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1. 发明申请

WO2014135674A1 SUBSTITUTED CHROMAN-6-YLOXY-CYCLOALKANES AND THEIR USE AS PHARMACEUTICALS 审中-公开
标题翻译：取代的色氨酸-60-环糊精及其作为药物的用途
公开(公告)号：WO2014135674A1
公开(公告)日：2014-09-12
申请号：PCT/EP2014/054417
申请日：2014-03-07
申请人： SANOFI
发明人： CZECHTIZKY, Werngard , WESTON, John , RACKELMANN, Nils , KRAFT, Volker , ARNDT, Petra , WIRTH, Klaus , GOEGELEIN, Heinz , RITZELER, Olaf
IPC分类号： C07D311/60 , C07D405/12 , C07D407/12 , C07D407/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07F9/09 , A61K31/353 , A61P9/00
CPC分类号： C07D311/60 , C07D405/12 , C07D407/12 , C07D407/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07F9/65522
摘要： The present invention relates to substituted chroman-6-yloxy-cycloalkanes of the formula (I) in which Ar, R1 to R4, p and q are as defined in the claims. The compounds of the formula (I) are inhibitors of the sodium-calcium exchanger (NCX), especially of the sodium-calcium exchanger of subtype 1 (NCX1), and are suitable for the treatment of diverse disorders in which intracellular calcium homeostasis is disturbed, such as arrhythmias, heart failure and stroke. 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.
摘要翻译：本发明涉及式（I）的取代的苯并二氢吡喃-6-基氧基 - 环烷烃，其中Ar，R 1至R 4，p和q如权利要求中所定义。式（I）的化合物是钠 - 钙交换剂（NCX）的抑制剂，特别是亚型1型（NCX1）的钠 - 钙交换剂的抑制剂，并且适用于治疗细胞内钙稳态受到干扰的多种疾病，如心律失常，心力衰竭和中风。本发明还涉及制备式（I）化合物，其作为药物的用途以及包含它们的药物组合物的方法。

2. 发明申请

WO2009052062A1 SUBSTITUTED N-PHENYL-BIPYRROLIDINE CARBOXAMIDES AND THERAPEUTIC USE THEREOF 审中-公开
标题翻译：取代的N-苯甲酰基吡啶羧酸酯及其治疗用途
公开(公告)号：WO2009052062A1
公开(公告)日：2009-04-23
申请号：PCT/US2008/079757
申请日：2008-10-14
申请人： SANOFI-AVENTIS , CZECHTIZKY, Werngard , GAO, Zhongli , HURST, William J. , SCHWINK, Lothar , STENGELIN, Siegfried
发明人： CZECHTIZKY, Werngard , GAO, Zhongli , HURST, William J. , SCHWINK, Lothar , STENGELIN, Siegfried
IPC分类号： C07D207/06 , C07D401/14 , C07D403/12 , C07D405/12 , C07D413/12 , A61K31/4025 , A61P25/00
CPC分类号： C07D413/12 , C07D207/06 , C07D401/14 , C07D403/12 , C07D405/12
摘要： The present invention discloses and claims a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I) as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted N-phenyl-bipyrrolidine carboxamides and intermediates therefor.
摘要翻译：本发明公开并要求一系列如本文所述的式（I）的取代的N-苯基 - 联吡咯烷甲酰胺。更具体地，本发明的化合物是H3受体的调节剂，因此可用作药剂，特别是用于治疗和/或预防由H3受体调节的各种疾病，包括与中枢神经系统相关的疾病。此外，本发明还公开了制备取代的N-苯基 - 联吡咯烷甲酰胺及其中间体的方法。

