公开(公告)号：US08669266B2

公开(公告)日：2014-03-11

申请号：US12573551

申请日：2009-10-05

Applicant: Marc Nazare ,  Gernot Zech ,  Melitta Just ,  Tilo Weiss ,  Gerhard Hessler ,  Joerg Czech

Inventor： Marc Nazare ,  Gernot Zech ,  Melitta Just ,  Tilo Weiss ,  Gerhard Hessler ,  Joerg Czech

IPC: A01N43/42 ,  A61K31/44

CPC classification number: C07D401/12 ,  C07D401/14 ,  C07D405/14

Abstract: The present invention relates to compounds of the formula I, in which R1; R2; R3; R4; R5; R6; Z; A; B; E; X; Q; J; 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 anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable e.g. for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 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 1; R2; R3; R4; R5; R6; Z; 一个; B; E; X; Q; J; 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。 它们对血小板表现出强烈的抗凝集作用，因此表现出抗血栓形成的作用， 用于治疗和预防心血管疾病如血栓栓塞性疾病或再狭窄。 它们是血小板ADP受体P2Y12的可逆拮抗剂，并且通常可用于其中存在血小板ADP受体P2Y12的不期望的活化或用于治疗或预防血小板ADP受体P2Y12的抑制的条件 。 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：US08598179B2

公开(公告)日：2013-12-03

申请号：US12817868

申请日：2010-06-17

Applicant: Marc Nazaré ,  Gernot Zech ,  Jochen Goerlitzer ,  Melitta Just ,  Tilo Weiss ,  Gerhard Hessler ,  Werngard Czechtizky ,  Sven Ruf

Inventor： Marc Nazaré ,  Gernot Zech ,  Jochen Goerlitzer ,  Melitta Just ,  Tilo Weiss ,  Gerhard Hessler ,  Werngard Czechtizky ,  Sven Ruf

IPC: A61K31/496 ,  C07D231/22 ,  C07D413/12 ,  C07D417/12 ,  A61K31/454 ,  A61K31/506 ,  C07D401/12 ,  C07D401/04

CPC classification number: C07D403/12

Abstract: The present invention relates to compounds of the formula I, wherein R1; R2; Z; A; B; D; Q; J; 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 anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable, e.g., for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 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R1; R2; Z; 一个; B; D; Q; J; 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。 它们对血小板表现出强烈的抗凝集作用并因此具有抗血栓形成作用，并且适合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。 它们是血小板ADP受体P2Y12的可逆拮抗剂，并且通常可用于其中存在血小板ADP受体P2Y12的不期望的活化或用于治疗或预防血小板ADP受体P2Y12的抑制的条件 。 本发明还涉及制备式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：US07910576B2

公开(公告)日：2011-03-22

申请号：US12639500

申请日：2009-12-16

Applicant: Otmar Klingler ,  Joerg Czech ,  Werngard Czechtizky ,  Tilo Weiss ,  Melitta Just

Inventor： Otmar Klingler ,  Joerg Czech ,  Werngard Czechtizky ,  Tilo Weiss ,  Melitta Just

IPC: A61K31/454 ,  A61K31/496 ,  C07D401/14 ,  C07D401/02 ,  C07D403/14 ,  C07D403/02

CPC classification number: C07D401/06 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14

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; A; B, D and E have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable e.g. for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 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 1; R2; R3; R4; R5 R6; R7; R8; R9; R10; R11; R12; R13; 一个; B，D和E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。 它们对血小板表现出强烈的抗凝集作用，因此表现出抗血栓形成的作用， 用于治疗和预防心血管疾病如血栓栓塞性疾病或再狭窄。 它们是血小板ADP受体P2Y12的可逆拮抗剂，并且通常可用于其中存在血小板ADP受体P2Y12的不期望的活化或用于治疗或预防血小板ADP受体P2Y12的抑制的条件 。 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：US20110039829A1

公开(公告)日：2011-02-17

申请号：US12817868

申请日：2010-06-17

Applicant: Marc NAZARÉ ,  Gernot ZECH ,  Jochen GOERLITZER ,  Melitta JUST ,  Tilo WEISS ,  Gerhard HESSLER ,  Werngard CZECHTIZKY ,  Sven RUF

Inventor： Marc NAZARÉ ,  Gernot ZECH ,  Jochen GOERLITZER ,  Melitta JUST ,  Tilo WEISS ,  Gerhard HESSLER ,  Werngard CZECHTIZKY ,  Sven RUF

IPC: A61K31/551 ,  C07D403/12 ,  A61K31/496 ,  C07D401/14 ,  A61K31/506 ,  C07D401/12 ,  A61K31/454 ,  C07D405/14 ,  A61P9/10 ,  A61P11/00

CPC classification number: C07D403/12

Abstract: The present invention relates to compounds of the formula I, wherein R1; R2; Z; A; B; D; Q; J; 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 anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable, e.g., for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 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R1; R2; Z; 一个; B; D; Q; J; 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。 它们对血小板表现出强烈的抗凝集作用并因此具有抗血栓形成作用，并且适合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。 它们是血小板ADP受体P2Y12的可逆拮抗剂，并且通常可用于其中存在血小板ADP受体P2Y12的不期望的活化或用于治疗或预防血小板ADP受体P2Y12的抑制的条件 。 本发明还涉及制备式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：US20100226918A1

