公开(公告)号：US5767132A

公开(公告)日：1998-06-16

申请号：US543727

申请日：1995-10-16

申请人： Henning Bottcher ,  Ralf DeVant ,  Hartmut Greiner ,  Gerd Bartoszyk ,  Jean-Jacques Berthelon ,  Marc Noblet ,  Jean-Jacques Zeiller ,  Michel Brunet

发明人： Henning Bottcher ,  Ralf DeVant ,  Hartmut Greiner ,  Gerd Bartoszyk ,  Jean-Jacques Berthelon ,  Marc Noblet ,  Jean-Jacques Zeiller ,  Michel Brunet

IPC分类号： C07D213/36 ,  A61K31/00 ,  A61K31/135 ,  A61K31/18 ,  A61K31/195 ,  A61K31/24 ,  A61K31/275 ,  A61K31/353 ,  A61K31/38 ,  A61K31/381 ,  A61K31/44 ,  A61K31/4433 ,  A61P25/00 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  C07C211/00 ,  C07C217/16 ,  C07C217/20 ,  C07C217/58 ,  C07C255/54 ,  C07D213/38 ,  C07D213/53 ,  C07D311/58 ,  C07D311/64 ,  C07D333/20 ,  C07D405/12

CPC分类号： C07D405/12 ,  C07C217/16 ,  C07C217/20 ,  C07C255/54 ,  C07D213/38 ,  C07D311/58 ,  C07D311/64 ,  C07D333/20

摘要： Amino(thio)ether derivatives of formula I ##STR1## wherein R.sup.0, R.sup.1, R.sup.2, R.sup.3, R.sup.6, R.sup.7, R.sup.8, R.sup.9, X and Z are as defined herein, and their salts, are active on the central nervous system.

摘要翻译： 其中R0，R1，R2，R3，R6，R7，R8，R9，X和Z如本文所定义的式I的氨基（硫代）醚衍生物及其盐在中枢神经系统上具有活性。

公开(公告)号：US07323458B1

公开(公告)日：2008-01-29

申请号：US10019683

申请日：2000-07-04

申请人： Jean-Jacques Berthelon ,  Daniel Guerrier ,  Michel Brunet ,  Jean-Jacques Zeiller ,  Francis Contard ,  Fréderic Ausseil

发明人： Jean-Jacques Berthelon ,  Daniel Guerrier ,  Michel Brunet ,  Jean-Jacques Zeiller ,  Francis Contard ,  Fréderic Ausseil

IPC分类号： A61P7/00 ,  A61K31/55 ,  C07D243/04

CPC分类号： C07D401/12 ,  C07D243/04 ,  C07D405/12 ,  C07D413/12 ,  C07D487/04 ,  C07D513/04 ,  C07D513/14

摘要： The invention concerns a benzodiazepin derivative of formula (I) and their use for treating dyslipidemia, atherosclerosis, diabetes and its complications.

摘要翻译： 本发明涉及式（I）的苯并二氮杂衍生物及其用于治疗血脂异常，动脉粥样硬化，糖尿病及其并发症的用途。

公开(公告)号：US5652252A

公开(公告)日：1997-07-29

申请号：US460866

申请日：1995-06-05

申请人： Jean Jacques Berthelon ,  Michel Brunet ,  Marc Noblet ,  Philippe Durbin ,  Daniel Guerrier ,  Trong Nghia Luong

发明人： Jean Jacques Berthelon ,  Michel Brunet ,  Marc Noblet ,  Philippe Durbin ,  Daniel Guerrier ,  Trong Nghia Luong

IPC分类号： C07D215/14 ,  A61K31/355 ,  A61K31/55 ,  A61P9/08 ,  A61P9/10 ,  A61P11/00 ,  A61P11/08 ,  A61P17/00 ,  A61P21/02 ,  A61P25/02 ,  C07C57/30 ,  C07C59/68 ,  C07D213/24 ,  C07D213/30 ,  C07D213/57 ,  C07D213/60 ,  C07D213/89 ,  C07D313/08 ,  C07D405/04 ,  C07D409/04 ,  C07D493/04 ,  A61K31/44 ,  C07D213/04

CPC分类号： C07D213/30 ,  C07D213/57 ,  C07D213/89 ,  C07D405/04 ,  C07D409/04 ,  C07D493/04 ,  Y02P20/55

摘要： The subject of the invention is compounds of general formula: ##STR1## in which: X represents O or CHR,R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which are identical or different, represent a hydrogen atom or a C.sub.1 -C.sub.7 alkyl group, it being possible for R.sub.1 to additionally form a bond with R;R.sub.5 represents a hydrogen atom, a hydroxyl group or R.sub.5, taken together with R.sub.7, forms a bond or a>O; group;R.sub.6 represents a group of formula: ##STR2## in which R.sub.10 and R.sub.11, taken together with the carbon atom to which they are attached, form a nitrogenous heterocyclic group,and their N-oxides and pharmaceutically acceptable salts.These compounds are powerful activators of potassium channels.

