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1. 发明授权

US09051289B2 Process and intermediates for preparing GPR40 agonists 有权
标题翻译：制备GPR40激动剂的方法和中间体
公开(公告)号：US09051289B2
公开(公告)日：2015-06-09
申请号：US14494631
申请日：2014-09-24
申请人： Georg Dahmann , Holger Wagner , Matthias Eckhardt , Markus Frank , Marco Santagostino , Juergen Schnaubelt , Uwe Stertz , Thorsten Pachur
发明人： Georg Dahmann , Holger Wagner , Matthias Eckhardt , Markus Frank , Marco Santagostino , Juergen Schnaubelt , Uwe Stertz , Thorsten Pachur
IPC分类号： C07D307/80 , C07D407/12 , C07D405/12 , C07D513/04
CPC分类号： C07D307/80 , C07D405/12 , C07D407/12 , C07D513/04
摘要： The present invention relates to compounds of formula I wherein RS denotes F or CF3, Ra denotes H or C1-4-alkyl and Z denotes a leaving group or an optionally substituted or protected hydroxyl group, suitable as intermediates in the synthesis of indanyloxydihydrobenzofuranylacetic acids, which are GPR40 agonists, to a process for preparing these intermediates and to the process for preparing the GPR40 agonists making use of an asymmetric catalytic hydrogenation reaction in the presence of a transition metal catalyst and a chiral auxiliary.
摘要翻译：本发明涉及式I化合物，其中RS表示F或CF 3，R a表示H或C 1-4 - 烷基，Z表示离去基团或任选取代或保护的羟基，适合于合成二氢氧化二氢苯并呋喃基乙酸的中间体，其是GPR40激动剂，涉及制备这些中间体的方法和制备在过渡金属催化剂和手性助剂存在下使用不对称催化氢化反应的GPR40激动剂的方法。

2. 发明授权

US08742115B2 Co-crystals and salts of CCR3-inhibitors 有权
标题翻译： CCR3抑制剂的共晶和盐
公开(公告)号：US08742115B2
公开(公告)日：2014-06-03
申请号：US13267417
申请日：2011-10-06
申请人： Markus Frank , Hans Haeberle , Manuel Henry , Thorsten Pachur , Marco Santagostino , Uwe Stertz , Thomas Trebing , Ulrike Werthmann
发明人： Markus Frank , Hans Haeberle , Manuel Henry , Thorsten Pachur , Marco Santagostino , Uwe Stertz , Thomas Trebing , Ulrike Werthmann
IPC分类号： A61K31/445 , C07D211/68
CPC分类号： C07D401/14 , C07D211/58 , C07D213/81 , C07D401/04
摘要： This invention relates to co-crystals and salts of CCR3 inhibitors of formula 1, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases related with the CCR3-receptor.
摘要翻译：本发明涉及式1的CCR3抑制剂的共晶和盐，含有它的药物组合物及其用作治疗和/或预防与CCR3受体有关的疾病的药剂的方法。

3. 发明申请

US20120264729A1 CO-CRYSTALS AND SALTS OF CCR3-INHIBITORS 有权
标题翻译： CCR3抑制剂的CO晶体和盐
公开(公告)号：US20120264729A1
公开(公告)日：2012-10-18
申请号：US13267417
申请日：2011-10-06
申请人： Markus Frank , Hans Haeberle , Manuel Henry , Thorsten Pachur , Marco Santagostino , Uwe Stertz , Thomas Trebing , Ulrike Werthmann
发明人： Markus Frank , Hans Haeberle , Manuel Henry , Thorsten Pachur , Marco Santagostino , Uwe Stertz , Thomas Trebing , Ulrike Werthmann
IPC分类号： A61K31/4545 , C07D413/14 , A61K31/5377 , C07D213/81 , C07D211/58 , C07D401/04 , A61P29/00 , A61P31/00 , A61P37/00 , A61P11/06 , A61P37/08 , A61P11/00 , A61P31/12 , A61P9/10 , A61P27/02 , C07D401/14
CPC分类号： C07D401/14 , C07D211/58 , C07D213/81 , C07D401/04
摘要： This invention relates to co-crystals and salts of CCR3 inhibitors of formula 1, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases related with the CCR3-receptor.
摘要翻译：本发明涉及式1的CCR3抑制剂的共晶和盐，含有它的药物组合物及其用作治疗和/或预防与CCR3受体有关的疾病的药剂的方法。

