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公开(公告)号：US09126987B2
公开(公告)日：2015-09-08
申请号：US11946101
申请日：2007-11-28
IPC分类号： C07D413/04
CPC分类号： C07D413/04
摘要： The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, wherein R1 represents heteroaryl, -carbocyclyl-heteroaryl, -alkenylheteroaryl or -alkylheteroaryl; R2 represents alkyl; carbocyclyl which may optionally be substituted by alkyl; alkenyl; alkynyl, provided a triple bond is not adjacent to X; -alkyl-aryl; -alkyl-heteroaryl; -alkyl-heterocyclyl in which heterocyclyl may optionally be substituted by alkyl; -alkyl-carbocyclyl in which carbocyclyl may optionally be substituted by alkyl; aryl; heteroaryl; or H; X represents S or NR3; R3 represents H or C1-4 alkyl.
摘要翻译： 本发明涉及式（I）化合物，其用于疾病治疗的组合和用途，其中R 1表示杂芳基， - 碳环基 - 杂芳基， - 烯基杂芳基或 - 烷基杂芳基; R2代表烷基; 可任意被烷基取代的碳环基; 烯基; 炔基，条件是三键不与X相邻; - 烷基 - 芳基; - 烷基 - 杂芳基; - 烷基 - 杂环基，其中杂环基可以任选被烷基取代; - 烷基 - 碳环基，其中碳环基可以任选地被烷基取代; 芳基; 杂芳基; 或H; X表示S或NR 3; R 3表示H或C 1-4烷基。
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公开(公告)号：US08530670B2
公开(公告)日：2013-09-10
申请号：US13422619
申请日：2012-03-16
申请人： Ulrich Heiser , Daniel Ramsbeck
发明人： Ulrich Heiser , Daniel Ramsbeck
IPC分类号： A61K31/4184 , C07D401/14 , C07D403/04 , C07D413/14
CPC分类号： C07D403/04 , A61K31/4184 , A61K31/4409 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K38/2026 , A61K38/21 , A61K45/06 , C07D401/14 , C07D413/14 , C07D417/14 , A61K2300/00
摘要： Novel heterocyclic derivatives of formula (I): or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein Ra, n, R1 and R2 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5).
摘要翻译： 式（I）的新型杂环衍生物：或其药学上可接受的盐，溶剂化物或多晶型物，包括其所有互变异构体和立体异构体，其中R a，n，R 1和R 2如本文所定义，作为谷氨酰胺酰环化酶抑制剂（QC，EC2.3 .2.5）。
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公开(公告)号：US08518948B2
公开(公告)日：2013-08-27
申请号：US12932955
申请日：2011-03-10
申请人： Lutz Zeitlmann , Andre Niestroj , Ulrich Heiser
发明人： Lutz Zeitlmann , Andre Niestroj , Ulrich Heiser
IPC分类号： C07D213/72 , C07D401/12 , A61K31/444
CPC分类号： A61K31/496 , A61K31/4418 , A61K31/443 , A61K31/4439 , A61K31/444 , A61K31/4545 , C07D213/72 , C07D213/75 , C07D401/12 , C07D401/14 , C07D409/12 , C07D417/12 , Y02A50/385 , Y02A50/411
摘要： Compounds of general Formula (I): wherein R1, R2, R3, Ra, A, B and x are as defined herein are inhibitors of protein kinases in particular members of the cyclin-dependent kinase family and/or the glycogen synthase kinase 3 family and are useful in preventing and/or treating any type of pain, inflammatory disorders, cancer, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases, metabolic disorders, renal diseases, neurologic and neuropsychiatric diseases and neurodegenerative diseases.
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公开(公告)号：US20110224225A1
公开(公告)日：2011-09-15
申请号：US12932955
申请日：2011-03-10
申请人： Lutz Zeitlmann , Andre Niestroj , Ulrich Heiser
发明人： Lutz Zeitlmann , Andre Niestroj , Ulrich Heiser
IPC分类号： A61K31/4418 , C07D213/72 , C07D401/12 , A61K31/4545 , A61K31/4439 , A61K31/444 , C07D409/12 , A61K31/4436 , A61K31/496 , C07D401/14 , C07D417/12 , A61P29/00 , A61P37/00 , A61P35/00 , A61P31/00 , A61P9/00 , A61P25/00
CPC分类号： A61K31/496 , A61K31/4418 , A61K31/443 , A61K31/4439 , A61K31/444 , A61K31/4545 , C07D213/72 , C07D213/75 , C07D401/12 , C07D401/14 , C07D409/12 , C07D417/12 , Y02A50/385 , Y02A50/411
摘要： Compounds of general Formula (I): wherein R1, R2, R3, Ra, A, B and x are as defined herein are inhibitors of protein kinases in particular members of the cyclin-dependent kinase family and/or the glycogen synthase kinase 3 family and are useful in preventing and/or treating any type of pain, inflammatory disorders, cancer, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases, metabolic disorders, renal diseases, neurologic and neuropsychiatric diseases and neurodegenerative diseases.
