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1. 发明申请

US20100273835A1 NOVEL COMPOUNDS 审中-公开
标题翻译：新型化合物
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。

2. 发明申请

US20080286231A1 NOVEL INHIBITORS OF GLUTAMINYL CYCLASE 有权
公开(公告)号：US20080286231A1
公开(公告)日：2008-11-20
申请号：US12105703
申请日：2008-04-18
申请人： Mirko Buchholz , Ulrich Heiser , Andre J. Niestroj , Robert Sommer
发明人： Mirko Buchholz , Ulrich Heiser , Andre J. Niestroj , Robert Sommer
IPC分类号： A61K38/20 , A61K31/4174 , C07D233/61 , A61K31/4184 , A61K38/21 , A61P9/10 , A61P25/28 , C07D405/12 , C07D413/12 , A61K31/5377
CPC分类号： C07D401/12 , C07D233/64 , C07D235/06 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
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 B, R1, R2, R3, R4, R5, R6 and Z are as defined throughout the description and the claims.

3. 发明申请

US20080293618A1 CYCLOPROPYL-FUSED PYRROLIDINE DERIVATIVES AS DIPEPTIDYL PEPTIDASE IV INHIBITORS 失效
标题翻译：作为DIPEPTIDYL PEPTIDASE IV抑制剂的环丙基 - 氟化吡咯烷衍生物
公开(公告)号：US20080293618A1
公开(公告)日：2008-11-27
申请号：US12120595
申请日：2008-05-14
申请人： Ulrich Heiser , Andre J. Niestroj , Ulf-Torsten Gaertner , Hans-Ulrich Demuth
发明人： Ulrich Heiser , Andre J. Niestroj , Ulf-Torsten Gaertner , Hans-Ulrich Demuth
IPC分类号： A61K31/403 , C07D209/52 , A61K31/69 , A61K31/7088 , A61P3/00 , A61P35/00 , A61K38/28 , C07F5/02
CPC分类号： C07F5/025
摘要： The present invention relates to DP IV-inhibitors of formula (1) for the treatment and/or prophylaxis of diseases of mammals including cancer and tumors, metastasis and tumor colonization; and metabolic diseases.
摘要翻译：本发明涉及用于治疗和/或预防包括癌症和肿瘤在内的哺乳动物疾病，转移和肿瘤定植的式（1）的DP IV抑制剂; 和代谢疾病。

4. 发明授权

US07381537B2 Use of inhibitors of glutaminyl cyclases for treatment and prevention of disease 有权
标题翻译：使用谷氨酰胺酰环化酶抑制剂治疗和预防疾病
公开(公告)号：US07381537B2
公开(公告)日：2008-06-03
申请号：US10839017
申请日：2004-05-05
申请人： Hans-Ulrich Demuth , Torsten Hoffmann , Andre J. Niestroj , Stephan Schilling , Ulrich Heiser
发明人： Hans-Ulrich Demuth , Torsten Hoffmann , Andre J. Niestroj , Stephan Schilling , Ulrich Heiser
IPC分类号： C12Q1/34
CPC分类号： C07F9/6561 , A61K31/00 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/4192 , C07D231/12 , C07D233/54 , C07D403/06 , C07D405/06 , C07D409/06 , C07D471/04 , C07F9/572 , C07F9/59 , C07F9/6506
摘要： The present invention provides novel physiological substrates of mammalian glutaminyl cyclase (QC, EC 2.3.2.5), new effectors of QC, methods for screeing for such effectors, and the use of such effectors and pharmaceutical compositions comprising such effectors for the treatment of conditions that can be treated by modulation of QC-activity. Preferred compositions additionally comprise inhibitors of DP IV or DP IV-like enzymes for the treatment or alleviation of conditions that can be treated by modulation of QC- and DP IV-activity.
摘要翻译：本发明提供哺乳动物谷氨酰胺酰环化酶（QC，EC 2.3.2.5）的新生理底物，QC的新效应物，这种效应物的筛选方法，以及包含这些效果子的这种效应物和药物组合物的用途，用于治疗可以通过调节QC活性来治疗。优选的组合物另外包含用于治疗或减轻可以通过调节QC和DP IV-活性治疗的病症的DP IV或DP IV样酶的抑制剂。

