公开(公告)号：US20090298853A1

公开(公告)日：2009-12-03

申请号：US12339349

申请日：2008-12-19

申请人： Udo Andreas Bauer ,  Jonas Gunnar Barlind ,  Petra Johannesson ,  Jan Magnus Johansson ,  Alexander Tobias Noeske ,  Annika Ulrika Petersson ,  Alan Martin Birch ,  Roger John Butlin ,  Clive Green ,  Andrew Leach ,  Ragnar Hovland

发明人： Udo Andreas Bauer ,  Jonas Gunnar Barlind ,  Petra Johannesson ,  Jan Magnus Johansson ,  Alexander Tobias Noeske ,  Annika Ulrika Petersson ,  Alan Martin Birch ,  Roger John Butlin ,  Clive Green ,  Andrew Leach ,  Ragnar Hovland

IPC分类号： A61K31/4965 ,  C07D241/18 ,  A61P3/10

CPC分类号： C07D213/81 ,  C07D213/82 ,  C07D241/24 ,  C07D401/04 ,  C07D401/10 ,  C07D403/10

摘要： DGAT-1 inhibitor compounds of formula (I), pharmaceutically-acceptable salts and pro-drugs thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, obesity wherein, for example, Ring A is optionally substituted 2,6-pyrazindiyl; X is ═O; Ring B is optionally substituted 1,4-phenylene; Y1 is a direct bond or —O—; Y2 is —(CH2)r— wherein r is 2 or 3; n is 0 or n is 1 when Y1 is a direct bond between Ring B and Ring C and when Ring B is 1,4-phenylene and Ring C is (4-6C)cycloalkane; Ring C is optionally substituted (4-6C)cycloalkane, (7-10C)bicycloalkane, (8-12C)tricycloalkane, phenylene or pryidindiyl; L is a direct bond or —O—; p is 0, 1 or 2 and when p is 1 or 2 RA1 and RA2 are each independently hydrogen or (1-4C)alkyl; Z is carboxy or a mimic or bioisostere thereof.

摘要翻译： 与药物组合物一起描述式（I）的DGAT-1抑制剂化合物，其药学上可接受的盐和前药与制备它们的方法及其用于治疗例如肥胖症的用途，其中例如环A为 任选取代的2,6-吡嗪二基; X为-O; 环B为任选取代的1,4-亚苯基; Y1是直接键或-O-键; Y2是 - （CH2）r-，其中r是2或3; 当Y 1是环B和环C之间的直接键，当环B是1,4-亚苯基且环C是（4-6C）环烷烃时，n是0或n是1; 环C是任选取代的（4-6C）环烷烃，（7-10C）双环烷烃，（8-12C）三环烷烃，亚苯基或辛基二辛基; L是直接键或-O-键; p为0,1或2，当p为1或2时，RA1和RA2各自独立地为氢或（1-4C）烷基; Z是羧基或其模拟物或生物电子等排体。

公开(公告)号：US07994179B2

公开(公告)日：2011-08-09

申请号：US12339349

申请日：2008-12-19

申请人： Petra Johannesson ,  Jan Magnus Johansson ,  Annika Ulrika Petersson ,  Alan Martin Birch ,  Roger John Butlin

发明人： Petra Johannesson ,  Jan Magnus Johansson ,  Annika Ulrika Petersson ,  Alan Martin Birch ,  Roger John Butlin

IPC分类号： A61K31/4965

CPC分类号： C07D213/81 ,  C07D213/82 ,  C07D241/24 ,  C07D401/04 ,  C07D401/10 ,  C07D403/10

摘要： DGAT-1 inhibitor compounds of formula (I), pharmaceutically-acceptable salts and pro-drugs thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, obesity wherein, for example, Ring A is optionally substituted 2,6-pyrazindiyl; X is ═O; Ring B is optionally substituted 1,4-phenylene; Y1 is a direct bond or —O—; Y2 is —(CH2)r— wherein r is 2 or 3; n is 0 or n is 1 when Y1 is a direct bond between Ring B and Ring C and when Ring B is 1,4-phenylene and Ring C is (4-6C)cycloalkane; Ring C is optionally substituted (4-6C)cycloalkane, (7-10C)bicycloalkane, (8-12C)tricycloalkane, phenylene or pryidindiyl; L is a direct bond or —O—; p is 0, 1 or 2 and when p is 1 or 2 RA1 and RA2 are each independently hydrogen or (1-4C)alkyl; Z is carboxy or a mimic or bioisostere thereof.

