    申请人： Chad Cori Huval ,  Stephen Randall Holmes-Farley ,  John S. Petersen ,  Pradeep K. Dhal

    发明人： Chad Cori Huval ,  Stephen Randall Holmes-Farley ,  John S. Petersen ,  Pradeep K. Dhal

    IPC分类号： A61K31787

    CPC分类号： A61K31/785 ,  Y10S514/824

    摘要： The invention relates to methods for treating hypercholesterolemia and atherosclerosis, and reducing serum cholesterol in a mammal. The methods of the invention comprise administering to a mammal a first amount of a bile acid sequestrant compound which is an unsubstituted polydiallylamine polymer and a second amount of an HMG Co-A reductase inhibitor compound. The first and second amounts together comprise a therapeutically effective amount. The invention further relates to pharmaceutical compositions useful for the treatment of hypercholesterolemia and atherosclerosis, and for reducing serum cholesterol. The pharmaceutical compositions comprise a combination of a first amount of an unsubstituted polydiallylamine polymer compound and a second amount of an HMG Co-A reductase inhibitor compound. The first and second amounts comprise a therapeutically effective amount. The pharmaceutical compositions of the present invention may optionally contain a pharmaceutically acceptable carrier.

    摘要翻译： 本发明涉及治疗高胆固醇血症和动脉粥样硬化以及降低哺乳动物血清胆固醇的方法。 本发明的方法包括向哺乳动物施用第一量的胆汁酸多价螯合剂化合物，其是未取代的聚二烯丙基胺聚合物和第二量的HMG Co-A还原酶抑制剂化合物。 第一和第二量一起包含治疗有效量。本发明还涉及可用于治疗高胆固醇血症和动脉粥样硬化以及降低血清胆固醇的药物组合物。 药物组合物包含第一量的未取代的聚二烯丙基胺聚合物化合物和第二量的HMG Co-A还原酶抑制剂化合物的组合。 第一和第二量包括治疗有效量。 本发明的药物组合物可任选地含有药学上可接受的载体。

    Combination therapy for treating hypercholesterolemia
    3.
    发明申请
    Combination therapy for treating hypercholesterolemia 审中-公开
    联合治疗高胆固醇血症

    公开(公告)号：US20100266526A1

    公开(公告)日：2010-10-21

    申请号：US12590511

    申请日：2009-11-09

    申请人： Chad Cori Huval ,  Stephen Randall Holmes-Farley ,  John S. Petersen ,  Pradeep K. Dhal

    发明人： Chad Cori Huval ,  Stephen Randall Holmes-Farley ,  John S. Petersen ,  Pradeep K. Dhal

    IPC分类号： A61K31/785 ,  A61P3/06 ,  A61K31/787

    CPC分类号： A61K31/785 ,  Y10S514/824

    摘要： The invention relates to methods for treating hypercholesterolemia and atherosclerosis, and reducing serum cholesterol in a mammal. The methods of the invention comprise administering to a mammal a first amount of a bile acid sequestrant compound which is an unsubstituted polydiallylamine polymer and a second amount of a cholesterol-lowering agent. The first and second amounts together comprise a therapeutically effective amount.The invention further relates to pharmaceutical compositions useful for the treatment of hypercholesterolemia and atherosclerosis, and for reducing serum cholesterol. The pharmaceutical compositions comprise a combination of a first amount of an unsubstituted polydiallylamine polymer compound and a second amount of a cholesterol-lowering agent. The first and second amounts comprise a therapeutically effective amount. The pharmaceutical compositions of the present invention may optionally contain a pharmaceutically acceptable carrier.

    摘要翻译： 本发明涉及治疗高胆固醇血症和动脉粥样硬化以及降低哺乳动物血清胆固醇的方法。 本发明的方法包括向哺乳动物施用第一量的胆汁酸多价螯合剂化合物，其是未取代的聚二烯丙基胺聚合物和第二量的降胆固醇剂。 第一和第二量一起包括治疗有效量。 本发明还涉及可用于治疗高胆固醇血症和动脉粥样硬化以及降低血清胆固醇的药物组合物。 药物组合物包含第一量的未取代的聚二烯丙基胺聚合物化合物和第二量的降胆固醇剂的组合。 第一和第二量包括治疗有效量。 本发明的药物组合物可任选地含有药学上可接受的载体。

    Combination therapy for treating hypercholesterolemia
    5.
    发明授权
    Combination therapy for treating hypercholesterolemia 有权
    联合治疗高胆固醇血症

    公开(公告)号：US06365186B1

    公开(公告)日：2002-04-02

    申请号：US09311103

    申请日：1999-05-13

    申请人： Chad Cori Huval ,  Stephen Randall Holmes-Farley ,  John S. Petersen ,  Pradeep K. Dhal

    发明人： Chad Cori Huval ,  Stephen Randall Holmes-Farley ,  John S. Petersen ,  Pradeep K. Dhal

    IPC分类号： A61K910

    CPC分类号： A61K31/785 ,  Y10S514/824

    摘要： The invention relates to methods for treating hypercholesterolemia and atherosclerosis, and reducing serum cholesterol in a mammal. The methods of the invention comprise administering to a mammal a first amount of a bile acid sequestrant compound which is an unsubstituted polydiallylamine polymer and a second amount of a cholesterol-lowering agent. The first and second amounts together comprise a therapeutically effective amount. The invention further relates to pharmaceutical compositions useful for the treatment of hypercholesterolemia and atherosclerosis, and for reducing serum cholesterol. The pharmaceutical compositions comprise a combination of a first amount of an unsubstituted polydiallylamine polymer compound and a second amount of a cholesterol-lowering agent. The first and second amounts comprise a therapeutically effective amount. The pharmaceutical compositions of the present invention may optionally contain a pharmaceutically acceptable carrier.

    摘要翻译： 本发明涉及治疗高胆固醇血症和动脉粥样硬化以及降低哺乳动物血清胆固醇的方法。 本发明的方法包括向哺乳动物施用第一量的胆汁酸多价螯合剂化合物，其是未取代的聚二烯丙基胺聚合物和第二量的降胆固醇剂。 第一和第二量一起包含治疗有效量。本发明还涉及可用于治疗高胆固醇血症和动脉粥样硬化以及降低血清胆固醇的药物组合物。 药物组合物包含第一量的未取代的聚二烯丙基胺聚合物化合物和第二量的降胆固醇剂的组合。 第一和第二量包括治疗有效量。 本发明的药物组合物可任选地含有药学上可接受的载体。

    Aryl boronic acids for treating obesity
    7.
    发明授权
    Aryl boronic acids for treating obesity 有权

    公开(公告)号：US07456156B2

    公开(公告)日：2008-11-25

    申请号：US11343598

    申请日：2006-01-31

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

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

    IPC分类号： A61K31/69 ,  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—(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.

    Aryl boronic acids for treating obesity
    8.
    发明授权
    Aryl boronic acids for treating obesity 有权

    公开(公告)号：US07049304B2

    公开(公告)日：2006-05-23

    申请号：US11027643

    申请日：2004-12-30

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

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

    IPC分类号： A61K31/69 ,  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—(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.

    Aryl boronic acids for treating obesity
    10.
    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

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

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

    IPC分类号： A61K31/69 ,  A61K31/74 ,  A61K31/785 ,  A61P3/04 ,  A61P3/06 ,  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—(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.

    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。