公开(公告)号：US08735586B2

公开(公告)日：2014-05-27

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: C07D235/08 ,  C07D235/16 ,  C07D235/18 ,  C07D471/04

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：US08487109B2

公开(公告)日：2013-07-16

申请号：US12645509

申请日：2009-12-23

Applicant: Omar Rkyek ,  Marc Nazare ,  Andreas Lindenschmidt ,  Matthias Urmann ,  Nis Halland ,  Jorge Alonso

Inventor： Omar Rkyek ,  Marc Nazare ,  Andreas Lindenschmidt ,  Matthias Urmann ,  Nis Halland ,  Jorge Alonso

IPC: C07D211/60 ,  C07D333/22 ,  C07C229/38 ,  C07C45/00 ,  C07C233/03

CPC classification number: C07C17/263 ,  C07B37/04 ,  C07C17/35 ,  C07C41/30 ,  C07C43/225 ,  C07C45/61 ,  C07C45/70 ,  C07C231/12 ,  C07C253/30 ,  C07C2601/16 ,  C07D295/00 ,  C07D333/20 ,  C07C25/24 ,  C07C49/84 ,  C07C47/548 ,  C07C233/07 ,  C07C233/43 ,  C07C233/54 ,  C07C255/33 ,  C07C255/50 ,  C07C255/51 ,  C07C255/53 ,  C07C255/54 ,  C07C255/58

Abstract: The present invention relates to a process for the regioselective synthesis of compounds of the formula (I), wherein R1; R2; R3; R4; R5; J and W have the meanings indicated in the claims. The present invention provides an efficient and general palladium-catalyzed coupling process for aryl tosylates with terminal alkynes to a wide variety of substituted, multifunctional aryl-1-alkynes of the formula I.

Abstract translation: 本发明涉及用于区域选择性合成式（I）化合物的方法，其中R1; R2; R3; R4; R5; J和W具有权利要求中所示的含义。 本发明提供了对具有末端炔烃的芳基甲苯磺酸酯与式I的多种取代的多官能芳基-1-炔烃的有效且一般的钯催化偶联方法。

公开(公告)号：US08329725B2

公开(公告)日：2012-12-11

申请号：US12996784

申请日：2009-05-22

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

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

IPC: A61K31/44 ,  A01N43/42

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

Abstract: The invention relates to annelated pyrrolidin 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: 本发明涉及具有恶二唑酮头基的环状吡咯烷磺酰胺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PPARα激动剂活性。 所描述的是式（I）的化合物，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：US20120122853A1

公开(公告)日：2012-05-17

申请号：US12996692

申请日：2009-05-22

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

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

IPC: A61K31/55 ,  C07D471/04 ,  C07D413/14 ,  C07D498/04 ,  A61K31/4375 ,  A61P3/00 ,  A61K31/4709 ,  A61K31/5383 ,  A61P3/10 ,  A61P3/06 ,  A61P25/00 ,  C07D413/12 ,  A61K31/538

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：US20100234601A1

公开(公告)日：2010-09-16

申请号：US12644371

申请日：2009-12-22

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

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

IPC: C07D471/04 ,  C07D231/56 ,  C07D401/06

CPC classification number: C07D231/56

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 transition metal catalyzed process to a wide variety of multifunctional 2H-indazoles or 2H-azaindazoles of the formula (I) from 2-halo-phenylacetylenes or (2-sulfonato)phenylacetylenes and monosubstituted hydrazines.

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。 本发明提供了对2-卤代苯基乙炔或（2-磺酸基）苯基乙炔和单取代肼的多种式（I）的多官能2H-吲唑或2H-氮杂吲唑的直接过渡金属催化方法。

公开(公告)号：US20100216988A1

公开(公告)日：2010-08-26

申请号：US12644379

申请日：2009-12-22

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

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

IPC: C07D451/00 ,  C07D487/14 ,  C07D471/14 ,  C07D491/22

CPC classification number: C07D487/04 ,  C07D471/04 ,  C07D471/14 ,  C07D491/14

Abstract: The present invention relates to a process for the regioselective synthesis of compounds of the formula I, wherein R1; R2; R3; R4; J1; J2; J3; J4 and G have the meanings indicated in the claims. The present invention provides a direct metal, e.g. palladium or 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: 本发明涉及用于区域选择性合成式I化合物的方法，其中R1; R2; R3; R4; J1; J2; J3; J4和G具有权利要求中所示的含义。 本发明提供直接金属，例如， 钯或铜，催化的区域选择性方法，由2-卤代 - 硝基芳烃和N-取代的酰胺开始制备各种不对称，多官能的式I化合物的N-取代的苯并咪唑或氮杂苯并咪唑。

公开(公告)号：US07772252B2

公开(公告)日：2010-08-10

申请号：US12425731

申请日：2009-04-17

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

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

IPC: A61K31/4535 ,  C07D409/04 ,  C07D409/14 ,  C07D495/04

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 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D3受体的选择性结合的杂环取代的羰基衍生物。 另一方面，本发明涉及一种治疗需要这种治疗的患者中与多巴胺D3受体活性相关的中枢神经系统障碍的方法，其包括向受试者施用治疗有效量的所述化合物以减轻这种病症。 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。 本发明还涉及本文所述化合物的制备方法以及制备和使用化合物作为多巴胺D3受体的显像剂的方法。

公开(公告)号：US20100144862A1

公开(公告)日：2010-06-10

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: A61K31/351 ,  C07D309/40 ,  C07D309/38 ,  A61P1/04 ,  A61P3/04 ,  A61P3/10 ,  A61P9/10 ,  A61P3/06 ,  A61P1/18 ,  A61P35/00 ,  A61P25/28 ,  A61P25/16 ,  A61P17/10 ,  A61P17/00 ,  A61P11/06

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：US07449560B2

公开(公告)日：2008-11-11

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: C07K1/00 ,  C07K14/00 ,  C07K16/00 ,  C07K17/00

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。

公开(公告)号：US07049416B2

公开(公告)日：2006-05-23

申请号：US10470606

申请日：2003-07-03

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

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

IPC: C07K1/00 ,  C07K14/00 ,  C07K16/00 ,  C07K17/00

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.