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1.发明申请Modified amino acids, pharmaceuticals containing these compounds and method for their production 审中-公开改性氨基酸，含有这些化合物的药物及其生产方法公开(公告)号：US20090163480A1
公开(公告)日：2009-06-25
申请号：US12336858
申请日：2008-12-17
申请人： Klaus RUDOLF , Wolfgang EBERLEIN , Wolfhard ENGEL , Helmut PIEPER , Henri DOODS , Gerhard HALLERMAYER , Michael ENTZEROTH , Wolfgang WIENEN
发明人： Klaus RUDOLF , Wolfgang EBERLEIN , Wolfhard ENGEL , Helmut PIEPER , Henri DOODS , Gerhard HALLERMAYER , Michael ENTZEROTH , Wolfgang WIENEN
IPC分类号： A61K31/496 , C07D241/04 , C07D413/14 , A61K31/549 , A61P11/06 , A61P17/00 , A61P3/00 , A61P9/00 , A61P37/08 , A61K31/5377 , C07D285/16
CPC分类号： G01N33/58 , A61K31/4745 , A61K31/513 , A61K31/517 , A61K31/519 , A61K31/549 , G01N33/9406
摘要： The present invention relates to modified amino acids of general formula wherein A, Z, X, n, m, R, R2, R3, R4 and R11 are defined as in claims 1 to 5, their tautomers, their diastereomers, their enantiomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them as well as their use for the production and purification of antibodies and as labelled compounds in RIA- and ELISA assays and as diagnostic or analytical aids in neurotransmitter research.
摘要翻译： 本发明涉及通式的改性氨基酸，其中A，Z，X，n，m，R，R 2，R 3，R 4和R 11如权利要求1至5中所定义，它们的互变异构体，它们的非对映体，其对映异构体， 其混合物及其盐，特别是其与无机或有机酸或碱的生理学上可接受的盐，含有这些化合物的药物组合物，其用途及其制备方法及其用于生产和纯化抗体及标记 RIA-和ELISA测定中的化合物以及神经递质研究中的诊断或分析辅助。
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2.发明申请Arylalkanes, arylalkenes and aryl-azaalkanes, pharmaceutical compositions containing these compounds and processes for preparing them 审中-公开芳基烷烃，芳基烯烃和芳基 - 氮杂烷烃，含有这些化合物的药物组合物及其制备方法公开(公告)号：US20070208036A1
公开(公告)日：2007-09-06
申请号：US11743393
申请日：2007-05-02
申请人： Klaus RUDOLF , Wolfgang EBERLEIN , Wolfhard ENGEL , Henri DOODS , Gerhard HALLERMAYER , Eckhart BAUER
发明人： Klaus RUDOLF , Wolfgang EBERLEIN , Wolfhard ENGEL , Henri DOODS , Gerhard HALLERMAYER , Eckhart BAUER
IPC分类号： A61K31/495 , C07C49/04 , C07C49/12 , C07D205/02 , C07D401/04 , C07F5/02
CPC分类号： C07D401/04 , C07D211/58 , C07D471/04
摘要： The present invention relates to compounds of general formula R-Z1-Z2-Z3-R (I), wherein R, R1 and Z1 to Z3 are defined as in claim 1, the tautomers, the diastereomers, the enantiomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, particularly CGRP-antagonistic properties, pharmaceutical compositions containing these compounds, their use and processes for preparing them.
摘要翻译： 本发明涉及通式<β-in-line-formula description =“In-line Formulas”end =“lead”→RZ -Z <3> -R（I），<？在线公式描述=“在线公式”end =“tail”？>其中R，R 1， Z 1至Z 3如权利要求1中所定义，互变异构体，非对映异构体，对映异构体，其混合物及其盐，特别是其生理上可接受的盐 具有有价值的药理学特性，特别是CGRP拮抗性的无机或有机酸或碱，含有这些化合物的药物组合物，其用途和制备方法。
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公开(公告)号：US20130245009A1
公开(公告)日：2013-09-19
申请号：US13869388
申请日：2013-04-24
申请人： Dirk GOTTSCHLING , Georg DAHMANN , Henri DOODS , Annekatrin HEIMANN , Stephan Georg MUELLER , Klaus RUDOLF , Gerhard Georg SCHAENZLE , Dirk STENKAMP
发明人： Dirk GOTTSCHLING , Georg DAHMANN , Henri DOODS , Annekatrin HEIMANN , Stephan Georg MUELLER , Klaus RUDOLF , Gerhard Georg SCHAENZLE , Dirk STENKAMP
IPC分类号： C07D471/10 , C07D498/20 , C07D471/04
CPC分类号： C07D471/10 , C07D471/04 , C07D498/20 , C07D519/00
摘要： The present invention relates to new CGRP-antagonists of general formulae Ia and Ib wherein R1, R2, R3, R4 and R5 are defined as mentioned below, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates, the mixtures and the salts thereof as well as the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, 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Ia和Ib的新CGRP拮抗剂，其中R 1，R 2，R 3，R 4和R 5如下所定义，互变异构体，异构体，非对映异构体，对映异构体，水合物，混合物和 其盐以及盐的水合物，特别是其与无机或有机酸或碱的生理上可接受的盐，含有这些化合物的药物组合物，其用途及其制备方法。
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4.发明申请CGRP-antagonists, process for preparing them and their use as pharmaceutical compositions 有权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：US20090186881A1
公开(公告)日：2009-07-23
申请号：US12363175
申请日：2009-01-30
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： A61K31/551 , C07D243/04 , C07D401/14 , A61K31/496 , C07D239/72 , A61K31/517 , C07D265/04 , A61K31/537 , A61P3/00 , A61P9/00 , A61P29/00
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.
