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1. 发明申请

US20110245263A1 2-HETEROARYL-PYRROLO[3,4-C]PYRROLE DERIVATIVES AND THEIR USE AS SCD 审中-公开
标题翻译： 2-异丙基吡咯并[3,4-C]吡咯并吡喃衍生物及其作为SCD
公开(公告)号：US20110245263A1
公开(公告)日：2011-10-06
申请号：US13160705
申请日：2011-06-15
申请人： Gerhard Zoller , Marc Dietrich Voss , Stefanie Keil , Andreas Herling , Hans Matter
发明人： Gerhard Zoller , Marc Dietrich Voss , Stefanie Keil , Andreas Herling , Hans Matter
IPC分类号： A61K31/501 , C07D487/04 , A61K31/506 , A61K31/4439 , A61P9/00 , A61P25/00 , A61P3/10 , A61P3/04 , A61K31/427 , A61K31/517 , A61P3/00 , A61P25/28 , A61P25/18
CPC分类号： C07D487/04
摘要： The invention relates to heterocyclic derivatives of formula I wherein R, R1, A, B, D, M, L and n are as defined herein, or their physiologically compatible salts, their pharmaceutical compositions and their uses as SCD1 inhibitors.
摘要翻译：本发明涉及式I的杂环衍生物，其中R，R 1，A，B，D，M，L和n如本文所定义，或其生理上相容的盐，其药物组合物及其作为SCD1抑制剂的用途。

2. 发明授权

US08003677B2 2-heteroaryl-pyrrolo[3,4-c]pyrrole derivatives and their use as SCD inhibitors 有权
标题翻译： 2-杂芳基 - 吡咯并[3,4-c]吡咯衍生物及其作为SCD抑制剂的用途
公开(公告)号：US08003677B2
公开(公告)日：2011-08-23
申请号：US12605631
申请日：2009-10-26
申请人： Gerhard Zoller , Marc Dietrich Voss , Stefanie Keil , Andreas Herling , Hans Matter
发明人： Gerhard Zoller , Marc Dietrich Voss , Stefanie Keil , Andreas Herling , Hans Matter
IPC分类号： A61K31/426
CPC分类号： C07D487/04
摘要： The invention relates to heterocyclic derivatives of formula I wherein R, R1, A, B, D, M, L and n are as defined herein, or their physiologically compatible salts, their pharmaceutical compositions and their uses as SCD1 inhibitors.
摘要翻译：本发明涉及式I的杂环衍生物，其中R，R 1，A，B，D，M，L和n如本文所定义，或其生理上相容的盐，其药物组合物及其作为SCD1抑制剂的用途。

3. 发明授权

US08673917B2 2-heteroaryl-pyrrolo [3,4-C]pyrrole derivatives, and use thereof as SCD inhibitors 有权
标题翻译： 2-杂芳基 - 吡咯并[3,4-C]吡咯衍生物及其作为SCD抑制剂的用途
公开(公告)号：US08673917B2
公开(公告)日：2014-03-18
申请号：US13063088
申请日：2009-09-02
申请人： Gerhard Zoller , Marc Dietrich Voss , Hans Matter , Andreas Herling
发明人： Gerhard Zoller , Marc Dietrich Voss , Hans Matter , Andreas Herling
IPC分类号： C07D401/14 , A61K31/4402 , A61K31/501 , A61P3/00 , A61P3/04 , A61P3/10 , A61P9/00
CPC分类号： C07D487/04
摘要： 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.
摘要翻译：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。

4. 发明申请

US20120028986A1 2-HETEROARYL-PYRROLO [3,4-C]PYRROLE DERIVATIVES, AND USE THEREOF AS SCD INHIBITORS 有权
标题翻译： 2-异丙基 - 吡咯并[3,4-C]吡咯烷酮衍生物及其作为SCD抑制剂的用途
公开(公告)号：US20120028986A1
公开(公告)日：2012-02-02
申请号：US13063088
申请日：2009-09-02
申请人： Gerhard Zoller , Marc Dietrich Voss , Hans Matter , Andreas Herling
发明人： Gerhard Zoller , Marc Dietrich Voss , Hans Matter , Andreas Herling
IPC分类号： A61K31/501 , A61K31/4439 , A61P3/06 , A61P9/10 , A61P35/00 , A61P1/04 , A61P29/00 , A61P25/16 , A61P25/28 , A61P17/10 , A61P17/00 , A61P31/20 , A61P3/04 , A61P11/06 , A61P19/02 , A61P19/06 , A61P31/12 , A61P21/00 , C07D487/04
CPC分类号： C07D487/04
摘要： 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.
摘要翻译：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。

