公开(公告)号：US20110152236A1

公开(公告)日：2011-06-23

申请号：US13058913

申请日：2009-08-13

申请人： Patrick Bernardelli ,  Jean-Francois Sabuco ,  Corinne Terrier

发明人： Patrick Bernardelli ,  Jean-Francois Sabuco ,  Corinne Terrier

IPC分类号： A61K31/427 ,  C07D417/12 ,  C07D403/12 ,  C07D413/12 ,  C07D401/12 ,  A61K31/4178 ,  A61K31/433 ,  A61K31/422 ,  A61K31/4427 ,  A61K31/506 ,  A61K31/4155 ,  A61K31/4245 ,  A61K31/4196 ,  A61K31/41 ,  A61K31/497 ,  A61P25/30 ,  A61P25/34 ,  A61P25/00 ,  A61P25/28 ,  A61P3/00 ,  A61P3/10 ,  A61P3/04 ,  A61P3/06 ,  A61P25/20 ,  A61P25/04 ,  A61P1/08 ,  A61P1/04 ,  A61P1/00 ,  A61P1/12 ,  A61P9/00 ,  A61P5/00 ,  A61P7/00 ,  A61P1/16 ,  A61P37/02 ,  A61P29/00 ,  A61P25/16 ,  A61P25/18 ,  A61P11/06 ,  A61P11/00 ,  A61P27/06 ,  A61P15/00 ,  A61P31/00 ,  A61P31/12 ,  A61P35/00 ,  A61P19/10

CPC分类号： C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12

摘要： The invention relates to compounds of the formula (I) where: R is a (C1-C6)alkyl group, a halo(C1-C6)alkyl group; R1 is a hydrogen atom; R2 is a heteroaromatic group or a heteroaromatic(C1-C4)alkyl group, said groups being optionally substituted; R3 and R4 represent independently from each other an optionally substituted phenyl group; Y is a hydrogen atom, a halogen, a cyano, a (C1-C6)alkyl group, a halo(C1-C6)alkyl group, a (C1-C6)alkoxy group, a halo(C1-C6)alkoxy group or a (C1-C6)alkylS(O)p group; and p is 0 to 2. Said compounds can be in the form— of a base or a salt for addition to an acid. The invention also relates to a method for preparing same and to the therapeutic application thereof.

摘要翻译： 本发明涉及式（I）的化合物，其中：R为（C 1 -C 6）烷基，卤代（C 1 -C 6）烷基; R1是氢原子; R2是杂芳基或杂芳族（C1-C4）烷基，所述基团任选被取代; R3和R4彼此独立地表示任选取代的苯基; Y是氢原子，卤素，氰基，（C1-C6）烷基，卤代（C1-C6）烷基，（C1-C6）烷氧基，卤代（C1-C6）烷氧基或 （C 1 -C 6）烷基S（O）p基团; 并且p为0至2.所述化合物可以为碱或盐的形式，以加入酸中。 本发明还涉及其制备方法及其治疗应用。

公开(公告)号：US20080262052A1

公开(公告)日：2008-10-23

申请号：US12133408

申请日：2008-06-05

申请人： Stefanie KEIL ,  Wolfgang Wendler ,  Maike Glien ,  Jochen Goerlitzer ,  Karen Chandross ,  Daniel G. McGarry ,  Jean Merrill ,  Patrick Bernardelli ,  Baptiste Ronan ,  Corinne Terrier

发明人： Stefanie KEIL ,  Wolfgang Wendler ,  Maike Glien ,  Jochen Goerlitzer ,  Karen Chandross ,  Daniel G. McGarry ,  Jean Merrill ,  Patrick Bernardelli ,  Baptiste Ronan ,  Corinne Terrier

IPC分类号： A61K31/4245 ,  C07D271/06 ,  A61P3/10 ,  A61P25/28

CPC分类号： C07D417/12 ,  C07D413/12

摘要： The invention relates to oxadiazolones and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta agonist activity.What is described are compounds of the formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved; neurodegenerative diseases and/or de-myelinating disorders of the central and peripheral nervous systems and/or neurological diseases involving neuro-inflammatory processes and/or other peripheral neuropathies.

