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71. 发明授权

US07803810B2 Inhibitors 有权
标题翻译：抑制剂
公开(公告)号：US07803810B2
公开(公告)日：2010-09-28
申请号：US12045163
申请日：2008-03-10
申请人： Daniel Ramsbeck , Ulrich Heiser , Mirko Buchholz , Andre J. Niestroj
发明人： Daniel Ramsbeck , Ulrich Heiser , Mirko Buchholz , Andre J. Niestroj
IPC分类号： C07D471/04 , A61K31/437 , A61P25/00
CPC分类号： C07D471/04
摘要： Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt or solvate thereof, including all tautomers, stereoisomers and polymorphs thereof wherein: R1 represents C2-8alkyl; C2-8alkenyl; —(C1-6alkyl)-aryl; —(C1-6alkyl)-heteroaryl; —(C1-6alkyl)-carbocyclyl; —(C1-6alkyl)-heterocyclyl; -aryl; -heteroaryl; -carbocyclyl or -heterocyclyl; wherein said aryl or heteroaryl groups may be optionally substituted by one or more substituents selected from, C1-4alkyl, C1-4-fluoroalkyl, C1-4alkoxy, C1-4-fluoroalkoxy, hydroxy, —SO2(C1-4alkyl), —SO2N(C1-4alkyl)(C1-4alkyl), —SOC1-4alkyl, —SOC3-6cycloalkyl —C(O)O(C1-4alkyl), benzyloxy and phenyl; and wherein said carbocyclyl and heterocyclyl groups may be optionally substituted by one or more substituents selected from —C1-4 alkyl, —C1-4 alkoxy, hydroxyl, halogen and oxo; R2 represents H; C1-4alkyl or halogen; R3 represents H; C1-4alkyl or halogen; and R4 represents H; C1-4alkyl or halogen.
摘要翻译：式（I）的化合物，其用于疾病治疗的组合和用途，或其药学上可接受的盐或溶剂合物，包括所有互变异构体，立体异构体和多晶型物，其中：R1代表C2-8烷基; C2-8烯基; - （C 1-6烷基） - 芳基; - （C 1-6烷基） - 杂芳基; - （C 1-6烷基） - 碳环基; - （C 1-6烷基） - 杂环基; 芳基杂芳基碳环基或杂环基; 其中所述芳基或杂芳基可以任选地被一个或多个选自C 1-4烷基，C 1-4 - 氟烷基，C 1-4烷氧基，C 1-4 - 氟烷氧基，羟基，-SO 2（C 1-4烷基），-SO 2 N （C 1-4烷基）（C 1-4烷基），-SOC 1-4烷基，-SOC 3 - 6环烷基-C（O）O（C 1-4烷基），苄氧基和苯基; 并且其中所述碳环基和杂环基可任选被一个或多个选自-C 1-4烷基，-C 1-4烷氧基，羟基，卤素和氧代的取代基取代; R2表示H; C 1-4烷基或卤素; R3表示H; C 1-4烷基或卤素; 且R 4表示H; C 1-4烷基或卤素。

72. 发明申请

US20080267911A1 NOVEL INHIBITORS OF GLUTAMINYL CYCLASE 有权
标题翻译： GLUTAMINYL CYCLASE的新型抑制剂
公开(公告)号：US20080267911A1
公开(公告)日：2008-10-30
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： A61K31/517 , C07D403/06 , C07D495/04 , A61K38/20 , A61P1/00 , A61P25/00 , A61P35/00 , A61K38/21 , A61K39/395 , A61K31/519
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）的化合物，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：R 1表示和R 2 R 3，R 4，R 4，R 5，R 6，X 1， X 2，X 3，X 4，Y和Z如整个说明书和权利要求中所定义。

73. 发明申请

US20080262065A1 NOVEL INHIBITORS OF GLUTAMINYL CYCLASES 有权
标题翻译：谷氨酰胺循环的新型抑制剂
公开(公告)号：US20080262065A1
公开(公告)日：2008-10-23
申请号：US12105808
申请日：2008-04-18
申请人： Mirko Buchholz , Ulrich Heiser , Antje Harmann
发明人： Mirko Buchholz , Ulrich Heiser , Antje Harmann
IPC分类号： A61K31/4164 , C07D233/64 , A61K31/4178 , A61P37/00 , A61P19/00 , A61P25/00 , A61P17/00 , A61P35/00 , C07D405/12
CPC分类号： C07D233/61 , C07D233/64 , C07D405/12
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 R1, B and Y are as described 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，包括其所有互变异构体和立体异构体，其中：A表示和R 1，B和Y 如在整个说明书和权利要求书中所描述的。

74. 发明授权

US09126987B2 Inhibitors of glutaminyl cyclase 有权
标题翻译：谷氨酰胺环化酶抑制剂
公开(公告)号：US09126987B2
公开(公告)日：2015-09-08
申请号：US11946101
申请日：2007-11-28
申请人： Ulrich Heiser , Daniel Ramsbeck , Mirko Buchholz , Andre J. Niestroj
发明人： Ulrich Heiser , Daniel Ramsbeck , Mirko Buchholz , Andre J. Niestroj
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。

75. 发明授权

US08530670B2 Inhibitors 有权
标题翻译：抑制剂
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）。

76. 发明授权

US08518948B2 Inhibitors of protein kinases 失效
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.

