公开(公告)号：US20050107389A1

公开(公告)日：2005-05-19

申请号：US10960399

申请日：2004-10-07

Applicant: James Hendrix ,  Joseph Strupczeski ,  Kenneth Bordeau ,  Matthias Urmann ,  Gregory Shutske ,  Horst Hemmerle ,  John Jurcak ,  Harpal Gill ,  Franz Weiberth ,  Thaddeus Nieduzak ,  Sharon Jackson ,  Xu-Yang Zhao ,  Paul Mueller

Inventor： James Hendrix ,  Joseph Strupczeski ,  Kenneth Bordeau ,  Matthias Urmann ,  Gregory Shutske ,  Horst Hemmerle ,  John Jurcak ,  Harpal Gill ,  Franz Weiberth ,  Thaddeus Nieduzak ,  Sharon Jackson ,  Xu-Yang Zhao ,  Paul Mueller

IPC: A61K31/33 ,  C07D333/58 ,  C07D333/66 ,  C07D333/68 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D451/02 ,  C07D471/04 ,  C07D495/04 ,  C07D498/04 ,  C07D521/00 ,  C07D471/02 ,  A61K31/4745 ,  A61K31/503 ,  C07D487/04

CPC classification number: A61K31/33 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D333/58 ,  C07D333/66 ,  C07D333/68 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D451/02 ,  C07D471/04 ,  C07D495/04

Abstract: The invention relates to heterocyclic substituted amide derivatives that display selective binding to dopamine D3 receptors. In another aspect, the invention relates to a method for treating central nervous system disorders associated with the dopamine D3 receptor activity in a patient in need of such treatment comprising administering to the subject a therapeutically effective amount of said compounds for alleviation of such disorder. The central nervous system disorders that may be treated with these compounds include Psychotic Disorders, Substance Dependence, Substance Abuse, Dyskinetic Disorders (e.g. Parkinson's Disease, Parkinsonism, Neuroleptic-Induced Tardive Dyskinesia, Gilles de la Tourette Syndrome and Huntington's Disease), Dementia, Anxiety Disorders, Sleep Disorders, Circadian Rhythm Disorders and Mood Disorders. The subject invention is also directed towards processes for the preparation of the compounds described herein as well as methods for making and using the compounds as imaging agents for dopamine D3 receptors.

Abstract translation: 本发明涉及显示与多巴胺D 3受体的选择性结合的杂环取代的酰胺衍生物。 另一方面，本发明涉及在需要这种治疗的患者中治疗与多巴胺D 3 N 3受体活性相关的中枢神经系统障碍的方法，包括向所述受试者施用治疗有效量的所述 用于缓解这种病症的化合物。 可能用这些化合物治疗的中枢神经系统疾病包括心理障碍，物质依赖性，物质滥用，运动障碍（例如帕金森病，帕金森综合征，神经灵敏诱导的迟发性运动障碍，杜氏综合征和亨廷顿疾病），痴呆，焦虑 疾病，睡眠障碍，昼夜节律紊乱和情绪障碍。 本发明还涉及制备本文所述化合物的方法以及制备和使用化合物作为多巴胺D 3受体的显像剂的方法。

公开(公告)号：US08946212B2

公开(公告)日：2015-02-03

申请号：US12996692

申请日：2009-05-22

Applicant: Stefanie Keil ,  Matthias Urmann ,  Maike Glien ,  Hans Matter ,  Eugen Falk ,  Ulrike Wendler

Inventor： Stefanie Keil ,  Matthias Urmann ,  Wolfgang Wendler ,  Maike Glien ,  Hans Matter ,  Eugen Falk

IPC: A61K31/538 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/10 ,  C07D471/04 ,  C07D498/04

CPC classification number: C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/10 ,  C07D471/04 ,  C07D498/04

Abstract: Annelated N-heterocyclic sulfonamides with oxadiazolone headgroup, processes for their preparation and their use as pharmaceuticals The invention relates to annelated N-heterocyclic sulfonamides with oxadiazolone headgroup and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARalpha 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 and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.

