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1. 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。

2. 发明申请

US20050143419A1 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：US20050143419A1
公开(公告)日：2005-06-30
申请号：US10886312
申请日：2004-07-07
申请人： Anuschirwan Peyman , David Will , Uwe Gerlach , Marc Nazare , Gerhard Zoller , Hans-Peter Nestler , Hans Matter , Fahad Al-Obeidi
发明人： Anuschirwan Peyman , David Will , Uwe Gerlach , Marc Nazare , Gerhard Zoller , Hans-Peter Nestler , Hans Matter , Fahad Al-Obeidi
IPC分类号： A61K31/445 , A61K31/4545 , A61P7/02 , A61P43/00 , C07D211/26 , C07D211/34 , C07D401/12 , C07D413/02 , A61K31/4245 , A61K31/4439 , A61K31/454
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。

3. 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。

4. 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。

5. 发明授权

US06953857B2 Oxybenzamide derivatives useful for inhibiting factor Xa or viia 失效
标题翻译：用于抑制因子Xa或vii的氧苯甲酰胺衍生物
公开(公告)号：US06953857B2
公开(公告)日：2005-10-11
申请号：US10023933
申请日：2001-12-21
申请人： Marc Nazaré , David William Will , Anuschirwan Peyman , Hans Matter , Gerhard Zoller , Uwe Gerlach
发明人： Marc Nazaré , David William 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 , C07D211/06
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

US20050009828A1 Azaindole-derivatives as factor Xa inhibitors 有权
标题翻译： Azaindole衍生物作为因子Xa抑制剂
公开(公告)号：US20050009828A1
公开(公告)日：2005-01-13
申请号：US10849089
申请日：2004-05-19
申请人： Marc Nazare , Volkmar Wehner , David Will , Kurt Ritter , Matthias Urmann , Hans Matter
发明人： Marc Nazare , Volkmar Wehner , David Will , Kurt Ritter , Matthias Urmann , Hans Matter
IPC分类号： C07D471/04 , A61K31/525 , A61K31/517 , A61K31/52
CPC分类号： C07D471/04
摘要： The present invention relates to compounds of the formula I wherein R0, R1, R2, R3, 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.
摘要翻译：本发明涉及式I化合物，其中R 0，R 1，R 2，R 3，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。

7. 发明申请

US20050043302A1 New indole derivatives as factor Xa inhibitors 审中-公开
标题翻译：新的吲哚衍生物作为因子Xa抑制剂
公开(公告)号：US20050043302A1
公开(公告)日：2005-02-24
申请号：US10926909
申请日：2004-08-26
申请人： Marc Nazare , Melanie Essrich , David Will , Hans Matter , Kurt Ritter , Volkmar Wehner
发明人： Marc Nazare , Melanie Essrich , David Will , Hans Matter , Kurt Ritter , Volkmar Wehner
IPC分类号： A61K31/404 , A61K31/405 , A61K31/422 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4725 , A61K31/496 , A61K31/506 , A61K31/517 , A61P7/02 , A61P9/00 , A61P9/08 , A61P9/10 , A61P29/00 , A61P43/00 , C07D209/22 , C07D209/42 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/14 , C07D413/14 , C07D417/14 , A61K31/541 , A61K31/4709 , A61K31/502 , A61K31/5377
CPC分类号： C07D413/14 , C04B35/632 , C07D209/22 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/14 , C07D417/14
摘要： The present invention relates to compounds of formula I, in which R0; R1; R2; R3; R4; R5; R6; R7; Q; V, G and M have the meanings indicated in the claims. The 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 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 Vila is indicated. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, in particular as pharmaceuticals for treating the foregoing conditions, and pharmaceutical preparations comprising them.
摘要翻译：本发明涉及式I化合物，其中R 0; R 1; R 2; R 3; R 4; R 5; R 6; R 7; 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。本发明还涉及制备式I化合物的方法，其用途，特别是作为用于治疗上述病症的药物，以及包含它们的药物制剂。

8. 发明授权

US07465806B2 Pyrrole-derivatives as factor Xa inhibitors 有权
标题翻译：吡咯衍生物作为因子Xa抑制剂
公开(公告)号：US07465806B2
公开(公告)日：2008-12-16
申请号：US11467277
申请日：2006-08-25
申请人： Armin Bauer , Michael Wagner , Marc Nazare , Volkmar Wehner , Matthias Urmann , Hans Matter
发明人： Armin Bauer , Michael Wagner , Marc Nazare , Volkmar Wehner , Matthias Urmann , Hans Matter
IPC分类号： C07D261/06 , C07D207/32
CPC分类号： C07D401/12 , C07D401/14 , C07D413/14
摘要： 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.
摘要翻译：本发明涉及式I和Ia的化合物，其中R 0; R1; 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。

9. 发明申请

US20080280946A1 Azaindole-Derivatives As Factor Xa Inhibitors 审中-公开
标题翻译：阿魏酸衍生物作为因子Xa抑制剂
公开(公告)号：US20080280946A1
公开(公告)日：2008-11-13
申请号：US11934177
申请日：2007-11-02
申请人： Marc NAZARE , Volkmar Wehner , David William Will , Kurt Ritter , Matthias Urmann , Hans Matter
发明人： Marc NAZARE , Volkmar Wehner , David William Will , Kurt Ritter , Matthias Urmann , Hans Matter
IPC分类号： A61K31/437 , C07D471/02 , A61P7/00 , A61P9/00
CPC分类号： C07D471/04
摘要： Indazole-derivatives as factor Xa inhibitors The present invention relates to compounds of the formula I wherein R0, R1, R2, R3, 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 VIa 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：作为因子Xa抑制剂的吲唑衍生物本发明涉及式I化合物，其中R 0，R 1，R 2，R 2， SEQ ID NO 3，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VIa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。

10. 发明授权

US07429581B2 Pyrazole-derivatives as factor Xa inhibitors 有权
标题翻译：吡唑衍生物作为因子Xa抑制剂
公开(公告)号：US07429581B2
公开(公告)日：2008-09-30
申请号：US10744744
申请日：2003-12-23
申请人： Marc Nazare , Volkmar Wehner , David W. Will , Hans Matter
发明人： Marc Nazare , Volkmar Wehner , David W. Will , Hans Matter
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/496
CPC分类号： C07D413/14 , C07D401/12 , C07D401/14 , C07D409/14 , C07D417/14
摘要： The present invention is directed to a compound of formula I, in which R0; R1; R2; R3; R4; Q; V, G and M have the meanings indicated below. The compound of formula I is a pharmacologically active compound. It exhibits a strong anti-thrombotic effect and is suitable, for example, for the therapy and prophylaxis of a cardio-vascular disorder like a thromboembolic disease or restenosis. It is a reversible inhibitor 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 is directed to a process for the preparation of the compound of formula I, and pharmaceutical preparation comprising it.
摘要翻译：本发明涉及式I化合物，其中R 0为0或0; R＆lt; 1＆gt;; R 2; 3＆lt; 3＆gt; R 4; Q; V，G和M具有以下含义。式I化合物是药理活性化合物。它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，并且通常可以在其中存在因子Xa和/或因子VIIa的不希望的活性或对于治疗或预防因素Xa和/或因子VIIa的抑制。本发明还涉及制备式I化合物的方法和包含其的药物制剂。

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