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1. 发明授权

US08962860B2 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：US08962860B2
公开(公告)日：2015-02-24
申请号：US12554611
申请日：2009-09-04
申请人： Ulrich Heiser , Robert Sommer , Ulf-Torsten Gaertner , Antje Hamann , Michael Almstetter , Michael Thormann , Andreas Treml , Hans-Ulrich Demuth , Torsten Hoffman
发明人： Ulrich Heiser , Robert Sommer , Ulf-Torsten Gaertner , Antje Hamann , Michael Almstetter , Michael Thormann , Andreas Treml , Hans-Ulrich Demuth , Torsten Hoffman
IPC分类号： C07D403/04 , C07D403/06 , C07D417/04 , C07D471/04 , C07D405/14 , C07D417/14
CPC分类号： C07D403/04 , C07D403/06 , C07D405/14 , C07D417/04 , C07D417/14 , C07D471/04
摘要： Compounds of general formula (I): wherein R1, R2, R3, R4, X and Y are as defined herein are inhibitors of glutaminyl cyclase and are therefore useful in treating conditions that can be treated by modulation of glutaminyl cyclase activity.
摘要翻译：通式（I）的化合物：其中R1，R2，R3，R4，X和Y如本文所定义，是谷氨酰胺酰环化酶的抑制剂，因此可用于治疗可通过调节谷氨酰胺酰环化酶活性治疗的病症。

2. 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.

3. 发明申请

US20120329785A1 Novel kinase inhibitors 有权
标题翻译：新型激酶抑制剂
公开(公告)号：US20120329785A1
公开(公告)日：2012-12-27
申请号：US13506509
申请日：2012-04-23
申请人： Michael Thormann , Andreas Treml , Michael Almstetter , Roland Koestler , Nasser Yehia
发明人： Michael Thormann , Andreas Treml , Michael Almstetter , Roland Koestler , Nasser Yehia
IPC分类号： C07D471/04 , C07D401/14 , A61K31/496 , A61K31/5513 , A61P27/02 , A61K31/5377 , A61P29/00 , A61P37/06 , A61P37/08 , A61K31/437 , C07D413/14
CPC分类号： C07D471/04
摘要： The present invention relates to novel compounds of formula (I) that are capable of inhibiting one or more kinases, especially SYK (Spleen Tyrosine Kinase), LRRK2 (Leucine-rich repeat kinase 2) and/or MYLK (Myosin light chain kinase) or mutants thereof. The compounds find applications in the treatment of a variety of diseases.
摘要翻译：本发明涉及能够抑制一种或多种激酶，特别是SYK（脾脏酪氨酸激酶），LRRK2（富含亮氨酸重复激酶2）和/或MYLK（肌球蛋白轻链激酶）的新型的式（I）化合物或其突变体。该化合物可用于治疗各种疾病。

4. 发明申请

US20100234397A1 ENZYME INHIBITORS 审中-公开
标题翻译：酶抑制剂
公开(公告)号：US20100234397A1
公开(公告)日：2010-09-16
申请号：US12750930
申请日：2010-03-31
申请人： Michael Thormann , Michael Almstetter , Andreas Treml
发明人： Michael Thormann , Michael Almstetter , Andreas Treml
IPC分类号： A61K31/497 , A61K31/4164 , A61K31/4439 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/08 , A61P25/18 , A61P29/00 , A61P37/00 , A61P35/00 , A61P37/06
CPC分类号： C07D409/06 , C07D233/64 , C07D401/06 , C07D403/06 , C07D405/06
摘要： There is disclosed herein methods for using compounds of formula (I), wherein: R1, R2, R3, R4 and R5 are defined throughout the description and the claims. The compounds of formula (I) are useful for the treatment of neurological diseases and neurodegenerative diseases, e.g. anxiety, depression, Alzheimer's disease etc.
摘要翻译：本文公开了使用式（I）化合物的方法，其中：在整个说明书和权利要求书中限定了R1，R2，R3，R4和R5。式（I）化合物可用于治疗神经疾病和神经变性疾病，例如，焦虑，抑郁，阿尔茨海默病等

