公开(公告)号：US20070093482A1

公开(公告)日：2007-04-26

申请号：US11461189

申请日：2006-07-31

Applicant: Manfred SCHUDOK ,  Hans MATTER ,  Armin HOFMEISTER ,  Maxime LAMPILAS

Inventor： Manfred SCHUDOK ,  Hans MATTER ,  Armin HOFMEISTER ,  Maxime LAMPILAS

IPC: A61K31/5377 ,  A61K31/496 ,  A61K31/4743 ,  C07D498/02

CPC classification number: C07D495/04

Abstract: The invention is directed to a compound of the formula I wherein the variables are as defined herein, or a stereoisomeric form thereof, mixture of stereoisomeric forms, in any ratio, or a salt thereof. Another aspect of the present invention is directed to a pharmaceutical composition comprising, a pharmaceutically effective amount of one or more compounds of formula I according to claim 1 in admixture with a pharmaceutically acceptable carrier. The invention is also directed to a method for effecting the prophylaxis and therapy of degenerative joint diseases such as osteoarthroses, spondyloses, cartilage loss following joint trauma or a relatively long period of joint immobilization following meniscus or patella injuries or ligament ruptures, diseases of the connective tissue such as collagenoses, periodontal diseases, wound healing disturbances and chronic diseases of the locomotory apparatus such as inflammatory, immunological or metabolism-associated acute and chronic arthritides, arthropathies, myalgias and disturbances of bone metabolism, for the treatment of ulceration, atheroscleroses and stenoses, and for the treatment of inflammations, cancer diseases, tumor metastasis formation, cachexia, anorexia, cardiac insufficiency and septic shock or for the prophylaxis of myocardial and cerebral infarctions, in a patient in need thereof, comprising administering to the patient a pharmaceutically effective amount of the compound of formula I according to claim 1, or a pharmaceutically acceptable salt, solvate or prodrug thereof. Furthermore the invention is directed to a method for preparing a compound of formula I.

Abstract translation: 本发明涉及式I化合物，其中变量如本文所定义，或其立体异构形式，立体异构体形式的任何比例的混合物或其盐。 本发明的另一方面涉及一种药物组合物，其包含药学有效量的一种或多种根据权利要求1的式I化合物与药学上可接受的载体的混合物。 本发明还涉及一种用于预防和治疗退行性关节疾病如骨关节炎，椎关节强硬，关节创伤后的软骨损失或半月板或髌骨损伤或韧带断裂后相对较长的关节固定的方法，连接性疾病 诸如胶原蛋白，牙周病，伤口愈合障碍和诸如炎症，免疫学或代谢相关的急性和慢性关节炎的关节病，关节病，肌痛和骨骼代谢紊乱的运动器官的组织，用于治疗溃疡，动脉粥样硬化和狭窄 ，并且用于在有需要的患者中治疗炎症，癌症疾病，肿瘤转移形成，恶病质，厌食症，心脏功能不全和败血性休克或用于预防心肌和脑梗死，包括向患者施用药学有效量 的compou 根据权利要求1的式I的或其药学上可接受的盐，溶剂合物或前药。 此外，本发明涉及制备式I化合物的方法。

公开(公告)号：US20070088041A1

公开(公告)日：2007-04-19

申请号：US11552283

申请日：2006-10-24

Applicant: Swen Hoelder ,  Karl Schoenafinger ,  David Will ,  Hans Matter ,  Guenter Mueller ,  Martin Bossart

Inventor： Swen Hoelder ,  Karl Schoenafinger ,  David Will ,  Hans Matter ,  Guenter Mueller ,  Martin Bossart

IPC: A61K31/501 ,  C07D487/02

CPC classification number: C07D401/14 ,  C07D403/04 ,  C07D471/04

Abstract: The present invention relates to compounds according to the general formula (I), with the definitions of the substituents X, R1 and R2 given below in the text, as well as their physiologically acceptable salts, methods for producing these compounds and their use as pharmaceuticals. These compounds are kinase inhibitors, in particular inhibitors of the kinase GSK-3β(glycogen synthase kinase-3β).

Abstract translation: 本发明涉及根据通式（I）的化合物，以及下面在文中给出的取代基X，R 1和R 2的定义，以及 作为其生理上可接受的盐，这些化合物的制备方法及其作为药物的用途。 这些化合物是激酶抑制剂，特别是激酶GSK-3β（糖原合成酶激酶-3β）的抑制剂。

公开(公告)号：US20070049573A1

公开(公告)日：2007-03-01

申请号：US11467277

申请日：2006-08-25

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

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

IPC: A61K31/553 ,  A61K31/55 ,  A61K31/541 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/52 ,  A61K31/4709 ,  A61K31/405 ,  A61K31/4025

