专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

US20100099681A1 SUBSTITUTED 5-AMINOPYRAZOLES AND USE THEREOF 审中-公开
标题翻译：取代的5-氨基吡唑及其用途
公开(公告)号：US20100099681A1
公开(公告)日：2010-04-22
申请号：US12540657
申请日：2009-08-13
申请人： Lars Bärfacker , Raimund Kast , Nils Griebenow , Heinrich Meier , Peter Kolkhof , Barbara Albrecht-Küpper , Adam Nitsche , Nicole Teusch , Johannes-Peter Stasch , Dirk Schneider
发明人： Lars Bärfacker , Raimund Kast , Nils Griebenow , Heinrich Meier , Peter Kolkhof , Barbara Albrecht-Küpper , Adam Nitsche , Nicole Teusch , Johannes-Peter Stasch , Dirk Schneider
IPC分类号： A61K31/498 , A61K31/517 , A61K31/437 , A61K31/4709 , A61K31/415 , C07D403/10 , C07D231/38 , A61P9/00
CPC分类号： C07D403/04 , C07D401/04 , C07D417/04 , C07D471/04
摘要： The present application relates to novel substituted 5-aminopyrazoles, methods of production thereof, use thereof alone or in combinations for the treatment and/or prophylaxis of diseases and use thereof for the production of medicinal products for the treatment and/or prophylaxis of diseases.
摘要翻译：本申请涉及新型取代的5-氨基吡唑，其制备方法，单独使用或组合用于治疗和/或预防疾病及其用于生产用于治疗和/或预防疾病的药物的用途。

2. 发明授权

US09073939B2 Indazolyl-substituted dihydroisoxa-zolopyridines and methods of use thereof 有权
标题翻译：吲唑基取代的二氢异恶唑并吡咯嗪及其使用方法
公开(公告)号：US09073939B2
公开(公告)日：2015-07-07
申请号：US13383223
申请日：2010-07-07
申请人： Martin Michels , Markus Follmann , Alexandros Vakalopoulos , Katja Zimmermann , Nicole Teusch , Mario Lobell
发明人： Martin Michels , Markus Follmann , Alexandros Vakalopoulos , Katja Zimmermann , Nicole Teusch , Mario Lobell
IPC分类号： C07D498/04 , A61K31/437
CPC分类号： C07D498/04 , A61K31/437
摘要： This invention relates to novel 4-(indazol-5-yl)-4,7-dihydroisoxazolo[5,4-b]pyridine derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly cancer and other proliferative disorders.
摘要翻译：本发明涉及具有蛋白酪氨酸激酶抑制活性的新型4-（吲唑-5-基）-4,7-二氢异恶唑并[5,4-b]吡啶衍生物及其制备方法及其用途治疗c-Met介导的疾病或c-Met介导的病症，特别是癌症和其他增殖性疾病。

3. 发明申请

US20110172221A1 ANNELLATED 4-(INDAZOLYL)-1,4-DIHYDROPYRIDINE DERIVATIVES AND METHODS OF USE THEREOF 有权
标题翻译：苯并4-（茚基）-1,4-二氢吡啶衍生物及其使用方法
公开(公告)号：US20110172221A1
公开(公告)日：2011-07-14
申请号：US12996499
申请日：2009-05-29
申请人： Martin Michels , Markus Follmann , Alexandros Vakalopoulos , Katja Zimmermann , Nicole Teusch , Karen Engel
发明人： Martin Michels , Markus Follmann , Alexandros Vakalopoulos , Katja Zimmermann , Nicole Teusch , Karen Engel
IPC分类号： A61K31/5383 , C07D498/04 , A61P35/00
CPC分类号： C07D498/04
摘要： This invention relates to novel annellated 4-(indazolyl)-1,4-dihydropyridine derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly cancer and other proliferative disorders.
摘要翻译：本发明涉及具有蛋白酪氨酸激酶抑制活性的新型环状4-（吲唑基）-1,4-二氢吡啶衍生物及其制备方法及其用于治疗c-Met介导的疾病或c- Met介导的病症，特别是癌症和其他增殖性疾病。