摘要翻译： 本发明的主题是以下通式的化合物：其中：X表示O或CHR，R 1，R 2，R 3和R 4相同或不同，表示氢原子或C 1 -C 7烷基， R1可以另外与R形成键; R5代表氢原子，羟基或R5与R7一起形成键或a O; 组; R 6表示下式的基团：其中R 10和R 11与它们所连接的碳原子一起形成含氮杂环基，以及它们的N-氧化物和药学上可接受的盐。 这些化合物是钾通道的强大激活剂。

公开(公告)号：US20060167078A1

公开(公告)日：2006-07-27

申请号：US10539515

申请日：2003-11-27

申请人： Timo Heinrich ,  Henning Boettcher ,  Kai Schiemann ,  Geunter Holzemann ,  Christoph van Amsterdam ,  Gerd Bartoszyk ,  Hartmut Greiner ,  Christoph Seyfried ,  Michel Brunet ,  Jean Zeiller ,  Jean Berthelon

发明人： Timo Heinrich ,  Henning Boettcher ,  Kai Schiemann ,  Geunter Holzemann ,  Christoph van Amsterdam ,  Gerd Bartoszyk ,  Hartmut Greiner ,  Christoph Seyfried ,  Michel Brunet ,  Jean Zeiller ,  Jean Berthelon

IPC分类号： A61K31/405 ,  C07D407/02

CPC分类号： C07D405/12

摘要： Benzodioxepines of the formula (I) and physiologically tolerated salts and solvates thereof, in which R1, R2, R3, R4, A, B, a and b have the meanings indicated in claim 1, are ligands of the 5HT1A receptors and/or the 5HT4 receptors with simultaneously strong serotonin reuptake inhibition. They can be employed for the treatment and prophylaxis of various diseases.

摘要翻译： 式（I）的苯并二氧杂环庚烷及其生理上耐受的盐和溶剂合物，其中R 1，R 2，R 3，R SUP > 4，A，B，a和b具有权利要求1中所示的含义，是具有同时强烈的5-羟色胺再摄取抑制的5HT1A受体和/或5HT4受体的配体。 可用于治疗和预防各种疾病。

公开(公告)号：US07253202B2

公开(公告)日：2007-08-07

申请号：US10539515

申请日：2003-11-27

申请人： Timo Heinrich ,  Henning Böttcher ,  Kai Schiemann ,  Günter Hölzemann ,  Christoph van Amsterdam ,  Gerd Bartoszyk ,  Hartmut Greiner ,  Christoph Seyfried ,  Michel Brunet ,  Jean Zeiller ,  Jean Berthelon

发明人： Timo Heinrich ,  Henning Böttcher ,  Kai Schiemann ,  Günter Hölzemann ,  Christoph van Amsterdam ,  Gerd Bartoszyk ,  Hartmut Greiner ,  Christoph Seyfried ,  Michel Brunet ,  Jean Zeiller ,  Jean Berthelon

IPC分类号： C07D405/12 ,  A61K31/357 ,  A61K31/404

CPC分类号： C07D405/12

摘要： Benzodioxepines of the formula (I) and physiologically tolerated salts and solvates thereof, in which R1, R2, R3, R4, A, B, a and b have the meanings indicated in claim 1, are ligands of the 5HT1A receptors and/or the 5HT4 receptors with simultaneously strong serotonin reuptake inhibition. They can be employed for the treatment and prophylaxis of various diseases

摘要翻译： 式（I）的苯并二氧杂环庚烷及其生理上耐受的盐和溶剂合物，其中R 1，R 2，R 3，R SUP > 4，A，B，a和b具有权利要求1中所示的含义，是具有同时强烈的5-羟色胺再摄取抑制的5HT1A受体和/或5HT4受体的配体。 可用于治疗和预防各种疾病

公开(公告)号：US20060052447A1

公开(公告)日：2006-03-09

申请号：US10530022

申请日：2003-08-11

申请人： Michel Brunet ,  Jean-Jacques Zeiller ,  Gerard Ferrand ,  Yves Bonhomme

发明人： Michel Brunet ,  Jean-Jacques Zeiller ,  Gerard Ferrand ,  Yves Bonhomme

IPC分类号： C07C69/76 ,  A61K31/235 ,  A61K31/192

CPC分类号： C07C69/738 ,  C07C67/343

摘要： The invention relates to compounds of the formula I: and to the pharmaceutically acceptable salts thereof, to processes for the preparation of them and to pharmaceutical compositions comprising them, which are useful especially for the treatment and prevention of dyslipidaemia, atherosclerosis and diabetes.

