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1. 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。

2. 发明申请

WO2013171316A1 PYRIDINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF CONDITIONS ASSOCIATED WITH PATHOLOGICAL THROMBUS FORMATION 审中-公开
标题翻译：吡啶衍生物及其在治疗与病理性血栓形成相关的病症中的用途
公开(公告)号：WO2013171316A1
公开(公告)日：2013-11-21
申请号：PCT/EP2013/060169
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： C07D213/30 , A61K31/4418 , A61P7/02
CPC分类号： C07D213/30
摘要： The present invention relates to compounds of the formula (I), wherein the residues R 1 to R 6 , 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 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R1至R6，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组合物。

3. 发明申请

WO2009000411A1 A TRANSITION METAL CATALYZED SYNTHESIS OF 2H-INDAZOLES 审中-公开
标题翻译： 2H-INDAZOLES的过渡金属催化合成
公开(公告)号：WO2009000411A1
公开(公告)日：2008-12-31
申请号：PCT/EP2008/004637
申请日：2008-06-11
申请人： SANOFI-AVENTIS , HALLAND, Nis , NAZARÉ, Marc , LINDENSCHMIDT, Andreas , ALONSO, Jorge , R'KYEK, Omar , URMANN, Matthias
发明人： HALLAND, Nis , NAZARÉ, Marc , LINDENSCHMIDT, Andreas , ALONSO, Jorge , R'KYEK, Omar , URMANN, Matthias
IPC分类号： C07D231/56
CPC分类号： C07D231/56
摘要： The present invention relates to a process for the regioselective synthesis of compounds of the formula (I), wherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4; Q and J have the meanings indicated in the claims. The present invention provides a direct transition metal catalyzed process to a wide variety of multifunctional 2H-indazoles or 2H-azaindazoles of the formula (I) from 2-halo-phenylacetylenes or (2-sulfonato)phenylacetylenes and monosubstituted hydrazines, useful for the production of pharmaceuticals, diagnostic agents, liquid crystals, polymers, herbicides, fungicidals, nematicidals, parasiticides, insecticides, acaricides and arthropodicides.
摘要翻译：本发明涉及一种用于区域选择性合成式（I）化合物的方法，其中R 0; R1; R2; R3; R4; R5; A1; A2; A3; A4; Q和J具有权利要求中所示的含义。本发明提供了一种直接过渡金属催化的方法，用于从2-卤代 - 苯基乙炔或（2-磺酸基）苯基乙炔和单取代的肼的多种多功能2H-吲唑或式（I）的2H-氮杂吲唑，其可用于生产药物，诊断剂，液晶，聚合物，除草剂，杀真菌剂，杀线虫剂，杀寄生虫剂，杀虫剂，杀螨剂和节肢动物杀虫剂。

4. 发明申请

WO2008009348A1 A REGIOSELECTIVE PALLADIUM CATALYZED SYNTHESIS OF BENZIMIDAZOLES AND AZABENZIMIDAZOLES 审中-公开
标题翻译：苯并咪唑和AZABENZIMIDAZOLES的选择性催化合成
公开(公告)号：WO2008009348A1
公开(公告)日：2008-01-24
申请号：PCT/EP2007/005816
申请日：2007-06-30
申请人： SANOFI-AVENTIS , ALONSO, Jorge , LINDENSCHMIDT, Andreas , NAZARÉ, Marc , HALLAND, Nis , RKYEK, Omar , URMANN, Matthias
发明人： ALONSO, Jorge , LINDENSCHMIDT, Andreas , NAZARÉ, Marc , HALLAND, Nis , RKYEK, Omar , URMANN, Matthias
IPC分类号： C07D235/10 , C07D235/12 , C07D235/08 , C07D235/02 , C07D487/04
CPC分类号： C07D235/10 , C07D235/08 , C07D235/16 , C07D401/04 , C07D471/04
摘要： The present invention relates to a process for the regioselective synthesis of compounds of the formula (I), wherein RO; R1; R2; R3; R4; R5; A1; A2; A3; A4, Q and J have the meanings indicated in the claims. The present invention provides a direct palladium catalyzed, regioselective process to a wide variety of unsymmetrical, multifunctional N -substituted benzimidazoles or azabenzimidazoles of formula (I) starting from 2-halo-nitroarenes and Λ/-substituted amides useful for the production of pharmaceuticals, diagnostic agents, liquid crystals, polymers, herbicides, fungicidals, nematicidals, parasiticides, insecticides, acaricitdes and arthropodicides.
摘要翻译：本发明涉及一种用于区域选择性合成式（I）化合物的方法，其中RO; R1; R2; R3; R4; R5; A1; A2; A3; A4，Q和J具有权利要求中所示的含义。本发明提供了直接钯催化的区域选择性方法，其可从用于制备药物的2-卤代 - 硝基芳烃和β-取代的酰胺开始，从多种不对称，多官能的式（I）的N-取代的苯并咪唑或氮杂苯并咪唑开始，诊断剂，液晶，聚合物，除草剂，杀真菌剂，杀线虫剂，杀寄生虫剂，杀虫剂，螨类和节肢动物杀虫剂。