5. 发明申请

US20100029597A1 RECA INHIBITORS WITH ANTIBIOTIC ACTIVITY, COMPOSITIONS AND METHODS OF USE 有权
标题翻译：具有抗生物活性的RECA抑制剂，组合物和使用方法
公开(公告)号：US20100029597A1
公开(公告)日：2010-02-04
申请号：US12279243
申请日：2007-02-13
申请人： Guillaume Cottarel , Jamey Wierzbowski , Kollol Pal , Michael Kohanski , Daniel Dwyer , James Collins , Michael Almstetter , Michael Thormann , Andreas Treml
发明人： Guillaume Cottarel , Jamey Wierzbowski , Kollol Pal , Michael Kohanski , Daniel Dwyer , James Collins , Michael Almstetter , Michael Thormann , Andreas Treml
IPC分类号： A61K31/65 , A61K31/352 , A61K31/382 , A61K31/47 , A61P31/04
CPC分类号： A61K45/06 , A61K38/12 , C12Q1/18 , G01N33/5023 , A61K2300/00
摘要： The present invention is directed to the use of RecA inhibitors as antibiotic agents, and provides RecA inhibitors useful in treating infections. Also provided are various compositions and methods associated with RecA inhibition.
摘要翻译：本发明涉及使用RecA抑制剂作为抗生素，并提供可用于治疗感染的RecA抑制剂。还提供了与RecA抑制相关的各种组合物和方法。

6. 发明授权

US09155792B2 RecA inhibitors with antibiotic activity, compositions and methods of use 有权
标题翻译：具有抗生素活性的RecA抑制剂，组合物和使用方法
公开(公告)号：US09155792B2
公开(公告)日：2015-10-13
申请号：US12279243
申请日：2007-02-13
申请人： Guillaume Cottarel , Jamey Wierzbowski , Kollol Pal , Michael Kohanski , Daniel Dwyer , James Collins , Michael Almstetter , Michael Thormann , Andreas Treml
发明人： Guillaume Cottarel , Jamey Wierzbowski , Kollol Pal , Michael Kohanski , Daniel Dwyer , James Collins , Michael Almstetter , Michael Thormann , Andreas Treml
IPC分类号： A61K49/00 , C07H19/16 , A61K38/00 , A61K45/06 , A61K38/12 , C12Q1/18 , G01N33/50
CPC分类号： A61K45/06 , A61K38/12 , C12Q1/18 , G01N33/5023 , A61K2300/00
摘要： The present invention is directed to the use of RecA inhibitors as antibiotic agents, and provides RecA inhibitors useful in treating infections. Also provided are various compositions and methods associated with RecA inhibition.
摘要翻译：本发明涉及使用RecA抑制剂作为抗生素，并提供可用于治疗感染的RecA抑制剂。还提供了与RecA抑制有关的各种组合物和方法。

7. 发明授权

US08889709B2 Use of isoQC inhibitors in the treatment and prevention of inflammatory diseases or conditions 有权
标题翻译：使用isoQC抑制剂治疗和预防炎性疾病或病症
公开(公告)号：US08889709B2
公开(公告)日：2014-11-18
申请号：US12554584
申请日：2009-09-04
申请人： Hans-Ulrich Demuth , Stephan Schilling , Michael Wermann , Holger Cynis , Astrid Kehlen , Daniel Friedrich , Torsten Hoffmann , Kathrin Gans , Jens-Ulrich Rahfeld , Ulrich Heiser , Michael Almstetter , Robert Sommer , Ulf-Torsten Gaertner , Antje Hamann , Michael Thormann , Andreas Treml
发明人： Hans-Ulrich Demuth , Stephan Schilling , Michael Wermann , Holger Cynis , Astrid Kehlen , Daniel Friedrich , Torsten Hoffmann , Kathrin Gans , Jens-Ulrich Rahfeld , Ulrich Heiser , Michael Almstetter , Robert Sommer , Ulf-Torsten Gaertner , Antje Hamann , Michael Thormann , Andreas Treml
IPC分类号： A01N43/42 , C12N9/00 , C12N9/10 , C12N1/20 , C12N15/00 , C07H21/04 , C07D417/12 , C07D405/12 , C07D233/61 , C07D409/12 , C07D403/12 , C07D413/12 , C07D403/06 , C07D401/12 , C07D233/54 , C07D235/06
CPC分类号： C07D233/54 , C07D233/61 , C07D235/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C12N9/104
摘要： The present invention relates in general to an inhibitor of a glutaminyl peptide cyclotransferase-like protein (QPCTL), and the use thereof for the treatment and/or prevention of an inflammatory disease or disorder selected from the group consisting of (a) chronic and acute inflammations, e.g. rheumatoid arthritis, atherosclerosis, restenosis, pancreatitis; (b) other inflammatory diseases, e.g. neuropathic pain, graft rejection/graft failure/graft vasculopathy, HIV infections/AIDS, gestosis, tuberous sclerosis, Guillain-Barré syndrome, chronic inflammatory demyelinizing polyradiculoneuropathy and multiple sclerosis; (c) neuroinflammation; and (d) neurodegenerative diseases, e.g. mild cognitive impairment (MCI), Alzheimer's disease, neurodegeneration in Down Syndrome, Familial British Dementia, and Familial Danish Dementia, which may result from neuroinflammation.
摘要翻译：本发明一般涉及谷氨酰胺肽环转移酶样蛋白（QPCTL）的抑制剂及其用于治疗和/或预防炎性疾病或病症的用途，所述炎性疾病或病症选自（a）慢性和急性炎症，例如类风湿关节炎，动脉粥样硬化，再狭窄，胰腺炎; （b）其他炎性疾病，例如艾滋病，睾丸炎，结节性硬化症，吉兰巴利综合征，慢性炎性脱髓鞘性多发性神经系统疾病和多发性硬化; （c）神经炎症; 和（d）神经变性疾病，例如轻度认知障碍（MCI），阿尔茨海默氏症，唐氏综合征神经变性，家族性英国痴呆和家族性丹麦痴呆，可能由神经炎症引起。