公开(公告)日：2010-09-09

申请号：US12639500

申请日：2009-12-16

Applicant: Otmar KLINGLER ,  Joerg CZECH ,  Werngard CZECHTIZKY ,  Tilo WEISS ,  Melitta JUST

Inventor： Otmar KLINGLER ,  Joerg CZECH ,  Werngard CZECHTIZKY ,  Tilo WEISS ,  Melitta JUST

IPC: A61K31/496 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14 ,  C07D401/14 ,  C07D401/06 ,  A61K31/454 ,  A61K31/727 ,  A61K31/616 ,  A61K39/395 ,  A61K38/12 ,  A61K31/551 ,  A61K31/5377 ,  A61P7/02 ,  A61P9/10 ,  A61P9/00

CPC classification number: C07D401/06 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14

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; A; B, D and E have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable e.g. for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 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 1; R2; R3; R4; R5; R6; R7; R8; R9; R10; R11; R12; R13; 一个; B，D和E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。 它们对血小板表现出强烈的抗凝集作用，因此表现出抗血栓形成的作用， 用于治疗和预防心血管疾病如血栓栓塞性疾病或再狭窄。 它们是血小板ADP受体P2Y12的可逆拮抗剂，并且通常可用于其中存在血小板ADP受体P2Y12的不期望的活化或用于治疗或预防血小板ADP受体P2Y12的抑制的条件 。 本发明还涉及制备式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：US20100135999A1

公开(公告)日：2010-06-03

申请号：US12573551

申请日：2009-10-05

Applicant: Marc Nazaré ,  Gernot ZECH ,  Melitta JUST ,  Tilo WEISS ,  Gerhard HESSLER ,  Joerg Czech

Inventor： Marc Nazaré ,  Gernot ZECH ,  Melitta JUST ,  Tilo WEISS ,  Gerhard HESSLER ,  Joerg Czech

IPC: A61K39/395 ,  C07D401/14 ,  A61K31/496 ,  C07D241/04 ,  C07D205/04 ,  A61K31/397 ,  C07D413/14 ,  A61K31/5377 ,  C07D243/08 ,  A61K31/551 ,  C07D487/04 ,  A61K31/4985 ,  A61K31/70 ,  A61K31/56 ,  A61K31/554 ,  A61K31/54 ,  A61K31/60 ,  A61K31/727 ,  A61K31/715 ,  A61K38/02 ,  A61K38/49 ,  A61K38/48 ,  A61K31/704 ,  A61K38/28 ,  A61K38/13 ,  A61P9/00 ,  A61P11/00 ,  A61P35/00 ,  A61P31/00

CPC classification number: C07D401/12 ,  C07D401/14 ,  C07D405/14

Abstract: The present invention relates to compounds of the formula I, in which R1; R2; R3; R4; R5; R6; Z; A; B; E; X; Q; J; 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 anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable e.g. for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 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 1; R2; R3; R4; R5; R6; Z; 一个; B; E; X; Q; J; 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。 它们对血小板表现出强烈的抗凝集作用，因此表现出抗血栓形成的作用， 用于治疗和预防心血管疾病如血栓栓塞性疾病或再狭窄。 它们是血小板ADP受体P2Y12的可逆拮抗剂，并且通常可用于其中存在血小板ADP受体P2Y12的不期望的活化或用于治疗或预防血小板ADP受体P2Y12的抑制的条件 。 本发明还涉及制备式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：US20060024710A1

公开(公告)日：2006-02-02

申请号：US11155457

申请日：2005-06-16

Applicant: Tilo Weiss ,  Stefan Stumpe ,  Friedhelm Siepmann ,  Andreas Thuenchen ,  Frank Wienhausen ,  Andreas Katerkamp ,  Michael Heinzel ,  Roland Breves ,  Mirko Weide

Inventor： Tilo Weiss ,  Stefan Stumpe ,  Friedhelm Siepmann ,  Andreas Thuenchen ,  Frank Wienhausen ,  Andreas Katerkamp ,  Michael Heinzel ,  Roland Breves ,  Mirko Weide

IPC: C12Q1/68 ,  G01N33/554 ,  G01N33/569 ,  C12Q1/04

CPC classification number: C12Q1/24

Abstract: A method for quantitative and/or qualitative determination of germs in a liquid sample comprises the steps of: (1) passing the sample through a filter thereby depositing the germs on a major portion of the filter so that a minor portion of the filter is free of germ deposits; (2) applying a fluorescent label to at least a portion of the deposited germs; (3) determining the presence and/or the amount of labeled germs by fluorescent reflection photometry. The method according to the present invention is suitable, for example, for quantitative and/or qualitative determination of germs in foodstuffs, surfactant-containing products such as washing and cleaning agents, surface treatment agents, dispersion products, cosmetics, hygiene products and personal care products, pharmaceuticals, adhesives, coolant lubricants, coatings and coating coagulations, as well as raw materials and starting materials for the aforesaid products.