摘要翻译： 通式（I）的化合物：其中R 1，R 2，R 3，R a，A，B和x如本文所定义，是细胞周期蛋白依赖性激酶家族和/或糖原合酶激酶3家族的特别成员的蛋白激酶的抑制剂 并且可用于预防和/或治疗任何类型的疼痛，炎性疾病，癌症，免疫疾病，增殖性疾病，感染性疾病，心血管疾病，代谢障碍，肾脏疾病，神经和神经精神疾病和神经变性疾病。
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公开(公告)号：US20080262063A1
公开(公告)日：2008-10-23
申请号：US12105753
申请日：2008-04-18
申请人： Mirko Buchholz , Ulrich Heiser , Andre J. Niestroj
发明人： Mirko Buchholz , Ulrich Heiser , Andre J. Niestroj
IPC分类号： A61K31/4184 , C07D233/54 , A61K31/4164 , A61P35/00 , A61P3/00 , A61P9/00 , A61P25/00 , C07D235/04
CPC分类号： C07D235/06 , C07D233/61 , C07D233/64
摘要： Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein: A represents and B, R1, R2, R3, R4, R5, R6 and Z are as defined throughout the description and the claims.
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公开(公告)号：US20080214620A1
公开(公告)日：2008-09-04
申请号：US11946101
申请日：2007-11-28
IPC分类号： A61K31/4245 , C07D413/02 , C07D413/14 , A61P31/00 , A61P19/00 , A61P25/00 , A61K31/4439
CPC分类号： C07D413/04
摘要： The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, wherein R1 represents heteroaryl, -carbocyclyl-heteroaryl, -alkenylheteroaryl or -alkylheteroaryl; R2 represents alkyl; carbocyclyl which may optionally be substituted by alkyl; alkenyl; alkynyl, provided a triple bond is not adjacent to X; -alkyl-aryl; -alkyl-heteroaryl; -alkyl-heterocyclyl in which heterocyclyl may optionally be substituted by alkyl; -alkyl-carbocyclyl in which carbocyclyl may optionally be substituted by alkyl; aryl; heteroaryl; or H; X represents S or NR3; R3 represents H or C1-4 alkyl.
摘要翻译： 本发明涉及式（I）化合物，其用于疾病治疗的组合和用途，其中R 1表示杂芳基，碳环基 - 杂芳基， - 烯基杂芳基或 - 烷基杂芳基; R 2表示烷基; 可任意被烷基取代的碳环基; 烯基; 炔基，条件是三键不与X相邻; - 烷基 - 芳基; - 烷基 - 杂芳基; - 烷基 - 杂环基，其中杂环基可以任选被烷基取代; - 烷基 - 碳环基，其中碳环基可以任选地被烷基取代; 芳基; 杂芳基; 或H; X表示S或NR 3; R 3表示H或C 1-4烷基。
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公开(公告)号：US09034907B2
公开(公告)日：2015-05-19
申请号：US12105849
申请日：2008-04-18
申请人： Mirko Buchholz , Ulrich Heiser
发明人： Mirko Buchholz , Ulrich Heiser
IPC分类号： C07D495/04 , C07D403/06 , A61P25/28 , A61P25/16 , A61P9/10 , A61P37/06 , A61P19/02
CPC分类号： C07D495/04 , C07D403/06
摘要： Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein: R1 represents and R2, R3, R4, R5, R6, X1, X2, X3, X4, Y and Z are as defined throughout the description and the claims.