摘要翻译： 本发明涉及式I化合物：

公开(公告)号：US07737176B2

公开(公告)日：2010-06-15

申请号：US10530022

申请日：2003-08-11

申请人： Michel Brunet ,  Jean-Jacques Zeiller ,  Gérard Ferrand ,  Yves Bonhomme

发明人： Michel Brunet ,  Jean-Jacques Zeiller ,  Gérard Ferrand ,  Yves Bonhomme

IPC分类号： A61K31/38 ,  A61K31/20 ,  C07C69/00 ,  C07C59/00

CPC分类号： C07C69/738 ,  C07C67/343

摘要： The invention relates to compounds of the formula I: and to the pharmaceutically acceptable salts thereof, to processes for the preparation of them and to pharmaceutical compositions comprising them, which are useful especially for the treatment and prevention of dyslipidaemia, atherosclerosis and diabetes.

摘要翻译： 本发明涉及式I化合物及其药学上可接受的盐，其制备方法和包含它们的药物组合物，其特别用于治疗和预防血脂障碍，动脉粥样硬化和糖尿病。

公开(公告)号：US07482484B2

公开(公告)日：2009-01-27

申请号：US10542028

申请日：2003-12-16

申请人： Nathalie Adje ,  Michel Brunet ,  Didier Roche ,  Jean-Jacques Zeiller ,  Stéphane Yvon ,  Valérie Guyard-Dangremont ,  Francis Contard ,  Daniel Guerrier ,  Gérard Ferrand ,  Yves Bonhomme

发明人： Nathalie Adje ,  Michel Brunet ,  Didier Roche ,  Jean-Jacques Zeiller ,  Stéphane Yvon ,  Valérie Guyard-Dangremont ,  Francis Contard ,  Daniel Guerrier ,  Gérard Ferrand ,  Yves Bonhomme

IPC分类号： C07C62/00 ,  C07C229/40 ,  C07C251/20

CPC分类号： C07C323/56 ,  C07C45/46 ,  C07C45/673 ,  C07C45/68 ,  C07C49/747 ,  C07C49/755 ,  C07C59/72 ,  C07C59/90 ,  C07C65/40 ,  C07C67/30 ,  C07C67/31 ,  C07C69/712 ,  C07C69/736 ,  C07C69/76 ,  C07C205/45 ,  C07C211/60 ,  C07C229/18 ,  C07C233/33 ,  C07C251/44 ,  C07C255/40 ,  C07C309/65 ,  C07C317/44 ,  C07C323/22 ,  C07C323/52 ,  C07C2602/08 ,  C07C2602/10 ,  C07C2602/42 ,  C07C47/575

摘要： Disclosed are Compounds of formula I And methods of use thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes.

摘要翻译： 公开了式I的化合物及其用于治疗血脂异常，动脉粥样硬化和糖尿病的方法。

公开(公告)号：US20060111445A1

公开(公告)日：2006-05-25

申请号：US10542028

申请日：2003-12-16

申请人： Nathalie Adje ,  Michel Brunet ,  Didier Roche ,  Jean-Jacques Zeiller ,  Stephane Yvon ,  Valerie Guyard-Dangremont ,  Francis Contard ,  Daniel Guerrier ,  Gerard Ferrand

发明人： Nathalie Adje ,  Michel Brunet ,  Didier Roche ,  Jean-Jacques Zeiller ,  Stephane Yvon ,  Valerie Guyard-Dangremont ,  Francis Contard ,  Daniel Guerrier ,  Gerard Ferrand

IPC分类号： A61K31/195 ,  A61K31/192 ,  C07C251/44 ,  C07C321/24

CPC分类号： C07C323/56 ,  C07C45/46 ,  C07C45/673 ,  C07C45/68 ,  C07C49/747 ,  C07C49/755 ,  C07C59/72 ,  C07C59/90 ,  C07C65/40 ,  C07C67/30 ,  C07C67/31 ,  C07C69/712 ,  C07C69/736 ,  C07C69/76 ,  C07C205/45 ,  C07C211/60 ,  C07C229/18 ,  C07C233/33 ,  C07C251/44 ,  C07C255/40 ,  C07C309/65 ,  C07C317/44 ,  C07C323/22 ,  C07C323/52 ,  C07C2602/08 ,  C07C2602/10 ,  C07C2602/42 ,  C07C47/575