4. 发明授权

US07528129B2 CGRP-antagonists, process for preparing them and their use as pharmaceutical compositions 有权
公开(公告)号：US07528129B2
公开(公告)日：2009-05-05
申请号：US11277177
申请日：2006-03-22
申请人： Stephan Georg Mueller , Klaus Rudolf , Philipp Lustenberger , Dirk Stenkamp , Marco Santagostino , Fabio Paleari , Gerhard Schaenzle , Kirsten Arndt , Henri Doods
发明人： Stephan Georg Mueller , Klaus Rudolf , Philipp Lustenberger , Dirk Stenkamp , Marco Santagostino , Fabio Paleari , Gerhard Schaenzle , Kirsten Arndt , Henri Doods
IPC分类号： C07D401/14 , C07D413/04 , A61K31/551 , A61P25/06
CPC分类号： C07D405/12 , C07D405/14 , C07D413/14
摘要： The present invention relates to the CGRP-antagonists of general formula I wherein R1, R2, R3, R4 and X are defined as in claim 1, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates, mixtures and salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, as well as those compounds of general formula I in which one or more hydrogen atoms are replaced by deuterium, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.

5. 发明授权

US07423146B2 Process for the manufacturing of pharmaceutically active 3,1-benzoxazine-2-ones 失效
标题翻译：制备药学活性3,1-苯并恶嗪-2-酮的方法
公开(公告)号：US07423146B2
公开(公告)日：2008-09-09
申请号：US11586237
申请日：2006-10-25
申请人： Marco Santagostino , Werner Rall , Rainer Soyka
发明人： Marco Santagostino , Werner Rall , Rainer Soyka
IPC分类号： C07D265/18
CPC分类号： C07D265/18 , Y02P20/55
摘要： A process for making a compound of formula 1 or a salt thereof, wherein: R1 and R2 are each independently H, halogen, or C1-4-alkyl, or R1 and R2 together are C1-6-alkylene; and R3 is H, halogen, OH, C1-4-alkyl, or O—C1-4-alkyl, the process comprising: (a) reacting a compound of formula 6 wherein R4 is benzyl, diphenylmethyl, or trityl, each optionally substituted at, if available, an aryl group or an aliphatic carbon atom, with a compound of formula 7 or a salt thereof, to obtain a compound of formula 5, or a salt thereof (b) reducing the nitro group of the compound of formula 5 to an amine group and mesylating this amine group and cleaving the protecting group during the reduction step or after the mesylation step to obtain the compound of formula 1.
摘要翻译：制备式1化合物或其盐的方法，其中：R 1和R 2各自独立地为H，卤素或C 1-4 R 1，R 2，R 2和R 2一起是C 1-6 - 亚烷基; 且R 3是H，卤素，OH，C 1-4 - 烷基或OC 1-4 - 烷基，所述方法包括：（a）使式6化合物（其中R 4）为苄基，二苯基甲基或三苯甲基，各自任选地在芳基或脂族碳原子上被取代，与式7的化合物或其盐，得到式5的化合物或其盐（b）将式5的化合物的硝基还原成胺基，并在该还原步骤中或之后在该还原步骤或之后将该胺基甲基化并裂解保护基团得到式1化合物的甲磺酰化步骤。

