公开(公告)号：US08067584B2

公开(公告)日：2011-11-29

申请号：US10546005

申请日：2004-02-23

申请人： Ingemar Starke ,  Suzanne Alenfalk ,  Mats Peter Nordberg ,  Mikael Ulf Johan Dahlstrom ,  Stig Jonas Bostrom ,  Malin Anita Lemurell ,  Andreas Christer Wallberg

发明人： Ingemar Starke ,  Suzanne Alenfalk ,  Mats Peter Nordberg ,  Mikael Ulf Johan Dahlstrom ,  Stig Jonas Bostrom ,  Malin Anita Lemurell ,  Andreas Christer Wallberg

IPC分类号： C07D281/10 ,  A61K31/554

CPC分类号： C07D281/10 ,  C07D337/08

摘要： Compounds of formula: (1) pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and their use as ileal bile acid transport (IBAT) inhibitors for the treatment of hyperlipidaemia are described. Processes for their manufacture and pharmaceutical compositions containing them are also described.

摘要翻译： 描述了下列化合物：（1）其药学上可接受的盐，溶剂化物，这些盐及其前体药物的溶剂合物及其作为回肠胆汁酸转运（IBAT）抑制剂用于治疗高脂血症的用途。 还描述了其制备方法和含有它们的药物组合物。

公开(公告)号：US07238684B2

公开(公告)日：2007-07-03

申请号：US10511984

申请日：2003-04-23

申请人： Ingemar Starke ,  Mikael Ulf Johan Dahlstrom ,  Mats Peter Nordberg ,  Suzanne Alenfalk ,  Andreas Christer Wallberg ,  Stig Jonas Bostrom

发明人： Ingemar Starke ,  Mikael Ulf Johan Dahlstrom ,  Mats Peter Nordberg ,  Suzanne Alenfalk ,  Andreas Christer Wallberg ,  Stig Jonas Bostrom

IPC分类号： C07D285/36 ,  A61K31/554

CPC分类号： C07D285/36

摘要： The present invention relates to compounds of formula (I): wherein Rv, R1, R2, Rx, Ry, R3, R4, R5, R6, Rz and v are as defined within; pharmaceutically acceptable salts, solvates, solvates or such salts and prodrugs thereof and their use as ileal bile acid transport (IBAT) inhibitors for the treatment of hyperlipidaemia. Processes for their manufacture and pharmaceutical compositions containing them are also described.

摘要翻译： 本发明涉及式（I）化合物：其中R 1，R 2，R 2，R x， R S，R 3，R 3，R 4，R 5，R 6， V S，R z如上所定义; 药学上可接受的盐，溶剂合物，溶剂化物或其盐和前药，以及它们作为回肠胆汁酸转运（IBAT）抑制剂用于治疗高脂血症的用途。 还描述了其制备方法和含有它们的药物组合物。

公开(公告)号：US07192946B2

公开(公告)日：2007-03-20

申请号：US10488540

申请日：2002-08-30

申请人： Ingemar Starke ,  Mikael Ulf Johan Dahlstrom ,  David Blomberg ,  Suzanne Alenfalk ,  Peter Nordberg ,  Andreas Christer Wallberg ,  Stig Jonas Bostrom

发明人： Ingemar Starke ,  Mikael Ulf Johan Dahlstrom ,  David Blomberg ,  Suzanne Alenfalk ,  Peter Nordberg ,  Andreas Christer Wallberg ,  Stig Jonas Bostrom

IPC分类号： A61P3/06 ,  A61K31/554 ,  C07D281/10

CPC分类号： C07D417/12 ,  C07D281/10

摘要： The present invention relates to compounds of formula (I), wherein variable groups are as defined within; pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and their use as ileal bile acid transport (IBAT) inhibitors for the treatment of hyperlipidaemia. Processes for their manufacture and pharmaceutical compositions containing them are also described

摘要翻译： 本发明涉及式（I）化合物，其中可变基团如本文所定义; 药学上可接受的盐，溶剂合物，这些盐的溶剂合物和前药，以及它们作为回肠胆汁转运（IBAT）抑制剂用于治疗高脂血症的用途。 还描述了其制备方法和含有它们的药物组合物

公开(公告)号：US20050032808A1

公开(公告)日：2005-02-10

申请号：US10499054

申请日：2002-12-18

申请人： Anna Berggren ,  Stig Jonas Bostrom ,  Stig Elebring ,  Peter Greasley ,  Emma Terricabras ,  Johan Wilstermann

发明人： Anna Berggren ,  Stig Jonas Bostrom ,  Stig Elebring ,  Peter Greasley ,  Emma Terricabras ,  Johan Wilstermann

IPC分类号： C07D241/24 ,  A61K20060101 ,  A61K31/495 ,  A61K31/4965 ,  A61K31/497 ,  A61P20060101 ,  A61P3/04 ,  A61P7/00 ,  A61P9/10 ,  A61P15/00 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P37/00 ,  A61P43/00 ,  C07D20060101

CPC分类号： C07D241/24

摘要： The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts, prodrugs, solvates and crystalline forms thereof, in which R1 and R2 independently represent: a C1-6alkyl group; an optionally substituted (amino)C1-4alkyl-group; an optionally substituted non-aromatic C3-15carbocyclic group; a (C3-12cycloalkyl)C1-3alkyl-group; a group —(CH2)r(phenyl)s in which r is 0, 1, 2, 3 or 4, s is 1 when r is 0 otherwise s is 1 or 2 and the phenyl groups are optionally independently substituted by Z; naphthyl; anthracenyl; an optionally substituted saturated 5 to 8 membered heterocyclic group containing one nitrogen and optionally one of the following: oxygen, sulphur or an additional nitrogen; 1-adamantylmethyl; a group —(CH2)t Het in which t is 0, 1, 2, 3 or 4, and the alkylene chain is optionally substituted and Het represents an optionally substituted aromatic heterocycle; or R1 represents H and R2 is as defined above; or R1 and R2 together with the nitrogen atom to which they are attached represent a saturated optionally substituted 5 to 8 membered heterocyclic group as defined above; X is CO or SO2; Y is absent or represents NH optionally substitututed by a C1-3alkyl group; R3 and R4 independently represent phenyl, thienyl or pyridyl substituted by Z; Z represents a C1-3alkyl group, a C1-3alkoxy group, hydroxy, halo, trifluoromethyl, trifluoromethylthio, trifluoromethoxy, trifluoromethylsulphonyl, nitro, amino, mono or di C1-3alkylamino, mono or di C1-3alkylamido, C1-3alkylsulphonyl, C1-3alkoxycarbonyl, carboxy, cyano, carbamoyl, mono or di C1-3alkyl carbamoyl, sulphamoyl and acetyl; and R5 is H, a C1-3alkyl group, a C1-3alkoxymethyl group, trifluoromethyl, a hydroxyC1-3alkyl group, C1-3alkoxycarbonyl, carboxy, cyano, carbamoyl, mono or di C1-3alkylcarbamoyl, acetyl, or hydrazinocarbonyl of formula —CONHNRaRb; with the provisos; and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them.