Abstract translation: 具有恶二唑酮头基的神经化N-杂环磺酰胺，其制备方法及其作为药物的用途本发明涉及具有恶二唑酮头基的环状N-杂环磺酰胺及其生理学上可接受的盐和生理功能衍生物，其显示PPARδ或PPARα和PPARα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：US08748483B2

公开(公告)日：2014-06-10

申请号：US12504198

申请日：2009-07-16

Applicant: Harm Brummerhop ,  Siegfried Stengelin ,  Hubert Heuer ,  Susanne Kilp ,  Andreas Herling ,  Thomas Klabunde ,  Dieter Kadereit ,  Matthias Urmann

Inventor： Harm Brummerhop ,  Siegfried Stengelin ,  Hubert Heuer ,  Susanne Kilp ,  Andreas Herling ,  Thomas Klabunde ,  Dieter Kadereit ,  Matthias Urmann

IPC: A01N43/16 ,  A61K31/35 ,  C09B3/00 ,  C07D209/80 ,  C09B7/00

CPC classification number: A61K31/351

Abstract: The invention relates to the use of substituted pyranone acid derivatives and of their physiologically acceptable salts for producing medicaments for treating the metabolic syndrome.

Abstract translation: 本发明涉及取代的吡喃酮酸衍生物及其生理学上可接受的盐用于制备用于治疗代谢综合征的药物的用途。

公开(公告)号：US08173674B2

公开(公告)日：2012-05-08

申请号：US12480974

申请日：2009-06-09

Applicant: Stefanie Keil ,  Matthias Urmann ,  Karl Schoenafinger ,  Wolfgang Wendler ,  Maike Glien ,  Hans-Ludwig Schaefer ,  Eugen Falk

Inventor： Stefanie Keil ,  Matthias Urmann ,  Karl Schoenafinger ,  Wolfgang Wendler ,  Maike Glien ,  Hans-Ludwig Schaefer ,  Eugen Falk

IPC: C07D401/02 ,  A61K31/47

CPC classification number: C07D413/12

Abstract: The invention relates to sulfonyl-phenyl-oxadiazolones and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARgamma 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.

Abstract translation: 本发明涉及磺酰基 - 苯基 - 恶二唑酮及其生理上可接受的盐和生理功能衍生物，其显示PPARδ或PPARδ和PPARγ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：US20100261909A1

公开(公告)日：2010-10-14

申请号：US12644401

申请日：2009-12-22

Applicant: Jorge ALONSO ,  Andreas LINDENSCHMIDT ,  Marc NAZARÉ ,  Matthias URMANN ,  Nis HALLAND ,  Omar RKYEK

Inventor： Jorge ALONSO ,  Andreas LINDENSCHMIDT ,  Marc NAZARÉ ,  Matthias URMANN ,  Nis HALLAND ,  Omar RKYEK

IPC: C07D471/04 ,  C07D235/08 ,  C07D401/04

CPC classification number: C07D235/08 ,  C07D235/16 ,  C07D235/18 ,  C07D401/04 ,  C07D471/04

Abstract: The present invention relates to a process for the regioselective synthesis of compounds of the formula I, wherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4, Q and J have the meanings indicated in the claims. The present invention provides a direct copper catalyzed regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides.

Abstract translation: 本发明涉及一种用于区域选择性合成式I化合物的方法，其中R 0; R1; R2; R3; R4; R5; A1; A2; A3; A4，Q和J具有权利要求中所示的含义。 本发明提供了从2-卤代 - 硝基芳烃和N-取代的酰胺开始的多种不同的式（I）的非对称，多官能的N-取代的苯并咪唑或氮杂苯并咪唑的直接铜催化的区域选择性方法。

公开(公告)号：US20100261900A1

公开(公告)日：2010-10-14

申请号：US12645508

申请日：2009-12-23

Applicant: Omar RKYEK ,  Marc NAZARE ,  Andreas LINDENSCHMIDT ,  Jorge ALONSO ,  Matthias URMANN ,  Nis HALLAND

Inventor： Omar RKYEK ,  Marc NAZARE ,  Andreas LINDENSCHMIDT ,  Jorge ALONSO ,  Matthias URMANN ,  Nis HALLAND

IPC: C07D239/26 ,  C07D231/12 ,  C07D409/06 ,  C07D333/38 ,  C07D231/56 ,  C07D471/04 ,  C07D213/16 ,  C07D213/30 ,  C07D213/26 ,  C07D215/14

CPC classification number: C07D231/12 ,  C07D213/127 ,  C07D213/26 ,  C07D213/30 ,  C07D215/12 ,  C07D215/14 ,  C07D231/56 ,  C07D239/26 ,  C07D333/38 ,  C07D409/06 ,  C07D471/04

Abstract: A process for the palladium-catalyzed coupling of terminal alkynes with heteroaryl tosylates and heteroaryl benzenesulfonatesThe present invention relates to a process for the regioselective synthesis of compounds of the formula (I), wherein D, J and W have the meanings indicated in the claims. The present invention provides an efficient and general palladium-catalyzed coupling process of heteroaryl tosylates with terminal alkynes to a wide variety of substituted, multifunctional heteroaryl-1-alkynes of the formula I.