5. 发明授权

US08809010B2 Method for prophylactic treatment of alzheimer's disease using inhibitors of glutaminyl cyclase and glutamate cyclases 有权
标题翻译：使用谷氨酰胺环化酶和谷氨酸环化酶抑制剂预防性治疗阿尔茨海默病的方法
公开(公告)号：US08809010B2
公开(公告)日：2014-08-19
申请号：US12506823
申请日：2009-07-21
申请人： Torsten Hoffmann , Stephan Schilling , Andre J. Niestroj , Hans-Ulrich Demuth , Ulrich Heiser , Mirko Buchholz
发明人： Torsten Hoffmann , Stephan Schilling , Andre J. Niestroj , Hans-Ulrich Demuth , Ulrich Heiser , Mirko Buchholz
IPC分类号： C12Q1/34
CPC分类号： A61K31/4178 , A61K31/00 , A61K31/4184 , A61K31/4188 , A61K31/4192 , A61K31/4439 , A61K31/454 , A61K31/517 , A61K31/5377 , C07D231/12 , C07D233/54 , C07D403/06 , C07D405/06 , C07D409/06 , C07D471/04 , C07F9/572 , C07F9/59 , C07F9/6506 , C07F9/6561
摘要： Provided herein are methods for treating and preventing neurodegenerative disease in a mammal by administering an inhibitor of glutaminyl cyclase (QC). Neurodegenerative diseases treatable or preventable according to methods described herein include mild cognitive impairment (MCI), Alzheimer's disease, neurodegeneration in Down Syndrome, Familial British Dementia, and Familial Danish Dementia.
摘要翻译：本文提供了通过施用谷氨酰胺环化酶（QC）抑制剂来治疗和预防哺乳动物中的神经变性疾病的方法。根据本文描述的方法可治疗或可预防的神经变性疾病包括轻度认知障碍（MCI），阿尔茨海默病，唐氏综合征中的神经变性，家族性的痴呆和家族性丹麦痴呆。

6. 发明授权

US08420684B2 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：US08420684B2
公开(公告)日：2013-04-16
申请号：US11937146
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： A61K31/4166 , A61K31/4178 , C07D233/70 , C07D233/88
CPC分类号： C07D405/14 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D409/14 , C07D417/14
摘要： The present invention relates to 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 heteroaryl; -carbocyclyl-heteroaryl; -alkenylheteroaryl or -alkylheteroaryl; R2 represents alkyl which may optionally be substituted by hydroxy; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl and hydroxy; aryl; -aryl-heteroaryl; -heteroaryl-aryl; -aryl-heterocyclyl; H; heteroaryl; or heterocyclyl, which may optionally be substituted by one or more groups selected from alkyl oxo and hydroxy; R3 represents alkyl which may optionally be substituted by one of more groups selected from alkoxy, amine, hydroxy and —C(O)Oalkyl; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl haloalkyl, alkoxy, amine, hydroxy and —C(O)Oalkyl; -alkyl-aryl; -alkyl(aryl)2; -alkyl-heteroaryl; -alkyl(heteroaryl)2; -alkyl(heteroaryl)(aryl); -aryl-O-aryl; aryl; heterocyclyl, -alkyl-C(O)-heterocyclyl, -alkyl-heterocyclyl, -alkyl-C(O)—NR5-heterocyclyl or -alkyl(heterocyclyl)2 in any of which groups heterocyclyl may be optionally substituted by one or more groups selected from alkyl hydroxy and oxo; -heteroaryl; or -hydroxyalkylaryl; R4 represents H or C1-3 alkyl; R5 represents H or C1-3 alkyl; and X represents O or S.
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，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 1表示杂芳基; 羧基 - 杂芳基; - 烯基杂芳基或 - 烷基杂芳基; R 2表示可任意被羟基取代的烷基; 碳环基，其可任选被一个或多个选自烷基和羟基的基团取代; 芳基; 芳基 - 杂芳基; - 杂芳基 - 芳基; 芳基 - 杂环基 H; 杂芳基; 或杂环基，其可任选被一个或多个选自烷基氧基和羟基的基团取代; R3表示可以任选被选自烷氧基，胺，羟基和-C（O）O烷基的更多个基团之一取代的烷基; 碳环基，其可任选被一个或多个选自烷基卤代烷基，烷氧基，胺，羟基和-C（O）O烷基的基团取代; - 烷基 - 芳基; - 烷基（芳基）2; - 烷基 - 杂芳基 - 烷基（杂芳基）2; - 烷基（杂芳基）（芳基）; 芳基-O-芳基; 芳基; 杂环基， - 烷基-C（O） - 杂环基， - 烷基 - 杂环基， - 烷基-C（O）-NR5 - 杂环基或 - 烷基（杂环基）2，其中任意一个组杂环基可以任选被一个或多个基团取代选自烷基羟基和氧代; 杂芳基或 - 羟基烷基芳基; R 4表示H或C 1-3烷基; R5表示H或C1-3烷基; X表示O或S.