摘要翻译： 与药物组合物一起描述式（I）的DGAT-1抑制剂化合物，其药学上可接受的盐和前药与制备它们的方法及其用于治疗例如肥胖症的用途，其中例如环A为 任选取代的2,6-吡嗪二基; X是= O; 环B为任选取代的1,4-亚苯基; Y1是直接键或-O-键; Y2是 - （CH2）r-，其中r是2或3; 当Y 1是环B和环C之间的直接键，当环B是1,4-亚苯基且环C是（4-6C）环烷烃时，n是0或n是1; 环C是任选取代的（4-6C）环烷烃，（7-10C）双环烷烃，（8-12C）三环烷烃，亚苯基或辛基二辛基; L是直接键或-O-键; p为0,1或2，当p为1或2时，RA1和RA2各自独立地为氢或（1-4C）烷基; Z是羧基或其模拟物或生物电子等排体。

公开(公告)号：US20090105305A1

公开(公告)日：2009-04-23

申请号：US11961850

申请日：2007-12-20

申请人： Roger John Butlin ,  Peter William Rodney Caulkett ,  Petra Johannesson ,  Laurent Daniel Knerr ,  Andrew Leach ,  Nicholas John Newcombe ,  Charles John O'Donnell ,  Helen Pointon ,  James Matthew Wood

发明人： Roger John Butlin ,  Peter William Rodney Caulkett ,  Petra Johannesson ,  Laurent Daniel Knerr ,  Andrew Leach ,  Nicholas John Newcombe ,  Charles John O'Donnell ,  Helen Pointon ,  James Matthew Wood

IPC分类号： A61K31/451 ,  C07D211/60 ,  A61P35/00 ,  A61P3/10 ,  A61P3/04

CPC分类号： C07D211/34 ,  C07D401/10 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D413/10 ,  C07D413/12 ,  C07D417/10 ,  C07D513/04

摘要： A compound of formula I or a pharmaceutically acceptable salt thereof, processes for preparing such compounds, their use as Fatty Acid Synthase inhibitors, methods for their therapeutic use, particularly in the treatment of obesity and diabetes mellitus, cancer and infection and pharmaceutical compositions containing them.

摘要翻译： 式I化合物或其药学上可接受的盐，制备这些化合物的方法，它们作为脂肪酸合酶抑制剂的用途，其治疗用途的方法，特别是治疗肥胖和糖尿病，癌症和感染以及含有它们的药物组合物 。

公开(公告)号：US20090306133A1

公开(公告)日：2009-12-10

申请号：US12339600

申请日：2008-12-19

申请人： David Blomberg ,  Anders Holmen ,  Petra Johannesson ,  Pernilla Sorme ,  Pernilla Stahlberg ,  Kay Brickmann ,  Volker Schnecke ,  Eric Wellner ,  Ragnar Hovland ,  Asa Mansson ,  Alleyn Plowright

发明人： David Blomberg ,  Anders Holmen ,  Petra Johannesson ,  Pernilla Sorme ,  Pernilla Stahlberg ,  Kay Brickmann ,  Volker Schnecke ,  Eric Wellner ,  Ragnar Hovland ,  Asa Mansson ,  Alleyn Plowright

IPC分类号： A61K31/4709 ,  C07D215/38 ,  C07D401/14 ,  A61P9/10 ,  A61P3/10 ,  A61K31/47

CPC分类号： C07C311/45 ,  C07C271/20 ,  C07C311/18 ,  C07C311/19 ,  C07C2601/14 ,  C07D213/81 ,  C07D213/82 ,  C07D215/36 ,  C07D215/52 ,  C07D217/02 ,  C07D271/06 ,  C07D277/54 ,  C07D277/64 ,  C07D277/82 ,  C07D309/04 ,  C07D319/18 ,  C07D333/34 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04

摘要： The present invention relates to Acetyl Coenzyme A Carboxylase (ACC) inhibitors according to formula (I), or an enantiomer thereof, or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5, E, L, Z and n are as defined herein, to processes for preparing such compounds, to pharmaceutical compositions containing them, to the use of such inhibitors and to methods for their therapeutic use, particularly in the treatments of obesity and diabetes mellitus.

摘要翻译： 本发明涉及式（I）的乙酰辅酶A羧化酶（ACC）抑制剂或其对映异构体或其药学上可接受的盐，其中R1，R2，R3，R4，R5，E，L，Z和n 本文定义的方法，制备此类化合物的方法，含有它们的药物组合物，使用这些抑制剂及其治疗用途的方法，特别是在治疗肥胖症和糖尿病中。