3. 发明申请

WO2009052068A1 SUBSTITUTED N-PHENYL-BIPYRROLIDINE UREAS AND THERAPEUTIC USE THEREOF 审中-公开
标题翻译：取代的N-苯甲酰基吡咯烷酮及其治疗方法
公开(公告)号：WO2009052068A1
公开(公告)日：2009-04-23
申请号：PCT/US2008/079763
申请日：2008-10-14
申请人： SANOFI-AVENTIS , CZECHTIZKY, Werngard , GAO, Zhongli , HURST, William J. , SCHWINK, Lothar , STENGELIN, Siegfried
发明人： CZECHTIZKY, Werngard , GAO, Zhongli , HURST, William J. , SCHWINK, Lothar , STENGELIN, Siegfried
IPC分类号： C07D207/06 , C07D403/12 , C07D409/12 , A61K31/4025 , A61P25/00
CPC分类号： C07D207/06 , C07D403/12 , C07D409/12
摘要： The present invention discloses and claims a series of substituted N-phenyl-bipyrrolidine ureas of formula (I) as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted N-phenyl-bipyrrolidine ureas and intermediates therefor.
摘要翻译：本发明公开并要求一系列如本文所述的式（I）的取代的N-苯基 - 联吡咯烷脲。更具体地，本发明的化合物是H3受体的调节剂，因此可用作药剂，特别是用于治疗和/或预防由H3受体调节的各种疾病，包括与中枢神经系统相关的疾病。此外，本发明还公开了制备取代的N-苯基 - 联吡咯烷脲及其中间体的方法。

4. 发明申请

WO2008067909A2 HARNSTOFF- UND SULFAMIDDERIVATE ALS INHIBITOREN VON TAFIA 审中-公开
标题翻译：脲和磺酰胺衍生物作为对TAFIa抑制剂的
公开(公告)号：WO2008067909A2
公开(公告)日：2008-06-12
申请号：PCT/EP2007/010101
申请日：2007-11-22
申请人： SANOFI-AVENTIS , KALLUS, Christopher , BROENSTRUP, Mark , CZECHTIZKY, Werngard , EVERS, Andreas , FOLLMANN, Markus , HALLAND, Nis , SCHREUDER, Herman
发明人： KALLUS, Christopher , BROENSTRUP, Mark , CZECHTIZKY, Werngard , EVERS, Andreas , FOLLMANN, Markus , HALLAND, Nis , SCHREUDER, Herman
IPC分类号： A61K31/17 , A61K31/36 , A61K31/381 , A61K31/40 , A61K31/4164 , A61K31/4184 , A61K31/4402 , A61K31/4409 , A61P9/10
CPC分类号： A61K31/4164 , A61K31/17 , A61K31/18 , A61K31/198 , A61K31/223 , A61K31/36 , A61K31/381 , A61K31/40 , A61K31/4184 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4453 , A61K31/4465 , A61K45/06 , C07C307/06 , C07D207/06 , C07D209/20 , C07D211/34 , C07D211/58 , C07D213/40 , C07D213/55 , C07D213/73 , C07D235/14 , C07D261/08 , C07D295/185 , C07D317/58 , C07D333/20 , C07D487/08 , A61K2300/00
摘要： Die Erfindung betrifft Verbindungen der Formel (I) die Inhibitoren von aktivierter Thrombin-aktivierbarer Fibrinolyse Inhibitor sind. Die Verbindungen der Formel (I) eignen sich zur Herstellung von Arzneimitteln zur Prophylaxe, Sekundärprevention und Therapie von einer oder mehrerer Erkrankungen, die mit Thrombosen, Embolien, Hyperkoagulabilität oder fibrotischen Veränderungen einhergehen.
摘要翻译：本发明涉及式（I）的化合物是活化的凝血酶激活纤维蛋白溶解抑制剂是。式（I）的化合物是适用于生产药物用于预防，二级预防和治疗与血栓形成，栓塞，高凝状态或纤维化改变相关联的一种或多种疾病。