摘要翻译： 本发明涉及恶二唑酮及其生理上可接受的盐和生理功能衍生物，显示出PPARδ激动剂活性。 所描述的是式I化合物，其中自由基如所定义，以及它们的生理上可接受的盐及其制备方法。 该化合物适用于治疗和/或预防脂肪酸代谢紊乱和葡萄糖利用障碍以及涉及胰岛素抵抗的疾病; 神经变性疾病和/或中枢和周围神经系统的脱髓鞘疾病和/或涉及神经炎症过程和/或其它周围神经病变的神经疾病。

公开(公告)号：US07851493B2

公开(公告)日：2010-12-14

申请号：US12474838

申请日：2009-05-29

申请人： Patrick Bernardelli ,  Stefanie Keil ,  Matthias Urmann ,  Hans Matter ,  Wolfgang Wendler ,  Maike Glien ,  Karen Chandross ,  Lan Lee ,  Corinne Terrier ,  Herve Minoux

发明人： Patrick Bernardelli ,  Stefanie Keil ,  Matthias Urmann ,  Hans Matter ,  Wolfgang Wendler ,  Maike Glien ,  Karen Chandross ,  Lan Lee ,  Corinne Terrier ,  Herve Minoux

IPC分类号： A61K31/4245 ,  C07D271/113

CPC分类号： C07D417/14 ,  C07D277/24 ,  C07D417/12

摘要： The invention relates to phenyl-1,2,4-oxadiazolone derivatives with phenyl group and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta agonist activity.What are described are compounds of the formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.

摘要翻译： 本发明涉及具有苯基的苯基-1,2,4-恶二唑酮衍生物及其生理上可接受的盐和生理功能衍生物，显示出PPARδ激动剂活性。 描述的是式I化合物，其中基团如所定义，以及它们的生理上可接受的盐及其制备方法。 该化合物适用于治疗和/或预防脂肪酸代谢紊乱和葡萄糖利用障碍以及其中涉及胰岛素抵抗和中枢神经和周围神经系统的脱髓鞘和其它神经变性疾病的疾病。

公开(公告)号：US20110183961A1

公开(公告)日：2011-07-28

申请号：US13058885

申请日：2009-08-13

申请人： Florian Auger ,  Patrick Bernardelli ,  Jean-François Sabuco ,  Corinne Terrier

发明人： Florian Auger ,  Patrick Bernardelli ,  Jean-François Sabuco ,  Corinne Terrier

IPC分类号： A61K31/397 ,  C07D403/12 ,  A61K31/4025 ,  C07D409/12 ,  C07D401/12 ,  A61K31/4523 ,  A61K31/4178 ,  A61P25/04 ,  A61P31/12 ,  A61P19/00 ,  A61P11/00 ,  A61P35/00 ,  A61P9/00 ,  A61P3/00

CPC分类号： C07D401/12 ,  C07D403/12 ,  C07D409/12

摘要： The invention relates to compounds of the formula (I) where: R is a (C1-C6)alkyl group, a halo(C1-C6)alkyl group; R1 is a hydrogen atom; R2 is a heterocyclic group bound by a carbon atom, a heterocyclic-(C1-C4)alkyl group, said groups being optionally substituted; R3 and R4 represent independently from each other an optionally substituted phenyl group; X is a hydrogen atom, a halogen, a cyano, a (C1-C6)alkyl group, a halo(C1-C6)alkyl group, a (C1-C6)alkoxy group, a halo(C1-C6)alkoxy group or a (C1-C6)alkylS(0)p group; and p is 0 to 2. The invention also relates to a method for preparing same and to the therapeutic application thereof.