77. 发明授权

US08278345B2 Inhibitors of glutaminyl cyclase 有权
标题翻译：谷氨酰胺环化酶抑制剂
公开(公告)号：US08278345B2
公开(公告)日：2012-10-02
申请号：US11937149
申请日：2007-11-08
申请人： Michael Thormann , Michael Altmstetter , Andreas Treml , Ulrich Heiser , Mirko Buchholz , Andre J. Niestroj
发明人： Michael Thormann , Michael Altmstetter , Andreas Treml , Ulrich Heiser , Mirko Buchholz , Andre J. Niestroj
IPC分类号： A61K31/4025 , A61K31/4178 , C07D207/00 , C07D403/06 , C07D233/56
CPC分类号： C07D403/06 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/04
摘要： The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, R1 represents heteroaryl, -carbocyclyl-heteroaryl, -alkenylheteroaryl or -alkylheteroaryl; R2 represents hydrogen; halogen; alkenyl; alkynyl; -alkenylaryl; -alkenylheteroaryl; alkyl, which may optionally be substituted by one or more groups selected from halogen, hydroxyl, alkoxy-, -thioalkyl, —C(O)OH and —C(O)O-alkyl; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl, halogen, hydroxyl, alkoxy-, -thioalkyl, —C(O)OH and —C(O)O-alkyl; -alkylcarbocyclyl; -alkylheterocyclyl; aryl; heteroaryl; heterocyclyl; -alkylaryl; -alkyl(aryl)2, -alkylheteroaryl; -aryl-heteroaryl; -heterocyclyl-aryl; -aryl-aryl; -heteroaryl-aryl; -heteroaryl-heteroaryl, and —C(O)R4; R3 represents halogen; alkyl optionally substituted by one or more groups selected from halogen, hydroxyl, alkoxy, thioalkyl, —C(O)OH and —C(O)O-alkyl; aryl; heteroaryl; —C(O)R5; R4 and R5 independently represent alkyl, aryl, heteroaryl, -alkylaryl, -alkylheteroaryl, carbocyclyl, heterocyclyl, -alkylcarbocyclyl and -alkylheterocyclyl, with the proviso that, when R1 is imidazolyl, -carbocyclyl-imidazolyl, -alkenyl-imidazolyl or -alkyl-imidazolyl, then R3 may not be —C(O)R5.
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，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表示氢; 卤素; 烯基; 炔基; - 烯基芳基; 烯基杂芳基烷基，其可任选被一个或多个选自卤素，羟基，烷氧基 - ， - 硫代烷基，-C（O）OH和-C（O）O-烷基的基团取代; 碳环基，其可任选被一个或多个选自烷基，卤素，羟基，烷氧基 - ， - 硫代烷基，-C（O）OH和-C（O）O-烷基的基团取代; - 烷基羧基 - 烷基杂环基芳基; 杂芳基; 杂环基 - 烷基芳基; - 烷基（芳基）2， - 烷基杂芳基; 芳基 - 杂芳基; - 杂环基 - 芳基; 芳基 - 芳基; - 杂芳基 - 芳基; - 杂芳基 - 杂芳基和-C（O）R 4; R3表示卤素; 任选被一个或多个选自卤素，羟基，烷氧基，硫代烷基，-C（O）OH和-C（O）O-烷基的基团取代的烷基; 芳基; 杂芳基; -C（O）R 5; R 4和R 5独立地表示烷基，芳基，杂芳基， - 烷基芳基， - 烷基杂芳基，碳环基，杂环基， - 烷基碳环基和 - 烷基杂环基，条件是当R 1是咪唑基， - 环保基 - 咪唑基， - 烯基 - 咪唑基或 - 咪唑基，那么R 3可以不是-C（O）R 5。

78. 发明申请

US20110224225A1 Inhibitors of protein kinases 失效
标题翻译：蛋白激酶抑制剂
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。

79. 发明申请

US20080262063A1 NOVEL INHIBITORS OF GLUTAMINYL CYCLASE 有权
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.

80. 发明申请

US20080260688A1 NOVEL INHIBITORS OF GLUTAMINYL CYCLASE 有权
标题翻译： GLUTAMINYL CYCLASE的新型抑制剂
公开(公告)号：US20080260688A1
公开(公告)日：2008-10-23
申请号：US12105832
申请日：2008-04-18
申请人： Mirko Buchholz , Ulrich Heiser , Robert Sommer
发明人： Mirko Buchholz , Ulrich Heiser , Robert Sommer
IPC分类号： A61K38/20 , C07D401/02 , A61K31/506 , A61P35/00 , A61P25/00 , A61P3/00 , A61P9/00 , A61P37/02 , A61P31/00 , A61K38/21 , A61K39/395
CPC分类号： C07D403/12 , C07D401/14 , C07D405/14
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, R7, 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：A表示和B，R 1，R R 2，R 3，R 4，R 5，R 6，R 6，R 4，在整个说明书和权利要求书中，Y和Z如所定义。

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