5. 发明申请

WO2013171318A1 BENZO[1,3]DIOXINE DERIVATIVES AND THEIR USE AS LPAR5 ANTAGONISTS 审中-公开
标题翻译：苯并[1,3]二氧化物衍生物及其作为LPAR5拮抗剂的用途
公开(公告)号：WO2013171318A1
公开(公告)日：2013-11-21
申请号：PCT/EP2013/060172
申请日：2013-05-16
申请人： SANOFI
发明人： NAZARÉ, Marc , KOZIAN, Detlef , BOSSART, Martin , CZECHTIZKY, Werngard , EVERS, Andreas
IPC分类号： C07D319/08 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D413/04 , A61K31/357 , A61K31/4025 , A61K31/41 , A61K31/4433 , A61P9/00
CPC分类号： C07D319/08 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D413/04
摘要： The present invention relates to compounds of the formula (I), wherein the residues A, R 1 to R 5 , Z 1 and Z 2 have the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmacologically active compounds for use in the treatment of diverse disorders, for example cardiovascular disorders like thromboembolic diseases or restenoses. The compounds of the invention are effective antagonists of the platelet LPA receptor LPAR5 (GPR92) and can in general be applied in conditions in which an undesired activation of the platelet LPA receptor LPAR5, the mast cell LPA receptor LPAR5 or the microglia cell LPA receptor LPAR5 is present or for the cure or prevention of which an inhibition of the platelet, mast cell or microglia cell LPA receptor LPAR5 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 medicaments, and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及式（I）化合物，其中残基A，R1至R5，Z1和Z2具有权利要求中所示的含义。式（I）的化合物是用于治疗各种疾病例如血栓栓塞性疾病或再狭窄的心血管疾病的有价值的药理活性化合物。本发明的化合物是血小板LPA受体LPAR5（GPR92）的有效拮抗剂，通常可以在血小板LPA受体LPAR5，肥大细胞LPA受体LPAR5或小神经胶质细胞LPA受体LPAR5的不希望的活化存在或用于治疗或预防血小板，肥大细胞或小胶质细胞LPA受体LPAR5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组合物。

6. 发明申请

WO2013037724A1 SUBSTITUTED 2-(CHROMAN-6-YLOXY)-THIAZOLES AND THEIR USE AS PHARMACEUTICALS 审中-公开
标题翻译：取代的2-（CHROMAN-6-YLOXY）-THIAZOLES及其作为药物的用途
公开(公告)号：WO2013037724A1
公开(公告)日：2013-03-21
申请号：PCT/EP2012/067622
申请日：2012-09-10
申请人： SANOFI , CZECHTIZKY, Werngard , WESTON, John , RACKELMANN, Nils , PODESCHWA, Michael , ARNDT, Petra , WIRTH, Klaus , GOEGELEIN, Heinz , RITZELER, Olaf , KRAFT, Volker , BELLEVERGUE, Patrice , McCort, Gary
发明人： CZECHTIZKY, Werngard , WESTON, John , RACKELMANN, Nils , PODESCHWA, Michael , ARNDT, Petra , WIRTH, Klaus , GOEGELEIN, Heinz , RITZELER, Olaf , KRAFT, Volker , BELLEVERGUE, Patrice , McCort, Gary
IPC分类号： C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , A61K31/427 , A61P9/06 , A61P9/10
CPC分类号： C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07F9/655345
摘要： The present invention relates to substituted 2-(chroman-6-yloxy)-thiazoles of the formula I in which Ar, R2, R3 and R4 are as defined in the claims. The compounds of the formula I are inhibitors of the sodium-calcium exchanger (NCX), especially of the sodium-calcium exchanger of subtype 1 (NCX1 ), and are suitable for the treatment of diverse disorders in which intracellular calcium homeostasis is disturbed, such as arrhythmias, heart failure and stroke. 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.
摘要翻译：本发明涉及式I中的取代的2-（色满-6-基氧基） - 噻唑，其中Ar，R 2，R 3和R 4如权利要求中所定义。式I的化合物是钠 - 钙交换剂（NCX）的抑制剂，特别是亚型1型（NCX1）的钠 - 钙交换剂的抑制剂，并且适用于治疗细胞内钙稳态被扰乱的多种疾病，例如作为心律失常，心力衰竭和中风。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。