8. 发明申请

US20100119475A1 NOVEL INHIBITORS OF GLUTAMINYL CYCLASE 有权
标题翻译： GLUTAMINYL CYCLASE的新型抑制剂
公开(公告)号：US20100119475A1
公开(公告)日：2010-05-13
申请号：US12554611
申请日：2009-09-04
申请人： Ulrich Heiser , Robert Sommer , Ulf-Torsten Gaertner , Antje Hamann , Michael Almstetter , Michael Thormann , Andreas Treml , Hans-Ulrich Demuth , Torsten Hoffman
发明人： Ulrich Heiser , Robert Sommer , Ulf-Torsten Gaertner , Antje Hamann , Michael Almstetter , Michael Thormann , Andreas Treml , Hans-Ulrich Demuth , Torsten Hoffman
IPC分类号： A61K31/4184 , C07D417/14 , C07D403/10 , C07D405/14 , C07D471/04 , A61K31/433 , A61K31/4439 , A61K39/395 , A61K38/20 , A61K38/21 , A61P35/00 , A61P3/00 , A61P25/00
CPC分类号： C07D403/04 , C07D403/06 , C07D405/14 , C07D417/04 , C07D417/14 , C07D471/04
摘要： Compounds of general formula (I): wherein R1, R2, R3, R4, X and Y are as defined herein are inhibitors of glutaminyl cyclase and are therefore useful in treating conditions that can be treated by modulation of glutaminyl cyclase activity.
摘要翻译：通式（I）的化合物：其中R1，R2，R3，R4，X和Y如本文所定义，是谷氨酰胺酰环化酶的抑制剂，因此可用于治疗可通过调节谷氨酰胺酰环化酶活性治疗的病症。

9. 发明申请

US20070244177A1 ENZYME INHIBITORS 失效
标题翻译：酶抑制剂
公开(公告)号：US20070244177A1
公开(公告)日：2007-10-18
申请号：US11734369
申请日：2007-04-12
申请人： Michael Thormann , Michael Almstetter , Andreas Treml
发明人： Michael Thormann , Michael Almstetter , Andreas Treml
IPC分类号： A61K31/416 , A61K31/4152 , C07D403/02 , C07D231/12
CPC分类号： C07D409/06 , C07D233/64 , C07D401/06 , C07D403/06 , C07D405/06
摘要： There is dislosed herein compounds of formula (I), wherein:R1, R2, R3, R4 and R5 are defined throughout the description and the claims. The compounds of formula (I) are useful for the treatment of neurological diseases and neurodegenerative diseases, e.g. anxiety, depression, Alzheimer's disease etc.
摘要翻译：在本文中，式（I）的化合物是非离子的，其中：R 1，R 2，R 3，R 4，在整个说明书和权利要求书中限定了SUP＆gt;和R＆lt; 5＆gt;。式（I）化合物可用于治疗神经疾病和神经变性疾病，例如，焦虑，抑郁，阿尔茨海默病等

10. 发明授权

US09499535B2 Kinase inhibitors 有权
标题翻译：激酶抑制剂
公开(公告)号：US09499535B2
公开(公告)日：2016-11-22
申请号：US13506509
申请日：2012-04-23
申请人： Michael Thormann , Andreas Treml , Michael Almstetter , Roland Koestler , Nasser Yehia
发明人： Michael Thormann , Andreas Treml , Michael Almstetter , Roland Koestler , Nasser Yehia
IPC分类号： A61K31/55 , A61K31/54 , A61K31/535 , C07D471/04
CPC分类号： C07D471/04
摘要： The present invention relates to novel compounds of formula (I) that are capable of inhibiting one or more kinases, especially SYK (Spleen Tyrosine Kinase), LRRK2 (Leucine-rich repeat kinase 2) and/or MYLK (Myosin light chain kinase) or mutants thereof. The compounds find applications in the treatment of a variety of diseases.

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