Abstract translation: 用于定量和/或定性地测定液体样品中的细菌的方法包括以下步骤：（1）使样品通过过滤器，由此将细菌沉积在过滤器的主要部分上，使得过滤器的一小部分是游离的 的细菌沉积; （2）向沉积的细菌的至少一部分施加荧光标记; （3）通过荧光反射测光法测定标记的细菌的存在和/或数量。 根据本发明的方法适用于例如定量和/或定性测定食品中的细菌，含表面活性剂的产品如洗涤和清洁剂，表面处理剂，分散体产品，化妆品，卫生产品和个人护理 产品，药品，粘合剂，冷却剂润滑剂，涂料和涂料凝结剂，以及上述产品的原料和原料。

公开(公告)号：US08426420B2

公开(公告)日：2013-04-23

申请号：US12817873

申请日：2010-06-17

Applicant: Marc Nazaré ,  Gernot Zech ,  Melitta Just ,  Tilo Weiss ,  Gerhard Hessler ,  Markus Kohlmann

Inventor： Marc Nazaré ,  Gernot Zech ,  Melitta Just ,  Tilo Weiss ,  Gerhard Hessler ,  Markus Kohlmann

IPC: A61K31/496 ,  A61K31/454 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

CPC classification number: C07D403/14

Abstract: The present invention relates to compounds of the formula I, wherein R1; R2; Z; A; B; D; Q; J; 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 anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable, e.g., for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 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R1; R2; Z; 一个; B; D; Q; J; 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。 它们对血小板表现出强烈的抗凝集作用并因此具有抗血栓形成作用，并且适合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。 它们是血小板ADP受体P2Y12的可逆拮抗剂，并且通常可用于其中存在血小板ADP受体P2Y12的不期望的活化或用于治疗或预防血小板ADP受体P2Y12的抑制的条件 。 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：US20130072493A1

公开(公告)日：2013-03-21

申请号：US13236027

申请日：2011-09-19

Applicant: Marc NAZARE ,  Nis Halland ,  Friedemann Schmidt ,  Tilo Weiss ,  Uwe Dietz ,  Armin Hofmeister

Inventor： Marc NAZARE ,  Nis Halland ,  Friedemann Schmidt ,  Tilo Weiss ,  Uwe Dietz ,  Armin Hofmeister

IPC: A61K31/4985 ,  A61P19/02 ,  A61P19/04 ,  A61P9/10 ,  A61P9/00 ,  A61P43/00 ,  A61P29/00 ,  A61P35/00 ,  C07D487/04 ,  A61P3/10

CPC classification number: A61K31/4985 ,  C07D487/04

Abstract: The present invention relates to N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides of the formula I, wherein Ar, R1, R2 and n have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds which modulate protein kinase activity, specifically the activity of serum and glucocorticoid regulated kinase (SGK), in particular of serum and glucocorticoid regulated kinase isoform 1 (SGK-1, SGK1), and are suitable for the treatment of diseases in which SGK activity is inappropriate, for example degenerative joint disorders or inflammatory processes such as osteoarthritis or rheumatism. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.

Abstract translation: 本发明涉及式I的N- [4-（1H-吡唑并[3,4-b]吡嗪-6-基） - 苯基] - 磺酰胺，其中Ar，R 1，R 2和n具有如 索赔。 式I的化合物是调节蛋白激酶活性，特别是血清和糖皮质激素调节激酶（SGK）的活性，特别是血清和糖皮质激素调节激酶同工型1（SGK-1，SGK1）的活性的有价值的药理活性化合物，并且是 适合于治疗SGK活动不适当的疾病，例如退行性关节疾病或炎性过程如骨关节炎或风湿病。 本发明还涉及式I化合物的制备方法，它们作为药物的用途，以及包含它们的药物组合物。

公开(公告)号：US20110021537A1

公开(公告)日：2011-01-27

申请号：US12817873

申请日：2010-06-17

Applicant: Marc Nazaré ,  Gernot Zech ,  Melitta Just ,  Tilo Weiss ,  Gerhard Hessler ,  Markus Kohlmann

Inventor： Marc Nazaré ,  Gernot Zech ,  Melitta Just ,  Tilo Weiss ,  Gerhard Hessler ,  Markus Kohlmann

IPC: A61K31/497 ,  C07D403/14 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P7/02

CPC classification number: C07D403/14

Abstract: The present invention relates to compounds of the formula I, wherein R1; R2; Z; A; B; D; Q; J; 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 anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable, e.g., for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 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R1; R2; Z; 一个; B; D; Q; J; 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。 它们对血小板表现出强烈的抗凝集作用并因此具有抗血栓形成作用，并且适合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。 它们是血小板ADP受体P2Y12的可逆拮抗剂，并且通常可用于其中存在血小板ADP受体P2Y12的不期望的活化或用于治疗或预防血小板ADP受体P2Y12的抑制的条件 。 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。