7. 发明申请

WO2013037388A1 SUBSTITUTED 2-(CHROMAN-6-YLOXY)-THIAZOLES AND THEIR USE AS PHARMACEUTICALS 审中-公开
标题翻译：取代的2-（CHROMAN-6-YLOXY）-THIAZOLES及其作为药物的用途
公开(公告)号：WO2013037388A1
公开(公告)日：2013-03-21
申请号：PCT/EP2011/065712
申请日：2011-09-12
申请人： SANOFI , CZECHTIZKY, Werngard , WESTON, John , RACKELMANN, Nils , PODESCHWA, Michael , ARNDT, Petra , WIRTH, Klaus , GOEGELEIN, Heinz , RITZELER, Olaf , KRAFT, Volker , BELLEVERGUE, Patrice , MCCORT, Gary
发明人： CZECHTIZKY, Werngard , WESTON, John , RACKELMANN, Nils , PODESCHWA, Michael , ARNDT, Petra , WIRTH, Klaus , GOEGELEIN, Heinz , RITZELER, Olaf , KRAFT, Volker , BELLEVERGUE, Patrice , MCCORT, Gary
IPC分类号： C07D417/12 , C07D417/14 , A61K31/427
CPC分类号： C07D417/12 , C07D417/14
摘要： The present invention relates to substituted 2-(chroman-6-yloxy)-thiazoles of the formula (I), in which Ar, R2, R3 and R4 are as defined in the claims. The compounds of the formula (I) are inhibitors of the sodium-calcium exchanger (NCX), especially of the sodium-calcium exchanger of subtype 1 (NCX1), and are suitable for the treatment of diverse disorders in which intracellular calcium homeostasis is disturbed, such as arrhythmias, heart failure and stroke. 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.
摘要翻译：本发明涉及式（I）的取代的2-（色满-6-基氧基） - 噻唑，其中Ar，R 2，R 3和R 4如权利要求中所定义。式（I）的化合物是钠 - 钙交换剂（NCX）的抑制剂，特别是亚型1型（NCX1）的钠 - 钙交换剂的抑制剂，并且适用于治疗细胞内钙稳态受到干扰的多种疾病，如心律失常，心力衰竭和中风。本发明还涉及制备式（I）化合物，其作为药物的用途以及包含它们的药物组合物的方法。

8. 发明申请

WO2009135590A1 ACYLAMINO-SUBSTITUTED FUSED CYCLOPENTANECARBOXYLIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS 审中-公开
标题翻译： ACYLAMINO-取代的氟化环戊烷羧酸衍生物及其作为药物的用途
公开(公告)号：WO2009135590A1
公开(公告)日：2009-11-12
申请号：PCT/EP2009/002917
申请日：2009-04-22
申请人： SANOFI-AVENTIS , SCHAEFER, Matthias , PERNERSTORFER, Josef , KADEREIT, Dieter , STROBEL, Hartmut , CZECHTIZKY, Werngard , CHEN, L., Charlie , SAFAROVA, Alena , WEICHSEL, Aleksandra , PATEK, Marcel
发明人： SCHAEFER, Matthias , PERNERSTORFER, Josef , KADEREIT, Dieter , STROBEL, Hartmut , CZECHTIZKY, Werngard , CHEN, L., Charlie , SAFAROVA, Alena , WEICHSEL, Aleksandra , PATEK, Marcel
IPC分类号： A61K31/4402 , A61K31/38 , A61K31/16 , A61P9/00 , A61P29/00 , C07D333/80 , C07D333/32 , C07C323/19 , C07C235/54 , C07C235/84 , C07C323/62 , C07D213/64 , C07D277/56
CPC分类号： C07C235/54 , A61K31/196 , A61K31/216 , A61K31/277 , A61K31/381 , A61K31/439 , A61K31/44 , A61K31/4409 , A61K31/445 , A61K31/495 , A61K31/4965 , C07C231/02 , C07C235/62 , C07C235/84 , C07C237/38 , C07C255/54 , C07C255/57 , C07C255/58 , C07C307/10 , C07C309/73 , C07C311/08 , C07C315/04 , C07C317/22 , C07C317/46 , C07C319/12 , C07C319/20 , C07C321/26 , C07C323/12 , C07C323/19 , C07C323/42 , C07C323/62 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07D207/08 , C07D207/09 , C07D207/263 , C07D209/12 , C07D209/44 , C07D211/22 , C07D213/30 , C07D213/65 , C07D213/68 , C07D213/73 , C07D213/74 , C07D213/75 , C07D213/81 , C07D213/82 , C07D221/04 , C07D231/12 , C07D233/54 , C07D233/64 , C07D233/84 , C07D235/12 , C07D235/18 , C07D241/38 , C07D249/06 , C07D261/04 , C07D261/20 , C07D263/32 , C07D271/08 , C07D277/24 , C07D277/56 , C07D285/06 , C07D295/08 , C07D295/20 , C07D305/06 , C07D307/12 , C07D309/06 , C07D319/06 , C07D319/12 , C07D319/20 , C07D333/16 , C07D333/38 , C07D333/56 , C07D333/78 , C07D413/04 , C07D417/04 , C07D453/02 , C07D471/08
摘要： The present invention relates to compounds of the formula (I), wherein A, Y, Z, R 3 to R 6 , R 20 to R 22 and R 50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA 1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, 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.
摘要翻译：本发明涉及式（I）化合物，其中A，Y，Z，R 3至R 6，R 20至R 22和R 50具有权利要求中所示的含义，其为有价值的药物活性化合物。具体来说，它们是由溶血磷脂酸（LPA）激活的内皮分化基因受体2（Edg-2，EDG2）的抑制剂，也被称为LPA1受体，可用于治疗动脉粥样硬化，心肌的疾病梗死和心力衰竭。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。