6. 发明授权

US07423035B2 Substituted cycloalkyl derivatives, process for the manufacture thereof and use thereof as medicament 有权
标题翻译：取代的环烷基衍生物，其制备方法及其作为药物的用途
公开(公告)号：US07423035B2
公开(公告)日：2008-09-09
申请号：US11125757
申请日：2005-05-10
申请人： Ingo Konetzki , Thierry Bouyssou , Philipp Lustenberger , Andreas Schnapp , Christoph Hoenke , Klaus Rudolf , Marco Santagostino
发明人： Ingo Konetzki , Thierry Bouyssou , Philipp Lustenberger , Andreas Schnapp , Christoph Hoenke , Klaus Rudolf , Marco Santagostino
IPC分类号： C07D265/36 , A61K31/538 , A61K31/138
CPC分类号： C07D265/36 , C07C215/60 , C07C215/68 , C07C217/74 , C07C311/08 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D215/227
摘要： The present invention relates to compounds of formula 1 wherein the groups R1, R2, R3, R4, R5, R6, R7, R8, n, m and X may have the meanings given in the claims and in the specification, and the use thereof as pharmaceutical compositions, particularly for the treatment of inflammatory and obstructive respiratory complaints.
摘要翻译：本发明涉及式1化合物，其中基团R 1，R 2，R 3，R 4， >，R 5，R 6，R 7，R 8，n，m和X可以具有在权利要求和说明书中给出的含义，以及作为药物组合物的用途，特别是用于治疗炎性和阻塞性呼吸道疾病。

7. 发明申请

US20060252750A1 Selected CGRP-antagonists, process for preparing them and their use as pharmaceutical compositions 有权
标题翻译：选择的CGRP拮抗剂，其制备方法及其作为药物组合物的用途
公开(公告)号：US20060252750A1
公开(公告)日：2006-11-09
申请号：US11277175
申请日：2006-03-22
申请人： Stephan Mueller , Klaus Rudolf , Philipp Lustenberger , Dirk Stenkamp , Alexander Dreyer , Kirsten Arndt , Gerhard Schaenzle , Henri Doods , Marco Santagostino , Fabio Paleari
发明人： Stephan Mueller , Klaus Rudolf , Philipp Lustenberger , Dirk Stenkamp , Alexander Dreyer , Kirsten Arndt , Gerhard Schaenzle , Henri Doods , Marco Santagostino , Fabio Paleari
IPC分类号： A61K31/5513 , C07D403/14
CPC分类号： C07D401/14
摘要： The present invention relates to the CGRP antagonists of general formula wherein A, X, D, E, G, M, Q and R1 to R3 are defined as in claim 1, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates thereof, the mixtures thereof and the salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.
摘要翻译：本发明涉及通式C的CGRP拮抗剂，其中A，X，D，E，G，M，Q和R 1至R 3定义如权利要求 1，互变异构体，异构体，非对映异构体，对映异构体，其水合物，其混合物及其盐以及盐，特别是其与无机或有机酸的生理上可接受的盐的水合物，含有这些化合物的药物组合物，其用途及其制备方法。

8. 发明申请

US20050277632A1 Beta agonists for the treatment of respiratory diseases 有权
标题翻译： β激动剂治疗呼吸系统疾病
公开(公告)号：US20050277632A1
公开(公告)日：2005-12-15
申请号：US11125890
申请日：2005-05-10
申请人： Ingo Konetzki , Thierry Bouyssou , Philipp Lustenberger , Andreas Schnapp , Marco Santagostino , Christoph Hoenke
发明人： Ingo Konetzki , Thierry Bouyssou , Philipp Lustenberger , Andreas Schnapp , Marco Santagostino , Christoph Hoenke
IPC分类号： A61K31/423 , A61K31/428 , A61K31/538 , A61K31/5415 , C07D215/22 , C07D215/227 , C07D215/26 , C07D263/58 , C07D265/36 , C07D279/16
CPC分类号： C07D215/227 , C07D215/26 , C07D263/58 , C07D265/36
摘要： The present invention relates to compounds of general formula 1 wherein the groups n, A, B, R1, R2 and R3 may have the meanings given in the claims and in the specification, processes for preparing them, and their use as pharmaceutical compositions, particularly as pharmaceutical compositions for the treatment of respiratory complaints.
摘要翻译：本发明涉及通式1的化合物，其中基团n，A，B，R 1，R 2和R 3可以具有在权利要求和说明书中给出的含义，其制备方法，以及它们作为药物组合物的用途，特别是用作治疗呼吸道疾病的药物组合物。