5. 发明申请

WO2014140065A1 N-(4-(AZAINDAZOL-6-YL)-PHENYL)-SULFONAMIDES AND THEIR USE AS PHARMACEUTICALS 审中-公开
标题翻译： N-（4-（AZAINDAZOL-6-YL） - 苯基） - 磺酰胺及其作为药物的用途
公开(公告)号：WO2014140065A1
公开(公告)日：2014-09-18
申请号：PCT/EP2014/054770
申请日：2014-03-12
申请人： SANOFI
发明人： NAZARÉ, Marc , HALLAND, Nis , SCHMIDT, Friedemann , KLEEMANN, Heinz-Werner , WEISS, Tilo , SAAS, Joachim , STRUEBING, Carsten
IPC分类号： C07D471/04 , C07D487/04 , A61K31/437 , A61K31/52 , A61P9/00 , A61P19/02
CPC分类号： C07D487/04 , A61K31/4162 , C07D471/04
摘要： N-(4-(Azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals The present invention relates to N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides of the formula I, wherein Ar, n, X, Z, R1, R2 and R3 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.
摘要翻译： N-（4-（苯并恶唑-6-基） - 苯基） - 磺酰胺及其作为药物的用途本发明涉及式I的N-（4-（氮杂唑-6-基） - 苯基） - 磺酰胺，其中 Ar，n，X，Z，R 1，R 2和R 3具有权利要求中所示的含义。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学活性化合物，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。

6. 发明申请

WO2013041119A1 N-[4-(1H-PYRAZOLO[3,4-B]PYRAZIN-6-YL)-PHENYL]-SULFONAMIDES AND THEIR USE AS PHARMACEUTICALS 审中-公开
标题翻译： N- [4-（1H-吡唑并[3,4-B]吡嗪-6-基） - 苯基] - 磺酰胺及其作为药物的用途
公开(公告)号：WO2013041119A1
公开(公告)日：2013-03-28
申请号：PCT/EP2011/066220
申请日：2011-09-19
申请人： SANOFI , NAZARÉ, Marc , HALLAND, Nis , SCHMIDT, Friedemann , WEISS, Tilo , DIETZ, Uwe , HOFMEISTER, Armin
发明人： NAZARÉ, Marc , HALLAND, Nis , SCHMIDT, Friedemann , WEISS, Tilo , DIETZ, Uwe , HOFMEISTER, Armin
IPC分类号： C07D487/04 , A61K31/4985 , A61P19/02
CPC分类号： C07D487/04
摘要： 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.
摘要翻译：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学活性化合物，并且是适用于治疗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。

7. 发明申请

WO2009000413A1 A REGIOSELECTIVE COPPER CATALYZED SYNTHESIS OF BENZIMIDAZOLES AND AZABENZIMIDAZOLES 审中-公开
标题翻译：苯并咪唑和氨苄青霉素的选择性铜催化合成
公开(公告)号：WO2009000413A1
公开(公告)日：2008-12-31
申请号：PCT/EP2008/004639
申请日：2008-06-11
申请人： SANOFI-AVENTIS , ALONSO, Jorge , LINDENSCHMIDT, Andreas , NAZARÉ, Marc , URMANN, Matthias , HALLAND, Nis , R'KYEK, Omar
发明人： ALONSO, Jorge , LINDENSCHMIDT, Andreas , NAZARÉ, Marc , URMANN, Matthias , HALLAND, Nis , R'KYEK, Omar
IPC分类号： C07D235/08 , C07D235/16 , C07D235/18 , C07D401/04 , C07D471/04
CPC分类号： C07D235/08 , C07D235/16 , C07D235/18 , C07D401/04 , C07D471/04
摘要： The present invention relates to a process for the regioselective synthesis of compounds of the formula (I), wherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4; Q and J have the meanings indicated in the claims. The present invention provides a direct copper catalyzed regioselective process to a wide variety of unsymmetrical, multifunctional N /-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N /-substituted amides. The process is useful for the production of pharmaceuticals, diagnostic agents, liquid crystals, polymers, herbicides, fungicidals, nematicidals, parasiticides, insecticides, acaricides and arthropodicides.
摘要翻译：本发明涉及一种用于区域选择性合成式（I）化合物的方法，其中R 0; R1; R2; R3; R4; R5; A1; A2; A3; A4; Q和J具有权利要求中所示的含义。本发明为从2-卤代 - 硝基芳烃和N-取代的酰胺开始的多种不对称的，多官能的N-取代的苯并咪唑或式I的氮杂苯并咪唑提供直接铜催化的区域选择性方法。该方法可用于生产药物，诊断剂，液晶，聚合物，除草剂，杀真菌剂，杀线虫剂，杀寄生虫剂，杀虫剂，杀螨剂和节肢动物杀虫剂。

