公开(公告)号：US20090012131A1

公开(公告)日：2009-01-08

申请号：US12062769

申请日：2008-04-04

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

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

IPC: A61K31/433 ,  C07D285/135 ,  A61P3/00 ,  A61P3/10

CPC classification number: C07D285/135 ,  C07D417/12

Abstract: The present invention comprises 4-Oxy-N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides, the derivatives thereof and salts thereof as well as processes for their preparation and methods for their use as pharmaceutical compositions. More specifically, the invention relates to 4-oxy-N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides and to their physiologically acceptable salts and physiologically functional derivatives that exhibit peroxisome proliferator activator receptor (PPAR) PPARalpha, PPARdelta and PPARgamma agonist activity. The compounds themselves are defined by the structure of the formula I, wherein the various unnamed substituents are defined herein. The compounds are suitable for the treatment of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved as well as demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.

Abstract translation: 本发明包括4-氧基-N- [1,3,4] - 噻二唑-2-基 - 苯磺酰胺及其衍生物及其盐，以及其制备方法及其用作药物组合物的方法。 更具体地，本发明涉及4-氧-N- [1,3,4] - 噻二唑-2-基 - 苯磺酰胺及其生理上可接受的盐和生理功能衍生物，其表现出过氧化物酶体增殖物激活受体（PPAR）PPARα， PPARδ和PPARgamma激动剂活性。 化合物本身由式I的结构定义，其中各种未命名的取代基在本文中定义。 该化合物适用于治疗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：US20080287409A1

公开(公告)日：2008-11-20

申请号：US12055793

申请日：2008-03-26

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

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

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

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

Abstract: 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.

Abstract translation: 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：US07435747B2

公开(公告)日：2008-10-14

申请号：US10886312

申请日：2004-07-07

Applicant: Anuschirwan Peyman ,  David William Will ,  Uwe Gerlach ,  Marc Nazaré ,  Gerhard Zoller ,  Hans-Peter Nestler ,  Hans Matter ,  Fahad Al-Obeidi

Inventor： Anuschirwan Peyman ,  David William Will ,  Uwe Gerlach ,  Marc Nazaré ,  Gerhard Zoller ,  Hans-Peter Nestler ,  Hans Matter ,  Fahad Al-Obeidi

IPC: A61K31/445 ,  C07D211/26

CPC classification number: C07D401/12 ,  C07D211/26 ,  C07D211/34

Abstract: The present invention relates to compounds of the formula I, in which R0; Q; X; Q′, D, R10 and V have the meanings indicated in the claims. 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 VIIa 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: 本发明涉及式I化合物，其中R 0是 Q; X; Q'，D，R 10和V具有权利要求中所示的含义。 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VIIa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：US20080167346A1

公开(公告)日：2008-07-10

申请号：US11940654

申请日：2007-11-15

Applicant: Michael WAGNER ,  Matthias URMANN ,  Volkmar WEHNER ,  Martin LORENZ ,  Armin BAUER ,  Marc NAZARE ,  Hans MATTER

Inventor： Michael WAGNER ,  Matthias URMANN ,  Volkmar WEHNER ,  Martin LORENZ ,  Armin BAUER ,  Marc NAZARE ,  Hans MATTER

IPC: A61K31/4535 ,  C07C233/57 ,  A61K31/166 ,  A61P11/00 ,  A61P9/00 ,  C07D409/12

CPC classification number: C07D211/58 ,  C07D333/38 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D419/14

Abstract: The present invention relates to compounds of the formula I, which exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses.

Abstract translation: 本发明涉及式I化合物，其具有强的抗血栓形成作用，并且适用于治疗和预防心血管疾病如血栓栓塞性疾病或再狭窄。

公开(公告)号：US20080090821A1

公开(公告)日：2008-04-17

申请号：US11862818

申请日：2007-09-27

Applicant: Armin HOFMEISTER ,  Manfred Schudok ,  Hans Matter ,  Kristin Breitschopf ,  Antonio Ugolini

Inventor： Armin HOFMEISTER ,  Manfred Schudok ,  Hans Matter ,  Kristin Breitschopf ,  Antonio Ugolini

IPC: A61K31/472 ,  A61K31/496 ,  A61K31/5377 ,  A61P19/00 ,  A61P29/00 ,  A61P35/00 ,  A61P9/00 ,  C07D401/02 ,  C07D413/02

CPC classification number: C07D217/26 ,  C07D403/12

Abstract: The present invention is directed to a compound of formula (1), wherein R1, R2, R3, R4, A, L and n are as defined herein, its pharmaceutical composition, preparation and uses as a MMP inhibitor.