9. 发明授权

US06677476B1 Process for preparing R-(-) -carnitine from S-(-)-chlorosuccinic acid or from a derivative thereof 失效
标题翻译：从S - （ - ） - 氯代琥珀酸或其衍生物制备R - （ - ） - 肉碱的方法
公开(公告)号：US06677476B1
公开(公告)日：2004-01-13
申请号：US09959717
申请日：2001-11-06
申请人： Piero Melloni , Alberto Cerri , Marco Santagostino
发明人： Piero Melloni , Alberto Cerri , Marco Santagostino
IPC分类号： C07C6940
CPC分类号： C07C309/66 , C07B2200/07 , C07C51/377 , C07C51/48 , C07C51/56 , C07C69/63 , C07C227/08 , C07C227/32 , C07C55/32 , C07C229/22
摘要： An inner salt of L-carnitine is prepared by reduction, with a suitable reducing agent, of a compound of formula (I): where X1 and X2, which may be the same or different, are hydroxy, C1-C4 alkoxy, phenoxy, halogen, or X1 and X2, when taken together are an oxygen atom and the resulting compound is a derivative of succinic anhydride; Y is halogen, the mesyloxy or the tosyloxy group: and subsequent treatment with water, then with a base and then with trimethylamine.
摘要翻译：通过用合适的还原剂还原式（I）化合物制备L-肉毒碱的内盐：其中X1和X2可以相同或不同，为羟基，C1-C4烷氧基，苯氧基，卤素或X 1和X 2，当一起为氧原子时，所得化合物为琥珀酸酐的衍生物; Y是卤素，甲磺酰氧基或甲苯磺酰氧基：然后用水处理，然后用碱，然后用三甲胺处理。

10. 发明授权

US07754756B2 Indol-containing beta-agonists, methods for the preparation thereof and their use as pharmaceutical compositions 有权
标题翻译：含吲哚的β-激动剂，其制备方法及其作为药物组合物的用途
公开(公告)号：US07754756B2
公开(公告)日：2010-07-13
申请号：US11550830
申请日：2006-10-19
申请人： Rainer Walter , Bradford S. Hamilton , Thomas Trieselmann , Matthew R. Netherton , Marco Santagostino , Ingo Konetzki
发明人： Rainer Walter , Bradford S. Hamilton , Thomas Trieselmann , Matthew R. Netherton , Marco Santagostino , Ingo Konetzki
IPC分类号： A61K31/4045 , A61K31/404 , C07D209/24 , C07D209/18 , C07D413/02
CPC分类号： C07D209/08 , C07D209/18 , C07D209/42 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D413/12
摘要： The present invention relates to new beta-agonists of general formula (I) wherein the groups R1 and R2 have the meanings given in the claims and specification, the tautomers, racemates, enantiomers, diastereomers, solvates, hydrates, mixtures thereof, the prodrugs thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, methods of preparing these compounds and their use as pharmaceutical compositions.
摘要翻译：本发明涉及通式（I）的新β-激动剂，其中基团R 1和R 2具有权利要求和说明书中给出的含义，互变异构体，外消旋体，对映异构体，非对映异构体，溶剂合物，水合物，其混合物，其前药其盐，特别是其与无机或有机酸或碱的生理学上可接受的盐，制备这些化合物的方法及其作为药物组合物的用途。

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