摘要翻译： 本发明涉及通式I的CGRP拮抗剂，其中R 1，R 2，R 3，R 4和X如权利要求1中所定义，互变异构体，异构体，非对映异构体，对映体，水合物，混合物和盐以及 盐，特别是其与无机或有机酸或碱的生理上可接受的盐的水合物，以及其中一个或多个氢原子被氘代替的通式I的那些化合物，含有这些化合物的药物组合物的用途，其用途 及其制备方法。
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5.发明申请Selected CGRP antagonists, processes for preparing them and their use as pharmaceutical compositions 审中-公开选择的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：US20100113411A1
公开(公告)日：2010-05-06
申请号：US12536759
申请日：2009-08-06
申请人： Klaus RUDOLF , Stephan Georg MUELLER , Dirk STENKAMP , Philipp LUSTENBERGER , Alexander DREYER , Eckhart BAUER , Marcus SCHINDLER , Kirsten ARNDT , Henri DOODS
发明人： Klaus RUDOLF , Stephan Georg MUELLER , Dirk STENKAMP , Philipp LUSTENBERGER , Alexander DREYER , Eckhart BAUER , Marcus SCHINDLER , Kirsten ARNDT , Henri DOODS
IPC分类号： A61K31/517 , C07D401/14 , C07D471/04 , A61K31/5513 , A61P25/00 , A61P25/06
CPC分类号： C07D401/04 , C07D401/14
摘要： The present invention relates to CGRP antagonists of general formula wherein A, U, V, W, X and R1 to R3 are defined as in claim 1, the tautomers, diastereomers, enantiomers, hydrates, mixtures thereof and the salts thereof as well as 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 preparing them.
摘要翻译： 本发明涉及以下通式的CGRP拮抗剂：其中A，U，V，W，X和R 1至R 3如权利要求1中所定义，互变异构体，非对映异构体，对映异构体，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。
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公开(公告)号：US20140343065A1
公开(公告)日：2014-11-20
申请号：US14275879
申请日：2014-05-12
申请人： Riccardo GIOVANNINI , Yunhai CUI , Henri DOODS , Marco FERRARA , Stefan JUST , Raimund KUELZER , Iain LINGARD , Rocco MAZZAFERRO , Klaus RUDOLF
发明人： Riccardo GIOVANNINI , Yunhai CUI , Henri DOODS , Marco FERRARA , Stefan JUST , Raimund KUELZER , Iain LINGARD , Rocco MAZZAFERRO , Klaus RUDOLF
IPC分类号： C07D209/52 , C07D471/04 , C07D405/12 , C07D417/12 , C07D403/12 , C07D487/04 , C07D401/12
CPC分类号： A61K31/403 , A61K31/4155 , A61K31/416 , A61K31/423 , A61K31/426 , A61K31/429 , A61K31/437 , A61K31/4375 , A61K31/4439 , A61K31/4709 , A61K31/4725 , A61K31/497 , A61K31/501 , A61K31/502 , A61K31/5025 , A61K31/506 , A61K31/517 , A61K31/519 , C07D209/52 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04
摘要： 3-aza-bicyclo[3.1.0]hexane-6-carboxylic acid amide derivatives which are agonists of somatostatin receptor subtype 4 (SSTR4), useful for preventing or treating medical disorders related to SSTR4.
摘要翻译： 3-氮杂 - 双环[3.1.0]己烷-6-羧酸酰胺衍生物，其是生长抑素受体亚型4（SSTR4）的激动剂，可用于预防或治疗与SSTR4相关的医学障碍。
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公开(公告)号：US20120149676A1
公开(公告)日：2012-06-14
申请号：US13314561
申请日：2011-12-08
申请人： Henning PRIEPKE , Henri DOODS , Alexander HEIM-RIETHER , Raimund KUELZER , Roland PFAU , Klaus RUDOLF , Dirk STENKAMP
发明人： Henning PRIEPKE , Henri DOODS , Alexander HEIM-RIETHER , Raimund KUELZER , Roland PFAU , Klaus RUDOLF , Dirk STENKAMP
IPC分类号： A61K31/4184 , C07D235/30 , C07D403/10 , C07D413/10 , C07D409/12 , C07D413/14 , C07D401/14 , C07D487/04 , C07D513/04 , C07D409/14 , C07D491/107 , C07D491/048 , C07D417/10 , C07D498/08 , C07D403/12 , C07D417/14 , C07D403/14 , A61K31/454 , A61K31/429 , A61K31/5377 , A61K31/4985 , A61K31/496 , A61K31/4725 , A61K31/4439 , A61K31/4545 , A61K31/438 , A61K31/541 , A61K31/5386 , A61K31/4196 , A61K31/497 , A61P29/00 , C07D487/10 , C07D491/08 , A61K31/439 , C07D401/10
CPC分类号： C07D235/30 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/04 , C07D417/14 , C07D487/04 , C07D487/08 , C07D491/04 , C07D491/08 , C07D491/10 , C07D498/08 , C07D513/04
摘要： This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, L, M, W, R1, R2, R3, R4, R6, R7, R9, Ra, Rb have meanings given in the description.