9. 发明申请

WO2009080227A3 PYRAZOLE-CARBOXAMIDE DERIVATIVES AS P2Y12 ANTAGONISTS 审中-公开
公开(公告)号：WO2009080227A3
公开(公告)日：2009-07-02
申请号：PCT/EP2008/010573
申请日：2008-12-12
申请人： SANOFI-AVENTIS , NAZARÉ, Marc , ZECH, Gernot , GOERLITZER, Jochen , JUST, Melitta , WEISS, Tilo , HESSLER, Gerhard , CZECHTIZKY, Werngard , RUF, Sven
发明人： NAZARÉ, Marc , ZECH, Gernot , GOERLITZER, Jochen , JUST, Melitta , WEISS, Tilo , HESSLER, Gerhard , CZECHTIZKY, Werngard , RUF, Sven
IPC分类号： C07D403/12 , A61K31/496 , A61P7/02
摘要： 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.

10. 发明申请

WO2013171317A1 PYRAZOLE DERIVATIVES AND THEIR USE AS LPAR5 ANTAGONISTS 审中-公开
标题翻译：吡咯衍生物及其作为LPAR5拮抗剂的用途
公开(公告)号：WO2013171317A1
公开(公告)日：2013-11-21
申请号：PCT/EP2013/060171
申请日：2013-05-16
申请人： SANOFI
发明人： NAZARÉ, Marc , KOZIAN, Detlef , EVERS, Andreas , CZECHTIZKY, Werngard
IPC分类号： C07D231/12 , C07D409/04 , A61K31/415 , A61K31/4155 , A61P7/02
CPC分类号： C07D231/12 , A61K31/415 , C07D231/56 , C07D409/04
摘要： The present invention relates to compounds of the formula (I), wherein theresidues R 1 to R 5 , V, G and M have the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmacologically active compounds for use in thetreatmentof diverse disorders, for example cardiovascular disorders like thromboembolic diseases or restenoses. The compounds of the invention are effective antagonists of the platelet LPA receptor LPAR5 (GPR92) and can in general be applied in conditions in which an undesired activation of the platelet LPA receptor LPAR5, the mast cell LPA receptor LPAR5 or the microglia cell LPA receptor LPAR5 is present or for the cure or prevention of which an inhibition of the platelet, mast cell or microglia cell LPA receptor LPAR5 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 medicaments, and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及式（I）化合物，其中残基R1至R5，V，G和M具有权利要求中所示的含义。式（I）的化合物是用于治疗多种疾病，例如心血管疾病如血栓栓塞性疾病或再狭窄的有价值的药理学活性化合物。本发明的化合物是血小板LPA受体LPAR5（GPR92）的有效拮抗剂，通常可以在血小板LPA受体LPAR5，肥大细胞LPA受体LPAR5或小神经胶质细胞LPA受体LPAR5的不希望的活化存在或用于治疗或预防血小板，肥大细胞或小胶质细胞LPA受体LPAR5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组合物。

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