Abstract translation: 本发明涉及式（1）的化合物，其中R 1，R 2，R 3，R 4 A，L和n如本文所定义，其药物组合物，制剂和用作MMP抑制剂。

公开(公告)号：US07358268B2

公开(公告)日：2008-04-15

申请号：US10728339

申请日：2003-12-04

Applicant: Marc Nazare ,  Armin Bauer ,  Volkmar Wehner ,  David W. Will ,  Hans Matter ,  Michael Wagner ,  Herman Schreuder

Inventor： Marc Nazare ,  Armin Bauer ,  Volkmar Wehner ,  David W. Will ,  Hans Matter ,  Michael Wagner ,  Herman Schreuder

IPC: A61K31/42 ,  C07D261/04 ,  C07D413/04

CPC classification number: C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14

Abstract: This invention is directed to the compound of formula (I) which is useful for inhibiting the activity of Factor Xa. The present invention is also directed to compositions containing said compounds, processes for their preparation, their use, such as in inhibiting the formation of thrombin or for therapeutically or prophylactically treating a patient suffering from, or subject to, or associated with a disease state associated with a cardiovascular disorder.

Abstract translation: 本发明涉及可用于抑制因子Xa的活性的式（I）化合物。 本发明还涉及包含所述化合物的组合物，其制备方法，其用途，例如抑制凝血酶的形成或用于治疗或预防性地治疗患有或与疾病状态有关的患者或与之相关的患者 伴有心血管疾病。

公开(公告)号：US20070179122A1

公开(公告)日：2007-08-02

申请号：US11469513

申请日：2006-09-01

Applicant: Matthias Urmann ,  Marc Nazare ,  Volkmar Wehner ,  Hans Matter ,  Armin Bauer ,  Michael Wagner

Inventor： Matthias Urmann ,  Marc Nazare ,  Volkmar Wehner ,  Hans Matter ,  Armin Bauer ,  Michael Wagner

IPC: A61K31/553 ,  A61K31/551 ,  A61K31/55 ,  A61K31/541 ,  A61K31/496 ,  A61K31/5377 ,  C07D417/02 ,  C07D413/02 ,  C07D403/02

CPC classification number: C07K5/0202 ,  C07D265/32 ,  C07D265/33 ,  C07D291/06 ,  C07D295/112 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D419/12

Abstract: The present invention relates to compounds of the formula I, in which R0; R1; R2; R3; R4; R5, R, Q; V, G and M have the meanings indicated in the claims. 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 thromboemboic 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 VIIa 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: 本发明涉及式I化合物，其中R 0， R＆lt; 1＆gt;; R 2; 3＆lt; 3＆gt; R 4; R 5，R，Q; V，G和M具有权利要求中所示的含义。 式I的化合物是有价值的药理活性化合物。 它们表现出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VIIa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：US07205315B2

公开(公告)日：2007-04-17

申请号：US10950802

申请日：2004-09-27

Applicant: Manfred Schudok ,  Hans Matter ,  Armin Hofmeister

Inventor： Manfred Schudok ,  Hans Matter ,  Armin Hofmeister

IPC: A61K31/4725 ,  C07D217/22 ,  C07D217/24

CPC classification number: C07D217/26 ,  C07D405/12

Abstract: The present invention is directed to a compound of formula (I), or a stereoisomer or a mixture of stereoisomer thereof in any ratio, or its physiologically tolerable salt, which is useful as an inhibitor of matrix metalloproteinase. The present invention is also directed to a pharmaceutical preparation comprising a pharmaceutically effective amount of at least one compound of formula (I); processes for their preparation; the use of a compound of formula (I) having activity as an matrix metalloproteinase inhibitor; and for the prophylaxis and therapy of disease states that involve an increase in the activity of matrix metalloproteinase.

Abstract translation: 本发明涉及式（I）化合物或其任何比例的立体异构体或其立体异构体的混合物或其生理上可耐受的盐，其可用作基质金属蛋白酶的抑制剂。 本发明还涉及包含药学有效量的至少一种式（I）化合物的药物制剂; 其准备过程; 使用具有活性的式（I）化合物作为基质金属蛋白酶抑制剂; 以及用于预防和治疗涉及基质金属蛋白酶活性增加的疾病状态。

公开(公告)号：US06953857B2

公开(公告)日：2005-10-11

申请号：US10023933

申请日：2001-12-21

Applicant: Marc Nazaré ,  David William Will ,  Anuschirwan Peyman ,  Hans Matter ,  Gerhard Zoller ,  Uwe Gerlach