8. 发明申请

WO2006122661A1 HETEROARYL-CARBOXYLIC ACID (SULFAMOYL ALKYL) AMIDE - DERIVATIVES AS FACTOR XA INHIBITORS 审中-公开
标题翻译：异硫氰酸（磺酰氨基）酰胺 - 衍生物作为因子XA抑制剂
公开(公告)号：WO2006122661A1
公开(公告)日：2006-11-23
申请号：PCT/EP2006/004255
申请日：2006-05-06
申请人： SANOFI-AVENTIS DEUTSCHLAND GMBH , WAGNER, Michael , URMANN, Matthias , WEHNER, Volkmar , LORENZ, Martin , BAUER, Armin , NAZARÉ, Marc , MATTER, Hans
发明人： WAGNER, Michael , URMANN, Matthias , WEHNER, Volkmar , LORENZ, Martin , BAUER, Armin , NAZARÉ, Marc , MATTER, Hans
IPC分类号： C07D409/12 , A61K31/4535 , A61P7/02 , C07D409/14 , C07D333/38 , C07D405/12 , C07D211/58 , C07D401/12 , C07D413/14 , C07D417/14 , C07D419/14
CPC分类号： C07D211/58 , C07D333/38 , C07D401/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D419/14
摘要： The present invention relates to compounds of the Formula (I), in which R1; R2; R3; V; G1 and G2 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, and can in general be applied in conditions in which an undesired activity of factor Xa is present or for the cure or prevention of which an inhibition of factor Xa 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）的化合物，其中R 1; R2; R3; V; G1和G2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的可逆抑制剂，并且通常可以在其中存在不需要的因子Xa的活性或用于治疗或预防因子Xa的抑制的条件下使用。本发明还涉及式（I）化合物的制备方法，其用途，特别是药物中的活性成分，以及包含它们的药物制剂。

9. 发明申请

WO2014037394A1 FLUORESCENCE-LABELLED FATTY ACIDS AND USES THEREOF 审中-公开
标题翻译：荧光标记的脂肪酸及其用途
公开(公告)号：WO2014037394A1
公开(公告)日：2014-03-13
申请号：PCT/EP2013/068275
申请日：2013-09-04
申请人： SANOFI
发明人： PETRY, Stefan , NAZARÉ, Marc , SCHMIDT, Thorsten , MATTER, Hans
IPC分类号： G01N33/58 , G01N33/92
CPC分类号： G01N33/582 , G01N33/92 , G01N2405/00 , G01N2500/00
摘要： The present invention relates to a composition comprising (i) a fluorescent-labelled fatty acid and (ii) a fatty acid binding compound, wherein (a) the fatty acid component of the fluorescent- labelled fatty acid binds the fatty acid binding compound and (b) the fluorescent component of the fluorescent-labelled fatty acid and the fatty acid binding compound interact to elicit FRET (Förster resonance energy transfer) effects. Moreover, the invention is directed to a method for identifying and/or characterizing a compound of interest by contacting a fluorescent-labelled fatty acid with a fatty acid binding compound under conditions that allow for binding and for FRET (Förster resonance energy transfer) effects, and then contacting the fluorescent-labelled fatty acid bound to the fatty acid binding compound with a compound of interest and determining the change in fluorescence. In addition, the invention pertains to corresponding kits of parts and uses of the compositions and methods.
摘要翻译：本发明涉及包含（i）荧光标记的脂肪酸和（ii）脂肪酸结合化合物的组合物，其中（a）荧光标记的脂肪酸的脂肪酸组分结合脂肪酸结合化合物和（ b）荧光标记的脂肪酸和脂肪酸结合化合物的荧光组分相互作用以引发FRET（Förster共振能量转移）效应。此外，本发明涉及通过在允许结合和FRET（Förster共振能量转移）效应的条件下使荧光标记的脂肪酸与脂肪酸结合化合物接触来鉴定和/或表征目的化合物的方法，然后将与脂肪酸结合化合物结合的荧光标记的脂肪酸与感兴趣的化合物接触，并确定荧光的变化。此外，本发明涉及组合物和方法的相应的部件和用途的试剂盒。

10. 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。

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