5. 发明授权

US07067665B2 Oxybenzamide derivatives useful for inhibiting factor Xa or Vlla 失效
标题翻译：用于抑制因子Xa或Vlla的氧苯甲酰胺衍生物
公开(公告)号：US07067665B2
公开(公告)日：2006-06-27
申请号：US11039107
申请日：2005-01-19
申请人： Marc Nazare , David William Will , Anuschirwan Peyman , Hans Matter , Gerhard Zoller , Uwe Gerlach
发明人： Marc Nazare , David William Will , Anuschirwan Peyman , Hans Matter , Gerhard Zoller , Uwe Gerlach
IPC分类号： C07D401/04 , A61K31/505
CPC分类号： 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
摘要： 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.
摘要翻译：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。

6. 发明申请

US20050165058A1 Oxybenzamide derivatives useful for inhibiting factor Xa or Vlla 失效
标题翻译：用于抑制因子Xa或Vlla的氧苯甲酰胺衍生物
公开(公告)号：US20050165058A1
公开(公告)日：2005-07-28
申请号：US11039107
申请日：2005-01-19
申请人： Marc Nazare , David Will , Anuschirwan Peyman , Hans Matter , Gerhard Zoller , Uwe Gerlach
发明人： Marc Nazare , David Will , Anuschirwan Peyman , Hans Matter , Gerhard Zoller , Uwe Gerlach
IPC分类号： 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 , C07D41/14
CPC分类号： 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
摘要： 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.
摘要翻译：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。

7. 发明授权

US06395737B1 Malonic acid derivatives, processes for their preparation, for their use and pharmaceutical compositions containing them 有权
标题翻译：丙二酸衍生物，其制备方法，用途及含有它们的药物组合物
公开(公告)号：US06395737B1
公开(公告)日：2002-05-28
申请号：US09473053
申请日：1999-12-28
申请人： Elisabeth Defossa , Uwe Heinelt , Otmar Klingler , Gerhard Zoller , Hans Matter , Fahad A. Al-Obeidi , Armin Walser , Peter Wildgoose
发明人： Elisabeth Defossa , Uwe Heinelt , Otmar Klingler , Gerhard Zoller , Hans Matter , Fahad A. Al-Obeidi , Armin Walser , Peter Wildgoose
IPC分类号： A61K31165
CPC分类号： C07C257/18 , C07C279/14
摘要： New compounds for the inhibition of blood clotting proteins, and more particularly, to malonic acid derivatives of the formula I, wherein R(1), R(2), R(3), R(4), R(5), and R(6) have the meanings indicated in the claims. The compounds of formula I are inhibitors of the blood clotting enzyme factor Xa. Processes for the preparation of the compounds of formula I, methods of inhibiting factor Xa activity and of inhibiting blood clotting, use of the compounds of formula I in the treatment and prophylaxis of diseases, which can be treated or prevented by the inhibition of factor Xa activity such as thromboembolic diseases, and use of the compounds of formula I in the preparation of medicaments to be applied in such diseases. Compositions containing a compound of formula I in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula I together with pharmaceutically acceptable carrier substances and auxiliary substances.
摘要翻译：用于抑制血液凝固蛋白质的新化合物，更具体地，涉及式I的丙二酸衍生物，其中R（1），R（2），R（3），R（4），R（5）和 R（6）具有权利要求中所示的含义。式I化合物是凝血酶因子Xa的抑制剂。用于制备式I化合物的方法，抑制因子Xa活性和抑制血液凝固的方法，式I化合物在治疗和预防疾病中的用途，其可以通过抑制因子Xa来治疗或预防活性如血栓栓塞性疾病，以及式I化合物在制备用于这些疾病的药物中的应用。含有式I化合物的组合物与惰性载体混合或以其它方式结合，特别是含有式I化合物的药物组合物以及药学上可接受的载体物质和辅助物质。