摘要翻译： 本发明涉及式（I）的化合物，其中：R为（C 1 -C 6）烷基，卤代（C 1 -C 6）烷基; R1是氢原子; R2是由碳原子键合的杂环基，杂环 - （C1-C4）烷基，所述基团任选被取代; R3和R4彼此独立地表示任选取代的苯基; X是氢原子，卤素，氰基，（C1-C6）烷基，卤代（C1-C6）烷基，（C1-C6）烷氧基，卤代（C1-C6）烷氧基或 （C 1 -C 6）烷基S（O）p基团; 并且p为0至2.本发明还涉及其制备方法及其治疗应用。

公开(公告)号：US20090281084A1

公开(公告)日：2009-11-12

申请号：US12474838

申请日：2009-05-29

申请人： Patrick Bernardelli ,  Stefanie Keil ,  Matthias Urmann ,  Hans Matter ,  Wolfgang Wendler ,  Maike Glien ,  Karen Chandross ,  Lan Lee ,  Corinne Terrier ,  Herve Minoux

发明人： Patrick Bernardelli ,  Stefanie Keil ,  Matthias Urmann ,  Hans Matter ,  Wolfgang Wendler ,  Maike Glien ,  Karen Chandross ,  Lan Lee ,  Corinne Terrier ,  Herve Minoux

IPC分类号： A61K31/55 ,  A61K31/541 ,  A61K31/5377 ,  A61K31/454 ,  A61K31/427 ,  A61K31/426 ,  C07D415/00 ,  C07D277/22

CPC分类号： C07D417/14 ,  C07D277/24 ,  C07D417/12

摘要： The invention relates to phenyl-1,2,4-oxadiazolone derivatives with phenyl group and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta agonist activity.What are described are compounds of the formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.

摘要翻译： 本发明涉及具有苯基的苯基-1,2,4-恶二唑酮衍生物及其生理上可接受的盐和生理功能衍生物，显示出PPARδ激动剂活性。 描述的是式I化合物，其中基团如所定义，以及它们的生理上可接受的盐及其制备方法。 该化合物适用于治疗和/或预防脂肪酸代谢紊乱和葡萄糖利用障碍以及其中涉及胰岛素抵抗和中枢神经和周围神经系统的脱髓鞘和其它神经变性疾病的疾病。

公开(公告)号：US20080287409A1

公开(公告)日：2008-11-20

申请号：US12055793

申请日：2008-03-26

申请人： Patrick Bernardelli ,  Stefanie Keil ,  Matthias Urmann ,  Hans Matter ,  Wolfgang Wendler ,  Maike Glien ,  Karen Chandross ,  Lan Lee ,  Corinne Terrier ,  Herve Minoux

发明人： Patrick Bernardelli ,  Stefanie Keil ,  Matthias Urmann ,  Hans Matter ,  Wolfgang Wendler ,  Maike Glien ,  Karen Chandross ,  Lan Lee ,  Corinne Terrier ,  Herve Minoux

IPC分类号： A61K31/427 ,  A61K31/454 ,  C07D413/14 ,  C07D417/14 ,  A61P3/10 ,  A61P3/00 ,  A61K31/5377 ,  C07D417/12

CPC分类号： C07D417/14 ,  C07D277/24 ,  C07D417/12

摘要： The present invention comprises phenyl and pyridinyl 1,2,4-oxadiazolone compounds their physiologically acceptable salts and physiologically functional derivatives that exhibit peroxisome proliferator activator receptor (PPAR) delta agonist activity. Also described and claimed are processes for their preparation and their use as pharmaceuticals. These are compounds of formula I, in which the R-group substituents are defined herein. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and de-myelinating and other neurodegenerative disorders of the central and peripheral nervous system.

