公开(公告)号：US20080280959A1

公开(公告)日：2008-11-13

申请号：US12062753

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: A61K31/433 ,  C07D285/135 ,  A61P3/00

CPC classification number: C07D417/12 ,  C07D285/135

Abstract: The present invention comprises cyclic N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides, their functional derivatives 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 R1-R9 substituents are defined herein. 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: 本发明包括环状N- [1,3,4] - 噻二唑-2-基 - 苯磺酰胺，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R1-R9取代基在本文中定义。 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：US20080262036A1

公开(公告)日：2008-10-23

申请号：US12055764

申请日：2008-03-26

Applicant: Stefanie Keil ,  Patrick Bernardelli ,  Matthias Urmann ,  Hans Matter ,  Wolfgang Wendler ,  Maike Glien ,  Karen Chandross ,  Lan Lee

Inventor： Stefanie Keil ,  Patrick Bernardelli ,  Matthias Urmann ,  Hans Matter ,  Wolfgang Wendler ,  Maike Glien ,  Karen Chandross ,  Lan Lee

IPC: A61K31/4709 ,  C07D417/12 ,  A61K31/427 ,  A61P3/10 ,  A61P3/00 ,  A61K31/454 ,  C07D417/14

CPC classification number: C07D417/14 ,  C07D277/24 ,  C07D417/12

Abstract: The present invention comprises phenyl-[1,2,4]-oxadiazol-5-one derivatives of the general formula I: wherein the R1-R10 and B, U, V, W, X, Y and Z substituents are defined herein. The claimed invention also comprises the compounds isomers and their physiologically acceptable salts as well as 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 and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.

Abstract translation: 本发明包括通式I的苯基 - [1,2,4] - 恶二唑-5-酮衍生物：其中R1-R10和B，U，V，W，X，Y和Z取代基在本文中定义。 所要求保护的发明还包括化合物异构体及其生理学上可接受的盐以及其制备方法。 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：US20080261979A1

公开(公告)日：2008-10-23

申请号：US12055780

申请日：2008-03-26

Applicant: Stefanie Keil ,  Matthias Urmann ,  Patrick Bernardelli ,  Maike Glien ,  Wolfgang Wendler ,  Karen Chandross ,  Lan Lee

Inventor： Stefanie Keil ,  Matthias Urmann ,  Patrick Bernardelli ,  Maike Glien ,  Wolfgang Wendler ,  Karen Chandross ,  Lan Lee

IPC: A61K31/5377 ,  C07D413/12 ,  A61K31/4245 ,  A61P3/00 ,  C07D413/14

CPC classification number: C07D417/12 ,  C07D417/14

Abstract: The inventive compounds of the present invention are comprised of phenyl and pyridinyl-1,2,4-oxadiazolone derivatives and their physiologically acceptable salts and functional derivatives that are shown to provide peroxisome proliferator activator receptor (PPARdelta) agonist activity. The compounds of the present invention are comprised of the formula: wherein the substituents R1-R5 and R7-R10 are defined herein. The compounds are therapeutically effective in the regulation and modulation of lipid and carbohydrate metabolism in mammals and are thus suitable for the treatment of diseases such as type-2 diabetes, atherosclerosis, cardiovascular disorders and the like.

Abstract translation: 本发明的本发明化合物包括苯基和吡啶基-1,2,4-恶二唑酮衍生物及其生理上可接受的盐和功能性衍生物，其被证明能提供过氧化物酶体增殖物激活剂受体（PPARδ）激动剂活性。 本发明的化合物由下式构成：其中取代基R 1 -R 5和R 7 -R 10在本文中定义。 该化合物在哺乳动物中调节和调节脂质和碳水化合物代谢方面具有治疗上的有效性，因此适用于治疗诸如2型糖尿病，动脉粥样硬化，心血管疾病等疾病。

公开(公告)号：US20070142351A1

公开(公告)日：2007-06-21

申请号：US11643594

申请日：2006-12-21

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

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

IPC: A61K31/498 ,  A61K31/46 ,  C07D451/02 ,  C07D487/04

CPC classification number: C07D249/08 ,  C07D231/12 ,  C07D233/56 ,  C07D333/58 ,  C07D333/66 ,  C07D333/68 ,  C07D333/70 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  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：US20060160142A1

公开(公告)日：2006-07-20

申请号：US11377531

申请日：2006-03-16

Applicant: Guenter Mueller ,  Wendelin Frick ,  Stefan Petry ,  Rudolf Schneider ,  Matthias Urmann

Inventor： Guenter Mueller ,  Wendelin Frick ,  Stefan Petry ,  Rudolf Schneider ,  Matthias Urmann

IPC: G01N33/53

CPC classification number: C07K14/4713 ,  A61K38/1709

Abstract: The invention refers to a protein from plasma membrane of adipocytes. The protein has specific binding affinity to phosphoinositoylglycans. It regulates glucose uptake by circumventing the insulin signaling cascade.

Abstract translation: 本发明涉及脂肪细胞质膜的蛋白质。 该蛋白质对磷酸肌醇蛋白具有特异性结合亲和力。 它通过绕过胰岛素信号级联来调节葡萄糖摄取。