摘要翻译： 本发明涉及式I化合物，其用作微粒体前列腺素E2合酶-1（mPGES-1）的抑制剂，含有它们的药物组合物及其作为用于治疗和/或预防炎性疾病及相关病症的药物的用途。 A，L，M，W，R 1，R 2，R 3，R 4，R 6，R 7，R 9，R a，R b具有说明书中给出的含义。
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8.发明申请公开(公告)号：US20100249114A1
公开(公告)日：2010-09-30
申请号：US12712801
申请日：2010-02-25
申请人： Stephan Georg MUELLER , Klaus RUDOLF , Philipp LUSTENBERGER , Dirk STENKAMP , Alexander DREYER , Kirsten ARNDT , Henri DOODS , Gerhard SCHAENZLE , Marco SANTAGOSTINO , Fabio PALEARI
发明人： Stephan Georg MUELLER , Klaus RUDOLF , Philipp LUSTENBERGER , Dirk STENKAMP , Alexander DREYER , Kirsten ARNDT , Henri DOODS , Gerhard SCHAENZLE , Marco SANTAGOSTINO , Fabio PALEARI
IPC分类号： A61K31/551 , C07D243/04 , C07D401/14 , A61K31/497 , A61K31/445 , C07D471/04 , A61K31/4745 , C07D239/72 , A61K31/517 , C07D495/14 , A61K31/519 , A61P29/00
CPC分类号： C07D401/04 , C07D401/12 , C07D401/14 , C07D471/04 , C07D495/04
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.
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公开(公告)号：US20100152171A1
公开(公告)日：2010-06-17
申请号：US12706840
申请日：2010-02-17
申请人： Klaus RUDOLF , Stephan Georg MUELLER , Dirk STENKAMP , Philipp LUSTENBERGER , Alexander DREYER , Eckhart BAUER , Marcus SCHINDLER , Kirsten ARNDT , Henri DOODS
发明人： Klaus RUDOLF , Stephan Georg MUELLER , Dirk STENKAMP , Philipp LUSTENBERGER , Alexander DREYER , Eckhart BAUER , Marcus SCHINDLER , Kirsten ARNDT , Henri DOODS
IPC分类号： A61K31/5513 , C07D243/24 , C07D239/72 , C07D401/14 , A61K31/517 , A61K31/497 , A61P11/06 , A61P9/10 , A61P3/10 , A61P25/06
CPC分类号： C07D471/04 , C07D401/14 , C07D471/08 , C07D495/04
摘要： CGRP antagonists of the formula of which the following are exemplary: (1) 4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidine-1-carboxylic acid-{(R)-1-(3,4-diethyl-benzyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amide, (2) 4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidine-1-carboxylic acid-{(R)-1-(3,4-diethyl-benzyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amide.
摘要翻译： 具有下式的CGRP拮抗剂是示例性的：（1）4-（2-氧代-1,2,4,5-四氢-1,3-苯并二氮杂-3-基） - 哌啶-1-甲酸 - {（R）-1-（3,4-二乙基 - 苄基）-2- [4-（1-甲基 - 哌啶-4-基） - 哌嗪-1-基] -2-氧代 - 乙基} - 酰胺， （2）4-（2-氧代-1,2,4,5-四氢-1,3-苯并二氮杂-3-基） - 哌啶-1-羧酸 - {（R）-1-（3,4- 乙基 - 苄基）-2- [4-（4-甲基 - 哌嗪-1-基） - 哌啶-1-基] -2-氧代 - 乙基} - 酰胺。
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10.发明申请New CGRP-antagonists, process for preparing them and their use as pharmaceutical compositions 审中-公开新的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：US20100144716A1
公开(公告)日：2010-06-10
申请号：US12707890
申请日：2010-02-18
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： A61K31/551 , C07D401/14 , A61K31/4545 , A61K31/497 , C07D405/14 , A61K31/55
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.
摘要翻译： 本发明涉及通式I的CGRP拮抗剂，其中R 1，R 2，R 3，R 4和X如权利要求1中所定义，互变异构体，异构体，非对映异构体，对映体，水合物，混合物和盐以及 盐，特别是其与无机或有机酸或碱的生理上可接受的盐的水合物，以及其中一个或多个氢原子被氘代替的通式I的那些化合物，含有这些化合物的药物组合物的用途，其用途 及其制备方法。
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