摘要翻译： 本发明包括苯基和吡啶基-1,2,4-恶二唑酮化合物，其生理上可接受的盐和生理功能衍生物显示出过氧化物酶体增殖物激活受体（PPAR）δ激动剂活性。 还描述和要求保护的是其制备方法及其作为药物的用途。 这些是式I化合物，其中R基团取代基在本文中定义。 所述化合物适用于治疗和/或预防脂肪酸代谢紊乱和葡萄糖利用障碍以及涉及胰岛素抵抗的疾病以及中枢和周围神经系统的脱髓鞘和其它神经变性疾病。

公开(公告)号：US07709509B2

公开(公告)日：2010-05-04

申请号：US12133405

申请日：2008-06-05

申请人： Stefanie Keil ,  Wolfgang Wendler ,  Maike Glien ,  Jochen Goerlitzer ,  Karen Chandross ,  Daniel G. McGarry ,  Jean Merrill ,  Patrick Bernardelli ,  Baptiste Ronan ,  Corinne Terrier

发明人： Stefanie Keil ,  Wolfgang Wendler ,  Maike Glien ,  Jochen Goerlitzer ,  Karen Chandross ,  Daniel G. McGarry ,  Jean Merrill ,  Patrick Bernardelli ,  Baptiste Ronan ,  Corinne Terrier

IPC分类号： A61K31/4245 ,  A61K31/422 ,  A61K31/427 ,  C07D277/20 ,  C07D271/07 ,  C07D263/30

CPC分类号： C07D417/12 ,  C07D413/12

摘要： The invention relates to oxadiazolones and to their physiologically acceptable salts and physiologically functional derivatives showing peroxisome proliferator activator receptor (PPAR) delta agonist activity comprising compounds of formula I, in which the R1-R7 substituents as well as the U, V, W, X Y and z radicals are as defined herein, and their physiologically acceptable salts and processes for their preparation. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved; neurodegenerative diseases and/or demyelinating disorders of the central and peripheral nervous systems and/or neurological diseases involving neuro-inflammatory processes and/or other peripheral neuropathies.

摘要翻译： 本发明涉及恶二唑酮及其生理上可接受的盐和生理功能性衍生物，其显示包含式I化合物的过氧化物酶体增殖物激活剂受体（PPAR）δ激动剂活性，其中R 1 -R 7取代基以及U，V，W，XY 和z基团如本文所定义，以及它们的生理上可接受的盐及其制备方法。 该化合物适用于治疗和/或预防脂肪酸代谢紊乱和葡萄糖利用障碍以及涉及胰岛素抵抗的疾病; 中枢和周围神经系统的神经变性疾病和/或脱髓鞘疾病和/或涉及神经炎症过程和/或其它周围神经病变的神经疾病。

公开(公告)号：US07541464B2

公开(公告)日：2009-06-02

申请号：US11681923

申请日：2007-03-05

申请人： Stefanie Keil ,  Maike Glien ,  Hans-Ludwig Schaefer ,  Wolfgang Wendler ,  Patrick Bernardelli ,  Corinne Terrier ,  Baptiste Ronan

发明人： Stefanie Keil ,  Maike Glien ,  Hans-Ludwig Schaefer ,  Wolfgang Wendler ,  Patrick Bernardelli ,  Corinne Terrier ,  Baptiste Ronan

IPC分类号： C07D471/00 ,  C07D471/02 ,  A61K31/01 ,  A61K31/03 ,  A01N47/00 ,  A61K31/015 ,  A61K31/02 ,  A61K31/025

CPC分类号： C07D471/04

摘要： The present invention relates generally to compounds and compositions for the treatment of metabolic diseases and specifically, the present invention relates to compounds that therapeutically modulation and control lipid and/or carbohydrate metabolism and are thus suitable for the prevention and/or treatment of diseases such as type 2 diabetes, atherosclerosis, and the diverse manifestations thereof. The present invention relates to 7-azaindoles, their physiologically acceptable salts and functional derivatives thereof that exhibit a high degree of peroxisome proliferator-activated receptors (PPAR) agonist activity. Compounds of the present invention are described by formula I: in which the R-groups are herein defined, together with their pharmaceutically acceptable salts, therapeutic methods for their use and processes for their preparation. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved.