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

Abstract: The present invention relates to compounds of the formulae (I) and (Ia), wherein R0; R1; R3; R4; R22, Q; V, G and M have the meanings indicated in the claims. The compounds of the formulae (I) and (Ia) are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable 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 formulae (I) and (Ia), their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

Abstract translation: 本发明涉及式（I）和（Ia）的化合物，其中R 0， R＆lt; 1＆gt;; R3; R4; R22，Q; V，G和M具有权利要求中所示的含义。 式（I）和（Ia）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，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。 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。 本发明还涉及制备式（I）和（Ia）化合物的方法，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：US07153876B2

公开(公告)日：2006-12-26

申请号：US10634827

申请日：2003-08-06

Applicant: Manfred Schudok ,  Otmar Klingler ,  Hans-Peter Nestler ,  Hans Matter ,  Herman Schreuder

Inventor： Manfred Schudok ,  Otmar Klingler ,  Hans-Peter Nestler ,  Hans Matter ,  Herman Schreuder

IPC: C07D213/75 ,  A61K31/44 ,  A61P7/02 ,  A61P9/10

CPC classification number: A61K31/27 ,  A61K31/167 ,  A61K31/225 ,  C07C257/18 ,  C07C257/20

Abstract: Compounds of formula I, in which R1, R2, A, and B having the definitions set forth in the claims, are valuable pharmacologically active compounds, which exhibit a strong antithrombotic effect and are suitable, for example, for treating thromboembolic diseases and restenoses. They are reversible inhibitors of the blood clotting enzyme factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. Also disclosed are processes for the preparation of compounds of formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

Abstract translation: 具有权利要求中所述定义的R 1，R 2，A和B的式I化合物是有价值的药理学活性化合物，其表现出强烈的 抗血栓形成作用，并且适用于例如治疗血栓栓塞性疾病和再狭窄。 它们是血液凝固酶因子VIIa的可逆抑制剂，并且通常可以在其中存在不需要的因子VIIa的活性或用于治疗或预防因子VIIa的抑制的条件下使用。 还公开了制备式I化合物的方法，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：US20050143419A1

公开(公告)日：2005-06-30

申请号：US10886312

申请日：2004-07-07

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

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

IPC: A61K31/445 ,  A61K31/4545 ,  A61P7/02 ,  A61P43/00 ,  C07D211/26 ,  C07D211/34 ,  C07D401/12 ,  C07D413/02 ,  A61K31/4245 ,  A61K31/4439 ,  A61K31/454

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：US06759420B1

公开(公告)日：2004-07-06

申请号：US09472936

申请日：1999-12-28

Applicant: Elisabeth Defossa ,  Uwe Heinelt ,  Otmar Klingler ,  Gerhard Zoller ,  Hans Matter ,  Fahad A. Al-Obeidi ,  Armin Walser ,  Peter Wildgoose

Inventor： Elisabeth Defossa ,  Uwe Heinelt ,  Otmar Klingler ,  Gerhard Zoller ,  Hans Matter ,  Fahad A. Al-Obeidi ,  Armin Walser ,  Peter Wildgoose

IPC: A61K3134

CPC classification number: C07D213/40 ,  A61K38/00 ,  C07C257/18 ,  C07C279/14 ,  C07C2601/14 ,  C07D211/26 ,  C07D213/56 ,  C07D233/20 ,  C07D233/74 ,  C07D271/07 ,  C07D413/12 ,  C07K5/0205 ,  C07K5/06078

Abstract: The present invention is directed to new compounds for the inhibition of blood clotting proteins and factor Xa activity, and more particularly, to arylalkanoyl derivatives of the formula (I): wherein R(1), R(2), R(3), R(4), R(5), R(6a), and R(6b) have the meanings indicated in the claims. The invention also relates to processes for the preparation of the compounds of formula (I), to methods of inhibiting factor Xa activity and of inhibiting blood clotting, to the use of the compounds of formula (I) in the treatment and prophylaxis of diseases whcih can be treated or prevented by the inhibition of factor Xa activity, such as cardiovascular or thromboembolic diseases, and to the use of the compounds of formula (I) in the preparation of medicaments to be applied in such diseases.

Abstract translation: 本发明涉及用于抑制凝血蛋白和因子Xa活性的新化合物，更具体地说，涉及式（I）的芳基烷酰基衍生物：其中R（1），R（2），R（3）， R（4），R（5），R（6a）和R（6b）具有权利要求中所示的含义。 本发明还涉及制备式（I）化合物的方法，抑制因子Xa活性和抑制血液凝固的方法，涉及使用式（I）化合物治疗和预防疾病的方法 可以通过抑制因子Xa活性（例如心血管或血栓栓塞性疾病）以及式（I）化合物在制备用于这些疾病的药物中的用途来治疗或预防。