4. 发明授权

US09291621B2 AGER-peptides and use thereof 有权
标题翻译： AGER-肽及其用途
公开(公告)号：US09291621B2
公开(公告)日：2016-03-22
申请号：US11795282
申请日：2006-01-18
申请人： Alfred Hahn , Ralf Loebbert , Nicole Teusch , Achim Möller , Ulrich Ebert , Martin Schmidt
发明人： Alfred Hahn , Ralf Loebbert , Nicole Teusch , Achim Möller , Ulrich Ebert , Martin Schmidt
IPC分类号： A61K39/00 , G01N33/564 , C07K16/28
CPC分类号： C07K16/2803 , A61K39/395 , A61K45/06 , A61K2039/505 , A61K2039/507 , C07K7/08 , C07K2317/24 , C12N15/85 , C12P21/005 , C12P21/02 , G01N33/564 , G01N33/566 , G01N2333/70503 , G01N2500/00
摘要： The present invention relates to the identification, functionality and use of domains from the N terminus of the receptor for Advanced Glycation End Products (AGER). These domains, called receptor multimerization epitope (RME), are highly conserved in all AGER protein sequences. They represent the mediators for AGER self-association and heteromerization with other proteins. The invention likewise relates to the identification, functionality and use of peptides derived from the C domain of AGER (AGER-CDP). The AGER RMEs and AGER-CDPs of the invention are suitable as target for identifying AGER ligands which modulate the natural ligand interaction; as immunogen for active or passive immunization of individuals, as diagnostic means for identifying immunogenic reactions, and as peptide ligands for modulating protein-protein interactions involving AGER.
摘要翻译：本发明涉及来自高级糖化终产物（AGER）的受体的N末端的结构域的鉴定，功能和用途。称为受体多聚表位（RME）的这些结构域在所有AGER蛋白质序列中都是高度保守的。它们代表AGER与其他蛋白质自身结合和异源化的介质。本发明同样涉及衍生自AGER（AGER-CDP）的C结构域的肽的鉴定，功能和用途。本发明的AGER RME和AGER-CDP适用于鉴定调节天然配体相互作用的AGER配体的靶标; 作为用于个体的主动或被动免疫的免疫原，作为用于鉴定免疫原性反应的诊断手段，以及用于调节涉及AGER的蛋白质 - 蛋白质相互作用的肽配体。

5. 发明申请

US20090203690A1 5-SUBSTITUTED INDAZOLES AS KINASE INHIBITORS 有权
标题翻译：作为激素抑制剂的5-取代的吲哚美辛
公开(公告)号：US20090203690A1
公开(公告)日：2009-08-13
申请号：US12327991
申请日：2008-12-04
申请人： Irini Akritopoulou-Zanze , Brian D. Wakefield , Helmut Mack , Sean C. Turner , Alan F. Gasiecki , Vijaya J. Gracias , Kathy A. Sarris , Douglas M. Kalvin , Melissa J. Michmerhuizen , Qi Shuai , Jyoti R. Patel , Margaretha H.M. Bakker , Nicole Teusch , Eric F. Johnson , Peter J. Kovar , Stevan W. Djuric , Andrew J. Long , Anil Vasudevan , Dawn George , Lu Wang , Biqin Li , N. St. John Moore , Adrian D. Hobson , Keith W. Woods , Julie M. Miyashiro , Steven L. Swann, JR. , Thomas D. Penning
发明人： Irini Akritopoulou-Zanze , Brian D. Wakefield , Helmut Mack , Sean C. Turner , Alan F. Gasiecki , Vijaya J. Gracias , Kathy A. Sarris , Douglas M. Kalvin , Melissa J. Michmerhuizen , Qi Shuai , Jyoti R. Patel , Margaretha H.M. Bakker , Nicole Teusch , Eric F. Johnson , Peter J. Kovar , Stevan W. Djuric , Andrew J. Long , Anil Vasudevan , Dawn George , Lu Wang , Biqin Li , N. St. John Moore , Adrian D. Hobson , Keith W. Woods , Julie M. Miyashiro , Steven L. Swann, JR. , Thomas D. Penning
IPC分类号： A61K31/5377 , C07D403/04 , A61K31/4192 , C07D413/14 , C12N9/99 , A61P25/28 , A61P35/00
CPC分类号： C07D413/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A, R1, R2, R3 and m, are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as Glycogen Synthase kinase 3 (GSK-3), Rho kinase (ROCK), Janus Kinases (JAK), Cdc7, AKT, PAK4, PLK, CK2, KDR, MK2, JNK1, aurora, pim 1 and nek 2.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，其中A，R 1，R 2，R 3和m在说明书中定义。本发明还涉及制备所述化合物的方法和含有所述化合物的组合物，其可用于抑制激酶例如糖原合成酶激酶3（GSK-3），Rho激酶（ROCK），Janus激酶（JAK），Cdc7，AKT ，PAK4，PLK，CK2，KDR，MK2，JNK1，极光，pim1和nek2。