Abstract translation: 末端炔烃与杂芳基甲苯磺酸酯和杂芳基苯磺酸盐的钯催化偶合的方法本发明涉及式（I）化合物的区域选择性合成方法，其中D，J和W具有权利要求书中所示的含义 。 本发明提供了一种有效且一般的钯催化的杂芳基甲苯磺酸酯与末端炔烃与多种式I的取代的多官能杂芳基-1-炔烃的偶联方法。

公开(公告)号：US20090298871A1

公开(公告)日：2009-12-03

申请号：US12480974

申请日：2009-06-09

Applicant: Stefanie KEIL ,  Matthias URMANN ,  Karl SCHOENAFINGER ,  Wolfgang WENDLER ,  Maike GLIEN ,  Hans-Ludwig SCHAEFER ,  Eugen FALK

Inventor： Stefanie KEIL ,  Matthias URMANN ,  Karl SCHOENAFINGER ,  Wolfgang WENDLER ,  Maike GLIEN ,  Hans-Ludwig SCHAEFER ,  Eugen FALK

IPC: A61K31/4725 ,  C07D413/12 ,  A61K31/4245

CPC classification number: C07D413/12

Abstract: The invention relates to sulfonyl-phenyl-oxadiazolones and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARgamma 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.

Abstract translation: 本发明涉及磺酰基 - 苯基 - 恶二唑酮及其生理上可接受的盐和生理功能衍生物，其显示PPARδ或PPARδ和PPARγ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：US20080293780A1

公开(公告)日：2008-11-27

申请号：US12062759

申请日：2008-04-04

Applicant: Karl SCHOENAFINGER ,  Stefanie KEIL ,  Matthias URMANN ,  Hans MATTER ,  Maike GLIEN ,  Wolfgang WENDLER

Inventor： Karl SCHOENAFINGER ,  Stefanie KEIL ,  Matthias URMANN ,  Hans MATTER ,  Maike GLIEN ,  Wolfgang WENDLER

IPC: A61K31/41 ,  C07D285/08 ,  A61P3/10

CPC classification number: C07D417/12 ,  C07D285/135

Abstract: The present invention comprises bicyclic aryl-sulfonic acid [1,3,4]-thiadiazol-2-yl-amides, their functional derivatives thereof as well as their physiologically acceptable salts and pharmaceutical compositions thereof that exhibit peroxisome proliferator activated receptor (PPAR) PPARdelta and PPARgamma agonist activity. The structure of the compounds of the invention are defined by Formula I below, wherein the various substituents are defined herein, including their physiologically acceptable salts. Processes for the compounds preparation are also disclosed. The compounds are suitable for the treatment of fatty acid metabolism and glucose utilization disorders, disorders relating to insulin resistance are involved as well as demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.

Abstract translation: 本发明包括双环芳基磺酸[1,3,4] - 噻二唑-2-基 - 酰胺，它们的功能衍生物及其生理上可接受的盐和药物组合物，其表现出过氧化物酶体增殖物激活受体（PPAR）PPARδ 和PPARγ激动剂活性。 本发明化合物的结构由下式I定义，其中各种取代基在本文中定义，包括其生理上可接受的盐。 还公开了化合物制备的方法。 该化合物适用于治疗脂肪酸代谢和葡萄糖利用障碍，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他神经变性疾病。

公开(公告)号：US20080280946A1

公开(公告)日：2008-11-13

申请号：US11934177

申请日：2007-11-02

Applicant: Marc NAZARE ,  Volkmar Wehner ,  David William Will ,  Kurt Ritter ,  Matthias Urmann ,  Hans Matter

Inventor： Marc NAZARE ,  Volkmar Wehner ,  David William Will ,  Kurt Ritter ,  Matthias Urmann ,  Hans Matter