摘要翻译： 本发明一般涉及用于治疗代谢疾病的化合物和组合物，具体而言，本发明涉及治疗性调节和控制脂质和/或碳水化合物代谢并因此适合于预防和/或治疗疾病如 2型糖尿病，动脉粥样硬化及其多种表现。 本发明涉及显示出高度过氧化物酶体增殖物激活受体（PPAR）激动剂活性的7-氮杂吲哚，它们的生理上可接受的盐和功能衍生物。 本发明的化合物由式I描述：其中本文定义R基团及其药学上可接受的盐，其用途的治疗方法及其制备方法。 该化合物适用于治疗和/或预防脂肪酸代谢紊乱和葡萄糖利用障碍以及涉及胰岛素抵抗的疾病。

公开(公告)号：US20080255212A1

公开(公告)日：2008-10-16

申请号：US12133405

申请日：2008-06-05

申请人： Stefanie KEIL ,  Wolfgang Wendler ,  Maike Glien ,  Jochen Goerlitzer ,  Karen Chandross ,  Danie G. McGarry ,  Jean Merrill ,  Patrick Bernardelli ,  Baptiste Ronan ,  Corinne Terrier

发明人： Stefanie KEIL ,  Wolfgang Wendler ,  Maike Glien ,  Jochen Goerlitzer ,  Karen Chandross ,  Danie G. McGarry ,  Jean Merrill ,  Patrick Bernardelli ,  Baptiste Ronan ,  Corinne Terrier

IPC分类号： A61K31/4245 ,  C07D271/07 ,  A61P3/00

CPC分类号： C07D417/12 ,  C07D413/12

摘要： The invention relates to oxadiazolones and to their physiologically acceptable salts and physiologically functional derivatives showing peroxisome proliferator activator receptor (PPAR) delta agonist activity comprising compounds of formula I, in which the R1-R7 substituents as well as the U, V, W, X Y and z radicals are as defined herein, and their physiologically acceptable salts and processes for their preparation. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved; neurodegenerative diseases and/or de-myelinating disorders of the central and peripheral nervous systems and/or neurological diseases involving neuro-inflammatory processes and/or other peripheral neuropathies.

摘要翻译： 本发明涉及恶二唑酮及其生理上可接受的盐和生理功能性衍生物，其显示包含式I化合物的过氧化物酶体增殖物激活剂受体（PPAR）δ激动剂活性，其中R 1 -R 7取代基以及U，V，W，XY 和z基团如本文所定义，以及它们的生理上可接受的盐及其制备方法。 该化合物适用于治疗和/或预防脂肪酸代谢紊乱和葡萄糖利用障碍以及涉及胰岛素抵抗的疾病; 神经变性疾病和/或中枢和周围神经系统的脱髓鞘疾病和/或涉及神经炎症过程和/或其它周围神经病变的神经疾病。

公开(公告)号：US07214676B2

公开(公告)日：2007-05-08

申请号：US10852404

申请日：2004-05-24

申请人： Patrick Bernardelli ,  Pierre Ducrot ,  Edwige Lorthiois ,  Febrice Vergne

发明人： Patrick Bernardelli ,  Pierre Ducrot ,  Edwige Lorthiois ,  Febrice Vergne

IPC分类号： A61K31/535 ,  A61K31/497 ,  A61K31/517 ,  C07D273/01

CPC分类号： C07D239/70 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D405/12 ,  C07D413/12

摘要： The invention provides compounds which are PDE7 inhibitors, having the following formula (I), (II) and (III) in which X1, X2, X3, X4, X, Y, Z, A and Z1 are as defined in the description, methods for preparing them and their use for the treatment of disorders for which therapy by a PDE7 inhibitor is relevant.

摘要翻译： 本发明提供了具有下列式（I），（II）和（III）的PDE7抑制剂的化合物，其中X 1，X 2，X 3， 3 X，X 4，X，Y，Z，A和Z 1如说明书中所定义，其制备方法及其用于治疗的方法 的PDE7抑制剂治疗相关的疾病。