公开(公告)号：US09073975B2

公开(公告)日：2015-07-07

申请号：US13818444

申请日：2011-07-27

Applicant: Otmar Klingler ,  Horst Blum ,  Andreas Lindenschmidt ,  Hans Matter

Inventor： Otmar Klingler ,  Horst Blum ,  Andreas Lindenschmidt ,  Hans Matter

IPC: C07K7/64 ,  C07K7/06 ,  C07K7/56 ,  A61K38/00

CPC classification number: C07K7/64 ,  A61K38/00 ,  C07K7/06 ,  C07K7/56

Abstract: The present invention relates to compounds of the Formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, X1, X2, X3 and X4 have the meanings indicated in the claims, and which are valuable pharmacologically active compounds. They are reversible inhibitors of the interaction between the plasma protein von Willebrand factor (vWF) and the blood platelet receptor glycoprotein Ib-IX-V complex (GPIb), and are suitable, for example, for the therapy and prophylaxis of athero-thrombotic diseases. The invention furthermore relates to processes for the preparation of compounds of the Formula (I), their use, in particular as active ingredients in medicaments, and pharmaceutical compositions comprising them.

Abstract translation: 本发明涉及式（I）化合物，其中R1，R2，R3，R4，R5，R6，R7，R8，R9，R10，R11，R12，R13，R14，R15，R16，R17，R18 X1，X2，X3和X4具有权利要求中所示的含义，并且它们是有价值的药理活性化合物。 它们是血浆蛋白血管性血友病因子（vWF）和血小板受体糖蛋白Ib-IX-V复合物（GPIb）之间的相互作用的可逆抑制剂，并且适合于例如治疗和预防动脉粥样硬化血栓性疾病 。 本发明还涉及制备式（I）化合物，其用途，特别是作为药物中的活性成分的方法，以及包含它们的药物组合物。

公开(公告)号：US08673917B2

公开(公告)日：2014-03-18

申请号：US13063088

申请日：2009-09-02

Applicant: Gerhard Zoller ,  Marc Dietrich Voss ,  Hans Matter ,  Andreas Herling

Inventor： Gerhard Zoller ,  Marc Dietrich Voss ,  Hans Matter ,  Andreas Herling

IPC: C07D401/14 ,  A61K31/4402 ,  A61K31/501 ,  A61P3/00 ,  A61P3/04 ,  A61P3/10 ,  A61P9/00

CPC classification number: C07D487/04

Abstract: The invention relates to compounds of the formula (I), where the groups R1, M, A, B, D, L, and R have the specified meanings, and to the physiologically compatible salts thereof. The compounds are suitable, for example, for treating metabolic syndrome, insulin resistance, obesity, and diabetes.

Abstract translation: 本发明涉及式（I）化合物，其中基团R 1，M，A，B，D，L和R具有特定含义，以及其生理上相容的盐。 该化合物适用于例如治疗代谢综合征，胰岛素抵抗，肥胖症和糖尿病。

公开(公告)号：US08580813B2

公开(公告)日：2013-11-12

申请号：US12845324

申请日：2010-07-28

Applicant: Henning Steinhagen ,  Bodo Scheiper ,  Hans Matter ,  Gary Mccort

Inventor： Henning Steinhagen ,  Bodo Scheiper ,  Hans Matter ,  Gary Mccort

IPC: A61K31/44

CPC classification number: C07D471/04

Abstract: The present invention relates to cyclic azaindole-3-carboxamides of the formula I, wherein A, R, R10, R20, R30, R40, Y1, Y2, Y3, Y4, n, p and q have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they inhibit the enzyme renin and modulate the activity of the renin-angiotensin system, and are useful for the treatment of diseases such as hypertension, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.

Abstract translation: 本发明涉及式I的环状氮杂吲哚-3-甲酰胺，其中A，R，R10，R20，R30，R40，Y1，Y2，Y3，Y4，n，p和q具有权利要求中所示的含义， 这是有价值的药物活性化合物。 具体地说，它们抑制酶肾素并调节肾素 - 血管紧张素系统的活性，并且可用于治疗例如高血压等疾病。 本发明还涉及制备式I化合物的方法，其用途和包含它们的药物组合物。

公开(公告)号：US08344004B2

公开(公告)日：2013-01-01

申请号：US12796886

申请日：2010-06-09

Applicant: Karl Schoenafinger ,  Stefanie Keil ,  Matthias Urmann ,  Hans Matter ,  Maike Glien ,  Wolfgang Wendler ,  Ulrike Wendler, legal representative

Inventor： Karl Schoenafinger ,  Stefanie Keil ,  Matthias Urmann ,  Hans Matter ,  Maike Glien ,  Wolfgang Wendler

IPC: A61K31/4439 ,  A61K31/433 ,  C07D417/12

CPC classification number: C07D417/12

Abstract: The invention relates to cyclic N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARgamma 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: 本发明涉及环状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，其显示出PPARdta或PPARδ和PPARγ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。