6. 发明授权

US09018234B2 Fluoro-substituted 2-aryl-3,5-dicyano-4-indazolyl-6-methyl-1,4-dihydropyridines and uses thereof 有权
标题翻译：氟取代的2-芳基-3,5-二氰基-4-吲唑基-6-甲基-1,4-二氢吡啶及其用途
公开(公告)号：US09018234B2
公开(公告)日：2015-04-28
申请号：US13509047
申请日：2010-11-08
申请人： Alexandros Vakalopoulos , Martin Michels , Katja Zimmermann , Nicole Teusch , Mario Lobell , Karen Engel
发明人： Alexandros Vakalopoulos , Martin Michels , Katja Zimmermann , Nicole Teusch , Mario Lobell , Karen Engel
IPC分类号： A01N43/40 , A61K31/44 , C07D211/02 , C07D401/00 , C07D413/14 , C07D401/04 , C07D401/14
CPC分类号： C07D413/14 , C07D401/04 , C07D401/14
摘要： The present invention relates to novel, fluoro-substituted 2-aryl-3,5-dicyano-4-(1H-indazol-5-yl)-6-methyl-1,4-dihydropyridine derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly Cancer and other proliferative disorders.
摘要翻译：本发明涉及具有蛋白酪氨酸激酶抑制活性的新的氟取代的2-芳基-3,5-二氰基-4-（1H-吲唑-5-基）-6-甲基-1,4-二氢吡啶衍生物，其制备方法及其用于治疗c-Met介导的疾病或c-Met介导的病症，特别是癌症和其它增殖性疾病的用途。

7. 发明申请

US20130005773A1 FLUORO-SUBSTITUTED 2-ARYL-3,5-DICYANO-4-INDAZOLYL-6-METHYL-1,4-DIHYDROPYRIDINES AND USES THEREOF 有权
标题翻译：氟代取代的2-芳基-3,5-二基-4-异吲哚-6-甲基-1,4-二氢吡啶并及其用途
公开(公告)号：US20130005773A1
公开(公告)日：2013-01-03
申请号：US13509047
申请日：2010-11-08
申请人： Alexandros Vakalopoulos , Martin Michels , Katja Zimmermann , Nicole Teusch , Mario Lobell , Karen Engel
发明人： Alexandros Vakalopoulos , Martin Michels , Katja Zimmermann , Nicole Teusch , Mario Lobell , Karen Engel
IPC分类号： A61K31/4439 , C07D401/14 , A61P35/04 , C07D413/14 , A61P35/00 , C07D401/10 , A61K31/444
CPC分类号： C07D413/14 , C07D401/04 , C07D401/14
摘要： The present invention relates to novel, fluoro-substituted 2-aryl-3,5-dicyano-4-(1H-indazol-5-yl)-6-methyl-1,4-dihydropyridine derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly Cancer and other proliferative disorders.
摘要翻译：本发明涉及具有蛋白酪氨酸激酶抑制活性的新的氟取代的2-芳基-3,5-二氰基-4-（1H-吲唑-5-基）-6-甲基-1,4-二氢吡啶衍生物，其制备方法及其用于治疗c-Met介导的疾病或c-Met介导的病症，特别是癌症和其它增殖性疾病的用途。