IPC: A61K31/437 ,  C07D471/02 ,  A61P7/00 ,  A61P9/00

CPC classification number: C07D471/04

Abstract: Indazole-derivatives as factor Xa inhibitors The present invention relates to compounds of the formula I wherein R0, R1, R2, R3, Q, V, G and M are as defined herein. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

Abstract translation: 作为因子Xa抑制剂的吲唑衍生物本发明涉及式I化合物，其中R 0，R 1，R 2，R 2， SEQ ID NO 3，Q，V，G和M如本文所定义。 式I的化合物是有价值的药理活性化合物。 它们具有强烈的抗血栓形成作用，并且适用于例如治疗和预防心血管疾病如血栓栓塞性疾病或再狭窄。 它们是血液凝固酶因子Xa（FXa）和/或因子VIIa（FVIIa）的可逆抑制剂，并且通常可用于存在因子Xa和/或因子VIa的不期望活性或用于治愈 或预防因子Xa和/或因子VIIa的抑制。 本发明还涉及式I化合物的制备方法，其用途，特别是作为药物中的活性成分，以及包含它们的药物制剂。

公开(公告)号：US20070161641A1

公开(公告)日：2007-07-12

申请号：US11714047

申请日：2007-03-05

Applicant: James Hendrix ,  Horst Hemmerle ,  Matthias Urmann ,  Gregory Shutske ,  Joseph Strupczewski ,  Kenneth Bordeau ,  John Jurcak ,  Thaddeus Nieduzak ,  Sharon Jackson ,  Paul Angell ,  James Carey ,  George Lee ,  David Fink ,  Jean-Francois Sabuco ,  Yulin Chiang ,  Nicola Collar

Inventor： James Hendrix ,  Horst Hemmerle ,  Matthias Urmann ,  Gregory Shutske ,  Joseph Strupczewski ,  Kenneth Bordeau ,  John Jurcak ,  Thaddeus Nieduzak ,  Sharon Jackson ,  Paul Angell ,  James Carey ,  George Lee ,  David Fink ,  Jean-Francois Sabuco ,  Yulin Chiang ,  Nicola Collar

IPC: A61K31/498 ,  A61K31/497 ,  A61K31/496

CPC classification number: A61K31/496 ,  C07D209/08 ,  C07D213/74 ,  C07D215/40 ,  C07D231/12 ,  C07D233/56 ,  C07D239/42 ,  C07D241/04 ,  C07D241/20 ,  C07D249/08 ,  C07D261/20 ,  C07D295/14 ,  C07D295/155 ,  C07D307/66 ,  C07D307/68 ,  C07D317/58 ,  C07D333/58 ,  C07D333/66 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D471/06 ,  C07D495/04 ,  C07D498/04

Abstract: The invention relates to heterocyclic substituted carbonyl derivatives that display selective binding to dopamine D3 receptors. In another aspect, the invention relates is to a method for treating central nervous system disorders associated with the dopamine D3 receptor activity in a patient in need of such treatment comprising administering to the subject a therapeutically effective amount of said compounds for alleviation of such disorder. The central nervous system disorders that may be treated with these compounds include Psychotic Disorders, Substance Dependence, Substance Abuse, Dyskinetic Disorders (e.g. Parkinson's Disease, Parkinsonism, Neuroleptic-Induced Tardive Dyskinesia, Gilles de la Tourette Syndrome and Huntington's Disease), Dementia, Anxiety Disorders, Sleep Disorders, Circadian Rhythm Disorders and Mood Disorders. The subject invention is also directed towards processes for the preparation of the compounds described herein as well as methods for making and using the compounds as imaging agents for dopamine D3 receptors.

Abstract translation: 本发明涉及显示与多巴胺D 3受体的选择性结合的杂环取代的羰基衍生物。 另一方面，本发明涉及在需要这种治疗的患者中治疗与多巴胺D 3 N 3受体活性相关的中枢神经系统障碍的方法，包括向受试者施用治疗有效量的 所述化合物用于缓解这种病症。 可能用这些化合物治疗的中枢神经系统疾病包括心理障碍，物质依赖性，物质滥用，运动障碍（例如帕金森病，帕金森综合征，神经灵敏诱导的迟发性运动障碍，杜氏杜勒氏综合征和亨廷顿病），痴呆，焦虑 疾病，睡眠障碍，昼夜节律紊乱和情绪障碍。 本发明还涉及制备本文所述化合物的方法以及制备和使用化合物作为多巴胺D 3受体的显像剂的方法。