7. 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。

8. 发明授权

US07371871B2 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：US07371871B2
公开(公告)日：2008-05-13
申请号：US10838993
申请日：2004-05-05
申请人： Stephan Schilling , Andre J. Niestroj , Ulrich Heiser , Mirko Buchholz , Hans-Ulrich Demuth
发明人： Stephan Schilling , Andre J. Niestroj , Ulrich Heiser , Mirko Buchholz , Hans-Ulrich Demuth
IPC分类号： A61K31/4174 , C07D233/61
CPC分类号： C07D207/08 , A61K31/00 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/4192 , C07D207/10 , C07D207/12 , C07D207/16 , C07D207/20 , C07D207/22 , C07D207/24 , C07D231/04 , C07D231/06 , C07D233/02 , C07D233/06 , C07D233/28 , C07D233/42 , C07D233/54 , C07D249/04 , C07D249/08 , C07D249/10 , C07D257/04 , C07D261/04 , C07D263/04 , C07D263/06 , C07D277/04 , C07D277/06 , C07D295/185 , C07D403/04 , C07D413/04 , C07D417/04 , C07D471/04 , C07D487/04 , C07F9/572 , C07F9/59 , C07F9/6506 , C07F9/6561
摘要： The present invention relates to compounds that act as inhibitors of QC including those represented by the general formulae 1 to 9: and combinations thereof for the treatment of neuronal disorders, especially Alzheimer's disease, Down Syndrome, Parkinson disease, Corea Huntington, pathogenic psychotic conditions, schizophrenia, impaired food intake, sleep-wakefulness, impaired homeostatic regulation of energy metabolism, impaired autonomic function, impaired hormonal balance, impaired regulation, body fluids, hypertension, fever, sleep dysregulation, anorexia, anxiety related disorders including depression, seizures including epilepsy, drug withdrawal and alcoholism, neurodegenerative disorders including cognitive dysfunction and dementia.
摘要翻译：本发明涉及作为QC抑制剂的化合物，包括由通式1至9表示的化合物及其组合用于治疗神经元疾病，特别是阿尔茨海默氏病，唐氏综合征，帕金森病，柯达亨廷顿病，致病性精神病症状，精神分裂症，食物摄取受损，睡眠觉醒，能量代谢的稳态调节受损，自主神经功能受损，激素平衡受损，调节受损，体液，高血压，发热，睡眠失调，厌食，焦虑相关障碍，包括癫痫发作，药物戒断和酒精中毒，神经变性疾病，包括认知功能障碍和痴呆。