8. 发明授权

US06500803B1 Factor VIIa inhibitors 有权
标题翻译：因子VIIa抑制剂
公开(公告)号：US06500803B1
公开(公告)日：2002-12-31
申请号：US09588651
申请日：2000-06-07
申请人： Otmar Klingler , Manfred Schudok , Gerhard Zoller , Uwe Heinelt , Elisabeth Defossa , Hans Matter , Pavel Safar
发明人： Otmar Klingler , Manfred Schudok , Gerhard Zoller , Uwe Heinelt , Elisabeth Defossa , Hans Matter , Pavel Safar
IPC分类号： A61K3805
CPC分类号： C07K5/06086 , A61K38/00
摘要： The present invention relates to compounds of formula I, in which R1, R2, R91, R92, R93, R94, R95, R96, R97, r, s, and t have the meanings indicated in the claims. Compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of thromboembolic diseases or 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 conditions in which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
摘要翻译：本发明涉及式Ⅰ化合物，其中R1，R2，R91，R92，R93，R94，R95，R96，R97，r，s和t具有权利要求中所示的含义。式I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血栓栓塞性疾病或再狭窄。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活性的条件下或用于治疗或预防预期因子VIIa的抑制的病症。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。

9. 发明授权

US06337344B1 Indole derivatives as inhibitors or factor Xa 有权
标题翻译：吲哚衍生物作为抑制剂或因子Xa
公开(公告)号：US06337344B1
公开(公告)日：2002-01-08
申请号：US09582344
申请日：2000-08-14
申请人： Elisabeth Defossa , Uwe Heinelt , Otmar Klingler , Gerhard Zoller , Fahad A. Al-Obeidi , Armin Walser , Peter Wildgoose , Hans Matter
发明人： Elisabeth Defossa , Uwe Heinelt , Otmar Klingler , Gerhard Zoller , Fahad A. Al-Obeidi , Armin Walser , Peter Wildgoose , Hans Matter
IPC分类号： A61K3144
CPC分类号： C07D401/06 , C07D209/42 , C07D401/12 , C07D403/10 , C07D471/04
摘要： The present invention relates to the inhibition of blood clotting proteins, and more particularly, to indole derivatives of formula (I), in which R1a, R1b, R1c R1d, R2, R3, R4 and A are defined as indicated in the claims. The compounds of formula (I) are inhibitors of the blood clotting enzyme factor Xa. 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 use of the compounds of formula (I) in the treatment and prophylaxis of diseases which can be cured or prevented by the inhibition of factor Xa activity such as thromboembolic diseases, and to the use of the compounds of formula (I) in the preparation of medicaments to be applied in such diseases. The invention further relates to compositions containing a compound of formula (I) in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula (I) together with pharmaceutically acceptable carrier substances and/or auxiliary substances.
摘要翻译：本发明涉及抑制血液凝固蛋白质，更具体地说，涉及式（I）的吲哚衍生物，其中R1a，R1b，R1c R1d，R2，R3，R4和A如权利要求中所示定义。式（I）的化合物是凝血酶因子Xa的抑制剂。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，使用式（I）化合物治疗和预防可以通过抑制诸如血栓栓塞性疾病的因子Xa活性而被治愈或预防，以及式（I）化合物在制备用于这些疾病的药物中的用途。本发明还涉及包含与惰性载体混合或以其它方式结合的式（I）化合物的组合物，特别是含有式（I）化合物与药学上可接受的载体物质和/或辅助物质的药物组合物。

10. 发明授权

US07435747B2 Guanidine and amidine derivatives as factor Xa inhibitors 失效
标题翻译：胍和脒衍生物作为因子Xa抑制剂
公开(公告)号：US07435747B2
公开(公告)日：2008-10-14
申请号：US10886312
申请日：2004-07-07
申请人： Anuschirwan Peyman , David William Will , Uwe Gerlach , Marc Nazaré , Gerhard Zoller , Hans-Peter Nestler , Hans Matter , Fahad Al-Obeidi
发明人： Anuschirwan Peyman , David William Will , Uwe Gerlach , Marc Nazaré , Gerhard Zoller , Hans-Peter Nestler , Hans Matter , Fahad Al-Obeidi
IPC分类号： A61K31/445 , C07D211/26
CPC分类号： C07D401/12 , C07D211/26 , C07D211/34
摘要： 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.
摘要翻译：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。

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