摘要翻译： 式（I）化合物，其用于疾病治疗的组合和用途，或其药学上可接受的盐，溶剂化物或多晶型物，包括所有互变异构体和立体异构体，其中：R1表示和R2，R3，R4，R5，R6，X1，X2 X3，X4，Y和Z如在说明书和权利要求书中所定义。
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公开(公告)号：US08716296B2
公开(公告)日：2014-05-06
申请号：US12226286
申请日：2008-10-13
申请人： Hans Allgeier , Martin Augustin , Anke Müller , Lutz Zeitlmann , Andreas Marquardt , Michael A. Pleiss , Ulrich Heiser , André Johannes Niestroj
发明人： Hans Allgeier , Martin Augustin , Anke Müller , Lutz Zeitlmann , Andreas Marquardt , Michael A. Pleiss , Ulrich Heiser , André Johannes Niestroj
IPC分类号： A01N43/54 , C07D401/00
CPC分类号： C07D403/12 , C07D239/42 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/04 , C07D487/04
摘要： Compounds of general formula (I): are useful as inhibitors of cyclin dependent kinases such as CDK9.
摘要翻译： 通式（I）的化合物：可用作细胞周期依赖性激酶如CDK9的抑制剂。
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公开(公告)号：US20120237475A1
公开(公告)日：2012-09-20
申请号：US13422619
申请日：2012-03-16
申请人： Ulrich Heiser , Daniel Ramsbeck
发明人： Ulrich Heiser , Daniel Ramsbeck
IPC分类号： A61K38/20 , A61K31/4184 , C07D413/14 , A61K31/5377 , C07D401/14 , A61K31/454 , C07D417/14 , A61K31/541 , C07D405/14 , C07D409/14 , C07D403/14 , A61K31/496 , A61K33/14 , A61K39/395 , A61K38/21 , A61K31/4409 , A61K38/10 , A61P25/00 , A61P25/16 , A61P25/24 , A61P25/22 , A61P25/18 , A61P37/02 , A61P37/06 , A61P1/04 , A61P35/00 , A61P31/04 , A61P15/08 , A61P29/00 , A61P35/04 , A61P17/06 , A61P37/00 , A61P3/00 , A61P5/00 , A61P7/00 , A61P25/28 , A61P19/02 , A61P9/10 , A61P1/18 , A61P9/00 , C07D403/10
CPC分类号： C07D403/04 , A61K31/4184 , A61K31/4409 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K38/2026 , A61K38/21 , A61K45/06 , C07D401/14 , C07D413/14 , C07D417/14 , A61K2300/00
摘要： Novel heterocyclic derivatives of formula (I): or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein Ra, n, R1 and R2 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5).
摘要翻译： 式（I）的新型杂环衍生物：或其药学上可接受的盐，溶剂化物或多晶型物，包括其所有互变异构体和立体异构体，其中R a，n，R 1和R 2如本文所定义，作为谷氨酰胺酰环化酶抑制剂（QC，EC2.3 .2.5）。
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公开(公告)号：US20100273835A1
公开(公告)日：2010-10-28
申请号：US12665502
申请日：2008-07-10
申请人： Ulrich Heiser , Andre J. Niestroj , Ingo Schulz
发明人： Ulrich Heiser , Andre J. Niestroj , Ingo Schulz
IPC分类号： A61K31/4402 , C07D277/68 , A61K31/428 , C07D333/38 , A61K31/381 , C07D277/56 , A61K31/427 , C07D213/78 , C07D307/68 , A61K31/341 , C07D403/06 , A61K31/404 , A61P25/28 , A61P25/16 , A61P25/18 , A61P25/24 , A61P9/00 , A61P7/02
CPC分类号： C07C271/22 , C07D213/50 , C07D277/24 , C07D277/64 , C07D307/46 , C07D333/22 , C07D333/56 , C07D417/06
摘要： The invention provides compounds of general formula (I) or a pharmaceutically acceptable salt, polymorph or solvate thereof, including all tautomers and stereoisomers thereof, wherein K, W, X; Y and Z are described throughout the description and claims.The compounds of the present invention are useful as inhibitors of prolyl endopeptidase (PEP, EC 3.4.21.26) and/or IL-6.
摘要翻译： 本发明提供了通式（I）的化合物或其药学上可接受的盐，多晶型物或溶剂化物，包括其互变异构体和立体异构体，其中K，W，X; 在整个说明书和权利要求书中描述了Y和Z。 本发明的化合物可用作脯氨酰内肽酶（PEP，EC 3.4.21.26）和/或IL-6的抑制剂。
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