9. 发明授权

US07732162B2 Inhibitors of glutaminyl cyclase for treating neurodegenerative diseases 有权
标题翻译：用于治疗神经变性疾病的谷氨酰胺环化酶抑制剂
公开(公告)号：US07732162B2
公开(公告)日：2010-06-08
申请号：US11685881
申请日：2007-03-14
申请人： Torsten Hoffman , Stephan Schilling , Andre J. Niestroj , Hans-Ulrich Demuth , Ulrich Heiser , Mirko Buchholz
发明人： Torsten Hoffman , Stephan Schilling , Andre J. Niestroj , Hans-Ulrich Demuth , Ulrich Heiser , Mirko Buchholz
IPC分类号： C12Q1/34
CPC分类号： A61K31/4178 , A61K31/00 , A61K31/4184 , A61K31/4188 , A61K31/4192 , A61K31/4439 , A61K31/454 , A61K31/517 , A61K31/5377 , C07D231/12 , C07D233/54 , C07D403/06 , C07D405/06 , C07D409/06 , C07D471/04 , C07F9/572 , C07F9/59 , C07F9/6506 , C07F9/6561
摘要： The present invention provides novel physiological substrates of mammalian glutaminyl cyclase (QC, EC 2.3.2.5), new effectors of QC, methods for screening for such effectors, and the use of such effectors and pharmaceutical compositions comprising such effectors for the treatment of conditions that can be treated by modulation of QC-activity. Preferred compositions additionally comprise inhibitors of DP IV or DP IV-like enzymes for the treatment or alleviation of conditions that can be treated by modulation of QC- and DP IV-activity.
摘要翻译：本发明提供哺乳动物谷氨酰胺酰环化酶（QC，EC 2.3.2.5）的新生理底物，QC的新效应物，用于筛选此类效应物的方法，以及使用这些效应物和包含这些效应物的药物组合物，用于治疗可以通过调节QC活性来治疗。优选的组合物另外包含用于治疗或减轻可以通过调节QC和DP IV-活性治疗的病症的DP IV或DP IV样酶的抑制剂。

10. 发明申请

US20100040575A1 USE OF INHIBITORS OF GLUTAMINYL CYCLASE AND GLUTAMATE CYCLASE FOR TREATMENT AND PREVENTION OF NEURODEGENERATIVE DISEASES 有权
标题翻译：谷氨酰胺环糊精和谷氨酸环化酶抑制剂用于治疗和预防神经病变性疾病的使用
公开(公告)号：US20100040575A1
公开(公告)日：2010-02-18
申请号：US12506823
申请日：2009-07-21
申请人： Torsten Hoffmann , Stephan Schilling , Andre J. Niestroj , Hans-Ulrich Demuth , Ulrich Heiser , Mirko Buchholz
发明人： Torsten Hoffmann , Stephan Schilling , Andre J. Niestroj , Hans-Ulrich Demuth , Ulrich Heiser , Mirko Buchholz
IPC分类号： A61K31/4164 , A61P25/00 , A61P25/28 , A61K31/4184 , A61K31/428 , A61K31/517 , A61K31/5415 , A61K39/395 , A61K38/21 , A61K45/00
CPC分类号： A61K31/4178 , A61K31/00 , A61K31/4184 , A61K31/4188 , A61K31/4192 , A61K31/4439 , A61K31/454 , A61K31/517 , A61K31/5377 , C07D231/12 , C07D233/54 , C07D403/06 , C07D405/06 , C07D409/06 , C07D471/04 , C07F9/572 , C07F9/59 , C07F9/6506 , C07F9/6561
摘要： Physiological substrates of mammalian glutaminyl cyclase (QC, EC 2.3.2.5), new effectors of QC, methods for screening for such effectors, and the use of such effectors and pharmaceutical compositions comprising such effectors for the treatment of conditions that can be treated by modulation of QC-activity. Preferred compositions additionally comprise inhibitors of DP IV or DP IV-like enzymes for the treatment or alleviation of conditions that can be treated by modulation of QC- and DP IV-activity.
摘要翻译：哺乳动物谷氨酰胺酰环化酶（QC，EC 2.3.2.5）的生理底物，QC的新效应物，用于筛选此类效应物的方法，以及使用这些效应物和包含这些效应物的药物组合物用于治疗可通过调节的QC活动。优选的组合物另外包含用于治疗或减轻可以通过调节QC和DP IV-活性治疗的病症的DP IV或DP IV样酶的抑制剂。

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