8. 发明申请

US20110207731A1 SUBSTITUTED 4-(INDAZOLYL)-1,4-DIHYDROPYRIDINES AND METHODS OF USE THEREOF 有权
标题翻译：取代的4-（吲哚基）-1,4-二氢吡啶并及其使用方法
公开(公告)号：US20110207731A1
公开(公告)日：2011-08-25
申请号：US12996465
申请日：2009-05-29
申请人： Martin Michels , Markus Follmann , Alexandros Vakalopoulos , Katja Zimmermann , Nicole Teusch , Karen Engel
发明人： Martin Michels , Markus Follmann , Alexandros Vakalopoulos , Katja Zimmermann , Nicole Teusch , Karen Engel
IPC分类号： A61K31/5377 , C07D401/10 , A61K31/4439 , C07D401/14 , C07D413/14 , A61K31/4545 , A61P35/00
CPC分类号： C07D401/04
摘要： This invention relates to novel 4-(indazolyl)-1,4-dihydropyridine og the following formula (I) derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly cancer and other proliferative disorders.
摘要翻译：本发明涉及具有蛋白酪氨酸激酶抑制活性的下式（I）衍生物的新的4-（吲唑基）-1,4-二氢吡啶，其制备方法及其用于治疗c-Met 介导的疾病或c-Met介导的病症，特别是癌症和其他增殖性疾病。

9. 发明申请

US20100273828A1 4-(4-PYRIDINYL)-BENZAMIDES AND THEIR USE AS ROCK ACTIVITY MODULATORS 有权
标题翻译： 4-（4-吡啶基） - 苯甲酸酯及其作为岩石活性调节剂的用途
公开(公告)号：US20100273828A1
公开(公告)日：2010-10-28
申请号：US12675430
申请日：2008-08-26
申请人： Helmut Mack , Nicole Teusch , Bernhard K. Müller , Wilfried Hornberger , Michael F. Jarvis , Daryl Sauer , Steve Swann, JR. , Anil Vasudevan
发明人： Helmut Mack , Nicole Teusch , Bernhard K. Müller , Wilfried Hornberger , Michael F. Jarvis , Daryl Sauer , Steve Swann, JR. , Anil Vasudevan
IPC分类号： A61K31/4545 , A61K31/444 , A61K31/4439 , A61K31/44 , C07D401/02 , C07D213/56 , A61P25/16 , A61K9/00 , A61P35/00 , A61P11/06 , A61P25/00 , A61P25/28
CPC分类号： C07D401/12 , C07D213/56 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12
摘要： The present invention relates to novel 4-(4-pyridyl)-benzamides of the formula (I). The compounds I possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of Rho kinases (ROCKs). R1 and R2 are, independently of each other, hydrogen, hydroxy, cyano, C1-C8-alkyl, C1-C8-haloalkyl, C1-C8-alkoxy or C1-C8-haloalkoxy; R3, R4, R5 and R6 are, independently of each other, hydrogen, hydroxy, halogen, cyano, C1-C8-alkyl, C1-C8-haloalkyl, C1-C8-alkoxy, C1-C8-haloalkoxy, amino, C1-C8-alkylamino or di-(C1-C8-alkyl)-amino; R7 is hydrogen, C1-C8-alkyl, C1-C8-haloalkyl, aryl or aryl-C1-C8-alkyl; R8 is a group of the formula —X—W, where X is a single bond, C1-C4-alkylene or C1-C4-alkylene-O—, where the alkylene group in the three last-mentioned radicals may be linear or branched and may be partly or fully halogenated and/or may be substituted by a hydroxyl group and/or may be interrupted by an oxygen atom; and W is a cyclic radical selected from phenyl and a 5- or 6-membered saturated, partly unsaturated or aromatic heterocyclic ring which contains as ring members 1, 2 or 3 heteroatoms selected from O, S and N and optionally 1 or 2 carbonyl groups; R9 is a group of the formula —Y—Z, where Z is hydrogen, halogen, OR11, NR12R13, S(O)m—R14, phenyl which may carry 1, 2, 3 or 4 substituents R15 or a 5- or 6-membered saturated, partly unsaturated or aromatic heterocyclic ring; and Y is linear or branched C1C4-alkylene which may be partly or fully halogenated and/or may be substituted by a hydroxyl group and/or a phenyl ring; or, in case Z is phenyl or the 5- or 6-membered heterocyclic ring as defined above, Y can also be a single bond.
摘要翻译：本发明涉及式（I）的新型4-（4-吡啶基） - 苯甲酰胺。化合物I具有有价值的治疗特性，特别适用于治疗对Rho激酶（ROCK）的调节作用的疾病。 R 1和R 2彼此独立地为氢，羟基，氰基，C 1 -C 8 - 烷基，C 1 -C 8 - 卤代烷基，C 1 -C 8 - 烷氧基或C 1 -C 8 - 卤代烷氧基; R3，R4，R5和R6彼此独立地为氢，羟基，卤素，氰基，C1-C8-烷基，C1-C8-卤代烷基，C1-C8-烷氧基，C1-C8-卤代烷氧基，氨基，C1- C 8 - 烷基氨基或二 - （C 1 -C 8 - 烷基） - 氨基; R 7是氢，C 1 -C 8 - 烷基，C 1 -C 8 - 卤代烷基，芳基或芳基-C 1 -C 8 - 烷基; R8是式-X-W的基团，其中X是单键，C1-C4-亚烷基或C1-C4-亚烷基-O-，其中三个最后提到的基团中的亚烷基可以是直链或支链并且可以部分或完全卤化和/或可以被羟基取代和/或可以被氧原子中断; 并且W是选自苯基和5-或6-元饱和，部分不饱和或芳族杂环的环状基团，其含有作为环成员1,2或3的选自O，S和N的杂原子以及任选的1或2个羰基 ; R 9是式-Y-Z的基团，其中Z是氢，卤素，OR 11，NR 12 R 13，S（O）m -R 14，可带有1,2,3或4个取代基R 15或5-或6的苯基饱和的，部分不饱和的或芳族的杂环; Y是可部分或完全卤化和/或可被羟基和/或苯环取代的直链或支链C 1 -C 4亚烷基; 或者Z为苯基或上述5-或6-元杂环的情况下，Y也可以是单键。