Inventor： Marc Nazaré ,  David William Will ,  Anuschirwan Peyman ,  Hans Matter ,  Gerhard Zoller ,  Uwe Gerlach

IPC: C07D243/08 ,  A61K31/166 ,  A61K31/167 ,  A61K31/18 ,  A61K31/277 ,  A61K31/38 ,  A61K31/4184 ,  A61K31/422 ,  A61K31/435 ,  A61K31/4355 ,  A61K31/437 ,  A61K31/44 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/445 ,  A61K31/4453 ,  A61K31/4465 ,  A61K31/4468 ,  A61K31/451 ,  A61K31/4525 ,  A61K31/453 ,  A61K31/4535 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/495 ,  A61K31/496 ,  A61K31/4965 ,  A61K31/497 ,  A61K31/505 ,  A61K31/506 ,  A61K31/551 ,  A61K31/635 ,  A61P7/00 ,  A61P7/02 ,  A61P7/04 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P11/00 ,  A61P29/00 ,  A61P43/00 ,  C07C235/50 ,  C07C237/42 ,  C07C255/60 ,  C07C311/46 ,  C07C311/51 ,  C07D211/26 ,  C07D211/58 ,  C07D211/96 ,  C07D213/30 ,  C07D213/38 ,  C07D213/40 ,  C07D213/64 ,  C07D213/74 ,  C07D213/89 ,  C07D235/06 ,  C07D235/08 ,  C07D239/42 ,  C07D239/69 ,  C07D241/12 ,  C07D295/12 ,  C07D295/13 ,  C07D295/18 ,  C07D295/192 ,  C07D317/58 ,  C07D333/16 ,  C07D333/58 ,  C07D401/00 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/08 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D491/04 ,  C07D491/048 ,  C07D211/06

CPC classification number: C07D213/40 ,  C07C235/50 ,  C07C311/46 ,  C07C2601/14 ,  C07D211/26 ,  C07D211/58 ,  C07D211/96 ,  C07D213/38 ,  C07D213/74 ,  C07D213/89 ,  C07D235/06 ,  C07D239/42 ,  C07D295/13 ,  C07D295/192 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/08 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D471/04 ,  C07D491/04

Abstract: The present invention relates to compounds comprising the following formula: R0—Q—X—Q′—W—U—V—G—M  (I) These compounds are useful as pharmacologically active compounds. They exhibit an antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders such as thromboembolic diseases or restenoses. These compounds are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can generally be used to treat, prevent, or cure conditions in which an undesired activity of factor Xa and/or factor VIIa is present, or where inhibition of factor Xa and/or factor VIIa is intended. The invention further relates to processes for the preparation of these compounds, methods of their use (e.g., as active ingredients in pharmaceuticals), and pharmaceutical preparations comprising them.

Abstract translation: 本发明涉及包含下列化学式的化合物：<？in-line-formula description =“In-line formula”end =“lead”？> R 0 -QX-Q'-WUVGM（ I）<？in-line-formula description =“In-line Formulas”end =“tail”？>这些化合物可用作药物活性化合物。 它们具有抗血栓形成作用，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。 这些化合物是血液凝固酶因子Xa（FXa）和/或因子VIIa（FVIIa）的可逆抑制剂，并且通常可用于治疗，预防或治愈其中因子Xa和/或因子VIIa的不期望的活性 存在，或其中旨在抑制因子Xa和/或因子VIIa。 本发明还涉及制备这些化合物的方法，其使用方法（例如作为药物中的活性成分）和包含它们的药物制剂。

公开(公告)号：US20050009829A1

公开(公告)日：2005-01-13

申请号：US10849436

申请日：2004-05-19

Applicant: Marc Nazare ,  Michael Wagner ,  Volkmar Wehner ,  Hans Matter ,  Matthias Urmann ,  Kurt Ritter

Inventor： Marc Nazare ,  Michael Wagner ,  Volkmar Wehner ,  Hans Matter ,  Matthias Urmann ,  Kurt Ritter

IPC: C07D235/24 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D473/08 ,  C07D495/04 ,  A61K31/52 ,  A61K31/4709 ,  A61K31/513 ,  A61K31/517 ,  C07D473/02 ,  C07

CPC classification number: C07D235/24 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D473/08 ,  C07D495/04

Abstract: The present invention relates to compounds of the formula I, wherein R0, R1, R2, 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 VIIa 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: 本发明涉及式I化合物，其中R 0，R 1，R 2，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VIIa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。