摘要： The present invention relates to a compound of the formula ((I): in which: n is an integer chosen from 1, 2 and 3; Y represents O; N—OR9, in which R9 represents H or a saturated hydrocarbon-based aliphatic group; CR10R11, in which R10 and R11, which may be identical or different, represent H or a saturated hydrocarbon-based aliphatic group; R1 and R2, which may be identical or different, represent H or a saturated aliphatic hydrocarbon-based chain; or alternatively R1 and R2 together form an optionally substituted saturated aliphatic hydrocarbon-based chain; the radicals R3 and R4, which may be identical or different, take any of the is meanings given above for R1 and R2, or alternatively R1 and the group R4 borne by the carbon alpha to CR1R2 represent nothing and a double bond links the CR1R2 carbon to the alpha CR3R4 carbon; or alternatively one of the radicals R1 and R2 forms with one of the radicals R3 and R4 an optionally substituted saturated or unsaturated aliphatic hydrocarbon-based chain; one of the radicals R5 and R6 represents W, and the other represents Z which is chosen from a saturated or unsaturated aliphatic hydrocarbon-based radical; an optionally substituted, saturated, unsaturated and/or aromatic carbocyclic or heterocyclic radical; a radical -alk-Cy, in which alk represents an alkylene chain and Cy represents an optionally substituted saturated, unsaturated and/or aromatic heterocyclic or carbocyclic radical; W represents —XL-CO2R7; —X-L-Tet, in which X and L are as defined below and Tet represents optionally substituted tetrazole; in which L represents a saturated or unsaturated aliphatic hydrocarbon-based chain, which is optionally substituted and/or optionally interrupted by optionally substituted arylene; X represents O; NR8, in which R8 represents H; a saturated aliphatic hydrocarbon-based group; a group —CO—R′ or —SO2—R′, in which R′ takes any of the meanings given below for R7 with the exception of H; or R8 represents an optionally substituted aromatic carbocyclic group; or X represent S(O)m, in which m is chosen from 0, 1 and 2; R7 represents H; a saturated or unsaturated aliphatic hydrocarbon-based group; an optionally substituted, saturated, unsaturated and/or aromatic carbocyclic group; an optionally substituted, saturated, unsaturated and/or aromatic heterocyclic group; and the pharmaceutically acceptable derivatives, salts, solvates and stereoisomers thereof, and also mixtures thereof in all proportions, which can be used in the treatment of dyslipidaemia, atherosclerosis and diabetes.

公开(公告)号：US5602152A

公开(公告)日：1997-02-11

申请号：US284454

申请日：1994-08-05

申请人： Jean J. Berthelon ,  Michel Brunet ,  Marc Noblet ,  Philippe Durbin ,  Daniel Guerrier ,  Trong N. Luong

发明人： Jean J. Berthelon ,  Michel Brunet ,  Marc Noblet ,  Philippe Durbin ,  Daniel Guerrier ,  Trong N. Luong

IPC分类号： C07D215/14 ,  A61K31/355 ,  A61K31/55 ,  A61P9/08 ,  A61P9/10 ,  A61P11/00 ,  A61P11/08 ,  A61P17/00 ,  A61P21/02 ,  A61P25/02 ,  C07C57/30 ,  C07C59/68 ,  C07D213/24 ,  C07D213/30 ,  C07D213/57 ,  C07D213/60 ,  C07D213/89 ,  C07D313/08 ,  C07D405/04 ,  C07D409/04 ,  C07D493/04 ,  A61K31/44

CPC分类号： C07D213/30 ,  C07D213/57 ,  C07D213/89 ,  C07D405/04 ,  C07D409/04 ,  C07D493/04 ,  Y02P20/55

摘要： The subject of the invention is compounds of general formula: ##STR1## in which: X represents O or CHR,R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which are identical or different, represent a hydrogen atom or a C.sub.1 -C.sub.7 alkyl group, it being possible for R.sub.1 to additionally form a bond with R;R.sub.5 represents a hydrogen atom, a hydroxyl group or R.sub.5, taken together with R.sub.7, forms a bond or a >O; group;R.sub.6 represents a group of formula: ##STR2## in which R.sub.10 and R.sub.11, taken together with the carbon atom to which they are attached, form a nitrogenous heterocyclic group, and their N-oxides and pharmaceutically acceptable salts. These compounds are powerful activators of potassium channels.

摘要翻译： PCT No.PCT / EP93 / 03445 371日期：1994年8月5日 102（e）日期1994年8月5日PCT 1993年12月7日PCT公布。 公开号WO94 / 13658 日期1994年6月23日本发明的主题是以下通式的化合物：其中：X表示O或CHR，R1，R2，R3和R4相同或不同，表示氢原子或C1 -C 7烷基，R1可以另外与R形成键; R5代表氢原子，羟基或R5与R7一起形成键或a O; 组; R 6表示下式的基团：其中R 10和R 11与它们所连接的碳原子一起形成含氮杂环基，以及它们的N-氧化物和药学上可接受的盐。 这些化合物是钾通道的强大激活剂。