10. 发明申请

US20100226915A1 AGER-Peptides and Use Thereof 有权
标题翻译： AGER-肽及其用途
公开(公告)号：US20100226915A1
公开(公告)日：2010-09-09
申请号：US11795282
申请日：2006-01-18
申请人： Alfred Hahn , Ralph Loebbert , Nicole Teusch , Achim Möller
发明人： Alfred Hahn , Ralph Loebbert , Nicole Teusch , Achim Möller
IPC分类号： A61K39/395 , C07K16/18 , G01N33/566 , A61K39/00 , A61K31/7088 , A61K38/43 , C12N15/63 , C12N1/00 , C12N5/16 , C12P21/06 , C07K14/00
CPC分类号： C07K16/2803 , A61K39/395 , A61K45/06 , A61K2039/505 , A61K2039/507 , C07K7/08 , C07K2317/24 , C12N15/85 , C12P21/005 , C12P21/02 , G01N33/564 , G01N33/566 , G01N2333/70503 , G01N2500/00
摘要： The present invention relates to the identification, functionality and use of domains from the N terminus of the receptor for Advanced Glycation End Products (AGER). These domains, called receptor mulitimerization epitope (RME), are highly conserved in all AGER protein sequences. They represent the mediators for AGER self-association and heteromerization with other proteins. The invention likewise relates to the identification, functionality and use of peptides derived from the C domain of AGER (AGER-CDP). The AGER RMEs and AGER-CDPs of the invention are suitable as target for identifying AGER ligands which modulate the natural ligand interaction; as immunogen for active or passive immunization of individuals, as diagnostic means for identifying immunogenic reactions, and as peptide ligands for modulating protein-protein interactions involving AGER.
摘要翻译：本发明涉及来自高级糖化终产物（AGER）的受体的N末端的结构域的鉴定，功能和用途。称为受体多聚表位（RME）的这些结构域在所有AGER蛋白质序列中都是高度保守的。它们代表AGER与其他蛋白质自身结合和异源化的介质。本发明同样涉及衍生自AGER（AGER-CDP）的C结构域的肽的鉴定，功能和用途。本发明的AGER RME和AGER-CDP适用于鉴定调节天然配体相互作用的AGER配体的靶标; 作为用于个体的主动或被动免疫的免疫原，作为用于鉴定免疫原性反应的诊断手段，以及用于调节涉及AGER的蛋白质 - 蛋白质相互作用的肽配体。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式